{
	"10305": {"label": 3, "data": {"text": "Selective inhibition of PDE5 is a rational therapeutic approach in ED, as proved by the clinical success of sildenafil.", "entity1": "PDE5", "entity2": "sildenafil", "span1": [24, 28], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8422": {"label": 8, "data": {"text": "Furthermore, knockdown of OPN enhanced cell death caused by other drugs, including paclitaxel, doxorubicin, actinomycin-D, and rapamycin, which are also P-gp substrates.", "entity1": "P-gp", "entity2": "paclitaxel", "span1": [153, 157], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8486": {"label": 3, "data": {"text": "Furthermore, no impact on cytokine release (i.e., on IL-10, IL-6, IL-12/23p40 and TNF\u03b1 levels) was seen in LPS-stimulated human PBMCs, except with JWH-210 and JWH-122 which caused a decrease of TNF\u03b1 and IL-12/23p40.", "entity1": "IL-12", "entity2": "JWH-210", "span1": [203, 208], "span2": [147, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6254": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "norepinephrine transporter", "entity2": "chlorpromazine", "span1": [182, 208], "span2": [210, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1801": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "Tarceva", "span1": [0, 32], "span2": [144, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"82": {"label": 1, "data": {"text": "The high-affinity binding of L-noradrenaline to phenylalanine hydroxylase, as studied by equilibrium microdialysis (anaerobically) and ultrafiltration (aerobically), shows positive cooperativity (h = 1.9); at pH 7.2 and 20 degrees C the rat enzyme binds about 0.5 mol L-noradrenaline/mol subunit with a half-maximal binding (S50) at 0.25 microM L-noradrenaline.", "entity1": "phenylalanine hydroxylase", "entity2": "L-noradrenaline", "span1": [48, 73], "span2": [268, 283]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5981": {"label": 8, "data": {"text": "Tyrosinase catalyzes an unusual oxidative decarboxylation of 3,4-dihydroxymandelate.", "entity1": "Tyrosinase", "entity2": "3,4-dihydroxymandelate", "span1": [0, 10], "span2": [61, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6865": {"label": 9, "data": {"text": "Jo2-induced activation of caspase-3 or -9 in liver tissues was inhibited by minocycline pretreatment, and yet the direct addition of minocycline to liver extracts from Jo2-challenged mice failed to block caspase activation in vitro.", "entity1": "caspase", "entity2": "minocycline", "span1": [204, 211], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9540": {"label": 2, "data": {"text": "Lintitript markedly increased postprandial plasma CCK release (P<0.001) while distinctly reducing postprandial PP levels (P<0.01) as compared to placebo.", "entity1": "CCK", "entity2": "Lintitript", "span1": [50, 53], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13166": {"label": 1, "data": {"text": "Progestin induction of the cyclin D1 gene, which lacks a progesterone response element, was dependent on PR activation of the Src/MAPK pathway, whereas induction of the Sgk (serum and glucocorticoid regulated kinase) gene that contains a functional progesterone response element was unaffected by mutations that interfere with PR activation of Src.", "entity1": "Sgk", "entity2": "Progestin", "span1": [169, 172], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15588": {"label": 1, "data": {"text": "Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse.", "entity1": "VMAT2", "entity2": "N", "span1": [79, 84], "span2": [24, 25]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2013": {"label": 3, "data": {"text": "Pranlukast-induced inhibition of IL-5 mRNA expression was noted in various cells, irrespective of their CysLTR1 mRNA expression status.", "entity1": "IL-5", "entity2": "Pranlukast", "span1": [33, 37], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4064": {"label": 3, "data": {"text": "Among the isolated compounds, trans-dihydromorin (8), oxyresveratrol (9), and steppogenin (12) were found to exhibit significant tyrosinase inhibition activities.", "entity1": "tyrosinase", "entity2": "trans-dihydromorin", "span1": [129, 139], "span2": [30, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2878": {"label": 3, "data": {"text": "Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin.", "entity1": "dipeptidyl peptidase-4", "entity2": "sitagliptin", "span1": [27, 49], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11828": {"label": 3, "data": {"text": "To explore the molecular basis for CPT hypersensitivity in Top2\u03b2-deficient cells, we found that upon CPT exposure, the RNA polymerase II large subunit (RNAP LS) became progressively depleted, followed by recovery to nearly the original level in wild-type MEFs, whereas RNAP LS remained depleted without recovery in Top2\u03b2-deficient cells.", "entity1": "RNA polymerase II large subunit", "entity2": "CPT", "span1": [119, 150], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14046": {"label": 2, "data": {"text": "Aspirin and metformin (an activator of AMPK) increased inhibition of mTOR and Akt, as well as autophagy in CRC cells.", "entity1": "AMPK", "entity2": "metformin", "span1": [39, 43], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10088": {"label": 3, "data": {"text": "A series of studies is reviewed that assesses the relationship between cytokines released at the site of tissue injury and NSAID analgesia, and the in vivo selectivity of a selective cyclooxygenase (COX)-2 inhibitor (celecoxib) in comparison to a dual COX-1/COX-2 inhibitor (ketorolac).", "entity1": "COX-2", "entity2": "ketorolac", "span1": [258, 263], "span2": [275, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14461": {"label": 1, "data": {"text": "Loss of agonist binding was observed on intact human embryonic kidney 293 cells expressing the W203A receptor, conditions where high GTP levels are present; however, high affinity binding [(3)H]PGE(2) was observed in broken cell preparations washed free of GTP.", "entity1": "W203A", "entity2": "[(3)H]PGE(2)", "span1": [95, 100], "span2": [188, 200]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5908": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "VLDL", "entity2": "probucol", "span1": [133, 137], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1499": {"label": 3, "data": {"text": "Sulindac sulfide inhibits epidermal growth factor-induced phosphorylation of extracellular-regulated kinase 1/2 and Bad in human colon cancer cells.", "entity1": "Bad", "entity2": "Sulindac sulfide", "span1": [116, 119], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4491": {"label": 2, "data": {"text": "The hemoglobin A1c (HbA1c) of all patients improved significantly from 8.1\u00b11.2% to 7.6\u00b11.1% after 12 weeks of add-on therapy with sitagliptin (p<0.01), and the insulin dosage was reduced from 27.3\u00b115.8 U/day to 24.5\u00b116.5 U/day (p<0.001).", "entity1": "HbA1c", "entity2": "sitagliptin", "span1": [20, 25], "span2": [130, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9342": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "AMPA", "span1": [72, 77], "span2": [189, 193]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13752": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "L-type calcium channel", "entity2": "1,4-dihydropyridine", "span1": [4, 26], "span2": [81, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6466": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "glycinamide ribonucleotide formyl transferase", "entity2": "LY231514", "span1": [141, 186], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2721": {"label": 1, "data": {"text": "Cisapride was found to bind the human ether-a-go-go-related gene (HERG) potassium channel, which provides a plausible mechanism for QTc interval prolongation/arrhythmia.", "entity1": "human ether-a-go-go-related gene (HERG) potassium channel", "entity2": "Cisapride", "span1": [32, 89], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12577": {"label": 0, "data": {"text": "This cDNA clone, designated EAA3a, shares a 90% nucleotide identity with the previously reported rat GluR5-2b cDNA splice variant and differed from human GluR5-1d in the amino and carboxy terminal regions.", "entity1": "human GluR5-1d", "entity2": "amino", "span1": [148, 162], "span2": [170, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4294": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B1", "entity2": "dehydroepiandrosterone sulfate", "span1": [258, 265], "span2": [94, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1604": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE2", "entity2": "5-(N,N-dimethyl)-amiloride", "span1": [113, 117], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11794": {"label": 3, "data": {"text": "Fisetin treatment showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), NF-kB p65 unit (in pancreas) and IL-1\u03b2 (plasma), serum nitric oxide (NO) with an elevation in plasma insulin.", "entity1": "glycosylated hemoglobin", "entity2": "Fisetin", "span1": [79, 102], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3035": {"label": 1, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "prostanoid receptors EP(1)", "entity2": "PGE(2)", "span1": [171, 197], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11899": {"label": 8, "data": {"text": "Cytochrome P450 epoxygenase 2J2 (CYP2J2) metabolizes arachidonic acids to form epoxyeicosatrienoic acids (EETs), which possess various beneficial effects on the cardiovascular system.", "entity1": "Cytochrome P450 epoxygenase 2J2", "entity2": "arachidonic acids", "span1": [0, 31], "span2": [53, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7163": {"label": 3, "data": {"text": "The deletion and mutation analysis of the AT1R gene promoter indicated that a GC box located in the proximal promoter region is responsible for the telmisartan-induced downregulation.", "entity1": "AT1R", "entity2": "telmisartan", "span1": [42, 46], "span2": [148, 159]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1252": {"label": 3, "data": {"text": "The effects of theophylline (unspecific PDE inhibitor), vinpocetine (PDE1 inhibitor), EHNA (PDE2 inhibitor) and the PDE5 inhibitors zaprinast and E 4021 were weak.", "entity1": "PDE5", "entity2": "zaprinast", "span1": [116, 120], "span2": [132, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13172": {"label": 2, "data": {"text": "These results highlight the importance of PR activation of the Src/MAPK signaling pathway for progesterone-induced transcription of select target genes and cell cycle progression.", "entity1": "Src", "entity2": "progesterone", "span1": [63, 66], "span2": [94, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"422": {"label": 1, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "SNAP 1069", "span1": [258, 286], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15340": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "2'-methoxyflavone", "span1": [39, 48], "span2": [131, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13073": {"label": 1, "data": {"text": "There is a modest salutary effect when the pemetrexed target is GARFT alone.", "entity1": "GARFT", "entity2": "pemetrexed", "span1": [64, 69], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10150": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "ER", "entity2": "ICI 164,384", "span1": [129, 131], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6396": {"label": 5, "data": {"text": "The glucocorticoid receptor antagonist RU-486 (mifepristone) significantly counteracted the effect of dexamethasone on glucocorticoid receptor activation, indicating that the dexamethasone effect is specific and is mediated through the glucocorticoid receptor.", "entity1": "glucocorticoid receptor", "entity2": "RU-486", "span1": [4, 27], "span2": [39, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5759": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "parkin", "entity2": "MPTP", "span1": [233, 239], "span2": [140, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3799": {"label": 3, "data": {"text": "The synthetic stereoisomer, [+]-Hup A, is less toxic due to poor AChE inhibition and is suitable for both pre-/post-exposure treatments of nerve agent toxicity.", "entity1": "AChE", "entity2": "[+]-Hup A", "span1": [65, 69], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5587": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "5-FU", "span1": [121, 123], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"9511": {"label": 5, "data": {"text": "In conclusion, these findings indicate that [3H]SR 142948A is a new potent antagonist radioligand which recognizes with high affinity both neurotensin NT1 and NT2 receptors and represents thus an excellent tool to study neurotensin receptors in the rat brain.", "entity1": "neurotensin NT1", "entity2": "[3H]SR 142948A", "span1": [139, 154], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9881": {"label": 5, "data": {"text": "JTH-601 is expected to be an effective alpha(1)-adrenoceptor antagonist for the treatment of urinary outlet obstruction by benign prostatic hypertrophy with a minimum effect on the cardiovascular system.", "entity1": "alpha(1)-adrenoceptor", "entity2": "JTH-601", "span1": [39, 60], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7830": {"label": 4, "data": {"text": "Cellular release of AChE by SH-SY5Y is significantly enhanced by the muscarinic acetylcholine receptor (mAChR) agonists carbachol or muscarine, with the effect of carbachol blocked by the mAChR antagonist atropine.", "entity1": "mAChR", "entity2": "muscarine", "span1": [104, 109], "span2": [133, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6719": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "quinoxaline", "span1": [273, 279], "span2": [62, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9815": {"label": 3, "data": {"text": "Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels.", "entity1": "calcium channels", "entity2": "Mibefradil", "span1": [74, 90], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9482": {"label": 1, "data": {"text": "The human ether-a-go-go-related gene (HERG), which encodes the rapidly activating delayed rectifier K+ current and is important in cardiac repolarization, may serve as a target for the action of cisapride.", "entity1": "HERG", "entity2": "cisapride", "span1": [38, 42], "span2": [195, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4494": {"label": 9, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES2", "entity2": "ibuprofen-\u03b2-d-glucuronide", "span1": [300, 305], "span2": [57, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8675": {"label": 2, "data": {"text": "The expression kinetics of TAp63, c-Abl and TAp73 suggest that cisplatin activates TAp63-dependent expression of c-Abl and TAp73 and, in turn, the activation of TAp73 by c-Abl-induced BAX expression.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [113, 118], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1977": {"label": 3, "data": {"text": "The inhibitory effect of sodium nitroprusside on HIF-1 activation is not dependent on nitric oxide-soluble guanylyl cyclase pathway.", "entity1": "HIF-1", "entity2": "sodium nitroprusside", "span1": [49, 54], "span2": [25, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13727": {"label": 3, "data": {"text": "When RAD51, which is a central component of HR, was depleted by siRNA cells were sensitized to raltitrexed (RTX), which specifically inhibits TS.", "entity1": "TS", "entity2": "RTX", "span1": [142, 144], "span2": [108, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5011": {"label": 3, "data": {"text": "These five CGPs also inhibited [(3)H]E217\u03b2G uptake by MRP4.", "entity1": "MRP4", "entity2": "CGPs", "span1": [54, 58], "span2": [11, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12618": {"label": 3, "data": {"text": "Among the other bisphosphonates studied, alendronate was more potent and selective for PTPmeg1.", "entity1": "PTPmeg1", "entity2": "alendronate", "span1": [87, 94], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2922": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "ion channel", "entity2": "bepridil", "span1": [9, 20], "span2": [64, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13623": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-l(R)-aminoindan] is a second-generation propargylamine pharmacophore that selectively and irreversibly inhibits brain MAO-B and is specifically designed for the treatment of Parkinson's disease (PD).", "entity1": "MAO-B", "entity2": "N-propargyl-l(R)-aminoindan", "span1": [142, 147], "span2": [12, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14077": {"label": 3, "data": {"text": "SB203580 (a specific inhibitor of p38 kinase) markedly suppressed the increased expression of collagen type I and \u03b1-SMA in TGF-\u03b21-induced NPDFs.", "entity1": "TGF-\u03b21", "entity2": "SB203580", "span1": [123, 129], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10202": {"label": 8, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP8", "entity2": "BSP", "span1": [37, 42], "span2": [52, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7800": {"label": 9, "data": {"text": "However, 4'G-RSV, but not 3G-RSV, induced SIRT1-dependent histone H3 deacetylation and SOD2 expression in mouse C2C12 skeletal myoblasts; as with RSV, SIRT1 knockdown blunted these effects.", "entity1": "SIRT1", "entity2": "3G-RSV", "span1": [42, 47], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2373": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "PDGFR", "entity2": "Nexavar", "span1": [133, 138], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9753": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "alpha(2)-adrenergic receptors", "entity2": "yohimbine", "span1": [73, 102], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10916": {"label": 2, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "EGFR", "entity2": "PP2", "span1": [172, 176], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3306": {"label": 1, "data": {"text": "Steady-state fluorescence was utilized to assess Ca(2+) affinity in isolated cardiac (c)TnCs containing F27W and did not necessarily mirror the fiber Ca(2+) sensitivity.", "entity1": "cardiac (c)TnCs", "entity2": "Ca(2+)", "span1": [77, 92], "span2": [49, 55]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10823": {"label": 3, "data": {"text": "Carvedilol prevents cardiac hypertrophy and overexpression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in pressure-overloaded rat heart.", "entity1": "vascular endothelial growth factor", "entity2": "Carvedilol", "span1": [98, 132], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7875": {"label": 8, "data": {"text": "Renal clearance of unbound anagliptin and unbound M1 far exceeded glomerular filtration rate, indicating active renal elimination: that might reflect the fact that anagliptin may be a substrate of OAT1, OAT3, MDR1 and MRP2, and M1 a substrate of OAT3, BCRP, MRP2 and MRP4.", "entity1": "MDR1", "entity2": "anagliptin", "span1": [209, 213], "span2": [164, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11857": {"label": 8, "data": {"text": "The calcium homeostasis proteins sarcoendoplasmic reticulum ATPase 2a (SERCA2a), sodium calcium exchanger-1, phospholamban (PLB), phospho-PLB, and calsequestrin 2 are important for contraction and relaxation.", "entity1": "SERCA2a", "entity2": "calcium", "span1": [71, 78], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"49": {"label": 3, "data": {"text": "Comparison of the monoamine oxidase inhibiting properties of two reversible and selective monoamine oxidase-A inhibitors moclobemide and toloxatone, and assessment of their effect on psychometric performance in healthy subjects.", "entity1": "monoamine oxidase-A", "entity2": "moclobemide", "span1": [90, 109], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15831": {"label": 8, "data": {"text": "However, enzymes contributing to oxidative metabolism of anandamide, namely cyclooxygenase-1 and Cyp2D6, were increased in the brain of aged mice, possibly enhancing the oxidative breakdown of anandamide.", "entity1": "Cyp2D6", "entity2": "anandamide", "span1": [97, 103], "span2": [193, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15921": {"label": 1, "data": {"text": "DEHP exposure significantly decreased the levels of these four FAs only in pregnant mPPAR\u03b1 mice.", "entity1": "mPPAR\u03b1", "entity2": "DEHP", "span1": [84, 90], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1282": {"label": 1, "data": {"text": "Rheumatoid synovial cells expressed PPARgamma mRNA, and the PPARgamma ligands 15-deoxy-Delta(12,14)-prostaglandin J(2) and troglitazone reduced the proliferation and induced apoptosis in synovial cells.", "entity1": "PPARgamma", "entity2": "troglitazone", "span1": [36, 45], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15698": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "ASICs", "entity2": "CAT", "span1": [63, 68], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8822": {"label": 3, "data": {"text": "New series of pyrrolidine mercaptosulfide, 2-mercaptocyclopentane arylsulfonamide, and 3-mercapto-4-arylsulfonamido pyrrolidine matrix metalloproteinase inhibitors (MMPIs) were designed, synthesized, and evaluated.", "entity1": "matrix metalloproteinase", "entity2": "pyrrolidine mercaptosulfide", "span1": [128, 152], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3499": {"label": 9, "data": {"text": "The study showed that fenofibrate did not attenuate increased blood pressure induced by PE, AII and ET1 but caused enhanced vasodilation by Ach, SNP and ISO.", "entity1": "ET1", "entity2": "fenofibrate", "span1": [100, 103], "span2": [22, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1082": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "edrophonium", "span1": [51, 71], "span2": [134, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2043": {"label": 3, "data": {"text": "Docetaxel is a semisynthetic taxane that inhibit tumor growth by induction of microtubule stabilization and promotion of bcl-2 inactivation, which induce apoptosis.", "entity1": "bcl-2", "entity2": "Docetaxel", "span1": [121, 126], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"376": {"label": 3, "data": {"text": "In conclusion, the production of IL-4 and IL-5 by T-cell clones (derived either from BAL or blood) was more sensitive to inhibition by DEX than that of IFN-gamma, which may account for the therapeutic effects of glucocorticosteroids in patients with asthma.", "entity1": "IL-5", "entity2": "DEX", "span1": [42, 46], "span2": [135, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"982": {"label": 2, "data": {"text": "Moreover, BH(4) treatment of the fructose-fed rats markedly reduced the lipid peroxide content of both aortic and cardiac tissues and inhibited the activation of 2 redox-sensitive transcription factors, nuclear factor-kappaB and activating protein-1, which were increased in fructose-fed rats.", "entity1": "nuclear factor-kappaB", "entity2": "fructose", "span1": [203, 224], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12019": {"label": 1, "data": {"text": "Using electrophysiologic techniques, the present study assessed the in vivo action of brexpiprazole on serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, and 5-HT2A; dopamine (DA) D2 autoreceptors, and alpha1- and alpha2-adrenergic receptors.", "entity1": "serotonin (5-HT) receptor", "entity2": "brexpiprazole", "span1": [103, 128], "span2": [86, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10286": {"label": 3, "data": {"text": "An inhibitor of type B monoamine oxidase (MAO-B), (-)deprenyl (selegiline), was reported to have neuroprotective activity, but clinical trials failed to confirm it.", "entity1": "MAO-B", "entity2": "(-)deprenyl", "span1": [42, 47], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8472": {"label": 1, "data": {"text": "Of the new compounds, Dmt(1)-(R)-\u03b2Pro(2)-Trp(3)-(2-furyl)Map(4) (analogue 12) displayed the highest affinity toward MOR, in the picomolar range (Ki(\u03bc) = 3.72 pM).", "entity1": "MOR", "entity2": "(R)-\u03b2Pro", "span1": [116, 119], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13169": {"label": 1, "data": {"text": "Progestin induction of cell cycle progression was also abrogated in cells expressing PR-BDeltaSH3, and no effect of progestin on cyclin D1 expression and cell cycle was observed in the presence of PR-A.", "entity1": "PR-A", "entity2": "progestin", "span1": [197, 201], "span2": [116, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15589": {"label": 8, "data": {"text": "A series of N-substituted lobelane analogues was synthesized and evaluated for their [(3)H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [(3)H]dopamine uptake.", "entity1": "vesicular monoamine transporter", "entity2": "[(3)H]dopamine", "span1": [136, 167], "span2": [206, 220]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4909": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "LDH", "entity2": "glucose", "span1": [155, 158], "span2": [276, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"272": {"label": 1, "data": {"text": "Drosophila GABA-gated chloride channel: modified [3H]EBOB binding site associated with Ala-->Ser or Gly mutants of Rdl subunit.", "entity1": "Drosophila GABA-gated chloride channel", "entity2": "[3H]EBOB", "span1": [0, 38], "span2": [49, 57]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"126": {"label": 3, "data": {"text": "Again, inhibition of the actin-activated myosin Mg2+-ATPase and myosin filament assembly by felodipine and the p-chloro analogue could be reversed by raising the calmodulin concentration.", "entity1": "Mg2+-ATPase", "entity2": "p-chloro", "span1": [48, 59], "span2": [111, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15690": {"label": 1, "data": {"text": "Finally, the involvement of PKC and PKA was also studied, and we showed that both play a role in the antinociceptive mechanism of CAT.", "entity1": "PKA", "entity2": "CAT", "span1": [36, 39], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6722": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "bis(1H-2-indolyl)-1-methanone", "span1": [268, 272], "span2": [86, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3675": {"label": 3, "data": {"text": "Taken together, these findings indicate that the inhibition of melanogenesis by artemisinic acid occurs through reduced expression of the HMG CoA reductase gene, which is mediated by C/EBP \u03b1 inhibition and suggest that artemisinic acid may be useful as a hyperpigmentation inhibitor.", "entity1": "HMG CoA reductase", "entity2": "artemisinic acid", "span1": [138, 155], "span2": [80, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10702": {"label": 4, "data": {"text": "Denufosol tetrasodium (INS37217) is a selective P2Y(2) agonist that stimulates ciliary beat frequency and Cl(-) secretion in normal and cystic fibrosis (CF) airway epithelia, and is being investigated as an inhaled treatment for CF.", "entity1": "P2Y(2)", "entity2": "Denufosol tetrasodium", "span1": [48, 54], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13221": {"label": 9, "data": {"text": "Here we report that glutamate stimulation caused a rapid reduction in protein levels of GRIP1, but not that of glutamate receptor (GluR) 1, GluR2 and protein interacting with C kinase 1 (PICK1) in rat primary cortical neuron cultures.", "entity1": "(GluR) 1", "entity2": "glutamate", "span1": [130, 138], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14563": {"label": 2, "data": {"text": "Liver X Receptor (LXR) \u03b1 and LXR \u03b2 are nuclear receptors activated by oxysterols, oxidized derivatives of cholesterol.", "entity1": "LXR \u03b2", "entity2": "oxysterols", "span1": [29, 34], "span2": [70, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13531": {"label": 1, "data": {"text": "However, upon addition of NO to CDO in the presence of substrate l-cysteine, a low-spin {FeNO}7 (S = 1/2) signal that accounts for approximately 85% of the iron within the enzyme develops.", "entity1": "CDO", "entity2": "NO", "span1": [32, 35], "span2": [26, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13761": {"label": 3, "data": {"text": "A comparison of bosutinib with dasatinib across the whole kinase panel revealed overlapping, but distinct, inhibition profiles.", "entity1": "kinase", "entity2": "dasatinib", "span1": [58, 64], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8586": {"label": 3, "data": {"text": "In addition, fisetin supplementation significantly reduced hepatic mRNA abundance of FAS, ATPCL and G6Pase compared to the control group.", "entity1": "FAS", "entity2": "fisetin", "span1": [85, 88], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10033": {"label": 9, "data": {"text": "Rofecoxib is a selective cyclo-oxygenase (COX)-2 inhibitor which has little or no effect on the COX-1 isoenzyme at doses up to 1000 mg/day.", "entity1": "COX-1", "entity2": "Rofecoxib", "span1": [96, 101], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7593": {"label": 9, "data": {"text": "However, holo-alpha-lactalbumin was unable to bind fatty acids as measured by this technique.", "entity1": "holo-alpha-lactalbumin", "entity2": "fatty acids", "span1": [9, 31], "span2": [51, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"502": {"label": 1, "data": {"text": "Felodipine and nicardipine have similar affinities for 60-kDa CaMPDE isozymes but bring about different levels of enzyme inhibition, suggesting the possibility of designing specific drugs that can protect the enzyme from inhibition by dihydropyridine Ca2+-channel blockers.", "entity1": "CaMPDE", "entity2": "nicardipine", "span1": [62, 68], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7557": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "endothelial nitric oxide synthase", "entity2": "L-citrulline", "span1": [123, 156], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"14573": {"label": 2, "data": {"text": "The aim of the present work was to evaluate the effectiveness of such an antidote by testing whether doxorubicin (DOX), a known P-gp inducer, could efficiently protect Caco-2 cells against PQ cytotoxicity, 6 h after the incubation with the herbicide, reflecting a real-life intoxication scenario.", "entity1": "P-gp", "entity2": "DOX", "span1": [128, 132], "span2": [114, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12693": {"label": 0, "data": {"text": "Identification and characterization of a novel flavin-containing spermine oxidase of mammalian cell origin.", "entity1": "spermine oxidase", "entity2": "flavin", "span1": [65, 81], "span2": [47, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5321": {"label": 3, "data": {"text": "The structure-activity relationships revealed that the free hydroxyl group at position 5 and phosphate group at position 7 of the phosphorylated flavonoids are favorable to the inhibition of CEase.", "entity1": "CEase", "entity2": "hydroxyl", "span1": [191, 196], "span2": [60, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14324": {"label": 2, "data": {"text": "Results showed that DMF increased nuclear levels of Nrf2, and both DMF and adenovirus-mediated overexpression of Nrf2 (Ad-Nrf2) decreased PAI-1, alpha-smooth muscle actin (alpha-SMA), fibronectin and type 1 collagen expression in TGF-beta-treated rat mesangial cells (RMCs) and renal fibroblast cells (NRK-49F).", "entity1": "Nrf2", "entity2": "DMF", "span1": [113, 117], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6351": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "losartan", "span1": [18, 21], "span2": [213, 221]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2302": {"label": 9, "data": {"text": "Inhibition of ERK1/2 with U0126 induces apoptosis but fails to activate JNK phosphorylation or down-regulate beta-catenin protein expression.", "entity1": "JNK", "entity2": "U0126", "span1": [72, 75], "span2": [26, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13421": {"label": 8, "data": {"text": "Furthermore, the enzymatic activity of alanine aminotransferase (ALT), which converts the critical gluconeogenic amino acid alanine into pyruvate, is decreased (approximately 50%) in KLF15-/- hepatocytes.", "entity1": "alanine aminotransferase", "entity2": "alanine", "span1": [39, 63], "span2": [124, 131]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"1066": {"label": 3, "data": {"text": "Troglitazone, a second ACS4 inhibitor, inhibited ACS activity <10% in microsomes and mitochondria and 45% in MAM.", "entity1": "ACS4", "entity2": "Troglitazone", "span1": [23, 27], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10": {"label": 1, "data": {"text": "Iloprost was the most potent: 50% inhibition occurred at 5 nM, a concentration close to the reported dissociation constant for iloprost binding to the platelet prostacyclin receptor.", "entity1": "prostacyclin receptor", "entity2": "iloprost", "span1": [160, 181], "span2": [127, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13277": {"label": 8, "data": {"text": "ABCA1-facilitated cholesterol efflux and lipid parameters did not differ between equol-producing and non-equol-producing women.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [0, 5], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"3317": {"label": 1, "data": {"text": "Mutations in the Ca(2+) sensor, troponin C (TnC), were generated to increase/decrease the Ca(2+) sensitivity of cardiac skinned fibers to create the characteristic effects of DCM, HCM, and RCM.", "entity1": "TnC", "entity2": "Ca(2+)", "span1": [44, 47], "span2": [90, 96]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15643": {"label": 9, "data": {"text": "In contrast, the latter pathway likely involves MHC binding peptides displayed as a consequence of abacavir exposure, but not abacavir itself.", "entity1": "MHC", "entity2": "abacavir", "span1": [48, 51], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"791": {"label": 1, "data": {"text": "We now show that mutation of the 769R/ G desensitization site (Lomeli, H.M.J., Melcher, T., Hoger, T., Geiger, J.R., Kuner, T., Monyer, H., Higuchi, M.B.A. and Seeburg, P.H, Control of kinetic properties of AMPAAMPA receptor channels by nuclear RNA editing.", "entity1": "AMPA receptor", "entity2": "AMPA", "span1": [211, 224], "span2": [207, 211]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8940": {"label": 1, "data": {"text": "The negatively charged estramustine phosphate has been found previously to be a microtubule-associated protein (MAP)-dependent microtubule inhibitor [Wallin M, Deinum J and Friden B, FEBS Lett 179: 289-293, 1985].", "entity1": "MAP", "entity2": "estramustine phosphate", "span1": [112, 115], "span2": [23, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13816": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "Tarceva", "span1": [233, 246], "span2": [178, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13848": {"label": 1, "data": {"text": "A series of 4,5-diaryloxazole analogs were designed and the interaction between oxaprozin and cyclooxygenase-2 studied by the docking method to improve the biological activity and reduce the gastrointestinal side effects of oxaprozin.", "entity1": "cyclooxygenase-2", "entity2": "oxaprozin", "span1": [94, 110], "span2": [80, 89]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2103": {"label": 4, "data": {"text": "The selective beta1AR antagonists atenolol and metoprolol blocked isoproterenol-induced enhancement, with apparent K(b) values of 85 +/- 36 and 3.9 +/- 1.7 nM, respectively.", "entity1": "beta1AR", "entity2": "isoproterenol", "span1": [14, 21], "span2": [66, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11427": {"label": 1, "data": {"text": "We report that a known functional polymorphism in CYP2C9 is highly associated with the maximum dose of phenytoin (P = 0.0066).", "entity1": "CYP2C9", "entity2": "phenytoin", "span1": [50, 56], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1935": {"label": 8, "data": {"text": "Carnitine acetyltransferases (CrAT) catalyze the reversible conversion of acetyl-CoA and carnitine to acetylcarnitine and free CoA.", "entity1": "Carnitine acetyltransferases", "entity2": "acetyl-CoA", "span1": [0, 28], "span2": [74, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"7605": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(2)", "entity2": "Lixivaptan", "span1": [44, 48], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1040": {"label": 1, "data": {"text": "Third, using ciprofloxacin competition assay, TOP2-mediated DNA cleavage induced by ATP-sensitive but not ATP-insensitive poisons was shown to be antagonized by ciprofloxacin.", "entity1": "TOP2", "entity2": "ciprofloxacin", "span1": [46, 50], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11806": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "c-jun", "entity2": "2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine", "span1": [131, 136], "span2": [11, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13957": {"label": 3, "data": {"text": "Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug.", "entity1": "monoamine oxidase (MAO)-B", "entity2": "Rasagiline", "span1": [81, 106], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7598": {"label": 4, "data": {"text": "In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use.", "entity1": "OT", "entity2": "carbetocin", "span1": [112, 114], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5854": {"label": 5, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT3", "entity2": "renzapride", "span1": [5, 10], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5149": {"label": 0, "data": {"text": "This structure, together with biochemical experiments, revealed the existence of a novel binding region in addition to the canonical phosphotyrosine-314 binding site of Cbp.", "entity1": "Cbp", "entity2": "phosphotyrosine", "span1": [169, 172], "span2": [133, 148]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12969": {"label": 1, "data": {"text": "gammaPKC directly associated with DGKgamma through its accessory domain (AD), depending on Ca2+ as well as phosphatidylserine/diolein in vitro.", "entity1": "gammaPKC", "entity2": "Ca2+", "span1": [0, 8], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15523": {"label": 1, "data": {"text": "This effect appeared to be due to both competition between S-nitrosocysteine and Prx1 for the Trx system and direct modulation by S-nitrosocysteine of Trx reductase activity.", "entity1": "Trx", "entity2": "S-nitrosocysteine", "span1": [94, 97], "span2": [59, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12014": {"label": 1, "data": {"text": "We investigated the diurnal expression of clock genes and clock-controlled genes (CCGs) in 3-hour intervals for a 24-h period in the livers of male streptozotocin (STZ)-treated rats, male spontaneous type 1 diabetic LEW.1AR1-iddm (Iddm) rats, and Iddm rats treated for 10 days with insulin.", "entity1": "clock", "entity2": "STZ", "span1": [42, 47], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3660": {"label": 3, "data": {"text": "Using paraoxon as a reference acetylcholinesterase (AChE) inhibitor, the objective of this study was to develop an adverse outcome pathway (AOP) that provided quantitative linkages across levels of biological organization during zebrafish embryogenesis.", "entity1": "acetylcholinesterase", "entity2": "paraoxon", "span1": [30, 50], "span2": [6, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10527": {"label": 2, "data": {"text": "Whether metformin or the satiety factor leptin, which also stimulates AMPK in muscle, regulates this enzyme in pancreatic islets is unknown.", "entity1": "AMPK", "entity2": "metformin", "span1": [70, 74], "span2": [8, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8329": {"label": 3, "data": {"text": "In particular, we showed that Paeoniflorin significantly reduced the formation of intracellular reactive oxygen species (ROS), the level of malondialdehyde (MDA) and lactate dehydrogenase (LDH) leakage, and enhanced production of the endogenous antioxidants, glutathione (GSH) and superoxide dismutase (SOD) in EA.hy926 cells.", "entity1": "lactate dehydrogenase", "entity2": "Paeoniflorin", "span1": [166, 187], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4421": {"label": 3, "data": {"text": "We describe here the isolation and biochemical characterization of the marine natural sesquiterpene palinurin as a GSK-3\u03b2 inhibitor.", "entity1": "GSK-3\u03b2", "entity2": "sesquiterpene", "span1": [115, 121], "span2": [86, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3126": {"label": 2, "data": {"text": "AMPK activators metformin and AICAR partly prevented the cell cycle block, oxidative stress and apoptosis induced by compound C. The small interfering RNA (siRNA) targeting of human AMPK mimicked compound C-induced G(2)/M cell cycle arrest, but failed to induce oxidative stress and apoptosis in U251 glioma cells.", "entity1": "AMPK", "entity2": "AICAR", "span1": [0, 4], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13537": {"label": 1, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha2", "entity2": "Wy-14643", "span1": [188, 198], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10351": {"label": 9, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "BrBK1-5", "entity2": "GW660511X", "span1": [58, 65], "span2": [7, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7786": {"label": 3, "data": {"text": "The PARP inhibitor PJ34 modifies proliferation, NIS expression and epigenetic marks in thyroid cancer cell lines.", "entity1": "PARP", "entity2": "PJ34", "span1": [4, 8], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4282": {"label": 3, "data": {"text": "Interestingly, ursolic acid increased the phosphorylation of AMPK and coenzyme A carboxylase and also enhanced phosphorylation of GSK3\u03b2 at inactive form serine 9, whereas ursolic acid attenuated the phosphorylation of AKT and mTOR in HepG2 cells.", "entity1": "mTOR", "entity2": "ursolic acid", "span1": [226, 230], "span2": [171, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3333": {"label": 3, "data": {"text": "Etoposide (VP-16) is a topoisomerase-II (topo II) inhibitor chemotherapeutic agent.", "entity1": "topoisomerase-II", "entity2": "VP-16", "span1": [23, 39], "span2": [11, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14641": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "DCK", "entity2": "2',2'-difluorodeoxycytidine", "span1": [117, 120], "span2": [19, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15382": {"label": 1, "data": {"text": "These results provide an example that attachment of a bulky side chain to the C-7\u03b1 position of E2 can produce ER antagonists with ER affinity comparable to that of ICI-182,780.", "entity1": "ER", "entity2": "ICI-182,780", "span1": [130, 132], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14459": {"label": 9, "data": {"text": "Unlike the majority of G protein-coupled receptors, the prostaglandin E(2) (PGE(2)) E-prostanoid 3 (EP3) receptor binds agonist with high affinity that is insensitive to the presence of guanosine 5[prime]-O-(3-thio)triphosphate (GTP\u03b3S).", "entity1": "prostaglandin E(2) (PGE(2)) E-prostanoid 3 (EP3) receptor", "entity2": "guanosine 5[prime]-O-(3-thio)triphosphate", "span1": [56, 113], "span2": [186, 227]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6497": {"label": 5, "data": {"text": "The following alpha(2)-adrenoceptor antagonists were applied: BRL44408 (alpha(2A)-selective), ARC239 (alpha(2B)- and alpha(2C)-selective), and prazosin (alpha(2B)- and alpha(2C)-selective).", "entity1": "alpha(2C)", "entity2": "ARC239", "span1": [117, 126], "span2": [94, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9620": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBF1", "entity2": "glibenclamide", "span1": [269, 273], "span2": [120, 133]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2454": {"label": 1, "data": {"text": "CONCLUSION: The peptide sequences containing Tyr, Phe conservative residues identified in this study can bind to cell surface IL-2Ralpha.", "entity1": "IL-2Ralpha", "entity2": "Phe", "span1": [126, 136], "span2": [50, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5867": {"label": 4, "data": {"text": "Therefore, in the present studies, animals were rendered tolerant to the delta-opioid receptor-selective agonist [D-Pen2,D-Pen5]enkephalin (DPDPE), and receptor binding activities were measured.", "entity1": "delta-opioid receptor", "entity2": "DPDPE", "span1": [73, 94], "span2": [140, 145]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3309": {"label": 1, "data": {"text": "Circular dichroism of mutant cTnCs revealed a trend where increased alpha-helical content correlated with increased Ca(2+) sensitivity in skinned fibers and vice versa.", "entity1": "cTnCs", "entity2": "Ca(2+)", "span1": [29, 34], "span2": [116, 122]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8041": {"label": 1, "data": {"text": "Exposure of H9c2 cells to high glucose reduced AMPK activity, inhibited Jun NH2-terminal kinase 1 (JNK1)-B-cell lymphoma 2 (Bcl-2) signaling, and promoted Beclin1 binding to Bcl-2.", "entity1": "Bcl-2", "entity2": "glucose", "span1": [174, 179], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11355": {"label": 8, "data": {"text": "Voltage-gated sodium (Na) channelssodium (Na) channels are a critical component of electrically excitable cells.", "entity1": "Voltage-gated sodium (Na) channels", "entity2": "sodium", "span1": [0, 34], "span2": [34, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1732": {"label": 1, "data": {"text": "Agonist competition assays with [3H]DHA showed the following rank order of potency: isoproterenol>epinephrine> norepinephrine, consistent with beta2AR interaction.", "entity1": "beta2AR", "entity2": "epinephrine", "span1": [143, 150], "span2": [98, 109]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14356": {"label": 3, "data": {"text": "Met-RANTES treatment also reduced the levels of cathepsin K and metalloproteinase 13 (MMP13).", "entity1": "cathepsin K", "entity2": "Met", "span1": [48, 59], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9061": {"label": 1, "data": {"text": "7-Hydroxy levomepromazine, 3-hydroxy levomepromazine and 7-hydroxy fluphenazine had only 10% of the potency of the parent drug in histamine H1 receptor binding, while the 7-hydroxy-metabolites of chlorpromazine and perphenazine had about 75% of the potency of the parent drug in this binding system.", "entity1": "histamine H1 receptor", "entity2": "chlorpromazine", "span1": [130, 151], "span2": [196, 210]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7356": {"label": 2, "data": {"text": "Stimulated P-selectin and integrin alpha(IIb)beta(3) expression were also higher in the upper tertile both before and after aspirin.", "entity1": "integrin alpha(IIb)beta(3)", "entity2": "aspirin", "span1": [26, 52], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6354": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "losartan", "span1": [25, 28], "span2": [104, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7380": {"label": 3, "data": {"text": "RAMH inhibition of cholangiocyte growth was associated with decreased cAMP levels and PKA/ERK1/2/Elk-1 phosphorylation.", "entity1": "Elk-1", "entity2": "RAMH", "span1": [97, 102], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9936": {"label": 3, "data": {"text": "The aim of this study was to define the molecular mechanism by which sulfasalazine inhibits NF-kappaB activation.", "entity1": "NF-kappaB", "entity2": "sulfasalazine", "span1": [92, 101], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13592": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "cocaine", "span1": [6, 10], "span2": [281, 288]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"750": {"label": 1, "data": {"text": "The inhibitory effect of endothelin-1 on the contraction induced by 5-HT is abolished by deendothelialization, by the endothelin ET(B) receptor antagonist RES 701-1, by indomethacin, or by glibenclamide.", "entity1": "endothelin-1", "entity2": "glibenclamide", "span1": [25, 37], "span2": [189, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8672": {"label": 2, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "Bax", "entity2": "cisplatin", "span1": [258, 261], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9506": {"label": 1, "data": {"text": "In conclusion, these findings indicate that [3H]SR 142948A is a new potent antagonist radioligand which recognizes with high affinity both neurotensin NT1 and NT2 receptors and represents thus an excellent tool to study neurotensin receptors in the rat brain.", "entity1": "NT2 receptors", "entity2": "[3H]SR 142948A", "span1": [159, 172], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13937": {"label": 3, "data": {"text": "Thalidomide initiates its teratogenic effects by binding to CRBN and inhibiting the associated ubiquitin ligase activity.", "entity1": "ubiquitin ligase", "entity2": "Thalidomide", "span1": [95, 111], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13392": {"label": 2, "data": {"text": "Cytosolic [AMP] reported metabolically active AMP, which triggered increased AMPK activity, but measures of total AMP did not.", "entity1": "AMPK", "entity2": "AMP", "span1": [77, 81], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2524": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "human b5R", "entity2": "hydroxylamines", "span1": [297, 306], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3399": {"label": 9, "data": {"text": "In addition, PSE inhibited the transcriptional activity of NFAT without interfering with the calcium-induced NFAT dephosphorylation event, which represents the major signaling pathway for its activation.", "entity1": "NFAT", "entity2": "PSE", "span1": [109, 113], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13474": {"label": 8, "data": {"text": "In contrast, the RA catabolising enzymes Cyp26A1 and Cyp26B1 which are known to be RA-responsive were not expressed at all in the developing eye.", "entity1": "Cyp26B1", "entity2": "RA", "span1": [53, 60], "span2": [17, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10140": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "ketoprofen", "span1": [34, 37], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3129": {"label": 1, "data": {"text": "The neuronal vesicular monoamine transporter (VMAT2) is the target molecule of action of some psychostimulants, such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA).", "entity1": "neuronal vesicular monoamine transporter", "entity2": "3,4-methylenedioxymethamphetamine", "span1": [4, 44], "span2": [140, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13465": {"label": 4, "data": {"text": "OBJECTIVE: The aim of this study was to assess the efficacy and tolerability of nebulized arformoterol tartrate (a selective, long-acting beta(2)-adrenergic agonist that is the [R,R] isomer of formoterol) and salmeterol xinafoate versus placebo in patients with chronic obstructive pulmonary disease (COPD).", "entity1": "beta(2)-adrenergic", "entity2": "arformoterol tartrate", "span1": [138, 156], "span2": [90, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5885": {"label": 0, "data": {"text": "Using a similar procedure to analyze ODC labeled by reaction with [5-14C]DFMO, it was found that lysine 69 and cysteine 360 formed covalent adducts with the inhibitor.", "entity1": "ODC", "entity2": "lysine", "span1": [37, 40], "span2": [97, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1612": {"label": 3, "data": {"text": "In whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala, topiramate at low concentrations (IC50, approximately 0.5 microm) selectively inhibited pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit.", "entity1": "GluR5", "entity2": "topiramate", "span1": [284, 289], "span2": [95, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7799": {"label": 5, "data": {"text": "Serotonin-induced or neurotensin-induced reversal was blocked by \u03b2-ARK1 inhibitor, dynasore, or cPKC antagonist 5,6,7,13-tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4c]carbazole-12-propanenitrile (G\u00f66976).", "entity1": "cPKC", "entity2": "G\u00f66976", "span1": [96, 100], "span2": [207, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7751": {"label": 3, "data": {"text": "Further, we used this model to test the efficacy of GDC-0941, a PI3K inhibitor, in clinical development, and showed that the tumors respond to PI3K inhibition.", "entity1": "PI3K", "entity2": "GDC-0941", "span1": [143, 147], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12562": {"label": 1, "data": {"text": "The subtypes of alpha 1-adrenoceptor mediating contractions to exogenous noradrenaline (NA) in rat aorta have been examined in both biochemical and functional studies.", "entity1": "alpha 1-adrenoceptor", "entity2": "NA", "span1": [16, 36], "span2": [88, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9932": {"label": 2, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "NF-kappaB", "entity2": "12-O-tetradecanoylphorbol-13-acetate", "span1": [9, 18], "span2": [72, 108]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11332": {"label": 1, "data": {"text": "In the present study, we measured the enzyme activity of thymidine kinase (TK), thymidine phosphorylase (TP) and thymidilate synthase (TS) in human cancer xenografts to investigate the contribution of these enzymes to the sensitivity of TAS-102.", "entity1": "thymidine kinase", "entity2": "TAS-102", "span1": [57, 73], "span2": [237, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"822": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "sulprostone", "span1": [258, 275], "span2": [119, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9356": {"label": 2, "data": {"text": "Expressions of insulin and PC3, but not PC2, are coordinately regulated by glucose, consistent with the important role of PC3 in regulating proinsulin processing.", "entity1": "PC3", "entity2": "glucose", "span1": [27, 30], "span2": [75, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11327": {"label": 1, "data": {"text": "Receptor trafficking demonstrated surface expression of beta2AR with vehicle treatment and internalization following isoproterenol treatment.", "entity1": "beta2AR", "entity2": "isoproterenol", "span1": [56, 63], "span2": [117, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"321": {"label": 0, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "RNase A", "entity2": "alanine", "span1": [97, 104], "span2": [128, 135]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8688": {"label": 3, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "BAX", "entity2": "imatinib", "span1": [152, 155], "span2": [27, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3761": {"label": 2, "data": {"text": "Sulfhydration of sulfonylurea receptor 2B (SUR2B) was induced by NaHS and colonic inflammation.", "entity1": "sulfonylurea receptor 2B", "entity2": "NaHS", "span1": [17, 41], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7416": {"label": 5, "data": {"text": "MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate), a noncompetitive NMDA receptor antagonist, partially prevented the decrease in cell viability and the energy impairment.", "entity1": "NMDA receptor", "entity2": "(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate", "span1": [100, 113], "span2": [8, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8481": {"label": 0, "data": {"text": "Interestingly, insulin treatment of \u03b1XBPKD cells reduced tyrosine phosphorylation of IRS-1 (pY(896)), and phosphorylation of Akt, while enhancing serine phosphorylation (pS(307)) of IRS-1.", "entity1": "IRS-1", "entity2": "tyrosine", "span1": [85, 90], "span2": [57, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1928": {"label": 8, "data": {"text": "Carnitine acetyltransferases (CrAT) catalyze the reversible conversion of acetyl-CoA and carnitine to acetylcarnitine and free CoA.", "entity1": "CrAT", "entity2": "carnitine", "span1": [30, 34], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"14376": {"label": 3, "data": {"text": "These findings suggest that NFD inhibited the EGF-induced invasion and migration of MDA-MB-231 cells via EGFR-dependent PI3K/Akt signaling, leading to the down-regulation of MMP-9 expression.", "entity1": "MMP-9", "entity2": "NFD", "span1": [174, 179], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13087": {"label": 1, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "sulfonylurea receptor", "entity2": "sulfonylureas", "span1": [84, 105], "span2": [135, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1431": {"label": 3, "data": {"text": "They included the COX-1 inhibitor indomethacin; the COX-2 inhibitor NS-398; the mixed COX-1/COX-2 inhibitor ibuprofen; the nitric oxide (NO) derivatives of indomethacin, ibuprofen and flurbiprofen; the 5-LOX inhibitor REV 5901; and the 5-LOX activating protein (FLAP) inhibitor MK-886.", "entity1": "COX-2", "entity2": "NS-398", "span1": [52, 57], "span2": [68, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10261": {"label": 8, "data": {"text": "Our observations indicate an OCT-mediated transmembrane transport of [3H]-MPP+.", "entity1": "OCT", "entity2": "[3H]-MPP+", "span1": [29, 32], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5447": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "AR", "entity2": "juglone", "span1": [100, 102], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15830": {"label": 8, "data": {"text": "However, enzymes contributing to oxidative metabolism of anandamide, namely cyclooxygenase-1 and Cyp2D6, were increased in the brain of aged mice, possibly enhancing the oxidative breakdown of anandamide.", "entity1": "cyclooxygenase-1", "entity2": "anandamide", "span1": [76, 92], "span2": [193, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4529": {"label": 2, "data": {"text": "Our results showed that low dose BPA and E2 could influence the mammosphere area of iDMECs and upregulate the expression level of Oct4 and Nanog proteins, while only BPA could downregulate the expression of E-cadherin protein.", "entity1": "Nanog", "entity2": "BPA", "span1": [139, 144], "span2": [33, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3987": {"label": 3, "data": {"text": "In addition, BGG-mediated inhibition of AR prevented LPS-induced activation of JNK and p38 and lowered ROS levels, which could inhibit LPS-induced apoptosis.", "entity1": "JNK", "entity2": "BGG", "span1": [79, 82], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3182": {"label": 2, "data": {"text": "CDCA induced dose-dependent expression of Cdx2 and MUC2 at both the mRNA and protein levels.", "entity1": "MUC2", "entity2": "CDCA", "span1": [51, 55], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1471": {"label": 8, "data": {"text": "These results suggest that the altered gamma-glutamyl kinase results in stabilization of the complex or has an indirect effect on gamma-glutamyl phosphate reductase activity, which leads to an increase in L-proline production in Saccharomyces cerevisiae.", "entity1": "gamma-glutamyl kinase", "entity2": "L-proline", "span1": [39, 60], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11369": {"label": 1, "data": {"text": "In intact CHO-K1 cells, I3A was able to translocate different green fluorescent protein-tagged PKC isoforms, visualized by confocal microscopy, with equal or higher potency than PMA.", "entity1": "PKC", "entity2": "PMA", "span1": [95, 98], "span2": [178, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3515": {"label": 1, "data": {"text": "TZD effects on osteoblast viability, oleic acid uptake, alkaline phosphatase and osteocalcin production are independent of their effects on aromatase.", "entity1": "osteocalcin", "entity2": "TZD", "span1": [81, 92], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13696": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "gardiquimod", "span1": [100, 104], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14734": {"label": 3, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "p66Shc", "entity2": "Apocynin", "span1": [169, 175], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6124": {"label": 8, "data": {"text": "In addition, another drug that is both a substrate of uptake1 and a MAO inhibitor, debrisoquine, was investigated in the study.", "entity1": "uptake1", "entity2": "debrisoquine", "span1": [54, 61], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"2429": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "mitochondrial arginase II", "entity2": "L-arginine", "span1": [234, 259], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1829": {"label": 1, "data": {"text": "As is the case with BLTs, glyburide increased the apparent affinity of HDL binding to SR-BI.", "entity1": "SR-BI", "entity2": "glyburide", "span1": [86, 91], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6559": {"label": 3, "data": {"text": "In contrast, the mutants T844A, F972A and Q975A showed increased K(i) for cilostazol but no difference for milrinone from the recombinant PDE3A.", "entity1": "F972A", "entity2": "milrinone", "span1": [32, 37], "span2": [107, 116]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11399": {"label": 1, "data": {"text": "Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties.", "entity1": "KCNQ2/Q3", "entity2": "Meclofenamic acid", "span1": [53, 61], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14332": {"label": 3, "data": {"text": "Results showed that DMF increased nuclear levels of Nrf2, and both DMF and adenovirus-mediated overexpression of Nrf2 (Ad-Nrf2) decreased PAI-1, alpha-smooth muscle actin (alpha-SMA), fibronectin and type 1 collagen expression in TGF-beta-treated rat mesangial cells (RMCs) and renal fibroblast cells (NRK-49F).", "entity1": "type 1 collagen", "entity2": "DMF", "span1": [200, 215], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2117": {"label": 1, "data": {"text": "Pre-treatment of animals with dexamethasone or indomethacin reduced DEC's efficacy by almost 90% or 56%, respectively, supporting a role for the arachidonic acid and cyclooxygenase pathways in vivo.", "entity1": "cyclooxygenase", "entity2": "indomethacin", "span1": [166, 180], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15533": {"label": 2, "data": {"text": "CK significantly inhibited DMN-induced increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, fibrosis score, and hepatic malondialdehyde and collagen content.", "entity1": "ALT", "entity2": "DMN", "span1": [84, 87], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11975": {"label": 1, "data": {"text": "Furanodiene Presents Synergistic Anti-proliferative Activity With Paclitaxel Via Altering Cell Cycle and Integrin Signaling in 95-D Lung Cancer Cells.", "entity1": "Integrin", "entity2": "Paclitaxel", "span1": [105, 113], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13724": {"label": 2, "data": {"text": "RTX treatment also induced foci of RAD51, gamma-H2AX, phospho-Chk1, and phospho-NBS1, although the extent of co-localization with RPA2 foci varied.", "entity1": "gamma-H2AX", "entity2": "RTX", "span1": [42, 52], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6469": {"label": 8, "data": {"text": "Diacylglycerol kinase (DGK) catalyzes the conversion of diacylglycerol to phosphatidic acid, making it an attractive candidate for a signal transduction component.", "entity1": "Diacylglycerol kinase", "entity2": "phosphatidic acid", "span1": [0, 21], "span2": [74, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"12003": {"label": 3, "data": {"text": "CP[c]Ph has, comparably to B[a]P, a potential to repress expression of tumor suppressor p53, in the head kidney of rainbow trout.", "entity1": "tumor suppressor p53", "entity2": "CP[c]Ph", "span1": [71, 91], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15812": {"label": 3, "data": {"text": "Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.", "entity1": "CHK1", "entity2": "imidazo[1,2-c]pyrimidine", "span1": [23, 27], "span2": [78, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11580": {"label": 1, "data": {"text": "In large, well designed phase III trials in patients with type 2 diabetes mellitus, sitagliptin 100 or 200mg once daily alone or in combination with other antihyperglycaemics was associated with significant improvements relative to placebo in overall glycaemic control and indices for insulin response and beta-cell function.", "entity1": "insulin", "entity2": "sitagliptin", "span1": [285, 292], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10988": {"label": 4, "data": {"text": "Preincubation (30 min) of bovine tracheal smooth muscle with various concentrations (0.1, 1 and 10 microM) of fenoterol decreased isoprenaline-induced maximal relaxation (E(max)) of methacholine-contracted preparations in a concentration dependent fashion, indicating desensitization of the beta(2)-adrenoceptor.", "entity1": "beta(2)-adrenoceptor", "entity2": "isoprenaline", "span1": [291, 311], "span2": [130, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13948": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g.", "entity1": "beta(2)-adrenoceptor", "entity2": "salmeterol", "span1": [35, 55], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3591": {"label": 1, "data": {"text": "Taken together, these results suggest that wogonoside partially inhibits MDA-MB-231 cell growth by inducing autophagy through the MAPK-mTOR pathway and may be a promising anti-tumor agent.", "entity1": "mTOR", "entity2": "wogonoside", "span1": [135, 139], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11428": {"label": 1, "data": {"text": "In the presence of alphaAR blockade, concentration-response curves for isoproterenol, norepinephrine, and epinephrine suggested that a beta1AR was involved in this response, and the rank order of potency was isoproterenol > norepinephrine = epinephrine.", "entity1": "beta1AR", "entity2": "isoproterenol", "span1": [135, 142], "span2": [71, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14672": {"label": 3, "data": {"text": "Here, we report that genistein at physiologically relevant concentrations (0.1-10 \u03bcM) significantly inhibited thrombin-induced increase in endothelial monolayer permeability.", "entity1": "thrombin", "entity2": "genistein", "span1": [110, 118], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11707": {"label": 2, "data": {"text": "DBDCT also caused the phosphorylation of JNK and p38(MAPK).", "entity1": "JNK", "entity2": "DBDCT", "span1": [41, 44], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15174": {"label": 2, "data": {"text": "Correlating with FSH\u03b2 activation, both PKA activity and levels of pCREB were increased to a greater extent by low compared with high GnRH pulse frequencies, and the induction of pCREB was also attenuated by overexpression of DNPKA at both low and high pulse frequencies.", "entity1": "pCREB", "entity2": "GnRH", "span1": [66, 71], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9646": {"label": 5, "data": {"text": "Our data indicate that estramustine phosphate metabolites perform as androgen antagonists of AR, an additional mechanism involved in the therapeutic effect of estramustine phosphate in patients with prostate cancer.", "entity1": "AR", "entity2": "estramustine phosphate", "span1": [93, 95], "span2": [23, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12317": {"label": 8, "data": {"text": "Although acetylcholinesterase (AChE) is primarily a hydrolytic enzyme, metabolising the neurotransmitter acetylcholine in cholinergic synapses, it also has some non-catalytic functions in the brain which are far less well characterised.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [9, 29], "span2": [105, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6179": {"label": 3, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "Cl- channels", "entity2": "ibuprofen", "span1": [187, 199], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2515": {"label": 3, "data": {"text": "Auranofin, as an anti-rheumatic gold compound, suppresses LPS-induced homodimerization of TLR4.", "entity1": "TLR4", "entity2": "Auranofin", "span1": [90, 94], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"371": {"label": 3, "data": {"text": "GCS therapy results in reduced mRNA expression of interleukin-4 (IL-4) and IL-5 in cells from bronchoalveolar lavage (BAL) but not of IFN-gamma.", "entity1": "IL-5", "entity2": "GCS", "span1": [75, 79], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12847": {"label": 1, "data": {"text": "However, there were some significant differences among Captopril (30 mg/kg or 45 mg/kg), enalapril (20 mg/kg), and N-acetylcysteine particular in the activity of PON1 and ACE.", "entity1": "ACE", "entity2": "N-acetylcysteine", "span1": [171, 174], "span2": [115, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7042": {"label": 5, "data": {"text": "Functional and bioenergetic consequences of AT1 antagonist olmesartan medoxomil in hearts with postinfarction LV remodeling.", "entity1": "AT1", "entity2": "olmesartan medoxomil", "span1": [44, 47], "span2": [59, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10976": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "protein kinase C", "entity2": "PMA", "span1": [35, 51], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9818": {"label": 4, "data": {"text": "Iontophoresis of +/- propranolol, whose serotonergic actions include antagonism and partial agonism at 5-HT1 receptors, also increased serotonin and decreased firing (n=4).", "entity1": "5-HT1", "entity2": "+/- propranolol", "span1": [103, 108], "span2": [17, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6885": {"label": 1, "data": {"text": "ABCG5 and ABCG8 themselves are regulated by cholesterol via liver X receptors (LXRs), which are also activated by oxysterols and some derivatives of plant sterols.", "entity1": "ABCG8", "entity2": "cholesterol", "span1": [10, 15], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13939": {"label": 1, "data": {"text": "With the pentapeptide linked through the C7alpha position of estradiol, the resulting PROTAC shows the most effective ER degradation and highest affinity for the estrogen receptor.", "entity1": "estrogen receptor", "entity2": "estradiol", "span1": [162, 179], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7413": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "NR2A", "entity2": "glycine", "span1": [19, 23], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1675": {"label": 2, "data": {"text": "In alpha2B-receptor-expressing HEK293 cells, etomidate rapidly increased phosphorylation of the extracellular signal-related kinases ERK1/2.", "entity1": "ERK1/2", "entity2": "etomidate", "span1": [133, 139], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14769": {"label": 1, "data": {"text": "Electrical Stimuli Release ATP to Increase GLUT4 Translocation and Glucose Uptake via PI3K\u03b3-Akt-AS160 in Skeletal Muscle Cells.", "entity1": "AS160", "entity2": "ATP", "span1": [96, 101], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7333": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT1", "entity2": "glutamine", "span1": [235, 240], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5860": {"label": 5, "data": {"text": "A number of selective 5-HT3 antagonists have been developed including ondansetron, granisetron, tropisetron renzapride and zacopride.", "entity1": "5-HT3", "entity2": "renzapride", "span1": [22, 27], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13052": {"label": 4, "data": {"text": "CONTEXT: Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for insomnia treatment.", "entity1": "MT2 melatonin receptor", "entity2": "Ramelteon", "span1": [38, 60], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6085": {"label": 1, "data": {"text": "These results suggest that amantadine induction of Fos in the rat striatum is related to dopamine D1 and NMDA receptors.", "entity1": "NMDA receptors", "entity2": "amantadine", "span1": [105, 119], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4612": {"label": 8, "data": {"text": "Although glutathione S-transferase omega 1 (GSTO1) and arsenic methyltransferase have been shown or thought to catalyze DMAs(V) reduction, their role in DMAs(V) reduction in vivo, or in cell extracts is uncertain.", "entity1": "arsenic methyltransferase", "entity2": "DMAs(V)", "span1": [55, 80], "span2": [120, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5775": {"label": 9, "data": {"text": "This binding was not significantly inhibited by the lysine analogue epsilon-amino caproic acid (EACA), indicating that plasminogen binding was not just through lysine binding sites as suggested for other plasminogen binding sites.", "entity1": "plasminogen", "entity2": "epsilon-amino caproic acid", "span1": [119, 130], "span2": [68, 94]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1159": {"label": 9, "data": {"text": "Patch-clamp analysis using inside-out recording configuration showed that mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 microM).", "entity1": "SUR2B", "entity2": "mitiglinide", "span1": [241, 246], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12091": {"label": 8, "data": {"text": "The results suggest that most of the HVA in plasma is derived from deamination of DA by MAO-A in peripheral neurons; that DOPAC in plasma is derived from cells outside the central nervous system; that DHPG in plasma is derived virtually exclusively from the metabolism of norepinephrine in sympathetic nerve endings and that residual levels of HVA after treatment with debrisoquin provide an improved but limited indication of central dopaminergic activity.", "entity1": "MAO-A", "entity2": "HVA", "span1": [88, 93], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11802": {"label": 1, "data": {"text": "In this study, we assessed the antitumor activity of PTE against human osteosarcoma cells and explored the role of JAK2/STAT3 and apoptosis-related signaling pathways on the activity of PTE.", "entity1": "JAK2", "entity2": "PTE", "span1": [115, 119], "span2": [186, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3270": {"label": 1, "data": {"text": "Remarkably, TFP binding results in the assembly of five Ca(2+)-S100A4/TFP dimers into a tightly packed pentameric ring.", "entity1": "S100A4", "entity2": "TFP", "span1": [63, 69], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12535": {"label": 1, "data": {"text": "Adenosine analogs in particular the N6-substituted compounds are more potent at A1 receptors than at A2 receptors.", "entity1": "A1 receptors", "entity2": "N6", "span1": [80, 92], "span2": [36, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12108": {"label": 3, "data": {"text": "Molecular determinants of dofetilide block of HERG K+ channels.", "entity1": "K+ channels", "entity2": "dofetilide", "span1": [51, 62], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7743": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "RET", "entity2": "XL184", "span1": [120, 123], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7707": {"label": 3, "data": {"text": "atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans.", "entity1": "AChE", "entity2": "OP", "span1": [10, 14], "span2": [166, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"777": {"label": 3, "data": {"text": "Preferential block of late sodium current in the LQT3 DeltaKPQ mutant by the class I(C) antiarrhythmic flecainide.", "entity1": "LQT3 DeltaKPQ mutant", "entity2": "flecainide", "span1": [49, 69], "span2": [103, 113]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3217": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "gallic acid", "span1": [286, 296], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13218": {"label": 9, "data": {"text": "The GRIP1 reduction was inhibited by MK-801, an N-methyl-d-aspartate (NMDA) receptor antagonist, but not by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an AMPA receptor antagonist.", "entity1": "GRIP1", "entity2": "6-cyano-7-nitroquinoxaline-2,3-dione", "span1": [4, 9], "span2": [108, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11971": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "pip5k1\u03b2", "entity2": "PI(4)P", "span1": [68, 75], "span2": [193, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9981": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "NSD-1015", "span1": [80, 84], "span2": [201, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"914": {"label": 1, "data": {"text": "Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists.", "entity1": "Na(+) channels", "entity2": "Betaxolol", "span1": [121, 135], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12306": {"label": 1, "data": {"text": "It was hypothesized that because Hg accumulates in the proximal tubules (PTs), glutathione-S-transferases (GST)-\u03b1 (suggestive of kidney damage at the level of PT) would be expected to be more related to Hg exposure than GST-\u03c0 (suggestive of kidney damage at the level of the distal tubules).", "entity1": "glutathione-S-transferases (GST)-\u03b1", "entity2": "Hg", "span1": [79, 113], "span2": [203, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10900": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "CDKs", "entity2": "(R)-Roscovitine", "span1": [102, 106], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3130": {"label": 1, "data": {"text": "The neuronal vesicular monoamine transporter (VMAT2) is the target molecule of action of some psychostimulants, such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA).", "entity1": "VMAT2", "entity2": "3,4-methylenedioxymethamphetamine", "span1": [46, 51], "span2": [140, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10413": {"label": 1, "data": {"text": "RESULTS: Rolipram unmasked the inhibitory effect of beta(2)-adrenoceptor stimulation with salmeterol and significantly attenuated the stimulated release of AA and subsequent LTC(4).", "entity1": "beta(2)-adrenoceptor", "entity2": "Rolipram", "span1": [52, 72], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8804": {"label": 8, "data": {"text": "Rates of benzydamine N-oxygenation (catalyzed by FMO3) varied (approximately 20-fold) among the 28 cynomolgus livers and were significantly correlated with FMO3 protein expression, indicating that the inter-animal variations in benzydamine N-oxygenation might be partly accounted for by the variable FMO3 expression.", "entity1": "FMO3", "entity2": "benzydamine", "span1": [49, 53], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6995": {"label": 2, "data": {"text": "On the other hand, holocarboxylase synthetase (HCS) mRNA levels were markedly low in the deficient animals, and increased upon biotin injection.", "entity1": "holocarboxylase synthetase", "entity2": "biotin", "span1": [19, 45], "span2": [127, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10359": {"label": 2, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK1-8", "entity2": "GW660511X", "span1": [59, 66], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"11718": {"label": 1, "data": {"text": "CYP3A activity and protein levels in rat liver microsomes pretreated with oral AC were also measured using in vitro buspirone metabolism and Western blot.", "entity1": "CYP3A", "entity2": "buspirone", "span1": [0, 5], "span2": [116, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5031": {"label": 5, "data": {"text": "Synthesis and in Vitro Characterisation of Ifenprodil-Based Fluorescein Conjugates as GluN1/GluN2B N-Methyl-D-aspartate Receptor Antagonists.", "entity1": "N-Methyl-D-aspartate Receptor", "entity2": "Ifenprodil", "span1": [99, 128], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11168": {"label": 1, "data": {"text": "Both the phosphotriesterase and physostigmine treatments protected the brain AChE activities measured 24 h after sarin exposure.", "entity1": "AChE", "entity2": "sarin", "span1": [77, 81], "span2": [113, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14964": {"label": 1, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANK", "entity2": "serine", "span1": [158, 162], "span2": [84, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8965": {"label": 4, "data": {"text": "The Schild plots for the competitive antagonists WB4101 and 5-methyl-urapidil against alpha 1a-adrenoceptor-selective agonist methoxamine-induced contraction were linear and had slopes not significantly different from unity, with a pA2 of 9.07 +/- 0.07 (n = 5) for WB4101 and 9.09 +/- 0.05 (n = 3) for 5-methyl-urapidil.", "entity1": "alpha 1a-adrenoceptor", "entity2": "methoxamine", "span1": [86, 107], "span2": [126, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8162": {"label": 3, "data": {"text": "Furthermore, DPEP inhibited the LPS-induced phosphorylation of inhibitor \u03baB (I\u03baB)-\u03b1 and NF-\u03baB p50.", "entity1": "p50", "entity2": "DPEP", "span1": [94, 97], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5269": {"label": 2, "data": {"text": "In fact, we demonstrated a significant stimulation of Nox4 activity by 4 quinone derivatives (AA-861, tBuBHQ, tBuBQ, and duroquinone) observed in 3 different cellular models, HEK293E, T-REx\u2122, and chondrocyte cell lines.", "entity1": "Nox4", "entity2": "quinone", "span1": [54, 58], "span2": [73, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4424": {"label": 3, "data": {"text": "Moreover, molecular dynamics simulations have identified an allosteric mechanism by which binding of palinurin leads to GSK-3\u03b2 inhibition.", "entity1": "GSK-3\u03b2", "entity2": "palinurin", "span1": [120, 126], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"329": {"label": 1, "data": {"text": "The folding rate monitored by 2'CMP binding to the major slow-folding species of Pro42Ala RNase A is faster than the folding rate monitored by tyrosine burial; however, the folding rate monitored by inhibitor binding to the minor slow-folding species is decreased significantly over the folding rate monitored by tyrosine burial, indicating that the major and minor slow-folding species of Pro42Ala fold to the native state with different transition-state conformations in the rate-determining step.", "entity1": "RNase A", "entity2": "tyrosine", "span1": [90, 97], "span2": [313, 321]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"946": {"label": 3, "data": {"text": "Endogenously produced asymmetrically methylated arginine residues are competitive inhibitors of all three isoforms of nitric oxide synthase (NOS).", "entity1": "nitric oxide synthase", "entity2": "arginine", "span1": [118, 139], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10379": {"label": 3, "data": {"text": "In this work a novel approach combining HPLC-UV on-line with oaTOF-MS and ICPMS was applied to investigate in human and rat plasma the metabolism of labelled BK (79/81 Br-Phe5) BrBK in the presence of two new dual ACE/NEP inhibitors (GW660511X and omapatrilat) currently under clinical trial.", "entity1": "NEP", "entity2": "omapatrilat", "span1": [218, 221], "span2": [248, 259]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8200": {"label": 3, "data": {"text": "In addition, derivatives of caffeic acid and sinapic acid efficiently inhibited tyrosinase activity and reduced melanin content in melanocytes Mel-Ab cell.", "entity1": "tyrosinase", "entity2": "caffeic acid", "span1": [80, 90], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15457": {"label": 3, "data": {"text": "Based on our previously published work on CXCR4 antagonists, we have synthesized a series of aryl sulfonamides that inhibit the CXCR4/CXCL12 interaction.", "entity1": "CXCR4", "entity2": "aryl sulfonamides", "span1": [128, 133], "span2": [93, 110]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6510": {"label": 3, "data": {"text": "There was a dose-dependent decrease in plasma renin activity, Ang I, and Ang II following single doses of Aliskiren starting with 40 mg. Inhibition was still marked and significant after repeated dosing with maximal decreases in Ang II levels by 89% and 75% on Days 1 and 8, respectively, when the highest dose of Aliskiren was compared with placebo.", "entity1": "Ang I", "entity2": "Aliskiren", "span1": [62, 67], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15198": {"label": 3, "data": {"text": "In another experiment, topical application of CFB, CFE or CLS prior to UVB irradiation (200mJ/cm(2)) on BALB/c mice, inhibited the UVB-elevated protein levels of COX-2, iNOS, and TNF-\u03b1.", "entity1": "TNF-\u03b1", "entity2": "CLS", "span1": [179, 184], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3090": {"label": 4, "data": {"text": "Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders.", "entity1": "MT1", "entity2": "ramelteon", "span1": [39, 42], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14186": {"label": 3, "data": {"text": "Mass spectral analysis of CBDP-inhibited BChE digested with Glu-C showed an o-hydroxybenzyl adduct (+106amu) on lysine 499, a residue far from the active site, but not on His-438.", "entity1": "BChE", "entity2": "CBDP", "span1": [41, 45], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2042": {"label": 8, "data": {"text": "L-serine dehydratase (SDH), a member of the beta-family of pyridoxal phosphate-dependent (PLP) enzymes, catalyzes the deamination of L-serine and L-threonine to yield pyruvate or 2-oxobutyrate.", "entity1": "SDH", "entity2": "L-threonine", "span1": [22, 25], "span2": [146, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6421": {"label": 2, "data": {"text": "Since it has been proposed that UCP-3 could be involved in the regulation of the use of fatty acids as fuel substrates, the UCP-3 induction achieved after bezafibrate and Wy-14, 643 treatment may indicate a higher oxidation of fatty acids, limiting their availability to be stored as triglycerides.", "entity1": "UCP-3", "entity2": "Wy-14, 643", "span1": [124, 129], "span2": [171, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7447": {"label": 9, "data": {"text": "Further, treatment of female mice depleted of GSH with L-BOAA did not induce inhibition of complex I indicating that GSH levels were not critical for maintaining complex I activity in female mice unlike their male counterpart.", "entity1": "complex I", "entity2": "L-BOAA", "span1": [91, 100], "span2": [55, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9701": {"label": 5, "data": {"text": "Pretreatment with the 5-HT1A antagonist WAY-100,635 (10 micrograms/kg i.v.) prevented the ziprasidone-induced inhibition; the same dose of WAY-100,635 had little effect on the inhibition produced by clozapine and olanzapine.", "entity1": "5-HT1A", "entity2": "WAY-100,635", "span1": [22, 28], "span2": [139, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14309": {"label": 8, "data": {"text": "Cu-dependent tyrosinase activity was also markedly reduced in both types of CLDN knockdown cells when incubated with the substrate l-DOPA.", "entity1": "tyrosinase", "entity2": "l-DOPA", "span1": [13, 23], "span2": [131, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1621": {"label": 3, "data": {"text": "The cytosine analog 5-aza-2'-deoxycytidine (decitabine) hypomethylates DNA by inhibiting DNA methyltransferase.", "entity1": "DNA methyltransferase", "entity2": "5-aza-2'-deoxycytidine", "span1": [89, 110], "span2": [20, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8727": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "amitriptyline", "span1": [178, 184], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5307": {"label": 8, "data": {"text": "Introduction: 5-Lipoxygenase (5-LO) is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) with the help of FLAP, the 5-LO-activating protein.", "entity1": "5-LO", "entity2": "arachidonic acid", "span1": [30, 34], "span2": [63, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10179": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "human organic anion transporting polypeptide 8", "entity2": "rifamycin SV", "span1": [171, 217], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11262": {"label": 4, "data": {"text": "D-Serine was previously identified in mammalian brain and was shown to be a co-agonist at the 'glycine' site of the N-methyl-D-aspartate (NMDA)-type receptors.", "entity1": "N-methyl-D-aspartate (NMDA)-type receptors", "entity2": "D-Serine", "span1": [116, 158], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8123": {"label": 2, "data": {"text": "The reduction of BiFC signal mediated by nutlin-3 was correlated with an increase in Puma transactivation, PARP cleavage, and cell death.", "entity1": "Puma", "entity2": "nutlin-3", "span1": [85, 89], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4662": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "NOX4", "entity2": "resveratrol", "span1": [159, 163], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15939": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "insulin", "entity2": "metformin", "span1": [139, 146], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14412": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "Akt", "entity2": "nucleotide", "span1": [288, 291], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4407": {"label": 1, "data": {"text": "NCFP binds to the CPPHA site on mGlu5 and potentiates mGlu5-mediated responses in both recombinant and native systems.", "entity1": "mGlu5", "entity2": "NCFP", "span1": [32, 37], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6541": {"label": 3, "data": {"text": "Chronic treatment with the NET inhibitor, desipramine (DMI), reduced NET levels in both control and Dbh -/- mice, demonstrating that NE is not required for the regulation of NET by antidepressant drugs.", "entity1": "NET", "entity2": "desipramine", "span1": [27, 30], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2487": {"label": 3, "data": {"text": "Licofelone reduced intima/media ratio in injured arteries, the macrophages infiltration in the neointimal area, monocyte chemoattractant protein-1 (MCP-1) gene expression, and the activation of nuclear factor-kappaB in rabbit atheroma.", "entity1": "MCP-1", "entity2": "Licofelone", "span1": [148, 153], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5964": {"label": 3, "data": {"text": "These data suggested that ambenonium had a dual effect on tissue responses to acetylcholine-producing potentiation by blockade of acetylcholinesterase and concomitant antagonism by blockade of muscarinic receptors.", "entity1": "muscarinic receptors", "entity2": "ambenonium", "span1": [193, 213], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4030": {"label": 3, "data": {"text": "We show that both darapladib and a novel class of structurally distinct carbamate inhibitors inactivate Lp-PLA(2) in mouse tissues and human cell lines with high selectivity.", "entity1": "Lp-PLA(2)", "entity2": "carbamate", "span1": [104, 113], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5440": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "ScCA", "entity2": "tyrphostine", "span1": [196, 200], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10350": {"label": 9, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK2-8", "entity2": "omapatrilat", "span1": [107, 114], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"6430": {"label": 3, "data": {"text": "The group treated with pyridostigmine alone showed decreased plasma butyrylcholinesterase (BChE) activity (87% of control), whereas pyridostigmine plus exercise significantly decreased the BChE activity (79% of control), indicating an interactive effect of the combination.", "entity1": "butyrylcholinesterase", "entity2": "pyridostigmine", "span1": [68, 89], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3895": {"label": 3, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "Myc", "entity2": "N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine", "span1": [60, 63], "span2": [85, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14117": {"label": 3, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "Lenalidomide", "span1": [62, 66], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9489": {"label": 3, "data": {"text": "Monoamine uptake inhibitors structurally analogous to cocaine (cocaethylene, CFT, betaCIT, CPT, (+)-cocaine, norcocaine, and benztropine) also produced this rapid pressor response, whereas structurally unrelated uptake inhibitors with diverse monoamine transporter selectivities (BTCP, indatraline, GBR 12935, mazindol, nomifensine, and zimeldine) either did not produce a rapid pressor response or produced only a small pressor response.", "entity1": "monoamine transporter", "entity2": "BTCP", "span1": [243, 264], "span2": [280, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, 9]},
	"7422": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "D6D", "entity2": "docosahexaenoic acid", "span1": [31, 34], "span2": [102, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13187": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "DAT", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane", "span1": [278, 281], "span2": [0, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3894": {"label": 3, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "c-Myc", "entity2": "N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine", "span1": [53, 58], "span2": [85, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8006": {"label": 3, "data": {"text": "In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-\u03b1-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.", "entity1": "PAI-1", "entity2": "hyperoside", "span1": [101, 106], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13214": {"label": 9, "data": {"text": "Triflusal (30 mg/kg) also significantly decreased the protein levels of IL-Ibeta but not nuclear factor kappa B or tumor necrosis factor-alpha in the cortex ipsilateral to the middle cerebral artery occlusion.", "entity1": "tumor necrosis factor-alpha", "entity2": "Triflusal", "span1": [115, 142], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2310": {"label": 2, "data": {"text": "Sulindac metabolites simultaneously (a) increase cellular cyclic GMP and subsequently activate cyclic GMP-dependent protein kinase (PKG); (b) activate c-jun NH2-terminal kinase (JNK); (c) inhibit extracellular signal-regulated kinase 1/2 (ERK1/2); and (d) decrease beta-catenin protein expression at times and doses consistent with apoptosis.", "entity1": "PKG", "entity2": "Sulindac", "span1": [132, 135], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12134": {"label": 1, "data": {"text": "In contrast to UCP-3, UCP-2 mRNA levels were only slightly modified by bezafibrate in adipocytes.", "entity1": "UCP-3", "entity2": "bezafibrate", "span1": [15, 20], "span2": [71, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15587": {"label": 1, "data": {"text": "Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse.", "entity1": "VMAT2", "entity2": "nor-lobelane", "span1": [79, 84], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8754": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "imipramine", "span1": [178, 184], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5311": {"label": 9, "data": {"text": "Despite normal binding, autoactivation of mutants D22G and K23_I24insIDK was not stimulated by calcium.", "entity1": "D22G", "entity2": "calcium", "span1": [50, 54], "span2": [95, 102]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7179": {"label": 3, "data": {"text": "Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4(3H)-quinazolinone analogs.", "entity1": "dihydrofolate reductase", "entity2": "4(3H)-quinazolinone", "span1": [11, 34], "span2": [107, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4937": {"label": 3, "data": {"text": "The mechanism of action of Fc11a-2 was related to the inhibition of the cleavage of pro-caspase-1, pro-IL-1\u03b2 and pro-IL-18 which in turn suppressed the activation of NLRP3 inflammasome.", "entity1": "pro-IL-18", "entity2": "Fc11a-2", "span1": [113, 122], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12465": {"label": 1, "data": {"text": "The responses to 5-FU, with respect to both toxicity and efficacy, vary among racial groups, potentially because of variability in the activity levels of the enzyme dihydropyrimidine dehydrogenase (DPD, encoded by the DPYD gene).", "entity1": "DPYD", "entity2": "5-FU", "span1": [218, 222], "span2": [17, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1065": {"label": 3, "data": {"text": "Consistent with these locations, N-ethylmaleimide, an inhibitor of ACS4, inhibited ACS activity 47% in MAM and 28% in endoplasmic reticulum.", "entity1": "ACS", "entity2": "N-ethylmaleimide", "span1": [83, 86], "span2": [33, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8228": {"label": 1, "data": {"text": "Together these findings suggest that ICA binds to the same site in EAG and ERG channels to elicit opposite functional effects.", "entity1": "ERG", "entity2": "ICA", "span1": [75, 78], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12993": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "delta 14 reductase", "entity2": "phenylmorpholines", "span1": [142, 160], "span2": [4, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11038": {"label": 3, "data": {"text": "Analysis of tumour-conditioned medium indicated that bexarotene decreased the secretion of angiogenic factors and matrix metalloproteinases and increased the tissue inhibitor of matrix metalloproteinases.", "entity1": "matrix metalloproteinases", "entity2": "bexarotene", "span1": [114, 139], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11523": {"label": 1, "data": {"text": "Dexamethasone probes glucocorticoid receptor (GR) function, while prednisolone probes both GR and mineralocorticoid receptor (MR) function.", "entity1": "MR", "entity2": "prednisolone", "span1": [126, 128], "span2": [66, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6532": {"label": 3, "data": {"text": "Thalidomide--removed from widespread clinical use by 1962 because of severe teratogenicity--has anti-angiogenic and immunomodulatory effects, including the inhibition of TNF alpha.", "entity1": "TNF alpha", "entity2": "Thalidomide", "span1": [170, 179], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8507": {"label": 1, "data": {"text": "Previous studies have revealed that the ATP binding step is crucial both for the power stroke to produce motility and for the inter-domain regulation of ATPase activity to guarantee the processive movement of dimeric KIFs.", "entity1": "KIFs", "entity2": "ATP", "span1": [217, 221], "span2": [40, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4391": {"label": 3, "data": {"text": "Altogether, our findings support a model in which Top2\u03b2 deficiency promotes CPT-induced apoptosis in quiescent non-S-phase cells, possibly due to RNAP LS depletion and p53 accumulation.", "entity1": "RNAP LS", "entity2": "CPT", "span1": [146, 153], "span2": [76, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2382": {"label": 3, "data": {"text": "Further characterization of sorafenib revealed that this molecule was a multikinase inhibitor that targeted the vascular endothelial growth factor receptor family (VEGFR-2 and VEGFR-3) and platelet-derived growth factor receptor family (PDGFR-beta and Kit), which play key roles in tumor progression and angiogenesis.", "entity1": "Kit", "entity2": "sorafenib", "span1": [252, 255], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8502": {"label": 3, "data": {"text": "Our study demonstrated that curcumin inhibited OVA-induced increases in eosinophil count; interleukin (IL)-17A level were recovered in bronchoalveolar lavage fluid increased IL-10 level in bronchoalveolar lavage fluid.", "entity1": "OVA", "entity2": "curcumin", "span1": [47, 50], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10409": {"label": 1, "data": {"text": "Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.", "entity1": "ORL1", "entity2": "GTPgammaS", "span1": [100, 104], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1277": {"label": 8, "data": {"text": "We also shortly discuss the ongoing debate on whether NO is the actual reaction product of NOS catalysis, as well as the phenomenon of NO-mediated autoinhibition.", "entity1": "NOS", "entity2": "NO", "span1": [91, 94], "span2": [54, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"13714": {"label": 5, "data": {"text": "Irbesartan (Aprovel, Avapro, Irbetan, Karvea), an angiotensin II receptor type 1 antagonist, is approved in many countries worldwide for the treatment of hypertension.", "entity1": "angiotensin II receptor type 1", "entity2": "Aprovel", "span1": [50, 80], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13437": {"label": 3, "data": {"text": "TGF-beta1 and high D-glucose increased p42/44(mapk) and Smad2 phosphorylation, an effect blocked by PD-98059 (MEK1/2 inhibitor).", "entity1": "Smad2", "entity2": "PD-98059", "span1": [56, 61], "span2": [100, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4737": {"label": 3, "data": {"text": "Additionally, the expression of hepatic fibrosis-related factors such as \u03b1-smooth muscle actin and transforming growth factor-\u03b21 (TGF-\u03b21), were reduced in rats treated with sinapic acid.", "entity1": "transforming growth factor-\u03b21", "entity2": "sinapic acid", "span1": [99, 128], "span2": [173, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13174": {"label": 2, "data": {"text": "Progestin activation of Src/MAPK occurred outside the nucleus with the B isoform of PR that was distributed between the cytoplasm and nucleus, but not with PR-A that was predominantly nuclear.", "entity1": "Src", "entity2": "Progestin", "span1": [24, 27], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3228": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "ellagic acid", "span1": [282, 284], "span2": [175, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7366": {"label": 2, "data": {"text": "The temporal and anatomical determinants of cocaine-induced CREB activity may indicate functional differences among NAc shell subregions and suggest the involvement of CREB in early and late cocaine effects.", "entity1": "CREB", "entity2": "cocaine", "span1": [60, 64], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4135": {"label": 2, "data": {"text": "Here, we have determined the molecular mechanism of this male-specific activation of the Kcnk1 gene and characterized KCNK1 as a phenobarbital-inducible antihyperplasia factor.", "entity1": "KCNK1", "entity2": "phenobarbital", "span1": [118, 123], "span2": [129, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2590": {"label": 5, "data": {"text": "The non-selective adenosine receptor antagonist (caffeine), and the selective adenosine A1 receptor antagonist (DPCPX), injected 15 min before the application of pentetrazole and flumazenil, were able to intensify BDZ withdrawal signs in mice.", "entity1": "adenosine A1 receptor", "entity2": "DPCPX", "span1": [78, 99], "span2": [112, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3784": {"label": 2, "data": {"text": "These results indicate that phillyrin prevents lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation, suggesting that phillyrin is a novel AMPK activator with a role in the prevention and treatment of obesity.", "entity1": "AMPK", "entity2": "phillyrin", "span1": [141, 145], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11387": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "SNP", "span1": [143, 148], "span2": [135, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13452": {"label": 2, "data": {"text": "These findings demonstrate that n-3 and n-6 PUFA increased PPARgamma activity is necessary for the COX-2 induction in HaCaT human keratinocyte cells.", "entity1": "PPARgamma", "entity2": "n-3 and n-6 PUFA", "span1": [59, 68], "span2": [32, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5892": {"label": 3, "data": {"text": "Mouse ornithine decarboxylase (ODC) was expressed in Escherichia coli and the purified recombinant enzyme used for determination of the binding site for pyridoxal 5'-phosphate and of the residues modified in the inactivation of the enzyme by the enzyme-activated irreversible inhibitor, alpha-difluoromethylornithine (DFMO).", "entity1": "ODC", "entity2": "alpha-difluoromethylornithine", "span1": [31, 34], "span2": [287, 316]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14542": {"label": 3, "data": {"text": "Protein tyrosine phosphatase 1B inhibitory effect by dammarane-type triterpenes from hydrolyzate of total Gynostemma pentaphyllum saponins.", "entity1": "Protein tyrosine phosphatase 1B", "entity2": "saponins", "span1": [0, 31], "span2": [130, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14687": {"label": 3, "data": {"text": "However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition.", "entity1": "BCRP", "entity2": "GSK1292263", "span1": [30, 34], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2183": {"label": 2, "data": {"text": "Furthermore, tPA induced rapid tyrosine phosphorylation on the beta subunit of LRP-1, which was followed by the activation of Mek1 and its downstream Erk-1 and -2.", "entity1": "Erk-1 and -2", "entity2": "tyrosine", "span1": [150, 162], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16059": {"label": 8, "data": {"text": "Drug-drug interactions are dependent on statins' pharmacokinetic profile: simvastatin, lovastatin and atorvastatin are metabolized through cytochrome P450 (CYP) 3A, while the metabolism of the other statins is independent of this CYP.", "entity1": "cytochrome P450 (CYP) 3A", "entity2": "simvastatin", "span1": [139, 163], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9181": {"label": 1, "data": {"text": "Binding of penicillins to penicillin-binding protein 1Bs produces lysis, binding to penicillin-binding protein 2 produces round cells, and binding to penicillin-binding protein 3 produces long filaments.", "entity1": "penicillin-binding protein 2", "entity2": "penicillins", "span1": [84, 112], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14864": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "protein kinase C", "entity2": "bisindolylmaleimide", "span1": [74, 90], "span2": [115, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11874": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "CYP1A1", "entity2": "petunidin", "span1": [150, 156], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12017": {"label": 1, "data": {"text": "Diabetic STZ and Iddm rats, as well as insulin-substituted Iddm rats, exhibited a significant diurnal expression pattern of clock genes as determined by Cosinor analysis; however, the MESOR (midline estimating statistic of rhythm) of Bmal1, Per2, and Clock transcript expression was altered in Iddm and insulin-substituted Iddm rats.", "entity1": "clock", "entity2": "STZ", "span1": [124, 129], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8171": {"label": 1, "data": {"text": "In contrast to wild-type pol \u03b2, the ternary complex of the R283K mutant with an incoming dATP-analogue and templating 8-oxoG resembles a G-A mismatched structure with 8-oxoG adopting an anti-conformation.", "entity1": "R283K", "entity2": "8-oxoG", "span1": [59, 64], "span2": [118, 124]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1148": {"label": 3, "data": {"text": "The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.", "entity1": "HER2", "entity2": "Iressa", "span1": [108, 112], "span2": [39, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6000": {"label": 2, "data": {"text": "Sodium-dependent norepinephrine-induced currents in norepinephrine-transporter-transfected HEK-293 cells blocked by cocaine and antidepressants.", "entity1": "norepinephrine-transporter", "entity2": "norepinephrine", "span1": [52, 78], "span2": [17, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8283": {"label": 3, "data": {"text": "Moreover, the D2R inhibitor raclopride blocked the increase of both GDNF and Zif268 expression following potassium-evoked dopamine release in SH-SY5Y cells.", "entity1": "GDNF", "entity2": "raclopride", "span1": [68, 72], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12423": {"label": 3, "data": {"text": "GTLE pretreatment completely reversed the damaging effects of AlCl3 on AA and superoxide dismutase activity, markedly corrected COX and AChE activities, and moderately improved TGC.", "entity1": "AChE", "entity2": "AlCl3", "span1": [136, 140], "span2": [62, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7460": {"label": 8, "data": {"text": "Interestingly, the VIAAT ortholog from Caenorhabditis elegans (UNC-47), a species lacking glycine transmission, also supports glycine exocytosis in the presence of GlyT2, and a point mutation of UNC-47 that abolishes GABA transmission in the worm confers glycine specificity.", "entity1": "GlyT2", "entity2": "glycine", "span1": [164, 169], "span2": [126, 133]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12670": {"label": 8, "data": {"text": "In conclusion, OMCD tubules from deoxycorticosterone pivalate-treated rats secrete Cl- into the luminal fluid through NKCC1-mediated Cl- uptake across the basolateral membrane in series with Cl- efflux across the apical membrane.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [118, 123], "span2": [133, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12446": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "ML172", "span1": [173, 175], "span2": [129, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14698": {"label": 9, "data": {"text": "Proteins Aus1 and Dan1 were not found to be involved in steroid import.", "entity1": "Aus1", "entity2": "steroid", "span1": [9, 13], "span2": [56, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11467": {"label": 0, "data": {"text": "Apolipoprotein E was chemically bound via linkers to loperamide-loaded HSA-NP.", "entity1": "HSA", "entity2": "loperamide", "span1": [71, 74], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11979": {"label": 8, "data": {"text": "Doxorubicin is mainly excreted into the bile via P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (Mrp2) in hepatobiliary route and metabolized via cytochrome P450 (CYP) 3A subfamily.", "entity1": "P-glycoprotein", "entity2": "Doxorubicin", "span1": [49, 63], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14069": {"label": 1, "data": {"text": "Oncogenic K-ras expression is associated with derangement of the cAMP/PKA pathway and forskolin-reversible alterations of mitochondrial dynamics and respiration.", "entity1": "PKA", "entity2": "forskolin", "span1": [70, 73], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14397": {"label": 3, "data": {"text": "The specific PI3K inhibitor, wortmannin, blocked significantly EGF-induced cell migration and invasion.", "entity1": "PI3K", "entity2": "wortmannin", "span1": [13, 17], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13544": {"label": 2, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha1", "entity2": "ETYA", "span1": [41, 51], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1230": {"label": 3, "data": {"text": "Inhibition of MCP-1 and MIP-2 transcription and translation by mimosine in muscle tissue infected with the parasite Trichinella spiralis.", "entity1": "MCP-1", "entity2": "mimosine", "span1": [14, 19], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4229": {"label": 3, "data": {"text": "The data indicated that PhIP could cause stomach injury, oxidative stress in rat stomachs as well as the activation of c-fos and c-jun and inactivation of p16, which may play a role in the pathogenesis of PhIP-associated stomach cancer.", "entity1": "p16", "entity2": "PhIP", "span1": [155, 158], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3389": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "VMAT2", "entity2": "amphetamine", "span1": [234, 239], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5691": {"label": 5, "data": {"text": "In a neuronal cell line, we found that selective CB(2) receptor agonists upregulate \u03b2-Arrestin 2, an effect that was prevented by selective CB(2) receptor antagonist JTE-907 and CB(2) shRNA lentiviral particles.", "entity1": "CB(2)", "entity2": "JTE-907", "span1": [178, 183], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8165": {"label": 3, "data": {"text": "Taken together, the results of this study demonstrate that DPEP inhibits LPS-stimulated inflammation by blocking the NF-\u03baB and MAPK pathways in macrophages.", "entity1": "NF-\u03baB", "entity2": "DPEP", "span1": [117, 122], "span2": [59, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5392": {"label": 3, "data": {"text": "Also, methylphenidate decreased DAT Km in WIS OFC.", "entity1": "DAT", "entity2": "methylphenidate", "span1": [32, 35], "span2": [6, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6372": {"label": 4, "data": {"text": "The related piperidines ohmefentanyl and sufentanil and the nonselective opioid receptor agonist etorphine were less potent nociceptin receptor agonists.", "entity1": "nociceptin receptor", "entity2": "piperidines", "span1": [124, 143], "span2": [12, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15372": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "RXRs", "entity2": "atRA", "span1": [227, 231], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1922": {"label": 8, "data": {"text": "Kinetic constants of the mutant CrAT showed modification in favor of longer acyl-CoAs as substrates.", "entity1": "CrAT", "entity2": "acyl-CoAs", "span1": [32, 36], "span2": [76, 85]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10237": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "polyamine oxidase", "entity2": "putrescine", "span1": [156, 173], "span2": [206, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2518": {"label": 3, "data": {"text": "Our results demonstrated that auranofin suppressed TLR4-mediated activation of transcription factors, NF-kappaB and IRF3, and expression of COX-2, a pro-inflammatory enzyme.", "entity1": "IRF3", "entity2": "auranofin", "span1": [116, 120], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3824": {"label": 3, "data": {"text": "We report here the optimization of human 17\u03b2-HSD2 inhibitors in the 2,5-thiophene amide class by varying the size of the linker (n equals 0 and 2) between the amide moiety and the phenyl group.", "entity1": "human 17\u03b2-HSD2", "entity2": "2,5-thiophene amide", "span1": [35, 49], "span2": [68, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5868": {"label": 4, "data": {"text": "Therefore, in the present studies, animals were rendered tolerant to the delta-opioid receptor-selective agonist [D-Pen2,D-Pen5]enkephalin (DPDPE), and receptor binding activities were measured.", "entity1": "delta-opioid receptor", "entity2": "[D-Pen2,D-Pen5]enkephalin", "span1": [73, 94], "span2": [113, 138]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8356": {"label": 3, "data": {"text": "SAR and lead optimization studies for Rock inhibitors based on amino acid-derived quinazolines are described.", "entity1": "Rock", "entity2": "quinazolines", "span1": [38, 42], "span2": [82, 94]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5497": {"label": 3, "data": {"text": "4) High concentrations of I- inhibited the catalatic activity of thyroid peroxidase and lactoperoxidase in a manner similar to that described previously for peroxidase-catalyzed iodination.", "entity1": "lactoperoxidase", "entity2": "I-", "span1": [88, 103], "span2": [26, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12117": {"label": 9, "data": {"text": "Disodium cromoglycate affected neither the rightward shift of beta 2-adrenoceptor-mediated responses nor the small rightward shift in beta 1-adrenoceptor-mediated exercise tachycardia after 2 weeks' administration of terbutaline.", "entity1": "beta 1-adrenoceptor", "entity2": "Disodium cromoglycate", "span1": [134, 153], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4675": {"label": 1, "data": {"text": "Using cultured human keratinocytes and diabetic rat model, the current study showed that high-glucose environment enhanced IL-8 production via epidermal growth factor receptor (EGFR) -extracelluar signal-regulated kinase (ERK) pathway in a reactive oxygen species (ROS)-dependent manner in keratinocytes.", "entity1": "ERK", "entity2": "glucose", "span1": [222, 225], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1874": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "DGAT", "entity2": "prenylflavonoids", "span1": [253, 257], "span2": [5, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3345": {"label": 1, "data": {"text": "Dfbp-o also increased the affinity of cTnI for cTnC.", "entity1": "cTnC", "entity2": "Dfbp-o", "span1": [47, 51], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"704": {"label": 5, "data": {"text": "The potency of the selective alpha 1D-adrenoceptor antagonist BMY 7378 against noradrenaline (pA2 = 6.16 +/- 0.13) and of the selective alpha 1A-adrenoceptor antagonist RS-17053 against noradrenaline (pKB = 8.35 +/- 0.10) and against the selective alpha 1A-adrenoceptor agonist A-61603 (pKB = 8.40 +/- 0.09) were too low to account for alpha 1D- and alpha 1A-adrenoceptor involvement.", "entity1": "alpha 1A-adrenoceptor", "entity2": "RS-17053", "span1": [136, 157], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7300": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "Bile acid-coenzyme A:amino acid N-acyltransferase", "entity2": "bile acids", "span1": [12, 61], "span2": [141, 151]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3857": {"label": 3, "data": {"text": "HSYA treatment also decreased NF-\u03baB p65 nuclear translocation and inhibited the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK).", "entity1": "NF-\u03baB", "entity2": "HSYA", "span1": [30, 35], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6788": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-2", "entity2": "etodolac", "span1": [257, 262], "span2": [192, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8590": {"label": 2, "data": {"text": "Western blot assay demonstrated that DICO decreased Bcl-2 level and induced Bax translocation to cause cytochrome c release.", "entity1": "cytochrome c", "entity2": "DICO", "span1": [103, 115], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13839": {"label": 8, "data": {"text": "Mammalian glutamate dehydrogenase (GDH) is a homohexameric enzyme that catalyzes the reversible oxidative deamination of l-glutamate to 2-oxoglutarate using NAD(P)(+) as coenzyme.", "entity1": "Mammalian glutamate dehydrogenase", "entity2": "l-glutamate", "span1": [0, 33], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12269": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1a)", "entity2": "vasopressin", "span1": [133, 138], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9652": {"label": 3, "data": {"text": "The current study evaluates the effects of a selective COX-2 inhibitor (SC-236) on renal function in cirrhotic rats with ascites.", "entity1": "COX-2", "entity2": "SC-236", "span1": [55, 60], "span2": [72, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15247": {"label": 8, "data": {"text": "In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17\u03b2-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated.", "entity1": "OATP2B1", "entity2": "estrone-3-sulfate", "span1": [97, 104], "span2": [114, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8836": {"label": 3, "data": {"text": "RESULTS: By Western blot analysis of spinal cord tissues, we have demonstrated that treatment with bioactive RS -GRA significantly decreased nuclear factor (NF)-kB translocation, pro-inflammatory cytokine production such as interleukin-1\u03b2 (IL-1\u03b2), and apoptosis (Bax and caspase 3 expression).", "entity1": "cytokine", "entity2": "RS -GRA", "span1": [196, 204], "span2": [109, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"388": {"label": 0, "data": {"text": "The replacement of the conserved cysteine residues in e2 of CB2 by serine also eliminated CP 55,940 binding, but replacement of those in CB1 resulted in the sequestration of the mutated receptors in the cell cytoplasm.", "entity1": "CB2", "entity2": "serine", "span1": [60, 63], "span2": [67, 73]}, "weak_labels": [-1, 0, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9255": {"label": 2, "data": {"text": "Ergovaline binding and activation of D2 dopamine receptors in GH4ZR7 cells.", "entity1": "D2 dopamine receptors", "entity2": "Ergovaline", "span1": [37, 58], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15436": {"label": 9, "data": {"text": "When mice were treated ip with the major neonicotinoid imidacloprid (IMI), metabolism by CYP oxidation reactions was not appreciably affected, whereas the AOX-generated nitrosoguanidine metabolite was decreased by 30% with tungsten and 56% with hydralazine and 86% in the AOX-deficient mice.", "entity1": "CYP", "entity2": "IMI", "span1": [89, 92], "span2": [69, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"530": {"label": 2, "data": {"text": "Together, our findings suggest the critical role of 'Rac and subsequent activation of phospholipase A2' in ceramide-signalling to nucleus.", "entity1": "phospholipase A2", "entity2": "ceramide", "span1": [86, 102], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3858": {"label": 3, "data": {"text": "HSYA treatment also decreased NF-\u03baB p65 nuclear translocation and inhibited the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK).", "entity1": "p65", "entity2": "HSYA", "span1": [36, 39], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"928": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "5-Fluorouracil", "span1": [216, 236], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1311": {"label": 5, "data": {"text": "The effect was counteracted by the D(2) antagonist eticlopride, pertussis toxin, the inhibitor of intracellular Ca(2+) release TMB-8, incubation in Ca(2+)-free experimental medium, and PKC desensitization obtained by chronic pretreatment with the phorbol ester TPA.", "entity1": "D(2)", "entity2": "eticlopride", "span1": [35, 39], "span2": [51, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4571": {"label": 2, "data": {"text": "The values of mean corpuscular hemoglobin concentration and mean corpuscular hemoglobin increased in the STX group.", "entity1": "hemoglobin", "entity2": "STX", "span1": [77, 87], "span2": [105, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7051": {"label": 3, "data": {"text": "The concentration of imatinib necessary to inhibit RET in vitro, however, makes it impossible to conclude that imatinib monotherapy will be a good option for systemic therapy of MTC.", "entity1": "RET", "entity2": "imatinib", "span1": [51, 54], "span2": [21, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"328": {"label": 1, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "RNase A", "entity2": "disulfide", "span1": [97, 104], "span2": [46, 55]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8520": {"label": 3, "data": {"text": "CYP3A5 carrier status had no influence on midazolam oral clearance or its inhibition by ketoconazole.", "entity1": "CYP3A5", "entity2": "ketoconazole", "span1": [0, 6], "span2": [88, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7019": {"label": 1, "data": {"text": "Inhibition of [3H]5-HT or [3H]NE uptake by DVS for the hSERT or hNET produced IC50 values of 47.3 +/- 19.4 and 531.3 +/- 113.0 nM, respectively.", "entity1": "hNET", "entity2": "DVS", "span1": [64, 68], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15069": {"label": 1, "data": {"text": "The tocolytic agent ritodrine acts on the \u03b22-adrenoceptor and is an effective treatment option for preterm labor.", "entity1": "\u03b22-adrenoceptor", "entity2": "ritodrine", "span1": [42, 57], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9655": {"label": 8, "data": {"text": "Selective inhibition of cyclooxygenase 2 spares renal function and prostaglandin synthesis in cirrhotic rats with ascites.", "entity1": "cyclooxygenase 2", "entity2": "prostaglandin", "span1": [24, 40], "span2": [67, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4890": {"label": 3, "data": {"text": "The parent phenol of this compound inhibits aromatase with an IC50 value of 0.028\u2005nM in the same assay.", "entity1": "aromatase", "entity2": "phenol", "span1": [44, 53], "span2": [11, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4883": {"label": 3, "data": {"text": "Separate 5-aza-2'-deoxycytidine pretreatment or in combination with trichostatin A reduced (m)CpG and specific small interference RNAs targeting Mecp2 and Creb1 separately or together depleting Mecp2 and/or Creb1 binding of glut3-(m)CpGs reduced glut3 expression in HT22 cells.", "entity1": "Mecp2", "entity2": "5-aza-2'-deoxycytidine", "span1": [145, 150], "span2": [9, 31]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14180": {"label": 0, "data": {"text": "CBDP irreversibly inhibits butyrylcholinesterase (BChE) in human plasma by forming adducts on the active site serine (Ser-198).", "entity1": "BChE", "entity2": "serine", "span1": [50, 54], "span2": [110, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6041": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "MK 212", "span1": [63, 69], "span2": [146, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"953": {"label": 2, "data": {"text": "A prerequisite for this hypothesis was the unproved assumption that rabbit and human alpha(2A)-adrenoceptors are equally activated by rilmenidine.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "rilmenidine", "span1": [85, 108], "span2": [134, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7613": {"label": 1, "data": {"text": "In a Phase III trial comparing lapatinib and capecitabine with capecitabine alone in women with HER2-positive, locally advanced breast cancer or MBC that had progressed after treatment with an anthracycline, a taxane, and trastuzumab, the combination of lapatinib and capecitabine was associated with a numeric improvement in response rate compared with capecitabine alone (22% vs 14%, respectively; P = NS) and a significant increase in time to progression (6.2 vs 4.3 months; hazard ratio = 0.57; 95% CI, 0.43-0.77; P < 0.001).", "entity1": "HER2", "entity2": "lapatinib", "span1": [96, 100], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15656": {"label": 3, "data": {"text": "Cholesterol also increases Amyloid \u03b2 (A\u03b2) deposition and tau pathology.", "entity1": "tau", "entity2": "Cholesterol", "span1": [57, 60], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13686": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "human TLR7", "entity2": "gardiquimod", "span1": [118, 128], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12399": {"label": 2, "data": {"text": "Number and area of preneoplastic foci positive for glutathione S-transferase placental form (GST-P) were consistently higher in these groups than the sum of individual values in the groups treated with HEP or HCB alone.", "entity1": "GST-P", "entity2": "HEP", "span1": [93, 98], "span2": [202, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4946": {"label": 3, "data": {"text": "The mechanism of action of Fc11a-2 was related to the inhibition of the cleavage of pro-caspase-1, pro-IL-1\u03b2 and pro-IL-18 which in turn suppressed the activation of NLRP3 inflammasome.", "entity1": "NLRP3", "entity2": "Fc11a-2", "span1": [166, 171], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10683": {"label": 5, "data": {"text": "Oxytocin antagonist (OTA), TT-235, was developed by our group and shown to inhibit either spontaneous or oxytocin-induced uterine contractions in primates.", "entity1": "Oxytocin", "entity2": "TT-235", "span1": [0, 8], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10385": {"label": 3, "data": {"text": "Investigation of bradykinin metabolism in human and rat plasma in the presence of the dual ACE/NEP inhibitors GW660511X and omapatrilat.", "entity1": "NEP", "entity2": "omapatrilat", "span1": [95, 98], "span2": [124, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1509": {"label": 4, "data": {"text": "OBJECTIVE: Preclinical evaluation of DRF 2655, a peroxisome proliferator-activated receptor alpha (PPARalpha) and PPARgamma agonist, as a body-weight lowering, hypolipidemic and euglycemic agent.", "entity1": "PPARalpha", "entity2": "DRF 2655", "span1": [99, 108], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2883": {"label": 2, "data": {"text": "In hippocampal dentate gyrus, MPH-receiving rats showed a 51% decrease in NET-ir density and a 61% expanded distribution of the new-cell marker PSA-NCAM (polysialylated form of neural cell adhesion molecule).", "entity1": "NCAM", "entity2": "MPH", "span1": [148, 152], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10492": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "pindolol", "span1": [392, 423], "span2": [301, 309]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14639": {"label": 8, "data": {"text": "The higher in vitro catalytic efficiency of DCK24Val toward dFdC monophosphorylation may be relevant to dFdC clinical response.", "entity1": "DCK", "entity2": "dFdC", "span1": [44, 47], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13891": {"label": 3, "data": {"text": "In addition, the factor Xa inhibitor apixaban is in late-stage clinical development.", "entity1": "factor Xa", "entity2": "apixaban", "span1": [17, 26], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2092": {"label": 3, "data": {"text": "The purpose of the present study was to test our hypothesis that amiloride, a specific u-PA inhibitor, effectively decreases u-PA activity in cornea as well as in tear fluid and favourably affects corneal healing.", "entity1": "u-PA", "entity2": "amiloride", "span1": [125, 129], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5545": {"label": 2, "data": {"text": "Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice.", "entity1": "alpha(2A)-adrenergic receptor", "entity2": "Methamphetamine", "span1": [42, 71], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"161": {"label": 3, "data": {"text": "The effect of the four mono- and bisquaternary ammonium compounds tetramethylammonium (TMA), hexamethonium, decamethonium and suxamethonium on the reactivatability of soman-inhibited, solubilized AChE from human erythrocytes was investigated in vitro.", "entity1": "AChE", "entity2": "soman", "span1": [196, 200], "span2": [167, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14933": {"label": 1, "data": {"text": "Further studies of the role of these steroids and SERMs in regulating responses mediated by ER\u03b1 and ER\u03b2 a variety of tissues, during different stages of development, are likely to uncover additional estrogenic activities.", "entity1": "ER\u03b2", "entity2": "steroids", "span1": [100, 103], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4687": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "TCDD", "span1": [103, 109], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"962": {"label": 5, "data": {"text": "The sympathetic nerves of both the human atrial appendages and rabbit pulmonary artery are endowed with alpha(2A)-autoreceptors, at which, however, both rilmenidine and oxymetazoline exhibit different properties (antagonism and agonism, respectively).", "entity1": "alpha(2A)-autoreceptors", "entity2": "rilmenidine", "span1": [104, 127], "span2": [153, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1480": {"label": 8, "data": {"text": "Mouse brain serine racemase catalyzes specific elimination of L-serine to pyruvate.", "entity1": "Mouse brain serine racemase", "entity2": "pyruvate", "span1": [0, 27], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6978": {"label": 1, "data": {"text": "Bisoprolol reduced dobutamine-induced heart rate and contractility increases and diastolic blood pressure decreases more potently in Arg389- versus Gly389-beta1AR subjects.", "entity1": "beta1AR", "entity2": "dobutamine", "span1": [155, 162], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12853": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "vascular-endothelial growth factor (VEGFR)-2", "entity2": "sorafenib", "span1": [163, 207], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8104": {"label": 3, "data": {"text": "We found that wogonin can suppress the H2O2-stimulated actin remodeling and albumin uptake of HUVECs, as well as transendothelial cell migration of the human breast carcinoma cell MDA-MB-231.", "entity1": "actin", "entity2": "wogonin", "span1": [55, 60], "span2": [14, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15791": {"label": 2, "data": {"text": "During repetitive stimulation of skeletal muscle, extracellular ATP levels raise, activating purinergic receptors, increasing Ca(2+) influx, and enhancing contractile force, a response called potentiation.", "entity1": "purinergic receptors", "entity2": "ATP", "span1": [93, 113], "span2": [64, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7722": {"label": 3, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LH", "entity2": "buserelin", "span1": [260, 262], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14630": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "CDA", "entity2": "Gemcitabine", "span1": [86, 89], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15055": {"label": 8, "data": {"text": "Cellular zinc is controlled by zinc-chelating proteins and by zinc transporters.", "entity1": "zinc-chelating proteins", "entity2": "zinc", "span1": [31, 54], "span2": [9, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11957": {"label": 8, "data": {"text": "We have developed a convenient quantitative multi-well plate assay to measure the glucuronidation rate of 7-hydroxy-4-trifluoromethylcoumarin (HFC) for several UGTs.", "entity1": "UGTs", "entity2": "7-hydroxy-4-trifluoromethylcoumarin", "span1": [160, 164], "span2": [106, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3649": {"label": 2, "data": {"text": "DBDCT up-regulated the expression of Bax, down-regulated the expression of Bcl-2, and significantly increased the ratio of Bax/Bcl-2.", "entity1": "Bax", "entity2": "DBDCT", "span1": [123, 126], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"275": {"label": 1, "data": {"text": "Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha 2-adrenergic receptors and may act as a neurotransmitter.", "entity1": "alpha 2-adrenergic receptors", "entity2": "Agmatine", "span1": [111, 139], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12711": {"label": 1, "data": {"text": "We demonstrated that the coexpressed HG1 and GAB-1 receptors are GABA-responsive, and provide evidence for the possible involvement of GABA receptors in the mechanism of ivermectin resistance.", "entity1": "GABA receptors", "entity2": "ivermectin", "span1": [135, 149], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13552": {"label": 5, "data": {"text": "In this study we investigated the effects of combination chemotherapy with melarsoprol and a humanised SP receptor antagonist aprepitant (EMEND) in this mouse model.", "entity1": "humanised SP receptor", "entity2": "EMEND", "span1": [93, 114], "span2": [138, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9454": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "M&B-28767", "span1": [4, 7], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15703": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "TRP channels", "entity2": "menthol", "span1": [46, 58], "span2": [165, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9959": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [166, 171], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3973": {"label": 1, "data": {"text": "To control for possible interactions between the expression of the estrogen receptor genes and other learning-related steroid receptors, androgen receptors (AR), corticosterone-binding glucocorticoid receptors (GR) and mineralocorticoid receptors (MR) were also measured.", "entity1": "MR", "entity2": "corticosterone", "span1": [248, 250], "span2": [162, 176]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13875": {"label": 1, "data": {"text": "These findings support that PPARgamma plays an essential role in mediating the RhoA-inhibiting effect of ibuprofen.", "entity1": "PPARgamma", "entity2": "ibuprofen", "span1": [28, 37], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12422": {"label": 3, "data": {"text": "GTLE pretreatment completely reversed the damaging effects of AlCl3 on AA and superoxide dismutase activity, markedly corrected COX and AChE activities, and moderately improved TGC.", "entity1": "COX", "entity2": "AlCl3", "span1": [128, 131], "span2": [62, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5422": {"label": 5, "data": {"text": "Local LC citalopram effect was abolished by LC presence of the 5-HT3 receptor antagonist MDL72222 (1\u00a0\u03bcM) but not the 5-HT1/2 receptor antagonist methiothepin (1\u00a0\u03bcM).", "entity1": "5-HT1/2", "entity2": "methiothepin", "span1": [117, 124], "span2": [145, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12263": {"label": 8, "data": {"text": "Caution is necessary only when it is coadministered with drugs metabolised by CYP2D6, such as metoprolol, or administered to the elderly or patients with severe hepatic or renal impairment.", "entity1": "CYP2D6", "entity2": "metoprolol", "span1": [78, 84], "span2": [94, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"637": {"label": 3, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "PLA2", "entity2": "AACOCF3", "span1": [80, 84], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7730": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "Luteinizing hormone-releasing hormone", "entity2": "leuprorelin", "span1": [0, 37], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13140": {"label": 2, "data": {"text": "Levels of mRNA encoding insulin 1, ICA512, and PC1/3 were increased in the pancreatic islets of GalN-treated rats.", "entity1": "ICA512", "entity2": "GalN", "span1": [35, 41], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9077": {"label": 2, "data": {"text": "In contrast, serum alkaline phosphatase was elevated in animals dosed with 13cisRA or 4HPR but not in those dose with ROAc.", "entity1": "alkaline phosphatase", "entity2": "13cisRA", "span1": [19, 39], "span2": [75, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"945": {"label": 3, "data": {"text": "Kinetic parameters for PAM inactivation by 4-oxo-5-acetamido-6-phenyl-hex-2-enoic acid and 4-oxo-5-acetamido-6-(2-thienyl)-hex-2-enoic acid were obtained by using both the conventional dilution assay method and the more complex progress curve method.", "entity1": "PAM", "entity2": "4-oxo-5-acetamido-6-phenyl-hex-2-enoic acid and 4-oxo-5-acetamido-6-(2-thienyl)-hex-2-enoic acid", "span1": [23, 26], "span2": [43, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4353": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "cyclin D1", "entity2": "pinosylvin", "span1": [271, 280], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15565": {"label": 2, "data": {"text": "Puerarin administration enhanced glutathione (GSH) activity, glial cell line-derived neurotrophic factor (GDNF) expression and PI3K/Akt pathway activation, which might ameliorate MPTP injection-induced progressive elevation of reactive oxygen species (ROS) formation in mice.", "entity1": "glial cell line-derived neurotrophic factor", "entity2": "Puerarin", "span1": [61, 104], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6310": {"label": 8, "data": {"text": "We found that 5-HT stimulated the conversion of [3H]L-arginine ([3H]L-Arg) to [3H]L-Cit, indicating eNOS activation.", "entity1": "eNOS", "entity2": "[3H]L-Cit", "span1": [100, 104], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5912": {"label": 8, "data": {"text": "accelerating reverse transport of cholesteryl esters from high-density lipoproteins to lower-density lipoproteins.", "entity1": "high-density lipoproteins", "entity2": "cholesteryl esters", "span1": [58, 83], "span2": [34, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10229": {"label": 3, "data": {"text": "Moreover, thalidomide reduced the LPS-induced TNF-alpha production by KCs by decreasing TNF-alpha messenger RNA.", "entity1": "TNF-alpha", "entity2": "thalidomide", "span1": [46, 55], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1899": {"label": 2, "data": {"text": "I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction.", "entity1": "cytokine", "entity2": "PMA", "span1": [60, 68], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11394": {"label": 3, "data": {"text": "Using whole-cell voltage clamp, we examined mibefradil block of four Na+ channel isoforms expressed in human embryonic kidney cells: Nav1.5 (cardiac), Nav1.4 (skeletal muscle), Nav1.2 (brain), and Nav1.7 (peripheral nerve).", "entity1": "Nav1.5", "entity2": "mibefradil", "span1": [133, 139], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1534": {"label": 3, "data": {"text": "However, topiramate at low concentrations causes slow inhibition of GluR5 kainate receptor-mediated synaptic currents in the basolateral amygdala, indicating that it may protect against seizures, at least in part, through suppression of GluR5 kainate receptor responses.", "entity1": "kainate receptor", "entity2": "topiramate", "span1": [74, 90], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7147": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "vardenafil", "span1": [146, 165], "span2": [78, 88]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9934": {"label": 3, "data": {"text": "The suppression of NF-kappaB activation by inhibition of the IKKs contributes to the well-known anti-inflammatory and immunosuppressive effects of sulfasalazine.", "entity1": "NF-kappaB", "entity2": "sulfasalazine", "span1": [19, 28], "span2": [147, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5676": {"label": 2, "data": {"text": "Data suggest that bisphosphonates via modulation of the activity of small-GTPases induce apoptosis in neoplastic cells by DNA-CpG-demethylation and stimulation of FAS-expression.", "entity1": "FAS", "entity2": "bisphosphonates", "span1": [163, 166], "span2": [18, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15260": {"label": 2, "data": {"text": "Further investigation demonstrated that 8k reduced H2O2-induced activation of mitochondrial apoptosis by inhibiting the expression of Bax and elevating the expression of Bcl-2.", "entity1": "Bax", "entity2": "H2O2", "span1": [134, 137], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13271": {"label": 2, "data": {"text": "However, as a novel finding, isoflavone treatment increased a subclass of high-density lipoprotein, the pre-beta high-density lipoprotein levels by 18% without affecting any other serum lipid concentrations.", "entity1": "pre-beta high-density lipoprotein", "entity2": "isoflavone", "span1": [104, 137], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3995": {"label": 8, "data": {"text": "Aldose reductase (AR) catalyzes the reduction of toxic lipid aldehydes to their alcohol products and mediates inflammatory signals triggered by lipopolysaccharide (LPS).", "entity1": "AR", "entity2": "alcohol", "span1": [18, 20], "span2": [80, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"6107": {"label": 5, "data": {"text": "In extending these initial findings, we have shown that cardiac fibrosis (i) is not reversed by correction of mineralocorticoid-induced hypokalemia; (ii) appears not to involve the plasma or tissue renin-angiotensin systems, as fibrosis is largely unaffected by concurrent administration of Losartan or Perindopril; (iii) is independent of cardiac hypertrophy, in that it is equally seen in right and left ventricles, and in rats rendered hypertensive without cardiac hypertrophy by the administration of 9 alpha-fluorocortisol; (iv) is independent of elevated blood pressure, in that it is found in normotensive animals infused peripherally with aldosterone and intracerebroventricularly with the mineralocorticoid receptor (MR) antagonist RU28318; (v) is via classical MR, in that it is blocked by concurrent administration of the MR antagonist potassium canrenoate; and (vi) may or may not be a direct cardiac effect, inasmuch as data for in vivo effects on collagen formation by cardiac fibroblasts are conflicting.", "entity1": "mineralocorticoid receptor", "entity2": "RU28318", "span1": [698, 724], "span2": [741, 748]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2366": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "VEGFR", "entity2": "BAY 43-9006", "span1": [127, 132], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1777": {"label": 2, "data": {"text": "(125)I-Cyanopindolol saturation binding in Adv.beta(1) myocytes demonstrated approximately 18-fold increase in beta(1)-adrenoceptors.", "entity1": "beta(1)-adrenoceptors", "entity2": "(125)I-Cyanopindolol", "span1": [111, 132], "span2": [0, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12038": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "EO", "entity2": "I-", "span1": [48, 50], "span2": [69, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7362": {"label": 5, "data": {"text": "At least 4 h of estrogen pre-treatment was required to elicit protection, an effect that was blocked by the ER antagonist, ICI 182,780.", "entity1": "ER", "entity2": "ICI 182,780", "span1": [108, 110], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9324": {"label": 3, "data": {"text": "RESULTS: Nedocromil sodium inhibited the chemotactic response toward FMLP and NAF/IL-8 of GM-CSF primed eosinophils approximately 60% (inhibitory concentration of 50% [IC50] approximately 1 to 10 nmol/L), whereas these responses of IL-3 primed eosinophils was completely inhibited (IC50 approximately 1 nmol/L).", "entity1": "NAF", "entity2": "Nedocromil sodium", "span1": [78, 81], "span2": [9, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2850": {"label": 2, "data": {"text": "cAspAT activity, as well as the incorporation of [(14)C]aspartate into the neutral lipid fraction of 3T3-F442A adipocytes was stimulated by the thiazolidinedione (TZD) rosiglitazone.", "entity1": "cAspAT", "entity2": "thiazolidinedione", "span1": [0, 6], "span2": [144, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12898": {"label": 3, "data": {"text": "Here, we show that at noncytotoxic concentrations, H(2)S was able to inhibit NO production and inducible NO synthase (iNOS) expression via heme oxygenase (HO-1) expression in RAW264.7 macrophages stimulated with lipopolysaccharide (LPS).", "entity1": "inducible NO synthase", "entity2": "H(2)S", "span1": [95, 116], "span2": [51, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8059": {"label": 3, "data": {"text": "Furthermore, metformin was able to not only decrease the paclitaxel-induced p38 MAPK-mediated ERCC1 expression, but also augment the cytotoxic effect induced by paclitaxel.", "entity1": "ERCC1", "entity2": "metformin", "span1": [94, 99], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9317": {"label": 3, "data": {"text": "One possible explanation is that, in our model, remikiren in contrast to CGP 38560A and enalkiren is able to inhibit renin in a functionally important extraplasmatic compartment.", "entity1": "renin", "entity2": "remikiren", "span1": [117, 122], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"675": {"label": 3, "data": {"text": "Of the PDE inhibitors tested, dipyridamole was most effective, with IC50 values of 1.2 and 0.45 microM for inhibition of cAMP and cGMP hydrolysis, respectively.", "entity1": "PDE", "entity2": "dipyridamole", "span1": [7, 10], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3496": {"label": 3, "data": {"text": "A significant decrease of aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase (LDH) activities and glutathione (GSH) levels and an increase of malondialdehyde (MDA) quantity was observed after CCl4 and PC administration alone.", "entity1": "lactate dehydrogenase", "entity2": "CCl4", "span1": [80, 101], "span2": [217, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12771": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "UFT", "span1": [0, 20], "span2": [104, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7890": {"label": 1, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "FAS", "entity2": "farnesylpyrophosphate", "span1": [32, 35], "span2": [213, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9634": {"label": 2, "data": {"text": "Binding of hydroxyflutamide to m-AR in LNCaP cells resulted in a concentration-dependent stimulation of PSA expression, suggesting that hydroxyflutamide acted as an agonist of the m-AR.", "entity1": "PSA", "entity2": "hydroxyflutamide", "span1": [104, 107], "span2": [11, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"23": {"label": 3, "data": {"text": "The inhibitory effects of iloprost on tissue factor expression were also potentiated by isobutylmethylxanthine and mimicked by forskolin and dibutyryl cyclic AMP but not dibutyryl cyclic GMP.", "entity1": "tissue factor", "entity2": "forskolin", "span1": [38, 51], "span2": [127, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1160": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "[3H]glibenclamide", "span1": [161, 165], "span2": [140, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7414": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "Abeta(1-40)", "entity2": "glycine", "span1": [122, 133], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6101": {"label": 3, "data": {"text": "bolus); finally, 8 rabbits received aurintrycarboxilic acid (ATA), an inhibitor of platelet glycoprotein Ib/von Willebrand factor interaction (10 mg/kg i.v.", "entity1": "von Willebrand factor", "entity2": "ATA", "span1": [108, 129], "span2": [61, 64]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5786": {"label": 9, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "EC 3.5.1.14", "entity2": "L-aspartic acid", "span1": [109, 120], "span2": [248, 263]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8394": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "glutathione reductase", "entity2": "Cd", "span1": [193, 214], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3667": {"label": 3, "data": {"text": "Additionally, the mRNA levels of melanogenesis-related genes (c-KIT, stem cell factor (SCF), and macrophage migration inhibitory factor (MIF)) were down-regulated by artemisinic acid.", "entity1": "c-KIT", "entity2": "artemisinic acid", "span1": [62, 67], "span2": [166, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13188": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "NET", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane", "span1": [287, 290], "span2": [0, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10245": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "spermidine/spermine N(1)-acetyltransferase", "entity2": "polyamine", "span1": [77, 119], "span2": [7, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4220": {"label": 2, "data": {"text": "With the elevated doses of PhIP, malondialdehyde (MDA) contents, protein carbonyl (PCO) contents and DNA-protein crosslinks (DPC) coefficients were significantly raised in a dose-dependent manner; (3) PhIP at the doses of 10mg/kg and/or 15mg/kg significantly inhibited p16 mRNA and protein expression, whereas enhanced c-fos and c-jun expression relative to control.", "entity1": "c-jun", "entity2": "PhIP", "span1": [329, 334], "span2": [201, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4854": {"label": 3, "data": {"text": "The major ingredient of ginger, [6]-gingerol, could inhibit angiotensin II type 1 receptor activation, which partially clarified the mechanism of ginger regulating blood pressure and strengthening heart in the cardiovascular system.", "entity1": "angiotensin II type 1 receptor", "entity2": "[6]-gingerol", "span1": [60, 90], "span2": [32, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14886": {"label": 9, "data": {"text": "The induction of HO-1 by EIH was inhibited by SB203580 but not by SP600125, PD98059, nor LY294002.", "entity1": "HO-1", "entity2": "LY294002", "span1": [17, 21], "span2": [89, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8419": {"label": 3, "data": {"text": "However, the involvement of the caspase-dependent pathway in the process of cell death induced by either BSC 3g or 3n is discarded since cell death could not be prevented by pretreatment with the pancaspase inhibitor z-VAD-fmk.", "entity1": "caspase", "entity2": "z-VAD-fmk", "span1": [199, 206], "span2": [217, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3367": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-VGCCs", "entity2": "neurosteroids", "span1": [153, 160], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9110": {"label": 9, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "calmodulin", "entity2": "clonidine", "span1": [165, 175], "span2": [137, 146]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3198": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "p-coumaric acid", "span1": [282, 284], "span2": [87, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2875": {"label": 3, "data": {"text": "These effects were fully counteracted by dietary phenolics which inhibited ROS overproduction and GSH consumption, rendered the reactive transcription of glutathione-associated enzymes unnecessary and blocked the intracellular signals leading to the overexpression and rearrangement of p66Shc signalling molecule.", "entity1": "p66Shc", "entity2": "phenolics", "span1": [286, 292], "span2": [49, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7501": {"label": 1, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "Na+K+ATPase", "entity2": "AICAR", "span1": [283, 294], "span2": [45, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9683": {"label": 3, "data": {"text": "Inhibition of the human ether-a-go-go-related gene (HERG) potassium channel by cisapride: affinity for open and inactivated states.", "entity1": "human ether-a-go-go-related gene (HERG) potassium channel", "entity2": "cisapride", "span1": [18, 75], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1562": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "kynurenine aminotransferase I", "entity2": "glutamine", "span1": [57, 86], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"10367": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-7", "entity2": "omapatrilat", "span1": [64, 71], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9886": {"label": 1, "data": {"text": "UNLABELLED: Apparent muscarinic acetylcholine (mAch) receptor occupancy in mouse cerebral cortex, hippocampus, and striatum by scopolamine, an antagonist, and biperiden, a relatively selective M1 antagonist, was estimated with competitive binding studies using two different radioligands: 3H-N-methyl piperidyl benzilate (3H-NMPB) and 3H-quinuclidinyl benzilate (3H-QNB).", "entity1": "muscarinic acetylcholine (mAch) receptor", "entity2": "3H-quinuclidinyl benzilate", "span1": [21, 61], "span2": [335, 361]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13219": {"label": 9, "data": {"text": "The GRIP1 reduction was inhibited by MK-801, an N-methyl-d-aspartate (NMDA) receptor antagonist, but not by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an AMPA receptor antagonist.", "entity1": "GRIP1", "entity2": "CNQX", "span1": [4, 9], "span2": [146, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9861": {"label": 3, "data": {"text": "Among the various enzymes, dicoumarol inhibitable cytosolic NAD(P)H:quinone oxidoreductase1 (NQO1) was shown to catalyse bioreductive activation of MMC leading to cross-linking of the DNA and cytotoxicity.", "entity1": "NQO1", "entity2": "dicoumarol", "span1": [93, 97], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14372": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "EGF", "entity2": "NFD", "span1": [14, 17], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2793": {"label": 2, "data": {"text": "Caerulein increased the levels of H(2)S and CSE mRNA expression while CBS mRNA expression was decreased.", "entity1": "CSE", "entity2": "Caerulein", "span1": [44, 47], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8696": {"label": 8, "data": {"text": "Among the possible transporters involved in the uptake of Cd(2+) and Mn(2+), the expression of ZIP8 (Zrt-, Irt-related protein 8), encoded by Slc39a8, showed a marked suppression in both RBL-Cdr and RBL-Mnr cells.", "entity1": "ZIP8", "entity2": "Mn(2+)", "span1": [95, 99], "span2": [69, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9984": {"label": 1, "data": {"text": "In a search for less flexible analogues of caproctamine (1), a diamine diamide endowed with an interesting AChE affinity profile, we discovered compound 2, in which the terminal 2-methoxybenzyl groups of 1 have been incorporated into a tricyclic system.", "entity1": "AChE", "entity2": "diamine", "span1": [107, 111], "span2": [63, 70]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11907": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "TAGs", "span1": [174, 179], "span2": [61, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15486": {"label": 0, "data": {"text": "Electrophilic chemicals activate both insect and vertebrate TRPA1 via covalent modification of cysteine residues in the amino-terminal region.", "entity1": "TRPA1", "entity2": "cysteine", "span1": [60, 65], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2635": {"label": 8, "data": {"text": "They all expressed ASS, but not ornithine transcarbamylase (OTC), the enzyme that converts ornithine, the product of degradation of arginine with rhArg, to citrulline, which is converted back to arginine via ASS.", "entity1": "rhArg", "entity2": "arginine", "span1": [146, 151], "span2": [132, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, 9]},
	"10668": {"label": 3, "data": {"text": "Especially, the compound 1 showed strong inhibition (IC50=1.33 microM) against the enzyme tyrosinase, as compared to the standard tyrosinase inhibitors kojic acid (IC50=16.67 microM) and L-mimosine (IC50=3.68 microM), indicating its potential used for the treatment of hyperpigmentation associated with the high production of melanocytes.", "entity1": "tyrosinase", "entity2": "kojic acid", "span1": [90, 100], "span2": [152, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10807": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-1", "entity2": "carprofen", "span1": [0, 5], "span2": [71, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10831": {"label": 9, "data": {"text": "The reported mechanism of imatinib resistance in GISTs involves missense mutation in the kinase domain of KIT, including Thr670Ile, Tyr823Asp, and Val654Ala.", "entity1": "Val654Ala", "entity2": "imatinib", "span1": [147, 156], "span2": [26, 34]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4400": {"label": 1, "data": {"text": "These findings highlight that the interaction between M6P/IGF2R and M6P-modified ligands is not only important for intracellular accumulation of lysosomal enzymes and formation of dense lysosomes, but is also crucial for the ability of the receptor to suppress SCC-VII growth and invasion.", "entity1": "IGF2R", "entity2": "M6P", "span1": [58, 63], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13403": {"label": 1, "data": {"text": "Histamine H1 receptor involvement in prepulse inhibition and memory function: relevance for the antipsychotic actions of clozapine.", "entity1": "Histamine H1 receptor", "entity2": "clozapine", "span1": [0, 21], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7132": {"label": 1, "data": {"text": "All PDE5 constructs had similar affinities for 3-isobutyl-1-methylxanthine, sildenafil, tadalafil, and UK-122764, but mutants containing a complete GAF-B had 7- to 18-fold higher affinity for vardenafil-based compounds compared with those lacking a complete GAF-B.", "entity1": "GAF-B", "entity2": "3-isobutyl-1-methylxanthine", "span1": [148, 153], "span2": [47, 74]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9751": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "5-HT(1B)", "entity2": "yohimbine", "span1": [132, 140], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14432": {"label": 1, "data": {"text": "Through identification of mammary ABCG2 as a novel target gene of pesticide prochloraz and dioxin, our results may therefore help to improve the protection of breast-feeding infants and the consumer of dairy products.", "entity1": "ABCG2", "entity2": "prochloraz", "span1": [34, 39], "span2": [76, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6886": {"label": 1, "data": {"text": "ABCG5 and ABCG8 themselves are regulated by cholesterol via liver X receptors (LXRs), which are also activated by oxysterols and some derivatives of plant sterols.", "entity1": "liver X receptors", "entity2": "cholesterol", "span1": [60, 77], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1344": {"label": 8, "data": {"text": "Among the [Fe-S] cluster biosynthetic proteins are included a pyridoxal phosphate-dependent enzyme (NifS) that is involved in the activation of sulphur from l-cysteine, and a molecular scaffold protein (NifU) upon which [Fe-S] cluster precursors are formed.", "entity1": "NifS", "entity2": "l-cysteine", "span1": [100, 104], "span2": [157, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2367": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "PDGFR", "entity2": "BAY 43-9006", "span1": [133, 138], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1191": {"label": 3, "data": {"text": "The inhibition of aminopeptidase activity in the presence of bestatin and puromycin inhibitors was also investigated.", "entity1": "aminopeptidase", "entity2": "puromycin", "span1": [18, 32], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6844": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "methylenetetrahydrofolate reductase", "entity2": "Hcy", "span1": [82, 117], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"770": {"label": 9, "data": {"text": "Preferential block of late sodium current in the LQT3 DeltaKPQ mutant by the class I(C) antiarrhythmic flecainide.", "entity1": "LQT3 DeltaKPQ mutant", "entity2": "sodium", "span1": [49, 69], "span2": [27, 33]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9226": {"label": 3, "data": {"text": "The binding of FHA-HIS was inhibited on 35-79% of the platelets by the histamine H1 receptor antagonists diphenhydramine and clemastine.", "entity1": "FHA", "entity2": "clemastine", "span1": [15, 18], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2783": {"label": 8, "data": {"text": "This study examined the inward transport of l-[(14)C]alanine, an ASCT2 preferential substrate, in monolayers of immortalized renal proximal tubular epithelial (PTE) cells from Wistar-Kyoto (WKY) and spontaneously hypertensive (SHR) rats.", "entity1": "ASCT2", "entity2": "l-[(14)C]alanine", "span1": [65, 70], "span2": [44, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"285": {"label": 5, "data": {"text": "Eight normal males received single oral doses of BRL35135 8 mg (BRL) or the selective beta 2-adrenoceptor agonist salbutamol 8 mg (SAL), after pretreatment with either placebo (PL), bisoprolol 5 mg (B5) as a selective beta 1-adrenoceptor antagonist, or nadolol 20 mg (N20) to block beta 1- and beta 2- but not beta 3-receptors.", "entity1": "beta 1-adrenoceptor", "entity2": "bisoprolol", "span1": [218, 237], "span2": [182, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1982": {"label": 1, "data": {"text": "We further probed the interaction of mibefradil with inactivated Nav1.5 channels.", "entity1": "Nav1.5", "entity2": "mibefradil", "span1": [65, 71], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9020": {"label": 1, "data": {"text": "The mitogenic effect of DHT on bone cells was inhibited by antiandrogens (hydroxyflutamide and cyproterone acetate) which compete for binding to the androgen receptor.", "entity1": "androgen receptor", "entity2": "hydroxyflutamide", "span1": [149, 166], "span2": [74, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2553": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "platelet derived growth factor (PDGF) receptor", "entity2": "imatinib mesylate", "span1": [135, 181], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8607": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "ALP", "entity2": "TAA", "span1": [41, 44], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3601": {"label": 1, "data": {"text": "We found distinct differences in the action of ifenprodil at GluN1/GluN2B in comparison with previous studies on the effect of zinc on GluN1/GluN2A gating, which may arise due to their unique binding sites.", "entity1": "GluN2B", "entity2": "ifenprodil", "span1": [67, 73], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6566": {"label": 3, "data": {"text": "We changed the residues to alanine using site-directed mutagenesis technique, expressed the mutants in a baculovirus/Sf9 cell system, and analyzed the kinetic characteristics of inhibition of the mutant enzymes by milrinone and cilostazol, specific inhibitors of PDE3.", "entity1": "PDE3", "entity2": "cilostazol", "span1": [263, 267], "span2": [228, 238]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4754": {"label": 3, "data": {"text": "In cultured vascular smooth muscle cells (VSMCs), rAAV-mediated CYP2J2 overexpression and EETs markedly suppressed Ang II-induced inflammatory cytokine expression.", "entity1": "Ang II", "entity2": "EETs", "span1": [115, 121], "span2": [90, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8791": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "Rb", "entity2": "CAPE", "span1": [209, 211], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15541": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "tissue inhibitor of metalloproteinase-1", "entity2": "DMN", "span1": [173, 212], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12460": {"label": 2, "data": {"text": "This report concerns the marked up-regulation in differentiated CaCo-2 colonic epithelial cells of two key inflammatory interleukins, IL-6 and IL-8, caused by a mixture of oxysterols representative of a high cholesterol diet.", "entity1": "IL-8", "entity2": "cholesterol", "span1": [143, 147], "span2": [208, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2141": {"label": 1, "data": {"text": "The effect of troglitazone on ENT1 was PPAR(gamma)-independent and kinetic studies revealed that troglitazone was a competitive inhibitor of ENT1.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [30, 34], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15240": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B1", "entity2": "silychristin", "span1": [0, 7], "span2": [280, 292]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"14985": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "cip1", "entity2": "ATO", "span1": [76, 80], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1342": {"label": 4, "data": {"text": "The esterified-BM, however, had only partial transactivation agonistic activity in cells transfected with rat GR, whereas BM and esterified-DEX had full transactivation agonistic activity.", "entity1": "rat GR", "entity2": "BM", "span1": [106, 112], "span2": [15, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7296": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "Bile acid-coenzyme A:amino acid N-acyltransferase", "entity2": "taurine", "span1": [12, 61], "span2": [155, 162]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10100": {"label": 3, "data": {"text": "Acute and chronic PLZ administration increase brain GABA levels, an effect due, at least in part, to an inhibition of the activity of the GABA metabolizing enzyme, GABA transaminase (GABA-T).", "entity1": "GABA transaminase", "entity2": "PLZ", "span1": [164, 181], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14323": {"label": 2, "data": {"text": "Results showed that DMF increased nuclear levels of Nrf2, and both DMF and adenovirus-mediated overexpression of Nrf2 (Ad-Nrf2) decreased PAI-1, alpha-smooth muscle actin (alpha-SMA), fibronectin and type 1 collagen expression in TGF-beta-treated rat mesangial cells (RMCs) and renal fibroblast cells (NRK-49F).", "entity1": "Nrf2", "entity2": "DMF", "span1": [52, 56], "span2": [20, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8239": {"label": 5, "data": {"text": "As a result of this study, microgrewiapine A (1) was found to be a selective cytotoxic agent for colon cancer cells over normal colon cells and to exhibit nicotinic receptor antagonistic activity for both the h\u03b13\u03b24 and h\u03b14\u03b22 receptor subtypes.", "entity1": "nicotinic receptor", "entity2": "microgrewiapine A", "span1": [155, 173], "span2": [27, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2771": {"label": 3, "data": {"text": "Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.", "entity1": "cyclooxygenase-2", "entity2": "lumiracoxib", "span1": [55, 71], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7434": {"label": 1, "data": {"text": "The D1-SPD structure shows that the K-167_EL-2-E-302_EL-3 (EL-2: extracellular loop 2; EL-3: extracellular loop 3) salt bridge plays an important role for both the conformational change of the extracellular domain and the binding of SPD.", "entity1": "D1", "entity2": "SPD", "span1": [4, 6], "span2": [7, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13660": {"label": 1, "data": {"text": "High-resolution NMR spectroscopy was used to determine the docking of a substrate (prostaglandin H2) mimic (U46619) to the engineered prostacyclin (PGI2) synthase (PGIS) in solution.", "entity1": "prostacyclin (PGI2) synthase", "entity2": "U46619", "span1": [134, 162], "span2": [108, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10978": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "PKC", "entity2": "PMA", "span1": [199, 202], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9892": {"label": 1, "data": {"text": "A similar discrepancy in sensitivity to competitors between 3H-NMPB and 3H-QNB was also observed when biperiden was used as a competitor, indicating that binding to different subtypes of the mAch receptor could not account for the observed differences in sensitivity to competition.", "entity1": "mAch receptor", "entity2": "biperiden", "span1": [191, 204], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10981": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "PKC", "entity2": "phorbol 12-myristate 13-acetate", "span1": [199, 202], "span2": [68, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9516": {"label": 5, "data": {"text": "Saturation and competition studies in the presence or absence of the histamine H1 receptor antagonist, levocabastine, revealed that [3H]SR 142948A bound with similar affinities to both the levocabastine-insensitive neurotensin NT1 receptors (20% of the total binding population) and the recently cloned levocabastine-sensitive neurotensin NT2 receptors (80% of the receptors) (Kd = 6.8 and 4.8 nM, respectively).", "entity1": "histamine H1 receptor", "entity2": "levocabastine", "span1": [69, 90], "span2": [103, 116]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5005": {"label": 1, "data": {"text": "This study is the first to identify Class V CGPs with their distinctive methine or trimethine linkage between two disubstituted pyrylium moieties as a particularly potent class of MRP modulators and also show that within this core structure, differences in the electronegativity associated with a chalcogen atom can be the sole determinant of whether a compound will stimulate or inhibit MRP2.", "entity1": "MRP", "entity2": "methine", "span1": [180, 183], "span2": [72, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1103": {"label": 3, "data": {"text": "Carvedilol reduced the risk of death or heart failure in patients with above-median levels of N-BNP or adrenomedullin, or both, to rates not significantly different from those observed in patients with levels below the median value.", "entity1": "adrenomedullin", "entity2": "Carvedilol", "span1": [103, 117], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9339": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "6,7-dinitroquinoxaline-2,3-dione", "span1": [72, 77], "span2": [140, 172]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10050": {"label": 1, "data": {"text": "Long-chain alkanols are general anesthetics which can also act as uncharged noncompetitive inhibitors of the peripheral nicotinic acetylcholine receptor (AChR) by binding to one or more specific sites on the AChR.", "entity1": "AChR", "entity2": "Long-chain alkanols", "span1": [208, 212], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10257": {"label": 9, "data": {"text": "No trans-stimulation of [3H]-MPP+ outflow was observed by the OCTN1 and OCTN2 substrate carnitine at 100 microM.", "entity1": "OCTN2", "entity2": "[3H]-MPP+", "span1": [72, 77], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14327": {"label": 3, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "TGF-beta", "entity2": "DMF", "span1": [194, 202], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10816": {"label": 9, "data": {"text": "Treatment with valsartan, doxazosin, or N-acetylcysteine did not significantly affect HIF-1alpha and VEGF proteins expression in the banding groups.", "entity1": "HIF-1alpha", "entity2": "valsartan", "span1": [86, 96], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15788": {"label": 0, "data": {"text": "Phosphorylation on Ser and Thr residues of pannexin1 was increased during potentiation, possibly mediating HC opening.", "entity1": "pannexin1", "entity2": "Ser", "span1": [43, 52], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8545": {"label": 2, "data": {"text": "Compounds 8\u2009b and 10\u2009c selectively inhibited HDAC6 at the nanomolar level, whereas the other hydroxamates effected an increase in acetyl-\u03b1-tubulin levels in human acute myeloid leukemia U937 cells.", "entity1": "acetyl-\u03b1-tubulin", "entity2": "hydroxamates", "span1": [130, 146], "span2": [93, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5537": {"label": 1, "data": {"text": "Labeling with [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and [125I]IAS migrated at the same position on an SDS-PAGE gel as the beta 2AR labeled by the antagonist photoaffinity label [125I]iodoazidobenzylpindolol ([125I]IABP).", "entity1": "beta 2AR", "entity2": "[(125)I]IAS", "span1": [178, 186], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9600": {"label": 1, "data": {"text": "All GCs including the antagonistic compound RU486 efficiently reduced NF-kappaB-mediated transactivation to comparable extents, suggesting that ligand-induced nuclear localization of the GR is sufficient for transrepression.", "entity1": "GR", "entity2": "RU486", "span1": [187, 189], "span2": [44, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4841": {"label": 9, "data": {"text": "Cucurbitacin I inhibits rac1 activation in breast cancer cells by a reactive oxygen species-mediated mechanism and independently of janus tyrosine kinase 2 and p-rex1.", "entity1": "p-rex1", "entity2": "Cucurbitacin I", "span1": [160, 166], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7294": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "furin", "entity2": "PFD", "span1": [175, 180], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"1285": {"label": 3, "data": {"text": "N-[2-(cyclohexyloxyl)-4-nitrophenyl]-methanesulfonamide (NS-398), a selective cyclooxygenase-2 inhibitor, also inhibited cell proliferation, whereas it did not cause apoptosis.", "entity1": "cyclooxygenase-2", "entity2": "NS-398", "span1": [78, 94], "span2": [57, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4565": {"label": 4, "data": {"text": "The A2A adenosine receptor agonist CGS21680 (C23H29N7O6.HCl.xH2O) (0.001-0.1 \u03bcM) did not alter NE oxidation currents.", "entity1": "A2A adenosine receptor", "entity2": "C23H29N7O6.HCl.xH2O", "span1": [4, 26], "span2": [45, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1887": {"label": 1, "data": {"text": "I3A bound to PKC-alpha in the presence of phosphatidylserine with high affinity; however, under these assay conditions, little PKC isoform selectivity was observed.", "entity1": "PKC", "entity2": "I3A", "span1": [127, 130], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15787": {"label": 9, "data": {"text": "MRS2179, a P2Y1R blocker, prevented potentiation in EDL, but not soleus muscles, suggesting that in fast muscles ATP activates P2Y1 but not P2X receptors.", "entity1": "P2X receptors", "entity2": "ATP", "span1": [140, 153], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1440": {"label": 3, "data": {"text": "To determine whether 3,4-methylenedioxymethamphetamine (MDMA)-induced reductions in SERT density could be related to such a mechanism, p-chlorophenylalanine or MDMA was administered to rats, and brain serotonin and SERT density were measured.", "entity1": "SERT", "entity2": "MDMA", "span1": [84, 88], "span2": [56, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11603": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "cystathionine-gamma-lyase", "entity2": "Hydrogen sulphide", "span1": [75, 100], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7577": {"label": 1, "data": {"text": "In both rodent and primate animal models, the binding of radiolabeled d-MPH to dopamine transporter was found to be selective, saturable, and reversible, whereas binding of l-MPH was diffuse and nonspecific.", "entity1": "dopamine transporter", "entity2": "d-MPH", "span1": [79, 99], "span2": [70, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6017": {"label": 5, "data": {"text": "Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use.", "entity1": "histamine H1", "entity2": "emedastine", "span1": [56, 68], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15709": {"label": 3, "data": {"text": "Xanthohumol and 2-hydroxychalcone induced apoptosis by Bcl-2 downregulation.", "entity1": "Bcl-2", "entity2": "2-hydroxychalcone", "span1": [55, 60], "span2": [16, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7648": {"label": 3, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "Panx1", "entity2": "GTP", "span1": [78, 83], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8323": {"label": 2, "data": {"text": "Our findings confirmed that Paeoniflorin protected EA.hy926 cells against radiation-induced injury through the Nrf2/HO-1 pathway.", "entity1": "Nrf2", "entity2": "Paeoniflorin", "span1": [111, 115], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1166": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "repaglinide", "span1": [68, 72], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14838": {"label": 1, "data": {"text": "From the resolved free and bound NADH fluorescence signatures, the KD values for both NADH conformations in ALDH1A1 ranged from about 24 \u03bcM to 1 \u03bcM for Mg(2+) ion concentrations of 0-6000 \u03bcM, respectively.", "entity1": "ALDH1A1", "entity2": "NADH", "span1": [108, 115], "span2": [86, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1364": {"label": 8, "data": {"text": "Several active analogues were also evaluated for their ability to block uptake of DA, 5-HT, and NE and inhibit binding of [(125)I] RTI-55 at HEK-hDAT, HEK-hSERT, and HEK-hNET cells.", "entity1": "hSERT", "entity2": "5-HT", "span1": [155, 160], "span2": [86, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10515": {"label": 3, "data": {"text": "Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance.", "entity1": "kinase", "entity2": "GW572016", "span1": [25, 31], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6401": {"label": 0, "data": {"text": "The attachment of a fatty acid chain to LysB29 provided insulin detemir with reduced receptor affinities and metabolic and mitogenic potencies but did not change the balance between mitogenic and metabolic potencies.", "entity1": "insulin", "entity2": "fatty acid", "span1": [56, 63], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"418": {"label": 1, "data": {"text": "RS 17053 showed high affinity and selectivity for alpha 1A adrenoceptors (pKi 8.6) relative to alpha 1B (pKi = 7.3) and alpha 1D (pKi = 7.1) subtypes.", "entity1": "alpha 1A adrenoceptors", "entity2": "RS 17053", "span1": [50, 72], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9259": {"label": 3, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "ergovaline", "span1": [50, 53], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15303": {"label": 3, "data": {"text": "The effects of the phosphodiesterase type 5 inhibitor vardenafil on cognitive performance in healthy adults: a behavioral- electroencephalography study.", "entity1": "phosphodiesterase type 5", "entity2": "vardenafil", "span1": [19, 43], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15937": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "insulin", "entity2": "metformin", "span1": [139, 146], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2782": {"label": 8, "data": {"text": "In conclusion, immortalized SHR and WKY PTE cells take up l-alanine mainly through a high-affinity Na(+)-dependent amino acid transporter, with functional features of ASCT2 transport.", "entity1": "ASCT2", "entity2": "l-alanine", "span1": [167, 172], "span2": [58, 67]}, "weak_labels": [0, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"358": {"label": 1, "data": {"text": "dSERT1 shows little transport of other monoamines and is Na+ and Cl- dependent.", "entity1": "dSERT1", "entity2": "Cl-", "span1": [0, 6], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11316": {"label": 3, "data": {"text": "Ten IU/mL urokinase was also incubated with pooled plasma of stroke patients, that was previously oxidized with the singlet oxygen (1O2) donor chloramine T (CT), to destroy plasmatic PAI-1 and alpha2-antiplasmin.", "entity1": "plasmatic PAI-1", "entity2": "CT", "span1": [173, 188], "span2": [157, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1094": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "ambenonium", "span1": [51, 71], "span2": [73, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"349": {"label": 1, "data": {"text": "Affinities for the major nonadrenergic [125I]PIC binding site were highly comparable to human subtype-I1 imidazol(in)e receptor sites in the brain stem (rank order: moxonidine > clonidine > cirazoline > IDX > amiloride).", "entity1": "human subtype-I1 imidazol(in)e receptor", "entity2": "clonidine", "span1": [88, 127], "span2": [178, 187]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7614": {"label": 3, "data": {"text": "CONCLUSIONS: Lapatinib is a dual inhibitor of the EGFR and HER2 tyrosine kinases.", "entity1": "EGFR", "entity2": "Lapatinib", "span1": [50, 54], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5334": {"label": 3, "data": {"text": "No effects were observed when fenclozic acid was assessed for P450-dependent and P450-independent cytotoxicity to THLE cell lines, time-dependent inhibition of five major human cytochrome P450 enzymes, inhibition of the biliary efflux transporters BSEP and MRP2 or mitochondrial toxicity to THLE or HepG2 cells.", "entity1": "human cytochrome P450", "entity2": "fenclozic acid", "span1": [171, 192], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8780": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "Akt2", "entity2": "CAPE", "span1": [62, 66], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7645": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "niflumic acid", "span1": [34, 39], "span2": [356, 369]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13683": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imiquimod", "span1": [138, 142], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9685": {"label": 3, "data": {"text": "2 In a chronic transfection model using CHO-K1 cells, cisapride inhibited HERG tail currents after a step to +25 mV with similar potency at room and physiological temperatures (IC50 16.", "entity1": "HERG", "entity2": "cisapride", "span1": [74, 78], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12877": {"label": 2, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "phosphatidylethanolamine", "span1": [13, 19], "span2": [195, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9837": {"label": 3, "data": {"text": "Geldanamycin also disrupts the T-cell receptor-mediated activation of nuclear factor of activated T-cells (NF-AT).", "entity1": "nuclear factor of activated T-cells", "entity2": "Geldanamycin", "span1": [70, 105], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14139": {"label": 1, "data": {"text": "When combined, mianserin antagonized the effects of the full kappa-opioid receptor agonists in [(35)S]GTPgammaS assays and reduced the stimulation of p38 MAPK and ERK1/2 phosphorylation by dynorphin A.", "entity1": "kappa-opioid receptor", "entity2": "[(35)S]GTPgammaS", "span1": [61, 82], "span2": [95, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12790": {"label": 2, "data": {"text": "By contrast, telmisartan attenuated 11beta-hydroxysteroid dehydrogenase type 1 mRNA level in differentiated adipocytes.", "entity1": "11beta-hydroxysteroid dehydrogenase type 1", "entity2": "telmisartan", "span1": [36, 78], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15002": {"label": 3, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "cytokine", "entity2": "DHA", "span1": [123, 131], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7095": {"label": 8, "data": {"text": "Furthermore, D-aspartate-induced currents in outside-out patches from IPCs exhibited larger steady-state currents than responses elicited by L-glutamate, a prominent feature of GLAST, and examination of cochlea from GLAST-Discosoma red (DsRed) promoter reporter mice revealed that DsRed expression was restricted to IPCs and other supporting cells surrounding IHCs.", "entity1": "GLAST", "entity2": "L-glutamate", "span1": [177, 182], "span2": [141, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4167": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "NF-\u03baB", "entity2": "2-oxaisodauc-5-en-12-al", "span1": [173, 178], "span2": [124, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11366": {"label": 1, "data": {"text": "The relatively high D(2) receptor occupancy, even at trough plasma levels, suggests that ziprasidone is more similar to risperidone and olanzapine in receptor occupancy profile than to clozapine and quetiapine.", "entity1": "D(2) receptor", "entity2": "clozapine", "span1": [20, 33], "span2": [185, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10113": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "Cyclooxygenase-1", "entity2": "ketoprofen", "span1": [0, 16], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7303": {"label": 8, "data": {"text": "The recombinant strains of the flavinogenic yeast Candida famata, which contain the DNA fragment consisting of the FMN1 gene (encoding the riboflavin kinase, enzyme that converts riboflavin to flavinmononucleotide) driven by the strong promoters (the regulated RIB1 or constitutive TEF1 promoter) were isolated.", "entity1": "riboflavin kinase", "entity2": "flavinmononucleotide", "span1": [139, 156], "span2": [193, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"11517": {"label": 3, "data": {"text": "Rofecoxib only diminished COX-2 protein expression and MCP-1 gene expression in vascular atheroma.", "entity1": "COX-2", "entity2": "Rofecoxib", "span1": [26, 31], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1142": {"label": 3, "data": {"text": "ZD1839 (\"Iressa\"), a quinazoline tyrosine kinase inhibitor selective for the EGFR, has shown good activity in preclinical studies and in the early phase of clinical trials.", "entity1": "tyrosine kinase", "entity2": "ZD1839", "span1": [33, 48], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15264": {"label": 2, "data": {"text": "Three variables of cardiac vagal effects (the root mean square of successive differences [rMSSD] in the interbeat interval of the heart rate [IBI], heart-rate variability [HRV] caused by peak-valley respiratory sinus arrhythmia [pvRSA], and high-frequency power [HF]) and heart rate (HR) were obtained at seven time points during the clamps, characterised by increasing levels of insulin (achieved by administering insulin plus glucose, glucose only, glucose and GLP-1, and glucose and GLP-1 combined with arginine).", "entity1": "insulin", "entity2": "glucose", "span1": [380, 387], "span2": [437, 444]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10775": {"label": 3, "data": {"text": "Imatinib mesylate is a tyrosine kinase inhibitor of the ABL, platelet-derived growth factor receptor (PDGFR), and c-kit kinases.", "entity1": "PDGFR", "entity2": "Imatinib mesylate", "span1": [102, 107], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13624": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-l(R)-aminoindan] is a second-generation propargylamine pharmacophore that selectively and irreversibly inhibits brain MAO-B and is specifically designed for the treatment of Parkinson's disease (PD).", "entity1": "MAO-B", "entity2": "propargylamine", "span1": [142, 147], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5148": {"label": 0, "data": {"text": "Here we report the solution structure of the SH2 domain of C-terminal Src kinase (Csk) in complex with a longer phosphopeptide from Csk-binding protein (Cbp).", "entity1": "Csk", "entity2": "C", "span1": [82, 85], "span2": [59, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7483": {"label": 3, "data": {"text": "Phenserine apparently reduces translational efficiency of APP mRNA into protein, a process that may involve an interaction with iron and/or an iron-responsive element.", "entity1": "APP", "entity2": "Phenserine", "span1": [58, 61], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8802": {"label": 2, "data": {"text": "Although fisetin greatly increases the stability of both Nrf2 and ATF4, only the effect on ATF4 is dependent on protein kinase activity.", "entity1": "ATF4", "entity2": "fisetin", "span1": [66, 70], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12288": {"label": 1, "data": {"text": "Alpha-2B adrenergic receptor mediated hemodynamic profile of etomidate.", "entity1": "Alpha-2B adrenergic receptor", "entity2": "etomidate", "span1": [0, 28], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14662": {"label": 0, "data": {"text": "Genistein also reduced the formation of stress fibers by thrombin and suppressed thrombin-induced phosphorylation of myosin light chain (MLC) on Ser(19)/Thr(18) in endothelial cells (ECs).", "entity1": "MLC", "entity2": "Thr", "span1": [137, 140], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7297": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "BAAT", "entity2": "taurine", "span1": [63, 67], "span2": [155, 162]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14407": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "Rap1", "entity2": "ESI-09", "span1": [268, 272], "span2": [145, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4222": {"label": 2, "data": {"text": "The results showed that (1) 15mg/kg body weight PhIP induced obvious histopathological changes in gastric mucosa; (2) PhIP (10 and/or 15mg/kg) significantly decreased superoxide dismutase (SOD) and glutathioneperoxidase (GPx) activities, while increased catalase (CAT) activity compared with the control.", "entity1": "catalase", "entity2": "PhIP", "span1": [254, 262], "span2": [118, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14316": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "ARE", "entity2": "DMF", "span1": [61, 64], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5742": {"label": 5, "data": {"text": "SB225002 (SB) is an IL-8 receptor B (IL-8RB) antagonist that has previously been shown to inhibit IL-8-based cancer cell invasion, and to possess in vivo anti-inflammatory and anti-nociceptive effects.", "entity1": "IL-8RB", "entity2": "SB225002", "span1": [37, 43], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5529": {"label": 4, "data": {"text": "To determine the position of the phenyl ring of the aralkyloxyalkyl side chain of salmeterol in the beta 2AR binding site, we designed and synthesized the agonist photoaffinity label [(125)I]iodoazidosalmeterol ([125I]IAS).", "entity1": "beta 2AR", "entity2": "[125I]IAS", "span1": [100, 108], "span2": [212, 221]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10563": {"label": 5, "data": {"text": "Irbesartan is a long-acting angiotensin II antagonist acting specifically at the level of the Type 1-receptor subtype (AT1-receptor).", "entity1": "angiotensin II", "entity2": "Irbesartan", "span1": [28, 42], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4958": {"label": 3, "data": {"text": "The results suggested that fisetin treatment inhibits mTORC1 activity in an Akt-dependent manner.", "entity1": "Akt", "entity2": "fisetin", "span1": [76, 79], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15896": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "PKS", "entity2": "benzopyranopyrrole", "span1": [80, 83], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6782": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-2", "entity2": "carprofen", "span1": [257, 262], "span2": [148, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4785": {"label": 3, "data": {"text": "Taken together, these data demonstrate that baicalin inhibits the metabolism of DXM in a concentration-dependent manner in rats, possibly through inhibiting hepatic CYP2D and CYP3A activities.", "entity1": "CYP3A", "entity2": "baicalin", "span1": [175, 180], "span2": [44, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15515": {"label": 1, "data": {"text": "We found that, both in a cell-free system and in cells, NO/SNO donors such as S-nitrosocysteine and S-nitrosoglutathione readily induced the S-nitrosylation of Prx1, causing structural and functional alterations.", "entity1": "Prx1", "entity2": "NO", "span1": [160, 164], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9754": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "(AR)s", "entity2": "fluparoxan", "span1": [103, 108], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5532": {"label": 2, "data": {"text": "In direct adenylyl cyclase activation, in effects on adenylyl cyclase after pretreatment of intact cells, and in guinea pig tracheal relaxation assays, IAS and the parent drug salmeterol behave essentially the same.", "entity1": "adenylyl cyclase", "entity2": "IAS", "span1": [53, 69], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4957": {"label": 3, "data": {"text": "The results suggested that fisetin treatment inhibits mTORC1 activity in an Akt-dependent manner.", "entity1": "mTORC1", "entity2": "fisetin", "span1": [54, 60], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7827": {"label": 4, "data": {"text": "Cellular release of AChE by SH-SY5Y is significantly enhanced by the muscarinic acetylcholine receptor (mAChR) agonists carbachol or muscarine, with the effect of carbachol blocked by the mAChR antagonist atropine.", "entity1": "muscarinic acetylcholine receptor", "entity2": "carbachol", "span1": [69, 102], "span2": [120, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2974": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "Y612F", "entity2": "IBMX", "span1": [64, 69], "span2": [56, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7703": {"label": 2, "data": {"text": "atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans.", "entity1": "AChE", "entity2": "diazepam", "span1": [10, 14], "span2": [127, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15507": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "Prx1", "entity2": "cysteines", "span1": [163, 167], "span2": [90, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12784": {"label": 8, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "2-deoxythymidine-5-monophosphate", "span1": [22, 24], "span2": [216, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6464": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "thymidylate synthase", "entity2": "Alimta", "span1": [90, 110], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2650": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "8-methoxymethyl-3-isobutyl-1-methylxanthine", "span1": [397, 414], "span2": [18, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6357": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "candesartan", "span1": [25, 28], "span2": [172, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8584": {"label": 3, "data": {"text": "The high fat diet significantly increased hepatic mRNA expressions of PPAR\u03b3, SREBP1C and SCD-1 genes in comparison to the control diet, which was subsequently reversed by supplementation with fisetin.", "entity1": "SREBP1C", "entity2": "fisetin", "span1": [77, 84], "span2": [192, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2877": {"label": 3, "data": {"text": "AIM: To assess the efficacy and safety of a 24-week treatment with sitagliptin, a highly selective once-daily oral dipeptidyl peptidase-4 (DPP-4) inhibitor, in patients with type 2 diabetes who had inadequate glycaemic control [glycosylated haemoglobin (HbA(1c)) >or=7.5% and <or=10.5%] while on glimepiride alone or in combination with metformin.", "entity1": "DPP-4", "entity2": "sitagliptin", "span1": [139, 144], "span2": [67, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9577": {"label": 5, "data": {"text": "The observed inhibition on IFN-gamma, GM-CSF, and IL-3 mRNA was blocked by the selective beta2AR antagonist ICI 118,551 (10(-6) M) and by timolol (10(-6) M), a nonselective antagonist.", "entity1": "beta2AR", "entity2": "timolol", "span1": [89, 96], "span2": [138, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"707": {"label": 3, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "AChE", "entity2": "organophosphorus", "span1": [130, 134], "span2": [22, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11821": {"label": 1, "data": {"text": "The expression pattern of Sim2 and Drebrin correspond to 50mmol/L glucose (hyperglycaemia) was also found in primary cultured neurons.", "entity1": "Drebrin", "entity2": "glucose", "span1": [35, 42], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7328": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT2", "entity2": "MNI", "span1": [235, 240], "span2": [123, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13574": {"label": 3, "data": {"text": "The next large phase III adjuvant trial for this subset of breast cancer is an international collaboration designed to evaluate the added or alternative benefit of an oral tyrosine kinase inhibitor targeting HER2/neu as well as the epidermal growth factor receptor (EGFR), lapatinib.", "entity1": "neu", "entity2": "lapatinib", "span1": [213, 216], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3529": {"label": 9, "data": {"text": "2-Deoxyglucose increased phosphorylation of tuberous sclerosis complex 2 (TSC2) on AMPK consensus sites but did not change the amount of TSC1 bound to TSC2.", "entity1": "TSC1", "entity2": "2-Deoxyglucose", "span1": [137, 141], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1050": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "mitoxantrone", "span1": [162, 166], "span2": [205, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1734": {"label": 1, "data": {"text": "beta2AR density measured with [3H]dihydroalprenolol ([3H]DHA) increased either 13- or 77-fold in infected cells compared to mock infected controls depending on the culture conditions used.", "entity1": "beta2AR", "entity2": "[3H]dihydroalprenolol", "span1": [0, 7], "span2": [30, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"734": {"label": 2, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "Human and rat renin", "entity2": "cilazapril", "span1": [0, 19], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8146": {"label": 2, "data": {"text": "Increased urinary excretion of albumin, hemopexin, transferrin and VDBP correlates with chronic sensitization to gentamicin nephrotoxicity in rats.", "entity1": "hemopexin", "entity2": "gentamicin", "span1": [40, 49], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14390": {"label": 3, "data": {"text": "These findings suggest that NFD inhibited the EGF-induced invasion and migration of MDA-MB-231 cells via EGFR-dependent PI3K/Akt signaling, leading to the down-regulation of MMP-9 expression.", "entity1": "EGFR", "entity2": "NFD", "span1": [105, 109], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1163": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "nateglinide", "span1": [161, 165], "span2": [36, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"261": {"label": 0, "data": {"text": "In contrast, the Ala-->Gly replacement has less impact in protecting the chloride channel from the action of insecticidal blockers.", "entity1": "chloride channel", "entity2": "Ala", "span1": [73, 89], "span2": [17, 20]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6384": {"label": 8, "data": {"text": "Ornithine decarboxylase (ODC) catalyses the first step in the synthesis of the polyamines putrescine, spermidine and spermine.", "entity1": "ODC", "entity2": "spermine", "span1": [25, 28], "span2": [117, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11432": {"label": 1, "data": {"text": "In the presence of alphaAR blockade, concentration-response curves for isoproterenol, norepinephrine, and epinephrine suggested that a beta1AR was involved in this response, and the rank order of potency was isoproterenol > norepinephrine = epinephrine.", "entity1": "beta1AR", "entity2": "norepinephrine", "span1": [135, 142], "span2": [224, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"551": {"label": 8, "data": {"text": "N-Acetylglucosamine-1-phosphodiester alpha-N-Acetylglucosaminidase (EC 3.1.4.45; phosphodiester alpha-GlcNAcase) catalyzes the second step in the synthesis of the mannose 6-phosphate determinant required for efficient intracellular targeting of newly synthesized lysosomal hydrolases to the lysosome.", "entity1": "EC 3.1.4.45", "entity2": "mannose 6-phosphate", "span1": [68, 79], "span2": [163, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14129": {"label": 1, "data": {"text": "Celastrol highlights the therapeutic potential of agents targeting TAK1 as a key node in this pro-oncogenic TGF-\u03b2-NF-\u03baB signal pathway.", "entity1": "NF-\u03baB", "entity2": "Celastrol", "span1": [114, 119], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5910": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "LDL", "entity2": "probucol", "span1": [172, 175], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10364": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-5", "entity2": "GW660511X", "span1": [52, 59], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12420": {"label": 1, "data": {"text": "Tetrodotoxin-sensitive spontaneous cholinergic neurotransmission was blocked >80% by 1\u00a0pM BoNT/A despite cleaving <20% of the SNAP-25.", "entity1": "SNAP-25", "entity2": "Tetrodotoxin", "span1": [126, 133], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14205": {"label": 1, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "eseroline", "span1": [83, 88], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8648": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b2", "entity2": "melatonin", "span1": [31, 35], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8529": {"label": 2, "data": {"text": "In macrophages, levels of TNF-\u03b1, IFN-\u03b3, NO, IL-6 and IL-10 were increased by CDM used alone or in combination with HSV-2.", "entity1": "TNF-\u03b1", "entity2": "CDM", "span1": [26, 31], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4846": {"label": 2, "data": {"text": "Lastly, we found that RhoA activation by cucurbitacin I is mediated by reactive oxygen species (ROS).", "entity1": "RhoA", "entity2": "cucurbitacin I", "span1": [22, 26], "span2": [41, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11628": {"label": 1, "data": {"text": "CONCLUSIONS: The data advance the novel hypothesis that central sympatholysis with dexmedetomidine constitutes a highly effective countermeasure for cocaine's sympathomimetic actions on the human cardiovascular system, even in individuals carrying the alpha2CDel322-325 polymorphism.", "entity1": "alpha2C", "entity2": "dexmedetomidine", "span1": [252, 259], "span2": [83, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1056": {"label": 3, "data": {"text": "In contrast, in the presence of Ca UFH accelerated the inhibition of factor Xa by antithrombin 10-fold more efficiently than comparable concentrations of the high affinity fractions of enoxaparin and fragmin.", "entity1": "factor Xa", "entity2": "Ca", "span1": [69, 78], "span2": [32, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10036": {"label": 1, "data": {"text": "Fibrates bind to the peroxisome proliferator-activated receptor (PPAR)-alpha, and thiazolidinediones are ligands of PPAR-gamma.", "entity1": "PPAR-gamma", "entity2": "thiazolidinediones", "span1": [116, 126], "span2": [82, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15132": {"label": 3, "data": {"text": "The fecal elimination, IC, and systemic clearance of apixaban were increased upon AC administration in both BDC rats and dogs and were decreased in BDC rats dosed with GF-120918, a dual BCRP and P-gp inhibitor).", "entity1": "P-gp", "entity2": "GF-120918", "span1": [195, 199], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3477": {"label": 6, "data": {"text": "Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu\u2084 receptor.", "entity1": "mGlu\u2084", "entity2": "Lu AF21934", "span1": [120, 125], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, 9]},
	"4763": {"label": 3, "data": {"text": "Previously, we have found that BRN-103, a nicotinamide derivative, inhibits vascular endothelial growth factor (VEGF)-mediated angiogenesis signaling in human endothelial cells.", "entity1": "vascular endothelial growth factor", "entity2": "nicotinamide", "span1": [76, 110], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9269": {"label": 8, "data": {"text": "Ergovaline inhibition of radioligand binding to the D2 dopamine receptor and ergot alkaloid inhibition of vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production in GH4ZR7 cells, stably transfected with a rat D2 dopamine receptor, were evaluated.", "entity1": "VIP", "entity2": "cyclic AMP", "span1": [137, 140], "span2": [153, 163]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3167": {"label": 1, "data": {"text": "A few compounds, 17alpha-methyltestosterone (17alpha-MT), vinclozolin and linuron, were studied using a real world scenario, i.e., assuming that their interaction with the AR was not known: A prescreening for agonism and true, competitive antagonism was used to select conditions such as the appropriate mode of action, and the working range excluding cytotoxicity for the final screening.", "entity1": "AR", "entity2": "vinclozolin", "span1": [172, 174], "span2": [58, 69]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10509": {"label": 0, "data": {"text": "RESULTS: GW572016 inhibited constitutive and/or ligand-induced EGFR or HER2 tyrosine phosphorylation of all five cell lines, which correlated with the antiproliferative response in all but one cell line.", "entity1": "EGFR", "entity2": "tyrosine", "span1": [63, 67], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5363": {"label": 3, "data": {"text": "All these results demonstrate that vitamin C prevents CS(E)-induced NF-\u03baB activation and thus it could be used for the prevention of CS-induced inflammatory diseases.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [68, 73], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12828": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "pyridoxine 5'-phosphate oxidase", "entity2": "PLP", "span1": [123, 154], "span2": [69, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15516": {"label": 1, "data": {"text": "We found that, both in a cell-free system and in cells, NO/SNO donors such as S-nitrosocysteine and S-nitrosoglutathione readily induced the S-nitrosylation of Prx1, causing structural and functional alterations.", "entity1": "Prx1", "entity2": "SNO", "span1": [160, 164], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5409": {"label": 2, "data": {"text": "Type I deiodinase, liver fatty-acid binding protein and cytochrome P450 (CYP) 3A37 mRNA levels were significantly induced by TCPP, while TDCPP induced CYP3A37 and CYP2H1.", "entity1": "cytochrome P450 (CYP) 3A37", "entity2": "TCPP", "span1": [56, 82], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15749": {"label": 2, "data": {"text": "Quercetin (100\u03bcM) induced HO-1 and depleted heme pool when incubated to human hepatocytes.", "entity1": "HO-1", "entity2": "Quercetin", "span1": [26, 30], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2819": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "VEGF", "entity2": "Dexamethasone", "span1": [56, 60], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12088": {"label": 3, "data": {"text": "), both MAO-A and MAO-B by nialamide (75 mg/kg i.p.)", "entity1": "MAO-A", "entity2": "nialamide", "span1": [8, 13], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3261": {"label": 3, "data": {"text": "The contractions to 5-HT were inhibited by ketanserin and alosetron indicating involvement of 5-HT(2A) and 5-HT(3) receptors, respectively.", "entity1": "5-HT(3)", "entity2": "alosetron", "span1": [107, 114], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"756": {"label": 5, "data": {"text": "Synthesis and antagonistic activity at muscarinic receptor subtypes of some 2-carbonyl derivatives of diphenidol.", "entity1": "muscarinic receptor", "entity2": "diphenidol", "span1": [39, 58], "span2": [102, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13295": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "PDGFR", "entity2": "Nexavar", "span1": [244, 249], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14994": {"label": 9, "data": {"text": "In monocytes, both EPA and DHA increased interleukin (IL)-10 without affecting tumor necrosis factor (TNF)-\u03b1 and IL-6.", "entity1": "tumor necrosis factor (TNF)-\u03b1", "entity2": "DHA", "span1": [79, 108], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1582": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines", "span1": [59, 64], "span2": [163, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3513": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "AKRs", "entity2": "o-quinones", "span1": [22, 26], "span2": [142, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4987": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bax", "entity2": "vitamin E", "span1": [151, 154], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3046": {"label": 8, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "PGES", "entity2": "PGE(2)", "span1": [100, 104], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9179": {"label": 8, "data": {"text": "Staining around the edges of the brown fat cells was observed with the SSAO substrates, tyramine and benzylamine.", "entity1": "SSAO", "entity2": "tyramine", "span1": [71, 75], "span2": [88, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3760": {"label": 3, "data": {"text": "The significantly decreased levels of p-PI3K and p-AKT expression were observed in SGC-7901 cells after \u03b2-ionone treatments in a time- and dose-dependent manner (P\u00a0<\u00a00.01).", "entity1": "p-AKT", "entity2": "\u03b2-ionone", "span1": [49, 54], "span2": [104, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5027": {"label": 8, "data": {"text": "ACTH-stimulated peak cortisol, delta cortisol, and delta DHEA-S levels are decreased during hyperthyroidism, probably due to increased turnover.", "entity1": "ACTH", "entity2": "delta DHEA", "span1": [0, 4], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4476": {"label": 1, "data": {"text": "Exposure to sibutramine was higher in subjects with the CYP2B6*6/*6 genotype, but no statistical difference was observed among the CYP2B6 genotypes.", "entity1": "CYP2B6", "entity2": "sibutramine", "span1": [56, 62], "span2": [12, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9838": {"label": 3, "data": {"text": "Geldanamycin also disrupts the T-cell receptor-mediated activation of nuclear factor of activated T-cells (NF-AT).", "entity1": "NF-AT", "entity2": "Geldanamycin", "span1": [107, 112], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3787": {"label": 2, "data": {"text": "These results indicate that phillyrin prevents lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation, suggesting that phillyrin is a novel AMPK activator with a role in the prevention and treatment of obesity.", "entity1": "AMPK", "entity2": "phillyrin", "span1": [195, 199], "span2": [174, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8400": {"label": 9, "data": {"text": "Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD.", "entity1": "kinase domain", "entity2": "AC220", "span1": [66, 79], "span2": [50, 55]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9045": {"label": 1, "data": {"text": "The apparent affinity of benzodiazepine receptors for clonazepam in mice receiving alprazolam (0.05 mg/kg) was unchanged from that in untreated control mice, an observation suggesting that low doses of alprazolam increased receptor number.", "entity1": "benzodiazepine receptors", "entity2": "clonazepam", "span1": [25, 49], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8980": {"label": 3, "data": {"text": "The suppressive effect of ceruletide on barrel rotation could be partially countered by MK-329, a selective peripheral CCK (CCK-A) receptor antagonist.", "entity1": "(CCK-A) receptor", "entity2": "ceruletide", "span1": [123, 139], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15572": {"label": 1, "data": {"text": "After 18\u00a0h incubation with 0.5\u00a0\u03bcM Py3MeO-TBPo and subsequent red light irradiation (3.6\u00a0J/cm(2)), a high number of cells die by apoptosis, as evaluated by morphological alterations, immunofluorescent relocalization of Bax from cytosol to mitochondria, and TUNEL assay.", "entity1": "Bax", "entity2": "Py3MeO-TBPo", "span1": [218, 221], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"625": {"label": 3, "data": {"text": "Pretreatment of the splenocytes with both BPB and AACOCF3 suppressed phorbol 12-myristate 13-acetate plus ionomycin-induced IL-2 secretion in a concentration-dependent manner.", "entity1": "IL-2", "entity2": "BPB", "span1": [124, 128], "span2": [42, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4295": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B3", "entity2": "dehydroepiandrosterone sulfate", "span1": [269, 276], "span2": [94, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5249": {"label": 3, "data": {"text": "A series of carbamoylmethylene linked prodrugs of 1 (BMS-582949), a clinical p38\u03b1 inhibitor, were synthesized and evaluated.", "entity1": "p38\u03b1", "entity2": "BMS-582949", "span1": [77, 81], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8812": {"label": 1, "data": {"text": "Interestingly, SB203580, a selective inhibitor of p38 MAPK, blocked STIM1 phosphorylation and led to sustained STIM1-puncta formation and Ca2+ entry.", "entity1": "STIM1", "entity2": "SB203580", "span1": [111, 116], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13012": {"label": 3, "data": {"text": "It has been known for decades that lithium chloride (LiCl) leads to D-myo-inositol 1-phosphate accumulation on GPCR activation by inhibiting inositol monophosphatase, the final enzyme of the IP3 metabolic cascade.", "entity1": "inositol monophosphatase", "entity2": "lithium chloride", "span1": [141, 165], "span2": [35, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8596": {"label": 2, "data": {"text": "Further, both the flavonoids were also found to increase the expression of some of the prominent markers for differentiation of osteoblast like osteopontin, osterix, RunX2, osteoprotegerin and osteocalcin.", "entity1": "RunX2", "entity2": "flavonoids", "span1": [166, 171], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12338": {"label": 1, "data": {"text": "In sum, identification of PIM-1 as an ER\u03b1 target gene adds a novel potential mechanism by which estrogens can contribute to breast cancer cell proliferation and carcinogenesis.", "entity1": "PIM-1", "entity2": "estrogens", "span1": [26, 31], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12520": {"label": 1, "data": {"text": "These findings suggest that ceruletide specifically suppresses the barrel rotation evoked by SMS 201-995 in a long-lasting manner possibly acting through CCK-A receptor.", "entity1": "CCK-A receptor", "entity2": "SMS 201-995", "span1": [154, 168], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8985": {"label": 1, "data": {"text": "Role of extracellular calcium and calmodulin in prolactin secretion induced by hyposmolarity, thyrotropin-releasing hormone, and high K+ in GH4C1 cells.", "entity1": "prolactin", "entity2": "calcium", "span1": [48, 57], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8014": {"label": 3, "data": {"text": "In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-\u03b1-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.", "entity1": "TNF-\u03b1", "entity2": "hyperoside", "span1": [73, 78], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13807": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "ABL", "entity2": "BMS-354825", "span1": [101, 104], "span2": [76, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12780": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "Xeloda", "span1": [22, 24], "span2": [134, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9576": {"label": 5, "data": {"text": "The observed inhibition on IFN-gamma, GM-CSF, and IL-3 mRNA was blocked by the selective beta2AR antagonist ICI 118,551 (10(-6) M) and by timolol (10(-6) M), a nonselective antagonist.", "entity1": "beta2AR", "entity2": "ICI 118,551", "span1": [89, 96], "span2": [108, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6266": {"label": 1, "data": {"text": "In vitro and in vivo studies have shown that argatroban has advantages over heparin for the inhibition of clot-bound thrombin and for the enhancement of thrombolysis with TPA.", "entity1": "TPA", "entity2": "argatroban", "span1": [171, 174], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2283": {"label": 2, "data": {"text": "In addition to this evidence (for the involvement of EP2 receptors), evidence for the involvement of EP1 receptors in the PGE1 mediated stimulation of Na,K-ATPase beta subunit gene transcription includes the stimulatory effect of 17-phenyl trinor PGE2, as well as the inhibitory effects of SC-51089.", "entity1": "Na,K-ATPase beta", "entity2": "17-phenyl trinor PGE2", "span1": [151, 167], "span2": [230, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"352": {"label": 1, "data": {"text": "Affinities for the major nonadrenergic [125I]PIC binding site were highly comparable to human subtype-I1 imidazol(in)e receptor sites in the brain stem (rank order: moxonidine > clonidine > cirazoline > IDX > amiloride).", "entity1": "human subtype-I1 imidazol(in)e receptor", "entity2": "amiloride", "span1": [88, 127], "span2": [209, 218]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2855": {"label": 2, "data": {"text": "Finally, the amounts of RORalpha and cAspAT mRNAs were similarly increased by TZD treatment of human adipose tissue explants, confirming coordinated regulation.", "entity1": "RORalpha", "entity2": "TZD", "span1": [24, 32], "span2": [78, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5119": {"label": 3, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "HO-1", "entity2": "NO", "span1": [192, 196], "span2": [140, 142]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8442": {"label": 5, "data": {"text": "RATIONALE: Histamine H3 receptor antagonists, such as ABT-288, have been shown to possess cognitive-enhancing and wakefulness-promoting effects.", "entity1": "Histamine H3 receptor", "entity2": "ABT-288", "span1": [11, 32], "span2": [54, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9318": {"label": 3, "data": {"text": "One possible explanation is that, in our model, remikiren in contrast to CGP 38560A and enalkiren is able to inhibit renin in a functionally important extraplasmatic compartment.", "entity1": "renin", "entity2": "CGP 38560A", "span1": [117, 122], "span2": [73, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6488": {"label": 4, "data": {"text": "The segments were contracted with the alpha(2)-adrenoceptor agonists brimonidine, apraclonidine, and oxymetazoline.", "entity1": "alpha(2)-adrenoceptor", "entity2": "oxymetazoline", "span1": [38, 59], "span2": [101, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12228": {"label": 2, "data": {"text": "Furthermore, because S-(+)-isomers of METH and AMPH are reported to be more potent and efficacious in vivo than R-(-), we determined the enantiomeric selectivity of all three species of TAAR1.", "entity1": "TAAR1", "entity2": "METH", "span1": [186, 191], "span2": [38, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"379": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "IL-5", "entity2": "Dexamethasone", "span1": [71, 75], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12045": {"label": 1, "data": {"text": "These suggest that the repeated administration of low-doses of METH causes quantitative changes of the signaling of alpha(2A)-AR in the mouse hippocampus.", "entity1": "alpha(2A)-AR", "entity2": "METH", "span1": [116, 128], "span2": [63, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9534": {"label": 8, "data": {"text": "System y+ cationic amino acid transport is mediated by proteins encoded by a family of genes, Cat1, Cat2, and Cat3.", "entity1": "System y+", "entity2": "amino acid", "span1": [0, 9], "span2": [19, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10271": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "transmembrane transporters", "entity2": "MPP+", "span1": [135, 161], "span2": [55, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"10306": {"label": 3, "data": {"text": "Therefore, in men with ED, elevation of cGMP in corpus cavernosal tissue via selective inhibition of cGMP-specific PDE5 is a means of improving erectile function at minimal risk of adverse events.", "entity1": "PDE5", "entity2": "cGMP", "span1": [115, 119], "span2": [101, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"307": {"label": 4, "data": {"text": "In contrast, the D-1997-induced responses were potently and concentration-dependently antagonized by the mixed 5-HT1-like and 5-HT2 receptor antagonist methiothepin (0.01-1 microM).", "entity1": "5-HT1-like", "entity2": "D-1997", "span1": [111, 121], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10638": {"label": 3, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "bile salt export pump", "entity2": "glibenclamide", "span1": [53, 74], "span2": [27, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15704": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "ASICs", "entity2": "menthol", "span1": [63, 68], "span2": [165, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9168": {"label": 7, "data": {"text": "Phenylbutazone (PB), a nonsteroidal anti-inflammatory drug, is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS).", "entity1": "PHS", "entity2": "Phenylbutazone", "span1": [151, 154], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"12810": {"label": 3, "data": {"text": "However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [164, 169], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11282": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "EC 2.1.1.10", "entity2": "Gly", "span1": [116, 127], "span2": [198, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5125": {"label": 3, "data": {"text": "In this study, we found that 5-hydroxy-3,6,7,8,3'4'-hexamethoxyflavone (5HHMF) from Hizikia fusiforme considerably inhibits lipopolysaccharide (LPS)-stimulated NO production by suppressing the expression of inducible NO synthase (iNOS) in BV2 microglia.", "entity1": "iNOS", "entity2": "5-hydroxy-3,6,7,8,3'4'-hexamethoxyflavone", "span1": [230, 234], "span2": [29, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13004": {"label": 1, "data": {"text": "D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation.", "entity1": "G protein-coupled receptor", "entity2": "D-myo-inositol 1-phosphate", "span1": [92, 118], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5719": {"label": 8, "data": {"text": "CRPC is characterized by reactivation of the androgen axis due to changes in androgen receptor signaling and/or adaptive intratumoral androgen biosynthesis.", "entity1": "androgen receptor", "entity2": "androgen", "span1": [77, 94], "span2": [45, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12999": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "delta 8-delta 7 isomerase", "entity2": "amorolfine", "span1": [173, 198], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5760": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "parkin", "entity2": "MPTP", "span1": [233, 239], "span2": [185, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10540": {"label": 1, "data": {"text": "A transcription factor-transcription factor binding array analysis of nuclear lysate from RA-treated cells indicated several prominent RARalpha binding partners; among these, Oct1, NFATc3, and CREB2 were identified by competition EMSA and supershift and chromatin immunoprecipitation assays as components of the complex.", "entity1": "NFATc3", "entity2": "RA", "span1": [181, 187], "span2": [90, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4508": {"label": 3, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "human carboxylesterases 1", "entity2": "acyl glucuronides", "span1": [102, 127], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1891": {"label": 1, "data": {"text": "I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance.", "entity1": "C1b domain", "entity2": "diacylglycerol", "span1": [62, 72], "span2": [148, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13887": {"label": 3, "data": {"text": "Elucidation of the novel molecular mechanisms linking ibuprofen to RhoA inhibition may provide additional therapeutic targets to the disorders characterized by RhoA activation, including spinal cord injuries and Alzheimer's disease.", "entity1": "RhoA", "entity2": "ibuprofen", "span1": [67, 71], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11371": {"label": 1, "data": {"text": "PKC-delta in particular showed a different pattern of translocation in response to I3A and PMA.", "entity1": "PKC-delta", "entity2": "PMA", "span1": [0, 9], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1289": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "GAD", "entity2": "gamma-aminobutyric acid", "span1": [50, 53], "span2": [109, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"6455": {"label": 3, "data": {"text": "RESULTS: Halothane anesthesia reversibly inhibited metabolic rhodopsin regeneration and thus prevented rhodopsin from absorbing high numbers of photons during light exposure.", "entity1": "rhodopsin", "entity2": "Halothane", "span1": [103, 112], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4043": {"label": 3, "data": {"text": "In addition, we found that neoechinulin A significantly suppressed the production of neurotoxic inflammatory mediator tumour necrosis factor-\u03b1 (TNF-\u03b1), interleukin-1\u03b2 (IL-1\u03b2), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) in activated BV-2 cells.", "entity1": "IL-6", "entity2": "neoechinulin A", "span1": [191, 195], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13256": {"label": 2, "data": {"text": "The inhibitory effect of the leukotriene receptor antagonist on leukotriene D4-induced MUC2/5AC gene expression and mucin secretion in human airway epithelial cells.", "entity1": "MUC2/5AC", "entity2": "leukotriene D4", "span1": [87, 95], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5232": {"label": 2, "data": {"text": "In further evaluation, the representative compound N,N-diethyl-N-(2-(N-methyltetradecanamido)ethyl)prop-2-en-1-aminium bromide (3b) exhibited potent pro-apoptotic activity, through RhoB activation, in HeLa cells.", "entity1": "RhoB", "entity2": "N,N-diethyl-N-(2-(N-methyltetradecanamido)ethyl)prop-2-en-1-aminium bromide", "span1": [181, 185], "span2": [51, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1763": {"label": 1, "data": {"text": "This study demonstrates enhanced cardiostimulation by CGP 12177A (in the presence of propranolol) in rat ventricular myocytes overexpressing beta(1)-adrenoceptors, mediated by a Gs/cAMP signalling pathway.", "entity1": "beta(1)-adrenoceptors", "entity2": "CGP 12177A", "span1": [141, 162], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7805": {"label": 2, "data": {"text": "RSV targets and activates the NAD(+)-dependent protein deacetylase SIRT1; in turn, SIRT1 induces an intracellular antioxidative mechanism by inducing mitochondrial superoxide dismutase (SOD2).", "entity1": "NAD(+)-dependent protein deacetylase SIRT1", "entity2": "RSV", "span1": [30, 72], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11381": {"label": 1, "data": {"text": "Thus, the cranio-selective vasoconstriction elicited by ergotamine in dogs is predominantly mediated by 5-HT1B receptors as well as alpha2A/2C-adrenoceptor subtypes and, to a lesser extent, by alpha1-adrenoceptors.", "entity1": "alpha1-adrenoceptors", "entity2": "ergotamine", "span1": [193, 213], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8270": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "CYP3A4", "entity2": "Methadone", "span1": [91, 97], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9398": {"label": 0, "data": {"text": "In Drosophila, glutamyl-prolyl-tRNA synthetase is a multifunctional synthetase encoded by a unique gene and composed of three domains: the amino- and carboxy-terminal domains catalyze the aminoacylation of glutamic acid and proline tRNA species, respectively, and the central domain is made of 75 amino acids repeated six times amongst which 46 are highly conserved and constitute the repeated motifs [Cerini, C., Kerjan, P., Astier, M., Gratecos, D., Mirande, M. & Semeriva, M. (1991) EMBO J.", "entity1": "glutamyl-prolyl-tRNA synthetase", "entity2": "carboxy", "span1": [15, 46], "span2": [150, 157]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8909": {"label": 3, "data": {"text": "Combined application of dexamethasone and amrinone caused additive inhibition of TNF biosynthesis in vitro.", "entity1": "TNF", "entity2": "dexamethasone", "span1": [81, 84], "span2": [24, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8610": {"label": 3, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "ALP", "entity2": "NAC", "span1": [41, 44], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4949": {"label": 1, "data": {"text": "The inhibitory effect of fisetin on adipogenesis is dependent of mTOR activity, suggesting that fisetin inhibits adipogenesis and the accumulation of intracellular triglycerides during adipocyte differentiation by targeting mTORC1 signaling.", "entity1": "mTOR", "entity2": "fisetin", "span1": [65, 69], "span2": [25, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8659": {"label": 2, "data": {"text": "The expression kinetics of TAp63, c-Abl and TAp73 suggest that cisplatin activates TAp63-dependent expression of c-Abl and TAp73 and, in turn, the activation of TAp73 by c-Abl-induced BAX expression.", "entity1": "TAp73", "entity2": "cisplatin", "span1": [161, 166], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3338": {"label": 3, "data": {"text": "Rasagiline is a propargylamine and irreversible monoamine oxidase (MAO) B inhibitor used for the treatment of Parkinson's disease (PD).", "entity1": "monoamine oxidase (MAO) B", "entity2": "Rasagiline", "span1": [48, 73], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2627": {"label": 3, "data": {"text": "We show that sorafenib (BAY 43-9006, Nexavar) potently inhibits FLT3 enzymatic and signaling activities.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [64, 68], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10577": {"label": 2, "data": {"text": "In peripheral lymphocytes of healthy and diseased subjects, IMQ induced a significant increase of perforin(+) CTLs within 12h in all experiments performed.", "entity1": "perforin", "entity2": "IMQ", "span1": [98, 106], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9626": {"label": 1, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "NBF1", "entity2": "MgATP", "span1": [200, 204], "span2": [142, 147]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15535": {"label": 2, "data": {"text": "CK significantly inhibited DMN-induced increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, fibrosis score, and hepatic malondialdehyde and collagen content.", "entity1": "AST", "entity2": "DMN", "span1": [121, 124], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7518": {"label": 2, "data": {"text": "The AMPK inhibitor Compound C prevented the action of metformin and AICAR but not phenformin.", "entity1": "AMPK", "entity2": "phenformin", "span1": [4, 8], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14497": {"label": 1, "data": {"text": "Estrogen effects are mediated not only through nuclear ERs but also through cytoplasmic/membrane ERs and G-protein-coupled ERs.", "entity1": "G-protein", "entity2": "Estrogen", "span1": [105, 114], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12906": {"label": 3, "data": {"text": "Hydrogen sulfide inhibits nitric oxide production and nuclear factor-kappaB via heme oxygenase-1 expression in RAW264.7 macrophages stimulated with lipopolysaccharide.", "entity1": "nuclear factor-kappaB", "entity2": "Hydrogen sulfide", "span1": [54, 75], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8209": {"label": 2, "data": {"text": "Pb and BaP treatments significantly increased active caspase-3 levels in a time-dependent manner.", "entity1": "caspase-3", "entity2": "Pb", "span1": [53, 62], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14191": {"label": 9, "data": {"text": "After SU5416 treatment, cell viability, PARP-1, and caspase-3 protein levels were not changed.", "entity1": "caspase-3", "entity2": "SU5416", "span1": [52, 61], "span2": [6, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7456": {"label": 8, "data": {"text": "We have expressed VIAAT and the plasmalemmal transporters for glycine and GABA in a neuroendocrine cell line and measured the quantal release of glycine and GABA using a novel double-sniffer patch-clamp technique.", "entity1": "VIAAT", "entity2": "GABA", "span1": [18, 23], "span2": [74, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1459": {"label": 3, "data": {"text": "), did not induce the behavioural hyperactivity syndrome which is seen following inhibition of both MAO-A and MAO-B by tranylcypromine together with the monoamine precursors.", "entity1": "MAO-B", "entity2": "tranylcypromine", "span1": [110, 115], "span2": [119, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7000": {"label": 8, "data": {"text": "These observations strongly suggest that the up-regulation of terminal PGESs that are preferentially coupled with COX-1, especially mPGES-2, plays the pivotal role in PS liposome-induced PGE2 production by microglia.", "entity1": "PGESs", "entity2": "PGE2", "span1": [71, 76], "span2": [187, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11011": {"label": 1, "data": {"text": "Cyproheptadine is a piperidine antihistamine that increases appetite through its antiserotonergic effect on 5-HT2 receptors in the brain.", "entity1": "5-HT2", "entity2": "antihistamine", "span1": [108, 113], "span2": [31, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12719": {"label": 1, "data": {"text": "It is suggested that HSP expression at the time of H2O2 exposure protects astrocytes from oxidative injury and apoptotic cell death by means of pro-survival Akt.", "entity1": "Akt", "entity2": "H2O2", "span1": [157, 160], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3725": {"label": 3, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "MEK", "entity2": "N", "span1": [228, 231], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13280": {"label": 9, "data": {"text": "The imatinib-resistant KIT(D816V) mutant, associated with systemic mastocytosis, was found to be resistant to sorafenib.", "entity1": "KIT", "entity2": "sorafenib", "span1": [23, 26], "span2": [110, 119]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14189": {"label": 2, "data": {"text": "We previously demonstrated that the somatostatinergic system, implicated in neuronal survival control, can be modulated by \u03b1-tocopherol in the rat dentate gyrus, increasing cyclic adenosine monophosphate response element binding protein phosphorylation.", "entity1": "cyclic adenosine monophosphate response element binding protein", "entity2": "\u03b1-tocopherol", "span1": [173, 236], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13707": {"label": 3, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.4", "entity2": "4-iodopropofol", "span1": [150, 158], "span2": [94, 108]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12988": {"label": 1, "data": {"text": "The C677T polymorphism of the methylene-tetrahydrofolate reductase (MTHFR) gene is associated with a reduction of catalytic activity and is suggested to modify cancer risk differently depending on folate status.", "entity1": "MTHFR", "entity2": "folate", "span1": [68, 73], "span2": [197, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4364": {"label": 2, "data": {"text": "Administration of a single dose of DEX-P showed a temporal increase in CYP3A activity in both tissues and the induction ratios reached maximum values at 12\u2009h after DEX-P administration.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [71, 76], "span2": [35, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11735": {"label": 1, "data": {"text": "These results show that the robust effects of TCDD on the mRNA expression of Snrpn, Peg3 and Igf2r genes in the sperm and of Igf2r in the muscle and liver are unrelated to changes in methylation in their respective genes.", "entity1": "Snrpn", "entity2": "TCDD", "span1": [77, 82], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6482": {"label": 3, "data": {"text": "Patients who received oxime prior to hospitalization had a higher rate of intermediate syndrome and lower levels of BuChE at admission than those who had not.", "entity1": "BuChE", "entity2": "oxime", "span1": [116, 121], "span2": [22, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12187": {"label": 1, "data": {"text": "Several variables associated to thymidylate synthase (TS), the biological target of 5-fluorouracil (5FU) have been studied for their possible role as predictors of the clinical outcome and response to chemotherapy in colorectal cancer (CRC) patients.", "entity1": "thymidylate synthase", "entity2": "5FU", "span1": [32, 52], "span2": [100, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9053": {"label": 1, "data": {"text": "Chlorpromazine, levomepromazine, and their metabolites had 5-30 times higher binding affinities for muscarinic cholinergic receptors than fluphenazine, perphenazine and their metabolites.", "entity1": "muscarinic cholinergic receptors", "entity2": "perphenazine", "span1": [100, 132], "span2": [152, 164]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12170": {"label": 1, "data": {"text": "After 3 weeks' bupropion treatment we studied the change in DAT activity, which corresponds to the occupancy of bupropion.", "entity1": "DAT", "entity2": "bupropion", "span1": [60, 63], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6048": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "m-CPP", "span1": [73, 79], "span2": [128, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12760": {"label": 3, "data": {"text": "Ang II level in plasma and mesenteric arteries in SHR group was the same or lower than that in WKY group, and was higher in irbesartan group and lower in imidapril group.", "entity1": "Ang II", "entity2": "imidapril", "span1": [0, 6], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5184": {"label": 1, "data": {"text": "Dioscin-induced autophagy via ERK1/2 and JNK1/2 pathways may provide a protective mechanism for cell survival against dioscin-induced apoptosis to act as a cytoprotective reaction.", "entity1": "ERK1/2", "entity2": "Dioscin", "span1": [30, 36], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4688": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "TCDD", "span1": [111, 117], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6696": {"label": 3, "data": {"text": "Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively).", "entity1": "TRPM8", "entity2": "thio-BCTC", "span1": [96, 101], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7497": {"label": 1, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Activation of alpha1-AMPK is associated with inhibition of apical amiloride-sensitive Na(+) channels (ENaC), which has important implications for the clinical use of metformin.", "entity1": "alpha1-AMPK", "entity2": "metformin", "span1": [44, 55], "span2": [196, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5932": {"label": 3, "data": {"text": "4-MA, a well known 5 alpha-reductase inhibitor, is also a potent inhibitor of 3 beta-HSD with a Ki value of 56 nM.", "entity1": "3 beta-HSD", "entity2": "4-MA", "span1": [78, 88], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14789": {"label": 2, "data": {"text": "Human immortalized corneal fibroblasts were treated with TGF-\u03b2 in the presence of TSA, the NAD(P)H oxidase inhibitor diphenyleneiodonium (DPI), the antioxidant N-acetyl-cysteine (NAC), the NF-E2-related factor 2-antioxidant response element (Nrf2-ARE) activator sulforaphane, or small interfering RNA.", "entity1": "NF-E2-related factor 2", "entity2": "sulforaphane", "span1": [189, 211], "span2": [262, 274]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15634": {"label": 3, "data": {"text": "In conclusion, nobiletin attenuates HGF-induced HepG2 cells metastasis involving both ERK and PI3K/Akt pathways and are potentially useful as anti-metastatic agents for the treatment of hepatoma.", "entity1": "ERK", "entity2": "nobiletin", "span1": [86, 89], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13099": {"label": 4, "data": {"text": "Among the measured compounds, gliquidone and glipizide (two sulfonylureas), as well as nateglinide (a glinide), exhibit PPARgamma agonistic activity at concentrations comparable with those reached under pharmacological treatment.", "entity1": "PPARgamma", "entity2": "glinide", "span1": [120, 129], "span2": [102, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6244": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-HT1D", "entity2": "sumatriptan", "span1": [115, 121], "span2": [17, 28]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3953": {"label": 0, "data": {"text": "Moreover, VK2-2,3 epoxide, an intracellular metabolite of VK2, was shown to covalently bind to the cysteine-166 residue of Bak.", "entity1": "Bak", "entity2": "cysteine", "span1": [123, 126], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11121": {"label": 1, "data": {"text": "Rec 15/2739, WB 4101, SL 89,0591, (+)- and (-)- tamsulosin showed selectivity for alpha 1A and alpha 1D adrenoceptors relative to the alpha 1B subtype.", "entity1": "alpha 1B subtype", "entity2": "WB 4101", "span1": [134, 150], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3547": {"label": 2, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "p65", "entity2": "LTD4", "span1": [56, 59], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8563": {"label": 2, "data": {"text": "Under NaCl and sorbitol stresses, catalase (CAT) activity in wnk8 mutant was 1.92- and 3.7-times of that in Col-0, respectively.", "entity1": "catalase", "entity2": "NaCl", "span1": [34, 42], "span2": [6, 10]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15552": {"label": 2, "data": {"text": "Extrinsic apoptotic pathway markers such as Fas levels and caspase-8 activity increased as a result of CdTe-QD exposure.", "entity1": "caspase-8", "entity2": "CdTe", "span1": [59, 68], "span2": [103, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7007": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "VEGFRs", "entity2": "sunitinib", "span1": [220, 226], "span2": [173, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10719": {"label": 3, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "activator protein (AP)-1", "entity2": "Dimemorfan", "span1": [93, 117], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14596": {"label": 3, "data": {"text": "17-Allylamino-17-demethoxygeldanamycin (17-AAG), an Hsp90 inhibitor, is currently under evaluation for its anticancer activity in clinical trials.", "entity1": "Hsp90", "entity2": "17-Allylamino-17-demethoxygeldanamycin", "span1": [52, 57], "span2": [0, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4016": {"label": 3, "data": {"text": "The anti-inflammatory actions of curcumin on colitis may involve inhibition of the TLR4/NF-\u03baB signaling pathway and of IL-27 expression.", "entity1": "IL-27", "entity2": "curcumin", "span1": [119, 124], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4855": {"label": 5, "data": {"text": "[6]-Gingerol derived from Zingiber officinale Roscoe (ginger) was identified as a novel angiotensin II type 1 receptor antagonist, with an IC50 value of 8.173 \u00b5M.", "entity1": "angiotensin II type 1 receptor", "entity2": "[6]-Gingerol", "span1": [88, 118], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10058": {"label": 3, "data": {"text": "It showed high rat lymphoma growth-inhibitory and lytic activity in vitro (IC50 = 0.16 mM), based specifically on inhibition of x(c)--mediated cystine uptake, in contrast to its colonic metabolites, sulfapyridine and 5-aminosalicylic acid.", "entity1": "x(c)", "entity2": "5-aminosalicylic acid", "span1": [128, 132], "span2": [217, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4253": {"label": 2, "data": {"text": "Furthermore, butein treatment caused nuclear accumulation of nuclear factor-E2-related factor 2 (Nrf2) and increased the promoter activity of antioxidant response elements (AREs).", "entity1": "Nrf2", "entity2": "butein", "span1": [97, 101], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1876": {"label": 1, "data": {"text": "Monodemethylated mifepristone bound to rabbit thymic GR with higher affinity than monodemethylated CDB-2914 or CDB-4124.", "entity1": "rabbit thymic GR", "entity2": "CDB-2914", "span1": [39, 55], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4891": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "aromatase", "entity2": "F", "span1": [148, 157], "span2": [99, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7292": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "TGF-beta", "entity2": "PFD", "span1": [143, 151], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14572": {"label": 2, "data": {"text": "The aim of the present work was to evaluate the effectiveness of such an antidote by testing whether doxorubicin (DOX), a known P-gp inducer, could efficiently protect Caco-2 cells against PQ cytotoxicity, 6 h after the incubation with the herbicide, reflecting a real-life intoxication scenario.", "entity1": "P-gp", "entity2": "doxorubicin", "span1": [128, 132], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13778": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Tykerb", "span1": [14, 16], "span2": [126, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9961": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [166, 171], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6822": {"label": 3, "data": {"text": "The induction of apoA-I by statins disappeared with addition of mevalonate, which indicates that the effect is HMG-CoA reductase inhibition-dependent.", "entity1": "apoA-I", "entity2": "mevalonate", "span1": [17, 23], "span2": [64, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2149": {"label": 3, "data": {"text": "The effect of troglitazone on ENT1 was PPAR(gamma)-independent and kinetic studies revealed that troglitazone was a competitive inhibitor of ENT1.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [141, 145], "span2": [97, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14787": {"label": 1, "data": {"text": "Treatment with TSA and the Nrf2-ARE activator resulted in increased inhibition of the TGF-\u03b2-induced myofibroblast differentiation as compared with treatment with DPI or NAC.", "entity1": "TGF-\u03b2", "entity2": "DPI", "span1": [86, 91], "span2": [162, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3922": {"label": 3, "data": {"text": "Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group facilitates both enhancement of PDE4-inhibitory activity and restoration of potent PDE3 inhibition.", "entity1": "PDE3", "entity2": "6-aryl-4,5-dihydropyridazin-3(2H)-one", "span1": [166, 170], "span2": [14, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9822": {"label": 9, "data": {"text": "Treatment with geldanamycin, however, does not affect the activation of lysophosphatide acyltransferase, which is a plasma membrane enzyme coupled to the T-cell receptor after T-cell stimulation.", "entity1": "lysophosphatide acyltransferase", "entity2": "geldanamycin", "span1": [72, 103], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11703": {"label": 2, "data": {"text": "The results showed that wogonoside promotes the expression of LC3-II and Beclin-1.", "entity1": "LC3-II", "entity2": "wogonoside", "span1": [62, 68], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15021": {"label": 3, "data": {"text": "Interestingly, AdOx disrupted actin cytoskeleton structures, leading to morphological changes, and suppressed the formation of a signaling complex composed of Src and p85/PI3K, which is linked to various tumorigenic responses.", "entity1": "actin", "entity2": "AdOx", "span1": [30, 35], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9565": {"label": 2, "data": {"text": "Secretion of GM-CSF protein in the presence of increasing concentrations of isoproterenol followed a similar pattern as observed for GM-CSF mRNA.", "entity1": "GM-CSF", "entity2": "isoproterenol", "span1": [13, 19], "span2": [76, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13078": {"label": 8, "data": {"text": "Methylthioadenosine phosphorylase (MTAP) salvages purines by releasing adenine from methylthioadenosine and is often deleted in mesothelioma.", "entity1": "MTAP", "entity2": "methylthioadenosine", "span1": [35, 39], "span2": [84, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7821": {"label": 5, "data": {"text": "Efficacy of the GluK1/AMPA receptor antagonist LY293558 against seizures and neuropathology in a soman-exposure model without pretreatment and its pharmacokinetics after intramuscular administration.", "entity1": "GluK1", "entity2": "LY293558", "span1": [16, 21], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12855": {"label": 1, "data": {"text": "BACKGROUND AND AIMS: Thymidylate synthase (TS) is an important enzyme for DNA synthesis and the target for 5-fluorouracil (5-FU).", "entity1": "Thymidylate synthase", "entity2": "5-fluorouracil", "span1": [21, 41], "span2": [107, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10659": {"label": 2, "data": {"text": "Treatment of both differentiating adipocytes and fully differentiated adipocytes with telmisartan caused a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin.", "entity1": "PPARgamma", "entity2": "telmisartan", "span1": [150, 159], "span2": [86, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14661": {"label": 0, "data": {"text": "Genistein also reduced the formation of stress fibers by thrombin and suppressed thrombin-induced phosphorylation of myosin light chain (MLC) on Ser(19)/Thr(18) in endothelial cells (ECs).", "entity1": "myosin light chain", "entity2": "Thr", "span1": [117, 135], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13823": {"label": 9, "data": {"text": "Atomoxetine has a high affinity and selectivity for norepinephrine transporters, but little or no affinity for various neurotransmitter receptors.", "entity1": "neurotransmitter receptors", "entity2": "Atomoxetine", "span1": [119, 145], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12296": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Apoa4", "entity2": "Quercetin", "span1": [135, 140], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15379": {"label": 8, "data": {"text": "Studies on the kinetics of the hSULT2A1-catalyzed sulfation of dehydroepiandrosterone (DHEA) showed the effects of disulfide bond formation on the substrate inhibition characteristics of the enzyme.", "entity1": "hSULT2A1", "entity2": "DHEA", "span1": [31, 39], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"5505": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "[-]-cyclazocine", "span1": [108, 126], "span2": [303, 318]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12980": {"label": 8, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "DGK", "entity2": "phosphatidic acid", "span1": [132, 135], "span2": [99, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"7881": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "protease", "entity2": "ritonavir", "span1": [15, 23], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7001": {"label": 8, "data": {"text": "These observations strongly suggest that the up-regulation of terminal PGESs that are preferentially coupled with COX-1, especially mPGES-2, plays the pivotal role in PS liposome-induced PGE2 production by microglia.", "entity1": "COX-1", "entity2": "PGE2", "span1": [114, 119], "span2": [187, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8845": {"label": 2, "data": {"text": "Moreover, calycopterin, in presence of H2O2 inhibited the decrease caused by oxidative stress in stress-sensing transcription factors, CREB and Nrf2, which play an important role in antioxidant capacity of the cell.", "entity1": "CREB", "entity2": "calycopterin", "span1": [135, 139], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2571": {"label": 3, "data": {"text": "Brain tissue analyses revealed that neonatal quinpirole treatment produced a significant decrease in hippocampal NGF, BDNF and ChAT that was eliminated by olanzapine treatment.", "entity1": "ChAT", "entity2": "quinpirole", "span1": [127, 131], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10115": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "Cyclooxygenase-1", "entity2": "ketrolack", "span1": [0, 16], "span2": [66, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5458": {"label": 2, "data": {"text": "The TSA-induced uc002mbe.2 expression was positively correlated with the apoptotic effect of TSA in HCC cells.", "entity1": "uc002mbe.2", "entity2": "TSA", "span1": [16, 26], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5574": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "human CA", "entity2": "acetazolamide", "span1": [69, 77], "span2": [211, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"740": {"label": 5, "data": {"text": "Combination treatment with the selective 5-HT1A antagonist WAY100635 produced a dose-dependent augmentation of venlafaxine-induced (3-30 mg/kg s.c) extracellular 5-HT concentrations, but had no further effect on NA above that produced by venlafaxine alone.", "entity1": "5-HT1A", "entity2": "WAY100635", "span1": [41, 47], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9378": {"label": 1, "data": {"text": "However, recovery from modulation by cyclothiazide was twofold slower for GluR-AiBi than for homomeric GluR-Ai, indicating that the GluR-A and GluR-B subunits are not functionally equivalent in controlling sensitivity to cyclothiazide.", "entity1": "GluR-A", "entity2": "cyclothiazide", "span1": [132, 138], "span2": [221, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13418": {"label": 8, "data": {"text": "Furthermore, the enzymatic activity of alanine aminotransferase (ALT), which converts the critical gluconeogenic amino acid alanine into pyruvate, is decreased (approximately 50%) in KLF15-/- hepatocytes.", "entity1": "ALT", "entity2": "pyruvate", "span1": [65, 68], "span2": [137, 145]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"10035": {"label": 1, "data": {"text": "Fibrates bind to the peroxisome proliferator-activated receptor (PPAR)-alpha, and thiazolidinediones are ligands of PPAR-gamma.", "entity1": "peroxisome proliferator-activated receptor (PPAR)-alpha", "entity2": "Fibrates", "span1": [21, 76], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7206": {"label": 1, "data": {"text": "Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism.", "entity1": "ERalpha", "entity2": "Cadmium", "span1": [64, 71], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4807": {"label": 3, "data": {"text": "The modification of the inhibitor scaffold of 1 and 2 from a dihydroquinolinone core to a tetrahydropyrazolopyridinone core led to discovery of a new series of potent KAT II inhibitors with excellent physicochemical properties.", "entity1": "KAT II", "entity2": "tetrahydropyrazolopyridinone", "span1": [167, 173], "span2": [90, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3336": {"label": 1, "data": {"text": "We demonstrate that rasagiline protects against cell death induced by the combination of free radicals generated by paraquat and either wild-type or A53T mutant alpha-synuclein over-expression.", "entity1": "alpha-synuclein", "entity2": "rasagiline", "span1": [161, 176], "span2": [20, 30]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14400": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "insulin", "entity2": "ESI-09", "span1": [334, 341], "span2": [145, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3553": {"label": 2, "data": {"text": "LTD4 also induced expression of cysteinyl leukotriene receptor 1 (CysLT(1)R) and NF-\u03baB p65 in the hippocampus and cortex.", "entity1": "cysteinyl leukotriene receptor 1", "entity2": "LTD4", "span1": [32, 64], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2193": {"label": 1, "data": {"text": "Crystal structures of protein phosphatase-1 bound to motuporin and dihydromicrocystin-LA: elucidation of the mechanism of enzyme inhibition by cyanobacterial toxins.", "entity1": "protein phosphatase-1", "entity2": "motuporin", "span1": [22, 43], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9424": {"label": 1, "data": {"text": "The hydrolysis of fluorescein diphosphate by PTP epsilon and PTPmeg1 was sensitive to alendronate, with IC50 values of less than 1 microM; PTPsigma, however, under the same conditions, was inhibited by only 50% with 141 microM alendronate.", "entity1": "PTP epsilon", "entity2": "alendronate", "span1": [45, 56], "span2": [86, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6445": {"label": 2, "data": {"text": "This study demonstrates that CB1093 and clenbuterol stimulate NGF levels in vitro and that AP-1 binding could be a commonality between the mechanism of NGF induction of these two compounds.", "entity1": "NGF", "entity2": "clenbuterol", "span1": [152, 155], "span2": [40, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8008": {"label": 3, "data": {"text": "In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-\u03b1-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.", "entity1": "t-PA", "entity2": "IMG", "span1": [181, 185], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5917": {"label": 3, "data": {"text": "Acetylation of phenelzine at the N2 position presumably interferes with the inhibition of the transaminase enzymes for gamma-aminobutyric acid and alanine.", "entity1": "transaminase", "entity2": "gamma-aminobutyric acid", "span1": [94, 106], "span2": [119, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3159": {"label": 0, "data": {"text": "Insulin receptor substrates (IRS) serine phosphorylation is a time-controlled physiological feedback mechanism in insulin signaling that is hijacked by metabolic and inflammatory stresses to promote insulin resistance.", "entity1": "Insulin receptor substrates", "entity2": "serine", "span1": [0, 27], "span2": [34, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8287": {"label": 4, "data": {"text": "We found that treatment of both differentiated dopaminergic-like SH-SY5Y cells and rat midbrain slices with the dopamine D2 receptor (D2R) agonist, quinpirole, triggered an increase in the expression of GDNF that was temporally preceded by an increase in the levels of zinc-finger protein 268 (Zif268), a DNA-binding transcription factor encoded by an immediate-early gene.", "entity1": "D2R", "entity2": "quinpirole", "span1": [134, 137], "span2": [148, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11075": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "calmodulin-dependent enzymes", "entity2": "p-chloro", "span1": [56, 84], "span2": [234, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15082": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "AmpC \u00df-lactamases", "entity2": "ceftazidime", "span1": [250, 267], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5015": {"label": 8, "data": {"text": "Of 9 CGPs with IC50's \u22642 \u03bcM, two belonged to Class I, two to Class III and five to Class V. When tested in the intact cells, only 4 of 16 CGPs (at 10 \u03bcM) inhibited MRP1-mediated calcein efflux by >50% (III-1, V-3, -4, -6) while a fifth (I-5) inhibited efflux by just 23%.", "entity1": "MRP1", "entity2": "calcein", "span1": [164, 168], "span2": [178, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15337": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "flavanone", "span1": [39, 48], "span2": [242, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1341": {"label": 4, "data": {"text": "Dexamethasone (DEX), betamethasone (BM), and their esterified-derivatives had full transrepression agonistic activity in a reporter assay using CV-1 cells transfected with either human or rat GR.", "entity1": "human or rat GR", "entity2": "BM", "span1": [179, 194], "span2": [36, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14381": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "Akt", "entity2": "AG1478", "span1": [168, 171], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15739": {"label": 3, "data": {"text": "Wattakaka volubilis steroidal glycoside mixture (WVSM) and PPG (1-50\u03bcM) significantly inhibited the COX-2 and iNOS enzymes resulting in low levels of PGE2 and NO in LPS-induced RAW 264.7 macrophage cells.", "entity1": "iNOS", "entity2": "steroidal glycoside", "span1": [110, 114], "span2": [20, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15203": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "buthanol", "span1": [340, 363], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12130": {"label": 1, "data": {"text": "A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy.", "entity1": "dopamine D2 receptor", "entity2": "quetiapine", "span1": [145, 165], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15398": {"label": 1, "data": {"text": "Here, we provide evidence that p14ARF physically interacts with AR and functions as an AR corespressor in both an androgen-dependent and androgen-independent manner.", "entity1": "AR", "entity2": "androgen", "span1": [87, 89], "span2": [114, 122]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8019": {"label": 3, "data": {"text": "Optimization of 5-hydroxytryptamines as dual function inhibitors targeting phospholipase A2 and leukotriene A4 hydrolase.", "entity1": "phospholipase A2", "entity2": "5-hydroxytryptamines", "span1": [75, 91], "span2": [16, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15525": {"label": 1, "data": {"text": "Our findings that NO/SNO target both Prx and Trx reductase may have implications for understanding the impact of nitrosylation on cellular redox homeostasis.", "entity1": "Prx", "entity2": "NO", "span1": [37, 40], "span2": [18, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1123": {"label": 3, "data": {"text": "Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action.", "entity1": "carbonic anhydrase", "entity2": "acetazolamide", "span1": [85, 103], "span2": [114, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11140": {"label": 1, "data": {"text": "However, because clozapine competes with endogenous dopamine, the in vivo concentration of clozapine (to occupy dopamine D4 receptors) can be derived to be about 13 nM, agreeing with the value of 12 to 20 nM in the plasma water or spinal fluid observed in treated patients.", "entity1": "dopamine D4 receptors", "entity2": "dopamine", "span1": [112, 133], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5558": {"label": 2, "data": {"text": "Experimental manipulation of the intracellular GSSG concentration during inhibition of cellular prooxidant production demonstrated that increased intracellular GSSG is a primary signal that is directly or indirectly required for CpG-induced NF-kappaB activation but is not in itself sufficient to trigger this in the absence of CpG ODN.", "entity1": "NF-kappaB", "entity2": "GSSG", "span1": [241, 250], "span2": [160, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"276": {"label": 1, "data": {"text": "Clonidine, an antihypertensive drug, binds to alpha 2-adrenergic and imidazoline receptors.", "entity1": "alpha 2-adrenergic and imidazoline receptors", "entity2": "Clonidine", "span1": [46, 90], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13535": {"label": 8, "data": {"text": "Mammalian cysteine dioxygenase (CDO) is a non-heme iron metalloenzyme that catalyzes the first committed step in oxidative cysteine catabolism.", "entity1": "Mammalian cysteine dioxygenase", "entity2": "cysteine", "span1": [0, 30], "span2": [123, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3021": {"label": 3, "data": {"text": "In the subsequent enzymatic assay, it was shown that lovastatin inhibited HDAC2 activity competitively with a K(i) value of 31.6 micromol/L.", "entity1": "HDAC2", "entity2": "lovastatin", "span1": [74, 79], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14891": {"label": 1, "data": {"text": "FMO3 expression is induced by dietary bile acids by a mechanism that involves the farnesoid X receptor (FXR), a bile acid-activated nuclear receptor.", "entity1": "farnesoid X receptor", "entity2": "bile acids", "span1": [82, 102], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14295": {"label": 3, "data": {"text": "In utero exposure to valproic acid (VPA), a histone deacetylase (HDAC) inhibitor, causes neural tube, heart, and limb defects.", "entity1": "HDAC", "entity2": "valproic acid", "span1": [65, 69], "span2": [21, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6172": {"label": 3, "data": {"text": "Selegiline (deprenyl), a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B) is widely used in the treatment of Parkinson's disease.", "entity1": "MAO-B", "entity2": "deprenyl", "span1": [88, 93], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13325": {"label": 3, "data": {"text": "Sulfasalazine (also as a representative of the salicylates) inhibited the diabetes-induced upregulation of several inflammatory gene products, which are regulated by NF-kappaB, including vascular cell adhesion molecule, intracellular adhesion molecule-1, inducible nitric oxide synthase, and cyclooxygenase-2 in whole-retinal lysate.", "entity1": "NF-kappaB", "entity2": "Sulfasalazine", "span1": [166, 175], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4445": {"label": 3, "data": {"text": "Among a series of 6-benzyloxyphthalides bearing substituents on the para position of the phenyl ring the general order of potency was CF(3) > I > Br > Cl > F > CH(3) > H. The results also show that the binding modes of representative phthalides are reversible and competitive at both MAO isoforms.", "entity1": "MAO", "entity2": "phthalides", "span1": [284, 287], "span2": [234, 244]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3625": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol", "span1": [14, 17], "span2": [280, 334]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5763": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "ubiquitin carboxy-terminal hydrolase L-1", "entity2": "MPTP", "span1": [244, 284], "span2": [185, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15727": {"label": 4, "data": {"text": "Most parabens showing estrogenic activity exhibited ER\u03b2-agonistic activity at lower concentrations than those inducing ER\u03b1-agonistic activity.", "entity1": "ER\u03b2", "entity2": "parabens", "span1": [52, 55], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11507": {"label": 1, "data": {"text": "BHMT is expressed at high levels in rat liver and its expression is regulated by dietary Met and choline.", "entity1": "BHMT", "entity2": "Met", "span1": [0, 4], "span2": [89, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4477": {"label": 1, "data": {"text": "In this study, we assessed the effects of clopidogrel and clarithromycin, known CYP2B6 and CYP3A inhibitors, respectively, on the enantioselective disposition of racemic sibutramine in conjunction with CYP2B6 polymorphisms in humans.", "entity1": "CYP2B6", "entity2": "racemic sibutramine", "span1": [202, 208], "span2": [162, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"862": {"label": 2, "data": {"text": "Addition of putrescine restored the induction of apoptosis as indicated by an increase in the number of detached cells and caspase 3 activity.", "entity1": "caspase 3", "entity2": "putrescine", "span1": [123, 132], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3148": {"label": 1, "data": {"text": "Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization.", "entity1": "TrkB", "entity2": "Amitriptyline", "span1": [85, 89], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4861": {"label": 0, "data": {"text": "Saturated palmitic and stearic acids increased ceramides, up-regulated PTP1B, and had AKt and PTP1B phosphorylation at Ser 50 impaired.", "entity1": "PTP1B", "entity2": "Ser", "span1": [94, 99], "span2": [119, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3062": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "chemokine", "entity2": "bicyclam", "span1": [101, 110], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14168": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "cyclooxygenase", "entity2": "chalcones", "span1": [67, 81], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15238": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B3", "entity2": "silybin B", "span1": [10, 17], "span2": [214, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"3581": {"label": 3, "data": {"text": "); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [50, 53], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14293": {"label": 3, "data": {"text": "VPA caused a significant concentration- dependent increase in limb abnormalities, which was correlated with its HDAC inhibitory effect.", "entity1": "HDAC", "entity2": "VPA", "span1": [112, 116], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"956": {"label": 4, "data": {"text": "The sympathetic nerves of both the human atrial appendages and rabbit pulmonary artery are endowed with alpha(2A)-autoreceptors, at which, however, both rilmenidine and oxymetazoline exhibit different properties (antagonism and agonism, respectively).", "entity1": "alpha(2A)-autoreceptors", "entity2": "oxymetazoline", "span1": [104, 127], "span2": [169, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10825": {"label": 3, "data": {"text": "Increased immunohistochemical labeling of HIF-1alpha, VEGF, and BNP in the ventricular myocardium was observed in the banding group and carvedilol again normalized the labeling.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [54, 58], "span2": [136, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3990": {"label": 3, "data": {"text": "Beta-glucogallin (BGG), a recently described AR inhibitor, was purified from extracts of the Indian gooseberry (Emblica officinalis).", "entity1": "AR", "entity2": "Beta-glucogallin", "span1": [45, 47], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4300": {"label": 8, "data": {"text": "Transport by OATP1B1 and OATP1B3 enhances the cytotoxicity of epigallocatechin 3-O-gallate and several quercetin derivatives.", "entity1": "OATP1B1", "entity2": "quercetin", "span1": [13, 20], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1994": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "EL3", "entity2": "Pro", "span1": [91, 94], "span2": [37, 40]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5948": {"label": 1, "data": {"text": "We conclude that pimozide and thioridazine may be useful in the control of estradiol- and polypeptide hormone-induced growth of ER-positive and ER-negative human breast tumors.", "entity1": "polypeptide hormone", "entity2": "thioridazine", "span1": [90, 109], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3791": {"label": 3, "data": {"text": "These results indicate that phillyrin prevents lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation, suggesting that phillyrin is a novel AMPK activator with a role in the prevention and treatment of obesity.", "entity1": "FAS", "entity2": "phillyrin", "span1": [124, 127], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8655": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRB", "entity2": "melatonin", "span1": [28, 31], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7397": {"label": 3, "data": {"text": "Consequently, PDE4 inhibitors including cilomilast and AWD 12-281 have been tested in several models of allergic and irritant skin inflammation.", "entity1": "PDE4", "entity2": "cilomilast", "span1": [14, 18], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7157": {"label": 1, "data": {"text": "Since previous studies have demonstrated that PPARgamma activators suppressed AT1R expression, we examined whether telmisartan affects AT1R expression in vascular smooth muscle cells.", "entity1": "AT1R", "entity2": "telmisartan", "span1": [135, 139], "span2": [115, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"595": {"label": 9, "data": {"text": "The action of 15d-PGJ2 does not appear to involve its nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) because troglitazone, a specific ligand of PPARgamma, was unable to inhibit iNOS induction, and neither troglitazone nor 15d-PGJ2 could stimulate the activity of a PPAR-dependent promoter in the absence of cotransfected PPARgamma.", "entity1": "PPAR", "entity2": "15d-PGJ2", "span1": [296, 300], "span2": [253, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11139": {"label": 1, "data": {"text": "However, because clozapine competes with endogenous dopamine, the in vivo concentration of clozapine (to occupy dopamine D4 receptors) can be derived to be about 13 nM, agreeing with the value of 12 to 20 nM in the plasma water or spinal fluid observed in treated patients.", "entity1": "dopamine D4 receptors", "entity2": "clozapine", "span1": [112, 133], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7175": {"label": 8, "data": {"text": "Upon differentiation, osteoclasts express vesicular glutamate transporter 1 (VGLUT1), which is essential for vesicular storage and subsequent exocytosis of glutamate in neurons.", "entity1": "VGLUT1", "entity2": "glutamate", "span1": [77, 83], "span2": [156, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5026": {"label": 8, "data": {"text": "ACTH-stimulated peak cortisol, delta cortisol, and delta DHEA-S levels are decreased during hyperthyroidism, probably due to increased turnover.", "entity1": "ACTH", "entity2": "delta cortisol", "span1": [0, 4], "span2": [31, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6059": {"label": 3, "data": {"text": "In NE-desensitized cells, phorbol esters and bradykinin each caused the expected down-regulation of alpha-AR mRNA.", "entity1": "alpha-AR", "entity2": "NE", "span1": [100, 108], "span2": [3, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9843": {"label": 1, "data": {"text": "gamma-Butyrobetaine hydroxylase catalyse the last step in carnitine biosynthesis, the formation of L-carnitine from gamma-butyrobetaine, a reaction dependent on Fe2+, alpha-ketoglutarate, ascorbate and oxygen.", "entity1": "gamma-Butyrobetaine hydroxylase", "entity2": "ascorbate", "span1": [0, 31], "span2": [188, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15826": {"label": 8, "data": {"text": "In terms of the mechanisms, we found that fatty acid amide hydrolase (FAAH) which degrades anandamide, was upregulated after nerve injury at both ages, so that this upregulation likely did not account for the age-dependent differences.", "entity1": "FAAH", "entity2": "anandamide", "span1": [70, 74], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5552": {"label": 2, "data": {"text": "Accumulation of glutathione disulfide mediates NF-kappaB activation during immune stimulation with CpG DNA.", "entity1": "NF-kappaB", "entity2": "glutathione disulfide", "span1": [47, 56], "span2": [16, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9519": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "ligand-activated gene transcription factors", "entity2": "retinoid", "span1": [53, 96], "span2": [4, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9623": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBF2", "entity2": "MgADP", "span1": [232, 236], "span2": [217, 222]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15803": {"label": 2, "data": {"text": "When dual angiogenic growth factors (GFs), such as platelet-derived GF (PDGF) and vascular endothelial GF (VEGF), are encapsulated separately in the core and shell domains, respectively, the VEGF release rate is much greater than that of PDGF, and the difference of the cumulative release percentage between the two GFs is about 30% on day 7 with LMW core PLGA and more than 45% with HMW core PLGA.", "entity1": "VEGF", "entity2": "PLGA", "span1": [191, 195], "span2": [356, 360]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3912": {"label": 1, "data": {"text": "To clarify the cause of age differences on selenite cataract formation in rats, mRNA expression of GPx1, MsrA and MsrB1, as well as GPx activity in Wistar rat lens at different ages were assayed, level of lipid peroxidation, extent of lens damage induced by sodium selenite and barricade function of blood-retinal barrier (BRB) were investigated.", "entity1": "MsrB1", "entity2": "sodium selenite", "span1": [114, 119], "span2": [258, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7951": {"label": 2, "data": {"text": "A reporter construct driven by 4 kb of the chicken ras-dva 5'-flanking region, containing six putative pituitary-specific transcription factor-1 (Pit-1) binding sites and two potential glucocorticoid receptor (GR) binding sites, was highly activated in embryonic pituitary cells and up-regulated by corticosterone.", "entity1": "pituitary-specific transcription factor-1 (Pit-1) binding sites", "entity2": "corticosterone", "span1": [103, 166], "span2": [299, 313]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9980": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "3-hydroxybenzylhydrazine", "span1": [80, 84], "span2": [175, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11050": {"label": 3, "data": {"text": "For some, pharmacologic inhibitors are available, including sorafenib for BRAF, farnesyltransferase inhibitors for NRAS, PD-0325901 for mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, rapamycin analogues for mammalian target of rapamycin, and agents that inhibit either vascular endothelial growth factor or its receptors.", "entity1": "mitogen-activated protein kinase", "entity2": "PD-0325901", "span1": [136, 168], "span2": [121, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1609": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE3", "entity2": "DMA", "span1": [127, 131], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9047": {"label": 1, "data": {"text": "The apparent affinity of benzodiazepine receptors for clonazepam in mice receiving alprazolam (0.05 mg/kg) was unchanged from that in untreated control mice, an observation suggesting that low doses of alprazolam increased receptor number.", "entity1": "benzodiazepine receptors", "entity2": "alprazolam", "span1": [25, 49], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6446": {"label": 2, "data": {"text": "The present studies were undertaken to compare two compounds, a vitamin D(3) analogue (CB1093) with minimal calcaemic effects, and clenbuterol, a long-acting beta(2)-adrenoceptor agonist, both of which induce NGF synthesis in vivo.", "entity1": "NGF", "entity2": "CB1093", "span1": [209, 212], "span2": [87, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3983": {"label": 0, "data": {"text": "Bioinformatic analyses of several vertebrate genomes were undertaken using known ALDH2 and ALDH1B1 amino acid sequences.", "entity1": "ALDH2", "entity2": "amino acid", "span1": [81, 86], "span2": [99, 109]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14976": {"label": 2, "data": {"text": "The activation of Rac1 was induced by silica nanoparticles as well as BCG DNA and is suggested as the critical signaling event inducing both cytoskeleton changes as well as inflammatory cell activation.", "entity1": "Rac1", "entity2": "silica", "span1": [18, 22], "span2": [38, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7261": {"label": 3, "data": {"text": "The metallic taste reported as a side effect after the treatment with systemic sulfonamides may be due to the inhibition of the salivary CA VI.", "entity1": "salivary CA VI", "entity2": "sulfonamides", "span1": [128, 142], "span2": [79, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7701": {"label": 2, "data": {"text": "atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans.", "entity1": "AChE", "entity2": "obidoxime", "span1": [10, 14], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8152": {"label": 3, "data": {"text": "DPEP induced dose-dependent reduction of the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and concomitant reduction in the production of NO and prostaglandin E(2) (PGE(2)).", "entity1": "cyclooxygenase-2", "entity2": "DPEP", "span1": [106, 122], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9456": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "11-deoxy-PGE1", "span1": [4, 7], "span2": [98, 111]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8657": {"label": 9, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "p53", "entity2": "imatinib", "span1": [113, 116], "span2": [6, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"973": {"label": 3, "data": {"text": "Expression of the dominant negative mutants rab5A-N133I or rab7-N125I blunted U50,488H-induced down-regulation.", "entity1": "N125I", "entity2": "U50,488H", "span1": [64, 69], "span2": [78, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8484": {"label": 1, "data": {"text": "Toxicological profiles of selected synthetic cannabinoids showing high binding affinities to the cannabinoid receptor subtype CB1.", "entity1": "cannabinoid receptor subtype CB1", "entity2": "cannabinoids", "span1": [97, 129], "span2": [45, 57]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14210": {"label": 3, "data": {"text": "Galantamine is a reversible, competitive acetylcholinesterase (AChE) inhibitor and allosteric potentiating ligand of nicotinic acetylcholine receptors (nAChR-APL) that shares many common structural elements with morphinan-based opioids.", "entity1": "AChE", "entity2": "Galantamine", "span1": [63, 67], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"3673": {"label": 3, "data": {"text": "Moreover, attempts to elucidate a possible mechanism underlying the artemisinic acid-mediated effects revealed that artemisinic acid regulated melanogenesis by inhibiting cholesterol synthesis through downregulation of the hydroxymethylglutaryl CoA (HMG CoA) reductase gene, which was mediated through reduced expression of the CCAAT/enhancer-binding protein (C/EBP) \u03b1 gene.", "entity1": "CCAAT/enhancer-binding protein (C/EBP) \u03b1", "entity2": "artemisinic acid", "span1": [328, 368], "span2": [116, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14705": {"label": 3, "data": {"text": "Inhibition of Th1/Th17 responses via suppression of STAT1 and STAT3 activation contributes to the amelioration of murine experimental colitis by a natural flavonoid glucoside icariin.", "entity1": "STAT3", "entity2": "icariin", "span1": [62, 67], "span2": [175, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4390": {"label": 2, "data": {"text": "Altogether, our findings support a model in which Top2\u03b2 deficiency promotes CPT-induced apoptosis in quiescent non-S-phase cells, possibly due to RNAP LS depletion and p53 accumulation.", "entity1": "p53", "entity2": "CPT", "span1": [168, 171], "span2": [76, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8692": {"label": 8, "data": {"text": "Among the possible transporters involved in the uptake of Cd(2+) and Mn(2+), the expression of ZIP8 (Zrt-, Irt-related protein 8), encoded by Slc39a8, showed a marked suppression in both RBL-Cdr and RBL-Mnr cells.", "entity1": "Slc39a8", "entity2": "Cd(2+)", "span1": [142, 149], "span2": [58, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1414": {"label": 1, "data": {"text": "Lisuride produced a significant dose-related increase in flat body posture, forepaw treading, and lower-lip retraction which reflect a modulation of behavior by action at central 5-HT(1A) receptors.", "entity1": "5-HT(1A)", "entity2": "Lisuride", "span1": [179, 187], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7840": {"label": 2, "data": {"text": "We observed that ribavirin enhanced ELL3 recruitment to F7, whereas knockdown of ELL3 diminished ribavirin-induced FVII mRNA up-regulation.", "entity1": "ELL3", "entity2": "ribavirin", "span1": [36, 40], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10675": {"label": 3, "data": {"text": "In conclusion, TT-235 may inhibit the uterine response to oxytocin by decreasing oxytocin receptor numbers and oxytocin binding affinity, which might explain the prolonged oxytocin antagonist activity of TT-235.", "entity1": "oxytocin receptor", "entity2": "TT-235", "span1": [81, 98], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"148": {"label": 3, "data": {"text": "In all patients loperamide induced a significant fall in plasma ACTH levels.", "entity1": "ACTH", "entity2": "loperamide", "span1": [64, 68], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13593": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester", "span1": [6, 10], "span2": [296, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5371": {"label": 3, "data": {"text": "Suppression of T\u03b2R1 by the pharmacological inhibitor (SB431542) markedly reduced VEGF release by HFL-1 in response to CSE and this effect was confirmed by T\u03b2R1 siRNA.", "entity1": "T\u03b2R1", "entity2": "SB431542", "span1": [15, 19], "span2": [54, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1823": {"label": 3, "data": {"text": "Kinetic mechanism of quinone oxidoreductase 2 and its inhibition by the antimalarial quinolines.", "entity1": "quinone oxidoreductase 2", "entity2": "quinolines", "span1": [21, 45], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4379": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "cytochrome P450 3A", "entity2": "midazolam", "span1": [151, 169], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1010": {"label": 0, "data": {"text": "Insulin-like growth factor (IGF)-binding protein (IGFBP)-related proteins (IGFBP-rPs) are newly described cysteine-rich proteins that share significant aminoterminal structural similarity with the conventional IGFBPs and are involved in a diversity of biological functions, including growth regulation.", "entity1": "IGFBP-rPs", "entity2": "cysteine", "span1": [75, 84], "span2": [106, 114]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5549": {"label": 2, "data": {"text": "This study investigates the involvement of alpha(2)-adrenergic receptors (AR) in mouse brain induced by a low dose of methamphetamine (METH, 2 mg/kg).", "entity1": "alpha(2)-adrenergic receptors", "entity2": "METH", "span1": [43, 72], "span2": [135, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6369": {"label": 4, "data": {"text": "The nonselective opioid receptor partial agonist buprenorphine and the nonselective opioid receptor antagonist (-)-quadazocine exhibited pure antagonism at rat brain receptors, but displayed partial agonism at human ORL1 receptors.", "entity1": "opioid receptor", "entity2": "buprenorphine", "span1": [17, 32], "span2": [49, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14335": {"label": 3, "data": {"text": "Finally, DMF suppressed unilateral ureteral obstruction (UUO)-induced renal fibrosis and alpha-SMA, fibronectin and type 1 collagen expression in the obstructed kidneys from UUO mice, along with increased and decreased expression of Nrf2 and phospho-Smad3, respectively.", "entity1": "alpha-SMA", "entity2": "DMF", "span1": [89, 98], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2941": {"label": 1, "data": {"text": "The structure shows that the conformation of the H-loop in the PDE5A1-vardenafil complex is different from those of any known structures of the unliganded PDE5 and its complexes with the inhibitors.", "entity1": "PDE5A1", "entity2": "vardenafil", "span1": [63, 69], "span2": [70, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1725": {"label": 3, "data": {"text": "Ginseng total saponins, ginsenosides Rb2, Rg1 and Rd administered intraperitoneally attenuated the immobilization stress-induced increase in plasma IL-6 level.", "entity1": "IL-6", "entity2": "ginsenosides Rb2, Rg1 and Rd", "span1": [148, 152], "span2": [24, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4496": {"label": 9, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES2", "entity2": "(S)-naproxen-\u03b2-d-glucuronide", "span1": [300, 305], "span2": [118, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6769": {"label": 2, "data": {"text": "Novel mechanism of action for hydralazine: induction of hypoxia-inducible factor-1alpha, vascular endothelial growth factor, and angiogenesis by inhibition of prolyl hydroxylases.", "entity1": "hypoxia-inducible factor-1alpha", "entity2": "hydralazine", "span1": [56, 87], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15902": {"label": 1, "data": {"text": "The results were congruent and highly significant: Ca(2+) /H(+) -antiport activity is detectable only in acidic organelles expressing functional synaptotagmin-1.", "entity1": "synaptotagmin-1", "entity2": "Ca(2+)", "span1": [145, 160], "span2": [51, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8372": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "IR", "entity2": "BPA", "span1": [64, 66], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9651": {"label": 3, "data": {"text": "In order to address one aspect of the feasibility of performing time-resolved studies on AChE, a data set has been collected using the Laue technique on a trigonal crystal of Torpedo californica AChE soaked with the reversible inhibitor edrophonium, using a total X-ray exposure time of 24 ms. Electron-density maps obtained from the Laue data, which are of surprisingly good quality compared with similar maps from monochromatic data, show essentially the same features.", "entity1": "Torpedo californica AChE", "entity2": "edrophonium", "span1": [175, 199], "span2": [237, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5155": {"label": 2, "data": {"text": "Moreover, treatment of U937 cells with 2-hydroxy-3-methylanthraquinone resulted in activation of caspase-3.", "entity1": "caspase-3", "entity2": "2-hydroxy-3-methylanthraquinone", "span1": [97, 106], "span2": [39, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10573": {"label": 2, "data": {"text": "Imiquimod (IMQ), an activator of Toll-like receptor-7 (TLR-7), induces by several routes a profound anti-viral and anti-tumor effect in vivo.", "entity1": "Toll-like receptor-7", "entity2": "Imiquimod", "span1": [33, 53], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8092": {"label": 0, "data": {"text": "We aim to \"tilt\" the stability of the H1 loop structure from a noncanonical conformation to a (humanized) type 1 canonical conformation by studying the effect of selected mutations to the amino acid sequence of the H1, H2, and proximal residues.", "entity1": "H2", "entity2": "amino acid", "span1": [219, 221], "span2": [188, 198]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6854": {"label": 1, "data": {"text": "However, MS A2756G was significantly associated with cobalamin levels (AA genotype: 290 +/- 122 pmol/l; AG: 381 +/- 151 pmol/l and GG: 415 +/- 100 pmol/l), as was MTRR A66G (AA: 478 +/- 219 pmol/l, AG: 306 +/- 124 pmol/l and GG: 306 +/- 123 pmol/l).", "entity1": "MTRR", "entity2": "cobalamin", "span1": [163, 167], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2735": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "kinase", "entity2": "Dasatinib", "span1": [62, 68], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2680": {"label": 9, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "V654A", "entity2": "IM", "span1": [57, 62], "span2": [93, 95]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12168": {"label": 1, "data": {"text": "After 3 weeks' bupropion treatment we studied the change in DAT activity, which corresponds to the occupancy of bupropion.", "entity1": "DAT", "entity2": "bupropion", "span1": [60, 63], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4153": {"label": 1, "data": {"text": "To this end, we built pharmacokinetic and pharmacodynamic models that describe the relationship of the concentrations of TAK-441 plasma to the responses of Gli1 mRNA in the tumor (target) and skin (surrogate) and to tumor growth inhibition in mice bearing xenografts of human pancreatic tumors (PAN-04).", "entity1": "Gli1", "entity2": "TAK-441", "span1": [156, 160], "span2": [121, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2794": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "substance P", "entity2": "caerulein", "span1": [13, 24], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2601": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "D(1) receptors", "entity2": "risperidone", "span1": [285, 299], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15913": {"label": 4, "data": {"text": "To examine receptor mediation of estradiol effects, Ovx mice replaced for 2 days with either the ER\u03b1-selective agonist PPT or the ER\u03b2-selective agonist DPN were compared to Sham mice, and mice lacking either ER\u03b1 (\u03b1ERKO) or ER\u03b2 (\u03b2ERKO) were compared to WT littermates.", "entity1": "ER\u03b1", "entity2": "PPT", "span1": [97, 100], "span2": [119, 122]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9290": {"label": 5, "data": {"text": "ICI118,551 HCl (1.25-5 mg/kg, IP), a selective beta 2-adrenoceptor antagonist, also blocked the desipramine-induced enhancement of aggressive behavior in a dose-dependent manner, whereas metoprolol tartrate (5-20 mg/kg, IP), a selective beta 1-adrenoceptor antagonist, did not affect it.", "entity1": "beta 2-adrenoceptor", "entity2": "ICI118,551 HCl", "span1": [47, 66], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11758": {"label": 1, "data": {"text": "MDMA catechol metabolites were neurotoxic to SH-SY5Y neurons, leading to caspase 3-independent cell death in a concentration- and time-dependent manner.", "entity1": "caspase 3", "entity2": "MDMA", "span1": [73, 82], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5991": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "human [Glu1]plasminogen", "entity2": "EACA", "span1": [18, 41], "span2": [226, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12803": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "PDGFRA", "entity2": "Gleevec", "span1": [109, 115], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14340": {"label": 3, "data": {"text": "In summary, DMF attenuated renal fibrosis via the Nrf2-mediated inhibition of TGF-beta/Smad3 signaling in an ARE-independent manner, suggesting that DMF could be used to treat renal fibrosis.", "entity1": "Smad3", "entity2": "DMF", "span1": [87, 92], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"817": {"label": 1, "data": {"text": "It was concluded that PGE1 selectively reduces both N- and R-type Ca2+ currents by activating a G-protein probably through the EP3 receptor in paratracheal ganglion cells.", "entity1": "EP3 receptor", "entity2": "PGE1", "span1": [127, 139], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5270": {"label": 2, "data": {"text": "In fact, we demonstrated a significant stimulation of Nox4 activity by 4 quinone derivatives (AA-861, tBuBHQ, tBuBQ, and duroquinone) observed in 3 different cellular models, HEK293E, T-REx\u2122, and chondrocyte cell lines.", "entity1": "Nox4", "entity2": "AA-861", "span1": [54, 58], "span2": [94, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8766": {"label": 5, "data": {"text": "SB225002 (SB) is an IL-8 receptor B (IL-8RB) antagonist that has previously been shown to inhibit IL-8-based cancer cell invasion, and to possess in vivo anti-inflammatory and anti-nociceptive effects.", "entity1": "IL-8 receptor B", "entity2": "SB225002", "span1": [20, 35], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6214": {"label": 1, "data": {"text": "This study therefore characterized the binding of DF to the sigma receptors and NMDA-linked PCP sites and examined the anticonvulsant as well as locomotor effects of DF in mice in comparison with those of DM and DR. We found that DF, DM, and DR were relative high-affinity ligands at sigma-1 receptors (Ki=151, 205, 144 nM, respectively) while all of them were with low affinity at sigma-2 receptors (Ki=4-11 microM).", "entity1": "sigma-1 receptors", "entity2": "DR", "span1": [284, 301], "span2": [242, 244]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9228": {"label": 5, "data": {"text": "The binding of FHA-HIS was inhibited on 35-79% of the platelets by the histamine H1 receptor antagonists diphenhydramine and clemastine.", "entity1": "histamine H1 receptor", "entity2": "diphenhydramine", "span1": [71, 92], "span2": [105, 120]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"377": {"label": 3, "data": {"text": "In conclusion, the production of IL-4 and IL-5 by T-cell clones (derived either from BAL or blood) was more sensitive to inhibition by DEX than that of IFN-gamma, which may account for the therapeutic effects of glucocorticosteroids in patients with asthma.", "entity1": "IFN-gamma", "entity2": "DEX", "span1": [152, 161], "span2": [135, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6629": {"label": 9, "data": {"text": "Similarly, pranlukast did not modulate IL-5- or FMLP-activated eosinophil adhesion to the resting endothelial cells.", "entity1": "IL-5", "entity2": "pranlukast", "span1": [39, 43], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16069": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "B-cell antigen receptor", "entity2": "Imbruvica(R)", "span1": [142, 165], "span2": [11, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6957": {"label": 1, "data": {"text": "Maraviroc inhibited binding of [125I]-MIP-1beta to CCR5 from macaque and human with similar potency (IC50 = 17.50 +/- 1.24 nM and 7.18 +/- 0.93 nM, respectively) and antagonised MIP-1beta induced intracellular calcium release mediated through CCR5 from macaque and human with similar potency (IC50 = 17.50 +/- 3.30 nM and 12.07 +/- 1.89, respectively).", "entity1": "CCR5", "entity2": "Maraviroc", "span1": [51, 55], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11232": {"label": 1, "data": {"text": "The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide.", "entity1": "insulin", "entity2": "KAD-1229", "span1": [98, 105], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4214": {"label": 1, "data": {"text": "Time-lapsed confocal microscopy indicates that Mn can promote trafficking of cell surface DAT into intracellular compartments which may account for the decrease in DA uptake and DA efflux in these cells.", "entity1": "DAT", "entity2": "Mn", "span1": [90, 93], "span2": [47, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15246": {"label": 8, "data": {"text": "In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17\u03b2-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated.", "entity1": "OATP1B3", "entity2": "estradiol-17\u03b2-glucuronide", "span1": [43, 50], "span2": [60, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7090": {"label": 5, "data": {"text": "These currents were produced by glutamate-aspartate transporters (GLAST) (excitatory amino acid transporter 1) because they were weakly inhibited by dihydrokainate, an antagonist of glutamate transporter-1 (excitatory amino acid transporter 2) and were absent from IPCs in GLAST-/- cochleas.", "entity1": "glutamate transporter-1", "entity2": "dihydrokainate", "span1": [182, 205], "span2": [149, 163]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"3451": {"label": 1, "data": {"text": "R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less.", "entity1": "DAT", "entity2": "R-modafinil", "span1": [49, 52], "span2": [0, 11]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9457": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "16,16-dimethyl-PGE2", "span1": [4, 7], "span2": [113, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10392": {"label": 3, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "BuChE", "entity2": "rivastigmine", "span1": [242, 247], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15124": {"label": 3, "data": {"text": "Mn exposure (20\u00a0mg/kg) increased p38(MAPK) and Akt phosphorylation, but decreased DARPP-32-Thr-34 phosphorylation.", "entity1": "DARPP-32", "entity2": "Mn", "span1": [82, 90], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15177": {"label": 3, "data": {"text": "GnRH stimulation of CREB phosphorylation (pCREB) in the gonadotrope-derived L\u03b2T2 cell line was attenuated by a protein kinase A (PKA) inhibitor, H89.", "entity1": "protein kinase A", "entity2": "H89", "span1": [111, 127], "span2": [145, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6278": {"label": 3, "data": {"text": "Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects.", "entity1": "cyclooxygenase-1", "entity2": "meloxicam", "span1": [38, 54], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4750": {"label": 3, "data": {"text": "A combination of in vitro metabolism experiments and a pharmacokinetic study in monkeys with the inhibitor 4-methylpyrazole provided strong evidence that alcohol dehydrogenase, potentially in association with aldehyde dehydrogenase, is the primary enzyme involved in the formation of the M3 metabolite.", "entity1": "alcohol dehydrogenase", "entity2": "4-methylpyrazole", "span1": [154, 175], "span2": [107, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4355": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "c-Myc", "entity2": "pinosylvin", "span1": [292, 297], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12633": {"label": 3, "data": {"text": "We conclude that cisapride is a potent blocker of HERG channels expressed in HEK293 cells.", "entity1": "HERG", "entity2": "cisapride", "span1": [50, 54], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6306": {"label": 5, "data": {"text": "These responses were effectively blocked by the 5-HT1B receptor antagonist, isamoltane, the 5-HT1B/5-HT2 receptor antagonist, methiothepin, and the eNOS selective antagonists (0.01-10 microM): L-Nomega -monomethyl-L-arginine (L-NMMA) and L-N omega-iminoethyl-L-ornithine (L-NIO).", "entity1": "eNOS", "entity2": "L-N omega-iminoethyl-L-ornithine", "span1": [148, 152], "span2": [238, 270]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10388": {"label": 3, "data": {"text": "The development of specific BuChE inhibitors and further experience with the dual enzyme inhibitor rivastigmine will improve understanding of the aetiology of AD and should lead to a wider variety of potent treatment options.", "entity1": "BuChE", "entity2": "rivastigmine", "span1": [28, 33], "span2": [99, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4993": {"label": 2, "data": {"text": "Phenobarbital (PB), a typical CAR activator, increased the gene expression of HIF-target genes in the livers of mice, including erythropoietin, heme oxygenase-1 and vascular endothelial growth factor-a.", "entity1": "CAR", "entity2": "Phenobarbital", "span1": [30, 33], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2401": {"label": 3, "data": {"text": "Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.", "entity1": "albumin", "entity2": "anthranilic acid sulfonamides", "span1": [146, 153], "span2": [30, 59]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5686": {"label": 2, "data": {"text": "Sprague-Dawley rats treated with a non-selective cannabinoid agonist (CP55940, 50\u03bcg/kg, 7 days, i.p.) showed enhanced co-immunoprecipitation of \u03b2-Arrestin 2 and ERK1/2, enhanced pERK protein levels, and enhanced expression of \u03b2-Arrestin 2 mRNA and protein levels in PFCx.", "entity1": "ERK1/2", "entity2": "CP55940", "span1": [161, 167], "span2": [70, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5998": {"label": 3, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "tissue plasminogen activator", "entity2": "Cl-", "span1": [91, 119], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13238": {"label": 3, "data": {"text": "Our results suggest that glutamate induces GRIP1 degradation by proteasome through an NMDA receptor-Ca2+ pathway and that GRIP1 degradation may play an important role in regulating GluR2 surface expression.", "entity1": "GRIP1", "entity2": "glutamate", "span1": [43, 48], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9350": {"label": 5, "data": {"text": "Tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist.", "entity1": "alpha 1A-adrenoceptor", "entity2": "Tamsulosin", "span1": [41, 62], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13234": {"label": 2, "data": {"text": "The GRIP1 reduction was inhibited by MK-801, an N-methyl-d-aspartate (NMDA) receptor antagonist, but not by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an AMPA receptor antagonist.", "entity1": "GRIP1", "entity2": "MK-801", "span1": [4, 9], "span2": [37, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1837": {"label": 3, "data": {"text": "The reciprocal inhibition of SR-BI and ABCA1 by BLT-4 and glyburide raises the possibility that these proteins may share similar or common steps in their mechanisms of lipid transport.", "entity1": "ABCA1", "entity2": "glyburide", "span1": [39, 44], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11290": {"label": 8, "data": {"text": "Firstly, transgenic plants overexpressing formate dehydrogenase (FDH, EC 1.2.1.2) were used to continue our previous studies on the function of FDH in formate metabolism.", "entity1": "EC 1.2.1.2", "entity2": "formate", "span1": [70, 80], "span2": [151, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5424": {"label": 2, "data": {"text": "Additionally, MPTP significantly down-regulated Bcl-2 expression in the mitochondria of dopaminergic cells in the SN, followed by an increase in Bax expression, cytochrome C translocation to the cytosol, andcleaved-caspase-3 expression, whereas these were inhibited by CRE or EB treatment.", "entity1": "Bax", "entity2": "MPTP", "span1": [145, 148], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2527": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "aromatic amine", "span1": [311, 317], "span2": [66, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5463": {"label": 4, "data": {"text": "In the hippocampus, brexpiprazole acted as a full agonist at 5-HT1A receptors on pyramidal neurons.", "entity1": "5-HT1A", "entity2": "brexpiprazole", "span1": [61, 67], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10338": {"label": 2, "data": {"text": "The results show that transient arsenite pre-treatment induces Hsp72, HO-1 and, to a lesser extent, Hsp27; it reduces H2O2-induced astrocyte death; and it causes selective activation of Akt following H2O2.", "entity1": "Akt", "entity2": "H2O2", "span1": [186, 189], "span2": [200, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12329": {"label": 0, "data": {"text": "Using site-directed mutagenesis, we identified three serines (Ser833, Ser836, and Ser840) within the membrane proximal region of the GluK5 C-terminal domain that, in combination, are required for mGlu1-mediated potentiation of KARs.", "entity1": "GluK5", "entity2": "C", "span1": [133, 138], "span2": [139, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7308": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT2", "entity2": "alanine", "span1": [235, 240], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"709": {"label": 8, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "AChE", "entity2": "acetylcholine", "span1": [130, 134], "span2": [193, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2983": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Q817A", "entity2": "cGMP", "span1": [216, 221], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12607": {"label": 1, "data": {"text": "It appears likely that the histamine H2 receptor blocked by cimetidine obviated the pulmonary vasodilator effect of tolazoline therapy.", "entity1": "histamine H2 receptor", "entity2": "tolazoline", "span1": [27, 48], "span2": [116, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13725": {"label": 2, "data": {"text": "RTX treatment also induced foci of RAD51, gamma-H2AX, phospho-Chk1, and phospho-NBS1, although the extent of co-localization with RPA2 foci varied.", "entity1": "phospho-Chk1", "entity2": "RTX", "span1": [54, 66], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7331": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SLC1", "entity2": "glutamine", "span1": [190, 194], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"933": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "5-fluoro-2'-deoxyuridine", "span1": [238, 240], "span2": [23, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8752": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "amitriptyline", "span1": [225, 231], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14948": {"label": 1, "data": {"text": "There has been much recent interest in lysophosphatidic acid (LPA) signaling through one of its receptors, LPA1, in fibrotic diseases, but the mechanisms by which LPA-LPA1 signaling promotes pathological fibrosis remain to be fully elucidated.", "entity1": "LPA1", "entity2": "lysophosphatidic acid", "span1": [107, 111], "span2": [39, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11851": {"label": 3, "data": {"text": "Apple polyphenols suppress antigen presentation of ovalbumin by THP-1-derived dendritic cells.", "entity1": "ovalbumin", "entity2": "polyphenols", "span1": [51, 60], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9662": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "rhIL-5", "entity2": "FP", "span1": [165, 171], "span2": [101, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15504": {"label": 4, "data": {"text": "Interestingly, following pBQN desensitization, wild-type TRPA1 had dramatically reduced response to the nonelectrophile agonist carvacrol, whereas the triple cysteine mutant TRPA1 retained its full response.", "entity1": "TRPA1", "entity2": "carvacrol", "span1": [57, 62], "span2": [128, 137]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9163": {"label": 3, "data": {"text": "Inactivation of prostaglandin H synthase and prostacyclin synthase by phenylbutazone.", "entity1": "prostaglandin H synthase", "entity2": "phenylbutazone", "span1": [16, 40], "span2": [70, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8399": {"label": 3, "data": {"text": "The solubility-driven structural modification of (pyridin-3-yl) benzoxazinyl-oxazolidinones is described, which resulted in the development of a new series of benzoxazinyl-oxazolidinone analogues with high antibacterial activity against Gram-positive pathogens, including that against linezolid-resistant strains and low hERG inhibition.", "entity1": "hERG", "entity2": "benzoxazinyl-oxazolidinone", "span1": [321, 325], "span2": [159, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4307": {"label": 1, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "PARP-1", "entity2": "AuF", "span1": [161, 167], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5501": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D2 receptor", "entity2": "raclopride", "span1": [304, 324], "span2": [336, 346]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"184": {"label": 5, "data": {"text": "The efficacy of astemizole, a new, long acting, oral histamine H1-receptor antagonist was compared to placebo for the treatment of allergic rhinitis and conjunctivitis during the grass pollen season of 1982.", "entity1": "histamine H1-receptor", "entity2": "astemizole", "span1": [53, 74], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5326": {"label": 1, "data": {"text": "Pasireotide (Signifor(\u00ae)) is a new subcutaneous somatostatin analogue that acts via somatostatin receptors to inhibit the secretion of corticotropin from the pituitary adenoma in patients with Cushing's disease.", "entity1": "somatostatin receptors", "entity2": "Signifor", "span1": [84, 106], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6211": {"label": 1, "data": {"text": "This study therefore characterized the binding of DF to the sigma receptors and NMDA-linked PCP sites and examined the anticonvulsant as well as locomotor effects of DF in mice in comparison with those of DM and DR. We found that DF, DM, and DR were relative high-affinity ligands at sigma-1 receptors (Ki=151, 205, 144 nM, respectively) while all of them were with low affinity at sigma-2 receptors (Ki=4-11 microM).", "entity1": "sigma-2 receptors", "entity2": "DM", "span1": [382, 399], "span2": [234, 236]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4173": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "tert-butylhydroquinone", "span1": [151, 155], "span2": [180, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8789": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "NF-\u03baB", "entity2": "CAPE", "span1": [180, 185], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3842": {"label": 1, "data": {"text": "These studies suggest a majority of arsenic-inhibited adipocyte differentiation, and metabolism requires endothelin-1 GPCRs and that As(III) effects on GPCR signaling are tissue and context specific.", "entity1": "GPCR", "entity2": "As(III)", "span1": [152, 156], "span2": [133, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4585": {"label": 0, "data": {"text": "Cellular protein labeling occurs only upon activation of two different promoters that drive expression of the N- and C-terminal fragments of the bisected MetRS.", "entity1": "MetRS", "entity2": "N", "span1": [154, 159], "span2": [110, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8591": {"label": 3, "data": {"text": "Western blot assay demonstrated that DICO decreased Bcl-2 level and induced Bax translocation to cause cytochrome c release.", "entity1": "Bcl-2", "entity2": "DICO", "span1": [52, 57], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5322": {"label": 3, "data": {"text": "The structure-activity relationships revealed that the free hydroxyl group at position 5 and phosphate group at position 7 of the phosphorylated flavonoids are favorable to the inhibition of CEase.", "entity1": "CEase", "entity2": "phosphate", "span1": [191, 196], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5994": {"label": 3, "data": {"text": "The presence of Cl- inhibits the stimulation of [Glu1]Pg activation that would normally occur in the presence of fibrinogen, a result of possible importance to the observation that some degree of systemic fibrinogenolysis accompanies therapeutic use of tissue plasminogen activator.", "entity1": "[Glu1]Pg", "entity2": "Cl-", "span1": [48, 56], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12683": {"label": 1, "data": {"text": "Different forms of therapy, potassium and magnesium substitution, spironolactone and indomethacin failed to fully correct hypokalemia and hypomagnesemia, but markedly improved growth velocity and normalized IGF-I levels in the three patients with short stature.", "entity1": "IGF-I", "entity2": "magnesium", "span1": [207, 212], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11985": {"label": 8, "data": {"text": "6-DHSG was metabolised by GSH to form a GSH conjugate (GS-6-DHSG) in RAW 264.7 cells, via a potential mechanism involving the catalytic activity of glutathione-S-transferase (GST).", "entity1": "GST", "entity2": "GS-6-DHSG", "span1": [175, 178], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10192": {"label": 3, "data": {"text": "In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2.", "entity1": "organic anion transporting polypeptides", "entity2": "rifamycin SV", "span1": [116, 155], "span2": [9, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1244": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "fluticasone", "span1": [115, 118], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13014": {"label": 7, "data": {"text": "It has the advantage over the traditional Ca2+ assay of allowing the measurement of inverse agonist activity as well as the analysis of PLC-beta activity in any nontransfected primary cultures.", "entity1": "PLC-beta", "entity2": "Ca2+", "span1": [136, 144], "span2": [42, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3563": {"label": 0, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u.", "entity1": "IR", "entity2": "tyrosine", "span1": [24, 26], "span2": [27, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12928": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CBS", "entity2": "L-cysteine", "span1": [160, 163], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6365": {"label": 4, "data": {"text": "Lofentanil exhibited full agonism for enhancement of [35S]GTPgammaS binding to human recombinant ORL1 receptors (EC(50) 50 nM).", "entity1": "ORL1", "entity2": "Lofentanil", "span1": [97, 101], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13005": {"label": 1, "data": {"text": "D-myo-inositol 1-phosphate as a surrogate of D-myo-inositol 1,4,5-tris phosphate to monitor G protein-coupled receptor activation.", "entity1": "G protein-coupled receptor", "entity2": "D-myo-inositol 1,4,5-tris phosphate", "span1": [92, 118], "span2": [45, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12345": {"label": 8, "data": {"text": "In this work, the metabolism of four frequently prescribed inhaled GCs, triamcinolone acetonide, flunisolide, budesonide, and fluticasone propionate, by the CYP3A family of enzymes was studied to identify differences in their rates of clearance and to identify their metabolites.", "entity1": "CYP3A", "entity2": "fluticasone propionate", "span1": [157, 162], "span2": [126, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12896": {"label": 2, "data": {"text": "Both H(2)S solution prepared by bubbling pure H(2)S gas and NaSH, a H(2)S donor, dose dependently induced HO-1 expression through the activation of the extracellular signal-regulated kinase (ERK).", "entity1": "HO-1", "entity2": "H(2)S", "span1": [106, 110], "span2": [5, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"568": {"label": 8, "data": {"text": "These and other data have generated a working hypothesis that activation of the terminal serotonin autoreceptor enhances the kinetics of 5-HT uptake through an effect on the serotonin transporter.", "entity1": "serotonin transporter", "entity2": "5-HT", "span1": [174, 195], "span2": [137, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9187": {"label": 2, "data": {"text": "This agent acts synergistically with many penicillins, such as ampicillin, carbenicillin, and the like, and with cephalosporins, cefazolin, cefamandole, or cefoxitin to inhibit gram-negative bacilli, probably on the basis of binding to different proteins needed for the production of the peptidoglycan of the bacterial cell wall.", "entity1": "peptidoglycan", "entity2": "penicillins", "span1": [288, 301], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13711": {"label": 3, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.2", "entity2": "4-chloropropofol", "span1": [195, 203], "span2": [175, 191]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9568": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "GM-CSF", "entity2": "isoproterenol", "span1": [42, 48], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3498": {"label": 9, "data": {"text": "The study showed that fenofibrate did not attenuate increased blood pressure induced by PE, AII and ET1 but caused enhanced vasodilation by Ach, SNP and ISO.", "entity1": "AII", "entity2": "fenofibrate", "span1": [92, 95], "span2": [22, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7502": {"label": 1, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "ENaC", "entity2": "phenformin", "span1": [141, 145], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6251": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "human serotonin transporter", "entity2": "fluperlapine", "span1": [58, 85], "span2": [108, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12096": {"label": 3, "data": {"text": "Under these conditions, blockade of monoamine oxidase with pargyline (100 microM for 15 min) caused a leftward displacement of concentration-effect curves for both 5-methoxytryptamine (5-MeO-T) and tryptamine.", "entity1": "monoamine oxidase", "entity2": "pargyline", "span1": [36, 53], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11612": {"label": 1, "data": {"text": "Nevertheless, PPARgamma is indirectly necessary for both cAspAT basal expression and TZD responsiveness because they are, respectively, diminished and abolished by ectopic overexpression of a dominant negative PPARgamma.", "entity1": "PPARgamma", "entity2": "TZD", "span1": [14, 23], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11125": {"label": 1, "data": {"text": "Risperidone was equipotent to prazosin at alpha 1A-adrenoceptors in rat vas deferens and kidney.", "entity1": "alpha 1A-adrenoceptors", "entity2": "prazosin", "span1": [42, 64], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7365": {"label": 2, "data": {"text": "Differential activation of cAMP response element binding protein in discrete nucleus accumbens subregions during early and late cocaine sensitization.", "entity1": "cAMP response element binding protein", "entity2": "cocaine", "span1": [27, 64], "span2": [128, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1866": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "DGAT", "entity2": "kushenol K", "span1": [253, 257], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10295": {"label": 1, "data": {"text": "Pentosan polysulfate sodium (PPS) has been shown to exert antitumor activity by antagonizing the binding of bFGF to cell surface receptors.", "entity1": "bFGF", "entity2": "sodium", "span1": [108, 112], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6601": {"label": 5, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "5-HT(1A)", "entity2": "WAY100635", "span1": [102, 110], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"402": {"label": 3, "data": {"text": "Association of PGE2 or acetazolamide to NSAIDs reduced NSAID-induced activation of CA I and CA II.", "entity1": "CA II", "entity2": "acetazolamide", "span1": [92, 97], "span2": [23, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8821": {"label": 8, "data": {"text": "Mitochondria in the steroidogenic cells of the adrenal, gonad, placenta and brain contain the cholesterol side-chain cleavage enzyme, P450scc, and its two electron-transfer partners, ferredoxin reductase and ferredoxin.", "entity1": "P450scc", "entity2": "cholesterol", "span1": [134, 141], "span2": [94, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2678": {"label": 9, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "kinase domain", "entity2": "IM", "span1": [26, 39], "span2": [93, 95]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1910": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "fluoropyrimidine carbamate", "span1": [96, 119], "span2": [13, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4876": {"label": 3, "data": {"text": "Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.", "entity1": "V600E", "entity2": "N-(thiophen-2-yl) benzamide", "span1": [80, 85], "span2": [32, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7713": {"label": 5, "data": {"text": "Oral palonosetron is likely to be a useful addition to oral formulations of other 5-HT3 receptor antagonists in preventing CINV in patients receiving MEC.", "entity1": "5-HT3 recepto", "entity2": "palonosetron", "span1": [82, 95], "span2": [5, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6394": {"label": 4, "data": {"text": "In alpha(2A)-adrenoceptor transfected cells the rank order of agonist potency was A-54741 (mean pEC(50)=8.96)>dexmedetomidine (8.88)>UK-14304 (8.42)>B-HT 920 (7.05)>noradrenaline (6.92).", "entity1": "alpha(2A)-adrenoceptor", "entity2": "noradrenaline", "span1": [3, 25], "span2": [165, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7779": {"label": 1, "data": {"text": "The PARP inhibitor PJ34 modifies proliferation, NIS expression and epigenetic marks in thyroid cancer cell lines.", "entity1": "NIS", "entity2": "PJ34", "span1": [48, 51], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6813": {"label": 2, "data": {"text": "Further study revealed that pitavastatin increased ABCA1 mRNA in HMG-CoA reductase-dependent manner and that Rho and Rho kinase inhibitor (C3T and Y27632) increased apoA-I production in the HepG2 cells.", "entity1": "apoA-I", "entity2": "Y27632", "span1": [165, 171], "span2": [147, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6608": {"label": 3, "data": {"text": "The effects of histamine H1-receptor antagonists, promethazine and homochlorcyclizine, both of which are inhibitors of CYP2D6, on the steady-state plasma concentrations (Css) of haloperidol and reduced haloperidol were studied in 23 schizophrenic inpatients receiving haloperidol, 12 to 36 mg/d, for 2 to 29 weeks.", "entity1": "CYP2D6", "entity2": "homochlorcyclizine", "span1": [119, 125], "span2": [67, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8412": {"label": 3, "data": {"text": "Ponatinib (AP24534) is a multikinase inhibitor with in vitro and clinical activity in tyrosine kinase inhibitor (TKI)-resistant chronic myeloid leukemia, irrespective of BCR-ABL KD mutation.", "entity1": "multikinase", "entity2": "AP24534", "span1": [25, 36], "span2": [11, 18]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15326": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "2,3-dihydroxy-2,3-dihydrofluoranthene", "span1": [287, 296], "span2": [49, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13311": {"label": 3, "data": {"text": "INTERPRETATION AND CONCLUSIONS: These results warrant further clinical studies of sorafenib for the treatment of myeloid malignancies expressing activated forms of PDGFRbeta and FLT3.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [178, 182], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1835": {"label": 3, "data": {"text": "Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide.", "entity1": "ABCA1", "entity2": "glyburide", "span1": [31, 36], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7927": {"label": 1, "data": {"text": "Altogether, our results suggest that a high dose of glucosamine may inhibit cell proliferation through apoptosis and disturb cell cycle progression with a halt at G(0)/G(1) phase, and that this occurs, at least in part, by a reduction in Rb phosphorylation together with modulation of p21, p53 and HO-1 expression, and nuclear p21 accumulation.", "entity1": "p53", "entity2": "glucosamine", "span1": [290, 293], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7899": {"label": 1, "data": {"text": "In conclusion, the CAG length dependent effect of TCDD on AR activity in PNT1A, but not in PC-3 cells, indicates as a cell-specific effect of TCDD on AR activity.", "entity1": "AR", "entity2": "TCDD", "span1": [150, 152], "span2": [142, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11625": {"label": 1, "data": {"text": "The immunosuppressive effects of T3 SCI were caused by NE acting at beta2-adrenergic receptors (beta2AR) and could be reversed using beta2AR blockers.", "entity1": "beta2AR", "entity2": "NE", "span1": [96, 103], "span2": [55, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"720": {"label": 1, "data": {"text": "Infrared spectroscopic studies revealed a reduced thermal stability both of the apo-and the holo-hTH1 on binding of H4biopterin and Lerythro-dihydrobiopterin (H2biopterin).", "entity1": "hTH1", "entity2": "Lerythro-dihydrobiopterin", "span1": [97, 101], "span2": [132, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9394": {"label": 2, "data": {"text": "We thus speculated that activation of PGHS-1 might be a mechanism by which minoxidil (2,4-diamino-6-piperidinopyrimidine-3-oxyde) stimulates hair growth in vivo.", "entity1": "PGHS-1", "entity2": "minoxidil", "span1": [38, 44], "span2": [75, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11669": {"label": 1, "data": {"text": "The Ca(2+)-S100A4/prochlorperazine (PCP) complex exhibits a similar pentameric assembly.", "entity1": "S100A4", "entity2": "prochlorperazine", "span1": [11, 17], "span2": [18, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7712": {"label": 1, "data": {"text": "RESULTS: (18)F-AV-45 displayed a high binding affinity and specificity to Abeta plaques (K(d), 3.72 +/- 0.30 nM).", "entity1": "Abeta", "entity2": "(18)F-AV-45", "span1": [74, 79], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12515": {"label": 1, "data": {"text": "These results demonstrate the presence of a dehydrogenase activity separate from the nicotinamide-adenine dinucleotide phosphate (NADP)-dependent 11 beta hydroxysteroid dehydrogenase recently purified and cloned from rat liver.", "entity1": "11 beta hydroxysteroid dehydrogenase", "entity2": "nicotinamide-adenine dinucleotide phosphate", "span1": [146, 182], "span2": [85, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3997": {"label": 8, "data": {"text": "Aldose reductase (AR) catalyzes the reduction of toxic lipid aldehydes to their alcohol products and mediates inflammatory signals triggered by lipopolysaccharide (LPS).", "entity1": "AR", "entity2": "aldehydes", "span1": [18, 20], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"11218": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "glibenclamide", "span1": [4, 11], "span2": [64, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2049": {"label": 3, "data": {"text": "Increased immunohistochemical labeling of HIF-1alpha, VEGF, and BNP in the ventricular myocardium was observed in the shunt group and carvedilol again normalized the labeling.", "entity1": "BNP", "entity2": "carvedilol", "span1": [64, 67], "span2": [134, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9094": {"label": 3, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "5-lipoxygenase", "entity2": "diethylcarbamazine", "span1": [194, 208], "span2": [15, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15041": {"label": 1, "data": {"text": "It had higher levels of oleocanthal (p-HPEA-EDA), a nutraceutical compound exerting actions against COX1 and COX2 (cycloxygenases).", "entity1": "COX2", "entity2": "p-HPEA-EDA", "span1": [109, 113], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12370": {"label": 8, "data": {"text": "A., Ventura, F. V., Houten, S. M. Carnitine palmitoyltransferase 2 and carnitine/acylcarnitine translocase are involved in the mitochondrial synthesis and export of acylcarnitines.", "entity1": "Carnitine palmitoyltransferase 2", "entity2": "acylcarnitines", "span1": [34, 66], "span2": [165, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5616": {"label": 8, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "K+", "span1": [71, 75], "span2": [76, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5038": {"label": 3, "data": {"text": "Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.", "entity1": "cyclooxygenase-2", "entity2": "1,5-diarylpyrrole nitrooxyalkyl ethers", "span1": [106, 122], "span2": [42, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10428": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "RARbeta", "entity2": "acetylenic retinoid", "span1": [132, 139], "span2": [17, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1153": {"label": 8, "data": {"text": "ZD1839 (\"Iressa\"), a quinazoline tyrosinetyrosine kinase inhibitor selective for the EGFR, has shown good activity in preclinical studies and in the early phase of clinical trials.", "entity1": "tyrosine kinase", "entity2": "quinazoline tyrosine", "span1": [41, 56], "span2": [21, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3387": {"label": 6, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "GABA(A)R", "entity2": "BDZs", "span1": [24, 32], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8208": {"label": 1, "data": {"text": "Stenesen and colleagues (2012) activate AMPK both directly and indirectly by altering AMP biosynthesis to slow aging in Drosophila, highlighting AMPK as a conserved life span modulator that links energy sensing to longevity.", "entity1": "AMPK", "entity2": "AMP", "span1": [40, 44], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13655": {"label": 0, "data": {"text": "The distances between the protons H20 and H2, H18 and H2, and H18 and H4 are shorter following their binding to the PGIS in solution-down to within 5 A.", "entity1": "PGIS", "entity2": "H18", "span1": [116, 120], "span2": [62, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14150": {"label": 2, "data": {"text": "In [(35)S]GTPgammaS assays, mianserin selectively activated kappa-opioid receptors.", "entity1": "kappa-opioid receptors", "entity2": "mianserin", "span1": [60, 82], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13252": {"label": 1, "data": {"text": "However, the relationship of leukotrienes with mucin genes expression is not clear.", "entity1": "mucin", "entity2": "leukotrienes", "span1": [47, 52], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2346": {"label": 1, "data": {"text": "We conclude that lutein and EPA interact through the PPARgamma and RXR pathways to modulate iNOS mRNA.", "entity1": "iNOS", "entity2": "EPA", "span1": [92, 96], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3077": {"label": 3, "data": {"text": "PURPOSE: To compare phenelzine (PLZ), an antidepressant drug with anxiolytic properties which inhibits monoamine oxidase (MAO) but also elevates rat brain levels of the amino acids ?-aminobutyric acid (GABA) and alanine (ALA), with vigabatrin (VIG), an anticonvulsant which elevates brain GABA by inhibition of GABA transaminase (GABA-T), with regard to their actions on brain levels of GABA and ALA and on activities of MAO, GABA-T and ALA transaminase (ALA-T).", "entity1": "MAO", "entity2": "PLZ", "span1": [122, 125], "span2": [32, 35]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15444": {"label": 8, "data": {"text": "Possible AOX involvement in IMI metabolism in insects was evaluated using AOX-expressing and AOX-deficient Drosophila, but no differences were found in IMI nitroreduction or sensitivity between the two strains.", "entity1": "AOX", "entity2": "IMI", "span1": [9, 12], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10522": {"label": 3, "data": {"text": "RESULTS: GW572016 inhibited constitutive and/or ligand-induced EGFR or HER2 tyrosine phosphorylation of all five cell lines, which correlated with the antiproliferative response in all but one cell line.", "entity1": "HER2", "entity2": "GW572016", "span1": [71, 75], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4082": {"label": 3, "data": {"text": "An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective \u03b3-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease.", "entity1": "\u03b3-secretase", "entity2": "SCH 900229", "span1": [159, 170], "span2": [122, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"364": {"label": 1, "data": {"text": "The differential effects of DEX on the proliferation of high and low IL-2 producers in vitro may implicate a selective outgrowth of Th1-like T cells in vivo in patients treated with steroids.", "entity1": "IL-2", "entity2": "DEX", "span1": [69, 73], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6517": {"label": 3, "data": {"text": "Aliskiren has the potential to become the first orally active renin inhibitor that provides a true alternative to ACE-inhibitors and Ang II receptor antagonists in therapy for hypertension and other cardiovascular and renal diseases.", "entity1": "ACE", "entity2": "Aliskiren", "span1": [114, 117], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8161": {"label": 3, "data": {"text": "DPEP inhibited LPS-induced phosphorylation of ERK, JNK, and p38.", "entity1": "p38", "entity2": "DPEP", "span1": [60, 63], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10658": {"label": 2, "data": {"text": "An angiotensin II AT1 receptor antagonist, telmisartan augments glucose uptake and GLUT4 protein expression in 3T3-L1 adipocytes.", "entity1": "GLUT4", "entity2": "telmisartan", "span1": [83, 88], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11410": {"label": 3, "data": {"text": "Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values.", "entity1": "BNP", "entity2": "carvedilol", "span1": [78, 81], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11052": {"label": 3, "data": {"text": "For some, pharmacologic inhibitors are available, including sorafenib for BRAF, farnesyltransferase inhibitors for NRAS, PD-0325901 for mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, rapamycin analogues for mammalian target of rapamycin, and agents that inhibit either vascular endothelial growth factor or its receptors.", "entity1": "mammalian target of rapamycin", "entity2": "rapamycin", "span1": [239, 268], "span2": [215, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6361": {"label": 8, "data": {"text": "The mNQO activity showed significantly higher affinity for NADH than NADPH as electron donors and catalyzed reduction of 2,6-dichlorophenolindophenol and menadione.", "entity1": "mNQO", "entity2": "menadione", "span1": [4, 8], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15668": {"label": 3, "data": {"text": "Subsequent optimization led to several novel 3HPT-based HDACi that are selective for HDAC 6 and HDAC 8.", "entity1": "HDAC 6", "entity2": "3HPT", "span1": [85, 91], "span2": [45, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5982": {"label": 1, "data": {"text": "Chloride functions as a result of its binding to [Glu1]Pg, with a Ki of approximately 9.0 mM, thereby rendering [Glu1]Pg a less effective substrate for two-chain rec-t-PA. EACA stimulates the activation in Cl-(-)containing solutions, with a Ka of approximately 4.0 mM, primarily by reversal of the Cl-(-)inhibitory effect.", "entity1": "[Glu1]Pg", "entity2": "Chloride", "span1": [49, 57], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14706": {"label": 3, "data": {"text": "Moreover, icariin treatment inhibited the phosphorylations of STAT1 and STAT3 in CD4(+) T cells, which were the crucial transcription factors for Th1 and Th17 respectively.", "entity1": "STAT1", "entity2": "icariin", "span1": [62, 67], "span2": [10, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7566": {"label": 5, "data": {"text": "Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12 receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes.", "entity1": "P2Y12", "entity2": "AZD6140", "span1": [65, 70], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11472": {"label": 1, "data": {"text": "Melatonin and N-acetyl-5-hydroxytryptamine (N-acetyl-5-HT), a ligand of MT3 biding site, also had no impairment on the performance, per se.", "entity1": "MT3", "entity2": "Melatonin", "span1": [72, 75], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11344": {"label": 3, "data": {"text": "Phenytoin (diphenylhydantoin, DPH) is an established sodium channel blocker and is a useful anticonvulsant and class 1b antiarrhythmic, and has been effectively used in the treatment of neuropathic pain.", "entity1": "sodium channel", "entity2": "Phenytoin", "span1": [53, 67], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2296": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "AH 6809", "span1": [74, 77], "span2": [249, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10861": {"label": 1, "data": {"text": "Interestingly, we identified 4-methylhistamine as a high-affinity H(4)R ligand (K(i) = 50 nM) that has a >100-fold selectivity for the hH(4)R over the other histamine receptor subtypes.", "entity1": "histamine receptor", "entity2": "4-methylhistamine", "span1": [157, 175], "span2": [29, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2829": {"label": 3, "data": {"text": "Pharmacological treatment has been studied and it could be demonstrated, that some mutant currents may be insufficiently suppressed by drugs targeted to block the specific current such as, e.g., sotalol or ibutilide in patients with a mutation in the IKr-coding gene KCNH2 (HERG).", "entity1": "IKr", "entity2": "ibutilide", "span1": [251, 254], "span2": [206, 215]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15465": {"label": 8, "data": {"text": "The present study demonstrated that human multidrug resistance-associated protein 3 vesicles accepted conjugated 3\u03b2-hydroxy-\u0394(5)-bile acids along with common bile acids such as glycocholic acid and taurolithocholic acid 3-sulfate.", "entity1": "human multidrug resistance-associated protein 3", "entity2": "bile acids", "span1": [36, 83], "span2": [158, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3614": {"label": 3, "data": {"text": "Also, SB365 showed anti-angiogenic activity by decreasing the expression of HIF-1\u03b1 and VEGF.", "entity1": "VEGF", "entity2": "SB365", "span1": [87, 91], "span2": [6, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2244": {"label": 3, "data": {"text": "BACKGROUND: Since the introduction of the first cholinesterase inhibitor (ChEI) in 1997, most clinicians and probably most patients would consider the cholinergic drugs, donepezil, galantamine and rivastigmine, to be the first line pharmacotherapy for mild to moderate Alzheimer's disease.The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase.", "entity1": "cholinesterase", "entity2": "donepezil", "span1": [48, 62], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14669": {"label": 1, "data": {"text": "These findings demonstrated that genistein improves thrombin-induced endothelial barrier dysfunction in ECs through PKA-mediated suppression of RhoA signaling.", "entity1": "thrombin", "entity2": "genistein", "span1": [52, 60], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8627": {"label": 1, "data": {"text": "In contrast, activation of Nrf2 by sulforaphane and tert-butylhydroquinone depend upon Keap1-C151 and not p62 (the canonical mechanism).", "entity1": "Keap1", "entity2": "tert-butylhydroquinone", "span1": [87, 92], "span2": [52, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5180": {"label": 1, "data": {"text": "Dioscin-induced autophagy mitigates cell apoptosis through modulation of PI3K/Akt and ERK and JNK signaling pathways in human lung cancer cell lines.", "entity1": "PI3K", "entity2": "Dioscin", "span1": [73, 77], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5283": {"label": 2, "data": {"text": "In concert with these results, we highlighted that the secretion of pro-inflammatory cytokine and NF-\u03baB activation induced by TCDD can be mediated by elevation of [Ca(2+)]i in HAPI microglial cells.", "entity1": "cytokine", "entity2": "TCDD", "span1": [85, 93], "span2": [126, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3194": {"label": 3, "data": {"text": "Phenols like the ones investigated here possess a CA inhibition mechanism distinct of that of the sulfonamides/sulfamates used clinically or the coumarins.", "entity1": "CA", "entity2": "sulfamates", "span1": [50, 52], "span2": [111, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4118": {"label": 8, "data": {"text": "These data suggest that G6pc2 represents a novel, negative regulator of basal GSIS that acts by hydrolyzing glucose-6-phosphate, thereby reducing glycolytic flux.", "entity1": "G6pc2", "entity2": "glucose-6-phosphate", "span1": [24, 29], "span2": [108, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13873": {"label": 1, "data": {"text": "Moreover, the effect of ibuprofen on RhoA activity and neurite growth in neuronal cultures is prevented by selective PPARgamma inhibition.", "entity1": "RhoA", "entity2": "ibuprofen", "span1": [37, 41], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"373": {"label": 3, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2R alpha", "entity2": "DEX", "span1": [219, 230], "span2": [177, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12831": {"label": 1, "data": {"text": "The angiotensin II (A-II) type 1 (AT1) receptor-mediated effects of A-II play a key role in the pathophysiology of hypertension.", "entity1": "angiotensin II (A-II) type 1 (AT1) receptor", "entity2": "A-II", "span1": [4, 47], "span2": [68, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16065": {"label": 3, "data": {"text": "In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684).", "entity1": "ALK", "entity2": "TAE684", "span1": [204, 207], "span2": [221, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12473": {"label": 9, "data": {"text": "UGT2B10 was inactive in the glucuronidation of desipramine, nortriptyline, carbamazepine and afloqualone.", "entity1": "UGT2B10", "entity2": "nortriptyline", "span1": [0, 7], "span2": [60, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15948": {"label": 9, "data": {"text": "4-Hydroxytamoxifen (OHT, tamoxifen's active form) failed to prevent E2-induced proteolysis of cyclin E and migration, but rather triggered cyclin E cleavage coincident with augmented migration.", "entity1": "cyclin E", "entity2": "4-Hydroxytamoxifen", "span1": [94, 102], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7045": {"label": 1, "data": {"text": "Since the effect of retinoic acid is mediated via retinoic acid receptors and retinoid X receptors, we investigated mRNA and protein expression of these receptors during injury-induced degeneration and regeneration.", "entity1": "retinoic acid receptors", "entity2": "retinoic acid", "span1": [50, 73], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7196": {"label": 2, "data": {"text": "ADP initiates platelet aggregation by 'simultaneous activation of two G protein-coupled receptors, P2Y1 and P2Y12.", "entity1": "G protein-coupled receptors", "entity2": "ADP", "span1": [70, 97], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2892": {"label": 4, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1D)-adrenoceptor", "entity2": "phenylephrine", "span1": [235, 257], "span2": [300, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1542": {"label": 9, "data": {"text": "The purified human enzyme also does not oxidize eight representative antitumor polyamine analogues; however, specific oligamine analogues were found to be potent inhibitors of the oxidation of spermine by PAOh1/SMO.", "entity1": "SMO", "entity2": "polyamine", "span1": [211, 214], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14675": {"label": 3, "data": {"text": "Genistein also reduced the formation of stress fibers by thrombin and suppressed thrombin-induced phosphorylation of myosin light chain (MLC) on Ser(19)/Thr(18) in endothelial cells (ECs).", "entity1": "myosin light chain", "entity2": "Genistein", "span1": [117, 135], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10667": {"label": 1, "data": {"text": "We tested the association of beta(2)AR genotypes with asthma severity and bronchodilator response to albuterol in Puerto Ricans and Mexicans with asthma.", "entity1": "beta(2)AR", "entity2": "albuterol", "span1": [29, 38], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"729": {"label": 9, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "rat ACE", "entity2": "cilazapril", "span1": [171, 178], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3097": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "[(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester", "span1": [354, 357], "span2": [209, 279]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2932": {"label": 0, "data": {"text": "AdSS from the thermophilic archaea, Methanocaldococcus jannaschii (MjAdSS) is 345 amino acids long against an average length of 430-457 amino acids for most mesophilic AdSS.", "entity1": "AdSS", "entity2": "amino acids", "span1": [168, 172], "span2": [136, 147]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13194": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "NET", "entity2": "mZIENT", "span1": [287, 290], "span2": [67, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10011": {"label": 4, "data": {"text": "In mice, AS-8112 (1.0 - 3.0 mg kg(-1) s.c.) potently inhibited hypothermia induced by the dopamine D3 receptor agonist; R(+)-7-OH-DPAT (R(+)-7-hydroxy-2-(N,N-di-n-propylamino)tetraline) (0.3 mg kg(-1) s.c.).", "entity1": "dopamine D3 receptor", "entity2": "R(+)-7-hydroxy-2-(N,N-di-n-propylamino)tetraline", "span1": [90, 110], "span2": [136, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2888": {"label": 3, "data": {"text": "In medial striatum, TH-ir decreased by 21%, and in hypothalamus neuropeptide Y-ir increased by 10% in MPH-exposed rats.", "entity1": "TH", "entity2": "MPH", "span1": [20, 22], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8168": {"label": 1, "data": {"text": "DNA polymerase minor groove interactions modulate mutagenic bypass of a templating 8-oxoguanine lesion.", "entity1": "DNA polymerase minor groove", "entity2": "8-oxoguanine", "span1": [0, 27], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13708": {"label": 3, "data": {"text": "High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues.", "entity1": "voltage-operated skeletal muscle and neuronal sodium channels", "entity2": "halogenated propofol", "span1": [26, 87], "span2": [91, 111]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8082": {"label": 9, "data": {"text": "E235-mediated induction of senescence was not dependent on p21 or p53; however, p21 conferred protection against the growth inhibitory effects of E235.", "entity1": "p53", "entity2": "E235", "span1": [66, 69], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8157": {"label": 3, "data": {"text": "Additionally, DPEP suppressed the production of inflammatory cytokines, including tumor necrosis factor-\u03b1 (TNF-\u03b1), interleukin (IL)-1\u03b2, and IL-6.", "entity1": "interleukin (IL)-1\u03b2", "entity2": "DPEP", "span1": [115, 134], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10992": {"label": 3, "data": {"text": "Tyrosine kinase inhibitors are quinazoline-derived, low molecular weight synthetic molecules that can block the intracellular tyrosine kinase domain of several receptors, including EGFR, Erb2, and vascular endothelial growth factor receptor, and thereby inhibit ligand-induced receptor phosphorylation and abrogate the biologic effect of EGFR signaling.", "entity1": "EGFR", "entity2": "quinazoline", "span1": [181, 185], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12490": {"label": 8, "data": {"text": "Cynomolgus FMO6 metabolized benzydamine only slightly, but minimal expression of FMO6 in all tissue precludes the importance of FMO6 in drug metabolism, unlike cynomolgus FMO1, FMO2, FMO3, and FMO5 which were all functional.", "entity1": "FMO2", "entity2": "benzydamine", "span1": [177, 181], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8654": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRA", "entity2": "melatonin", "span1": [20, 23], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14162": {"label": 5, "data": {"text": "The agonist activity was antagonized by the selective kappa-opioid blocker nor-binaltorphimine (nor-BNI).", "entity1": "kappa-opioid", "entity2": "nor-binaltorphimine", "span1": [54, 66], "span2": [75, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3620": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "WIN 55,212", "span1": [14, 17], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12282": {"label": 1, "data": {"text": "Chlorthalidone bound within the CA II active site is in an enolic (lactimic) tautomeric form, with the enolic OH also participating in two strong hydrogen bonds with Asn67 and a water molecule.", "entity1": "CA II", "entity2": "Chlorthalidone", "span1": [32, 37], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2778": {"label": 3, "data": {"text": "In the presence of the system L inhibitor BCH, Na(+)-dependent l-alanine uptake in WKY and SHR PTE cells was inhibited by alanine, serine, and cysteine, which is consistent with amino acid transport through ASCT2.", "entity1": "ASCT2", "entity2": "cysteine", "span1": [207, 212], "span2": [143, 151]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14408": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "Akt", "entity2": "ESI-09", "span1": [288, 291], "span2": [145, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5642": {"label": 2, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "transcription factor Sp1", "entity2": "matrine", "span1": [117, 141], "span2": [72, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3718": {"label": 3, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "mTOR", "entity2": "N", "span1": [106, 110], "span2": [13, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4804": {"label": 3, "data": {"text": "The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described.", "entity1": "BACE-1", "entity2": "dihydroisoquinoline", "span1": [71, 77], "span2": [51, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8717": {"label": 3, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "CAT", "entity2": "NaAsO2", "span1": [25, 28], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4158": {"label": 1, "data": {"text": "CNTs with linear poly(ethylene glycol) amphiphiles trigger the lectin pathway of the complement through both L-ficolin and mannan-binding lectin recognition.", "entity1": "lectin", "entity2": "poly(ethylene glycol)", "span1": [138, 144], "span2": [17, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1334": {"label": 4, "data": {"text": "The esterified-BM, however, had only partial transactivation agonistic activity in cells transfected with rat GR, whereas BM and esterified-DEX had full transactivation agonistic activity.", "entity1": "rat GR", "entity2": "BM", "span1": [106, 112], "span2": [122, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7191": {"label": 1, "data": {"text": "Because progesterone (1) affects both menstruation and gestation via the progesterone receptor (PR), research aimed at modulating its activity is usually surrounded by controversy.", "entity1": "PR", "entity2": "progesterone", "span1": [96, 98], "span2": [8, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15885": {"label": 2, "data": {"text": "Our study revealed that high glucose/Fe concentrations in MIN6 cells induced an increase of the Bcl2/Bax ratio, an indicator of increased cell apoptosis.", "entity1": "Bax", "entity2": "Fe", "span1": [101, 104], "span2": [37, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1919": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "M564G", "entity2": "acetyl-CoA", "span1": [4, 9], "span2": [210, 220]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6622": {"label": 0, "data": {"text": "In arginase, two cysteines at the C terminus of the protein are crucial for its epiarginase function but not for its catalytic activity and trimeric structure.", "entity1": "arginase", "entity2": "cysteines", "span1": [3, 11], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5706": {"label": 3, "data": {"text": "We previously demonstrated that developmental exposure to a mixture of polychlorinated biphenyls (PCBs) which was reconstituted according to the congener pattern found in human breast milk caused feminization of sweet preference as a sexually dimorphic behavior in adult male rats, following decreases in aromatase activity in the brain of newborn male pups.", "entity1": "aromatase", "entity2": "PCBs", "span1": [305, 314], "span2": [98, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5500": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D1 receptor", "entity2": "(-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine", "span1": [153, 173], "span2": [196, 294]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13447": {"label": 1, "data": {"text": "Finally, PLA2 inhibitor methyl arachidonyl fluorophosphonate blocked the PUFA effects on COX-2 induction, promoter activity and arachidonic acid mobilization suggesting involvement of AA metabolites in PPAR activation.", "entity1": "COX-2", "entity2": "PUFA", "span1": [89, 94], "span2": [73, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13489": {"label": 3, "data": {"text": "Modulation of the function of CD36 (CD36-/- mice), p38(MAPK) (SB203580), COX-1 (indomethacin), and glycoprotein Ib alpha (Nk-protease, 6D1 antibody) induced approximately 50% inhibition.", "entity1": "MAPK", "entity2": "SB203580", "span1": [55, 59], "span2": [62, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3685": {"label": 2, "data": {"text": "8-pCPT-2'-O-Me-cAMP-AM potentiation of insulin secretion stimulated by tolbutamide was markedly inhibited by 2-APB (25 \u03bcM) and enhanced by the PKC inhibitor bisindolylmaleimide I (1 \u03bcM).", "entity1": "insulin", "entity2": "bisindolylmaleimide I", "span1": [39, 46], "span2": [157, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1387": {"label": 3, "data": {"text": "Gemfibrozil, a lipid-lowering drug, inhibited cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes.", "entity1": "inducible nitric-oxide synthase", "entity2": "Gemfibrozil", "span1": [102, 133], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10041": {"label": 2, "data": {"text": "Rosiglitazone modestly increased apolipoprotein C-III mRNA and had no effect on expression of the other 2 genes in the liver but increased the expression of glucose transporter 4 and phosphoenolpyruvate carboxykinase in adipose tissue.", "entity1": "glucose transporter 4", "entity2": "Rosiglitazone", "span1": [157, 178], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8555": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "HDAC", "entity2": "2'-aminoanilides", "span1": [180, 184], "span2": [75, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15271": {"label": 0, "data": {"text": "We also show that removal of either the N- or C-terminal propeptide is required for VEGF-D to drive formation of VEGFR-2/VEGFR-3 heterodimers which have recently been shown to positively regulate angiogenic sprouting.", "entity1": "VEGF-D", "entity2": "C", "span1": [84, 90], "span2": [46, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13097": {"label": 4, "data": {"text": "Among the measured compounds, gliquidone and glipizide (two sulfonylureas), as well as nateglinide (a glinide), exhibit PPARgamma agonistic activity at concentrations comparable with those reached under pharmacological treatment.", "entity1": "PPARgamma", "entity2": "sulfonylureas", "span1": [120, 129], "span2": [60, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4262": {"label": 1, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "PARP", "entity2": "SB216763", "span1": [91, 95], "span2": [57, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3301": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mTOR", "entity2": "Afinitor((R)) Novartis", "span1": [75, 79], "span2": [20, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10617": {"label": 1, "data": {"text": "Furthermore, GABA receptors of horizontal cells were modulated by extracellular application of diazepam, zolpidem, methyl 6,7-dimethoxy-4-ethyl-beta-carboxylate, pentobarbital, and alphaxalone, thus showing typical pharmacological properties of CNS GABAA receptors.", "entity1": "GABA receptors", "entity2": "methyl 6,7-dimethoxy-4-ethyl-beta-carboxylate", "span1": [13, 27], "span2": [115, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12488": {"label": 8, "data": {"text": "Cynomolgus FMO6 metabolized benzydamine only slightly, but minimal expression of FMO6 in all tissue precludes the importance of FMO6 in drug metabolism, unlike cynomolgus FMO1, FMO2, FMO3, and FMO5 which were all functional.", "entity1": "Cynomolgus FMO6", "entity2": "benzydamine", "span1": [0, 15], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15116": {"label": 2, "data": {"text": "These findings are the first to show that long-term exposure to Mn during a critical period of neurodevelopment causes motor coordination dysfunction with parallel increment in oxidative stress markers, p38(MAPK) phosphorylation and caspase activity in the striatum.", "entity1": "caspase", "entity2": "Mn", "span1": [233, 240], "span2": [64, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15950": {"label": 9, "data": {"text": "4-Hydroxytamoxifen (OHT, tamoxifen's active form) failed to prevent E2-induced proteolysis of cyclin E and migration, but rather triggered cyclin E cleavage coincident with augmented migration.", "entity1": "cyclin E", "entity2": "tamoxifen", "span1": [94, 102], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9612": {"label": 1, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "NBF1", "entity2": "8-azido-ATP", "span1": [62, 66], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10839": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "STI571", "span1": [110, 113], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15530": {"label": 3, "data": {"text": "In this setting, S-nitrosocysteine (10 \u03bcm) effectively blocked the Trx-mediated regeneration of oxidized Prx1.", "entity1": "oxidized Prx1", "entity2": "S-nitrosocysteine", "span1": [96, 109], "span2": [17, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4359": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NQO1", "entity2": "\u03b2-Lap", "span1": [149, 153], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13549": {"label": 5, "data": {"text": "Combination chemotherapy with a substance P receptor antagonist (aprepitant) and melarsoprol in a mouse model of human African trypanosomiasis.", "entity1": "substance P receptor", "entity2": "aprepitant", "span1": [32, 52], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9985": {"label": 3, "data": {"text": "Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.", "entity1": "acetylcholinesterase", "entity2": "Hexahydrochromeno[4,3-b]pyrrole", "span1": [47, 67], "span2": [0, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9760": {"label": 5, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "h5-HT(1D)", "entity2": "yohimbine", "span1": [104, 113], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3827": {"label": 9, "data": {"text": "The inhibition of phosphoinositide 3-kinase using Ly294002 augmented a decrease in the p21 level induced by their combination, but it showed no significant effects on expression of Sp1 and cyclin D1.", "entity1": "Sp1", "entity2": "Ly294002", "span1": [181, 184], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1673": {"label": 2, "data": {"text": "Activation of alpha 2B-adrenoceptors mediates the cardiovascular effects of etomidate.", "entity1": "alpha 2B-adrenoceptors", "entity2": "etomidate", "span1": [14, 36], "span2": [76, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5213": {"label": 1, "data": {"text": "Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrial and non-mitochondrial-dependent mechanisms.", "entity1": "Ras homologous A protein", "entity2": "Vinblastine", "span1": [63, 87], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3783": {"label": 2, "data": {"text": "These results indicate that phillyrin prevents lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation, suggesting that phillyrin is a novel AMPK activator with a role in the prevention and treatment of obesity.", "entity1": "LKB1", "entity2": "phillyrin", "span1": [136, 140], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7299": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "BAAT", "entity2": "glycine", "span1": [63, 67], "span2": [167, 174]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11256": {"label": 0, "data": {"text": "Ntp and Ctp, synthetic peptides based on the N- and C-terminal sequences of K(IR)6.0, respectively, were used to probe gating of K(IR)6.0/SUR K(ATP) channels.", "entity1": "K(IR)6.0", "entity2": "N", "span1": [76, 84], "span2": [45, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"170": {"label": 1, "data": {"text": "The most potent compound, D,L-4-(3,4-dichlorobenzoylamino)-5-(dipentylamino)-5-oxo-pen tanoic acid (lorglumide, CR 1409), has a great affinity for the pancreatic CCK receptors and is a competitive, specific and potent CCK antagonist on the smooth muscles of the gall bladder and ileum of the guinea pig and on the CCK-induced amylase secretion of isolated pancreatic acini.", "entity1": "CCK receptors", "entity2": "D,L-4-(3,4-dichlorobenzoylamino)-5-(dipentylamino)-5-oxo-pen tanoic acid", "span1": [162, 175], "span2": [26, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10513": {"label": 3, "data": {"text": "Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance.", "entity1": "EGFR", "entity2": "GW572016", "span1": [15, 19], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2769": {"label": 3, "data": {"text": "Inhibition studies demonstrated that the methyl group on the phenylacetic acid ring is required for COX-2 selectivity.", "entity1": "COX-2", "entity2": "methyl", "span1": [100, 105], "span2": [41, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5538": {"label": 1, "data": {"text": "A model of IAS binding to the beta 2AR is proposed.", "entity1": "beta 2AR", "entity2": "IAS", "span1": [30, 38], "span2": [11, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12981": {"label": 8, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "DAG kinase", "entity2": "Diacylglycerol", "span1": [120, 130], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"6471": {"label": 8, "data": {"text": "Diacylglycerol kinase (DGK) catalyzes the conversion of diacylglycerol to phosphatidic acid, making it an attractive candidate for a signal transduction component.", "entity1": "Diacylglycerol kinase", "entity2": "diacylglycerol", "span1": [0, 21], "span2": [56, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"12287": {"label": 1, "data": {"text": "Preclinical properties of 18F-AV-45: a PET agent for Abeta plaques in the brain.", "entity1": "Abeta", "entity2": "18F-AV-45", "span1": [53, 58], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12882": {"label": 3, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "glycerophosphoserine", "span1": [14, 20], "span2": [120, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"1850": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "CA I", "entity2": "methazolamide", "span1": [134, 138], "span2": [229, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12942": {"label": 8, "data": {"text": "L-arg is converted to urea by arginase I in the liver and arginase II in the kidney.", "entity1": "arginase II", "entity2": "L-arg", "span1": [58, 69], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"8285": {"label": 3, "data": {"text": "Moreover, the D2R inhibitor raclopride blocked the increase of both GDNF and Zif268 expression following potassium-evoked dopamine release in SH-SY5Y cells.", "entity1": "D2R", "entity2": "raclopride", "span1": [14, 17], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"212": {"label": 5, "data": {"text": "Alprenolol and bromoacetylalprenololmenthane are competitive slowly reversible antagonists at the beta 1-adrenoceptors of rat left atria.", "entity1": "beta 1-adrenoceptors", "entity2": "Alprenolol", "span1": [98, 118], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8362": {"label": 1, "data": {"text": "The acetylated albumin had twofold weaker binding affinity for diflunisal as demonstrated by fluorescence quenching.", "entity1": "acetylated albumin", "entity2": "diflunisal", "span1": [4, 22], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6667": {"label": 0, "data": {"text": "In this study, we investigated the expression and function of p53R2 and hRRM2 after UV treatment in human prostate cancer PC3 cells, which possess mutant p53 with a truncated COOH-terminal, and in human oropharyngeal cancer KB cells, which possess wild-type p53.", "entity1": "p53", "entity2": "COOH", "span1": [154, 157], "span2": [175, 179]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1121": {"label": 3, "data": {"text": "abolishes the inhibitory effect of acetazolamide on CA.", "entity1": "CA", "entity2": "acetazolamide", "span1": [52, 54], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"519": {"label": 1, "data": {"text": "By reporter gene analysis following transient transfections with various plasmids expressing a dominant negative mutant form of Cdc42, Rac1 or RhoA, C2-ceramide-induced SRE activation was shown to be selectively repressed by pEXV-RacN17 encoding a dominant negative mutant of Rac1, suggesting that Rac activity is essential for the signalling cascade of ceramide to the nucleus.", "entity1": "Rac", "entity2": "ceramide", "span1": [298, 301], "span2": [354, 362]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2058": {"label": 1, "data": {"text": "This alternate conformation now causes a steric hindrance to the O4 hydroxyl group of the Gal moiety of UDP-Gal, probably causing the dissociation of UDP-Gal and the reduced k(cat) of the Gal-T reaction.", "entity1": "Gal-T", "entity2": "O4 hydroxyl", "span1": [188, 193], "span2": [65, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11801": {"label": 1, "data": {"text": "In this study, we assessed the antitumor activity of PTE against human osteosarcoma cells and explored the role of JAK2/STAT3 and apoptosis-related signaling pathways on the activity of PTE.", "entity1": "STAT3", "entity2": "PTE", "span1": [120, 125], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13728": {"label": 8, "data": {"text": "DNA damage is accepted as a consequence of thymidylate deprivation induced by chemotherapeutic inhibitors of thymidylate synthase (TS), but the types of damage and signaling responses remain incompletely understood.", "entity1": "thymidylate synthase", "entity2": "thymidylate", "span1": [109, 129], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15329": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "1-nitropyrene", "span1": [287, 296], "span2": [113, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13484": {"label": 3, "data": {"text": "The present findings confirm that PVN CB1 receptors, localized mainly in GABAergic synapses that control in an inhibitory fashion excitatory synapses, exert an inhibitory control on penile erection, demonstrating for the first time that chronic blockade of CB1 receptors by SR 141716A increases the density of these receptors in the PVN.", "entity1": "CB1 receptors", "entity2": "SR 141716A", "span1": [257, 270], "span2": [274, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13307": {"label": 3, "data": {"text": "RESULTS: We show that sorafenib is a potent inhibitor of ETV6-PDGFRbeta and FLT3 mutants, including some of the mutants that confer resistance to PKC412 and other FLT3 inhibitors.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [163, 167], "span2": [22, 31]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2816": {"label": 3, "data": {"text": "DXM and 1400W attenuated the mRNA expression of E-selectin and iNOS induced by the costimulation of reIL-4, reTNF-alpha, and LPS.", "entity1": "E-selectin", "entity2": "1400W", "span1": [48, 58], "span2": [8, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12814": {"label": 3, "data": {"text": "Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [72, 76], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15262": {"label": 1, "data": {"text": "Insulin levels were negatively correlated with variables of vagal control, reaching significance for rMSSD and log(10)HF, but not for pvRSA, during the last four phases of the hyperglycaemic clamp (hyperglycaemic second phase, GLP-1 first and second phases, and arginine).", "entity1": "Insulin", "entity2": "arginine", "span1": [0, 7], "span2": [262, 270]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2708": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "Trio", "entity2": "parathion", "span1": [37, 41], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2338": {"label": 1, "data": {"text": "NO rebinding in HNS from Staphylococcus aureus (SA-HNS) is faster than that measured for either Bacillus anthracis (BA-HNS) or for eNOS(HD) in both oxidized and reduced forms in the presence of arginine.", "entity1": "SA-HNS", "entity2": "NO", "span1": [48, 54], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13060": {"label": 3, "data": {"text": "Similar to AMR and AMROH, adriamycin and etoposide (VP-16) are DNA topoisomerase II inhibitors.", "entity1": "DNA topoisomerase II", "entity2": "AMROH", "span1": [63, 83], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14871": {"label": 1, "data": {"text": "These findings indicate that the neuroprotective effect of EHT against MPTP is through several mechanisms including its anti-inflammatory and antioxidant activities as well as its ability to modulate the methylation and hence activity of PP2A.", "entity1": "PP2A", "entity2": "MPTP", "span1": [238, 242], "span2": [71, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15030": {"label": 3, "data": {"text": "A series of MMP-1 inhibitors have been identified based upon a methyl rosmarinate scaffold using structure-based drug design methods.", "entity1": "MMP-1", "entity2": "methyl rosmarinate", "span1": [12, 17], "span2": [63, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2000": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "rat GnRHR", "entity2": "Ala", "span1": [158, 167], "span2": [121, 124]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8452": {"label": 9, "data": {"text": "While CRF increased spontaneous glutamate release in the CeAL, CRF caused no significant changes to optogenetically evoked glutamate release in this region.", "entity1": "CRF", "entity2": "glutamate", "span1": [63, 66], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3940": {"label": 3, "data": {"text": "Reactivators showed different activity in the reactivation of rat brain AChE after dichlorvos, paraoxon and tabun inhibition.", "entity1": "rat brain AChE", "entity2": "dichlorvos", "span1": [62, 76], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1868": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "kurarinone", "span1": [221, 251], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"64": {"label": 3, "data": {"text": "We evaluated the clinical effectiveness of esmolol, an ultra-short-acting beta 1-adrenergic receptor blocking drug, to control the sinus tachycardia and increase in arterial blood pressures induced by electroconvulsive therapy (ECT).", "entity1": "beta 1-adrenergic receptor", "entity2": "esmolol", "span1": [74, 100], "span2": [43, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10266": {"label": 8, "data": {"text": "Reuptake of extracellular noradrenaline (NA) into superior cervical ganglion (SCG) neurones is mediated by means of the noradrenaline transporter (NAT, uptake 1).", "entity1": "noradrenaline transporter", "entity2": "NA", "span1": [120, 145], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14557": {"label": 5, "data": {"text": "Additional SAR around a related M(1) allosteric agonist family (VU0357017) identified similar, subtle 'molecular switches' that modulated modes of pharmacology from allosteric agonism to pan-mAChR orthosteric antagonism.", "entity1": "mAChR", "entity2": "VU0357017", "span1": [191, 196], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"13498": {"label": 1, "data": {"text": "GT-2331 [(+)-1] is one of the most potent members of a class of chiral drug substances used to regulate the synthesis and release of histamine by the histamine H3 receptor, and as such, is an important biomarker for pharmaceutical companies conducting research in this field.", "entity1": "histamine H3 receptor", "entity2": "GT-2331", "span1": [150, 171], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14540": {"label": 3, "data": {"text": "Collectively, these results suggest that catalpol can exert inhibitory effects on the inflammatory reaction in astrocytes and that inactivation of NF-\u03baB could be the major determinant for its anti-inflammatory mechanism.", "entity1": "NF-\u03baB", "entity2": "catalpol", "span1": [147, 152], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5209": {"label": 1, "data": {"text": "No mutations in the serotonin related TPH1 and HTR1B genes in patients with monogenic sclerosing bone disorders.", "entity1": "TPH1", "entity2": "serotonin", "span1": [38, 42], "span2": [20, 29]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"591": {"label": 9, "data": {"text": "The action of 15d-PGJ2 does not appear to involve its nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) because troglitazone, a specific ligand of PPARgamma, was unable to inhibit iNOS induction, and neither troglitazone nor 15d-PGJ2 could stimulate the activity of a PPAR-dependent promoter in the absence of cotransfected PPARgamma.", "entity1": "peroxisome proliferator-activated receptor gamma", "entity2": "15d-PGJ2", "span1": [71, 119], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9433": {"label": 3, "data": {"text": "Alendronate inhibited PTPmeg1 with an IC50 value of 23 microM, PTPsigma with an IC50 value of 2 microM, and did not inhibit PTP epsilon at concentrations up to 1 mM.", "entity1": "PTPmeg1", "entity2": "Alendronate", "span1": [22, 29], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12878": {"label": 2, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "PE", "span1": [13, 19], "span2": [221, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6544": {"label": 2, "data": {"text": "Cilostazol decreases levels of serum triglycerides and causes some increase in HDL-cholesterol levels.", "entity1": "HDL", "entity2": "Cilostazol", "span1": [79, 82], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14181": {"label": 0, "data": {"text": "CBDP irreversibly inhibits butyrylcholinesterase (BChE) in human plasma by forming adducts on the active site serine (Ser-198).", "entity1": "butyrylcholinesterase", "entity2": "Ser", "span1": [27, 48], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14650": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala119Gly", "entity2": "cytarabine", "span1": [81, 90], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8710": {"label": 3, "data": {"text": "Finally, SA-induced AT1R expression was found to be prevented both by NAC and specific JNK inhibitor, SP6001325, strongly indicating that AT1R upregulation is a result of the ROS-mediated activation of the JNK signaling pathway.", "entity1": "JNK", "entity2": "SP6001325", "span1": [87, 90], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1237": {"label": 1, "data": {"text": "We report herein the location of the binding site for the inhaled anesthetic halothane at the amino acid residue level of resolution in the ligand binding cavity in a prototypical G protein-coupled receptor, bovine rhodopsin.", "entity1": "G protein-coupled receptor", "entity2": "halothane", "span1": [180, 206], "span2": [77, 86]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12666": {"label": 1, "data": {"text": "Various drugs used in the treatment of IBD, such as glucocorticoids, 5-aminosalicylic acid, and sulfasalazine, interfere with NF-kappaB/Rel signaling.", "entity1": "Rel", "entity2": "sulfasalazine", "span1": [136, 139], "span2": [96, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5582": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "fluoropyrimidine carbamate", "span1": [121, 123], "span2": [13, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5650": {"label": 3, "data": {"text": "Arsenic trioxide (As(2)O(3)), which is used to treat acute promyelocytic leukemia, can cause LQTS type 2 (LQT2) by reducing the hERG current through the diversion of hERG trafficking to the cytoplasmic membrane.", "entity1": "hERG", "entity2": "Arsenic trioxide", "span1": [128, 132], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11893": {"label": 8, "data": {"text": "Cycloxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) has been shown to be important in esophageal tumorigenesis.", "entity1": "Cycloxygenase-2", "entity2": "PGE2", "span1": [0, 15], "span2": [50, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11337": {"label": 7, "data": {"text": "In conclusion, TK and TPI effects on TP play important roles in the cytotoxic action of TAS-102, and it is possible to use the TK/TP ratio to predict more precisely individual resistance or sensitivity.", "entity1": "TP", "entity2": "TPI", "span1": [37, 39], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5289": {"label": 3, "data": {"text": "Vandetanib (Caprelsa(\u00ae), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60\u00a0% of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors.", "entity1": "tyrosine kinase", "entity2": "Vandetanib", "span1": [59, 74], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12619": {"label": 1, "data": {"text": "The EP1 receptor bound 17-phenyl-PGE2, sulprostone and iloprost in addition to PGE2 and PGE1, with Ki values of 14-36 nM.", "entity1": "EP1", "entity2": "17-phenyl-PGE2", "span1": [4, 7], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"685": {"label": 3, "data": {"text": "We evaluated the effects of angiotensin II and an angiotensin-converting enzyme inhibitor (cilazapril) on nerve blood flow (NBF) and electrophysiology in control and diabetic rats.", "entity1": "angiotensin II", "entity2": "cilazapril", "span1": [28, 42], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4555": {"label": 1, "data": {"text": "Alcohol modulates expression of DNA methyltranferases and methyl CpG-/CpG domain-binding proteins in murine embryonic fibroblasts.", "entity1": "methyl CpG-/CpG domain-binding proteins", "entity2": "Alcohol", "span1": [58, 97], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9172": {"label": 1, "data": {"text": "Phenoxybenzamine, an alpha-adrenergic antagonist containing a (chloroethyl)amine group, labels calmodulin in the presence of calcium.", "entity1": "calmodulin", "entity2": "Phenoxybenzamine", "span1": [95, 105], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15914": {"label": 4, "data": {"text": "To examine receptor mediation of estradiol effects, Ovx mice replaced for 2 days with either the ER\u03b1-selective agonist PPT or the ER\u03b2-selective agonist DPN were compared to Sham mice, and mice lacking either ER\u03b1 (\u03b1ERKO) or ER\u03b2 (\u03b2ERKO) were compared to WT littermates.", "entity1": "ER\u03b2", "entity2": "DPN", "span1": [130, 133], "span2": [152, 155]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1322": {"label": 3, "data": {"text": "The combination of nAChR and transporter inhibition produced by bupropion may contribute to its clinical efficacy as a smoking cessation agent.", "entity1": "nAChR", "entity2": "bupropion", "span1": [19, 24], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"1014": {"label": 3, "data": {"text": "Although the data collected on IGFBP-rP3 in prostate are modest, its role as a growth stimulator and/or protooncogene is supported by its preferential expression in cancerous cells and its down-regulation by atRA.", "entity1": "IGFBP-rP3", "entity2": "atRA", "span1": [31, 40], "span2": [208, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2552": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "ABL", "entity2": "imatinib mesylate", "span1": [123, 126], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14601": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "CDA", "entity2": "Ara-C", "span1": [34, 37], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13335": {"label": 1, "data": {"text": "These results suggest that the effect of fluoxetine on the expression of hSERT is post-translational and has shown itself to be independent of PKC and PKA activity.", "entity1": "hSERT", "entity2": "fluoxetine", "span1": [73, 78], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14093": {"label": 1, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "thalidomide", "span1": [179, 183], "span2": [149, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6097": {"label": 5, "data": {"text": "Pretreatment with the dopamine D1 receptor antagonist, SCH23390, and the NMDA receptor antagonist, MK-801, blocked amantadine induction of Fos in the striatum.", "entity1": "NMDA receptor", "entity2": "MK-801", "span1": [73, 86], "span2": [99, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"459": {"label": 9, "data": {"text": "These results indicate that the positive inotropic effect, mediated via (+/-)-tamsulosin- and oxymetazoline-sensitive subtype of alpha 1-adrenoceptors, is exerted by a subcellular mechanism that is independent of the accumulation of inositol phosphates.", "entity1": "alpha 1-adrenoceptors", "entity2": "inositol phosphates", "span1": [129, 150], "span2": [233, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15136": {"label": 3, "data": {"text": "A large number of aromatic/heterocyclic sulfonamides and some 5-mercapto-1,3,4-thiadiazoles were investigated as TcCA inhibitors.", "entity1": "TcCA", "entity2": "aromatic/heterocyclic sulfonamides", "span1": [113, 117], "span2": [18, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14711": {"label": 3, "data": {"text": "Furthermore, insulin-stimulated T-I cell proliferation and the expression of cell cycle regulatory proteins CDK4, CCND3 and PCNA were also blocked by rapamycin.", "entity1": "insulin", "entity2": "rapamycin", "span1": [13, 20], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"33": {"label": 9, "data": {"text": "Other agents, such as methimazole and sodium iodide, which influence thyroid cell function, do not directly interfere with the expression of M/TPO-Ag.", "entity1": "M/TPO-Ag", "entity2": "sodium iodide", "span1": [141, 149], "span2": [38, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4323": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "cyclin E", "entity2": "Pinosylvin", "span1": [157, 165], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4912": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "catalase", "entity2": "glucose", "span1": [193, 201], "span2": [276, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13088": {"label": 1, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "sulfonylurea receptor", "entity2": "glinides", "span1": [84, 105], "span2": [150, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15446": {"label": 8, "data": {"text": "This is the first study to establish the in vivo relevance of AOX in neonicotinoid metabolism in mammals and one of the first for xenobiotics in general.", "entity1": "AOX", "entity2": "neonicotinoid", "span1": [62, 65], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3429": {"label": 3, "data": {"text": "They display sensitivity to TK inhibitors, including gefitinib and erlotinib.", "entity1": "TK", "entity2": "gefitinib", "span1": [28, 30], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3057": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "CXCR4", "entity2": "AMD3100", "span1": [173, 178], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3745": {"label": 1, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "AhR", "entity2": "polycyclic aromatic hydrocarbons", "span1": [346, 349], "span2": [119, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9966": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [10, 15], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"454": {"label": 5, "data": {"text": "Pretreatment of the tissues with combined 5-HT1/5-HT2 antagonists, methysergide (1 microM) or methiothepin (0.1 microM), significantly attenuated the inhibitory effect of epinastine on the noncholinergic contraction.", "entity1": "5-HT2", "entity2": "methiothepin", "span1": [48, 53], "span2": [94, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5267": {"label": 2, "data": {"text": "Nox4 oxidase activity is thought to be constitutive and regulated at the transcriptional level; however, we challenge this point of view and suggest that specific quinone derivatives could modulate this activity.", "entity1": "Nox4", "entity2": "quinone", "span1": [0, 4], "span2": [163, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7217": {"label": 2, "data": {"text": "Cd rapidly increased c-jun, c-fos and PDGFA expression.", "entity1": "c-fos", "entity2": "Cd", "span1": [28, 33], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7053": {"label": 8, "data": {"text": "In eukaryotes, the most prominent Mo-enzymes are (1) sulfite oxidase, which catalyzes the final step in the degradation of sulfur-containing amino acids and is involved in detoxifying excess sulfite, (2) xanthine dehydrogenase, which is involved in purine catabolism and reactive oxygen production, (3) aldehyde oxidase, which oxidizes a variety of aldehydes and is essential for the biosynthesis of the phytohormone abscisic acid, and in autotrophic organisms also (4) nitrate reductase, which catalyzes the key step in inorganic nitrogen assimilation.", "entity1": "sulfite oxidase", "entity2": "sulfur", "span1": [53, 68], "span2": [123, 129]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"7105": {"label": 8, "data": {"text": "The apoptotic effect is specific for L-proline, detectable at 0.2 mM, maximal at 1 mM, and occurs during 48-72 h following the addition of L-proline to cells with maximally induced POX.", "entity1": "POX", "entity2": "L-proline", "span1": [181, 184], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11555": {"label": 1, "data": {"text": "CONCLUSIONS: We were able to demonstrate a moderate 5-HT(2A) and D(1) occupancy under clinically relevant doses of flupentixol, albeit lower than expected from in vitro data and clearly below saturation.", "entity1": "D(1)", "entity2": "flupentixol", "span1": [65, 69], "span2": [115, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6091": {"label": 2, "data": {"text": "Amantadine (1-aminoadamantane) induced Fos expression in the central, dorsal-medial and ventral-medial part of the striatum.", "entity1": "Fos", "entity2": "1-aminoadamantane", "span1": [39, 42], "span2": [12, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13731": {"label": 2, "data": {"text": "Nicotinic acid (NA), a widely used drug to lower elevated plasma lipid levels, induced NNMT enzyme activity in white adipose tissue of mice.", "entity1": "NNMT", "entity2": "NA", "span1": [87, 91], "span2": [16, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5486": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "progestagens", "span1": [68, 85], "span2": [258, 270]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3610": {"label": 1, "data": {"text": "SB365, Pulsatilla saponin D suppresses the proliferation of human colon cancer cells and induces apoptosis by modulating the AKT/mTOR signalling pathway.", "entity1": "mTOR", "entity2": "SB365", "span1": [129, 133], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11871": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "CYP1A1", "entity2": "peonidin", "span1": [150, 156], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6725": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "D-65476", "span1": [273, 279], "span2": [116, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10053": {"label": 3, "data": {"text": "Long-chain alkanols are general anesthetics which can also act as uncharged noncompetitive inhibitors of the peripheral nicotinic acetylcholine receptor (AChR) by binding to one or more specific sites on the AChR.", "entity1": "nicotinic acetylcholine receptor", "entity2": "Long-chain alkanols", "span1": [120, 152], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6262": {"label": 4, "data": {"text": "In humans, prolonged administration of the beta 2-adrenoceptor agonist terbutaline leads to a desensitization of beta 2-adrenoceptor-mediated cardiovascular responses, which can be blunted by concomitant administration of the antianaphylactic drug ketotifen.", "entity1": "beta 2-adrenoceptor", "entity2": "terbutaline", "span1": [43, 62], "span2": [71, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14890": {"label": 3, "data": {"text": "The induction of HO-1 by EIH was inhibited by SB203580 but not by SP600125, PD98059, nor LY294002.", "entity1": "HO-1", "entity2": "SB203580", "span1": [17, 21], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2698": {"label": 0, "data": {"text": "Mutation analysis of KYNU encoding kynureninase of the index case revealed homozygosity for a c.593 A > G substitution leading to a threonine-to-alanine (T198A) shift.", "entity1": "kynureninase", "entity2": "alanine", "span1": [35, 47], "span2": [145, 152]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8139": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "NADH-dehydrogenases", "entity2": "Isoproterenol", "span1": [366, 385], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5535": {"label": 5, "data": {"text": "Labeling with [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and [125I]IAS migrated at the same position on an SDS-PAGE gel as the beta 2AR labeled by the antagonist photoaffinity label [125I]iodoazidobenzylpindolol ([125I]IABP).", "entity1": "beta 2AR", "entity2": "[125I]IABP", "span1": [178, 186], "span2": [264, 274]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10208": {"label": 8, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP-B", "entity2": "BSP", "span1": [56, 62], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13525": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "2H1C class of non-heme iron enzymes", "entity2": "NO", "span1": [133, 168], "span2": [77, 79]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"969": {"label": 3, "data": {"text": "Coexpression of GRK2 or GRK2 and arrestin-2 permitted etorphine to induce down-regulation of the hkor, although expression of arrestin-2 or dynamin I alone did not.", "entity1": "hkor", "entity2": "etorphine", "span1": [97, 101], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11522": {"label": 1, "data": {"text": "Dexamethasone probes glucocorticoid receptor (GR) function, while prednisolone probes both GR and mineralocorticoid receptor (MR) function.", "entity1": "mineralocorticoid receptor", "entity2": "prednisolone", "span1": [98, 124], "span2": [66, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11263": {"label": 3, "data": {"text": "Cetrorelix completely blocked the rise of levels of the two most abundant species, 5.0 kb and 4.5 kb, of the GnRH-R mRNA, during both the infantile and the juvenile periods.", "entity1": "GnRH-R", "entity2": "Cetrorelix", "span1": [109, 115], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"613": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "AACOCF3", "span1": [178, 191], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6895": {"label": 1, "data": {"text": "[Change of dopamine transporter activity (DAT) during the action of bupropion (in depression)].", "entity1": "dopamine transporter", "entity2": "bupropion", "span1": [11, 31], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3888": {"label": 1, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "Myc", "entity2": "10074-G5", "span1": [198, 201], "span2": [75, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11608": {"label": 1, "data": {"text": "RESULTS: Eighty percent of CYP2C9*1/*1 patients stabilized on <4.0 mg/day warfarin had at least 1 VKORC1 -1639A allele.", "entity1": "CYP2C9", "entity2": "warfarin", "span1": [27, 33], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9289": {"label": 5, "data": {"text": "Intraperitoneal administration of (+/- )propranolol HCl (2.5-10 mg/kg), a nonselective beta-adrenoceptor antagonist, dose dependently attenuated the desipramine-induced enhancement of aggressive behavior without significantly affecting the basal aggressive responses.", "entity1": "beta-adrenoceptor", "entity2": "(+/- )propranolol HCl", "span1": [87, 104], "span2": [34, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9070": {"label": 1, "data": {"text": "The present study reports the in vitro binding affinities of the same compounds for muscarinic cholinergic receptors and for histamine H1 receptors in rat brain, using 3H-quinuclidinyl benzilate and 3H-mepyramine as radioligands.", "entity1": "histamine H1 receptors", "entity2": "3H-mepyramine", "span1": [125, 147], "span2": [199, 212]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14944": {"label": 1, "data": {"text": "Electron paramagnetic resonance (EPR) studies using nucleotide analog spin label probes showed that dephosphorylated myosin heads are highly ordered in the relaxed fibers and have very low ATPase activity.", "entity1": "ATPase", "entity2": "nucleotide", "span1": [189, 195], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4974": {"label": 3, "data": {"text": "Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson's disease and this Letter describes the SAR of a series of dihydropteridinone based Plk-2 inhibitors.", "entity1": "Plk-2", "entity2": "dihydropteridinone", "span1": [159, 164], "span2": [134, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4370": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "cytochrome P450 3A", "entity2": "DEX-P", "span1": [151, 169], "span2": [220, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13395": {"label": 2, "data": {"text": "Metformin and phenformin, which are biguanides, have been reported to increase AMPK activity without increasing AMP/ATP.", "entity1": "AMPK", "entity2": "biguanides", "span1": [79, 83], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15502": {"label": 4, "data": {"text": "Interestingly, following pBQN desensitization, wild-type TRPA1 had dramatically reduced response to the nonelectrophile agonist carvacrol, whereas the triple cysteine mutant TRPA1 retained its full response.", "entity1": "TRPA1", "entity2": "carvacrol", "span1": [174, 179], "span2": [128, 137]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7916": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "copper", "span1": [27, 32], "span2": [108, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13000": {"label": 3, "data": {"text": "The sordarins group are protein synthesis inhibitors that work by blocking the function of fungal translation elongation factor 2.", "entity1": "fungal translation elongation factor 2", "entity2": "sordarins", "span1": [91, 129], "span2": [4, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5828": {"label": 5, "data": {"text": "We also examined the effects of WEB 2086, a platelet-activating factor (PAF) receptor antagonist, in parallel.", "entity1": "platelet-activating factor (PAF) receptor", "entity2": "WEB 2086", "span1": [44, 85], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15664": {"label": 3, "data": {"text": "3-HPT inhibits HDAC 6 and HDAC 8 with an IC50 of 681 and 3675 nM, respectively.", "entity1": "HDAC 8", "entity2": "3-HPT", "span1": [26, 32], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3877": {"label": 2, "data": {"text": "However, combined treatment with cinobufagin and SB216367 resulted in a significant reduction in p65 and an increase in cleaved-PARP in U2OS cells.", "entity1": "PARP", "entity2": "SB216367", "span1": [128, 132], "span2": [49, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1205": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DA transporter", "entity2": "amphetamines", "span1": [149, 163], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1975": {"label": 3, "data": {"text": "SNP inhibits the accumulation of HIF-1alpha, the regulatory subunit of HIF-1, and the transcriptional activation of HIF-1alpha via a mechanism that is not dependent on either NO or soluble guanylate cyclase.", "entity1": "HIF-1alpha", "entity2": "SNP", "span1": [33, 43], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1561": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "KATI", "entity2": "KA", "span1": [88, 92], "span2": [53, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"2596": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "D(1) receptors", "entity2": "FLX", "span1": [285, 299], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14084": {"label": 3, "data": {"text": "SB203580 (a specific inhibitor of p38 kinase) markedly suppressed the increased expression of collagen type I and \u03b1-SMA in TGF-\u03b21-induced NPDFs.", "entity1": "p38", "entity2": "SB203580", "span1": [34, 37], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"536": {"label": 3, "data": {"text": "Because gastric AADC and COMT degrade levodopa, the drug is given with inhibitors of AADC (carbidopa or benserazide), and inhibitors of COMT will also enter clinical use.", "entity1": "AADC", "entity2": "carbidopa", "span1": [85, 89], "span2": [91, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6712": {"label": 3, "data": {"text": "Studies in rats, mice and monkeys show that GC-1 lowers cholesterol with 600- to 1400-fold more potency and approximately two- to threefold more efficacy than atorvastatin, a compound that blocks HMG-CoA reductase.", "entity1": "HMG-CoA reductase", "entity2": "atorvastatin", "span1": [196, 213], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5339": {"label": 1, "data": {"text": "Sphingosine-1-phosphate promotes the nuclear translocation of \u03b2-catenin and thereby induces osteoprotegerin gene expression in osteoblast-like cell lines.", "entity1": "\u03b2-catenin", "entity2": "Sphingosine-1-phosphate", "span1": [62, 71], "span2": [0, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14383": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "EGFR", "entity2": "AG1478", "span1": [17, 21], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"958": {"label": 5, "data": {"text": "In the rabbit pulmonary artery, rilmenidine and oxymetazoline are potent full agonists, whereas in the human atrial appendages they are antagonists at the alpha(2)-autoreceptors, sharing this property with rauwolscine, phentolamine, and idazoxan.", "entity1": "alpha(2)-autoreceptors", "entity2": "oxymetazoline", "span1": [155, 177], "span2": [48, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5375": {"label": 3, "data": {"text": "Rapamycin inhibits proteinase and selected peptidase activities of the catalytic core proteasome at low micromolar concentrations.", "entity1": "peptidase", "entity2": "Rapamycin", "span1": [43, 52], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15096": {"label": 3, "data": {"text": "Avibactam (formerly NXL104, AVE1330A) is a synthetic non-\u03b2-lactam, \u03b2-lactamase inhibitor that inhibits the activities of Ambler class A and C \u03b2-lactamases and some Ambler class D enzymes.", "entity1": "Ambler class D", "entity2": "AVE1330A", "span1": [164, 178], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7504": {"label": 1, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "ENaC", "entity2": "ouabain", "span1": [141, 145], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7759": {"label": 3, "data": {"text": "Rescue of both impaired extinction acquisition and deficient extinction consolidation/retrieval was achieved with prior extinction training administration of valproic acid (a GABAergic enhancer and HDAC inhibitor) or AMN082 [metabotropic glutamate receptor 7 (mGlu7) agonist], while MS-275 or PEPA (AMPA receptor potentiator) failed to affect extinction acquisition in S1 mice.", "entity1": "HDAC", "entity2": "valproic acid", "span1": [198, 202], "span2": [158, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13770": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "Sutent", "span1": [233, 246], "span2": [212, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15212": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "COX-2", "entity2": "methanol", "span1": [288, 293], "span2": [59, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4809": {"label": 3, "data": {"text": "PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency.", "entity1": "KAT II", "entity2": "PF-04859989", "span1": [113, 119], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12860": {"label": 7, "data": {"text": "Removal of Pro128 from the hepatic SDH consisting of 328 residues, which is missing in the corresponding position of the isoform consisting of 329 residues, significantly changed the Michaelis constants and Kd value for pyridoxal 5'-phosphate, whereas addition of a proline residue to the isoform was without effect.", "entity1": "SDH", "entity2": "pyridoxal 5'-phosphate", "span1": [35, 38], "span2": [220, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13817": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "kinase", "entity2": "Tarceva", "span1": [247, 253], "span2": [178, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10317": {"label": 1, "data": {"text": "Results indicate that imiquimod and resiquimod induce IFN-alpha and IFN-omega from purified pDC, and pDC are the principle IFN-producing cells in the blood.", "entity1": "IFN-alpha", "entity2": "resiquimod", "span1": [54, 63], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12252": {"label": 9, "data": {"text": "Treatment with rosiglitazone or cholestyramine had no effect on BAT activity in any subcellular compartment.", "entity1": "BAT", "entity2": "cholestyramine", "span1": [64, 67], "span2": [32, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11508": {"label": 1, "data": {"text": "BHMT is expressed at high levels in rat liver and its expression is regulated by dietary Met and choline.", "entity1": "BHMT", "entity2": "choline", "span1": [0, 4], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9010": {"label": 1, "data": {"text": "These findings suggest that limitation of SRF was produced by binding of BDZs, but not beta CCs, to voltage-dependent sodium channels and not to high affinity central BDZ receptors, and that BDZs limit SRF by slowing recovery of sodium channels from inactivation.", "entity1": "voltage-dependent sodium channels", "entity2": "BDZs", "span1": [100, 133], "span2": [73, 77]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12089": {"label": 3, "data": {"text": "), both MAO-A and MAO-B by nialamide (75 mg/kg i.p.)", "entity1": "MAO-B", "entity2": "nialamide", "span1": [18, 23], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10503": {"label": 1, "data": {"text": "The nonsteroidal anti-inflammatory drugs flurbiprofen and ibuprofen were modified in an attempt to alter the kinetics of inhibitor binding by COX-1.", "entity1": "COX-1", "entity2": "ibuprofen", "span1": [142, 147], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10112": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "COX-1", "entity2": "flurbiprofen", "span1": [18, 23], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14978": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "ATM", "entity2": "ATO", "span1": [101, 104], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10419": {"label": 3, "data": {"text": "OBJECTIVE: To determine (a) whether PDE4 inhibition alone with rolipram blocked secretions of arachidonic acid (AA) and leukotriene C(4) (LTC(4)) caused by activation of eosinophils with formyl-met-leu-phe plus cytochalasin B (FMLP/B), (b) to determine if PDE4 inhibition plus beta(2)-adrenoceptor agonist act additively to augment endogenous cAMP concentration, and (c) to determine the mechanism by which additive inhibition of AA and LTC(4) synthesis is regulated by cAMP.", "entity1": "PDE4", "entity2": "rolipram", "span1": [36, 40], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12467": {"label": 1, "data": {"text": "The DPYD-Y186C variant was unique to individuals of African ancestry, and DPD activity was 46% lower in carriers as compared with noncarriers (279\u2009\u00b1\u200935 vs. 514\u2009\u00b1\u2009168 pmol 5-FU min(-1) mg(-1); P = 0.00029).", "entity1": "Y186C", "entity2": "5-FU", "span1": [9, 14], "span2": [171, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12325": {"label": 2, "data": {"text": "It was reported previously that FVII gene (F7) expression was up-regulated by ribavirin treatment in hepatitis C virus-infected haemophilia patients; however, its precise mechanism is still unknown.", "entity1": "FVII", "entity2": "ribavirin", "span1": [32, 36], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1916": {"label": 0, "data": {"text": "We show for the first time that a single amino acid is able to determine the substrate specificity of CrAT and COT.", "entity1": "CrAT", "entity2": "amino acid", "span1": [102, 106], "span2": [41, 51]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2812": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "VEGF", "entity2": "1400W", "span1": [198, 202], "span2": [119, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"338": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "RNase A", "entity2": "2'CMP", "span1": [97, 104], "span2": [233, 238]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5696": {"label": 1, "data": {"text": "On the contrary, human TRPA1 could be concentration-dependently modulated by apomorphine.", "entity1": "human TRPA1", "entity2": "apomorphine", "span1": [17, 28], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10412": {"label": 1, "data": {"text": "Unlike OFQ II(1-17), high concentrations of its C-terminal extension, OFQ II(1-28), stimulated [35S]-GTPgammaS binding in a mu (mu) opioid receptor-like distribution and the effect was blocked by naloxone.", "entity1": "OFQ II(1-28)", "entity2": "[35S]-GTPgammaS", "span1": [70, 82], "span2": [95, 110]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6161": {"label": 1, "data": {"text": "A case of therapy-related acute myeloblastic leukemia with t(16;21)(q24;q22) after chemotherapy with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and the alkylating agent, cyclophosphamide.", "entity1": "DNA-topoisomerase II", "entity2": "cyclophosphamide", "span1": [101, 121], "span2": [188, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6489": {"label": 4, "data": {"text": "RESULTS: The alpha(2)-adrenoceptor agonists induced vasoconstriction in the porcine ciliary artery with the following potency order (EC(50)) expressed in nanomolar: brimonidine 2.11, oxymetazoline 5.26, and apraclonidine 13.0.", "entity1": "alpha(2)-adrenoceptor", "entity2": "brimonidine", "span1": [13, 34], "span2": [165, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1193": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "aminopeptidase N", "entity2": "4-methoxy-2-naphthylamide", "span1": [170, 186], "span2": [127, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6949": {"label": 3, "data": {"text": "Vitamin E supplementation was found to alter the plasma HDL-C-related factors; meanwhile, probucol supplementation was very effective in enhancing cholesterol metabolism, except for a negative effect that reduced plasma HDL-C concentration.", "entity1": "HDL", "entity2": "probucol", "span1": [220, 223], "span2": [90, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2870": {"label": 2, "data": {"text": "We also found that TRPV1 receptors are activated by CuSO(4), ZnSO(4), and FeSO(4), three salts known to produce a metallic taste sensation.", "entity1": "TRPV1", "entity2": "CuSO(4)", "span1": [19, 24], "span2": [52, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5113": {"label": 2, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "Nrf2", "entity2": "5HHMF", "span1": [93, 97], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14322": {"label": 1, "data": {"text": "In summary, DMF attenuated renal fibrosis via the Nrf2-mediated inhibition of TGF-beta/Smad3 signaling in an ARE-independent manner, suggesting that DMF could be used to treat renal fibrosis.", "entity1": "Nrf2", "entity2": "DMF", "span1": [50, 54], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5134": {"label": 3, "data": {"text": "Pyrrolidine dithiocarbamate (PDTC), a specific NF-\u03baB inhibitor, along with 20S proteasome inhibitor (PSI) significantly inhibited LPS-induced iNOS expression, which indirectly suggested that 5HHMF downregulated iNOS expression by suppressing NF-\u03baB activity.", "entity1": "NF-\u03baB", "entity2": "5HHMF", "span1": [242, 247], "span2": [191, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8262": {"label": 4, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2C", "entity2": "4-phenyl-2-N,N-dimethyl-aminotetralin", "span1": [159, 165], "span2": [110, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9144": {"label": 1, "data": {"text": "The subregion of the adenosine receptor that interacts with the N6-substituent is different for A1 and A2 receptors, particularly with respect to phenyl interactions, bulk tolerance and stereoselectivity.", "entity1": "adenosine receptor", "entity2": "N6", "span1": [21, 39], "span2": [64, 66]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12982": {"label": 8, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "DGK", "entity2": "Diacylglycerol", "span1": [132, 135], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"10014": {"label": 5, "data": {"text": "Other 5-HT3 receptor antagonists also produced such a shift in the following antagonistic-potency order: granisetron> ondansetron=AS-8112>>metoclopramide.", "entity1": "5-HT3 receptor", "entity2": "ondansetron", "span1": [6, 20], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2614": {"label": 4, "data": {"text": "The identification of the succinate receptor SUCNR1 in platelets is of particular interest, because physiologically relevant concentrations of succinate were shown to potentiate the effect of low doses of a variety of platelet agonists.", "entity1": "SUCNR1", "entity2": "succinate", "span1": [45, 51], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4622": {"label": 1, "data": {"text": "BPA induced sex-specific altered DNA methylation in specific CpG pairs in the calsequestrin 2 CpG island.", "entity1": "calsequestrin 2", "entity2": "BPA", "span1": [78, 93], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15922": {"label": 1, "data": {"text": "Taken together, the levels of plasma four FAs with shorter carbon chains were higher in pregnant mPPAR\u03b1 mice than in other genotypes, and DEHP exposure decreased these specific FA concentrations only in mPPAR\u03b1 mice, similarly to triglyceride levels.", "entity1": "mPPAR\u03b1", "entity2": "DEHP", "span1": [203, 209], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6385": {"label": 8, "data": {"text": "Ornithine decarboxylase (ODC) catalyses the first step in the synthesis of the polyamines putrescine, spermidine and spermine.", "entity1": "Ornithine decarboxylase", "entity2": "spermine", "span1": [0, 23], "span2": [117, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4655": {"label": 3, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "CYP1A1", "entity2": "delphinidin", "span1": [204, 210], "span2": [180, 191]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15039": {"label": 1, "data": {"text": "It had higher levels of oleocanthal (p-HPEA-EDA), a nutraceutical compound exerting actions against COX1 and COX2 (cycloxygenases).", "entity1": "cycloxygenases", "entity2": "oleocanthal", "span1": [115, 129], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4714": {"label": 3, "data": {"text": "Thus, the TCDD-induced reduction in canonical Wnt signaling is associated with a decrease in activators (Rspo2 and Rspo3) rather than an increase in inhibitors (Dkk1 and Dkk2) of the pathway.", "entity1": "Dkk2", "entity2": "TCDD", "span1": [170, 174], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11150": {"label": 0, "data": {"text": "Both forms of the enzyme reacted with a rabbit antibody raised to the amino-terminal peptide of the liver enzyme, suggesting that phosphodiester alpha-GlcNAcase is a type I membrane-spanning glycoprotein with its amino terminus in the lumen of the Golgi apparatus.", "entity1": "phosphodiester alpha-GlcNAcase", "entity2": "amino", "span1": [130, 160], "span2": [213, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11145": {"label": 3, "data": {"text": "We have examined the effect of dihydropyridine Ca2+-channel blockers felodipine and nicardipine on CaMPDE.", "entity1": "Ca2+-channel", "entity2": "dihydropyridine", "span1": [47, 59], "span2": [31, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8629": {"label": 2, "data": {"text": "Arsenic inhibits autophagic flux activating the Nrf2-Keap1 pathway in a p62-dependent manner.", "entity1": "Keap1", "entity2": "Arsenic", "span1": [53, 58], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13568": {"label": 1, "data": {"text": "A humanized antibody to HER2/neu, trastuzumab, is now FDA approved for the treatment of early stage, HER2/neu overexpressing breast cancer sequenced with chemotherapy including doxorubicin, cyclophosphamide, and paclitaxel.", "entity1": "neu", "entity2": "doxorubicin", "span1": [106, 109], "span2": [177, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8554": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "histone deacetylase", "entity2": "2'-aminoanilides", "span1": [159, 178], "span2": [75, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6832": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "VEGFR", "entity2": "SU11248", "span1": [338, 343], "span2": [170, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5979": {"label": 8, "data": {"text": "Tyrosinase usually catalyzes the conversion of monophenols to o-diphenols and oxidation of diphenols to the corresponding quinones.", "entity1": "Tyrosinase", "entity2": "monophenols", "span1": [0, 10], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"14578": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "P505-15", "span1": [103, 106], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13394": {"label": 2, "data": {"text": "Metformin and phenformin, which are biguanides, have been reported to increase AMPK activity without increasing AMP/ATP.", "entity1": "AMPK", "entity2": "phenformin", "span1": [79, 83], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9136": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "alkyl", "span1": [124, 136], "span2": [73, 78]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11210": {"label": 3, "data": {"text": "We conclude that erg3 can be blocked by certain antipsychotic drugs like sertindole and pimozide.", "entity1": "erg3", "entity2": "sertindole", "span1": [17, 21], "span2": [73, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6407": {"label": 2, "data": {"text": "BACKGROUND: This study examines the effects of nicorandil, a K(+) channel opener, on transmural dispersion of repolarization (TDR) and induction of torsade de pointes (TdP) under conditions mimicking the LQT1, LQT2, and LQT3 forms of the congenital long-QT syndrome (LQTS).", "entity1": "K(+) channel", "entity2": "nicorandil", "span1": [61, 73], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3158": {"label": 0, "data": {"text": "Insulin receptor substrates (IRS) serine phosphorylation is a time-controlled physiological feedback mechanism in insulin signaling that is hijacked by metabolic and inflammatory stresses to promote insulin resistance.", "entity1": "IRS", "entity2": "serine", "span1": [29, 32], "span2": [34, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3662": {"label": 3, "data": {"text": "The mRNA levels of microphthalmia-associated transcription factor (MITF) and its downstream genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 were reduced by artemisinic acid treatment.", "entity1": "microphthalmia-associated transcription factor", "entity2": "artemisinic acid", "span1": [19, 65], "span2": [172, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7569": {"label": 5, "data": {"text": "Oxybutynin (1) is a non-selective muscarinic receptor antagonist that is used clinically for the treatment of urinary incontinence.", "entity1": "muscarinic receptor", "entity2": "Oxybutynin", "span1": [34, 53], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3577": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [184, 187], "span2": [81, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8963": {"label": 1, "data": {"text": "Radioligand binding studies with the nonselective alpha 1-adrenoceptor antagonist radioligand 125I-BE2254 showed that 73-87% of the binding sites in rabbit aorta are CEC sensitive and they are predominantly low affinity sites both for WB4101 (pKd = 8.1) and for 5-methylurapidil (pKd = 7.1).", "entity1": "alpha 1-adrenoceptor", "entity2": "WB4101", "span1": [50, 70], "span2": [235, 241]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5476": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "progesterone", "span1": [106, 127], "span2": [306, 318]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5660": {"label": 2, "data": {"text": "Long-term treatment with 1 \u03bcM matrine or oxymatrine increased expression of the hERG protein and rescued the hERG surface expression disrupted by As(2)O(3).", "entity1": "hERG", "entity2": "matrine", "span1": [109, 113], "span2": [30, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"831": {"label": 3, "data": {"text": "The inhibitory effect of PGE1 or sulprostone was prevented by pretreatment with pertussis toxin [islet activating protein (IAP)] or phorbol-12-myristate-13-acetate (PMA), and the protein kinase C (PKC) inhibitor chelerythrine blocked the action of PMA.", "entity1": "PKC", "entity2": "chelerythrine", "span1": [197, 200], "span2": [212, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4921": {"label": 3, "data": {"text": "The vascular protective effects of kinsenoside were speculated to be attributed to oxidative stress inhibition and the reduction of nuclear factor kappa B (NF-\u03baB) mRNA expression levels in high glucose conditions.", "entity1": "NF-\u03baB", "entity2": "kinsenoside", "span1": [156, 161], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15447": {"label": 8, "data": {"text": "Currently, the most important insecticides are neonicotinoids, which are metabolized in vitro by AOX on reduction of the nitroimino group and by CYPs via oxidation reactions.", "entity1": "AOX", "entity2": "neonicotinoids", "span1": [97, 100], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"470": {"label": 5, "data": {"text": "(+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart.", "entity1": "alpha 1A-adrenoceptor", "entity2": "(+/-)-tamsulosin", "span1": [21, 42], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16016": {"label": 5, "data": {"text": "The involvement of the various DA receptor subtypes in the motor effects of N/OFQ and NOP receptor antagonists was evaluated pharmacologically, using D1/D5 (SCH23390), D2/D3 (raclopride, amisulpride) and D3 (S33084) receptor antagonists, and by using D2 receptor knockout mice.", "entity1": "D3", "entity2": "raclopride", "span1": [171, 173], "span2": [175, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14908": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "flavin mono-oxygenase", "entity2": "choline", "span1": [24, 45], "span2": [144, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1672": {"label": 1, "data": {"text": "The current study was performed to elucidate the possible interaction of etomidate with alpha2-adrenoceptors in mice lacking individual alpha2-adrenoceptor subtypes (alpha2-KO).", "entity1": "alpha2-adrenoceptor", "entity2": "etomidate", "span1": [136, 155], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8543": {"label": 3, "data": {"text": "Administration of bicuculline, a GABAA inhibitor, isolated a single response to \u03c9-agatoxin, which was characterized by a reduction in network activity.", "entity1": "GABAA", "entity2": "bicuculline", "span1": [33, 38], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"243": {"label": 1, "data": {"text": "The isomers of MDA produced a concentration dependent increase in phosphatidyl inositol (PI) hydrolysis at the 5-HT2A receptors, with the R(-) isomer of MDA being more potent than the S(+) at the 5-HT2A receptor.", "entity1": "5-HT2A", "entity2": "MDA", "span1": [111, 117], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6550": {"label": 0, "data": {"text": "We changed the residues to alanine using site-directed mutagenesis technique, expressed the mutants in a baculovirus/Sf9 cell system, and analyzed the kinetic characteristics of inhibition of the mutant enzymes by milrinone and cilostazol, specific inhibitors of PDE3.", "entity1": "PDE3", "entity2": "alanine", "span1": [263, 267], "span2": [27, 34]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14784": {"label": 3, "data": {"text": "Structure-based design, synthesis and evaluation of novel anthra[1,2-d]imidazole-6,11-dione derivatives as telomerase inhibitors and potential for cancer polypharmacology.", "entity1": "telomerase", "entity2": "anthra[1,2-d]imidazole-6,11-dione", "span1": [107, 117], "span2": [58, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15579": {"label": 8, "data": {"text": "Instead, radiolabeled nucleosides resulting from nuclease hydrolysis were observed.", "entity1": "nuclease", "entity2": "nucleosides", "span1": [49, 57], "span2": [22, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11518": {"label": 3, "data": {"text": "Rofecoxib only diminished COX-2 protein expression and MCP-1 gene expression in vascular atheroma.", "entity1": "MCP-1", "entity2": "Rofecoxib", "span1": [55, 60], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4822": {"label": 3, "data": {"text": "We previously employed a chemical genomic strategy to identify a novel small molecule, MAC13243, as a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.", "entity1": "bacterial lipoprotein", "entity2": "MAC13243", "span1": [126, 147], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2592": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "dopamine D(2)", "entity2": "FLX", "span1": [42, 55], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4442": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "monoamine oxidase", "entity2": "phthalimide", "span1": [128, 145], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11107": {"label": 1, "data": {"text": "Dopamine D2-receptor imaging with 123I-iodobenzamide SPECT in migraine patients abusing ergotamine: does ergotamine cross the blood brain barrier?", "entity1": "Dopamine D2-receptor", "entity2": "123I-iodobenzamide", "span1": [0, 20], "span2": [34, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12001": {"label": 1, "data": {"text": "Our previous results showed that methylphenidate treatment in adolescent SHR enhanced cocaine self-administration during adulthood, and alterations in DAT function in prefrontal cortex play a role in this response.", "entity1": "DAT", "entity2": "methylphenidate", "span1": [151, 154], "span2": [33, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3011": {"label": 1, "data": {"text": "Eprosartan acts at vascular AT1 receptors (postsynaptically) and at presynaptic AT1 receptors, where it inhibits noradrenaline release.", "entity1": "AT1 receptors", "entity2": "Eprosartan", "span1": [28, 41], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2307": {"label": 2, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "JNK", "entity2": "YC-1", "span1": [158, 161], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3574": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [53, 56], "span2": [240, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7424": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "D6D", "entity2": "DHA", "span1": [31, 34], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3923": {"label": 3, "data": {"text": "Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group facilitates both enhancement of PDE4-inhibitory activity and restoration of potent PDE3 inhibition.", "entity1": "PDE4", "entity2": "N", "span1": [115, 119], "span2": [69, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6089": {"label": 2, "data": {"text": "Amantadine induces c-fos in rat striatum: reversal with dopamine D1 and NMDA receptor antagonists.", "entity1": "c-fos", "entity2": "Amantadine", "span1": [19, 24], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4658": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor-\u03b1 (PPAR\u03b1) activation mimicked the effects of resveratrol while PPAR\u03b1 inhibition prevented the effects of this SIRT1 activator.", "entity1": "SIRT1", "entity2": "resveratrol", "span1": [153, 158], "span2": [88, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"621": {"label": 3, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "p-bromophenacyl bromide", "span1": [102, 115], "span2": [28, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3705": {"label": 9, "data": {"text": "The exposure of highly toxic aconitine does not significantly impact the activity and expression of cytochrome P450 3A in rats determined by a novel ultra performance liquid chromatography-tandem mass spectrometric method of a specific probe buspirone.", "entity1": "cytochrome P450 3A", "entity2": "aconitine", "span1": [100, 118], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4498": {"label": 9, "data": {"text": "Valproate-\u03b2-d-glucuronide and CGP 47292-\u03b2-d-glucuronide did not inhibit either hCES.", "entity1": "hCES", "entity2": "CGP 47292-\u03b2-d-glucuronide", "span1": [79, 83], "span2": [30, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3325": {"label": 2, "data": {"text": "Apoptosis studies (DAPI staining and caspase 3 activity) showed a marked increase in the presence of MXF and VP-16 compared to VP-16 alone.", "entity1": "caspase 3", "entity2": "VP-16", "span1": [37, 46], "span2": [109, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10911": {"label": 9, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "gastric mucin", "entity2": "PD98059", "span1": [4, 17], "span2": [224, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10045": {"label": 3, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "phosphoenolpyruvate carboxykinase", "entity2": "Fenofibrate", "span1": [136, 169], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15299": {"label": 3, "data": {"text": "The most potent compound 5 (HJC0123) has demonstrated to inhibit STAT3 promoter activity, downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values.", "entity1": "STAT3", "entity2": "HJC0123", "span1": [122, 127], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"785": {"label": 3, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "lipoxygenase", "entity2": "NDGA", "span1": [241, 253], "span2": [232, 236]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4350": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "BMP4", "entity2": "pinosylvin", "span1": [250, 254], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1100": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "tacrine", "span1": [51, 71], "span2": [111, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3371": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.2", "entity2": "dihydropyridine", "span1": [71, 79], "span2": [101, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4962": {"label": 2, "data": {"text": "Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo.", "entity1": "PXR", "entity2": "Amprenavir", "span1": [33, 36], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2835": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "amino acid", "span1": [83, 99], "span2": [12, 22]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"363": {"label": 1, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2R alpha", "entity2": "GCS", "span1": [110, 121], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1613": {"label": 3, "data": {"text": "Inhibition of GluR5 kainate receptors could represent a key mechanism underlying the anticonvulsant activity of topiramate.", "entity1": "GluR5", "entity2": "topiramate", "span1": [14, 19], "span2": [112, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2790": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "SP", "entity2": "NaHS", "span1": [213, 215], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5231": {"label": 1, "data": {"text": "OBJECTIVETo describe and make available an interactive, 24-variable homeostasis model assessment (iHOMA2) that extends the HOMA2 model, enabling the modeling of physiology and treatment effects, to present equations of the HOMA2 and iHOMA2 models, and to exemplify iHOMA2 in two widely differing scenarios: changes in insulin sensitivity with thiazolidinediones and changes in renal threshold with sodium glucose transporter (SGLT2) inhibition.RESEARCH DESIGN AND METHODSiHOMA2 enables a user of the available software to examine and modify the mathematical functions describing the organs and tissues involved in the glucose and hormonal compartments.", "entity1": "SGLT2", "entity2": "thiazolidinediones", "span1": [426, 431], "span2": [343, 361]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2947": {"label": 0, "data": {"text": "The results quantify the role of PDE5 catalytic-site residues for cGMP and inhibitors, indicate that Tyr-612, Gln-817, and Phe-820 are the most important cGMP or inhibitor contacts studied, and identify residues that contribute to selectivity among different classes of inhibitors.", "entity1": "PDE5", "entity2": "Tyr", "span1": [33, 37], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"47": {"label": 3, "data": {"text": "The effects of two reversible, predominantly monoamine oxidase-A (MAO-A) inhibitors, moclobemide (150 mg three times daily) and toloxatone (400-200-400 mg day-1) on monoamine metabolites and psychometric performance were compared in a double-blind placebo controlled crossover study in 12 healthy subjects.", "entity1": "monoamine oxidase-A", "entity2": "moclobemide", "span1": [45, 64], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1565": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "kynurenine aminotransferase I", "entity2": "oxoglutaramic acid", "span1": [57, 86], "span2": [156, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"11934": {"label": 1, "data": {"text": "To further our understanding of how fisetin negatively regulates mTORC1 signaling, we analyzed the phosphorylation of S6K1, mTOR and Akt in fisetin-treated TSC2-knockdown cells.", "entity1": "S6K1", "entity2": "fisetin", "span1": [118, 122], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11783": {"label": 3, "data": {"text": "There was no significant difference in TLR4, NF-\u03baB, and IL-27 mRNA and proteins between curcumin-treated and sulfasalazine-treated groups.", "entity1": "IL-27", "entity2": "sulfasalazine", "span1": [56, 61], "span2": [109, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2591": {"label": 5, "data": {"text": "The concomitant application of subconvulsive dose of pentetrazole (55.0 mg/kg) with low dose of flumazenil (5.0 mg/kg) - a BDZ receptor antagonist, immediately induced BDZ withdrawal signs in these animals.", "entity1": "BDZ receptor", "entity2": "flumazenil", "span1": [123, 135], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5146": {"label": 8, "data": {"text": "It has been claimed that hCTR1, the human high affinity copper transporter, is the major entry pathway for cDDP and related drugs via a mechanism that mimics copper.", "entity1": "human high affinity copper transporter", "entity2": "cDDP", "span1": [36, 74], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5632": {"label": 3, "data": {"text": "AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C.\tWe investigated the effect of compound C, a well-known inhibitor of the intracellular energy sensor AMP-activated protein kinase (AMPK), on proliferation and viability of human U251 and rat C6 glioma cell lines.", "entity1": "AMP-activated protein kinase", "entity2": "compound C", "span1": [220, 248], "span2": [150, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13019": {"label": 8, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "PLC-beta", "entity2": "inositol phosphate", "span1": [187, 195], "span2": [250, 268]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3853": {"label": 3, "data": {"text": "Nanobody-albumin nanoparticles (NANAPs) for the delivery of a multikinase inhibitor 17864 to EGFR overexpressing tumor cells.", "entity1": "multikinase", "entity2": "17864", "span1": [62, 73], "span2": [84, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11739": {"label": 1, "data": {"text": "GABA type A receptors (GABA(A)-R) are important for ethanol actions and it is of interest to link individual subunits with specific ethanol behaviors.", "entity1": "GABA type A receptors", "entity2": "ethanol", "span1": [0, 21], "span2": [52, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5227": {"label": 2, "data": {"text": "In addition, vinblastine induces the DNA-binding activities of the transcription factor NF-\u03baB, HSF1, AP-1, and ATF-2, together with the expression of HSP70 and Bax proteins.", "entity1": "HSP70", "entity2": "vinblastine", "span1": [150, 155], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14808": {"label": 2, "data": {"text": "Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist \u0394(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054.", "entity1": "CB(1)", "entity2": "AM4054", "span1": [52, 57], "span2": [22, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10548": {"label": 2, "data": {"text": "RA is known to induce expression of the Burkitt's lymphoma receptor 1 (BLR1) gene which propels RA-induced cell cycle arrest and differentiation of HL-60 human myeloblastic leukemia cells, motivating the present analysis of transcriptional regulation of blr1 expression by RA.", "entity1": "blr1", "entity2": "RA", "span1": [254, 258], "span2": [273, 275]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6706": {"label": 3, "data": {"text": "The inhibitory effects of tranylcypromine, a nonselective irreversible inhibitor of monoamine oxidase (MAO), on three cytochrome P450 (CYP) enzymes, namely CYP2C9, CYP2C19, and CYP2D6, have been evaluated in vitro.", "entity1": "monoamine oxidase", "entity2": "tranylcypromine", "span1": [84, 101], "span2": [26, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10939": {"label": 3, "data": {"text": "Therefore, decreases of PLK and PNPO in the hippocampal CA1 region of aged brains may be involved in aging processes related with gamma-aminobutyric acid (GABA) function.", "entity1": "PNPO", "entity2": "gamma-aminobutyric acid", "span1": [32, 36], "span2": [130, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11781": {"label": 3, "data": {"text": "There was no significant difference in TLR4, NF-\u03baB, and IL-27 mRNA and proteins between curcumin-treated and sulfasalazine-treated groups.", "entity1": "TLR4", "entity2": "sulfasalazine", "span1": [39, 43], "span2": [109, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3710": {"label": 2, "data": {"text": "Nitrogen-containing bisphosphonates induce apoptosis of hematopoietic tumor cells via inhibition of Ras signaling pathways and Bim-mediated activation of the intrinsic apoptotic pathway.", "entity1": "Bim", "entity2": "Nitrogen", "span1": [127, 130], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8996": {"label": 1, "data": {"text": "No effect of ethanol on blood or brain levels of [3H]R-PIA was noted and sufficient amount of the latter entered the brain to suggest adenosine receptor activation adequate to produce behavioral interaction with ethanol.", "entity1": "adenosine receptor", "entity2": "ethanol", "span1": [134, 152], "span2": [212, 219]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"1963": {"label": 3, "data": {"text": "These findings suggest that the anti-allodynia effect of CP-101,606 is ascribable to blockade of NR2B receptors at the brain, but not at the spinal cord.", "entity1": "NR2B", "entity2": "CP-101,606", "span1": [97, 101], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10993": {"label": 3, "data": {"text": "Tyrosine kinase inhibitors are quinazoline-derived, low molecular weight synthetic molecules that can block the intracellular tyrosine kinase domain of several receptors, including EGFR, Erb2, and vascular endothelial growth factor receptor, and thereby inhibit ligand-induced receptor phosphorylation and abrogate the biologic effect of EGFR signaling.", "entity1": "Erb2", "entity2": "quinazoline", "span1": [187, 191], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"544": {"label": 9, "data": {"text": "Interestingly, venlafaxine, a dual 5-HT and norepinephrine reuptake inhibitor, displayed only a moderate affinity for the 5-HT transporter (Ki = 74 nM) and a very low affinity for the norepinephrine transporter (Ki = 1.26 microM).", "entity1": "norepinephrine transporter", "entity2": "venlafaxine", "span1": [184, 210], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12637": {"label": 1, "data": {"text": "The sulfonylurea glibenclamide caused release of prebound 8-azido-[alpha-32P]ATP from SUR1 in the presence of MgADP or MgATP in a concentration-dependent manner.", "entity1": "SUR1", "entity2": "8-azido-[alpha-32P]ATP", "span1": [86, 90], "span2": [58, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9344": {"label": 5, "data": {"text": "Kainate-evoked currents showed partial desensitization that was reduced on incubation with concanavalin A (conA) but not cyclothiazide and were attenuated by the non-N-methyl-D-aspartate (NMDA) receptor antagonist CNQX (6-cyano-7-nitro-quinoxalinedione).", "entity1": "N-methyl-D-aspartate (NMDA) receptor", "entity2": "6-cyano-7-nitro-quinoxalinedione", "span1": [166, 202], "span2": [220, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10885": {"label": 1, "data": {"text": "Affinity chromatography investigations have shown that (R)-roscovitine also interacts with PDXK.", "entity1": "PDXK", "entity2": "(R)-roscovitine", "span1": [91, 95], "span2": [55, 70]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3752": {"label": 3, "data": {"text": "The pretreatment with 20\u00a0mg\u2009L(-1) La(III) could alleviate the effects of UV-B radiation on the activities of nitrate reductase, glutamine synthetase, glutamate synthase, and glutamate dehydrogenase, promoting amino acid conversion and protein synthesis in soybean seedlings.", "entity1": "glutamine synthetase", "entity2": "La(III)", "span1": [128, 148], "span2": [34, 41]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"9271": {"label": 1, "data": {"text": "Saturation experiments showed that [3H]prazosin labelled a single population of binding sites in the spleen (alpha 1B) and hippocampus (alpha 1A and alpha 1B) (dissociation constants (KD): 0.26 nM and 0.14 nM respectively).", "entity1": "alpha 1A", "entity2": "[3H]prazosin", "span1": [136, 144], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2556": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "kinase", "entity2": "imatinib mesylate", "span1": [55, 61], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14756": {"label": 1, "data": {"text": "These data suggest that jaceosidin, isolated from Japanese mugwort, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells.", "entity1": "ERK", "entity2": "jaceosidin", "span1": [82, 85], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13003": {"label": 1, "data": {"text": "We show here that IP1 can be used as a surrogate of IP3 to monitor GPCR activation.", "entity1": "GPCR", "entity2": "IP3", "span1": [67, 71], "span2": [52, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9127": {"label": 1, "data": {"text": "This interaction was found to be similar in some respects to the interaction between phenothiazines and calmodulin.", "entity1": "calmodulin", "entity2": "phenothiazines", "span1": [104, 114], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15309": {"label": 1, "data": {"text": "Hyperthyroidism-induced oxidative stress, reduction in cytochrome c oxidase activity, and myocardial ATP concentration were also significantly checked by Bzf.", "entity1": "cytochrome c oxidase", "entity2": "Bzf", "span1": [55, 75], "span2": [154, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2178": {"label": 0, "data": {"text": "Collectively, these results suggest that besides its classical proteolytic activity, tPA acts as a cytokine that binds to the cell membrane receptor LRP-1, induces its tyrosine phosphorylation, and triggers intracellular signal transduction, thereby inducing specific gene expression in renal interstitial fibroblasts.", "entity1": "LRP-1", "entity2": "tyrosine", "span1": [149, 154], "span2": [168, 176]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7603": {"label": 5, "data": {"text": "In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use.", "entity1": "OT", "entity2": "Tractocile", "span1": [243, 245], "span2": [232, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6621": {"label": 0, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "Glu", "span1": [3, 9], "span2": [101, 104]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10243": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "spermidine/spermine N(1)-acetyltransferase", "entity2": "spermidine", "span1": [77, 119], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5680": {"label": 3, "data": {"text": "We demonstrate that HZ mice are significantly more sensitive to local AChE inhibition (BW284c51), but remain insensitive to butyrylcholinesterase (BuChE) inhibition (bambuterol).", "entity1": "BuChE", "entity2": "bambuterol", "span1": [147, 152], "span2": [166, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15150": {"label": 2, "data": {"text": "The mRNA level for nestin (Nes, biomarker for stem Leydig cells) was significantly increased in the control testis on day 4 post-EDS, but not in the DEHP treated testes, suggesting that these nestin positive stem cells were differentiated into progenitor Leydig cells in the DEHP-treated testes.", "entity1": "nestin", "entity2": "EDS", "span1": [19, 25], "span2": [129, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7342": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SLC1", "entity2": "alanine", "span1": [190, 194], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11597": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "cystathionine-gamma-lyase", "entity2": "H(2)S", "span1": [75, 100], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11841": {"label": 1, "data": {"text": "The baseline HbA1c and glycated albumin levels were identified as factors that predicted the response to add-on therapy with sitagliptin.", "entity1": "glycated albumin", "entity2": "sitagliptin", "span1": [23, 39], "span2": [125, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"549": {"label": 1, "data": {"text": "Interestingly, venlafaxine, a dual 5-HT and norepinephrine reuptake inhibitor, displayed only a moderate affinity for the 5-HT transporter (Ki = 74 nM) and a very low affinity for the norepinephrine transporter (Ki = 1.26 microM).", "entity1": "5-HT transporter", "entity2": "venlafaxine", "span1": [122, 138], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5539": {"label": 1, "data": {"text": "Labeling with [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and [125I]IAS migrated at the same position on an SDS-PAGE gel as the beta 2AR labeled by the antagonist photoaffinity label [125I]iodoazidobenzylpindolol ([125I]IABP).", "entity1": "beta 2AR", "entity2": "(-)-alprenolol", "span1": [178, 186], "span2": [51, 65]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11914": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "TAGs", "span1": [174, 179], "span2": [61, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1236": {"label": 1, "data": {"text": "Radiosequence analysis of [(14)C]halothane-labeled rhodopsin revealed that halothane contacts an amino acid residue (Trp265) lining the ligand binding cavity in the transmembrane core of the receptor.", "entity1": "rhodopsin", "entity2": "[(14)C]halothane", "span1": [51, 60], "span2": [26, 42]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13836": {"label": 6, "data": {"text": "The recently discovered hyperinsulinism/hyperammonemia disorder showed that the loss of allosteric inhibition of GDH by GTP causes excessive secretion of insulin.", "entity1": "GDH", "entity2": "GTP", "span1": [113, 116], "span2": [120, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"13538": {"label": 1, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha2", "entity2": "5,8,11,14-eicosatetraynoic acid", "span1": [188, 198], "span2": [100, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"150": {"label": 3, "data": {"text": "CRH caused a rise in plasma ACTH after both loperamide (from 30 +/- 16.6 to a peak of 108 +/- 31 pmol/l) and placebo (from 98.5 +/- 47 to 211 +/- 61.7 pmol/l): the interaction between treatments and time was significant, and the first phase of CRH-induced ACTH secretion was significantly lower after loperamide.", "entity1": "ACTH", "entity2": "loperamide", "span1": [256, 260], "span2": [301, 311]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11808": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "c-fos", "entity2": "PhIP", "span1": [124, 129], "span2": [63, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"442": {"label": 1, "data": {"text": "Epinastine (WAL 801CL) is an antihistaminic drug with binding affinity at certain other receptors, including alpha-adrenergic receptors and various serotonin (5-HT) receptor subtypes.", "entity1": "serotonin (5-HT) receptor", "entity2": "Epinastine", "span1": [148, 173], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6647": {"label": 5, "data": {"text": "However, other alpha(1)-adrenoceptor antagonists (tamsulosin, WB4101 and corynanthine) did not inhibit the binding at a range of concentrations that generally exhibit alpha(1)-adrenoceptor antagonism, and noradrenaline, rauwolscine and propranolol were without effect on the [(3)H]prazosin binding.", "entity1": "alpha(1)-adrenoceptor", "entity2": "WB4101", "span1": [15, 36], "span2": [62, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8960": {"label": 1, "data": {"text": "Computer-assisted analysis of these curvilinear Schild plots in a two-receptor system indicated that alpha 1-adrenoceptor populations responsible for the constrictive response are predominantly (approximately 80-90%) low affinity sites for the two antagonists (pKd approximately 8.1 for WB4101 and pKd approximately 7.1 for 5-methyl-urapidil) and a small population (approximately 10-20%) are high affinity sites (pKd approximately 9.1 for both WB4101 and 5-methyl-urapidil), which was in good agreement with radioligand binding studies.", "entity1": "alpha 1-adrenoceptor", "entity2": "5-methyl-urapidil", "span1": [101, 121], "span2": [456, 473]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12681": {"label": 3, "data": {"text": "Rofecoxib has greater selectivity for COX-2 than celecoxib, meloxicam, diclofenac and indomethacin.", "entity1": "COX-2", "entity2": "Rofecoxib", "span1": [38, 43], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2907": {"label": 3, "data": {"text": "In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors.", "entity1": "COX-2", "entity2": "acetaminophen", "span1": [58, 63], "span2": [34, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3427": {"label": 1, "data": {"text": "The T790M mutation increases the ATP affinity of the G719S mutant, explaining the acquired drug resistance of the double mutant.", "entity1": "G719S", "entity2": "ATP", "span1": [53, 58], "span2": [33, 36]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6505": {"label": 3, "data": {"text": "Pemetrexed disodium (ALIMTA) is a novel antimetabolite that inhibits at least three folate-dependent enzymes, thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase.", "entity1": "glycinamide ribonucleotide formyltransferase", "entity2": "ALIMTA", "span1": [161, 205], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12236": {"label": 1, "data": {"text": "Photolytic release of free alanine results in the generation of significant transient current components in HEK293 cells expressing the ASCT2, SNAT1, and SNAT2 proteins.", "entity1": "SNAT2", "entity2": "alanine", "span1": [154, 159], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"815": {"label": 1, "data": {"text": "SC-51089 (10(-5) M), a selective EP1-receptor antagonist, showed no effect on the PGE1- or PGE2-induced inhibition of the HVA ICa, thereby indicating that PGE1- and PGE2-induced inhibition of the HVA Ca2+ channels is possibly mediated by the EP3 receptor.", "entity1": "EP3 receptor", "entity2": "PGE2", "span1": [242, 254], "span2": [165, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10038": {"label": 2, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "enoyl-CoA hydratase", "entity2": "Fenofibrate", "span1": [79, 98], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1634": {"label": 2, "data": {"text": "CONCLUSION: A long-term intake of ethanol solution down-regulates the phosphorylation of CREB in the nucleus accumbens, and those changes can be reversed by naloxone, which may be one kind of the molecular mechanisms associated with ethanol dependence.", "entity1": "CREB", "entity2": "naloxone", "span1": [89, 93], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7106": {"label": 3, "data": {"text": "The exception was bupropion, a dual norepinephrine transporter/dopamine transporter blocker, which tended to increase spontaneous locomotor activity.", "entity1": "norepinephrine transporter", "entity2": "bupropion", "span1": [36, 62], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1437": {"label": 3, "data": {"text": "Low levels of serotonin may reduce the density of the serotonin transporter (SERT) by either increasing trafficking or reducing synthesis; a \"neuroadaptive response\".", "entity1": "serotonin transporter", "entity2": "serotonin", "span1": [54, 75], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4465": {"label": 3, "data": {"text": "Catalpol reduced the expression of pro-inflammatory mediates, such as monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-\u03b1 (TNF-\u03b1), inducible NO synthase (iNOS), and receptor for AGE (RAGE).", "entity1": "MCP-1", "entity2": "Catalpol", "span1": [102, 107], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10116": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "COX-1", "entity2": "ketrolack", "span1": [18, 23], "span2": [66, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5482": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "levonorgestrel", "span1": [68, 85], "span2": [125, 139]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1753": {"label": 3, "data": {"text": "Increased phosphorylation of p95ErbB2 and AKT in response to HRG was abrogated to varying degrees by GW572016.", "entity1": "AKT", "entity2": "GW572016", "span1": [42, 45], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2863": {"label": 8, "data": {"text": "4-Hydroxynonenal (4-HNE) is a mutagenic alpha,beta-unsaturated aldehyde produced during oxidative injury that is conjugated by several glutathione S-transferase (GST) isoforms.", "entity1": "GST", "entity2": "4-Hydroxynonenal", "span1": [162, 165], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11951": {"label": 8, "data": {"text": "UGT1A6 exhibited a significantly higher Vmax and Km values toward both HFC and UDP-glucuronic acid than the other UGTs.", "entity1": "UGTs", "entity2": "HFC", "span1": [114, 118], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6790": {"label": 3, "data": {"text": "CONCLUSIONS AND CLINICAL RELEVANCE: Canine COX-2 was selectively inhibited by etodolac, nimesulide, and NS398; tolfenamic acid and carprofen also appeared to be preferential COX-2 inhibitors in dogs.", "entity1": "Canine COX-2", "entity2": "etodolac", "span1": [36, 48], "span2": [78, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12432": {"label": 8, "data": {"text": "Metabolism of Beclomethasone Dipropionate by Cytochrome P450 3A Enzymes.", "entity1": "Cytochrome P450 3A", "entity2": "Beclomethasone Dipropionate", "span1": [45, 63], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6594": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "5-HT(2A)", "entity2": "ziprasidone", "span1": [232, 240], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7643": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "probenecid", "span1": [34, 39], "span2": [324, 334]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14667": {"label": 1, "data": {"text": "Inhibition of PKA significantly attenuated the effect of genistein on thrombin-induced EC permeability, MLC phosphorylation, and RhoA membrane translocation in ECs.", "entity1": "MLC", "entity2": "genistein", "span1": [104, 107], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14231": {"label": 8, "data": {"text": "Modulation of the nitric oxide producing system (demonstrated via the NADPH-diaphorase histochemical reaction) by oestradiol has been established in several structures of the rat brain.", "entity1": "NADPH-diaphorase", "entity2": "nitric oxide", "span1": [70, 86], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9514": {"label": 5, "data": {"text": "The present study describes the characterization of the binding properties and autoradiographic distribution of a new nonpeptide antagonist of neurotensin receptors, [3H]SR 142948A (2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methyl carbamoyl)-2-isopropylphenyl)-1H-pyrazole-3-carbonyl]-amino]-ad amantane-2-carboxylic acid, hydrochloride), in the rat brain.", "entity1": "neurotensin receptors", "entity2": "2-[[5-(2,6-dimethoxyphenyl)-1-(4-(N-(3-dimethylaminopropyl)-N-methyl carbamoyl)-2-isopropylphenyl)-1H-pyrazole-3-carbonyl]-amino]-ad amantane-2-carboxylic acid, hydrochloride", "span1": [143, 164], "span2": [182, 356]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9082": {"label": 2, "data": {"text": "The order of effect was 4HPR greater than ROAc greater than 13cisRA, with increases in prothrombin times correlating with increases in hemorrhagic deaths.", "entity1": "prothrombin", "entity2": "13cisRA", "span1": [87, 98], "span2": [60, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1802": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "OSI-774", "span1": [0, 32], "span2": [153, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2705": {"label": 3, "data": {"text": "Sitagliptin, an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, improves glycaemic control by inhibiting DPP-4 inactivation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.", "entity1": "dipeptidyl peptidase-4", "entity2": "Sitagliptin", "span1": [21, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14166": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "heme oxygenase 1", "entity2": "chalcones", "span1": [43, 59], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13272": {"label": 8, "data": {"text": "CONCLUSION: In postmenopausal women, isolated isoflavone treatment does not affect ABCA1-dependent cholesterol efflux potential from macrophages but increases circulating pre-beta high-density lipoprotein level, which could provide beneficial vascular effects.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [83, 88], "span2": [99, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11348": {"label": 3, "data": {"text": "Block of human NaV1.5 sodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin.", "entity1": "human NaV1.5", "entity2": "phenytoin", "span1": [9, 21], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4567": {"label": 4, "data": {"text": "Adenosine and N(6)-cyclopentyl-adenosine (CPA, A1R agonist) constricted MVs but not MAs.", "entity1": "A1R", "entity2": "Adenosine", "span1": [47, 50], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6691": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "TRPM8", "entity2": "menthol", "span1": [0, 5], "span2": [88, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6897": {"label": 3, "data": {"text": "Bupropion has an antidepressant effect through blocking the dopamine transporter.", "entity1": "dopamine transporter", "entity2": "Bupropion", "span1": [60, 80], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13424": {"label": 9, "data": {"text": "TGF-beta1 and high D-glucose increased hCAT-1 mRNA expression ( approximately 8-fold) and maximal transport velocity (V(max)), L-[(3)H]citrulline formation from L-[(3)H]arginine (index of NO synthesis) and endothelial NO synthase (eNOS) protein abundance, but did not alter eNOS phosphorylation.", "entity1": "eNOS", "entity2": "L-[(3)H]arginine", "span1": [274, 278], "span2": [161, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"423": {"label": 1, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "RS 17053", "span1": [258, 286], "span2": [71, 79]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14236": {"label": 1, "data": {"text": "Verrucarin A sensitizes TRAIL-induced apoptosis via the upregulation of DR5 in an eIF2\u03b1/CHOP-dependent manner.", "entity1": "TRAIL", "entity2": "Verrucarin A", "span1": [24, 29], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4399": {"label": 0, "data": {"text": "The M6P (mannose 6-phosphate)/IGF2R (insulin-like growth factor II receptor) interacts with a variety of factors that impinge on tumour invasion and metastasis.", "entity1": "insulin-like growth factor II receptor", "entity2": "M6P", "span1": [37, 75], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14158": {"label": 4, "data": {"text": "The mianserin analogue mirtazapine also displayed kappa-opioid agonist activity.", "entity1": "kappa-opioid", "entity2": "mirtazapine", "span1": [50, 62], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9413": {"label": 4, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT4", "entity2": "benzamide", "span1": [142, 147], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3291": {"label": 8, "data": {"text": "Prednisolone also inhibited ACTH and cortisol secretion in response to exogenous CRH stimulation, inferring rapid feedback inhibition at the anterior pituitary.", "entity1": "CRH", "entity2": "cortisol", "span1": [81, 84], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13499": {"label": 5, "data": {"text": "An investigation of the absolute configuration of the potent histamine H3 receptor antagonist GT-2331 using vibrational circular dichroism.", "entity1": "histamine H3 receptor", "entity2": "GT-2331", "span1": [61, 82], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14746": {"label": 2, "data": {"text": "Furthermore, we found that arsenic trioxide activates the Pirh2 promoter and consequently induces Pirh2 expression.", "entity1": "Pirh2 promoter", "entity2": "arsenic trioxide", "span1": [58, 72], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8605": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "AST", "entity2": "TAA", "span1": [31, 34], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13478": {"label": 9, "data": {"text": "This report reviews published and unpublished data that suggest that aripiprazole acts as a selective partial agonist at the dopamine D(2) receptor and does not affect 5-HT receptors at therapeutic doses.", "entity1": "5-HT receptors", "entity2": "aripiprazole", "span1": [168, 182], "span2": [69, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6093": {"label": 3, "data": {"text": "Pretreatment with the dopamine D1 receptor antagonist, SCH23390, and the NMDA receptor antagonist, MK-801, blocked amantadine induction of Fos in the striatum.", "entity1": "Fos", "entity2": "SCH23390", "span1": [139, 142], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11984": {"label": 8, "data": {"text": "6-DHSG was metabolised by GSH to form a GSH conjugate (GS-6-DHSG) in RAW 264.7 cells, via a potential mechanism involving the catalytic activity of glutathione-S-transferase (GST).", "entity1": "glutathione-S-transferase", "entity2": "GS-6-DHSG", "span1": [148, 173], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3472": {"label": 3, "data": {"text": "In mechanistic studies, Silibinin decreased the protein level of p34cdc2, which might be the possible molecular mechanism of Silibinin efficacy on the growth inhibition in SGC-7901 cells.", "entity1": "p34cdc2", "entity2": "Silibinin", "span1": [65, 72], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8658": {"label": 2, "data": {"text": "The expression kinetics of TAp63, c-Abl and TAp73 suggest that cisplatin activates TAp63-dependent expression of c-Abl and TAp73 and, in turn, the activation of TAp73 by c-Abl-induced BAX expression.", "entity1": "TAp63", "entity2": "cisplatin", "span1": [83, 88], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5168": {"label": 8, "data": {"text": "At a substrate concentration of 20\u2009\u00b5M, the most active HFC glucuronidation catalysts were UGT1A10 followed by UGT1A6 >UGT1A7 >UGT2A1, whereas at 300\u2009\u00b5M UGT1A6 was about 10 times better catalyst than the other recombinant UGTs.", "entity1": "UGT1A6", "entity2": "HFC", "span1": [152, 158], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"13914": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "K(ATP)", "entity2": "Phenformin", "span1": [62, 68], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8662": {"label": 2, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [101, 106], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4286": {"label": 3, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "GSK3\u03b2", "entity2": "MG132", "span1": [69, 74], "span2": [35, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2717": {"label": 1, "data": {"text": "The in vivo effects of the non-steroid anti-inflammatory drug (NSAID) amtolmetin guacyl, a pro-drug of the NSAID tolmetin, on lipid peroxidation, glutathione levels and activity of antioxidant enzymes (superoxide dismutase, catalase, glutathione peroxidase and glutathione reductase) in rat gastric mucosa, colon mucosa and liver, were compared with the effects of non-selective (indomethacin, diclofenac) and COX-2 selective (celecoxib) NSAIDs.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [410, 415], "span2": [427, 436]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14875": {"label": 2, "data": {"text": "Additionally, in SH-SY5Y cells, MPP(+)-induced demethylation of phosphoprotein phosphatase 2A (PP2A), the master regulator of the cellular phosphoregulatory network, and cytotoxicity were ameliorated by EHT.", "entity1": "phosphoprotein phosphatase 2A", "entity2": "EHT", "span1": [64, 93], "span2": [203, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1391": {"label": 3, "data": {"text": "Similar to gemfibrozil, clofibrate, another fibrate drug, also inhibited the expression of iNOS.", "entity1": "iNOS", "entity2": "fibrate", "span1": [91, 95], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"796": {"label": 1, "data": {"text": "Specifically, aniracetam, which potentiates wild-type AMPAAMPA receptors, is ineffective on the non-desensitizing GluR3(L507Y) mutant, but has synergistic effects with lithium on wild-type receptors.", "entity1": "AMPA receptors", "entity2": "AMPA", "span1": [58, 72], "span2": [54, 58]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2540": {"label": 8, "data": {"text": "Polyclonal antisera to either b5R or cyt b5 significantly inhibited N-hydroxy-4-aminobiphenyl (NHOH-4-ABP) reduction by 95 and 89%, respectively, and immunoreactive cyt b5 protein content in individual HLM was significantly correlated with individual reduction of both NHOH-4-ABP and N-hydroxy-PhIP (NHOH-PhIP).", "entity1": "b5R", "entity2": "N-hydroxy-4-aminobiphenyl", "span1": [30, 33], "span2": [68, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7808": {"label": 2, "data": {"text": "RSV targets and activates the NAD(+)-dependent protein deacetylase SIRT1; in turn, SIRT1 induces an intracellular antioxidative mechanism by inducing mitochondrial superoxide dismutase (SOD2).", "entity1": "mitochondrial superoxide dismutase", "entity2": "RSV", "span1": [150, 184], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9941": {"label": 3, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "IKK-beta", "entity2": "sulfasalazine", "span1": [169, 177], "span2": [269, 282]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6506": {"label": 3, "data": {"text": "CONCLUSION: Rabeprazole is a well tolerated proton pump inhibitor.", "entity1": "proton pump", "entity2": "Rabeprazole", "span1": [44, 55], "span2": [12, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8677": {"label": 2, "data": {"text": "The expression kinetics of TAp63, c-Abl and TAp73 suggest that cisplatin activates TAp63-dependent expression of c-Abl and TAp73 and, in turn, the activation of TAp73 by c-Abl-induced BAX expression.", "entity1": "BAX", "entity2": "cisplatin", "span1": [184, 187], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15934": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "glucagon", "entity2": "Vildagliptin", "span1": [126, 134], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2656": {"label": 9, "data": {"text": "However, a lower concentration of dipyridamole (3 microM) that blocks PDE9, PDE10, and PDE11, but not PDE8, did not inhibit ecto-phosphodiesterase activity.", "entity1": "PDE8", "entity2": "dipyridamole", "span1": [102, 106], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11630": {"label": 3, "data": {"text": "Ex vivo IC(50) values (COX-1: 105.2 micromol/L; COX-2: 26.3 micromol/L) of acetaminophen compared favorably with its in vitro IC(50) values.", "entity1": "COX-1", "entity2": "acetaminophen", "span1": [23, 28], "span2": [75, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4923": {"label": 8, "data": {"text": "Cholesterol uptake from lipoproteins, intracellular vesicle transport and lipid transfer are also modified by oxysterols.", "entity1": "lipoproteins", "entity2": "Cholesterol", "span1": [24, 36], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11221": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "repaglinide", "span1": [4, 11], "span2": [135, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9868": {"label": 1, "data": {"text": "In this study, we investigated the effect of troglitazone, a ligand of the nuclear receptor peroxisome proliferator activated receptor-gamma, on PAI-1 expression and secretion in human adipocytes.", "entity1": "nuclear receptor", "entity2": "troglitazone", "span1": [75, 91], "span2": [45, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13158": {"label": 2, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "JNK", "entity2": "paclitaxel", "span1": [159, 162], "span2": [378, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9461": {"label": 1, "data": {"text": "7. 8-Epi-PGF2 alpha showed only weak binding to the IP, TP, FP, EP2 and EP3 receptor at 10 microM concentration.", "entity1": "EP3", "entity2": "7. 8-Epi-PGF2", "span1": [72, 75], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10542": {"label": 1, "data": {"text": "In sum the results of the present study indicate that RA-induced expression of blr1 expression depends on a novel RA response element.", "entity1": "RA response element", "entity2": "RA", "span1": [114, 133], "span2": [54, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7816": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "GluR5", "entity2": "(3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid", "span1": [183, 188], "span2": [270, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12398": {"label": 2, "data": {"text": "Number and area of preneoplastic foci positive for glutathione S-transferase placental form (GST-P) were consistently higher in these groups than the sum of individual values in the groups treated with HEP or HCB alone.", "entity1": "glutathione S-transferase placental form", "entity2": "HEP", "span1": [51, 91], "span2": [202, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3788": {"label": 2, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "fatty acid synthase", "entity2": "glucose", "span1": [50, 69], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14743": {"label": 1, "data": {"text": "Together, these data suggest that arsenic degrades \u0394Np63 protein at least in part via Pirh2-dependent proteolysis and that inhibition of \u0394Np63 expression facilitates tumor cells to arsenic-induced death.", "entity1": "Pirh2", "entity2": "arsenic", "span1": [86, 91], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10826": {"label": 3, "data": {"text": "Increased immunohistochemical labeling of HIF-1alpha, VEGF, and BNP in the ventricular myocardium was observed in the banding group and carvedilol again normalized the labeling.", "entity1": "BNP", "entity2": "carvedilol", "span1": [64, 67], "span2": [136, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1310": {"label": 3, "data": {"text": "Both the non-specific phospholipase A(2) inhibitor, quinacrine, and an inhibitor of cPLA(2) and iPLA(2), AACOF3, counteracted the effect; in contrast, a selective iPLA(2) inhibitor, BEL, and a selective sPLA(2) inhibitor, TAPC, were ineffective.", "entity1": "phospholipase A(2)", "entity2": "quinacrine", "span1": [22, 40], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"631": {"label": 3, "data": {"text": "Taken together, these data demonstrated that PLA2 inhibitors BPB and AACOCF3 are robust inhibitors of IL-2 expression at both the mRNA and protein levels in murine splenocytes.", "entity1": "PLA2", "entity2": "BPB", "span1": [45, 49], "span2": [61, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10628": {"label": 3, "data": {"text": "While fluoropyrimidine antimetabolites have other sites of action, antifolates ZD1694 (raltitrexed, Tomudex) and AG337 (Thymitag) are more specific and potent TS inhibitors.", "entity1": "TS", "entity2": "Tomudex", "span1": [159, 161], "span2": [100, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10514": {"label": 3, "data": {"text": "Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance.", "entity1": "HER2", "entity2": "GW572016", "span1": [20, 24], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14178": {"label": 0, "data": {"text": "Cresyl saligenin phosphate makes multiple adducts on free histidine, but does not form an adduct on histidine 438 of human butyrylcholinesterase.", "entity1": "human butyrylcholinesterase", "entity2": "histidine", "span1": [117, 144], "span2": [100, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4112": {"label": 3, "data": {"text": "To develop new drugs for treatment of Alzheimer's disease, a group of N'-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones was designed, synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase and aggregation of amyloid beta peptides (1-40, 1-42 and 1-40_1-42).", "entity1": "butyrylcholinesterase", "entity2": "N'-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones", "span1": [213, 234], "span2": [70, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1754": {"label": 3, "data": {"text": "GW572016, a reversible small molecule inhibitor of EGFR and ErbB2 tyrosine kinases, inhibits baseline p95ErbB2 phosphorylation in BT474 cells and tumor xenografts.", "entity1": "EGFR", "entity2": "GW572016", "span1": [51, 55], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7770": {"label": 1, "data": {"text": "GDC-0152 induces NF-\u03baB transcriptional activity leading to expression of several chemokines and cytokines, of which tumor necrosis factor alpha (TNF-\u03b1) is the most important for single-agent tumor activity.", "entity1": "TNF-\u03b1", "entity2": "GDC-0152", "span1": [145, 150], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12075": {"label": 1, "data": {"text": "Nicotinic acid and acipimox interfere with the biosynthesis of LDL and can also improve the clearance of VLDL/LDL.", "entity1": "VLDL", "entity2": "Nicotinic acid", "span1": [105, 109], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4979": {"label": 2, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "cytochrome c", "entity2": "DZN", "span1": [206, 218], "span2": [245, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5266": {"label": 1, "data": {"text": "Quinone compounds regulate the level of ROS production by the NADPH oxidase Nox4.", "entity1": "Nox4", "entity2": "Quinone", "span1": [76, 80], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11458": {"label": 8, "data": {"text": "These unexpected and intriguing complexities seem likely to have some as yet undefined role in regulating SSAT activity or stability as a part of polyamine homeostasis.", "entity1": "SSAT", "entity2": "polyamine", "span1": [106, 110], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5989": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "tissue plasminogen activator", "entity2": "epsilon-aminocaproic acid", "span1": [91, 119], "span2": [199, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4315": {"label": 5, "data": {"text": "Since the original discovery of azoles analogs as PXR antagonists, we have preliminarily defined an important PXR antagonist pharmacophore and developed less-toxic PXR antagonists.", "entity1": "PXR", "entity2": "azoles", "span1": [110, 113], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4621": {"label": 2, "data": {"text": "Consumption of alcohol for 8weeks induced severe liver damage with increases in prognostic indicators such as aspartate transaminase, alanine transaminase in serum whereas co-administration of CNF suppressed their increases.", "entity1": "alanine transaminase", "entity2": "alcohol", "span1": [134, 154], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4553": {"label": 1, "data": {"text": "The present study was designed to test the hypothesis that alcohol alters global DNA methylation, and modulates expression of the DNA methyltransferases (DNMTs) and various methyl CpG-binding proteins.", "entity1": "CpG-binding proteins", "entity2": "alcohol", "span1": [180, 200], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13693": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imiquimod", "span1": [100, 104], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2314": {"label": 3, "data": {"text": "Sulindac metabolites simultaneously (a) increase cellular cyclic GMP and subsequently activate cyclic GMP-dependent protein kinase (PKG); (b) activate c-jun NH2-terminal kinase (JNK); (c) inhibit extracellular signal-regulated kinase 1/2 (ERK1/2); and (d) decrease beta-catenin protein expression at times and doses consistent with apoptosis.", "entity1": "beta-catenin", "entity2": "Sulindac", "span1": [265, 277], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1655": {"label": 5, "data": {"text": "The potent histamine H(1)-receptor antagonist cetirizine (Zyrtec) is a racemic mixture of levocetirizine (now available under the trademark Xyzal and dextrocetirizine.", "entity1": "histamine H(1)-receptor", "entity2": "Zyrtec", "span1": [11, 34], "span2": [58, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12301": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Fdft1", "entity2": "Quercetin", "span1": [168, 173], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7522": {"label": 3, "data": {"text": "Previous studies have explored the protective effect of naproxen (non-selective COX-inhibitor) or rofecoxib (selective COX-2 inhibitor) against chemical kindling in mice.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [119, 124], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5248": {"label": 3, "data": {"text": "A series of carbamoylmethylene linked prodrugs of 1 (BMS-582949), a clinical p38\u03b1 inhibitor, were synthesized and evaluated.", "entity1": "p38\u03b1", "entity2": "carbamoylmethylene", "span1": [77, 81], "span2": [12, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7008": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "PDGFR-beta", "entity2": "sunitinib", "span1": [238, 248], "span2": [173, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7994": {"label": 2, "data": {"text": "Furthermore, U0126 (an ERK1/2 inhibitor) significantly enhanced the ISO-induced the Bax/Bcl-2 ratio, the release of cytochrome c to the cytosol fraction, and the levels of cleaved caspase-3.", "entity1": "Bcl-2", "entity2": "ISO", "span1": [88, 93], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15736": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b2", "entity2": "alkyl", "span1": [150, 153], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7165": {"label": 3, "data": {"text": "CONCLUSION: Our data provides a novel insight into an effect of telmisartan: telmisartan inhibits AT1R gene expression through PPARgamma activation.", "entity1": "AT1R", "entity2": "telmisartan", "span1": [98, 102], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7975": {"label": 1, "data": {"text": "Inhibitory effect of 1\u03b1,25-dihydroxyvitamin D\u2083 on excretion of JBP485 via organic anion transporters in rats.", "entity1": "organic anion transporters", "entity2": "1\u03b1,25-dihydroxyvitamin D\u2083", "span1": [74, 100], "span2": [21, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7852": {"label": 2, "data": {"text": "Protein kinase C (PKC) inhibition reduced the potentiation by mGlu1 of GluK2/GluK5, and conversely, direct activation of PKC by phorbol 12-myristate,13-acetate potentiated GluK2/GluK5.", "entity1": "PKC", "entity2": "phorbol 12-myristate,13-acetate", "span1": [121, 124], "span2": [128, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10493": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "BRL 37344", "span1": [392, 423], "span2": [311, 320]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2805": {"label": 3, "data": {"text": "In addition, cells pre-treated with DL-propargylglycine (PAG, 3 mM), a CSE inhibitor, reduced the formation of H(2)S in caerulein treated cells, suggesting that CSE may be the main enzyme involved in H(2)S formation in mouse acinar cells.", "entity1": "CSE", "entity2": "DL-propargylglycine", "span1": [71, 74], "span2": [36, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"410": {"label": 1, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "(+)-Tamsulosin", "span1": [258, 286], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8684": {"label": 3, "data": {"text": "Recently, the c-Abl kinase inhibitor imatinib mesylate (imatinib) has become the focus of research as a fertoprotective drug against cisplatin.", "entity1": "c-Abl", "entity2": "imatinib", "span1": [14, 19], "span2": [56, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"925": {"label": 5, "data": {"text": "Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists.", "entity1": "beta-adrenoceptor", "entity2": "Betaxolol", "span1": [159, 176], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10521": {"label": 3, "data": {"text": "RESULTS: GW572016 inhibited constitutive and/or ligand-induced EGFR or HER2 tyrosine phosphorylation of all five cell lines, which correlated with the antiproliferative response in all but one cell line.", "entity1": "EGFR", "entity2": "GW572016", "span1": [63, 67], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1306": {"label": 3, "data": {"text": "It was also antagonized by the non-specific cyclooxygenase (COX) inhibitor, indomethacin, and by the selective COX-2 inhibitor, NS-398, but not by the specific COX-1 inhibitor, valeryl salicylate.", "entity1": "cyclooxygenase", "entity2": "indomethacin", "span1": [44, 58], "span2": [76, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12107": {"label": 3, "data": {"text": "Molecular determinants of dofetilide block of HERG K+ channels.", "entity1": "HERG", "entity2": "dofetilide", "span1": [46, 50], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4931": {"label": 2, "data": {"text": "Little is known in terms of multi-matrix cytochrome P450 activity induction under repeated oral exposure to planar halogenated and polycyclic aromatic hydrocarbons (PHH, PAH).", "entity1": "cytochrome P450", "entity2": "halogenated and polycyclic aromatic hydrocarbons", "span1": [41, 56], "span2": [115, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5378": {"label": 6, "data": {"text": "The implications of our finding for mechanism of in vivo actions of rapamycin and for design of novel allosteric drugs targeting the proteasome are discussed.", "entity1": "proteasome", "entity2": "rapamycin", "span1": [133, 143], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"497": {"label": 9, "data": {"text": "Although FGF-2 strongly binds to basement membrane heparan sulfate in skin and most other tissue sites examined, FGF-7 fails to bind to basement membrane heparan sulfate in most locations.", "entity1": "FGF-7", "entity2": "sulfate", "span1": [113, 118], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9382": {"label": 0, "data": {"text": "The amino acid sequence deduced from the nucleotide sequence of the cloned PHBP cDNA exhibited significant homology to that of hepatocyte growth factor activator (HGFA).", "entity1": "PHBP", "entity2": "amino acid", "span1": [75, 79], "span2": [4, 14]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1526": {"label": 3, "data": {"text": "), which also block PP1, and calyculin-A (0.1 fg/mouse-1 ng/mouse, i.c.v. ), which inhibits equally both PP1 and PP2A, did not modify the morphine-induced antinociception.", "entity1": "PP2A", "entity2": "calyculin-A", "span1": [113, 117], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9078": {"label": 2, "data": {"text": "In contrast, serum alkaline phosphatase was elevated in animals dosed with 13cisRA or 4HPR but not in those dose with ROAc.", "entity1": "alkaline phosphatase", "entity2": "4HPR", "span1": [19, 39], "span2": [86, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4010": {"label": 3, "data": {"text": "Compared with the untreated colitis group, the curcumin-treated group showed significant decreases in the disease activity index, colonic mucosa damage index, histological score, myeloperoxidase activity, and expressions of NF-\u03baB mRNA, IL-27 mRNA, TLR4 protein, NF-\u03baB p65 protein, and IL-27 p28 protein (p < 0.05).", "entity1": "TLR4", "entity2": "curcumin", "span1": [248, 252], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6531": {"label": 0, "data": {"text": "Experimentation using isoforms of alefacept engineered to have amino acid substitutions in the IgG1 C(H)2 domain that impact Fc gamma R binding indicate that alefacept mediates cognate interactions between cells expressing human CD2 and CD16 to activate cells, e.g., increase extracellular signal-regulated kinase phosphorylation, up-regulate cell surface expression of the activation marker CD25, and induce release of granzyme B.", "entity1": "IgG1 C(H)2 domain", "entity2": "amino acid", "span1": [95, 112], "span2": [63, 73]}, "weak_labels": [0, -1, -1, 1, 1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13718": {"label": 1, "data": {"text": "When RAD51, which is a central component of HR, was depleted by siRNA cells were sensitized to raltitrexed (RTX), which specifically inhibits TS.", "entity1": "RAD51", "entity2": "raltitrexed", "span1": [5, 10], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13566": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase (DDAH) metabolizes asymmetric dimethylarginine to generate L-citrulline and is present in large quantities in the kidney.", "entity1": "DDAH", "entity2": "dimethylarginine", "span1": [41, 45], "span2": [70, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2084": {"label": 8, "data": {"text": "Phenytoin is principally metabolized by CYP2C9, and both are probable substrates of the drug transporter P-glycoprotein.", "entity1": "P-glycoprotein", "entity2": "Phenytoin", "span1": [105, 119], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"6829": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "VEGFR", "entity2": "imatinib", "span1": [338, 343], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2595": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "5-HT(2A)", "entity2": "FLX", "span1": [269, 277], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15838": {"label": 1, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "RXR", "entity2": "TO901317", "span1": [143, 146], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3393": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "VMAT2", "entity2": "cocaine", "span1": [234, 239], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9152": {"label": 1, "data": {"text": "Co-incubation with human serum albumin or poly-L-lysine but not lysine protected human and hamster LDH-X from gossypol.", "entity1": "human and hamster LDH-X", "entity2": "poly-L-lysine", "span1": [81, 104], "span2": [42, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11357": {"label": 8, "data": {"text": "ABCA1 mediates the efflux of unesterified cholesterol and phospholipids from cells to lipid-poor apolipoprotein A-I (apoA-I).", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [0, 5], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4129": {"label": 1, "data": {"text": "Here, we identify a Zn\u00b2\u207a-driven N-terminal to C-terminal tertiary interaction in PrP(C).", "entity1": "PrP(C)", "entity2": "Zn\u00b2\u207a", "span1": [81, 87], "span2": [20, 24]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9358": {"label": 1, "data": {"text": "Desipramine administration in the olfactory bulbectomized rat: changes in brain beta-adrenoceptor and 5-HT2A binding sites and their relationship to behaviour.", "entity1": "5-HT2A", "entity2": "Desipramine", "span1": [102, 108], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9357": {"label": 9, "data": {"text": "Administration of DMI for 14 or 21 days did not further reduce the number of beta-adrenoceptors.", "entity1": "beta-adrenoceptors", "entity2": "DMI", "span1": [77, 95], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7427": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "Delta 6 desaturase", "entity2": "alpha-linolenic acid", "span1": [11, 29], "span2": [63, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5338": {"label": 1, "data": {"text": "The inhibitors of PI3K and Akt suppressed S1P-induced nuclear localization of \u03b2-catenin.", "entity1": "\u03b2-catenin", "entity2": "S1P", "span1": [78, 87], "span2": [42, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10021": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Arg", "span1": [126, 138], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2691": {"label": 3, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "kinase", "entity2": "MP470", "span1": [146, 152], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7091": {"label": 5, "data": {"text": "These currents were produced by glutamate-aspartate transporters (GLAST) (excitatory amino acid transporter 1) because they were weakly inhibited by dihydrokainate, an antagonist of glutamate transporter-1 (excitatory amino acid transporter 2) and were absent from IPCs in GLAST-/- cochleas.", "entity1": "excitatory amino acid transporter 2", "entity2": "dihydrokainate", "span1": [207, 242], "span2": [149, 163]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"4345": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "\u03b2-catenin", "entity2": "pinosylvin", "span1": [65, 74], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"90": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "phenylalanine hydroxylase", "entity2": "noradrenaline", "span1": [112, 137], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9779": {"label": 4, "data": {"text": "In this study, the activity of the delta-opioid receptor subtype-selective agonist, SB 227122, was investigated in a guinea pig model of citric acid-induced cough.", "entity1": "delta-opioid receptor", "entity2": "SB 227122", "span1": [35, 56], "span2": [84, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5093": {"label": 1, "data": {"text": "Aldosterone regulates Na(+) transport in the distal nephron through multiple mechanisms that include the transcriptional control of epithelial sodium channel (ENaC) and Na(+)/K(+)-ATPase subunits.", "entity1": "Na(+)/K(+)-ATPase", "entity2": "Aldosterone", "span1": [169, 186], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8269": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "CYP2B6", "entity2": "Methadone", "span1": [79, 85], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2114": {"label": 1, "data": {"text": "Diethylcarbamazine activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway.", "entity1": "cyclooxygenase", "entity2": "Diethylcarbamazine", "span1": [120, 134], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10743": {"label": 3, "data": {"text": "The compounds 5'-azacytidine (AZC) and procainamide (PCA) belong to inhibitors of DNMT1, whose low activity correlates with increase in transcription of various genes.", "entity1": "DNMT1", "entity2": "PCA", "span1": [82, 87], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"717": {"label": 1, "data": {"text": "On phosphorylation of Ser40 by protein kinase A, the affinity for H4biopterin increased ([S]0.5 = 11 +/- 2 microM) and the negative cooperativity was amplified (h = 0.27 +/- 0.03).", "entity1": "protein kinase A", "entity2": "H4biopterin", "span1": [31, 47], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3560": {"label": 5, "data": {"text": "Pretreatment with pranlukast (1.5 ng/mouse, intracerebroventricularly), a CysLT(1)R antagonist, blocked LTD4-induced amyloidogenesis, memory deficits.", "entity1": "CysLT(1)R", "entity2": "pranlukast", "span1": [74, 83], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1452": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "monoamine oxidase", "entity2": "Rasagiline", "span1": [76, 93], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11742": {"label": 0, "data": {"text": "Albumin nanoparticles were surface-coated with bifunctional polyethylene glycol 3500 (PEG) and a nanobody-the single variable domain of an antibody-(Ega1) against the epidermal growth factor receptor (EGFR).", "entity1": "Albumin", "entity2": "polyethylene glycol", "span1": [0, 7], "span2": [60, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7046": {"label": 1, "data": {"text": "Since the effect of retinoic acid is mediated via retinoic acid receptors and retinoid X receptors, we investigated mRNA and protein expression of these receptors during injury-induced degeneration and regeneration.", "entity1": "retinoid X receptors", "entity2": "retinoic acid", "span1": [78, 98], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5435": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "EC 4.2.1.1", "entity2": "cyanoacrylamide", "span1": [153, 163], "span2": [46, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3561": {"label": 0, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u.", "entity1": "IRS-1", "entity2": "tyrosine", "span1": [42, 47], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6989": {"label": 3, "data": {"text": "RATIONALE: Several drugs used to treat bipolar disorder (lithium and carbamazepine), when administered chronically to rats, reduce the turnover of arachidonic acid, but not docosahexaenoic acid, in brain phospholipids by decreasing the activity of an arachidonic acid-selective phospholipase A(2).", "entity1": "phospholipase A(2)", "entity2": "carbamazepine", "span1": [278, 296], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4881": {"label": 2, "data": {"text": "Methylation-specific PCR and bisulfite sequencing identified methylation of this CpG ((m)CpG) island of the glut3 gene, frequency of methylation increasing 2.5-fold with a 1.6-fold increase in DNA methyl transferase 3a concentrations noted with advancing postnatal age (PN14 vs PN3).", "entity1": "DNA methyl transferase 3a", "entity2": "(m)CpG", "span1": [193, 218], "span2": [86, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3711": {"label": 2, "data": {"text": "Nitrogen-containing bisphosphonates induce apoptosis of hematopoietic tumor cells via inhibition of Ras signaling pathways and Bim-mediated activation of the intrinsic apoptotic pathway.", "entity1": "Bim", "entity2": "bisphosphonates", "span1": [127, 130], "span2": [20, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12390": {"label": 0, "data": {"text": "We apply DFTB in a QM/MM framework to perform vibrational analysis of buried aspartic acids in bacteriorhodopsin and channelrhodopsin-2.", "entity1": "bacteriorhodopsin", "entity2": "aspartic acids", "span1": [95, 112], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7442": {"label": 9, "data": {"text": "The Ki for mycophenolic acid inhibition of the L263F variant was comparable with the wild-type, and the variant Km for inosine 5'-monophosphate and nicotinamide adenine dinucleotide did not change significantly.", "entity1": "L263F", "entity2": "inosine 5'-monophosphate", "span1": [47, 52], "span2": [119, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6442": {"label": 2, "data": {"text": "This study demonstrates that CB1093 and clenbuterol stimulate NGF levels in vitro and that AP-1 binding could be a commonality between the mechanism of NGF induction of these two compounds.", "entity1": "NGF", "entity2": "CB1093", "span1": [62, 65], "span2": [29, 35]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1051": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "4'-(9-acridinylamino)methanesulfon-m-anisidide", "span1": [110, 114], "span2": [223, 269]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14499": {"label": 1, "data": {"text": "Taken together, our study suggested, for the first time, that the pro-apoptotic effects of TSN on HL-60 cells were mediated through JNK signaling pathway.", "entity1": "JNK", "entity2": "TSN", "span1": [132, 135], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"940": {"label": 1, "data": {"text": "In contrast, 2, 4-dioxo-5-acetamido-6-phenylhexanoic acid, which is a competitive inhibitor with respect to ascorbate, exhibits a low degree of stereospecificity in binding to the ascorbate sites of both PAM and dopamine-beta-hydroxylase.", "entity1": "PAM", "entity2": "2, 4-dioxo-5-acetamido-6-phenylhexanoic acid", "span1": [204, 207], "span2": [13, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2337": {"label": 1, "data": {"text": "NO rebinding in HNS from Staphylococcus aureus (SA-HNS) is faster than that measured for either Bacillus anthracis (BA-HNS) or for eNOS(HD) in both oxidized and reduced forms in the presence of arginine.", "entity1": "HNS", "entity2": "NO", "span1": [16, 19], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14858": {"label": 2, "data": {"text": "Regulation of sexual reproduction by estradiol involves the activation of estrogen receptors (ERs) in the hypothalamus.", "entity1": "ERs", "entity2": "estradiol", "span1": [94, 97], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13245": {"label": 3, "data": {"text": "EGTA and 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetra acetic acid tetrakis (BAPTA), two Ca2+ chelators, but not nifedipine, an L-type Ca2+ channel blocker, prevented GRIP1 degradation.", "entity1": "L-type Ca2+ channel", "entity2": "nifedipine", "span1": [128, 147], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11241": {"label": 1, "data": {"text": "Finally, we illustrate how BH4 might transform the NOS dimer into an efficient S-nitrosoglutathione synthase,and briefly touch on some more speculative aspects of the role of BH4 in NO synthesis.", "entity1": "NOS", "entity2": "BH4", "span1": [51, 54], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8261": {"label": 4, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2C", "entity2": "1-methylpsilocin", "span1": [23, 29], "span2": [85, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3892": {"label": 3, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "c-Myc", "entity2": "10074-G5", "span1": [53, 58], "span2": [75, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10405": {"label": 1, "data": {"text": "Orphanin FQ (OFQ) stimulated [35S]-GTPgammaS binding in a pattern similar to that described for [125I]-OFQ at the endogenous opioid receptor-like (ORL1) receptor.", "entity1": "OFQ", "entity2": "125I", "span1": [103, 106], "span2": [97, 101]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14306": {"label": 1, "data": {"text": "Claudin-3 and claudin-4 regulate sensitivity to cisplatin by controlling expression of the copper and cisplatin influx transporter CTR1.", "entity1": "Claudin-3", "entity2": "cisplatin", "span1": [0, 9], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15368": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "RXRs", "entity2": "all-trans retinoic acid", "span1": [227, 231], "span2": [82, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9993": {"label": 1, "data": {"text": "Furthermore, h[Gly2]-GLP-2 reduced chemotherapy-induced apoptosis, decreased activation of caspase-8 and -3, and inhibited poly(ADP-ribose) polymerase cleavage in heterologous cells transfected with the GLP-2 receptor.", "entity1": "GLP-2 receptor", "entity2": "Gly2", "span1": [203, 217], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6979": {"label": 1, "data": {"text": "RESULTS: With regard to PRA, dobutamine increased PRA more potently in Arg389-beta1AR versus Gly389-beta1AR subjects.", "entity1": "beta1AR", "entity2": "dobutamine", "span1": [78, 85], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"139": {"label": 3, "data": {"text": "Similarly, felodipine and the p-chloro analogue inhibited myosin light chain kinase activity whether the isolated 20 kD light chain (IC50 = 12.6 microM) or intact myosin (IC50 = 11.0 microM) was used as substrate.", "entity1": "myosin light chain kinase", "entity2": "felodipine", "span1": [58, 83], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10840": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "BCR", "entity2": "STI571", "span1": [115, 118], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11425": {"label": 1, "data": {"text": "We also show that an intronic polymorphism in the SCN1A gene shows significant association with maximum doses in regular usage of both carbamazepine and phenytoin (P = 0.0051 and P = 0.014, respectively).", "entity1": "SCN1A", "entity2": "carbamazepine", "span1": [50, 55], "span2": [135, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"535": {"label": 3, "data": {"text": "Because gastric AADC and COMT degrade levodopa, the drug is given with inhibitors of AADC (carbidopa or benserazide), and inhibitors of COMT will also enter clinical use.", "entity1": "AADC", "entity2": "benserazide", "span1": [85, 89], "span2": [104, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14113": {"label": 2, "data": {"text": "Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplified pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression.", "entity1": "p21", "entity2": "pomalidomide", "span1": [191, 194], "span2": [112, 124]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3058": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "chemokine", "entity2": "AMD3100", "span1": [101, 110], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4218": {"label": 2, "data": {"text": "The data indicated that PhIP could cause stomach injury, oxidative stress in rat stomachs as well as the activation of c-fos and c-jun and inactivation of p16, which may play a role in the pathogenesis of PhIP-associated stomach cancer.", "entity1": "c-fos", "entity2": "PhIP", "span1": [119, 124], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3469": {"label": 8, "data": {"text": "RESULTS: (+/-)-, R-, and S-modafinil bind to the DAT and inhibit DA uptake less potently than cocaine, with R-modafinil having approximately threefold higher affinity than its S-enantiomer.", "entity1": "DAT", "entity2": "DA", "span1": [49, 52], "span2": [65, 67]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"127": {"label": 3, "data": {"text": "Again, inhibition of the actin-activated myosin Mg2+-ATPase and myosin filament assembly by felodipine and the p-chloro analogue could be reversed by raising the calmodulin concentration.", "entity1": "myosin", "entity2": "p-chloro", "span1": [64, 70], "span2": [111, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4603": {"label": 8, "data": {"text": "In relation to zinc bioavailability, \u03b1-CPPs, \u03b2-CPPs, \u03b1(s1)-CN(64-74)4P and \u03b2-CN(1-25)4P increased zinc uptake.", "entity1": "\u03b2-CN", "entity2": "zinc", "span1": [75, 79], "span2": [98, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"221": {"label": 2, "data": {"text": "Both 5 alpha-NET and 3 beta,5 alpha-NET blocked the PR down-regulation induced by P4 as assessed by Western and Northern blot methods.", "entity1": "PR", "entity2": "5 alpha-NET", "span1": [52, 54], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1485": {"label": 1, "data": {"text": "Sulindac sulfide inhibits epidermal growth factor-induced phosphorylation of extracellular-regulated kinase 1/2 and Bad in human colon cancer cells.", "entity1": "extracellular-regulated kinase 1/2", "entity2": "Sulindac sulfide", "span1": [77, 111], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2566": {"label": 2, "data": {"text": "Brain tissue analyses revealed that neonatal quinpirole treatment produced a significant decrease in hippocampal NGF, BDNF and ChAT that was eliminated by olanzapine treatment.", "entity1": "BDNF", "entity2": "olanzapine", "span1": [118, 122], "span2": [155, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8541": {"label": 2, "data": {"text": "In DU-PM cells with acquired resistance to elisidepsin, ErbB3 expression was decreased, while Bcl2 was increased.", "entity1": "Bcl2", "entity2": "elisidepsin", "span1": [94, 98], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15335": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "galangin", "span1": [287, 296], "span2": [222, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6673": {"label": 1, "data": {"text": "These data suggest that, after SCI, minocycline treatment modulated expression of cytokines, attenuated cell death and the size of lesions, and improved functional recovery in the injured rat.", "entity1": "cytokines", "entity2": "minocycline", "span1": [82, 91], "span2": [36, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6015": {"label": 8, "data": {"text": "The daily administration of low-dose aspirin (40 mg), a selective inhibitor of platelet PGHS-1, caused a cumulative inhibition of urinary 11-dehydro-TXB2 and whole blood TXB2 production that recovered with a timecourse consistent with platelet turnover.", "entity1": "PGHS-1", "entity2": "TXB2", "span1": [88, 94], "span2": [170, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8245": {"label": 1, "data": {"text": "PURPOSE: To characterise further the previously observed cytochrome P450 3A4 (CYP3A4) interaction of the dual orexin receptor antagonist almorexant.", "entity1": "CYP3A4", "entity2": "almorexant", "span1": [78, 84], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1700": {"label": 1, "data": {"text": "Glycylsarcosine coadministration could inhibit the uptake of cefadroxil in PEPT2(+/+) mice (p < 0.01) but not PEPT2(-/-) mice.", "entity1": "PEPT2", "entity2": "Glycylsarcosine", "span1": [75, 80], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12249": {"label": 1, "data": {"text": "For the isolated PKCalpha C2 domain in the presence of physiological Ca2+ levels, the target lipids phosphatidylserine (PS) and phosphatidylinositol-4,5-bisphosphate (PIP2) are together sufficient to recruit the PKCalpha C2 domain to a lipid mixture mimicking the plasma membrane inner leaflet.", "entity1": "PKCalpha C2 domai", "entity2": "phosphatidylinositol-4,5-bisphosphate", "span1": [212, 229], "span2": [128, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9341": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "CNQX", "span1": [72, 77], "span2": [182, 186]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7003": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "kinase", "entity2": "sorafenib", "span1": [137, 143], "span2": [162, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2652": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one", "span1": [397, 414], "span2": [196, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4820": {"label": 1, "data": {"text": "Degradation of MAC13243 and studies of the interaction of resulting thiourea compounds with the lipoprotein targeting chaperone LolA.", "entity1": "LolA", "entity2": "thiourea", "span1": [128, 132], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5421": {"label": 5, "data": {"text": "Local LC citalopram effect was abolished by LC presence of the 5-HT3 receptor antagonist MDL72222 (1\u00a0\u03bcM) but not the 5-HT1/2 receptor antagonist methiothepin (1\u00a0\u03bcM).", "entity1": "5-HT3", "entity2": "MDL72222", "span1": [63, 68], "span2": [89, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4609": {"label": 3, "data": {"text": "Although thioredoxin reductase (TRR) inhibitors (aurothioglucose and Sb(III)) inhibited cytosolic DMAs(V) reduction, recombinant rat TRR plus NADPH, alone or when added to the cytosol, failed to support DMAs(V) reduction.", "entity1": "TRR", "entity2": "Sb(III)", "span1": [32, 35], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12416": {"label": 8, "data": {"text": "This methodology was subsequently used to assess the relative contribution of OATP1B1 uptake in human hepatocytes for olmesartan (42%-62%), valsartan (28%-81%), rosuvastatin (64%-72%), pitavastatin (84%-98%) and lopinavir (64%-89%).", "entity1": "OATP1B1", "entity2": "rosuvastatin", "span1": [78, 85], "span2": [161, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10754": {"label": 3, "data": {"text": "These findings suggest that the mechanism of antiproliferative toxicity of capecitabine is at least partly due to TS inhibitory activity of its active metabolite 5-fluoro-2'-deoxyuridine monophosphate (FdUMP).", "entity1": "TS", "entity2": "5-fluoro-2'-deoxyuridine monophosphate", "span1": [114, 116], "span2": [162, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13321": {"label": 3, "data": {"text": "All three salicylates inhibited the diabetes-induced translocation of p50 (a subunit of NF-kappaB) into nuclei of retinal vascular endothelial cells of the isolated retinal vasculature, as well as of p50 and p65 into nuclei of cells in the ganglion cell layer and inner nuclear layer on whole-retinal sections.", "entity1": "p65", "entity2": "salicylates", "span1": [208, 211], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"335": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "proline-42-to-alanine", "entity2": "2'CMP", "span1": [114, 135], "span2": [233, 238]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15518": {"label": 1, "data": {"text": "We found that, both in a cell-free system and in cells, NO/SNO donors such as S-nitrosocysteine and S-nitrosoglutathione readily induced the S-nitrosylation of Prx1, causing structural and functional alterations.", "entity1": "Prx1", "entity2": "S-nitrosoglutathione", "span1": [160, 164], "span2": [100, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7049": {"label": 3, "data": {"text": "RESULTS: Imatinib inhibited RET Y1062 phosphorylation in a dose-dependent manner after 1.5 hours of exposure.", "entity1": "Y1062", "entity2": "Imatinib", "span1": [32, 37], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"202": {"label": 1, "data": {"text": "Spiperone displayed high affinity and selectivity for alpha 1B adrenoceptors (pKi 8.8 +/- 0.16).", "entity1": "alpha 1B adrenoceptors", "entity2": "Spiperone", "span1": [54, 76], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14196": {"label": 1, "data": {"text": "In conclusion, these results suggest that CHOP may sensitize FRO ATC cells to SU5416 thereby inhibiting cell survival by modulating p21 and PI3K/Akt signal pathway.", "entity1": "p21", "entity2": "SU5416", "span1": [132, 135], "span2": [78, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6933": {"label": 8, "data": {"text": "On the other hand, the FUM1 (fumarase) gene disrupted mutant produced significantly higher levels of fumarate but did not form malate at all.", "entity1": "fumarase", "entity2": "fumarate", "span1": [29, 37], "span2": [101, 109]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"14419": {"label": 2, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C. Furthermore, the AMPK activator 5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) significantly inhibited ghrelin secretion.", "entity1": "AMPK", "entity2": "5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide", "span1": [187, 191], "span2": [202, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12458": {"label": 2, "data": {"text": "This report concerns the marked up-regulation in differentiated CaCo-2 colonic epithelial cells of two key inflammatory interleukins, IL-6 and IL-8, caused by a mixture of oxysterols representative of a high cholesterol diet.", "entity1": "interleukins", "entity2": "cholesterol", "span1": [120, 132], "span2": [208, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14441": {"label": 2, "data": {"text": "Fungicide prochloraz and environmental pollutant dioxin induce the ABCG2 transporter in bovine mammary epithelial cells by the arylhydrocarbon receptor signaling pathway.", "entity1": "ABCG2", "entity2": "dioxin", "span1": [67, 72], "span2": [49, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12157": {"label": 9, "data": {"text": "CONCLUSION: Nandrolone phenylpropionate up-regulated the density of AR in liver tissue, whereas it had no significant effects on the density of AR in testis and ovary tissues.", "entity1": "AR", "entity2": "Nandrolone phenylpropionate", "span1": [144, 146], "span2": [12, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10481": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "isoproterenol", "span1": [392, 423], "span2": [127, 140]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9476": {"label": 4, "data": {"text": "M&B-28767, a putative EP3 agonist, and misoprostol, a putative EP2/EP3 agonist, also bound to this receptor with Ki values of 120 nM.", "entity1": "EP2", "entity2": "misoprostol", "span1": [63, 66], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14449": {"label": 1, "data": {"text": "We found that Ag NPs were highly cytotoxic to hepatocytes (LC(50) lactate dehydrogenase: 2.5 \u03bcg/cm(2)) and affected hepatocyte homeostasis by reducing albumin release.", "entity1": "lactate dehydrogenase", "entity2": "Ag", "span1": [66, 87], "span2": [14, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15241": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B3", "entity2": "silychristin", "span1": [10, 17], "span2": [280, 292]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"7169": {"label": 5, "data": {"text": "However, the expression of AT1R was not suppressed by other AT1R antagonists such as candesartan or olmesartan.", "entity1": "AT1R", "entity2": "candesartan", "span1": [60, 64], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10578": {"label": 2, "data": {"text": "This effect was most pronounced in CTLs of patients suffering from atopic dermatitis, a model disorder for subnormal perforin expression: as compared to perforin(+) CTLs detected at time point zero (100%), up to 270% of perforin(+) CTLs were induced by 2.5 microg/ml [corrected] IMQ.", "entity1": "perforin", "entity2": "IMQ", "span1": [220, 228], "span2": [279, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12388": {"label": 1, "data": {"text": "Clinical trials should now investigate the effectiveness of oxytocin as a novel intervention for psychostimulant addiction and should aim to determine its specific role in the therapeutic properties of MDMA that are currently being investigated.", "entity1": "oxytocin", "entity2": "MDMA", "span1": [60, 68], "span2": [202, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11665": {"label": 8, "data": {"text": "Thymidine kinase-1 (TK-1) and thymidylate synthase (TS) are key enzymes for salvage and de novo pyrimidine synthesis, respectively.", "entity1": "TS", "entity2": "pyrimidine", "span1": [52, 54], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5096": {"label": 2, "data": {"text": "Aldosterone-induced ENaC and basal Na(+)/K(+)-ATPase trafficking via protein kinase D1-phosphatidylinositol 4-kinaseIII\u03b2 trans Golgi signalling in M1 cortical collecting duct cells.", "entity1": "ENaC", "entity2": "Aldosterone", "span1": [20, 24], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1516": {"label": 8, "data": {"text": "The scientific basis of this treatment of ED includes relaxation of the corpus cavernosum smooth muscle tissue by inhibition of PDE5 that breaks down cGMP, the key pathway for the production of erectile function in humans.", "entity1": "PDE5", "entity2": "cGMP", "span1": [128, 132], "span2": [150, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4556": {"label": 3, "data": {"text": "In addition, ethanol induced degradation of DNA methyltransferases (DNMT-1, DNMT-3a, and DNMT-3b), as well as the methyl CpG-binding proteins (MeCP-2, MBD-2 and MBD-3), in MEF cells by the proteasomal pathway.", "entity1": "DNA methyltransferases", "entity2": "ethanol", "span1": [44, 66], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9823": {"label": 3, "data": {"text": "In this study, we demonstrate that geldanamycin treatment blocks interleukin (IL)-2 secretion, IL-2 receptor expression, and proliferation of stimulated T-lymphocytes.", "entity1": "interleukin (IL)-2", "entity2": "geldanamycin", "span1": [65, 83], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5909": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "low-density lipoproteins", "entity2": "probucol", "span1": [146, 170], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11766": {"label": 0, "data": {"text": "The CBC physically associates with these complexes to recruit them during transcription and mediates phosphorylation at Ser-2 of the C-terminal domain (CTD) of RNA polymerase II.", "entity1": "RNA polymerase II", "entity2": "C", "span1": [160, 177], "span2": [133, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7887": {"label": 9, "data": {"text": "In contrast, ibandronate did not affect FAS and DNMT1 expression in MC3T3-E1 non-neoplastic cells.", "entity1": "FAS", "entity2": "ibandronate", "span1": [40, 43], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11589": {"label": 2, "data": {"text": "Differences in magnitude of Na(+)-dependent l-alanine uptake through ASCT2 between WKY and SHR PTE cells correlated positively with differences in ASCT2 protein expression, this being more abundant in WKY PTE cells.", "entity1": "ASCT2", "entity2": "l-alanine", "span1": [147, 152], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9906": {"label": 1, "data": {"text": "The impaired expression of the UCP-3 gene is consistent with the involvement of UCP-3 gene regulation in the reduction of the use of fatty acids as fuel by the skeletal muscle and in impaired adaptative thermogenesis, both of which are major metabolic adaptations that occur during lactation.", "entity1": "UCP-3", "entity2": "fatty acids", "span1": [80, 85], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13904": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR2B", "entity2": "metformin", "span1": [173, 178], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11787": {"label": 1, "data": {"text": "The acyl esters could be correlated with expression of alcohol acyl-transferase EEB1 and the acyl esterase IAH1.", "entity1": "alcohol acyl-transferase EEB1", "entity2": "acyl esters", "span1": [55, 84], "span2": [4, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14269": {"label": 8, "data": {"text": "Thus, despite the similar structures of TETA and SpmTrien, SSAT2 is the main acetylator of TETA, whereas SpmTrien is primarily acetylated by SSAT1.", "entity1": "SSAT2", "entity2": "TETA", "span1": [59, 64], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3241": {"label": 1, "data": {"text": "METH is well known to produce effects on the monoamine systems but it is unclear how METH affects SERT and memory.", "entity1": "SERT", "entity2": "METH", "span1": [98, 102], "span2": [85, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8473": {"label": 4, "data": {"text": "Design, Synthesis, and Pharmacological Characterization of Novel Endomorphin-1 Analogues as Extremely Potent \u03bc-Opioid Agonists.", "entity1": "\u03bc-Opioid", "entity2": "Endomorphin-1", "span1": [109, 117], "span2": [65, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12396": {"label": 1, "data": {"text": "Dexamethasone suppressed IL-11 gene transcription enhanced by PTH(1-34) without affecting \u0394FosB expression or Smad1 phosphorylation, and dexamethasone-GC receptor complex was bound to JunD, which forms heterodimers with \u0394FosB.", "entity1": "\u0394FosB", "entity2": "dexamethasone", "span1": [220, 225], "span2": [137, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8151": {"label": 3, "data": {"text": "DPEP induced dose-dependent reduction of the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and concomitant reduction in the production of NO and prostaglandin E(2) (PGE(2)).", "entity1": "iNOS", "entity2": "DPEP", "span1": [96, 100], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14945": {"label": 1, "data": {"text": "Electron paramagnetic resonance (EPR) studies using nucleotide analog spin label probes showed that dephosphorylated myosin heads are highly ordered in the relaxed fibers and have very low ATPase activity.", "entity1": "dephosphorylated myosin", "entity2": "nucleotide", "span1": [100, 123], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"110": {"label": 5, "data": {"text": "Terfenadine and astemizole are chemically unrelated to histamine H1-receptor antagonists such as diphenhydramine and chlorpheniramine.", "entity1": "histamine H1-receptor", "entity2": "chlorpheniramine", "span1": [55, 76], "span2": [117, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"949": {"label": 9, "data": {"text": "The antagonistic property of rilmenidine at human alpha(2A)-adrenoceptors indicates that in contrast to the suggestion based on rabbit data, the hypotensive property of the drug in humans is not due to activation of alpha(2A)-adrenoceptors but other, presumably I(1)-imidazoline receptors, are probably involved.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "rilmenidine", "span1": [216, 239], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3813": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Ile", "span1": [66, 71], "span2": [58, 61]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3780": {"label": 1, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "sterol regulatory element-binding protein-1c", "entity2": "Phillyrin", "span1": [101, 145], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5937": {"label": 3, "data": {"text": "Inhibitory effect of synthetic progestins, 4-MA and cyanoketone on human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase activity.", "entity1": "human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase", "entity2": "progestins", "span1": [67, 139], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9493": {"label": 3, "data": {"text": "Monoamine uptake inhibitors structurally analogous to cocaine (cocaethylene, CFT, betaCIT, CPT, (+)-cocaine, norcocaine, and benztropine) also produced this rapid pressor response, whereas structurally unrelated uptake inhibitors with diverse monoamine transporter selectivities (BTCP, indatraline, GBR 12935, mazindol, nomifensine, and zimeldine) either did not produce a rapid pressor response or produced only a small pressor response.", "entity1": "monoamine transporter", "entity2": "nomifensine", "span1": [243, 264], "span2": [320, 331]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, 9]},
	"2946": {"label": 3, "data": {"text": "Conformational variations of both phosphodiesterase-5 and inhibitors provide the structural basis for the physiological effects of vardenafil and sildenafil.", "entity1": "phosphodiesterase-5", "entity2": "sildenafil", "span1": [34, 53], "span2": [146, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"872": {"label": 8, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ODC", "entity2": "spermidine", "span1": [143, 146], "span2": [25, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16006": {"label": 5, "data": {"text": "Treatment with the ER antagonist ICI 182,780 abolishes the above actions of puerarin on osteoblast-derived cells.", "entity1": "ER", "entity2": "ICI 182,780", "span1": [19, 21], "span2": [33, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15952": {"label": 1, "data": {"text": "4-Hydroxytamoxifen (OHT, tamoxifen's active form) failed to prevent E2-induced proteolysis of cyclin E and migration, but rather triggered cyclin E cleavage coincident with augmented migration.", "entity1": "cyclin E", "entity2": "OHT", "span1": [139, 147], "span2": [20, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7762": {"label": 4, "data": {"text": "Rescue of both impaired extinction acquisition and deficient extinction consolidation/retrieval was achieved with prior extinction training administration of valproic acid (a GABAergic enhancer and HDAC inhibitor) or AMN082 [metabotropic glutamate receptor 7 (mGlu7) agonist], while MS-275 or PEPA (AMPA receptor potentiator) failed to affect extinction acquisition in S1 mice.", "entity1": "metabotropic glutamate receptor 7", "entity2": "AMN082", "span1": [225, 258], "span2": [217, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11845": {"label": 1, "data": {"text": "A multivariable model adjusted for age, sex, population group, immigrant status, BMI, season of vitamin D measurement, LDL and HDL cholesterol, triglycerides, estimated glomerular filtration rate, history of hypertension or cardiovascular disease, Charlson comorbidity index, smoking, and socioeconomic status revealed an inverse association between 25-OHD and the risk of progression to IFG and diabetes.", "entity1": "LDL", "entity2": "25-OHD", "span1": [119, 122], "span2": [350, 356]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14155": {"label": 4, "data": {"text": "We previously reported that tricyclic antidepressants act as agonists at distinct opioid receptors.", "entity1": "opioid receptors", "entity2": "tricyclic", "span1": [82, 98], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7777": {"label": 0, "data": {"text": "Tub tyrosine phosphorylation (Tub-p-tyr) is modulated by nutritional status.", "entity1": "Tub", "entity2": "tyr", "span1": [0, 3], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15175": {"label": 3, "data": {"text": "GnRH stimulation of CREB phosphorylation (pCREB) in the gonadotrope-derived L\u03b2T2 cell line was attenuated by a protein kinase A (PKA) inhibitor, H89.", "entity1": "CREB", "entity2": "H89", "span1": [20, 24], "span2": [145, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5518": {"label": 3, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "AChE", "entity2": "OP", "span1": [130, 134], "span2": [40, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11460": {"label": 8, "data": {"text": "Spermidine/spermine N1-acetyltransferase (SSAT) is a key enzyme in the control of polyamine levels in human cells, as acetylation of spermidine and spermine triggers export or degradation.", "entity1": "Spermidine/spermine N1-acetyltransferase", "entity2": "spermidine", "span1": [0, 40], "span2": [133, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4635": {"label": 1, "data": {"text": "Pelargonidin activates the AhR and induces CYP1A1 in primary human hepatocytes and human cancer cell lines HepG2 and LS174T.", "entity1": "CYP1A1", "entity2": "Pelargonidin", "span1": [43, 49], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13950": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g.", "entity1": "beta(2)-adrenoceptor", "entity2": "formoterol", "span1": [35, 55], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9101": {"label": 3, "data": {"text": "Inhibition of the leukotriene synthetase of rat basophil leukemia cells by diethylcarbamazine, and synergism between diethylcarbamazine and piriprost, a 5-lipoxygenase inhibitor.", "entity1": "leukotriene synthetase", "entity2": "diethylcarbamazine", "span1": [18, 40], "span2": [75, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3996": {"label": 8, "data": {"text": "Aldose reductase (AR) catalyzes the reduction of toxic lipid aldehydes to their alcohol products and mediates inflammatory signals triggered by lipopolysaccharide (LPS).", "entity1": "Aldose reductase", "entity2": "aldehydes", "span1": [0, 16], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"12907": {"label": 3, "data": {"text": "Moreover, NO production in LPS-stimulated macrophages that are expressing CSE mRNA was significantly reduced by the addition of L-Cys, a substrate for H(2)S, but enhanced by the selective CSE inhibitor beta-cyano-L-alanine but not by the CBS inhibitor aminooxyacetic acid.", "entity1": "CBS", "entity2": "aminooxyacetic acid", "span1": [238, 241], "span2": [252, 271]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"13338": {"label": 1, "data": {"text": "Collectively then, these results indicate that LFA-1 contributes to the regulation of lymphocytic cholinergic activity via CD11a-mediated pathways and suggest that simvastatin exerts its immunosuppressive effects in part via modification of lymphocytic cholinergic activity.", "entity1": "CD11a", "entity2": "simvastatin", "span1": [123, 128], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14265": {"label": 8, "data": {"text": "Metabolism of triethylenetetramine and 1,12-diamino-3,6,9-triazadodecane by the spermidine/spermine-N(1)-acetyltransferase and thialysine acetyltransferase.", "entity1": "thialysine acetyltransferase", "entity2": "triethylenetetramine", "span1": [127, 155], "span2": [14, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3724": {"label": 3, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "Ras", "entity2": "N", "span1": [224, 227], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12076": {"label": 1, "data": {"text": "Nicotinic acid and acipimox interfere with the biosynthesis of LDL and can also improve the clearance of VLDL/LDL.", "entity1": "LDL", "entity2": "Nicotinic acid", "span1": [110, 113], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1816": {"label": 8, "data": {"text": "In this study, we have synthesized novel alpha-hydroxyphenylamide analogues of diphenylhydantoin and examined their ability to inhibit human Na(V)1.5 sodiumsodium channels expressed in Chinese Hamster Ovary (CHO-K1) cells.", "entity1": "sodium channels", "entity2": "sodium", "span1": [156, 171], "span2": [150, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11349": {"label": 3, "data": {"text": "Phenytoin (diphenylhydantoin, DPH) is an established sodium channel blocker and is a useful anticonvulsant and class 1b antiarrhythmic, and has been effectively used in the treatment of neuropathic pain.", "entity1": "sodium channel", "entity2": "diphenylhydantoin", "span1": [53, 67], "span2": [11, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10610": {"label": 1, "data": {"text": "LEV and related compounds bind to SV2A expressed in fibroblasts, indicating that SV2A is sufficient for LEV binding.", "entity1": "SV2A", "entity2": "LEV", "span1": [34, 38], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4357": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NQO1", "entity2": "\u03b2-Lapachone", "span1": [149, 153], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7862": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "tyrosine kinase", "entity2": "lavendustin A", "span1": [290, 305], "span2": [316, 329]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3778": {"label": 5, "data": {"text": "Both 5'-AMN and 5'-MABN had high affinity for \u03ba-receptors (K (i) 1.36 \u00b1 0.98 and 0.27 \u00b1 0.08, respectively) and were revealed as potent \u03ba-antagonists (pA(2) 7.43 and 8.18, respectively) and \u03bc-receptor antagonists (pA(2) 7.62 and 7.85, respectively) in the ileum.", "entity1": "\u03bc-receptor", "entity2": "5'-AMN", "span1": [190, 200], "span2": [5, 11]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4036": {"label": 8, "data": {"text": "Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4).", "entity1": "LTA(4)H", "entity2": "LTA(4)", "span1": [28, 35], "span2": [114, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5310": {"label": 2, "data": {"text": "The reduction of P2X3 expression levels was reversed by the proteasomal inhibitor MG-132.", "entity1": "P2X3", "entity2": "MG-132", "span1": [17, 21], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6775": {"label": 1, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX", "entity2": "meclofenamic acid", "span1": [119, 122], "span2": [56, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11409": {"label": 3, "data": {"text": "Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [72, 76], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10925": {"label": 3, "data": {"text": "The inhibition of ERK, moreover, did not cause attenuation in mucin secretion in response to cAMP and forskolin.", "entity1": "ERK", "entity2": "forskolin", "span1": [18, 21], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15078": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "extended-spectrum \u00df-lactamase", "entity2": "ceftazidime", "span1": [161, 190], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12605": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "serine protease domain", "entity2": "N", "span1": [283, 305], "span2": [316, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11448": {"label": 1, "data": {"text": "DAT occupancy was between 66 and 82% and <10-41% for doses of dimethocaine and procaine that maintained maximum response rates, respectively.", "entity1": "DAT", "entity2": "dimethocaine", "span1": [0, 3], "span2": [62, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2535": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine", "span1": [311, 317], "span2": [158, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2508": {"label": 3, "data": {"text": "The potent and selective third-generation aromatase inhibitors anastrozole, letrozole and exemestane were introduced to the market as endocrine therapy in postmenopausal patients failing anti-estrogen therapy alone, or multiple hormonal therapies.", "entity1": "aromatase", "entity2": "anastrozole", "span1": [42, 51], "span2": [63, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5288": {"label": 3, "data": {"text": "Vandetanib (Caprelsa(\u00ae), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60\u00a0% of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors.", "entity1": "epidermal growth-factor receptors", "entity2": "Vandetanib", "span1": [291, 324], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3006": {"label": 3, "data": {"text": "In this report, we show that the hypolipidemic agent atorvastatin is a competitive inhibitor of porcine DPP-IV in vitro, with K(i)=57.8+/-2.3 microM.", "entity1": "porcine DPP-IV", "entity2": "atorvastatin", "span1": [96, 110], "span2": [53, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8441": {"label": 2, "data": {"text": "HENA failed to activate the channels made of cbv1 + \u03b22, \u03b23, \u03b24, or \u03b21T169A, indicating that this drug selectively targets \u03b21-containing BK channels via the BK \u03b21 steroid-sensing site.", "entity1": "\u03b21-containing BK channels", "entity2": "HENA", "span1": [122, 147], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14061": {"label": 3, "data": {"text": "mTOR was still inhibited by aspirin in CRC cells after siRNA knockdown of AMPKalpha, indicating AMPK-dependent and AMPK-independent mechanisms of aspirin-induced inhibition of mTOR.", "entity1": "mTOR", "entity2": "aspirin", "span1": [0, 4], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3741": {"label": 1, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "AhR", "entity2": "2,3,7,8-tetrachlorodibenzo-p-dioxin", "span1": [346, 349], "span2": [73, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1248": {"label": 3, "data": {"text": "Amrinone and milrinone, selective PDE3 inhibitors, suppressed TNF secretion to a lesser extent.", "entity1": "PDE3", "entity2": "Amrinone", "span1": [34, 38], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9484": {"label": 3, "data": {"text": "Block of HERG with cisapride after channel activation was voltage dependent.", "entity1": "HERG", "entity2": "cisapride", "span1": [9, 13], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14518": {"label": 2, "data": {"text": "Moreover, 5-ASA treatment restored membranous expression of adhesion molecules E-cadherin and \u03b2-catenin.", "entity1": "E-cadherin", "entity2": "5-ASA", "span1": [79, 89], "span2": [10, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10186": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "SLC21A3", "entity2": "rifamycin SV", "span1": [356, 363], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1545": {"label": 8, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "PAOh1", "entity2": "N(1)-acetylspermine", "span1": [9, 14], "span2": [64, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6967": {"label": 1, "data": {"text": "As CRABPI was elevated far more than any other genes, we observed that the retinoids, all-trans retinoic acid and 9-cis retinoic acid, that bind CRABPI, promoted nitroblue tetrazolium-associated functional cell differentiation in p75NTR PC-3 cells, but not in neo control PC-3 cells.", "entity1": "p75NTR", "entity2": "retinoids", "span1": [230, 236], "span2": [75, 84]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3482": {"label": 9, "data": {"text": "Swertiamarin treatment had no significant effect on adipogenesis, or the mRNA expression of PPAR-\u03b3 and GLUT-4; however, there was a significant increase in the mRNA expression of adiponectin.", "entity1": "GLUT-4", "entity2": "Swertiamarin", "span1": [103, 109], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15980": {"label": 5, "data": {"text": "In the current study, we show that systematic modification of an aminoalkylindole scaffold identifies two new compounds with dual CB1R antagonist/CB2R agonist activity.", "entity1": "CB1R", "entity2": "aminoalkylindole", "span1": [130, 134], "span2": [65, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13821": {"label": 3, "data": {"text": "Currently, the use of orally administered MAO inhibitor antidepressants (eg, phenelzine, tranylcypromine) is limited by the risk of tyramine-provoked events (eg, acute hypertension and headache, also known as the \"cheese reaction\") when combined with dietary tyramine.", "entity1": "MAO", "entity2": "phenelzine", "span1": [42, 45], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5384": {"label": 9, "data": {"text": "Further, methylphenidate did not alter DAT cellular localization, indicating that methylphenidate treatment during adolescence regulated DAT function in SHR mPFC in a trafficking-independent manner.", "entity1": "DAT", "entity2": "methylphenidate", "span1": [39, 42], "span2": [9, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6352": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "eprosartan", "span1": [18, 21], "span2": [226, 236]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14920": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "5\u03b1-androstanediol", "span1": [266, 269], "span2": [56, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6907": {"label": 0, "data": {"text": "Unlike transferrin receptor, the protease domain of PSMA contains a binuclear zinc site, catalytic residues, and a proposed substrate-binding arginine patch.", "entity1": "PSMA", "entity2": "arginine", "span1": [52, 56], "span2": [142, 150]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6309": {"label": 8, "data": {"text": "Here, we tested the hypothesis that 5-HT receptors mediate eNOS activation by measuring agonist-stimulated [3H]L-citrulline ([3H]L-Cit) formation in BAEC cultures.", "entity1": "eNOS", "entity2": "[3H]L-Cit", "span1": [59, 63], "span2": [125, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5761": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "ubiquitin carboxy-terminal hydrolase L-1", "entity2": "1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine", "span1": [244, 284], "span2": [94, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2150": {"label": 1, "data": {"text": "2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.", "entity1": "CXC chemokine receptor 1", "entity2": "2-Arylpropionic", "span1": [16, 40], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4469": {"label": 3, "data": {"text": "Catalpol reduced the expression of pro-inflammatory mediates, such as monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-\u03b1 (TNF-\u03b1), inducible NO synthase (iNOS), and receptor for AGE (RAGE).", "entity1": "iNOS", "entity2": "Catalpol", "span1": [166, 170], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11054": {"label": 9, "data": {"text": "Similar to the plasma membrane PS transporter, Atp8a1 is activated only by the naturally occurring sn-1,2-glycerol isomer of PS and not the sn-2,3-glycerol stereoisomer.", "entity1": "Atp8a1", "entity2": "sn-2,3-glycerol", "span1": [47, 53], "span2": [140, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"680": {"label": 8, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "GTP cyclohydrolase I", "entity2": "tetrahydrobiopterin", "span1": [56, 76], "span2": [131, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"14020": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "IkappaB kinase", "entity2": "colchicoside", "span1": [151, 165], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7983": {"label": 1, "data": {"text": "MAPK signaling pathways regulate mitochondrial-mediated apoptosis induced by isoorientin in human hepatoblastoma cancer cells.", "entity1": "MAPK", "entity2": "isoorientin", "span1": [0, 4], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6830": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "receptor tyrosine kinase", "entity2": "SU11248", "span1": [120, 144], "span2": [170, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10616": {"label": 1, "data": {"text": "Furthermore, GABA receptors of horizontal cells were modulated by extracellular application of diazepam, zolpidem, methyl 6,7-dimethoxy-4-ethyl-beta-carboxylate, pentobarbital, and alphaxalone, thus showing typical pharmacological properties of CNS GABAA receptors.", "entity1": "GABA receptors", "entity2": "zolpidem", "span1": [13, 27], "span2": [105, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15224": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "COX-2", "entity2": "CLS", "span1": [288, 293], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13269": {"label": 2, "data": {"text": "CONCLUSION: In postmenopausal women, isolated isoflavone treatment does not affect ABCA1-dependent cholesterol efflux potential from macrophages but increases circulating pre-beta high-density lipoprotein level, which could provide beneficial vascular effects.", "entity1": "pre-beta high-density lipoprotein", "entity2": "isoflavone", "span1": [171, 204], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13089": {"label": 1, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "peroxisome proliferator-activated receptor", "entity2": "thiazolidinediones", "span1": [175, 217], "span2": [260, 278]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1147": {"label": 3, "data": {"text": "The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.", "entity1": "HER2", "entity2": "ZD1839", "span1": [57, 61], "span2": [30, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15352": {"label": 0, "data": {"text": "In contrast, the EL2 sequence showed well-defined structure only near its C-terminal residues.", "entity1": "EL2", "entity2": "C", "span1": [17, 20], "span2": [74, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1783": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1aAR", "entity2": "doxazosin", "span1": [40, 49], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15388": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "activin receptor-like kinase 5", "entity2": "TASP0382088", "span1": [197, 227], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7740": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "MET", "entity2": "cabozantinib", "span1": [55, 58], "span2": [16, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15659": {"label": 8, "data": {"text": "In the current study, we extend these findings to show that the ability of astrocytes to buffer extracellular glutamate is reduced when CaMKII is inhibited.", "entity1": "CaMKII", "entity2": "glutamate", "span1": [136, 142], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9608": {"label": 1, "data": {"text": "The KATP channel is a heterooligomeric complex of SUR1 subunits of the ATP-binding-cassette superfamily with two nucleotide-binding folds (NBF1 and NBF2) and the pore-forming Kir6.2 subunits.", "entity1": "NBF1", "entity2": "ATP", "span1": [139, 143], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8794": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "cyclin D1", "entity2": "CAPE", "span1": [246, 255], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5553": {"label": 3, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "glutathione reductase", "entity2": "BCNU", "span1": [40, 61], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1292": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "GAD", "entity2": "GABA", "span1": [50, 53], "span2": [134, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"2639": {"label": 1, "data": {"text": "Exogenous all-trans-retinol, all-trans-13,14-dihydroretinol, or all-trans-7,8-dihydroretinol led to the strong induction of the expression of the retinoic acid-metabolizing enzyme, Cyp26A1, arguing for an active signaling function of dihydroretinoid metabolites in zebrafish.", "entity1": "Cyp26A1", "entity2": "all-trans-7,8-dihydroretinol", "span1": [181, 188], "span2": [64, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12189": {"label": 1, "data": {"text": "Several variables associated to thymidylate synthase (TS), the biological target of 5-fluorouracil (5FU) have been studied for their possible role as predictors of the clinical outcome and response to chemotherapy in colorectal cancer (CRC) patients.", "entity1": "thymidylate synthase", "entity2": "5-fluorouracil", "span1": [32, 52], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12782": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "S-1", "span1": [22, 24], "span2": [147, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3420": {"label": 2, "data": {"text": "The treatment with arsenic exhibited a significant increase in some serum hepatic and renal biochemical parameters (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total protein, albumin, bilirubin, cholesterol, urea and creatinine).", "entity1": "albumin", "entity2": "arsenic", "span1": [207, 214], "span2": [19, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14406": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "ESI-09", "span1": [254, 258], "span2": [145, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3801": {"label": 2, "data": {"text": "An increase in the ADP/ATP ratio opens K(ATP) channels, leading to membrane hyperpolarization.", "entity1": "K(ATP) channels", "entity2": "ATP", "span1": [39, 54], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15907": {"label": 1, "data": {"text": "Therefore, in addition to its previously described functions, synaptotagmin-1 is involved in a rapid vesicular Ca(2+) sequestration through a Ca(2+) /H(+) antiport.", "entity1": "synaptotagmin-1", "entity2": "Ca(2+)", "span1": [62, 77], "span2": [142, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7298": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "Bile acid-coenzyme A:amino acid N-acyltransferase", "entity2": "glycine", "span1": [12, 61], "span2": [167, 174]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12608": {"label": 3, "data": {"text": "It appears likely that the histamine H2 receptor blocked by cimetidine obviated the pulmonary vasodilator effect of tolazoline therapy.", "entity1": "histamine H2 receptor", "entity2": "cimetidine", "span1": [27, 48], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7996": {"label": 2, "data": {"text": "While SP600125 (a JNK inhibitor) and SB203580 (a p38 inhibitor) markedly prevented the expression of these proteins induced by ISO.", "entity1": "p38", "entity2": "ISO", "span1": [49, 52], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12079": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase", "entity2": "pregnenolone", "span1": [0, 72], "span2": [132, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6195": {"label": 3, "data": {"text": "The cardiovascular effects of three different acetylcholinesterase inhibitors: physostigmine, tacrine and rivastigmine injected by intravenous (i.v.)", "entity1": "acetylcholinesterase", "entity2": "rivastigmine", "span1": [46, 66], "span2": [106, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14410": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "nucleotide", "span1": [254, 258], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7505": {"label": 1, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "Na+K+ATPase", "entity2": "ouabain", "span1": [283, 294], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"433": {"label": 1, "data": {"text": "Ka values in nM for rauwolscine (19), WB-4101 (265), SKF-104078 (197), spiroxatrine (128), and prazosin (1531) for blocking relaxation in rat arteries were consistent with their affinities for binding at the alpha-2D adrenoceptor subtype.", "entity1": "alpha-2D adrenoceptor", "entity2": "WB-4101", "span1": [208, 229], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4026": {"label": 3, "data": {"text": "Central and peripheral administration of kisspeptin stimulates the hypothalamic-pituitary-gonadal (HPG) axis whilst pre-administration of a gonadotrophin releasing hormone (GnRH) antagonist abolishes this effect.", "entity1": "kisspeptin", "entity2": "gonadotrophin releasing hormone", "span1": [41, 51], "span2": [140, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10482": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "fenoterol", "span1": [392, 423], "span2": [142, 151]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6153": {"label": 1, "data": {"text": "Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C.", "entity1": "cardiac troponin C", "entity2": "bepridil", "span1": [68, 86], "span2": [36, 44]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5058": {"label": 2, "data": {"text": "Taken together, our results suggested that Rg1 protected against A\u03b225-35-induced apoptosis at least in part by two complementary GR-dependent ERK phosphorylation pathways: (1) down-regulating HIF-1\u03b1 initiated protein nitrotyrosination, and (2) inhibiting mitochondrial apoptotic cascades.", "entity1": "ERK", "entity2": "Rg1", "span1": [142, 145], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3253": {"label": 1, "data": {"text": "The other endogenous steroids, androstenedione (ANE) and dihydrotestosterone (DHT), had considerably lower hAR transport rates.", "entity1": "hAR", "entity2": "dihydrotestosterone", "span1": [107, 110], "span2": [57, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10661": {"label": 2, "data": {"text": "Treatment of both differentiating adipocytes and fully differentiated adipocytes with telmisartan caused a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin.", "entity1": "adiponectin", "entity2": "telmisartan", "span1": [189, 200], "span2": [86, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6307": {"label": 5, "data": {"text": "These responses were effectively blocked by the 5-HT1B receptor antagonist, isamoltane, the 5-HT1B/5-HT2 receptor antagonist, methiothepin, and the eNOS selective antagonists (0.01-10 microM): L-Nomega -monomethyl-L-arginine (L-NMMA) and L-N omega-iminoethyl-L-ornithine (L-NIO).", "entity1": "eNOS", "entity2": "L-NIO", "span1": [148, 152], "span2": [272, 277]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3848": {"label": 1, "data": {"text": "Using the viral mimic polyinosinic:polycytidylic acid and the IFN\u03b1/\u03b2 antagonist B18R we furthermore demonstrate the capability of endogenous IFN to promote IL-22-induced STAT1 activation and expression of CXCL10.", "entity1": "STAT1", "entity2": "polyinosinic:polycytidylic acid", "span1": [170, 175], "span2": [22, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8140": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "cytochrome-C-oxidase", "entity2": "Isoproterenol", "span1": [387, 407], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1383": {"label": 2, "data": {"text": "Since gemfibrozil is known to activate peroxisome proliferator-activated receptor-alpha (PPAR-alpha), we investigated the role of PPAR-alpha in gemfibrozil-mediated inhibition of iNOS.", "entity1": "PPAR-alpha", "entity2": "gemfibrozil", "span1": [130, 140], "span2": [144, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11875": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "pelargonidin", "span1": [118, 143], "span2": [97, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12936": {"label": 3, "data": {"text": "CONCLUSIONS: Although CRF does not change the abundance or intrinsic properties of arginase, the inherent rise in urea concentration inhibits its enzymatic activity.", "entity1": "arginase", "entity2": "urea", "span1": [83, 91], "span2": [114, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2434": {"label": 9, "data": {"text": "Qualitatively similar but significantly attenuated responses to the catecholamines were observed in tissue from ANXA1-null mice, an effect that was not associated with changes in beta-adrenoceptor mRNA expression.", "entity1": "beta-adrenoceptor", "entity2": "catecholamines", "span1": [179, 196], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7531": {"label": 3, "data": {"text": "While vitamin C is essential for PHD activity in vitro, N-acetyl-L-cysteine had no effect, and gallic acid or n-propyl gallate efficiently inhibited the activity of all three PHDs, demonstrating different functions of these antioxidants.", "entity1": "PHDs", "entity2": "n-propyl gallate", "span1": [175, 179], "span2": [110, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2417": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "arginase I", "entity2": "nitric oxide", "span1": [219, 229], "span2": [21, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11301": {"label": 8, "data": {"text": "The protein exhibited modest H(2)O(2)-dependent peroxidase activities with guaiacol, potassium iodide, and 2,2(')-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS).", "entity1": "peroxidase", "entity2": "ABTS", "span1": [48, 58], "span2": [164, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10349": {"label": 9, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK4-8", "entity2": "omapatrilat", "span1": [95, 102], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"11528": {"label": 3, "data": {"text": "The results suggest that the suppression of TLR4 activity by auranofin may be the molecular mechanism through which auranofin exerts anti-rheumatic activity.", "entity1": "TLR4", "entity2": "auranofin", "span1": [44, 48], "span2": [116, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2890": {"label": 4, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1)-adrenoceptor", "entity2": "phenylephrine", "span1": [23, 44], "span2": [300, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"448": {"label": 4, "data": {"text": "These results suggest that epinastine, although identified as a 5-HT antagonist, acts as a 5-HT1 agonist and that it inhibits the noncholinergic contraction in guinea-pig airways through stimulation of a prejunctional 5-HT1-like receptor, located to sensory nerves.", "entity1": "5-HT1", "entity2": "epinastine", "span1": [91, 96], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11955": {"label": 8, "data": {"text": "UGT1A6 exhibited a significantly higher Vmax and Km values toward both HFC and UDP-glucuronic acid than the other UGTs.", "entity1": "UGTs", "entity2": "glucuronic acid", "span1": [114, 118], "span2": [83, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9219": {"label": 1, "data": {"text": "Three lines of evidence suggest that calmodulin inhibition is not responsible for the inhibition of binding and endocytosis: 1) Promethazine, a phenothiazine that is a poor inhibitor of calmodulin, is nearly as effective as TFP at inhibiting endocytosis; calmidazolium, a potent inhibitor of several calmodulin functions, did not cause a loss of binding; 2) the microinjection of calmodulin into cells did not reverse the effects of W-7; using pressure microinjection, we introduced up to a 100-fold excess of calmodulin over native levels into individual gerbil fibroma cells; using rhodamine-labeled alpha 2-macroglobulin, we saw that the W-7 induced inhibition of receptor-mediated endocytosis was the same in injected and uninjected cells; 3) we injected calcineurin, a calmodulin-binding protein, into cells (1-3 pg/cell) and observed no effect on the receptor-mediated endocytosis of rhodamine-labeled alpha 2-macroglobulin.", "entity1": "alpha 2-macroglobulin", "entity2": "rhodamine", "span1": [908, 929], "span2": [890, 899]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10820": {"label": 9, "data": {"text": "Treatment with valsartan, doxazosin, or N-acetylcysteine did not significantly affect HIF-1alpha and VEGF proteins expression in the banding groups.", "entity1": "HIF-1alpha", "entity2": "N-acetylcysteine", "span1": [86, 96], "span2": [40, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6572": {"label": 1, "data": {"text": "The comparison between MalP structures shows that His377, through a hydrogen bond with the 6-hydroxyl group of Glc1P substrate, triggers a conformational change of the 380s loop.", "entity1": "MalP", "entity2": "6-hydroxyl", "span1": [23, 27], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15598": {"label": 1, "data": {"text": "TCPOBOP, a CAR ligand, modestly induced mdr1a.fLUC in pxr(+/+) and pxr(-/-) strains, consistent with CAR's minor role in mdr1a regulation.", "entity1": "CAR", "entity2": "TCPOBOP", "span1": [11, 14], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12583": {"label": 3, "data": {"text": "After 7 days of DMI administration the number of beta-adrenoceptors was lower in frontal and occipital cortex and hippocampus.", "entity1": "beta-adrenoceptors", "entity2": "DMI", "span1": [49, 67], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3155": {"label": 3, "data": {"text": "INTRODUCTION: In this study, we examined the effects of the alpha-glucosidase inhibitors acarbose and voglibose on postprandial plasma glucose and serum triglyceride levels in patients with type 2 diabetes mellitus.", "entity1": "alpha-glucosidase", "entity2": "voglibose", "span1": [60, 77], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8319": {"label": 2, "data": {"text": "The food contaminant deoxynivalenol activates the mitogen activated protein kinases in the intestine: interest of ex vivo models as an alternative to in vivo experiments.", "entity1": "mitogen activated protein kinases", "entity2": "deoxynivalenol", "span1": [50, 83], "span2": [21, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7997": {"label": 3, "data": {"text": "ISO is able to induce apoptosis through mitochondrial dysfunction and inhibition of PI3K/Akt signaling pathway in HepG2 cells, however, the effects of ISO on MAPK signaling pathways remain unknown.", "entity1": "PI3K", "entity2": "ISO", "span1": [84, 88], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11537": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "TDI", "span1": [103, 106], "span2": [217, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10641": {"label": 8, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "Bsep", "entity2": "taurocholate", "span1": [76, 80], "span2": [99, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6270": {"label": 3, "data": {"text": "In both vascular preparations, candesartan caused a marked decrease in the maximal contractile response of the angiotensin II (Ang II) concentration-response curve.", "entity1": "angiotensin II", "entity2": "candesartan", "span1": [111, 125], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9764": {"label": 5, "data": {"text": "In guinea pigs, antagonist actions of yohimbine at 5-HT(1B) receptors are revealed by blockade of hypothermia evoked by the 5-HT(1B) agonist, GR46,611.", "entity1": "5-HT(1B)", "entity2": "yohimbine", "span1": [51, 59], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8916": {"label": 1, "data": {"text": "Carvedilol produced significant inhibition of the alpha 1 adrenoceptor mediated pressor response to cirazoline in the pithed rat, but had no effect on the alpha 2 adrenoceptor mediated pressor response to B-HT 933, suggesting that carvedilol is also an alpha 1 adrenoceptor antagonist at antihypertensive doses.", "entity1": "alpha 1 adrenoceptor", "entity2": "cirazoline", "span1": [50, 70], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4221": {"label": 2, "data": {"text": "With the elevated doses of PhIP, malondialdehyde (MDA) contents, protein carbonyl (PCO) contents and DNA-protein crosslinks (DPC) coefficients were significantly raised in a dose-dependent manner; (3) PhIP at the doses of 10mg/kg and/or 15mg/kg significantly inhibited p16 mRNA and protein expression, whereas enhanced c-fos and c-jun expression relative to control.", "entity1": "c-fos", "entity2": "PhIP", "span1": [319, 324], "span2": [201, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10511": {"label": 1, "data": {"text": "GW572016 radiosensitized EGFR-overexpressing cell lines, but HER2-overexpressing cells were unable to form colonies after brief exposure to GW572016 even in the absence of radiation, and thus could not be evaluated for radiosensitization.", "entity1": "EGFR", "entity2": "GW572016", "span1": [25, 29], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13819": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "kinase", "entity2": "Sunitinib", "span1": [247, 253], "span2": [191, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6279": {"label": 3, "data": {"text": "Dose-dependent inhibition of platelet cyclooxygenase-1 and monocyte cyclooxygenase-2 by meloxicam in healthy subjects.", "entity1": "cyclooxygenase-2", "entity2": "meloxicam", "span1": [68, 84], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10378": {"label": 3, "data": {"text": "In this work a novel approach combining HPLC-UV on-line with oaTOF-MS and ICPMS was applied to investigate in human and rat plasma the metabolism of labelled BK (79/81 Br-Phe5) BrBK in the presence of two new dual ACE/NEP inhibitors (GW660511X and omapatrilat) currently under clinical trial.", "entity1": "ACE", "entity2": "omapatrilat", "span1": [214, 217], "span2": [248, 259]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1458": {"label": 3, "data": {"text": "), did not induce the behavioural hyperactivity syndrome which is seen following inhibition of both MAO-A and MAO-B by tranylcypromine together with the monoamine precursors.", "entity1": "MAO-A", "entity2": "tranylcypromine", "span1": [100, 105], "span2": [119, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5687": {"label": 2, "data": {"text": "Sprague-Dawley rats treated with a non-selective cannabinoid agonist (CP55940, 50\u03bcg/kg, 7 days, i.p.) showed enhanced co-immunoprecipitation of \u03b2-Arrestin 2 and ERK1/2, enhanced pERK protein levels, and enhanced expression of \u03b2-Arrestin 2 mRNA and protein levels in PFCx.", "entity1": "pERK", "entity2": "CP55940", "span1": [178, 182], "span2": [70, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7421": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "Delta 6 desaturase", "entity2": "docosahexaenoic acid", "span1": [11, 29], "span2": [102, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2616": {"label": 9, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "T700A", "entity2": "foscarnet", "span1": [97, 102], "span2": [79, 88]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13930": {"label": 3, "data": {"text": "Both drugs at the tested doses (0.042-0.33 mug/kg) suppressed PTH mRNA expression and serum PTH effectively in the 5/6 NX rats, but paricalcitol was less potent in raising serum Ca than doxercalciferol.", "entity1": "PTH", "entity2": "paricalcitol", "span1": [92, 95], "span2": [132, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11198": {"label": 1, "data": {"text": "BACKGROUND: SerotoninSerotonin 5-HT(4) receptors are located on enteric cholinergic neurones and may regulate peristalsis.", "entity1": "Serotonin 5-HT(4) receptors", "entity2": "Serotonin", "span1": [21, 48], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2059": {"label": 1, "data": {"text": "This alternate conformation now causes a steric hindrance to the O4 hydroxyl group of the Gal moiety of UDP-Gal, probably causing the dissociation of UDP-Gal and the reduced k(cat) of the Gal-T reaction.", "entity1": "Gal-T", "entity2": "UDP-Gal", "span1": [188, 193], "span2": [150, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11998": {"label": 1, "data": {"text": "We found that in vitro rapamycin also regulates the proteasome, an essential intracellular protease of the ubiquitin-proteasome pathway.", "entity1": "ubiquitin", "entity2": "rapamycin", "span1": [107, 116], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6456": {"label": 3, "data": {"text": "Protective effect of halothane anesthesia on retinal light damage: inhibition of metabolic rhodopsin regeneration.", "entity1": "rhodopsin", "entity2": "halothane", "span1": [91, 100], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6438": {"label": 4, "data": {"text": "RESULT(S): Buserelin acetate, a GnRH agonist (0.1-10 ng/mL), had no significant effect on MCP-1 expression, whereas danazol (10(-7)-10(-5) M), a testosterone analog, and dexamethasone, an anti-inflammatory glucocorticoid hormone (10(-12)-10(-6)M), showed a direct and a dose-dependent inhibitory effect on MCP-1 expression.", "entity1": "GnRH", "entity2": "Buserelin acetate", "span1": [32, 36], "span2": [11, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1771": {"label": 1, "data": {"text": "We have adenovirally overexpressed beta(1)-adrenoceptors in isolated, cultured adult rat ventricular cardiomyocytes and observed the inotropic potency of isoprenaline and CGP 12177A (in the presence of 1 microm propranolol).", "entity1": "beta(1)-adrenoceptors", "entity2": "CGP 12177A", "span1": [35, 56], "span2": [171, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3606": {"label": 6, "data": {"text": "Ifenprodil is an allosteric inhibitor of GluN1/GluN2B N-methyl-D-aspartate receptors.", "entity1": "GluN1", "entity2": "Ifenprodil", "span1": [41, 46], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"14082": {"label": 3, "data": {"text": "In TGF-\u03b21-induced NPDFs, berberine significantly inhibited the expression of \u03b1-SMA and collagen type I mRNA and reduced \u03b1-SMA and collagen protein levels.", "entity1": "collagen", "entity2": "berberine", "span1": [130, 138], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15431": {"label": 2, "data": {"text": "In lymphocytes, the NTPDase and ADA activities were increased in all groups treated with caffeic acid when compared to control (P<0.05).", "entity1": "ADA", "entity2": "caffeic acid", "span1": [32, 35], "span2": [89, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15281": {"label": 6, "data": {"text": "Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.", "entity1": "CC-chemokine receptor 4", "entity2": "indazole arylsulfonamides", "span1": [90, 113], "span2": [50, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"12992": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "Erg24p", "entity2": "phenylmorpholines", "span1": [134, 140], "span2": [4, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7769": {"label": 1, "data": {"text": "GDC-0152 induces NF-\u03baB transcriptional activity leading to expression of several chemokines and cytokines, of which tumor necrosis factor alpha (TNF-\u03b1) is the most important for single-agent tumor activity.", "entity1": "tumor necrosis factor alpha", "entity2": "GDC-0152", "span1": [116, 143], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13978": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Msx1", "entity2": "chlorcyclizine", "span1": [112, 116], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13177": {"label": 2, "data": {"text": "Progestin induction of the cyclin D1 gene, which lacks a progesterone response element, was dependent on PR activation of the Src/MAPK pathway, whereas induction of the Sgk (serum and glucocorticoid regulated kinase) gene that contains a functional progesterone response element was unaffected by mutations that interfere with PR activation of Src.", "entity1": "Src", "entity2": "Progestin", "span1": [126, 129], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4726": {"label": 3, "data": {"text": "We discovered that each RSPO alone or in combination partially rescues TCDD inhibition of both canonical Wnt signaling and prostatic bud formation.", "entity1": "Wnt", "entity2": "TCDD", "span1": [105, 108], "span2": [71, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6341": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "irbesartan", "span1": [25, 28], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14339": {"label": 3, "data": {"text": "In summary, DMF attenuated renal fibrosis via the Nrf2-mediated inhibition of TGF-beta/Smad3 signaling in an ARE-independent manner, suggesting that DMF could be used to treat renal fibrosis.", "entity1": "TGF-beta", "entity2": "DMF", "span1": [78, 86], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"176": {"label": 5, "data": {"text": "Derivatives of 5-(dipentylamino)-5-oxo-pentanoic acid are a new class of non-peptide cholecystokinin (CCK) antagonists.", "entity1": "cholecystokinin", "entity2": "5-(dipentylamino)-5-oxo-pentanoic acid", "span1": [85, 100], "span2": [15, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5328": {"label": 3, "data": {"text": "Pasireotide (Signifor(\u00ae)) is a new subcutaneous somatostatin analogue that acts via somatostatin receptors to inhibit the secretion of corticotropin from the pituitary adenoma in patients with Cushing's disease.", "entity1": "corticotropin", "entity2": "Pasireotide", "span1": [135, 148], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11283": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "serine hydroxymethyltransferase", "entity2": "Gly", "span1": [133, 164], "span2": [198, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15560": {"label": 1, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "Akt", "entity2": "puerarin", "span1": [147, 150], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3938": {"label": 2, "data": {"text": "AChE was easier reactivated after paraoxon treatment.", "entity1": "AChE", "entity2": "paraoxon", "span1": [0, 4], "span2": [34, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11509": {"label": 8, "data": {"text": "Choline dehydrogenase (CHDH) and betaine-homocysteine methyltransferase (BHMT) are 2 enzymes involved in choline oxidation.", "entity1": "Choline dehydrogenase", "entity2": "choline", "span1": [0, 21], "span2": [105, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9284": {"label": 5, "data": {"text": "Incubation of rat aortic membranes with the irreversible alpha 1B-adrenoceptor antagonist, chloroethylclonidine (CEC: 10 microM) did not change the KD of [3H]-prazosin binding in comparison to untreated membranes, but reduced by 88% the total number of binding sites (Bmax).", "entity1": "alpha 1B-adrenoceptor", "entity2": "CEC", "span1": [57, 78], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6796": {"label": 0, "data": {"text": "The x-ray structure of the enzyme revealed an important structural difference between this protein and other aldehyde dehydrogenases of the same enzyme superfamily; a 20-amino acid span in the substrate access channel in retinaldehyde dehydrogenase II is disordered, whereas in other aldehyde dehydrogenases this region forms a well defined wall of the substrate access channel.", "entity1": "retinaldehyde dehydrogenase II", "entity2": "amino acid", "span1": [221, 251], "span2": [170, 180]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2528": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "human b5R", "entity2": "4-aminobiphenyl", "span1": [297, 306], "span2": [81, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5391": {"label": 3, "data": {"text": "In both OFC and mPFC, no strain differences in Vmax or Km for dopamine uptake into synaptosomes were found between vehicle-treated SHR, WKY and WIS. Methylphenidate increased DAT Vmax in SHR mPFC and decreased DAT Vmax in WKY OFC.", "entity1": "DAT", "entity2": "Methylphenidate", "span1": [210, 213], "span2": [149, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15429": {"label": 3, "data": {"text": "In non-pre-treated cells, only efflux transporters were down-regulated by 7-ketosterols, showing a greater influence upon ABCG5 expression.", "entity1": "efflux transporters", "entity2": "7-ketosterols", "span1": [31, 50], "span2": [74, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9302": {"label": 3, "data": {"text": "The present study utilized blood from normal volunteers and 125I-fibrinogen in a dilute whole blood clot assay to determine the relative concentrations of lysine analogues required for inhibition of clot lysis induced by exogenous t-PA. AMCA (0.06 mM) and EACA (0.6 mM) were effective in prolonging clot lysis if (1) whole blood clots were formed and then exposed to a lysine analogue and exogenous t-PA or if (2) whole blood clots were formed in the presence of exogenous t-PA and a lysine analogue.", "entity1": "t-PA", "entity2": "AMCA", "span1": [473, 477], "span2": [237, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10665": {"label": 8, "data": {"text": "Of note, we demonstrated for the first time that telmisartan augmented GLUT4 protein expression and 2-deoxy glucose uptake both in basal and insulin-stimulated state of adipocytes, which may contribute, at least partly, to its insulin-sensitizing ability.", "entity1": "GLUT4", "entity2": "2-deoxy glucose", "span1": [71, 76], "span2": [100, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14970": {"label": 3, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "TRAP", "entity2": "cysteine", "span1": [196, 200], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6111": {"label": 3, "data": {"text": "The results when considered with previous reports in the literature show that amezinium is about 1000 times more potent and debrisoquine is about 20 times more potent for MAO inhibition in rat lungs than in tissue homogenates, and the reason for their high potencies in the intact lungs is transport and accumulation of the drugs in the pulmonary endothelial cells by uptake1.", "entity1": "MAO", "entity2": "amezinium", "span1": [171, 174], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6587": {"label": 8, "data": {"text": "It is caused by a deficiency of propionyl-CoA carboxylase (PCC, EC 6.4.1.3), a biotin-dependent enzyme that catalyzes the carboxylation of propionyl-CoA to D-methylmalonyl-CoA.", "entity1": "PCC", "entity2": "D-methylmalonyl-CoA", "span1": [59, 62], "span2": [156, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5336": {"label": 3, "data": {"text": "No effects were observed when fenclozic acid was assessed for P450-dependent and P450-independent cytotoxicity to THLE cell lines, time-dependent inhibition of five major human cytochrome P450 enzymes, inhibition of the biliary efflux transporters BSEP and MRP2 or mitochondrial toxicity to THLE or HepG2 cells.", "entity1": "BSEP", "entity2": "fenclozic acid", "span1": [248, 252], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10459": {"label": 8, "data": {"text": "Formation of pyruvate by SDH is a two-step reaction in which the hydroxyl group of serine is cleaved to produce aminoacrylate, and then the aminoacrylate is deaminated by nonenzymatic hydrolysis to produce pyruvate.", "entity1": "SDH", "entity2": "aminoacrylate", "span1": [25, 28], "span2": [112, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5755": {"label": 3, "data": {"text": "All these results demonstrate that vitamin C prevents CS(E)-induced NF-\u03baB activation and thus it could be used for the prevention of CS-induced inflammatory diseases.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [68, 73], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10517": {"label": 3, "data": {"text": "CONCLUSION: GW572016 potently inhibits receptor phosphorylation in either EGFR- or HER2-overexpressing cell lines and has both antiproliferative and radiosensitizing effects.", "entity1": "EGFR", "entity2": "GW572016", "span1": [74, 78], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5559": {"label": 2, "data": {"text": "Experimental manipulation of the intracellular GSSG concentration during inhibition of cellular prooxidant production demonstrated that increased intracellular GSSG is a primary signal that is directly or indirectly required for CpG-induced NF-kappaB activation but is not in itself sufficient to trigger this in the absence of CpG ODN.", "entity1": "NF-kappaB", "entity2": "GSSG", "span1": [241, 250], "span2": [47, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"7651": {"label": 2, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-9", "entity2": "monocrotaline", "span1": [10, 15], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8315": {"label": 1, "data": {"text": "Refining the UGT1A haplotype associated with irinotecan-induced hematological toxicity in metastatic colorectal cancer patients treated with 5-fluorouracil/irinotecan-based regimens.", "entity1": "UGT1A", "entity2": "5-fluorouracil", "span1": [13, 18], "span2": [141, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1889": {"label": 1, "data": {"text": "I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance.", "entity1": "C1b domain", "entity2": "PMA", "span1": [62, 72], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2509": {"label": 8, "data": {"text": "In breast cancer, intratumoural aromatase is the source for local estrogen production in the tissue.", "entity1": "aromatase", "entity2": "estrogen", "span1": [32, 41], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5121": {"label": 3, "data": {"text": "In addition, 5HHMF blocked LPS-induced phosphorylation of I\u03baB, resulting in suppression of the nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) subunits, namely p65 and p50, which are important molecules involved in the regulation of iNOS expression.", "entity1": "NF-\u03baB", "entity2": "5HHMF", "span1": [139, 144], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4851": {"label": 3, "data": {"text": "Moreover, they established that the inhibitory effect of cucurbitacin I on Rac1 activity involves the alteration of the balance between Rho and Rac.", "entity1": "Rac1", "entity2": "cucurbitacin I", "span1": [75, 79], "span2": [57, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8348": {"label": 4, "data": {"text": "High throughput screening led to the identification of a novel series of quinolone \u03b17 nicotinic acetylcholine receptor (nAChR) agonists.", "entity1": "nAChR", "entity2": "quinolone", "span1": [120, 125], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5072": {"label": 9, "data": {"text": "In addition to CYP2B6, anisomycin co-treatment potentiated an increase in CYP2A7 and CYP2C9 mRNAs but not CYP3A4 or UDP-glucuronosyltransferase 1A1 mRNAs.", "entity1": "UDP-glucuronosyltransferase 1A1", "entity2": "anisomycin", "span1": [116, 147], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10929": {"label": 8, "data": {"text": "Both inhibitors, moreover, blunted the mucin secretory responses to beta-adrenergic agonist-generated second messenger, cAMP as well as adenylate cyclase activator, forskolin.", "entity1": "adenylate cyclase", "entity2": "cAMP", "span1": [136, 153], "span2": [120, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14990": {"label": 9, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "CD69", "entity2": "DHA", "span1": [277, 281], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12628": {"label": 1, "data": {"text": "The FP receptor bound PGF2 alpha and fluprostenol with Ki values of 3-4 nM.", "entity1": "FP receptor", "entity2": "fluprostenol", "span1": [4, 15], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"369": {"label": 3, "data": {"text": "GCS therapy results in reduced mRNA expression of interleukin-4 (IL-4) and IL-5 in cells from bronchoalveolar lavage (BAL) but not of IFN-gamma.", "entity1": "interleukin-4", "entity2": "GCS", "span1": [50, 63], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11012": {"label": 2, "data": {"text": "The mean body weight at baseline (52.59 kg) did not differ significantly from that at 1 week after treatment (52.84 kg; P > .05), but the mean leptin level after 1 week of treatment with cyproheptadine (3.14 ng/mL) was 14.2% higher than that at baseline (2.75 ng/mL; P < .05).", "entity1": "leptin", "entity2": "cyproheptadine", "span1": [143, 149], "span2": [187, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6382": {"label": 8, "data": {"text": "Ornithine decarboxylase (ODC) catalyses the first step in the synthesis of the polyamines putrescine, spermidine and spermine.", "entity1": "ODC", "entity2": "spermidine", "span1": [25, 28], "span2": [102, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1059": {"label": 8, "data": {"text": "Follicle-stimulating hormone (FSH), a dimeric glycoprotein synthesized in the anterior pituitary gland, is important for the production of sex steroids and gametes.", "entity1": "FSH", "entity2": "steroids", "span1": [30, 33], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3713": {"label": 2, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "Bim", "entity2": "BPs", "span1": [159, 162], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11595": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "cystathionine-beta-synthase", "entity2": "H(2)S", "span1": [111, 138], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13023": {"label": 8, "data": {"text": "Once formed, the molecule can be converted to glycine by alanine-glyoxylate aminotransferase (AGAT).", "entity1": "AGAT", "entity2": "glycine", "span1": [94, 98], "span2": [46, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"13553": {"label": 0, "data": {"text": "PURPOSE: Cellular retinaldehyde-binding protein (CRALBP), transcribed from the RLBP1 gene, is a 36-kDa water-soluble protein with 316 amino acids found in the retinal pigment epithelium (RPE) and in retinal Muller cells.", "entity1": "36-kDa water-soluble protein", "entity2": "amino acids", "span1": [96, 124], "span2": [134, 145]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15011": {"label": 1, "data": {"text": "Involvement of Src and the actin cytoskeleton in the antitumorigenic action of adenosine dialdehyde.", "entity1": "actin", "entity2": "adenosine dialdehyde", "span1": [27, 32], "span2": [79, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3573": {"label": 2, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u. ), exercise training also increased it in both groups (control, 13.6\u00a0\u00b1\u00a00.1; MSG, 22.2\u00a0\u00b1\u00a01.1\u00a0a.u.).", "entity1": "pIRS-1", "entity2": "MSG", "span1": [74, 80], "span2": [209, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15646": {"label": 1, "data": {"text": "With the former, abacavir seemingly participates in the MHC T-cell receptor binding interaction.", "entity1": "MHC", "entity2": "abacavir", "span1": [56, 59], "span2": [17, 25]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4659": {"label": 2, "data": {"text": "SIRT1 co-precipitated with PPAR\u03b1 and nicotinamide increased the acetylation of the PPAR\u03b1 coactivator PGC-1\u03b1, which was suppressed by resveratrol.", "entity1": "PGC-1\u03b1", "entity2": "nicotinamide", "span1": [101, 107], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6845": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "MTHFR", "entity2": "Hcy", "span1": [119, 124], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1693": {"label": 5, "data": {"text": "Like other NMDA receptor antagonists, memantine at high concentrations can inhibit mechanisms of synaptic plasticity that are believed to underlie learning and memory.", "entity1": "NMDA receptor", "entity2": "memantine", "span1": [11, 24], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7172": {"label": 5, "data": {"text": "OBJECTIVE: Telmisartan, an angiotensin II type 1 receptor (AT1R) antagonist, was found to have a unique property: it is a partial agonist of peroxisome proliferator-activated receptor gamma (PPARgamma).", "entity1": "AT1R", "entity2": "Telmisartan", "span1": [59, 63], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2495": {"label": 3, "data": {"text": "Licofelone, a dual anti-inflammatory drug that inhibits 5-lipoxygenase (LOX) and cyclooxygenase (COX) enzymes, may have a better cardiovascular profile that cycloxygenase-2 inhibitors due to cycloxygenase-1 blockade-mediated antithrombotic effect and a better gastrointestinal tolerability.", "entity1": "5-lipoxygenase", "entity2": "Licofelone", "span1": [56, 70], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12212": {"label": 1, "data": {"text": "This mechanism involves the calcium-dependent tyrosine kinase Pyk2, the non-receptor tyrosine kinase c-Src and the focal adhesion protein/steroid receptor co-factor, Hic-5.", "entity1": "steroid receptor co-factor", "entity2": "calcium", "span1": [138, 164], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11367": {"label": 1, "data": {"text": "The relatively high D(2) receptor occupancy, even at trough plasma levels, suggests that ziprasidone is more similar to risperidone and olanzapine in receptor occupancy profile than to clozapine and quetiapine.", "entity1": "D(2) receptor", "entity2": "quetiapine", "span1": [20, 33], "span2": [199, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"493": {"label": 2, "data": {"text": "There is, however, much information on the direct (acute and chronic) effects of alcohol on the binding properties of opioid receptors, as well as modulation of opioid peptide synthesis and secretion (e.g. a suggested increase in beta-endorphin release).", "entity1": "beta-endorphin", "entity2": "alcohol", "span1": [230, 244], "span2": [81, 88]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1132": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "cardiac K(+) channel", "entity2": "pimozide", "span1": [143, 163], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1898": {"label": 2, "data": {"text": "I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction.", "entity1": "interleukin 6", "entity2": "PMA", "span1": [69, 82], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"290": {"label": 0, "data": {"text": "Investigation of a site-specific mutant of CA V containing the replacement Tyr64-->His showed that the unique kinetic properties of CA V are not due to the presence of tyrosine at position 64.", "entity1": "CA V", "entity2": "tyrosine", "span1": [132, 136], "span2": [168, 176]}, "weak_labels": [-1, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4878": {"label": 1, "data": {"text": "Sequential chromatin IP uncovered the glut3-(m)CpGs to bind Mecp2 exponentially upon recruitment of Creb1 rather than histone deacetylase 1.", "entity1": "glut3", "entity2": "(m)CpGs", "span1": [38, 43], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4805": {"label": 3, "data": {"text": "Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.", "entity1": "BACE-1", "entity2": "dihydroisoquinoline", "span1": [52, 58], "span2": [32, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9288": {"label": 5, "data": {"text": "Taken together with our previous finding that the desipramine-induced enhancement of aggressive behavior can be blocked by yohimbine, an alpha 2-adrenoceptor antagonist, the present results indicate that not only alpha 2- but also beta 2-adrenoceptor stimulation plays important roles in modulation of aggressive behavior in long-term isolated mice.", "entity1": "alpha 2-adrenoceptor", "entity2": "yohimbine", "span1": [137, 157], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10126": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "indomethacin", "span1": [34, 37], "span2": [152, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4893": {"label": 3, "data": {"text": "Synthesis and Structure-Activity Relationship Studies of Derivatives of the Dual Aromatase-Sulfatase Inhibitor 4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate.", "entity1": "Aromatase", "entity2": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate", "span1": [81, 90], "span2": [111, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10070": {"label": 8, "data": {"text": "The transport amiloride-sensitive mechanism, that decreased the acidic intracellular pH change occurring in this medium, would correspond to Na+-H+ exchange (NHE1 isoform).", "entity1": "NHE1", "entity2": "H+", "span1": [158, 162], "span2": [145, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7291": {"label": 3, "data": {"text": "Pirfenidone inhibits TGF-beta expression in malignant glioma cells.", "entity1": "TGF-beta", "entity2": "Pirfenidone", "span1": [21, 29], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6187": {"label": 5, "data": {"text": "These data indicate that mixed 5-HT1/5-HT2 receptor antagonists such as pizotifen and methysergide, and mixed 5-HT and catecholamine antagonists such as mianserin and mirtazapine are more potent antagonists of mCPP-induced behavioural inhibition in rats than the more selective 5-HT2A/5-HT2C antagonist ritanserin.", "entity1": "5-HT2C", "entity2": "ritanserin", "span1": [285, 291], "span2": [303, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"838": {"label": 3, "data": {"text": "Felbamate produced a rapid, concentration-dependent block of currents evoked by 50 microM NMDA and 10 microM glycine in human embryonic kidney 293 cells expressing the rat NR1a subunit, and either the NR2A, NR2B or NR2C subunits; the IC50 values for block were 2.6, 0.52 and 2.4 mM, respectively (holding potential, - 60 mV).", "entity1": "NR2A", "entity2": "Felbamate", "span1": [201, 205], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2904": {"label": 3, "data": {"text": "In vitro, acetaminophen elicited a 4.4-fold selectivity toward COX-2 inhibition (IC(50)=113.7 micromol/L for COX-1; IC(50)=25.8 micromol/L for COX-2).", "entity1": "COX-2", "entity2": "acetaminophen", "span1": [143, 148], "span2": [10, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"609": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "BPB", "span1": [178, 191], "span2": [121, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"510": {"label": 3, "data": {"text": "Felodipine and nicardipine have similar affinities for 60-kDa CaMPDE isozymes but bring about different levels of enzyme inhibition, suggesting the possibility of designing specific drugs that can protect the enzyme from inhibition by dihydropyridine Ca2+-channel blockers.", "entity1": "Ca2+-channel", "entity2": "dihydropyridine", "span1": [251, 263], "span2": [235, 250]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5234": {"label": 2, "data": {"text": "To confirm this novel mechanism of bleomycin-induced fibrogenesis, we attempted to upregulate Nrf2 and related antioxidant proteins in bleomycin-treated fibroblasts using a putative Nrf2 activator, caffeic acid phenethyl ester, and the results showed that bleomycin-induced fibroblast proliferation and collagen content were attenuated through improved redox balance.", "entity1": "Nrf2", "entity2": "caffeic acid phenethyl ester", "span1": [182, 186], "span2": [198, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4547": {"label": 8, "data": {"text": "The in vivo inhibitory effect of harmaline on CYP2D6-catalyzed bufotenine formation was confirmed by in vitro study using purified CYP2D6.", "entity1": "CYP2D6", "entity2": "bufotenine", "span1": [46, 52], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13847": {"label": 5, "data": {"text": "Ambrisentan is the first ET(A) selective ERA approved for use in the US.", "entity1": "ET(A)", "entity2": "Ambrisentan", "span1": [25, 30], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12876": {"label": 2, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "phosphatidylglycerol", "span1": [13, 19], "span2": [171, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9146": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "methyl", "span1": [124, 136], "span2": [19, 25]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7944": {"label": 2, "data": {"text": "Distinct roles of methamphetamine in modulating spatial memory consolidation, retrieval, reconsolidation and the accompanying changes of ERK and CREB activation in hippocampus and prefrontal cortex.", "entity1": "ERK", "entity2": "methamphetamine", "span1": [137, 140], "span2": [18, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5412": {"label": 1, "data": {"text": "In addition, ATM7 potentiates 3,4-methylenedioxy-N-methylamphetamine (MDMA, \"Ecstasy\")-induced reversed transport by SERT.", "entity1": "SERT", "entity2": "3,4-methylenedioxy-N-methylamphetamine", "span1": [117, 121], "span2": [30, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6417": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes.", "entity1": "uncoupling protein-3", "entity2": "Wy-14,643", "span1": [109, 129], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5693": {"label": 2, "data": {"text": "The incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic peptide are secreted by enteroendocrine cells and augment glucose-induced insulin secretion in response to food ingestion in a glucose-dependent manner.", "entity1": "insulin", "entity2": "glucose", "span1": [157, 164], "span2": [141, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14722": {"label": 4, "data": {"text": "We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenine moiety.", "entity1": "TLR7", "entity2": "tertiary amines", "span1": [57, 61], "span2": [141, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5519": {"label": 3, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "acetylcholinesterase", "entity2": "organophosphorus", "span1": [108, 128], "span2": [22, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4395": {"label": 0, "data": {"text": "The initial fragment hits were thoroughly validated biophysically by isothermal titration calorimetry (ITC) and NMR techniques and observed by X-ray crystallography to bind in a shallow surface pocket that is occupied in the native complex by the side chain of a phenylalanine from the conserved FxxA interaction motif found in BRCA2.", "entity1": "BRCA2", "entity2": "phenylalanine", "span1": [328, 333], "span2": [263, 276]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4947": {"label": 3, "data": {"text": "Taken together, our results demonstrate the ability of Fc11a-2 to inhibit NLRP3 inflammasome activation and its potential use in the treatment of inflammatory bowel diseases.", "entity1": "NLRP3", "entity2": "Fc11a-2", "span1": [74, 79], "span2": [55, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11519": {"label": 1, "data": {"text": "Dexamethasone probes glucocorticoid receptor (GR) function, while prednisolone probes both GR and mineralocorticoid receptor (MR) function.", "entity1": "glucocorticoid receptor", "entity2": "Dexamethasone", "span1": [21, 44], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14396": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "Akt", "entity2": "NFD", "span1": [106, 109], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5721": {"label": 9, "data": {"text": "Indomethacin, used to inhibit cyclooxygenase, also inhibits AKR1C3 and displays selectivity over AKR1C1/AKR1C2.", "entity1": "AKR1C1", "entity2": "Indomethacin", "span1": [97, 103], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14529": {"label": 3, "data": {"text": "In contrast, EGCG markedly downregulated major bile acid transporters (Asbt and Ost\u03b1) and regulatory molecules (Shp and Fgf15) in the ileum.", "entity1": "Fgf15", "entity2": "EGCG", "span1": [120, 125], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6900": {"label": 1, "data": {"text": "In vitro studies demonstrated that the retinoid X receptor (RXR) retinoid, bexarotene, at biologically relevant concentrations of 10(-6) M to 10(-8) M, upregulated both the p55 and p75 subunits of the IL-2R and enhanced 5- to 10-fold the susceptibility of T-cell leukemia cells to denileukin diftitox.", "entity1": "RXR", "entity2": "bexarotene", "span1": [60, 63], "span2": [75, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8613": {"label": 2, "data": {"text": "Oxysterol-dependent NOX1 activation, as well as interleukin synthesis, were completely prevented by Cannonau red wine extract that contains an abundant phenolic fraction, in particular phenolic acids and flavonoids.", "entity1": "interleukin", "entity2": "Oxysterol", "span1": [48, 59], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8937": {"label": 1, "data": {"text": "The Kd for the binding of estramustine phosphate to MAP2 was estimated to be 20 microM at 4 degrees, and for the binding of tau, 200 microM.", "entity1": "MAP2", "entity2": "estramustine phosphate", "span1": [52, 56], "span2": [26, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10904": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "CDKs", "entity2": "Seliciclib", "span1": [102, 106], "span2": [25, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14749": {"label": 3, "data": {"text": "Together, these data suggest that arsenic degrades \u0394Np63 protein at least in part via Pirh2-dependent proteolysis and that inhibition of \u0394Np63 expression facilitates tumor cells to arsenic-induced death.", "entity1": "\u0394Np63", "entity2": "arsenic", "span1": [51, 56], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11944": {"label": 8, "data": {"text": "We confirm the correlation between higher hCTR1 levels and higher Pt-drug uptake in tumor cells sensitive to the drug.", "entity1": "hCTR1", "entity2": "Pt", "span1": [42, 47], "span2": [66, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12144": {"label": 2, "data": {"text": "BACKGROUND: The novel antiepileptic drug retigabine is the first selective M-current potassium channel opener for KCNQ2/3 and KCNQ3/5 channels.", "entity1": "KCNQ2/3", "entity2": "retigabine", "span1": [114, 121], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5053": {"label": 3, "data": {"text": "Blockade of JAK and ERK pathways with AG490 and U0126, respectively, abrogated the myocardial infarct size reduction by NDP-\u03b1-MSH.", "entity1": "ERK", "entity2": "U0126", "span1": [20, 23], "span2": [48, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11148": {"label": 8, "data": {"text": "Levodopa is absorbed in the small bowel and is rapidly catabolized by aromatic-L-amino-acid decarboxylase (AADC) and catechol-O-methyltransferase (COMT).", "entity1": "catechol-O-methyltransferase", "entity2": "Levodopa", "span1": [117, 145], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9844": {"label": 1, "data": {"text": "gamma-Butyrobetaine hydroxylase catalyse the last step in carnitine biosynthesis, the formation of L-carnitine from gamma-butyrobetaine, a reaction dependent on Fe2+, alpha-ketoglutarate, ascorbate and oxygen.", "entity1": "gamma-Butyrobetaine hydroxylase", "entity2": "oxygen", "span1": [0, 31], "span2": [202, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7658": {"label": 3, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-2", "entity2": "captopril", "span1": [0, 5], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4103": {"label": 1, "data": {"text": "Thus, SFO contributes to the instability of atherosclerotic plaque in apoE(-/-) mice through activating p75(NTR) and IL-8 and cell apoptosis in plaque.", "entity1": "apoE", "entity2": "SFO", "span1": [70, 74], "span2": [6, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4394": {"label": 0, "data": {"text": "The initial fragment hits were thoroughly validated biophysically by isothermal titration calorimetry (ITC) and NMR techniques and observed by X-ray crystallography to bind in a shallow surface pocket that is occupied in the native complex by the side chain of a phenylalanine from the conserved FxxA interaction motif found in BRCA2.", "entity1": "FxxA interaction motif", "entity2": "phenylalanine", "span1": [296, 318], "span2": [263, 276]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10171": {"label": 2, "data": {"text": "Thus we have shown that low-dose theophylline exerts an anti-asthma effect through increasing activation of HDAC which is subsequently recruited by corticosteroids to suppress inflammatory genes.", "entity1": "HDAC", "entity2": "theophylline", "span1": [108, 112], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3348": {"label": 1, "data": {"text": "The high resolution NMR solution structure of the cTnC-cTnI-dfbp-o ternary complex showed that dfbp-o bound at the hydrophobic interface formed by cTnC and cTnI making critical interactions with residues such as Arg147 of cTnI.", "entity1": "cTnC", "entity2": "dfbp-o", "span1": [147, 151], "span2": [95, 101]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2874": {"label": 7, "data": {"text": "Clinical trials have demonstrated that candesartan is well tolerated in combination with diuretics or calcium channel blockers (CCBs), making it a suitable treatment option for patients whose hypertension is not adequately controlled by monotherapy.", "entity1": "calcium channel", "entity2": "candesartan", "span1": [102, 117], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11619": {"label": 8, "data": {"text": "We isolated partial cDNAs that codified for enzymes implicated in the anthocyanin biosynthesis such as l-phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS), and an antioxidant enzyme such as ascorbate peroxidase (APX).", "entity1": "PAL", "entity2": "anthocyanin", "span1": [134, 137], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4970": {"label": 3, "data": {"text": "One exception is tranexamic acid (TXA), which, as a lysine mimetic, inhibits binding of plasminogen to fibrin.", "entity1": "plasminogen", "entity2": "lysine", "span1": [88, 99], "span2": [52, 58]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1506": {"label": 4, "data": {"text": "RESULTS: DRF 2655 showed concentration-dependent transactivation of PPARalpha and PPARgamma.", "entity1": "PPARgamma", "entity2": "DRF 2655", "span1": [82, 91], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13274": {"label": 8, "data": {"text": "We studied in a clinical trial whether isolated isoflavone treatment in postmenopausal women could affect reverse cholesterol transport as evaluated by adenosine triphosphate-binding cassette A1- (ABCA1), dependent cholesterol efflux from macrophages.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [197, 202], "span2": [215, 226]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15539": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "matrix metalloproteinase-13", "entity2": "DMN", "span1": [135, 162], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13477": {"label": 2, "data": {"text": "Incretin-receptor activation leads to glucose-dependent insulin secretion, induction of beta-cell proliferation, and enhanced resistance to apoptosis.", "entity1": "insulin", "entity2": "glucose", "span1": [56, 63], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15534": {"label": 2, "data": {"text": "CK significantly inhibited DMN-induced increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, fibrosis score, and hepatic malondialdehyde and collagen content.", "entity1": "aspartate aminotransferase", "entity2": "DMN", "span1": [93, 119], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15322": {"label": 5, "data": {"text": "Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.", "entity1": "(AMPA) receptor", "entity2": "IKM-159", "span1": [76, 91], "span2": [103, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9125": {"label": 1, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c.", "entity1": "cytochrome c", "entity2": "calcium", "span1": [122, 134], "span2": [50, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1873": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "prenylflavonoids", "span1": [221, 251], "span2": [5, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8540": {"label": 1, "data": {"text": "In addition, high ErbB3 and Muc1 expression was correlated with sensitivity to elisidepsin, whereas the presence of KRAS activating mutations was associated with resistance.", "entity1": "Muc1", "entity2": "elisidepsin", "span1": [28, 32], "span2": [79, 90]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5697": {"label": 3, "data": {"text": "Whereas the addition of apomorphine in the low micromolar range produced an irreversible activation of the channel, application of higher concentrations caused a reversible voltage-dependent inhibition of heterologously expressed TRPA1 channels, resulting from a reduction of single-channel open times.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [230, 235], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14973": {"label": 3, "data": {"text": "Results confirmed that YR-11 peptide inhibited pro-inflammatory cytokines in the sera and hind paw tissues of AIA rats through its suppressive effect on RANKL induced nuclear translocation of NF-\u03baB.", "entity1": "cytokines", "entity2": "YR-11", "span1": [64, 73], "span2": [23, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5748": {"label": 3, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "I-\u03baB\u03b5", "entity2": "vitamin C", "span1": [134, 139], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8826": {"label": 3, "data": {"text": "Exhibiting unique properties over other MMPIs (e.g., hydroxamates), these newly reported compounds are capable of modulating activities of several MMPs in the low nanomolar range, including MMP-2 (~2 to 50 nM), MMP-13 (~2 to 50 nM), and MMP-14 (~4 to 60 nM).", "entity1": "MMP-14", "entity2": "hydroxamates", "span1": [237, 243], "span2": [53, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12322": {"label": 2, "data": {"text": "Ribavirin also enhanced recruitment of CDK9 (cyclin-dependent kinase 9) and AFF4 to F7.", "entity1": "cyclin-dependent kinase 9", "entity2": "Ribavirin", "span1": [45, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2795": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "SP", "entity2": "caerulein", "span1": [26, 28], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5455": {"label": 1, "data": {"text": "Therefore, TSA-induced apoptosis of HCC cells is uc002mbe.2 dependent and reduced expression of uc002mbe.2 may be associated with liver carcinogenesis.", "entity1": "uc002mbe.2", "entity2": "TSA", "span1": [49, 59], "span2": [11, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5043": {"label": 3, "data": {"text": "New classes of pyrrole-derived nitrooxyalkyl inverse esters, carbonates, and ethers (7-10) as COX-2 selective inhibitors and NO donors were synthesized and are herein reported.", "entity1": "COX-2", "entity2": "ethers", "span1": [94, 99], "span2": [77, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14507": {"label": 1, "data": {"text": "Orexin-A (a glucose-sensing neuropeptide in the hypothalamus) and brain-derived neurotrophic factor (BDNF; a member of the neurotrophin family) play roles in many physiologic functions, including regulation of glucose metabolism.", "entity1": "Orexin-A", "entity2": "glucose", "span1": [0, 8], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7412": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "NR1", "entity2": "glycine", "span1": [15, 18], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3093": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine", "span1": [354, 357], "span2": [59, 107]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1833": {"label": 3, "data": {"text": "Reciprocally, glyburide blocked SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC(50) approximately 275-300 microM).", "entity1": "SR-BI", "entity2": "glyburide", "span1": [32, 37], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9157": {"label": 3, "data": {"text": "The inhibitory effect of (+)-, (-)-, (+/-)-gossypol and (+/-)-gossypol acetic acid upon testicular cytosolic LDH-X was measured in vitro.", "entity1": "LDH-X", "entity2": "(+/-)-gossypol acetic acid", "span1": [109, 114], "span2": [56, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8640": {"label": 2, "data": {"text": "MT1R was increased in ovaries and uteri of melatonin-treated rats.", "entity1": "MT1R", "entity2": "melatonin", "span1": [0, 4], "span2": [43, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3689": {"label": 2, "data": {"text": "Insulin secretion stimulated by both 200 \u03bcM tolbutamide and 20 \u03bcM gliclazide, concentrations that had equivalent effects on membrane potential, was inhibited by thapsigargin (1 \u03bcM) or the L-type Ca(2+) channel blocker nicardipine (2 \u03bcM) and was potentiated by 8-pCPT-2'-O-Me-cAMP-AM at concentrations \u22652 \u03bcM in INS-1 cells.", "entity1": "Insulin", "entity2": "8-pCPT-2'-O-Me-cAMP-AM", "span1": [0, 7], "span2": [260, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15428": {"label": 2, "data": {"text": "In non-pre-treated cells, HMG-CoA was up-regulated by both 7-ketosterols.", "entity1": "HMG-CoA", "entity2": "7-ketosterols", "span1": [26, 33], "span2": [59, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13947": {"label": 1, "data": {"text": "denopamine for beta(1); clenbuterol, AZ 40140d, salbutamol for beta(2)) were found to have subtype-selective intrinsic efficacy.", "entity1": "beta(2)", "entity2": "AZ 40140d", "span1": [63, 70], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13353": {"label": 2, "data": {"text": "PR isoform B levels were low in virgin control mice and increased after progestin treatment in both strains.", "entity1": "PR isoform B", "entity2": "progestin", "span1": [0, 12], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13257": {"label": 2, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "MUC2/5AC", "entity2": "leukotriene D(4)", "span1": [85, 93], "span2": [60, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13057": {"label": 3, "data": {"text": "Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction.", "entity1": "topoisomerase II", "entity2": "amrubicin", "span1": [35, 51], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4125": {"label": 0, "data": {"text": "Here, we identify a Zn\u00b2\u207a-driven N-terminal to C-terminal tertiary interaction in PrP(C).", "entity1": "PrP(C)", "entity2": "C", "span1": [81, 87], "span2": [46, 47]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4779": {"label": 0, "data": {"text": "We show that CIQ does not bind to the amino-terminal domain of the NMDA receptor and does not share structural determinants with modulators acting at the agonist-binding domain dimer interface or ion channel pore.", "entity1": "NMDA receptor", "entity2": "amino", "span1": [67, 80], "span2": [38, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2316": {"label": 3, "data": {"text": "Sulindac metabolites simultaneously (a) increase cellular cyclic GMP and subsequently activate cyclic GMP-dependent protein kinase (PKG); (b) activate c-jun NH2-terminal kinase (JNK); (c) inhibit extracellular signal-regulated kinase 1/2 (ERK1/2); and (d) decrease beta-catenin protein expression at times and doses consistent with apoptosis.", "entity1": "JNK", "entity2": "Sulindac", "span1": [178, 181], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7230": {"label": 2, "data": {"text": "GnRH-induced Pyk2 activation opposed the association of Hic-5 with androgen receptor as overexpression of a dominant negative Pyk2 enhanced the GnRH-induced nuclear translocation of a green fluorescent protein-tagged human androgen receptor.", "entity1": "Pyk2", "entity2": "GnRH", "span1": [13, 17], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11761": {"label": 0, "data": {"text": "The protein is formed by an N-terminal helicase-like domain, a CC-terminal DNA polymerase domain, and a large central domain that spans between the two.", "entity1": "C-terminal DNA polymerase domain", "entity2": "C", "span1": [64, 96], "span2": [63, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5520": {"label": 3, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "AChE", "entity2": "organophosphorus", "span1": [130, 134], "span2": [22, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2658": {"label": 3, "data": {"text": "These data support the conclusion that renal ecto-phosphodiesterase activity is not mediated by PDE1, PDE2, PDE3, PDE4, PDE5, PDE6, PDE7, PDE9, PDE10, or PDE11 and is inhibited by high concentrations of dipyridamole.", "entity1": "phosphodiesterase", "entity2": "dipyridamole", "span1": [50, 67], "span2": [203, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5278": {"label": 1, "data": {"text": "In concert with these results, we highlighted that the secretion of pro-inflammatory cytokine and NF-\u03baB activation induced by TCDD can be mediated by elevation of [Ca(2+)]i in HAPI microglial cells.", "entity1": "cytokine", "entity2": "Ca(2+)", "span1": [85, 93], "span2": [164, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1222": {"label": 8, "data": {"text": "In addition to affecting DAT function, MDMA rapidly decreased vesicular DA transport as assessed in striatal vesicles prepared from treated rats.", "entity1": "DAT", "entity2": "DA", "span1": [25, 28], "span2": [72, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1461": {"label": 3, "data": {"text": "), did not induce the behavioural hyperactivity syndrome which is seen following inhibition of both MAO-A and MAO-B by tranylcypromine together with the monoamine precursors.", "entity1": "MAO-B", "entity2": "monoamine", "span1": [110, 115], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10411": {"label": 1, "data": {"text": "Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.", "entity1": "preproorphanin precursor peptide", "entity2": "GTPgammaS", "span1": [51, 83], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5856": {"label": 5, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT4", "entity2": "tropisetron", "span1": [193, 198], "span2": [153, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15681": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Histone 3", "entity2": "EVn-50", "span1": [177, 186], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10121": {"label": 3, "data": {"text": "A TXA2 synthetase inhibitor (OKY-046) attenuated the contraction to a small extent only at high concentrations.", "entity1": "TXA2 synthetase", "entity2": "OKY-046", "span1": [2, 17], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6012": {"label": 8, "data": {"text": "Moreover, the production of TXB2 during whole blood clotting was assessed as an index of the cyclooxygenase activity of platelet PGHS-1 ex vivo.", "entity1": "cyclooxygenase", "entity2": "TXB2", "span1": [93, 107], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9418": {"label": 5, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT2", "entity2": "benzamide", "span1": [172, 177], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9310": {"label": 5, "data": {"text": "The enhancement of the depolarizing afterpotential by histamine was mimicked by the histamine H1-receptor agonist 2-thiazolylethylamine and was reduced or blocked by the H1-receptor antagonist promethazine, but was not blocked or reduced in the presence of the histamine H2-receptor antagonist, cimetidine.", "entity1": "H1-receptor", "entity2": "promethazine", "span1": [170, 181], "span2": [193, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1402": {"label": 3, "data": {"text": "These results suggest that gemfibrozil inhibits the induction of iNOS probably by inhibiting the activation of NF-kappaB, AP-1, and C/EBPbeta and that gemfibrozil, a prescribed drug for humans, may further find its therapeutic use in neuroinflammatory diseases.", "entity1": "NF-kappaB", "entity2": "gemfibrozil", "span1": [111, 120], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4730": {"label": 1, "data": {"text": "Luciferase reporter assays showed that transcription of FDX1 was synergistically activated by the NR5A family and 8Br-cAMP treatment through two SF-1 binding sites and a CRE-like sequence in a human ovarian granulosa cell line, KGN.", "entity1": "SF-1", "entity2": "8Br-cAMP", "span1": [145, 149], "span2": [114, 122]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15004": {"label": 8, "data": {"text": "In the in vitro model we observed high permeability of imperatorin and isoimperatorin with the P-gp-mediated efflux ratios of 0.53 and 0.06, as well as medium permeability of cnidilin with 0.82.", "entity1": "P-gp", "entity2": "imperatorin", "span1": [95, 99], "span2": [55, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6126": {"label": 8, "data": {"text": "Amezinium and debrisoquine are substrates of uptake1 and potent inhibitors of monoamine oxidase in perfused lungs of rats.", "entity1": "uptake1", "entity2": "debrisoquine", "span1": [45, 52], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3342": {"label": 1, "data": {"text": "The affinities of dfbp and dfbp-o for the regulatory domain of cTnC were measured in the absence and presence of cTnI by NMR spectroscopy, and dfbp-o was found to bind more strongly than dfbp.", "entity1": "cTnC", "entity2": "dfbp-o", "span1": [63, 67], "span2": [143, 149]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3220": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "syringic acid", "span1": [282, 284], "span2": [145, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7117": {"label": 0, "data": {"text": "This indicated that the N-terminal 46 amino acids in GAF-B are required for high vardenafil potency.", "entity1": "GAF-B", "entity2": "amino acids", "span1": [53, 58], "span2": [38, 49]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9021": {"label": 1, "data": {"text": "The mitogenic effect of DHT on bone cells was inhibited by antiandrogens (hydroxyflutamide and cyproterone acetate) which compete for binding to the androgen receptor.", "entity1": "androgen receptor", "entity2": "cyproterone acetate", "span1": [149, 166], "span2": [95, 114]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12115": {"label": 3, "data": {"text": "State-dependent cocaine block of sodium channel isoforms, chimeras, and channels coexpressed with the beta1 subunit.", "entity1": "sodium channel", "entity2": "cocaine", "span1": [33, 47], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1157": {"label": 9, "data": {"text": "Patch-clamp analysis using inside-out recording configuration showed that mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 microM).", "entity1": "SUR2A", "entity2": "mitiglinide", "span1": [225, 230], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2825": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "iNOS", "entity2": "1400W", "span1": [152, 156], "span2": [119, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14188": {"label": 3, "data": {"text": "CBDP irreversibly inhibits butyrylcholinesterase (BChE) in human plasma by forming adducts on the active site serine (Ser-198).", "entity1": "BChE", "entity2": "CBDP", "span1": [50, 54], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7251": {"label": 2, "data": {"text": "The discovery that METH and AMPH activate the rTAAR1 motivated us to study the effect of these drugs on the mouse TAAR1 (mTAAR1) and a human-rat chimera (hrChTAAR1).", "entity1": "rTAAR1", "entity2": "AMPH", "span1": [46, 52], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5677": {"label": 8, "data": {"text": "In comparison to homozygous, wild type (WT) mice, HZ mice show a 40% reduction of AChE activity in the brain, while their hippocampal ACh levels are increased by 56% as measured by microdialysis; choline acetyltransferase levels remain unaltered, and choline uptake increases 2-fold.", "entity1": "choline acetyltransferase", "entity2": "choline", "span1": [196, 221], "span2": [251, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7199": {"label": 3, "data": {"text": "Our results imply that P2Y12 has the potential to be inhibited by ADP/ATP analogs, and it suggests that P2Y12 acts as a target of new drugs that inhibit platelet aggregation.", "entity1": "P2Y12", "entity2": "ADP", "span1": [23, 28], "span2": [66, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9092": {"label": 1, "data": {"text": "Kinetic analysis revealed that the inhibition of the leukotriene C synthetase reaction by diethylcarbamazine was competitive with respect to LTA4.", "entity1": "leukotriene C synthetase", "entity2": "LTA4", "span1": [53, 77], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1392": {"label": 3, "data": {"text": "Inhibition of human iNOS promoter-driven luciferase activity by gemfibrozil in cytokine-stimulated U373MG astroglial cells suggests that this compound inhibits the transcription of iNOS.", "entity1": "human iNOS promoter", "entity2": "gemfibrozil", "span1": [14, 33], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2078": {"label": 2, "data": {"text": "These data demonstrated that 1) gemcitabine and pemetrexed synergistically interact against NSCLC cells through the suppression of Akt phosphorylation and induction of apoptosis; 2) the gene expression profile of critical genes may predict for drug chemosensitivity; and 3) pemetrexed enhances dCK and hENT1 expression, thus suggesting the role of gene-expression modulation for rational development of chemotherapy combinations.", "entity1": "hENT1", "entity2": "pemetrexed", "span1": [302, 307], "span2": [274, 284]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13299": {"label": 3, "data": {"text": "We investigated the efficacy of sorafenib at inhibiting mutants of the receptor tyrosine kinases PDGFRbeta, KIT, and FLT3, which are implicated in the pathogenesis of myeloid malignancies.", "entity1": "PDGFRbeta", "entity2": "sorafenib", "span1": [97, 106], "span2": [32, 41]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14026": {"label": 3, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Together, these data suggest that thiocolchicoside significantly suppressed osteoclastogenesis induced by RANKL and tumour cells via the NF-kappaB signalling pathway.", "entity1": "RANKL", "entity2": "thiocolchicoside", "span1": [136, 141], "span2": [64, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5812": {"label": 9, "data": {"text": "Loperamide, an opiate agonist of high specificity for mu-receptors, was recently reported to suppress ACTH and cortisol levels in normal subjects, but not in patients with proven ACTH-dependent Cushing's disease.", "entity1": "ACTH", "entity2": "Loperamide", "span1": [179, 183], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1691": {"label": 3, "data": {"text": "Blockade of NMDA receptors by memantine could theoretically confer disease-modifying activity in AD by inhibiting the \"weak\" NMDA receptor-dependent excitotoxicity that has been hypothesized to play a role in the progressive neuronal loss that underlies the evolving dementia.", "entity1": "NMDA receptor", "entity2": "memantine", "span1": [125, 138], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6305": {"label": 5, "data": {"text": "These responses were effectively blocked by the 5-HT1B receptor antagonist, isamoltane, the 5-HT1B/5-HT2 receptor antagonist, methiothepin, and the eNOS selective antagonists (0.01-10 microM): L-Nomega -monomethyl-L-arginine (L-NMMA) and L-N omega-iminoethyl-L-ornithine (L-NIO).", "entity1": "eNOS", "entity2": "L-NMMA", "span1": [148, 152], "span2": [226, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15512": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "peroxidase", "entity2": "Cys", "span1": [188, 198], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15046": {"label": 8, "data": {"text": "Its head-space aroma displayed new volatile phytomolecules and also had higher levels of green volatiles from the lipoxygenase (LOX)-pathway (one having as precursors the polyunsaturated fatty acids containing a cis-cis-1,4-pentadiene system).", "entity1": "LOX", "entity2": "cis-cis-1,4-pentadiene", "span1": [128, 131], "span2": [212, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"626": {"label": 3, "data": {"text": "Pretreatment of the splenocytes with both BPB and AACOCF3 suppressed phorbol 12-myristate 13-acetate plus ionomycin-induced IL-2 secretion in a concentration-dependent manner.", "entity1": "IL-2", "entity2": "AACOCF3", "span1": [124, 128], "span2": [50, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8511": {"label": 1, "data": {"text": "To overcome this limitation, we de novo synthesized a conjugate that covalently combines a Gd-based MRI contrast agent, encaged with a chelating agent (DOTA), with pantoprazole, which is a widely used proton pump inhibitor that binds to proton pumps in the stomach and colon.", "entity1": "proton pumps", "entity2": "DOTA", "span1": [237, 249], "span2": [152, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12250": {"label": 1, "data": {"text": "For the isolated PKCalpha C2 domain in the presence of physiological Ca2+ levels, the target lipids phosphatidylserine (PS) and phosphatidylinositol-4,5-bisphosphate (PIP2) are together sufficient to recruit the PKCalpha C2 domain to a lipid mixture mimicking the plasma membrane inner leaflet.", "entity1": "PKCalpha C2 domai", "entity2": "PIP2", "span1": [212, 229], "span2": [167, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8852": {"label": 1, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "AhR", "entity2": "I3S", "span1": [61, 64], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9641": {"label": 3, "data": {"text": "The levels of PSA mRNA decreased 56 and 90% when LNCaP cells were treated with 5 and 10 microM of estramustine, respectively (IC50 = 10.97 +/- 1.68 microM).", "entity1": "PSA", "entity2": "estramustine", "span1": [14, 17], "span2": [98, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10858": {"label": 1, "data": {"text": "Most of the tested H(2)R agonists and imidazole-based H(3)R ligands show micromolar-to-nanomolar range hH(4)R affinity, and these ligands exert different intrinsic hH(4)R activities, ranging from full agonists to inverse agonists.", "entity1": "hH(4)R", "entity2": "imidazole", "span1": [103, 109], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9690": {"label": 1, "data": {"text": "The goal of the present study was to examine the 5-HT1A properties of ziprasidone in vivo using as a marker of central 5-HT1A activity the inhibition of firing of serotonin-containing neurons in the dorsal raphe nucleus.", "entity1": "5-HT1A", "entity2": "ziprasidone", "span1": [49, 55], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1656": {"label": 5, "data": {"text": "The potent histamine H(1)-receptor antagonist cetirizine (Zyrtec) is a racemic mixture of levocetirizine (now available under the trademark Xyzal and dextrocetirizine.", "entity1": "histamine H(1)-receptor", "entity2": "levocetirizine", "span1": [11, 34], "span2": [90, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4227": {"label": 3, "data": {"text": "The results showed that (1) 15mg/kg body weight PhIP induced obvious histopathological changes in gastric mucosa; (2) PhIP (10 and/or 15mg/kg) significantly decreased superoxide dismutase (SOD) and glutathioneperoxidase (GPx) activities, while increased catalase (CAT) activity compared with the control.", "entity1": "GPx", "entity2": "PhIP", "span1": [221, 224], "span2": [118, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3085": {"label": 3, "data": {"text": "CONCLUSIONS: At the doses studied, PLZ was as effective as VIG at elevating brain GABA levels, but, unlike VIG, also inhibited MAO and ALA-T (and increased brain ALA levels).", "entity1": "ALA-T", "entity2": "VIG", "span1": [135, 140], "span2": [107, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10479": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "epinephrine", "span1": [392, 423], "span2": [98, 109]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15514": {"label": 1, "data": {"text": "Our findings that NO/SNO target both Prx and Trx reductase may have implications for understanding the impact of nitrosylation on cellular redox homeostasis.", "entity1": "Trx reductase", "entity2": "SNO", "span1": [45, 58], "span2": [21, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6568": {"label": 3, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "D950A", "entity2": "milrinone", "span1": [15, 20], "span2": [60, 69]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14220": {"label": 1, "data": {"text": "Treatment options for DUB are: combined oral contraceptives (COCs), progestogens, non steroidal anti inflammatory drugs (NSAIDs), tranexamic acid (anti-fibrinolytic), GnRH analogues, Danazol and Levonorgestrel releasing intra uterine system (LNG IUS).", "entity1": "GnRH", "entity2": "Levonorgestrel", "span1": [167, 171], "span2": [195, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3521": {"label": 8, "data": {"text": "We have previously reported that TZDs reduce estrogen synthesis by inhibiting aromatase activity in human granulosa cells (HGC).", "entity1": "aromatase", "entity2": "estrogen", "span1": [78, 87], "span2": [45, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2075": {"label": 2, "data": {"text": "Synergistic cytotoxicity was demonstrated, and pemetrexed significantly decreased the amount of phosphorylated Akt, enhanced apoptosis, and increased the expression of dCK in A549 and Calu-6 cells, as well as the expression of the human nucleoside equilibrative transporter 1 (hENT1) in all cell lines.", "entity1": "human nucleoside equilibrative transporter 1", "entity2": "pemetrexed", "span1": [231, 275], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15485": {"label": 0, "data": {"text": "Our results suggest that modification of multiple cysteine residues by electrophilic compounds can generate both activation and desensitization of the TRPA1 channel.", "entity1": "TRPA1", "entity2": "cysteine", "span1": [151, 156], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3617": {"label": 4, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "CB1", "entity2": "AM4054", "span1": [48, 51], "span2": [60, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14439": {"label": 2, "data": {"text": "Induction of AhR by TCDD and prochloraz resulted in a time- and dose-dependent increase of ABCG2 gene expression and transporter protein levels.", "entity1": "ABCG2", "entity2": "prochloraz", "span1": [91, 96], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10159": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "ER", "entity2": "fulvestrant", "span1": [129, 131], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5547": {"label": 2, "data": {"text": "This study investigates the involvement of alpha(2)-adrenergic receptors (AR) in mouse brain induced by a low dose of methamphetamine (METH, 2 mg/kg).", "entity1": "alpha(2)-adrenergic receptors", "entity2": "methamphetamine", "span1": [43, 72], "span2": [118, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3502": {"label": 2, "data": {"text": "For AII and ET1, MAP was also increased for the fenofibrate group but not in a dose-dependent fashion.", "entity1": "ET1", "entity2": "fenofibrate", "span1": [12, 15], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13771": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "kinase", "entity2": "Sutent", "span1": [247, 253], "span2": [212, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5849": {"label": 4, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT4", "entity2": "metoclopramide", "span1": [232, 237], "span2": [58, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1968": {"label": 5, "data": {"text": "In contrast, intrathecal injection of a non-selective NMDA antagonist, memantine, significantly inhibited CCI-induced mechanical allodynia at a dose of 300 nmol, indicating the difference in the site of action between the non-selective NMDA antagonist and the NR2B-specific NMDA antagonist.", "entity1": "NMDA", "entity2": "memantine", "span1": [54, 58], "span2": [71, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10873": {"label": 2, "data": {"text": "Early-onset diarrhea is observed immediately after CPT-11 infusion and probably due to the inhibition of acetylcholinesterase activity, which can be eliminated by administration of atropine.", "entity1": "acetylcholinesterase", "entity2": "atropine", "span1": [105, 125], "span2": [181, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7791": {"label": 3, "data": {"text": "We examined in cats the 1) ulcerogenic effects of selective COX-1 (SC-560, ketorolac) and COX-2 (celecoxib, meloxicam) inhibitors on the gastrointestinal mucosa, 2) effect of feeding and cimetidine on the expression of COX isoforms and prostaglandin E(2) (PGE(2)) level in the duodenum, and 3) localization of COX isoforms in the duodenum.", "entity1": "COX-1", "entity2": "SC-560", "span1": [60, 65], "span2": [67, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1362": {"label": 3, "data": {"text": "Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.", "entity1": "cocaine binding site", "entity2": "Mazindol", "span1": [50, 70], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4328": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "c-Myc", "entity2": "Pinosylvin", "span1": [217, 222], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5969": {"label": 3, "data": {"text": "However, betaxolol produces less systemic beta 2- and possibly beta 1-adrenergic receptor blockade than either timolol or levobunolol.", "entity1": "beta 1-adrenergic receptor", "entity2": "betaxolol", "span1": [63, 89], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2217": {"label": 4, "data": {"text": "Two beta(2)-agonists, formoterol and salmeterol, are approved for treating asthma and have an extended duration of action and increased safety, associated with greater beta(2)-adrenoceptor selectivity.", "entity1": "beta(2)-adrenoceptor", "entity2": "formoterol", "span1": [168, 188], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2375": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "MEK", "entity2": "Nexavar", "span1": [75, 78], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11402": {"label": 1, "data": {"text": "Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties.", "entity1": "potassium channel", "entity2": "diclofenac", "span1": [62, 79], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2452": {"label": 3, "data": {"text": "ATB-429-induced antinociception was reversed by glibenclamide, a ATP-sensitive K(+) (K(ATP)) channel inhibitor.", "entity1": "ATP-sensitive K(+) (K(ATP)) channel", "entity2": "glibenclamide", "span1": [65, 100], "span2": [48, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1079": {"label": 1, "data": {"text": "The capacity of acetylcholinesterase inhibitors, with the exception of tacrine and ambenonium, to displace bound [3H]-oxotremorine-M in preference to [3H]quinuclinidyl benzilate predicts that the former compounds could act as potential agonists at muscarinic receptors.", "entity1": "muscarinic receptors", "entity2": "[3H]quinuclinidyl benzilate", "span1": [248, 268], "span2": [150, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3099": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "[(125)I]RTI-55", "span1": [354, 357], "span2": [330, 344]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2586": {"label": 8, "data": {"text": "Methionine synthase reductase (MTRR) is an enzyme involved in the conversion of Hcy to methionine.", "entity1": "MTRR", "entity2": "Hcy", "span1": [31, 35], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"11100": {"label": 9, "data": {"text": "The R(-) and S(+) isomers of MDMA were significantly less efficacious at the 5-HT2A receptor as compared to MDA; S(+)MDMA had no effect.", "entity1": "5-HT2A", "entity2": "R(-) and S(+) isomers of MDMA", "span1": [77, 83], "span2": [4, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11657": {"label": 1, "data": {"text": "Testosterone (TEST) had the fastest translocation rate for the hAR of 0.0525 min(-1).", "entity1": "hAR", "entity2": "Testosterone", "span1": [63, 66], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14719": {"label": 3, "data": {"text": "Pharmacological inhibition of MTORC1 with rapamycin abrogated the insulin-induced phosphorylation of EIF4EBP1, RPS6KB1 and its downstream effector, RPS6.", "entity1": "RPS6", "entity2": "rapamycin", "span1": [148, 152], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13028": {"label": 1, "data": {"text": "By contrast, 11beta-HSD2 plays a pivotal role in aldosterone target tissues where it catalyses the opposite reaction (i.e.", "entity1": "11beta-HSD2", "entity2": "aldosterone", "span1": [13, 24], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15992": {"label": 1, "data": {"text": "Here we show that puerarin increases proliferation and differentiation and opposes cisplatin-induced apoptosis in human osteoblastic MG-63 cells containing two estrogen receptor (ER) isoforms.", "entity1": "ER", "entity2": "cisplatin", "span1": [179, 181], "span2": [83, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14915": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "estrogen receptor-\u03b1", "entity2": "\u0394(5)-androstenediol", "span1": [236, 255], "span2": [35, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10467": {"label": 3, "data": {"text": "Thus, Ras utilizes autocrine signaling through EGFR to increase radioresistance, and the EGFR KI GW572016 acts as a radiosensitizer.", "entity1": "EGFR", "entity2": "GW572016", "span1": [89, 93], "span2": [97, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4443": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "MAO", "entity2": "phthalimide", "span1": [147, 150], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12122": {"label": 8, "data": {"text": "Before dosing and 24 h after the seventh dose of each regimen, heparinized whole blood samples were incubated with lipopolysaccharide (10 microgram/ml) for 24 h at 37 degrees C, and prostaglandin E2 was measured in plasma as an index of monocyte COX-2 activity.", "entity1": "COX-2", "entity2": "prostaglandin E2", "span1": [246, 251], "span2": [182, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14074": {"label": 1, "data": {"text": "Berberine inhibits myofibroblast differentiation in nasal polyp-derived fibroblasts via the p38 pathway.", "entity1": "p38", "entity2": "Berberine", "span1": [92, 95], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8414": {"label": 1, "data": {"text": "However, the involvement of the caspase-dependent pathway in the process of cell death induced by either BSC 3g or 3n is discarded since cell death could not be prevented by pretreatment with the pancaspase inhibitor z-VAD-fmk.", "entity1": "caspase", "entity2": "BSC", "span1": [32, 39], "span2": [105, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6654": {"label": 8, "data": {"text": "The potency of MrIA was greater for inhibition of uptake by hNET of [3H]norepinephrine (Ki 1.89 microM) than [3H]dopamine (Ki 4.33 microM), and the human dopamine transporter and serotonin transporter were not inhibited by MrIA (to 7 microM).", "entity1": "hNET", "entity2": "[3H]dopamine", "span1": [60, 64], "span2": [109, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"11892": {"label": 8, "data": {"text": "Cycloxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) has been shown to be important in esophageal tumorigenesis.", "entity1": "COX-2", "entity2": "prostaglandin E2", "span1": [17, 22], "span2": [32, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8946": {"label": 9, "data": {"text": "Unlike bacterial 3-keto-5-ene-steroid isomerase, the human isomerase reaction is stimulated by diphosphopyridine nucleotides (NADH, NAD+).", "entity1": "3-keto-5-ene-steroid isomerase", "entity2": "NAD+", "span1": [17, 47], "span2": [132, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9375": {"label": 1, "data": {"text": "Recovery from modulation by cyclothiazide was slower for GluR-AiBi and GluR-AoBi than for GluR-AiBo and GluR-AoBo.", "entity1": "GluR-AoBi", "entity2": "cyclothiazide", "span1": [71, 80], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12435": {"label": 1, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "mAChR", "entity2": "VU0467903", "span1": [273, 278], "span2": [188, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"93": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "phenylalanine hydroxylase", "entity2": "dopamine", "span1": [112, 137], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15031": {"label": 3, "data": {"text": "Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1).", "entity1": "MMP-1", "entity2": "methyl rosmarinate", "span1": [115, 120], "span2": [28, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2982": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Y612A", "entity2": "cGMP", "span1": [173, 178], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4940": {"label": 3, "data": {"text": "Moreover, protein and mRNA levels of DSS-induced proinflammatory cytokines in colon, including TNF-\u03b1, IL-1\u03b2, IL-18, IL-17A and IFN-\u03b3, were markedly suppressed by Fc11a-2.", "entity1": "IL-1\u03b2", "entity2": "Fc11a-2", "span1": [102, 107], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1489": {"label": 3, "data": {"text": "Similarly, pretreatment with sulindac sulfide blocks the ability of EGF to induce ERK1/2 and Bad phosphorylation, but also down-regulates total Bad but not ERK1/2 protein levels.", "entity1": "Bad", "entity2": "sulindac sulfide", "span1": [144, 147], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7438": {"label": 4, "data": {"text": "(-)-Stepholidine (SPD), an active ingredient of the Chinese herb Stephania, is the first compound found to have dual function as a dopamine receptor D1 agonist and D2 antagonist.", "entity1": "dopamine receptor D1", "entity2": "SPD", "span1": [131, 151], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15602": {"label": 1, "data": {"text": "All three agents induced mdr1a.fLUC expression (bioluminescence), but only PCN and docetaxel appeared to act primarily via PXR.", "entity1": "mdr1a", "entity2": "docetaxel", "span1": [25, 30], "span2": [83, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4201": {"label": 3, "data": {"text": "Furthermore, PTE treatment directly inhibited the phosphorylation of JAK2 at Tyr 1007 and the downstream activation of STAT3.", "entity1": "JAK2", "entity2": "PTE", "span1": [69, 73], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8132": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "GDNF", "entity2": "Sal", "span1": [117, 121], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15567": {"label": 3, "data": {"text": "In addition to the effect on ROS, puerarin ameliorated MPTP-reduced lysosome-associated membrane protein type 2A (Lamp 2A) expression.", "entity1": "Lamp 2A", "entity2": "puerarin", "span1": [114, 121], "span2": [34, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"72": {"label": 9, "data": {"text": "Aspirin (ASA) and other non-steroidal anti-inflammatory drugs, which are cyclooxygenase (COX) inhibitors, precipitate asthmatic attacks in ASA-intolerant patients, while sodium salicylate, hardly active on COX by itself, is well tolerated by these patients.", "entity1": "COX", "entity2": "sodium salicylate", "span1": [206, 209], "span2": [170, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8624": {"label": 1, "data": {"text": "Arsenic inhibits autophagic flux activating the Nrf2-Keap1 pathway in a p62-dependent manner.", "entity1": "p62", "entity2": "Arsenic", "span1": [72, 75], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13901": {"label": 3, "data": {"text": "Captopril directly inhibits matrix metalloproteinase-2 activity in continuous ambulatory peritoneal dialysis therapy.", "entity1": "matrix metalloproteinase-2", "entity2": "Captopril", "span1": [28, 54], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15766": {"label": 0, "data": {"text": "We observed that the administration of ICI at 08:00h on proestrus day produced a 15% inhibition of luminal epithelial cell proliferation, reduced uterine wet weight by 21% and caused reduction of Akt phosphorylation at Ser 473 as compared to vehicle-treated animals, whereas ICI treatment at 00:00h on estrus day had no effect on these parameters.", "entity1": "Akt", "entity2": "Ser", "span1": [196, 199], "span2": [219, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4756": {"label": 1, "data": {"text": "Regucalcin (RGN/SMP30) was originally discovered in 1978 as a unique calcium-binding protein that does not contain the EF-hand motif of calcium-binding domain.", "entity1": "Regucalcin", "entity2": "calcium", "span1": [0, 10], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11609": {"label": 1, "data": {"text": "RESULTS: Eighty percent of CYP2C9*1/*1 patients stabilized on <4.0 mg/day warfarin had at least 1 VKORC1 -1639A allele.", "entity1": "VKORC1", "entity2": "warfarin", "span1": [98, 104], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9710": {"label": 1, "data": {"text": "A novel missense mutation, G663A, in exon 5 of the erythroid-specific delta-aminolevulinate synthase gene (ALAS2) was identified in a Japanese male with pyridoxine-responsive sideroblastic anemia.", "entity1": "G663A", "entity2": "pyridoxine", "span1": [27, 32], "span2": [153, 163]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12351": {"label": 3, "data": {"text": "NAC also suppressed the p-JNK and p-p38, but failed to reverse the effects of ISO.", "entity1": "p-p38", "entity2": "NAC", "span1": [34, 39], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15377": {"label": 0, "data": {"text": "Modification of the Catalytic Function of Human Hydroxysteroid Sulfotransferase hSULT2A1 by Formation of Disulfide Bonds.", "entity1": "Human Hydroxysteroid Sulfotransferase hSULT2A1", "entity2": "Disulfide", "span1": [42, 88], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6119": {"label": 3, "data": {"text": "Amezinium and debrisoquine are substrates of uptake1 and potent inhibitors of monoamine oxidase in perfused lungs of rats.", "entity1": "monoamine oxidase", "entity2": "debrisoquine", "span1": [78, 95], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9935": {"label": 3, "data": {"text": "The suppression of NF-kappaB activation by inhibition of the IKKs contributes to the well-known anti-inflammatory and immunosuppressive effects of sulfasalazine.", "entity1": "IKKs", "entity2": "sulfasalazine", "span1": [61, 65], "span2": [147, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8334": {"label": 5, "data": {"text": "Aprepitant, the first and only agent clinically available in the NK1 receptor antagonist drug class has been used effectively as an additive agent to the 5-HT3 receptor antagonists and dexamethasone to control CINV.", "entity1": "NK1 receptor", "entity2": "Aprepitant", "span1": [65, 77], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5406": {"label": 2, "data": {"text": "Combined treatment of Mn and DA further augments cell toxicity, ROS production and JNK phosphorylation in LRRK2 deficient cells compared to controls.", "entity1": "JNK", "entity2": "Mn", "span1": [83, 86], "span2": [22, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15713": {"label": 3, "data": {"text": "3-Hydroxy-5-(2-phenylethyl)pyridine-2(1H)-one exhibited the predicted binding mode and demonstrated high inhibitory activity for human DAAO in enzyme- and cell-based assays.", "entity1": "human DAAO", "entity2": "3-Hydroxy-5-(2-phenylethyl)pyridine-2(1H)-one", "span1": [129, 139], "span2": [0, 45]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10956": {"label": 3, "data": {"text": "We examined the effects of the high dose of granulocyte-colony stimulating factor (G-CSF), which is capable of increasing peripheral neutrophils, and a specific neutrophil elastase inhibitor (ONO-5046) on acid lung injury in rats.", "entity1": "neutrophil elastase", "entity2": "ONO-5046", "span1": [161, 180], "span2": [192, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3949": {"label": 8, "data": {"text": "Role of organic cation/carnitine transporter 1 in uptake of phenformin and inhibitory effect on complex I respiration in mitochondria.", "entity1": "organic cation/carnitine transporter 1", "entity2": "phenformin", "span1": [8, 46], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11119": {"label": 1, "data": {"text": "Indoramin and SNAP 1069 showed selectivity for alpha 1A and alpha 1B adrenoceptors relative to the alpha 1D subtype.", "entity1": "alpha 1D subtype", "entity2": "SNAP 1069", "span1": [99, 115], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2009": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Pro", "span1": [121, 125], "span2": [89, 92]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12921": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine gamma-lyase", "entity2": "Hydrogen sulfide", "span1": [92, 117], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8581": {"label": 3, "data": {"text": "Arsenic trioxide depletes cancer stem-like cells and inhibits repopulation of neurosphere derived from glioblastoma by downregulation of Notch pathway.", "entity1": "Notch", "entity2": "Arsenic trioxide", "span1": [137, 142], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5790": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "acetylalanine", "span1": [125, 145], "span2": [261, 274]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1365": {"label": 8, "data": {"text": "Several active analogues were also evaluated for their ability to block uptake of DA, 5-HT, and NE and inhibit binding of [(125)I] RTI-55 at HEK-hDAT, HEK-hSERT, and HEK-hNET cells.", "entity1": "hNET", "entity2": "NE", "span1": [170, 174], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"749": {"label": 1, "data": {"text": "The inhibitory effect of endothelin-1 on the contraction induced by 5-HT is abolished by deendothelialization, by the endothelin ET(B) receptor antagonist RES 701-1, by indomethacin, or by glibenclamide.", "entity1": "endothelin-1", "entity2": "indomethacin", "span1": [25, 37], "span2": [169, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"224": {"label": 3, "data": {"text": "As determined by Western and Northern blot analyses, 5 alpha-NET inhibited the P4-induced UG gene expression in a dose-dependent manner.", "entity1": "UG", "entity2": "5 alpha-NET", "span1": [90, 92], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6943": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "naproxen", "span1": [81, 86], "span2": [118, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2055": {"label": 0, "data": {"text": "Mutation of arginine 228 to lysine enhances the glucosyltransferase activity of bovine beta-1,4-galactosyltransferase I.", "entity1": "bovine beta-1,4-galactosyltransferase I", "entity2": "lysine", "span1": [80, 119], "span2": [28, 34]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5604": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "risperidone", "span1": [59, 65], "span2": [151, 162]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4966": {"label": 3, "data": {"text": "One exception is tranexamic acid (TXA), which, as a lysine mimetic, inhibits binding of plasminogen to fibrin.", "entity1": "plasminogen", "entity2": "tranexamic acid", "span1": [88, 99], "span2": [17, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15944": {"label": 1, "data": {"text": "We also recorded a significant correlation between M value increase and the decrease of vaspin, visfatin, and omentin-1 obtained with vildagliptin+metformin.", "entity1": "visfatin", "entity2": "metformin", "span1": [96, 104], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4532": {"label": 3, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "MAO-A", "entity2": "harmaline", "span1": [69, 74], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9824": {"label": 3, "data": {"text": "In this study, we demonstrate that geldanamycin treatment blocks interleukin (IL)-2 secretion, IL-2 receptor expression, and proliferation of stimulated T-lymphocytes.", "entity1": "IL-2 receptor", "entity2": "geldanamycin", "span1": [95, 108], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14112": {"label": 2, "data": {"text": "Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplified pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression.", "entity1": "WAF-1", "entity2": "pomalidomide", "span1": [195, 200], "span2": [112, 124]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4360": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NAD(P)H:quinone oxidoreductase-1", "entity2": "1,2-orthonaphthoquinone", "span1": [115, 147], "span2": [25, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"389": {"label": 1, "data": {"text": "The CB1 and CB2 second extracellular loops, e2, were exchanged, modifications that had no effect on SR 141716A binding in the CB1 variant but that eliminated CP 55,940 binding in both mutants.", "entity1": "CB1", "entity2": "SR 141716A", "span1": [126, 129], "span2": [100, 110]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6425": {"label": 2, "data": {"text": "Schisandrin B protects against menadione-induced hepatotoxicity by enhancing DT-diaphorase activity.", "entity1": "DT-diaphorase", "entity2": "Schisandrin B", "span1": [77, 90], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1713": {"label": 0, "data": {"text": "Interestingly, all exchanges identified involved amino acids which are conserved in the squalene epoxidases of yeasts and mammals.", "entity1": "squalene epoxidases", "entity2": "amino acids", "span1": [88, 107], "span2": [49, 60]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6416": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes.", "entity1": "uncoupling protein-3", "entity2": "bezafibrate", "span1": [109, 129], "span2": [73, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14638": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "deoxycytidine kinase", "entity2": "dFdC", "span1": [95, 115], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8959": {"label": 1, "data": {"text": "Computer-assisted analysis of these curvilinear Schild plots in a two-receptor system indicated that alpha 1-adrenoceptor populations responsible for the constrictive response are predominantly (approximately 80-90%) low affinity sites for the two antagonists (pKd approximately 8.1 for WB4101 and pKd approximately 7.1 for 5-methyl-urapidil) and a small population (approximately 10-20%) are high affinity sites (pKd approximately 9.1 for both WB4101 and 5-methyl-urapidil), which was in good agreement with radioligand binding studies.", "entity1": "alpha 1-adrenoceptor", "entity2": "WB4101", "span1": [101, 121], "span2": [445, 451]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1024": {"label": 2, "data": {"text": "Activation of endogenous somatostatin receptor subtype 2 (sst2) by somatostatin-14 or activation of transiently transfected rat D2 dopamine receptors (rD2(long)) by quinpirole had no effect.", "entity1": "sst2", "entity2": "somatostatin-14", "span1": [58, 62], "span2": [67, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"374": {"label": 3, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2", "entity2": "DEX", "span1": [301, 305], "span2": [287, 290]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12171": {"label": 1, "data": {"text": "A G-protein coupled receptor to niacin (nicotinic acid) was identified recently but the physiological/pharmacological role of the receptor remains poorly defined.", "entity1": "G-protein coupled receptor", "entity2": "niacin", "span1": [2, 28], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3712": {"label": 2, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "Bim", "entity2": "N", "span1": [159, 162], "span2": [13, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8928": {"label": 5, "data": {"text": "We therefore conclude that carvedilol, at antihypertensive doses, is an antagonist of beta 1, beta 2, and alpha 1 adrenoceptors, and also of calcium channels in vascular smooth muscle.", "entity1": "calcium channels", "entity2": "carvedilol", "span1": [141, 157], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5731": {"label": 5, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "glucocorticoid receptor", "entity2": "RU486", "span1": [43, 66], "span2": [83, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2361": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "PDGFR", "entity2": "Sorafenib", "span1": [133, 138], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7804": {"label": 2, "data": {"text": "However, 4'G-RSV, but not 3G-RSV, induced SIRT1-dependent histone H3 deacetylation and SOD2 expression in mouse C2C12 skeletal myoblasts; as with RSV, SIRT1 knockdown blunted these effects.", "entity1": "SIRT1", "entity2": "4'G-RSV", "span1": [42, 47], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9235": {"label": 8, "data": {"text": "The holo activity of AGT 2 with a high Km for L-alanine decreased more slowly than AGT 1 (by 33% in 14 days, by 60% in 28 days).", "entity1": "AGT 2", "entity2": "L-alanine", "span1": [21, 26], "span2": [46, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5466": {"label": 4, "data": {"text": "In the locus coeruleus, brexpiprazole reversed the inhibitory effect of the preferential 5-HT2A receptor agonist DOI (2,5-dimethoxy-4-iodoamphetamine) on norepinephrine neuronal firing (ED50 = 110 mug/kg), demonstrating 5-HT2A antagonistic action.", "entity1": "5-HT2A", "entity2": "DOI", "span1": [89, 95], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6389": {"label": 1, "data": {"text": "The selective alpha(2)-adrenoceptor ligand rauwolscine antagonized acidification rate changes with an affinity independent of the agonist used; the affinity (mean pK(B)) against noradrenaline was 8.43.", "entity1": "alpha(2)-adrenoceptor", "entity2": "noradrenaline", "span1": [14, 35], "span2": [178, 191]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10982": {"label": 3, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "beta(2)-adrenoceptor", "entity2": "PMA", "span1": [225, 245], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13994": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "MET", "entity2": "Cabozantinib", "span1": [86, 89], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"693": {"label": 1, "data": {"text": "Prazosin antagonized all agonists with a low potency (pA2: 8.29-8.80) indicating the involvement of alpha 1L-rather than alpha 1A-adrenoceptors.", "entity1": "alpha 1L", "entity2": "Prazosin", "span1": [100, 108], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9699": {"label": 4, "data": {"text": "While it is an antagonist at these latter receptors, ziprasidone behaves as a 5-HT1A agonist in vitro in adenylate cyclase measurements.", "entity1": "5-HT1A", "entity2": "ziprasidone", "span1": [78, 84], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13633": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "Top1p", "entity2": "Tyr", "span1": [0, 5], "span2": [160, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11123": {"label": 1, "data": {"text": "Rec 15/2739, WB 4101, SL 89,0591, (+)- and (-)- tamsulosin showed selectivity for alpha 1A and alpha 1D adrenoceptors relative to the alpha 1B subtype.", "entity1": "alpha 1B subtype", "entity2": "(+)- and (-)- tamsulosin", "span1": [134, 150], "span2": [34, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14325": {"label": 2, "data": {"text": "Finally, DMF suppressed unilateral ureteral obstruction (UUO)-induced renal fibrosis and alpha-SMA, fibronectin and type 1 collagen expression in the obstructed kidneys from UUO mice, along with increased and decreased expression of Nrf2 and phospho-Smad3, respectively.", "entity1": "Nrf2", "entity2": "DMF", "span1": [233, 237], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2051": {"label": 0, "data": {"text": "In this study, we show that mutation of Arg228, a residue in the vicinity of Glu317, to lysine (R228K-Gal-T1) results in a 15-fold higher Glc-T activity, which is further enhanced by LA to nearly 25% of the Gal-T activity of the wild type.", "entity1": "Gal-T1", "entity2": "lysine", "span1": [102, 108], "span2": [88, 94]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15387": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor", "entity2": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole", "span1": [129, 181], "span2": [0, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2657": {"label": 9, "data": {"text": "However, a lower concentration of dipyridamole (3 microM) that blocks PDE9, PDE10, and PDE11, but not PDE8, did not inhibit ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "dipyridamole", "span1": [129, 146], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1685": {"label": 9, "data": {"text": "While the neurobiological basis for the therapeutic activity of memantine is not fully understood, the drug is not a cholinesterase inhibitor and, therefore, acts differently from current AD therapies.", "entity1": "cholinesterase", "entity2": "memantine", "span1": [117, 131], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2143": {"label": 2, "data": {"text": "Thiazolidinediones are a new class of anti-diabetic agents which increase insulin sensitivity by binding to the peroxisome proliferator-activated receptor gamma (PPAR(gamma)) and stimulating the expression of insulin-responsive genes involved in glucose and lipid metabolism.", "entity1": "insulin", "entity2": "Thiazolidinediones", "span1": [209, 216], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15606": {"label": 1, "data": {"text": "TCPOBOP, a CAR ligand, modestly induced mdr1a.fLUC in pxr(+/+) and pxr(-/-) strains, consistent with CAR's minor role in mdr1a regulation.", "entity1": "CAR", "entity2": "TCPOBOP", "span1": [101, 104], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8942": {"label": 1, "data": {"text": "Two new negatively charged estramustine derivatives, estramustine sulphate and estramustine glucuronide, were found to be similar MAP-dependent microtubule inhibitors.", "entity1": "MAP", "entity2": "estramustine sulphate", "span1": [130, 133], "span2": [53, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11759": {"label": 1, "data": {"text": "MDMA catechol metabolites were neurotoxic to SH-SY5Y neurons, leading to caspase 3-independent cell death in a concentration- and time-dependent manner.", "entity1": "caspase 3", "entity2": "catechol", "span1": [73, 82], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5100": {"label": 1, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "iNOS", "entity2": "5HHMF", "span1": [96, 100], "span2": [43, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1738": {"label": 3, "data": {"text": "On the other hand, in patients with a mean serum carvedilol level (Cmin) of less than 2.5 nmol/l up to 2 weeks after the start ofcarvedilol therapy, the degree of reduction in the BNP value after the 3rd month was significantly larger, relative to the patient group with Cmin over 2.5 nmol/l.", "entity1": "BNP", "entity2": "carvedilol", "span1": [180, 183], "span2": [49, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1279": {"label": 8, "data": {"text": "COX-1 inhibition was measured as percentage inhibition of serum TXB2 generation in clotting whole blood, and as closure time with use of the platelet function analyser PFA-100.", "entity1": "COX-1", "entity2": "TXB2", "span1": [0, 5], "span2": [64, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14825": {"label": 3, "data": {"text": "FXa inhibitors, e.g. rivaroxaban and apixaban, are potent, oral direct inhibitors of prothrombinase-bound, clot-associated or free FXa.", "entity1": "FXa", "entity2": "rivaroxaban", "span1": [0, 3], "span2": [21, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8318": {"label": 2, "data": {"text": "Taken together these results indicate that in vivo or ex vivo exposure of intestinal tissue to DON lead to similar intestinal lesions and activation of MAPK.", "entity1": "MAPK", "entity2": "DON", "span1": [152, 156], "span2": [95, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4859": {"label": 0, "data": {"text": "Unsaturated FFAs increased DAGs, TAGs and PTP1B expression significantly, but cells remained insulin sensitive as assessed by robust AKt and PTP1B phosphorylation at serine (Ser) 50, Ser 398 and tyrosine 152.", "entity1": "PTP1B", "entity2": "Ser", "span1": [141, 146], "span2": [174, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8926": {"label": 5, "data": {"text": "In anesthetized spontaneously hypertensive rats, the antihypertensive activity of carvedilol was nearly abolished by combined pretreatment of the rats with high doses of the alpha 1 adrenoceptor antagonist, prazosin (1 mg/kg, iv), and the nonselective beta adrenoceptor antagonist, propranolol (3 mg/kg, iv), suggesting that the majority of the antihypertensive response produced by carvedilol may be accounted for by blockade of beta and alpha 1 adrenoceptors.", "entity1": "alpha 1 adrenoceptor", "entity2": "prazosin", "span1": [174, 194], "span2": [207, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"681": {"label": 8, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "GTPCH", "entity2": "tetrahydrobiopterin", "span1": [78, 83], "span2": [131, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"10606": {"label": 1, "data": {"text": "The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam.", "entity1": "synaptic vesicle protein SV2A", "entity2": "levetiracetam", "span1": [4, 33], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4705": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "TCDD", "span1": [111, 117], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2273": {"label": 8, "data": {"text": "CONCLUSIONS: Total vitamin B6 is abnormally high in autism, consistent with previous reports of an impaired pyridoxal kinase for the conversion of pyridoxine and pyridoxal to PLP.", "entity1": "pyridoxal kinase", "entity2": "pyridoxine", "span1": [108, 124], "span2": [147, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5525": {"label": 1, "data": {"text": "To determine the position of the phenyl ring of the aralkyloxyalkyl side chain of salmeterol in the beta 2AR binding site, we designed and synthesized the agonist photoaffinity label [(125)I]iodoazidosalmeterol ([125I]IAS).", "entity1": "beta 2AR", "entity2": "salmeterol", "span1": [100, 108], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4827": {"label": 1, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "Akt", "entity2": "7\u03b2OHC", "span1": [194, 197], "span2": [67, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14511": {"label": 5, "data": {"text": "Small interfering RNA directed BDNF, orexin-A, and SB334867 [N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea; a specific orexin-1 receptor antagonist] were administered directly into the hypothalamus.", "entity1": "orexin-1 receptor", "entity2": "N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea", "span1": [131, 148], "span2": [61, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1909": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "fluoropyrimidine carbamate", "span1": [121, 123], "span2": [13, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3417": {"label": 2, "data": {"text": "The treatment with arsenic exhibited a significant increase in some serum hepatic and renal biochemical parameters (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total protein, albumin, bilirubin, cholesterol, urea and creatinine).", "entity1": "alanine aminotransferase", "entity2": "arsenic", "span1": [116, 140], "span2": [19, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5088": {"label": 1, "data": {"text": "PKD1 and PI4KIII\u03b2 localize to the TGN, and aldosterone induced an interaction between PKD1 and PI4KIII\u03b2 following aldosterone treatment.", "entity1": "PI4KIII\u03b2", "entity2": "aldosterone", "span1": [95, 103], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7892": {"label": 1, "data": {"text": "Data suggest that bisphosphonates via modulation of the activity of small-GTPases induce apoptosis in neoplastic cells by DNA-CpG-demethylation and stimulation of FAS-expression.", "entity1": "CpG", "entity2": "bisphosphonates", "span1": [126, 129], "span2": [18, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7143": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "GAF-B domain", "entity2": "sildenafil", "span1": [47, 59], "span2": [102, 112]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3902": {"label": 0, "data": {"text": "Finally, the Pak1(-/-) mice exhibited reduced brainstem gcg level and abolished \u03b2-cat Ser675 phosphorylation in brain neurons after insulin treatment.", "entity1": "\u03b2-cat", "entity2": "Ser", "span1": [80, 85], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15042": {"label": 1, "data": {"text": "It had higher levels of oleocanthal (p-HPEA-EDA), a nutraceutical compound exerting actions against COX1 and COX2 (cycloxygenases).", "entity1": "cycloxygenases", "entity2": "p-HPEA-EDA", "span1": [115, 129], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"315": {"label": 5, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "alpha 1-adrenoceptor", "entity2": "prazosin", "span1": [411, 431], "span2": [443, 451]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3744": {"label": 1, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "AhR", "entity2": "polycyclic aromatic hydrocarbons", "span1": [61, 64], "span2": [119, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3143": {"label": 1, "data": {"text": "Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization.", "entity1": "TrkB", "entity2": "Amitriptyline", "span1": [62, 66], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15962": {"label": 2, "data": {"text": "4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells.", "entity1": "cyclin E", "entity2": "4-Hydroxytamoxifen", "span1": [44, 52], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6635": {"label": 5, "data": {"text": "The alpha(2)-adrenoceptor antagonist, rauwolscine (0.5 mg/kg), was without antagonistic effects.", "entity1": "alpha(2)-adrenoceptor", "entity2": "rauwolscine", "span1": [4, 25], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1592": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "butyrylcholinesterase", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine", "span1": [36, 57], "span2": [381, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4406": {"label": 1, "data": {"text": "However, one mGlu5 PAM, CPPHA (N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide), interacts with a separate allosteric site on mGlu5.", "entity1": "mGlu5", "entity2": "N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide", "span1": [167, 172], "span2": [31, 119]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"7954": {"label": 2, "data": {"text": "However, mutating putative GR binding sites did not substantially reduce induction of ras-dva promoter activity by corticosterone, suggesting additional DNA elements within the 5'-flanking region are responsible for glucocorticoid regulation.", "entity1": "ras-dva promoter", "entity2": "corticosterone", "span1": [86, 102], "span2": [115, 129]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"943": {"label": 3, "data": {"text": "In contrast, 2, 4-dioxo-5-acetamido-6-phenylhexanoic acid, which is a competitive inhibitor with respect to ascorbate, exhibits a low degree of stereospecificity in binding to the ascorbate sites of both PAM and dopamine-beta-hydroxylase.", "entity1": "PAM", "entity2": "2, 4-dioxo-5-acetamido-6-phenylhexanoic acid", "span1": [204, 207], "span2": [13, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1566": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "KATI", "entity2": "oxoglutaramic acid", "span1": [88, 92], "span2": [156, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"6533": {"label": 3, "data": {"text": "As a prodrug leflunomide is completely converted to its active metabolite A 77 1726 (M1) which blocks the dihydroorotate dehydrogenase, a key enzyme of the pyrimidine de novo synthesis.", "entity1": "dihydroorotate dehydrogenase", "entity2": "leflunomide", "span1": [106, 134], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"162": {"label": 3, "data": {"text": "Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex.", "entity1": "Acetylcholinesterase", "entity2": "organophosphate", "span1": [0, 20], "span2": [45, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12188": {"label": 1, "data": {"text": "Several variables associated to thymidylate synthase (TS), the biological target of 5-fluorouracil (5FU) have been studied for their possible role as predictors of the clinical outcome and response to chemotherapy in colorectal cancer (CRC) patients.", "entity1": "TS", "entity2": "5FU", "span1": [54, 56], "span2": [100, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8201": {"label": 3, "data": {"text": "In addition, derivatives of caffeic acid and sinapic acid efficiently inhibited tyrosinase activity and reduced melanin content in melanocytes Mel-Ab cell.", "entity1": "tyrosinase", "entity2": "sinapic acid", "span1": [80, 90], "span2": [45, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11064": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "azathioprine", "span1": [89, 95], "span2": [375, 387]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13471": {"label": 8, "data": {"text": "Acetyl-coenzyme A carboxylase (ACC) enzymes exist as two isoforms, ACC1 and ACC2, which play critical roles in fatty acid biosynthesis and oxidation.", "entity1": "ACC1", "entity2": "fatty acid", "span1": [67, 71], "span2": [111, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3188": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "p-hydroxybenzoic acid", "span1": [248, 261], "span2": [64, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5716": {"label": 3, "data": {"text": "Parallel synthetic strategies were used to generate libraries of indomethacin analogues, which exhibit reduced cyclooxygenase inhibitory activity but retain AKR1C3 inhibitory potency and selectivity.", "entity1": "AKR1C3", "entity2": "indomethacin", "span1": [157, 163], "span2": [65, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1213": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DA transporter", "entity2": "MDMA", "span1": [149, 163], "span2": [123, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4316": {"label": 5, "data": {"text": "Since the original discovery of azoles analogs as PXR antagonists, we have preliminarily defined an important PXR antagonist pharmacophore and developed less-toxic PXR antagonists.", "entity1": "PXR", "entity2": "azoles", "span1": [164, 167], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5095": {"label": 2, "data": {"text": "Aldosterone also induces the rapid phosphorylation of Protein Kinase D1 (PKD1).", "entity1": "PKD1", "entity2": "Aldosterone", "span1": [73, 77], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12910": {"label": 8, "data": {"text": "While either blockage of HO activity by the HO inhibitor, tin protoporphyrin IX, or down-regulation of HO-1 expression by HO-1 small interfering RNA (siRNA) reversed the inhibitory effects of H(2)S on iNOS expression and NO production, HO-1 overexpression produced the same inhibitory effects of H(2)S. In addition, LPS-induced nuclear factor (NF)-kappaB activation was diminished in RAW264.7 macrophages preincubated with H(2)S. Interestingly, the inhibitory effect of H(2)S on NF-kappaB activation was reversed by the transient transfection with HO-1 siRNA, but was mimicked by either HO-1 gene transfection or treatment with carbon monoxide (CO), an end product of HO-1.", "entity1": "HO-1", "entity2": "carbon monoxide", "span1": [668, 672], "span2": [628, 643]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11693": {"label": 2, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "TNF-\u03b1", "entity2": "pioglitazone", "span1": [153, 158], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11276": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "EC 2.1.1.10", "entity2": "glycine", "span1": [116, 127], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1141": {"label": 3, "data": {"text": "Amiloride is a specific inhibitor of uPA but does not inhibit tPA.", "entity1": "uPA", "entity2": "Amiloride", "span1": [37, 40], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5282": {"label": 2, "data": {"text": "However, Ca(2+) blockers also obviously attenuated NF-\u03baB activation and transnuclear transport induced by TCDD.", "entity1": "NF-\u03baB", "entity2": "TCDD", "span1": [51, 56], "span2": [106, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6159": {"label": 1, "data": {"text": "Drug dependent changes in the NMR heteronuclear single-quantum coherence spectra of [methyl-13C]Met-labeled cTnC indicate that bepridil and trifluoperazine bind to similar sites but only in the presence of Ca2+.", "entity1": "cTnC", "entity2": "Ca2+", "span1": [108, 112], "span2": [206, 210]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10332": {"label": 4, "data": {"text": "Here, we characterize the activation of human pDC with the TLR7 agonists imiquimod and resiquimod.", "entity1": "TLR7", "entity2": "resiquimod", "span1": [59, 63], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13387": {"label": 3, "data": {"text": "We identified suramin as a compound that binds to human SIRT5 and showed that it inhibits SIRT5 NAD(+)-dependent deacetylase activity with an IC(50) value of 22 microM.", "entity1": "SIRT5 NAD(+)-dependent deacetylase", "entity2": "suramin", "span1": [90, 124], "span2": [14, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1945": {"label": 9, "data": {"text": "Several purinergic receptors have been described on platelets; P2X (1), a calcium channel, and P2Y1 a Gq-coupled seven-transmembrane domain receptor, have been found not to be antagonized by clopidogrel.", "entity1": "calcium channel", "entity2": "clopidogrel", "span1": [74, 89], "span2": [191, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9940": {"label": 3, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "IKK-alpha", "entity2": "sulfasalazine", "span1": [158, 167], "span2": [269, 282]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10841": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "STI571", "span1": [119, 122], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12114": {"label": 3, "data": {"text": "Cocaine block of human cardiac (hH1) and rat skeletal (mu1) muscle sodium channels was examined under whole-cell voltage clamp in transiently transfected HEK293t cells.", "entity1": "rat skeletal (mu1) muscle sodium channels", "entity2": "Cocaine", "span1": [41, 82], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14521": {"label": 3, "data": {"text": "We propose that inhibition of PAK1 expression by 5-ASA can impede with neoplastic progression in colorectal carcinogenesis.", "entity1": "PAK1", "entity2": "5-ASA", "span1": [30, 34], "span2": [49, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11773": {"label": 8, "data": {"text": "The bupropion metabolic ratio appears to detect known differences in CYP2B6 activity associated with genetic polymorphism, across different ethnic groups.", "entity1": "CYP2B6", "entity2": "bupropion", "span1": [69, 75], "span2": [4, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12312": {"label": 9, "data": {"text": "In an effort to understand the shedding process of AChE, we have used several pharmacological treatments, which showed that it is likely to be mediated in part by an EDTA- and batimastat-sensitive, but GM6001-insensitive metalloprotease, with the possible additional involvement of a thiol isomerase.", "entity1": "metalloprotease", "entity2": "GM6001", "span1": [221, 236], "span2": [202, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10016": {"label": 5, "data": {"text": "Other 5-HT3 receptor antagonists also produced such a shift in the following antagonistic-potency order: granisetron> ondansetron=AS-8112>>metoclopramide.", "entity1": "5-HT3 receptor", "entity2": "metoclopramide", "span1": [6, 20], "span2": [139, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4210": {"label": 2, "data": {"text": "In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OST\u03b2, and a down-regulation of CYP27A1.", "entity1": "SHP", "entity2": "GW4064", "span1": [97, 100], "span2": [66, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3326": {"label": 2, "data": {"text": "Apoptosis studies (DAPI staining and caspase 3 activity) showed a marked increase in the presence of MXF and VP-16 compared to VP-16 alone.", "entity1": "caspase 3", "entity2": "VP-16", "span1": [37, 46], "span2": [127, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6344": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "E3174", "span1": [25, 28], "span2": [246, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7874": {"label": 8, "data": {"text": "Renal clearance of unbound anagliptin and unbound M1 far exceeded glomerular filtration rate, indicating active renal elimination: that might reflect the fact that anagliptin may be a substrate of OAT1, OAT3, MDR1 and MRP2, and M1 a substrate of OAT3, BCRP, MRP2 and MRP4.", "entity1": "OAT3", "entity2": "anagliptin", "span1": [203, 207], "span2": [164, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11588": {"label": 2, "data": {"text": "Differences in magnitude of Na(+)-dependent l-alanine uptake through ASCT2 between WKY and SHR PTE cells correlated positively with differences in ASCT2 protein expression, this being more abundant in WKY PTE cells.", "entity1": "ASCT2", "entity2": "Na(+)", "span1": [147, 152], "span2": [28, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2006": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Leu", "span1": [121, 125], "span2": [70, 73]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4095": {"label": 2, "data": {"text": "In this study, aldosterone (ALD)-induced apoptosis of cardiomyocyte was evaluated based on the previous studies, and the roles of calpain signaling were clarified.", "entity1": "calpain", "entity2": "aldosterone", "span1": [130, 137], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2120": {"label": 2, "data": {"text": "The positive correlation between vitamin A and immunoglobulin A concentrations might be the result of the vitamin A inductive effect during immunoglobulins A synthesis.", "entity1": "immunoglobulin A", "entity2": "vitamin A", "span1": [47, 63], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8561": {"label": 3, "data": {"text": "Discovery of a synthetic Aminopeptidase N inhibitor LB-4b as a potential anticancer agent.", "entity1": "Aminopeptidase N", "entity2": "LB-4b", "span1": [25, 41], "span2": [52, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4686": {"label": 1, "data": {"text": "The present study demonstrates that there is a differential modulation of Cyp1a1 by V(5+) in C57BL/6 mice livers and isolated hepatocytes and demonstrates Hb as an in vivo specific modulator.", "entity1": "Cyp1a1", "entity2": "V(5+)", "span1": [74, 80], "span2": [84, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6779": {"label": 1, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX", "entity2": "indomethacin", "span1": [119, 122], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12881": {"label": 3, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "lysophosphatidylserine", "span1": [14, 20], "span2": [96, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"15657": {"label": 1, "data": {"text": "While the function of N-type calcium channels within astrocytes is controversial, these voltage-gated calcium channels have been linked to calcium-dependent vesicular gliotransmitter release.", "entity1": "N-type calcium channels", "entity2": "calcium", "span1": [22, 45], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9733": {"label": 1, "data": {"text": "Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors.", "entity1": "h5-HT(1D)", "entity2": "Yohimbine", "span1": [138, 147], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12278": {"label": 3, "data": {"text": "This study identified four clinically approved antihypertensive drugs (efonidipine, felodipine, isradipine, and nitrendipine) as potent T-channel blockers (IC(50) < 3 microM).", "entity1": "T-channel", "entity2": "efonidipine", "span1": [136, 145], "span2": [71, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11307": {"label": 3, "data": {"text": "The decrement of p-CREB protein in the nucleus accumbens remained at 24 h (-35 %) and 72 h (-28 %) of ethanol withdrawal, which recovered toward control level after 7 d of ethanol withdrawal.", "entity1": "p-CREB", "entity2": "ethanol", "span1": [17, 23], "span2": [172, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4085": {"label": 2, "data": {"text": "ALD increased calpain expression and caspase-3 activity and promoted Bid cleavage.", "entity1": "caspase-3", "entity2": "ALD", "span1": [37, 46], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8620": {"label": 3, "data": {"text": "Besides this direct activity, an excess of phenolic compounds detectable in red wine, may exert an additional indirect action by blocking oxysterol-related NOX1 induction, thus totally preventing the pro-oxidant and pro-inflammatory events triggered by dietary oxysterols.", "entity1": "NOX1", "entity2": "phenolic", "span1": [156, 160], "span2": [43, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15076": {"label": 1, "data": {"text": "Although not a \u03b2-lactam, the chemical structure of avibactam closely resembles portions of the cephem bicyclic ring system, and avibactam has been shown to bond covalently to \u03b2-lactamases.", "entity1": "\u03b2-lactamases", "entity2": "cephem", "span1": [175, 187], "span2": [95, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8268": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "cytochrome P4502B6", "entity2": "Methadone", "span1": [59, 77], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5420": {"label": 5, "data": {"text": "In the local presence into the LC of the \u03b12-adrenoceptor antagonist RS79948 (1\u00a0\u03bcM), systemic citalopram increased NA in the LC (Emax\u2009=\u2009157\u2009\u00b1\u200925\u00a0%) and PFC (Emax\u2009=\u2009175\u2009\u00b1\u200924\u00a0%).", "entity1": "\u03b12-adrenoceptor", "entity2": "RS79948", "span1": [41, 56], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11204": {"label": 8, "data": {"text": "These results suggest that ACS1 and ACS4 may be linked to triacylglycerol synthesis.", "entity1": "ACS4", "entity2": "triacylglycerol", "span1": [36, 40], "span2": [58, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8477": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "high-temperature requirement A1", "entity2": "Gly", "span1": [38, 69], "span2": [254, 257]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2160": {"label": 3, "data": {"text": "Thalidomide inhibits growth of tumors through COX-2 degradation independent of antiangiogenesis.", "entity1": "COX-2", "entity2": "Thalidomide", "span1": [46, 51], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15353": {"label": 8, "data": {"text": "PURPOSE: Omeprazole has (R)- and (S)-enantiomers, which exhibit different pharmacokinetics (PK) among patients with cytochrome P450 (CYP) 2C19 genotype groups.", "entity1": "cytochrome P450 (CYP) 2C19", "entity2": "Omeprazole", "span1": [116, 142], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12598": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "serine protease domain", "entity2": "N", "span1": [107, 129], "span2": [140, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13186": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "SERT", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane", "span1": [272, 276], "span2": [0, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"768": {"label": 0, "data": {"text": "The inhibitor binds at the base of the active site gorge of TcAChE, interacting with both the choline-binding site (Trp-84) and the acyl-binding pocket (Phe-288, Phe-290).", "entity1": "acyl-binding pocket", "entity2": "Phe", "span1": [132, 151], "span2": [162, 165]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15147": {"label": 1, "data": {"text": "However, there were detectable concentrations of Lhcgr, Cyp11a1 and Cyp17a1 mRNAs but undetectable concentrations of Insl3, Hsd17b3 and Hsd11b1 in the DEHP-treated testes, indicating that these 3\u03b2-HSD(pos) cells were newly formed progenitor Leydig cells.", "entity1": "Lhcgr", "entity2": "DEHP", "span1": [49, 54], "span2": [151, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"51": {"label": 3, "data": {"text": "Comparison of the monoamine oxidase inhibiting properties of two reversible and selective monoamine oxidase-A inhibitors moclobemide and toloxatone, and assessment of their effect on psychometric performance in healthy subjects.", "entity1": "monoamine oxidase-A", "entity2": "toloxatone", "span1": [90, 109], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10393": {"label": 1, "data": {"text": "Angiotensin II acting on angiotensin AT1 receptors at the central nervous system appears to have an important role in these modulatory processes.", "entity1": "angiotensin AT1 receptors", "entity2": "Angiotensin II", "span1": [25, 50], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15511": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "Prx1", "entity2": "Cys", "span1": [163, 167], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3180": {"label": 2, "data": {"text": "We investigated the involvement of the farnesoid X receptor (FXR), a nuclear receptor for bile acids, in the chenodeoxycholic acid (CDCA)-induced expression of Cdx2 and MUC2 in normal rat gastric epithelial cells (RGM-1 cells).", "entity1": "MUC2", "entity2": "CDCA", "span1": [169, 173], "span2": [132, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4728": {"label": 1, "data": {"text": "In lymphoblastoid cells induced to undergo endoplasmic reticulum (ER) stress by treatment of tunicamycin, higher fold change of TCF7L2 and VEGFA mRNA levels were observed in rs7903146-TT cells than that in rs7903146-CC cells (P = 0.02 for TCF7L2; P = 0.004 for VEGFA), suggesting ER stress plays a role in PDR pathogenesis.", "entity1": "TCF7L2", "entity2": "tunicamycin", "span1": [128, 134], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15706": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "ASICs", "entity2": "acetic acid", "span1": [63, 68], "span2": [212, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11658": {"label": 1, "data": {"text": "Testosterone (TEST) had the fastest translocation rate for the hAR of 0.0525 min(-1).", "entity1": "hAR", "entity2": "TEST", "span1": [63, 66], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"439": {"label": 9, "data": {"text": "Chlorpheniramine (10 microM), another histamine H1 receptor antagonist without significant 5-HT receptor binding affinity, did not produce any inhibition of the eNANC contraction.", "entity1": "5-HT receptor", "entity2": "Chlorpheniramine", "span1": [91, 104], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"7043": {"label": 1, "data": {"text": "Experiments with Schwann cell primary cultures revealed an effect of retinoic acid on the expression of the neuregulin receptor ErbB3, suggesting that one function of retinoic acid consists in the regulation of neuroglial interactions after peripheral nerve injury.", "entity1": "neuregulin receptor", "entity2": "retinoic acid", "span1": [108, 127], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10381": {"label": 3, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "ACE", "entity2": "GW660511X", "span1": [99, 102], "span2": [126, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4653": {"label": 3, "data": {"text": "Enzyme kinetic analyses using human liver microsomes revealed inhibition of CYP1A1 activity by delphinidin (IC50 78 \u03bcM) and pelargonidin (IC50 33 \u03bcM).", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [76, 82], "span2": [124, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"894": {"label": 1, "data": {"text": "Contrasting effects of N5-substituted tetrahydrobiopterin derivatives on phenylalanine hydroxylase, dihydropteridine reductase and nitric oxide synthase.", "entity1": "dihydropteridine reductase", "entity2": "N5-substituted tetrahydrobiopterin", "span1": [100, 126], "span2": [23, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8907": {"label": 2, "data": {"text": "Abrupt removal of amrinone or pentoxifylline from the culture medium prior to LPS stimulation, however, caused significantly augmented TNF production.", "entity1": "TNF", "entity2": "pentoxifylline", "span1": [135, 138], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14296": {"label": 3, "data": {"text": "In utero exposure to valproic acid (VPA), a histone deacetylase (HDAC) inhibitor, causes neural tube, heart, and limb defects.", "entity1": "histone deacetylase", "entity2": "VPA", "span1": [44, 63], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1403": {"label": 3, "data": {"text": "These results suggest that gemfibrozil inhibits the induction of iNOS probably by inhibiting the activation of NF-kappaB, AP-1, and C/EBPbeta and that gemfibrozil, a prescribed drug for humans, may further find its therapeutic use in neuroinflammatory diseases.", "entity1": "AP-1", "entity2": "gemfibrozil", "span1": [122, 126], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11184": {"label": 3, "data": {"text": "Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit.", "entity1": "NR2B", "entity2": "Felbamate", "span1": [83, 87], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10185": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "human organic anion transporting polypeptide A", "entity2": "rifamycin SV", "span1": [308, 354], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13393": {"label": 2, "data": {"text": "Metformin and phenformin, which are biguanides, have been reported to increase AMPK activity without increasing AMP/ATP.", "entity1": "AMPK", "entity2": "Metformin", "span1": [79, 83], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14637": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "CDA", "entity2": "dFdC", "span1": [86, 89], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13970": {"label": 3, "data": {"text": "METHODS: We conducted a case-control study to measure the association between selective cox-2 inhibitors, particularly celecoxib, rofecoxib, valdecoxib and non-specific NSAID subgroups, and breast cancer risk.", "entity1": "cox-2", "entity2": "rofecoxib", "span1": [88, 93], "span2": [130, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7005": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "PDGFR-beta", "entity2": "sorafenib", "span1": [238, 248], "span2": [162, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2920": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "ion channel", "entity2": "dronedarone", "span1": [9, 20], "span2": [51, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"869": {"label": 8, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ornithine decarboxylase", "entity2": "putrescine", "span1": [118, 141], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7582": {"label": 8, "data": {"text": "threo-methylphenidate inhibits the dopamine transporter and the norepinephrine transporter, resulting in elevations of these monoamines after impulse release.", "entity1": "dopamine transporter", "entity2": "monoamines", "span1": [35, 55], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10130": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "ketoprofen", "span1": [34, 37], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7767": {"label": 1, "data": {"text": "GDC-0152 induces NF-\u03baB transcriptional activity leading to expression of several chemokines and cytokines, of which tumor necrosis factor alpha (TNF-\u03b1) is the most important for single-agent tumor activity.", "entity1": "chemokines", "entity2": "GDC-0152", "span1": [81, 91], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9867": {"label": 8, "data": {"text": "A unique cytosolic activity related but distinct from NQO1 catalyses metabolic activation of mitomycin C.", "entity1": "NQO1", "entity2": "mitomycin C", "span1": [54, 58], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1177": {"label": 3, "data": {"text": "Nateglinide inhibits Kir6.2/SUR1 and Kir6.2/SUR2B channels at 100 nM, and inhibits Kir6.2/SUR2A channels at high concentrations (1 microM).", "entity1": "Kir6.2", "entity2": "Nateglinide", "span1": [21, 27], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15451": {"label": 3, "data": {"text": "Recommended management may include use of acetylcholinesterase inhibitors (e.g. neostigmine) and wound care on a case-by-case basis.", "entity1": "acetylcholinesterase", "entity2": "neostigmine", "span1": [42, 62], "span2": [80, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9247": {"label": 2, "data": {"text": "Cells propagated in medium containing N5-methyltetrahydrofolate and homocysteine showed a substantial increase in MS activity which paralleled the increase in the intracellular concentration of Me-Cbl and the Cbl bound to the enzyme.", "entity1": "MS", "entity2": "homocysteine", "span1": [114, 116], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7775": {"label": 0, "data": {"text": "In hypothalamus of mice administered a high-fat diet, there is a reduction in leptin and insulin-induced Tub-p-tyr and nuclear translocation, which is reversed by reducing protein tyrosine phosphatase 1B expression.", "entity1": "Tub", "entity2": "tyr", "span1": [105, 108], "span2": [111, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8528": {"label": 1, "data": {"text": "The antiherpetic action of CDM was measured by plaque reduction assay, and the immunomodulatory effect was determined by measuring the cytokine production using a bioassay and ELISA method.", "entity1": "cytokine", "entity2": "CDM", "span1": [135, 143], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9520": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "RAR beta", "entity2": "adapalene", "span1": [121, 129], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11351": {"label": 8, "data": {"text": "This information may be useful in the development of more potent sodiumsodium channel blockers.", "entity1": "sodium channel", "entity2": "sodium", "span1": [71, 85], "span2": [65, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12414": {"label": 8, "data": {"text": "This methodology was subsequently used to assess the relative contribution of OATP1B1 uptake in human hepatocytes for olmesartan (42%-62%), valsartan (28%-81%), rosuvastatin (64%-72%), pitavastatin (84%-98%) and lopinavir (64%-89%).", "entity1": "OATP1B1", "entity2": "olmesartan", "span1": [78, 85], "span2": [118, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13577": {"label": 1, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "fibronectin", "entity2": "l-glutamate", "span1": [422, 433], "span2": [304, 315]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"683": {"label": 8, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "GTPCH", "entity2": "BH4", "span1": [78, 83], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"820": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "STA2", "span1": [258, 275], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3934": {"label": 2, "data": {"text": "The reactivation of brain AChE inhibited with tabun demonstrated better activity of new compound BT-07-4M, TMB-4 and obidoxime from symmetric oximes, and BT-05 and BT-03 possessing asymmetric structure.", "entity1": "AChE", "entity2": "obidoxime", "span1": [26, 30], "span2": [117, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10686": {"label": 3, "data": {"text": "This manuscript presents the preclinical profile of lumiracoxib, a novel cyclooxygenase-2 (COX-2) selective inhibitor.", "entity1": "COX-2", "entity2": "lumiracoxib", "span1": [91, 96], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10401": {"label": 1, "data": {"text": "Taken together, these findings support the view that (1) OFQ is the only ppOFQ peptide that binds to and activates the ORL1 receptor and (2) OFQ II(1-28) does not bind or stimulate [35S]-GTPgammaS binding in cells expressing the mu opioid receptor.", "entity1": "ppOFQ", "entity2": "[35S]-GTPgammaS", "span1": [73, 78], "span2": [181, 196]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3611": {"label": 1, "data": {"text": "SB365, Pulsatilla saponin D suppresses the proliferation of human colon cancer cells and induces apoptosis by modulating the AKT/mTOR signalling pathway.", "entity1": "AKT", "entity2": "Pulsatilla saponin D", "span1": [125, 128], "span2": [7, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15325": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "fluoranthene", "span1": [287, 296], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12919": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine beta-synthase", "entity2": "Hydrogen sulfide", "span1": [131, 158], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3316": {"label": 1, "data": {"text": "Mutations in the Ca(2+) sensor, troponin C (TnC), were generated to increase/decrease the Ca(2+) sensitivity of cardiac skinned fibers to create the characteristic effects of DCM, HCM, and RCM.", "entity1": "troponin C", "entity2": "Ca(2+)", "span1": [32, 42], "span2": [90, 96]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8806": {"label": 8, "data": {"text": "Rates of benzydamine N-oxygenation (catalyzed by FMO3) varied (approximately 20-fold) among the 28 cynomolgus livers and were significantly correlated with FMO3 protein expression, indicating that the inter-animal variations in benzydamine N-oxygenation might be partly accounted for by the variable FMO3 expression.", "entity1": "FMO3", "entity2": "benzydamine", "span1": [300, 304], "span2": [228, 239]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6031": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "renzapride", "span1": [73, 79], "span2": [220, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2532": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "human b5R", "entity2": "heterocyclic amine", "span1": [297, 306], "span2": [139, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10032": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Lys", "span1": [199, 208], "span2": [63, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7415": {"label": 5, "data": {"text": "MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate), a noncompetitive NMDA receptor antagonist, partially prevented the decrease in cell viability and the energy impairment.", "entity1": "NMDA receptor", "entity2": "MK-801", "span1": [100, 113], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10834": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "BCR", "entity2": "Imatinib", "span1": [115, 118], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14798": {"label": 2, "data": {"text": "In addition, TSA induced Nrf2 nuclear translocation and up-regulated the expression of Nrf2-ARE downstream antioxidant genes, whereas Nrf2 knockdown by RNA interference blocked the inhibition of TSA on myofibroblast differentiation.", "entity1": "ARE", "entity2": "TSA", "span1": [92, 95], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"183": {"label": 3, "data": {"text": "In vitro studies, however, revealed that EO inhibits fibrin clot formation because of the Ca2+-chelating ability of its constituent ethanolamine, although oleate or benzyl alcohol exhibited procoagulant activity in FPA formation in vitro.", "entity1": "fibrin", "entity2": "EO", "span1": [53, 59], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10321": {"label": 2, "data": {"text": "Results indicate that imiquimod and resiquimod induce IFN-alpha and IFN-omega from purified pDC, and pDC are the principle IFN-producing cells in the blood.", "entity1": "IFN-alpha", "entity2": "imiquimod", "span1": [54, 63], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12337": {"label": 1, "data": {"text": "The two subtypes of mammalian G protein-coupled melatonin receptors are primarily responsible for mediating the actions of melatonin.", "entity1": "mammalian G protein-coupled melatonin receptors", "entity2": "melatonin", "span1": [20, 67], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12836": {"label": 3, "data": {"text": "To test the role of nicotinic receptors in the drugs' effects on [3H]-ACh release, mecamylamine (MEC) 100 microM was used to block such receptors.", "entity1": "nicotinic receptors", "entity2": "MEC", "span1": [20, 39], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6597": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "D(2)", "entity2": "WAY100635", "span1": [245, 249], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"684": {"label": 1, "data": {"text": "We topically applied the nitric oxide synthase (NOS) inhibitor, NG-nitro-L-arginine, on sciatic nerve and observed reduced inhibition of NBF in EDN, which was correctable with a cilazapril diet.", "entity1": "nitric oxide synthase", "entity2": "cilazapril", "span1": [25, 46], "span2": [178, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3347": {"label": 1, "data": {"text": "The high resolution NMR solution structure of the cTnC-cTnI-dfbp-o ternary complex showed that dfbp-o bound at the hydrophobic interface formed by cTnC and cTnI making critical interactions with residues such as Arg147 of cTnI.", "entity1": "cTnI", "entity2": "dfbp-o", "span1": [55, 59], "span2": [60, 66]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9108": {"label": 9, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "calmodulin", "entity2": "prazosin", "span1": [165, 175], "span2": [113, 121]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2750": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "ABL", "entity2": "BMS-354825", "span1": [99, 102], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8704": {"label": 2, "data": {"text": "Taken together, our results indicate that arsenic indeed upregulates the AT1R expression, thus highlighting a role of arsenic-induced aberrant AT1R signaling in the pathogenesis of hypertension.", "entity1": "AT1R", "entity2": "arsenic", "span1": [73, 77], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"700": {"label": 4, "data": {"text": "The potency of the selective alpha 1D-adrenoceptor antagonist BMY 7378 against noradrenaline (pA2 = 6.16 +/- 0.13) and of the selective alpha 1A-adrenoceptor antagonist RS-17053 against noradrenaline (pKB = 8.35 +/- 0.10) and against the selective alpha 1A-adrenoceptor agonist A-61603 (pKB = 8.40 +/- 0.09) were too low to account for alpha 1D- and alpha 1A-adrenoceptor involvement.", "entity1": "alpha 1A-adrenoceptor", "entity2": "A-61603", "span1": [248, 269], "span2": [278, 285]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5045": {"label": 3, "data": {"text": "Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 2.", "entity1": "ACAT2", "entity2": "pyripyropene A", "span1": [140, 145], "span2": [49, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1331": {"label": 3, "data": {"text": "In clinical trials eprosartan has proven to be at least as effective as the ACE inhibitor enalapril in reducing BP, but with a significantly lower incidence of side effects.", "entity1": "ACE", "entity2": "eprosartan", "span1": [76, 79], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"921": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "carteolol", "span1": [22, 39], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7853": {"label": 2, "data": {"text": "Protein kinase C (PKC) inhibition reduced the potentiation by mGlu1 of GluK2/GluK5, and conversely, direct activation of PKC by phorbol 12-myristate,13-acetate potentiated GluK2/GluK5.", "entity1": "GluK2", "entity2": "phorbol 12-myristate,13-acetate", "span1": [172, 177], "span2": [128, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15641": {"label": 3, "data": {"text": "Furthermore, nobiletin could inhibit HGF-induced the membrane localization of phosphorylated c-Met, ERK2, and Akt, but not phosphorylated JNK1/2 and p38.", "entity1": "ERK2", "entity2": "nobiletin", "span1": [100, 104], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11404": {"label": 1, "data": {"text": "Here, we show that meclofenamic acid (meclofenamate) and diclofenac, two related molecules previously used as anti-inflammatory drugs, act as novel KCNQ2/Q3 channel openers.", "entity1": "KCNQ2/Q3", "entity2": "meclofenamate", "span1": [148, 156], "span2": [38, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10914": {"label": 1, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "gastric mucin", "entity2": "isoproterenol", "span1": [4, 17], "span2": [41, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14566": {"label": 2, "data": {"text": "Furthermore, knockdown of Brms1L significantly attenuated GnRH-induced FSH\u03b2 expression.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [71, 75], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"303": {"label": 2, "data": {"text": "It is concluded that D-1997 contracts the canine basilar artery by stimulating 5-HT1-like receptors unrelated to either the 5-HT1A or 5-HT1B receptor subtypes.", "entity1": "5-HT1B", "entity2": "D-1997", "span1": [134, 140], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14898": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "flavin mono-oxygenase", "entity2": "TMAO", "span1": [24, 45], "span2": [156, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3109": {"label": 3, "data": {"text": "Tacrine, the first of the cholinesterase inhibitors to undergo extensive trials for this purpose, was associated with significant adverse effects including hepatotoxicity.", "entity1": "cholinesterase", "entity2": "Tacrine", "span1": [26, 40], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13671": {"label": 9, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imidazoquinoline", "span1": [138, 142], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7379": {"label": 3, "data": {"text": "RAMH inhibition of cholangiocyte growth was associated with decreased cAMP levels and PKA/ERK1/2/Elk-1 phosphorylation.", "entity1": "ERK1/2", "entity2": "RAMH", "span1": [90, 96], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11345": {"label": 3, "data": {"text": "Block of human NaV1.5 sodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin.", "entity1": "sodium channels", "entity2": "alpha-hydroxyphenylamide", "span1": [22, 37], "span2": [47, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13991": {"label": 3, "data": {"text": "Collectively, these data suggest that cabozantinib is a promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling.", "entity1": "MET", "entity2": "cabozantinib", "span1": [150, 153], "span2": [38, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5653": {"label": 3, "data": {"text": "Arsenic trioxide (As(2)O(3)), which is used to treat acute promyelocytic leukemia, can cause LQTS type 2 (LQT2) by reducing the hERG current through the diversion of hERG trafficking to the cytoplasmic membrane.", "entity1": "hERG", "entity2": "As(2)O(3)", "span1": [166, 170], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4457": {"label": 2, "data": {"text": "Cadmium activates NADPH oxidase.", "entity1": "NADPH oxidase", "entity2": "Cadmium", "span1": [18, 31], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9797": {"label": 3, "data": {"text": "Another inhibitor, brequinar was previously reported to be a slow-binding inhibitor of the human dihydroorotate dehydrogenase [W. Knecht, M. Loffler, Species-related inhibition of human and rat dihyroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives, Biochem.", "entity1": "human and rat dihyroorotate dehydrogenase", "entity2": "cinchoninic acid", "span1": [180, 221], "span2": [256, 272]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"793": {"label": 1, "data": {"text": "Lithium modulates desensitization of the glutamateglutamate receptor subtype gluR3 in Xenopus oocytes.", "entity1": "glutamate receptor", "entity2": "glutamate", "span1": [50, 68], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8457": {"label": 3, "data": {"text": "Hinokitiol inhibited the phosphorylation of phospholipase C (PLC)\u03b32, protein kinase C (PKC), mitogen-activated protein kinases (MAPKs), and Akt in collagen-activated human platelets, and significantly reduced intracellular calcium mobilization and hydroxyl radical (OH) formation.", "entity1": "protein kinase C", "entity2": "Hinokitiol", "span1": [69, 85], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6661": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [80, 85], "span2": [211, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2087": {"label": 3, "data": {"text": "In addition, VEGF-induced formation of tube-like structures in vitro and neovascularization in mouse corneas were significantly inhibited by Am80.", "entity1": "VEGF", "entity2": "Am80", "span1": [13, 17], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6931": {"label": 8, "data": {"text": "When cultured in YPD medium containing 15% glucose under aerobic conditions, the KGD1 (alpha-ketoglutarate dehydrogenase) gene disrupted mutant produced a lower level of succinate than the wild-type strain, while the SDH1 (succinate dehydrogenase) gene-disrupted mutant produced an increased level of succinate.", "entity1": "succinate dehydrogenase", "entity2": "succinate", "span1": [223, 246], "span2": [301, 310]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10490": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "bisoprolol", "span1": [392, 423], "span2": [277, 287]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10773": {"label": 2, "data": {"text": "Imatinib stimulated the rapid release of soluble HB-EGF and the subsequent induction of membrane-bound HB-EGF, which correlated with biphasic MAPK activation.", "entity1": "HB-EGF", "entity2": "Imatinib", "span1": [103, 109], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5263": {"label": 0, "data": {"text": "Interestingly, Nox4 activity is also stimulated by reducing agents that possibly act by reducing the disulfide bridge (Cys226, Cys270) located in the extracellular E-loop of Nox4.", "entity1": "Nox4", "entity2": "Cys", "span1": [174, 178], "span2": [119, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4778": {"label": 9, "data": {"text": "We show that CIQ does not bind to the amino-terminal domain of the NMDA receptor and does not share structural determinants with modulators acting at the agonist-binding domain dimer interface or ion channel pore.", "entity1": "ion channel", "entity2": "CIQ", "span1": [196, 207], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13663": {"label": 1, "data": {"text": "High-resolution NMR spectroscopy was used to determine the docking of a substrate (prostaglandin H2) mimic (U46619) to the engineered prostacyclin (PGI2) synthase (PGIS) in solution.", "entity1": "PGIS", "entity2": "prostaglandin H2", "span1": [164, 168], "span2": [83, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2290": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP2", "entity2": "butaprost", "span1": [127, 130], "span2": [149, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3339": {"label": 3, "data": {"text": "Rasagiline is a propargylamine and irreversible monoamine oxidase (MAO) B inhibitor used for the treatment of Parkinson's disease (PD).", "entity1": "monoamine oxidase (MAO) B", "entity2": "propargylamine", "span1": [48, 73], "span2": [16, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15184": {"label": 2, "data": {"text": "Moreover, compared with the model group, sophocarpine could significantly increase P-AMPK\u03b1 (>5.82-fold), AMPK\u03b1 (>1.29-fold) and ACC (>3.27-fold) protein expressions, and reduce P-ACC (<0.30-fold) and HNF-4\u03b1 (<0.20-fold) protein expression.", "entity1": "AMPK\u03b1", "entity2": "sophocarpine", "span1": [105, 110], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6859": {"label": 5, "data": {"text": "Effect of bosentan (ETA/ETB receptor antagonist) on metabolic changes during stress and diabetes.", "entity1": "ETA", "entity2": "bosentan", "span1": [20, 23], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15721": {"label": 9, "data": {"text": "Fourteen of 17 parabens exhibited hER\u03b1 and/or hER\u03b2 agonistic activity at concentrations of \u2a7d1\u00d710(-5)M, whereas none of the 17 parabens showed AR agonistic or antagonistic activity.", "entity1": "AR", "entity2": "parabens", "span1": [142, 144], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15764": {"label": 9, "data": {"text": "Both ICI treatments, induced a significant decrease (p<0.01) in uterine estrogen receptor alpha (ER\u03b1) content, had no effect on uterine progesterone receptor (PR) protein expression and caused marked nuclear localization of cyclin D1, in both luminal and glandular uterine epithelium, as compared to vehicle-treated animals.", "entity1": "progesterone receptor", "entity2": "ICI", "span1": [136, 157], "span2": [5, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4964": {"label": 3, "data": {"text": "Pregnane X Receptor Mediates Dyslipidemia Induced by the HIV Protease Inhibitor Amprenavir in Mice.", "entity1": "HIV Protease", "entity2": "Amprenavir", "span1": [57, 69], "span2": [80, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9218": {"label": 1, "data": {"text": "Three lines of evidence suggest that calmodulin inhibition is not responsible for the inhibition of binding and endocytosis: 1) Promethazine, a phenothiazine that is a poor inhibitor of calmodulin, is nearly as effective as TFP at inhibiting endocytosis; calmidazolium, a potent inhibitor of several calmodulin functions, did not cause a loss of binding; 2) the microinjection of calmodulin into cells did not reverse the effects of W-7; using pressure microinjection, we introduced up to a 100-fold excess of calmodulin over native levels into individual gerbil fibroma cells; using rhodamine-labeled alpha 2-macroglobulin, we saw that the W-7 induced inhibition of receptor-mediated endocytosis was the same in injected and uninjected cells; 3) we injected calcineurin, a calmodulin-binding protein, into cells (1-3 pg/cell) and observed no effect on the receptor-mediated endocytosis of rhodamine-labeled alpha 2-macroglobulin.", "entity1": "alpha 2-macroglobulin", "entity2": "rhodamine", "span1": [602, 623], "span2": [584, 593]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6584": {"label": 8, "data": {"text": "It is caused by a deficiency of propionyl-CoA carboxylase (PCC, EC 6.4.1.3), a biotin-dependent enzyme that catalyzes the carboxylation of propionyl-CoA to D-methylmalonyl-CoA.", "entity1": "PCC", "entity2": "propionyl-CoA", "span1": [59, 62], "span2": [139, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14143": {"label": 1, "data": {"text": "Mianserin and mirtazapine increased ERK1/2 phosphorylation in CHO cells expressing kappa-opioid receptors and C6 cells, and these effects were antagonized by nor-BNI.", "entity1": "kappa-opioid receptors", "entity2": "mirtazapine", "span1": [83, 105], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12032": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "EO", "entity2": "EOI", "span1": [75, 77], "span2": [155, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1269": {"label": 3, "data": {"text": "We find that minocycline inhibits mitochondrial permeability-transition-mediated cytochrome c release.", "entity1": "cytochrome c", "entity2": "minocycline", "span1": [81, 93], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4643": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A2", "entity2": "pelargonidin", "span1": [11, 17], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6603": {"label": 3, "data": {"text": "METHODS: Using a cutaneous full-thickness, sutured, incisional wound model in hairless SKH-1 mice, we evaluated the role of COX-2 in the wound healing process by comparing the effects of a nonselective COX inhibitor, diclofenac, with a selective COX-2 inhibitor, SC-791.", "entity1": "COX", "entity2": "diclofenac", "span1": [202, 205], "span2": [217, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14965": {"label": 1, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANKL", "entity2": "serine", "span1": [163, 168], "span2": [84, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8317": {"label": 1, "data": {"text": "Refining the UGT1A haplotype associated with irinotecan-induced hematological toxicity in metastatic colorectal cancer patients treated with 5-fluorouracil/irinotecan-based regimens.", "entity1": "UGT1A", "entity2": "irinotecan", "span1": [13, 18], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1520": {"label": 9, "data": {"text": "Neither okadaic acid nor cantharidin (1-10000 nM) displaced [3H]naloxone from its specific binding sites, which indicates that they do not interact at the opioid receptor level.", "entity1": "opioid receptor", "entity2": "cantharidin", "span1": [155, 170], "span2": [25, 36]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8673": {"label": 2, "data": {"text": "Surprisingly, the conditional deletion of Trp63, but not \u0394Np63, in oocytes inhibited apoptosis, as well as the accumulation of c-Abl and TAp73 caused by cisplatin.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [127, 132], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7565": {"label": 5, "data": {"text": "Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12 receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes.", "entity1": "P2Y12", "entity2": "clopidogrel", "span1": [65, 70], "span2": [106, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6029": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "sumatriptan", "span1": [63, 69], "span2": [207, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7942": {"label": 2, "data": {"text": "We show that the expression of PIM-1 is induced in response to estradiol in MCF-7 cells and that the induction is mediated by ER\u03b1-regulated enhancers located distally upstream from the gene.", "entity1": "ER\u03b1", "entity2": "estradiol", "span1": [126, 129], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15994": {"label": 1, "data": {"text": "Puerarin stimulates proliferation and differentiation and protects against cell death in human osteoblastic MG-63 cells via ER-dependent MEK/ERK and PI3K/Akt activation.", "entity1": "ER", "entity2": "Puerarin", "span1": [124, 126], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2887": {"label": 3, "data": {"text": "In hippocampal dentate gyrus, MPH-receiving rats showed a 51% decrease in NET-ir density and a 61% expanded distribution of the new-cell marker PSA-NCAM (polysialylated form of neural cell adhesion molecule).", "entity1": "NET", "entity2": "MPH", "span1": [74, 77], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9300": {"label": 3, "data": {"text": "The data suggest that lysine analogues, even at low concentrations, reduce the rate of t-PA induced whole blood clot lysis by several mechanisms.", "entity1": "t-PA", "entity2": "lysine", "span1": [87, 91], "span2": [22, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13322": {"label": 3, "data": {"text": "Oral aspirin (as a representative of the salicylate family) inhibited diabetes-induced increase in NF-kappaB DNA-binding affinity in electrophoretic mobility shift assay and transcription factor array in nuclear extract isolated from whole retina.", "entity1": "NF-kappaB", "entity2": "aspirin", "span1": [99, 108], "span2": [5, 12]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15863": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "Human Serum Albumin", "entity2": "Lys", "span1": [46, 65], "span2": [151, 154]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"412": {"label": 1, "data": {"text": "The quinazoline antagonists, prazosin, doxazosin and alfuzosin displayed high affinity but were non selective for the three cloned human alpha 1 adrenoceptors.", "entity1": "human alpha 1 adrenoceptors", "entity2": "quinazoline", "span1": [131, 158], "span2": [4, 15]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8773": {"label": 9, "data": {"text": "Overexpression of Akt1 or Akt2 in TW2.6 cells rescued growth inhibition caused by CAPE treatment.", "entity1": "Akt2", "entity2": "CAPE", "span1": [26, 30], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14713": {"label": 3, "data": {"text": "Furthermore, insulin-stimulated T-I cell proliferation and the expression of cell cycle regulatory proteins CDK4, CCND3 and PCNA were also blocked by rapamycin.", "entity1": "CDK4", "entity2": "rapamycin", "span1": [108, 112], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10276": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "OCT", "entity2": "amantadine", "span1": [123, 126], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"200": {"label": 1, "data": {"text": "WB 4101, benoxathian and phentolamine displayed high affinity for alpha 1A and alpha 1D adrenoceptors compared to the alpha 1B subtype.", "entity1": "alpha 1A and alpha 1D adrenoceptors", "entity2": "benoxathian", "span1": [66, 101], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8932": {"label": 1, "data": {"text": "Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release.", "entity1": "5-hydroxytryptamine1B", "entity2": "[125I]iodocyanopindolol", "span1": [20, 41], "span2": [75, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12309": {"label": 8, "data": {"text": "Recent studies, however, have demonstrated a promising potential treatment option with the help of the serum enzyme butyrylcholinesterase (BChE), which is capable of breaking down naturally occurring (-)-cocaine before the drug can influence the reward centers of the brain or affect other areas of the body.", "entity1": "butyrylcholinesterase", "entity2": "(-)-cocaine", "span1": [116, 137], "span2": [200, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14821": {"label": 3, "data": {"text": "Dabigatran has an advantage over the indirect thrombin inhibitors, unfractionated heparin and low-molecular-weight heparin, in that it inhibits free and fibrin-bound thrombin.", "entity1": "thrombin", "entity2": "Dabigatran", "span1": [46, 54], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5729": {"label": 3, "data": {"text": "Rg1 attenuated the A\u03b225-35-associated mitochondrial apoptotic events, accompanied by inhibiting HIF-1\u03b1 expression followed by intracellular reactive nitrogen species generation, and protein nitrotyrosination.", "entity1": "A\u03b225-35", "entity2": "Rg1", "span1": [19, 26], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13666": {"label": 1, "data": {"text": "For example, Trp282 could be one of the most important residues and is suspected to play a role in the determination of specific catalytic function, which has been established by the docking studies using the NMR structure of the PGIS-bound form of U46619 and the PGIS crystal structure.", "entity1": "PGIS", "entity2": "U46619", "span1": [264, 268], "span2": [249, 255]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13668": {"label": 3, "data": {"text": "This overview focuses on the indirect antithrombin dependent pentasaccharide derivatives of idraparinux and on the most advanced oral direct inhibitors to factor Xa (rivaroxaban and apixaban) and IIa (dabigatran).", "entity1": "factor Xa", "entity2": "rivaroxaban", "span1": [155, 164], "span2": [166, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15661": {"label": 3, "data": {"text": "We have identified 3-hydroxypyridin-2-thione (3-HPT) as a novel ZBG that is compatible with HDAC inhibition.", "entity1": "HDAC", "entity2": "3-hydroxypyridin-2-thione", "span1": [92, 96], "span2": [19, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10556": {"label": 1, "data": {"text": "The retention and slow diffusion of DMI and nisoxetine from membranes may contribute to their pharmacological and modulatory action on NET.", "entity1": "NET", "entity2": "nisoxetine", "span1": [135, 138], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8378": {"label": 3, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "GLUT4", "entity2": "BPA", "span1": [185, 190], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2207": {"label": 3, "data": {"text": "Doxycycline was shown to decrease cerebral MMP-9 activities and angiogenesis induced by vascular endothelial growth factor (VEGF).", "entity1": "VEGF", "entity2": "Doxycycline", "span1": [124, 128], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14668": {"label": 1, "data": {"text": "Inhibition of PKA significantly attenuated the effect of genistein on thrombin-induced EC permeability, MLC phosphorylation, and RhoA membrane translocation in ECs.", "entity1": "RhoA", "entity2": "genistein", "span1": [129, 133], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7211": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "c-fos", "entity2": "Cd", "span1": [165, 170], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14670": {"label": 1, "data": {"text": "These findings demonstrated that genistein improves thrombin-induced endothelial barrier dysfunction in ECs through PKA-mediated suppression of RhoA signaling.", "entity1": "PKA", "entity2": "genistein", "span1": [116, 119], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"436": {"label": 1, "data": {"text": "Ka values in nM for rauwolscine (19), WB-4101 (265), SKF-104078 (197), spiroxatrine (128), and prazosin (1531) for blocking relaxation in rat arteries were consistent with their affinities for binding at the alpha-2D adrenoceptor subtype.", "entity1": "alpha-2D adrenoceptor", "entity2": "prazosin", "span1": [208, 229], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5663": {"label": 3, "data": {"text": "Long-term treatment with 1 \u03bcM matrine or oxymatrine increased expression of the hERG protein and rescued the hERG surface expression disrupted by As(2)O(3).", "entity1": "hERG", "entity2": "As(2)O(3)", "span1": [80, 84], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9766": {"label": 5, "data": {"text": "In distinction to yohimbine, fluparoxan shows only modest partial agonist actions at h5-HT(1A) sites versus marked antagonist actions at halpha(2)-ARs.", "entity1": "halpha(2)-ARs", "entity2": "yohimbine", "span1": [137, 150], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9471": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "IP", "entity2": "isocabacyclin", "span1": [210, 212], "span2": [192, 205]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3497": {"label": 3, "data": {"text": "A significant decrease of aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase (LDH) activities and glutathione (GSH) levels and an increase of malondialdehyde (MDA) quantity was observed after CCl4 and PC administration alone.", "entity1": "LDH", "entity2": "CCl4", "span1": [103, 106], "span2": [217, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9103": {"label": 8, "data": {"text": "Similar concentrations also inhibited the formation of leukotriene C4 (LTC4) by LTC synthetase, a detergent-solubilized cell free particulate enzyme from RBL cells which is capable of coupling LTA4 to glutathione.", "entity1": "LTC synthetase", "entity2": "LTC4", "span1": [80, 94], "span2": [71, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14730": {"label": 3, "data": {"text": "The porcine heart malate dehydrogenase (MDH) refolding assay revealed that compound 1l inhibited human Hsp60 chaperone activity (IC(50): 6.80 \u00b1 0.25 \u03bcM) and this inhibition activity was higher than that of ETB (IC(50): 10.9 \u00b1 0.63 \u03bcM).", "entity1": "human Hsp60", "entity2": "ETB", "span1": [97, 108], "span2": [206, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13665": {"label": 1, "data": {"text": "For example, Trp282 could be one of the most important residues and is suspected to play a role in the determination of specific catalytic function, which has been established by the docking studies using the NMR structure of the PGIS-bound form of U46619 and the PGIS crystal structure.", "entity1": "PGIS", "entity2": "U46619", "span1": [230, 234], "span2": [249, 255]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"492": {"label": 2, "data": {"text": "Conversely, opioid antagonists such as naloxone and naltrexone (which bind to non-selectively opioid receptors) have been shown to decrease alcohol consumption under various experimental conditions.", "entity1": "opioid receptors", "entity2": "naltrexone", "span1": [94, 110], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7083": {"label": 2, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "TRPA1", "entity2": "camphor", "span1": [111, 116], "span2": [25, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9079": {"label": 2, "data": {"text": "In the high-dose ROAc group, there was a twofold increase in prothrombin times but only after prolonged dosing.", "entity1": "prothrombin", "entity2": "ROAc", "span1": [61, 72], "span2": [17, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6313": {"label": 8, "data": {"text": "Activation of endothelial nitric oxide synthase (eNOS) results in the production of nitric oxide (NO) that mediates the vasorelaxing properties of endothelial cells.", "entity1": "endothelial nitric oxide synthase", "entity2": "NO", "span1": [14, 47], "span2": [98, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13616": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "PDGFR-beta", "entity2": "sunitinib", "span1": [210, 220], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11175": {"label": 1, "data": {"text": "OBJECTIVE: To determine the expression of progesterone receptor (PR) mRNA and PR protein levels in the myometrium and leiomyomata from untreated and mifepristone pretreated women with leiomyoma and to examine the mechanism of mifepristone treatment on uterine leiomyomata.", "entity1": "PR", "entity2": "mifepristone", "span1": [65, 67], "span2": [149, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7878": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "BSEP", "entity2": "lopinavir", "span1": [84, 88], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7607": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(2)", "entity2": "Conivaptan", "span1": [187, 191], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5684": {"label": 8, "data": {"text": "HZ mice are also more sensitive to the peripheral application of the selective AChE inhibitor donepezil or the mixed inhibitor physostigmine; extracellular ACh levels rise significantly after administration of both drugs; also glucose levels are moderately increased indicating potentially non-cholinergic effects of donepezil.", "entity1": "AChE", "entity2": "ACh", "span1": [79, 83], "span2": [156, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12945": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "lixivaptan", "span1": [39, 59], "span2": [119, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4833": {"label": 2, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "Mcl-1", "entity2": "7\u03b2OHC", "span1": [247, 252], "span2": [67, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3655": {"label": 8, "data": {"text": "The results show that CYP2E1 inhibits CYP2B4-mediated metabolism of benzphetamine (BNZ) with a K(i) of 0.04 \u00b5M.", "entity1": "CYP2B4", "entity2": "BNZ", "span1": [38, 44], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8183": {"label": 1, "data": {"text": "Although tamoxifen (TAM), a selective estrogen receptor modulator, has been widely used in the treatment of hormone-responsive breast cancer, its estrogen-like effect increases the risk of endometrial cancer.", "entity1": "estrogen receptor", "entity2": "TAM", "span1": [38, 55], "span2": [20, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12869": {"label": 2, "data": {"text": "Similar to the plasma membrane PS transporter, Atp8a1 is activated only by the naturally occurring sn-1,2-glycerol isomer of PS and not the sn-2,3-glycerol stereoisomer.", "entity1": "plasma membrane PS transporter", "entity2": "sn-1,2-glycerol", "span1": [15, 45], "span2": [99, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"6056": {"label": 3, "data": {"text": "Actinomycin D caused alpha-AR mRNA level to decrease with a half-life of 3.2 +/- 0.4 h and blocked the effect of H-7 to decrease basal alpha-AR mRNA level.", "entity1": "alpha-AR", "entity2": "Actinomycin D", "span1": [135, 143], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4000": {"label": 3, "data": {"text": "Mechanisms limiting distribution of the threonine-protein kinase B-RaF(V600E) inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain metastases.", "entity1": "threonine-protein kinase B-RaF", "entity2": "dabrafenib", "span1": [40, 70], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15102": {"label": 3, "data": {"text": "Moreover, treatment of high-fat-diet-fed apelin-knockout mice with a selective cyclooxygenase-2 inhibitor, celecoxib, improved vascular function, and also attenuated obesity.", "entity1": "cyclooxygenase-2", "entity2": "celecoxib", "span1": [79, 95], "span2": [107, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6882": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "CBS", "entity2": "L-cysteine", "span1": [65, 68], "span2": [78, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11000": {"label": 1, "data": {"text": "Interestingly, exposure to a lower concentration (1 microM) of the antidepressants tended to increase T-cell-derived IL-10 production, with significant effects elicited by the noradrenaline reuptake inhibitors reboxetine and desipramine.", "entity1": "IL-10", "entity2": "reboxetine", "span1": [117, 122], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9294": {"label": 5, "data": {"text": "In beta-escin-skinned strips of chloroethylclonidine-pretreated smooth muscle, the enhancement of Ca2+ contraction produced by norepinephrine was significantly decreased, whereas the amplitude was the same as that produced by methoxamine or clonidine; this enhancement was inhibited by the selective alpha 1A-adrenoceptor antagonist WB 4101 (100 nM).", "entity1": "alpha 1A-adrenoceptor", "entity2": "WB 4101", "span1": [300, 321], "span2": [333, 340]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9635": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "prostate-specific antigen", "entity2": "estramustine", "span1": [19, 44], "span2": [85, 97]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2490": {"label": 3, "data": {"text": "Moreover, licofelone inhibited COX-2 and 5-LOX protein expression in vascular lesions.", "entity1": "5-LOX", "entity2": "licofelone", "span1": [41, 46], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11999": {"label": 1, "data": {"text": "We found that in vitro rapamycin also regulates the proteasome, an essential intracellular protease of the ubiquitin-proteasome pathway.", "entity1": "proteasome", "entity2": "rapamycin", "span1": [117, 127], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10114": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "COX-1", "entity2": "ketoprofen", "span1": [18, 23], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1254": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "beclomethasone", "span1": [277, 280], "span2": [43, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1625": {"label": 3, "data": {"text": "This led to the discovery of aliskiren, a highly potent and selective inhibitor of human renin in vitro, and in vivo; once-daily oral doses of aliskiren inhibit renin and lower blood pressure in sodium-depleted marmosets and hypertensive human patients.", "entity1": "renin", "entity2": "aliskiren", "span1": [161, 166], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"576": {"label": 2, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cyclin E", "entity2": "Tomudex", "span1": [35, 43], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14476": {"label": 3, "data": {"text": "The reaction was inhibited by the specific CYP2D inhibitors quinine and fluoxetine.", "entity1": "CYP2D", "entity2": "quinine", "span1": [43, 48], "span2": [60, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1395": {"label": 3, "data": {"text": "However, DeltahPPAR-alpha was unable to abrogate gemfibrozil-mediated inhibition of iNOS suggesting that gemfibrozil inhibits iNOS independent of PPAR-alpha.", "entity1": "iNOS", "entity2": "gemfibrozil", "span1": [126, 130], "span2": [105, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6980": {"label": 1, "data": {"text": "RESULTS: With regard to PRA, dobutamine increased PRA more potently in Arg389-beta1AR versus Gly389-beta1AR subjects.", "entity1": "beta1AR", "entity2": "dobutamine", "span1": [100, 107], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12064": {"label": 1, "data": {"text": "Chronic effect of [D-Pen2,D-Pen5]enkephalin on rat brain opioid receptors.", "entity1": "rat brain opioid receptors", "entity2": "[D-Pen2,D-Pen5]enkephalin", "span1": [47, 73], "span2": [18, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12958": {"label": 0, "data": {"text": "Previously, we reported that l-glutamic acid decarboxylase isoform 65 (GAD65) could be cleaved in vitro to release a stable truncated form which lacks amino acid 1-69 from the N-terminus, GAD65(Delta1-69).", "entity1": "GAD65(Delta1-69)", "entity2": "N", "span1": [188, 204], "span2": [176, 177]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9056": {"label": 1, "data": {"text": "7-Hydroxy levomepromazine, 3-hydroxy levomepromazine and 7-hydroxy fluphenazine had only 10% of the potency of the parent drug in histamine H1 receptor binding, while the 7-hydroxy-metabolites of chlorpromazine and perphenazine had about 75% of the potency of the parent drug in this binding system.", "entity1": "histamine H1 receptor", "entity2": "7-Hydroxy levomepromazine", "span1": [130, 151], "span2": [0, 25]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8604": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "ALP", "entity2": "CCl4", "span1": [41, 44], "span2": [78, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10884": {"label": 9, "data": {"text": "To understand this interaction, we determined the crystal structure of PDXK in complex with (R)-roscovitine, N6-methyl-(R)-roscovitine, and O6-(R)-roscovitine, the two latter derivatives being designed to bind to PDXK but not to CDKs.", "entity1": "CDKs", "entity2": "O6-(R)-roscovitine", "span1": [229, 233], "span2": [140, 158]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1239": {"label": 3, "data": {"text": "The selective PDE 4 inhibitors, and to a certain extent the PDE3 inhibitors amrinone and milrinone, reduced the GM-CSF release in a concentration dependent manner.", "entity1": "GM-CSF", "entity2": "milrinone", "span1": [112, 118], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12259": {"label": 1, "data": {"text": "Isothiocyanates, thought to be responsible for the chemopreventive properties of this food group, are conjugated to glutathione by glutathione S-transferases (GSTs) before urinary excretion.", "entity1": "glutathione S-transferases", "entity2": "Isothiocyanates", "span1": [131, 157], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4463": {"label": 3, "data": {"text": "Catalpol also suppressed AGE-induced phosphorylation of mitogen activated protein (MAP) kinases, degradation of I\u03baB\u03b1 and the nuclear localization of NF-\u03baB.", "entity1": "I\u03baB\u03b1", "entity2": "Catalpol", "span1": [112, 116], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10902": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "CDKs", "entity2": "CYC202", "span1": [102, 106], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8351": {"label": 3, "data": {"text": "This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.", "entity1": "Rock", "entity2": "amino acid", "span1": [22, 26], "span2": [51, 61]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2181": {"label": 2, "data": {"text": "Tissue-type plasminogen activator (tPA), a serine protease well known for generating plasmin, has been demonstrated to induce matrix metalloproteinase-9 (MMP-9) gene expression and protein secretion in renal interstitial fibroblasts.", "entity1": "plasmin", "entity2": "serine", "span1": [85, 92], "span2": [43, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4151": {"label": 3, "data": {"text": "Lung inflammation, IL-4 production, and airway mast cell activity were also prevented under this early short-term treatment with PGE2.", "entity1": "IL-4", "entity2": "PGE2", "span1": [19, 23], "span2": [129, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14385": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "PI3K", "entity2": "AG1478", "span1": [137, 141], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1507": {"label": 4, "data": {"text": "OBJECTIVE: Preclinical evaluation of DRF 2655, a peroxisome proliferator-activated receptor alpha (PPARalpha) and PPARgamma agonist, as a body-weight lowering, hypolipidemic and euglycemic agent.", "entity1": "PPARgamma", "entity2": "DRF 2655", "span1": [114, 123], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5452": {"label": 3, "data": {"text": "Take together, our results demonstrated that juglone might induce the apoptosis in LNCaP cell via down-regulation of AR expression.", "entity1": "AR", "entity2": "juglone", "span1": [117, 119], "span2": [45, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15685": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "cyclin B1", "entity2": "EVn-50", "span1": [245, 254], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"487": {"label": 1, "data": {"text": "The atypical neuroleptics remoxipride, clozapine, perlapine, seroquel, and melperone had low affinity for the dopamine D2 receptor (radioligand-independent dissociation constants of 30 to 90 nM).", "entity1": "D2 receptor", "entity2": "melperone", "span1": [119, 130], "span2": [75, 84]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5365": {"label": 3, "data": {"text": "Vitamin C forestalls cigarette smoke induced NF-\u03baB activation in alveolar epithelial cells.", "entity1": "NF-\u03baB", "entity2": "Vitamin C", "span1": [45, 50], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"993": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "endothelial NO synthase", "entity2": "BH(4)", "span1": [89, 112], "span2": [59, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"3978": {"label": 8, "data": {"text": "The influence of sex, ethnicity, and CYP2B6 genotype on bupropion metabolism as an index of hepatic CYP2B6 activity in humans.", "entity1": "CYP2B6", "entity2": "bupropion", "span1": [37, 43], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13235": {"label": 2, "data": {"text": "EGTA and 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetra acetic acid tetrakis (BAPTA), two Ca2+ chelators, but not nifedipine, an L-type Ca2+ channel blocker, prevented GRIP1 degradation.", "entity1": "GRIP1", "entity2": "EGTA", "span1": [167, 172], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13609": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "VEGFR-2", "entity2": "Sorafenib", "span1": [142, 149], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3083": {"label": 3, "data": {"text": "This pretreament had no effect on the inhibition of GABA-T or the elevation of brain GABA levels produced by VIG.", "entity1": "GABA-T", "entity2": "VIG", "span1": [52, 58], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14114": {"label": 3, "data": {"text": "Overexpression of CRBN wild-type protein, but not CRBN(YW/AA) mutant protein, in KMS12 myeloma cells, amplified pomalidomide-mediated reductions in c-myc and IRF4 expression and increases in p21(WAF-1) expression.", "entity1": "c-myc", "entity2": "pomalidomide", "span1": [148, 153], "span2": [112, 124]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3886": {"label": 0, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "c-Myc", "entity2": "arginine", "span1": [53, 58], "span2": [233, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3381": {"label": 6, "data": {"text": "Benzodiazepines (BDZs) depress neuronal excitability via positive allosteric modulation of inhibitory GABA(A) receptors (GABA(A)R).", "entity1": "GABA(A)R", "entity2": "BDZs", "span1": [121, 129], "span2": [17, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"12794": {"label": 3, "data": {"text": "In a human whole blood assay, IC(50) values for lumiracoxib were 0.13 microM for COX-2 and 67 microM for COX-1 (COX-1/COX-2 selectivity ratio 515).", "entity1": "COX-1", "entity2": "lumiracoxib", "span1": [105, 110], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1382": {"label": 2, "data": {"text": "Since gemfibrozil is known to activate peroxisome proliferator-activated receptor-alpha (PPAR-alpha), we investigated the role of PPAR-alpha in gemfibrozil-mediated inhibition of iNOS.", "entity1": "PPAR-alpha", "entity2": "gemfibrozil", "span1": [89, 99], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2814": {"label": 3, "data": {"text": "DXM and 1400W attenuated the mRNA expression of E-selectin and iNOS induced by the costimulation of reIL-4, reTNF-alpha, and LPS.", "entity1": "E-selectin", "entity2": "DXM", "span1": [48, 58], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10147": {"label": 8, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "cyclooxygenase", "entity2": "arachidonic acid", "span1": [77, 91], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9522": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "ligand-activated gene transcription factors", "entity2": "adapalene", "span1": [53, 96], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4384": {"label": 1, "data": {"text": "Camptothecin (CPT), a topoisomerase (Top) I-targeting drug that stabilizes Top1-DNA covalent adducts, can induce S-phase-specific cytotoxicity due to the arrest of progressing replication forks.", "entity1": "topoisomerase (Top) I", "entity2": "Camptothecin", "span1": [22, 43], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9472": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "TP", "entity2": "S-145", "span1": [248, 250], "span2": [218, 223]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4209": {"label": 2, "data": {"text": "Moreover, GCs have a synergistic effect on GW4064-induced FXR activation, whereas chenodeoxycholate and GW4064 have an additive effect.", "entity1": "FXR", "entity2": "GW4064", "span1": [58, 61], "span2": [43, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7581": {"label": 3, "data": {"text": "threo-methylphenidate inhibits the dopamine transporter and the norepinephrine transporter, resulting in elevations of these monoamines after impulse release.", "entity1": "norepinephrine transporter", "entity2": "threo-methylphenidate", "span1": [64, 90], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15164": {"label": 2, "data": {"text": "Taken together, these data indicate that a PKA-mediated signaling pathway mediates GnRH activation of CREB at low-pulse frequencies, playing a significant role in the decoding of the hypothalamic GnRH signal to result in frequency-dependent FSH\u03b2 activation.", "entity1": "CREB", "entity2": "GnRH", "span1": [102, 106], "span2": [83, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11010": {"label": 1, "data": {"text": "Cyproheptadine is a piperidine antihistamine that increases appetite through its antiserotonergic effect on 5-HT2 receptors in the brain.", "entity1": "5-HT2", "entity2": "piperidine", "span1": [108, 113], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15482": {"label": 1, "data": {"text": "The model accurately predicted CYP19A mRNA fold changes for controls and three FAD doses (0, 0.5, and 3 \u00b5g/l) and plasma E2 dose response from the 4-day study.", "entity1": "CYP19A", "entity2": "FAD", "span1": [31, 37], "span2": [79, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5041": {"label": 3, "data": {"text": "New classes of pyrrole-derived nitrooxyalkyl inverse esters, carbonates, and ethers (7-10) as COX-2 selective inhibitors and NO donors were synthesized and are herein reported.", "entity1": "COX-2", "entity2": "esters", "span1": [94, 99], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2791": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "PPT-A", "entity2": "NaHS", "span1": [248, 253], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9480": {"label": 1, "data": {"text": "The structures of TK complexed with ADP at the ATP-site and deoxythymidine-5'-monophosphate (dTMP), deoxythymidine (dT), or idoxuridine-5'-phosphate (5-iodo-dUMP) at the substrate-site were refined to 2.75 A, 2.8 A, and 3.0 A resolution, respectively.", "entity1": "TK", "entity2": "ADP", "span1": [18, 20], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8841": {"label": 1, "data": {"text": "CONCLUSION: We provided documentation of neuroprotective effect of a natural flavone, calycopterin, against H2O2-induced oxidative stress in differentiated PC12 cells by modulating the level of CREB phosphorylation and Nrf2 pathway.", "entity1": "Nrf2", "entity2": "H2O2", "span1": [219, 223], "span2": [108, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2139": {"label": 1, "data": {"text": "Although incubating HASMCs for 48h with thiazolidinediones had no effect on ENT1 mRNA and protein levels, troglitazone acutely inhibited [3H]adenosine uptake and [3H]NBMPR binding of HASMCs with IC50 values of 2.35+/-0.35 and 3.99+/-0.57microM, respectively.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [76, 80], "span2": [106, 118]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10487": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "alprenolol", "span1": [392, 423], "span2": [243, 253]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13457": {"label": 2, "data": {"text": "We demonstrate that only treatment of HaCaT with GLA and EPA or a PPARgamma ligand (roziglitazone), induced COX-2 expression (protein and mRNA).", "entity1": "COX-2", "entity2": "roziglitazone", "span1": [108, 113], "span2": [84, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15133": {"label": 8, "data": {"text": "BCRP appeared to play a more important role for absorption and intestinal and renal elimination of apixaban than P-gp in transporter-KO rats after oral and i.v.", "entity1": "BCRP", "entity2": "apixaban", "span1": [0, 4], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12676": {"label": 0, "data": {"text": "Moreover, certain basic residues of this site, particularly Arg(165) and Lys(169), play a key role in factor Va and/or prothrombin recognition by factor Xa in the prothrombinase complex.", "entity1": "factor Xa", "entity2": "Lys", "span1": [146, 155], "span2": [73, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13470": {"label": 8, "data": {"text": "Acetyl-coenzyme A carboxylase (ACC) enzymes exist as two isoforms, ACC1 and ACC2, which play critical roles in fatty acid biosynthesis and oxidation.", "entity1": "ACC", "entity2": "fatty acid", "span1": [31, 34], "span2": [111, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10258": {"label": 3, "data": {"text": "The ensuing radioactive outflow from these cultures was enhanced by desipramine and reserpine, but reduced (in the presence of desipramine) by the OCT3 inhibitors cyanine 863, oestradiol and corticosterone.", "entity1": "OCT3", "entity2": "oestradiol", "span1": [147, 151], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2641": {"label": 8, "data": {"text": "Unlike mouse RetSat (mRetSat), zRetSat A had an altered bond specificity saturating either the 13-14 or 7-8 double bonds of all-trans-retinol to produce either all-trans-13,14-dihydroretinol or all-trans-7,8-dihydroretinol, respectively.", "entity1": "zRetSat A", "entity2": "all-trans-7,8-dihydroretinol", "span1": [31, 40], "span2": [194, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7950": {"label": 2, "data": {"text": "A reporter construct driven by 4 kb of the chicken ras-dva 5'-flanking region, containing six putative pituitary-specific transcription factor-1 (Pit-1) binding sites and two potential glucocorticoid receptor (GR) binding sites, was highly activated in embryonic pituitary cells and up-regulated by corticosterone.", "entity1": "chicken ras-dva", "entity2": "corticosterone", "span1": [43, 58], "span2": [299, 313]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8953": {"label": 3, "data": {"text": "The affinity labeling nucleotide analog, 5'-[p-(fluorosulfonyl)benzoyl]adenosine (FSA), inactivates the dehydrogenase and isomerase activities at similar rates in an irreversible manner which follows first order kinetics with respect to both time and alkylator concentration (0.2-0.6 mM).", "entity1": "dehydrogenase", "entity2": "FSA", "span1": [104, 117], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2407": {"label": 1, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "arginases", "entity2": "Nor-NOHA", "span1": [203, 212], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11974": {"label": 1, "data": {"text": "Furanodiene Presents Synergistic Anti-proliferative Activity With Paclitaxel Via Altering Cell Cycle and Integrin Signaling in 95-D Lung Cancer Cells.", "entity1": "Integrin", "entity2": "Furanodiene", "span1": [105, 113], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12491": {"label": 8, "data": {"text": "Cynomolgus FMO6 metabolized benzydamine only slightly, but minimal expression of FMO6 in all tissue precludes the importance of FMO6 in drug metabolism, unlike cynomolgus FMO1, FMO2, FMO3, and FMO5 which were all functional.", "entity1": "FMO3", "entity2": "benzydamine", "span1": [183, 187], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9233": {"label": 8, "data": {"text": "The holo activity of combined peroxisomal and mitochondrial AGT 1 with a low Km for L-alanine rapidly decreased after a lag time of about 2 days during feeding of the vitamin B6-deficient diet (by 50% in 5 days, by 86% in 14 days).", "entity1": "AGT 1", "entity2": "L-alanine", "span1": [60, 65], "span2": [84, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4702": {"label": 2, "data": {"text": "Furthermore, V(5+) significantly inhibited the TCDD-induced AhR-dependent luciferase activity.", "entity1": "AhR", "entity2": "TCDD", "span1": [60, 63], "span2": [47, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4347": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "Akt", "entity2": "pinosylvin", "span1": [112, 115], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6955": {"label": 1, "data": {"text": "To do this we cloned and expressed CCR5 from rhesus macaque and compared the binding properties of [125I]-MIP-1beta and [3H]-maraviroc with human recombinant CCR5.", "entity1": "human recombinant CCR5", "entity2": "[3H]-maraviroc", "span1": [140, 162], "span2": [120, 134]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4930": {"label": 2, "data": {"text": "EROD activity induction in peripheral blood lymphocytes, liver and brain tissues of rats orally exposed to polycyclic aromatic hydrocarbons.", "entity1": "EROD", "entity2": "polycyclic aromatic hydrocarbons", "span1": [0, 4], "span2": [107, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8309": {"label": 3, "data": {"text": "Cellular responses to DNA damage induced by etoposide or doxorubicin include down-regulation of endogenous supervillin coincident with increases in p53.", "entity1": "supervillin", "entity2": "doxorubicin", "span1": [107, 118], "span2": [57, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3040": {"label": 5, "data": {"text": "EP(1) and EP(3) receptor antagonists ONO-8713 and ONO-AE3-240, but not the EP(4) antagonists ONO-AE3-208 and AH 23848, inhibited tumor cell proliferation, indicating the significance of EP(1) and EP(3) but not EP(4) for MB growth.", "entity1": "EP(3) receptor", "entity2": "ONO-AE3-240", "span1": [10, 24], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"970": {"label": 3, "data": {"text": "Expression of the dominant negative mutants rab5A-N133I or rab7-N125I blunted U50,488H-induced down-regulation.", "entity1": "rab5A", "entity2": "U50,488H", "span1": [44, 49], "span2": [78, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4287": {"label": 1, "data": {"text": "Flavonoids such as green tea catechins and quercetin glycosides have been shown to modulate the function of some OATPs.", "entity1": "OATPs", "entity2": "Flavonoids", "span1": [113, 118], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13716": {"label": 5, "data": {"text": "Irbesartan (Aprovel, Avapro, Irbetan, Karvea), an angiotensin II receptor type 1 antagonist, is approved in many countries worldwide for the treatment of hypertension.", "entity1": "angiotensin II receptor type 1", "entity2": "Irbetan", "span1": [50, 80], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12497": {"label": 1, "data": {"text": "Involvement of p-CREB and phase II detoxifying enzyme system in neuroprotection mediated by the flavonoid calycopterin isolated from Dracocephalum kotschyi.", "entity1": "p-CREB", "entity2": "calycopterin", "span1": [15, 21], "span2": [106, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14391": {"label": 3, "data": {"text": "NFD suppressed EGF-mediated protein levels of c-Jun and c-Fos, and reduced MMP-9 expression and activity, concomitantly with a marked inhibition on cell migration and invasion without obvious cellular cytotoxicity.", "entity1": "MMP-9", "entity2": "NFD", "span1": [75, 80], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2672": {"label": 3, "data": {"text": "However, a lower concentration of dipyridamole (3 microM) that blocks PDE9, PDE10, and PDE11, but not PDE8, did not inhibit ecto-phosphodiesterase activity.", "entity1": "PDE10", "entity2": "dipyridamole", "span1": [76, 81], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15358": {"label": 8, "data": {"text": "CONCLUSION: Our findings demonstrate that (R)-omeprazole HI correlated better with CYP2C19 genotype groups than racemic-omeprazole HI, and these results may be useful for classification among patients in CYP2C19 genotype groups prior to omeprazole treatment.", "entity1": "CYP2C19", "entity2": "racemic-omeprazole", "span1": [83, 90], "span2": [112, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3800": {"label": 2, "data": {"text": "An increase in the ADP/ATP ratio opens K(ATP) channels, leading to membrane hyperpolarization.", "entity1": "K(ATP) channels", "entity2": "ADP", "span1": [39, 54], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1008": {"label": 5, "data": {"text": "METHODS: Part A compared the effects of placebo to four doses of a 5-HT(4) receptor antagonist (SB-207266) on the cisapride mediated increase in plasma aldosterone (a 5-HT(4) mediated response) and orocaecal transit in 18 subjects.", "entity1": "5-HT(4)", "entity2": "SB-207266", "span1": [67, 74], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6374": {"label": 5, "data": {"text": "The kappa(1)+kappa(3)-opioid receptor agonist/mu-opioid receptor antagonist naloxone benzoylhydrazone was a pure antagonist at both rat brain and human ORL1 receptors.", "entity1": "ORL1", "entity2": "naloxone benzoylhydrazone", "span1": [152, 156], "span2": [76, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11313": {"label": 1, "data": {"text": "Synthesis and in vitro pharmacology at AMPA and kainate preferring glutamate receptors of 4-heteroarylmethylidene glutamate analogues.", "entity1": "glutamate receptors", "entity2": "4-heteroarylmethylidene glutamate", "span1": [67, 86], "span2": [90, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6405": {"label": 3, "data": {"text": "In a physiological K(+) gradient, TWIK-2 is half inhibited by 0.1 mm Ba(2+), quinine, and quinidine.", "entity1": "TWIK-2", "entity2": "quinine", "span1": [34, 40], "span2": [77, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13551": {"label": 5, "data": {"text": "In this study we investigated the effects of combination chemotherapy with melarsoprol and a humanised SP receptor antagonist aprepitant (EMEND) in this mouse model.", "entity1": "humanised SP receptor", "entity2": "aprepitant", "span1": [93, 114], "span2": [126, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6789": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-1", "entity2": "etodolac", "span1": [268, 273], "span2": [192, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14276": {"label": 8, "data": {"text": "We recently showed that TETA is metabolized in vitro by polyamine catabolic enzyme spermidine/spermine-N(1)-acetyltransferase (SSAT1) and by thialysine acetyltransferase (SSAT2) to its monoacetylated derivative (MAT).", "entity1": "SSAT1", "entity2": "polyamine", "span1": [127, 132], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4503": {"label": 3, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES1", "entity2": "clopidogrel-\u03b2-d-glucuronide", "span1": [169, 174], "span2": [28, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4973": {"label": 3, "data": {"text": "Coupling this computational technique with a high-quality low-throughput screen identified 5-(4-piperidyl)-3-isoxazolol (4-PIOL) as a potent plasminogen binding inhibitor with the potential for the treatment of various bleeding disorders.", "entity1": "plasminogen", "entity2": "4-PIOL", "span1": [141, 152], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"48": {"label": 3, "data": {"text": "Comparison of the monoamine oxidase inhibiting properties of two reversible and selective monoamine oxidase-A inhibitors moclobemide and toloxatone, and assessment of their effect on psychometric performance in healthy subjects.", "entity1": "monoamine oxidase", "entity2": "moclobemide", "span1": [18, 35], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"755": {"label": 5, "data": {"text": "A series of 2-carbonyl analogues of the muscarinic antagonist diphenidol bearing 1-substituents of different lipophilic, electronic, and steric properties was synthesized and their affinity for the M2 and M3 muscarinic receptor subtypes was evaluated by functional tests.", "entity1": "M2 and M3 muscarinic receptor", "entity2": "diphenidol", "span1": [198, 227], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"711": {"label": 1, "data": {"text": "In the present study, the ability of different concentrations of torasemide to modify angiotensin II (Ang II)-induced vascular responses was examined, with the use of an organ bath system, in endothelium-denuded aortic rings from spontaneously hypertensive rats.", "entity1": "Ang II", "entity2": "torasemide", "span1": [102, 108], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15417": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-10", "entity2": "cholesterol", "span1": [77, 82], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"3747": {"label": 3, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "Cx43", "entity2": "2,3,7,8-tetrachlorodibenzo-p-dioxin", "span1": [189, 193], "span2": [73, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5235": {"label": 2, "data": {"text": "In a cell-based model, bleomycin suppressed Nrf2 activation via extracellular signal-related kinase phosphorylation, enhancing intracellular reactive oxygen species in lung fibroblasts and stimulating abnormal cell proliferation and collagen secretion.", "entity1": "extracellular signal-related kinase", "entity2": "bleomycin", "span1": [64, 99], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5206": {"label": 0, "data": {"text": "We analysed the role of the MBD in MeCP2-chromatin associations in vivo using an MeCP2 mutant Rett syndrome mouse model (Mecp2(tm)(1)(. )(1)(Jae)) in which exon 3 deletion results in an N-terminal truncation of the protein, including most of the MBD.", "entity1": "Mecp2", "entity2": "N", "span1": [121, 126], "span2": [186, 187]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5068": {"label": 5, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "estrogen receptor \u03b1", "entity2": "ICI 82,780", "span1": [126, 145], "span2": [157, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7346": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "sodium-coupled neutral amino acid transporter 1", "entity2": "alanine", "span1": [274, 321], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7704": {"label": 2, "data": {"text": "atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans.", "entity1": "AChE", "entity2": "atropine", "span1": [10, 14], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14094": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "thalidomide", "span1": [121, 125], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13737": {"label": 8, "data": {"text": "Homocysteine, the atherogenic product of the NNMT-catalyzed reaction, was secreted from 3T3-L1 cells or adipose tissue cultures.", "entity1": "NNMT", "entity2": "Homocysteine", "span1": [45, 49], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"14458": {"label": 9, "data": {"text": "Moreover, mutation of ECII can alter this coupled equilibrium from GTP-insensitive agonist binding to more conventional GTP-sensitive binding.", "entity1": "ECII", "entity2": "GTP", "span1": [22, 26], "span2": [120, 123]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13370": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "small proline-rich protein-2A", "entity2": "estrogen", "span1": [144, 173], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11211": {"label": 3, "data": {"text": "We conclude that erg3 can be blocked by certain antipsychotic drugs like sertindole and pimozide.", "entity1": "erg3", "entity2": "pimozide", "span1": [17, 21], "span2": [88, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13098": {"label": 4, "data": {"text": "Among the measured compounds, gliquidone and glipizide (two sulfonylureas), as well as nateglinide (a glinide), exhibit PPARgamma agonistic activity at concentrations comparable with those reached under pharmacological treatment.", "entity1": "PPARgamma", "entity2": "nateglinide", "span1": [120, 129], "span2": [87, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16038": {"label": 3, "data": {"text": "These compounds resulted from our efforts to merge the pharmacophores of selective factor Xa inhibitor rivaroxaban with a mimic of the Arg-Gly-Asp (RGD) sequence of fibrinogen to obtain designed multiple ligands with potential antithrombotic activity.", "entity1": "factor Xa", "entity2": "rivaroxaban", "span1": [83, 92], "span2": [103, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6756": {"label": 2, "data": {"text": "Thus, hydralazine activates the HIF pathway through inhibition of PHD activity and initiates a pro-angiogenic phenotype.", "entity1": "HIF", "entity2": "hydralazine", "span1": [32, 35], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10971": {"label": 3, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "RAR-alpha", "entity2": "retinoid", "span1": [16, 25], "span2": [154, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4552": {"label": 1, "data": {"text": "The present study was designed to test the hypothesis that alcohol alters global DNA methylation, and modulates expression of the DNA methyltransferases (DNMTs) and various methyl CpG-binding proteins.", "entity1": "DNMTs", "entity2": "alcohol", "span1": [154, 159], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14647": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala70Thr", "entity2": "cytarabine", "span1": [52, 60], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7478": {"label": 2, "data": {"text": "Additionally, Na+ and Cl- ions coactivate GluR6 receptors by establishing a dipole, accounting for their common effect on KARs.", "entity1": "GluR6", "entity2": "Na+", "span1": [42, 47], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14721": {"label": 1, "data": {"text": "We demonstrate that the PHD1-PHD2 region is essential for viability and that the first PHD finger contributes to the preferred binding of PHD1-PHD2 to lysine 4-methylated histone H3 tails.", "entity1": "PHD1-PHD2", "entity2": "lysine", "span1": [138, 147], "span2": [151, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5296": {"label": 0, "data": {"text": "These results support the hypothesis that apoplastic amino acids acting through heteromeric GLR3.2/GLR3.4 channels affect lateral root development via Ca(2+) signaling in the phloem.", "entity1": "GLR3.2", "entity2": "amino acids", "span1": [92, 98], "span2": [53, 64]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14216": {"label": 6, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "eseroline", "span1": [193, 198], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15708": {"label": 3, "data": {"text": "Xanthohumol and 2-hydroxychalcone induced apoptosis by Bcl-2 downregulation.", "entity1": "Bcl-2", "entity2": "Xanthohumol", "span1": [55, 60], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1097": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "neostigmine", "span1": [242, 262], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9975": {"label": 1, "data": {"text": "For lung tumor lines (carcinoid, two SCLC, and one large cell lung carcinoma), AAAD activity was correlated with the potency of carbidopa-induced cytotoxicity.", "entity1": "AAAD", "entity2": "carbidopa", "span1": [79, 83], "span2": [128, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7113": {"label": 4, "data": {"text": "Tamoxifen blocks the action of estrogen by binding to the ER, and possesses both ER-agonist and antagonist properties.", "entity1": "ER", "entity2": "Tamoxifen", "span1": [81, 83], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6074": {"label": 0, "data": {"text": "Within the conserved transmembrane domains, the sequences exhibit approximately 52%, 59%, 65%, and 68% amino acid identity with the known rat 5-HT1A, rat 5-HT1B, rat 5-HT1D, and human 5-HT1E receptors, respectively.", "entity1": "rat 5-HT1B", "entity2": "amino acid", "span1": [150, 160], "span2": [103, 113]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9738": {"label": 1, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "h5-HT(1D)", "entity2": "(35)S", "span1": [104, 113], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9587": {"label": 3, "data": {"text": "All three compounds displayed antagonistic properties against oxytocin in vitro, with carbetocin being the strongest inhibitor (pA2 = 8.21) and carbetocin metabolite II (pA2 = 8.01) being stronger than carbetocin metabolite I (pA2 = 7.81).", "entity1": "oxytocin", "entity2": "carbetocin", "span1": [62, 70], "span2": [202, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14648": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "DCK", "entity2": "cytarabine", "span1": [66, 69], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7572": {"label": 2, "data": {"text": "Administration of cevimeline hydrochloride, an M3 muscarinic receptor agonist (10 mg/kg for 7 days po), but not pilocarpine (0.3 mg/kg for 7 days po), recovered the AQP5 protein level reduced by CTD and increased the AQP1 protein level above the control one.", "entity1": "AQP1", "entity2": "cevimeline hydrochloride", "span1": [217, 221], "span2": [18, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11057": {"label": 9, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "glycerophosphoserine", "span1": [236, 242], "span2": [120, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"10928": {"label": 3, "data": {"text": "Using [(3)H]glucosamine-labeled gastric mucosal cells, we show that stimulatory effect of beta-adrenergic agonist, isoproterenol, on mucin secretion was inhibited by EGFR kinase inhibitor, PD153035, as well as wortmannin, a specific inhibitor of PI3K.", "entity1": "PI3K", "entity2": "wortmannin", "span1": [246, 250], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10962": {"label": 9, "data": {"text": "Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors.", "entity1": "nicotinic receptors", "entity2": "galantamine", "span1": [130, 149], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8699": {"label": 3, "data": {"text": "Detailed structure-activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione inhibitors of HIV capsid (CA) assembly are described.", "entity1": "HIV capsid", "entity2": "1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione", "span1": [192, 202], "span2": [134, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3916": {"label": 3, "data": {"text": "(-)-6-(7-Methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one (KCA-1490) exhibits moderate dual PDE3/4-inhibitory activity and promises as a combined bronchodilatory/anti-inflammatory agent.", "entity1": "PDE3/4", "entity2": "KCA-1490", "span1": [139, 145], "span2": [106, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8765": {"label": 3, "data": {"text": "SB225002 (SB) is an IL-8 receptor B (IL-8RB) antagonist that has previously been shown to inhibit IL-8-based cancer cell invasion, and to possess in vivo anti-inflammatory and anti-nociceptive effects.", "entity1": "IL-8", "entity2": "SB225002", "span1": [98, 102], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9883": {"label": 5, "data": {"text": "We examined the effect of JTH-601 (3- inverted question markN-[2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethyl]-N-methylaminom ethyl inverted question mark-4-methoxy-2,5,6-trimethylphenol hemifumarate), a new alpha(1L)-adrenoceptor antagonist, on prostatic function in isolated canine prostate and in anesthetized dogs.", "entity1": "alpha(1L)-adrenoceptor", "entity2": "JTH-601", "span1": [208, 230], "span2": [26, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8224": {"label": 1, "data": {"text": "Mutations introduced into EAG to replicate the ICA binding site in ERG did not alter the functional response to ICA.", "entity1": "ERG", "entity2": "ICA", "span1": [67, 70], "span2": [47, 50]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14963": {"label": 1, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANKL", "entity2": "cysteine", "span1": [163, 168], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5240": {"label": 9, "data": {"text": "Fluoride treatment also increased phosphorylation of JNK and ERK, but not p38, and apoptosis induced by fluoride was notably or partly suppressed by treatment with JNK or ERK inhibitors, respectively.", "entity1": "p38", "entity2": "Fluoride", "span1": [74, 77], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1923": {"label": 8, "data": {"text": "In the reverse case, mutation of the orthologous glycine (Gly553) to methionine in carnitine octanoyltransferase (COT) decreased activity toward its natural substrates, medium- and long-chain acyl-CoAs, and increased activity toward short-chain acyl-CoAs.", "entity1": "carnitine octanoyltransferase", "entity2": "acyl-CoAs", "span1": [83, 112], "span2": [192, 201]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14842": {"label": 3, "data": {"text": "As the Mg(2+) ion concentration was increased, there was a consistent decrease of the enzyme catalytic turnover from 0.31 s(-1) (0 \u03bcM Mg(2+)) to 0.050 s(-1) (6000 \u03bcM Mg(2+)) and a distinct shift in steady-state conformational population from one that favors the ALDH1-NADH complex with the shorter fluorescence lifetime (33% excess) in the absence of magnesium ion to one that favors the ALDH1-NADH complex with the longer fluorescence lifetime (13% excess) at 6000 \u03bcM Mg(2+).", "entity1": "ALDH1", "entity2": "Mg(2+)", "span1": [262, 267], "span2": [7, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1943": {"label": 9, "data": {"text": "Several purinergic receptors have been described on platelets; P2X (1), a calcium channel, and P2Y1 a Gq-coupled seven-transmembrane domain receptor, have been found not to be antagonized by clopidogrel.", "entity1": "purinergic receptors", "entity2": "clopidogrel", "span1": [8, 28], "span2": [191, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4811": {"label": 3, "data": {"text": "Structure-activity relationship studies indicated that 5-(p-toluenesulfonylamino)phthalimide moiety is a favorable scaffold to exert the \u03b1-glucosidase inhibitory activity and substituents at the N2 position have considerable influence on the efficacy of the inhibition activities.", "entity1": "\u03b1-glucosidase", "entity2": "5-(p-toluenesulfonylamino)phthalimide", "span1": [137, 150], "span2": [55, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11482": {"label": 1, "data": {"text": "CONCLUSIONS: Ketorolac is relatively COX-1 selective while bromfenac is potently selective for COX-2 over COX-1.", "entity1": "COX-1", "entity2": "Ketorolac", "span1": [37, 42], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5370": {"label": 3, "data": {"text": "Suppression of T\u03b2R1 by the pharmacological inhibitor (SB431542) markedly reduced VEGF release by HFL-1 in response to CSE and this effect was confirmed by T\u03b2R1 siRNA.", "entity1": "VEGF", "entity2": "SB431542", "span1": [81, 85], "span2": [54, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3266": {"label": 8, "data": {"text": "TAS-102 is a novel drug containing trifluorothymidine, which is phosphorylated by TK-1 to its active monophosphated form, that in turn can inhibit TS.", "entity1": "TK-1", "entity2": "trifluorothymidine", "span1": [82, 86], "span2": [35, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14268": {"label": 8, "data": {"text": "Metabolism of triethylenetetramine and 1,12-diamino-3,6,9-triazadodecane by the spermidine/spermine-N(1)-acetyltransferase and thialysine acetyltransferase.", "entity1": "spermidine/spermine-N(1)-acetyltransferase", "entity2": "1,12-diamino-3,6,9-triazadodecane", "span1": [80, 122], "span2": [39, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8650": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRA", "entity2": "ethanol", "span1": [20, 23], "span2": [61, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5323": {"label": 3, "data": {"text": "The structure-activity relationships revealed that the free hydroxyl group at position 5 and phosphate group at position 7 of the phosphorylated flavonoids are favorable to the inhibition of CEase.", "entity1": "CEase", "entity2": "phosphorylated flavonoids", "span1": [191, 196], "span2": [130, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7182": {"label": 1, "data": {"text": "Administration of m-chlorophenylpiperazine and fenfluramine, both of which induce anorexic effects via 5-HT2C receptors and/or 5-HT1B receptors, suppressed food intake in 5- and 8-wk-old Ay mice, whereas the anorexic effects were attenuated in food-restricted Ay mice.", "entity1": "5-HT2C", "entity2": "fenfluramine", "span1": [103, 109], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6637": {"label": 5, "data": {"text": "alpha(1A)-Adrenoceptor selective antagonists, 2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane (WB-4101; 0.1-1 mg/kg) and 5-methylurapidil (0.1-1 mg/kg), the alpha(1B)-adrenoceptor selective antagonist, 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765314; 0.3-1 mg/kg), as well as the alpha(1D)-adrenoceptor selective antagonist, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY-7378; 1 mg/kg), were used to delineate the adrenoceptor subtypes involved.", "entity1": "alpha(1A)-Adrenoceptor", "entity2": "WB-4101", "span1": [0, 22], "span2": [107, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11689": {"label": 8, "data": {"text": "Stable ABCC1, ABCC2 and ABCC3 knockdown cell lines were generated, thus making it possible to demonstrate that ABCC1 mediates the basolateral and ABCC2 the apical excretion of BPDE glutathione conjugates.", "entity1": "ABCC1", "entity2": "BPDE glutathione", "span1": [111, 116], "span2": [176, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15167": {"label": 2, "data": {"text": "We hypothesized that CREB is activated by a distinct signaling pathway in response to pulsatile GnRH in a frequency-dependent manner to dictate the FSH\u03b2 transcriptional response.", "entity1": "CREB", "entity2": "GnRH", "span1": [21, 25], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12752": {"label": 2, "data": {"text": "The c-Jun absorbed light value/GAPDH absorbed light value of mesenteric arteries in the SHR group was 0.850+/-0.015, which was significantly higher than that in the WKY, imidapril, and irbesartan groups (0.582+/-0.013, 0.743+/-0.012, and 0.789+/-0.013, respectively, P<0.01), and was significantly lower in imidapril group than in irbesartan group (P<0.05).", "entity1": "c-Jun", "entity2": "irbesartan", "span1": [4, 9], "span2": [185, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10866": {"label": 4, "data": {"text": "The identification of 4-methylhistamine as a potent H(4)R agonist is of major importance for future studies to unravel the physiological roles of the H(4)R.", "entity1": "H(4)R", "entity2": "4-methylhistamine", "span1": [52, 57], "span2": [22, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4237": {"label": 1, "data": {"text": "Functional and biochemical studies indicated that TES signaling involved activity of the phosphoinositide 3 (PI3) kinase-protein kinase B (Akt) cascade initiated by activation of the androgen receptor and culminated in enhanced production of cGMP and microvascular vasodilation.", "entity1": "Akt", "entity2": "TES", "span1": [139, 142], "span2": [50, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7441": {"label": 5, "data": {"text": "(-)-Stepholidine (SPD), an active ingredient of the Chinese herb Stephania, is the first compound found to have dual function as a dopamine receptor D1 agonist and D2 antagonist.", "entity1": "D2", "entity2": "SPD", "span1": [164, 166], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8225": {"label": 1, "data": {"text": "Mutations introduced into EAG to replicate the ICA binding site in ERG did not alter the functional response to ICA.", "entity1": "EAG", "entity2": "ICA", "span1": [26, 29], "span2": [112, 115]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9073": {"label": 9, "data": {"text": "Some of these effects are known to be influenced by dietary levels of vitamin K. We therefore compared the toxic effects of 13-cis-retinoic acid (13cisRA), retinyl acetate (ROAc), and N-(4-hydroxyphenyl)retinamide (4HPR) in male Sprague-Dawley rats maintained on diets containing different levels of vitamin K. Animals were fed either an NIH-07 diet supplemented with menadione (3.1 ppm vitamin K3), an NIH-07 diet not supplemented with menadione, or an AIN-076 purified diet devoid of vitamin K. The retinoids had no effect on prothrombin times of animals fed the supplemented diet.", "entity1": "prothrombin", "entity2": "retinoids", "span1": [528, 539], "span2": [501, 510]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7857": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "KARs", "entity2": "BAPTA", "span1": [32, 36], "span2": [207, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12649": {"label": 1, "data": {"text": "It has no influence on the rate of association of (125)I-ET-1 to ETA receptors.", "entity1": "ET-1", "entity2": "(125)I", "span1": [57, 61], "span2": [50, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7964": {"label": 1, "data": {"text": "A domain in the carboxy-terminus of TSPO was identified and characterized as the cholesterol recognition/interaction amino acid consensus (CRAC).", "entity1": "TSPO", "entity2": "cholesterol", "span1": [36, 40], "span2": [81, 92]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14799": {"label": 3, "data": {"text": "In conclusion, this study provides the first evidence implicating that TSA inhibits TGF-\u03b2-induced ROS accumulation and myofibroblast differentiation via enhanced Nrf2-ARE signaling.", "entity1": "TGF-\u03b2", "entity2": "TSA", "span1": [84, 89], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13304": {"label": 3, "data": {"text": "RESULTS: We show that sorafenib is a potent inhibitor of ETV6-PDGFRbeta and FLT3 mutants, including some of the mutants that confer resistance to PKC412 and other FLT3 inhibitors.", "entity1": "ETV6", "entity2": "sorafenib", "span1": [57, 61], "span2": [22, 31]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7228": {"label": 1, "data": {"text": "We then demonstrated that GnRH can also stimulate androgen receptor mobilization in human prostate PC3, BPH-1 and LNCaP cells, and in cultured rat ventral prostate cells through the same mechanism.", "entity1": "androgen receptor", "entity2": "GnRH", "span1": [50, 67], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11393": {"label": 3, "data": {"text": "Using whole-cell voltage clamp, we examined mibefradil block of four Na+ channel isoforms expressed in human embryonic kidney cells: Nav1.5 (cardiac), Nav1.4 (skeletal muscle), Nav1.2 (brain), and Nav1.7 (peripheral nerve).", "entity1": "Na+ channel", "entity2": "mibefradil", "span1": [69, 80], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12626": {"label": 1, "data": {"text": "The EP1 receptor bound 17-phenyl-PGE2, sulprostone and iloprost in addition to PGE2 and PGE1, with Ki values of 14-36 nM.", "entity1": "EP1", "entity2": "PGE2", "span1": [4, 7], "span2": [79, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1766": {"label": 1, "data": {"text": "Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology.", "entity1": "beta 1-adrenoceptors", "entity2": "CGP 12177A", "span1": [18, 38], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8849": {"label": 3, "data": {"text": "Herein, we investigated the effect of a natural neuroprotective flavonoid, calycopterin, on H2O2-induced disruption of phase II detoxifying enzyme system and cAMP response element binding protein (CREB) phosphorylation.", "entity1": "CREB", "entity2": "H2O2", "span1": [197, 201], "span2": [92, 96]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11535": {"label": 1, "data": {"text": "The effects of adulthood olanzapine treatment on cognitive performance and neurotrophic factor content in male and female rats neonatally treated with quinpirole.", "entity1": "neurotrophic factor", "entity2": "quinpirole", "span1": [75, 94], "span2": [151, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11813": {"label": 8, "data": {"text": "The mouse CYP2J subfamily includes members that have wide tissue distribution and are active in the metabolism of arachidonic acid (AA), linoleic acid (LA), and other lipids and xenobiotics.", "entity1": "CYP2J", "entity2": "arachidonic acid", "span1": [10, 15], "span2": [114, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4673": {"label": 3, "data": {"text": "This is described in a case study of the expedited review and approval of peramivir, a novel neuraminidase inhibitor, in Japan in the context of the emergence of new strain of influenza in 2009.", "entity1": "neuraminidase", "entity2": "peramivir", "span1": [93, 106], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5141": {"label": 1, "data": {"text": "An intermediate GTX2,3-aldehyde was first synthesized by activating the NH2 group of the 2nd and 8th amino acid residues with three different aldehydes and two artificial complete antigens GTX2,3-aldehyde-bovine serum albumin (BSA) and GTX2,3-aldehyde- keyhole limpet hemocyanin (KLH) were then prepared by cross-linking the intermediate with BSA or KLH.", "entity1": "BSA", "entity2": "GTX2,3-aldehyde", "span1": [227, 230], "span2": [189, 204]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15715": {"label": 3, "data": {"text": "We identified a series of 4-hydroxypyridazin-3(2H)-one derivatives as novel DAAO inhibitors with high potency and substantial cell permeability using fragment-based drug design.", "entity1": "DAAO", "entity2": "4-hydroxypyridazin-3(2H)-one", "span1": [76, 80], "span2": [26, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7319": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT1", "entity2": "amino acids", "span1": [235, 240], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"201": {"label": 1, "data": {"text": "WB 4101, benoxathian and phentolamine displayed high affinity for alpha 1A and alpha 1D adrenoceptors compared to the alpha 1B subtype.", "entity1": "alpha 1A and alpha 1D adrenoceptors", "entity2": "phentolamine", "span1": [66, 101], "span2": [25, 37]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10997": {"label": 8, "data": {"text": "The functional characteristics of rabbit PAT1 in either mammalian cells or renal BBMV suggest that PAT1 is the low-affinity transporter of proline, glycine and hydroxyproline believed to be defective in patients with iminoglycinuria.", "entity1": "PAT1", "entity2": "proline", "span1": [99, 103], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11836": {"label": 1, "data": {"text": "We investigated the association of HSD11B2 variant with glucose homeostasis.", "entity1": "HSD11B2", "entity2": "glucose", "span1": [35, 42], "span2": [56, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2654": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "BRL-50481", "span1": [397, 414], "span2": [306, 315]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4734": {"label": 1, "data": {"text": "Furthermore, sinapic acid reduced hepatic hydroxyproline content, which correlated with a reduction in the expression of type I collagen mRNA and histological analysis of collagen in liver tissue.", "entity1": "collagen", "entity2": "sinapic acid", "span1": [171, 179], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10313": {"label": 1, "data": {"text": "These results demonstrate that imidazoquinoline molecules directly induce pDC maturation as determined by cytokine induction, CCR7 and co-stimulatory marker expression and prolonging viability.", "entity1": "CCR7", "entity2": "imidazoquinoline", "span1": [126, 130], "span2": [31, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12717": {"label": 1, "data": {"text": "Initial studies showed that yohimbine was about 4- and 15-fold more selective for the human alpha2C-adrenoceptor in comparison with the alpha2A- and alpha2B-adrenoceptors, respectively.", "entity1": "human alpha2C-adrenoceptor", "entity2": "yohimbine", "span1": [86, 112], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8483": {"label": 1, "data": {"text": "Because data concerning their toxicological properties are scarce, the cytotoxic, genotoxic, immunomodulatory, and hormonal activities of four naphthoylindole compounds (JWH-018, JWH-073, JWH-122 and JWH-210) and of one benzoylindole (AM-694) were studied in human cell lines and primary cells; tetrahydrocannabinol was included as the classical non-endogenous cannabinoid receptor ligand.", "entity1": "cannabinoid receptor", "entity2": "tetrahydrocannabinol", "span1": [361, 381], "span2": [295, 315]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15684": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Cdk1", "entity2": "VB1", "span1": [216, 220], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6842": {"label": 1, "data": {"text": "Differences in cobalamin and folate levels with the MTRR A66G and MS A2756G polymorphisms were noted.", "entity1": "MS", "entity2": "cobalamin", "span1": [66, 68], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5428": {"label": 8, "data": {"text": "Cholesterol esterase (CE) induced surface erosion of poly(ethylene carbonate) (PEC) and drug release from PEC under mild physiological environment was investigated.", "entity1": "CE", "entity2": "PEC", "span1": [22, 24], "span2": [79, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15053": {"label": 8, "data": {"text": "The recent identification of zinc permeability of the lysosomal ion channel TRPML1 (transient receptor potential mucolipin 1), and the evidence of abnormal zinc levels in cells deficient in TRPML1, suggested a role for TRPML1\u00a0in zinc transport.", "entity1": "transient receptor potential mucolipin 1", "entity2": "zinc", "span1": [84, 124], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10451": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "EC 4.3.1.17", "entity2": "pyruvate", "span1": [27, 38], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2852": {"label": 2, "data": {"text": "cAspAT activity, as well as the incorporation of [(14)C]aspartate into the neutral lipid fraction of 3T3-F442A adipocytes was stimulated by the thiazolidinedione (TZD) rosiglitazone.", "entity1": "cAspAT", "entity2": "rosiglitazone", "span1": [0, 6], "span2": [168, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4490": {"label": 2, "data": {"text": "The hemoglobin A1c (HbA1c) of all patients improved significantly from 8.1\u00b11.2% to 7.6\u00b11.1% after 12 weeks of add-on therapy with sitagliptin (p<0.01), and the insulin dosage was reduced from 27.3\u00b115.8 U/day to 24.5\u00b116.5 U/day (p<0.001).", "entity1": "hemoglobin A1c", "entity2": "sitagliptin", "span1": [4, 18], "span2": [130, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4383": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "MDZ", "span1": [280, 285], "span2": [242, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9249": {"label": 1, "data": {"text": "Our results indicate that ergot compounds, especially ergovaline, bind to D2 dopamine receptors and elicit second messenger responses similar to that of dopamine.", "entity1": "D2 dopamine receptors", "entity2": "ergovaline", "span1": [74, 95], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9512": {"label": 5, "data": {"text": "In conclusion, these findings indicate that [3H]SR 142948A is a new potent antagonist radioligand which recognizes with high affinity both neurotensin NT1 and NT2 receptors and represents thus an excellent tool to study neurotensin receptors in the rat brain.", "entity1": "NT2 receptors", "entity2": "[3H]SR 142948A", "span1": [159, 172], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14846": {"label": 8, "data": {"text": "Aldehyde dehydrogenase 1 (ALDH1A1) catalyzes the oxidation of toxic aldehydes to carboxylic acids.", "entity1": "Aldehyde dehydrogenase 1", "entity2": "aldehydes", "span1": [0, 24], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8380": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "lactate dehydrogenase", "entity2": "Cd", "span1": [125, 146], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11278": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "SHMT", "entity2": "glycine", "span1": [166, 170], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"601": {"label": 3, "data": {"text": "Cyclopentenone prostaglandins suppress activation of microglia: down-regulation of inducible nitric-oxide synthase by 15-deoxy-Delta12,14-prostaglandin J2.", "entity1": "inducible nitric-oxide synthase", "entity2": "Cyclopentenone prostaglandins", "span1": [83, 114], "span2": [0, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8505": {"label": 1, "data": {"text": "Structural Basis for the ATP-Induced Isomerization of Kinesin.", "entity1": "Kinesin", "entity2": "ATP", "span1": [54, 61], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5580": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "fluoropyrimidine carbamate", "span1": [96, 119], "span2": [13, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15223": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "cyclooxygenase-2", "entity2": "CLS", "span1": [270, 286], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12839": {"label": 8, "data": {"text": "When expressed heterologously in a mammalian cell line, rabbit PAT1 mediates pH-dependent, Na(+)-independent uptake of proline, glycine, l-alanine and alpha-(methylamino)isobutyric acid.", "entity1": "rabbit PAT1", "entity2": "glycine", "span1": [56, 67], "span2": [128, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12162": {"label": 1, "data": {"text": "Collagen prolyl hydroxylase is a known target of hydralazine.", "entity1": "Collagen prolyl hydroxylase", "entity2": "hydralazine", "span1": [0, 27], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1072": {"label": 1, "data": {"text": "However, fasciculin-2, a potent peptide inhibitor of acetylcholinesterase (IC50 24 nM), did prevent catabolism of acetylcholine in rat brain membranes with an atypical inhibition isotherm of [3H]-oxotremorine-M binding, thus permitting an estimation of the \"global affinity\" of acetylcholine (Ki 85 nM) for [3H]-oxotremorine-M-labelled muscarinic receptors in rat brain.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [336, 356], "span2": [191, 210]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16024": {"label": 1, "data": {"text": "These results show that haloperidol promotes mTORC1- and S6K1-dependent phosphorylation of rpS6 at Ser240/244, in a subpopulation of striatal MSNs expressing D2Rs.", "entity1": "S6K1", "entity2": "haloperidol", "span1": [57, 61], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7742": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "VEGFR2", "entity2": "XL184", "span1": [107, 113], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11205": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel.", "entity1": "erg3", "entity2": "sertindole", "span1": [54, 58], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11956": {"label": 8, "data": {"text": "UGT1A6 exhibited a significantly higher Vmax and Km values toward both HFC and UDP-glucuronic acid than the other UGTs.", "entity1": "UGT1A6", "entity2": "glucuronic acid", "span1": [0, 6], "span2": [83, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"53": {"label": 3, "data": {"text": "Clinical pharmacology of enalkiren, a novel, dipeptide renin inhibitor.", "entity1": "renin", "entity2": "enalkiren", "span1": [55, 60], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7908": {"label": 2, "data": {"text": "We found that helenalin markedly induced endoplasmic reticulum (ER) stress-related genes, such as regulated in development and DNA damage responses (REDD) 1, activating transcription factor-4 (ATF4) and/or the CCAAT enhancer-binding protein-homologous protein (CHOP).", "entity1": "regulated in development and DNA damage responses (REDD) 1", "entity2": "helenalin", "span1": [98, 156], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1623": {"label": 3, "data": {"text": "Aliskiren represents the first in a novel class of renin inhibitors with the potential for treatment of hypertension and related cardiovascular diseases.", "entity1": "renin", "entity2": "Aliskiren", "span1": [51, 56], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4630": {"label": 9, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "AhR", "entity2": "anthocyanidins", "span1": [56, 59], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8311": {"label": 2, "data": {"text": "Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).", "entity1": "pro-opiomelanocortin", "entity2": "acylethanolamide", "span1": [97, 117], "span2": [6, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12222": {"label": 1, "data": {"text": "Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.", "entity1": "Trace amine-associated receptor 1", "entity2": "amphetamine", "span1": [0, 33], "span2": [111, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7266": {"label": 3, "data": {"text": "DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors.", "entity1": "human secretory isoform VI", "entity2": "sulfonamide", "span1": [61, 87], "span2": [106, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6283": {"label": 3, "data": {"text": "Although the IC50 value of meloxicam for inhibition of COX-1 was 10-fold higher than the IC50 value of COX-2 in vitro, this biochemical selectivity was inadequate to clearly separate the effects of meloxicam on the two isozymes after oral dosing as a function of the daily dose and interindividual variation in steady-state plasma levels.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [103, 108], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10131": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "suprofen", "span1": [34, 37], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6518": {"label": 3, "data": {"text": "We tested the new orally active nonpeptidic renin inhibitor SPP100 (Aliskiren, an octanamide with a 50% inhibitory concentration [IC50] in the low nanomolar range) in 18 healthy volunteers on a constant 100 mmol/d sodium diet using a double-blind, 3-way crossover protocol.", "entity1": "renin", "entity2": "SPP100", "span1": [44, 49], "span2": [60, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12151": {"label": 0, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "Lys", "span1": [150, 156], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13657": {"label": 1, "data": {"text": "The binding of U46619 to the PGIS protein was demonstrated by 1D NMR titration, and the significant perturbation of the chemical shifts of protons at C-11, H2C, and H20 of U46619 were observed upon U46619 binding to the engineered PGIS in a concentration-dependent manner.", "entity1": "PGIS", "entity2": "U46619", "span1": [29, 33], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4897": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "aromatase", "entity2": "Cl", "span1": [148, 157], "span2": [102, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"870": {"label": 8, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ODC", "entity2": "putrescine", "span1": [143, 146], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6467": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "thymidylate synthase", "entity2": "LY231514", "span1": [90, 110], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14193": {"label": 1, "data": {"text": "CCAAT/Enhancer-binding protein-homologous protein sensitizes to SU5416 by modulating p21 and PI3K/Akt signal pathway in FRO anaplastic thyroid carcinoma cells.", "entity1": "p21", "entity2": "SU5416", "span1": [85, 88], "span2": [64, 70]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"780": {"label": 9, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "COX", "entity2": "exisulind", "span1": [188, 191], "span2": [109, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10026": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Lys", "span1": [199, 208], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8187": {"label": 3, "data": {"text": "miR-200, a miRNA family with tumor suppressive functions in a wide range of cancers, was found reduced in response to TAM treatment.", "entity1": "miR-200", "entity2": "TAM", "span1": [0, 7], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3388": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "DAT", "entity2": "amphetamine", "span1": [178, 181], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4339": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "ERK", "entity2": "Pinosylvin", "span1": [151, 154], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"520": {"label": 1, "data": {"text": "Exogenous C2-ceramide activates c-fos serum response element via Rac-dependent signalling pathway.", "entity1": "Rac", "entity2": "C2-ceramide", "span1": [65, 68], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15714": {"label": 3, "data": {"text": "4-Hydroxypyridazin-3(2H)-one Derivatives as Novel d-Amino Acid Oxidase Inhibitors.", "entity1": "d-Amino Acid Oxidase", "entity2": "4-Hydroxypyridazin-3(2H)-one", "span1": [50, 70], "span2": [0, 28]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8029": {"label": 2, "data": {"text": "In addition, we provide evidence that apomorphine also acts on endogenous TRPA1 in cultured dorsal root ganglion neurons from rats and in the enterochromaffin model cell line QGP-1, from which serotonin is released upon activation of TRPA1.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [234, 239], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1991": {"label": 2, "data": {"text": "Extracellular application of meclofenamate (EC(50) = 25 microM) and diclofenac (EC(50) = 2.6 microM) resulted in the activation of KCNQ2/Q3 K(+) currents, heterologously expressed in Chinese hamster ovary cells.", "entity1": "KCNQ2/Q3", "entity2": "diclofenac", "span1": [131, 139], "span2": [68, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2414": {"label": 3, "data": {"text": "However, despite activation of L-arginine uptake, the inhibition of arginase activity by Nor-NOHA was still significant.", "entity1": "arginase", "entity2": "Nor-NOHA", "span1": [68, 76], "span2": [89, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7181": {"label": 1, "data": {"text": "Administration of m-chlorophenylpiperazine and fenfluramine, both of which induce anorexic effects via 5-HT2C receptors and/or 5-HT1B receptors, suppressed food intake in 5- and 8-wk-old Ay mice, whereas the anorexic effects were attenuated in food-restricted Ay mice.", "entity1": "5-HT1B", "entity2": "m-chlorophenylpiperazine", "span1": [127, 133], "span2": [18, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11567": {"label": 1, "data": {"text": "Metabolism of vitamin A, all-trans-retinol, leads to the formation of 11-cis-retinaldehyde, the visual chromophore, and all-trans-retinoic acid, which is involved in the regulation of gene expression through the retinoic acid receptor.", "entity1": "retinoic acid receptor", "entity2": "all-trans-retinoic acid", "span1": [212, 234], "span2": [120, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10145": {"label": 8, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "cyclooxygenase", "entity2": "thromboxanes", "span1": [77, 91], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6527": {"label": 3, "data": {"text": "The earliest known AChE inhibitors, namely, physostigmine and tacrine, performed poorly in clinical trials (e.g., poor oral activity, brain penetration, and hepatotoxic liability).", "entity1": "AChE", "entity2": "physostigmine", "span1": [19, 23], "span2": [44, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12418": {"label": 1, "data": {"text": "Plasma glucose, active GLP-1 (7-36) amide concentration and insulin levels were measured after glucose loading.", "entity1": "insulin", "entity2": "glucose", "span1": [60, 67], "span2": [95, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1295": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "GAD", "entity2": "glutamate", "span1": [50, 53], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"7859": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "phosphatase", "entity2": "okadaic acid", "span1": [232, 243], "span2": [254, 266]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6149": {"label": 0, "data": {"text": "For example, it is clear that the closed conformation of the regulatory N-terminal domain in Ca2+-bound cardiac troponin C (cTnC) presents a much different binding surface for Ca2+-sensitizing compounds than previously thought.", "entity1": "cTnC", "entity2": "N", "span1": [124, 128], "span2": [72, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1858": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "DGAT", "entity2": "kuraridin", "span1": [253, 257], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4102": {"label": 1, "data": {"text": "Safrole-2',3'-oxide induces atherosclerotic plaque vulnerability in apolipoprotein E-knockout mice.", "entity1": "apolipoprotein E", "entity2": "Safrole-2',3'-oxide", "span1": [68, 84], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11558": {"label": 1, "data": {"text": "Warfarin dose and the pharmacogenomics of CYP2C9 and VKORC1 - rationale and perspectives.", "entity1": "VKORC1", "entity2": "Warfarin", "span1": [53, 59], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15383": {"label": 5, "data": {"text": "Computational docking analysis was conducted to model the interaction of these antagonists with the human ER\u03b1 and showed that they could tightly bind to the ER\u03b1 in a manner similar to that of ICI-182,780, a pure ER antagonist.", "entity1": "ER", "entity2": "ICI-182,780", "span1": [212, 214], "span2": [192, 203]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1075": {"label": 1, "data": {"text": "In the present study, the capacity of acetylcholinesterase inhibitors to interact with muscarinic receptors was assessed by their ability to displace both [3H]-oxotremorine-M and [3H]-quinuclinidyl benzilate binding in rat brain membranes.", "entity1": "muscarinic receptors", "entity2": "[3H]-quinuclinidyl benzilate", "span1": [87, 107], "span2": [179, 207]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7054": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARgamma", "entity2": "tamibarotene", "span1": [74, 82], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13434": {"label": 2, "data": {"text": "High D-glucose increases L-arginine transport and eNOS expression following TbetaRII activation by TGF-beta1 involving p42/44(mapk) and Smad2 in HUVEC.", "entity1": "eNOS", "entity2": "D-glucose", "span1": [50, 54], "span2": [5, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10366": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-5", "entity2": "omapatrilat", "span1": [52, 59], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7664": {"label": 1, "data": {"text": "Examining the four X-ray crystal structures of their CA II adducts, we observed several (2-3) active site water molecules interacting with the chlorthalidone, trichloromethiazide, and furosemide scaffolds which may be responsible for this important difference of activity.", "entity1": "CA II", "entity2": "trichloromethiazide", "span1": [53, 58], "span2": [159, 178]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3450": {"label": 1, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "DAT", "entity2": "[(3)H]WIN 35428", "span1": [195, 198], "span2": [140, 155]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13963": {"label": 1, "data": {"text": "Consistent with the results of a computer analysis, the binding of R316C to triiodothyronine (T3) was significantly decreased to 38% that of the wild type.", "entity1": "R316C", "entity2": "triiodothyronine", "span1": [67, 72], "span2": [76, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7749": {"label": 0, "data": {"text": "Whole-exome analysis of the Pik3ca(H1047R)-driven mammary tumors identified multiple mutations, including Trp53 mutations that appeared spontaneously during the development of adenocarinoma and spindle cell tumors.", "entity1": "H1047R", "entity2": "Trp", "span1": [35, 41], "span2": [106, 109]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15884": {"label": 2, "data": {"text": "Our study revealed that high glucose/Fe concentrations in MIN6 cells induced an increase of the Bcl2/Bax ratio, an indicator of increased cell apoptosis.", "entity1": "Bcl2", "entity2": "Fe", "span1": [96, 100], "span2": [37, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2214": {"label": 1, "data": {"text": "Two beta(2)-agonists, formoterol and salmeterol, are approved for treating asthma and have an extended duration of action and increased safety, associated with greater beta(2)-adrenoceptor selectivity.", "entity1": "beta(2)-adrenoceptor", "entity2": "salmeterol", "span1": [168, 188], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4181": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "aldo-keto reductase (AKR) 1C1", "entity2": "cinnamic aldehyde", "span1": [262, 291], "span2": [204, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4306": {"label": 1, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "caspase-3", "entity2": "AuF", "span1": [130, 139], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7885": {"label": 8, "data": {"text": "The altered activities of key enzymes such as glucose-6-phosphatase and fructose-1,6-bisphosphatase of carbohydrate metabolism significantly (p<0.05) increased whereas hexokinase, pyruvate kinase, glucose-6-phosphate dehydrogenase and glycogen content significantly (p<0.05) decreased in the liver of diabetic rats and also increased activities of aspartate transaminase (AST), alanine transaminase (ALT) and alkaline phosphatase (ALP).", "entity1": "glucose-6-phosphatase", "entity2": "carbohydrate", "span1": [46, 67], "span2": [103, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3734": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates induce apoptosis of hematopoietic tumor cells via inhibition of Ras signaling pathways and Bim-mediated activation of the intrinsic apoptotic pathway.", "entity1": "Ras", "entity2": "Nitrogen", "span1": [100, 103], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"481": {"label": 1, "data": {"text": "Extensive inhibitions of TREK-1 activity are observed after activation of protein kinases A and C. TREK-1 currents are sensitive to extracellular K+ and Na+.", "entity1": "TREK-1", "entity2": "K+", "span1": [99, 105], "span2": [146, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9407": {"label": 9, "data": {"text": "On the contrary, pretreatment with 5-HT worsened ethanol-induced erosions, however, did not affect gastric mucus secretion, glycoprotein content or PGE2 levels, although the non-protein SH fraction was significantly decreased.", "entity1": "glycoprotein", "entity2": "5-HT", "span1": [124, 136], "span2": [35, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11720": {"label": 1, "data": {"text": "Apoptosis initiation of \u03b2-ionone in SGC-7901 gastric carcinoma cancer cells via a PI3K-AKT pathway.", "entity1": "AKT", "entity2": "\u03b2-ionone", "span1": [87, 90], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9524": {"label": 3, "data": {"text": "Isoform-specific inhibition of L-type calcium channels by dihydropyridines is independent of isoform-specific gating properties.", "entity1": "L-type calcium channels", "entity2": "dihydropyridines", "span1": [31, 54], "span2": [58, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9999": {"label": 8, "data": {"text": "Bumetanide-sensitive Cl- secretion was dependent on extracellular Na+ and either K+ or NH, consistent with the ion dependency of NKCC1-mediated Cl- transport.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [129, 134], "span2": [144, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8530": {"label": 2, "data": {"text": "In macrophages, levels of TNF-\u03b1, IFN-\u03b3, NO, IL-6 and IL-10 were increased by CDM used alone or in combination with HSV-2.", "entity1": "IFN-\u03b3", "entity2": "CDM", "span1": [33, 38], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11898": {"label": 8, "data": {"text": "Cytochrome P450 epoxygenase 2J2 (CYP2J2) metabolizes arachidonic acids to form epoxyeicosatrienoic acids (EETs), which possess various beneficial effects on the cardiovascular system.", "entity1": "CYP2J2", "entity2": "epoxyeicosatrienoic acids", "span1": [33, 39], "span2": [79, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"689": {"label": 1, "data": {"text": "Combined concentration-ratio analysis demonstrated that tamsulosin, which does not discriminate between alpha 1A- and alpha 1L-adrenoceptors, and RS-17053 competed for binding at the same site in the SMA.", "entity1": "alpha 1A", "entity2": "tamsulosin", "span1": [104, 112], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6674": {"label": 2, "data": {"text": "Furthermore, RT-PCR analyses revealed that minocycline treatment increased expression of interleukin-10 mRNA but decreased tumor necrosis factor-alpha expression.", "entity1": "interleukin-10", "entity2": "minocycline", "span1": [89, 103], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9774": {"label": 5, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "alpha(2)-adrenergic receptors", "entity2": "fluparoxan", "span1": [73, 102], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6586": {"label": 8, "data": {"text": "It is caused by a deficiency of propionyl-CoA carboxylase (PCC, EC 6.4.1.3), a biotin-dependent enzyme that catalyzes the carboxylation of propionyl-CoA to D-methylmalonyl-CoA.", "entity1": "propionyl-CoA carboxylase", "entity2": "D-methylmalonyl-CoA", "span1": [32, 57], "span2": [156, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10299": {"label": 8, "data": {"text": "These findings suggest that RhBG and RhCG may play important and cell-specific roles in ammonium transport and signaling in these regions of the kidney.", "entity1": "RhCG", "entity2": "ammonium", "span1": [37, 41], "span2": [88, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15738": {"label": 3, "data": {"text": "Wattakaka volubilis steroidal glycoside mixture (WVSM) and PPG (1-50\u03bcM) significantly inhibited the COX-2 and iNOS enzymes resulting in low levels of PGE2 and NO in LPS-induced RAW 264.7 macrophage cells.", "entity1": "COX-2", "entity2": "steroidal glycoside", "span1": [100, 105], "span2": [20, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4165": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "NF-\u03baB", "entity2": "sesquiterpene", "span1": [173, 178], "span2": [109, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"21": {"label": 3, "data": {"text": "This effect was potentiated by isobutylmethylxanthine, an inhibitor of phosphodiesterase.", "entity1": "phosphodiesterase", "entity2": "isobutylmethylxanthine", "span1": [71, 88], "span2": [31, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"881": {"label": 5, "data": {"text": "In the present study, we compared the pharmacology of (+/-)pindolol, WAY-100635 (a 5-HT(1A) antagonist), GR127935 (a 5-HT(1B/1D) antagonist), and isamoltane (a 5-HT(1B) antagonist), when given acutely in combination with fluoxetine, using in vivo microdialysis in the frontal cortex of the freely moving rat.", "entity1": "5-HT(1A)", "entity2": "WAY-100635", "span1": [83, 91], "span2": [69, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7012": {"label": 3, "data": {"text": "Sorafenib has the added advantage of inhibiting multiple different Raf isoforms, which enables it to target TGF-alpha/EGFR signaling and may also enhance its inhibition of VEGFR and PDGFR-beta.", "entity1": "Raf", "entity2": "Sorafenib", "span1": [67, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10439": {"label": 1, "data": {"text": "The holo-SDH contained PLP-OMS aldimine in the active site, indicating that OMS can form the Schiff base linkage with PLP, but the subsequent dehydration did not occur.", "entity1": "holo-SDH", "entity2": "OMS", "span1": [4, 12], "span2": [76, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11639": {"label": 8, "data": {"text": "Risperidone is metabolized to its active metabolite, 9-hydroxyrisperidone, mainly by the cytochrome P450 enzymes CYP2D6 and 3A4.", "entity1": "cytochrome P450", "entity2": "Risperidone", "span1": [89, 104], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5890": {"label": 1, "data": {"text": "Mouse ornithine decarboxylase (ODC) was expressed in Escherichia coli and the purified recombinant enzyme used for determination of the binding site for pyridoxal 5'-phosphate and of the residues modified in the inactivation of the enzyme by the enzyme-activated irreversible inhibitor, alpha-difluoromethylornithine (DFMO).", "entity1": "ODC", "entity2": "pyridoxal 5'-phosphate", "span1": [31, 34], "span2": [153, 175]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9212": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "alpha 2-macroglobulin", "entity2": "trifluoperazine", "span1": [209, 230], "span2": [142, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7213": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "PDGFA", "entity2": "Cd", "span1": [182, 187], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2617": {"label": 9, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "N495K", "entity2": "foscarnet", "span1": [107, 112], "span2": [79, 88]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2609": {"label": 1, "data": {"text": "Pharmacogenetic analysis of two genes, the warfarin metabolic enzyme CYP2C9 and warfarin target enzyme, vitamin K epoxide reductase complex 1 VKORC1, confirmed their influence on warfarin maintenance dose.", "entity1": "VKORC1", "entity2": "warfarin", "span1": [142, 148], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15705": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "TRP channels", "entity2": "acetic acid", "span1": [46, 58], "span2": [212, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1455": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "MAO", "entity2": "TVP1012", "span1": [95, 98], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8731": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A3", "entity2": "imipramine", "span1": [189, 195], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5279": {"label": 1, "data": {"text": "In concert with these results, we highlighted that the secretion of pro-inflammatory cytokine and NF-\u03baB activation induced by TCDD can be mediated by elevation of [Ca(2+)]i in HAPI microglial cells.", "entity1": "NF-\u03baB", "entity2": "Ca(2+)", "span1": [98, 103], "span2": [164, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4090": {"label": 2, "data": {"text": "Activation of an apoptotic signal transduction pathway involved in the upregulation of calpain and apoptosis-inducing factor in aldosterone-induced primary cultured cardiomyocytes.", "entity1": "apoptosis-inducing factor", "entity2": "aldosterone", "span1": [99, 124], "span2": [128, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12501": {"label": 8, "data": {"text": "The results suggest that individuals with high Vmax beta 2-ADH and deficient in low-Km mitochondrial ALDH2, accounting for approximately 45% of the Chinese population, may end up with acetaldehyde accumulation during alcohol consumption, rendering them vulnerable to tissue injury caused by this highly reactive and toxic metabolite.", "entity1": "ALDH2", "entity2": "acetaldehyde", "span1": [101, 106], "span2": [184, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"593": {"label": 9, "data": {"text": "The action of 15d-PGJ2 does not appear to involve its nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) because troglitazone, a specific ligand of PPARgamma, was unable to inhibit iNOS induction, and neither troglitazone nor 15d-PGJ2 could stimulate the activity of a PPAR-dependent promoter in the absence of cotransfected PPARgamma.", "entity1": "iNOS", "entity2": "troglitazone", "span1": [208, 212], "span2": [140, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7635": {"label": 9, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "purine receptors", "entity2": "GTP", "span1": [125, 141], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13366": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "anterior gradient-2", "entity2": "estrogen", "span1": [80, 99], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12531": {"label": 8, "data": {"text": "Differential lactose/lactulose/L-rhamnose absorption provides a non-invasive and sensitive index of small intestinal integrity of value for the interpretation of prolonged or otherwise complicated enteritis and the distinction of primary secondary intestinal lactase deficiency.", "entity1": "lactase", "entity2": "lactulose", "span1": [259, 266], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4184": {"label": 2, "data": {"text": "Whereas, the levels of both the basal and sulforaphane-inducible expression of AKR1C1 were significantly reduced in NRF2-silenced stable U937 cells compared to the control cells.", "entity1": "AKR1C1", "entity2": "sulforaphane", "span1": [79, 85], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4444": {"label": 3, "data": {"text": "In most instances, C6-substituted phthalides exhibit MAO-B specific inhibition.", "entity1": "MAO-B", "entity2": "phthalides", "span1": [53, 58], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15711": {"label": 3, "data": {"text": "Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone.", "entity1": "MMP-9", "entity2": "xanthohumol", "span1": [108, 113], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6420": {"label": 2, "data": {"text": "Since it has been proposed that UCP-3 could be involved in the regulation of the use of fatty acids as fuel substrates, the UCP-3 induction achieved after bezafibrate and Wy-14, 643 treatment may indicate a higher oxidation of fatty acids, limiting their availability to be stored as triglycerides.", "entity1": "UCP-3", "entity2": "bezafibrate", "span1": [124, 129], "span2": [155, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7671": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "CA", "entity2": "Thiazide", "span1": [113, 115], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4606": {"label": 3, "data": {"text": "Although thioredoxin reductase (TRR) inhibitors (aurothioglucose and Sb(III)) inhibited cytosolic DMAs(V) reduction, recombinant rat TRR plus NADPH, alone or when added to the cytosol, failed to support DMAs(V) reduction.", "entity1": "thioredoxin reductase", "entity2": "aurothioglucose", "span1": [9, 30], "span2": [49, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13056": {"label": 3, "data": {"text": "Late INa induced by the VGSC long QT mutant R1623Q was reduced by resveratrol and quercetin.", "entity1": "R1623Q", "entity2": "quercetin", "span1": [44, 50], "span2": [82, 91]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4246": {"label": 1, "data": {"text": "Butein protects human dental pulp cells from hydrogen peroxide-induced oxidative toxicity via Nrf2 pathway-dependent heme oxygenase-1 expressions.", "entity1": "Nrf2", "entity2": "Butein", "span1": [94, 98], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"292": {"label": 0, "data": {"text": "The carbonic anhydrase V produced by a vector containing the full coding sequence, which includes a possible NH2-terminal mitochondrial targeting signal, was proteolytically processed by E. coli and contained several amino-terminal ends.", "entity1": "The carbonic anhydrase V", "entity2": "amino", "span1": [0, 24], "span2": [217, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2967": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "H613A", "entity2": "vardenafil", "span1": [71, 76], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14009": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "AXL", "entity2": "XL184", "span1": [249, 252], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12284": {"label": 1, "data": {"text": "The results lend support that (18)F-AV-45 may be a useful PET agent for detecting Abeta plaques in the living human brain.", "entity1": "Abeta", "entity2": "(18)F-AV-45", "span1": [82, 87], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"669": {"label": 3, "data": {"text": "OBJECTIVE: To evaluate the extent of human cyclooxygenase-1 (COX-1) inhibition by meloxicam, which has been reported to preferentially inhibit cyclooxygenase-2 (COX-2).", "entity1": "human cyclooxygenase-1", "entity2": "meloxicam", "span1": [37, 59], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7459": {"label": 8, "data": {"text": "The vesicular inhibitory phenotype was gradually altered from glycinergic to GABAergic through mixed events when GABA is introduced into the secretory cell and competes for uptake by VIAAT.", "entity1": "VIAAT", "entity2": "GABA", "span1": [183, 188], "span2": [113, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1052": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "4'-(9-acridinylamino)methanesulfon-m-anisidide", "span1": [162, 166], "span2": [223, 269]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13016": {"label": 7, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "PLC-beta", "entity2": "Ca2+", "span1": [22, 30], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3362": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-type voltage-gated calcium channels", "entity2": "barbiturates", "span1": [114, 151], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11129": {"label": 1, "data": {"text": "Prazosin was found to be unselective; 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101), 5-methyl-urapidil, indoramin and (+)-niguldipine were confirmed as selective for the alpha 1A-adrenoceptor, whereas spiperone was weakly alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptor", "entity2": "indoramin", "span1": [192, 213], "span2": [126, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8600": {"label": 2, "data": {"text": "LPO was increased while as GSH, CAT and GPx decreased by the administration of CCl4 and TAA (p<0.001); co-administration of NAC restored these liver markers to normal levels (p<0.001).", "entity1": "CAT", "entity2": "NAC", "span1": [32, 35], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2105": {"label": 5, "data": {"text": "The selective beta1AR antagonists atenolol and metoprolol blocked isoproterenol-induced enhancement, with apparent K(b) values of 85 +/- 36 and 3.9 +/- 1.7 nM, respectively.", "entity1": "beta1AR", "entity2": "atenolol", "span1": [14, 21], "span2": [34, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11585": {"label": 3, "data": {"text": "As add-on therapy in patients with suboptimal glycaemic control despite oral antihyperglycaemic treatment, sitagliptin improved HbA(1c) to a significantly greater extent than placebo when added to metformin or pioglitazone and was noninferior to glipizide when added to metformin.", "entity1": "HbA(1c)", "entity2": "metformin", "span1": [128, 135], "span2": [270, 279]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11089": {"label": 1, "data": {"text": "Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease.", "entity1": "corticotropin-releasing hormone", "entity2": "Loperamide", "span1": [88, 119], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13736": {"label": 8, "data": {"text": "These data support the concept that adipose tissue NNMT contributes to the increased plasma homocysteine levels in patients treated with NA.", "entity1": "NNMT", "entity2": "homocysteine", "span1": [51, 55], "span2": [92, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11685": {"label": 1, "data": {"text": "Thiazolidinediones (TZDs) are insulin sensitizers used for treatment of diabetes.", "entity1": "insulin", "entity2": "TZDs", "span1": [30, 37], "span2": [20, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3867": {"label": 3, "data": {"text": "HSYA treatment also decreased NF-\u03baB p65 nuclear translocation and inhibited the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK).", "entity1": "p38", "entity2": "HSYA", "span1": [137, 140], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5762": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "ubiquitin carboxy-terminal hydrolase L-1", "entity2": "MPTP", "span1": [244, 284], "span2": [140, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3234": {"label": 1, "data": {"text": "In untrained and trained treated animals with the amnesic dose (1.0mg/kg) of METH SERT binding in several areas including hippocampus and cortex decreased, more remarkably in the trained animals.", "entity1": "SERT", "entity2": "METH", "span1": [82, 86], "span2": [77, 81]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1325": {"label": 3, "data": {"text": "To eliminate the interaction of bupropion with DAT or NET, nomifensine or desipramine, respectively, was included in the superfusion buffer.", "entity1": "DAT", "entity2": "bupropion", "span1": [47, 50], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15208": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "iNOS", "entity2": "ethylacetate", "span1": [329, 333], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13987": {"label": 8, "data": {"text": "An essential control in experiments using Gy mice is to demonstrate that the abnormal phenotypes exhibited by these mice are abolished by providing replacement spermine and this can be accomplished by breeding with CAG-SMS mice that express SpmS from a ubiquitous promoter.", "entity1": "SMS", "entity2": "spermine", "span1": [219, 222], "span2": [160, 168]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10580": {"label": 4, "data": {"text": "Imiquimod, a Toll-like receptor-7 agonist, induces perforin in cytotoxic T lymphocytes in vitro.", "entity1": "Toll-like receptor-7", "entity2": "Imiquimod", "span1": [13, 33], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7190": {"label": 1, "data": {"text": "Because progesterone (1) affects both menstruation and gestation via the progesterone receptor (PR), research aimed at modulating its activity is usually surrounded by controversy.", "entity1": "progesterone receptor", "entity2": "progesterone", "span1": [73, 94], "span2": [8, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14501": {"label": 3, "data": {"text": "Western blot analysis indicated that TSN inhibits the CDC42/MEKK1/JNK pathway.", "entity1": "CDC42", "entity2": "TSN", "span1": [54, 59], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2663": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE2", "entity2": "erythro-9-(2-hydroxy-3-nonyl)adenine", "span1": [76, 80], "span2": [82, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"323": {"label": 1, "data": {"text": "The folding rate monitored by 2'CMP binding to the major slow-folding species of Pro42Ala RNase A is faster than the folding rate monitored by tyrosine burial; however, the folding rate monitored by inhibitor binding to the minor slow-folding species is decreased significantly over the folding rate monitored by tyrosine burial, indicating that the major and minor slow-folding species of Pro42Ala fold to the native state with different transition-state conformations in the rate-determining step.", "entity1": "RNase A", "entity2": "2'CMP", "span1": [90, 97], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2675": {"label": 8, "data": {"text": "In kidneys, stimulation of adenylyl cyclase causes egress of cAMP, conversion of cAMP to AMP by ecto-phosphodiesterase, and metabolism of AMP to adenosine by ecto-5'-nucleotidase.", "entity1": "ecto-5'-nucleotidase", "entity2": "adenosine", "span1": [158, 178], "span2": [145, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4801": {"label": 1, "data": {"text": "The neurotrophic factors pleiotrophin (PTN) and midkine (MK) have been shown to modulate amphetamine-induced neurotoxicity.", "entity1": "MK", "entity2": "amphetamine", "span1": [57, 59], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5473": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "medroxy-progesterone acetate", "span1": [106, 127], "span2": [217, 245]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13605": {"label": 0, "data": {"text": "The key difference in structure of Lp(a) and plasminogen is replacement of Arg with Ser at position 560.", "entity1": "Lp(a)", "entity2": "Arg", "span1": [35, 40], "span2": [75, 78]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1144": {"label": 3, "data": {"text": "ZD1839 (\"Iressa\"), a quinazoline tyrosine kinase inhibitor selective for the EGFR, has shown good activity in preclinical studies and in the early phase of clinical trials.", "entity1": "tyrosine kinase", "entity2": "Iressa", "span1": [33, 48], "span2": [9, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12445": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "ML129", "span1": [173, 175], "span2": [123, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"169": {"label": 3, "data": {"text": "If the effectors were added after 5 min of aging they increased the activity of soman-inhibited AChE, but to a considerably smaller extent than HI 6.", "entity1": "AChE", "entity2": "soman", "span1": [96, 100], "span2": [80, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8995": {"label": 1, "data": {"text": "Enprofylline, a weak adenosine antagonist but potent inhibitor of cyclic AMP phosphodiesterase, did not alter ethanol's motor incoordination, further supporting involvement of brain adenosine receptor mechanism(s) in ethanol-adenosine interactions.", "entity1": "adenosine receptor", "entity2": "ethanol", "span1": [182, 200], "span2": [217, 224]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2095": {"label": 8, "data": {"text": "Therefore, comparative histochemical and biochemical studies of u-PA and the effects of amiloride were performed on rabbit corneas and tear fluid using the sensitive fluorogenic substrate Z-Gly-Gly-Arg-7-amino-4-trifluoromethylcoumarin.", "entity1": "u-PA", "entity2": "Z-Gly-Gly-Arg-7-amino-4-trifluoromethylcoumarin", "span1": [64, 68], "span2": [188, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6468": {"label": 3, "data": {"text": "We took advantage of the previous observations that phosphatidylserine inhibits DGK-delta (reviewed by Sakane, F., Imai, S., Kai, M., Wada, I., and Kanoh, H. (1996) J. Biol.", "entity1": "DGK-delta", "entity2": "phosphatidylserine", "span1": [80, 89], "span2": [52, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5700": {"label": 2, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "human TRPA1", "entity2": "apomorphine", "span1": [21, 32], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3504": {"label": 1, "data": {"text": "These results suggest that AKRs induction by PAHs in smokers' PBLs is associated with BMI; therefore, the role of adipose tissue accumulation in PAHs' effects needs further investigation.", "entity1": "AKRs", "entity2": "PAHs", "span1": [27, 31], "span2": [45, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8179": {"label": 3, "data": {"text": "Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.", "entity1": "aldosterone synthase", "entity2": "Tetrahydropyrroloquinolinone", "span1": [63, 83], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1665": {"label": 1, "data": {"text": "In membranes from HEK293 cells transfected with alpha2-receptors, etomidate inhibited binding of the alpha2-antagonist, [3H]RX821002, with higher potency from alpha2B- and alpha2C-receptors than from alpha2A-receptors (Ki alpha2A 208 microm, alpha2B 26 microm, alpha2C 56 microm).", "entity1": "alpha2A-receptors", "entity2": "etomidate", "span1": [200, 217], "span2": [66, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5132": {"label": 3, "data": {"text": "Pyrrolidine dithiocarbamate (PDTC), a specific NF-\u03baB inhibitor, along with 20S proteasome inhibitor (PSI) significantly inhibited LPS-induced iNOS expression, which indirectly suggested that 5HHMF downregulated iNOS expression by suppressing NF-\u03baB activity.", "entity1": "NF-\u03baB", "entity2": "Pyrrolidine dithiocarbamate", "span1": [47, 52], "span2": [0, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2231": {"label": 1, "data": {"text": "Computer modeling suggests that the KITD816V mutation destabilizes the inactive conformation of the KIT activation loop to which imatinib binds, but it is not predicted to impair binding of KIT by dasatinib.", "entity1": "KIT", "entity2": "dasatinib", "span1": [190, 193], "span2": [197, 206]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3340": {"label": 1, "data": {"text": "The affinities of dfbp and dfbp-o for the regulatory domain of cTnC were measured in the absence and presence of cTnI by NMR spectroscopy, and dfbp-o was found to bind more strongly than dfbp.", "entity1": "cTnC", "entity2": "dfbp", "span1": [63, 67], "span2": [18, 22]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3936": {"label": 2, "data": {"text": "The reactivation of brain AChE inhibited with tabun demonstrated better activity of new compound BT-07-4M, TMB-4 and obidoxime from symmetric oximes, and BT-05 and BT-03 possessing asymmetric structure.", "entity1": "AChE", "entity2": "BT-05", "span1": [26, 30], "span2": [154, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4232": {"label": 2, "data": {"text": "Quantitative real-time polymerase chain reaction analysis showed that following the exposure of cells to SiO(2) NPs, the messenger RNA level of apoptotic genes (caspase-3 and caspase-9) were upregulated in a dose-dependent manner.", "entity1": "caspase-3", "entity2": "SiO(2)", "span1": [161, 170], "span2": [105, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3377": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-VGCCs", "entity2": "BDZs", "span1": [153, 160], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13024": {"label": 1, "data": {"text": "11Beta-HSD1 activates cortisone to cortisol to facilitate glucocorticoid receptor (GR)-mediated action.", "entity1": "glucocorticoid receptor", "entity2": "cortisone", "span1": [58, 81], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4844": {"label": 2, "data": {"text": "Subsequent analysis revealed that cucurbitacin I strongly activates RhoA and the Rho effector Rho kinase (ROCK) in breast cancer cells and induces the formation of stress fibers.", "entity1": "Rho kinase", "entity2": "cucurbitacin I", "span1": [94, 104], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15724": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b2", "entity2": "heptylparaben", "span1": [150, 153], "span2": [77, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15277": {"label": 5, "data": {"text": "CONCLUSIONS: These findings confirm that the CRF(1) receptor antagonist SSR125543 is able to attenuate the behavioral effects of traumatic stress exposure and indicate that these effects are associated with a normalization of hippocampal neuronal excitability impaired by stress.", "entity1": "CRF(1) receptor", "entity2": "SSR125543", "span1": [45, 60], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15954": {"label": 1, "data": {"text": "OHT-induced cyclin E truncation also occurred in SK-BR-3 cells that express GPR30 and lack ER\u03b1, but not in MDA-MB-231 cells that express neither GPR30 nor ER\u03b1.", "entity1": "cyclin E", "entity2": "OHT", "span1": [12, 20], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10025": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Lys", "span1": [126, 138], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10620": {"label": 5, "data": {"text": "GABA-evoked currents were completely and reversibly blocked by the competitive GABAA receptor antagonist bicuculline (IC50 = 1.7 microM), indicating expression of GABAA but not GABAC receptors.", "entity1": "GABAA receptor", "entity2": "bicuculline", "span1": [79, 93], "span2": [105, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13740": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "LTCC", "entity2": "DHP", "span1": [28, 32], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13182": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "NET", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane", "span1": [287, 290], "span2": [82, 148]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12366": {"label": 1, "data": {"text": "These results suggest that ganglioside-bound A\u03b2 (GA\u03b2), which acts as an endogenous seed for A\u03b2 fibril formation in AD brains, is generated on ASIGN on synaptosomal membranes.", "entity1": "A\u03b2", "entity2": "ganglioside", "span1": [50, 52], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3187": {"label": 5, "data": {"text": "RGM-1 cells were treated with CDCA or GW4064, an FXR agonist, in the presence or absence of guggulsterone, an FXR antagonist.", "entity1": "FXR", "entity2": "guggulsterone", "span1": [110, 113], "span2": [92, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4919": {"label": 3, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "CAT", "entity2": "kinsenoside", "span1": [203, 206], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4535": {"label": 3, "data": {"text": "Our recent study has demonstrated that coadministration of monoamine oxidase A (MAO-A) inhibitor harmaline (5 mg/kg) increases systemic exposure to 5-MeO-DMT (2 mg/kg) and active metabolite bufotenine.", "entity1": "monoamine oxidase A", "entity2": "harmaline", "span1": [59, 78], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13065": {"label": 2, "data": {"text": "It was, therefore, proposed that H. pylori may in fact, antagonize, aspirin-induced delay of ulcer healing due to suppression of acid secretion by the enhancement in PGE(2) possibly derived from COX-2 expression and activity and to the overexpression of growth factors such as TGF alpha and VEGF.", "entity1": "COX-2", "entity2": "aspirin", "span1": [195, 200], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4595": {"label": 3, "data": {"text": "Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.", "entity1": "PI3K", "entity2": "5-morpholino-7H-thieno[3,2-b]pyran-7-ones", "span1": [131, 135], "span2": [61, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10529": {"label": 3, "data": {"text": "Incubation with metformin (0.2-1 mM) activated AMPK in both human islets and MIN6 beta-cells in parallel with an inhibition of insulin secretion, whereas leptin (10-100 nM) was without effect in MIN6 cells.", "entity1": "insulin", "entity2": "metformin", "span1": [127, 134], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12650": {"label": 1, "data": {"text": "It has no influence on the rate of association of (125)I-ET-1 to ETA receptors.", "entity1": "ETA receptors", "entity2": "(125)I", "span1": [65, 78], "span2": [50, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12832": {"label": 3, "data": {"text": "A review of the structural and functional features of olmesartan medoxomil, an angiotensin receptor blocker.", "entity1": "angiotensin receptor", "entity2": "olmesartan medoxomil", "span1": [79, 99], "span2": [54, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"874": {"label": 8, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ODC", "entity2": "spermine", "span1": [143, 146], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5347": {"label": 2, "data": {"text": "These findings suggest that S1P activates the PI3K/Akt signaling pathway leading to the promotion of nuclear translocation of \u03b2-catenin in osteoblast-like cells, resulting in the upregulation of osteoptotegerin and osteoblast differentiation markers including alkaline phosphatase, probably relating to the inhibition of osteoclast formation and the mineralization, respectively.", "entity1": "\u03b2-catenin", "entity2": "S1P", "span1": [126, 135], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13697": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "human TLR7", "entity2": "gardiquimod", "span1": [118, 128], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9579": {"label": 1, "data": {"text": "Only carbetocin bound to the renal vasopressin V2 receptor though the binding affinity was very low (61.3 +/- 14.6 nM).", "entity1": "vasopressin V2 receptor", "entity2": "carbetocin", "span1": [35, 58], "span2": [5, 15]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10592": {"label": 3, "data": {"text": "There was significantly less thioredoxin reductase activity in rat liver extracts, whereas the level of glutathione activity remained unchanged, demonstrating that the dose of auranofin used was able to selectively inhibit one of these enzyme systems.", "entity1": "thioredoxin reductase", "entity2": "auranofin", "span1": [29, 50], "span2": [176, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13961": {"label": 9, "data": {"text": "Supplementation with levothyroxine at a dose of >350 microg/day did not normalize the serum TSH level; however, the patient showed normal growth and intelligence at 14 years of age.", "entity1": "TSH", "entity2": "levothyroxine", "span1": [92, 95], "span2": [21, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14801": {"label": 3, "data": {"text": "Human immortalized corneal fibroblasts were treated with TGF-\u03b2 in the presence of TSA, the NAD(P)H oxidase inhibitor diphenyleneiodonium (DPI), the antioxidant N-acetyl-cysteine (NAC), the NF-E2-related factor 2-antioxidant response element (Nrf2-ARE) activator sulforaphane, or small interfering RNA.", "entity1": "NAD(P)H oxidase", "entity2": "DPI", "span1": [91, 106], "span2": [138, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5117": {"label": 3, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "Nrf2", "entity2": "NO", "span1": [159, 163], "span2": [60, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3585": {"label": 1, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "ERK1/2", "entity2": "Wogonoside", "span1": [184, 190], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4581": {"label": 3, "data": {"text": "Co-treatment of astrocytes with antofine and the intracellular Ca(2+) chelator BAPTA-AM prevented downregulation of Cx43 and inhibition of GJIC.", "entity1": "Cx43", "entity2": "antofine", "span1": [116, 120], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3642": {"label": 1, "data": {"text": "In the resveratrol+As(2)O(3) group, activities of superoxide dismutase, catalase in serum and GSH/GSSG were significantly increased, histopathological effects were reduced, and arsenic accumulation markedly decreased in the liver, compared with the As(2)O(3)-treated group.", "entity1": "superoxide dismutase", "entity2": "As(2)O(3)", "span1": [50, 70], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1211": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "vesicular monoamine transporter-2", "entity2": "methylenedioxymethamphetamine", "span1": [174, 207], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2711": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "Notch-4", "entity2": "parathion", "span1": [63, 70], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12778": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "capecitabine", "span1": [22, 24], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9768": {"label": 5, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "(AR)s", "entity2": "yohimbine", "span1": [103, 108], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5091": {"label": 1, "data": {"text": "Aldosterone regulates Na(+) transport in the distal nephron through multiple mechanisms that include the transcriptional control of epithelial sodium channel (ENaC) and Na(+)/K(+)-ATPase subunits.", "entity1": "sodium channel", "entity2": "Aldosterone", "span1": [143, 157], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8618": {"label": 3, "data": {"text": "Oxysterol-dependent NOX1 activation, as well as interleukin synthesis, were completely prevented by Cannonau red wine extract that contains an abundant phenolic fraction, in particular phenolic acids and flavonoids.", "entity1": "NOX1", "entity2": "phenolic acids", "span1": [20, 24], "span2": [185, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6944": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "ibuprofen", "span1": [81, 86], "span2": [131, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12058": {"label": 2, "data": {"text": "Sustained resistance to acute MPTP toxicity by hypothalamic dopamine neurons following chronic neurotoxicant exposure is associated with sustained up-regulation of parkin protein.", "entity1": "parkin", "entity2": "MPTP", "span1": [164, 170], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13519": {"label": 0, "data": {"text": "The active site coordination of CDO comprises a mononuclear iron ligated by the Nepsilon atoms of three protein-derived histidines, thus representing a new variant on the 2-histidine-1-carboxylate (2H1C) facial triad motif.", "entity1": "CDO", "entity2": "histidines", "span1": [32, 35], "span2": [120, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2306": {"label": 2, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "JNK", "entity2": "U0126", "span1": [158, 161], "span2": [17, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3293": {"label": 3, "data": {"text": "Rasagiline is a novel, potent, and irreversible monoamine oxidase type B (MAO-B) inhibitor which has been approved for treatment of PD.", "entity1": "MAO-B", "entity2": "Rasagiline", "span1": [74, 79], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15360": {"label": 9, "data": {"text": "Neither oxycodone nor its metabolites activated PXR, CAR, or AhR.", "entity1": "CAR", "entity2": "oxycodone", "span1": [53, 56], "span2": [8, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3684": {"label": 2, "data": {"text": "Both tolbutamide and gliclazide stimulated phospholipase C activity; however, only gliclazide did so independently of its activity at K(ATP) channels, and this activity was partially inhibited by pertussis toxin.", "entity1": "K(ATP) channels", "entity2": "gliclazide", "span1": [134, 149], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14658": {"label": 9, "data": {"text": "Genistein had no effect on resting intracellular [Ca(2+)] or thrombin-induced increase in Ca(2+) mobilization.", "entity1": "thrombin", "entity2": "Genistein", "span1": [61, 69], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4821": {"label": 1, "data": {"text": "Degradation of MAC13243 and studies of the interaction of resulting thiourea compounds with the lipoprotein targeting chaperone LolA.", "entity1": "lipoprotein", "entity2": "thiourea", "span1": [96, 107], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9990": {"label": 3, "data": {"text": "When the anti-corticosterone drug aminoglutethimide (CYP11A1 inhibitor) was administered to B16F10 mice, corticosterone levels in splenic tissue or serum and CYP11A1 mRNA expression were decreased at 14 days after tumor inoculation.", "entity1": "CYP11A1", "entity2": "aminoglutethimide", "span1": [53, 60], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15380": {"label": 8, "data": {"text": "The human cytosolic sulfotransferase hSULT2A1 catalyzes the sulfation of a broad range of xenobiotics, as well as endogenous hydroxysteroids and bile acids.", "entity1": "human cytosolic sulfotransferase hSULT2A1", "entity2": "hydroxysteroids", "span1": [4, 45], "span2": [125, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14105": {"label": 1, "data": {"text": "Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.", "entity1": "Cereblon", "entity2": "lenalidomide", "span1": [0, 8], "span2": [93, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12023": {"label": 1, "data": {"text": "Using electrophysiologic techniques, the present study assessed the in vivo action of brexpiprazole on serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, and 5-HT2A; dopamine (DA) D2 autoreceptors, and alpha1- and alpha2-adrenergic receptors.", "entity1": "dopamine (DA) D2 autoreceptors", "entity2": "brexpiprazole", "span1": [166, 196], "span2": [86, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5170": {"label": 1, "data": {"text": "Results of RT-PCR analysis showed decrease of p53 mRNA level and no significant difference in Bcl-2 and Bax mRNA expressions in DEX-treated rats.", "entity1": "Bcl-2", "entity2": "DEX", "span1": [94, 99], "span2": [128, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15719": {"label": 8, "data": {"text": "d-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor.", "entity1": "d-Amino acid oxidase", "entity2": "d-amino acids", "span1": [0, 20], "span2": [55, 68]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15239": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP2B1", "entity2": "silybin B", "span1": [24, 31], "span2": [214, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"14262": {"label": 8, "data": {"text": "By contrast, 1,12-diamino-3,6,9-triazadodecane(SpmTrien), a charge-deficient spermine analog, was an extremely poor substrate of human recombinant SSAT2 and was metabolized by SSAT1 in HEPG2 cells and in wild-type primary hepatocytes.", "entity1": "human recombinant SSAT2", "entity2": "SpmTrien", "span1": [129, 152], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11950": {"label": 8, "data": {"text": "A high throughput assay for the glucuronidation of 7-hydroxy-4-trifluoromethylcoumarin by recombinant human UDP-glucuronosyltransferases and liver microsomes.", "entity1": "human UDP-glucuronosyltransferases", "entity2": "7-hydroxy-4-trifluoromethylcoumarin", "span1": [102, 136], "span2": [51, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2864": {"label": 8, "data": {"text": "4-Hydroxynonenal (4-HNE) is a mutagenic alpha,beta-unsaturated aldehyde produced during oxidative injury that is conjugated by several glutathione S-transferase (GST) isoforms.", "entity1": "glutathione S-transferase", "entity2": "alpha,beta-unsaturated aldehyde", "span1": [135, 160], "span2": [40, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4025": {"label": 0, "data": {"text": "Kisspeptin is a 54-amino acid peptide which is encoded by the KiSS-1 gene and activates the G protein-coupled receptor GPR54.", "entity1": "Kisspeptin", "entity2": "amino acid", "span1": [0, 10], "span2": [19, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13570": {"label": 1, "data": {"text": "A humanized antibody to HER2/neu, trastuzumab, is now FDA approved for the treatment of early stage, HER2/neu overexpressing breast cancer sequenced with chemotherapy including doxorubicin, cyclophosphamide, and paclitaxel.", "entity1": "neu", "entity2": "cyclophosphamide", "span1": [106, 109], "span2": [190, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"692": {"label": 1, "data": {"text": "Combined concentration-ratio analysis demonstrated that tamsulosin, which does not discriminate between alpha 1A- and alpha 1L-adrenoceptors, and RS-17053 competed for binding at the same site in the SMA.", "entity1": "alpha 1L-adrenoceptors", "entity2": "RS-17053", "span1": [118, 140], "span2": [146, 154]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13203": {"label": 7, "data": {"text": "Herein, comparative genomics and experimental analyses revealed that the mammalian Sec synthase (SecS) is the previously identified pyridoxal phosphate-containing protein known as the soluble liver antigen.", "entity1": "SecS", "entity2": "pyridoxal phosphate", "span1": [97, 101], "span2": [132, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5772": {"label": 2, "data": {"text": "Resistance of TIDA neurons to MPTP toxicity was correlated with a transient increase in UCHL-1 and a sustained elevation in parkin in the arcuate nucleus.", "entity1": "parkin", "entity2": "MPTP", "span1": [124, 130], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14349": {"label": 3, "data": {"text": "mRNA levels of receptor activator of nuclear factor kappa-B (RANK), its ligand RANKL, tumor necrosis factor alpha (TNF-\u03b1) and RANKL/osteoprotegerin (OPG) ratio were diminished in the periodontium of CCL3(-/-) mice and in the group treated with Met-RANTES.", "entity1": "RANK", "entity2": "Met", "span1": [61, 65], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11378": {"label": 8, "data": {"text": "We conclude that Met564 blocks the entry of medium- and long-chain acyl-CoAs to the catalytic site of CrAT.", "entity1": "CrAT", "entity2": "acyl-CoAs", "span1": [102, 106], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1695": {"label": 3, "data": {"text": "BACKGROUND: Rivastigmine is a carbamate drug designed to inhibit both acetylcholinesterase and butyrylcholinesterase by reversibly covalently bonding to these enzymes.", "entity1": "acetylcholinesterase", "entity2": "Rivastigmine", "span1": [70, 90], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10489": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "metoprolol", "span1": [392, 423], "span2": [265, 275]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2789": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "NK1-R", "entity2": "sodium hydrosulphide", "span1": [258, 263], "span2": [119, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10959": {"label": 3, "data": {"text": "Effects of granulocyte colony-stimulating factor (G-CSF) and neutrophil elastase inhibitor (ONO-5046) on acid-induced lung injury in rats.", "entity1": "neutrophil elastase", "entity2": "ONO-5046", "span1": [61, 80], "span2": [92, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2122": {"label": 2, "data": {"text": "The positive correlation between vitamin A and immunoglobulin A concentrations might be the result of the vitamin A inductive effect during immunoglobulins A synthesis.", "entity1": "immunoglobulin A", "entity2": "vitamin A", "span1": [47, 63], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"311": {"label": 5, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "5-HT2 receptor", "entity2": "ketanserin", "span1": [92, 106], "span2": [118, 128]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"78": {"label": 3, "data": {"text": "Aspirin (ASA) and other non-steroidal anti-inflammatory drugs, which are cyclooxygenase (COX) inhibitors, precipitate asthmatic attacks in ASA-intolerant patients, while sodium salicylate, hardly active on COX by itself, is well tolerated by these patients.", "entity1": "COX", "entity2": "ASA", "span1": [89, 92], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11061": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "prednisone", "span1": [89, 95], "span2": [225, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6717": {"label": 1, "data": {"text": "STI571 binding to Flt3 is prevented by the phenylalanine 691 side-chain in the ATP binding center and mutating this site to threonine renders the corresponding Flt3 mutant sensitive to STI571.", "entity1": "Flt3", "entity2": "STI571", "span1": [18, 22], "span2": [0, 6]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2755": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "Val-349 to Ile", "entity2": "2,6-dichloro", "span1": [17, 31], "span2": [92, 104]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10760": {"label": 1, "data": {"text": "Together, these results suggested that imatinib affects EGFR activation and signaling pathways through rapid release and increased expression of endogenous EGFR-activating ligands.", "entity1": "EGFR", "entity2": "imatinib", "span1": [56, 60], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9718": {"label": 3, "data": {"text": "Plasma BuChE activity was significantly lower after rivastigmine than after placebo, but this was not clinically relevant.", "entity1": "BuChE", "entity2": "rivastigmine", "span1": [7, 12], "span2": [52, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11960": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "PIP5K1B", "entity2": "phosphatidylinositol-4,5-bisphosphate", "span1": [0, 7], "span2": [213, 250]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5069": {"label": 5, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "glucocorticoid receptor", "entity2": "RU486", "span1": [43, 66], "span2": [83, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2243": {"label": 3, "data": {"text": "Dasatinib (BMS-354825) is a novel orally bioavailable SRC/ABL inhibitor that has activity against multiple imatinib-resistant BCR-ABL isoforms in vitro that is presently showing considerable promise in early-phase clinical trials of chronic myeloid leukemia (CML).", "entity1": "ABL", "entity2": "BMS-354825", "span1": [58, 61], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4197": {"label": 3, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "Bcl-xL", "entity2": "PTE", "span1": [100, 106], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5300": {"label": 1, "data": {"text": "In addition, prunetin inhibits NF-\u03baB-dependent inflammatory responses by modulating I\u03baB kinase (IKK)-inhibitor \u03baB\u03b1 (I\u03baB\u03b1)-NF-\u03baB signaling.", "entity1": "inhibitor \u03baB\u03b1", "entity2": "prunetin", "span1": [101, 114], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7595": {"label": 1, "data": {"text": "Apo-alpha-lactalbumin, obtained by treatment with EDTA, displays one binding site for fatty acids, the association constants for oleic and palmitic acids being 1.9.10(6) and 4.2.10(5) M(-1), respectively.", "entity1": "Apo-alpha-lactalbumin", "entity2": "oleic and palmitic acids", "span1": [0, 21], "span2": [129, 153]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8550": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "histone deacetylase", "entity2": "benzene", "span1": [159, 178], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2914": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "NCX", "entity2": "cibenzoline", "span1": [129, 132], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5560": {"label": 3, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "NF-kappaB", "entity2": "GSH", "span1": [173, 182], "span2": [134, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2961": {"label": 1, "data": {"text": "Affinity of V782A for cGMP, vardenafil, sildenafil, tadalafil, or IBMX was reduced 5.5-, 23-, 10-, 3-, and 12-fold, respectively.", "entity1": "V782A", "entity2": "IBMX", "span1": [12, 17], "span2": [66, 70]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15926": {"label": 1, "data": {"text": "Interestingly, polySia chains of secreted NCAM neutralized the cytotoxic activity of extracellular histones as well as DNA/histone-network-containing \"neutrophil extracellular traps\", which are formed during invasion of microorganisms.", "entity1": "histones", "entity2": "polySia", "span1": [99, 107], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13002": {"label": 1, "data": {"text": "We show here that IP1 can be used as a surrogate of IP3 to monitor GPCR activation.", "entity1": "GPCR", "entity2": "IP1", "span1": [67, 71], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3465": {"label": 8, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "human dopamine transporter", "entity2": "[(3)H] dopamine", "span1": [167, 193], "span2": [108, 123]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4829": {"label": 2, "data": {"text": "Thus, in 158N cells, the ability of oxysterols to trigger a mode of cell death by apoptosis involving GSK-3 and caspase-3 activation is independent of the increase in the Ca(2+) level and of their accumulation in lipid raft microdomains.", "entity1": "GSK-3", "entity2": "oxysterols", "span1": [102, 107], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15963": {"label": 2, "data": {"text": "17\u03b2-Estradiol (E2) has been recently shown to induce cyclin E processing in breast cancer cells.", "entity1": "cyclin E", "entity2": "17\u03b2-Estradiol", "span1": [53, 61], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3027": {"label": 1, "data": {"text": "Taxanes with affinities for microtubules well above their affinities for P-glycoprotein are shown not to be affected by multidrug resistance.", "entity1": "microtubules", "entity2": "Taxanes", "span1": [28, 40], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11754": {"label": 1, "data": {"text": "Around five times as potent as the lead with an IC(50) of 33 \u03bcM for disruption of the Myc-Max heterodimer, JY-3-094 demonstrated excellent selectivity over Max-Max homodimers, with no apparent effect at 100 \u03bcM.", "entity1": "Max", "entity2": "JY-3-094", "span1": [90, 93], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6688": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "TRPM8", "entity2": "eucalyptol", "span1": [0, 5], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15466": {"label": 8, "data": {"text": "The present study demonstrated that human multidrug resistance-associated protein 3 vesicles accepted conjugated 3\u03b2-hydroxy-\u0394(5)-bile acids along with common bile acids such as glycocholic acid and taurolithocholic acid 3-sulfate.", "entity1": "human multidrug resistance-associated protein 3", "entity2": "glycocholic acid", "span1": [36, 83], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13410": {"label": 5, "data": {"text": "In summary, the therapeutic effect of clozapine in reversing PPI impairment was mimicked by the H(1) antagonist pyrilamine, while pyrilamine had a mixed effect on cognition.", "entity1": "H(1)", "entity2": "pyrilamine", "span1": [96, 100], "span2": [112, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12358": {"label": 3, "data": {"text": "Previous report demonstrated that thyroid hormone (TH) negatively regulates mouse SCD-1 gene promoter before SREBP-1c was revealed.", "entity1": "mouse SCD-1 gene promoter", "entity2": "thyroid hormone", "span1": [76, 101], "span2": [34, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11980": {"label": 8, "data": {"text": "Doxorubicin is mainly excreted into the bile via P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (Mrp2) in hepatobiliary route and metabolized via cytochrome P450 (CYP) 3A subfamily.", "entity1": "P-gp", "entity2": "Doxorubicin", "span1": [65, 69], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4166": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "p65", "entity2": "sesquiterpene", "span1": [180, 183], "span2": [109, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3350": {"label": 1, "data": {"text": "The high resolution NMR solution structure of the cTnC-cTnI-dfbp-o ternary complex showed that dfbp-o bound at the hydrophobic interface formed by cTnC and cTnI making critical interactions with residues such as Arg147 of cTnI.", "entity1": "cTnI", "entity2": "dfbp-o", "span1": [222, 226], "span2": [95, 101]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10913": {"label": 9, "data": {"text": "The inhibition of ERK, moreover, did not cause attenuation in mucin secretion in response to cAMP and forskolin.", "entity1": "mucin", "entity2": "forskolin", "span1": [62, 67], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11651": {"label": 1, "data": {"text": "The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone.", "entity1": "Cdx2", "entity2": "CDCA", "span1": [48, 52], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3452": {"label": 1, "data": {"text": "R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less.", "entity1": "Y156F", "entity2": "R-modafinil", "span1": [53, 58], "span2": [0, 11]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6671": {"label": 8, "data": {"text": "Ribonucleotide reductase (RR) is responsible for the de novo conversion of the ribonucleoside diphosphates to deoxyribonucleoside diphosphates, which are essential for DNA synthesis and repair.", "entity1": "RR", "entity2": "ribonucleoside diphosphates", "span1": [26, 28], "span2": [79, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15434": {"label": 0, "data": {"text": "We demonstrate that activation of STAT3 serine-727 and tyrosine-705 phosphorylations is promoted by B-RAF(V600E) activity and that the Mcl-1 promoter is dependent on a STAT consensus-site for B-RAF-mediated activation.", "entity1": "STAT3", "entity2": "tyrosine", "span1": [34, 39], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15881": {"label": 2, "data": {"text": "The Bcl2/Bax ratio increased and Mfn2 expression decreased in MIN6 cells after glucose stimulation.", "entity1": "Bax", "entity2": "glucose", "span1": [9, 12], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7946": {"label": 2, "data": {"text": "In contrast, activation of both ERK and CREB in the PFC was found following memory retrieval but not other processes in METH-treated mouse groups.", "entity1": "ERK", "entity2": "METH", "span1": [32, 35], "span2": [120, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1811": {"label": 3, "data": {"text": "In this study, we have synthesized novel alpha-hydroxyphenylamide analogues of diphenylhydantoin and examined their ability to inhibit human Na(V)1.5 sodium channels expressed in Chinese Hamster Ovary (CHO-K1) cells.", "entity1": "sodium channels", "entity2": "diphenylhydantoin", "span1": [150, 165], "span2": [79, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5888": {"label": 1, "data": {"text": "Using a similar procedure to analyze ODC labeled by reaction with [5-14C]DFMO, it was found that lysine 69 and cysteine 360 formed covalent adducts with the inhibitor.", "entity1": "ODC", "entity2": "[5-14C]DFMO", "span1": [37, 40], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"43": {"label": 3, "data": {"text": "In contrast to adrenaline and somatostatin, galanin, another inhibitor of insulin secretion, reduced Ca2+ currents by about 40% in a pertussis toxin-insensitive manner.", "entity1": "insulin", "entity2": "adrenaline", "span1": [74, 81], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1594": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine", "span1": [59, 64], "span2": [381, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13373": {"label": 3, "data": {"text": "Estrogen-regulated genes including cytokeratin 1-19 and Cyp2a4 were over-expressed, although Cyp3a25 was suppressed.", "entity1": "Cyp3a25", "entity2": "Estrogen", "span1": [93, 100], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13426": {"label": 1, "data": {"text": "High D-glucose increases L-arginine transport and eNOS expression following TbetaRII activation by TGF-beta1 involving p42/44(mapk) and Smad2 in HUVEC.", "entity1": "TGF-beta1", "entity2": "D-glucose", "span1": [99, 108], "span2": [5, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5804": {"label": 8, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "ACY-1", "entity2": "N-acylated L-amino acids", "span1": [101, 106], "span2": [216, 240]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15279": {"label": 5, "data": {"text": "A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists.", "entity1": "human CCR4", "entity2": "indazole arylsulfonamides", "span1": [71, 81], "span2": [12, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3247": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "ANE", "span1": [13, 16], "span2": [202, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10491": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "carvedilol", "span1": [392, 423], "span2": [289, 299]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3136": {"label": 3, "data": {"text": "These results suggest that fluoxetine inhibited the activity of VMAT2 by a mechanism different from that of reserpine and did not directly interact with the active site of VMAT2.", "entity1": "VMAT2", "entity2": "fluoxetine", "span1": [64, 69], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1689": {"label": 3, "data": {"text": "Moreover, recent in vitro studies suggest that memantine abrogates beta-amyloid (Abeta) toxicity and possibly inhibits Abeta production.", "entity1": "Abeta", "entity2": "memantine", "span1": [119, 124], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1546": {"label": 8, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "SMO", "entity2": "N(1)-acetylspermine", "span1": [15, 18], "span2": [64, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5809": {"label": 1, "data": {"text": "The reducing activity of alpha N-acetyl beta-endorphin-(1-31) upon morphine- and beta-endorphin-induced analgesia was not exhibited in mice undergoing treatment with pertussis toxin or N-ethylmaleimide, agents known to impair the function of Gi/Go transducer proteins.", "entity1": "Gi", "entity2": "N-ethylmaleimide", "span1": [242, 244], "span2": [185, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13212": {"label": 9, "data": {"text": "Triflusal (30 mg/kg) or aspirin treatment (30 mg/kg) did not reduce the levels of GFAP or Hsp27 immunostaining.", "entity1": "Hsp27", "entity2": "aspirin", "span1": [90, 95], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6617": {"label": 9, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "arginase", "entity2": "ornithine", "span1": [186, 194], "span2": [142, 151]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11027": {"label": 3, "data": {"text": "Further characterization showed that sorafenib suppresses both wild-type and V599E mutant B-Raf activity in vitro.", "entity1": "V599E", "entity2": "sorafenib", "span1": [77, 82], "span2": [37, 46]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8952": {"label": 3, "data": {"text": "The affinity labeling nucleotide analog, 5'-[p-(fluorosulfonyl)benzoyl]adenosine (FSA), inactivates the dehydrogenase and isomerase activities at similar rates in an irreversible manner which follows first order kinetics with respect to both time and alkylator concentration (0.2-0.6 mM).", "entity1": "dehydrogenase", "entity2": "5'-[p-(fluorosulfonyl)benzoyl]adenosine", "span1": [104, 117], "span2": [41, 80]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13025": {"label": 1, "data": {"text": "11Beta-HSD1 activates cortisone to cortisol to facilitate glucocorticoid receptor (GR)-mediated action.", "entity1": "GR", "entity2": "cortisone", "span1": [83, 85], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5073": {"label": 1, "data": {"text": "Here, we have now found that activation of p38 MAPK by anisomycin potentiated induction of CYP2B6 mRNA by CAR ligand in HepG2 cells to levels observed in ligand-treated human primary hepatocytes.", "entity1": "CAR", "entity2": "anisomycin", "span1": [106, 109], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6838": {"label": 1, "data": {"text": "However, MS A2756G was significantly associated with cobalamin levels (AA genotype: 290 +/- 122 pmol/l; AG: 381 +/- 151 pmol/l and GG: 415 +/- 100 pmol/l), as was MTRR A66G (AA: 478 +/- 219 pmol/l, AG: 306 +/- 124 pmol/l and GG: 306 +/- 123 pmol/l).", "entity1": "MS", "entity2": "cobalamin", "span1": [9, 11], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9313": {"label": 3, "data": {"text": "Finally, the three drugs were compared with the angiotensin converting enzyme inhibitor cilazapril.", "entity1": "angiotensin converting enzyme", "entity2": "cilazapril", "span1": [48, 77], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14235": {"label": 1, "data": {"text": "Therefore, we examined whether verrucarin A (VA) sensitize TRAIL-induced apoptosis in cancer cells by induction of ER stress.", "entity1": "TRAIL", "entity2": "verrucarin A", "span1": [59, 64], "span2": [31, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12355": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "mTRPV4", "entity2": "apomorphine", "span1": [47, 53], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3911": {"label": 1, "data": {"text": "To clarify the cause of age differences on selenite cataract formation in rats, mRNA expression of GPx1, MsrA and MsrB1, as well as GPx activity in Wistar rat lens at different ages were assayed, level of lipid peroxidation, extent of lens damage induced by sodium selenite and barricade function of blood-retinal barrier (BRB) were investigated.", "entity1": "MsrA", "entity2": "sodium selenite", "span1": [105, 109], "span2": [258, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5516": {"label": 2, "data": {"text": "In phosphotriesterase and physostigmine-treated mice, a 4- and 2-fold higher sarin dose, respectively, was needed to cause a 50% inhibition of brain AChE activity.", "entity1": "AChE", "entity2": "physostigmine", "span1": [149, 153], "span2": [26, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7641": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "5-nitro-2-(3-phenylpropylamino)benzoic acid", "span1": [34, 39], "span2": [250, 293]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1620": {"label": 3, "data": {"text": "The cytosine analog 5-aza-2'-deoxycytidine (decitabine) hypomethylates DNA by inhibiting DNA methyltransferase.", "entity1": "DNA methyltransferase", "entity2": "cytosine", "span1": [89, 110], "span2": [4, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2125": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "MCTs", "entity2": "monocarboxylates", "span1": [30, 34], "span2": [101, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12305": {"label": 1, "data": {"text": "Overall, the present study, using a different and more sensitive statistical model than the parent study, revealed a statistically significant dose-dependent correlation between cumulative exposure to Hg from dental amalgams and urinary levels of GST-\u03b1, after covariate adjustment; where as, a nonsignificant relationship was observed with urinary levels of GST-\u03c0.", "entity1": "GST-\u03c0", "entity2": "Hg", "span1": [358, 363], "span2": [201, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1280": {"label": 1, "data": {"text": "Rheumatoid synovial cells expressed PPARgamma mRNA, and the PPARgamma ligands 15-deoxy-Delta(12,14)-prostaglandin J(2) and troglitazone reduced the proliferation and induced apoptosis in synovial cells.", "entity1": "PPARgamma", "entity2": "15-deoxy-Delta(12,14)-prostaglandin J(2)", "span1": [36, 45], "span2": [78, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2776": {"label": 3, "data": {"text": "In the presence of the system L inhibitor BCH, Na(+)-dependent l-alanine uptake in WKY and SHR PTE cells was inhibited by alanine, serine, and cysteine, which is consistent with amino acid transport through ASCT2.", "entity1": "ASCT2", "entity2": "alanine", "span1": [207, 212], "span2": [122, 129]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12308": {"label": 1, "data": {"text": "Furthermore, elevations in blood neutrophil count, serum monocyte chemoattractant protein-1, and other markers of inflammation corresponded to GDC-0152 exposure and toxicity and thus may have utility as safety biomarkers.", "entity1": "monocyte chemoattractant protein-1", "entity2": "GDC-0152", "span1": [57, 91], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15344": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "acenaphthylene", "span1": [39, 48], "span2": [197, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13367": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "trefoil factor-1", "entity2": "estrogen", "span1": [101, 117], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15097": {"label": 3, "data": {"text": "Avibactam (formerly NXL104, AVE1330A) is a synthetic non-\u03b2-lactam, \u03b2-lactamase inhibitor that inhibits the activities of Ambler class A and C \u03b2-lactamases and some Ambler class D enzymes.", "entity1": "\u03b2-lactamase", "entity2": "AVE1330A", "span1": [67, 78], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14809": {"label": 4, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1)", "entity2": "AM4054", "span1": [266, 271], "span2": [285, 291]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15369": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "polymorphic retinoic acid (RA) response elements", "entity2": "all-trans retinoic acid", "span1": [246, 294], "span2": [82, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11822": {"label": 2, "data": {"text": "Moreover, curcumin alleviated Sim2 expression, and reversely raised Drebrin expression in neurons treated with hyperglycaemia.", "entity1": "Sim2", "entity2": "curcumin", "span1": [30, 34], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7312": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "ASCT2", "entity2": "4-methoxy-7-nitroindolinyl", "span1": [217, 222], "span2": [95, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15765": {"label": 9, "data": {"text": "Both ICI treatments, induced a significant decrease (p<0.01) in uterine estrogen receptor alpha (ER\u03b1) content, had no effect on uterine progesterone receptor (PR) protein expression and caused marked nuclear localization of cyclin D1, in both luminal and glandular uterine epithelium, as compared to vehicle-treated animals.", "entity1": "PR", "entity2": "ICI", "span1": [159, 161], "span2": [5, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15923": {"label": 1, "data": {"text": "Interestingly, polySia chains of secreted NCAM neutralized the cytotoxic activity of extracellular histones as well as DNA/histone-network-containing \"neutrophil extracellular traps\", which are formed during invasion of microorganisms.", "entity1": "NCAM", "entity2": "polySia", "span1": [42, 46], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5135": {"label": 3, "data": {"text": "5-Hydroxy-3,6,7,8,3'4'-hexamethoxyflavone inhibits nitric oxide production in lipopolysaccharide-stimulated BV2 microglia via NF-\u03baB suppression and Nrf-2-dependent heme oxygenase-1 induction.", "entity1": "NF-\u03baB", "entity2": "5-Hydroxy-3,6,7,8,3'4'-hexamethoxyflavone", "span1": [126, 131], "span2": [0, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3881": {"label": 3, "data": {"text": "Transduction with constitutively active forms of GSK-3\u03b2 could protect against the downregulation of p65 and upregulation of cleaved-PARP that are induced by cinobufagin treatment.", "entity1": "p65", "entity2": "cinobufagin", "span1": [100, 103], "span2": [157, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9799": {"label": 3, "data": {"text": "With respect to the substrate dihydroorotate, atovaquone was an uncompetitive inhibitor of human dihydroorotate dehydrogenase (Kiu = 11.6 microM) and a non-competitive inhibitor of the rat enzyme (Kiu = 905/ Kic = 1,012 nM).", "entity1": "human dihydroorotate dehydrogenase", "entity2": "atovaquone", "span1": [91, 125], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4035": {"label": 8, "data": {"text": "Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4).", "entity1": "Leukotriene A(4) hydrolase", "entity2": "LTB(4)", "span1": [0, 26], "span2": [124, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1268": {"label": 3, "data": {"text": "Minocycline inhibits cytochrome c release and delays progression of amyotrophic lateral sclerosis in mice.", "entity1": "cytochrome c", "entity2": "Minocycline", "span1": [21, 33], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7406": {"label": 8, "data": {"text": "Bile acid coenzyme A:amino acid N-acyltransferase (BAT) is responsible for the amidation of bile acids with the amino acids glycine and taurine.", "entity1": "Bile acid coenzyme A:amino acid N-acyltransferase", "entity2": "bile acids", "span1": [0, 49], "span2": [92, 102]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13618": {"label": 1, "data": {"text": "One is that the binding of retinoids to nuclear retinoic acid receptors (RARs) does not match their therapeutic efficacy: acitretin activates the three receptor subtypes, RAR-alpha, -beta and -gamma, without measurable receptor binding, whereas tazarotene preferentially binds to and activates RAR-beta and -gamma in preference to RAR-alpha.", "entity1": "retinoic acid receptors", "entity2": "retinoids", "span1": [48, 71], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1884": {"label": 9, "data": {"text": "I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance.", "entity1": "C1b domain", "entity2": "I3A", "span1": [62, 72], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3735": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates induce apoptosis of hematopoietic tumor cells via inhibition of Ras signaling pathways and Bim-mediated activation of the intrinsic apoptotic pathway.", "entity1": "Ras", "entity2": "bisphosphonates", "span1": [100, 103], "span2": [20, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"235": {"label": 1, "data": {"text": "In all cases at both the 5-HT2A and 5-HT2C receptors, the affinities of the isomers of MDMA and MDA were at least 2-3 orders of magnitude less than 5-HT.", "entity1": "5-HT2A", "entity2": "MDMA", "span1": [25, 31], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12581": {"label": 0, "data": {"text": "PC3 is a type I proinsulin-processing enzyme that initiates the sequential processing of proinsulin to insulin by cleaving the proinsulin molecule on the COOH-terminal side of the dibasic peptide, Arg31-Arg32, joining the B-chain and C-peptide.", "entity1": "proinsulin", "entity2": "C", "span1": [89, 99], "span2": [234, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1416": {"label": 4, "data": {"text": "RESULTS: In drug discrimination studies, lisuride fully mimicked the 5-HT(1A) agonist LY 293284, only partially substituted for LSD and DOI, and failed to substitute for (+)-amphetamine.", "entity1": "5-HT(1A)", "entity2": "lisuride", "span1": [69, 77], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4746": {"label": 8, "data": {"text": "We conclude that mPGES1 mediates acid-induced increase in PGE2 production and cell proliferation.", "entity1": "mPGES1", "entity2": "PGE2", "span1": [17, 23], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7741": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "vascular endothelial growth factor receptor 2", "entity2": "cabozantinib", "span1": [60, 105], "span2": [16, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9065": {"label": 1, "data": {"text": "Their histamine H1 receptor binding affinities indicate that metabolites may contribute to the sedative effects of chlorpromazine and levomepromazine.", "entity1": "histamine H1 receptor", "entity2": "levomepromazine", "span1": [6, 27], "span2": [134, 149]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15789": {"label": 0, "data": {"text": "Phosphorylation on Ser and Thr residues of pannexin1 was increased during potentiation, possibly mediating HC opening.", "entity1": "pannexin1", "entity2": "Thr", "span1": [43, 52], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14962": {"label": 1, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANK", "entity2": "cysteine", "span1": [158, 162], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4100": {"label": 3, "data": {"text": "Furthermore, treatment with spironoclactone not only attenuated the pro-apoptotic effect of ALD but reversed the ALD-induced increase of calpain and AIF levels.", "entity1": "AIF", "entity2": "spironoclactone", "span1": [149, 152], "span2": [28, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4460": {"label": 3, "data": {"text": "However, after 12h CdCl2 treatment, cell viability diminished in 50%, accompanied by a drastic decrease of metallothionein-II production, and an increase in p53 activation and the pro-apoptotic protein Bax.", "entity1": "metallothionein-II", "entity2": "CdCl2", "span1": [107, 125], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2259": {"label": 2, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "nuclear pregnane X receptor", "entity2": "rifampicin", "span1": [70, 97], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7886": {"label": 8, "data": {"text": "The altered activities of key enzymes such as glucose-6-phosphatase and fructose-1,6-bisphosphatase of carbohydrate metabolism significantly (p<0.05) increased whereas hexokinase, pyruvate kinase, glucose-6-phosphate dehydrogenase and glycogen content significantly (p<0.05) decreased in the liver of diabetic rats and also increased activities of aspartate transaminase (AST), alanine transaminase (ALT) and alkaline phosphatase (ALP).", "entity1": "fructose-1,6-bisphosphatase", "entity2": "carbohydrate", "span1": [72, 99], "span2": [103, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1742": {"label": 8, "data": {"text": "CPT I (carnitine palmitoyltransferase I) catalyses the conversion of palmitoyl-CoA into palmitoylcarnitine in the presence of L-carnitine, facilitating the entry of fatty acids into mitochondria.", "entity1": "carnitine palmitoyltransferase I", "entity2": "palmitoylcarnitine", "span1": [7, 39], "span2": [88, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"3152": {"label": 4, "data": {"text": "Thus, amitriptyline acts as a TrkA and TrkB agonist and possesses marked neurotrophic activity.", "entity1": "TrkA", "entity2": "amitriptyline", "span1": [30, 34], "span2": [6, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4142": {"label": 3, "data": {"text": "The therapeutic potential of directly inhibiting prosurvival proteins was unveiled with the development of navitoclax, a selective inhibitor of both BCL-2 and BCL-2-like 1 (BCL-X(L)), which has shown clinical efficacy in some BCL-2-dependent hematological cancers.", "entity1": "BCL-X(L)", "entity2": "navitoclax", "span1": [173, 181], "span2": [107, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4697": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "TCDD", "span1": [111, 117], "span2": [72, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3653": {"label": 1, "data": {"text": "Additionally, CYP2E1 increased the apparent K(M) of CYP2B4 for BNZ by 8-fold and the apparent K(M) did not decrease to its original value when saturating concentrations of CPR were used.", "entity1": "CYP2B4", "entity2": "BNZ", "span1": [52, 58], "span2": [63, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8847": {"label": 3, "data": {"text": "Herein, we investigated the effect of a natural neuroprotective flavonoid, calycopterin, on H2O2-induced disruption of phase II detoxifying enzyme system and cAMP response element binding protein (CREB) phosphorylation.", "entity1": "phase II detoxifying enzyme", "entity2": "H2O2", "span1": [119, 146], "span2": [92, 96]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4896": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "sulfatase", "entity2": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate", "span1": [162, 171], "span2": [0, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11037": {"label": 2, "data": {"text": "Analysis of tumour-conditioned medium indicated that bexarotene decreased the secretion of angiogenic factors and matrix metalloproteinases and increased the tissue inhibitor of matrix metalloproteinases.", "entity1": "matrix metalloproteinases", "entity2": "bexarotene", "span1": [178, 203], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10129": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "rofecoxib", "span1": [34, 37], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11295": {"label": 8, "data": {"text": "BACKGROUND & AIMS: Of the 2 genes (MAT1A, MAT2A) encoding methionine adenosyltransferase, the enzyme that synthesizes S-adenosylmethionine, MAT1A, is expressed in liver, whereas MAT2A is expressed in extrahepatic tissues.", "entity1": "MAT2A", "entity2": "S-adenosylmethionine", "span1": [42, 47], "span2": [118, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11820": {"label": 1, "data": {"text": "The expression pattern of Sim2 and Drebrin correspond to 50mmol/L glucose (hyperglycaemia) was also found in primary cultured neurons.", "entity1": "Sim2", "entity2": "glucose", "span1": [26, 30], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9275": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "spiperone", "span1": [166, 186], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4848": {"label": 3, "data": {"text": "Cucurbitacin I inhibits rac1 activation in breast cancer cells by a reactive oxygen species-mediated mechanism and independently of janus tyrosine kinase 2 and p-rex1.", "entity1": "rac1", "entity2": "Cucurbitacin I", "span1": [24, 28], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6186": {"label": 5, "data": {"text": "These data indicate that mixed 5-HT1/5-HT2 receptor antagonists such as pizotifen and methysergide, and mixed 5-HT and catecholamine antagonists such as mianserin and mirtazapine are more potent antagonists of mCPP-induced behavioural inhibition in rats than the more selective 5-HT2A/5-HT2C antagonist ritanserin.", "entity1": "5-HT2A", "entity2": "ritanserin", "span1": [278, 284], "span2": [303, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7924": {"label": 8, "data": {"text": "The uptake of copper by both cultured rat DRG neurons and HEK/rCtr1 cells was saturable and inhibited by cold temperature, silver and zinc, consistent with it being mediated by rCtr1.", "entity1": "rCtr1", "entity2": "copper", "span1": [62, 67], "span2": [14, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3855": {"label": 0, "data": {"text": "The cDNAs of the full-length version of Ves a 1s revealed that the Ves a 1 gene consists of a 1005-bp ORF, which encodes 334 amino acid residues, and 67- and 227-bp 5' and 3' UTRs, respectively.", "entity1": "Ves a 1s", "entity2": "amino acid", "span1": [40, 48], "span2": [125, 135]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8438": {"label": 1, "data": {"text": "The endogenous steroid lithocholic acid (LCA) dilates cerebral arteries via BK channel activation, which requires recognition by a BK \u03b21 site that includes Thr169.", "entity1": "BK channel", "entity2": "steroid", "span1": [76, 86], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8784": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "GSK3\u03b2", "entity2": "CAPE", "span1": [115, 120], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14747": {"label": 2, "data": {"text": "Furthermore, we found that arsenic trioxide activates the Pirh2 promoter and consequently induces Pirh2 expression.", "entity1": "Pirh2", "entity2": "arsenic trioxide", "span1": [98, 103], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10921": {"label": 3, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "tyrosine kinase", "entity2": "PP2", "span1": [117, 132], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3946": {"label": 3, "data": {"text": "Inhibition by phenformin of oxygen consumption via complex I respiration in isolated rat liver mitochondria was greater than that in heart mitochondria, whereas inhibitory effect of phenformin on complex I respiration was similar in inside-out structured submitochondrial particles prepared from rat livers and hearts.", "entity1": "complex I", "entity2": "phenformin", "span1": [196, 205], "span2": [182, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1550": {"label": 8, "data": {"text": "Even though the activities of MAT and GNMT were elevated, the concentration of liver S-adenosylmethionine was decreased (24%, p<0.001) and S-adenosylhomocysteine increased (113%, p<0.001) in the dwarf mice.", "entity1": "MAT", "entity2": "S-adenosylhomocysteine", "span1": [30, 33], "span2": [139, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3177": {"label": 2, "data": {"text": "We investigated the involvement of the farnesoid X receptor (FXR), a nuclear receptor for bile acids, in the chenodeoxycholic acid (CDCA)-induced expression of Cdx2 and MUC2 in normal rat gastric epithelial cells (RGM-1 cells).", "entity1": "Cdx2", "entity2": "chenodeoxycholic acid", "span1": [160, 164], "span2": [109, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4863": {"label": 2, "data": {"text": "Saturated palmitic and stearic acids increased ceramides, up-regulated PTP1B, and had AKt and PTP1B phosphorylation at Ser 50 impaired.", "entity1": "PTP1B", "entity2": "palmitic and stearic acids", "span1": [94, 99], "span2": [10, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8390": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "catalase", "entity2": "Cd", "span1": [144, 152], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7436": {"label": 4, "data": {"text": "Dopamine D1 receptor agonist and D2 receptor antagonist effects of the natural product (-)-stepholidine: molecular modeling and dynamics simulations.", "entity1": "Dopamine D1 receptor", "entity2": "(-)-stepholidine", "span1": [0, 20], "span2": [87, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12124": {"label": 9, "data": {"text": "In addition, the stereospecificity required at opioid receptors appears to be retained at the nociceptin receptor, since (+)-quadazocine is inactive at both receptors.", "entity1": "opioid receptors", "entity2": "(+)-quadazocine", "span1": [47, 63], "span2": [121, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12688": {"label": 8, "data": {"text": "As with GABA, the metabolism of alanine involves a pyridoxal phosphate-dependent transaminase.", "entity1": "pyridoxal phosphate-dependent transaminase", "entity2": "alanine", "span1": [51, 93], "span2": [32, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4787": {"label": 3, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP3A", "entity2": "baicalin", "span1": [148, 153], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11695": {"label": 2, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "NF-\u03baB", "entity2": "pioglitazone", "span1": [185, 190], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3069": {"label": 3, "data": {"text": "The effects of PLZ on both amino acids and their transaminases were blocked by pre-treatment with the MAO inhibitor tranylcypromine.", "entity1": "transaminases", "entity2": "tranylcypromine", "span1": [49, 62], "span2": [116, 131]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14988": {"label": 2, "data": {"text": "Furthermore, a mixture of isoflavonoid parent compounds, and a mixture of isoflavonoid metabolites were found to have PPAR\u03b3 activating abilities.", "entity1": "PPAR\u03b3", "entity2": "isoflavonoid", "span1": [118, 123], "span2": [74, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15148": {"label": 1, "data": {"text": "However, there were detectable concentrations of Lhcgr, Cyp11a1 and Cyp17a1 mRNAs but undetectable concentrations of Insl3, Hsd17b3 and Hsd11b1 in the DEHP-treated testes, indicating that these 3\u03b2-HSD(pos) cells were newly formed progenitor Leydig cells.", "entity1": "Cyp11a1", "entity2": "DEHP", "span1": [56, 63], "span2": [151, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5514": {"label": 4, "data": {"text": "The present findings indicate that dezocine shares similar stimulus effects with both mu and delta agonists, its stimulus effects are reversed by mu-selective antagonists, and its rate-decreasing effects are not mediated by activity at mu, kappa or delta opioid receptors.", "entity1": "mu and delta", "entity2": "dezocine", "span1": [86, 98], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6956": {"label": 1, "data": {"text": "[125I]-MIP-1beta bound with similar high affinity to CCR5 from macaque (K(d) = 0.24 +/- 0.05 nM) and human (K(d) = 0.23 +/- 0.05 nM) and with similar kinetic properties.", "entity1": "CCR5", "entity2": "125I", "span1": [53, 57], "span2": [1, 5]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10303": {"label": 3, "data": {"text": "Sildenafil exhibits inhibitory potency against PDE5 and a 10-fold lower dose-related inhibitory potency against rod outer segment PDE6, the predominant PDE in the phototransduction cascade in rods.", "entity1": "PDE6", "entity2": "Sildenafil", "span1": [130, 134], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3016": {"label": 3, "data": {"text": "Inhibitor of cGMP-specific PDE5 (zaprinast; 0.1-10 microM) did not affect eosinophil apoptosis and only slightly increased spontaneous neutrophil apoptosis.", "entity1": "cGMP-specific PDE5", "entity2": "zaprinast", "span1": [13, 31], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6850": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "A2756G", "entity2": "Hcy", "span1": [169, 175], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4888": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "bile acid", "span1": [83, 86], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6731": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "SU11248", "span1": [273, 279], "span2": [152, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14611": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "DCK", "entity2": "dFdC", "span1": [66, 69], "span2": [230, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2026": {"label": 3, "data": {"text": "CONCLUSION: Oral quinidine is effective in suppressing the gain of function in IKr responsible for some cases of short QT syndrome with a mutation in HERG and thus restoring normal rate dependence of the QT interval and rendering ventricular tachycardia/ventricular fibrillation noninducible.", "entity1": "IKr", "entity2": "quinidine", "span1": [79, 82], "span2": [17, 26]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6329": {"label": 3, "data": {"text": "Citalopram protected against the RTI-76-induced inhibition of SERT binding.", "entity1": "SERT", "entity2": "RTI-76", "span1": [62, 66], "span2": [33, 39]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5543": {"label": 2, "data": {"text": "CONCLUSION: Oral treatment of healthy volunteers with triflusal stimulated NO production and eNOS protein expression in their neutrophils.", "entity1": "eNOS", "entity2": "triflusal", "span1": [93, 97], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11649": {"label": 8, "data": {"text": "These results strongly suggest that ABCA1 is substantially involved in hepatic alpha-tocopherol secretion.", "entity1": "ABCA1", "entity2": "alpha-tocopherol", "span1": [36, 41], "span2": [79, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6909": {"label": 8, "data": {"text": "PSMA acts as a glutamate carboxypeptidase (GCPII) on small molecule substrates, including folate, the anticancer drug methotrexate, and the neuropeptide N-acetyl-l-aspartyl-l-glutamate.", "entity1": "glutamate carboxypeptidase", "entity2": "folate", "span1": [15, 41], "span2": [90, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15873": {"label": 3, "data": {"text": "The selective CaMKII\u03b1 inhibitor KN-62 reversed the blockade produced by ionomycin and K(+)-depolarization.", "entity1": "CaMKII\u03b1", "entity2": "KN-62", "span1": [14, 21], "span2": [32, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1339": {"label": 4, "data": {"text": "Dexamethasone (DEX), betamethasone (BM), and their esterified-derivatives had full transrepression agonistic activity in a reporter assay using CV-1 cells transfected with either human or rat GR.", "entity1": "human or rat GR", "entity2": "DEX", "span1": [179, 194], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14708": {"label": 3, "data": {"text": "Inhibition of Th1/Th17 responses via suppression of STAT1 and STAT3 activation contributes to the amelioration of murine experimental colitis by a natural flavonoid glucoside icariin.", "entity1": "STAT1", "entity2": "flavonoid", "span1": [52, 57], "span2": [155, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4600": {"label": 8, "data": {"text": "In relation to zinc bioavailability, \u03b1-CPPs, \u03b2-CPPs, \u03b1(s1)-CN(64-74)4P and \u03b2-CN(1-25)4P increased zinc uptake.", "entity1": "\u03b1-CPPs", "entity2": "zinc", "span1": [37, 43], "span2": [98, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15627": {"label": 3, "data": {"text": "Next, nobiletin significantly decreased the levels of phospho-ERK2 and phospho-Akt in ERK2 or Akt siRNA-transfected cells concomitantly with a marked reduction on cell invasion and migration.", "entity1": "phospho-Akt", "entity2": "nobiletin", "span1": [71, 82], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5449": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "PSA", "entity2": "juglone", "span1": [135, 138], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11166": {"label": 8, "data": {"text": "To begin to examine whether these changes are mediated by alterations in gene expression for tryptophan hydroxylase (TPH), the rate-limiting enzyme in 5-HT biosynthesis, we quantitated its mRNA levels by competitive reverse transcription-polymerase chain reaction (RT-PCR).", "entity1": "TPH", "entity2": "5-HT", "span1": [117, 120], "span2": [151, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15255": {"label": 1, "data": {"text": "Selective oxidation of \u03c9-tertiary amine self-assembled thiol monolayers to tertiary amine N-oxides is shown to transform the adhesion of model proteins lysozyme and fibrinogen upon them.", "entity1": "fibrinogen", "entity2": "\u03c9-tertiary amine", "span1": [165, 175], "span2": [23, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2437": {"label": 0, "data": {"text": "The Turkish patient and her affected relatives all had a heterozygous A to G transition at codon 557 (AAG-->GAG) of exon 10 of MEN1 that results in a replacement of lysine by glutamic acid.", "entity1": "MEN1", "entity2": "lysine", "span1": [127, 131], "span2": [165, 171]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14642": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "cytidine deaminase", "entity2": "2',2'-difluorodeoxycytidine", "span1": [66, 84], "span2": [19, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14285": {"label": 9, "data": {"text": "In contrast, VPD had little effect on limb morphology and no significant effect on HDAC activity or the expression of marker genes.", "entity1": "HDAC", "entity2": "VPD", "span1": [83, 87], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4196": {"label": 3, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "STAT3", "entity2": "PTE", "span1": [42, 47], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14197": {"label": 1, "data": {"text": "In conclusion, these results suggest that CHOP may sensitize FRO ATC cells to SU5416 thereby inhibiting cell survival by modulating p21 and PI3K/Akt signal pathway.", "entity1": "PI3K", "entity2": "SU5416", "span1": [140, 144], "span2": [78, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3628": {"label": 4, "data": {"text": "Methanandamide (10.0 mg/kg) had lesser effect than other CB agonists, and the CB2 agonist AM1241 [1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole], the anandamide transport inhibitor AM404, and the CB antagonist rimonabant did not have diuretic effects.", "entity1": "CB2", "entity2": "AM404", "span1": [78, 81], "span2": [198, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"13349": {"label": 1, "data": {"text": "In addition, BALB/c and C57BL/6 females were treated with progesterone or MPA for 1 or 2 months, and mammary glands were excised for histologic studies and for immunohistochemical and Western blot evaluation of ER and PR.", "entity1": "PR", "entity2": "progesterone", "span1": [218, 220], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10340": {"label": 2, "data": {"text": "Induction of heat shock proteins (HSPs) by sodium arsenite in cultured astrocytes and reduction of hydrogen peroxide-induced cell death.", "entity1": "HSPs", "entity2": "sodium arsenite", "span1": [34, 38], "span2": [43, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"367": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "IL-5", "entity2": "DEX", "span1": [71, 75], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4348": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "GSK-3\u03b2", "entity2": "pinosylvin", "span1": [116, 122], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15478": {"label": 3, "data": {"text": "Upon nicotine pre-exposure, brain acetylcholinesterase increased, while monoamine oxidase (MAO) decreased.", "entity1": "MAO", "entity2": "nicotine", "span1": [91, 94], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8522": {"label": 8, "data": {"text": "A Nanogram Dose of the CYP3A Probe Substrate Midazolam to Evaluate Drug Interactions.", "entity1": "CYP3A", "entity2": "Midazolam", "span1": [23, 28], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12556": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "transcobalamin", "entity2": "[57Co]cyanocobalamin", "span1": [212, 226], "span2": [154, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15610": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "p38", "entity2": "galangin", "span1": [118, 121], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6883": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "Cystathionine-gamma-lyase", "entity2": "L-cysteine", "span1": [0, 25], "span2": [78, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"774": {"label": 3, "data": {"text": "Compared with WT, DeltaKPQ I(Na) was more sensitive to flecainide, and flecainide preferentially inhibited late I(Na) (mean current between 20 and 23.5 ms after depolarization) compared with peak I(Na).", "entity1": "DeltaKPQ", "entity2": "flecainide", "span1": [18, 26], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3086": {"label": 4, "data": {"text": "Ramelteon (Rozerem; Takeda Pharmaceutical Company Limited, Osaka, Japan) is an orally active, highly selective melatonin MT(1)/MT(2) receptor agonist.", "entity1": "MT(1)", "entity2": "Ramelteon", "span1": [121, 126], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"222": {"label": 2, "data": {"text": "Both 5 alpha-NET and 3 beta,5 alpha-NET blocked the PR down-regulation induced by P4 as assessed by Western and Northern blot methods.", "entity1": "PR", "entity2": "3 beta,5 alpha-NET", "span1": [52, 54], "span2": [21, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8974": {"label": 5, "data": {"text": "Using the alpha 1-adrenoceptor subtype-selective antagonists chlorethylclonidine (CEC), WB4101, and 5-methyl-urapidil, we have examined the possible heterogeneity in the alpha 1-adrenoceptor populations in rabbit aorta.", "entity1": "alpha 1-adrenoceptor", "entity2": "WB4101", "span1": [10, 30], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"300": {"label": 1, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "5-HT1B", "entity2": "(+/-)-pindolol", "span1": [351, 357], "span2": [372, 386]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4342": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "Akt", "entity2": "Pinosylvin", "span1": [204, 207], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6320": {"label": 3, "data": {"text": "We report that the radiation-induced activation of the kinase Cds1 [4] (also known as Chk2 [5]) is inhibited by caffeine in vivo and that ATM kinase activity is directly inhibited by caffeine in vitro.", "entity1": "kinase", "entity2": "caffeine", "span1": [55, 61], "span2": [112, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14024": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "NF-kappaB", "entity2": "colchicoside", "span1": [279, 288], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15976": {"label": 4, "data": {"text": "In the current study, we show that systematic modification of an aminoalkylindole scaffold identifies two new compounds with dual CB1R antagonist/CB2R agonist activity.", "entity1": "CB2R", "entity2": "aminoalkylindole", "span1": [146, 150], "span2": [65, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2668": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE7", "entity2": "5-nitro-2,N,N-trimethylbenzenesulfonamide", "span1": [300, 304], "span2": [317, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12160": {"label": 2, "data": {"text": "RESULTS: The density of AR in liver tissue in NP group was higher than that in control group (P < 0.05).", "entity1": "AR", "entity2": "NP", "span1": [24, 26], "span2": [46, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12638": {"label": 1, "data": {"text": "Although electrophysiological studies provide clues to the complex control of KATP channels by ATP, MgADP, and pharmacological agents, the molecular mechanism of KATP-channel regulation remains unclear.", "entity1": "KATP channels", "entity2": "ATP", "span1": [78, 91], "span2": [95, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"574": {"label": 2, "data": {"text": "Tomudex treatment resulted in the decrease in p27(kip1) expression, with an increase in cyclin E and cdk2 protein expression and kinase activities 24 h after a 2-h exposure.", "entity1": "cyclin E", "entity2": "Tomudex", "span1": [88, 96], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5813": {"label": 9, "data": {"text": "In six patients with Cushing's disease and one patient with secondary adrenal insufficiency due to hypothalamic failure, neither basal ACTH and cortisol levels nor CRH-stimulated levels were influenced by loperamide.", "entity1": "ACTH", "entity2": "loperamide", "span1": [135, 139], "span2": [205, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7688": {"label": 3, "data": {"text": "Sergliflozin etabonate, a selective SGLT2 inhibitor, improves glycemic control in streptozotocin-induced diabetic rats and Zucker fatty rats.", "entity1": "SGLT2", "entity2": "Sergliflozin etabonate", "span1": [36, 41], "span2": [0, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11710": {"label": 2, "data": {"text": "Based on these studies, the frequency of spontaneous tail contractions at 26 hpf - a developmental stage with minimal AChE expression and activity - was significantly higher following exposure to paraoxon concentrations as low as 31.2 nM.", "entity1": "AChE", "entity2": "paraoxon", "span1": [118, 122], "span2": [196, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15332": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "2,5,2',5'-tetrachlorobiphenyl", "span1": [287, 296], "span2": [160, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1067": {"label": 3, "data": {"text": "Troglitazone, a second ACS4 inhibitor, inhibited ACS activity <10% in microsomes and mitochondria and 45% in MAM.", "entity1": "ACS", "entity2": "Troglitazone", "span1": [49, 52], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14086": {"label": 9, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "Lenalidomide", "span1": [179, 183], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6212": {"label": 1, "data": {"text": "This study therefore characterized the binding of DF to the sigma receptors and NMDA-linked PCP sites and examined the anticonvulsant as well as locomotor effects of DF in mice in comparison with those of DM and DR. We found that DF, DM, and DR were relative high-affinity ligands at sigma-1 receptors (Ki=151, 205, 144 nM, respectively) while all of them were with low affinity at sigma-2 receptors (Ki=4-11 microM).", "entity1": "sigma-1 receptors", "entity2": "DM", "span1": [284, 301], "span2": [234, 236]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1681": {"label": 5, "data": {"text": "In membranes from HEK293 cells transfected with alpha2-receptors, etomidate inhibited binding of the alpha2-antagonist, [3H]RX821002, with higher potency from alpha2B- and alpha2C-receptors than from alpha2A-receptors (Ki alpha2A 208 microm, alpha2B 26 microm, alpha2C 56 microm).", "entity1": "alpha2A-receptors", "entity2": "[3H]RX821002", "span1": [200, 217], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2360": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "VEGFR", "entity2": "Sorafenib", "span1": [127, 132], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5039": {"label": 3, "data": {"text": "New classes of pyrrole-derived nitrooxyalkyl inverse esters, carbonates, and ethers (7-10) as COX-2 selective inhibitors and NO donors were synthesized and are herein reported.", "entity1": "COX-2", "entity2": "pyrrole", "span1": [94, 99], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9756": {"label": 5, "data": {"text": "In conclusion, the alpha(2)-AR antagonist properties of yohimbine increase DA and NAD levels both alone and in association with fluoxetine.", "entity1": "alpha(2)-AR", "entity2": "yohimbine", "span1": [19, 30], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7559": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "endothelial nitric oxide synthase", "entity2": "L-arginine", "span1": [123, 156], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"5572": {"label": 3, "data": {"text": "Carbonic anhydrase inhibitors: aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity.", "entity1": "Carbonic anhydrase", "entity2": "aromatic and heterocyclic sulfonamides", "span1": [0, 18], "span2": [31, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4969": {"label": 3, "data": {"text": "One exception is tranexamic acid (TXA), which, as a lysine mimetic, inhibits binding of plasminogen to fibrin.", "entity1": "fibrin", "entity2": "TXA", "span1": [103, 109], "span2": [34, 37]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6919": {"label": 9, "data": {"text": "We present our studies to demonstrate that HM74A, but not HM74, binds niacin at high affinities and effectively mediates Gi signaling events in human embryonic kidney HEK293 cells as well as in 3T3L1 adipocytes expressing HM74A.", "entity1": "HM74", "entity2": "niacin", "span1": [58, 62], "span2": [70, 76]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6836": {"label": 3, "data": {"text": "The objective of the present study was to compare the anti-inflammatory effects of the preferential COX-2 inhibitor etodolac with the non-selective COX inhibitor phenylbutazone in horses with lipopolysaccharide (LPS)-induced synovitis.", "entity1": "COX", "entity2": "phenylbutazone", "span1": [148, 151], "span2": [162, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13884": {"label": 3, "data": {"text": "Ibuprofen is a nonsteroidal anti-inflammatory drug widely used to relieve pain and inflammation in many disorders via inhibition of cyclooxygenases.", "entity1": "cyclooxygenases", "entity2": "Ibuprofen", "span1": [132, 147], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4205": {"label": 3, "data": {"text": "Taken together, PTE is a potent inhibitor of osteosarcoma cell growth that targets the JAK2/STAT3 signaling pathway.", "entity1": "STAT3", "entity2": "PTE", "span1": [92, 97], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11626": {"label": 8, "data": {"text": "Indoleamine 2,3-dioxygenase (IDO), a tryptophan catabolizing enzyme, has been implicated in the pathogenesis of various neurological disorders.", "entity1": "IDO", "entity2": "tryptophan", "span1": [29, 32], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3666": {"label": 3, "data": {"text": "The mRNA levels of microphthalmia-associated transcription factor (MITF) and its downstream genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 were reduced by artemisinic acid treatment.", "entity1": "TRP-2", "entity2": "artemisinic acid", "span1": [150, 155], "span2": [172, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8874": {"label": 9, "data": {"text": "TCDD treatment of the cells largely prevented the activation of eukaryotic translation initiation factor 4E-binding protein 1, a regulator of translation initiation and substrate of the mammalian target of rapamycin (mTOR).", "entity1": "eukaryotic translation initiation factor 4E-binding protein 1", "entity2": "TCDD", "span1": [64, 125], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12817": {"label": 3, "data": {"text": "Treatment with carvedilol is associated with a reversal of abnormal regulation of HIF-1alpha, VEGF, BNP, and NGF-beta in the hypertrophic myocardium.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [94, 98], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7435": {"label": 1, "data": {"text": "Insights into dynamical behaviors of D1 and D2 receptors and their interaction modes with SPD are crucial in understanding the structural and functional characteristics of dopamine receptors.", "entity1": "dopamine receptors", "entity2": "SPD", "span1": [172, 190], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7991": {"label": 2, "data": {"text": "Furthermore, U0126 (an ERK1/2 inhibitor) significantly enhanced the ISO-induced the Bax/Bcl-2 ratio, the release of cytochrome c to the cytosol fraction, and the levels of cleaved caspase-3.", "entity1": "Bax", "entity2": "U0126", "span1": [84, 87], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15642": {"label": 3, "data": {"text": "Furthermore, nobiletin could inhibit HGF-induced the membrane localization of phosphorylated c-Met, ERK2, and Akt, but not phosphorylated JNK1/2 and p38.", "entity1": "Akt", "entity2": "nobiletin", "span1": [110, 113], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12357": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPM3", "entity2": "apomorphine", "span1": [78, 84], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7295": {"label": 3, "data": {"text": "In addition, PFD reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-beta target gene and furin substrate involved in carcinogenesis.", "entity1": "TGF-beta", "entity2": "PFD", "span1": [88, 96], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2685": {"label": 1, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "V654A", "entity2": "MP470", "span1": [57, 62], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5635": {"label": 3, "data": {"text": "The mechanisms underlying the pro-apoptotic action of compound C involved induction of oxidative stress and downregulation of antiapoptotic molecule Bcl-2, while no alteration of pro-apoptotic Bax was observed.", "entity1": "Bcl-2", "entity2": "compound C", "span1": [149, 154], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14688": {"label": 3, "data": {"text": "However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition.", "entity1": "OATP1B1", "entity2": "GSK1292263", "span1": [39, 46], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7343": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "alanine serine cysteine transporter 1", "entity2": "alanine", "span1": [196, 233], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5876": {"label": 1, "data": {"text": "In vitro binding studies showed that both amoxapine and amitriptyline interact in the nanomolar range with 5-HT2 receptors labelled by [3H]ketanserin in cortical membranes.", "entity1": "5-HT2", "entity2": "amitriptyline", "span1": [107, 112], "span2": [56, 69]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14379": {"label": 3, "data": {"text": "NFD suppressed EGF-mediated protein levels of c-Jun and c-Fos, and reduced MMP-9 expression and activity, concomitantly with a marked inhibition on cell migration and invasion without obvious cellular cytotoxicity.", "entity1": "MMP-9", "entity2": "NFD", "span1": [75, 80], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8174": {"label": 1, "data": {"text": "These results demonstrate that the incoming nucleotide is unable to induce a syn-8-oxoG conformation without minor groove DNA polymerase interactions that influence templating (anti-/syn-equilibrium) of 8-oxoG while modulating fidelity.", "entity1": "DNA polymerase", "entity2": "nucleotide", "span1": [122, 136], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3586": {"label": 1, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "mitogen-activated protein kinase", "entity2": "Wogonoside", "span1": [209, 241], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4305": {"label": 1, "data": {"text": "Unable to reverse ERK1/2 phosphorylation, TXM-CB3 (NAc-Cys-Pro-Cys amide) appeared to function in part, through inhibiting ASK1-Trx dissociation.", "entity1": "Trx", "entity2": "NAc-Cys-Pro-Cys amide", "span1": [128, 131], "span2": [51, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12425": {"label": 1, "data": {"text": "Here, we report the first crystal structure of KIF4 complexed with the non-hydrolyzable ATP analog, AMPPNP (adenylyl imidodiphosphate), at 1.7\u00c5 resolution.", "entity1": "KIF4", "entity2": "AMPPNP", "span1": [47, 51], "span2": [100, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9672": {"label": 3, "data": {"text": "FMLP/CB-stimulated translocation of cPLA2 to the nuclear envelope assessed by specific immunohistochemical staining also was blocked by FP.", "entity1": "cPLA2", "entity2": "FP", "span1": [36, 41], "span2": [136, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14425": {"label": 3, "data": {"text": "Metformin treatment is also associated with lower circulating levels of the orexigenic hormone ghrelin.", "entity1": "orexigenic hormone", "entity2": "Metformin", "span1": [76, 94], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13687": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "gardiquimod", "span1": [138, 142], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7985": {"label": 2, "data": {"text": "These results demonstrated for the first time that ISO induces apoptosis in HepG2 cells through inactivating ERK1/2 kinase and activating JNK and p38 kinases, and ROS stimulated by ISO is able to activate the MAPK singaling pathway as the upstream signaling molecules.", "entity1": "p38", "entity2": "ISO", "span1": [146, 149], "span2": [51, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7457": {"label": 8, "data": {"text": "We have expressed VIAAT and the plasmalemmal transporters for glycine and GABA in a neuroendocrine cell line and measured the quantal release of glycine and GABA using a novel double-sniffer patch-clamp technique.", "entity1": "plasmalemmal transporters", "entity2": "GABA", "span1": [32, 57], "span2": [74, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2398": {"label": 1, "data": {"text": "As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening.", "entity1": "MetAP2", "entity2": "anthranilic acid sulfonamides", "span1": [72, 78], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10272": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "OCT", "entity2": "guanidine", "span1": [123, 126], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"5826": {"label": 3, "data": {"text": "In summary, loperamide is able to reduce basal and CRH-induced ACTH and cortisol levels in normal subjects, but not in patients with Cushing's disease or secondary adrenal failure of hypothalamic origin.", "entity1": "CRH", "entity2": "loperamide", "span1": [51, 54], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6876": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "CSE", "entity2": "H2S", "span1": [27, 30], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4474": {"label": 3, "data": {"text": "Moreover, the production of intracellular reactive oxygen species (ROS) elicited by AGE was also suppressed by catalpol treatment, through dual action of reducing ROS itself and inhibiting NADPH oxidase activity.", "entity1": "NADPH oxidase", "entity2": "catalpol", "span1": [189, 202], "span2": [111, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9599": {"label": 7, "data": {"text": "Crystallographic comparison with the structurally related rat tyrosine hydroxylase binary complex with the oxidized cofactor 7,8-dihydrobiopterin revealed overlapping binding sites for the catechols and the cofactor, compatible with a competitive type of inhibition of the catechols versus BH4.", "entity1": "rat tyrosine hydroxylase", "entity2": "7,8-dihydrobiopterin", "span1": [58, 82], "span2": [125, 145]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"15290": {"label": 3, "data": {"text": "The monoacylglycerol lipase (MAGL) inhibitor JZL184 produces antinociceptive and anti-inflammatory effects.", "entity1": "monoacylglycerol lipase", "entity2": "JZL184", "span1": [4, 27], "span2": [45, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12643": {"label": 4, "data": {"text": "), attenuated the antitussive effects of codeine or SB 227122, indicating that the antitussive activity of both compounds is opioid receptor-mediated.", "entity1": "opioid receptor", "entity2": "SB 227122", "span1": [125, 140], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11269": {"label": 8, "data": {"text": "The ratio between the GDC/SHMT and C1-THF synthase/SHMT pathways of Ser synthesis from [alpha-(13)C]Gly and [(13)C]formate, respectively, in Arabidopsis shoots was 21 : 1; in roots, 9 : 1.", "entity1": "SHMT", "entity2": "Ser", "span1": [51, 55], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10964": {"label": 3, "data": {"text": "Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors.", "entity1": "AChE", "entity2": "galantamine", "span1": [98, 102], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5426": {"label": 3, "data": {"text": "Additionally, MPTP significantly down-regulated Bcl-2 expression in the mitochondria of dopaminergic cells in the SN, followed by an increase in Bax expression, cytochrome C translocation to the cytosol, andcleaved-caspase-3 expression, whereas these were inhibited by CRE or EB treatment.", "entity1": "Bcl-2", "entity2": "MPTP", "span1": [48, 53], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2253": {"label": 1, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "glucuronosyltransferases", "entity2": "rifampicin", "span1": [137, 161], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4486": {"label": 3, "data": {"text": "Potentiation was prevented by catalase, the catalase/superoxide dismutase mimetic manganese porphyrin and the NADPH oxidase inhibitor apocynin.", "entity1": "NADPH oxidase", "entity2": "apocynin", "span1": [110, 123], "span2": [134, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3299": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mTOR", "entity2": "RAD001", "span1": [75, 79], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8938": {"label": 1, "data": {"text": "Our results suggest that only negatively charged estramustine derivatives have a MAP-dependent microtubule inhibitory effect.", "entity1": "MAP", "entity2": "estramustine", "span1": [81, 84], "span2": [49, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5540": {"label": 2, "data": {"text": "RESULTS: After treatment with triflusal, there was an increase in NO production by neutrophils and an increase in endothelial nitric oxide synthase (eNOS) protein expression in neutrophils.", "entity1": "endothelial nitric oxide synthase", "entity2": "triflusal", "span1": [114, 147], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9857": {"label": 6, "data": {"text": "Aspirin and sodium salicylate inhibit endothelin ETA receptors by an allosteric type of mechanism.", "entity1": "ETA receptors", "entity2": "Aspirin", "span1": [49, 62], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"16000": {"label": 2, "data": {"text": "Puerarin stimulates proliferation and differentiation and protects against cell death in human osteoblastic MG-63 cells via ER-dependent MEK/ERK and PI3K/Akt activation.", "entity1": "Akt", "entity2": "Puerarin", "span1": [154, 157], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1871": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "chalcone", "span1": [221, 251], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5752": {"label": 3, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.", "entity1": "I-\u03baB\u03b5", "entity2": "vitamin C", "span1": [93, 98], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5629": {"label": 8, "data": {"text": "BACKGROUND: Norepinephrine transporter (NET) is involved in the regulation of norepinephrine (NE) turnover and metabolism.", "entity1": "Norepinephrine transporter", "entity2": "NE", "span1": [12, 38], "span2": [94, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13800": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "Abl", "entity2": "Imatinib mesylate", "span1": [118, 121], "span2": [60, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15170": {"label": 2, "data": {"text": "A dominant negative PKA (DNPKA) reduced GnRH-stimulated pCREB and markedly decreased GnRH stimulation of FSH\u03b2 mRNA and FSH\u03b2LUC activity, but had little effect on LH\u03b2LUC activity, indicating relative specificity of this pathway.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [105, 109], "span2": [85, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9408": {"label": 1, "data": {"text": "On the contrary, pretreatment with 5-HT worsened ethanol-induced erosions, however, did not affect gastric mucus secretion, glycoprotein content or PGE2 levels, although the non-protein SH fraction was significantly decreased.", "entity1": "glycoprotein", "entity2": "ethanol", "span1": [124, 136], "span2": [49, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2607": {"label": 3, "data": {"text": "RESULTS: Following administration of the highest of the GAL doses used (2.5; 5; 10 mg/kg i.m. ), AChE activity decreased mainly in the frontal cortex, hippocampus and hypophysis.", "entity1": "AChE", "entity2": "GAL", "span1": [97, 101], "span2": [56, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14488": {"label": 8, "data": {"text": "Of the rat CYP isoforms studied, CYP2D isoforms were the most efficient in catalyzing the O-demethylation of 5-methoxytryptamine to serotonin, but they were less effective than the human isoform CYP2D6.", "entity1": "human isoform CYP2D6", "entity2": "5-methoxytryptamine", "span1": [181, 201], "span2": [109, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13869": {"label": 6, "data": {"text": "Because these speeds are significantly faster than the responses to antagonists, these data indicate that gallamine and dimethyl-W84 are allosteric ligands and actively induce a conformation of the M(2) receptor with a reduced affinity for its agonists.", "entity1": "M(2) receptor", "entity2": "gallamine", "span1": [198, 211], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 4, 5, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"4819": {"label": 1, "data": {"text": "Degradation of MAC13243 and studies of the interaction of resulting thiourea compounds with the lipoprotein targeting chaperone LolA.", "entity1": "chaperone", "entity2": "thiourea", "span1": [118, 127], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1937": {"label": 8, "data": {"text": "Carnitine acetyltransferases (CrAT) catalyze the reversible conversion of acetyl-CoA and carnitine to acetylcarnitine and free CoA.", "entity1": "Carnitine acetyltransferases", "entity2": "acetylcarnitine", "span1": [0, 28], "span2": [102, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"11171": {"label": 1, "data": {"text": "In addition a deletion in one of the alleles of the deoxycytidine kinase was detected in the fludarabine-resistant line.", "entity1": "deoxycytidine kinase", "entity2": "fludarabine", "span1": [52, 72], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7488": {"label": 3, "data": {"text": "Phenserine, a derivative of physostigmine, was first described as an inhibitor of acetylcholinesterase (AChE) and was shown to improve cognition in various experimental paradigms in rodents and dogs.", "entity1": "acetylcholinesterase", "entity2": "Phenserine", "span1": [82, 102], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1109": {"label": 2, "data": {"text": "Indomethacin completely antagonizes CA activity, i.e. abolishes the inhibitory effect of acetazolamide on CA.", "entity1": "CA", "entity2": "Indomethacin", "span1": [106, 108], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13916": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR2B", "entity2": "Phenformin", "span1": [173, 178], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8366": {"label": 1, "data": {"text": "To reduce the binding affinity of diflunisal to albumin, we designed and synthesized the prodrug acetyldiflunisal.", "entity1": "albumin", "entity2": "diflunisal", "span1": [48, 55], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5925": {"label": 2, "data": {"text": "The concentration of estramustine phosphate required to inhibit the assembly or to induce the disassembly of chick brain MAP2:tubulin microtubules is markedly dependent upon the microtubule protein concentration.", "entity1": "chick brain MAP2", "entity2": "estramustine phosphate", "span1": [109, 125], "span2": [21, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8095": {"label": 3, "data": {"text": "PKAA/anti-TNF-\u03b1 siRNA nanocomplexes significantly reduced the ALT (alanine transaminase) and the hepatic cellular damages in APAP-intoxicated mice.", "entity1": "alanine transaminase", "entity2": "PKAA", "span1": [67, 87], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10663": {"label": 5, "data": {"text": "An angiotensin II AT1 receptor antagonist, telmisartan augments glucose uptake and GLUT4 protein expression in 3T3-L1 adipocytes.", "entity1": "angiotensin II AT1 receptor", "entity2": "telmisartan", "span1": [3, 30], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15459": {"label": 3, "data": {"text": "These data demonstrate that benzenesulfonamides are a unique class of CXCR4 inhibitors with high potency.", "entity1": "CXCR4", "entity2": "benzenesulfonamides", "span1": [70, 75], "span2": [28, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3023": {"label": 3, "data": {"text": "Flavopiridol, a cyclin-dependent kinase inhibitor, arrests cell division and causes apoptosis in non-small lung cancer cells [283660].", "entity1": "cyclin-dependent kinase", "entity2": "Flavopiridol", "span1": [16, 39], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1645": {"label": 1, "data": {"text": "Compounds 4b-h were either inactive (4e,f) or weaker than 4a as affinity ligands for GluR1-4 and GluR5 with relative potencies comparable with those of the corresponding AMPA analogues as AMPA receptor agonists.", "entity1": "GluR1-4", "entity2": "AMPA", "span1": [85, 92], "span2": [170, 174]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1965": {"label": 5, "data": {"text": "In order to examine the site of action of an NR2B subtype-selective NMDA antagonist CP-101,606, we investigated its analgesic effect in a rat model of neuropathic pain at various routes of administration.", "entity1": "NMDA", "entity2": "CP-101,606", "span1": [68, 72], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2977": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "F786A", "entity2": "IBMX", "span1": [88, 93], "span2": [56, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1206": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DAT", "entity2": "amphetamines", "span1": [165, 168], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12774": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "LV", "span1": [22, 24], "span2": [108, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15091": {"label": 3, "data": {"text": "Avibactam (formerly NXL104, AVE1330A) is a synthetic non-\u03b2-lactam, \u03b2-lactamase inhibitor that inhibits the activities of Ambler class A and C \u03b2-lactamases and some Ambler class D enzymes.", "entity1": "\u03b2-lactamase", "entity2": "NXL104", "span1": [67, 78], "span2": [20, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"841": {"label": 3, "data": {"text": "The higher affinity of felbamate block of NMDA receptors containing the NR2B subunit could be accounted for by more rapid association and slower dissociation from these sites.", "entity1": "NMDA receptors", "entity2": "felbamate", "span1": [42, 56], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8508": {"label": 0, "data": {"text": "In addition, putative osteogenic actions of PTHrP might be ascribed not only to its N-terminal domain but also to its PTH-unrelated C-terminal region.", "entity1": "PTHrP", "entity2": "N", "span1": [44, 49], "span2": [84, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3583": {"label": 1, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "extracellular signal-regulated kinase", "entity2": "Wogonoside", "span1": [145, 182], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2341": {"label": 1, "data": {"text": "Dynamics of NO rebinding to the heme domain of NO synthase-like proteins from bacterial pathogens.", "entity1": "heme domain of NO synthase-like proteins", "entity2": "NO", "span1": [32, 72], "span2": [12, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7512": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMPK", "entity2": "metformin", "span1": [54, 58], "span2": [76, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11843": {"label": 8, "data": {"text": "Methods: The stability of six acyl glucuronides in the presence of hCES1, hCES2, and buffer alone (100 mM potassium phosphate, pH 7.4, 37\u00b0C) were investigated.", "entity1": "hCES1", "entity2": "acyl glucuronides", "span1": [67, 72], "span2": [30, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3434": {"label": 2, "data": {"text": "Epi increased the activity of the human WNT6 promoter through Cav1-dependent binding of \u03b2-catenin to the proximal WNT6 promoter.", "entity1": "WNT6 promoter", "entity2": "Epi", "span1": [114, 127], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3738": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates (N-BPs) induce apoptosis in tumor cells by inhibiting the prenylation of small G-proteins.", "entity1": "G-proteins", "entity2": "N", "span1": [115, 125], "span2": [37, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3629": {"label": 5, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "CB1", "entity2": "rimonabant", "span1": [48, 51], "span2": [221, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10281": {"label": 2, "data": {"text": "Rasagiline prevented the PT in mitochondria directly and also indirectly through induction of antiapoptotic Bcl-2 and a neurotrophic factor, glial cell line-derived neurotrophic factor (GDNF).", "entity1": "Bcl-2", "entity2": "Rasagiline", "span1": [108, 113], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8838": {"label": 1, "data": {"text": "CONCLUSION: We provided documentation of neuroprotective effect of a natural flavone, calycopterin, against H2O2-induced oxidative stress in differentiated PC12 cells by modulating the level of CREB phosphorylation and Nrf2 pathway.", "entity1": "CREB", "entity2": "calycopterin", "span1": [194, 198], "span2": [86, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10722": {"label": 1, "data": {"text": "In contrast, the binding of barusiban was significantly improved when the transmembrane domains 1 and 2 were transferred from the oxytocin receptor to the vasopressin V2 receptor.", "entity1": "vasopressin V2 receptor", "entity2": "barusiban", "span1": [155, 178], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14484": {"label": 8, "data": {"text": "The obtained results indicate that rat brain CYP2D isoforms catalyze the formation of serotonin from 5-methoxytryptamine, and that the deficit or genetic defect of CYP2D may affect serotonin metabolism in the brain.", "entity1": "CYP2D", "entity2": "serotonin", "span1": [164, 169], "span2": [181, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8249": {"label": 0, "data": {"text": "N-terminal sequencing indicated that pro-BMP-2 was cleaved by FSAP at the canonical PC cleavage site, giving rise to mature BMP-2 (Arg(282)\u2193Gln(283)), as well as in the N-terminal heparin binding region of mature BMP-2, generating a truncated mature BMP-2 peptide (Arg(289)\u2193Lys(290)).", "entity1": "pro-BMP-2", "entity2": "N", "span1": [37, 46], "span2": [0, 1]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1047": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "etoposide", "span1": [110, 114], "span2": [194, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7837": {"label": 1, "data": {"text": "These data suggest that ribavirin-induced intracellular GTP depletion recruits a super elongation complex containing P-TEFb, AFF4 and ELL3, to F7, and modulates FVII mRNA transcription elongation.", "entity1": "FVII", "entity2": "ribavirin", "span1": [161, 165], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12949": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "tolvaptan", "span1": [39, 59], "span2": [164, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13079": {"label": 1, "data": {"text": "Our work shows that sulfonylureas and glinides additionally bind to PPARgamma and exhibit PPARgamma agonistic activity.", "entity1": "PPARgamma", "entity2": "sulfonylureas", "span1": [68, 77], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10275": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "transmembrane transporters", "entity2": "choline", "span1": [135, 161], "span2": [72, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"1235": {"label": 1, "data": {"text": "We report herein the location of the binding site for the inhaled anesthetic halothane at the amino acid residue level of resolution in the ligand binding cavity in a prototypical G protein-coupled receptor, bovine rhodopsin.", "entity1": "bovine rhodopsin", "entity2": "halothane", "span1": [208, 224], "span2": [77, 86]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6005": {"label": 0, "data": {"text": "The protein that binds TSG-6 was purified from human serum and identified as inter-alpha-inhibitor (I alpha I) by N-terminal microsequencing.", "entity1": "inter-alpha-inhibitor", "entity2": "N", "span1": [77, 98], "span2": [114, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15762": {"label": 8, "data": {"text": "Ethanol-stimulated (100mM) CYP2E1 upregulation was suppressed by quercetin but further enhanced by HO-1 inhibition with resultant heme accumulation.", "entity1": "HO-1", "entity2": "heme", "span1": [99, 103], "span2": [130, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9272": {"label": 1, "data": {"text": "Saturation experiments showed that [3H]prazosin labelled a single population of binding sites in the spleen (alpha 1B) and hippocampus (alpha 1A and alpha 1B) (dissociation constants (KD): 0.26 nM and 0.14 nM respectively).", "entity1": "alpha 1B", "entity2": "[3H]prazosin", "span1": [149, 157], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14462": {"label": 1, "data": {"text": "The [(3)H]PGE(2) binding of W203A in broken cell membrane fractions was inhibited by addition of GTP\u03b3S (IC(50) 21 \u00b1 1.8 nM).", "entity1": "W203A", "entity2": "[(3)H]PGE(2)", "span1": [28, 33], "span2": [4, 16]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2264": {"label": 1, "data": {"text": "Ethanol withdrawal significantly increased the packing density of GS- and GFAP-IR astrocytes in the PLC of P rats as compared with P rats with continuous access to ethanol.", "entity1": "GFAP", "entity2": "Ethanol", "span1": [74, 78], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9208": {"label": 1, "data": {"text": "Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides.", "entity1": "alpha 2-macroglobulin", "entity2": "phenothiazines", "span1": [8, 29], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4291": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B3", "entity2": "estradiol 17\u03b2-glucuronide", "span1": [269, 276], "span2": [44, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14764": {"label": 3, "data": {"text": "These data suggest that jaceosidin, isolated from Japanese mugwort, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells.", "entity1": "Cdc2", "entity2": "jaceosidin", "span1": [137, 141], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"571": {"label": 2, "data": {"text": "These results suggest that the megabase DNA fragmentation is induced as a consequence of inhibition of thymidylate synthase by Tomudex and kilobase DNA fragmentation may correlate with the reduction of p27(kip1) expression and the increase in cyclin E and cdk2 kinase activities.", "entity1": "cyclin E", "entity2": "Tomudex", "span1": [243, 251], "span2": [127, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11298": {"label": 8, "data": {"text": "The protein exhibited modest H(2)O(2)-dependent peroxidase activities with guaiacol, potassium iodide, and 2,2(')-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS).", "entity1": "peroxidase", "entity2": "guaiacol", "span1": [48, 58], "span2": [75, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10224": {"label": 1, "data": {"text": "BACKGROUND & AIMS: Sensitization of Kupffer cells (KCs) to lipopolysaccharide (LPS) and overproduction of tumor necrosis factor (TNF) alpha are critical for progression of alcoholic liver injury.", "entity1": "tumor necrosis factor (TNF) alpha", "entity2": "alcoholic", "span1": [106, 139], "span2": [172, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4349": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "\u03b2-catenin", "entity2": "pinosylvin", "span1": [191, 200], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4423": {"label": 3, "data": {"text": "Experimental studies performed for characterizing the inhibitory mechanism indicate that GSK-3\u03b2 inhibition by palinurin cannot be competed out by ATP nor peptide substrate.", "entity1": "GSK-3\u03b2", "entity2": "palinurin", "span1": [89, 95], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"9533": {"label": 8, "data": {"text": "The majority of L-Arg transport is mediated by System y+, although several other carriers have been kinetically defined.", "entity1": "System y+", "entity2": "L-Arg", "span1": [47, 56], "span2": [16, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13751": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "LTCC", "entity2": "1,4-dihydropyridine", "span1": [28, 32], "span2": [81, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13565": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase (DDAH) metabolizes asymmetric dimethylarginine to generate L-citrulline and is present in large quantities in the kidney.", "entity1": "Dimethylarginine dimethylaminohydrolase", "entity2": "dimethylarginine", "span1": [0, 39], "span2": [70, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11294": {"label": 8, "data": {"text": "BACKGROUND & AIMS: Of the 2 genes (MAT1A, MAT2A) encoding methionine adenosyltransferase, the enzyme that synthesizes S-adenosylmethionine, MAT1A, is expressed in liver, whereas MAT2A is expressed in extrahepatic tissues.", "entity1": "MAT1A", "entity2": "S-adenosylmethionine", "span1": [35, 40], "span2": [118, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9027": {"label": 5, "data": {"text": "The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma.", "entity1": "histamine-H1 receptor", "entity2": "terfenadine", "span1": [14, 35], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2682": {"label": 0, "data": {"text": "In GIST-R, AXL is tyrosine phosphorylated and its ligand growth-arrest-specific gene 6 is overexpressed implying autocrine activation.", "entity1": "AXL", "entity2": "tyrosine", "span1": [11, 14], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12093": {"label": 0, "data": {"text": "The C-terminal half of TSG-6 contains a so-called CUB domain, characteristic for developmentally regulated proteins.", "entity1": "TSG-6", "entity2": "C", "span1": [23, 28], "span2": [4, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12931": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine beta-synthase", "entity2": "L-Cys", "span1": [131, 158], "span2": [182, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7513": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMP-activated protein kinase", "entity2": "phenformin", "span1": [24, 52], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"108": {"label": 5, "data": {"text": "Terfenadine and astemizole are chemically unrelated to histamine H1-receptor antagonists such as diphenhydramine and chlorpheniramine.", "entity1": "histamine H1-receptor", "entity2": "astemizole", "span1": [55, 76], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6837": {"label": 1, "data": {"text": "However, MS A2756G was significantly associated with cobalamin levels (AA genotype: 290 +/- 122 pmol/l; AG: 381 +/- 151 pmol/l and GG: 415 +/- 100 pmol/l), as was MTRR A66G (AA: 478 +/- 219 pmol/l, AG: 306 +/- 124 pmol/l and GG: 306 +/- 123 pmol/l).", "entity1": "A66G", "entity2": "cobalamin", "span1": [168, 172], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7359": {"label": 1, "data": {"text": "Neuroprotection by estrogen against MPP+-induced dopamine neuron death is mediated by ERalpha in primary cultures of mouse mesencephalon.", "entity1": "ERalpha", "entity2": "estrogen", "span1": [86, 93], "span2": [19, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1552": {"label": 8, "data": {"text": "Even though the activities of MAT and GNMT were elevated, the concentration of liver S-adenosylmethionine was decreased (24%, p<0.001) and S-adenosylhomocysteine increased (113%, p<0.001) in the dwarf mice.", "entity1": "MAT", "entity2": "S-adenosylmethionine", "span1": [30, 33], "span2": [85, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1894": {"label": 2, "data": {"text": "The in vitro kinase activity of PKC-alpha induced by I3A was lower than that induced by PMA.", "entity1": "PKC-alpha", "entity2": "I3A", "span1": [32, 41], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1984": {"label": 3, "data": {"text": "Mibefradil blocked currents of all Na+ channel isoforms with similar affinity and a dependence on holding potential, and drug off-rate was slowed at depolarized potentials (k(off) was 0.024/s at -130 mV and 0.007/s at -100 mV for Nav1.5).", "entity1": "Na+ channel", "entity2": "Mibefradil", "span1": [35, 46], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7941": {"label": 4, "data": {"text": "Characterization of substituted phenylpropylamides as highly selective agonists at the melatonin MT2 receptor.", "entity1": "melatonin MT2 receptor", "entity2": "phenylpropylamides", "span1": [87, 109], "span2": [32, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11666": {"label": 8, "data": {"text": "Immunohistochemical characterization of pyrimidine synthetic enzymes, thymidine kinase-1 and thymidylate synthase, in various types of cancer.", "entity1": "thymidine kinase-1", "entity2": "pyrimidine", "span1": [70, 88], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7915": {"label": 8, "data": {"text": "DRG neurons display substantial capacity for accumulating copper via a transport process mediated by rCtr1, but appear able to resist copper toxicity and use alternative mechanisms to take up oxaliplatin.", "entity1": "rCtr1", "entity2": "oxaliplatin", "span1": [101, 106], "span2": [192, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3510": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "Aldo-keto reductases", "entity2": "PAHs", "span1": [0, 20], "span2": [111, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9088": {"label": 3, "data": {"text": "However, in the presence of 100 mM Na+, which is required for opiate inhibition of adenylate cyclase activity, analysis of competition binding data revealed three sites: the first, consisting of 17.5% of total receptor population has a Kd = 0.38 +/- 0.18 nM; the second, 50.6% of the population, has a Kd = 6.8 +/- 2.2 nM; and the third, 31.9% of the population, has a Kd of 410 +/- 110 nM.", "entity1": "adenylate cyclase", "entity2": "Na+", "span1": [83, 100], "span2": [35, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2593": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "D(1)", "entity2": "FLX", "span1": [57, 61], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14122": {"label": 1, "data": {"text": "Emerging data suggest that crizotinib may also have activity in other subsets of lung cancer, including tumors demonstrating amplification or mutation of the MET oncogene, or translocation of the ROS1 oncogene.", "entity1": "MET", "entity2": "crizotinib", "span1": [158, 161], "span2": [27, 37]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6831": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "PDGFR", "entity2": "SU11248", "span1": [200, 205], "span2": [170, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14951": {"label": 1, "data": {"text": "We hypothesized that styrene metabolites have lower affinity than styrene toward CYP2E1 and limited ability to induce cooperative effects during metabolism.", "entity1": "CYP2E1", "entity2": "styrene", "span1": [81, 87], "span2": [21, 28]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10770": {"label": 2, "data": {"text": "Treatment of head and neck squamous carcinoma cells with clinically relevant concentrations of imatinib-induced changes in cell morphology and growth similar to changes associated with epidermal growth factor receptor (EGFR) activation.", "entity1": "EGFR", "entity2": "imatinib", "span1": [219, 223], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6768": {"label": 2, "data": {"text": "In vivo, hydralazine induced HIF-1alpha and VEGF protein in tissue extracts and elevated plasma VEGF levels.", "entity1": "HIF-1alpha", "entity2": "hydralazine", "span1": [29, 39], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9107": {"label": 8, "data": {"text": "The EC50 for inhibition of the leukotriene C synthetase of RBL cells was directly proportional to the LTA4 concentration in the incubations, ranging from 1.5 mM at 10 microM LTA4 to over 40 mM at 500 microM LTA4.", "entity1": "leukotriene C synthetase", "entity2": "LTA4", "span1": [31, 55], "span2": [102, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8460": {"label": 3, "data": {"text": "Hinokitiol inhibited the phosphorylation of phospholipase C (PLC)\u03b32, protein kinase C (PKC), mitogen-activated protein kinases (MAPKs), and Akt in collagen-activated human platelets, and significantly reduced intracellular calcium mobilization and hydroxyl radical (OH) formation.", "entity1": "MAPKs", "entity2": "Hinokitiol", "span1": [128, 133], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12264": {"label": 9, "data": {"text": "The mRNA level of AQP5 was scarcely affected by CTD and cevimeline hydrochloride administration.", "entity1": "AQP5", "entity2": "cevimeline hydrochloride", "span1": [18, 22], "span2": [56, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12320": {"label": 2, "data": {"text": "Ribavirin unregulated ELL (eleven-nineteen lysine-rich leukaemia) 3 mRNA expression before F7 up-regulation.", "entity1": "F7", "entity2": "Ribavirin", "span1": [91, 93], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11347": {"label": 3, "data": {"text": "Block of human NaV1.5 sodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin.", "entity1": "sodium channels", "entity2": "phenytoin", "span1": [22, 37], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2777": {"label": 3, "data": {"text": "In the presence of the system L inhibitor BCH, Na(+)-dependent l-alanine uptake in WKY and SHR PTE cells was inhibited by alanine, serine, and cysteine, which is consistent with amino acid transport through ASCT2.", "entity1": "ASCT2", "entity2": "serine", "span1": [207, 212], "span2": [131, 137]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11014": {"label": 9, "data": {"text": "It was found that a single intragastric gavage by L-methionine resulted in inhibition of endothelium-dependent relaxation, markedly increased the serum level of malondialdehyde and decreased the activity of PON1 and SOD, similarly decreased the level of NO in the serum; but had no effects on endothelium-independent relaxation and angiotensin-converting enzyme activity compared with the control group.", "entity1": "angiotensin-converting enzyme", "entity2": "L-methionine", "span1": [332, 361], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15210": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "TNF- \u03b1", "entity2": "ethylacetate", "span1": [365, 371], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15364": {"label": 1, "data": {"text": "Taken together, these findings identify a signature hepatic gene-network associated with repeated oxycodone administration in rats and demonstrate that oxycodone alters the expression of many transporters and DMEs (without direct activation of PXR, CAR, and AhR), which could lead to undesirable DDIs after coadministration of substrates of these transporters/DMEs with oxycodone.", "entity1": "AhR", "entity2": "oxycodone", "span1": [258, 261], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"11188": {"label": 2, "data": {"text": "Orlistat treatment also results in modest improvements in total cholesterol, low-density lipoprotein, blood pressure, and fasting glucose and insulin concentrations.", "entity1": "low-density lipoprotein", "entity2": "Orlistat", "span1": [77, 100], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8254": {"label": 1, "data": {"text": "In\u00a0vitro molecular pharmacology studies showed that 5-HT2C agonists potent for attenuating the DOI-elicited-HTR also reduced the efficacy of DOI to activate mouse 5-HT2C receptor-mediated PLC signaling in HEK cells.", "entity1": "PLC", "entity2": "DOI", "span1": [188, 191], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16046": {"label": 1, "data": {"text": "In addition, the expression of nucleus-encoded RNA polymerase dependent transcripts is specifically induced by lincomycin, and the splicing of ndhB transcripts is significantly reduced in the albino mutants and inhibitor-treated seedlings.", "entity1": "RNA polymerase", "entity2": "lincomycin", "span1": [47, 61], "span2": [111, 121]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8055": {"label": 2, "data": {"text": "Moreover, paclitaxel-induced ERCC1 protein and mRNA levels significantly decreased via the downregulation of p38 activity by either a p38 MAPK inhibitor SB202190 or p38 knockdown with specific small interfering RNA (siRNA).", "entity1": "ERCC1", "entity2": "paclitaxel", "span1": [29, 34], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10248": {"label": 8, "data": {"text": "Substrate specificity using lysates of oxidase-transfected HEK-293 cells revealed that the newly identified oxidase strongly favoured spermine over N (1)-acetylspermine and that it failed to act on N (1)-acetylspermidine, spermidine or the preferred PAO substrate, N (1), N (12)-diacetylspermine.", "entity1": "PAO", "entity2": "N (1), N (12)-diacetylspermine", "span1": [250, 253], "span2": [265, 295]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11413": {"label": 0, "data": {"text": "Comparison of the crystal structures of UDP-Gal- and UDP-Glc-bound beta4Gal-T1 reveals that the O4 hydroxyl group in both Gal and Glc moieties forms a hydrogen bond with the side chain carboxylate group of Glu317.", "entity1": "beta4Gal-T1", "entity2": "carboxylate", "span1": [67, 78], "span2": [185, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5780": {"label": 1, "data": {"text": "Inhibition of binding of both plasminogen and plasmin to gp330 by benzamidine was similar, although EACA inhibited the binding of plasmin to gp330 slightly more than the binding of plasminogen to gp330.", "entity1": "gp330", "entity2": "EACA", "span1": [196, 201], "span2": [100, 104]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14434": {"label": 1, "data": {"text": "TCDD or prochloraz doubled ABCG2-mediated Hoechst H33342 secretion.", "entity1": "ABCG2", "entity2": "TCDD", "span1": [27, 32], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9147": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "theophylline", "span1": [124, 136], "span2": [36, 48]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3300": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mammalian target of rapamycin", "entity2": "RAD001", "span1": [81, 110], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9333": {"label": 1, "data": {"text": "Kainate and AMPA activated the heteromeric channel with significantly higher affinities than observed for EAA3a alone.", "entity1": "EAA3a", "entity2": "Kainate", "span1": [106, 111], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3703": {"label": 2, "data": {"text": "In addition, the number and area of glutathione S-transferase placental form (GST-P) positive foci and proliferating cell nuclear antigen (PCNA) positive cell ratios in the hepatocytes were significantly increased in the male and female rats that were administered 100mg/kg MEG compared with the control animals.", "entity1": "proliferating cell nuclear antigen", "entity2": "MEG", "span1": [103, 137], "span2": [274, 277]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1450": {"label": 3, "data": {"text": "Rasagiline does not modify CNS monoamine tissue levels or monoamine-induced behavioural syndromes at doses which selectively inhibit MAO-B but not MAO-A.", "entity1": "MAO-B", "entity2": "Rasagiline", "span1": [133, 138], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5513": {"label": 9, "data": {"text": "The present findings indicate that dezocine shares similar stimulus effects with both mu and delta agonists, its stimulus effects are reversed by mu-selective antagonists, and its rate-decreasing effects are not mediated by activity at mu, kappa or delta opioid receptors.", "entity1": "mu, kappa or delta opioid receptors", "entity2": "dezocine", "span1": [236, 271], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3944": {"label": 3, "data": {"text": "Role of organic cation/carnitine transporter 1 in uptake of phenformin and inhibitory effect on complex I respiration in mitochondria.", "entity1": "complex I", "entity2": "phenformin", "span1": [96, 105], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3707": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "caspase-3", "entity2": "N", "span1": [158, 167], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7843": {"label": 2, "data": {"text": "We observed that ribavirin enhanced ELL3 recruitment to F7, whereas knockdown of ELL3 diminished ribavirin-induced FVII mRNA up-regulation.", "entity1": "FVII", "entity2": "ribavirin", "span1": [115, 119], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2942": {"label": 1, "data": {"text": "Vardenafil has higher affinity to phosphodiesterase-5 (PDE5) than sildenafil and lower administered dosage for the treatment of erectile dysfunction.", "entity1": "phosphodiesterase-5", "entity2": "sildenafil", "span1": [34, 53], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7615": {"label": 3, "data": {"text": "CONCLUSIONS: Lapatinib is a dual inhibitor of the EGFR and HER2 tyrosine kinases.", "entity1": "HER2", "entity2": "Lapatinib", "span1": [59, 63], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12846": {"label": 1, "data": {"text": "However, there were some significant differences among Captopril (30 mg/kg or 45 mg/kg), enalapril (20 mg/kg), and N-acetylcysteine particular in the activity of PON1 and ACE.", "entity1": "PON1", "entity2": "N-acetylcysteine", "span1": [162, 166], "span2": [115, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1363": {"label": 3, "data": {"text": "Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.", "entity1": "dopamine transporter", "entity2": "Mazindol", "span1": [78, 98], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15127": {"label": 3, "data": {"text": "Notably, the antioxidant Trolox\u2122 reversed the Mn (20\u00a0mg/kg)-dependent augmentation in p38(MAPK) phosphorylation and reduced the Mn (20\u00a0mg/kg)-induced caspase activity and F(2)-isoprostane production.", "entity1": "caspase", "entity2": "Trolox", "span1": [150, 157], "span2": [25, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"1156": {"label": 9, "data": {"text": "Patch-clamp analysis using inside-out recording configuration showed that mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 microM).", "entity1": "Kir6.2", "entity2": "mitiglinide", "span1": [218, 224], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6131": {"label": 5, "data": {"text": "We have investigated the effects of CP-99,994 [(+)-(2s,3s)-3-(2-methoxybenzylamino)-2-phenylpiperidine], a tachykinin NK1 receptor antagonist, HOE 140 (D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin), a bradykinin B2 receptor antagonist, and ketotifen (4-(1-methyl-4-piperidylidene)4 H-benzo[4,5]cycloheptal[1,2-b]thiophen-10(9H)-one hydrogen fumarate), a histamine H1 receptor antagonist with mast cell-stabilizing properties, on microvascular leakage induced by gaseous formaldehyde.", "entity1": "bradykinin B2 receptor", "entity2": "HOE 140", "span1": [195, 217], "span2": [143, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15517": {"label": 1, "data": {"text": "We found that, both in a cell-free system and in cells, NO/SNO donors such as S-nitrosocysteine and S-nitrosoglutathione readily induced the S-nitrosylation of Prx1, causing structural and functional alterations.", "entity1": "Prx1", "entity2": "S-nitrosocysteine", "span1": [160, 164], "span2": [78, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9260": {"label": 3, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "ergonovine", "span1": [50, 53], "span2": [121, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15747": {"label": 1, "data": {"text": "However, the precise mechanism by which quercetin counteracts CYP2E1-mediated ethanol hepatotoxicity through HO-1 system is still remained unclear.", "entity1": "HO-1", "entity2": "quercetin", "span1": [109, 113], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14870": {"label": 1, "data": {"text": "These findings indicate that the neuroprotective effect of EHT against MPTP is through several mechanisms including its anti-inflammatory and antioxidant activities as well as its ability to modulate the methylation and hence activity of PP2A.", "entity1": "PP2A", "entity2": "EHT", "span1": [238, 242], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9979": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "MFMD", "span1": [80, 84], "span2": [164, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5637": {"label": 3, "data": {"text": "Compound C diminished AMPK phosphorylation and enzymatic activity, resulting in reduced phosphorylation of its target acetyl CoA carboxylase.", "entity1": "acetyl CoA carboxylase", "entity2": "Compound C", "span1": [118, 140], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5244": {"label": 1, "data": {"text": "Taken together, these findings suggest that NaF induces apoptosis in OLC odontoblasts through a JNK-dependent mitochondrial pathway.", "entity1": "JNK", "entity2": "NaF", "span1": [96, 99], "span2": [44, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"540": {"label": 3, "data": {"text": "Two mechanisms of action have been identified for A77 1726: inhibition of dihydroorotate dehydrogenase (DHODH) and inhibition of tyrosine kinases.", "entity1": "DHODH", "entity2": "A77 1726", "span1": [104, 109], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2699": {"label": 2, "data": {"text": "Improvements from baseline in mean glycosylated haemoglobin (HbA(1c)) were significantly greater with sitagliptin monotherapy than with placebo in patients with type 2 diabetes.", "entity1": "glycosylated haemoglobin", "entity2": "sitagliptin", "span1": [35, 59], "span2": [102, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"909": {"label": 1, "data": {"text": "In this study, we examined whether betaxolol and other beta-adrenoceptor antagonists interact directly with neurotoxin binding to sites 1 and 2 of the voltage-sensitive sodium channel (Na(+) channel) in rat cerebrocortical synaptosomes.", "entity1": "Na(+) channel", "entity2": "betaxolol", "span1": [185, 198], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9902": {"label": 1, "data": {"text": "Conversely, when mice are fed a high-fat diet after parturition, the downregulation of UCP-3 mRNA and UCP-3 protein levels due to lactation is partially reversed, as is the reduction in serum free fatty acid levels.", "entity1": "UCP-3", "entity2": "fatty acid", "span1": [102, 107], "span2": [197, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4141": {"label": 3, "data": {"text": "The therapeutic potential of directly inhibiting prosurvival proteins was unveiled with the development of navitoclax, a selective inhibitor of both BCL-2 and BCL-2-like 1 (BCL-X(L)), which has shown clinical efficacy in some BCL-2-dependent hematological cancers.", "entity1": "BCL-2-like 1", "entity2": "navitoclax", "span1": [159, 171], "span2": [107, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11815": {"label": 1, "data": {"text": "In the present study, the extent to which six substituted quercetin derivatives (1-6) affected the function of OATP1B1 and OATP1B3 was investigated.", "entity1": "OATP1B1", "entity2": "quercetin", "span1": [111, 118], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13826": {"label": 8, "data": {"text": "It undergoes extensive biotransformation, which is affected by poor metabolism by cytochrome P450 (CYP) 2D6 in a small percentage of the population; these patients have greater exposure to and slower elimination of atomoxetine than extensive metabolizers.", "entity1": "cytochrome P450 (CYP) 2D6", "entity2": "atomoxetine", "span1": [82, 107], "span2": [215, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1124": {"label": 3, "data": {"text": "CONCLUSIONS: Our results show that indomethacin, a known cyclooxygenase (COX) inhibitor, is also an activator of CA.", "entity1": "cyclooxygenase", "entity2": "indomethacin", "span1": [57, 71], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14424": {"label": 3, "data": {"text": "Our results show that Metformin directly inhibits stomach ghrelin production and secretion through AMPK.", "entity1": "ghrelin", "entity2": "Metformin", "span1": [58, 65], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11285": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "EC 2.1.2.1", "entity2": "Gly", "span1": [172, 182], "span2": [198, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7734": {"label": 5, "data": {"text": "Two pure GnRH antagonists have been developed, abarelix and degarelix, that are devoid of any agonist effect on the GnRH receptor and consequently do not result in testosterone flare.", "entity1": "GnRH", "entity2": "abarelix", "span1": [9, 13], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7525": {"label": 3, "data": {"text": "These results suggested that nimesulide, a preferential COX-2 inhibitor offered neuroprotection against PTZ-induced kindling in mice.", "entity1": "COX-2", "entity2": "nimesulide", "span1": [56, 61], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15813": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFbeta receptor", "entity2": "Tyr", "span1": [70, 87], "span2": [149, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12097": {"label": 3, "data": {"text": "Phorbol esters and norepinephrine destabilize alpha 1B-adrenergic receptor mRNA in vascular smooth muscle cells.", "entity1": "alpha 1B-adrenergic receptor", "entity2": "norepinephrine", "span1": [46, 74], "span2": [19, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12060": {"label": 1, "data": {"text": "These results confirm and strengthen the idea of alpha N-acetyl beta-endorphin-(1-31) acting as a non-competitive regulator of mu opioid- and alpha 2-adrenoceptor-mediated supraspinal antinociception.", "entity1": "alpha 2-adrenoceptor", "entity2": "N-acetyl", "span1": [142, 162], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6743": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "CT53518", "span1": [268, 272], "span2": [234, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5935": {"label": 3, "data": {"text": "Cyproterone acetate, a progestin used in the treatment of hirsutism, acne and prostate cancer as well as norgestrel and norethindrone that are widely used as oral contraceptives also inhibit 3 beta-HSD activity at Ki values of 1.5, 1.7 and 2.5 microM, respectively.", "entity1": "3 beta-HSD", "entity2": "norgestrel", "span1": [191, 201], "span2": [105, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7329": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "neutral amino acid transporters", "entity2": "glutamine", "span1": [133, 164], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6239": {"label": 1, "data": {"text": "The affinity of eletriptan ((R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1H-indole) for a range of 5-HT receptors was compared to values obtained for other 5-HT1B/1D receptor agonists known to be effective in the treatment of migraine.", "entity1": "5-HT receptors", "entity2": "eletriptan", "span1": [122, 136], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3354": {"label": 1, "data": {"text": "The Ca(2+) dependent interaction between troponin I (cTnI) and troponin C (cTnC) triggers contraction in heart muscle.", "entity1": "troponin C", "entity2": "Ca(2+)", "span1": [63, 73], "span2": [4, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8047": {"label": 3, "data": {"text": "Exposure of H9c2 cells to high glucose reduced AMPK activity, inhibited Jun NH2-terminal kinase 1 (JNK1)-B-cell lymphoma 2 (Bcl-2) signaling, and promoted Beclin1 binding to Bcl-2.", "entity1": "Bcl-2", "entity2": "glucose", "span1": [124, 129], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9677": {"label": 1, "data": {"text": "Desipramine treatment decreases 3H-nisoxetine binding and norepinephrine transporter mRNA in SK-N-SHSY5Y cells.", "entity1": "norepinephrine transporter", "entity2": "3H-nisoxetine", "span1": [58, 84], "span2": [32, 45]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2572": {"label": 3, "data": {"text": "Neonatal quinpirole treatment produced a significant decrease in BDNF and ChAT in the frontal cortex that was unaffected by olanzapine treatment.", "entity1": "BDNF", "entity2": "quinpirole", "span1": [65, 69], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15227": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "CLS", "span1": [340, 363], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2387": {"label": 3, "data": {"text": "Sorafenib inhibited the kinase activity of both C-RAF and B-RAF (wild type and V600E mutant).", "entity1": "B-RAF", "entity2": "Sorafenib", "span1": [58, 63], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"580": {"label": 3, "data": {"text": "Tomudex treatment resulted in the decrease in p27(kip1) expression, with an increase in cyclin E and cdk2 protein expression and kinase activities 24 h after a 2-h exposure.", "entity1": "p27(kip1)", "entity2": "Tomudex", "span1": [46, 55], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15593": {"label": 4, "data": {"text": "Oral lorcaserin (BELVIQ(\u00ae)), a selective serotonin 5-HT2C receptor agonist, is indicated in the US as an adjunct to diet and exercise in the chronic weight management of obese adults, or overweight adults with at least one weight-related comorbidity (e.g.", "entity1": "5-HT2C", "entity2": "lorcaserin", "span1": [51, 57], "span2": [5, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8642": {"label": 3, "data": {"text": "Ovarian AR was not influenced by either treatment, and oviduct AR was reduced after ethanol-melatonin combination.", "entity1": "AR", "entity2": "melatonin", "span1": [63, 65], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1547": {"label": 8, "data": {"text": "The purified human enzyme also does not oxidize eight representative antitumor polyamine analogues; however, specific oligamine analogues were found to be potent inhibitors of the oxidation of spermine by PAOh1/SMO.", "entity1": "PAOh1", "entity2": "spermine", "span1": [205, 210], "span2": [193, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"852": {"label": 3, "data": {"text": "Troglitazone inhibited LTB(4) production by the supernatant fraction of RBL-2H3 cell lysate with similar potency to zileuton, suggesting that troglitazone inhibits LT production by direct inhibition of 5-LOX activity.", "entity1": "5-LOX", "entity2": "troglitazone", "span1": [202, 207], "span2": [142, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13748": {"label": 1, "data": {"text": "(+)-[(3)H]isradipine binding to Ca(v)1.2DHP(-/-) and Ca(v)-DM brains was reduced to 15.1 and 4.4% of wild type, respectively, indicating that Ca(v)1.3 accounts for 10.7% of brain LTCCs.", "entity1": "Ca(v)", "entity2": "(+)-[(3)H]isradipine", "span1": [53, 58], "span2": [0, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5878": {"label": 5, "data": {"text": "Complementary experiments using the 5-HT3-dependent Bezold-Jarisch reflex confirmed that amoxapine really acts in vivo as a 5-HT3 antagonist (IC50 = 50 micrograms/kg i.v.", "entity1": "5-HT3", "entity2": "amoxapine", "span1": [124, 129], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4755": {"label": 8, "data": {"text": "However, whether increasing EETs production by CYP2J2 overexpression in vivo could prevent abdominal aortic aneurysm (AAA) remains unknown.", "entity1": "CYP2J2", "entity2": "EETs", "span1": [47, 53], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14321": {"label": 1, "data": {"text": "Dimethylfumarate attenuates renal fibrosis via NF-E2-related factor 2-mediated inhibition of transforming growth factor-beta/Smad signaling.", "entity1": "NF-E2-related factor 2", "entity2": "Dimethylfumarate", "span1": [47, 69], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10345": {"label": 3, "data": {"text": "Arsenite triggered strong induction of HSPs, which was prevented by 1 micro g/mL cycloheximide (CXH).", "entity1": "HSPs", "entity2": "cycloheximide", "span1": [39, 43], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13662": {"label": 1, "data": {"text": "High-resolution NMR spectroscopy was used to determine the docking of a substrate (prostaglandin H2) mimic (U46619) to the engineered prostacyclin (PGI2) synthase (PGIS) in solution.", "entity1": "prostacyclin (PGI2) synthase", "entity2": "prostaglandin H2", "span1": [134, 162], "span2": [83, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"136": {"label": 3, "data": {"text": "Calmodulin was relatively ineffective in preventing inhibition of cAMP phosphodiesterase by felodipine and the p-chloro analogue.", "entity1": "cAMP phosphodiesterase", "entity2": "p-chloro", "span1": [66, 88], "span2": [111, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1813": {"label": 3, "data": {"text": "In comparison to diphenylhydantoin, the novel chloro-substituted alpha-hydroxyphenylamide compounds produced as much as a 20-fold greater tonic and frequency-dependent blockade of Na(V)1.5 channels with an IC(50) value of 14.5 microM.", "entity1": "Na(V)1.5", "entity2": "chloro", "span1": [180, 188], "span2": [46, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9008": {"label": 9, "data": {"text": "These findings suggest that limitation of SRF was produced by binding of BDZs, but not beta CCs, to voltage-dependent sodium channels and not to high affinity central BDZ receptors, and that BDZs limit SRF by slowing recovery of sodium channels from inactivation.", "entity1": "voltage-dependent sodium channels", "entity2": "beta CCs", "span1": [100, 133], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"3311": {"label": 1, "data": {"text": "The main findings from this study were as follows: 1) cTnC mutants demonstrated distinct functional phenotypes reminiscent of bona fide HCM, RCM, and DCM mutations; 2) a region in cTnC associated with increased Ca(2+) sensitivity in skinned fibers was identified; and 3) the F27W reporter mutation affected Ca(2+) sensitivity, maximal force, and ATPase activation of some mutants.", "entity1": "cTnC", "entity2": "Ca(2+)", "span1": [180, 184], "span2": [211, 217]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3142": {"label": 1, "data": {"text": "Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization.", "entity1": "TrkA", "entity2": "Amitriptyline", "span1": [53, 57], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"192": {"label": 9, "data": {"text": "The nonsteroidal antiandrogen RU 23908 ( Anandron ) weakly interacts with the prostatic cytosolic androgen receptor and shows a fast dissociation rate.", "entity1": "androgen receptor", "entity2": "RU 23908", "span1": [98, 115], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13925": {"label": 1, "data": {"text": "In pig parathyroid cells, paricalcitol and the active form of doxercalciferol induced VDR translocation from the cytoplasm into the nucleus, suppressed PTH mRNA expression and inhibited cell proliferation in a similar manner, although paricalcitol induced the expression of CaSR mRNA more effectively.", "entity1": "VDR", "entity2": "doxercalciferol", "span1": [86, 89], "span2": [62, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7519": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMP-activated protein kinase", "entity2": "5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside", "span1": [24, 52], "span2": [120, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1615": {"label": 5, "data": {"text": "Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topiramate in rat basolateral amygdala neurons.", "entity1": "GluR5", "entity2": "topiramate", "span1": [24, 29], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13208": {"label": 8, "data": {"text": "SecS required selenophosphate and O-phosphoseryl-tRNA([Ser]Sec) as substrates to generate selenocysteyl-tRNA([Ser]Sec).", "entity1": "SecS", "entity2": "selenophosphate", "span1": [0, 4], "span2": [14, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8313": {"label": 3, "data": {"text": "Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).", "entity1": "NPY", "entity2": "acylethanolamide", "span1": [158, 161], "span2": [6, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1649": {"label": 5, "data": {"text": "The 5-HT(1/2/5/7)-receptor antagonist methysergide and the 5-HT(2A/2B/2C)-receptor antagonist LY 53857 enhanced clomipramine-induced hyperglycemia, while the 5-HT(1A/1B)-receptor antagonist (-)-propranolol and the 5-HT(3/4)-receptor antagonist tropisetron did not affect it.", "entity1": "5-HT(1A/1B)-receptor", "entity2": "(-)-propranolol", "span1": [158, 178], "span2": [190, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7371": {"label": 1, "data": {"text": "Furthermore, with respect to GSTM1 and GSTT1 there were statistically significant differences in TTCA-levels between genotypes among exposed workers but not among controls.", "entity1": "GSTM1", "entity2": "TTCA", "span1": [29, 34], "span2": [97, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15542": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "TIMP-1", "entity2": "DMN", "span1": [214, 220], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3746": {"label": 3, "data": {"text": "Although both intracellular and membrane Cx43 pools were markedly reduced in cells released from contact inhibition by TCDD, siRNA-mediated Cx43 knock-down was not sufficient to stimulate proliferation in contact-inhibited cells.", "entity1": "Cx43", "entity2": "TCDD", "span1": [140, 144], "span2": [119, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10188": {"label": 3, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP8", "entity2": "Rifampicin", "span1": [37, 42], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10585": {"label": 1, "data": {"text": "Plasma from duloxetine-treated subjects (ex vivo effect) dose-dependently decreased radioligand binding to human NET (maximum inhibition was 60%) (P=0.02).", "entity1": "human NET", "entity2": "duloxetine", "span1": [107, 116], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14736": {"label": 3, "data": {"text": "We hypothesized that hypoxia induced testicular damage is mediated by an activated NADPH oxidase (NOX), therefore, APO (apocynin) an inhibitor of NOX and raisanberine (RS), a calcium influx inhibitor were tested if they could attenuate hypoxic toxicity to the testis.", "entity1": "NOX", "entity2": "APO", "span1": [146, 149], "span2": [115, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6190": {"label": 5, "data": {"text": "These data indicate that mixed 5-HT1/5-HT2 receptor antagonists such as pizotifen and methysergide, and mixed 5-HT and catecholamine antagonists such as mianserin and mirtazapine are more potent antagonists of mCPP-induced behavioural inhibition in rats than the more selective 5-HT2A/5-HT2C antagonist ritanserin.", "entity1": "5-HT1", "entity2": "methysergide", "span1": [31, 36], "span2": [86, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14095": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "thalidomide", "span1": [142, 146], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2369": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "MEK", "entity2": "BAY 43-9006", "span1": [75, 78], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"769": {"label": 9, "data": {"text": "Compared with WT, DeltaKPQ I(Na) was more sensitive to flecainide, and flecainide preferentially inhibited late I(Na) (mean current between 20 and 23.5 ms after depolarization) compared with peak I(Na).", "entity1": "DeltaKPQ", "entity2": "Na", "span1": [18, 26], "span2": [29, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10815": {"label": 3, "data": {"text": "We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays.", "entity1": "cyclooxygenases", "entity2": "meloxicam", "span1": [111, 126], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10505": {"label": 9, "data": {"text": "Exploration of potential mechanisms of resistance in SUM185 cells revealed failure of GW572016 to inhibit downstream ERK and Akt activation, despite inhibition of HER2 phosphorylation.", "entity1": "ERK", "entity2": "GW572016", "span1": [117, 120], "span2": [86, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14239": {"label": 2, "data": {"text": "Furthermore, salubrinal, a specific eIF2\u03b1 phosphorylation-inducing agent, increased CHOP and DR5 expression in the presence of VA.", "entity1": "DR5", "entity2": "salubrinal", "span1": [93, 96], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12125": {"label": 9, "data": {"text": "In addition, the stereospecificity required at opioid receptors appears to be retained at the nociceptin receptor, since (+)-quadazocine is inactive at both receptors.", "entity1": "nociceptin receptor", "entity2": "(+)-quadazocine", "span1": [94, 113], "span2": [121, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4825": {"label": 1, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "Akt", "entity2": "7KC", "span1": [194, 197], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3777": {"label": 1, "data": {"text": "Both 5'-AMN and 5'-MABN had high affinity for \u03ba-receptors (K (i) 1.36 \u00b1 0.98 and 0.27 \u00b1 0.08, respectively) and were revealed as potent \u03ba-antagonists (pA(2) 7.43 and 8.18, respectively) and \u03bc-receptor antagonists (pA(2) 7.62 and 7.85, respectively) in the ileum.", "entity1": "\u03ba-receptors", "entity2": "5'-MABN", "span1": [46, 57], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2392": {"label": 0, "data": {"text": "The x-ray co-crystal structure of LeuRS showed that a C-terminal extension of about 60 amino acids forms a discrete domain, which is unique among the LeuRSs and interacts with the corner of the L-shaped tRNALeu.", "entity1": "LeuRSs", "entity2": "amino acids", "span1": [150, 156], "span2": [87, 98]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7321": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SLC38", "entity2": "amino acids", "span1": [258, 263], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6133": {"label": 5, "data": {"text": "We have investigated the effects of CP-99,994 [(+)-(2s,3s)-3-(2-methoxybenzylamino)-2-phenylpiperidine], a tachykinin NK1 receptor antagonist, HOE 140 (D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin), a bradykinin B2 receptor antagonist, and ketotifen (4-(1-methyl-4-piperidylidene)4 H-benzo[4,5]cycloheptal[1,2-b]thiophen-10(9H)-one hydrogen fumarate), a histamine H1 receptor antagonist with mast cell-stabilizing properties, on microvascular leakage induced by gaseous formaldehyde.", "entity1": "histamine H1 receptor", "entity2": "ketotifen", "span1": [348, 369], "span2": [234, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11068": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "cAMP phosphodiesterase", "entity2": "Ca2+", "span1": [86, 108], "span2": [181, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11450": {"label": 1, "data": {"text": "The present study examined the reinforcing and DAT effects of the local anesthetics dimethocaine, procaine and cocaine using in vivo techniques.", "entity1": "DAT", "entity2": "dimethocaine", "span1": [47, 50], "span2": [84, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13781": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "CI-1033", "span1": [14, 16], "span2": [158, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13743": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "Ca(v)1.3", "entity2": "DHP", "span1": [56, 64], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8999": {"label": 4, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "R-PIA", "span1": [0, 9], "span2": [53, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8455": {"label": 3, "data": {"text": "In the present study, hinokitiol (1 and 2\u03bcM) inhibited the collagen-induced aggregation of human platelets, but did not inhibit the activation of platelets by other agonists, including thrombin, arachidonic acid, and ADP.", "entity1": "collagen", "entity2": "hinokitiol", "span1": [59, 67], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1182": {"label": 3, "data": {"text": "Nateglinide inhibits Kir6.2/SUR1 and Kir6.2/SUR2B channels at 100 nM, and inhibits Kir6.2/SUR2A channels at high concentrations (1 microM).", "entity1": "SUR2A", "entity2": "Nateglinide", "span1": [90, 95], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14174": {"label": 2, "data": {"text": "LXRs are thought to be activated predominantly by oxysterols generated enzymatically from cholesterol in different cell organelles.", "entity1": "LXRs", "entity2": "oxysterols", "span1": [0, 4], "span2": [50, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5114": {"label": 2, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "Nrf2", "entity2": "5HHMF", "span1": [58, 62], "span2": [126, 131]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14287": {"label": 9, "data": {"text": "Valpromide (VPD), the amide derivative of VPA, does not inhibit HDAC activity and is a weak teratogen in vivo.", "entity1": "HDAC", "entity2": "Valpromide", "span1": [64, 68], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8255": {"label": 1, "data": {"text": "Results indicate that 5-HT2C receptor agonists and antagonists attenuate the DOI-elicited-HTR in C57Bl/6J mice, and suggest that structurally diverse 5-HT2C ligands result in different 5-HT2C receptor signaling outcomes compared to DOI.", "entity1": "5-HT2C", "entity2": "DOI", "span1": [185, 191], "span2": [232, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7150": {"label": 2, "data": {"text": "Binding of cGMP to GAF-A increases cNPK phosphorylation of PDE5 and improves catalytic site affinity for cGMP or inhibitors.", "entity1": "cNPK", "entity2": "cGMP", "span1": [35, 39], "span2": [11, 15]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6981": {"label": 1, "data": {"text": "Bisoprolol markedly suppressed the dobutamine-induced PRA increase in Arg389- but only marginally in Gly389-beta1AR subjects.", "entity1": "beta1AR", "entity2": "Bisoprolol", "span1": [108, 115], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1846": {"label": 8, "data": {"text": "Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [31, 36], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8462": {"label": 3, "data": {"text": "Hinokitiol inhibited the phosphorylation of phospholipase C (PLC)\u03b32, protein kinase C (PKC), mitogen-activated protein kinases (MAPKs), and Akt in collagen-activated human platelets, and significantly reduced intracellular calcium mobilization and hydroxyl radical (OH) formation.", "entity1": "collagen", "entity2": "Hinokitiol", "span1": [147, 155], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11947": {"label": 8, "data": {"text": "Ketamine is primarily metabolized to norketamine by hepatic cytochrome P450 (CYP) 2B6 and CYP3A4-mediated N-demethylation.", "entity1": "CYP3A4", "entity2": "Ketamine", "span1": [90, 96], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7241": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "POHA", "span1": [231, 237], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10422": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "RARbeta", "entity2": "tazarotenic acid", "span1": [132, 139], "span2": [61, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14652": {"label": 3, "data": {"text": "A series of compounds based on a 4-phenyl-2-phenylaminopyridine scaffold that are potent and selective inhibitors of Traf2- and Nck-interacting kinase (TNIK) activity are described.", "entity1": "Traf2- and Nck-interacting kinase", "entity2": "4-phenyl-2-phenylaminopyridine", "span1": [117, 150], "span2": [33, 63]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9885": {"label": 1, "data": {"text": "UNLABELLED: Apparent muscarinic acetylcholine (mAch) receptor occupancy in mouse cerebral cortex, hippocampus, and striatum by scopolamine, an antagonist, and biperiden, a relatively selective M1 antagonist, was estimated with competitive binding studies using two different radioligands: 3H-N-methyl piperidyl benzilate (3H-NMPB) and 3H-quinuclidinyl benzilate (3H-QNB).", "entity1": "muscarinic acetylcholine (mAch) receptor", "entity2": "3H-NMPB", "span1": [21, 61], "span2": [322, 329]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13368": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "CRP-ductin", "entity2": "estrogen", "span1": [119, 129], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13992": {"label": 3, "data": {"text": "Collectively, these data suggest that cabozantinib is a promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling.", "entity1": "VEGFR", "entity2": "cabozantinib", "span1": [158, 163], "span2": [38, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2323": {"label": 1, "data": {"text": "The binding of [3H]prazosin to alpha1-adrenergic receptors in the cerebral cortex of NET-/- mice was also decreased, most probably as an adaptive response to the sustained elevation of extracellular NE levels observed in these mice.", "entity1": "alpha1-adrenergic receptors", "entity2": "[3H]prazosin", "span1": [31, 58], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10054": {"label": 3, "data": {"text": "Cembranoids are naturally occurring, uncharged noncompetitive inhibitors of peripheral and neuronal AChRs, which have no demonstrable general anesthetic activity in vivo.", "entity1": "AChRs", "entity2": "Cembranoids", "span1": [100, 105], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15232": {"label": 3, "data": {"text": "In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17\u03b2-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated.", "entity1": "OATP1B3", "entity2": "flavonolignans", "span1": [43, 50], "span2": [179, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15316": {"label": 4, "data": {"text": "Moreover, the effects of the DRD3 agonist 7-hydroxy-N,N-dipropyl-2-aminotetralin (7-OH-DPAT)-induced locomotor hypoactivity were significantly increased when DRD3 proteins were abundant.", "entity1": "DRD3", "entity2": "7-OH-DPAT", "span1": [29, 33], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8947": {"label": 9, "data": {"text": "The 3 beta-hydroxysteroid substrate, pregnenolone, protects isomerase as well as dehydrogenase from inactivation by FSA.", "entity1": "dehydrogenase", "entity2": "3 beta-hydroxysteroid", "span1": [81, 94], "span2": [4, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4788": {"label": 3, "data": {"text": "Lineweaver-Burk plots demonstrated that baicalin inhibited the activities of CYP2D and CYP3A in a non-competitive manner in rat liver microsomes (RLMs).", "entity1": "CYP2D", "entity2": "baicalin", "span1": [77, 82], "span2": [40, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3106": {"label": 2, "data": {"text": "Prolonged use of tolvaptan leads to increased endogenous levels of AVP and perhaps over-stimulation of V(1A) receptors.", "entity1": "AVP", "entity2": "tolvaptan", "span1": [67, 70], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12200": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "LA", "span1": [282, 285], "span2": [220, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5416": {"label": 8, "data": {"text": "In functional transport assays, we found that one of the identified molecules, ATM7, increased the reuptake of serotonin, possibly by facilitating the interaction of serotonin with transport-ready conformations of SERT when concentrations of serotonin were low and rate limiting.", "entity1": "SERT", "entity2": "serotonin", "span1": [214, 218], "span2": [242, 251]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6721": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "AG1296", "span1": [273, 279], "span2": [74, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1283": {"label": 1, "data": {"text": "Rheumatoid synovial cells expressed PPARgamma mRNA, and the PPARgamma ligands 15-deoxy-Delta(12,14)-prostaglandin J(2) and troglitazone reduced the proliferation and induced apoptosis in synovial cells.", "entity1": "PPARgamma", "entity2": "troglitazone", "span1": [60, 69], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7203": {"label": 1, "data": {"text": "Estradiol (E2) stimulates BC cells proliferation by binding the estrogen receptor (ER).", "entity1": "ER", "entity2": "Estradiol", "span1": [83, 85], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12789": {"label": 3, "data": {"text": "Valdecoxib showed similar activity in the human whole-blood COX assay (COX-2 IC(50) = 0.24 microM; COX-1 IC(50) = 21.9 microM).", "entity1": "COX-1", "entity2": "Valdecoxib", "span1": [99, 104], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4862": {"label": 0, "data": {"text": "Only FFAs that increased ceramides caused impairment of AKt and PTP1B phosphorylation at Ser 50.", "entity1": "PTP1B", "entity2": "Ser", "span1": [64, 69], "span2": [89, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14161": {"label": 4, "data": {"text": "In rat striatum and nucleus accumbens, mianserin stimulated [35S]GTPgammaS binding in a nor-BNI-sensitive manner with maximal effects lower than those of the full kappa-opioid agonists (-)-U50,488 and dynorphin A.", "entity1": "kappa-opioid", "entity2": "dynorphin A", "span1": [163, 175], "span2": [201, 212]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3569": {"label": 1, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u.", "entity1": "IR", "entity2": "MSG", "span1": [24, 26], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7819": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "GluR5", "entity2": "LY293558", "span1": [183, 188], "span2": [360, 368]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3545": {"label": 2, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "CysLT(1)R", "entity2": "LTD4", "span1": [36, 45], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6146": {"label": 0, "data": {"text": "There are 3-4 drug binding sites in the N- and C-terminal domains of intact cTnC that exhibit fast exchange on the NMR time scale.", "entity1": "cTnC", "entity2": "N", "span1": [76, 80], "span2": [40, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12764": {"label": 1, "data": {"text": "This study compared the sedative profiles of the second-generation antihistamines, fexofenadine and cetirizine, using 3 different criteria: subjective sleepiness evaluated by the Stanford Sleepiness Scale, objective psychomotor tests (simple and choice reaction time tests and visual discrimination tests at 4 different exposure durations), and measurement of histamine H1-receptor occupancy (H1RO) in the brain.", "entity1": "histamine H1-receptor", "entity2": "cetirizine", "span1": [360, 381], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8944": {"label": 9, "data": {"text": "Unlike bacterial 3-keto-5-ene-steroid isomerase, the human isomerase reaction is stimulated by diphosphopyridine nucleotides (NADH, NAD+).", "entity1": "3-keto-5-ene-steroid isomerase", "entity2": "diphosphopyridine nucleotides", "span1": [17, 47], "span2": [95, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14041": {"label": 5, "data": {"text": "Both outward currents were significantly reduced by the mGluR antagonist MCPG and the CHPG-induced current was blocked by the specific mGluR(5) antagonist MTEP.", "entity1": "mGluR(5)", "entity2": "MTEP", "span1": [135, 143], "span2": [155, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16027": {"label": 1, "data": {"text": "Administration of haloperidol increased Ser240/244 phosphorylation in a subpopulation of GABA-ergic medium spiny neurons (MSNs), which express dopamine D2 receptors (D2Rs).", "entity1": "D2Rs", "entity2": "haloperidol", "span1": [166, 170], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1827": {"label": 8, "data": {"text": "QR2 catalyzes the two-electron reduction of menadione via the oxidation of N-alkylated or N-ribosylated nicotinamides.", "entity1": "QR2", "entity2": "N-alkylated", "span1": [0, 3], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14505": {"label": 0, "data": {"text": "Keap1 is expressed in differentiating osteoclast-like cells and the S349T mutation selectively impairs the SQSTM1-Keap1 interaction in co-immunoprecipitations, which molecular modelling indicates results from effects on critical hydrogen bonds required to stabilise the KIR-Keap1 complex.", "entity1": "KIR", "entity2": "hydrogen", "span1": [270, 273], "span2": [229, 237]}, "weak_labels": [-1, -1, 0, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6255": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "norepinephrine transporter", "entity2": "zotepine", "span1": [182, 208], "span2": [226, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15230": {"label": 1, "data": {"text": "The extent of silymarin-drug interactions depends on OATP isoform specificity and concentrations of flavonolignans at the site of drug transport.", "entity1": "OATP", "entity2": "flavonolignans", "span1": [53, 57], "span2": [100, 114]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9590": {"label": 5, "data": {"text": "These results indicate that carbetocin is a partial agonist/antagonist to the oxytocin receptor while the two metabolites carbetocin metabolite I and carbetocin metabolite II are pure antagonists.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [78, 95], "span2": [122, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8360": {"label": 3, "data": {"text": "Amino acid derived quinazolines as Rock/PKA inhibitors.", "entity1": "PKA", "entity2": "quinazolines", "span1": [40, 43], "span2": [19, 31]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7375": {"label": 1, "data": {"text": "Histamine regulates many functions by binding to four histamine G-coupled receptor proteins (H1R, H2R, H3R and H4R).", "entity1": "histamine G-coupled receptor proteins", "entity2": "Histamine", "span1": [54, 91], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2988": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Y612A", "entity2": "sildenafil", "span1": [173, 178], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4510": {"label": 3, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "hCES2", "entity2": "acyl glucuronides", "span1": [143, 148], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13036": {"label": 8, "data": {"text": "By contrast, 11beta-HSD2 plays a pivotal role in aldosterone target tissues where it catalyses the opposite reaction (i.e. inactivation of cortisol to cortisone) to prevent activation of the mineralocorticoid receptor (MR) by cortisol.", "entity1": "11beta-HSD2", "entity2": "cortisol", "span1": [13, 24], "span2": [139, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9775": {"label": 4, "data": {"text": "Parenteral administration of selective agonists of the delta-opioid receptor (SB 227122), mu-opioid receptor (codeine and hydrocodone), and kappa-opioid receptor (BRL 52974) produced dose-related inhibition of citric acid-induced cough with ED(50) values of 7.3, 5.2, 5.1, and 5.3 mg/kg, respectively.", "entity1": "kappa-opioid receptor", "entity2": "BRL 52974", "span1": [140, 161], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1025": {"label": 2, "data": {"text": "Activation of endogenous somatostatin receptor subtype 2 (sst2) by somatostatin-14 or activation of transiently transfected rat D2 dopamine receptors (rD2(long)) by quinpirole had no effect.", "entity1": "rat D2 dopamine receptors", "entity2": "quinpirole", "span1": [124, 149], "span2": [165, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7035": {"label": 2, "data": {"text": "Further, cholesterol metabolites, predominantly the oxysterols, the natural ligands for liver X receptor (LXR), induced these genes via upregulation of sterol regulatory element binding protein-1c (SREBP-1c) that bound to the regulatory regions of these genes.", "entity1": "SREBP-1c", "entity2": "oxysterols", "span1": [198, 206], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"564": {"label": 1, "data": {"text": "These results suggest that a complex of Ig module II and heparan sulfate is the base common active core of the FGFR ectodomain and that flanking structural domains modify FGF affinity and determine specificity.", "entity1": "Ig module II", "entity2": "sulfate", "span1": [40, 52], "span2": [65, 72]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14766": {"label": 1, "data": {"text": "Electrical Stimuli Release ATP to Increase GLUT4 Translocation and Glucose Uptake via PI3K\u03b3-Akt-AS160 in Skeletal Muscle Cells.", "entity1": "GLUT4", "entity2": "ATP", "span1": [43, 48], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12152": {"label": 0, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "Lys", "span1": [150, 156], "span2": [81, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8024": {"label": 8, "data": {"text": "Dual function inhibitors targeting phospholipase A(2) (PLA(2)) and leukotriene A(4) hydrolase (LTA(4)H) may balance the arachidonic acid (AA) metabolic network and be used as new anti-inflammatory drugs.", "entity1": "phospholipase A(2)", "entity2": "arachidonic acid", "span1": [35, 53], "span2": [120, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2485": {"label": 1, "data": {"text": "To address this issue and taking into account that effects of synthetic progestins are not only referable to action through the progesterone receptor but may also be mediated by other steroid receptors, we characterized cardiovascular function and inflammatory gene expression in aldosterone salt-treated rats on long-term administration of 17beta-estradiol, medroxyprogesterone acetate, and drospirenone, a new progestogen exhibiting antimineralocorticoid activity.", "entity1": "steroid receptors", "entity2": "progestins", "span1": [184, 201], "span2": [72, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"435": {"label": 1, "data": {"text": "Ka values in nM for rauwolscine (19), WB-4101 (265), SKF-104078 (197), spiroxatrine (128), and prazosin (1531) for blocking relaxation in rat arteries were consistent with their affinities for binding at the alpha-2D adrenoceptor subtype.", "entity1": "alpha-2D adrenoceptor", "entity2": "spiroxatrine", "span1": [208, 229], "span2": [71, 83]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4904": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "matrix metalloproteinases", "entity2": "kinsenoside", "span1": [352, 377], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8064": {"label": 3, "data": {"text": "Moreover, paclitaxel-induced ERCC1 protein and mRNA levels significantly decreased via the downregulation of p38 activity by either a p38 MAPK inhibitor SB202190 or p38 knockdown with specific small interfering RNA (siRNA).", "entity1": "MAPK", "entity2": "SB202190", "span1": [138, 142], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6479": {"label": 2, "data": {"text": "The temporal profile of butyrylcholinesterase (BuChE) and in vitro pralidoxime-reactivated BuChE was studied in a cohort of 25 organophosphate-poisoned patients to examine their relationship to the development of intermediate syndrome and to understand reasons for lack of efficacy of oxime treatment.", "entity1": "BuChE", "entity2": "pralidoxime", "span1": [91, 96], "span2": [67, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"710": {"label": 1, "data": {"text": "In the present study, the ability of different concentrations of torasemide to modify angiotensin II (Ang II)-induced vascular responses was examined, with the use of an organ bath system, in endothelium-denuded aortic rings from spontaneously hypertensive rats.", "entity1": "angiotensin II", "entity2": "torasemide", "span1": [86, 100], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8602": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "AST", "entity2": "CCl4", "span1": [31, 34], "span2": [78, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15763": {"label": 3, "data": {"text": "Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors.", "entity1": "acetylcholinesterase", "entity2": "tetrahydrocurcuminoid dihydropyrimidinone", "span1": [76, 96], "span2": [14, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"214": {"label": 5, "data": {"text": "Alprenolol and BAAM also caused surmountable antagonism of isoprenaline responses, and this beta 1-adrenoceptor antagonism was slowly reversible.", "entity1": "beta 1-adrenoceptor", "entity2": "Alprenolol", "span1": [92, 111], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6994": {"label": 2, "data": {"text": "On the other hand, holocarboxylase synthetase (HCS) mRNA levels were markedly low in the deficient animals, and increased upon biotin injection.", "entity1": "HCS", "entity2": "biotin", "span1": [47, 50], "span2": [127, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10234": {"label": 3, "data": {"text": "The PAO inhibitor, MDL-72,527, only partially blocked oxidation of spermine while a previously reported PAO substrate, N (1)-( n -octanesulphonyl)spermine, potently inhibited the reaction.", "entity1": "PAO", "entity2": "MDL-72,527", "span1": [4, 7], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13967": {"label": 3, "data": {"text": "With exposure to rofecoxib, a selective COX-2 inhibitor, breast cancer risk reduction was appreciable (46%), suggesting a possible role for selective COX-2 inhibitors in breast cancer prophylaxis.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [40, 45], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2500": {"label": 8, "data": {"text": "Licofelone almost abolished 5-LOX activity by inhibiting leukotriene B4 generation in rabbit neutrophils and prevented platelet thromboxane B2 production from whole blood.", "entity1": "5-LOX", "entity2": "leukotriene B4", "span1": [28, 33], "span2": [57, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"137": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited Ca2+/calmodulin-dependent caldesmon kinase with similar potencies (IC50 = 17.4 microM), whereas the oxidized and t-butyl analogues caused no inhibition.", "entity1": "caldesmon kinase", "entity2": "Felodipine", "span1": [73, 89], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15961": {"label": 1, "data": {"text": "Collectively, our data indicate that OHT contributes to the production of proteolyzed cyclin E via GPR30 with augmented migration in MCF-7 cells.", "entity1": "GPR30", "entity2": "OHT", "span1": [99, 104], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11799": {"label": 1, "data": {"text": "Thus, COL8A2 was identified as the key protein involved in the enhancement of cell adhesion of atRA under serum-free conditions.", "entity1": "COL8A2", "entity2": "atRA", "span1": [6, 12], "span2": [95, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7334": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT2", "entity2": "glutamine", "span1": [247, 252], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2758": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "human COX-2", "entity2": "2,6-dimethyl", "span1": [75, 86], "span2": [107, 119]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2048": {"label": 3, "data": {"text": "Increased immunohistochemical labeling of HIF-1alpha, VEGF, and BNP in the ventricular myocardium was observed in the shunt group and carvedilol again normalized the labeling.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [54, 58], "span2": [134, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"861": {"label": 2, "data": {"text": "The above results indicate that polyamine depletion delays the onset of apoptosis in IEC-6 cells and confers protection against DNA damaging agents, suggesting that polyamines might be involved in the caspase activating signal cascade.", "entity1": "caspase", "entity2": "polyamines", "span1": [201, 208], "span2": [165, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7077": {"label": 2, "data": {"text": "Menthol, popularly known for its cooling effect, activates TRPM8--a cold-activated thermoTRP ion channel.", "entity1": "TRPM8", "entity2": "Menthol", "span1": [59, 64], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4960": {"label": 1, "data": {"text": "Computational docking studies combined with site-direct mutagenesis identified several key residues within the ligand binding pocket of PXR that constitute points of interaction with amprenavir.", "entity1": "PXR", "entity2": "amprenavir", "span1": [136, 139], "span2": [183, 193]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1167": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "mitiglinide", "span1": [161, 165], "span2": [180, 191]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7069": {"label": 2, "data": {"text": "Retinoid is a collective term for compounds which bind to and activate retinoic acid receptors (RARalpha, beta, gamma and RXRalpha, beta, gamma), members of nuclear hormone receptor superfamily.", "entity1": "retinoic acid receptors", "entity2": "Retinoid", "span1": [71, 94], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13599": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "tricyclic", "span1": [379, 383], "span2": [420, 429]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13488": {"label": 3, "data": {"text": "Modulation of the function of CD36 (CD36-/- mice), p38(MAPK) (SB203580), COX-1 (indomethacin), and glycoprotein Ib alpha (Nk-protease, 6D1 antibody) induced approximately 50% inhibition.", "entity1": "p38", "entity2": "SB203580", "span1": [51, 54], "span2": [62, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7386": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "Delta(1)-pyrroline-5-carboxylate dehydrogenase", "entity2": "glutamate", "span1": [34, 80], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12866": {"label": 1, "data": {"text": "This aminophospholipid \"flippase\" selectively transports PS to the cytosolic leaflet of the bilayer and is sensitive to vanadate, Ca(2+), and modification by sulfhydryl reagents.", "entity1": "flippase", "entity2": "vanadate", "span1": [24, 32], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11982": {"label": 8, "data": {"text": "Doxorubicin is mainly excreted into the bile via P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (Mrp2) in hepatobiliary route and metabolized via cytochrome P450 (CYP) 3A subfamily.", "entity1": "Mrp2", "entity2": "Doxorubicin", "span1": [118, 122], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7044": {"label": 1, "data": {"text": "Experiments with Schwann cell primary cultures revealed an effect of retinoic acid on the expression of the neuregulin receptor ErbB3, suggesting that one function of retinoic acid consists in the regulation of neuroglial interactions after peripheral nerve injury.", "entity1": "ErbB3", "entity2": "retinoic acid", "span1": [128, 133], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5166": {"label": 8, "data": {"text": "At a substrate concentration of 20\u2009\u00b5M, the most active HFC glucuronidation catalysts were UGT1A10 followed by UGT1A6 >UGT1A7 >UGT2A1, whereas at 300\u2009\u00b5M UGT1A6 was about 10 times better catalyst than the other recombinant UGTs.", "entity1": "UGT1A7", "entity2": "HFC", "span1": [118, 124], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"14081": {"label": 3, "data": {"text": "In TGF-\u03b21-induced NPDFs, berberine significantly inhibited the expression of \u03b1-SMA and collagen type I mRNA and reduced \u03b1-SMA and collagen protein levels.", "entity1": "\u03b1-SMA", "entity2": "berberine", "span1": [120, 125], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7998": {"label": 3, "data": {"text": "ISO is able to induce apoptosis through mitochondrial dysfunction and inhibition of PI3K/Akt signaling pathway in HepG2 cells, however, the effects of ISO on MAPK signaling pathways remain unknown.", "entity1": "Akt", "entity2": "ISO", "span1": [89, 92], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14308": {"label": 1, "data": {"text": "Cu-dependent tyrosinase activity was also markedly reduced in both types of CLDN knockdown cells when incubated with the substrate l-DOPA.", "entity1": "tyrosinase", "entity2": "Cu", "span1": [13, 23], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13243": {"label": 3, "data": {"text": "Here we report that glutamate stimulation caused a rapid reduction in protein levels of GRIP1, but not that of glutamate receptor (GluR) 1, GluR2 and protein interacting with C kinase 1 (PICK1) in rat primary cortical neuron cultures.", "entity1": "GRIP1", "entity2": "glutamate", "span1": [88, 93], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6150": {"label": 1, "data": {"text": "Drug dependent changes in the NMR heteronuclear single-quantum coherence spectra of [methyl-13C]Met-labeled cTnC indicate that bepridil and trifluoperazine bind to similar sites but only in the presence of Ca2+.", "entity1": "cTnC", "entity2": "methyl-13C", "span1": [108, 112], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8158": {"label": 3, "data": {"text": "Additionally, DPEP suppressed the production of inflammatory cytokines, including tumor necrosis factor-\u03b1 (TNF-\u03b1), interleukin (IL)-1\u03b2, and IL-6.", "entity1": "IL-6", "entity2": "DPEP", "span1": [140, 144], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"805": {"label": 2, "data": {"text": "Specifically, aniracetam, which potentiates wild-type AMPA receptors, is ineffective on the non-desensitizing GluR3(L507Y) mutant, but has synergistic effects with lithium on wild-type receptors.", "entity1": "GluR3", "entity2": "lithium", "span1": [110, 115], "span2": [164, 171]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10418": {"label": 3, "data": {"text": "CONCLUSIONS: Inhibition of PDE4 by rolipram unmasks beta(2)-adrenergic blockade of LTC(4) synthesis caused by FMLP/B.", "entity1": "PDE4", "entity2": "rolipram", "span1": [27, 31], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15949": {"label": 9, "data": {"text": "4-Hydroxytamoxifen (OHT, tamoxifen's active form) failed to prevent E2-induced proteolysis of cyclin E and migration, but rather triggered cyclin E cleavage coincident with augmented migration.", "entity1": "cyclin E", "entity2": "OHT", "span1": [94, 102], "span2": [20, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5387": {"label": 2, "data": {"text": "Thus, the increase in mPFC DAT function was an SHR-specific long term consequence of methylphenidate treatment during adolescence, which may be responsible for the treatment-induced alterations in behavior including the observed increases in cocaine self-administration.", "entity1": "DAT", "entity2": "methylphenidate", "span1": [27, 30], "span2": [85, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5986": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "t-PA", "entity2": "epsilon-aminocaproic acid", "span1": [121, 125], "span2": [199, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11247": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "DAT", "entity2": "4',7,8-trichloro", "span1": [132, 135], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1872": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "DGAT", "entity2": "chalcone", "span1": [253, 257], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8114": {"label": 1, "data": {"text": "In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of fused oxadiazepines such as 7i which had an improved hERG inhibition profile and was a highly efficacious GSM in vitro and in vivo in rats.", "entity1": "hERG", "entity2": "oxadiazine", "span1": [102, 106], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12138": {"label": 2, "data": {"text": "To mechanistically evaluate this regional selectivity, we assessed cyclo-oxygenase-2 (COX-2) expression in the uninvolved mucosa and demonstrated a 3- to 4-fold excess in the distal relative to the proximal bowel in both MIN mice and AOM-treated rats.", "entity1": "COX-2", "entity2": "AOM", "span1": [86, 91], "span2": [234, 237]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3668": {"label": 3, "data": {"text": "Additionally, the mRNA levels of melanogenesis-related genes (c-KIT, stem cell factor (SCF), and macrophage migration inhibitory factor (MIF)) were down-regulated by artemisinic acid.", "entity1": "stem cell factor", "entity2": "artemisinic acid", "span1": [69, 85], "span2": [166, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8506": {"label": 1, "data": {"text": "Previous studies have revealed that the ATP binding step is crucial both for the power stroke to produce motility and for the inter-domain regulation of ATPase activity to guarantee the processive movement of dimeric KIFs.", "entity1": "ATPase", "entity2": "ATP", "span1": [153, 159], "span2": [40, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1857": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "kuraridin", "span1": [221, 251], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9038": {"label": 8, "data": {"text": "Inhibition of 5-lipoxygenase pathway of arachidonic acid metabolism in human neutrophils by sulfasalazine and 5-aminosalicylic acid.", "entity1": "5-lipoxygenase", "entity2": "arachidonic acid", "span1": [14, 28], "span2": [40, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14676": {"label": 3, "data": {"text": "Genistein also reduced the formation of stress fibers by thrombin and suppressed thrombin-induced phosphorylation of myosin light chain (MLC) on Ser(19)/Thr(18) in endothelial cells (ECs).", "entity1": "MLC", "entity2": "Genistein", "span1": [137, 140], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3868": {"label": 3, "data": {"text": "HSYA treatment also decreased NF-\u03baB p65 nuclear translocation and inhibited the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK).", "entity1": "MAPK", "entity2": "HSYA", "span1": [141, 145], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9348": {"label": 3, "data": {"text": "One group of experimental animals was treated with 5-lipoxygenase (5-LO) inhibitor, diethylcarbamazine (DEC, Sigma, St. Louis, Missouri) (50 mg/kg, i.v.", "entity1": "5-lipoxygenase", "entity2": "DEC", "span1": [51, 65], "span2": [104, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1686": {"label": 1, "data": {"text": "Memantine can interact with a variety of ligand-gated ion channels.", "entity1": "ligand-gated ion channels", "entity2": "Memantine", "span1": [41, 66], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11115": {"label": 1, "data": {"text": "Finally, a third nonadrenergic internal membrane site, labeled by [3H]IDX, was consistent with a subtype-I2 imidazol(in)e receptor site (rank order: cirazoline > IDX >> amiloride > moxonidine > clonidine).", "entity1": "subtype-I2 imidazol(in)e receptor", "entity2": "clonidine", "span1": [97, 130], "span2": [194, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"278": {"label": 4, "data": {"text": "Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha 2-adrenergic receptors and may act as a neurotransmitter.", "entity1": "imidazoline receptors", "entity2": "Agmatine", "span1": [59, 80], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8742": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "ketotifen", "span1": [18, 25], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14102": {"label": 1, "data": {"text": "CRBN mediated antiproliferative activities of lenalidomide and pomalidomide in myeloma cells, as well as lenalidomide- and pomalidomide-induced cytokine production in T cells.", "entity1": "CRBN", "entity2": "lenalidomide", "span1": [0, 4], "span2": [46, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11163": {"label": 8, "data": {"text": "Recombinant PDE10A transfected and expressed in COS-7 cells hydrolyzed cAMP and cGMP with Km values of 0.26 and 7.2 microM, respectively, and Vmax with cGMP was almost twice that with cAMP.", "entity1": "PDE10A", "entity2": "cGMP", "span1": [12, 18], "span2": [152, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4708": {"label": 3, "data": {"text": "Furthermore, V(5+) significantly inhibited the TCDD-induced AhR-dependent luciferase activity.", "entity1": "AhR", "entity2": "V(5+)", "span1": [60, 63], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10965": {"label": 5, "data": {"text": "After that, a wide range of concentrations of drugs, concomitantly with ATR (0.1 microM), was studied in the presence of haloperidol (HAL; 0.01 microM), a dopamine D2 antagonist.", "entity1": "dopamine D2", "entity2": "haloperidol", "span1": [155, 166], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4001": {"label": 3, "data": {"text": "Mechanisms limiting distribution of the threonine-protein kinase B-RaF(V600E) inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain metastases.", "entity1": "V600E", "entity2": "dabrafenib", "span1": [71, 76], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2788": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "PPT-A", "entity2": "sodium hydrosulphide", "span1": [248, 253], "span2": [119, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12557": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "TC", "entity2": "[57Co]cyanocobalamin", "span1": [228, 230], "span2": [154, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4094": {"label": 2, "data": {"text": "Furthermore, treatment with spironoclactone not only attenuated the pro-apoptotic effect of ALD but reversed the ALD-induced increase of calpain and AIF levels.", "entity1": "AIF", "entity2": "ALD", "span1": [149, 152], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10637": {"label": 3, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "Bsep", "entity2": "bosentan", "span1": [76, 80], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2912": {"label": 8, "data": {"text": "Coagulation-induced thromboxane B(2) and lipopolysaccharide-induced prostaglandin E(2) were measured ex vivo and in vitro in human whole blood as indices of COX-1 and COX-2 activity.", "entity1": "COX-2", "entity2": "prostaglandin E(2)", "span1": [167, 172], "span2": [68, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10853": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Glivec", "span1": [119, 122], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3650": {"label": 2, "data": {"text": "DBDCT up-regulated the expression of Bax, down-regulated the expression of Bcl-2, and significantly increased the ratio of Bax/Bcl-2.", "entity1": "Bcl-2", "entity2": "DBDCT", "span1": [127, 132], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7487": {"label": 3, "data": {"text": "Phenserine, a derivative of physostigmine, was first described as an inhibitor of acetylcholinesterase (AChE) and was shown to improve cognition in various experimental paradigms in rodents and dogs.", "entity1": "AChE", "entity2": "Phenserine", "span1": [104, 108], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3181": {"label": 2, "data": {"text": "CDCA induced dose-dependent expression of Cdx2 and MUC2 at both the mRNA and protein levels.", "entity1": "Cdx2", "entity2": "CDCA", "span1": [42, 46], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"950": {"label": 0, "data": {"text": "In addition, a partial nucleotide and amino acid sequence of the rabbit alpha(2A)-adrenoceptor (a region known to substantially influence the pharmacological characteristics of the alpha(2)-adrenoceptor) revealed marked differences between the rabbit and the human alpha(2A)-adrenoceptor.", "entity1": "rabbit alpha(2A)-adrenoceptor", "entity2": "amino acid", "span1": [65, 94], "span2": [38, 48]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15330": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "1-acetylpyrene", "span1": [287, 296], "span2": [128, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5685": {"label": 2, "data": {"text": "Sprague-Dawley rats treated with a non-selective cannabinoid agonist (CP55940, 50\u03bcg/kg, 7 days, i.p.) showed enhanced co-immunoprecipitation of \u03b2-Arrestin 2 and ERK1/2, enhanced pERK protein levels, and enhanced expression of \u03b2-Arrestin 2 mRNA and protein levels in PFCx.", "entity1": "\u03b2-Arrestin 2", "entity2": "CP55940", "span1": [144, 156], "span2": [70, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6203": {"label": 3, "data": {"text": "Cocaine block of hH1 channels was greater than block of mu1 channels at voltages between -120 mV and -90 mV, suggesting that greater steady-state inactivation of hH1 channels in this voltage range makes them more susceptible to cocaine block.", "entity1": "mu1 channels", "entity2": "Cocaine", "span1": [56, 68], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4985": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bcl2", "entity2": "Crocin", "span1": [155, 159], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16058": {"label": 8, "data": {"text": "Atorvastatin is also a CYP3A substrate, but less potent drug-drug interactions have been reported with CYP3A inhibitors.", "entity1": "CYP3A", "entity2": "Atorvastatin", "span1": [23, 28], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5139": {"label": 3, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "NF-\u03baB", "entity2": "5HHMF", "span1": [127, 132], "span2": [43, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1457": {"label": 3, "data": {"text": "Reserpine-induced ptosis was reversed by rasagiline at doses above 2 mg x kg(-1) i.p., which inhibit MAO-A as well as MAO-B, but not at MAO-B-selective doses.", "entity1": "MAO-B", "entity2": "rasagiline", "span1": [118, 123], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5399": {"label": 9, "data": {"text": "Furthermore, estrogen responsive genes in fish liver, ER\u03b1 and VTG, are not induced by CP[c]Ph, suggesting that the compound has no endocrine disrupting potential.", "entity1": "VTG", "entity2": "CP[c]Ph", "span1": [62, 65], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8651": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRB", "entity2": "ethanol", "span1": [28, 31], "span2": [61, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13167": {"label": 1, "data": {"text": "Progestin induction of the cyclin D1 gene, which lacks a progesterone response element, was dependent on PR activation of the Src/MAPK pathway, whereas induction of the Sgk (serum and glucocorticoid regulated kinase) gene that contains a functional progesterone response element was unaffected by mutations that interfere with PR activation of Src.", "entity1": "serum and glucocorticoid regulated kinase", "entity2": "Progestin", "span1": [174, 215], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15927": {"label": 1, "data": {"text": "Interestingly, polySia chains of secreted NCAM neutralized the cytotoxic activity of extracellular histones as well as DNA/histone-network-containing \"neutrophil extracellular traps\", which are formed during invasion of microorganisms.", "entity1": "histone", "entity2": "polySia", "span1": [123, 130], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8094": {"label": 3, "data": {"text": "PKAA/anti-TNF-\u03b1 siRNA nanocomplexes significantly reduced the ALT (alanine transaminase) and the hepatic cellular damages in APAP-intoxicated mice.", "entity1": "ALT", "entity2": "PKAA", "span1": [62, 65], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8476": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "HTRA1", "entity2": "Ala", "span1": [207, 212], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7040": {"label": 2, "data": {"text": "Hypermethlyation of RELN and GAD67 promoters can be induced by treating mice with methionine, and these mice display brain and behavioral abnormalities similar to +/rl.", "entity1": "RELN and GAD67 promoters", "entity2": "methionine", "span1": [20, 44], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8987": {"label": 3, "data": {"text": "Removing medium Ca2+, blocking Ca2+ channels with 50 mumol/l verapamil, or inhibiting calmodulin activation with 20 mumol/l trifluoperazine, 10 mumol/l chlorpromazine or 10 mumol/l pimozide almost completely blocked hyposmolarity-induced secretion.", "entity1": "Ca2+ channels", "entity2": "verapamil", "span1": [31, 44], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15219": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "inducible nitric oxide synthase", "entity2": "clerosterol", "span1": [296, 327], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12956": {"label": 9, "data": {"text": "Calcium-chelating reagents such as EDTA and 1,2-bis-(o-aminphenoxy)-ethane-N,N,N',N'-tetra-acetic acid tetra-acetoxy-methyl ester prevented the cleavage of GAD65.", "entity1": "GAD65", "entity2": "EDTA", "span1": [156, 161], "span2": [35, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6454": {"label": 3, "data": {"text": "RESULTS: Halothane anesthesia reversibly inhibited metabolic rhodopsin regeneration and thus prevented rhodopsin from absorbing high numbers of photons during light exposure.", "entity1": "rhodopsin", "entity2": "Halothane", "span1": [61, 70], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9162": {"label": 3, "data": {"text": "Chromatographic analysis of the metabolism of 14C-labeled arachidonic acid in this system revealed that PB-dependent inactivation of PHS is markedly increased in the presence of 100 microM H2O2.", "entity1": "PHS", "entity2": "H2O2", "span1": [133, 136], "span2": [189, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7919": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "oxaliplatin", "span1": [54, 59], "span2": [116, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"543": {"label": 3, "data": {"text": "DHODH inhibition occurs at lower concentrations of A77 1726 than that of tyrosine kinases and is currently considered the major mode of action.", "entity1": "tyrosine kinases", "entity2": "A77 1726", "span1": [73, 89], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10918": {"label": 3, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "gastric mucin", "entity2": "PP2", "span1": [4, 17], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9291": {"label": 5, "data": {"text": "ICI118,551 HCl (1.25-5 mg/kg, IP), a selective beta 2-adrenoceptor antagonist, also blocked the desipramine-induced enhancement of aggressive behavior in a dose-dependent manner, whereas metoprolol tartrate (5-20 mg/kg, IP), a selective beta 1-adrenoceptor antagonist, did not affect it.", "entity1": "beta 1-adrenoceptor", "entity2": "metoprolol tartrate", "span1": [237, 256], "span2": [187, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10195": {"label": 3, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP-C", "entity2": "rifampicin", "span1": [36, 42], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9613": {"label": 1, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "NBF2", "entity2": "MgADP", "span1": [111, 115], "span2": [76, 81]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11873": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "AhR", "entity2": "petunidin", "span1": [145, 148], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5875": {"label": 1, "data": {"text": "In vitro binding studies showed that both amoxapine and amitriptyline interact in the nanomolar range with 5-HT2 receptors labelled by [3H]ketanserin in cortical membranes.", "entity1": "5-HT2", "entity2": "amoxapine", "span1": [107, 112], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6741": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "piperazonyl quinazoline", "span1": [268, 272], "span2": [210, 233]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13607": {"label": 0, "data": {"text": "The key difference in structure of Lp(a) and plasminogen is replacement of Arg with Ser at position 560.", "entity1": "Lp(a)", "entity2": "Ser", "span1": [35, 40], "span2": [84, 87]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15524": {"label": 1, "data": {"text": "This effect appeared to be due to both competition between S-nitrosocysteine and Prx1 for the Trx system and direct modulation by S-nitrosocysteine of Trx reductase activity.", "entity1": "Trx reductase", "entity2": "S-nitrosocysteine", "span1": [151, 164], "span2": [130, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12952": {"label": 3, "data": {"text": "BG also showed a protective effect in the presence of a DNA polymerase beta inhibitor (cytosine arabinoside-3-phosphate, Ara-C), demonstrating that BG does not act through an anti-mutagenic mechanism of action involving DNA polymerase beta.", "entity1": "DNA polymerase beta", "entity2": "Ara-C", "span1": [56, 75], "span2": [121, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5595": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "quetiapine", "span1": [171, 177], "span2": [188, 198]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6103": {"label": 3, "data": {"text": "These events are stimulated by NE and by guanethidine, an hNET substrate, and they are blocked by cocaine and the antidepressant desipramine.", "entity1": "hNET", "entity2": "desipramine", "span1": [58, 62], "span2": [129, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4020": {"label": 3, "data": {"text": "Curcumin improves TNBS-induced colitis in rats by inhibiting IL-27 expression via the TLR4/NF-\u03baB signaling pathway.", "entity1": "TLR4", "entity2": "Curcumin", "span1": [86, 90], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"823": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "sulprostone", "span1": [258, 275], "span2": [280, 291]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14054": {"label": 3, "data": {"text": "Aspirin and metformin (an activator of AMPK) increased inhibition of mTOR and Akt, as well as autophagy in CRC cells.", "entity1": "Akt", "entity2": "metformin", "span1": [78, 81], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14478": {"label": 8, "data": {"text": "Of the rat CYP isoforms studied, CYP2D isoforms were the most efficient in catalyzing the O-demethylation of 5-methoxytryptamine to serotonin, but they were less effective than the human isoform CYP2D6.", "entity1": "CYP2D", "entity2": "serotonin", "span1": [33, 38], "span2": [132, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15270": {"label": 0, "data": {"text": "We also show that removal of either the N- or C-terminal propeptide is required for VEGF-D to drive formation of VEGFR-2/VEGFR-3 heterodimers which have recently been shown to positively regulate angiogenic sprouting.", "entity1": "VEGF-D", "entity2": "N", "span1": [84, 90], "span2": [40, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4751": {"label": 2, "data": {"text": "The treatment of mice with Fe-NTA alone enhances ornithine decarboxylase activity to 4.6 folds, protein carbonyl formation increased up to 2.9 folds and DNA synthesis expressed in terms of [(3)H] thymidine incorporation increased to 3.2 folds, and antioxidants and antioxidant enzymes decreased to 1.8-2.5 folds, compared with the corresponding saline-treated controls.", "entity1": "ornithine decarboxylase", "entity2": "Fe-NTA", "span1": [49, 72], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10425": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "RARbeta", "entity2": "Tazarotene", "span1": [132, 139], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10871": {"label": 1, "data": {"text": "Late-onset diarrhea appears to be associated with intestinal exposure to SN-38 (7-ethyl-10-hydroxycamptothecin), the major active metabolite of CPT-11, which may bind to Topo I and induce apoptosis of intestinal epithelia, leading to the disturbance in the absorptive and secretory functions of mucosa.", "entity1": "Topo I", "entity2": "7-ethyl-10-hydroxycamptothecin", "span1": [170, 176], "span2": [80, 110]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1998": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "rat GnRHR", "entity2": "Leu", "span1": [158, 167], "span2": [99, 102]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9749": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "(AR)s", "entity2": "yohimbine", "span1": [103, 108], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1540": {"label": 9, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "SMO", "entity2": "spermidine", "span1": [15, 18], "span2": [123, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2255": {"label": 1, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "glucuronosyltransferases", "entity2": "rifampicin", "span1": [137, 161], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15860": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "HSA", "entity2": "Arg", "span1": [67, 70], "span2": [132, 135]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3407": {"label": 3, "data": {"text": "Pseudoephedrine inhibits T-cell activation by targeting NF-kappaB, NFAT and AP-1 signaling pathways.", "entity1": "AP-1", "entity2": "Pseudoephedrine", "span1": [76, 80], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4802": {"label": 1, "data": {"text": "We identified 13 differentially expressed phosphoproteins that are judged to be relevant in the neuroprotective roles of PTN and MK against amphetamine-induced neurotoxicity.", "entity1": "PTN", "entity2": "amphetamine", "span1": [121, 124], "span2": [140, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9409": {"label": 1, "data": {"text": "We suggest that 5-HT dependent mechanisms through 5-HT2 receptor blockade and 5-HT1 receptor activation could be also involved.", "entity1": "5-HT2", "entity2": "5-HT", "span1": [50, 55], "span2": [16, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8018": {"label": 3, "data": {"text": "In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A(2) (hnps-PLA(2)) and human leukotriene A(4) hydrolase (LTA(4)H-h) was found.", "entity1": "hnps-PLA(2)", "entity2": "JMC08-4", "span1": [186, 197], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15226": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "iNOS", "entity2": "CLS", "span1": [329, 333], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8096": {"label": 2, "data": {"text": "Moreover, wogonin repressed anisomycin-induced phosphorylation of p38, cav-1 and vascular permeability.", "entity1": "p38", "entity2": "anisomycin", "span1": [66, 69], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7563": {"label": 5, "data": {"text": "AZD6140 is a reversible oral P2Y(12) receptor antagonist that has been studied in ACS patients in comparison with clopidogrel (DISPERSE-2 study).", "entity1": "P2Y(12)", "entity2": "AZD6140", "span1": [29, 36], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15229": {"label": 1, "data": {"text": "Interaction of silymarin flavonolignans with organic anion-transporting polypeptides.", "entity1": "organic anion-transporting polypeptides", "entity2": "flavonolignans", "span1": [45, 84], "span2": [25, 39]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15751": {"label": 2, "data": {"text": "CO donor dose-dependently inactivated CYP2E1 of ethanol-incubated microsome, which was mimicked by HO-1 substrate but abolished by CO scavenger.", "entity1": "CYP2E1", "entity2": "ethanol", "span1": [38, 44], "span2": [48, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9410": {"label": 1, "data": {"text": "We suggest that 5-HT dependent mechanisms through 5-HT2 receptor blockade and 5-HT1 receptor activation could be also involved.", "entity1": "5-HT1", "entity2": "5-HT", "span1": [78, 83], "span2": [16, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2311": {"label": 3, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "beta-catenin", "entity2": "U0126", "span1": [167, 179], "span2": [17, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5956": {"label": 3, "data": {"text": "Levels of homovanillic acid (HVA), dihydroxyphenylacetic acid (DOPAC) and dihydroxyphenylglycol (DHPG) in plasma and the striatium were measured after inhibition of monoamine oxidase type A (MAO-A) by clorgyline (4 mg/kg i.p.", "entity1": "MAO-A", "entity2": "clorgyline", "span1": [191, 196], "span2": [201, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9361": {"label": 3, "data": {"text": "The DMI induced reduction in beta-adrenoceptors did not differ in OB and sham-operated control rats.", "entity1": "beta-adrenoceptors", "entity2": "DMI", "span1": [29, 47], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"123": {"label": 3, "data": {"text": "Again, inhibition of the actin-activated myosin Mg2+-ATPase and myosin filament assembly by felodipine and the p-chloro analogue could be reversed by raising the calmodulin concentration.", "entity1": "Mg2+-ATPase", "entity2": "felodipine", "span1": [48, 59], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11492": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "COX", "entity2": "ketorolac tromethamine", "span1": [42, 45], "span2": [139, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10713": {"label": 2, "data": {"text": "The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan.", "entity1": "sigma1 receptor", "entity2": "dimemorfan", "span1": [79, 94], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2212": {"label": 2, "data": {"text": "Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures.", "entity1": "CREB", "entity2": "naloxone", "span1": [66, 70], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4179": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "aldo-keto reductase (AKR) 1C1", "entity2": "sulforaphane", "span1": [262, 291], "span2": [166, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10553": {"label": 3, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "nuclear factor of activated T cells", "entity2": "RA", "span1": [195, 230], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14815": {"label": 4, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1)", "entity2": "rimonabant", "span1": [28, 33], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13427": {"label": 1, "data": {"text": "We studied whether D-glucose-stimulation of L-arginine transport and nitric oxide synthesis involves TGF-beta1 in primary cultures of HUVEC.", "entity1": "TGF-beta1", "entity2": "D-glucose", "span1": [101, 110], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6714": {"label": 9, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "Flt3", "entity2": "STI571", "span1": [52, 56], "span2": [99, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7564": {"label": 5, "data": {"text": "AZD6140 is a reversible oral P2Y(12) receptor antagonist that has been studied in ACS patients in comparison with clopidogrel (DISPERSE-2 study).", "entity1": "P2Y(12)", "entity2": "clopidogrel", "span1": [29, 36], "span2": [114, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6323": {"label": 3, "data": {"text": "Caffeine inhibits the checkpoint kinase ATM.", "entity1": "kinase", "entity2": "Caffeine", "span1": [33, 39], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9739": {"label": 1, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "hD(2)", "entity2": "(35)S", "span1": [119, 124], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14939": {"label": 3, "data": {"text": "We have previously reported a nanomolar inhibitor of antiapoptotic Mcl-1 protein, 3-thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1).", "entity1": "Mcl-1", "entity2": "3-thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile", "span1": [67, 72], "span2": [82, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14506": {"label": 0, "data": {"text": "Keap1 is expressed in differentiating osteoclast-like cells and the S349T mutation selectively impairs the SQSTM1-Keap1 interaction in co-immunoprecipitations, which molecular modelling indicates results from effects on critical hydrogen bonds required to stabilise the KIR-Keap1 complex.", "entity1": "Keap1", "entity2": "hydrogen", "span1": [274, 279], "span2": [229, 237]}, "weak_labels": [-1, -1, 0, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"464": {"label": 4, "data": {"text": "Phenylephrine elicited a concentration-dependent positive inotropic effect via alpha 1-adrenoceptors in the presence of either (+/-)-bupranolol or S(-)-timolol.", "entity1": "alpha 1-adrenoceptors", "entity2": "Phenylephrine", "span1": [79, 100], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9917": {"label": 1, "data": {"text": "This was the first study to investigate platelet [3H]paroxetine binding in alcohol-dependent and age-matched control subjects in relation to the 5-HTTLPR genotype.", "entity1": "5-HTTLPR", "entity2": "[3H]paroxetine", "span1": [145, 153], "span2": [49, 63]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13906": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR2B", "entity2": "metformin", "span1": [190, 195], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15550": {"label": 1, "data": {"text": "Further analyses revealed that CdTe-QD exposure resulted in apoptosis, indicated by changes in levels of caspase-3 activity, poly ADP-ribose polymerase (PARP) cleavage and phosphatidylserine externalization.", "entity1": "poly ADP-ribose polymerase", "entity2": "CdTe", "span1": [125, 151], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5106": {"label": 2, "data": {"text": "5-Hydroxy-3,6,7,8,3'4'-hexamethoxyflavone inhibits nitric oxide production in lipopolysaccharide-stimulated BV2 microglia via NF-\u03baB suppression and Nrf-2-dependent heme oxygenase-1 induction.", "entity1": "heme oxygenase-1", "entity2": "5-Hydroxy-3,6,7,8,3'4'-hexamethoxyflavone", "span1": [164, 180], "span2": [0, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5049": {"label": 0, "data": {"text": "Intravenous treatment, during coronary artery occlusion, with the melanocortin analogs [Nle(4), D-Phe(7)]\u03b1-melanocyte-stimulating hormone (NDP-\u03b1-MSH) and adrenocorticotropic hormone 1-24 [ACTH-(1-24)], induced a left ventricle up-regulation of pJAK2, pERK1/2 and pTyr-STAT3 (JAK-dependent), and a reduction in pJNK and TNF-\u03b1 levels; these effects of NDP-\u03b1-MSH and ACTH-(1-24) were associated with over-expression of the pro-survival proteins HO-1 and Bcl-XL, and marked decrease of the myocardial infarct size.", "entity1": "\u03b1-MSH", "entity2": "Nle", "span1": [143, 148], "span2": [88, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5528": {"label": 4, "data": {"text": "To determine the position of the phenyl ring of the aralkyloxyalkyl side chain of salmeterol in the beta 2AR binding site, we designed and synthesized the agonist photoaffinity label [(125)I]iodoazidosalmeterol ([125I]IAS).", "entity1": "beta 2AR", "entity2": "[(125)I]iodoazidosalmeterol", "span1": [100, 108], "span2": [183, 210]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4766": {"label": 3, "data": {"text": "Furthermore, BRN-250 inhibited the VEGF-induced phosphorylation and intracellular tyrosine kinase activity of VEGF receptor 2 (VEGFR2) and the activation of its downstream AKT pathway.", "entity1": "VEGF receptor 2", "entity2": "BRN-250", "span1": [110, 125], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11286": {"label": 8, "data": {"text": "An alternative THF-dependent pathway involves the C1-THF synthase/SHMT activities with formate as 1-C source.", "entity1": "C1-THF synthase", "entity2": "formate", "span1": [50, 65], "span2": [87, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11153": {"label": 8, "data": {"text": "From these data, it is inferred that both the SERT and NET contribute to the active clearance of exogenously applied 5-HT in the dentate gyrus.", "entity1": "NET", "entity2": "5-HT", "span1": [55, 58], "span2": [117, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13583": {"label": 9, "data": {"text": "In an initial search for molecular features that differentially define antagonist binding determinants, we document that Val148 in hNET transmembrane domain 3 selectively disrupts NIS binding but not that of DVS.", "entity1": "hNET transmembrane domain 3", "entity2": "NIS", "span1": [131, 158], "span2": [180, 183]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10958": {"label": 3, "data": {"text": "Effects of granulocyte colony-stimulating factor (G-CSF) and neutrophil elastase inhibitor (ONO-5046) on acid-induced lung injury in rats.", "entity1": "G-CSF", "entity2": "ONO-5046", "span1": [50, 55], "span2": [92, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4175": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "cinnamic aldehyde", "span1": [151, 155], "span2": [204, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10946": {"label": 3, "data": {"text": "This process was reduced by a protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, and a typical monocarboxylate transporter (MCT) inhibitor, alpha-cyano-4-hydroxycinnamic acid, suggesting that nicotinate uptake by rat astrocytes is mediated by H(+)-coupled monocarboxylate transport system.", "entity1": "monocarboxylate transporter", "entity2": "alpha-cyano-4-hydroxycinnamic acid", "span1": [109, 136], "span2": [154, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12617": {"label": 3, "data": {"text": "Among the other bisphosphonates studied, alendronate was more potent and selective for PTPmeg1.", "entity1": "PTPmeg1", "entity2": "bisphosphonates", "span1": [87, 94], "span2": [16, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2423": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "mitochondrial arginase II", "entity2": "NO", "span1": [234, 259], "span2": [35, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6216": {"label": 3, "data": {"text": "At 4 hours, losartan blocked 43% of the Ang II-induced systolic blood pressure increase; valsartan, 51%; and irbesartan, 88% (P<0.01 between drugs).", "entity1": "Ang II", "entity2": "valsartan", "span1": [40, 46], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1264": {"label": 1, "data": {"text": "OBJECTIVE: We examined the effect of CysLT antagonists (pranlukast and MCI-826) on antigen inhalation-induced eosinophilia in peripheral blood and lung, and on IL-5 activity in serum during late increase of airway resistance (late asthmatic response, LAR) in sensitized guinea-pigs.", "entity1": "IL-5", "entity2": "MCI-826", "span1": [160, 164], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7446": {"label": 9, "data": {"text": "Reducing GSH levels in female mice CNS by pretreatment with diethyl maleate or L-propargyl glycine did not result in inhibition of complex I activity, unlike male mice.", "entity1": "complex I", "entity2": "L-propargyl glycine", "span1": [131, 140], "span2": [79, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10410": {"label": 1, "data": {"text": "Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors.", "entity1": "opioid receptors", "entity2": "GTPgammaS", "span1": [109, 125], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1184": {"label": 2, "data": {"text": "Effect of fenoterol-induced constitutive beta(2)-adrenoceptor activity on contractile receptor function in airway smooth muscle.", "entity1": "beta(2)-adrenoceptor", "entity2": "fenoterol", "span1": [41, 61], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13448": {"label": 2, "data": {"text": "Moreover stimulation of COX-2 promoter activity was increased by those PUFAs or rosiglitazone.", "entity1": "COX-2 promoter", "entity2": "PUFAs", "span1": [24, 38], "span2": [71, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14997": {"label": 1, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "peroxisome proliferator-activated receptor (PPAR)\u03b3", "entity2": "DHA", "span1": [157, 207], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"360": {"label": 1, "data": {"text": "A cocaine-sensitive, high-affinity Drosophila serotonin (5-hydroxytryptamine; 5HT) transporter cDNA, denoted dSERT1, was isolated and characterized in oocytes.", "entity1": "Drosophila serotonin (5-hydroxytryptamine; 5HT) transporter", "entity2": "cocaine", "span1": [35, 94], "span2": [2, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"3059": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "stromal cell-derived factor-1", "entity2": "bicyclam", "span1": [111, 140], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4784": {"label": 3, "data": {"text": "Taken together, these data demonstrate that baicalin inhibits the metabolism of DXM in a concentration-dependent manner in rats, possibly through inhibiting hepatic CYP2D and CYP3A activities.", "entity1": "CYP2D", "entity2": "baicalin", "span1": [165, 170], "span2": [44, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8428": {"label": 8, "data": {"text": "Conclusively, protein malnutrition alters CP, FU and MMC metabolism in rat stomach by enhancing CCBL pathway for CP activation, delaying FU elimination and activating two-electron reduction of MMC, potentiating their gastrotoxicity.", "entity1": "CCBL", "entity2": "MMC", "span1": [96, 100], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12655": {"label": 1, "data": {"text": "Salicylic acid promotes dissociation of (125)I-ET-1 ETA receptor complexes both in the absence and the presence of unlabeled ET-1.", "entity1": "ET-1", "entity2": "Salicylic acid", "span1": [125, 129], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8855": {"label": 2, "data": {"text": "Activation of STAT3, which is phosphorylated by the IL-6 signaling pathways and thus is necessary for Th17 differentiation, was strongly stimulated by I3S and TCDD.", "entity1": "IL-6", "entity2": "TCDD", "span1": [52, 56], "span2": [159, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1807": {"label": 8, "data": {"text": "Moreover, a normal level of expression of PSS1 and/or PSS2 is not required for generating the pool of PtdSer externalized during apoptosis.", "entity1": "PSS2", "entity2": "PtdSer", "span1": [54, 58], "span2": [102, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14580": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "P505-15", "span1": [147, 150], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12224": {"label": 1, "data": {"text": "Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.", "entity1": "Trace amine-associated receptor 1", "entity2": "methamphetamine", "span1": [0, 33], "span2": [94, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1877": {"label": 1, "data": {"text": "In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone.", "entity1": "glucocorticoid receptor", "entity2": "CDB-2914", "span1": [74, 97], "span2": [163, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4415": {"label": 2, "data": {"text": "Notably, 17-HDHA treatment reduced adipose tissue expression of inflammatory cytokines, increased adiponectin expression and improved glucose tolerance parallel to insulin sensitivity in obese mice.", "entity1": "adiponectin", "entity2": "17-HDHA", "span1": [98, 109], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5012": {"label": 8, "data": {"text": "Five classes of chalcogenopyrylium dyes (CGPs) were examined for their ability to modulate transport of [(3)H]estradiol glucuronide (E217\u03b2G) (a prototypical MRP substrate) into MRP-enriched inside-out membrane vesicles.", "entity1": "MRP", "entity2": "[(3)H]estradiol glucuronide", "span1": [157, 160], "span2": [104, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, 8, 8, -1, -1, -1, -1]},
	"10944": {"label": 1, "data": {"text": "These results provide biochemical evidence of a H(+)-coupled and saturable transport system, presumed to be a low-affinity monocarboxylate transporter MCT4 or other unknown H(+)-coupled monocarboxylate transport system, for nicotinate in rat cerebrocortical astrocytes.", "entity1": "MCT4", "entity2": "H(+)", "span1": [151, 155], "span2": [48, 52]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7910": {"label": 2, "data": {"text": "We found that helenalin markedly induced endoplasmic reticulum (ER) stress-related genes, such as regulated in development and DNA damage responses (REDD) 1, activating transcription factor-4 (ATF4) and/or the CCAAT enhancer-binding protein-homologous protein (CHOP).", "entity1": "ATF4", "entity2": "helenalin", "span1": [193, 197], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12176": {"label": 2, "data": {"text": "However, plasma high-density lipoprotein-cholesterol (HDL-C) and HDL-C/total-C ratio levels and plasma paraoxonase activity were only significantly higher in vitamin E group after 8 weeks.", "entity1": "paraoxonase", "entity2": "vitamin E", "span1": [103, 114], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11359": {"label": 1, "data": {"text": "METHOD: The authors conducted a PET study to evaluate D(2) occupancy (using [(11)C]raclopride) and 5-HT(2) occupancy (using [(18)F]setoperone) in brain regions of interest in 16 patients with schizophrenia or schizoaffective disorder randomly assigned to receive 40, 80, 120, or 160 mg/day of ziprasidone, which reflected the recommended dose range.", "entity1": "5-HT(2)", "entity2": "[(18)F]setoperone", "span1": [99, 106], "span2": [124, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"895": {"label": 1, "data": {"text": "Contrasting effects of N5-substituted tetrahydrobiopterin derivatives on phenylalanine hydroxylase, dihydropteridine reductase and nitric oxide synthase.", "entity1": "nitric oxide synthase", "entity2": "N5-substituted tetrahydrobiopterin", "span1": [131, 152], "span2": [23, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9096": {"label": 3, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "5-lipoxygenase", "entity2": "piriprost", "span1": [194, 208], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13951": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g.", "entity1": "beta(3)", "entity2": "formoterol", "span1": [76, 83], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5230": {"label": 1, "data": {"text": "OBJECTIVETo describe and make available an interactive, 24-variable homeostasis model assessment (iHOMA2) that extends the HOMA2 model, enabling the modeling of physiology and treatment effects, to present equations of the HOMA2 and iHOMA2 models, and to exemplify iHOMA2 in two widely differing scenarios: changes in insulin sensitivity with thiazolidinediones and changes in renal threshold with sodium glucose transporter (SGLT2) inhibition.RESEARCH DESIGN AND METHODSiHOMA2 enables a user of the available software to examine and modify the mathematical functions describing the organs and tissues involved in the glucose and hormonal compartments.", "entity1": "sodium glucose transporter", "entity2": "thiazolidinediones", "span1": [398, 424], "span2": [343, 361]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4546": {"label": 8, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "CYP2D6", "entity2": "5-MeO-DMT", "span1": [237, 243], "span2": [174, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4866": {"label": 3, "data": {"text": "Cells were also evaluated in the presence of wortmannin, an inhibitor of phosphatidylinositol 3-kinases and thus AKt (0-100 nM).", "entity1": "AKt", "entity2": "wortmannin", "span1": [113, 116], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2330": {"label": 2, "data": {"text": "Theophylline exposure resulted in a sustained increase in mRNA expression for CysS and PDE3A, but PDE4D gene expression was unchanged.", "entity1": "CysS", "entity2": "Theophylline", "span1": [78, 82], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4906": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "MMP", "entity2": "kinsenoside", "span1": [430, 433], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13594": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "RTI-55", "span1": [6, 10], "span2": [360, 366]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2752": {"label": 9, "data": {"text": "Mutation of Ser-530 to Ala or Val-349 to Ala or Leu abolished the potent inhibition observed with wild-type human COX-2 and key lumiracoxib analogs.", "entity1": "Val-349 to Ala or Leu", "entity2": "lumiracoxib", "span1": [30, 51], "span2": [128, 139]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2891": {"label": 4, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1A)-adrenoceptor", "entity2": "phenylephrine", "span1": [79, 101], "span2": [300, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7305": {"label": 1, "data": {"text": "Pre-steady-state currents in neutral amino acid transporters induced by photolysis of a new caged alanine derivative.", "entity1": "neutral amino acid transporters", "entity2": "alanine", "span1": [29, 60], "span2": [98, 105]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"961": {"label": 5, "data": {"text": "In the rabbit pulmonary artery, rilmenidine and oxymetazoline are potent full agonists, whereas in the human atrial appendages they are antagonists at the alpha(2)-autoreceptors, sharing this property with rauwolscine, phentolamine, and idazoxan.", "entity1": "alpha(2)-autoreceptors", "entity2": "idazoxan", "span1": [155, 177], "span2": [237, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3714": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "Bim", "entity2": "N", "span1": [183, 186], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"721": {"label": 1, "data": {"text": "Infrared spectroscopic studies revealed a reduced thermal stability both of the apo-and the holo-hTH1 on binding of H4biopterin and Lerythro-dihydrobiopterin (H2biopterin).", "entity1": "hTH1", "entity2": "H2biopterin", "span1": [97, 101], "span2": [159, 170]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14628": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "DCK", "entity2": "Gemcitabine", "span1": [117, 120], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1617": {"label": 2, "data": {"text": "Weekly subcutaneous decitabine produces cumulative increases in HbF and total hemoglobin through a noncytotoxic mechanism of action.", "entity1": "HbF", "entity2": "decitabine", "span1": [64, 67], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3273": {"label": 2, "data": {"text": "Assays examining the ability of TFP to block S100A4-mediated disassembly of myosin-IIA filaments demonstrate that significant inhibition of S100A4 function occurs only at TFP concentrations that promote S100A4 oligomerization.", "entity1": "S100A4", "entity2": "TFP", "span1": [203, 209], "span2": [171, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14605": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ile24Val", "entity2": "Ara-C", "span1": [71, 79], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3030": {"label": 1, "data": {"text": "Optimization of taxane binding to microtubules: binding affinity dissection and incremental construction of a high-affinity analog of paclitaxel.", "entity1": "microtubules", "entity2": "taxane", "span1": [34, 46], "span2": [16, 22]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16061": {"label": 8, "data": {"text": "Drug-drug interactions are dependent on statins' pharmacokinetic profile: simvastatin, lovastatin and atorvastatin are metabolized through cytochrome P450 (CYP) 3A, while the metabolism of the other statins is independent of this CYP.", "entity1": "cytochrome P450 (CYP) 3A", "entity2": "atorvastatin", "span1": [139, 163], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4272": {"label": 2, "data": {"text": "Overall, our findings suggest that ursolic acid induced apoptosis in HepG2 cells via AMPK activation and GSK3\u03b2 phosphorylation as a potent chemopreventive agent.", "entity1": "AMPK", "entity2": "ursolic acid", "span1": [85, 89], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14597": {"label": 3, "data": {"text": "17-Allylamino-17-demethoxygeldanamycin (17-AAG), an Hsp90 inhibitor, is currently under evaluation for its anticancer activity in clinical trials.", "entity1": "Hsp90", "entity2": "17-AAG", "span1": [52, 57], "span2": [40, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5203": {"label": 3, "data": {"text": "Inhibition of mTOR by small dose of rapamycin reduces podocyte apoptosis, attenuates glomerular injury and albuminuria.", "entity1": "mTOR", "entity2": "rapamycin", "span1": [14, 18], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14575": {"label": 3, "data": {"text": "P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL.", "entity1": "B-cell receptor", "entity2": "P505-15", "span1": [44, 59], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4901": {"label": 3, "data": {"text": "A series of pyrido-quinazolines have been synthesised, characterised and tested for their in vitro EGFR tyrosine kinase inhibitory activity.", "entity1": "EGFR", "entity2": "pyrido-quinazolines", "span1": [99, 103], "span2": [12, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9225": {"label": 3, "data": {"text": "The binding of FHA-HIS was inhibited on 35-79% of the platelets by the histamine H1 receptor antagonists diphenhydramine and clemastine.", "entity1": "FHA", "entity2": "diphenhydramine", "span1": [15, 18], "span2": [105, 120]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4343": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "glycogen synthase kinase 3\u03b2", "entity2": "Pinosylvin", "span1": [209, 236], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10236": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "PAO", "entity2": "spermidine", "span1": [175, 178], "span2": [191, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14474": {"label": 2, "data": {"text": "Following CdCl\u2082 treatment, ICAM2 was found to be upregulated during restructuring of the seminiferous epithelium, with round spermatids becoming increasingly immunoreactive for ICAM2 by 6-16 h. Interestingly, there was a loss in the binding of ICAM2 to actin during CdCl\u2082-induced germ cell loss, suggesting that a loss of ICAM2-actin interactions might have facilitated junction restructuring.", "entity1": "ICAM2", "entity2": "CdCl\u2082", "span1": [27, 32], "span2": [10, 15]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2202": {"label": 3, "data": {"text": "In vitro, minocycline, but not doxycycline, inhibits MMP-9, at least in part, via the extracellular signaling-related kinase 1/2 (ERK1/2)-mediated pathway.", "entity1": "MMP-9", "entity2": "minocycline", "span1": [53, 58], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4137": {"label": 2, "data": {"text": "Upon activation by phenobarbital, nuclear receptor CAR binds the 97-bp response element (-2441/-2345) within the Kcnk1 promoter.", "entity1": "CAR", "entity2": "phenobarbital", "span1": [51, 54], "span2": [19, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13222": {"label": 9, "data": {"text": "Here we report that glutamate stimulation caused a rapid reduction in protein levels of GRIP1, but not that of glutamate receptor (GluR) 1, GluR2 and protein interacting with C kinase 1 (PICK1) in rat primary cortical neuron cultures.", "entity1": "GluR2", "entity2": "glutamate", "span1": [140, 145], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13705": {"label": 1, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Halogenated propofol analogues constitute a novel class of sodium channel-blocking drugs possessing almost 100-fold higher potency compared with the local anaesthetic and anti-arrhythmic drug lidocaine.", "entity1": "sodium channel", "entity2": "lidocaine", "span1": [89, 103], "span2": [222, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1456": {"label": 3, "data": {"text": "Reserpine-induced ptosis was reversed by rasagiline at doses above 2 mg x kg(-1) i.p., which inhibit MAO-A as well as MAO-B, but not at MAO-B-selective doses.", "entity1": "MAO-A", "entity2": "rasagiline", "span1": [101, 106], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"296": {"label": 3, "data": {"text": "In catalytic properties, mouse CA V is closest to CA I; however, in inhibition by acetazolamide, ethoxzolamide, and cyanate, CA V is very similar to CA II.", "entity1": "CA II", "entity2": "ethoxzolamide", "span1": [149, 154], "span2": [97, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14097": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "DDB1", "entity2": "thalidomide", "span1": [177, 181], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9046": {"label": 1, "data": {"text": "Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam.", "entity1": "Benzodiazepine receptor", "entity2": "alprazolam", "span1": [0, 23], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6770": {"label": 3, "data": {"text": "Hydralazine dose-dependently inhibited PHD activity and induced nonhydroxylated HIF-1alpha, evidence for HIF stabilization specifically by inhibition of PHD enzyme activity.", "entity1": "PHD", "entity2": "Hydralazine", "span1": [39, 42], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11134": {"label": 3, "data": {"text": "TREK-1 currents are insensitive to pharmacological agents that block TWIK-1 activity such as quinine and quinidine.", "entity1": "TWIK-1", "entity2": "quinine", "span1": [69, 75], "span2": [93, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3415": {"label": 3, "data": {"text": "Because clinical studies investigating interactions between garlic and human immunodeficiency virus protease inhibitors saquinavir and ritonavir have already been performed, we used these in vivo data to evaluate the in vitro results and the reliability of the models employed as screening tools for forecasting the potential of first-pass intestinal metabolism changes.", "entity1": "human immunodeficiency virus protease", "entity2": "saquinavir", "span1": [71, 108], "span2": [120, 130]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3956": {"label": 1, "data": {"text": "VK2 directly interacts with Bak and induces mitochondrial-mediated apoptosis.", "entity1": "Bak", "entity2": "VK2", "span1": [28, 31], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5445": {"label": 3, "data": {"text": "Juglone, isolated from Juglans mandshurica Maxim, induces apoptosis via down-regulation of AR expression in human prostate cancer LNCaP cells.", "entity1": "AR", "entity2": "Juglone", "span1": [91, 93], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2841": {"label": 7, "data": {"text": "The enzyme requires PLP and divalent cations such as Ca(2+), Mg(2+), or Mn(2+), but not ATP, whereas mammalian serine racemase activity is increased by ATP.", "entity1": "serine racemase", "entity2": "Ca(2+)", "span1": [111, 126], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13938": {"label": 3, "data": {"text": "Telmisartan is an angiotensin II receptor blocker (ARB) displaying unique pharmacologic properties, including a longer half life than any other ARB, that result in large and sustained reductions of blood pressure.", "entity1": "angiotensin II receptor", "entity2": "Telmisartan", "span1": [18, 41], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11194": {"label": 8, "data": {"text": "The enzyme dimethylarginine dimethylaminohydrolase (DDAH) specifically hydrolyzes these asymmetrically methylated arginine residues to citrulline and methylamines.", "entity1": "DDAH", "entity2": "arginine", "span1": [52, 56], "span2": [114, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15932": {"label": 1, "data": {"text": "Posttranslational modification of the neural cell adhesion molecule (NCAM) by polysialic acid (polySia) is well studied in the nervous system and described as a dynamic modulator of plastic processes like precursor cell migration, axon fasciculation, and synaptic plasticity.", "entity1": "NCAM", "entity2": "polysialic acid", "span1": [69, 73], "span2": [78, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3102": {"label": 1, "data": {"text": "SoRI-20041, which does not alter DAT-mediated DA release measured with [(3)H]DA, reversed the effect of SoRI-20040.", "entity1": "DAT", "entity2": "SoRI-20041", "span1": [33, 36], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2786": {"label": 2, "data": {"text": "Isolated islets displayed improved glucose-stimulated insulin secretion after GRA treatment (0.061 +/- 0.007 vs 0.030 +/- 0.004 pmol islet(-1) h(-1) at 16.7 mmol/l glucose; p < 0.001), without affecting islet glucose oxidation.", "entity1": "insulin", "entity2": "glucose", "span1": [54, 61], "span2": [35, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11102": {"label": 8, "data": {"text": "hCOX-1 had a specific activity of 18.8 mumol of O2/mg with a Km of 13.8 microM for arachidonate and Vmax.", "entity1": "hCOX-1", "entity2": "arachidonate", "span1": [0, 6], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14955": {"label": 2, "data": {"text": "Bile acids are signaling molecules that activate nuclear receptors, such as farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, and vitamin D receptor, and play a critical role in the regulation of lipid, glucose, energy, and drug metabolism.", "entity1": "constitutive androstane receptor", "entity2": "Bile acids", "span1": [119, 151], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1287": {"label": 0, "data": {"text": "A hybrid cDNA was created by fusing a human cDNA for amino acids 1-101 of GAD67 to a human cDNA for amino acids 96-585 of GAD65; the recombinant (r) protein was expressed in yeast and was shown to have equivalent immunoreactivity to mammalian brain GAD with diabetes sera.", "entity1": "GAD65", "entity2": "amino acids", "span1": [122, 127], "span2": [100, 111]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1284": {"label": 3, "data": {"text": "N-[2-(cyclohexyloxyl)-4-nitrophenyl]-methanesulfonamide (NS-398), a selective cyclooxygenase-2 inhibitor, also inhibited cell proliferation, whereas it did not cause apoptosis.", "entity1": "cyclooxygenase-2", "entity2": "N-[2-(cyclohexyloxyl)-4-nitrophenyl]-methanesulfonamide", "span1": [78, 94], "span2": [0, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"456": {"label": 5, "data": {"text": "Pretreatment with tropisetron (1 microM), a 5-HT3 antagonist, ketanserin (10 microM), a 5-HT2 antagonist, thioperamide (10 microM), a histamine H3 antagonist, or phentolamine (10 microM), an alpha-adrenergic antagonist, however, had no effect.", "entity1": "5-HT2", "entity2": "ketanserin", "span1": [88, 93], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8972": {"label": 5, "data": {"text": "Radioligand binding studies with the nonselective alpha 1-adrenoceptor antagonist radioligand 125I-BE2254 showed that 73-87% of the binding sites in rabbit aorta are CEC sensitive and they are predominantly low affinity sites both for WB4101 (pKd = 8.1) and for 5-methylurapidil (pKd = 7.1).", "entity1": "alpha 1-adrenoceptor", "entity2": "125I-BE2254", "span1": [50, 70], "span2": [94, 105]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4647": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [256, 262], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13603": {"label": 5, "data": {"text": "Desvenlafaxine succinate (DVS) is a recently introduced antagonist of the human norepinephrine and serotonin transporters (hNET and hSERT, respectively), currently in clinical development for use in the treatment of major depressive disorder and vasomotor symptoms associated with menopause.", "entity1": "hSERT", "entity2": "DVS", "span1": [132, 137], "span2": [26, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7071": {"label": 1, "data": {"text": "The cholesterol-lowering drug simvastatin inhibits LFA-1 signaling by binding to an allosteric site on CD11a (LFA-1 alpha chain), which leads to immunomodulation.", "entity1": "LFA-1 alpha chain", "entity2": "simvastatin", "span1": [110, 127], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"13894": {"label": 1, "data": {"text": "RESULTS: Captopril directly inhibited MMP-2 activity in peritoneal effluents from patients on CAPD (IC50; 48 micromol/l), and that captopril binding to the MMP-2 active site could be formed in each complex model without molecular distortion.", "entity1": "MMP-2", "entity2": "captopril", "span1": [156, 161], "span2": [131, 140]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12186": {"label": 1, "data": {"text": "Thymidylate synthase expression pattern, expression level and single nucleotide polymorphism are predictors for disease-free survival in patients of colorectal cancer treated with 5-fluorouracil.", "entity1": "Thymidylate synthase", "entity2": "5-fluorouracil", "span1": [0, 20], "span2": [180, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7599": {"label": 4, "data": {"text": "In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use.", "entity1": "V(2)", "entity2": "desmopressin", "span1": [145, 149], "span2": [131, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9862": {"label": 3, "data": {"text": "This activity, like NQO1, was inhibited by dicoumarol and immunologically related to NQO1.", "entity1": "NQO1", "entity2": "dicoumarol", "span1": [20, 24], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10830": {"label": 9, "data": {"text": "The reported mechanism of imatinib resistance in GISTs involves missense mutation in the kinase domain of KIT, including Thr670Ile, Tyr823Asp, and Val654Ala.", "entity1": "Tyr823Asp", "entity2": "imatinib", "span1": [132, 141], "span2": [26, 34]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"408": {"label": 3, "data": {"text": "Previous studies by this research team proved that vasodilating prostaglandins (PGs) E1, E2 and I2 inhibit carbonic anhydrase (CA) in vitro and in vivo, which suggested involvement of CA in gastric acid secretion inhibition and the increase of gastric mucosa blood flow produced by this group of PGs.", "entity1": "CA", "entity2": "PGs", "span1": [127, 129], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3981": {"label": 1, "data": {"text": "Since DNA methylation is regulated by DNA methyltransferases and methyl cytosine-binding proteins, this study assessed the extent to which developmental Pb exposure might affect expression of these proteins in the hippocampus.", "entity1": "DNA methyltransferases", "entity2": "Pb", "span1": [38, 60], "span2": [153, 155]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12220": {"label": 1, "data": {"text": "In response to METH, AMPH, or POHA exposure, the accumulation of cAMP by HEK-293 cells stably expressing different species of TAAR1 was concentration- and isomer-dependent.", "entity1": "TAAR1", "entity2": "AMPH", "span1": [126, 131], "span2": [21, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7146": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "GAF-B domain", "entity2": "tadalafil", "span1": [47, 59], "span2": [117, 126]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14545": {"label": 9, "data": {"text": "Neurodegeneration was related with decreased [(3)H]glutamate uptake and decreased Akt immunoreactivity, however phospho-GSK-3-\u03b2 (Ser9) was not altered in (PhTe)(2) injected rat.", "entity1": "phospho-GSK-3-\u03b2", "entity2": "(PhTe)(2)", "span1": [112, 127], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14017": {"label": 1, "data": {"text": "KEY RESULTS: Thiocolchicoside suppressed osteoclastogenesis induced by RANKL, and by breast cancer and multiple myeloma cells.", "entity1": "RANKL", "entity2": "Thiocolchicoside", "span1": [71, 76], "span2": [13, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6412": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes.", "entity1": "Peroxisome proliferator-activated receptor alpha", "entity2": "bezafibrate", "span1": [0, 48], "span2": [73, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5636": {"label": 9, "data": {"text": "The mechanisms underlying the pro-apoptotic action of compound C involved induction of oxidative stress and downregulation of antiapoptotic molecule Bcl-2, while no alteration of pro-apoptotic Bax was observed.", "entity1": "Bax", "entity2": "compound C", "span1": [193, 196], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2971": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "H613A", "entity2": "sildenafil", "span1": [71, 76], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"811": {"label": 1, "data": {"text": "PGE1 and PGE2 also inhibited the remaining ICa in a saturating concentration of nifedipine, omega-conotoxin-GVIA and omega-conotoxin-MVIIC, suggesting that R-type Ca2+ channels are involved.", "entity1": "R-type Ca2+ channels", "entity2": "PGE2", "span1": [156, 176], "span2": [9, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2502": {"label": 3, "data": {"text": "Chronic insulin (24 h) activates NHE3 through the classic phosphatidylinositol 3-kinase-serum- and glucocorticoid-dependent kinase 1 (PI3K-SGK1) pathway as insulin stimulates SGK1 phosphorylation and the insulin effect can be blocked by the PI3K inhibitor wortmannin or a dominant-negative SGK1.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "wortmannin", "span1": [58, 87], "span2": [256, 266]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3593": {"label": 3, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "p70S6K)", "entity2": "Wogonoside", "span1": [101, 108], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8361": {"label": 0, "data": {"text": "The crystal structure of HSA complexed with fatty acid and acetyldiflunisal revealed that acetyldiflunisal binds to the IIA subdomain and that upon binding, it acetylates lysine 199.", "entity1": "IIA subdomain", "entity2": "lysine", "span1": [120, 133], "span2": [171, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10720": {"label": 5, "data": {"text": "The anticonvulsant action of dextromethorphan or dimemorfan was significantly counteracted by a selective sigma1 receptor antagonist BD 1047, suggesting that the anticonvulsant action of dextromethorphan or dimemorfan is, at least in part, related to sigma1 receptor-activated modulation of AP-1 transcription factors.", "entity1": "sigma1 receptor", "entity2": "BD 1047", "span1": [106, 121], "span2": [133, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7011": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "PDGFR-beta", "entity2": "AG013736", "span1": [238, 248], "span2": [188, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6102": {"label": 3, "data": {"text": "These events are stimulated by NE and by guanethidine, an hNET substrate, and they are blocked by cocaine and the antidepressant desipramine.", "entity1": "hNET", "entity2": "cocaine", "span1": [58, 62], "span2": [98, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13562": {"label": 8, "data": {"text": "We present a new study that optimizes the Prescott-Jones colorimetric assay to measure DDAH-dependent L-citrulline generation in kidney homogenates.", "entity1": "DDAH", "entity2": "L-citrulline", "span1": [87, 91], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14604": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "DCK", "entity2": "Ara-C", "span1": [66, 69], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7893": {"label": 2, "data": {"text": "Ibandronate increases the expression of the pro-apoptotic gene FAS by epigenetic mechanisms in tumor cells.", "entity1": "FAS", "entity2": "Ibandronate", "span1": [63, 66], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1538": {"label": 5, "data": {"text": "The selective GluR5 kainate receptor agonist ATPA induces spontaneous epileptiform bursting that is sensitive to the GluR5 kainate receptor antagonist LY293558.", "entity1": "kainate receptor", "entity2": "LY293558", "span1": [123, 139], "span2": [151, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3882": {"label": 3, "data": {"text": "However, combined treatment with cinobufagin and SB216367 resulted in a significant reduction in p65 and an increase in cleaved-PARP in U2OS cells.", "entity1": "p65", "entity2": "cinobufagin", "span1": [97, 100], "span2": [33, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9447": {"label": 9, "data": {"text": "16,16-dimethyl-PGE2 and two putative EP1 antagonists, AH6809 and SC-19220, did not show any significant binding to this receptor.", "entity1": "EP1", "entity2": "AH6809", "span1": [37, 40], "span2": [54, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"44": {"label": 3, "data": {"text": "In contrast to adrenaline and somatostatin, galanin, another inhibitor of insulin secretion, reduced Ca2+ currents by about 40% in a pertussis toxin-insensitive manner.", "entity1": "insulin", "entity2": "somatostatin", "span1": [74, 81], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"270": {"label": 1, "data": {"text": "The non-competitive blocker site of the GABA-gated chloride ion channel in normal susceptible strains of Drosophila melanogaster and simulans binds 4-n-[3H]propyl-4'-ethynylbicycloorthobenzoate ([3H]EBOB) at specific sites with KdS of 1.6-1.9 nM and BmaxS of 171-181 fmol/mg protein.", "entity1": "GABA-gated chloride ion channel", "entity2": "4-n-[3H]propyl-4'-ethynylbicycloorthobenzoate", "span1": [40, 71], "span2": [148, 193]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6246": {"label": 1, "data": {"text": "The affinity of eletriptan ((R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1H-indole) for a range of 5-HT receptors was compared to values obtained for other 5-HT1B/1D receptor agonists known to be effective in the treatment of migraine.", "entity1": "5-HT receptors", "entity2": "(R)-3-(1-methyl-2-pyrrolidinylmethyl)-5-[2-(phenylsulphonyl )ethyl]-1H-indole", "span1": [122, 136], "span2": [28, 105]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13738": {"label": 8, "data": {"text": "Nicotinamide N-methyltransferase (NNMT) catalyses the conversion of nicotinamide to 1-methylnicotinamide and plays an important role in hepatic detoxification reactions.", "entity1": "Nicotinamide N-methyltransferase", "entity2": "nicotinamide", "span1": [0, 32], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"8943": {"label": 1, "data": {"text": "Two new negatively charged estramustine derivatives, estramustine sulphate and estramustine glucuronide, were found to be similar MAP-dependent microtubule inhibitors.", "entity1": "MAP", "entity2": "estramustine glucuronide", "span1": [130, 133], "span2": [79, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1174": {"label": 3, "data": {"text": "Mitiglinide (KAD-1229), a new anti-diabetic drug, is thought to stimulate insulin secretion by closing the ATP-sensitive K+ (K(ATP)) channels in pancreatic beta-cells.", "entity1": "ATP-sensitive K+ (K(ATP)) channels", "entity2": "Mitiglinide", "span1": [107, 141], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14255": {"label": 5, "data": {"text": "Other groups received either an infusion of the selective NMDA receptor antagonist (AP7; 10 nmol; intra-mPFC) or vehicle, 10 min prior to PILO preceding LFS600, or prior to a supra-threshold LTD protocol (900 pulses, 1 Hz; LFS900).", "entity1": "NMDA receptor", "entity2": "AP7", "span1": [58, 71], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8056": {"label": 2, "data": {"text": "Furthermore, metformin was able to not only decrease the paclitaxel-induced p38 MAPK-mediated ERCC1 expression, but also augment the cytotoxic effect induced by paclitaxel.", "entity1": "ERCC1", "entity2": "paclitaxel", "span1": [94, 99], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11864": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "AhR", "entity2": "delphinidin", "span1": [145, 148], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7571": {"label": 2, "data": {"text": "Administration of cevimeline hydrochloride, an M3 muscarinic receptor agonist (10 mg/kg for 7 days po), but not pilocarpine (0.3 mg/kg for 7 days po), recovered the AQP5 protein level reduced by CTD and increased the AQP1 protein level above the control one.", "entity1": "AQP5", "entity2": "cevimeline hydrochloride", "span1": [165, 169], "span2": [18, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9323": {"label": 3, "data": {"text": "RESULTS: Nedocromil sodium inhibited the chemotactic response toward FMLP and NAF/IL-8 of GM-CSF primed eosinophils approximately 60% (inhibitory concentration of 50% [IC50] approximately 1 to 10 nmol/L), whereas these responses of IL-3 primed eosinophils was completely inhibited (IC50 approximately 1 nmol/L).", "entity1": "IL-3", "entity2": "Nedocromil sodium", "span1": [232, 236], "span2": [9, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8617": {"label": 3, "data": {"text": "Oxysterol-dependent NOX1 activation, as well as interleukin synthesis, were completely prevented by Cannonau red wine extract that contains an abundant phenolic fraction, in particular phenolic acids and flavonoids.", "entity1": "interleukin", "entity2": "flavonoids", "span1": [48, 59], "span2": [204, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11007": {"label": 0, "data": {"text": "Leptin is a 167 amino acid protein encoded by the obesity gene that is synthesized in adipose tissue and interacts with receptors in the hypothalamus linked to the regulation of appetite and metabolism.", "entity1": "Leptin", "entity2": "amino acid", "span1": [0, 6], "span2": [16, 26]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10136": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "meclofenamic acid", "span1": [34, 37], "span2": [181, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2827": {"label": 3, "data": {"text": "Pharmacological treatment has been studied and it could be demonstrated, that some mutant currents may be insufficiently suppressed by drugs targeted to block the specific current such as, e.g., sotalol or ibutilide in patients with a mutation in the IKr-coding gene KCNH2 (HERG).", "entity1": "KCNH2", "entity2": "sotalol", "span1": [267, 272], "span2": [195, 202]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7508": {"label": 2, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "AMPK", "entity2": "ouabain", "span1": [256, 260], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"153": {"label": 5, "data": {"text": "A naloxone-steroid hybrid azine with selective and long-acting opioid antagonism at delta receptors in vitro.", "entity1": "delta receptors", "entity2": "naloxone-steroid hybrid azine", "span1": [84, 99], "span2": [2, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11255": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "DAT", "entity2": "mazindol", "span1": [151, 154], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7265": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "ethoxzolamide", "span1": [218, 224], "span2": [70, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8389": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "SOD", "entity2": "Cd", "span1": [138, 141], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7792": {"label": 3, "data": {"text": "We examined in cats the 1) ulcerogenic effects of selective COX-1 (SC-560, ketorolac) and COX-2 (celecoxib, meloxicam) inhibitors on the gastrointestinal mucosa, 2) effect of feeding and cimetidine on the expression of COX isoforms and prostaglandin E(2) (PGE(2)) level in the duodenum, and 3) localization of COX isoforms in the duodenum.", "entity1": "COX-1", "entity2": "ketorolac", "span1": [60, 65], "span2": [75, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5601": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "amisulpride", "span1": [111, 117], "span2": [200, 211]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9240": {"label": 3, "data": {"text": "Hence, triclosan has the ability to inhibit both the cyclo-oxygenase and lipoxygenase pathways of arachidonic acid metabolism with similar efficacy.", "entity1": "cyclo-oxygenase", "entity2": "triclosan", "span1": [53, 68], "span2": [7, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9159": {"label": 8, "data": {"text": "Gossypol and its isomers were non-competitive inhibitors of human and hamster LDH-X with respect to the coenzyme NADH, competitive inhibitors of human LDH-X and noncompetitive-competitive inhibitors of hamster LDH-X with respect to the substrate alpha-ketobutyrate.", "entity1": "hamster LDH-X", "entity2": "alpha-ketobutyrate", "span1": [202, 215], "span2": [246, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12233": {"label": 1, "data": {"text": "We used immunofluorescence microscopy and digitonin permeabilization assays to determine the subcellular location of endogenous BAAT in primary human and rat hepatocytes.", "entity1": "BAAT", "entity2": "digitonin", "span1": [128, 132], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15334": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "chrysin", "span1": [287, 296], "span2": [209, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15652": {"label": 2, "data": {"text": "Excess of cholesterol converted into 24OHC may up-regulate ApoE synthesis which is a scavenger for A\u03b2 and Tau.", "entity1": "ApoE", "entity2": "cholesterol", "span1": [59, 63], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5674": {"label": 9, "data": {"text": "In contrast, ibandronate did not affect FAS and DNMT1 expression in MC3T3-E1 non-neoplastic cells.", "entity1": "DNMT1", "entity2": "ibandronate", "span1": [48, 53], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6589": {"label": 1, "data": {"text": "These results indicate that quetiapine, iloperidone and melperone preferentially increase DA release in the mPFC, compared to the NAC via a 5-HT(1A)-related mechanism.", "entity1": "5-HT(1A)", "entity2": "quetiapine", "span1": [140, 148], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6217": {"label": 3, "data": {"text": "At 4 hours, losartan blocked 43% of the Ang II-induced systolic blood pressure increase; valsartan, 51%; and irbesartan, 88% (P<0.01 between drugs).", "entity1": "Ang II", "entity2": "irbesartan", "span1": [40, 46], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9582": {"label": 1, "data": {"text": "Both carbetocin, carbetocin metabolite I and carbetocin metabolite II displayed binding affinities to the myometrial oxytocin receptor of a similar magnitude as oxytocin.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [117, 134], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1504": {"label": 3, "data": {"text": "db/db mice treated with DRF 2655 showed 5- and 3.6-fold inhibition in phosphoenolpyruvate carboxykinase and glucose 6-phosphatase activity and 651% and 77% increases in the beta-oxidation enzymes carnitine palmitoyltransferase and carnitine acetyltransferase, respectively.", "entity1": "glucose 6-phosphatase", "entity2": "DRF 2655", "span1": [108, 129], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"532": {"label": 0, "data": {"text": "Mutation of a single amino acid residue in the potential BiP binding site increased the secretion efficiency of factor VIII by threefold.", "entity1": "BiP binding site", "entity2": "amino acid", "span1": [57, 73], "span2": [21, 31]}, "weak_labels": [0, -1, 0, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10619": {"label": 1, "data": {"text": "Furthermore, GABA receptors of horizontal cells were modulated by extracellular application of diazepam, zolpidem, methyl 6,7-dimethoxy-4-ethyl-beta-carboxylate, pentobarbital, and alphaxalone, thus showing typical pharmacological properties of CNS GABAA receptors.", "entity1": "GABA receptors", "entity2": "alphaxalone", "span1": [13, 27], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5620": {"label": 3, "data": {"text": "Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M.", "entity1": "HERG", "entity2": "cisapride", "span1": [36, 40], "span2": [13, 22]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9071": {"label": 1, "data": {"text": "Chlorpromazine, levomepromazine, and their metabolites had 5-30 times higher binding affinities for muscarinic cholinergic receptors than fluphenazine, perphenazine and their metabolites.", "entity1": "muscarinic cholinergic receptors", "entity2": "Chlorpromazine", "span1": [100, 132], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11959": {"label": 8, "data": {"text": "We have used this method to screen 11 recombinant human UGTs for HFC glucuronidation activity and studied the reaction kinetics with the most active enzymes.", "entity1": "human UGTs", "entity2": "HFC", "span1": [50, 60], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7828": {"label": 4, "data": {"text": "Cellular release of AChE by SH-SY5Y is significantly enhanced by the muscarinic acetylcholine receptor (mAChR) agonists carbachol or muscarine, with the effect of carbachol blocked by the mAChR antagonist atropine.", "entity1": "mAChR", "entity2": "carbachol", "span1": [104, 109], "span2": [120, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13264": {"label": 5, "data": {"text": "METHODS: The effect of leukotriene D(4) and the leukotriene receptor antagonist, pranlukast hydrate (ONO-1078) on the regulation of MUC2/5AC gene expression and mucin secretion were observed in human airway NCI-H292 epithelial cells.", "entity1": "leukotriene receptor", "entity2": "ONO-1078", "span1": [48, 68], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1931": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "CrAT", "entity2": "acyl-CoAs", "span1": [155, 159], "span2": [66, 75]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5633": {"label": 3, "data": {"text": "AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C.\tWe investigated the effect of compound C, a well-known inhibitor of the intracellular energy sensor AMP-activated protein kinase (AMPK), on proliferation and viability of human U251 and rat C6 glioma cell lines.", "entity1": "AMPK", "entity2": "compound C", "span1": [250, 254], "span2": [150, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"705": {"label": 3, "data": {"text": "In phosphotriesterase and physostigmine-treated mice, a 4- and 2-fold higher sarin dose, respectively, was needed to cause a 50% inhibition of brain AChE activity.", "entity1": "AChE", "entity2": "sarin", "span1": [149, 153], "span2": [77, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2145": {"label": 3, "data": {"text": "The difference in structure of troglitazone did not account for its inhibitory effect on ENT1 because Vitamin E did not inhibit [3H]adenosine uptake by HASMCs.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [89, 93], "span2": [31, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15390": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor", "entity2": "TASP0382088", "span1": [129, 181], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1179": {"label": 3, "data": {"text": "Nateglinide inhibits Kir6.2/SUR1 and Kir6.2/SUR2B channels at 100 nM, and inhibits Kir6.2/SUR2A channels at high concentrations (1 microM).", "entity1": "Kir6.2", "entity2": "Nateglinide", "span1": [37, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9435": {"label": 3, "data": {"text": "Alendronate inhibition of protein-tyrosine-phosphatase-meg1.", "entity1": "protein-tyrosine-phosphatase-meg1", "entity2": "Alendronate", "span1": [26, 59], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10194": {"label": 3, "data": {"text": "In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2.", "entity1": "Oatp2", "entity2": "rifamycin SV", "span1": [166, 171], "span2": [9, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3157": {"label": 3, "data": {"text": "INTRODUCTION: In this study, we examined the effects of the alpha-glucosidase inhibitors acarbose and voglibose on postprandial plasma glucose and serum triglyceride levels in patients with type 2 diabetes mellitus.", "entity1": "alpha-glucosidase", "entity2": "glucose", "span1": [60, 77], "span2": [135, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9304": {"label": 3, "data": {"text": "The present study utilized blood from normal volunteers and 125I-fibrinogen in a dilute whole blood clot assay to determine the relative concentrations of lysine analogues required for inhibition of clot lysis induced by exogenous t-PA. AMCA (0.06 mM) and EACA (0.6 mM) were effective in prolonging clot lysis if (1) whole blood clots were formed and then exposed to a lysine analogue and exogenous t-PA or if (2) whole blood clots were formed in the presence of exogenous t-PA and a lysine analogue.", "entity1": "t-PA", "entity2": "EACA", "span1": [473, 477], "span2": [256, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2600": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "5-HT(2A)", "entity2": "risperidone", "span1": [269, 277], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10288": {"label": 3, "data": {"text": "An inhibitor of type B monoamine oxidase (MAO-B), (-)deprenyl (selegiline), was reported to have neuroprotective activity, but clinical trials failed to confirm it.", "entity1": "MAO-B", "entity2": "selegiline", "span1": [42, 47], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9765": {"label": 5, "data": {"text": "Herein, we evaluate the interaction of the alpha(2)-AR antagonist, yohimbine, as compared to fluparoxan, at multiple monoaminergic receptors and examine their roles in the modulation of adrenergic, dopaminergic and serotonergic transmission in freely-moving rats.", "entity1": "alpha(2)-AR antagonist", "entity2": "fluparoxan", "span1": [43, 65], "span2": [93, 103]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"698": {"label": 1, "data": {"text": "In summary, data obtained in our experiments in rat SMA indicate that the alpha 1-adrenoceptor mediating noradrenaline-induced contraction displays a distinct alpha 1L-adrenoceptor pharmacology.", "entity1": "alpha 1-adrenoceptor", "entity2": "noradrenaline", "span1": [74, 94], "span2": [105, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1058": {"label": 8, "data": {"text": "Follicle-stimulating hormone (FSH), a dimeric glycoprotein synthesized in the anterior pituitary gland, is important for the production of sex steroids and gametes.", "entity1": "Follicle-stimulating hormone", "entity2": "steroids", "span1": [0, 28], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15111": {"label": 1, "data": {"text": "Characterization of cytosolic glutathione peroxidase and phospholipid-hydroperoxide glutathione peroxidase genes in rainbow trout (Oncorhynchus mykiss) and their modulation by in vitro selenium exposure.", "entity1": "phospholipid-hydroperoxide glutathione peroxidase", "entity2": "selenium", "span1": [57, 106], "span2": [185, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5659": {"label": 2, "data": {"text": "Long-term treatment with 1 \u03bcM matrine or oxymatrine increased expression of the hERG protein and rescued the hERG surface expression disrupted by As(2)O(3).", "entity1": "hERG", "entity2": "oxymatrine", "span1": [80, 84], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10510": {"label": 0, "data": {"text": "RESULTS: GW572016 inhibited constitutive and/or ligand-induced EGFR or HER2 tyrosine phosphorylation of all five cell lines, which correlated with the antiproliferative response in all but one cell line.", "entity1": "HER2", "entity2": "tyrosine", "span1": [71, 75], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2584": {"label": 8, "data": {"text": "Methionine synthase reductase (MTRR) is an enzyme involved in the conversion of Hcy to methionine.", "entity1": "MTRR", "entity2": "methionine", "span1": [31, 35], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"1251": {"label": 3, "data": {"text": "The effects of theophylline (unspecific PDE inhibitor), vinpocetine (PDE1 inhibitor), EHNA (PDE2 inhibitor) and the PDE5 inhibitors zaprinast and E 4021 were weak.", "entity1": "PDE1", "entity2": "vinpocetine", "span1": [69, 73], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7495": {"label": 9, "data": {"text": "The AMPK inhibitor Compound C prevented the action of metformin and AICAR but not phenformin.", "entity1": "AMPK", "entity2": "metformin", "span1": [4, 8], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3590": {"label": 1, "data": {"text": "Taken together, these results suggest that wogonoside partially inhibits MDA-MB-231 cell growth by inducing autophagy through the MAPK-mTOR pathway and may be a promising anti-tumor agent.", "entity1": "MAPK", "entity2": "wogonoside", "span1": [130, 134], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1203": {"label": 0, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "vesicular monoamine transporter-2", "entity2": "monoamine", "span1": [174, 207], "span2": [207, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15844": {"label": 2, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "ABCA1", "entity2": "retinoic acid", "span1": [18, 23], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7381": {"label": 4, "data": {"text": "(2) Does in vivo administration of (R)-(alpha)-(-)-methylhistamine dihydrobromide (RAMH) (H3R agonist), thioperamide maleate (H3R antagonist) or histamine, in the absence/presence of thioperamide maleate, to bile duct ligated (BDL) rats regulate cholangiocyte proliferation?", "entity1": "H3R", "entity2": "(R)-(alpha)-(-)-methylhistamine dihydrobromide", "span1": [90, 93], "span2": [35, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10177": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "SLC21A6", "entity2": "rifamycin SV", "span1": [152, 159], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1228": {"label": 3, "data": {"text": "In addition, we found that MCP-1 transcription and translation was completely inhibited by mimosine, while MIP-2 transcription and translation was partially inhibited at 30 and 40 days; yet it was totally inhibited after 10 and 20 days in encysted diaphragm tissue infected by T. spiralis.", "entity1": "MCP-1", "entity2": "mimosine", "span1": [27, 32], "span2": [91, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14134": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "TAK1", "entity2": "Celastrol", "span1": [13, 17], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5381": {"label": 6, "data": {"text": "Rapamycin is a canonical allosteric inhibitor of the mTOR kinase with immunosuppressive and pro-apoptotic activities.", "entity1": "kinase", "entity2": "Rapamycin", "span1": [58, 64], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"6529": {"label": 3, "data": {"text": "Donepezil hydrochloride inaugurates a new class of AChE inhibitors with longer and more selective action and with manageable adverse effects.", "entity1": "AChE", "entity2": "Donepezil hydrochloride", "span1": [51, 55], "span2": [0, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"313": {"label": 5, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "5-HT4", "entity2": "tropisetron", "span1": [160, 165], "span2": [197, 208]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3632": {"label": 5, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "CB2", "entity2": "(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)", "span1": [352, 355], "span2": [374, 460]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6556": {"label": 3, "data": {"text": "In contrast, the mutants T844A, F972A and Q975A showed increased K(i) for cilostazol but no difference for milrinone from the recombinant PDE3A.", "entity1": "Q975A", "entity2": "cilostazol", "span1": [42, 47], "span2": [74, 84]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12528": {"label": 8, "data": {"text": "The test procedure was verified with respect to intestinal lactose hydrolysis by demonstrating a linear relationship between lactose/lactulose excretion and log jejunal mucosal lactase activity by in vitro assay (R2 = 0.95) in a further group of subjects.", "entity1": "lactase", "entity2": "lactose", "span1": [177, 184], "span2": [125, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1883": {"label": 1, "data": {"text": "OBJECTIVE: Ziprasidone is an atypical antipsychotic drug that shows a higher affinity for serotonin 5-HT(2) receptors compared with dopamine D(2) receptors in vitro.", "entity1": "dopamine D(2) receptors", "entity2": "Ziprasidone", "span1": [132, 155], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11701": {"label": 1, "data": {"text": "We report that wogonoside triggered the formation of microtubule-associated protein-light chain 3 (MAP-LC3) positive autophagosomes and the accumulation of acidic vesicular and autolysosomes in MDA-MB-231 cells.", "entity1": "microtubule-associated protein-light chain 3", "entity2": "wogonoside", "span1": [53, 97], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13586": {"label": 1, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "DVS", "span1": [6, 10], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9149": {"label": 5, "data": {"text": "Xanthines are classical antagonists for adenosine receptors for many of their pharmacological actions may be due to blockade of adenosine receptors.", "entity1": "adenosine receptors", "entity2": "Xanthines", "span1": [40, 59], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8375": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "glucose transporter-4", "entity2": "BPA", "span1": [96, 117], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1598": {"label": 3, "data": {"text": "Moreover, S1611 and S3226, both specific inhibitors of NHE3 only, or perfusion with Na+-free solutions, dose dependently increased DBS, as measured by pH-stat and CO2-sensitive electrode, without affecting intracellular pH.", "entity1": "NHE3", "entity2": "S1611", "span1": [55, 59], "span2": [10, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1599": {"label": 3, "data": {"text": "Moreover, S1611 and S3226, both specific inhibitors of NHE3 only, or perfusion with Na+-free solutions, dose dependently increased DBS, as measured by pH-stat and CO2-sensitive electrode, without affecting intracellular pH.", "entity1": "NHE3", "entity2": "S3226", "span1": [55, 59], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5504": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "fentanyl", "span1": [108, 126], "span2": [293, 301]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2868": {"label": 2, "data": {"text": "Recently, it has been shown that the activation of particular T2R bitter taste receptors is partially involved with the bitter aftertaste sensation of saccharin and acesulfame-K. To more fully understand the biology behind these phenomena we have addressed the question of whether AS could stimulate transient receptor potential vanilloid-1 (TRPV1) receptors, as these receptors are activated by a large range of structurally different chemicals.", "entity1": "T2R", "entity2": "saccharin", "span1": [62, 65], "span2": [151, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1959": {"label": 1, "data": {"text": "Probing for a hydrophobic a binding register in prostate-specific membrane antigen with phenylalkylphosphonamidates.", "entity1": "prostate-specific membrane antigen", "entity2": "phenylalkylphosphonamidates", "span1": [48, 82], "span2": [88, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"217": {"label": 1, "data": {"text": "The inhibition of [125I]LSD binding by other serotonergic agonists and antagonists revealed a pharmacological profile that does not correlate with that of any previously described serotonin receptor subtype.", "entity1": "serotonin receptor", "entity2": "[125I]LSD", "span1": [180, 198], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9968": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "MK-0966", "span1": [10, 15], "span2": [84, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9498": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "prilocaine", "span1": [28, 42], "span2": [94, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8741": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "imipramine", "span1": [18, 25], "span2": [94, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1413": {"label": 1, "data": {"text": "CONCLUSION: We have demonstrated that the behavioral effects of low doses of lisuride are clearly mediated by stimulation of 5-HT(1A) receptors.", "entity1": "5-HT(1A)", "entity2": "lisuride", "span1": [125, 133], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9099": {"label": 3, "data": {"text": "Inhibition of the leukotriene synthetase of rat basophil leukemia cells by diethylcarbamazine, and synergism between diethylcarbamazine and piriprost, a 5-lipoxygenase inhibitor.", "entity1": "5-lipoxygenase", "entity2": "diethylcarbamazine", "span1": [153, 167], "span2": [117, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1249": {"label": 3, "data": {"text": "Amrinone and milrinone, selective PDE3 inhibitors, suppressed TNF secretion to a lesser extent.", "entity1": "PDE3", "entity2": "milrinone", "span1": [34, 38], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14936": {"label": 8, "data": {"text": "Phosphodiesterase type 5 (PDE5) mediates the degradation of cGMP in a variety of tissues including brain.", "entity1": "Phosphodiesterase type 5", "entity2": "cGMP", "span1": [0, 24], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4623": {"label": 2, "data": {"text": "DNA methyltransferase 3a expression was increased in all BPA males and BPA 0.5 females and reduced in BPA 200 females.", "entity1": "DNA methyltransferase 3a", "entity2": "BPA", "span1": [0, 24], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2399": {"label": 1, "data": {"text": "As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening.", "entity1": "human MetAP2", "entity2": "anthranilic acid sulfonamides", "span1": [153, 165], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7990": {"label": 2, "data": {"text": "ISO significantly inhibited the levels of ERK1/2 kinase and increased the expression of JNK and p38 kinases.", "entity1": "kinases", "entity2": "ISO", "span1": [100, 107], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14226": {"label": 5, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b1", "entity2": "MPP", "span1": [288, 291], "span2": [303, 306]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8721": {"label": 3, "data": {"text": "In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/substrate, methyl-3,5-di-O-caffeoylquinate showed competitive inhibition of rhAR.", "entity1": "rhAR", "entity2": "methyl-3,5-di-O-caffeoylquinate", "span1": [148, 152], "span2": [83, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10402": {"label": 1, "data": {"text": "Taken together, these findings support the view that (1) OFQ is the only ppOFQ peptide that binds to and activates the ORL1 receptor and (2) OFQ II(1-28) does not bind or stimulate [35S]-GTPgammaS binding in cells expressing the mu opioid receptor.", "entity1": "ORL1", "entity2": "[35S]-GTPgammaS", "span1": [119, 123], "span2": [181, 196]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9755": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "alpha(2)-adrenergic receptors", "entity2": "fluparoxan", "span1": [73, 102], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9702": {"label": 3, "data": {"text": "The nonselective and irreversible MAO inhibitors, phenelzine (3-10 mg/kg), tranylcypromine (1-3 mg/kg), and nialamide (30 mg/kg), decreased rates of responding maintained by ethanol reinforcement.", "entity1": "MAO", "entity2": "phenelzine", "span1": [34, 37], "span2": [50, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6223": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-ht1f", "entity2": "naratriptan", "span1": [135, 141], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5802": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "amino acid", "span1": [125, 145], "span2": [61, 71]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15072": {"label": 2, "data": {"text": "Serum amyloid A upsurge precedes standard biomarkers of hepatotoxicity in ritodrine-injected mice.", "entity1": "Serum amyloid A", "entity2": "ritodrine", "span1": [0, 15], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"857": {"label": 0, "data": {"text": "Removal of N- and O-linked oligosaccharides reduces the M(r) to approximately 160,000, suggesting that approximately 60% of the mass of SPACRCAN is carbohydrate.", "entity1": "SPACRCAN", "entity2": "O", "span1": [136, 144], "span2": [18, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7545": {"label": 3, "data": {"text": "Phenelzine (PLZ), a nonselective irreversible inhibitor of monoamine oxidase (MAO), also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels.", "entity1": "GABA-T", "entity2": "PLZ", "span1": [117, 123], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15463": {"label": 8, "data": {"text": "The analytical method was applied to measurements of transport activities in membrane vesicles obtained from human multidrug resistance-associated protein 2-, 3-, and human bile salt export pump-expressing Sf9 cells for conjugated 3\u03b2-hydroxy-\u0394(5)-bile acids.", "entity1": "human bile salt export pump", "entity2": "3\u03b2-hydroxy-\u0394(5)-bile acids", "span1": [167, 194], "span2": [231, 257]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2040": {"label": 8, "data": {"text": "L-serine dehydratase (SDH), a member of the beta-family of pyridoxal phosphate-dependent (PLP) enzymes, catalyzes the deamination of L-serine and L-threonine to yield pyruvate or 2-oxobutyrate.", "entity1": "SDH", "entity2": "L-serine", "span1": [22, 25], "span2": [133, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2130": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "Monocarboxylate transporters", "entity2": "ketone", "span1": [0, 28], "span2": [156, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14297": {"label": 3, "data": {"text": "In utero exposure to valproic acid (VPA), a histone deacetylase (HDAC) inhibitor, causes neural tube, heart, and limb defects.", "entity1": "HDAC", "entity2": "VPA", "span1": [65, 69], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10917": {"label": 3, "data": {"text": "Both inhibitors, moreover, blunted the mucin secretory responses to beta-adrenergic agonist-generated second messenger, cAMP as well as adenylate cyclase activator, forskolin.", "entity1": "mucin", "entity2": "forskolin", "span1": [39, 44], "span2": [165, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8": {"label": 5, "data": {"text": "It is concluded that labetalol and dilevalol are beta 1-adrenoceptor selective antagonists.", "entity1": "beta 1-adrenoceptor", "entity2": "dilevalol", "span1": [49, 68], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13038": {"label": 2, "data": {"text": "ATRA regulates gene expression via the activation of the retinoic acid receptor (RAR)alpha in human DCs, and RARalpha acutely regulates CD1d expression.", "entity1": "RARalpha", "entity2": "ATRA", "span1": [109, 117], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13278": {"label": 9, "data": {"text": "The imatinib-resistant KIT(D816V) mutant, associated with systemic mastocytosis, was found to be resistant to sorafenib.", "entity1": "KIT", "entity2": "imatinib", "span1": [23, 26], "span2": [4, 12]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8463": {"label": 3, "data": {"text": "Hinokitiol also reduced the PKC activation and platelet aggregation stimulated by PDBu.", "entity1": "PKC", "entity2": "Hinokitiol", "span1": [28, 31], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9416": {"label": 4, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT1", "entity2": "CNT", "span1": [152, 157], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11328": {"label": 1, "data": {"text": "Serum carvedilol concentration and its relation to change in plasma brain natriuretic peptide level in the treatment of heart failure: a preliminary study.", "entity1": "brain natriuretic peptide", "entity2": "carvedilol", "span1": [68, 93], "span2": [6, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11683": {"label": 8, "data": {"text": "Despite the importance of AKRs in PAHs metabolism, there are no studies that evaluate, in general human populations, the effect of PAHs on AKRs expression in peripheral blood lymphocytes (PBLs).", "entity1": "AKRs", "entity2": "PAHs", "span1": [26, 30], "span2": [34, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3976": {"label": 8, "data": {"text": "To identify important covariates associated with interindividual variation in CYP2B6 activity in vivo, we evaluated these effects in healthy volunteers using bupropion (Wellbutrin SR GlaxoSmithKline, Research Triangle Park, NC) as a CYP2B6 probe substrate.", "entity1": "CYP2B6", "entity2": "bupropion", "span1": [233, 239], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11356": {"label": 8, "data": {"text": "Phenytoin (diphenylhydantoin, DPH) is an established sodiumsodium channel blocker and is a useful anticonvulsant and class 1b antiarrhythmic, and has been effectively used in the treatment of neuropathic pain.", "entity1": "sodium channel", "entity2": "sodium", "span1": [59, 73], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4176": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "hydrogen peroxide", "span1": [118, 122], "span2": [227, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15265": {"label": 2, "data": {"text": "Three variables of cardiac vagal effects (the root mean square of successive differences [rMSSD] in the interbeat interval of the heart rate [IBI], heart-rate variability [HRV] caused by peak-valley respiratory sinus arrhythmia [pvRSA], and high-frequency power [HF]) and heart rate (HR) were obtained at seven time points during the clamps, characterised by increasing levels of insulin (achieved by administering insulin plus glucose, glucose only, glucose and GLP-1, and glucose and GLP-1 combined with arginine).", "entity1": "insulin", "entity2": "glucose", "span1": [380, 387], "span2": [451, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"419": {"label": 1, "data": {"text": "RS 17053 showed high affinity and selectivity for alpha 1A adrenoceptors (pKi 8.6) relative to alpha 1B (pKi = 7.3) and alpha 1D (pKi = 7.1) subtypes.", "entity1": "alpha 1B", "entity2": "RS 17053", "span1": [95, 103], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2865": {"label": 8, "data": {"text": "4-Hydroxynonenal (4-HNE) is a mutagenic alpha,beta-unsaturated aldehyde produced during oxidative injury that is conjugated by several glutathione S-transferase (GST) isoforms.", "entity1": "GST", "entity2": "alpha,beta-unsaturated aldehyde", "span1": [162, 165], "span2": [40, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1070": {"label": 3, "data": {"text": "Triacsin C, a competitive inhibitor of both ACS1 and ACS4, inhibited ACS activity similarly in endoplasmic reticulum, MAM, and mitochondria, suggesting that a hitherto unidentified triacsin-sensitive ACS is present in mitochondria.", "entity1": "ACS", "entity2": "Triacsin C", "span1": [69, 72], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6748": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "RTKs", "entity2": "Gleevec", "span1": [155, 159], "span2": [107, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7590": {"label": 1, "data": {"text": "Interaction with the hERG channel and cytotoxicity of amiodarone and amiodarone analogues.", "entity1": "hERG", "entity2": "amiodarone", "span1": [21, 25], "span2": [69, 79]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"639": {"label": 1, "data": {"text": "To establish the relative importance of these subtypes, we compared the effects of sumatriptan with those of a selective 5-HT1F receptor agonist (LY 344864) on c-fos protein expression in the trigeminal nucleus caudalis.", "entity1": "c-fos", "entity2": "sumatriptan", "span1": [160, 165], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2818": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "CXCL-8", "entity2": "Dexamethasone", "span1": [48, 54], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2385": {"label": 3, "data": {"text": "Sorafenib inhibited the kinase activity of both C-RAF and B-RAF (wild type and V600E mutant).", "entity1": "kinase", "entity2": "Sorafenib", "span1": [24, 30], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6084": {"label": 9, "data": {"text": "However, amantadine induction of Fos in the striatum was unaffected by the dopamine D2 receptor antagonist, sulpiride.", "entity1": "Fos", "entity2": "sulpiride", "span1": [33, 36], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5172": {"label": 1, "data": {"text": "In PFC, DEX caused activation of AKT, augmentation of pro-survival Bcl-2 protein and enhanced Bcl-2/Bax protein ratio, as well Bcl-2 translocation to mitochondria.", "entity1": "Bcl-2", "entity2": "DEX", "span1": [127, 132], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"726": {"label": 9, "data": {"text": "Endothelial NO synthase expression was increased by cilazapril but not by losartan.", "entity1": "Endothelial NO synthase", "entity2": "losartan", "span1": [0, 23], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3709": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "caspase-3", "entity2": "BPs", "span1": [158, 167], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2074": {"label": 2, "data": {"text": "Synergistic cytotoxicity was demonstrated, and pemetrexed significantly decreased the amount of phosphorylated Akt, enhanced apoptosis, and increased the expression of dCK in A549 and Calu-6 cells, as well as the expression of the human nucleoside equilibrative transporter 1 (hENT1) in all cell lines.", "entity1": "dCK", "entity2": "pemetrexed", "span1": [168, 171], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11085": {"label": 3, "data": {"text": "Effects of felodipine (a dihydropyridine calcium channel blocker) and analogues on calmodulin-dependent enzymes.", "entity1": "calcium channel", "entity2": "felodipine", "span1": [41, 56], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12385": {"label": 1, "data": {"text": "Evidence also outlines a role for oxytocin in the prosocial effects of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) in both rodents and humans.", "entity1": "oxytocin", "entity2": "3,4-methylenedioxymethamphetamine", "span1": [34, 42], "span2": [71, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4389": {"label": 1, "data": {"text": "In this study, we have identified topoisomerase II\u03b2 (Top2\u03b2) as a specific determinant for CPT sensitivity, but not for many other cytotoxic agents, in non-S-phase cells.", "entity1": "Top2\u03b2", "entity2": "CPT", "span1": [53, 58], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1590": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline", "span1": [59, 64], "span2": [313, 374]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4540": {"label": 3, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "MAO-A", "entity2": "harmaline", "span1": [69, 74], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"556": {"label": 5, "data": {"text": "Both the 5 alpha-reductase inhibitor finasteride and alpha 1-adrenoceptor antagonists (e.g. alfuzosin, doxazosin, prazosin, tamsulosin and terazosin) have been recommended as appropriate treatment options for patients with lower urinary tract symptoms (LUTS) associated with benign prostatic obstruction (BPO), and their efficacy has been proven in several placebo-controlled trials.", "entity1": "alpha 1-adrenoceptor", "entity2": "alfuzosin", "span1": [53, 73], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13171": {"label": 2, "data": {"text": "These results highlight the importance of PR activation of the Src/MAPK signaling pathway for progesterone-induced transcription of select target genes and cell cycle progression.", "entity1": "PR", "entity2": "progesterone", "span1": [42, 44], "span2": [94, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11679": {"label": 0, "data": {"text": "Antibodies to either the C- or N- terminus of VMAT-1 detected two proteins (73 and 55 kD) in transfected COS-1 cells.", "entity1": "VMAT-1", "entity2": "N", "span1": [46, 52], "span2": [31, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6222": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-HT1D", "entity2": "naratriptan", "span1": [115, 121], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8043": {"label": 2, "data": {"text": "Finally, chronic administration of metformin in diabetic mice restored cardiac autophagy by activating JNK1-Bcl-2 pathways and dissociating Beclin1 and Bcl-2.", "entity1": "Bcl-2", "entity2": "metformin", "span1": [108, 113], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13638": {"label": 0, "data": {"text": "Crystallographic data reveal that a conserved Gly residue (located at the juncture between the linker and C-terminal domains) is at one end of a short alpha-helix, which extends to the active site Tyr covalently linked to the DNA.", "entity1": "alpha-helix", "entity2": "C", "span1": [151, 162], "span2": [106, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4559": {"label": 3, "data": {"text": "In addition, ethanol induced degradation of DNA methyltransferases (DNMT-1, DNMT-3a, and DNMT-3b), as well as the methyl CpG-binding proteins (MeCP-2, MBD-2 and MBD-3), in MEF cells by the proteasomal pathway.", "entity1": "DNMT-3b", "entity2": "ethanol", "span1": [89, 96], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5896": {"label": 1, "data": {"text": "Fibric acids, in particular, act by stimulating the catabolism of VLDL and also, as a consequence, improving LDL delipidation, thus favoring receptor uptake.", "entity1": "LDL", "entity2": "Fibric acids", "span1": [109, 112], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"952": {"label": 1, "data": {"text": "The antagonistic property of rilmenidine at human alpha(2A)-adrenoceptors indicates that in contrast to the suggestion based on rabbit data, the hypotensive property of the drug in humans is not due to activation of alpha(2A)-adrenoceptors but other, presumably I(1)-imidazoline receptors, are probably involved.", "entity1": "I(1)-imidazoline receptors", "entity2": "rilmenidine", "span1": [262, 288], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1495": {"label": 3, "data": {"text": "Similarly, pretreatment with sulindac sulfide blocks the ability of EGF to induce ERK1/2 and Bad phosphorylation, but also down-regulates total Bad but not ERK1/2 protein levels.", "entity1": "EGF", "entity2": "sulindac sulfide", "span1": [68, 71], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14822": {"label": 3, "data": {"text": "Dabigatran has an advantage over the indirect thrombin inhibitors, unfractionated heparin and low-molecular-weight heparin, in that it inhibits free and fibrin-bound thrombin.", "entity1": "fibrin", "entity2": "Dabigatran", "span1": [153, 159], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1233": {"label": 0, "data": {"text": "We report herein the location of the binding site for the inhaled anesthetic halothane at the amino acid residue level of resolution in the ligand binding cavity in a prototypical G protein-coupled receptor, bovine rhodopsin.", "entity1": "G protein-coupled receptor", "entity2": "amino acid", "span1": [180, 206], "span2": [94, 104]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13692": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "porcine TLR7", "entity2": "imiquimod", "span1": [83, 95], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6032": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "8-hydroxy-2-(di-n-propylamino) tetralin", "span1": [63, 69], "span2": [235, 274]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5318": {"label": 3, "data": {"text": "Furthermore, these phosphorylated flavonoids demonstrated good to high selectivity for CEase over AChE, which only showed micromolar potency inhibition of AChE.", "entity1": "CEase", "entity2": "phosphorylated flavonoids", "span1": [87, 92], "span2": [19, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14536": {"label": 3, "data": {"text": "Data at transcriptional level also demonstrated that catalpol potently attenuated gene expressions involved in inflammation, such as iNOS, COX-2 and TLR4.", "entity1": "TLR4", "entity2": "catalpol", "span1": [149, 153], "span2": [53, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15840": {"label": 1, "data": {"text": "When the expression of ABCA1 and ABCG1 was induced, 24-OHC efflux was stimulated in the presence of high density lipoprotein (HDL), whereas apolipoprotein A-I was not an efficient acceptor.", "entity1": "HDL", "entity2": "24-OHC", "span1": [126, 129], "span2": [52, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7962": {"label": 0, "data": {"text": "A domain in the carboxy-terminus of TSPO was identified and characterized as the cholesterol recognition/interaction amino acid consensus (CRAC).", "entity1": "TSPO", "entity2": "carboxy", "span1": [36, 40], "span2": [16, 23]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15285": {"label": 1, "data": {"text": "In contrast, normal CB(1) receptor expression and function were maintained following repeated administration of low dose JZL184 (\u22648 mg/kg).", "entity1": "CB(1)", "entity2": "JZL184", "span1": [20, 25], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12765": {"label": 1, "data": {"text": "Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography.", "entity1": "histamine H1-receptor", "entity2": "fexofenadine", "span1": [121, 142], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2930": {"label": 0, "data": {"text": "AdSS from the thermophilic archaea, Methanocaldococcus jannaschii (MjAdSS) is 345 amino acids long against an average length of 430-457 amino acids for most mesophilic AdSS.", "entity1": "AdSS", "entity2": "amino acids", "span1": [0, 4], "span2": [82, 93]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2488": {"label": 3, "data": {"text": "Licofelone reduced intima/media ratio in injured arteries, the macrophages infiltration in the neointimal area, monocyte chemoattractant protein-1 (MCP-1) gene expression, and the activation of nuclear factor-kappaB in rabbit atheroma.", "entity1": "nuclear factor-kappaB", "entity2": "Licofelone", "span1": [194, 215], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14991": {"label": 9, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "CD69", "entity2": "EPA", "span1": [277, 281], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6889": {"label": 1, "data": {"text": "Studies in NPC1L1 knockout mice indicate that this transporter is essential for the intestinal uptake of sterols and that NPC1L1 might also be involved in the mechanism of action of ezetimibe.", "entity1": "NPC1L1", "entity2": "ezetimibe", "span1": [122, 128], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15871": {"label": 1, "data": {"text": "Presynaptic CaMKII\u03b1 modulates dopamine D3 receptor activation in striatonigral terminals of the rat brain in a Ca(2+) dependent manner.", "entity1": "CaMKII\u03b1", "entity2": "Ca(2+)", "span1": [12, 19], "span2": [111, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7289": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "furin", "entity2": "PFD", "span1": [175, 180], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15395": {"label": 0, "data": {"text": "p14ARF perturbs the androgen-induced interaction between the N terminus and C terminus of AR.", "entity1": "AR", "entity2": "N", "span1": [90, 92], "span2": [61, 62]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7934": {"label": 3, "data": {"text": "Glucosamine at 50\u00a0mM was demonstrated to elevate both the mRNA and protein expression of p53 and heme oxygenase-1 (HO-1), but also caused a reduction in p21 protein expression.", "entity1": "p21", "entity2": "Glucosamine", "span1": [153, 156], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5936": {"label": 3, "data": {"text": "Cyproterone acetate, a progestin used in the treatment of hirsutism, acne and prostate cancer as well as norgestrel and norethindrone that are widely used as oral contraceptives also inhibit 3 beta-HSD activity at Ki values of 1.5, 1.7 and 2.5 microM, respectively.", "entity1": "3 beta-HSD", "entity2": "norethindrone", "span1": [191, 201], "span2": [120, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7867": {"label": 2, "data": {"text": "Fingolimod (FTY720), a novel drug approved for the treatment of relapsing-remitting multiple sclerosis, activates different sphingosine-1-phosphate receptor (S1PR) subtypes.", "entity1": "sphingosine-1-phosphate receptor", "entity2": "FTY720", "span1": [124, 156], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6160": {"label": 1, "data": {"text": "A 59-year-old female suffering from malignant lymphoma developed therapy-related acute myeloblastic leukemia (t-AML) after chemotherapy consisting of treatment with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and an alkylating agent, cyclophosphamide.", "entity1": "DNA-topoisomerase II", "entity2": "cyclophosphamide", "span1": [165, 185], "span2": [251, 267]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15302": {"label": 3, "data": {"text": "Therefore, we examined whether the PDE5-I vardenafil improves memory and executive functioning and affect electroencephalography (EEG) in healthy young adults.", "entity1": "PDE5", "entity2": "vardenafil", "span1": [35, 39], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"902": {"label": 7, "data": {"text": "Tetrahydrobiopterin [(6R)-5,6,7,8-tetrahydro-L-biopterin, H(4)biopterin] is one of several cofactors of nitric oxide synthases (EC 1.14.13.39).", "entity1": "EC 1.14.13.39", "entity2": "Tetrahydrobiopterin", "span1": [128, 141], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"7530": {"label": 3, "data": {"text": "While vitamin C is essential for PHD activity in vitro, N-acetyl-L-cysteine had no effect, and gallic acid or n-propyl gallate efficiently inhibited the activity of all three PHDs, demonstrating different functions of these antioxidants.", "entity1": "PHDs", "entity2": "gallic acid", "span1": [175, 179], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4439": {"label": 3, "data": {"text": "Using the mTOR inhibitor PP242, we found that TGF\u03b2-induced both early and sustained activation of TORC1 and TORC2 was necessary for deptor suppression.", "entity1": "mTOR", "entity2": "PP242,", "span1": [10, 14], "span2": [25, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10172": {"label": 1, "data": {"text": "In conclusion, these results show that rifamycin SV and rifampicin interact with OATP-mediated substrate transport to different extents.", "entity1": "OATP", "entity2": "rifamycin SV", "span1": [81, 85], "span2": [39, 51]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"4087": {"label": 2, "data": {"text": "In this study, aldosterone (ALD)-induced apoptosis of cardiomyocyte was evaluated based on the previous studies, and the roles of calpain signaling were clarified.", "entity1": "calpain", "entity2": "ALD", "span1": [130, 137], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8402": {"label": 9, "data": {"text": "The switch control inhibitor DCC-2036 was similarly inactive against FLT3 AL mutations.", "entity1": "FLT3", "entity2": "DCC-2036", "span1": [69, 73], "span2": [29, 37]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11067": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "myosin light chain kinase", "entity2": "Ca2+", "span1": [131, 156], "span2": [181, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4903": {"label": 3, "data": {"text": "Synthesis and in vitro evaluation of N-Aryl pyrido-quinazolines derivatives as potent EGFR inhibitors.", "entity1": "EGFR", "entity2": "N-Aryl pyrido-quinazolines", "span1": [86, 90], "span2": [37, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1820": {"label": 1, "data": {"text": "Quinone oxidoreductase 2 (QR2) purified from human red blood cells was recently shown to be a potential target of the quinoline antimalarial compounds [Graves et al., (2002) Mol.", "entity1": "QR2", "entity2": "quinoline", "span1": [26, 29], "span2": [118, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3838": {"label": 3, "data": {"text": "The inhibition of phosphoinositide 3-kinase using Ly294002 augmented a decrease in the p21 level induced by their combination, but it showed no significant effects on expression of Sp1 and cyclin D1.", "entity1": "phosphoinositide 3-kinase", "entity2": "Ly294002", "span1": [18, 43], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12631": {"label": 1, "data": {"text": "Thymidine kinase from Herpes simplex virus type 1 (TK) was crystallized in an N-terminally truncated but fully active form.", "entity1": "Thymidine kinase", "entity2": "N", "span1": [0, 16], "span2": [78, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13656": {"label": 0, "data": {"text": "The distances between the protons H20 and H2, H18 and H2, and H18 and H4 are shorter following their binding to the PGIS in solution-down to within 5 A.", "entity1": "PGIS", "entity2": "H4", "span1": [116, 120], "span2": [70, 72]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3968": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "peptidyl-prolyl cis/trans-isomerase A1", "entity2": "Pro", "span1": [26, 64], "span2": [146, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"6615": {"label": 8, "data": {"text": "Thus, the current study suggests that coadministration of clinical doses of promethazine and homochlorcyclizine increases the Css of haloperidol and reduced haloperidol via the inhibitory effects on the CYP2D6-catalyzed metabolism of haloperidol and reduced haloperidol.", "entity1": "CYP2D6", "entity2": "haloperidol", "span1": [203, 209], "span2": [258, 269]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13415": {"label": 9, "data": {"text": "The mRNA expression of PtdSer synthase 1 (PSS1) and PtdSer synthase 2 (PSS2) was not reduced by ethanol.", "entity1": "PSS2", "entity2": "ethanol", "span1": [71, 75], "span2": [96, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13610": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "VEGFR-3", "entity2": "Sorafenib", "span1": [151, 158], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11330": {"label": 1, "data": {"text": "OBJECTIVE: To examine the influence of carvedilol dose and concentration in serum on plasma brain natriuretic peptide (BNP), a measure of heart failure progression.", "entity1": "BNP", "entity2": "carvedilol", "span1": [119, 122], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7396": {"label": 3, "data": {"text": "Results of early clinical trials with both topically (cipamfylline, CP80,633) and systemically (CC-10004) active PDE4 inhibitors demonstrated efficacy in atopic dermatitis and in the case of CC-10004, also in psoriasis.", "entity1": "PDE4", "entity2": "CP80,633", "span1": [113, 117], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15743": {"label": 1, "data": {"text": "However, the precise mechanism by which quercetin counteracts CYP2E1-mediated ethanol hepatotoxicity through HO-1 system is still remained unclear.", "entity1": "CYP2E1", "entity2": "ethanol", "span1": [62, 68], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6053": {"label": 2, "data": {"text": "Neither ryanodine nor EGTA inhibited down-regulation of alpha-AR mRNA by NE.", "entity1": "alpha-AR", "entity2": "ryanodine", "span1": [56, 64], "span2": [8, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10502": {"label": 1, "data": {"text": "The nonsteroidal anti-inflammatory drugs flurbiprofen and ibuprofen were modified in an attempt to alter the kinetics of inhibitor binding by COX-1.", "entity1": "COX-1", "entity2": "flurbiprofen", "span1": [142, 147], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12235": {"label": 1, "data": {"text": "Photolytic release of free alanine results in the generation of significant transient current components in HEK293 cells expressing the ASCT2, SNAT1, and SNAT2 proteins.", "entity1": "SNAT1", "entity2": "alanine", "span1": [143, 148], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6763": {"label": 2, "data": {"text": "In vivo, hydralazine induced HIF-1alpha and VEGF protein in tissue extracts and elevated plasma VEGF levels.", "entity1": "VEGF", "entity2": "hydralazine", "span1": [44, 48], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5111": {"label": 2, "data": {"text": "Thus, we found that 5HHMF enhances heme oxygenase-1 (HO-1) expression via nuclear factor-erythroid 2-related factor 2 (Nrf2) activation.", "entity1": "HO-1", "entity2": "5HHMF", "span1": [53, 57], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7274": {"label": 3, "data": {"text": "The best inhibitors were brinzolamide and sulpiride (KI values of 0.8-0.9 nM), the latter compound being also a CA VI-selective inhibitor.", "entity1": "CA VI", "entity2": "brinzolamide", "span1": [112, 117], "span2": [25, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14922": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "27-hydroxycholesterol", "span1": [257, 260], "span2": [78, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"989": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "eNOS", "entity2": "tetrahydrobiopterin", "span1": [180, 184], "span2": [38, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"5515": {"label": 3, "data": {"text": "In phosphotriesterase and physostigmine-treated mice, a 4- and 2-fold higher sarin dose, respectively, was needed to cause a 50% inhibition of brain AChE activity.", "entity1": "AChE", "entity2": "sarin", "span1": [149, 153], "span2": [77, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11059": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "(A) cyclosporine", "span1": [89, 95], "span2": [200, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5369": {"label": 9, "data": {"text": "Nicotine does not account for the CSE stimulation of VEGF in HFL-1.", "entity1": "VEGF", "entity2": "Nicotine", "span1": [53, 57], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1470": {"label": 8, "data": {"text": "When cultured in liquid minimal medium, yeast cells expressing the mutated gamma-glutamyl kinase were found to accumulate intracellular L-proline and showed a prominent increase in cell viability after freezing at -20 degrees C compared to the viability of cells harboring the wild-type PRO1 gene.", "entity1": "gamma-glutamyl kinase", "entity2": "L-proline", "span1": [75, 96], "span2": [136, 145]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6072": {"label": 0, "data": {"text": "Degenerate oligonucleotides corresponding to conserved amino acids from transmembrane domains III, V, and VI of known receptors [5-HT1A, 5-HT1C, and 5-HT2; 5-HT is serotonin (5-hydroxytryptamine)] were used as primers for the sequential reactions.", "entity1": "5-HT2", "entity2": "amino acids", "span1": [149, 154], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3096": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "SoRI-20041", "span1": [354, 357], "span2": [177, 187]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10868": {"label": 5, "data": {"text": "Moreover, 4-methylhistamine potently activated the hH(4)R (pEC(50) = 7.4 +/- 0.1; alpha = 1), and this response was competitively antagonized by the selective H(4)R antagonist JNJ 7777120 [1-[(5-chloro-1H-indol-2-yl)-carbonyl]-4-methylpiperazine] (pA(2) = 7.8).", "entity1": "H(4)R", "entity2": "JNJ 7777120", "span1": [159, 164], "span2": [176, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"509": {"label": 3, "data": {"text": "Felodipine and nicardipine have similar affinities for 60-kDa CaMPDE isozymes but bring about different levels of enzyme inhibition, suggesting the possibility of designing specific drugs that can protect the enzyme from inhibition by dihydropyridine Ca2+-channel blockers.", "entity1": "CaMPDE", "entity2": "dihydropyridine", "span1": [62, 68], "span2": [235, 250]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11515": {"label": 2, "data": {"text": "The beneficial role of 17beta-estradiol on blood pressure, cardiac hypertrophy, vascular osteopontin expression, perivascular fibrosis, and impaired NO-dependent relaxation of isolated aortic rings was completely abrogated by coadministration of medroxyprogesterone acetate.", "entity1": "osteopontin", "entity2": "17beta-estradiol", "span1": [89, 100], "span2": [23, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7538": {"label": 3, "data": {"text": "Phenelzine (PLZ), a nonselective irreversible inhibitor of monoamine oxidase (MAO), also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels.", "entity1": "GABA-T", "entity2": "Phenelzine", "span1": [117, 123], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1198": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "aminopeptidase A", "entity2": "L-glutamic acid", "span1": [304, 320], "span2": [284, 299]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14926": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "3\u03b2-hydroxyl", "span1": [266, 269], "span2": [144, 155]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9328": {"label": 1, "data": {"text": "Cell lines stably expressing EAA3a protein formed homomeric ligand-gated ion channels responsive, in order of decreasing affinity to domoate, kainate, L-glutamate and (RS)-alpha-amino-3-hydroxy-5- methylisoxazole-propionate (AMPA).", "entity1": "EAA3a", "entity2": "kainate", "span1": [29, 34], "span2": [142, 149]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15427": {"label": 1, "data": {"text": "These results suggest that internalization and excretion of 7-ketostigmasterol is probably influenced by [Ca]i, which also could mediate HMGCoA activity in POPs metabolism.", "entity1": "HMGCoA", "entity2": "Ca", "span1": [137, 143], "span2": [106, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1973": {"label": 3, "data": {"text": "SNP inhibits the accumulation of HIF-1alpha, the regulatory subunit of HIF-1, and the transcriptional activation of HIF-1alpha via a mechanism that is not dependent on either NO or soluble guanylate cyclase.", "entity1": "HIF-1alpha", "entity2": "SNP", "span1": [116, 126], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15268": {"label": 0, "data": {"text": "In a mouse tumor model, removal of only the C-terminal propeptide from full-length VEGF-D was sufficient to enhance angiogenesis and tumor growth.", "entity1": "VEGF-D", "entity2": "C", "span1": [83, 89], "span2": [44, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14319": {"label": 1, "data": {"text": "In summary, DMF attenuated renal fibrosis via the Nrf2-mediated inhibition of TGF-beta/Smad3 signaling in an ARE-independent manner, suggesting that DMF could be used to treat renal fibrosis.", "entity1": "ARE", "entity2": "DMF", "span1": [109, 112], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12932": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CBS", "entity2": "L-Cys", "span1": [160, 163], "span2": [182, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9759": {"label": 5, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "h5-HT(1B)", "entity2": "yohimbine", "span1": [93, 102], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5204": {"label": 0, "data": {"text": "We analysed the role of the MBD in MeCP2-chromatin associations in vivo using an MeCP2 mutant Rett syndrome mouse model (Mecp2(tm)(1)(. )(1)(Jae)) in which exon 3 deletion results in an N-terminal truncation of the protein, including most of the MBD.", "entity1": "MeCP2", "entity2": "N", "span1": [35, 40], "span2": [186, 187]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7738": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "VEGFR2", "entity2": "cabozantinib", "span1": [107, 113], "span2": [16, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2951": {"label": 0, "data": {"text": "Cocrystal structures of PDE5 catalytic (C) domain with inhibitors reveal a hydrogen bond and hydrophobic interactions with Tyr-612, hydrogen bonds with Gln-817, a hydrophobic clamp formed by Phe-820 and Val-782, and contacts with His-613, Leu-765, and Phe-786 [Sung et al.", "entity1": "PDE5 catalytic (C) domain", "entity2": "Gln", "span1": [24, 49], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9449": {"label": 1, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP2", "entity2": "butaprost", "span1": [90, 93], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4182": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "aldo-keto reductase (AKR) 1C1", "entity2": "hydrogen peroxide", "span1": [262, 291], "span2": [227, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11154": {"label": 1, "data": {"text": "Along with weight loss, orlistat also favourably affects blood pressure and glucose and insulin levels in obese individuals and in obese type 2 diabetic patients.", "entity1": "insulin", "entity2": "orlistat", "span1": [88, 95], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12448": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "ML326", "span1": [215, 217], "span2": [181, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9619": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBF2", "entity2": "glibenclamide", "span1": [232, 236], "span2": [120, 133]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11865": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "CYP1A1", "entity2": "delphinidin", "span1": [150, 156], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6220": {"label": 3, "data": {"text": "This study thus demonstrates that the first administration of the recommended starting dose of irbesartan induces a greater and longer lasting Ang II receptor blockade than that of valsartan and losartan in normotensive subjects.", "entity1": "Ang II receptor", "entity2": "losartan", "span1": [143, 158], "span2": [195, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9778": {"label": 4, "data": {"text": "The delta-receptor antagonist, SB 244525 (10 mg/kg, i.p. ), inhibited the antitussive effect of SB 227122 (20 mg/kg, i.p.).", "entity1": "delta-receptor", "entity2": "SB 227122", "span1": [4, 18], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12194": {"label": 1, "data": {"text": "A follow-up study of the expression of D6D and D5D genes in Chinese who live in European countries with high SFA and MUFA diets would be of interest.", "entity1": "D6D", "entity2": "SFA", "span1": [39, 42], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13878": {"label": 3, "data": {"text": "Recently, we have demonstrated that ibuprofen inhibits intracellular signaling of RhoA and promotes significant axonal growth and functional recovery following spinal cord lesions in rodents.", "entity1": "RhoA", "entity2": "ibuprofen", "span1": [82, 86], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3683": {"label": 2, "data": {"text": "Both tolbutamide and gliclazide stimulated phospholipase C activity; however, only gliclazide did so independently of its activity at K(ATP) channels, and this activity was partially inhibited by pertussis toxin.", "entity1": "phospholipase C", "entity2": "gliclazide", "span1": [43, 58], "span2": [21, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14806": {"label": 1, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1) receptor", "entity2": "SR141716A", "span1": [155, 169], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3032": {"label": 8, "data": {"text": "Both risperidone and 9-hydroxyrisperidone are substrates of P-glycoprotein (P-gp), a transport protein involved in drug absorption, distribution, and elimination.", "entity1": "P-gp", "entity2": "risperidone", "span1": [76, 80], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"3525": {"label": 8, "data": {"text": "Inhibition studies revealed that the multidrug resistance-associated proteins (ABCCs) are involved in the transport of BPDE glutathione conjugates.", "entity1": "ABCCs", "entity2": "BPDE glutathione", "span1": [79, 84], "span2": [119, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5990": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "t-PA", "entity2": "EACA", "span1": [121, 125], "span2": [226, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3248": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "DHT", "span1": [13, 16], "span2": [210, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11113": {"label": 1, "data": {"text": "Finally, a third nonadrenergic internal membrane site, labeled by [3H]IDX, was consistent with a subtype-I2 imidazol(in)e receptor site (rank order: cirazoline > IDX >> amiloride > moxonidine > clonidine).", "entity1": "subtype-I2 imidazol(in)e receptor", "entity2": "amiloride", "span1": [97, 130], "span2": [169, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10590": {"label": 3, "data": {"text": "Auranofin, an antirheumatic gold compound, is an inhibitor of selenocysteine enzymes, such as thioredoxin reductase and glutathione peroxidase.", "entity1": "selenocysteine enzymes", "entity2": "Auranofin", "span1": [62, 84], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1799": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "ZD1839", "span1": [0, 32], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5352": {"label": 2, "data": {"text": "S1P activated phosphatidylinositol 3-kinase (PI3K)/Akt signaling, leading to the inhibition of glycogen synthase kinase-3\u03b2 and the nuclear translocation of \u03b2-catenin, followed by the increase of the transcriptional activity by \u03b2-catenin/T-cell factor complex formation in both SaOS-2 cells and MC3T3-E1 cells.", "entity1": "Akt", "entity2": "S1P", "span1": [51, 54], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3962": {"label": 1, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "peptidyl-prolyl cis/trans-isomerase A1", "entity2": "HNE", "span1": [26, 64], "span2": [225, 228]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"5649": {"label": 2, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "K(+) channel", "entity2": "oxymatrine", "span1": [30, 42], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15092": {"label": 3, "data": {"text": "Avibactam (formerly NXL104, AVE1330A) is a synthetic non-\u03b2-lactam, \u03b2-lactamase inhibitor that inhibits the activities of Ambler class A and C \u03b2-lactamases and some Ambler class D enzymes.", "entity1": "Ambler class D", "entity2": "Avibactam", "span1": [164, 178], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3294": {"label": 3, "data": {"text": "Rasagiline inhibits MAO-B more potently than selegiline and has the advantage of once-daily dosing.", "entity1": "MAO-B", "entity2": "Rasagiline", "span1": [20, 25], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9808": {"label": 8, "data": {"text": "With respect to the quinone co-substrate of the dihydroorotate dehydrogenase, atovaquone (Kic = 2.7 microM) and dichloroally-lawsone (Kic = 9.8 nM) were shown to be competitive inhibitors of human dihydroorotate dehydrogenase.", "entity1": "dihydroorotate dehydrogenase", "entity2": "quinone", "span1": [48, 76], "span2": [20, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9491": {"label": 3, "data": {"text": "Monoamine uptake inhibitors structurally analogous to cocaine (cocaethylene, CFT, betaCIT, CPT, (+)-cocaine, norcocaine, and benztropine) also produced this rapid pressor response, whereas structurally unrelated uptake inhibitors with diverse monoamine transporter selectivities (BTCP, indatraline, GBR 12935, mazindol, nomifensine, and zimeldine) either did not produce a rapid pressor response or produced only a small pressor response.", "entity1": "monoamine transporter", "entity2": "GBR 12935", "span1": [243, 264], "span2": [299, 308]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, 9]},
	"15440": {"label": 3, "data": {"text": "Liver AOX activity was reduced by 45% with tungsten and 61% with hydralazine and 81% in AOX-deficient mice relative to controls.", "entity1": "AOX", "entity2": "hydralazine", "span1": [6, 9], "span2": [65, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7811": {"label": 8, "data": {"text": "These results provide a rationale for future design of therapeutic apolipoprotein mimetic peptides and provide new insights into the interaction of hydrophobic residues on apolipoproteins with phospholipids in the lipid microdomain created by the ABCA1 transporter during the cholesterol efflux process.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [247, 252], "span2": [276, 287]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13285": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "PDGFR", "entity2": "Sorafenib", "span1": [244, 249], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14447": {"label": 5, "data": {"text": "Receptor binding was significantly reduced by specific AhR antagonist salicyl amide.", "entity1": "AhR", "entity2": "salicyl amide", "span1": [55, 58], "span2": [70, 83]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2645": {"label": 8, "data": {"text": "The latter reaction, catalyzed by aspartoacylase (ASPA), produces acetyl groups plus aspartate and has been proposed to occur in both soluble and membranous subfractions of white matter.", "entity1": "aspartoacylase", "entity2": "aspartate", "span1": [34, 48], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"7462": {"label": 8, "data": {"text": "The mechanisms that specify the vesicular phenotype of inhibitory interneurons in vertebrates are poorly understood because the two main inhibitory transmitters, glycine and GABA, share the same vesicular inhibitory amino acid transporter (VIAAT) and are both present in neurons during postnatal development.", "entity1": "vesicular inhibitory amino acid transporter", "entity2": "glycine", "span1": [195, 238], "span2": [162, 169]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"10794": {"label": 3, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "ICAM-1", "entity2": "simvastatin", "span1": [67, 73], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14921": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "estrogen receptor-\u03b1", "entity2": "27-hydroxycholesterol", "span1": [236, 255], "span2": [78, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9537": {"label": 8, "data": {"text": "System y+ cationic amino acid transport is mediated by proteins encoded by a family of genes, Cat1, Cat2, and Cat3.", "entity1": "Cat3", "entity2": "amino acid", "span1": [110, 114], "span2": [19, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13964": {"label": 1, "data": {"text": "However, a glutathione-S-transferase pull-down assay showed reduced binding of R316C with NCoR in the absence of T3 and impaired release in the presence of T3.", "entity1": "R316C", "entity2": "T3", "span1": [79, 84], "span2": [156, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13539": {"label": 1, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha2", "entity2": "ETYA", "span1": [188, 198], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8163": {"label": 3, "data": {"text": "Furthermore, DPEP inhibited the LPS-induced phosphorylation of inhibitor \u03baB (I\u03baB)-\u03b1 and NF-\u03baB p50.", "entity1": "inhibitor \u03baB (I\u03baB)-\u03b1", "entity2": "DPEP", "span1": [63, 83], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2221": {"label": 9, "data": {"text": "Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.", "entity1": "KIT", "entity2": "imatinib", "span1": [32, 35], "span2": [45, 53]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2564": {"label": 2, "data": {"text": "Results showed that neonatal quinpirole treatment induced D2 priming that was eliminated by olanzapine treatment.", "entity1": "D2", "entity2": "quinpirole", "span1": [58, 60], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11044": {"label": 3, "data": {"text": "CONCLUSIONS: Atosiban reduces vasopressin-induced intrauterine pressure in both healthy volunteers and dysmenorrheics, and reported pain in subjects with dysmenorrhea.", "entity1": "vasopressin", "entity2": "Atosiban", "span1": [30, 41], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9098": {"label": 3, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "5-lipoxygenase", "entity2": "6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1", "span1": [194, 208], "span2": [56, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13018": {"label": 8, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "PLC-beta", "entity2": "IP3", "span1": [187, 195], "span2": [179, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5783": {"label": 3, "data": {"text": "Inhibition of binding of both plasminogen and plasmin to gp330 by benzamidine was similar, although EACA inhibited the binding of plasmin to gp330 slightly more than the binding of plasminogen to gp330.", "entity1": "plasmin", "entity2": "EACA", "span1": [130, 137], "span2": [100, 104]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10037": {"label": 2, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "acyl-coenzyme A (CoA) oxidase", "entity2": "Fenofibrate", "span1": [45, 74], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12511": {"label": 3, "data": {"text": "Monoclonal antibody 25B1 appears to be directed against a conformational epitope located in close proximity to the catalytic center of the enzyme and was found to be most suitable for studying the stabilization of the active site of acetylcholinesterase against denaturation by heat or guanidine following phosphorylation by organophosphorus anticholinesterase compounds.", "entity1": "acetylcholinesterase", "entity2": "guanidine", "span1": [233, 253], "span2": [286, 295]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12011": {"label": 1, "data": {"text": "We investigated the diurnal expression of clock genes and clock-controlled genes (CCGs) in 3-hour intervals for a 24-h period in the livers of male streptozotocin (STZ)-treated rats, male spontaneous type 1 diabetic LEW.1AR1-iddm (Iddm) rats, and Iddm rats treated for 10 days with insulin.", "entity1": "clock", "entity2": "streptozotocin", "span1": [42, 47], "span2": [148, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11795": {"label": 3, "data": {"text": "Fisetin treatment showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), NF-kB p65 unit (in pancreas) and IL-1\u03b2 (plasma), serum nitric oxide (NO) with an elevation in plasma insulin.", "entity1": "HbA1c", "entity2": "Fisetin", "span1": [104, 109], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12127": {"label": 8, "data": {"text": "Thymidylate synthase and thymidine kinase are key enzymes involved in the de novo and salvage pathways for pyrimidine nucleotide synthesis, respectively.", "entity1": "thymidine kinase", "entity2": "pyrimidine nucleotide", "span1": [25, 41], "span2": [107, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15220": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "iNOS", "entity2": "clerosterol", "span1": [329, 333], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7430": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "D6D", "entity2": "ALA", "span1": [31, 34], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13631": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "linker domain", "entity2": "C", "span1": [113, 126], "span2": [53, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5245": {"label": 2, "data": {"text": "Exposure of cells to 4mM NaF for 24h induced caspase-3 activation, ultrastructural alterations, and resulted in the translocation of Bax to the mitochondria and the release of cytochrome c from the mitochondrial inter-membrane space into the cytosol, indicating that fluoride-mediated apoptosis is mitochondria-dependent.", "entity1": "caspase-3", "entity2": "NaF", "span1": [45, 54], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1210": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DAT", "entity2": "methylenedioxymethamphetamine", "span1": [165, 168], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5605": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "quetiapine", "span1": [59, 65], "span2": [188, 198]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3112": {"label": 3, "data": {"text": "The potential for ketoconazole, the archetypal strong inhibitor of CYP3A4, to alter the pharmacokinetic profile of ambrisentan and its oxidative metabolite, 4-hydroxymethyl ambrisentan, was assessed in an open-label, nonrandomized, 2-period, single-sequence study in 16 healthy men.", "entity1": "CYP3A4", "entity2": "ketoconazole", "span1": [67, 73], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10480": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "norepinephrine", "span1": [392, 423], "span2": [111, 125]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15623": {"label": 3, "data": {"text": "Our results showed that galangin down-regulates mast cell-derived allergic inflammatory reactions by blocking histamine release and expression of pro-inflammatory cytokines.", "entity1": "cytokines", "entity2": "galangin", "span1": [163, 172], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"736": {"label": 7, "data": {"text": "Angiotensin-converting enzyme inhibition and AT1 receptor blockade modify the pressure-natriuresis relationship by additive mechanisms in rats with human renin and angiotensinogen genes.", "entity1": "human renin", "entity2": "Angiotensin", "span1": [148, 159], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2775": {"label": 2, "data": {"text": "In conclusion, immortalized SHR and WKY PTE cells take up l-alanine mainly through a high-affinity Na(+)-dependent amino acid transporter, with functional features of ASCT2 transport.", "entity1": "ASCT2", "entity2": "amino acid", "span1": [167, 172], "span2": [115, 125]}, "weak_labels": [0, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5280": {"label": 2, "data": {"text": "Further, TCDD exposure could induce phosphorylation- and ubiquitination-dependent degradation of I\u043aB\u03b1, and the translocation of NF-\u03baB p65 from the cytosol to the nucleus in this microglial cell line.", "entity1": "I\u043aB\u03b1", "entity2": "TCDD", "span1": [97, 101], "span2": [9, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9763": {"label": 5, "data": {"text": "In vivo, agonist actions of yohimbine at 5-HT(1A) sites are revealed by WAY100,635-reversible induction of hypothermia in the rat.", "entity1": "5-HT(1A)", "entity2": "WAY100,635", "span1": [41, 49], "span2": [72, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13362": {"label": 3, "data": {"text": "The expression of ER-alpha and PR isoform A in virgin mice was surprisingly much higher in BALB/c than in C57BL/6 mammary glands, and both receptors were downregulated in progestin-treated BALB/c mice (P < 0.05).", "entity1": "PR isoform A", "entity2": "progestin", "span1": [31, 43], "span2": [171, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1870": {"label": 3, "data": {"text": "The flavonoids inhibited DGAT activity in a dose-dependent manner with IC50 values of 10.9 microM ( 1), 9.8 microM ( 2), 8.6 microM ( 3), 142.0 microM ( 4) and 250 microM ( 5).", "entity1": "DGAT", "entity2": "flavonoids", "span1": [25, 29], "span2": [4, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1038": {"label": 3, "data": {"text": "Pranlukast is a new, orally active, selective inhibitor of CysLt1 leukotriene receptor.", "entity1": "leukotriene receptor", "entity2": "Pranlukast", "span1": [66, 86], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2695": {"label": 1, "data": {"text": "In PDE4B wild-type mice, rolipram dose-dependently suppressed CAR (ED(50) = 2.4 mg/kg); however, in knockout mice, their sensitivity to rolipram at the higher doses (1.0 and 3.2 mg/kg) was reduced, resulting in a threefold shift in the ED(50) (7.3 mg/kg), suggesting PDE4B is involved, at least in part, with the activity of rolipram.", "entity1": "PDE4B", "entity2": "rolipram", "span1": [267, 272], "span2": [325, 333]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2292": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "SC-51089", "span1": [74, 77], "span2": [221, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"840": {"label": 3, "data": {"text": "Felbamate produced a rapid, concentration-dependent block of currents evoked by 50 microM NMDA and 10 microM glycine in human embryonic kidney 293 cells expressing the rat NR1a subunit, and either the NR2A, NR2B or NR2C subunits; the IC50 values for block were 2.6, 0.52 and 2.4 mM, respectively (holding potential, - 60 mV).", "entity1": "NR2C", "entity2": "Felbamate", "span1": [215, 219], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4710": {"label": 9, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Dkks", "entity2": "TCDD", "span1": [589, 593], "span2": [655, 659]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14810": {"label": 4, "data": {"text": "Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist \u0394(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054.", "entity1": "CB(1)", "entity2": "\u0394(9)-tetrahydrocannabinol", "span1": [151, 156], "span2": [165, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6429": {"label": 2, "data": {"text": "Creatine phosphokinase activity in plasma increased slightly (compared to control, pyridostigmine or exercise group) in mice treated with pyridostigmine plus exercise, which may be indicative of perturbation in the integrity of the skeletal muscle due to combination.", "entity1": "Creatine phosphokinase", "entity2": "pyridostigmine", "span1": [0, 22], "span2": [138, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13135": {"label": 2, "data": {"text": "CONCLUSION(S): Short-term exposure of mifepristone in new starters of DMPA increases the expression of endometrial ERalpha, PRAB, PRB, and SRC-1 and promotes cell proliferation.", "entity1": "SRC-1", "entity2": "mifepristone", "span1": [139, 144], "span2": [38, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11592": {"label": 8, "data": {"text": "These results suggest that the pro-inflammatory effect of H(2)S may be mediated by SP-NK-1R related pathway in mouse pancreatic acinar cells.", "entity1": "SP", "entity2": "H(2)S", "span1": [83, 85], "span2": [58, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9057": {"label": 1, "data": {"text": "In vitro binding affinities of chlorpromazine, fluphenazine, levomepromazine, perphenazine and some of their metabolites for dopamine D2 receptors, alpha 1- and alpha 2 adrenoceptors in rat brain were previously reported from our laboratories.", "entity1": "dopamine D2 receptors", "entity2": "perphenazine", "span1": [125, 146], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5745": {"label": 1, "data": {"text": "SB225002 (SB) is an IL-8 receptor B (IL-8RB) antagonist that has previously been shown to inhibit IL-8-based cancer cell invasion, and to possess in vivo anti-inflammatory and anti-nociceptive effects.", "entity1": "IL-8", "entity2": "SB225002", "span1": [98, 102], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12116": {"label": 9, "data": {"text": "Disodium cromoglycate affected neither the rightward shift of beta 2-adrenoceptor-mediated responses nor the small rightward shift in beta 1-adrenoceptor-mediated exercise tachycardia after 2 weeks' administration of terbutaline.", "entity1": "beta 2-adrenoceptor", "entity2": "Disodium cromoglycate", "span1": [62, 81], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8998": {"label": 4, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "N6-(R-phenylisopropyl)adenosine", "span1": [0, 9], "span2": [20, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5843": {"label": 9, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT3", "entity2": "granisetron", "span1": [5, 10], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15965": {"label": 0, "data": {"text": "NMR spectroscopy was also used to examine the hSOD1 mutants C57A, C146A, and C57A/C146A, which are unable to form the structurally conserved disulfide bond in SOD1, in order to investigate the role of these cysteines during hSOD1 copper acquisition.", "entity1": "hSOD1", "entity2": "cysteines", "span1": [224, 229], "span2": [207, 216]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5173": {"label": 2, "data": {"text": "In PFC, DEX caused activation of AKT, augmentation of pro-survival Bcl-2 protein and enhanced Bcl-2/Bax protein ratio, as well Bcl-2 translocation to mitochondria.", "entity1": "AKT", "entity2": "DEX", "span1": [33, 36], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"778": {"label": 3, "data": {"text": "We conclude that DeltaKPQ interacts differently with flecainide than with WT, leading to increased block and slowed recovery, especially for late I(Na).", "entity1": "DeltaKPQ", "entity2": "flecainide", "span1": [17, 25], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"614": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "IL-2", "entity2": "AACOCF3", "span1": [193, 197], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3640": {"label": 1, "data": {"text": "In the resveratrol+As(2)O(3) group, activities of superoxide dismutase, catalase in serum and GSH/GSSG were significantly increased, histopathological effects were reduced, and arsenic accumulation markedly decreased in the liver, compared with the As(2)O(3)-treated group.", "entity1": "superoxide dismutase", "entity2": "resveratrol", "span1": [50, 70], "span2": [7, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5259": {"label": 3, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [201, 206], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11391": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "ISDN", "span1": [143, 148], "span2": [102, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15506": {"label": 0, "data": {"text": "We found that, both in a cell-free system and in cells, NO/SNO donors such as S-nitrosocysteine and S-nitrosoglutathione readily induced the S-nitrosylation of Prx1, causing structural and functional alterations.", "entity1": "Prx1", "entity2": "S", "span1": [160, 164], "span2": [141, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"569": {"label": 8, "data": {"text": "These and other data have generated a working hypothesis that activation of the terminal serotonin autoreceptor enhances the kinetics of 5-HT uptake through an effect on the serotonin transporter.", "entity1": "serotonin autoreceptor", "entity2": "5-HT", "span1": [89, 111], "span2": [137, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8720": {"label": 3, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "Txnrd1", "entity2": "Na2SeO3", "span1": [38, 44], "span2": [99, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"924": {"label": 5, "data": {"text": "Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists.", "entity1": "beta(1)-adrenoceptor", "entity2": "Betaxolol", "span1": [13, 33], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9479": {"label": 5, "data": {"text": "16,16-dimethyl-PGE2 and two putative EP1 antagonists, AH6809 and SC-19220, did not show any significant binding to this receptor.", "entity1": "EP1", "entity2": "SC-19220", "span1": [37, 40], "span2": [65, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16002": {"label": 2, "data": {"text": "Moreover, we also demonstrate that puerarin functions at least partially through activation of MEK/ERK and PI3K/Akt signaling.", "entity1": "ERK", "entity2": "puerarin", "span1": [99, 102], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14519": {"label": 2, "data": {"text": "Moreover, 5-ASA treatment restored membranous expression of adhesion molecules E-cadherin and \u03b2-catenin.", "entity1": "\u03b2-catenin", "entity2": "5-ASA", "span1": [94, 103], "span2": [10, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10814": {"label": 3, "data": {"text": "As expected, comparison of IC50 indicated that meloxicam and carprofen are more selective inhibitors of COX-2 than phenylbutazone and flunixin; meloxicam was the most advantageous for horses of four NSAIDs examined.", "entity1": "COX-2", "entity2": "flunixin", "span1": [104, 109], "span2": [134, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15695": {"label": 1, "data": {"text": "Conclusion The results of this work contribute information regarding the antinociceptive properties of CAT on acute pain and show that, at least in part, TRPV1, TRPM8, ASIC, glutamate receptors, PKC and PKA participate in CAT's antinociceptive mechanism.", "entity1": "PKC", "entity2": "CAT", "span1": [195, 198], "span2": [222, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"288": {"label": 0, "data": {"text": "The two NH2-terminal truncated vectors deleted, respectively, 1) the 29-amino acid putative targeting sequence and 2) 51 amino acids, yielding a protein equivalent to a carbonic anhydrase (CA) V isolated from mouse liver mitochondria; and both vectors produced homogeneous protein fractions.", "entity1": "carbonic anhydrase (CA) V", "entity2": "amino acids", "span1": [169, 194], "span2": [121, 132]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4169": {"label": 1, "data": {"text": "Whereas, the levels of both the basal and sulforaphane-inducible expression of AKR1C1 were significantly reduced in NRF2-silenced stable U937 cells compared to the control cells.", "entity1": "NRF2", "entity2": "sulforaphane", "span1": [116, 120], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6580": {"label": 8, "data": {"text": "The bacterial enzyme maltodextrin phosphorylase (MalP) catalyses the phosphorolysis of an alpha-1,4-glycosidic bond in maltodextrins, removing the non-reducing glucosyl residues of linear oligosaccharides as glucose-1-phosphate (Glc1P).", "entity1": "MalP", "entity2": "Glc1P", "span1": [49, 53], "span2": [229, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5566": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase 1 (DDAH1) is an enzyme that metabolizes methylated arginine to citrulline and methylamine, thus working to produce nitric oxide (NO).", "entity1": "Dimethylarginine dimethylaminohydrolase 1", "entity2": "methylated arginine", "span1": [0, 41], "span2": [80, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6993": {"label": 8, "data": {"text": "Valproic acid selectively inhibits conversion of arachidonic acid to arachidonoyl-CoA by brain microsomal long-chain fatty acyl-CoA synthetases: relevance to bipolar disorder.", "entity1": "brain microsomal long-chain fatty acyl-CoA synthetases", "entity2": "arachidonic acid", "span1": [89, 143], "span2": [49, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"11962": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "pip5k1\u03b2", "entity2": "phosphatidylinositol-4,5-bisphosphate", "span1": [68, 75], "span2": [213, 250]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15341": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "2-naphththalene propargyl ether", "span1": [39, 48], "span2": [150, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"809": {"label": 1, "data": {"text": "The modulation of high-voltage-activated (HVA) Ca2+ channels by the prostaglandin E series (PGE1 and PGE2) was studied in the paratracheal ganglion cells.", "entity1": "high-voltage-activated (HVA) Ca2+ channels", "entity2": "prostaglandin E", "span1": [18, 60], "span2": [68, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3055": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "stromal cell-derived factor-1", "entity2": "AMD3100", "span1": [111, 140], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13067": {"label": 2, "data": {"text": "It was, therefore, proposed that H. pylori may in fact, antagonize, aspirin-induced delay of ulcer healing due to suppression of acid secretion by the enhancement in PGE(2) possibly derived from COX-2 expression and activity and to the overexpression of growth factors such as TGF alpha and VEGF.", "entity1": "TGF alpha", "entity2": "aspirin", "span1": [277, 286], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4301": {"label": 8, "data": {"text": "Transport by OATP1B1 and OATP1B3 enhances the cytotoxicity of epigallocatechin 3-O-gallate and several quercetin derivatives.", "entity1": "OATP1B3", "entity2": "quercetin", "span1": [25, 32], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1840": {"label": 3, "data": {"text": "Here, we show that one BLT, [1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea] (BLT-4), blocked ABCA1-mediated cholesterol efflux to lipid-poor apoA-I at a potency similar to that for its inhibition of SR-BI (IC(50) approximately 55-60 microM).", "entity1": "ABCA1", "entity2": "BLT", "span1": [91, 96], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4358": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NAD(P)H:quinone oxidoreductase-1", "entity2": "\u03b2-Lap", "span1": [115, 147], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14607": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Pro122Ser", "entity2": "Ara-C", "span1": [96, 105], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13775": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "c-KIT", "entity2": "NS-187", "span1": [309, 314], "span2": [288, 294]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3613": {"label": 3, "data": {"text": "Also, SB365 showed anti-angiogenic activity by decreasing the expression of HIF-1\u03b1 and VEGF.", "entity1": "HIF-1\u03b1", "entity2": "SB365", "span1": [76, 82], "span2": [6, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10244": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "SSAT", "entity2": "polyamine", "span1": [121, 125], "span2": [7, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15430": {"label": 3, "data": {"text": "Cell-pre-incubation with bradykinin induced changes in ABCG expression levels after 7-ketostigmasterol-incubation; however, the energetic metabolism inhibition reduced NPC1L1 expression only in 7-ketocholesterol-incubated cells.", "entity1": "NPC1L1", "entity2": "7-ketocholesterol", "span1": [168, 174], "span2": [194, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11030": {"label": 3, "data": {"text": "Sorafenib, which belongs chemically to a class that can be described as bis-aryl ureas, was selected for further pharmacologic characterization based on potent inhibition of Raf-1 and its favorable kinase selectivity profile.", "entity1": "kinase", "entity2": "Sorafenib", "span1": [198, 204], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7345": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT2", "entity2": "alanine", "span1": [247, 252], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13476": {"label": 1, "data": {"text": "In contrast, GLP-1 exerts glucoregulatory actions via slowing of gastric emptying and glucose-dependent inhibition of glucagon secretion.", "entity1": "GLP-1", "entity2": "glucose", "span1": [13, 18], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"480": {"label": 0, "data": {"text": "Despite a low amino acid identity between TWIK-1 and TREK-1 (approximately 28%), both channel proteins share the same overall structural arrangement consisting of two pore-forming domains and four transmembrane segments (TMS).", "entity1": "TREK-1", "entity2": "amino acid", "span1": [53, 59], "span2": [14, 24]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13559": {"label": 8, "data": {"text": "Our optimized L-citrulline production assay to measure DDAH activity correlated closely with the direct measure of the rate of asymmetric dimethylarginine consumption.", "entity1": "DDAH", "entity2": "L-citrulline", "span1": [55, 59], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14037": {"label": 2, "data": {"text": "Mercury induces the expression of cyclooxygenase-2 and inducible nitric oxide synthase.", "entity1": "inducible nitric oxide synthase", "entity2": "Mercury", "span1": [55, 86], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6070": {"label": 0, "data": {"text": "Degenerate oligonucleotides corresponding to conserved amino acids from transmembrane domains III, V, and VI of known receptors [5-HT1A, 5-HT1C, and 5-HT2; 5-HT is serotonin (5-hydroxytryptamine)] were used as primers for the sequential reactions.", "entity1": "5-HT1A", "entity2": "amino acids", "span1": [129, 135], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8817": {"label": 3, "data": {"text": "Interestingly, SB203580, a selective inhibitor of p38 MAPK, blocked STIM1 phosphorylation and led to sustained STIM1-puncta formation and Ca2+ entry.", "entity1": "p38", "entity2": "SB203580", "span1": [50, 53], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5857": {"label": 5, "data": {"text": "A number of selective 5-HT3 antagonists have been developed including ondansetron, granisetron, tropisetron renzapride and zacopride.", "entity1": "5-HT3", "entity2": "ondansetron", "span1": [22, 27], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2481": {"label": 1, "data": {"text": "CP-690550, a JAK3 inhibitor is currently in phase II clinical trials.FK778, is a synthetic malononitrilamide that targets the critical enzyme of the de novo pyrimidine synthesis, dihydroorotic acid dehydrogenase, and receptor-associated tyrosine kinases has completed phase II trials.", "entity1": "dihydroorotic acid dehydrogenase", "entity2": "malononitrilamide", "span1": [179, 211], "span2": [91, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6028": {"label": 2, "data": {"text": "Anorexia induced by (+)-amphetamine, phentermine, diethylpropion and phenylpropanolamine seems to be the result of their ability to increase the release of noradrenaline and/or dopamine from nerve terminals and inhibit their reuptake or, in the case of phenylpropanolamine, to stimulate directly alpha 1-adrenoceptors.", "entity1": "alpha 1-adrenoceptors", "entity2": "phenylpropanolamine", "span1": [296, 317], "span2": [253, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7665": {"label": 1, "data": {"text": "Examining the four X-ray crystal structures of their CA II adducts, we observed several (2-3) active site water molecules interacting with the chlorthalidone, trichloromethiazide, and furosemide scaffolds which may be responsible for this important difference of activity.", "entity1": "CA II", "entity2": "furosemide", "span1": [53, 58], "span2": [184, 194]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11491": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "cyclooxygenase", "entity2": "ketorolac tromethamine", "span1": [26, 40], "span2": [139, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5817": {"label": 9, "data": {"text": "Loperamide has no significant effect on insulin-hypoglycemia-induced ACTH and cortisol levels and, therefore, no effect on stress-induced elevation of cortisol levels.", "entity1": "insulin", "entity2": "Loperamide", "span1": [40, 47], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12335": {"label": 8, "data": {"text": "Contributions of rat Ctr1 to the uptake and toxicity of copper and platinum anticancer drugs in dorsal root ganglion neurons.", "entity1": "rat Ctr1", "entity2": "copper", "span1": [17, 25], "span2": [56, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9215": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "alpha 2-macroglobulin", "entity2": "TFP", "span1": [209, 230], "span2": [159, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16041": {"label": 3, "data": {"text": "Rats intoxicated with Cd for 30 days, significantly increased tissue malondialdehyde (MDA) levels and significantly decreased enzymatic antioxidants superoxide dismutase, glutathione peroxidase and catalase in the frontal cortex tissue.", "entity1": "superoxide dismutase", "entity2": "Cd", "span1": [149, 169], "span2": [22, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"790": {"label": 1, "data": {"text": "Analysis of splice variants and site-directed mutants of the AMPA receptor GluR3 expressed in Xenopus oocytes has shown that lithium produces a large potentiation of the GluR3 flop splice variant and suggested that lithium might inhibit rapid desensitization, which is characteristic of this receptor (Karkanias, N. and Papke, R., Subtype-specific effects of lithium on glutamate receptor function.", "entity1": "GluR3", "entity2": "AMPA", "span1": [75, 80], "span2": [61, 65]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4933": {"label": 1, "data": {"text": "In the present study, we aimed at examining the effect of 1-ethyl-5-methyl-2-phenyl-1H-benzo[d]imidazole, a synthetic small molecular compound also named Fc11a-2, for the treatment of dextran sulfate sodium (DSS)-induced experimental colitis in mice via targeting NLRP3 inflammasome.", "entity1": "NLRP3", "entity2": "1-ethyl-5-methyl-2-phenyl-1H-benzo[d]imidazole", "span1": [264, 269], "span2": [58, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7677": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "CA", "entity2": "methazolamide", "span1": [113, 115], "span2": [219, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15796": {"label": 8, "data": {"text": "Consistent with two glucose uptake pathways, induced uptake of 2-NBDG, a fluorescent glucose derivative, was decreased by inhibition of HCs or glucose transporter (GLUT4), and blocked by dual blockade.", "entity1": "GLUT4", "entity2": "2-NBDG", "span1": [164, 169], "span2": [63, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14011": {"label": 3, "data": {"text": "Treatment with cabozantinib inhibited MET and VEGFR2 phosphorylation in vitro and in tumor models in vivo and led to significant reductions in cell invasion in vitro.", "entity1": "MET", "entity2": "cabozantinib", "span1": [38, 41], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13305": {"label": 3, "data": {"text": "RESULTS: We show that sorafenib is a potent inhibitor of ETV6-PDGFRbeta and FLT3 mutants, including some of the mutants that confer resistance to PKC412 and other FLT3 inhibitors.", "entity1": "PDGFRbeta", "entity2": "sorafenib", "span1": [62, 71], "span2": [22, 31]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4500": {"label": 9, "data": {"text": "Lastly, both hCES1 and hCES2 were shown not to catalyze the hydrolysis of the acyl glucuronides studied.", "entity1": "hCES1", "entity2": "acyl glucuronides", "span1": [13, 18], "span2": [78, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"13617": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "mTOR", "entity2": "temsirolimus", "span1": [248, 252], "span2": [229, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13533": {"label": 7, "data": {"text": "Mammalian cysteine dioxygenase (CDO) is a non-heme iron metalloenzyme that catalyzes the first committed step in oxidative cysteine catabolism.", "entity1": "CDO", "entity2": "iron", "span1": [32, 35], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14253": {"label": 1, "data": {"text": "Our results show that PILO converts a transient cortical depression induced by LFS600 into a robust LTD, stable for at least 4 h. When applied after LFS600, PILO does not change either mPFC basal neurotransmission or late LTD. Our data also indicate that NMDA receptor pre-activation is essential to the muscarinic enhancement of mPFC synaptic depression, since AP7 microinjection into the mPFC blocked the conversion of transient depression into long-lasting LTD produced by PILO.", "entity1": "NMDA receptor", "entity2": "PILO", "span1": [255, 268], "span2": [476, 480]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, 9]},
	"4871": {"label": 5, "data": {"text": "Although generally highly specific for angiotensin II type 1 receptors, some ARBs, particularly telmisartan, are partial agonists at peroxisome proliferator-activated receptor-\u03b3.", "entity1": "angiotensin II type 1 receptors", "entity2": "telmisartan", "span1": [39, 70], "span2": [96, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6954": {"label": 1, "data": {"text": "To do this we cloned and expressed CCR5 from rhesus macaque and compared the binding properties of [125I]-MIP-1beta and [3H]-maraviroc with human recombinant CCR5.", "entity1": "human recombinant CCR5", "entity2": "125I", "span1": [140, 162], "span2": [100, 104]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13314": {"label": 1, "data": {"text": "ENaC expression and activity could account for the low Na(+) concentration that is typical of milk.", "entity1": "ENaC", "entity2": "Na(+)", "span1": [0, 4], "span2": [55, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10347": {"label": 9, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK4-8", "entity2": "GW660511X", "span1": [95, 102], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12211": {"label": 1, "data": {"text": "P2Y12 has been shown to be the target of the thienopyridine drugs, ticlopidine and clopidogrel.", "entity1": "P2Y12", "entity2": "clopidogrel", "span1": [0, 5], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5350": {"label": 2, "data": {"text": "S1P activated phosphatidylinositol 3-kinase (PI3K)/Akt signaling, leading to the inhibition of glycogen synthase kinase-3\u03b2 and the nuclear translocation of \u03b2-catenin, followed by the increase of the transcriptional activity by \u03b2-catenin/T-cell factor complex formation in both SaOS-2 cells and MC3T3-E1 cells.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "S1P", "span1": [14, 43], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7025": {"label": 5, "data": {"text": "To mimic chronic selective serotonin reuptake inhibitor treatment and to block the inhibitory 5-HT(1A) autoreceptors, a 5-HT(1A) antagonist, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclo hexanecarboxamide maleate salt (WAY-100635) (0.3 mg/kg s.c.), was administered with DVS (30 mg/kg orally).", "entity1": "5-HT(1A)", "entity2": "WAY-100635", "span1": [120, 128], "span2": [239, 249]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9224": {"label": 3, "data": {"text": "Three lines of evidence suggest that calmodulin inhibition is not responsible for the inhibition of binding and endocytosis: 1) Promethazine, a phenothiazine that is a poor inhibitor of calmodulin, is nearly as effective as TFP at inhibiting endocytosis; calmidazolium, a potent inhibitor of several calmodulin functions, did not cause a loss of binding; 2) the microinjection of calmodulin into cells did not reverse the effects of W-7; using pressure microinjection, we introduced up to a 100-fold excess of calmodulin over native levels into individual gerbil fibroma cells; using rhodamine-labeled alpha 2-macroglobulin, we saw that the W-7 induced inhibition of receptor-mediated endocytosis was the same in injected and uninjected cells; 3) we injected calcineurin, a calmodulin-binding protein, into cells (1-3 pg/cell) and observed no effect on the receptor-mediated endocytosis of rhodamine-labeled alpha 2-macroglobulin.", "entity1": "calmodulin", "entity2": "TFP", "span1": [300, 310], "span2": [224, 227]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11101": {"label": 1, "data": {"text": "The R(-) and S(+) isomers of MDMA were significantly less efficacious at the 5-HT2A receptor as compared to MDA; S(+)MDMA had no effect.", "entity1": "5-HT2A", "entity2": "MDA", "span1": [77, 83], "span2": [108, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10977": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "PKC", "entity2": "PMA", "span1": [53, 56], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13630": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "alpha-helices", "entity2": "C", "span1": [98, 111], "span2": [53, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12433": {"label": 1, "data": {"text": "Genomic variation in the MAP3K5 gene is associated with \u03b2-thalassemia disease severity and hydroxyurea treatment efficacy.", "entity1": "MAP3K5", "entity2": "hydroxyurea", "span1": [25, 31], "span2": [91, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12920": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CBS", "entity2": "Hydrogen sulfide", "span1": [160, 163], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1449": {"label": 9, "data": {"text": "Reserpine-induced ptosis was reversed by rasagiline at doses above 2 mg x kg(-1) i.p., which inhibit MAO-A as well as MAO-B, but not at MAO-B-selective doses.", "entity1": "MAO-B", "entity2": "rasagiline", "span1": [136, 141], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15597": {"label": 3, "data": {"text": "Design, Synthesis, Biological Evaluation, and Docking Studies of (S)-Phenylalanine Derivatives with a 2-Cyanopyrrolidine Moiety as Potent Dipeptidyl Peptidase 4 Inhibitors.", "entity1": "Dipeptidyl Peptidase 4", "entity2": "(S)-Phenylalanine", "span1": [138, 160], "span2": [65, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3178": {"label": 2, "data": {"text": "We investigated the involvement of the farnesoid X receptor (FXR), a nuclear receptor for bile acids, in the chenodeoxycholic acid (CDCA)-induced expression of Cdx2 and MUC2 in normal rat gastric epithelial cells (RGM-1 cells).", "entity1": "MUC2", "entity2": "chenodeoxycholic acid", "span1": [169, 173], "span2": [109, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8122": {"label": 3, "data": {"text": "Both CE and E(2) alone increased DNA synthesis and reduced apoptosis with activation of MAPK, Akt, and p70S6K and up-regulation of antiapoptotic factors survivin, Bcl-2, and X-linked inhibitor of apoptosis protein, These effects could be completely blocked by BZA.", "entity1": "p70S6K", "entity2": "BZA", "span1": [103, 109], "span2": [260, 263]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14737": {"label": 3, "data": {"text": "We hypothesized that hypoxia induced testicular damage is mediated by an activated NADPH oxidase (NOX), therefore, APO (apocynin) an inhibitor of NOX and raisanberine (RS), a calcium influx inhibitor were tested if they could attenuate hypoxic toxicity to the testis.", "entity1": "NOX", "entity2": "apocynin", "span1": [146, 149], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9834": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "extracellular signal regulated kinase (ERK)-2", "entity2": "geldanamycin", "span1": [120, 165], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14972": {"label": 3, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "TRAP", "entity2": "serine", "span1": [196, 200], "span2": [84, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13013": {"label": 3, "data": {"text": "It has been known for decades that lithium chloride (LiCl) leads to D-myo-inositol 1-phosphate accumulation on GPCR activation by inhibiting inositol monophosphatase, the final enzyme of the IP3 metabolic cascade.", "entity1": "inositol monophosphatase", "entity2": "LiCl", "span1": [141, 165], "span2": [53, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4111": {"label": 3, "data": {"text": "To develop new drugs for treatment of Alzheimer's disease, a group of N'-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones was designed, synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase and aggregation of amyloid beta peptides (1-40, 1-42 and 1-40_1-42).", "entity1": "acetylcholinesterase", "entity2": "N'-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones", "span1": [191, 211], "span2": [70, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6937": {"label": 8, "data": {"text": "A double mutant of the two fumarate reductase isozyme genes (OSM1 and FRDS) showed a succinate productivity of 50% as compared to the parent when cells were incubated in glucose-buffered solution.", "entity1": "OSM1", "entity2": "succinate", "span1": [61, 65], "span2": [85, 94]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4803": {"label": 1, "data": {"text": "We identified 13 differentially expressed phosphoproteins that are judged to be relevant in the neuroprotective roles of PTN and MK against amphetamine-induced neurotoxicity.", "entity1": "MK", "entity2": "amphetamine", "span1": [129, 131], "span2": [140, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9679": {"label": 3, "data": {"text": "The antidepressant desipramine has been shown to decrease synaptic membrane concentrations of the norepinephrine re-uptake transporter (NET) in vivo and in vitro, on both an acute and a chronic basis.", "entity1": "NET", "entity2": "desipramine", "span1": [136, 139], "span2": [19, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9432": {"label": 3, "data": {"text": "The hydrolysis of fluorescein diphosphate by PTP epsilon and PTPmeg1 was sensitive to alendronate, with IC50 values of less than 1 microM; PTPsigma, however, under the same conditions, was inhibited by only 50% with 141 microM alendronate.", "entity1": "PTPsigma", "entity2": "alendronate", "span1": [139, 147], "span2": [227, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"20": {"label": 3, "data": {"text": "Prostacyclin analogues inhibit tissue factor expression in the human monocytic cell line THP-1 via a cyclic AMP-dependent mechanism.", "entity1": "tissue factor", "entity2": "Prostacyclin", "span1": [31, 44], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15040": {"label": 1, "data": {"text": "It had higher levels of oleocanthal (p-HPEA-EDA), a nutraceutical compound exerting actions against COX1 and COX2 (cycloxygenases).", "entity1": "COX1", "entity2": "p-HPEA-EDA", "span1": [100, 104], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11203": {"label": 8, "data": {"text": "These results suggest that ACS1 and ACS4 may be linked to triacylglycerol synthesis.", "entity1": "ACS1", "entity2": "triacylglycerol", "span1": [27, 31], "span2": [58, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"404": {"label": 3, "data": {"text": "Indomethacin abolished the inhibitory effect of acetazolamide on CA I and CA II.", "entity1": "CA II", "entity2": "acetazolamide", "span1": [74, 79], "span2": [48, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12739": {"label": 8, "data": {"text": "[(131)I]MIBG uptake in PC12 cells, which express the NET endogenously, was 20- to 28-fold lower than in transduced cells.", "entity1": "NET", "entity2": "[(131)I]MIBG", "span1": [53, 56], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5575": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "CA I", "entity2": "acetazolamide", "span1": [134, 138], "span2": [211, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6652": {"label": 8, "data": {"text": "A comparison of the results with previous data for desipramine and cocaine inhibition of norepinephrine uptake by the mutant hNETs reveals that MrIA binding to hNET occurs at a site that is distinct from but overlaps with the binding sites for tricyclic antidepressants and cocaine.", "entity1": "hNETs", "entity2": "norepinephrine", "span1": [125, 130], "span2": [89, 103]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10440": {"label": 1, "data": {"text": "These characteristics of the bound PLP suggest that SDH catalysis is not facilitated by forming the resonance-stabilized structure of the PLP-Ser aldimine as seen in aminotransferases.", "entity1": "aminotransferases", "entity2": "PLP-Ser aldimine", "span1": [166, 183], "span2": [138, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"3079": {"label": 3, "data": {"text": "RESULTS: Both PLZ and VIG inhibited GABA-T and elevated GABA levels.", "entity1": "GABA-T", "entity2": "VIG", "span1": [36, 42], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8426": {"label": 2, "data": {"text": "Compared with normally-fed counterparts, PM-CP rats exhibited higher glutathione S-transferase, aminopeptidase N and cysteine S-conjugate beta-lyase (CCBL) and lower gamma-glutamyltransferase activities, PM-FU rats exhibited decreased dihydropyrimidine dehydrogenase and cytochrome P450 1A1/2 activities and PM-MMC rats showed higher quinone reductase and depleted xanthine oxidase activities.", "entity1": "quinone reductase", "entity2": "MMC", "span1": [334, 351], "span2": [311, 314]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"521": {"label": 1, "data": {"text": "In a further study to analyse the downstream mediator of Rac in the ceramide-signalling pathway, we observed that either pretreatment with mepacrine, a potent and specific inhibitor of phospholipase A2, or co-transfection with antisense cytosolic phospholipase A2 (cPLA2) oligonucleotide repressed the C2-ceramide-induced SRE activation selectively, implying a critical role of cPLA2 in C2-ceramide-induced signalling to nucleus.", "entity1": "cPLA2", "entity2": "C2-ceramide", "span1": [378, 383], "span2": [387, 398]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1190": {"label": 3, "data": {"text": "The inhibition of aminopeptidase activity in the presence of bestatin and puromycin inhibitors was also investigated.", "entity1": "aminopeptidase", "entity2": "bestatin", "span1": [18, 32], "span2": [61, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14088": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "pomalidomide", "span1": [121, 125], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7417": {"label": 8, "data": {"text": "The parallel pattern of accumulation of 24:6n-3 and DHA in response to increasing concentrations of ALA suggests that the competition between 24:5n-3 and ALA for D6D may contribute to the limited accumulation of DHA in cell membranes.", "entity1": "D6D", "entity2": "DHA", "span1": [162, 165], "span2": [212, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10792": {"label": 2, "data": {"text": "The IL-18 production is located upstream of the cytokine cascade activated by simvastatin.", "entity1": "IL-18", "entity2": "simvastatin", "span1": [4, 9], "span2": [78, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7948": {"label": 2, "data": {"text": "Moreover, activation of the ERK and CREB signaling pathway in the hippocampus might be involved in METH-induced spatial memory changes.", "entity1": "ERK", "entity2": "METH", "span1": [28, 31], "span2": [99, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9757": {"label": 5, "data": {"text": "However, in contrast to the selective alpha(2)-AR antagonist, fluparoxan, the 5-HT(1A) agonist actions of yohimbine suppress 5-HT levels alone and underlie its inability to augment the influence of fluoxetine upon 5-HT levels.", "entity1": "alpha(2)-AR", "entity2": "fluparoxan", "span1": [38, 49], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3773": {"label": 1, "data": {"text": "Opioid receptor binding affinity and activity were assessed using [(3)H]-diprenorphine binding, guanosine-5'-O-(3-[35S]-thio) triphosphate ([(35)S]-GTP\u03b3S) binding and isolated guinea-pig ileum.", "entity1": "Opioid receptor", "entity2": "[(3)H]-diprenorphine", "span1": [0, 15], "span2": [66, 86]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1519": {"label": 9, "data": {"text": "Neither okadaic acid nor cantharidin (1-10000 nM) displaced [3H]naloxone from its specific binding sites, which indicates that they do not interact at the opioid receptor level.", "entity1": "opioid receptor", "entity2": "okadaic acid", "span1": [155, 170], "span2": [8, 20]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3887": {"label": 0, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "Myc", "entity2": "arginine", "span1": [60, 63], "span2": [233, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7880": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "BSEP", "entity2": "LPV", "span1": [84, 88], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8138": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "glutathione reductase", "entity2": "Isoproterenol", "span1": [271, 292], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6750": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "c-Kit", "entity2": "Gleevec", "span1": [208, 213], "span2": [107, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1831": {"label": 3, "data": {"text": "Here, we show that one BLT, [1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea] (BLT-4), blocked ABCA1-mediated cholesterol efflux to lipid-poor apoA-I at a potency similar to that for its inhibition of SR-BI (IC(50) approximately 55-60 microM).", "entity1": "SR-BI", "entity2": "BLT-4", "span1": [197, 202], "span2": [75, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13472": {"label": 8, "data": {"text": "Acetyl-coenzyme A carboxylase (ACC) enzymes exist as two isoforms, ACC1 and ACC2, which play critical roles in fatty acid biosynthesis and oxidation.", "entity1": "ACC2", "entity2": "fatty acid", "span1": [76, 80], "span2": [111, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13082": {"label": 1, "data": {"text": "This dual mode of action of sulfonylureas and glinides may open new perspectives for the molecular pharmacology of antidiabetic drugs, because it provides evidence that drugs can be designed that target both the sulfonylurea receptor and PPARgamma.", "entity1": "PPARgamma", "entity2": "sulfonylureas", "span1": [238, 247], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3156": {"label": 3, "data": {"text": "INTRODUCTION: In this study, we examined the effects of the alpha-glucosidase inhibitors acarbose and voglibose on postprandial plasma glucose and serum triglyceride levels in patients with type 2 diabetes mellitus.", "entity1": "alpha-glucosidase", "entity2": "acarbose", "span1": [60, 77], "span2": [89, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2738": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "ABL", "entity2": "Dasatinib", "span1": [99, 102], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9923": {"label": 1, "data": {"text": "By using the technique of site-directed spin labeling combined with EPR spectroscopy, we have observed that binding of arachidonic acid and nonsteroidal anti-inflammatory drugs induces conformational changes in the human prostaglandin endoperoxide H(2) synthase enzyme (PGHS-2).", "entity1": "PGHS-2", "entity2": "arachidonic acid", "span1": [270, 276], "span2": [119, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1926": {"label": 8, "data": {"text": "In the reverse case, mutation of the orthologous glycine (Gly553) to methionine in carnitine octanoyltransferase (COT) decreased activity toward its natural substrates, medium- and long-chain acyl-CoAs, and increased activity toward short-chain acyl-CoAs.", "entity1": "COT", "entity2": "acyl-CoAs", "span1": [114, 117], "span2": [245, 254]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10447": {"label": 7, "data": {"text": "The holo-SDH contained PLP-OMS aldimine in the active site, indicating that OMS can form the Schiff base linkage with PLP, but the subsequent dehydration did not occur.", "entity1": "holo-SDH", "entity2": "PLP", "span1": [4, 12], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15178": {"label": 3, "data": {"text": "GnRH stimulation of CREB phosphorylation (pCREB) in the gonadotrope-derived L\u03b2T2 cell line was attenuated by a protein kinase A (PKA) inhibitor, H89.", "entity1": "PKA", "entity2": "H89", "span1": [129, 132], "span2": [145, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5434": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "CA", "entity2": "benzenesulfonamides", "span1": [149, 151], "span2": [12, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14230": {"label": 5, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b2", "entity2": "4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol", "span1": [420, 423], "span2": [442, 514]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3918": {"label": 3, "data": {"text": "N-alkylation of the pyridazinone ring markedly enhances potency against PDE4 but suppresses PDE3 inhibition.", "entity1": "PDE3", "entity2": "N", "span1": [92, 96], "span2": [0, 1]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"555": {"label": 3, "data": {"text": "Both the 5 alpha-reductase inhibitor finasteride and alpha 1-adrenoceptor antagonists (e.g.", "entity1": "5 alpha-reductase", "entity2": "finasteride", "span1": [9, 26], "span2": [37, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8243": {"label": 0, "data": {"text": "Elimination of Ser26 phosphorylation promotes BAD proapoptotic activity, thereby accelerating TNF\u03b1-induced apoptosis in cultured cells and increasing mortality in animals.", "entity1": "BAD", "entity2": "Ser", "span1": [46, 49], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15777": {"label": 1, "data": {"text": "A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone.", "entity1": "OSC", "entity2": "aminopropylindenes", "span1": [123, 126], "span2": [12, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2140": {"label": 1, "data": {"text": "Although incubating HASMCs for 48h with thiazolidinediones had no effect on ENT1 mRNA and protein levels, troglitazone acutely inhibited [3H]adenosine uptake and [3H]NBMPR binding of HASMCs with IC50 values of 2.35+/-0.35 and 3.99+/-0.57microM, respectively.", "entity1": "ENT1", "entity2": "[3H]adenosine", "span1": [76, 80], "span2": [137, 150]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12000": {"label": 1, "data": {"text": "In the current study, SHR, Wistar-Kyoto (WKY) and Wistar (WIS) rats received a therapeutically relevant dose of methylphenidate (1.5mg/kg, p.o.) or vehicle during adolescence and then OFC and mPFC DAT function and cellular expression were assessed during adulthood.", "entity1": "DAT", "entity2": "methylphenidate", "span1": [197, 200], "span2": [112, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15958": {"label": 1, "data": {"text": "OHT-induced cyclin E truncation also occurred in SK-BR-3 cells that express GPR30 and lack ER\u03b1, but not in MDA-MB-231 cells that express neither GPR30 nor ER\u03b1.", "entity1": "GPR30", "entity2": "OHT", "span1": [76, 81], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8298": {"label": 3, "data": {"text": "The pharmacological inhibitors SB203580 (p38 inhibitor) and SP600125 (a JNK inhibitor) protected primary cultures of rat CGCs from LY294002-induced apoptosis.", "entity1": "p38", "entity2": "SB203580", "span1": [41, 44], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1018": {"label": 1, "data": {"text": "In COS cells transfected with alpha(1b) adrenoceptor cDNA and in DDT(1) MF-2 cells which express native alpha(1B) adrenoceptors, [(3)H]-prazosin was displaced by unlabelled prazosin in a normal equilibrium process, with no prazosin paradox in concentrations up to 10(-6) M. In DDT(1) MF-2 cells, [(3)H]-prazosin was displaced likewise by a series of alpha(1) adrenergic agonists, none of which increased the binding of [(3)H]-prazosin.", "entity1": "alpha(1b) adrenoceptor", "entity2": "prazosin", "span1": [30, 52], "span2": [173, 181]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1467": {"label": 8, "data": {"text": "Interestingly, the allele of PRO1 was shown to enhance the activities of gamma-glutamyl kinase and gamma-glutamyl phosphate reductase, both of which catalyze the first two steps of L-proline synthesis from L-glutamate and which together may form a complex in vivo.", "entity1": "gamma-glutamyl kinase", "entity2": "L-proline", "span1": [73, 94], "span2": [181, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6095": {"label": 5, "data": {"text": "However, amantadine induction of Fos in the striatum was unaffected by the dopamine D2 receptor antagonist, sulpiride.", "entity1": "dopamine D2 receptor", "entity2": "sulpiride", "span1": [75, 95], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9588": {"label": 4, "data": {"text": "These results indicate that carbetocin is a partial agonist/antagonist to the oxytocin receptor while the two metabolites carbetocin metabolite I and carbetocin metabolite II are pure antagonists.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [78, 95], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15207": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "inducible nitric oxide synthase", "entity2": "ethylacetate", "span1": [296, 327], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13388": {"label": 3, "data": {"text": "Structural basis of inhibition of the human NAD+-dependent deacetylase SIRT5 by suramin.", "entity1": "human NAD+-dependent deacetylase SIRT5", "entity2": "suramin", "span1": [38, 76], "span2": [80, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15849": {"label": 2, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "ABCG1", "entity2": "TO901317", "span1": [28, 33], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"866": {"label": 3, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ODC", "entity2": "DFMO", "span1": [143, 146], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8170": {"label": 1, "data": {"text": "In contrast to wild-type pol \u03b2, the ternary complex of the R283K mutant with an incoming dATP-analogue and templating 8-oxoG resembles a G-A mismatched structure with 8-oxoG adopting an anti-conformation.", "entity1": "R283K", "entity2": "dATP", "span1": [59, 64], "span2": [89, 93]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15435": {"label": 9, "data": {"text": "When mice were treated ip with the major neonicotinoid imidacloprid (IMI), metabolism by CYP oxidation reactions was not appreciably affected, whereas the AOX-generated nitrosoguanidine metabolite was decreased by 30% with tungsten and 56% with hydralazine and 86% in the AOX-deficient mice.", "entity1": "CYP", "entity2": "imidacloprid", "span1": [89, 92], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13008": {"label": 1, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "G protein-coupled receptor", "entity2": "D-myo-inositol 1,4,5-trisphosphate", "span1": [40, 66], "span2": [143, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3897": {"label": 2, "data": {"text": "Ozone plus PM(2.5) exposure, however, induced CRP, IL-6, CK, LDH and MDA increase, SOD and HRV decrease significantly in a dose-response way.", "entity1": "CRP", "entity2": "Ozone", "span1": [46, 49], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15118": {"label": 2, "data": {"text": "Mn exposure (20\u00a0mg/kg) increased p38(MAPK) and Akt phosphorylation, but decreased DARPP-32-Thr-34 phosphorylation.", "entity1": "MAPK", "entity2": "Mn", "span1": [37, 41], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6459": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "dihydrofolate reductase", "entity2": "Pemetrexed disodium", "span1": [112, 135], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"550": {"label": 8, "data": {"text": "N-Acetylglucosamine-1-phosphodiester alpha-N-Acetylglucosaminidase (EC 3.1.4.45; phosphodiester alpha-GlcNAcase) catalyzes the second step in the synthesis of the mannose 6-phosphate determinant required for efficient intracellular targeting of newly synthesized lysosomal hydrolases to the lysosome.", "entity1": "N-Acetylglucosamine-1-phosphodiester alpha-N-Acetylglucosaminidase", "entity2": "mannose 6-phosphate", "span1": [0, 66], "span2": [163, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8242": {"label": 0, "data": {"text": "IKK phosphorylates BAD at serine-26 (Ser26) and primes it for inactivation.", "entity1": "BAD", "entity2": "Ser", "span1": [19, 22], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7687": {"label": 3, "data": {"text": "In this report, we examined the antihyperglycemic effects of sergliflozin etabonate in normal and diabetic rats in comparison with those of a sulfonylurea (gliclazide) and an alpha-glucosidase inhibitor (voglibose).", "entity1": "alpha-glucosidase", "entity2": "voglibose", "span1": [175, 192], "span2": [204, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6460": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "glycinamide ribonucleotide formyl transferase", "entity2": "Pemetrexed disodium", "span1": [141, 186], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4676": {"label": 1, "data": {"text": "Using cultured human keratinocytes and diabetic rat model, the current study showed that high-glucose environment enhanced IL-8 production via epidermal growth factor receptor (EGFR) -extracelluar signal-regulated kinase (ERK) pathway in a reactive oxygen species (ROS)-dependent manner in keratinocytes.", "entity1": "epidermal growth factor receptor", "entity2": "glucose", "span1": [143, 175], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4183": {"label": 2, "data": {"text": "The treatment of U937 cells with NRF2 inducers including sulforaphane effectively elevated the expression of AKR1B1, 1B10, 1C1, 1C2, and 1C3.", "entity1": "AKR1B1, 1B10, 1C1, 1C2, and 1C3", "entity2": "sulforaphane", "span1": [109, 140], "span2": [57, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9872": {"label": 3, "data": {"text": "CONCLUSION/INTERPRETATION: This study provides evidence that troglitazone reduces PAI-1 production in human adipocytes, probably at the transcriptional level.", "entity1": "PAI-1", "entity2": "troglitazone", "span1": [82, 87], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15558": {"label": 1, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "GDNF", "entity2": "MPTP", "span1": [125, 129], "span2": [62, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14567": {"label": 2, "data": {"text": "Thus, our findings indicate that the expression of Brms1L depends on \u03b2-catenin activity and contributes to FSH\u03b2 induction by GnRH.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [107, 111], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15890": {"label": 8, "data": {"text": "Targeted disruption of the gene encoding the N-glycosyltransferase, prlH, abolished pyralomicin production, and recombinant expression of PrlA confirms the activity of this enzyme as a sugar phosphate cyclase involved in the formation of the C7-cyclitol moiety.", "entity1": "sugar phosphate cyclase", "entity2": "C7", "span1": [185, 208], "span2": [242, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13709": {"label": 3, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.4", "entity2": "4-bromopropofol", "span1": [150, 158], "span2": [110, 125]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12400": {"label": 2, "data": {"text": "Number and area of preneoplastic foci positive for glutathione S-transferase placental form (GST-P) were consistently higher in these groups than the sum of individual values in the groups treated with HEP or HCB alone.", "entity1": "glutathione S-transferase placental form", "entity2": "HCB", "span1": [51, 91], "span2": [209, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13357": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "PR", "entity2": "Medroxyprogesterone acetate", "span1": [115, 117], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11046": {"label": 8, "data": {"text": "Some of the new compounds proved in a slightly modified colorimetric Ellmann's assay to be potent inhibitors of acetylcholinesterase and of butyrylcholinesterase which is another catalytic enzyme hydrolysing acetylcholine.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [112, 132], "span2": [208, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5389": {"label": 3, "data": {"text": "Methylphenidate, an inhibitor of dopamine and norepinephrine transporters (DAT and NET, respectively), is a standard treatment for ADHD.", "entity1": "DAT", "entity2": "Methylphenidate", "span1": [75, 78], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3403": {"label": 3, "data": {"text": "We found that PSE inhibits interleukin-2 (IL-2) and tumor necrosis factor (TNF) alpha-gene transcription in stimulated Jurkat cells, a human T-cell leukemia cell line.", "entity1": "IL-2", "entity2": "PSE", "span1": [42, 46], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6666": {"label": 5, "data": {"text": "CONCLUSIONS: AT1 antagonism by eprosartan lowers heart rate variability and baroreflex gain.", "entity1": "AT1", "entity2": "eprosartan", "span1": [13, 16], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6286": {"label": 8, "data": {"text": "The production of thromboxane B2 in whole blood allowed to clot at 37 degrees C for 60 min was assessed as an index of platelet COX-1 activity.", "entity1": "COX-1", "entity2": "thromboxane B2", "span1": [128, 133], "span2": [18, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2764": {"label": 3, "data": {"text": "Using standard assays, lumiracoxib was found to be a poor inhibitor of purified ovine COX-1 and a relatively weak inhibitor of purified human COX-2.", "entity1": "ovine COX-1", "entity2": "lumiracoxib", "span1": [80, 91], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2195": {"label": 1, "data": {"text": "Comparisons of the structures of the cyanobacterial toxin:phosphatase complexes explain the biochemical mechanism by which microcystins but not nodularins permanently modify their protein phosphatase targets by covalent addition to an active site cysteine residue.", "entity1": "protein phosphatase", "entity2": "microcystins", "span1": [180, 199], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8846": {"label": 2, "data": {"text": "Moreover, calycopterin, in presence of H2O2 inhibited the decrease caused by oxidative stress in stress-sensing transcription factors, CREB and Nrf2, which play an important role in antioxidant capacity of the cell.", "entity1": "Nrf2", "entity2": "calycopterin", "span1": [144, 148], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7257": {"label": 4, "data": {"text": "Interestingly, both isomers of METH were full agonists at mTAAR1 and h-rChTAAR1, whereas both were partial agonists at rTAAR1.", "entity1": "rTAAR1", "entity2": "METH", "span1": [119, 125], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14779": {"label": 0, "data": {"text": "The CSN/IRF5 interaction occurred on the carboxyl and amino termini of IRF5; a single internal deletion from amino acids 455 to 466 (\u0394455-466) was found to significantly reduce IRF5 protein stability.", "entity1": "IRF5", "entity2": "carboxyl", "span1": [71, 75], "span2": [41, 49]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9445": {"label": 9, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP2", "entity2": "1-OH-PGE1", "span1": [186, 189], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1405": {"label": 8, "data": {"text": "Gemfibrozil, a lipid-lowering drug, inhibited cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes.", "entity1": "inducible nitric-oxide synthase", "entity2": "NO", "span1": [102, 133], "span2": [77, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1313": {"label": 1, "data": {"text": "Minocycline treatment prevents the formation of activated caspase-3, a known effector of apoptosis, as well as the appearance of a calpain cleaved substrate, a marker of excitotoxic/necrotic cell death.", "entity1": "calpain", "entity2": "Minocycline", "span1": [131, 138], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9625": {"label": 1, "data": {"text": "Here, we report that MgATP and MgADP, but not the Mg salt of gamma-thio-ATP, stabilize the binding of prebound 8-azido-[alpha-32P]ATP to SUR1.", "entity1": "SUR1", "entity2": "MgADP", "span1": [137, 141], "span2": [31, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1577": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "acetylcholinesterase", "entity2": "[1,8]naphthyridines", "span1": [4, 24], "span2": [135, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10354": {"label": 9, "data": {"text": "The production of Br-Phe5 was reduced with GW660511X while no significant change was observed with omapatrilat after 4 h of incubation.", "entity1": "Br-Phe5", "entity2": "omapatrilat", "span1": [18, 25], "span2": [99, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11159": {"label": 8, "data": {"text": "Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A).", "entity1": "PDE10A", "entity2": "cGMP", "span1": [100, 106], "span2": [94, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7972": {"label": 1, "data": {"text": "Quantitative polymerase chain reaction, western blotting, immunohistochemical analysis and immunofluorescence were used to determine the changes in the expression of organic anion transporter (Oat)1 and Oat3 in rat kidney in response to 1,25(OH)(2)D(3) treatment.", "entity1": "organic anion transporter", "entity2": "1,25(OH)(2)D(3)", "span1": [166, 191], "span2": [237, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15808": {"label": 3, "data": {"text": "Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.", "entity1": "kinase", "entity2": "imidazo[1,2-a]pyrazine", "span1": [109, 115], "span2": [50, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14219": {"label": 1, "data": {"text": "Treatment options for DUB are: combined oral contraceptives (COCs), progestogens, non steroidal anti inflammatory drugs (NSAIDs), tranexamic acid (anti-fibrinolytic), GnRH analogues, Danazol and Levonorgestrel releasing intra uterine system (LNG IUS).", "entity1": "GnRH", "entity2": "Danazol", "span1": [167, 171], "span2": [183, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11248": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "NET", "entity2": "4',7,8-trichloro", "span1": [147, 150], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7788": {"label": 3, "data": {"text": "Both apo-lycopenoic acids also decreased CSE-induced ROS production, 8-OHdG formation and reduced the increase in NOX-4 and COX-2 expressions caused by CSE.", "entity1": "COX-2", "entity2": "apo-lycopenoic acids", "span1": [124, 129], "span2": [5, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"112": {"label": 9, "data": {"text": "The oxidized and t-butyl analogues were relatively ineffective in inhibiting cAMP phosphodiesterase.", "entity1": "cAMP phosphodiesterase", "entity2": "t-butyl", "span1": [77, 99], "span2": [17, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5640": {"label": 3, "data": {"text": "In conclusion, our data indicate that AMPK inhibition is required, but not sufficient for compound C-mediated apoptotic death of glioma cells.", "entity1": "AMPK", "entity2": "compound C", "span1": [38, 42], "span2": [90, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15769": {"label": 2, "data": {"text": "Furthermore, we detected that ICI treatment induced glycogen synthase kinase (Gsk3-\u03b2) Ser 9 phosphorylation, which correlates with cyclin D1 nuclear localization.", "entity1": "glycogen synthase kinase", "entity2": "ICI", "span1": [52, 76], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12854": {"label": 1, "data": {"text": "The dysmenorrhea pain evoked by vasopressin correlated poorly with area under the curve, which may suggest that the effect is mediated by more than one V1a-like receptor.", "entity1": "V1a-like receptor", "entity2": "vasopressin", "span1": [152, 169], "span2": [32, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4012": {"label": 3, "data": {"text": "Compared with the untreated colitis group, the curcumin-treated group showed significant decreases in the disease activity index, colonic mucosa damage index, histological score, myeloperoxidase activity, and expressions of NF-\u03baB mRNA, IL-27 mRNA, TLR4 protein, NF-\u03baB p65 protein, and IL-27 p28 protein (p < 0.05).", "entity1": "p65", "entity2": "curcumin", "span1": [268, 271], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12447": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "ML326", "span1": [173, 175], "span2": [181, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5341": {"label": 1, "data": {"text": "S1P activated phosphatidylinositol 3-kinase (PI3K)/Akt signaling, leading to the inhibition of glycogen synthase kinase-3\u03b2 and the nuclear translocation of \u03b2-catenin, followed by the increase of the transcriptional activity by \u03b2-catenin/T-cell factor complex formation in both SaOS-2 cells and MC3T3-E1 cells.", "entity1": "\u03b2-catenin", "entity2": "S1P", "span1": [227, 236], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6410": {"label": 3, "data": {"text": "Isoproterenol (50 to 100 nmol/L) was used to mimic an increase in beta-adrenergic tone, d-sotalol (100 micromol/L) to block I(Kr) (LQT2 model), and ATX-II (20 nmol/L) to augment late I(Na) (LQT3 model).", "entity1": "I(Kr)", "entity2": "Isoproterenol", "span1": [124, 129], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13989": {"label": 9, "data": {"text": "Importantly, treatment with cabozantinib did not increase lung tumor burden in an experimental model of metastasis, which has been observed with inhibitors of VEGF signaling that do not target MET.", "entity1": "MET", "entity2": "cabozantinib", "span1": [193, 196], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8066": {"label": 3, "data": {"text": "Furthermore, metformin was able to not only decrease the paclitaxel-induced p38 MAPK-mediated ERCC1 expression, but also augment the cytotoxic effect induced by paclitaxel.", "entity1": "MAPK", "entity2": "metformin", "span1": [80, 84], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5992": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "( Glu1]Pg", "entity2": "EACA", "span1": [43, 52], "span2": [226, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11429": {"label": 1, "data": {"text": "In the presence of alphaAR blockade, concentration-response curves for isoproterenol, norepinephrine, and epinephrine suggested that a beta1AR was involved in this response, and the rank order of potency was isoproterenol > norepinephrine = epinephrine.", "entity1": "beta1AR", "entity2": "norepinephrine", "span1": [135, 142], "span2": [86, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3133": {"label": 3, "data": {"text": "Moreover, kinetic analysis revealed that inhibition by reserpine, a typical VMAT2 inhibitor, was uncompetitive, decreasing maximum velocity and affinity for dopamine.", "entity1": "VMAT2", "entity2": "reserpine", "span1": [76, 81], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13496": {"label": 2, "data": {"text": "CONCLUSIONS: Weight reduction with sibutramine is associated with altered gastric functions and increased peptide YY and is significantly associated with SLC6A4 genotype.", "entity1": "peptide YY", "entity2": "sibutramine", "span1": [106, 116], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4038": {"label": 3, "data": {"text": "In addition, we found that neoechinulin A significantly suppressed the production of neurotoxic inflammatory mediator tumour necrosis factor-\u03b1 (TNF-\u03b1), interleukin-1\u03b2 (IL-1\u03b2), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) in activated BV-2 cells.", "entity1": "tumour necrosis factor-\u03b1", "entity2": "neoechinulin A", "span1": [118, 142], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14590": {"label": 3, "data": {"text": "Although treatment with 17-AAG reduced AhR levels and AhR-regulated gene expression in lung AD cells, AhR expression increased anticancer activity of 17-AAG.", "entity1": "AhR", "entity2": "17-AAG", "span1": [54, 57], "span2": [24, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8166": {"label": 3, "data": {"text": "Taken together, the results of this study demonstrate that DPEP inhibits LPS-stimulated inflammation by blocking the NF-\u03baB and MAPK pathways in macrophages.", "entity1": "MAPK", "entity2": "DPEP", "span1": [127, 131], "span2": [59, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7440": {"label": 5, "data": {"text": "(-)-Stepholidine (SPD), an active ingredient of the Chinese herb Stephania, is the first compound found to have dual function as a dopamine receptor D1 agonist and D2 antagonist.", "entity1": "D2", "entity2": "(-)-Stepholidine", "span1": [164, 166], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11911": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "insulin", "entity2": "triglycerides", "span1": [118, 125], "span2": [46, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14328": {"label": 3, "data": {"text": "Results showed that DMF increased nuclear levels of Nrf2, and both DMF and adenovirus-mediated overexpression of Nrf2 (Ad-Nrf2) decreased PAI-1, alpha-smooth muscle actin (alpha-SMA), fibronectin and type 1 collagen expression in TGF-beta-treated rat mesangial cells (RMCs) and renal fibroblast cells (NRK-49F).", "entity1": "PAI-1", "entity2": "DMF", "span1": [138, 143], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11088": {"label": 1, "data": {"text": "Loperamide, an opiate analog, differently modifies the adrenocorticotropin responses to corticotropin-releasing hormone and lysine vasopressin in patients with Addison's disease.", "entity1": "lysine vasopressin", "entity2": "Loperamide", "span1": [124, 142], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5834": {"label": 8, "data": {"text": "The unique role of the enzyme 5-lipoxygenase (5-LO) in the production of leukotrienes (LTs) makes it a likely target for biochemical manipulation.", "entity1": "5-lipoxygenase", "entity2": "LTs", "span1": [30, 44], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7932": {"label": 2, "data": {"text": "Glucosamine at 50\u00a0mM was demonstrated to elevate both the mRNA and protein expression of p53 and heme oxygenase-1 (HO-1), but also caused a reduction in p21 protein expression.", "entity1": "heme oxygenase-1", "entity2": "Glucosamine", "span1": [97, 113], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2984": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "F820A", "entity2": "cGMP", "span1": [265, 270], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14512": {"label": 1, "data": {"text": "Filtering and analysis of data identified three oncogenic pathways interfered by 5-ASA: MAPK/ERK pathway, cell adhesion and \u03b2-catenin/Wnt signaling.", "entity1": "\u03b2-catenin", "entity2": "5-ASA", "span1": [124, 133], "span2": [81, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3048": {"label": 8, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "COX", "entity2": "arachidonic acid", "span1": [64, 67], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2289": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP2 receptors", "entity2": "butaprost", "span1": [27, 40], "span2": [149, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6235": {"label": 1, "data": {"text": "However, [3H]eletriptan had over 6-fold higher affinity than [3H]sumatriptan at the 5-HT1D receptor (K(D)): 0.92 and 6.58 nM, respectively) and over 3-fold higher affinity than [3H]sumatriptan at the 5-HT1B receptor (K(D): 3.14 and 11.07 nM, respectively).", "entity1": "5-HT1B", "entity2": "[3H]sumatriptan", "span1": [200, 206], "span2": [177, 192]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2364": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "ERK", "entity2": "Sorafenib", "span1": [79, 82], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15563": {"label": 2, "data": {"text": "Puerarin administration enhanced glutathione (GSH) activity, glial cell line-derived neurotrophic factor (GDNF) expression and PI3K/Akt pathway activation, which might ameliorate MPTP injection-induced progressive elevation of reactive oxygen species (ROS) formation in mice.", "entity1": "PI3K", "entity2": "Puerarin", "span1": [127, 131], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9770": {"label": 5, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "5-HT(1B)", "entity2": "yohimbine", "span1": [132, 140], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12280": {"label": 3, "data": {"text": "This study identified four clinically approved antihypertensive drugs (efonidipine, felodipine, isradipine, and nitrendipine) as potent T-channel blockers (IC(50) < 3 microM).", "entity1": "T-channel", "entity2": "isradipine", "span1": [136, 145], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8264": {"label": 5, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2A", "entity2": "M100907", "span1": [243, 249], "span2": [251, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5098": {"label": 0, "data": {"text": "This was confirmed by their ability to selectively abrogate the induction of IL-8 transcription, whereas the ICAM-1 gene, which is not transcribed selectively by an NF-\u03baB complex containing a form of p65 phosphorylated on Ser536, did not change.", "entity1": "p65", "entity2": "Ser", "span1": [200, 203], "span2": [222, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14071": {"label": 2, "data": {"text": "Exogenous stimulation of PKA activity, achieved by forskolin treatment, protected K-ras-transformed cells from apoptosis induced by glucose deprivation, enhanced complex I activity, intracellular adenosine triphosphate (ATP) levels, mitochondrial fusion and decreased intracellular reactive oxygen species (ROS) levels.", "entity1": "complex I", "entity2": "forskolin", "span1": [162, 171], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13481": {"label": 3, "data": {"text": "Mifepriston'e blocks glucocorticoid receptor activation without modifying cortisol synthesis.", "entity1": "glucocorticoid receptor", "entity2": "Mifepriston'e", "span1": [21, 44], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14702": {"label": 1, "data": {"text": "Promoter replacements conferring constitutive expression of MSH2 revealed that the transcriptional induction in response to MMS is required to maintain induced levels of Msh2.", "entity1": "Msh2", "entity2": "MMS", "span1": [170, 174], "span2": [124, 127]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6440": {"label": 2, "data": {"text": "Mobility shift assays on whole cell extracts showed that clenbuterol increased AP1 binding in 3T3 cells prior to increasing NGF synthesis.", "entity1": "NGF", "entity2": "clenbuterol", "span1": [124, 127], "span2": [57, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3755": {"label": 1, "data": {"text": "Thus, the apoptosis induction in SGC-7901 cells by \u03b2-ionone may be regulated through a PI3K-AKT pathway.", "entity1": "PI3K", "entity2": "\u03b2-ionone", "span1": [87, 91], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4292": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B1", "entity2": "estrone 3-sulfate", "span1": [258, 265], "span2": [71, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7187": {"label": 2, "data": {"text": "CONCLUSION: Intake of high SFAs and MUFAs appears to increase expression of PBMC D6D and D5D genes, whilst high EFAs intake appears to decrease expression of PBMC D6D and D5D genes.", "entity1": "D5D", "entity2": "MUFAs", "span1": [89, 92], "span2": [36, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11886": {"label": 8, "data": {"text": "Ferredoxin 1 (FDX1; adrenodoxin) is an iron-sulfur protein that is involved in various metabolic processes, including steroid hormone synthesis in mammalian tissues.", "entity1": "adrenodoxin", "entity2": "steroid", "span1": [20, 31], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13462": {"label": 5, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "PPARgamma", "entity2": "T0070907", "span1": [47, 56], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13754": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "Ca(v)1.3", "entity2": "1,4-dihydropyridine", "span1": [56, 64], "span2": [81, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1912": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "capecitabine", "span1": [96, 119], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12451": {"label": 0, "data": {"text": "S-nitrosation of glutathione transferase P1-1 is controlled by the conformation of a dynamic active-site helix.", "entity1": "glutathione transferase P1-1", "entity2": "S", "span1": [17, 45], "span2": [0, 1]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"277": {"label": 1, "data": {"text": "Agmatine binds to alpha 2-adrenergic and imidazoline receptors and stimulates release of catecholamines from adrenal chromaffin cells.", "entity1": "alpha 2-adrenergic and imidazoline receptors", "entity2": "Agmatine", "span1": [18, 62], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4255": {"label": 2, "data": {"text": "Butein also increased heme oxygenase-1 (HO-1) protein expression and HO activity.", "entity1": "HO", "entity2": "Butein", "span1": [69, 71], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2513": {"label": 3, "data": {"text": "Our results demonstrated that auranofin suppressed TLR4-mediated activation of transcription factors, NF-kappaB and IRF3, and expression of COX-2, a pro-inflammatory enzyme.", "entity1": "COX-2", "entity2": "auranofin", "span1": [140, 145], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5842": {"label": 9, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT4", "entity2": "ondansetron", "span1": [28, 33], "span2": [120, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12582": {"label": 0, "data": {"text": "PC3 is a type I proinsulin-processing enzyme that initiates the sequential processing of proinsulin to insulin by cleaving the proinsulin molecule on the COOH-terminal side of the dibasic peptide, Arg31-Arg32, joining the B-chain and C-peptide.", "entity1": "proinsulin", "entity2": "C", "span1": [127, 137], "span2": [234, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6972": {"label": 1, "data": {"text": "Recently, a G-protein-coupled receptor, termed GPR109A (HM74A in humans, PUMA-G in mice), was described and shown to mediate the nicotinic acid-induced antilipolytic effects in adipocytes.", "entity1": "G-protein-coupled receptor", "entity2": "nicotinic acid", "span1": [12, 38], "span2": [129, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2936": {"label": 8, "data": {"text": "Adenylosuccinate synthetase (AdSS) catalyzes the Mg2+ dependent condensation of a molecule of IMP with aspartate to form adenylosuccinate, in a reaction driven by the hydrolysis of GTP to GDP.", "entity1": "AdSS", "entity2": "adenylosuccinate", "span1": [29, 33], "span2": [121, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15779": {"label": 3, "data": {"text": "A N,N-dimethylaminopropyl derivative showed promising inhibition of Trypanosoma cruzi OSC in combination with low cytotoxicity, and showed significant reduction of cholesterol biosynthesis in a human cell line.", "entity1": "Trypanosoma cruzi OSC", "entity2": "N,N-dimethylaminopropyl", "span1": [68, 89], "span2": [2, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5320": {"label": 3, "data": {"text": "Furthermore, these phosphorylated flavonoids demonstrated good to high selectivity for CEase over AChE, which only showed micromolar potency inhibition of AChE.", "entity1": "AChE", "entity2": "phosphorylated flavonoids", "span1": [155, 159], "span2": [19, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11921": {"label": 1, "data": {"text": "Co-IP and coimmunolocalization confirmed that Creb1 associated with Mecp2 and cotransfection with glut3-(m)CpG in HT22 cells enhanced glut3 transcription.", "entity1": "glut3", "entity2": "(m)CpG", "span1": [98, 103], "span2": [104, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"919": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "levobetaxolol", "span1": [22, 39], "span2": [123, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4950": {"label": 1, "data": {"text": "The inhibitory effect of fisetin on adipogenesis is dependent of mTOR activity, suggesting that fisetin inhibits adipogenesis and the accumulation of intracellular triglycerides during adipocyte differentiation by targeting mTORC1 signaling.", "entity1": "mTORC1", "entity2": "fisetin", "span1": [224, 230], "span2": [96, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5903": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "plasma very-low-density lipoproteins", "entity2": "nicotinic acid", "span1": [95, 131], "span2": [32, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5291": {"label": 3, "data": {"text": "Vandetanib (Caprelsa(\u00ae), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60\u00a0% of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors.", "entity1": "RET", "entity2": "Vandetanib", "span1": [173, 176], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1245": {"label": 3, "data": {"text": "The selective PDE 4 inhibitors, and to a certain extent the PDE3 inhibitors amrinone and milrinone, reduced the GM-CSF release in a concentration dependent manner.", "entity1": "GM-CSF", "entity2": "amrinone", "span1": [112, 118], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2684": {"label": 1, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "c-Kit", "entity2": "MP470", "span1": [50, 55], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10182": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "human organic anion transporting polypeptide B", "entity2": "rifamycin SV", "span1": [237, 283], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5883": {"label": 0, "data": {"text": "The pyridoxal 5'-phosphate binding lysine in mouse ODC was identified as lysine 69 of the mouse sequence by reduction of the purified holoenzyme form with NaB[3H]4 followed by digestion of the carboxymethylated protein with endoproteinase Lys-C, radioactive peptide mapping using reversed-phase high pressure liquid chromatography and gas-phase peptide sequencing.", "entity1": "mouse ODC", "entity2": "lysine", "span1": [45, 54], "span2": [35, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2753": {"label": 1, "data": {"text": "Taken together with a recent crystal structure of a lumiracoxib-COX-2 complex, the kinetic analyses presented herein of the inhibition of mutant COX-2s by lumiracoxib allows the definition of the molecular basis of COX-2 inhibition.", "entity1": "COX-2", "entity2": "lumiracoxib", "span1": [64, 69], "span2": [52, 63]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10284": {"label": 2, "data": {"text": "Rasagiline prevented the PT in mitochondria directly and also indirectly through induction of antiapoptotic Bcl-2 and a neurotrophic factor, glial cell line-derived neurotrophic factor (GDNF).", "entity1": "GDNF", "entity2": "Rasagiline", "span1": [186, 190], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9376": {"label": 1, "data": {"text": "Recovery from modulation by cyclothiazide was slower for GluR-AiBi and GluR-AoBi than for GluR-AiBo and GluR-AoBo.", "entity1": "GluR-AiBo", "entity2": "cyclothiazide", "span1": [90, 99], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8263": {"label": 4, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2C", "entity2": "PAT", "span1": [159, 165], "span2": [149, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4317": {"label": 2, "data": {"text": "It was found that expression of Sim2 protein in cortical neurons was increased in streptozotocin-induced diabetes mellitus rat model.", "entity1": "Sim2", "entity2": "streptozotocin", "span1": [32, 36], "span2": [82, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"210": {"label": 5, "data": {"text": "We conclude that alprenolol and BAAM are competitive slowly reversible beta 1-adrenoceptor antagonists on rat left atria.", "entity1": "beta 1-adrenoceptor", "entity2": "alprenolol", "span1": [71, 90], "span2": [17, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8958": {"label": 8, "data": {"text": "Affinity alkylation with 2 alpha-bromoacetoxyprogesterone suggests that the dehydrogenase and isomerase substrate steroids bind at different sites on the same protein.", "entity1": "dehydrogenase", "entity2": "steroids", "span1": [76, 89], "span2": [114, 122]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3562": {"label": 0, "data": {"text": "Current research shows that the practice of swim training increases the tyrosine phosphorylation of IRS-1 which can modulate the effect caused by obesity in insulin receptors.", "entity1": "IRS-1", "entity2": "tyrosine", "span1": [100, 105], "span2": [72, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"104": {"label": 5, "data": {"text": "The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed.", "entity1": "histamine H1-receptor", "entity2": "astemizole", "span1": [114, 135], "span2": [161, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13201": {"label": 9, "data": {"text": "In addition, we found that selenophosphate synthetase 2 could synthesize monoselenophosphate in vitro but selenophosphate synthetase 1 could not.", "entity1": "selenophosphate synthetase 1", "entity2": "monoselenophosphate", "span1": [106, 134], "span2": [73, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4086": {"label": 2, "data": {"text": "The upregulation of calpain, tBid and caspase-3 activity were further inhibited by treatment with EGTA in the presence of ALD.", "entity1": "caspase-3", "entity2": "ALD", "span1": [38, 47], "span2": [122, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8981": {"label": 5, "data": {"text": "The suppressive effect of ceruletide on barrel rotation could be partially countered by MK-329, a selective peripheral CCK (CCK-A) receptor antagonist.", "entity1": "CCK", "entity2": "MK-329", "span1": [119, 122], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14625": {"label": 8, "data": {"text": "All three CDA proteins showed similar K(m) and V(max) for Ara-C and dFdC deamination, except for CDA70Thr, which had a 2.5-fold lower K(m) and 6-fold lower V(max) for Ara-C deamination.", "entity1": "CDA", "entity2": "Ara-C", "span1": [97, 100], "span2": [167, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4365": {"label": 2, "data": {"text": "Administration of a single dose of DEX-P showed a temporal increase in CYP3A activity in both tissues and the induction ratios reached maximum values at 12\u2009h after DEX-P administration.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [71, 76], "span2": [164, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13440": {"label": 1, "data": {"text": "We demonstrate that only treatment of HaCaT with GLA and EPA or a PPARgamma ligand (roziglitazone), induced COX-2 expression (protein and mRNA).", "entity1": "PPARgamma", "entity2": "roziglitazone", "span1": [66, 75], "span2": [84, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1258": {"label": 3, "data": {"text": "The selective PDE 4 inhibitors, and to a certain extent the PDE3 inhibitors amrinone and milrinone, reduced the GM-CSF release in a concentration dependent manner.", "entity1": "PDE3", "entity2": "amrinone", "span1": [60, 64], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4276": {"label": 2, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "AEG-1", "entity2": "MG132", "span1": [118, 123], "span2": [35, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15391": {"label": 3, "data": {"text": "Discovery of 7-methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole (TASP0382088): a potent and selective transforming growth factor-\u03b2 type I receptor inhibitor as a topical drug for alopecia.", "entity1": "transforming growth factor-\u03b2 type I receptor", "entity2": "7-methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole", "span1": [130, 174], "span2": [13, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1438": {"label": 3, "data": {"text": "Low levels of serotonin may reduce the density of the serotonin transporter (SERT) by either increasing trafficking or reducing synthesis; a \"neuroadaptive response\".", "entity1": "SERT", "entity2": "serotonin", "span1": [77, 81], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12016": {"label": 1, "data": {"text": "We investigated the diurnal expression of clock genes and clock-controlled genes (CCGs) in 3-hour intervals for a 24-h period in the livers of male streptozotocin (STZ)-treated rats, male spontaneous type 1 diabetic LEW.1AR1-iddm (Iddm) rats, and Iddm rats treated for 10 days with insulin.", "entity1": "CCGs", "entity2": "STZ", "span1": [82, 86], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15089": {"label": 3, "data": {"text": "Pharmacodynamic data suggest that ceftazidime-avibactam is rapidly bactericidal versus \u03b2-lactamase-producing Gram-negative bacilli that are not inhibited by ceftazidime alone.Clinical trials to date have reported that ceftazidime-avibactam is as effective as standard carbapenem therapy in complicated intra-abdominal infection and complicated urinary tract infection, including infection caused by cephalosporin-resistant Gram-negative isolates.", "entity1": "\u03b2-lactamase", "entity2": "avibactam", "span1": [87, 98], "span2": [46, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8857": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "c-Src", "entity2": "TCDD", "span1": [19, 24], "span2": [104, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"68": {"label": 4, "data": {"text": "While there is considerable indirect evidence to implicate histamine in the pathogenesis of asthma, a critical evaluation of H1-receptor antagonism in this condition has, until recently, proved difficult, as many of the early H1-receptor antagonists possessed additional actions, such as anti-cholinergic, local anaesthetic, alpha-adrenoceptor antagonistic and anti-serotonin activity.", "entity1": "H1-receptor", "entity2": "histamine", "span1": [226, 237], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10283": {"label": 2, "data": {"text": "Rasagiline prevented the PT in mitochondria directly and also indirectly through induction of antiapoptotic Bcl-2 and a neurotrophic factor, glial cell line-derived neurotrophic factor (GDNF).", "entity1": "glial cell line-derived neurotrophic factor", "entity2": "Rasagiline", "span1": [141, 184], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4771": {"label": 3, "data": {"text": "These results suggested that DMBT could inhibit invasion and angiogenesis by downregulation of VEGFand MMP-9, resulting from the inhibition of Akt pathway.", "entity1": "VEGF", "entity2": "DMBT", "span1": [95, 99], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3413": {"label": 1, "data": {"text": "Transfection of the brain cDNA into COS-1 cells resulted in transporter activity that was blocked by the VMAT inhibitor reserpine and a proton ionophore, but not by tetrabenazine, which has a high affinity for VMAT-2.", "entity1": "VMAT-2", "entity2": "tetrabenazine", "span1": [210, 216], "span2": [165, 178]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"3670": {"label": 3, "data": {"text": "Additionally, the mRNA levels of melanogenesis-related genes (c-KIT, stem cell factor (SCF), and macrophage migration inhibitory factor (MIF)) were down-regulated by artemisinic acid.", "entity1": "macrophage migration inhibitory factor", "entity2": "artemisinic acid", "span1": [97, 135], "span2": [166, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12694": {"label": 0, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "epsilon-amino", "span1": [79, 90], "span2": [273, 286]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15693": {"label": 1, "data": {"text": "Conclusion The results of this work contribute information regarding the antinociceptive properties of CAT on acute pain and show that, at least in part, TRPV1, TRPM8, ASIC, glutamate receptors, PKC and PKA participate in CAT's antinociceptive mechanism.", "entity1": "ASIC", "entity2": "CAT", "span1": [168, 172], "span2": [222, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15611": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "mitogen-activated protein kinase", "entity2": "galangin", "span1": [122, 154], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3042": {"label": 5, "data": {"text": "EP(1) and EP(3) receptor antagonists ONO-8713 and ONO-AE3-240, but not the EP(4) antagonists ONO-AE3-208 and AH 23848, inhibited tumor cell proliferation, indicating the significance of EP(1) and EP(3) but not EP(4) for MB growth.", "entity1": "EP(4)", "entity2": "AH 23848", "span1": [75, 80], "span2": [109, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10233": {"label": 0, "data": {"text": "A BLAST search using maize PAO sequences identified homologous mammalian cDNAs derived from human hepatoma and mouse mammary carcinoma: the encoded proteins differed by 20 amino acids.", "entity1": "maize PAO", "entity2": "amino acids", "span1": [21, 30], "span2": [172, 183]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7145": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "tadalafil", "span1": [27, 46], "span2": [117, 126]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13512": {"label": 1, "data": {"text": "Hydrogen peroxide-mediated oxidative stress disrupts calcium binding on calmodulin: more evidence for oxidative stress in vitiligo.", "entity1": "calmodulin", "entity2": "calcium", "span1": [72, 82], "span2": [53, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9954": {"label": 9, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-1", "entity2": "MK-0966", "span1": [180, 185], "span2": [84, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12564": {"label": 1, "data": {"text": "5-Methylurapidil and phentolamine were confirmed as selective for the alpha 1A-adrenoceptors, whereas spiperone was alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptors", "entity2": "phentolamine", "span1": [70, 92], "span2": [21, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10876": {"label": 3, "data": {"text": "Irinotecan (CPT-11, 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin) has exhibited clinical activities against a broad spectrum of carcinomas by inhibiting DNA topoisomerase I (Topo I).", "entity1": "DNA topoisomerase I", "entity2": "7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin", "span1": [175, 194], "span2": [20, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6922": {"label": 1, "data": {"text": "We present our studies to demonstrate that HM74A, but not HM74, binds niacin at high affinities and effectively mediates Gi signaling events in human embryonic kidney HEK293 cells as well as in 3T3L1 adipocytes expressing HM74A.", "entity1": "HM74A", "entity2": "niacin", "span1": [43, 48], "span2": [70, 76]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10897": {"label": 1, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "Pyridoxal kinase", "entity2": "Zn2+", "span1": [0, 16], "span2": [124, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13944": {"label": 1, "data": {"text": "denopamine for beta(1); clenbuterol, AZ 40140d, salbutamol for beta(2)) were found to have subtype-selective intrinsic efficacy.", "entity1": "beta(2)", "entity2": "salbutamol", "span1": [63, 70], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7378": {"label": 3, "data": {"text": "RAMH inhibition of cholangiocyte growth was associated with decreased cAMP levels and PKA/ERK1/2/Elk-1 phosphorylation.", "entity1": "PKA", "entity2": "RAMH", "span1": [86, 89], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11376": {"label": 8, "data": {"text": "Favorable enzyme profiles (high TP and low DPD) generate high intratumor levels of 5-FU that are effective against many tumors, especially those with low TS.", "entity1": "TP", "entity2": "5-FU", "span1": [32, 34], "span2": [83, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3047": {"label": 8, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "cyclooxygenases", "entity2": "arachidonic acid", "span1": [47, 62], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2550": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "tyrosine kinase", "entity2": "imatinib mesylate", "span1": [103, 118], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10833": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Imatinib", "span1": [110, 113], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"856": {"label": 0, "data": {"text": "Removal of N- and O-linked oligosaccharides reduces the M(r) to approximately 160,000, suggesting that approximately 60% of the mass of SPACRCAN is carbohydrate.", "entity1": "SPACRCAN", "entity2": "N", "span1": [136, 144], "span2": [11, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10777": {"label": 3, "data": {"text": "Imatinib mesylate is a tyrosine kinase inhibitor of the ABL, platelet-derived growth factor receptor (PDGFR), and c-kit kinases.", "entity1": "kinases", "entity2": "Imatinib mesylate", "span1": [120, 127], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2121": {"label": 2, "data": {"text": "The positive correlation between vitamin A and immunoglobulin A concentrations might be the result of the vitamin A inductive effect during immunoglobulins A synthesis.", "entity1": "immunoglobulins A", "entity2": "vitamin A", "span1": [140, 157], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13772": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "c-KIT", "entity2": "AMN107", "span1": [309, 314], "span2": [255, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12852": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "receptor tyrosine kinases", "entity2": "sorafenib", "span1": [73, 98], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"35": {"label": 2, "data": {"text": "Evidence has accumulated in the last few years that the expression of the microsomal/peroxidase antigen (M/TPO-Ag) in thyroid cells is induced by TSH, through pathways which involve intracellular cAMP accumulation and protein synthesis.", "entity1": "microsomal/peroxidase antigen", "entity2": "cAMP", "span1": [74, 103], "span2": [196, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13704": {"label": 1, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.2", "entity2": "4-chloropropofol", "span1": [195, 203], "span2": [175, 191]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6027": {"label": 8, "data": {"text": "Aspirin irreversibly inhibits PGHS-1, preventing this isozyme from forming PGH2 or any other oxygenated product; in contrast, aspirin treatment of PGHS-2 causes this enzyme to form 15-hydroxy-5c,8c,11c,13t-eicosatetraenoic acid (15-HETE) instead of PGH2.", "entity1": "PGHS-2", "entity2": "15-hydroxy-5c,8c,11c,13t-eicosatetraenoic acid", "span1": [147, 153], "span2": [181, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15066": {"label": 9, "data": {"text": "The increase in SAA expression is specific to ritodrine-induced liver damage, because SAA expression was not induced by other hepatotoxic drugs such as acetaminophen, valproic acid, or metformin.", "entity1": "SAA", "entity2": "metformin", "span1": [86, 89], "span2": [185, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"863": {"label": 3, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ornithine decarboxylase", "entity2": "DL-alpha-difluoromethylornithine", "span1": [118, 141], "span2": [53, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3626": {"label": 4, "data": {"text": "Methanandamide (10.0 mg/kg) had lesser effect than other CB agonists, and the CB2 agonist AM1241 [1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole], the anandamide transport inhibitor AM404, and the CB antagonist rimonabant did not have diuretic effects.", "entity1": "CB2", "entity2": "AM1241", "span1": [78, 81], "span2": [90, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"1888": {"label": 1, "data": {"text": "I3A bound to PKC-alpha in the presence of phosphatidylserine with high affinity; however, under these assay conditions, little PKC isoform selectivity was observed.", "entity1": "PKC-alpha", "entity2": "phosphatidylserine", "span1": [13, 22], "span2": [42, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6663": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [80, 85], "span2": [235, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"826": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "STA2", "span1": [258, 275], "span2": [303, 307]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10420": {"label": 8, "data": {"text": "Blockade of LTC4 synthesis caused by additive inhibition of gIV-PLA2 phosphorylation: Effect of salmeterol and PDE4 inhibition in human eosinophils.", "entity1": "gIV-PLA2", "entity2": "LTC4", "span1": [60, 68], "span2": [12, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14371": {"label": 3, "data": {"text": "NFD suppressed EGF-mediated protein levels of c-Jun and c-Fos, and reduced MMP-9 expression and activity, concomitantly with a marked inhibition on cell migration and invasion without obvious cellular cytotoxicity.", "entity1": "EGF", "entity2": "NFD", "span1": [15, 18], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3353": {"label": 1, "data": {"text": "The Ca(2+) dependent interaction between troponin I (cTnI) and troponin C (cTnC) triggers contraction in heart muscle.", "entity1": "cTnI", "entity2": "Ca(2+)", "span1": [53, 57], "span2": [4, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13205": {"label": 8, "data": {"text": "SecS required selenophosphate and O-phosphoseryl-tRNA([Ser]Sec) as substrates to generate selenocysteyl-tRNA([Ser]Sec).", "entity1": "SecS", "entity2": "selenocysteyl", "span1": [0, 4], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14450": {"label": 2, "data": {"text": "We observed similar effects of Ag NPs on inflammatory mediator expression in vitro and in vivo with increase of interleukin-8 (IL-8)/macrophage inflammatory protein 2, IL-1RI, and tumor necrosis factor-\u03b1 expression in both models and increased IL-8 protein release in vitro.", "entity1": "interleukin-8", "entity2": "Ag", "span1": [112, 125], "span2": [31, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8336": {"label": 5, "data": {"text": "Rolapitant and netupitant are other NK1 receptor antagonists that are currently in phase III clinical trials.", "entity1": "NK1 receptor", "entity2": "netupitant", "span1": [36, 48], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11181": {"label": 3, "data": {"text": "To investigate the possibility that felbamate's favorable toxicity profile could be related to NMDA receptor subtype selectivity, we examined the specificity of felbamate block of recombinant NMDA receptors composed of the NR1a subunit and various NR2 subunits.", "entity1": "NR1a", "entity2": "felbamate", "span1": [223, 227], "span2": [161, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7443": {"label": 9, "data": {"text": "The Ki for mycophenolic acid inhibition of the L263F variant was comparable with the wild-type, and the variant Km for inosine 5'-monophosphate and nicotinamide adenine dinucleotide did not change significantly.", "entity1": "L263F", "entity2": "nicotinamide adenine dinucleotide", "span1": [47, 52], "span2": [148, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10800": {"label": 3, "data": {"text": "We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays.", "entity1": "cyclooxygenases", "entity2": "carprofen", "span1": [111, 126], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"918": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "betaxolol", "span1": [22, 39], "span2": [99, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8598": {"label": 2, "data": {"text": "Further, both the flavonoids were also found to increase the expression of some of the prominent markers for differentiation of osteoblast like osteopontin, osterix, RunX2, osteoprotegerin and osteocalcin.", "entity1": "osteocalcin", "entity2": "flavonoids", "span1": [193, 204], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5480": {"label": 1, "data": {"text": "The stronger binding of 3-keto-desogestrel in intact cells was due to the higher stability of its complex with the progesterone receptor.", "entity1": "progesterone receptor", "entity2": "3-keto-desogestrel", "span1": [115, 136], "span2": [24, 42]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7629": {"label": 3, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "extracellular signal-regulated kinase", "entity2": "SB-277011-A", "span1": [63, 100], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8956": {"label": 7, "data": {"text": "Analysis of coenzyme binding by human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase and steroid 5----4-ene-isomerase using 5'-[p-(fluorosulfonyl)benzoyl]adenosine, an affinity labeling cofactor analog.", "entity1": "steroid 5----4-ene-isomerase", "entity2": "5'-[p-(fluorosulfonyl)benzoyl]adenosine", "span1": [95, 123], "span2": [130, 169]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"2925": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "NCX", "entity2": "aprindine", "span1": [129, 132], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5367": {"label": 1, "data": {"text": "Potent and selective: The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity.", "entity1": "protein kinases", "entity2": "ATP", "span1": [90, 105], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6808": {"label": 1, "data": {"text": "These results suggest that pitavastatin efficiently increases apoA-I in the culture medium of HepG2 cells by promoting apoA-I production through inhibition of HMG-CoA reductase and suppression of Rho activity and by protecting apoA-I from catabolism through ABCA1 induction and lipidation of apoA-I.", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [227, 233], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13180": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "SERT", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane", "span1": [272, 276], "span2": [82, 148]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"279": {"label": 2, "data": {"text": "Both BRL and SAL produced a significant increase in postural finger tremor in keeping with beta 2-adrenoceptor stimulation, and this response was totally abolished by pretreatment with N20.", "entity1": "beta 2-adrenoceptor", "entity2": "BRL", "span1": [91, 110], "span2": [5, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8693": {"label": 8, "data": {"text": "Among the possible transporters involved in the uptake of Cd(2+) and Mn(2+), the expression of ZIP8 (Zrt-, Irt-related protein 8), encoded by Slc39a8, showed a marked suppression in both RBL-Cdr and RBL-Mnr cells.", "entity1": "ZIP8", "entity2": "Cd(2+)", "span1": [95, 99], "span2": [58, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9712": {"label": 1, "data": {"text": "A novel missense mutation, G663A, in exon 5 of the erythroid-specific delta-aminolevulinate synthase gene (ALAS2) was identified in a Japanese male with pyridoxine-responsive sideroblastic anemia.", "entity1": "ALAS2", "entity2": "pyridoxine", "span1": [107, 112], "span2": [153, 163]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13572": {"label": 1, "data": {"text": "A humanized antibody to HER2/neu, trastuzumab, is now FDA approved for the treatment of early stage, HER2/neu overexpressing breast cancer sequenced with chemotherapy including doxorubicin, cyclophosphamide, and paclitaxel.", "entity1": "neu", "entity2": "paclitaxel", "span1": [106, 109], "span2": [212, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12080": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "3 beta-HSD", "entity2": "pregnenolone", "span1": [74, 84], "span2": [132, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"340": {"label": 3, "data": {"text": "The anti-inflammatory drugs sodium salicylate and aspirin inhibited the activation of NF-kappa B, which further explains the mechanism of action of these drugs.", "entity1": "NF-kappa B", "entity2": "sodium salicylate", "span1": [86, 96], "span2": [28, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10466": {"label": 3, "data": {"text": "Ras-CM and TGF-alpha also increase PI3-K activity downstream of the EGFR and increase postradiation survival, both of which are abrogated by GW572016.", "entity1": "EGFR", "entity2": "GW572016", "span1": [68, 72], "span2": [141, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9767": {"label": 5, "data": {"text": "In distinction to yohimbine, fluparoxan shows only modest partial agonist actions at h5-HT(1A) sites versus marked antagonist actions at halpha(2)-ARs.", "entity1": "halpha(2)-ARs", "entity2": "fluparoxan", "span1": [137, 150], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13983": {"label": 0, "data": {"text": "Using a photo incorporable analogue of the general anesthetic, R(+)etomidate, we identified two transmembrane amino acids that were affinity labelled in purified bovine brain GABA(A)-R.", "entity1": "bovine brain GABA(A)-R", "entity2": "amino acids", "span1": [162, 184], "span2": [110, 121]}, "weak_labels": [0, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7625": {"label": 2, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "extracellular signal-regulated kinase", "entity2": "Quinpirole", "span1": [63, 100], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4361": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NQO1", "entity2": "1,2-orthonaphthoquinone", "span1": [149, 153], "span2": [25, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10893": {"label": 1, "data": {"text": "Structural analysis revealed that these three roscovitines bind similarly in the pyridoxal-binding site of PDXK rather than in the anticipated ATP-binding site.", "entity1": "PDXK", "entity2": "ATP", "span1": [107, 111], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2132": {"label": 8, "data": {"text": "Interestingly, part of MCT2 immunoreactivity is located at postsynaptic sites, suggesting a particular role of monocarboxylates and their transporters in synaptic transmission.", "entity1": "MCT2", "entity2": "monocarboxylates", "span1": [23, 27], "span2": [111, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7995": {"label": 2, "data": {"text": "While SP600125 (a JNK inhibitor) and SB203580 (a p38 inhibitor) markedly prevented the expression of these proteins induced by ISO.", "entity1": "JNK", "entity2": "ISO", "span1": [18, 21], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3419": {"label": 2, "data": {"text": "The treatment with arsenic exhibited a significant increase in some serum hepatic and renal biochemical parameters (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total protein, albumin, bilirubin, cholesterol, urea and creatinine).", "entity1": "alkaline phosphatase", "entity2": "arsenic", "span1": [170, 190], "span2": [19, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4203": {"label": 3, "data": {"text": "PTE, used in combination with a known JAK2/STAT3 inhibitor, AG490, further decreased the viability of osteosarcoma cells.", "entity1": "STAT3", "entity2": "AG490", "span1": [43, 48], "span2": [60, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8811": {"label": 1, "data": {"text": "The Ca2+ sensor STIM1 is crucial for activation of store-operated Ca2+ entry (SOCE) through TRPC and Orai channels.", "entity1": "TRPC", "entity2": "Ca2+", "span1": [92, 96], "span2": [4, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2072": {"label": 8, "data": {"text": "Apolipoprotein E3 (apoE3) safeguards pig proximal tubular LLC-PK1 cells against reduction in SGLT1 activity induced by gentamicin C.\tMegalin, a family of endocytic receptors related to the low-density lipoprotein (LDL) receptor, is a major pathway for proximal tubular aminoglycoside accumulation.", "entity1": "low-density lipoprotein (LDL) receptor", "entity2": "aminoglycoside", "span1": [189, 227], "span2": [269, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8551": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "HDAC", "entity2": "benzene", "span1": [180, 184], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6105": {"label": 8, "data": {"text": "These events are stimulated by NE and by guanethidine, an hNET substrate, and they are blocked by cocaine and the antidepressant desipramine.", "entity1": "hNET", "entity2": "NE", "span1": [58, 62], "span2": [31, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6616": {"label": 8, "data": {"text": "Thus, the current study suggests that coadministration of clinical doses of promethazine and homochlorcyclizine increases the Css of haloperidol and reduced haloperidol via the inhibitory effects on the CYP2D6-catalyzed metabolism of haloperidol and reduced haloperidol.", "entity1": "CYP2D6", "entity2": "haloperidol", "span1": [203, 209], "span2": [234, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4724": {"label": 3, "data": {"text": "Thus, the TCDD-induced reduction in canonical Wnt signaling is associated with a decrease in activators (Rspo2 and Rspo3) rather than an increase in inhibitors (Dkk1 and Dkk2) of the pathway.", "entity1": "Wnt", "entity2": "TCDD", "span1": [46, 49], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1760": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "EGFR", "entity2": "GW572016", "span1": [39, 43], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9793": {"label": 3, "data": {"text": "New modes of therapy have recently been introduced, and data on the cyclooxygenase-2 (COX-2)-specific inhibitors celecoxib and rofecoxib suggest that these agents will meet the need for safe and effective therapeutic alternatives to conventional NSAIDs.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [86, 91], "span2": [127, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7771": {"label": 1, "data": {"text": "Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-\u03b1 pharmacology.", "entity1": "TNF-\u03b1", "entity2": "GDC-0152", "span1": [72, 77], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4984": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bax", "entity2": "Crocin", "span1": [151, 154], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13798": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "kinase", "entity2": "Imatinib mesylate", "span1": [31, 37], "span2": [60, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6292": {"label": 5, "data": {"text": "In distinction, the preferential beta 1-AR antagonist, betaxolol, and the preferential beta 2-AR antagonist, ICI118,551, did not increase basal levels of DA, NAD, or 5-HT.", "entity1": "beta 1-AR", "entity2": "betaxolol", "span1": [33, 42], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11527": {"label": 8, "data": {"text": "Estrogens are biosynthesised from androgens by the CYP450 enzyme complex called aromatase.", "entity1": "aromatase", "entity2": "androgens", "span1": [80, 89], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2760": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "human COX-2", "entity2": "2-chloro-6-methyl", "span1": [75, 86], "span2": [125, 142]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1698": {"label": 3, "data": {"text": "BACKGROUND: Rivastigmine is a carbamate drug designed to inhibit both acetylcholinesterase and butyrylcholinesterase by reversibly covalently bonding to these enzymes.", "entity1": "butyrylcholinesterase", "entity2": "carbamate", "span1": [95, 116], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14060": {"label": 3, "data": {"text": "RESULTS: Aspirin reduced mTOR signaling in CRC cells by inhibiting the mTOR effectors S6K1 and 4E-BP1.", "entity1": "4E-BP1", "entity2": "Aspirin", "span1": [95, 101], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"858": {"label": 0, "data": {"text": "The functional protein contains 1160 amino acids with a large central mucin domain, three consensus sites for glycosaminoglycan attachment, two epidermal growth factor-like repeats, a putative hyaluronan-binding motif, and a potential transmembrane domain near the C-terminal.", "entity1": "mucin domain", "entity2": "amino acids", "span1": [70, 82], "span2": [37, 48]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6245": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-ht1f", "entity2": "sumatriptan", "span1": [135, 141], "span2": [17, 28]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3210": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "phenolic acids", "span1": [248, 261], "span2": [12, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13228": {"label": 1, "data": {"text": "Down-regulation of GRIP1 by glutamate was blocked by carbobenzoxyl-leucinyl-leucinyl-leucinal (MG132), a proteasome inhibitor and by expression of K48R-ubiquitin, a dominant negative form of ubiquitin.", "entity1": "GRIP1", "entity2": "MG132", "span1": [19, 24], "span2": [95, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9989": {"label": 3, "data": {"text": "When the anti-corticosterone drug aminoglutethimide (CYP11A1 inhibitor) was administered to B16F10 mice, corticosterone levels in splenic tissue or serum and CYP11A1 mRNA expression were decreased at 14 days after tumor inoculation.", "entity1": "CYP11A1", "entity2": "aminoglutethimide", "span1": [158, 165], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13213": {"label": 9, "data": {"text": "Triflusal (30 mg/kg) also significantly decreased the protein levels of IL-Ibeta but not nuclear factor kappa B or tumor necrosis factor-alpha in the cortex ipsilateral to the middle cerebral artery occlusion.", "entity1": "nuclear factor kappa B", "entity2": "Triflusal", "span1": [89, 111], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5965": {"label": 3, "data": {"text": "Ambenonium is known to be an inhibitor of acetylcholinesterase, and recent data have shown this drug to antagonize muscarinic receptors as well.", "entity1": "acetylcholinesterase", "entity2": "Ambenonium", "span1": [42, 62], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6915": {"label": 8, "data": {"text": "PSMA acts as a glutamate carboxypeptidase (GCPII) on small molecule substrates, including folate, the anticancer drug methotrexate, and the neuropeptide N-acetyl-l-aspartyl-l-glutamate.", "entity1": "glutamate carboxypeptidase", "entity2": "N-acetyl-l-aspartyl-l-glutamate", "span1": [15, 41], "span2": [153, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5644": {"label": 3, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "hERG", "entity2": "Arsenic trioxide", "span1": [25, 29], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14062": {"label": 3, "data": {"text": "mTOR was still inhibited by aspirin in CRC cells after siRNA knockdown of AMPKalpha, indicating AMPK-dependent and AMPK-independent mechanisms of aspirin-induced inhibition of mTOR.", "entity1": "mTOR", "entity2": "aspirin", "span1": [176, 180], "span2": [146, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13302": {"label": 3, "data": {"text": "The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors.", "entity1": "PDGFRbeta", "entity2": "sorafenib", "span1": [46, 55], "span2": [15, 24]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11390": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "isosorbide dinitrate", "span1": [143, 148], "span2": [80, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2267": {"label": 2, "data": {"text": "Withdrawal from free-choice ethanol consumption results in increased packing density of glutamine synthetase-immunoreactive astrocytes in the prelimbic cortex of alcohol-preferring rats.", "entity1": "glutamine synthetase", "entity2": "ethanol", "span1": [88, 108], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"343": {"label": 3, "data": {"text": "Sodium salicylate and aspirin also inhibited NF-kappa B-dependent transcription from the Ig kappa enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells.", "entity1": "Ig kappa", "entity2": "Sodium salicylate", "span1": [89, 97], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10452": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "(L-serine dehydratase", "entity2": "pyruvate", "span1": [4, 25], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3045": {"label": 8, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "prostaglandin E synthases", "entity2": "PGE(2)", "span1": [73, 98], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3980": {"label": 2, "data": {"text": "The CYP3A4 activity could be induced 2-fold by rifampicin, whereas CYP2C9 activity remained equally high.", "entity1": "CYP2C9", "entity2": "rifampicin", "span1": [67, 73], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8305": {"label": 0, "data": {"text": "USP7 binds directly to the supervillin N terminus and can deubiquitinate and stabilize supervillin.", "entity1": "supervillin", "entity2": "N", "span1": [27, 38], "span2": [39, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12950": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "SR-121463", "span1": [39, 59], "span2": [180, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7082": {"label": 2, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "TRPV3", "entity2": "camphor", "span1": [101, 106], "span2": [25, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12668": {"label": 1, "data": {"text": "In conclusion, OMCD tubules from deoxycorticosterone pivalate-treated rats secrete Cl- into the luminal fluid through NKCC1-mediated Cl- uptake across the basolateral membrane in series with Cl- efflux across the apical membrane.", "entity1": "NKCC1", "entity2": "deoxycorticosterone pivalate", "span1": [118, 123], "span2": [33, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2986": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Q817A", "entity2": "vardenafil", "span1": [216, 221], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15676": {"label": 3, "data": {"text": "Moreover, curcumin could also down-regulate the expression and activity of matrix metalloproteinase-9 (MMP-9).", "entity1": "MMP-9", "entity2": "curcumin", "span1": [103, 108], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12002": {"label": 2, "data": {"text": "Interestingly, the CP[c]Ph dependent up-regulation of CYP1A mRNA is positively correlated with the incidences of clastogenic changes in rainbow trout erythrocytes.", "entity1": "CYP1A", "entity2": "CP[c]Ph", "span1": [54, 59], "span2": [19, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2644": {"label": 8, "data": {"text": "The latter reaction, catalyzed by aspartoacylase (ASPA), produces acetyl groups plus aspartate and has been proposed to occur in both soluble and membranous subfractions of white matter.", "entity1": "ASPA", "entity2": "acetyl", "span1": [50, 54], "span2": [66, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"11197": {"label": 2, "data": {"text": "The BH(4) treatment also partially improved the insulin sensitivity and blood pressure, as well as the serum triglyceride concentration, in the fructose-fed rats.", "entity1": "insulin", "entity2": "BH(4)", "span1": [48, 55], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15998": {"label": 2, "data": {"text": "Puerarin stimulates proliferation and differentiation and protects against cell death in human osteoblastic MG-63 cells via ER-dependent MEK/ERK and PI3K/Akt activation.", "entity1": "ERK", "entity2": "Puerarin", "span1": [141, 144], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13954": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g. isoprenaline) had little affinity-selectivity.", "entity1": "beta(3)", "entity2": "isoprenaline", "span1": [76, 83], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15045": {"label": 8, "data": {"text": "Its head-space aroma displayed new volatile phytomolecules and also had higher levels of green volatiles from the lipoxygenase (LOX)-pathway (one having as precursors the polyunsaturated fatty acids containing a cis-cis-1,4-pentadiene system).", "entity1": "lipoxygenase", "entity2": "cis-cis-1,4-pentadiene", "span1": [114, 126], "span2": [212, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2809": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "VEGF", "entity2": "1400W dihydrochloride", "span1": [198, 202], "span2": [96, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8851": {"label": 1, "data": {"text": "I3S increased expression of ROR\u03b3t, the master transcription factor for Th17 differentiation, and stimulated Th17 differentiation, in a comparative manner as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), a prototypical AhR ligand.", "entity1": "AhR", "entity2": "TCDD", "span1": [216, 219], "span2": [194, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9335": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "[3H]-kainate", "span1": [72, 77], "span2": [48, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7872": {"label": 3, "data": {"text": "Pharmacokinetics and metabolism of [(14)C]anagliptin, a novel dipeptidyl peptidase-4 inhibitor, in humans.", "entity1": "dipeptidyl peptidase-4", "entity2": "[(14)C]anagliptin", "span1": [62, 84], "span2": [35, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11968": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "pip5k1\u03b2", "entity2": "phosphatidylinositol 4-phosphate", "span1": [68, 75], "span2": [159, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2505": {"label": 3, "data": {"text": "The potent and selective third-generation aromatase inhibitors anastrozole, letrozole and exemestane were introduced to the market as endocrine therapy in postmenopausal patients failing anti-estrogen therapy alone, or multiple hormonal therapies.", "entity1": "aromatase", "entity2": "letrozole", "span1": [42, 51], "span2": [76, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"624": {"label": 3, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "IL-2", "entity2": "arachidonyl trifluoromethyl ketone", "span1": [117, 121], "span2": [56, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4536": {"label": 3, "data": {"text": "Our recent study has demonstrated that coadministration of monoamine oxidase A (MAO-A) inhibitor harmaline (5 mg/kg) increases systemic exposure to 5-MeO-DMT (2 mg/kg) and active metabolite bufotenine.", "entity1": "MAO-A", "entity2": "harmaline", "span1": [80, 85], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2902": {"label": 3, "data": {"text": "In vitro, acetaminophen elicited a 4.4-fold selectivity toward COX-2 inhibition (IC(50)=113.7 micromol/L for COX-1; IC(50)=25.8 micromol/L for COX-2).", "entity1": "COX-2", "entity2": "acetaminophen", "span1": [63, 68], "span2": [10, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9200": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "epidermal growth factor", "entity2": "N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide", "span1": [236, 259], "span2": [58, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3537": {"label": 2, "data": {"text": "Exposure to Cu NPs decreased cell viability to 73% (p<0.01) and significantly (p<0.05) elevated levels of lactate dehydrogenase, intracellular reactive oxygen species and interleukin-8 that mirrored our findings from subacute in vivo inhalation studies in mice.", "entity1": "interleukin-8", "entity2": "Cu", "span1": [171, 184], "span2": [12, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11769": {"label": 0, "data": {"text": "Furthermore, orbitrap MS data support the adduction of Cys-113 in the Pin1 active site upon HNE treatment of MDA-MB-231 cells.", "entity1": "Pin1", "entity2": "Cys", "span1": [70, 74], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15321": {"label": 5, "data": {"text": "(2R)-IKM-159 locks the GluA2 in an open form, consistent with a pharmacological action as competitive antagonist of AMPA receptors.", "entity1": "AMPA receptors", "entity2": "(2R)-IKM-159", "span1": [116, 130], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10627": {"label": 3, "data": {"text": "While fluoropyrimidine antimetabolites have other sites of action, antifolates ZD1694 (raltitrexed, Tomudex) and AG337 (Thymitag) are more specific and potent TS inhibitors.", "entity1": "TS", "entity2": "raltitrexed", "span1": [159, 161], "span2": [87, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9682": {"label": 1, "data": {"text": "6 In conclusion, HERG channel inhibition by cisapride exhibits features consistent with open and inactivated state binding and is sensitive to external potassium concentration.", "entity1": "HERG", "entity2": "potassium", "span1": [17, 21], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6127": {"label": 1, "data": {"text": "Role of tachykinin and bradykinin receptors and mast cells in gaseous formaldehyde-induced airway microvascular leakage in rats.", "entity1": "tachykinin and bradykinin receptors", "entity2": "formaldehyde", "span1": [8, 43], "span2": [70, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4468": {"label": 3, "data": {"text": "Catalpol reduced the expression of pro-inflammatory mediates, such as monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-\u03b1 (TNF-\u03b1), inducible NO synthase (iNOS), and receptor for AGE (RAGE).", "entity1": "inducible NO synthase", "entity2": "Catalpol", "span1": [143, 164], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12675": {"label": 0, "data": {"text": "Moreover, certain basic residues of this site, particularly Arg(165) and Lys(169), play a key role in factor Va and/or prothrombin recognition by factor Xa in the prothrombinase complex.", "entity1": "factor Xa", "entity2": "Arg", "span1": [146, 155], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1436": {"label": 3, "data": {"text": "This observation suggests that MDMA-induced reductions in SERT density do not represent neuroadaptive responses to decreased levels of brain serotonin, but may occur in response to some other stimulus or to the neurotoxic effects of MDMA.", "entity1": "SERT", "entity2": "MDMA", "span1": [58, 62], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9223": {"label": 3, "data": {"text": "Three lines of evidence suggest that calmodulin inhibition is not responsible for the inhibition of binding and endocytosis: 1) Promethazine, a phenothiazine that is a poor inhibitor of calmodulin, is nearly as effective as TFP at inhibiting endocytosis; calmidazolium, a potent inhibitor of several calmodulin functions, did not cause a loss of binding; 2) the microinjection of calmodulin into cells did not reverse the effects of W-7; using pressure microinjection, we introduced up to a 100-fold excess of calmodulin over native levels into individual gerbil fibroma cells; using rhodamine-labeled alpha 2-macroglobulin, we saw that the W-7 induced inhibition of receptor-mediated endocytosis was the same in injected and uninjected cells; 3) we injected calcineurin, a calmodulin-binding protein, into cells (1-3 pg/cell) and observed no effect on the receptor-mediated endocytosis of rhodamine-labeled alpha 2-macroglobulin.", "entity1": "calmodulin", "entity2": "phenothiazine", "span1": [300, 310], "span2": [144, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6679": {"label": 3, "data": {"text": "The pretreatment with salbutamol induced a 59% down-regulation of left ventricular beta(2)-adrenoceptors compared to control.", "entity1": "beta(2)-adrenoceptors", "entity2": "salbutamol", "span1": [83, 104], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12753": {"label": 2, "data": {"text": "The c-Jun absorbed light value/GAPDH absorbed light value of mesenteric arteries in the SHR group was 0.850+/-0.015, which was significantly higher than that in the WKY, imidapril, and irbesartan groups (0.582+/-0.013, 0.743+/-0.012, and 0.789+/-0.013, respectively, P<0.01), and was significantly lower in imidapril group than in irbesartan group (P<0.05).", "entity1": "GAPDH", "entity2": "irbesartan", "span1": [31, 36], "span2": [185, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15978": {"label": 5, "data": {"text": "We have recently reported that a mono-hydroxylated metabolite of the synthetic aminoalkylindole cannabinoid JHW-073 (3) exhibits neutral antagonist activity at CB1Rs and thus may serve as a promising lead for the development of novel alcohol abuse therapies.", "entity1": "CB1Rs", "entity2": "aminoalkylindole", "span1": [160, 165], "span2": [79, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5610": {"label": 1, "data": {"text": "Modulation of HERG inactivation was achieved by either changing extracellular K+ or Cs+ concentrations or by mutations of the channel.", "entity1": "HERG", "entity2": "K+", "span1": [14, 18], "span2": [78, 80]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12311": {"label": 8, "data": {"text": "This prompted the design of variants of BChE which exhibit significantly improved catalytic activity against (-)-cocaine.", "entity1": "BChE", "entity2": "(-)-cocaine", "span1": [40, 44], "span2": [109, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10895": {"label": 1, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "Pyridoxal kinase", "entity2": "ATP", "span1": [0, 16], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12820": {"label": 1, "data": {"text": "It could also aid in the design of roscovitine derivatives displaying strict selectivity for either PDXK or CDKs.", "entity1": "PDXK", "entity2": "roscovitine", "span1": [100, 104], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4533": {"label": 3, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "CYP2D6", "entity2": "harmaline", "span1": [80, 86], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13585": {"label": 1, "data": {"text": "Initial evaluation of the pharmacological properties of DVS (J Pharmacol Exp Ther 318:657-665, 2006) revealed significantly reduced potency for the hNET expressed in membranes compared with whole cells when competing for [(3)H]nisoxetine (NIS) binding.", "entity1": "hNET", "entity2": "NIS", "span1": [148, 152], "span2": [239, 242]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9731": {"label": 1, "data": {"text": "Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors.", "entity1": "h5-HT(1A)", "entity2": "Yohimbine", "span1": [116, 125], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9687": {"label": 1, "data": {"text": "Ziprasidone is a novel antipsychotic agent which binds with high affinity to 5-HT1A receptors (Ki = 3.4 nM), in addition to 5-HT1D, 5-HT2, and D2 sites.", "entity1": "5-HT2", "entity2": "Ziprasidone", "span1": [132, 137], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2626": {"label": 3, "data": {"text": "The demonstration that sorafenib exhibits potent target inhibition and efficacy in FLT3-driven models suggests that this compound may have a therapeutic benefit for patients with FLT3-driven leukemias.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [179, 183], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3212": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "phenolic acids", "span1": [282, 284], "span2": [12, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5977": {"label": 8, "data": {"text": "Present studies demonstrate that mushroom tyrosinase will also catalyze quinone methide production with the same active site copper if a suitable substrate such as 3,4-dihydroxymandelic acid is provided.", "entity1": "mushroom tyrosinase", "entity2": "quinone methide", "span1": [33, 52], "span2": [72, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, 8, -1, -1]},
	"9198": {"label": 1, "data": {"text": "The extent of EGF receptor loss is less than for alpha 2-macroglobulin, and the EGF receptors do not reappear at the surface when W-7 is removed.", "entity1": "EGF receptor", "entity2": "W-7", "span1": [14, 26], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2896": {"label": 5, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1A)-adrenoceptor", "entity2": "silodosin", "span1": [79, 101], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5603": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "olanzapine", "span1": [59, 65], "span2": [139, 149]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11692": {"label": 2, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "tumor necrosis factor alpha", "entity2": "pioglitazone", "span1": [124, 151], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8986": {"label": 3, "data": {"text": "The smooth muscle relaxant, W-7, which is believed relatively specific in inhibiting the Ca2(+)-calmodulin interaction, depressed hyposmolarity-induced PRL secretion in a dose-dependent manner (r = -0.991, p less than 0.01).", "entity1": "PRL", "entity2": "W-7", "span1": [152, 155], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"592": {"label": 9, "data": {"text": "The action of 15d-PGJ2 does not appear to involve its nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) because troglitazone, a specific ligand of PPARgamma, was unable to inhibit iNOS induction, and neither troglitazone nor 15d-PGJ2 could stimulate the activity of a PPAR-dependent promoter in the absence of cotransfected PPARgamma.", "entity1": "PPARgamma", "entity2": "15d-PGJ2", "span1": [121, 130], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15405": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "HMGCoA", "entity2": "7-ketosterols", "span1": [219, 225], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"91": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "EC 1.14.16.1", "entity2": "noradrenaline", "span1": [139, 151], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8357": {"label": 3, "data": {"text": "Amino acid derived quinazolines as Rock/PKA inhibitors.", "entity1": "Rock", "entity2": "Amino acid", "span1": [35, 39], "span2": [0, 10]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3232": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "phenol", "span1": [282, 284], "span2": [31, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5372": {"label": 1, "data": {"text": "The latter is the first in vivo open-ring metabolite of rapamycin that does not affect mTOR.", "entity1": "mTOR", "entity2": "rapamycin", "span1": [87, 91], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"472": {"label": 9, "data": {"text": "Thus, in functional experiments the presumed high selectivity of risperidone for the B subtype of alpha 1-adrenoceptors could not be confirmed, the drug instead appears to be moderately selective (10-fold) for the A subtype.", "entity1": "alpha 1-adrenoceptors", "entity2": "risperidone", "span1": [98, 119], "span2": [65, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3605": {"label": 3, "data": {"text": "At a low pH (pH 7.4), but not pH 7.9, ifenprodil reduces the mean open time of GluN1/GluN2B receptors, which may be responsible for its usefulness as a context-dependent inhibitor in conditions like ischemia and stroke, when the pH of the extracellular milieu becomes acidic.", "entity1": "GluN2B", "entity2": "ifenprodil", "span1": [85, 91], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12834": {"label": 3, "data": {"text": "This effect was reverted in the presence of atropine (ATR; 0.1 microM), which blocks the pre-synaptic muscarinic M2 receptor.", "entity1": "muscarinic M2 receptor", "entity2": "ATR", "span1": [102, 124], "span2": [54, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9528": {"label": 3, "data": {"text": "Nisoldipine (a DHP antagonist) blocks the smooth muscle channel more potently than the cardiac one, a phenomenon observed not only in native channels but also in expressed channels.", "entity1": "smooth muscle channel", "entity2": "DHP", "span1": [42, 63], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8229": {"label": 2, "data": {"text": "Although ICA greatly attenuates ERG inactivation by shifting its voltage dependence to more positive potentials, it enhances the rate and extent of EAG inactivation without altering its voltage dependence.", "entity1": "ERG", "entity2": "ICA", "span1": [32, 35], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7909": {"label": 2, "data": {"text": "We found that helenalin markedly induced endoplasmic reticulum (ER) stress-related genes, such as regulated in development and DNA damage responses (REDD) 1, activating transcription factor-4 (ATF4) and/or the CCAAT enhancer-binding protein-homologous protein (CHOP).", "entity1": "activating transcription factor-4", "entity2": "helenalin", "span1": [158, 191], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15638": {"label": 3, "data": {"text": "Data also showed nobiletin inhibited HGF-induced cell scattering and cytoskeleton changed such as filopodia and lamellipodia.", "entity1": "HGF", "entity2": "nobiletin", "span1": [37, 40], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14932": {"label": 1, "data": {"text": "Further studies of the role of these steroids and SERMs in regulating responses mediated by ER\u03b1 and ER\u03b2 a variety of tissues, during different stages of development, are likely to uncover additional estrogenic activities.", "entity1": "ER\u03b1", "entity2": "steroids", "span1": [92, 95], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7923": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "carboplatin", "span1": [54, 59], "span2": [143, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2010": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Pro", "span1": [121, 125], "span2": [104, 107]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14498": {"label": 1, "data": {"text": "Estrogen effects are mediated not only through nuclear ERs but also through cytoplasmic/membrane ERs and G-protein-coupled ERs.", "entity1": "ERs", "entity2": "Estrogen", "span1": [123, 126], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15919": {"label": 4, "data": {"text": "Reactive Metabolite Trapping Studies on Imidazo- and 2-Methylimidazo[2,1-b]thiazole-based Inverse Agonists of the Ghrelin Receptor.", "entity1": "Ghrelin Receptor", "entity2": "Imidazo- and 2-Methylimidazo[2,1-b]thiazole", "span1": [114, 130], "span2": [40, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5555": {"label": 2, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "NF-kappaB", "entity2": "BCNU", "span1": [173, 182], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10022": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Arg", "span1": [199, 208], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3207": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "ferulic acid", "span1": [262, 280], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4619": {"label": 2, "data": {"text": "Chronic consumption of alcohol also stimulated abrupt increases in pro-inflammatory cytokines such as nuclear factor (NF)-\u03baB, tumor necrosis factor (TNF)-\u03b1 and interleukin (IL)-1\u03b2 in liver otherwise co-administration of CNF effectively suppressed production of these cytokines dose-dependently.", "entity1": "interleukin (IL)-1\u03b2", "entity2": "alcohol", "span1": [160, 179], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3422": {"label": 0, "data": {"text": "The Met790 side chain of the G719S/T790M double mutant, in the apo form and gefitinib- and AMPPNP-bound forms, adopts different conformations that explain the accommodation of these ligands.", "entity1": "G719S", "entity2": "Met", "span1": [29, 34], "span2": [4, 7]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"804": {"label": 2, "data": {"text": "Specifically, aniracetam, which potentiates wild-type AMPA receptors, is ineffective on the non-desensitizing GluR3(L507Y) mutant, but has synergistic effects with lithium on wild-type receptors.", "entity1": "AMPA receptors", "entity2": "aniracetam", "span1": [54, 68], "span2": [14, 24]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11607": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "cystathionine-gamma-lyase", "entity2": "L-cysteine", "span1": [75, 100], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12373": {"label": 8, "data": {"text": "Carnitine palmitoyltransferase 2 and carnitine/acylcarnitine translocase are involved in the mitochondrial synthesis and export of acylcarnitines.", "entity1": "carnitine/acylcarnitine translocase", "entity2": "acylcarnitines", "span1": [37, 72], "span2": [131, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15694": {"label": 1, "data": {"text": "Conclusion The results of this work contribute information regarding the antinociceptive properties of CAT on acute pain and show that, at least in part, TRPV1, TRPM8, ASIC, glutamate receptors, PKC and PKA participate in CAT's antinociceptive mechanism.", "entity1": "glutamate receptors", "entity2": "CAT", "span1": [174, 193], "span2": [222, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7382": {"label": 4, "data": {"text": "(2) Does in vivo administration of (R)-(alpha)-(-)-methylhistamine dihydrobromide (RAMH) (H3R agonist), thioperamide maleate (H3R antagonist) or histamine, in the absence/presence of thioperamide maleate, to bile duct ligated (BDL) rats regulate cholangiocyte proliferation?", "entity1": "H3R", "entity2": "RAMH", "span1": [90, 93], "span2": [83, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6221": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "human 5-HT1B", "entity2": "naratriptan", "span1": [101, 113], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8301": {"label": 2, "data": {"text": "Today, we used cobalt chloride, a hypoxia mimetic that inhibits proteasomal HIF-1 degradation and generates reactive oxygen species (ROS).", "entity1": "HIF-1", "entity2": "cobalt chloride", "span1": [76, 81], "span2": [15, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7548": {"label": 3, "data": {"text": "Phenelzine (PLZ), a nonselective irreversible inhibitor of monoamine oxidase (MAO), also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels.", "entity1": "GABA-transaminase", "entity2": "PLZ", "span1": [98, 115], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8863": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "STAT3", "entity2": "TCDD", "span1": [438, 443], "span2": [327, 331]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"671": {"label": 0, "data": {"text": "The deduced amino acid sequence contains 779 amino acids, including a putative cGMP binding sequence in the amino-terminal portion of the molecule and a catalytic domain that is 16-47% identical in amino acid sequence to those of other PDE families.", "entity1": "PDE", "entity2": "amino acid", "span1": [236, 239], "span2": [12, 22]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9865": {"label": 8, "data": {"text": "However, the role of NQO1 in metabolic activation of MMC has been disputed.", "entity1": "NQO1", "entity2": "MMC", "span1": [21, 25], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9458": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "17-phenyl-PGE2", "span1": [4, 7], "span2": [137, 151]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11063": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "prednisone", "span1": [89, 95], "span2": [302, 312]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4685": {"label": 1, "data": {"text": "Modulation of cytochrome P450 1 (Cyp1) by vanadium in hepatic tissue and isolated hepatocyte of C57BL/6 mice.", "entity1": "Cyp1", "entity2": "vanadium", "span1": [33, 37], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12713": {"label": 2, "data": {"text": "However, when coapplied with 10 micro m GABA, ivermectin potentiated the GABA-evoked current of the GAB-1/HG1A receptor, but attenuated the GABA response of the GAB-1/HG1E receptor.", "entity1": "HG1A", "entity2": "ivermectin", "span1": [106, 110], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6841": {"label": 1, "data": {"text": "Differences in cobalamin and folate levels with the MTRR A66G and MS A2756G polymorphisms were noted.", "entity1": "A66G", "entity2": "cobalamin", "span1": [57, 61], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12424": {"label": 1, "data": {"text": "Here, we report the first crystal structure of KIF4 complexed with the non-hydrolyzable ATP analog, AMPPNP (adenylyl imidodiphosphate), at 1.7\u00c5 resolution.", "entity1": "KIF4", "entity2": "ATP", "span1": [47, 51], "span2": [88, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16050": {"label": 1, "data": {"text": "By contrast, the editing of some sites is completely lost or significantly reduced in other non-green tissues; for instance, the editing of ndhB-149, ndhB-1255, and ndhD-2 is completely lost in roots and in lincomycin-treated seedlings.", "entity1": "ndhD-2", "entity2": "lincomycin", "span1": [165, 171], "span2": [207, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5855": {"label": 5, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT3", "entity2": "zacopride", "span1": [5, 10], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5349": {"label": 2, "data": {"text": "These findings suggest that S1P activates the PI3K/Akt signaling pathway leading to the promotion of nuclear translocation of \u03b2-catenin in osteoblast-like cells, resulting in the upregulation of osteoptotegerin and osteoblast differentiation markers including alkaline phosphatase, probably relating to the inhibition of osteoclast formation and the mineralization, respectively.", "entity1": "alkaline phosphatase", "entity2": "S1P", "span1": [260, 280], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4": {"label": 5, "data": {"text": "Labetalol (> or = 3 x 10(-8) M) and dilevalol (> or = 10(-8) M) caused surmountable antagonism of the isoprenaline responses of the atria and the pA2 values were 8.60 and 8.98 at the beta 1-adrenoceptors of the rat left atria and 7.90 and 8.31, respectively, on the guinea-pig left atria which has functional beta 1- and beta 2-adrenoceptors.", "entity1": "beta 1-adrenoceptors", "entity2": "Labetalol", "span1": [183, 203], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3113": {"label": 5, "data": {"text": "Ambrisentan is an endothelin type A (ET(A))-selective receptor antagonist that is metabolized primarily by glucuronidation but also undergoes oxidative metabolism by CYP3A4.", "entity1": "endothelin type A (ET(A))-selective receptor", "entity2": "Ambrisentan", "span1": [18, 62], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"824": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "PGE2", "span1": [258, 275], "span2": [292, 296]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1993": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Cys", "span1": [121, 125], "span2": [108, 111]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3398": {"label": 9, "data": {"text": "To further characterize the inhibitory mechanisms of PSE at the transcriptional level, we examined the transcriptional activities of nuclear factor kappa B (NF-kappaB), nuclear factor of activated T cells (NFAT), and activator protein-1 (AP-1) transcription factors and found that PSE inhibited NF-kappaB-dependent transcriptional activity without affecting either the phosphorylation, the degradation of the cytoplasmic NF-kappaB inhibitory protein, IkappaBalpha or the DNA-binding activity.", "entity1": "IkappaBalpha", "entity2": "PSE", "span1": [451, 463], "span2": [281, 284]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2186": {"label": 7, "data": {"text": "Co-C bond activation in methylmalonyl-CoA mutase by stabilization of the post-homolysis product Co2+ cobalamin.", "entity1": "methylmalonyl-CoA mutase", "entity2": "cobalamin", "span1": [24, 48], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10899": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "cyclin-dependent kinases", "entity2": "(R)-Roscovitine", "span1": [76, 100], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8118": {"label": 3, "data": {"text": "Both CE and E(2) alone increased DNA synthesis and reduced apoptosis with activation of MAPK, Akt, and p70S6K and up-regulation of antiapoptotic factors survivin, Bcl-2, and X-linked inhibitor of apoptosis protein, These effects could be completely blocked by BZA.", "entity1": "Bcl-2", "entity2": "BZA", "span1": [163, 168], "span2": [260, 263]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2076": {"label": 2, "data": {"text": "Synergistic cytotoxicity was demonstrated, and pemetrexed significantly decreased the amount of phosphorylated Akt, enhanced apoptosis, and increased the expression of dCK in A549 and Calu-6 cells, as well as the expression of the human nucleoside equilibrative transporter 1 (hENT1) in all cell lines.", "entity1": "hENT1", "entity2": "pemetrexed", "span1": [277, 282], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"968": {"label": 3, "data": {"text": "Expression of the dominant negative mutants arrestin-2(319-418) or dynamin I-K44A significantly reduced U50,488H-induced down-regulation of the hkor.", "entity1": "hkor", "entity2": "U50,488H", "span1": [144, 148], "span2": [104, 112]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6676": {"label": 3, "data": {"text": "In addition, minocycline treatment significantly reduced the specific caspase-3 activity after SCI as compared to that of vehicle control.", "entity1": "caspase-3", "entity2": "minocycline", "span1": [70, 79], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10725": {"label": 1, "data": {"text": "Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin.", "entity1": "oxytocin receptor", "entity2": "barusiban", "span1": [23, 40], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7516": {"label": 2, "data": {"text": "KEY RESULTS: Phenformin, AICAR and metformin increased AMPK (alpha1) activity and decreased I(amiloride).", "entity1": "AMPK (alpha1)", "entity2": "AICAR", "span1": [55, 68], "span2": [25, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15725": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b1", "entity2": "pentylparaben", "span1": [142, 145], "span2": [100, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10910": {"label": 8, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "PDXK", "entity2": "pyridoxine", "span1": [18, 22], "span2": [86, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13767": {"label": 3, "data": {"text": "A comparison of bosutinib with dasatinib across the whole kinase panel revealed overlapping, but distinct, inhibition profiles.", "entity1": "kinase", "entity2": "bosutinib", "span1": [58, 64], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13647": {"label": 0, "data": {"text": "The binding of U46619 to the PGIS protein was demonstrated by 1D NMR titration, and the significant perturbation of the chemical shifts of protons at C-11, H2C, and H20 of U46619 were observed upon U46619 binding to the engineered PGIS in a concentration-dependent manner.", "entity1": "PGIS", "entity2": "C-11", "span1": [29, 33], "span2": [150, 154]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3442": {"label": 4, "data": {"text": "These results confirm the selective mGlu2 agonist and mGlu3 antagonist actions of LY541850.", "entity1": "mGlu2", "entity2": "LY541850", "span1": [36, 41], "span2": [82, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1309": {"label": 3, "data": {"text": "It was also antagonized by the non-specific cyclooxygenase (COX) inhibitor, indomethacin, and by the selective COX-2 inhibitor, NS-398, but not by the specific COX-1 inhibitor, valeryl salicylate.", "entity1": "COX-1", "entity2": "valeryl salicylate", "span1": [160, 165], "span2": [177, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2576": {"label": 2, "data": {"text": "Pretreatment with dexamethasone significantly suppressed nasal allergy-like behaviors, up-regulation of histamine content, HDC activity and HDC mRNA induced by TDI in TDI-sensitized rats.", "entity1": "HDC", "entity2": "TDI", "span1": [123, 126], "span2": [160, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15718": {"label": 8, "data": {"text": "d-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor.", "entity1": "DAAO", "entity2": "d-serine", "span1": [22, 26], "span2": [79, 87]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11566": {"label": 8, "data": {"text": "Therefore, pretreatment tumor gene expression profiling of ASS and OTC could aid in predicting tumor response to arginine depletion with arginine-depleting enzymes.", "entity1": "arginine-depleting enzymes", "entity2": "arginine", "span1": [137, 163], "span2": [113, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4831": {"label": 2, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "Mcl-1", "entity2": "7KC", "span1": [247, 252], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1138": {"label": 1, "data": {"text": "Significant differences were observed in a different region (loop B93-B101), that we identified as binding site of amiloride to the tissue plasminogen activator (tPA).", "entity1": "tissue plasminogen activator", "entity2": "amiloride", "span1": [132, 160], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8297": {"label": 3, "data": {"text": "LY294002, a specific PI3K/AKT inhibitor, selectively activated the p38 MAPK kinase pathway and enhanced c-Jun phosphorylation, but did not activate JNK.", "entity1": "AKT", "entity2": "LY294002", "span1": [26, 29], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12456": {"label": 2, "data": {"text": "This report concerns the marked up-regulation in differentiated CaCo-2 colonic epithelial cells of two key inflammatory interleukins, IL-6 and IL-8, caused by a mixture of oxysterols representative of a high cholesterol diet.", "entity1": "IL-6", "entity2": "oxysterols", "span1": [134, 138], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2872": {"label": 2, "data": {"text": "We also found that TRPV1 receptors are activated by CuSO(4), ZnSO(4), and FeSO(4), three salts known to produce a metallic taste sensation.", "entity1": "TRPV1", "entity2": "FeSO(4)", "span1": [19, 24], "span2": [74, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5415": {"label": 8, "data": {"text": "In functional transport assays, we found that one of the identified molecules, ATM7, increased the reuptake of serotonin, possibly by facilitating the interaction of serotonin with transport-ready conformations of SERT when concentrations of serotonin were low and rate limiting.", "entity1": "SERT", "entity2": "serotonin", "span1": [214, 218], "span2": [166, 175]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5720": {"label": 8, "data": {"text": "CRPC is characterized by reactivation of the androgen axis due to changes in androgen receptor signaling and/or adaptive intratumoral androgen biosynthesis.", "entity1": "androgen receptor", "entity2": "androgen", "span1": [77, 94], "span2": [134, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"398": {"label": 2, "data": {"text": "Indomethacin abolished the inhibitory effect of acetazolamide on CA I and CA II.", "entity1": "CA I", "entity2": "Indomethacin", "span1": [65, 69], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2021": {"label": 5, "data": {"text": "BACKGROUND: Pranlukast, a cysteinyl leukotriene receptor 1 (CysLTR1) antagonist, inhibits not only airway smooth muscle contraction, but also allergic inflammation.", "entity1": "cysteinyl leukotriene receptor 1", "entity2": "Pranlukast", "span1": [26, 58], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13651": {"label": 0, "data": {"text": "The distances between the protons H20 and H2, H18 and H2, and H18 and H4 are shorter following their binding to the PGIS in solution-down to within 5 A.", "entity1": "PGIS", "entity2": "H20", "span1": [116, 120], "span2": [34, 37]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10006": {"label": 1, "data": {"text": "Domperidone and haloperidol, which have affinity for dopamine D3 receptor, also inhibited R(+)-7-OH-DPAT-induced hypothermia.", "entity1": "dopamine D3 receptor", "entity2": "haloperidol", "span1": [53, 73], "span2": [16, 27]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3409": {"label": 3, "data": {"text": "However, phosphorylation of the p65/RelA subunit was clearly inhibited by PSE in stimulated cells.", "entity1": "RelA", "entity2": "PSE", "span1": [36, 40], "span2": [74, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2491": {"label": 3, "data": {"text": "We examined the anti-inflammatory effect of licofelone on atherosclerotic lesions as well as in isolated neutrophils from whole blood of rabbits compared with a selective inhibitor of COX-2, rofecoxib.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [184, 189], "span2": [191, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11220": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "nateglinide", "span1": [4, 11], "span2": [119, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11053": {"label": 9, "data": {"text": "Similar to the plasma membrane PS transporter, Atp8a1 is activated only by the naturally occurring sn-1,2-glycerol isomer of PS and not the sn-2,3-glycerol stereoisomer.", "entity1": "plasma membrane PS transporter", "entity2": "sn-2,3-glycerol", "span1": [15, 45], "span2": [140, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"2110": {"label": 3, "data": {"text": "On the basis of FIP1L1-PDGFRa fusion gene hypereosinophilic syndrome would be classified as a clonal disease and in the FIP1L1-PDGFRa positive cases the tyrosine kinase inhibitor imatinib mesylate (Glivec) would be effective.", "entity1": "tyrosine kinase", "entity2": "imatinib mesylate", "span1": [153, 168], "span2": [179, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7936": {"label": 3, "data": {"text": "Examination of phosphorylation in retinoblastoma (Rb) protein, we found an inhibitory effect by glucosamine at 20 and 50\u00a0mM.", "entity1": "retinoblastoma (Rb) protein", "entity2": "glucosamine", "span1": [34, 61], "span2": [96, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6863": {"label": 2, "data": {"text": "Pre-irradiation administration of RP-1 enhanced levels of GSH induced increase in complex I (upto 16 h), complex I/III (4 h) complex II/III activity (upto 24 h; p < 0.01) and inhibited the radiation-induced decrease in MMP significantly (24 h; p < 0.01).", "entity1": "complex I/III", "entity2": "GSH", "span1": [105, 118], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12291": {"label": 1, "data": {"text": "Cabozantinib may provide clinical benefit by simultaneously targeting multiple pathways of importance in MTC, including MET, VEGFR2, and RET.", "entity1": "RET", "entity2": "Cabozantinib", "span1": [137, 140], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11099": {"label": 9, "data": {"text": "The R(-) and S(+) isomers of MDMA were significantly less efficacious at the 5-HT2A receptor as compared to MDA; S(+)MDMA had no effect.", "entity1": "5-HT2A", "entity2": "S(+)MDMA", "span1": [77, 83], "span2": [113, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13283": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "receptor tyrosine kinases", "entity2": "Sorafenib", "span1": [168, 193], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7585": {"label": 1, "data": {"text": "Pharmacological and in silico investigations concerning the interactions of these compounds with the hERG channel revealed that compounds carrying a basic nitrogen in the side chain display a much higher affinity than those lacking such a group.", "entity1": "hERG", "entity2": "nitrogen", "span1": [101, 105], "span2": [155, 163]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3356": {"label": 1, "data": {"text": "The structural and functional data reveal that the levosimendan class of Ca(2+)-sensitizers work by binding to the regulatory domain of cTnC and stabilizing the pivotal cTnC-cTnI regulatory unit via a network of hydrophobic and electrostatic interactions, in contrast to the destabilizing effects of antagonists such as W7 at the same interface.", "entity1": "cTnC", "entity2": "levosimendan", "span1": [169, 173], "span2": [51, 63]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"62": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "renin", "entity2": "dipeptide", "span1": [41, 46], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8844": {"label": 2, "data": {"text": "There was also an increase in \u03b3-GCS and HO-1 levels in calycopterin pretreated cells.", "entity1": "HO-1", "entity2": "calycopterin", "span1": [40, 44], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14751": {"label": 3, "data": {"text": "Here we found that arsenic trioxide, a frontline agent for acute promyelocytic leukemia, inhibits \u0394Np63 but not TAp63 expression in time- and dose-dependent manners.", "entity1": "\u0394Np63", "entity2": "arsenic trioxide", "span1": [98, 103], "span2": [19, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"18": {"label": 3, "data": {"text": "Preincubation for 30 minutes with iloprost, ciprostene, and carbacyclin led to a dose-dependent inhibition of tissue factor expression induced by all three challenging agents.", "entity1": "tissue factor", "entity2": "ciprostene", "span1": [110, 123], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14847": {"label": 8, "data": {"text": "Aldehyde dehydrogenase 1 (ALDH1A1) catalyzes the oxidation of toxic aldehydes to carboxylic acids.", "entity1": "ALDH1A1", "entity2": "aldehydes", "span1": [26, 33], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4506": {"label": 3, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES1", "entity2": "(S)-naproxen-\u03b2-d-glucuronide", "span1": [169, 174], "span2": [118, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8557": {"label": 3, "data": {"text": "As a potent synthetic APN inhibitor (IC50=850nM, versus bestatin of 8.1\u03bcM), LB-4b was determined to have more significant block effects to cancer cell invasion and angiogenesis than bestatin.", "entity1": "APN", "entity2": "bestatin", "span1": [22, 25], "span2": [56, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7896": {"label": 2, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "DNMT1", "entity2": "farnesylpyrophosphate", "span1": [126, 131], "span2": [213, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3588": {"label": 1, "data": {"text": "Wogonoside induces autophagy in MDA-MB-231 cells by regulating MAPK-mTOR pathway.", "entity1": "MAPK", "entity2": "Wogonoside", "span1": [63, 67], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1701": {"label": 8, "data": {"text": "Glycylsarcosine coadministration could inhibit the uptake of cefadroxil in PEPT2(+/+) mice (p < 0.01) but not PEPT2(-/-) mice.", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [75, 80], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9035": {"label": 3, "data": {"text": "Inhibition of 5-lipoxygenase pathway of arachidonic acid metabolism in human neutrophils by sulfasalazine and 5-aminosalicylic acid.", "entity1": "5-lipoxygenase", "entity2": "5-aminosalicylic acid", "span1": [14, 28], "span2": [110, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11151": {"label": 0, "data": {"text": "Both forms of the enzyme reacted with a rabbit antibody raised to the amino-terminal peptide of the liver enzyme, suggesting that phosphodiester alpha-GlcNAcase is a type I membrane-spanning glycoprotein with its amino terminus in the lumen of the Golgi apparatus.", "entity1": "type I membrane-spanning glycoprotein", "entity2": "amino", "span1": [166, 203], "span2": [213, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11006": {"label": 3, "data": {"text": "The fact that trimipramine also suppressed IFN-gamma production and T-cell proliferation indicates that these immunomodulatory actions of antidepressants are most likely unrelated to inhibition of monoamine reuptake.", "entity1": "IFN-gamma", "entity2": "trimipramine", "span1": [43, 52], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13485": {"label": 5, "data": {"text": "[N-(piperidin-1-yl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxyamide] (SR 141716A), a selective cannabinoid CB1 receptor antagonist, injected into the paraventricular nucleus of the hypothalamus (PVN) of male rats, induces penile erection.", "entity1": "cannabinoid CB1 receptor", "entity2": "SR 141716A", "span1": [102, 126], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"541": {"label": 3, "data": {"text": "Two mechanisms of action have been identified for A77 1726: inhibition of dihydroorotate dehydrogenase (DHODH) and inhibition of tyrosine kinases.", "entity1": "tyrosine kinases", "entity2": "A77 1726", "span1": [129, 145], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13515": {"label": 1, "data": {"text": "Hydrogen peroxide-mediated oxidative stress disrupts calcium binding on calmodulin: more evidence for oxidative stress in vitiligo.", "entity1": "calmodulin", "entity2": "Hydrogen peroxide", "span1": [72, 82], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9962": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [10, 15], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7807": {"label": 2, "data": {"text": "However, 4'G-RSV, but not 3G-RSV, induced SIRT1-dependent histone H3 deacetylation and SOD2 expression in mouse C2C12 skeletal myoblasts; as with RSV, SIRT1 knockdown blunted these effects.", "entity1": "SOD2", "entity2": "4'G-RSV", "span1": [87, 91], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12985": {"label": 1, "data": {"text": "The effect of folic acid level on this end-point was modulated by the MTHFR genotype (P for interaction = 0.02), with TT cells grown at low folic acid concentration apparently resistant to the induction of radiation-induced bridges.", "entity1": "MTHFR", "entity2": "folic acid", "span1": [70, 75], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3163": {"label": 3, "data": {"text": "Furthermore, the Panx1 channel blockers carbenoxolone and Probenecid were less effective in inhibiting Panx1 currents when Kvbeta3 was co-expressed.", "entity1": "Panx1", "entity2": "carbenoxolone", "span1": [17, 22], "span2": [40, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2279": {"label": 3, "data": {"text": "The work of Chen and colleagues shows that dasatinib is a particularly potent inhibitor of PDGFR and that the compound also targets Src kinase.", "entity1": "Src kinase", "entity2": "dasatinib", "span1": [132, 142], "span2": [43, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8325": {"label": 2, "data": {"text": "In particular, we showed that Paeoniflorin significantly reduced the formation of intracellular reactive oxygen species (ROS), the level of malondialdehyde (MDA) and lactate dehydrogenase (LDH) leakage, and enhanced production of the endogenous antioxidants, glutathione (GSH) and superoxide dismutase (SOD) in EA.hy926 cells.", "entity1": "superoxide dismutase", "entity2": "Paeoniflorin", "span1": [281, 301], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7219": {"label": 3, "data": {"text": "Cd decreased ERalpha expression, but not ERbeta.", "entity1": "ERalpha", "entity2": "Cd", "span1": [13, 20], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12978": {"label": 6, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "PKC", "entity2": "DAG", "span1": [74, 77], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"1232": {"label": 0, "data": {"text": "Radiosequence analysis of [(14)C]halothane-labeled rhodopsin revealed that halothane contacts an amino acid residue (Trp265) lining the ligand binding cavity in the transmembrane core of the receptor.", "entity1": "rhodopsin", "entity2": "amino acid", "span1": [51, 60], "span2": [97, 107]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7229": {"label": 2, "data": {"text": "Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5.", "entity1": "human androgen receptor", "entity2": "testosterone", "span1": [87, 110], "span2": [56, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11834": {"label": 2, "data": {"text": "Dietary EPA/DHA treatment restored endogenous biosynthesis of n-3 derived lipid mediators in obesity while attenuating adipose tissue inflammation and improving insulin sensitivity.", "entity1": "insulin", "entity2": "EPA", "span1": [161, 168], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4614": {"label": 3, "data": {"text": "In this study, a novel series of 2-hydroxydiarylamide derivatives were synthesized and evaluated for inhibiting TMPRSS4 serine protease activity and suppressing cancer cell invasion.", "entity1": "serine protease", "entity2": "2-hydroxydiarylamide", "span1": [120, 135], "span2": [33, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"910": {"label": 1, "data": {"text": "Betaxolol inhibited specific [(3)H]-batrachotoxinin-A 20-alpha-benzoate ([(3)H]-BTX-B) binding to neurotoxin site 2 in a concentration-dependent manner with an IC(50) value of 9.8 microM.", "entity1": "neurotoxin site 2", "entity2": "Betaxolol", "span1": [98, 115], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13782": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Zactima", "span1": [14, 16], "span2": [168, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13059": {"label": 3, "data": {"text": "Similar to AMR and AMROH, adriamycin and etoposide (VP-16) are DNA topoisomerase II inhibitors.", "entity1": "DNA topoisomerase II", "entity2": "AMR", "span1": [63, 83], "span2": [11, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8504": {"label": 1, "data": {"text": "By combining our structure with previously solved KIF1A structures complexed with two ATP analogs, molecular snapshots during ATP binding reveal that the closure of the nucleotide-binding pocket during ATP binding is achieved by closure of the backdoor.", "entity1": "KIF1A", "entity2": "ATP", "span1": [50, 55], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8108": {"label": 3, "data": {"text": "Moreover, wogonin repressed anisomycin-induced phosphorylation of p38, cav-1 and vascular permeability.", "entity1": "p38", "entity2": "wogonin", "span1": [66, 69], "span2": [10, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6939": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "ketorolac", "span1": [81, 86], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5704": {"label": 2, "data": {"text": "Whereas the addition of apomorphine in the low micromolar range produced an irreversible activation of the channel, application of higher concentrations caused a reversible voltage-dependent inhibition of heterologously expressed TRPA1 channels, resulting from a reduction of single-channel open times.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [230, 235], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13493": {"label": 1, "data": {"text": "CONCLUSIONS: Weight reduction with sibutramine is associated with altered gastric functions and increased peptide YY and is significantly associated with SLC6A4 genotype.", "entity1": "SLC6A4", "entity2": "sibutramine", "span1": [154, 160], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8218": {"label": 1, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "EAG", "entity2": "ICA-105574", "span1": [101, 104], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4967": {"label": 3, "data": {"text": "One exception is tranexamic acid (TXA), which, as a lysine mimetic, inhibits binding of plasminogen to fibrin.", "entity1": "fibrin", "entity2": "tranexamic acid", "span1": [103, 109], "span2": [17, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10935": {"label": 5, "data": {"text": "Losartan: a selective angiotensin II type 1 (AT1) receptor antagonist for the treatment of heart failure.", "entity1": "angiotensin II type 1 (AT1) receptor", "entity2": "Losartan", "span1": [22, 58], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14108": {"label": 1, "data": {"text": "The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide.", "entity1": "cereblon", "entity2": "thalidomide", "span1": [45, 53], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5169": {"label": 8, "data": {"text": "At a substrate concentration of 20\u2009\u00b5M, the most active HFC glucuronidation catalysts were UGT1A10 followed by UGT1A6 >UGT1A7 >UGT2A1, whereas at 300\u2009\u00b5M UGT1A6 was about 10 times better catalyst than the other recombinant UGTs.", "entity1": "UGTs", "entity2": "HFC", "span1": [221, 225], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"12174": {"label": 1, "data": {"text": "Vitamin E supplementation alters HDL-cholesterol concentration and paraoxonase activity in rabbits fed high-cholesterol diet: comparison with probucol.", "entity1": "HDL", "entity2": "Vitamin E", "span1": [33, 36], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12652": {"label": 1, "data": {"text": "This study shows that aspirin and sodium salicylate, its major blood metabolite, reverse contractile actions of endothelin-1 (ET-1) in isolated rat aorta and human mammary arteries.", "entity1": "ET-1", "entity2": "aspirin", "span1": [126, 130], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1321": {"label": 3, "data": {"text": "Thus, bupropion acts as an antagonist at alpha3beta2* and alpha3beta4* nAChRs in rat striatum and hippocampus, respectively, across the same concentration range that inhibits DAT and NET function.", "entity1": "NET", "entity2": "bupropion", "span1": [183, 186], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3161": {"label": 0, "data": {"text": "Cellular mechanisms of insulin resistance: role of stress-regulated serine kinases and insulin receptor substrates (IRS) serine phosphorylation.", "entity1": "IRS", "entity2": "serine", "span1": [116, 119], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9782": {"label": 4, "data": {"text": "Parenteral administration of selective agonists of the delta-opioid receptor (SB 227122), mu-opioid receptor (codeine and hydrocodone), and kappa-opioid receptor (BRL 52974) produced dose-related inhibition of citric acid-induced cough with ED(50) values of 7.3, 5.2, 5.1, and 5.3 mg/kg, respectively.", "entity1": "delta-opioid receptor", "entity2": "SB 227122", "span1": [55, 76], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12838": {"label": 8, "data": {"text": "When expressed heterologously in a mammalian cell line, rabbit PAT1 mediates pH-dependent, Na(+)-independent uptake of proline, glycine, l-alanine and alpha-(methylamino)isobutyric acid.", "entity1": "rabbit PAT1", "entity2": "proline", "span1": [56, 67], "span2": [119, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5673": {"label": 9, "data": {"text": "In contrast, ibandronate did not affect FAS and DNMT1 expression in MC3T3-E1 non-neoplastic cells.", "entity1": "FAS", "entity2": "ibandronate", "span1": [40, 43], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10297": {"label": 1, "data": {"text": "Colocalization of RhBG with carbonic anhydrase II, the thiazide-sensitive transporter, and the anion exchangers AE1 and pendrin demonstrated RhBG immunoreactivity in all CNT cells and all CCD and ICT principal cells.", "entity1": "RhBG", "entity2": "thiazide", "span1": [18, 22], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14974": {"label": 3, "data": {"text": "Results confirmed that YR-11 peptide inhibited pro-inflammatory cytokines in the sera and hind paw tissues of AIA rats through its suppressive effect on RANKL induced nuclear translocation of NF-\u03baB.", "entity1": "RANKL", "entity2": "YR-11", "span1": [153, 158], "span2": [23, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13721": {"label": 1, "data": {"text": "Phosphorylation of replication protein A (RPA2 subunit) and formation of damage-induced foci were strikingly evident following IC(50) doses of RTX.", "entity1": "replication protein A", "entity2": "RTX", "span1": [19, 40], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3471": {"label": 2, "data": {"text": "In addition, Silibinin caused an increase in p53 and p21 protein level as well as mRNA levels.", "entity1": "p21", "entity2": "Silibinin", "span1": [53, 56], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12098": {"label": 1, "data": {"text": "Although there is a high probability that the action of aldosterone to cause cardiac fibrosis in this experimental model is an effect via non-epithelial MR, the locus of aldosterone action remains to be established, as do the molecular mechanisms linking MR occupancy by aldosterone and collagen deposition.", "entity1": "MR", "entity2": "aldosterone", "span1": [255, 257], "span2": [271, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10996": {"label": 8, "data": {"text": "In the presence of Na+ and under conditions in which PAT1 transport function was suppressed, a second proline uptake system was detected that exhibited functional characteristics similar to those of the IMINO system.", "entity1": "PAT1", "entity2": "proline", "span1": [53, 57], "span2": [102, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15931": {"label": 1, "data": {"text": "Posttranslational modification of the neural cell adhesion molecule (NCAM) by polysialic acid (polySia) is well studied in the nervous system and described as a dynamic modulator of plastic processes like precursor cell migration, axon fasciculation, and synaptic plasticity.", "entity1": "neural cell adhesion molecule", "entity2": "polysialic acid", "span1": [38, 67], "span2": [78, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12221": {"label": 1, "data": {"text": "In response to METH, AMPH, or POHA exposure, the accumulation of cAMP by HEK-293 cells stably expressing different species of TAAR1 was concentration- and isomer-dependent.", "entity1": "TAAR1", "entity2": "POHA", "span1": [126, 131], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13699": {"label": 2, "data": {"text": "Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimod.", "entity1": "TLR8", "entity2": "imiquimod", "span1": [8, 12], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11082": {"label": 1, "data": {"text": "These observations suggest that felodipine may act directly on the phosphodiesterase as well as through calmodulin.", "entity1": "calmodulin", "entity2": "felodipine", "span1": [104, 114], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10654": {"label": 3, "data": {"text": "Valdecoxib potently inhibits recombinant COX-2, with an IC(50) of 0.005 microM; this compares with IC values of 0.05 microM for celecoxib, 0.5 microM for rofecoxib, and 5 microM for etoricoxib.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [41, 46], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11267": {"label": 0, "data": {"text": "These differences were also present in bovine M-CPT 1, whose N-terminal sequence we determined.", "entity1": "bovine M-CPT 1", "entity2": "N", "span1": [39, 53], "span2": [61, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11881": {"label": 1, "data": {"text": "It remains to be fully elucidated whether use of metformin, an insulin sensitizer, and/or sulfonylureas, insulin secretagogues, affect cancer incidence in subjects with T2DM.", "entity1": "insulin", "entity2": "metformin", "span1": [63, 70], "span2": [49, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13405": {"label": 3, "data": {"text": "In summary, the therapeutic effect of clozapine in reversing PPI impairment was mimicked by the H(1) antagonist pyrilamine, while pyrilamine had a mixed effect on cognition.", "entity1": "H(1)", "entity2": "clozapine", "span1": [96, 100], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8111": {"label": 3, "data": {"text": "Wogonin inhibits H2O2-induced vascular permeability through suppressing the phosphorylation of caveolin-1.", "entity1": "caveolin-1", "entity2": "Wogonin", "span1": [95, 105], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"203": {"label": 1, "data": {"text": "The affinities of a number of alpha 1-adrenoceptor antagonists were determined by displacement of [3H]-prazosin binding from cloned human alpha 1A-adrenoceptors (previously designated cloned alpha 1c subtype), alpha 1B alpha 1D and rat alpha 1D-adrenoceptors, stably expressed in rat-1 fibroblasts.", "entity1": "human alpha 1A-adrenoceptors", "entity2": "[3H]-prazosin", "span1": [132, 160], "span2": [98, 111]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5679": {"label": 3, "data": {"text": "We demonstrate that HZ mice are significantly more sensitive to local AChE inhibition (BW284c51), but remain insensitive to butyrylcholinesterase (BuChE) inhibition (bambuterol).", "entity1": "butyrylcholinesterase", "entity2": "bambuterol", "span1": [124, 145], "span2": [166, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7499": {"label": 1, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Activation of alpha1-AMPK is associated with inhibition of apical amiloride-sensitive Na(+) channels (ENaC), which has important implications for the clinical use of metformin.", "entity1": "ENaC", "entity2": "metformin", "span1": [132, 136], "span2": [196, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7831": {"label": 5, "data": {"text": "Cellular release of AChE by SH-SY5Y is significantly enhanced by the muscarinic acetylcholine receptor (mAChR) agonists carbachol or muscarine, with the effect of carbachol blocked by the mAChR antagonist atropine.", "entity1": "mAChR", "entity2": "atropine", "span1": [188, 193], "span2": [205, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3759": {"label": 3, "data": {"text": "The significantly decreased levels of p-PI3K and p-AKT expression were observed in SGC-7901 cells after \u03b2-ionone treatments in a time- and dose-dependent manner (P\u00a0<\u00a00.01).", "entity1": "p-PI3K", "entity2": "\u03b2-ionone", "span1": [38, 44], "span2": [104, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7888": {"label": 9, "data": {"text": "In contrast, ibandronate did not affect FAS and DNMT1 expression in MC3T3-E1 non-neoplastic cells.", "entity1": "DNMT1", "entity2": "ibandronate", "span1": [48, 53], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9924": {"label": 1, "data": {"text": "Proteolysis protection assays had previously provided circumstantial evidence that binding of heme and non-steroidal anti-inflammatory drugs alters the conformation of PGHS, but the present experiments are the first to directly measure such changes.", "entity1": "PGHS", "entity2": "steroidal", "span1": [168, 172], "span2": [107, 116]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7484": {"label": 3, "data": {"text": "As a consequence, phenserine reduces beta-amyloid peptide (Abeta) formation in vitro and in vivo.", "entity1": "beta-amyloid", "entity2": "phenserine", "span1": [37, 49], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5191": {"label": 3, "data": {"text": "Treatment of A549 and H1299 cells with dioscin caused a dose-dependent increase in ERK1/2 and JNK1/2 activity, accompanied with a decreased PI3K expression and decreased phosphorylation of Akt and mTOR.", "entity1": "Akt", "entity2": "dioscin", "span1": [189, 192], "span2": [39, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15169": {"label": 2, "data": {"text": "GnRH stimulation of CREB phosphorylation (pCREB) in the gonadotrope-derived L\u03b2T2 cell line was attenuated by a protein kinase A (PKA) inhibitor, H89.", "entity1": "pCREB", "entity2": "GnRH", "span1": [42, 47], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8978": {"label": 1, "data": {"text": "Intracerebroventricular administration of SMS 201-995 (5 micrograms/rat), a somatostatin analogue, induced barrel rotation in rats.", "entity1": "somatostatin", "entity2": "SMS 201-995", "span1": [76, 88], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3844": {"label": 3, "data": {"text": "TCDD decreased the expression of the glucose transporter, SLC2A1, and most of the glycolytic transcripts, followed by decreases in glycolytic intermediates, including pyruvate.", "entity1": "SLC2A1", "entity2": "TCDD", "span1": [58, 64], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8451": {"label": 2, "data": {"text": "Oral l-glutamine increases active GLP-1 (7-36) amide secretion and improves glycemic control in stretpozotocin-nicotinamide induced diabetic rats.", "entity1": "GLP-1", "entity2": "l-glutamine", "span1": [34, 39], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6898": {"label": 1, "data": {"text": "Modulation of IL-2R expression was observed at or above a bexarotene dose of 150 mg/day.", "entity1": "IL-2R", "entity2": "bexarotene", "span1": [14, 19], "span2": [58, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9783": {"label": 4, "data": {"text": "Parenteral administration of selective agonists of the delta-opioid receptor (SB 227122), mu-opioid receptor (codeine and hydrocodone), and kappa-opioid receptor (BRL 52974) produced dose-related inhibition of citric acid-induced cough with ED(50) values of 7.3, 5.2, 5.1, and 5.3 mg/kg, respectively.", "entity1": "mu-opioid receptor", "entity2": "codeine", "span1": [90, 108], "span2": [110, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4452": {"label": 3, "data": {"text": "Guided by the acetylcholinesterase inhibiting activity, the bisindole alkaloid 3'-R/S-hydroxyvoacamine was isolated from a stem extract of Tabernaemontana divaricata, a plant used in Thailand in traditional rejuvenation remedies for improving the memory.", "entity1": "acetylcholinesterase", "entity2": "3'-R/S-hydroxyvoacamine", "span1": [14, 34], "span2": [79, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8606": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "ALT", "entity2": "TAA", "span1": [36, 39], "span2": [87, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"450": {"label": 4, "data": {"text": "Pretreatment of the tissues with combined 5-HT1/5-HT2 antagonists, methysergide (1 microM) or methiothepin (0.1 microM), significantly attenuated the inhibitory effect of epinastine on the noncholinergic contraction.", "entity1": "5-HT2", "entity2": "epinastine", "span1": [48, 53], "span2": [171, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7817": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor", "entity2": "(3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid", "span1": [190, 258], "span2": [270, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7637": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "carbenoxolone", "span1": [34, 39], "span2": [79, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3134": {"label": 3, "data": {"text": "These results suggest that fluoxetine inhibited the activity of VMAT2 by a mechanism different from that of reserpine and did not directly interact with the active site of VMAT2.", "entity1": "VMAT2", "entity2": "reserpine", "span1": [64, 69], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3197": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "p-coumaric acid", "span1": [262, 280], "span2": [87, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15665": {"label": 3, "data": {"text": "Small molecules bearing hydroxamic acid as the zinc binding group (ZBG) have been the most effective histone deacetylase inhibitors (HDACi) to date.", "entity1": "histone deacetylase", "entity2": "zinc", "span1": [101, 120], "span2": [47, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4178": {"label": 2, "data": {"text": "The treatment of U937 cells with NRF2 inducers including sulforaphane effectively elevated the expression of AKR1B1, 1B10, 1C1, 1C2, and 1C3.", "entity1": "NRF2", "entity2": "sulforaphane", "span1": [33, 37], "span2": [57, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15935": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "insulin", "entity2": "Vildagliptin", "span1": [139, 146], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9944": {"label": 3, "data": {"text": "Sulfasalazine inhibited tumor necrosis factor alpha-induced activation of endogenous IKK in Jurkat T cells and SW620 colon cells, as well as the catalytic activity of purified IKK-alpha and IKK-beta in vitro.", "entity1": "tumor necrosis factor alpha", "entity2": "Sulfasalazine", "span1": [24, 51], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3999": {"label": 0, "data": {"text": "Dabrafenib is a BRAF (gene encoding serine/threonine-protein kinase B-Raf) inhibitor that has been developed to selectively target the valine 600 to glutamic acid substitution (BRAF(V600E)), which is commonly found in metastatic melanoma.", "entity1": "BRAF", "entity2": "glutamic acid", "span1": [177, 181], "span2": [149, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4830": {"label": 2, "data": {"text": "Thus, in 158N cells, the ability of oxysterols to trigger a mode of cell death by apoptosis involving GSK-3 and caspase-3 activation is independent of the increase in the Ca(2+) level and of their accumulation in lipid raft microdomains.", "entity1": "caspase-3", "entity2": "oxysterols", "span1": [112, 121], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13757": {"label": 9, "data": {"text": "Bosutinib did not inhibit KIT or platelet-derived growth factor receptor, but prominently targeted the apoptosis-linked STE20 kinases.", "entity1": "platelet-derived growth factor receptor", "entity2": "Bosutinib", "span1": [33, 72], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4083": {"label": 3, "data": {"text": "Structure activity relationship studies of tricyclic bispyran sulfone \u03b3-secretase inhibitors.", "entity1": "\u03b3-secretase", "entity2": "tricyclic bispyran sulfone", "span1": [70, 81], "span2": [43, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3941": {"label": 3, "data": {"text": "Reactivators showed different activity in the reactivation of rat brain AChE after dichlorvos, paraoxon and tabun inhibition.", "entity1": "rat brain AChE", "entity2": "paraoxon", "span1": [62, 76], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13667": {"label": 1, "data": {"text": "The noted conformational changes where the C-6 position is closer to the C-9 position of U46619 provided the first experimental data for understanding the molecular mechanism of the catalytic function of PGIS in the isomerization of PGH2 to prostacyclin.", "entity1": "PGIS", "entity2": "U46619", "span1": [204, 208], "span2": [89, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7304": {"label": 8, "data": {"text": "The recombinant strains of the flavinogenic yeast Candida famata, which contain the DNA fragment consisting of the FMN1 gene (encoding the riboflavin kinase, enzyme that converts riboflavin to flavinmononucleotide) driven by the strong promoters (the regulated RIB1 or constitutive TEF1 promoter) were isolated.", "entity1": "riboflavin kinase", "entity2": "riboflavin", "span1": [139, 156], "span2": [179, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"8499": {"label": 2, "data": {"text": "Our study demonstrated that curcumin inhibited OVA-induced increases in eosinophil count; interleukin (IL)-17A level were recovered in bronchoalveolar lavage fluid increased IL-10 level in bronchoalveolar lavage fluid.", "entity1": "IL-10", "entity2": "curcumin", "span1": [174, 179], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2019": {"label": 5, "data": {"text": "Pranlukast, a leukotriene receptor antagonist, inhibits interleukin-5 production via a mechanism distinct from leukotriene receptor antagonism.", "entity1": "leukotriene receptor", "entity2": "Pranlukast", "span1": [111, 131], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13874": {"label": 1, "data": {"text": "Moreover, the effect of ibuprofen on RhoA activity and neurite growth in neuronal cultures is prevented by selective PPARgamma inhibition.", "entity1": "PPARgamma", "entity2": "ibuprofen", "span1": [117, 126], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"923": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "atenolol", "span1": [22, 39], "span2": [183, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13715": {"label": 5, "data": {"text": "Irbesartan (Aprovel, Avapro, Irbetan, Karvea), an angiotensin II receptor type 1 antagonist, is approved in many countries worldwide for the treatment of hypertension.", "entity1": "angiotensin II receptor type 1", "entity2": "Avapro", "span1": [50, 80], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1281": {"label": 1, "data": {"text": "Rheumatoid synovial cells expressed PPARgamma mRNA, and the PPARgamma ligands 15-deoxy-Delta(12,14)-prostaglandin J(2) and troglitazone reduced the proliferation and induced apoptosis in synovial cells.", "entity1": "PPARgamma", "entity2": "15-deoxy-Delta(12,14)-prostaglandin J(2)", "span1": [60, 69], "span2": [78, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14686": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "OCT2", "entity2": "GSK1292263", "span1": [139, 143], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7254": {"label": 4, "data": {"text": "Interestingly, both isomers of METH were full agonists at mTAAR1 and h-rChTAAR1, whereas both were partial agonists at rTAAR1.", "entity1": "mTAAR1", "entity2": "METH", "span1": [58, 64], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14451": {"label": 2, "data": {"text": "We observed similar effects of Ag NPs on inflammatory mediator expression in vitro and in vivo with increase of interleukin-8 (IL-8)/macrophage inflammatory protein 2, IL-1RI, and tumor necrosis factor-\u03b1 expression in both models and increased IL-8 protein release in vitro.", "entity1": "IL-8", "entity2": "Ag", "span1": [127, 131], "span2": [31, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6067": {"label": 3, "data": {"text": "The protein phosphatase inhibitor okadaic acid prolonged the normally transient effect of NE for at least 24 h. We conclude that protein kinase C exerts two opposing effects on alpha-AR mRNA levels, 1) a decrease in the stability of the mRNA that requires the sustained phosphorylation of a protein kinase C substrate and 2) a permissive effect on alpha-AR gene transcription.", "entity1": "protein phosphatase", "entity2": "okadaic acid", "span1": [4, 23], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7369": {"label": 2, "data": {"text": "Repeated cocaine resulted in CREB phosphorylation in all analyzed subregions of the NAc excluding the most ventrolateral region of the shell 2 weeks after cessation of repeated cocaine, but rats challenged after 2 drug-free days yielded a more localized activation of CREB in the 3 most dorsomedial zones of the shell.", "entity1": "CREB", "entity2": "cocaine", "span1": [29, 33], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7060": {"label": 1, "data": {"text": "Retinoid is a collective term for compounds which bind to and activate retinoic acid receptors (RARalpha, beta, gamma and RXRalpha, beta, gamma), members of nuclear hormone receptor superfamily.", "entity1": "nuclear hormone receptor", "entity2": "Retinoid", "span1": [157, 181], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5624": {"label": 3, "data": {"text": "Our results suggest that inactivation facilitates cisapride block of HERG channels through affecting the positioning of Phe-656.", "entity1": "HERG", "entity2": "cisapride", "span1": [69, 73], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11469": {"label": 1, "data": {"text": "From the present study, it may be concluded that mice lacking the NET may represent a good model of some aspects of depression-resistant behavior, paralleled with alterations in the expression of adrenergic receptors, which result as an adaptation to elevated levels of extracellular NE.", "entity1": "adrenergic receptors", "entity2": "NE", "span1": [196, 216], "span2": [284, 286]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3131": {"label": 1, "data": {"text": "The neuronal vesicular monoamine transporter (VMAT2) is the target molecule of action of some psychostimulants, such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA).", "entity1": "neuronal vesicular monoamine transporter", "entity2": "MDMA", "span1": [4, 44], "span2": [175, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3460": {"label": 1, "data": {"text": "Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C.", "entity1": "Y335A", "entity2": "cocaine", "span1": [17, 22], "span2": [124, 131]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8337": {"label": 3, "data": {"text": "Moderate inhibitory effect of LDL-C oxidation by phytosteryl phenolates was observed.", "entity1": "LDL", "entity2": "phytosteryl phenolates", "span1": [30, 33], "span2": [49, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12613": {"label": 3, "data": {"text": "Cyclothiazide prolonged the decay time constant of AMPA receptor-mediated e.p.s.cs (EC50 35.7 +/- 6.5 microM) with less pronounced effects in slowing e.p.s.c.", "entity1": "AMPA receptor", "entity2": "Cyclothiazide", "span1": [51, 64], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15433": {"label": 0, "data": {"text": "We demonstrate that activation of STAT3 serine-727 and tyrosine-705 phosphorylations is promoted by B-RAF(V600E) activity and that the Mcl-1 promoter is dependent on a STAT consensus-site for B-RAF-mediated activation.", "entity1": "STAT3", "entity2": "serine", "span1": [34, 39], "span2": [40, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7526": {"label": 3, "data": {"text": "Previous studies have explored the protective effect of naproxen (non-selective COX-inhibitor) or rofecoxib (selective COX-2 inhibitor) against chemical kindling in mice.", "entity1": "COX", "entity2": "naproxen", "span1": [80, 83], "span2": [56, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9543": {"label": 5, "data": {"text": "We studied the role of endogenous CCK in the emptying of a solid/liquid meal administering the new, highly specific and potent CCK-A receptor antagonist lintitript.", "entity1": "CCK-A receptor", "entity2": "lintitript", "span1": [127, 141], "span2": [153, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9567": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "IFN-gamma", "entity2": "isoproterenol", "span1": [31, 40], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11789": {"label": 1, "data": {"text": "Meanwhile, the serum level of KC (a functional homolog of IL-8 and the main proinflammatory alpha chemokine in mice) in apoE(-/-) mice was up to 357pg/ml in SFO-HD treated group.", "entity1": "apoE", "entity2": "SFO", "span1": [120, 124], "span2": [157, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12489": {"label": 8, "data": {"text": "Cynomolgus FMO6 metabolized benzydamine only slightly, but minimal expression of FMO6 in all tissue precludes the importance of FMO6 in drug metabolism, unlike cynomolgus FMO1, FMO2, FMO3, and FMO5 which were all functional.", "entity1": "FMO1", "entity2": "benzydamine", "span1": [171, 175], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1246": {"label": 3, "data": {"text": "The selective PDE 4 inhibitors, and to a certain extent the PDE3 inhibitors amrinone and milrinone, reduced the GM-CSF release in a concentration dependent manner.", "entity1": "PDE 4", "entity2": "milrinone", "span1": [14, 19], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5725": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "fibrates", "span1": [33, 36], "span2": [147, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"848": {"label": 1, "data": {"text": "The effect of troglitazone, an anti-diabetic drug with insulin-sensitizing action, on antigen-induced production of leukotriene (LT) B(4), C(4) and E(4) and prostaglandin D(2) (PGD(2)) was examined in dinitrophenol (DNP)-specific immunoglobulin E (IgE)-sensitized RBL-2H3 mast cells following stimulation by the antigen, DNP-conjugated human serum albumin.", "entity1": "insulin", "entity2": "troglitazone", "span1": [55, 62], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5591": {"label": 8, "data": {"text": "5-FU interferes with DNA synthesis by blocking thymidylate synthase (TS) but is inactivated by dihydropyrimidine dehydrogenase (DPD).", "entity1": "DPD", "entity2": "5-FU", "span1": [128, 131], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11733": {"label": 0, "data": {"text": "The 3D-structure of HmTx consists of three conserved alpha-helices: h1 (Lys24-His34), h2 (Cys59-Asp71), and h3 (Ala80-Phe89).", "entity1": "HmTx", "entity2": "Ala", "span1": [20, 24], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13049": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "retinaldehyde dehydrogenase type 2", "entity2": "retinal", "span1": [177, 211], "span2": [111, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5634": {"label": 2, "data": {"text": "Compound C caused G(2)/M cell cycle block, accompanied by apoptotic glioma cell death characterized by caspase activation, phosphatidylserine exposure and DNA fragmentation.", "entity1": "caspase", "entity2": "Compound C", "span1": [103, 110], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12444": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "phenethyl ether", "span1": [173, 175], "span2": [90, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15437": {"label": 3, "data": {"text": "The procedure was to reduce liver AOX activity by providing tungsten or hydralazine in the drinking water or to use the AOX-deficient DBA/2 mouse strain.", "entity1": "AOX", "entity2": "tungsten", "span1": [34, 37], "span2": [60, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5578": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "CA I", "entity2": "methazolamide", "span1": [134, 138], "span2": [229, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9964": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "SC-58635", "span1": [10, 15], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7156": {"label": 9, "data": {"text": "However, the expression of AT1R was not suppressed by other AT1R antagonists such as candesartan or olmesartan.", "entity1": "AT1R", "entity2": "olmesartan", "span1": [27, 31], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7352": {"label": 1, "data": {"text": "Immature (reticulated) platelets may modulate the antiplatelet effects of aspirin through uninhibited cyclooxygenase (COX)-1 and COX-2.", "entity1": "cyclooxygenase", "entity2": "aspirin", "span1": [102, 116], "span2": [74, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8374": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "protein kinase B", "entity2": "BPA", "span1": [74, 90], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14547": {"label": 2, "data": {"text": "Therefore, the present results show that the earlier cerebellar responses to (PhTe)(2) include disruption of cytoskeletal homeostasis that could be related with MAPK and PKA activation and reactive astrogliosis.", "entity1": "MAPK", "entity2": "(PhTe)(2)", "span1": [161, 165], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1090": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "gramine", "span1": [51, 71], "span2": [185, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2917": {"label": 3, "data": {"text": "Intriguingly, the inhibitory potency of benzyloxyphenyl NCX inhibitors is directly coupled to the rate of Na(+)(i)-dependent inactivation.", "entity1": "NCX", "entity2": "benzyloxyphenyl", "span1": [56, 59], "span2": [40, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10307": {"label": 8, "data": {"text": "PDE5 is the predominant PDE in the corpus cavernosum, and cGMP is its primary substrate.", "entity1": "PDE5", "entity2": "cGMP", "span1": [0, 4], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14610": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala70Thr", "entity2": "dFdC", "span1": [52, 60], "span2": [230, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6896": {"label": 1, "data": {"text": "[Change of dopamine transporter activity (DAT) during the action of bupropion (in depression)].", "entity1": "DAT", "entity2": "bupropion", "span1": [42, 45], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7455": {"label": 3, "data": {"text": "L-BOAA causes loss of GSH and inhibition of mitochondrial complex I in lumbosacral cord of male mice through oxidation of thiol groups, while female mice are resistant.", "entity1": "mitochondrial complex I", "entity2": "L-BOAA", "span1": [44, 67], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7367": {"label": 2, "data": {"text": "The present study examined the differential cocaine-induced activation of the cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) throughout discrete zones of analysis of the nucleus accumbens (NAc) in rats.", "entity1": "CREB", "entity2": "cocaine", "span1": [150, 154], "span2": [44, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4517": {"label": 8, "data": {"text": "Carboxylesterases hydrolyze esters, amides, and thioesters to produce carboxylic acids and resulting alcohols, amines, and thiols, respectively.", "entity1": "Carboxylesterases", "entity2": "carboxylic acids", "span1": [0, 17], "span2": [70, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1294": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "Glutamic acid decarboxylase", "entity2": "glutamate", "span1": [21, 48], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"8622": {"label": 9, "data": {"text": "In contrast, activation of Nrf2 by sulforaphane and tert-butylhydroquinone depend upon Keap1-C151 and not p62 (the canonical mechanism).", "entity1": "p62", "entity2": "sulforaphane", "span1": [106, 109], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1972": {"label": 9, "data": {"text": "The inhibitory effect of sodium nitroprusside on HIF-1 activation is not dependent on nitric oxide-soluble guanylyl cyclase pathway.", "entity1": "soluble guanylyl cyclase", "entity2": "sodium nitroprusside", "span1": [99, 123], "span2": [25, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8914": {"label": 9, "data": {"text": "Carvedilol produced significant inhibition of the alpha 1 adrenoceptor mediated pressor response to cirazoline in the pithed rat, but had no effect on the alpha 2 adrenoceptor mediated pressor response to B-HT 933, suggesting that carvedilol is also an alpha 1 adrenoceptor antagonist at antihypertensive doses.", "entity1": "alpha 2 adrenoceptor", "entity2": "Carvedilol", "span1": [155, 175], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7721": {"label": 2, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "gonadotrophin-releasing hormone (GnRH) receptor", "entity2": "triptorelin", "span1": [140, 187], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1076": {"label": 1, "data": {"text": "Differential inhibition of [3H]-oxotremorine-M and [3H]-quinuclinidyl benzilate binding to muscarinic receptors in rat brain membranes with acetylcholinesterase inhibitors.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [91, 111], "span2": [27, 46]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8003": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "thrombin", "entity2": "hyperoside", "span1": [182, 190], "span2": [147, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15025": {"label": 3, "data": {"text": "Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner.", "entity1": "SAHH", "entity2": "adenosine dialdehyde", "span1": [127, 131], "span2": [15, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10308": {"label": 8, "data": {"text": "PDE5 is the predominant PDE in the corpus cavernosum, and cGMP is its primary substrate.", "entity1": "PDE", "entity2": "cGMP", "span1": [24, 27], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10932": {"label": 3, "data": {"text": "Losartan is well-absorbed orally as an active drug and is rapidly converted via oxidation in the human liver to a more potent metabolite (designated E3174) with an affinity 20- to 30-times greater for the AT(1) receptor (non-competitive inhibition).", "entity1": "AT(1) receptor", "entity2": "Losartan", "span1": [205, 219], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"648": {"label": 1, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "metalloproteinase", "entity2": "batimastat", "span1": [164, 181], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2702": {"label": 2, "data": {"text": "Sitagliptin, an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, improves glycaemic control by inhibiting DPP-4 inactivation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.", "entity1": "glucagon-like peptide-1", "entity2": "Sitagliptin", "span1": [148, 171], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3954": {"label": 1, "data": {"text": "Vitamin K2 covalently binds to Bak and induces Bak-mediated apoptosis.", "entity1": "Bak", "entity2": "Vitamin K2", "span1": [31, 34], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14374": {"label": 3, "data": {"text": "These findings suggest that NFD inhibited the EGF-induced invasion and migration of MDA-MB-231 cells via EGFR-dependent PI3K/Akt signaling, leading to the down-regulation of MMP-9 expression.", "entity1": "PI3K", "entity2": "NFD", "span1": [120, 124], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7439": {"label": 5, "data": {"text": "Dopamine D1 receptor agonist and D2 receptor antagonist effects of the natural product (-)-stepholidine: molecular modeling and dynamics simulations.", "entity1": "D2 receptor", "entity2": "(-)-stepholidine", "span1": [33, 44], "span2": [87, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4062": {"label": 3, "data": {"text": "Jaspamide also inhibited other channels including Cav1.2, Cav3.2, and HCN2; however, the Kv11.1 (hERG) channel was minimally affected.", "entity1": "Cav3.2", "entity2": "Jaspamide", "span1": [58, 64], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5401": {"label": 1, "data": {"text": "Furthermore, estrogen responsive genes in fish liver, ER\u03b1 and VTG, are not induced by CP[c]Ph, suggesting that the compound has no endocrine disrupting potential.", "entity1": "VTG", "entity2": "estrogen", "span1": [62, 65], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15314": {"label": 4, "data": {"text": "Moreover, the effects of the DRD3 agonist 7-hydroxy-N,N-dipropyl-2-aminotetralin (7-OH-DPAT)-induced locomotor hypoactivity were significantly increased when DRD3 proteins were abundant.", "entity1": "DRD3", "entity2": "7-hydroxy-N,N-dipropyl-2-aminotetralin", "span1": [29, 33], "span2": [42, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2005": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Phe", "span1": [121, 125], "span2": [59, 62]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12457": {"label": 2, "data": {"text": "This report concerns the marked up-regulation in differentiated CaCo-2 colonic epithelial cells of two key inflammatory interleukins, IL-6 and IL-8, caused by a mixture of oxysterols representative of a high cholesterol diet.", "entity1": "IL-8", "entity2": "oxysterols", "span1": [143, 147], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6704": {"label": 1, "data": {"text": "Inhibitory effects of the monoamine oxidase inhibitor tranylcypromine on the cytochrome P450 enzymes CYP2C19, CYP2C9, and CYP2D6.", "entity1": "CYP2D6", "entity2": "tranylcypromine", "span1": [122, 128], "span2": [54, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7568": {"label": 1, "data": {"text": "Compounds 1 and 2 potently displaced (3)H-NMS binding at m1, m3 and m4 receptors, but were less potent at the m2 and m5 subtypes.", "entity1": "m5", "entity2": "(3)H-NMS", "span1": [117, 119], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12965": {"label": 0, "data": {"text": "Mass spectrometric analysis and mutation studies revealed that gammaPKC phosphorylated Ser-776 and Ser-779 in the AD of DGKgamma.", "entity1": "gammaPKC", "entity2": "phosphorylated Ser", "span1": [63, 71], "span2": [72, 90]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2714": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "beta catenin", "entity2": "parathion", "span1": [86, 98], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14968": {"label": 3, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "TRAP", "entity2": "YR-11", "span1": [196, 200], "span2": [12, 17]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2269": {"label": 8, "data": {"text": "Astrocytes may play a role in these manifestations because astrocytes are essential in the regulation of released glutamate and its conversion to glutamine through the enzyme glutamine synthetase (GS).", "entity1": "GS", "entity2": "glutamine", "span1": [197, 199], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3720": {"label": 3, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "ERK", "entity2": "BPs", "span1": [97, 100], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4456": {"label": 1, "data": {"text": "Also, ROS from NADPH oxidase favors ERK1/2 activation that phosphorylates Stat3 in serine, resulting in a compensatory or adaptive survival response such as production of metallothionein-II in short Cd exposure times.", "entity1": "metallothionein-II", "entity2": "Cd", "span1": [171, 189], "span2": [199, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7444": {"label": 3, "data": {"text": "The Ki for mycophenolic acid inhibition of the L263F variant was comparable with the wild-type, and the variant Km for inosine 5'-monophosphate and nicotinamide adenine dinucleotide did not change significantly.", "entity1": "L263F", "entity2": "mycophenolic acid", "span1": [47, 52], "span2": [11, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4858": {"label": 0, "data": {"text": "Unsaturated FFAs increased DAGs, TAGs and PTP1B expression significantly, but cells remained insulin sensitive as assessed by robust AKt and PTP1B phosphorylation at serine (Ser) 50, Ser 398 and tyrosine 152.", "entity1": "PTP1B", "entity2": "serine", "span1": [141, 146], "span2": [166, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2666": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE6", "entity2": "zaprinast", "span1": [267, 271], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3796": {"label": 3, "data": {"text": "Moreover, use of the pharmacological AMP-activated protein kinase (AMPK) inhibitor compound C revealed that AMPK is essential for suppressing SREBP-1c expression in phillyrin-treated cells.", "entity1": "AMPK", "entity2": "compound C", "span1": [108, 112], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15591": {"label": 3, "data": {"text": "IPI-926 is both a substrate and inhibitor (IC50\u2009=\u20091.9\u2009\u00b5M) of P-glycoprotein.", "entity1": "P-glycoprotein", "entity2": "IPI-926", "span1": [61, 75], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15798": {"label": 8, "data": {"text": "Opening of Panx1 HCs during repetitive activation allows efflux of ATP, influx of glucose and possibly Ca(2+) too, which are required for potentiation of contraction.", "entity1": "Panx1", "entity2": "ATP", "span1": [11, 16], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8680": {"label": 3, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "Bax", "entity2": "imatinib", "span1": [258, 261], "span2": [118, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14845": {"label": 8, "data": {"text": "Aldehyde dehydrogenase 1 (ALDH1A1) catalyzes the oxidation of toxic aldehydes to carboxylic acids.", "entity1": "ALDH1A1", "entity2": "carboxylic acids", "span1": [26, 33], "span2": [81, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15856": {"label": 8, "data": {"text": "High cholesterol turnover catalyzed by cholesterol 24-hydroxylase is essential for neural functions, especially learning.", "entity1": "cholesterol 24-hydroxylase", "entity2": "cholesterol", "span1": [39, 65], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8107": {"label": 3, "data": {"text": "The mechanism revealed that wogonin inhibited H2O2-induced phosphorylation of caveolin-1 (cav-1) associating with the suppression of stabilization of VE-cadherin and \u03b2-catenin.", "entity1": "\u03b2-catenin", "entity2": "wogonin", "span1": [166, 175], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13147": {"label": 2, "data": {"text": "CONCLUSION: CysLT1 receptor expression in neurons is upregulated after NMDA injection, and NMDA-induced responses are inhibited by CysLT1 receptor antagonists, indicating that the increased CysLT1 receptor is involved in NMDA excitotoxicity.", "entity1": "CysLT1 receptor", "entity2": "NMDA", "span1": [190, 205], "span2": [221, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6077": {"label": 3, "data": {"text": "HeLa cells transfected with the MR77 gene exhibited inhibition of adenylate cyclase in response to serotonin.", "entity1": "adenylate cyclase", "entity2": "serotonin", "span1": [66, 83], "span2": [99, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15858": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "HSA", "entity2": "amino acid", "span1": [67, 70], "span2": [112, 122]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5128": {"label": 3, "data": {"text": "Pyrrolidine dithiocarbamate (PDTC), a specific NF-\u03baB inhibitor, along with 20S proteasome inhibitor (PSI) significantly inhibited LPS-induced iNOS expression, which indirectly suggested that 5HHMF downregulated iNOS expression by suppressing NF-\u03baB activity.", "entity1": "iNOS", "entity2": "5HHMF", "span1": [211, 215], "span2": [191, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3608": {"label": 6, "data": {"text": "Ifenprodil is an allosteric inhibitor of GluN1/GluN2B N-methyl-D-aspartate receptors.", "entity1": "N-methyl-D-aspartate receptors", "entity2": "Ifenprodil", "span1": [54, 84], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"9972": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-2", "entity2": "sulindac", "span1": [159, 164], "span2": [54, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12725": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "BuChE", "entity2": "acetylcholine", "span1": [91, 96], "span2": [150, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7223": {"label": 1, "data": {"text": "In this setting there is a GnRH-induced association and nuclear translocation of the androgen receptor with Hic-5.", "entity1": "androgen receptor", "entity2": "GnRH", "span1": [85, 102], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8582": {"label": 2, "data": {"text": "Finally, epididymal mRNA abundance of GLUT4 was significantly increased by fisetin supplementation, compared to levels in the control and HF groups.", "entity1": "GLUT4", "entity2": "fisetin", "span1": [38, 43], "span2": [75, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12101": {"label": 1, "data": {"text": "By contrast, the closely related bovine ether-a-go-go channel (BEAG) is 100-fold less sensitive to dofetilide.", "entity1": "bovine ether-a-go-go channel", "entity2": "dofetilide", "span1": [33, 61], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15683": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Histone 3", "entity2": "VB1", "span1": [177, 186], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3974": {"label": 8, "data": {"text": "These results suggest that CYP2B6 genotype is the most important patient variable for predicting the level of CYP2B6 activity in women, when measured by the metabolism of bupropion.", "entity1": "CYP2B6", "entity2": "bupropion", "span1": [27, 33], "span2": [171, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1900": {"label": 3, "data": {"text": "PKC isoforms did show different sensitivity and selectivity for down-regulation by I3A and phorbol 12-myristate 13-acetate (PMA) in WEHI-231, HOP-92, and Colo-205 cells.", "entity1": "PKC", "entity2": "I3A", "span1": [0, 3], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9086": {"label": 1, "data": {"text": "Multiple affinity states of opiate receptor can be demonstrated further by Scatchard analysis of saturation binding studies with [3H]DADLE.", "entity1": "opiate receptor", "entity2": "[3H]DADLE", "span1": [28, 43], "span2": [129, 138]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13795": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "kinase", "entity2": "Imatinib", "span1": [31, 37], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2815": {"label": 3, "data": {"text": "DXM and 1400W attenuated the mRNA expression of E-selectin and iNOS induced by the costimulation of reIL-4, reTNF-alpha, and LPS.", "entity1": "iNOS", "entity2": "DXM", "span1": [63, 67], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10268": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "OCT", "entity2": "[3H]-MPP+", "span1": [123, 126], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"8240": {"label": 9, "data": {"text": "Thus, SN mDA neurons are represented by at least two distinct subpopulations including MPTP-resistant Pitx3-autonomous, calbindin-positive neurons, and calbindin-negative Pitx-3-dependent cells that display elevated vulnerability to toxic injury, and probably correspond to the subpopulation that degenerates in PD.", "entity1": "Pitx3", "entity2": "MPTP", "span1": [102, 107], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2335": {"label": 3, "data": {"text": "The Na channel block caused by lidocaine and RSD1235 can be through the open or inactivated states of the channel, but both equivalently inhibit a late component of Na current (I(Na)), recorded at 22 degrees C using whole-cell patch clamp of Nav 1.5 expressed in HEK cells.", "entity1": "Na channel", "entity2": "lidocaine", "span1": [4, 14], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14829": {"label": 3, "data": {"text": "rivaroxaban and apixaban, are potent, oral direct inhibitors of prothrombinase-bound, clot-associated or free FXa.", "entity1": "prothrombinase", "entity2": "apixaban", "span1": [64, 78], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7926": {"label": 1, "data": {"text": "Altogether, our results suggest that a high dose of glucosamine may inhibit cell proliferation through apoptosis and disturb cell cycle progression with a halt at G(0)/G(1) phase, and that this occurs, at least in part, by a reduction in Rb phosphorylation together with modulation of p21, p53 and HO-1 expression, and nuclear p21 accumulation.", "entity1": "p21", "entity2": "glucosamine", "span1": [285, 288], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5612": {"label": 3, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "cisapride", "span1": [71, 75], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11008": {"label": 1, "data": {"text": "This increase may suggest that both leptin and cyproheptadine may affect appetite via similar receptors and that cyproheptadine does not impair leptin activity through these receptors.", "entity1": "leptin", "entity2": "cyproheptadine", "span1": [36, 42], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15945": {"label": 1, "data": {"text": "We also recorded a significant correlation between M value increase and the decrease of vaspin, visfatin, and omentin-1 obtained with vildagliptin+metformin.", "entity1": "omentin-1", "entity2": "metformin", "span1": [110, 119], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1487": {"label": 1, "data": {"text": "Similarly, pretreatment with sulindac sulfide blocks the ability of EGF to induce ERK1/2 and Bad phosphorylation, but also down-regulates total Bad but not ERK1/2 protein levels.", "entity1": "ERK1/2", "entity2": "sulindac sulfide", "span1": [156, 162], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14753": {"label": 1, "data": {"text": "Jaceosidin induced G2/M phase cell cycle arrest and modulated the levels of cyclin B and p-Cdc2 in Hec1A cells.", "entity1": "cyclin B", "entity2": "Jaceosidin", "span1": [76, 84], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12121": {"label": 9, "data": {"text": "Losartan, EXP, and irbesartan caused a rightward parallel shift without any major effects on the maximal response to Ang II.", "entity1": "Ang II", "entity2": "irbesartan", "span1": [117, 123], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8465": {"label": 3, "data": {"text": "In conclusion, hinokitiol may inhibit platelet activation by inhibiting the PLC\u03b32-PKC cascade and hydroxyl radical formation, followed by suppressing the activation of MAPKs and Akt.", "entity1": "PKC", "entity2": "hinokitiol", "span1": [82, 85], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5665": {"label": 2, "data": {"text": "Therefore, matrine and oxymatrine may have the potential to cure LQT2 as a potassium channel activator by promoting hERG channel activation and increasing hERG channel expression.", "entity1": "hERG", "entity2": "matrine", "span1": [116, 120], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14918": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "estrogen receptor-\u03b1", "entity2": "5\u03b1-androstanediol", "span1": [236, 255], "span2": [56, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15477": {"label": 3, "data": {"text": "Upon nicotine pre-exposure, brain acetylcholinesterase increased, while monoamine oxidase (MAO) decreased.", "entity1": "monoamine oxidase", "entity2": "nicotine", "span1": [72, 89], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6545": {"label": 9, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "Y751A", "entity2": "cilostazol", "span1": [8, 13], "span2": [196, 206]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13780": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Canertinib", "span1": [14, 16], "span2": [146, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5600": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "quetiapine", "span1": [111, 117], "span2": [188, 198]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3564": {"label": 1, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "IR", "entity2": "MSG", "span1": [24, 26], "span2": [240, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8574": {"label": 3, "data": {"text": "We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold.", "entity1": "JAK3", "entity2": "5H-pyrrolo[2,3-b]pyrazine", "span1": [77, 81], "span2": [107, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6051": {"label": 1, "data": {"text": "Actinomycin D caused alpha-AR mRNA level to decrease with a half-life of 3.2 +/- 0.4 h and blocked the effect of H-7 to decrease basal alpha-AR mRNA level.", "entity1": "alpha-AR", "entity2": "H-7", "span1": [135, 143], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15859": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "Human Serum Albumin", "entity2": "Arg", "span1": [46, 65], "span2": [132, 135]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1053": {"label": 3, "data": {"text": "doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g. amonafide, batracylin, and menadione) was only slightly (less than 3-fold) affected.", "entity1": "TOP2", "entity2": "amonafide", "span1": [166, 170], "span2": [185, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14866": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "ER\u03b1", "entity2": "BIS", "span1": [13, 16], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5276": {"label": 2, "data": {"text": "Allicin treatment showed reduced production of pro-inflammatory cytokines and NO and increased HO-1 activity.", "entity1": "HO-1", "entity2": "Allicin", "span1": [95, 99], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15735": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b1", "entity2": "alkyl", "span1": [142, 145], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13818": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "Sunitinib", "span1": [233, 246], "span2": [191, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7020": {"label": 3, "data": {"text": "Competitive radioligand binding assays were performed using cells expressing either the human serotonin (5-HT) transporter (hSERT) or norepinephrine (NE) transporter (hNET) with K(i) values for DVS of 40.2 +/- 1.6 and 558.4 +/- 121.6 nM, respectively.", "entity1": "human serotonin (5-HT) transporter", "entity2": "DVS", "span1": [88, 122], "span2": [194, 197]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"179": {"label": 5, "data": {"text": "In vivo lorglumide antagonizes the contraction of the gall bladder of the guinea pig and of the dog provoked by i.v. CCK-8 or ceruletide (caerulein).", "entity1": "CCK-8", "entity2": "lorglumide", "span1": [117, 122], "span2": [8, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5792": {"label": 0, "data": {"text": "The amino acid sequence deduced from the nucleotide sequence of the cDNA from porcine liver was identical to that deduced for porcine kidney ACY-1.", "entity1": "porcine kidney ACY-1", "entity2": "amino acid", "span1": [126, 146], "span2": [4, 14]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2475": {"label": 4, "data": {"text": "The beta(2)-adrenoceptor (beta(2)-AR) agonists clenbuterol and fenoterol have similar beneficial effects in animal models of heart failure.", "entity1": "beta(2)-adrenoceptor", "entity2": "clenbuterol", "span1": [4, 24], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13380": {"label": 1, "data": {"text": "Monosodium urate crystals stimulate monocytes and macrophages to release IL-1beta through the NALP3 component of the inflammasome.", "entity1": "NALP3", "entity2": "Monosodium urate", "span1": [94, 99], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3100": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "[(3)H]dopamine", "span1": [354, 357], "span2": [383, 397]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5059": {"label": 2, "data": {"text": "Activating glucocorticoid receptor-ERK signaling pathway contributes to ginsenoside Rg1 protection against \u03b2-amyloid peptide-induced human endothelial cells apoptosis.", "entity1": "glucocorticoid receptor", "entity2": "ginsenoside Rg1", "span1": [11, 34], "span2": [72, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15190": {"label": 3, "data": {"text": "Upon studying the drug-drug interaction of darunavir with ketoconazole, data were indicative for an inhibitory effect of ketoconazole on P-gp as the main mechanism for the increased transport of darunavir across the small intestine.", "entity1": "P-gp", "entity2": "ketoconazole", "span1": [137, 141], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4447": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "MAO", "entity2": "phthalide", "span1": [195, 198], "span2": [236, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10403": {"label": 1, "data": {"text": "Orphanin FQ (OFQ) stimulated [35S]-GTPgammaS binding in a pattern similar to that described for [125I]-OFQ at the endogenous opioid receptor-like (ORL1) receptor.", "entity1": "Orphanin FQ", "entity2": "[35S]-GTPgammaS", "span1": [0, 11], "span2": [29, 44]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"36": {"label": 2, "data": {"text": "Evidence has accumulated in the last few years that the expression of the microsomal/peroxidase antigen (M/TPO-Ag) in thyroid cells is induced by TSH, through pathways which involve intracellular cAMP accumulation and protein synthesis.", "entity1": "M/TPO-Ag", "entity2": "cAMP", "span1": [105, 113], "span2": [196, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2047": {"label": 3, "data": {"text": "Increased immunohistochemical labeling of HIF-1alpha, VEGF, and BNP in the ventricular myocardium was observed in the shunt group and carvedilol again normalized the labeling.", "entity1": "HIF-1alpha", "entity2": "carvedilol", "span1": [42, 52], "span2": [134, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2131": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "MCTs", "entity2": "ketone", "span1": [30, 34], "span2": [156, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8316": {"label": 1, "data": {"text": "Refining the UGT1A haplotype associated with irinotecan-induced hematological toxicity in metastatic colorectal cancer patients treated with 5-fluorouracil/irinotecan-based regimens.", "entity1": "UGT1A", "entity2": "irinotecan", "span1": [13, 18], "span2": [156, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6596": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "5-HT(2A)", "entity2": "WAY100635", "span1": [232, 240], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11466": {"label": 1, "data": {"text": "Involvement of EP1 and EP2 receptors in the regulation of the Na,K-ATPase by prostaglandins in MDCK cells.", "entity1": "Na,K-ATPase", "entity2": "prostaglandins", "span1": [62, 73], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12498": {"label": 1, "data": {"text": "Involvement of p-CREB and phase II detoxifying enzyme system in neuroprotection mediated by the flavonoid calycopterin isolated from Dracocephalum kotschyi.", "entity1": "phase II detoxifying enzyme", "entity2": "calycopterin", "span1": [26, 53], "span2": [106, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12917": {"label": 8, "data": {"text": "Collectively, our results suggest that H(2)S can inhibit NO production and NF-kappaB activation in LPS-stimulated macrophages through a mechanism that involves the action of HO-1/CO.", "entity1": "HO-1", "entity2": "CO", "span1": [174, 178], "span2": [179, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14015": {"label": 3, "data": {"text": "Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.", "entity1": "MET", "entity2": "XL184", "span1": [30, 33], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11529": {"label": 3, "data": {"text": "Our results first demonstrate that auranofin suppresses the multiple steps in TLR4 signaling, especially the homodimerization of TLR4.", "entity1": "TLR4", "entity2": "auranofin", "span1": [78, 82], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10001": {"label": 8, "data": {"text": "Contribution of the Na+-K+-2Cl- cotransporter NKCC1 to Cl- secretion in rat OMCD.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [46, 51], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2450": {"label": 3, "data": {"text": "Colonic cyclooxygenase-2 and interkeukin-1beta mRNA and spinal c-FOS mRNA expression were significantly down-regulated by ATB-429, but not by mesalamine.", "entity1": "interkeukin-1beta", "entity2": "ATB-429", "span1": [29, 46], "span2": [122, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8798": {"label": 2, "data": {"text": "Here we show that fisetin rapidly increases the levels of both Nrf2 and ATF4 as well as Nrf2- and ATF4-dependent gene transcription via distinct mechanisms.", "entity1": "ATF4", "entity2": "fisetin", "span1": [72, 76], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11538": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "dexamethasone", "span1": [103, 106], "span2": [255, 268]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10707": {"label": 1, "data": {"text": "The anticonvulsant action of dextromethorphan or dimemorfan was significantly counteracted by a selective sigma1 receptor antagonist BD 1047, suggesting that the anticonvulsant action of dextromethorphan or dimemorfan is, at least in part, related to sigma1 receptor-activated modulation of AP-1 transcription factors.", "entity1": "sigma1 receptor", "entity2": "dextromethorphan", "span1": [251, 266], "span2": [187, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12502": {"label": 8, "data": {"text": "These findings indicate that human pulmonary ethanol-metabolizing activities differ significantly with respect to genetic polymorphism at both the ADH2 and the ALDH2 loci.", "entity1": "ADH2", "entity2": "ethanol", "span1": [147, 151], "span2": [45, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15346": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "1-acetylpyrene", "span1": [39, 48], "span2": [226, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5468": {"label": 4, "data": {"text": "Brexpiprazole reversed the inhibitory effect of the DA agonist apomorphine on VTA DA neurons (ED50 = 61 mug/kg), whereas it was ineffective when administered alone, indicating partial agonistic action on D2 receptors.", "entity1": "D2 receptors", "entity2": "apomorphine", "span1": [204, 216], "span2": [63, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2045": {"label": 1, "data": {"text": "Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure.", "entity1": "hypoxia-inducible factor-1alpha", "entity2": "Carvedilol", "span1": [39, 70], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9165": {"label": 7, "data": {"text": "Phenylbutazone (PB), a nonsteroidal anti-inflammatory drug, is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS).", "entity1": "prostaglandin H synthase", "entity2": "PB", "span1": [125, 149], "span2": [16, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"14558": {"label": 8, "data": {"text": "The objective of this article is to examine the effects of single and repeated administrations of silymarin on pharmacokinetics of a P-gp substrate, risperidone, and its major metabolite, 9-hydroxyrisperidone, in rats.", "entity1": "P-gp", "entity2": "risperidone", "span1": [133, 137], "span2": [149, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3214": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "gallic acid", "span1": [248, 261], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11662": {"label": 8, "data": {"text": "Thymidine kinase-1 (TK-1) and thymidylate synthase (TS) are key enzymes for salvage and de novo pyrimidine synthesis, respectively.", "entity1": "Thymidine kinase-1", "entity2": "pyrimidine", "span1": [0, 18], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"441": {"label": 1, "data": {"text": "Epinastine (WAL 801CL) is an antihistaminic drug with binding affinity at certain other receptors, including alpha-adrenergic receptors and various serotonin (5-HT) receptor subtypes.", "entity1": "alpha-adrenergic receptors", "entity2": "Epinastine", "span1": [109, 135], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2897": {"label": 5, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1D)-adrenoceptor", "entity2": "BMY-7378", "span1": [235, 257], "span2": [118, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12246": {"label": 8, "data": {"text": "The phosphodiesterase (PDE) 4 is the predominant cyclic AMP degrading enzyme in a variety of inflammatory cells including eosinophils, neutrophils, macrophages, T cells and monocytes.", "entity1": "phosphodiesterase (PDE) 4", "entity2": "cyclic AMP", "span1": [4, 29], "span2": [49, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"744": {"label": 1, "data": {"text": "Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain.", "entity1": "CD11a I-domain", "entity2": "lovastatin", "span1": [69, 83], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5702": {"label": 2, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "human TRPA1", "entity2": "apomorphine", "span1": [21, 32], "span2": [219, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2077": {"label": 2, "data": {"text": "These data demonstrated that 1) gemcitabine and pemetrexed synergistically interact against NSCLC cells through the suppression of Akt phosphorylation and induction of apoptosis; 2) the gene expression profile of critical genes may predict for drug chemosensitivity; and 3) pemetrexed enhances dCK and hENT1 expression, thus suggesting the role of gene-expression modulation for rational development of chemotherapy combinations.", "entity1": "dCK", "entity2": "pemetrexed", "span1": [294, 297], "span2": [274, 284]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2320": {"label": 8, "data": {"text": "Glufosinate inhibits glutamine synthetase and blocks biosynthesis of glutamine.", "entity1": "glutamine synthetase", "entity2": "glutamine", "span1": [21, 41], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9462": {"label": 1, "data": {"text": "7. 8-Epi-PGF2 alpha showed only weak binding to the IP, TP, FP, EP2 and EP3 receptor at 10 microM concentration.", "entity1": "IP", "entity2": "7. 8-Epi-PGF2", "span1": [52, 54], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1434": {"label": 1, "data": {"text": "To determine whether 3,4-methylenedioxymethamphetamine (MDMA)-induced reductions in SERT density could be related to such a mechanism, p-chlorophenylalanine or MDMA was administered to rats, and brain serotonin and SERT density were measured.", "entity1": "SERT", "entity2": "p-chlorophenylalanine", "span1": [215, 219], "span2": [135, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3534": {"label": 2, "data": {"text": "2-Deoxyglucose increased phosphorylation of tuberous sclerosis complex 2 (TSC2) on AMPK consensus sites but did not change the amount of TSC1 bound to TSC2.", "entity1": "tuberous sclerosis complex 2", "entity2": "2-Deoxyglucose", "span1": [44, 72], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"151": {"label": 1, "data": {"text": "The interaction of naloxone estrone azine (N-EH) with various opioid receptor types was studied in vitro.", "entity1": "opioid receptor", "entity2": "naloxone estrone azine", "span1": [62, 77], "span2": [19, 41]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13508": {"label": 6, "data": {"text": "Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors.", "entity1": "human muscarinic M2 receptors", "entity2": "vecuronium", "span1": [97, 126], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"1743": {"label": 8, "data": {"text": "CPT I (carnitine palmitoyltransferase I) catalyses the conversion of palmitoyl-CoA into palmitoylcarnitine in the presence of L-carnitine, facilitating the entry of fatty acids into mitochondria.", "entity1": "CPT I", "entity2": "palmitoyl-CoA", "span1": [0, 5], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"3327": {"label": 3, "data": {"text": "In conclusion, the results suggest that the enhancement in the reduction of topo II activity by the combined MXF/VP-16 treatments was probably due to the increase in the level of the DNA-enzyme cleavable complexes formed by both drugs.", "entity1": "topo II", "entity2": "MXF", "span1": [76, 83], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4758": {"label": 1, "data": {"text": "Regucalcin (RGN/SMP30) was originally discovered in 1978 as a unique calcium-binding protein that does not contain the EF-hand motif of calcium-binding domain.", "entity1": "SMP30", "entity2": "calcium", "span1": [16, 21], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"485": {"label": 1, "data": {"text": "The atypical neuroleptics remoxipride, clozapine, perlapine, seroquel, and melperone had low affinity for the dopamine D2 receptor (radioligand-independent dissociation constants of 30 to 90 nM).", "entity1": "D2 receptor", "entity2": "perlapine", "span1": [119, 130], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9257": {"label": 2, "data": {"text": "These findings suggest that some of the deleterious effects of consumption of endophyte-infected tall fescue, which contains several ergot alkaloids including ergovaline, may be due to D2 dopamine receptor activation.", "entity1": "D2 dopamine receptor", "entity2": "ergovaline", "span1": [185, 205], "span2": [159, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7006": {"label": 3, "data": {"text": "Significant advances in the treatment of clear-cell RCC have been derived from agents that target these pathways, including the multiple-kinase inhibitors (MKIs) sorafenib, sunitinib, and AG013736, which target multiple VEGFRs as well as PDGFR-beta.", "entity1": "kinase", "entity2": "sunitinib", "span1": [137, 143], "span2": [173, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2964": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "L765A", "entity2": "cGMP", "span1": [78, 83], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14479": {"label": 8, "data": {"text": "Of the rat CYP isoforms studied, CYP2D isoforms were the most efficient in catalyzing the O-demethylation of 5-methoxytryptamine to serotonin, but they were less effective than the human isoform CYP2D6.", "entity1": "human isoform CYP2D6", "entity2": "serotonin", "span1": [181, 201], "span2": [132, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14123": {"label": 1, "data": {"text": "Emerging data suggest that crizotinib may also have activity in other subsets of lung cancer, including tumors demonstrating amplification or mutation of the MET oncogene, or translocation of the ROS1 oncogene.", "entity1": "ROS1", "entity2": "crizotinib", "span1": [196, 200], "span2": [27, 37]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12372": {"label": 8, "data": {"text": "Carnitine palmitoyltransferase 2 and carnitine/acylcarnitine translocase are involved in the mitochondrial synthesis and export of acylcarnitines.", "entity1": "Carnitine palmitoyltransferase 2", "entity2": "acylcarnitines", "span1": [0, 32], "span2": [131, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6334": {"label": 1, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "telmisartan", "span1": [18, 21], "span2": [136, 147]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8948": {"label": 9, "data": {"text": "The 3 beta-hydroxysteroid substrate, pregnenolone, protects isomerase as well as dehydrogenase from inactivation by FSA.", "entity1": "dehydrogenase", "entity2": "pregnenolone", "span1": [81, 94], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8386": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "17\u03b2-HSD", "entity2": "Cd", "span1": [264, 271], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15047": {"label": 1, "data": {"text": "The contrasting activity of iodido versus chlorido ruthenium and osmium arene azo- and imino-pyridine anticancer complexes: control of cell selectivity, cross-resistance, p53 dependence, and apoptosis pathway.", "entity1": "p53", "entity2": "iodido", "span1": [171, 174], "span2": [28, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11691": {"label": 0, "data": {"text": "Swim training of monosodium L-glutamate-obese mice improves the impaired insulin receptor tyrosine phosphorylation in pancreatic islets.", "entity1": "insulin receptor", "entity2": "tyrosine", "span1": [73, 89], "span2": [90, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"641": {"label": 1, "data": {"text": "The effect of sumatriptan, but not of LY 344864, was prevented by pretreatment with the antagonist SDZ 21-009, which displays high affinity for rat 5-HT1B receptors.", "entity1": "rat 5-HT1B", "entity2": "sumatriptan", "span1": [144, 154], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14802": {"label": 3, "data": {"text": "Treatment with TSA and the Nrf2-ARE activator resulted in increased inhibition of the TGF-\u03b2-induced myofibroblast differentiation as compared with treatment with DPI or NAC.", "entity1": "TGF-\u03b2", "entity2": "TSA", "span1": [86, 91], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10614": {"label": 1, "data": {"text": "GABA-evoked currents were completely and reversibly blocked by the competitive GABAA receptor antagonist bicuculline (IC50 = 1.7 microM), indicating expression of GABAA but not GABAC receptors.", "entity1": "GABAA receptor", "entity2": "GABA", "span1": [79, 93], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1642": {"label": 1, "data": {"text": "2-Amino-3-[3-hydroxy-5-(2-thiazolyl)-4-isoxazolyl]propionic acid (1) is a potent AMPA receptor agonist with moderate affinity for native kainic acid (KA) receptors, whereas (S)-E-4-(2,2-dimethylpropylidene)glutamic acid (3) show high affinity for the GluR5 subtype of KA receptors and much lower affinity for the GluR2 subtype of AMPA receptors.", "entity1": "GluR2", "entity2": "(S)-E-4-(2,2-dimethylpropylidene)glutamic acid", "span1": [313, 318], "span2": [173, 219]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6393": {"label": 4, "data": {"text": "In alpha(2A)-adrenoceptor transfected cells the rank order of agonist potency was A-54741 (mean pEC(50)=8.96)>dexmedetomidine (8.88)>UK-14304 (8.42)>B-HT 920 (7.05)>noradrenaline (6.92).", "entity1": "alpha(2A)-adrenoceptor", "entity2": "B-HT 920", "span1": [3, 25], "span2": [149, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4296": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B1", "entity2": "DHEAS", "span1": [258, 265], "span2": [126, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15067": {"label": 9, "data": {"text": "Our in vitro studies showed that cyclic adenosine 3',5'-monophosphate (cAMP) accumulation was not a primary cause of the ritodrine-induced SAA increase.", "entity1": "SAA", "entity2": "cyclic adenosine 3',5'-monophosphate", "span1": [139, 142], "span2": [33, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15051": {"label": 3, "data": {"text": "In general, antiproliferative activity is greatly enhanced by low levels of the glutathione synthase inhibitor l-buthionine sulfoxime.", "entity1": "glutathione synthase", "entity2": "l-buthionine sulfoxime", "span1": [80, 100], "span2": [111, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9747": {"label": 4, "data": {"text": "In distinction to yohimbine, fluparoxan shows only modest partial agonist actions at h5-HT(1A) sites versus marked antagonist actions at halpha(2)-ARs.", "entity1": "h5-HT(1A)", "entity2": "yohimbine", "span1": [85, 94], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10566": {"label": 1, "data": {"text": "To verify the hypothesis that the non-conventional partial agonist (-)-CGP12177 binds at two beta(1)-adrenoceptor sites, human beta(1)-adrenoceptors, expressed in CHO cells, were labelled with (-)-[(3)H]-CGP12177.", "entity1": "beta(1)-adrenoceptor", "entity2": "(-)-[(3)H]-CGP12177", "span1": [93, 113], "span2": [193, 212]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11568": {"label": 8, "data": {"text": "Specificity of zebrafish retinol saturase: formation of all-trans-13,14-dihydroretinol and all-trans-7,8- dihydroretinol.", "entity1": "zebrafish retinol saturase", "entity2": "all-trans-13,14-dihydroretinol", "span1": [15, 41], "span2": [56, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10478": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "broxaterol", "span1": [392, 423], "span2": [201, 211]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9119": {"label": 1, "data": {"text": "The site at which phenoxybenzamine bound to calmodulin appears to be similar to that at which certain antipsychotic agents bind, since several of them, including penfluridol, pimozide and spiroperidol, prevented the binding of phenoxybenzamine to calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [247, 257], "span2": [227, 243]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4144": {"label": 3, "data": {"text": "Here we report the re-engineering of navitoclax to create a highly potent, orally bioavailable and BCL-2-selective inhibitor, ABT-199.", "entity1": "BCL-2", "entity2": "ABT-199", "span1": [99, 104], "span2": [126, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7793": {"label": 3, "data": {"text": "We examined in cats the 1) ulcerogenic effects of selective COX-1 (SC-560, ketorolac) and COX-2 (celecoxib, meloxicam) inhibitors on the gastrointestinal mucosa, 2) effect of feeding and cimetidine on the expression of COX isoforms and prostaglandin E(2) (PGE(2)) level in the duodenum, and 3) localization of COX isoforms in the duodenum.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [90, 95], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14548": {"label": 2, "data": {"text": "Therefore, the present results show that the earlier cerebellar responses to (PhTe)(2) include disruption of cytoskeletal homeostasis that could be related with MAPK and PKA activation and reactive astrogliosis.", "entity1": "PKA", "entity2": "(PhTe)(2)", "span1": [170, 173], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7119": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "GAF-B domain", "entity2": "N", "span1": [168, 180], "span2": [97, 98]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7124": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "PDE5Delta1-534", "entity2": "C", "span1": [355, 369], "span2": [322, 323]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4722": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Wif1", "entity2": "TCDD", "span1": [404, 408], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9715": {"label": 2, "data": {"text": "Activity of the mutant delta-aminolevulinate synthase protein expressed in vitro was 15.1% compared with the normal control, but was increased up to 34.5% by the addition of pyridoxal 5'-phosphate, consistent with the clinical response of the patient to pyridoxine treatment.", "entity1": "delta-aminolevulinate synthase", "entity2": "pyridoxal 5'-phosphate", "span1": [23, 53], "span2": [174, 196]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6152": {"label": 1, "data": {"text": "Drug dependent changes in the NMR heteronuclear single-quantum coherence spectra of [methyl-13C]Met-labeled cTnC indicate that bepridil and trifluoperazine bind to similar sites but only in the presence of Ca2+.", "entity1": "cTnC", "entity2": "trifluoperazine", "span1": [108, 112], "span2": [140, 155]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7252": {"label": 4, "data": {"text": "PEA was a potent and full agonist at each species of TAAR1, whereas TYR was a full agonist for the rodent TAAR1s but was a partial agonist at h-rChTAAR1.", "entity1": "TAAR1", "entity2": "PEA", "span1": [53, 58], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6835": {"label": 3, "data": {"text": "In addition, both drugs significantly reduced PGE2 levels (P<0.05) 6-h following LPS injection, whereas the probable COX-1 prostanoid TXB2 was significantly reduced by phenylbutazone (P<0.05), but not etodolac.", "entity1": "COX-1", "entity2": "phenylbutazone", "span1": [117, 122], "span2": [168, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4733": {"label": 8, "data": {"text": "These results indicate transcription of FDX1 is regulated by the NR5A family and cAMP signaling, and participates in steroid hormone production in ovarian granulosa cells.", "entity1": "FDX1", "entity2": "steroid", "span1": [40, 44], "span2": [117, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6618": {"label": 0, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "Asn", "span1": [3, 9], "span2": [70, 73]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3952": {"label": 2, "data": {"text": "CONCLUSIONS A diet that partially replaces carbohydrate with unsaturated fat may improve insulin sensitivity in a population at risk for cardiovascular disease.", "entity1": "insulin", "entity2": "carbohydrate", "span1": [89, 96], "span2": [43, 55]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12164": {"label": 1, "data": {"text": "Effects of minocycline on Fas-mediated fulminant hepatitis in mice.", "entity1": "Fas", "entity2": "minocycline", "span1": [26, 29], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14047": {"label": 2, "data": {"text": "CONCLUSIONS: Aspirin is an inhibitor of mTOR and an activator of AMPK, targeting regulators of intracellular energy homeostasis and metabolism.", "entity1": "AMPK", "entity2": "Aspirin", "span1": [65, 69], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"788": {"label": 1, "data": {"text": "Analysis of splice variants and site-directed mutants of the AMPA receptor GluR3 expressed in Xenopus oocytes has shown that lithium produces a large potentiation of the GluR3 flop splice variant and suggested that lithium might inhibit rapid desensitization, which is characteristic of this receptor (Karkanias, N. and Papke, R., Subtype-specific effects of lithium on glutamateglutamate receptor function.", "entity1": "glutamate receptor", "entity2": "glutamate", "span1": [379, 397], "span2": [370, 379]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3175": {"label": 2, "data": {"text": "Polymorphisms in dopamine transporter (SLC6A3) are associated with stimulant effects of D-amphetamine: an exploratory pharmacogenetic study using healthy volunteers.", "entity1": "SLC6A3", "entity2": "D-amphetamine", "span1": [39, 45], "span2": [88, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10652": {"label": 3, "data": {"text": "Valdecoxib potently inhibits recombinant COX-2, with an IC(50) of 0.005 microM; this compares with IC values of 0.05 microM for celecoxib, 0.5 microM for rofecoxib, and 5 microM for etoricoxib.", "entity1": "COX-2", "entity2": "Valdecoxib", "span1": [41, 46], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"73": {"label": 1, "data": {"text": "However, salicylate moiety appears to interfere with aspirin inhibitory action on platelets and vascular COX.", "entity1": "COX", "entity2": "salicylate", "span1": [105, 108], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2167": {"label": 0, "data": {"text": "Binding sites for hERG blockers have been mapped within the inner cavity of the channel and include aromatic residues in the S6 helix (Tyr-652, Phe-656) and residues in the pore helix (Thr-623, Ser-624, Val-625).", "entity1": "hERG", "entity2": "Ser", "span1": [18, 22], "span2": [194, 197]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6282": {"label": 3, "data": {"text": "Although the IC50 value of meloxicam for inhibition of COX-1 was 10-fold higher than the IC50 value of COX-2 in vitro, this biochemical selectivity was inadequate to clearly separate the effects of meloxicam on the two isozymes after oral dosing as a function of the daily dose and interindividual variation in steady-state plasma levels.", "entity1": "COX-1", "entity2": "meloxicam", "span1": [55, 60], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"890": {"label": 1, "data": {"text": "Here we compared the action of N(5)-substituted derivatives on recombinant rat neuronal nitric oxide synthase with their effects on dihydropteridine reductase (EC 1.6.99.7) and phenylalanine hydroxylase (EC 1.14.16.1),the well-studied classical H(4)biopterin-dependent reactions.", "entity1": "dihydropteridine reductase", "entity2": "N(5)", "span1": [132, 158], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2011": {"label": 9, "data": {"text": "In addition, cysteinyl leukotrienes per se failed to upregulate the IL-5 production.", "entity1": "IL-5", "entity2": "cysteinyl leukotrienes", "span1": [68, 72], "span2": [13, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15158": {"label": 2, "data": {"text": "In perifusion studies, FSH\u03b2 mRNA levels and FSH\u03b2LUC activities were increased by pulsatile GnRH, with significantly greater increases at low compared with high pulse frequencies.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [44, 48], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12610": {"label": 1, "data": {"text": "Cyclothiazide (330 microM) shifted the concentration-response curve for the effects of GYKI 52466 on AMPA receptor-mediated e.p.s.c.", "entity1": "AMPA receptor", "entity2": "GYKI 52466", "span1": [101, 114], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4530": {"label": 3, "data": {"text": "Our results showed that low dose BPA and E2 could influence the mammosphere area of iDMECs and upregulate the expression level of Oct4 and Nanog proteins, while only BPA could downregulate the expression of E-cadherin protein.", "entity1": "E-cadherin", "entity2": "BPA", "span1": [207, 217], "span2": [166, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8181": {"label": 8, "data": {"text": "Furthermore, MDZ caused mechanism-based inactivation of cytochrome P450 3A-dependent TRZ 1'-hydroxylation in mouse, rat and human intestinal microsomes with similar potencies.", "entity1": "cytochrome P450 3A", "entity2": "TRZ", "span1": [56, 74], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11549": {"label": 8, "data": {"text": "BACKGROUND: Histamine synthesized by histidine decarboxylase (HDC) from L-histidine is a major chemical mediator in the development of nasal allergy which is characterized by nasal hypersensitivity.", "entity1": "histidine decarboxylase", "entity2": "L-histidine", "span1": [37, 60], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3447": {"label": 1, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "human dopamine transporter", "entity2": "(+/-)-Modafinil", "span1": [167, 193], "span2": [9, 24]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2588": {"label": 8, "data": {"text": "GPxs reduce hydroperoxides to the corresponding alcohols by means of glutathione (GSH).", "entity1": "GPxs", "entity2": "alcohols", "span1": [0, 4], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14640": {"label": 8, "data": {"text": "The higher in vitro catalytic efficiency of DCK24Val toward dFdC monophosphorylation may be relevant to dFdC clinical response.", "entity1": "DCK", "entity2": "dFdC", "span1": [44, 47], "span2": [104, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5918": {"label": 3, "data": {"text": "Acetylation of phenelzine at the N2 position presumably interferes with the inhibition of the transaminase enzymes for gamma-aminobutyric acid and alanine.", "entity1": "transaminase", "entity2": "alanine", "span1": [94, 106], "span2": [147, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10154": {"label": 1, "data": {"text": "EM-800 and EM-652 are the most potent pure antiestrogens and EM-652 has the highest affinity of all antiestrogens to ER.", "entity1": "ER", "entity2": "EM-652", "span1": [117, 119], "span2": [11, 17]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"570": {"label": 2, "data": {"text": "Tomudex treatment resulted in the decrease in p27(kip1) expression, with an increase in cyclin E and cdk2 protein expression and kinase activities 24 h after a 2-h exposure.", "entity1": "kinase", "entity2": "Tomudex", "span1": [129, 135], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11992": {"label": 2, "data": {"text": "This initial action was accompanied by up-regulation of cyclooxygenase-2 (COX-2), an important inflammation marker within 1h after TCDD treatment.", "entity1": "cyclooxygenase-2", "entity2": "TCDD", "span1": [56, 72], "span2": [131, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15420": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "ABCG5/8", "entity2": "cholesterol", "span1": [210, 217], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"15847": {"label": 2, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "ABCG1", "entity2": "24-OHC", "span1": [28, 33], "span2": [49, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7726": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "Luteinizing hormone-releasing hormone", "entity2": "buserelin", "span1": [0, 37], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14913": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "steroids", "span1": [257, 260], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14656": {"label": 3, "data": {"text": "Here we present boronic and borinic acid derivatives as a new class of potent and nontoxic APT inhibitors.", "entity1": "APT", "entity2": "borinic acid", "span1": [91, 94], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3361": {"label": 3, "data": {"text": "Although L-VGCC inhibition by BDZs occurred at concentrations that are possibly too high to be clinically relevant and is not likely to play a role in the up-regulation of L-VGCCs during long-term treatment, pentobarbital and ethanol inhibited L-VGCCs at clinically relevant concentrations.", "entity1": "L-VGCCs", "entity2": "pentobarbital", "span1": [244, 251], "span2": [208, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6205": {"label": 3, "data": {"text": "Cocaine block of hH1 channels was greater than block of mu1 channels at voltages between -120 mV and -90 mV, suggesting that greater steady-state inactivation of hH1 channels in this voltage range makes them more susceptible to cocaine block.", "entity1": "hH1 channels", "entity2": "cocaine", "span1": [162, 174], "span2": [228, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11132": {"label": 9, "data": {"text": "TREK-1 currents are insensitive to pharmacological agents that block TWIK-1 activity such as quinine and quinidine.", "entity1": "TREK-1", "entity2": "quinine", "span1": [0, 6], "span2": [93, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11026": {"label": 3, "data": {"text": "It was found that a single intragastric gavage by L-methionine resulted in inhibition of endothelium-dependent relaxation, markedly increased the serum level of malondialdehyde and decreased the activity of PON1 and SOD, similarly decreased the level of NO in the serum; but had no effects on endothelium-independent relaxation and angiotensin-converting enzyme activity compared with the control group.", "entity1": "SOD", "entity2": "L-methionine", "span1": [216, 219], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15236": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP2B1", "entity2": "silybin A", "span1": [24, 31], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"12604": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "kringle domain", "entity2": "N", "span1": [261, 275], "span2": [316, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14320": {"label": 1, "data": {"text": "Results showed that DMF increased nuclear levels of Nrf2, and both DMF and adenovirus-mediated overexpression of Nrf2 (Ad-Nrf2) decreased PAI-1, alpha-smooth muscle actin (alpha-SMA), fibronectin and type 1 collagen expression in TGF-beta-treated rat mesangial cells (RMCs) and renal fibroblast cells (NRK-49F).", "entity1": "TGF-beta", "entity2": "DMF", "span1": [230, 238], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8705": {"label": 2, "data": {"text": "Taken together, our results indicate that arsenic indeed upregulates the AT1R expression, thus highlighting a role of arsenic-induced aberrant AT1R signaling in the pathogenesis of hypertension.", "entity1": "AT1R", "entity2": "arsenic", "span1": [143, 147], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2661": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE3", "entity2": "milrinone", "span1": [132, 136], "span2": [138, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12827": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "PLK", "entity2": "PLP", "span1": [114, 117], "span2": [69, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8057": {"label": 3, "data": {"text": "Metformin-mediated downregulation of p38 mitogen-activated protein kinase-dependent excision repair cross-complementing 1 decreases DNA repair capacity and sensitizes human lung cancer cells to paclitaxel.", "entity1": "p38", "entity2": "Metformin", "span1": [37, 40], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2608": {"label": 1, "data": {"text": "Pharmacogenetic analysis of two genes, the warfarin metabolic enzyme CYP2C9 and warfarin target enzyme, vitamin K epoxide reductase complex 1 VKORC1, confirmed their influence on warfarin maintenance dose.", "entity1": "vitamin K epoxide reductase complex 1", "entity2": "warfarin", "span1": [104, 141], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9490": {"label": 3, "data": {"text": "Monoamine uptake inhibitors structurally analogous to cocaine (cocaethylene, CFT, betaCIT, CPT, (+)-cocaine, norcocaine, and benztropine) also produced this rapid pressor response, whereas structurally unrelated uptake inhibitors with diverse monoamine transporter selectivities (BTCP, indatraline, GBR 12935, mazindol, nomifensine, and zimeldine) either did not produce a rapid pressor response or produced only a small pressor response.", "entity1": "monoamine transporter", "entity2": "indatraline", "span1": [243, 264], "span2": [286, 297]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, 9]},
	"9898": {"label": 1, "data": {"text": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid (WY-14,643), a specific ligand of the PPAR-alpha subtype, causes the most dramatic increase in UCP-3 mRNA, whereas troglitazone, a specific activator of PPAR-gamma, also significantly increases UCP-3 mRNA abundance in skeletal muscle of lactating mice.", "entity1": "PPAR-alpha", "entity2": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid", "span1": [94, 104], "span2": [0, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10809": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-1", "entity2": "meloxicam", "span1": [0, 5], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11494": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "COX", "entity2": "ketorolac", "span1": [42, 45], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4717": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "R-spondins", "entity2": "TCDD", "span1": [292, 302], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10343": {"label": 2, "data": {"text": "The results show that transient arsenite pre-treatment induces Hsp72, HO-1 and, to a lesser extent, Hsp27; it reduces H2O2-induced astrocyte death; and it causes selective activation of Akt following H2O2.", "entity1": "Hsp27", "entity2": "arsenite", "span1": [100, 105], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14595": {"label": 3, "data": {"text": "In addition, 17-AAG treatment reduced cell viability, CDK2, CDK4, cyclin E, cyclin D1, and phosphorylated Rb levels in AhR-expressing lung AD cells.", "entity1": "phosphorylated Rb", "entity2": "17-AAG", "span1": [91, 108], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5354": {"label": 2, "data": {"text": "Results: The administration of prallethrin 1.6% w/w created significant increased changes in the levels of total WBC, lymphocytes, RBC, hemoglobin, packed cell volume, platelets, mean corpuscular volume, and mean corpuscular hemoglobin in rats after 24, 48, and 72\u2009h of continuous inhalation; however, there was a significant reduction in neutrophils at transient reduction in the monocytes after 24 and 48\u2009h to return to normal after 72\u2009h. Significant increases in the levels of CK, \u03b3-GT, SOD, NO, MDA, AFP, IL-2, and TNF\u03b1 were recorded.", "entity1": "hemoglobin", "entity2": "prallethrin", "span1": [136, 146], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6539": {"label": 1, "data": {"text": "Regulation of norepinephrine transporter abundance by catecholamines and desipramine in vivo.", "entity1": "norepinephrine transporter", "entity2": "desipramine", "span1": [14, 40], "span2": [73, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"889": {"label": 1, "data": {"text": "Here we compared the action of N(5)-substituted derivatives on recombinant rat neuronal nitric oxide synthase with their effects on dihydropteridine reductase (EC 1.6.99.7) and phenylalanine hydroxylase (EC 1.14.16.1),the well-studied classical H(4)biopterin-dependent reactions.", "entity1": "rat neuronal nitric oxide synthase", "entity2": "N(5)", "span1": [75, 109], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14282": {"label": 0, "data": {"text": "The mutant Fc domain (AglycoT-Fc1004) contained a total of 5 amino acid substitutions that conferred an activating to inhibitory ratio of 25 (A/I ratio; FcyRIIa-R131:Fc\u03b3RIIb).", "entity1": "FcyRIIa", "entity2": "amino acid", "span1": [153, 160], "span2": [61, 71]}, "weak_labels": [0, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"738": {"label": 1, "data": {"text": "Using the alpha1 and alpha2-adrenoceptor antagonists, prazosin and idazoxane, we also demonstrate the role of the alpha-adrenoceptors in the augmentation of venlafaxine-induced changes.", "entity1": "alpha-adrenoceptors", "entity2": "venlafaxine", "span1": [114, 133], "span2": [157, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6345": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "losartan", "span1": [18, 21], "span2": [184, 192]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11667": {"label": 8, "data": {"text": "Immunohistochemical characterization of pyrimidine synthetic enzymes, thymidine kinase-1 and thymidylate synthase, in various types of cancer.", "entity1": "thymidylate synthase", "entity2": "pyrimidine", "span1": [93, 113], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"403": {"label": 3, "data": {"text": "Indomethacin abolished the inhibitory effect of acetazolamide on CA I and CA II.", "entity1": "CA I", "entity2": "acetazolamide", "span1": [65, 69], "span2": [48, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12319": {"label": 2, "data": {"text": "Ribavirin unregulated ELL (eleven-nineteen lysine-rich leukaemia) 3 mRNA expression before F7 up-regulation.", "entity1": "eleven-nineteen lysine-rich leukaemia) 3", "entity2": "Ribavirin", "span1": [27, 67], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5836": {"label": 3, "data": {"text": "Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida (Ki = 30 nM).", "entity1": "squalene epoxidase", "entity2": "Terbinafine", "span1": [53, 71], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"159": {"label": 2, "data": {"text": "Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex.", "entity1": "Acetylcholinesterase", "entity2": "oximes", "span1": [0, 20], "span2": [162, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15313": {"label": 1, "data": {"text": "The serum or dexamethasone-induced oscillation in the expression of DRD3 in cells was abrogated by the downregulation or overexpression of REV-ERB\u03b1, suggesting that REV-ERB\u03b1 functions as a regulator of DRD3 oscillations in the cellular autonomous clock.", "entity1": "REV-ERB\u03b1", "entity2": "dexamethasone", "span1": [139, 147], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8771": {"label": 3, "data": {"text": "In support of this observation, elongation can be reversed by the tyrosine kinase inhibitor SU5402, mRNA for the FGFR antagonist sprouty4, or FGF8 morpholino.", "entity1": "tyrosine kinase", "entity2": "SU5402", "span1": [66, 81], "span2": [92, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6291": {"label": 1, "data": {"text": "(-)-Pindolol, which possesses significant affinity for 5-HT1A, 5-HT1B, and beta 1/2-adrenergic receptors (AR)s, dose-dependently increased extracellular levels of dopamine (DA) and noradrenaline (NAD) versus 5-HT, in dialysates of the frontal cortex (FCX), but not accumbens and striatum, of freely-moving rats.", "entity1": "5-HT1B", "entity2": "(-)-Pindolol", "span1": [63, 69], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4050": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "MAPK", "entity2": "neoechinulin A", "span1": [129, 133], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10391": {"label": 3, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "AChE", "entity2": "rivastigmine", "span1": [233, 237], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13809": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "kinase", "entity2": "Gefitinib", "span1": [247, 253], "span2": [138, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5564": {"label": 2, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "IL-6", "entity2": "GSSG", "span1": [231, 235], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4796": {"label": 8, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP2D", "entity2": "DXM", "span1": [138, 143], "span2": [106, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9293": {"label": 2, "data": {"text": "Furthermore, the phosphorylation of myosin light chain produced by norepinephrine was greater than that produced by clonidine.", "entity1": "myosin light chain", "entity2": "clonidine", "span1": [36, 54], "span2": [116, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3337": {"label": 1, "data": {"text": "Rasagiline protects against alpha-synuclein induced sensitivity to oxidative stress in dopaminergic cells.", "entity1": "alpha-synuclein", "entity2": "Rasagiline", "span1": [28, 43], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10565": {"label": 1, "data": {"text": "To verify the hypothesis that the non-conventional partial agonist (-)-CGP12177 binds at two beta(1)-adrenoceptor sites, human beta(1)-adrenoceptors, expressed in CHO cells, were labelled with (-)-[(3)H]-CGP12177.", "entity1": "human beta(1)-adrenoceptors", "entity2": "(-)-[(3)H]-CGP12177", "span1": [121, 148], "span2": [193, 212]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6695": {"label": 3, "data": {"text": "Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively).", "entity1": "TRPM8", "entity2": "BCTC", "span1": [96, 101], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15023": {"label": 3, "data": {"text": "In agreement with these data, the exogenous treatment of SAH or inhibition of SAHH by specific siRNA or another type of inhibitor, 3-deazaadenosine (DAZA), similarly resulted in antitumorigenic responses, suppressive activity on Src, the alteration of actin cytoskeleton, and a change of the colocalization pattern between actin and Src.", "entity1": "SAHH", "entity2": "DAZA", "span1": [78, 82], "span2": [149, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"147": {"label": 3, "data": {"text": "CRH caused a rise in plasma ACTH after both loperamide (from 30 +/- 16.6 to a peak of 108 +/- 31 pmol/l) and placebo (from 98.5 +/- 47 to 211 +/- 61.7 pmol/l): the interaction between treatments and time was significant, and the first phase of CRH-induced ACTH secretion was significantly lower after loperamide.", "entity1": "CRH", "entity2": "loperamide", "span1": [244, 247], "span2": [301, 311]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3224": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "quercetin", "span1": [282, 284], "span2": [160, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10031": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Lys", "span1": [126, 138], "span2": [63, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7242": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "para-tyramine", "span1": [192, 229], "span2": [61, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14228": {"label": 5, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b1", "entity2": "1H-pyrazole dihydrochloride", "span1": [288, 291], "span2": [376, 403]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7349": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT4", "entity2": "alanine", "span1": [342, 347], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5688": {"label": 2, "data": {"text": "Sprague-Dawley rats treated with a non-selective cannabinoid agonist (CP55940, 50\u03bcg/kg, 7 days, i.p.) showed enhanced co-immunoprecipitation of \u03b2-Arrestin 2 and ERK1/2, enhanced pERK protein levels, and enhanced expression of \u03b2-Arrestin 2 mRNA and protein levels in PFCx.", "entity1": "\u03b2-Arrestin 2", "entity2": "CP55940", "span1": [226, 238], "span2": [70, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1791": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "kinase", "entity2": "PKI166", "span1": [175, 181], "span2": [132, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7848": {"label": 2, "data": {"text": "Collectively, we have elucidated a basal mechanism for ribavirin-induced FVII mRNA up-regulation by acceleration of transcription elongation, which may be crucial in understanding its pleiotropic functions in\u00a0vivo.", "entity1": "FVII", "entity2": "ribavirin", "span1": [73, 77], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3768": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "cyclooxygenase-2", "entity2": "CCl(4)", "span1": [192, 208], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4683": {"label": 1, "data": {"text": "For this purpose, C57BL6 mice were injected intraperitoneally with V(5+) (5\u00a0mg/kg) in the absence and presence of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) (15\u00a0\u03bcg/kg) for 6 and 24\u00a0h. Furthermore, isolated hepatocytes from C57BL6 mice were treated with V(5+) (5, 10, and 20\u00a0\u03bcM) in the absence and presence of TCDD (1 nM) for 3, 6, 12, and 24\u00a0h. In vivo, V(5+) alone did not significantly alter Cyp1a1, Cyp1a2, or Cyp1b1 mRNA, protein, or catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "V(5+)", "span1": [413, 419], "span2": [354, 359]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12234": {"label": 1, "data": {"text": "Photolytic release of free alanine results in the generation of significant transient current components in HEK293 cells expressing the ASCT2, SNAT1, and SNAT2 proteins.", "entity1": "ASCT2", "entity2": "alanine", "span1": [136, 141], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5757": {"label": 2, "data": {"text": "MNU-induced lesions presented markers indicative of an aggressive phenotype: lack of basal cells, rupture of the smooth muscle cell layer, loss of E-cadherin, and high MGMT staining.", "entity1": "MGMT", "entity2": "MNU", "span1": [168, 172], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14019": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "NF-kappaB", "entity2": "colchicoside", "span1": [115, 124], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14278": {"label": 5, "data": {"text": "In vitro metabolism of the 5-hydroxytryptamine1B receptor antagonist elzasonan.", "entity1": "5-hydroxytryptamine1B", "entity2": "elzasonan", "span1": [27, 48], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2459": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "adenosine triphosphate binding cassette (ABC)-transporter", "entity2": "paclitaxel", "span1": [4, 61], "span2": [161, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4557": {"label": 3, "data": {"text": "In addition, ethanol induced degradation of DNA methyltransferases (DNMT-1, DNMT-3a, and DNMT-3b), as well as the methyl CpG-binding proteins (MeCP-2, MBD-2 and MBD-3), in MEF cells by the proteasomal pathway.", "entity1": "DNMT-", "entity2": "ethanol", "span1": [68, 73], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14956": {"label": 2, "data": {"text": "Bile acids are signaling molecules that activate nuclear receptors, such as farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, and vitamin D receptor, and play a critical role in the regulation of lipid, glucose, energy, and drug metabolism.", "entity1": "vitamin D receptor", "entity2": "Bile acids", "span1": [157, 175], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6625": {"label": 1, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "ornithine", "span1": [3, 9], "span2": [142, 151]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10066": {"label": 3, "data": {"text": "Omapatrilat, the prototypical vasopeptidase inhibitor, inhibits not only ACE but also neutral endopeptidase.", "entity1": "vasopeptidase", "entity2": "Omapatrilat", "span1": [30, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2537": {"label": 8, "data": {"text": "Reductive detoxification of arylhydroxylamine carcinogens by human NADH cytochrome b5 reductase and cytochrome b5.", "entity1": "human NADH cytochrome b5 reductase", "entity2": "arylhydroxylamine", "span1": [61, 95], "span2": [28, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15710": {"label": 3, "data": {"text": "Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone.", "entity1": "MMP-9", "entity2": "2-hydroxychalcone", "span1": [108, 113], "span2": [13, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11775": {"label": 1, "data": {"text": "Western blot analyses showed significant effects of Pb exposure on DNMT1, DNMT3a, and MeCP2 expression, with effects often seen at the lowest level of exposure and modified by sex and developmental window of Pb exposure.", "entity1": "DNMT3a", "entity2": "Pb", "span1": [74, 80], "span2": [52, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14532": {"label": 1, "data": {"text": "These results reveal, for the first time, the differential distribution of P-CREB in fast- and slow-twitch muscles, which might support the crucial role of cAMP-dependent signaling in controlling the synapse-specific expression of ColQ-1a in fast-twitch muscles.", "entity1": "ColQ-1a", "entity2": "cAMP", "span1": [231, 238], "span2": [156, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16004": {"label": 2, "data": {"text": "Moreover, we also demonstrate that puerarin functions at least partially through activation of MEK/ERK and PI3K/Akt signaling.", "entity1": "PI3K", "entity2": "puerarin", "span1": [107, 111], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13952": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g. isoprenaline) had little affinity-selectivity.", "entity1": "beta(2)-adrenoceptor", "entity2": "isoprenaline", "span1": [35, 55], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1140": {"label": 1, "data": {"text": "Binding site of amiloride to urokinase plasminogen activator depends on species.", "entity1": "urokinase plasminogen activator", "entity2": "amiloride", "span1": [29, 60], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14586": {"label": 1, "data": {"text": "Alleles of RPB1 (RPO21) with elevated slippage rates were identified among 6-azauracil-sensitive mutants and were also isolated using a slippage-dependent reporter gene.", "entity1": "RPO21", "entity2": "6-azauracil", "span1": [17, 22], "span2": [75, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7901": {"label": 1, "data": {"text": "TCDD acts through the aryl hydrocarbon receptor (AhR), which interacts with the androgen receptor (AR).", "entity1": "AhR", "entity2": "TCDD", "span1": [49, 52], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9155": {"label": 3, "data": {"text": "The inhibitory effect of (+)-, (-)-, (+/-)-gossypol and (+/-)-gossypol acetic acid upon testicular cytosolic LDH-X was measured in vitro.", "entity1": "LDH-X", "entity2": "(+)-, (-)-, (+/-)-gossypol", "span1": [109, 114], "span2": [25, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3176": {"label": 2, "data": {"text": "Polymorphisms in dopamine transporter (SLC6A3) are associated with stimulant effects of D-amphetamine: an exploratory pharmacogenetic study using healthy volunteers.", "entity1": "dopamine transporter", "entity2": "D-amphetamine", "span1": [17, 37], "span2": [88, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4794": {"label": 8, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP2D", "entity2": "dextromethorphan", "span1": [138, 143], "span2": [88, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13503": {"label": 3, "data": {"text": "In this study the neuromuscular blocking drug vecuronium and the controls gallamine and pancuronium slowed the rate of atropine induced [(3)H]N-methylscopolamine dissociation from Chinese hamster ovary cells expressing recombinant human muscarinic M2 receptors K(off) values min(-1); vecuronium (125 nM), atropine 0.45+/-0.07+blocker 0.04+/-0.02; gallamine (21 nM), atropine 0.42+/-0.05+blocker 0.15+/-0.04; pancuronium(21 nM), atropine 0.36+/-0.03+blocker 0.03+/-0.01).", "entity1": "human muscarinic M2 receptors", "entity2": "gallamine", "span1": [231, 260], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9700": {"label": 5, "data": {"text": "Pretreatment with the 5-HT1A antagonist WAY-100,635 (10 micrograms/kg i.v.)", "entity1": "5-HT1A", "entity2": "WAY-100,635", "span1": [22, 28], "span2": [40, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3456": {"label": 1, "data": {"text": "RESULTS: (+/-)-, R-, and S-modafinil bind to the DAT and inhibit DA uptake less potently than cocaine, with R-modafinil having approximately threefold higher affinity than its S-enantiomer.", "entity1": "DAT", "entity2": "R-modafinil", "span1": [49, 52], "span2": [108, 119]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15600": {"label": 1, "data": {"text": "In the current study, we crossed mdr1a.fLUC mice into the pxr knockout (pxr(-/-)) genetic background and injected mice with pregnenolone-16\u03b1-carbonitrile (PCN), a strong PXR ligand, and two therapeutically relevant taxanes, paclitaxel and docetaxel.", "entity1": "PXR", "entity2": "PCN", "span1": [170, 173], "span2": [155, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9812": {"label": 1, "data": {"text": "To further analyze the mechanism governing the Ca2+ channel-Mibefradil interaction, we examined the effect of Mibefradil on various recombinant Ca2+ channels expressed in mammalian cells from their cloned cDNAs, using Ca2+ as the permeant ion at physiological concentration.", "entity1": "Ca2+ channel", "entity2": "Mibefradil", "span1": [47, 59], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12742": {"label": 1, "data": {"text": "Pertussis toxin normalised isoproterenol responses in NCX cells, indicating that beta2AR effects were mediated by Gi.", "entity1": "beta2AR", "entity2": "isoproterenol", "span1": [81, 88], "span2": [27, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13698": {"label": 2, "data": {"text": "Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimod.", "entity1": "TLR7", "entity2": "imiquimod", "span1": [17, 21], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2416": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "NOS", "entity2": "nitric oxide", "span1": [200, 203], "span2": [21, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"233": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D1 receptor", "entity2": "(-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine", "span1": [153, 173], "span2": [196, 294]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1906": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "5-fluorouracil", "span1": [96, 119], "span2": [71, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14772": {"label": 2, "data": {"text": "Exogenous ATP transiently activated Akt and, inhibiting phosphatidylinositol 3-kinase (PI3K) or Akt as well as dominant-negative Akt mutant, reduced ATP-dependent 2-NBDG uptake and Akt phosphorylation.", "entity1": "Akt", "entity2": "ATP", "span1": [36, 39], "span2": [10, 13]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13681": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imiquimod", "span1": [100, 104], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10093": {"label": 8, "data": {"text": "Three replicate studies in the oral surgery model of acute pain used submucosal microdialysis sample collection for the measurement of prostaglandin E2 (PGE2; a product of both COX-1 and COX-2) and thromboxane B2 (as a biomarker for COX-1 activity) with parallel assessments of pain.", "entity1": "COX-2", "entity2": "PGE2", "span1": [187, 192], "span2": [153, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10098": {"label": 1, "data": {"text": "These data indicate that a [3H]dofetilide binding assay using HERG membranes may help identify compounds that prolong the QT interval.", "entity1": "HERG", "entity2": "[3H]dofetilide", "span1": [62, 66], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5803": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "amino acids", "span1": [125, 145], "span2": [244, 255]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11571": {"label": 8, "data": {"text": "zRetSat A also saturated the 13-14 or 7-8 double bonds of all-trans-3,4-didehydroretinol (vitamin A2), a second endogenous form of vitamin A in zebrafish.", "entity1": "zRetSat A", "entity2": "all-trans-3,4-didehydroretinol", "span1": [0, 9], "span2": [58, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14223": {"label": 4, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b2", "entity2": "2,3-bis(4-hydroxyphenyl)-propionitrile", "span1": [218, 221], "span2": [235, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6649": {"label": 0, "data": {"text": "Of 18 mutations where hNET amino acid residues were exchanged with those of the human dopamine transporter, MrIA had increased potency for inhibition of [3H]norepinephrine uptake for three mutations (in predicted extracellular loops 3 and 4 and transmembrane domain (TMD) 8) and decreased potency for one mutation (in TMD6 and intracellular loop (IL) 3).", "entity1": "hNET", "entity2": "amino acid", "span1": [22, 26], "span2": [27, 37]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11043": {"label": 3, "data": {"text": "In subjects with dysmenorrhea the increase in pain following the administration of vasopressin was significantly lower during atosiban than during placebo infusion.", "entity1": "vasopressin", "entity2": "atosiban", "span1": [83, 94], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2347": {"label": 1, "data": {"text": "Lutein and eicosapentaenoic acid interact to modify iNOS mRNA levels through the PPARgamma/RXR pathway in chickens and HD11 cell lines.", "entity1": "iNOS", "entity2": "eicosapentaenoic acid", "span1": [52, 56], "span2": [11, 32]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12270": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1b)", "entity2": "vasopressin", "span1": [154, 159], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12024": {"label": 1, "data": {"text": "The specificity of progestagens for the progesterone receptors in the cytosol fraction of MCF-7 cells was similar to that for progesterone receptors in human and rabbit myometrial cytosol but different from that for the progesterone receptor in rat myometrial cytosol.", "entity1": "progesterone receptors", "entity2": "progestagens", "span1": [40, 62], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4569": {"label": 4, "data": {"text": "The A2A adenosine receptor agonist CGS21680 (C23H29N7O6.HCl.xH2O) (0.001-0.1 \u03bcM) did not alter NE oxidation currents.", "entity1": "A2A adenosine receptor", "entity2": "CGS21680", "span1": [4, 26], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10677": {"label": 3, "data": {"text": "The purpose of the present study was to confirm the duration of TT-235 to block oxytocin-induced uterine contractions in estrous rats.", "entity1": "oxytocin", "entity2": "TT-235", "span1": [80, 88], "span2": [64, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2662": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE1", "entity2": "8-methoxymethyl-3-isobutyl-1-methylxanthine", "span1": [12, 16], "span2": [18, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3657": {"label": 9, "data": {"text": "Overall, our data suggest that (1) normal AChE activity is not required for secondary motoneuron development and (2) spontaneous tail contractions at 26 hpf are sensitive to paraoxon exposure, an effect that may be independent of AChE inhibition.", "entity1": "AChE", "entity2": "paraoxon", "span1": [230, 234], "span2": [174, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13905": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "Kir6.2", "entity2": "metformin", "span1": [183, 189], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5608": {"label": 1, "data": {"text": "Intracellular K+ is required for the inactivation-induced high-affinity binding of cisapride to HERG channels.", "entity1": "HERG", "entity2": "K+", "span1": [96, 100], "span2": [14, 16]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5954": {"label": 5, "data": {"text": "Although numerous mechanisms of action of pimozide and thioridazine have been identified, both drugs are calmodulin antagonists at drug concentrations that inhibit breast cancer cell growth in vitro.", "entity1": "calmodulin", "entity2": "thioridazine", "span1": [105, 115], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12061": {"label": 9, "data": {"text": "In the insulin-hypoglycemia test (0.15 IU/kg BW), neither the ACTH peak nor the area under the curve of ACTH was affected by loperamide.", "entity1": "ACTH", "entity2": "loperamide", "span1": [62, 66], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13588": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "DVS", "span1": [6, 10], "span2": [159, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15748": {"label": 2, "data": {"text": "Our data showed that chronic ethanol over-activated CYP2E1 but suppressed HO-1 with concurrent hepatic oxidative damage, which was partially normalized by quercetin (100mg/kg.bw.).", "entity1": "CYP2E1", "entity2": "ethanol", "span1": [52, 58], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9874": {"label": 3, "data": {"text": "RESULTS: Exposure of in vitro differentiated subcutaneous adipocytes from young normal-weight females to 1 microgram/ml troglitazone for 72 h caused a reduction of both PAI-1 secretion (by 29 +/- 5%; p < 0.01) and PAI-1 mRNA expression (by 26 +/- 3%; p < 0.05).", "entity1": "PAI-1", "entity2": "troglitazone", "span1": [214, 219], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4983": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "CK-MB", "entity2": "Crocin", "span1": [91, 96], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2966": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "Y612F", "entity2": "vardenafil", "span1": [64, 69], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8656": {"label": 5, "data": {"text": "Intraplantar or intrathecal administered Ph\u03b11\u03b2 reduced both nocifensive behavior and mechanical hypersensitivity induced by capsaicin similarly to that observed with SB366791, a specific TRPV1 antagonist.", "entity1": "TRPV1", "entity2": "SB366791", "span1": [187, 192], "span2": [166, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9802": {"label": 3, "data": {"text": "Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid.", "entity1": "human and rat dihydroorotate dehydrogenase", "entity2": "atovaquone", "span1": [26, 68], "span2": [72, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6330": {"label": 8, "data": {"text": "The decrease and recovery of [3H]-5-HT uptake correlated highly (r = 0.93) with the recovery of SERT binding.", "entity1": "SERT", "entity2": "[3H]-5-HT", "span1": [96, 100], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14833": {"label": 1, "data": {"text": "As the Mg(2+) ion concentration was increased, there was a consistent decrease of the enzyme catalytic turnover from 0.31 s(-1) (0 \u03bcM Mg(2+)) to 0.050 s(-1) (6000 \u03bcM Mg(2+)) and a distinct shift in steady-state conformational population from one that favors the ALDH1-NADH complex with the shorter fluorescence lifetime (33% excess) in the absence of magnesium ion to one that favors the ALDH1-NADH complex with the longer fluorescence lifetime (13% excess) at 6000 \u03bcM Mg(2+).", "entity1": "ALDH1", "entity2": "NADH", "span1": [262, 267], "span2": [268, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3596": {"label": 0, "data": {"text": "Interestingly, recent crystallographic evidence identified that ifenprodil, unlike zinc, binds at the interface of the GluN1/GluN2B amino terminal domain dimer by an induced-fit mechanism.", "entity1": "GluN1", "entity2": "amino", "span1": [119, 124], "span2": [132, 137]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8454": {"label": 9, "data": {"text": "Hinokitiol did not influence the binding of a fluorescent triflavin probe to the \u03b1IIb\u03b23 integrin on platelet membrane, and neither ODQ nor SQ22536 significantly reversed the hinokitiol-mediated inhibition of platelet aggregation.", "entity1": "\u03b1IIb\u03b23 integrin", "entity2": "Hinokitiol", "span1": [81, 96], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9986": {"label": 3, "data": {"text": "Since this compound retains good AChE inhibitory activity and its hexahydrochromeno[4,3-b]pyrrole moiety is reminiscent of the hexahydropyrrolo[2,3-b]indole of physostigmine (3), we have designed and synthesized carbamates 4-6, and their biological evaluation has been assessed in vitro against human AChE and BChE.", "entity1": "AChE", "entity2": "hexahydrochromeno[4,3-b]pyrrole", "span1": [33, 37], "span2": [66, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7653": {"label": 2, "data": {"text": "These findings indicate that captopril attenuates the development of monocrotaline-induced right ventricular hypertrophy in association with inhibition of MMP-2 and MMP-9 in rats.", "entity1": "MMP-9", "entity2": "monocrotaline", "span1": [165, 170], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12496": {"label": 8, "data": {"text": "Recent literature shows that Brassica vegetables (Cruciferae) possess therapeutic effects particularly ascribed due to their content in glucosinolates, which upon myrosinase hydrolysis release the corresponding isothiocyanates.", "entity1": "myrosinase", "entity2": "glucosinolates", "span1": [163, 173], "span2": [136, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10184": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "OATP-B", "entity2": "rifamycin SV", "span1": [295, 301], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14363": {"label": 3, "data": {"text": "The quinolizidine alkaloids (natural products) such as oxymatrine, sophoridine, sophocarpine and matrine carry the common molecular structure of O=C=N-C-C-C-N that possessed positive ionotropic effect and hERG blocking activity.", "entity1": "hERG", "entity2": "quinolizidine alkaloids", "span1": [205, 209], "span2": [4, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"312": {"label": 5, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "5-HT3", "entity2": "tropisetron", "span1": [150, 155], "span2": [197, 208]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1297": {"label": 3, "data": {"text": "OBJECTIVE: Celecoxib and rofecoxib are two relatively new nonsteroidal anti-inflammatory drugs (NSAIDs) that selectively inhibit the cyclo-oxygenase-2 (COX-2) isoenzyme at therapeutic concentrations.", "entity1": "cyclo-oxygenase-2", "entity2": "rofecoxib", "span1": [133, 150], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7107": {"label": 3, "data": {"text": "The exception was bupropion, a dual norepinephrine transporter/dopamine transporter blocker, which tended to increase spontaneous locomotor activity.", "entity1": "dopamine transporter", "entity2": "bupropion", "span1": [63, 83], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12702": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "cysteine S-conjugates", "span1": [79, 90], "span2": [17, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5733": {"label": 3, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "p-ERK", "entity2": "U0126", "span1": [92, 97], "span2": [108, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15716": {"label": 4, "data": {"text": "d-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor.", "entity1": "N-methyl-d-aspartate receptor", "entity2": "d-serine", "span1": [108, 137], "span2": [79, 87]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3921": {"label": 3, "data": {"text": "Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group facilitates both enhancement of PDE4-inhibitory activity and restoration of potent PDE3 inhibition.", "entity1": "PDE4", "entity2": "6-aryl-4,5-dihydropyridazin-3(2H)-one", "span1": [115, 119], "span2": [14, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1806": {"label": 8, "data": {"text": "Moreover, a normal level of expression of PSS1 and/or PSS2 is not required for generating the pool of PtdSer externalized during apoptosis.", "entity1": "PSS1", "entity2": "PtdSer", "span1": [42, 46], "span2": [102, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9194": {"label": 9, "data": {"text": "W-7 did not induce a loss of cell surface beta 2-microglobulin, a membrane protein which is excluded from coated pits and which is not internalized, indicating that the effect of W-7 was specific for membrane receptors and not a result of bulk depletion of plasma membrane.", "entity1": "beta 2-microglobulin", "entity2": "W-7", "span1": [42, 62], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8939": {"label": 1, "data": {"text": "The negatively charged estramustine phosphate has been found previously to be a microtubule-associated protein (MAP)-dependent microtubule inhibitor [Wallin M, Deinum J and Friden B, FEBS Lett 179: 289-293, 1985].", "entity1": "microtubule-associated protein", "entity2": "estramustine phosphate", "span1": [80, 110], "span2": [23, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12346": {"label": 8, "data": {"text": "CYP3A5, which is particularly relevant to GC metabolism in the lungs, was also shown to efficiently metabolize triamcinolone acetonide, budesonide, and fluticasone propionate.", "entity1": "CYP3A5", "entity2": "triamcinolone acetonide", "span1": [0, 6], "span2": [111, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13122": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "TOP2A", "entity2": "doxorubicin", "span1": [64, 69], "span2": [82, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9946": {"label": 3, "data": {"text": "Sulfasalazine inhibited tumor necrosis factor alpha-induced activation of endogenous IKK in Jurkat T cells and SW620 colon cells, as well as the catalytic activity of purified IKK-alpha and IKK-beta in vitro.", "entity1": "IKK-alpha", "entity2": "Sulfasalazine", "span1": [176, 185], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"242": {"label": 1, "data": {"text": "At the 5-HT2C receptor, both R(-) and S(+)MDA were equipotent at stimulating PI hydrolysis, with the S(+) isomer of MDMA being more efficacious at the 5-HT2C receptor compared with the R(-) isomer.", "entity1": "5-HT2C", "entity2": "S(+) isomer of MDMA", "span1": [151, 157], "span2": [101, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7986": {"label": 2, "data": {"text": "These results demonstrated for the first time that ISO induces apoptosis in HepG2 cells through inactivating ERK1/2 kinase and activating JNK and p38 kinases, and ROS stimulated by ISO is able to activate the MAPK singaling pathway as the upstream signaling molecules.", "entity1": "kinases", "entity2": "ISO", "span1": [150, 157], "span2": [51, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4828": {"label": 1, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "GSK3", "entity2": "7\u03b2OHC", "span1": [202, 206], "span2": [67, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"365": {"label": 2, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2R alpha", "entity2": "DEX", "span1": [340, 351], "span2": [287, 290]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15636": {"label": 3, "data": {"text": "In conclusion, nobiletin attenuates HGF-induced HepG2 cells metastasis involving both ERK and PI3K/Akt pathways and are potentially useful as anti-metastatic agents for the treatment of hepatoma.", "entity1": "Akt", "entity2": "nobiletin", "span1": [99, 102], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8289": {"label": 3, "data": {"text": "Synthesis and biological evaluation of 1,3,4-thiadiazole analogues as novel AChE and BuChE inhibitors.", "entity1": "AChE", "entity2": "1,3,4-thiadiazole", "span1": [76, 80], "span2": [39, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11192": {"label": 1, "data": {"text": "Neostigmine enhances excitatory parasympathetic activity by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission and enhancing cholinergic action.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [107, 127], "span2": [75, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13378": {"label": 8, "data": {"text": "The expression of key genes important in methionine metabolism, such as methionine adenosyltransferase-1a, betaine-homocysteine methyltransferase and thioether S-methyltransferase, were suppressed.", "entity1": "betaine-homocysteine methyltransferase", "entity2": "methionine", "span1": [107, 145], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6642": {"label": 5, "data": {"text": "alpha(1A)-Adrenoceptor selective antagonists, 2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane (WB-4101; 0.1-1 mg/kg) and 5-methylurapidil (0.1-1 mg/kg), the alpha(1B)-adrenoceptor selective antagonist, 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765314; 0.3-1 mg/kg), as well as the alpha(1D)-adrenoceptor selective antagonist, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY-7378; 1 mg/kg), were used to delineate the adrenoceptor subtypes involved.", "entity1": "alpha(1D)-adrenoceptor", "entity2": "BMY-7378", "span1": [371, 393], "span2": [496, 504]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5101": {"label": 2, "data": {"text": "Thus, we found that 5HHMF enhances heme oxygenase-1 (HO-1) expression via nuclear factor-erythroid 2-related factor 2 (Nrf2) activation.", "entity1": "nuclear factor-erythroid 2-related factor 2", "entity2": "5HHMF", "span1": [74, 117], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2430": {"label": 1, "data": {"text": "SSTR2 and SSTR5 are usually expressed in GH-secreting pituitary tumors, and both octreotide and lanreotide bind preferentially to SSTR2 and, to a lesser extent, to SSTR5.", "entity1": "SSTR2", "entity2": "octreotide", "span1": [130, 135], "span2": [81, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7238": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "AMPH", "span1": [192, 229], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"835": {"label": 3, "data": {"text": "PR mRNA abundance in both myometruim and leiomyomata (center and marginal area) was significantly decreased in 4 patients continuing mifepristone treatment before the operation but not in the other 2 patients stopping RU486 1 month before operation.", "entity1": "PR mRNA", "entity2": "mifepristone", "span1": [0, 7], "span2": [133, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2990": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "F820A", "entity2": "sildenafil", "span1": [265, 270], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6019": {"label": 1, "data": {"text": "Aspirin irreversibly inhibits PGHS-1, preventing this isozyme from forming PGH2 or any other oxygenated product; in contrast, aspirin treatment of PGHS-2 causes this enzyme to form 15-hydroxy-5c,8c,11c,13t-eicosatetraenoic acid (15-HETE) instead of PGH2.", "entity1": "PGHS-2", "entity2": "aspirin", "span1": [147, 153], "span2": [126, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5273": {"label": 2, "data": {"text": "In fact, we demonstrated a significant stimulation of Nox4 activity by 4 quinone derivatives (AA-861, tBuBHQ, tBuBQ, and duroquinone) observed in 3 different cellular models, HEK293E, T-REx\u2122, and chondrocyte cell lines.", "entity1": "Nox4", "entity2": "duroquinone", "span1": [54, 58], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5536": {"label": 1, "data": {"text": "Labeling with [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and [125I]IAS migrated at the same position on an SDS-PAGE gel as the beta 2AR labeled by the antagonist photoaffinity label [125I]iodoazidobenzylpindolol ([125I]IABP).", "entity1": "beta 2AR", "entity2": "[125I]IAS", "span1": [178, 186], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9483": {"label": 3, "data": {"text": "At -20 mV, 10 nM cisapride reduced HERG tail-current amplitude by 5%, whereas, at + 20 mV, the tail-current amplitude was reduced by 45% (n = 4 cells).", "entity1": "HERG", "entity2": "cisapride", "span1": [35, 39], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"786": {"label": 9, "data": {"text": "Specifically, aniracetam, which potentiates wild-type AMPA receptors, is ineffective on the non-desensitizing GluR3(L507Y) mutant, but has synergistic effects with lithium on wild-type receptors.", "entity1": "GluR3", "entity2": "aniracetam", "span1": [110, 115], "span2": [14, 24]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7014": {"label": 3, "data": {"text": "Sorafenib has the added advantage of inhibiting multiple different Raf isoforms, which enables it to target TGF-alpha/EGFR signaling and may also enhance its inhibition of VEGFR and PDGFR-beta.", "entity1": "EGFR", "entity2": "Sorafenib", "span1": [118, 122], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14036": {"label": 2, "data": {"text": "Mercury induces the expression of cyclooxygenase-2 and inducible nitric oxide synthase.", "entity1": "cyclooxygenase-2", "entity2": "Mercury", "span1": [34, 50], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2424": {"label": 8, "data": {"text": "Mitochondrial arginase II modulates nitric-oxide synthesis through nonfreely exchangeable L-arginine pools in human endothelial cells.", "entity1": "Mitochondrial arginase II", "entity2": "nitric-oxide", "span1": [0, 25], "span2": [36, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11587": {"label": 1, "data": {"text": "Overexpression of PPARdelta by adenoviral transfer rescued 14-3-3epsilon proteins from elimination by sulindac or indomethacin.", "entity1": "14-3-3epsilon", "entity2": "indomethacin", "span1": [59, 72], "span2": [114, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9572": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "IL-3", "entity2": "fenoterol", "span1": [54, 58], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6201": {"label": 5, "data": {"text": "administration of the non-selective muscarinic receptor antagonist atropine (ID50 = 1.45 microg), the muscarinic M1 receptor antagonist pirenzepine (ID50 = 4.33 microg), the muscarinic M2 receptor antagonist methoctramine (ID50 = 1.39 microg) and the muscarinic M3 receptor antagonist para-fluoro-hexahydro-sila-difenidol (ID50 = 31.19 microg).", "entity1": "muscarinic M3 receptor", "entity2": "para-fluoro-hexahydro-sila-difenidol", "span1": [251, 273], "span2": [285, 321]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7498": {"label": 1, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Activation of alpha1-AMPK is associated with inhibition of apical amiloride-sensitive Na(+) channels (ENaC), which has important implications for the clinical use of metformin.", "entity1": "amiloride-sensitive Na(+) channels", "entity2": "metformin", "span1": [96, 130], "span2": [196, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13548": {"label": 2, "data": {"text": "Furthermore, the activities of the two torafugu PPARalphas were enhanced 4.3- and 7.6-fold by arachidonic acid, 4.4- and 5.2-fold by docosahexaenoic acid, and 6.7- and 8.0-fold by eicosapentaenoic acid each at 50 microM, respectively.", "entity1": "torafugu PPARalphas", "entity2": "eicosapentaenoic acid", "span1": [39, 58], "span2": [180, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13066": {"label": 2, "data": {"text": "Accumulated evidence in humans and animals shows that both aspirin and H. pylori upregulate the expression of cyclooxygenase (COX)-2 both at mRNA and protein levels at the ulcer margin, but failed to influence significantly that of COX-1.", "entity1": "cyclooxygenase (COX)-2", "entity2": "aspirin", "span1": [110, 132], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7920": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "cisplatin", "span1": [27, 32], "span2": [129, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"668": {"label": 3, "data": {"text": "OBJECTIVE: To evaluate the extent of human cyclooxygenase-1 (COX-1) inhibition by meloxicam, which has been reported to preferentially inhibit cyclooxygenase-2 (COX-2).", "entity1": "COX-2", "entity2": "meloxicam", "span1": [161, 166], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10732": {"label": 5, "data": {"text": "We have analyzed binding domains of the oxytocin receptor for barusiban, a highly selective oxytocin receptor antagonist, in comparison to the combined vasopressin V1A/oxytocin receptor antagonist atosiban and the agonists oxytocin and carbetocin.", "entity1": "vasopressin V1A/oxytocin receptor", "entity2": "atosiban", "span1": [152, 185], "span2": [197, 205]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5202": {"label": 3, "data": {"text": "Inhibition of mTOR by low dose rapamycin decreases HG-induced Nox4 and Nox1, NADPH oxidase activity and podocyte apoptosis.", "entity1": "NADPH oxidase", "entity2": "rapamycin", "span1": [77, 90], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7470": {"label": 2, "data": {"text": "Na+/Cl- dipole couples agonist binding to kainate receptor activation.", "entity1": "kainate receptor", "entity2": "Na+", "span1": [42, 58], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13128": {"label": 2, "data": {"text": "RESULT(S): The expression of endometrial ERalpha, PRAB, PRB, and SRC-1 was increased significantly after 1 week of mifepristone, but the increase was no longer seen after 10 weeks.", "entity1": "ERalpha", "entity2": "mifepristone", "span1": [41, 48], "span2": [115, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5124": {"label": 3, "data": {"text": "In this study, we found that 5-hydroxy-3,6,7,8,3'4'-hexamethoxyflavone (5HHMF) from Hizikia fusiforme considerably inhibits lipopolysaccharide (LPS)-stimulated NO production by suppressing the expression of inducible NO synthase (iNOS) in BV2 microglia.", "entity1": "inducible NO synthase", "entity2": "5-hydroxy-3,6,7,8,3'4'-hexamethoxyflavone", "span1": [207, 228], "span2": [29, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14222": {"label": 4, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b2", "entity2": "DPN", "span1": [218, 221], "span2": [230, 233]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11036": {"label": 2, "data": {"text": "The ability of bexarotene to inhibit angiogenesis and metastasis was dependent on activation of its heterodimerisation partner peroxisome proliferator-activated receptor gamma.", "entity1": "peroxisome proliferator-activated receptor gamma", "entity2": "bexarotene", "span1": [127, 175], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14148": {"label": 2, "data": {"text": "When combined, mianserin antagonized the effects of the full kappa-opioid receptor agonists in [(35)S]GTPgammaS assays and reduced the stimulation of p38 MAPK and ERK1/2 phosphorylation by dynorphin A.", "entity1": "MAPK", "entity2": "dynorphin A", "span1": [154, 158], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2583": {"label": 8, "data": {"text": "CONCLUSIONS: These findings indicate that increased synthesis of histamine through up-regulation of HDC gene expression and HDC activity in nasal mucosa plays an important role in the development of nasal hypersensitivity.", "entity1": "HDC", "entity2": "histamine", "span1": [124, 127], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9487": {"label": 1, "data": {"text": "Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine.", "entity1": "Monoamine transporter", "entity2": "cocaine", "span1": [0, 21], "span2": [85, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15099": {"label": 3, "data": {"text": "The addition of avibactam greatly (4-1024-fold minimum inhibitory concentration [MIC] reduction) improves the activity of ceftazidime versus most species of Enterobacteriaceae depending on the presence or absence of \u03b2-lactamase enzyme(s).", "entity1": "\u03b2-lactamase", "entity2": "ceftazidime", "span1": [216, 227], "span2": [122, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7448": {"label": 9, "data": {"text": "Further, treatment of female mice depleted of GSH with L-BOAA did not induce inhibition of complex I indicating that GSH levels were not critical for maintaining complex I activity in female mice unlike their male counterpart.", "entity1": "complex I", "entity2": "GSH", "span1": [162, 171], "span2": [117, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11457": {"label": 3, "data": {"text": "At the enzymatic activity level, doxycycline started to suppress MMP-9 activity at 5 mg/kg/day (P<0.001), while minocycline had an effect at a lower dose, 1 mg/kg/day (P<0.02).", "entity1": "MMP-9", "entity2": "doxycycline", "span1": [65, 70], "span2": [33, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12008": {"label": 2, "data": {"text": "The results showed that administration of AlCl3 resulted in a significant elevation in the levels of AchE activity, CRP, NF-\u03baB, and MCP-1 accompanied with a significant depletion in the Ach level.", "entity1": "MCP-1", "entity2": "AlCl3", "span1": [132, 137], "span2": [42, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4280": {"label": 3, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "AEG-1", "entity2": "ursolic acid", "span1": [118, 123], "span2": [135, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13867": {"label": 0, "data": {"text": "Cyan fluorescent protein was fused to the C terminus of the M(2) muscarinic receptor, and a specific binding sequence for the small fluorescent compound fluorescein arsenical hairpin binder, FlAsH, was inserted into the third intracellular loop; the latter site was labeled in intact cells by incubation with FlAsH.", "entity1": "M(2) muscarinic receptor", "entity2": "C", "span1": [60, 84], "span2": [42, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8226": {"label": 1, "data": {"text": "Mutations introduced into EAG to replicate the ICA binding site in ERG did not alter the functional response to ICA.", "entity1": "ERG", "entity2": "ICA", "span1": [67, 70], "span2": [112, 115]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4324": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "cyclin A", "entity2": "Pinosylvin", "span1": [167, 175], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"351": {"label": 1, "data": {"text": "Affinities for the major nonadrenergic [125I]PIC binding site were highly comparable to human subtype-I1 imidazol(in)e receptor sites in the brain stem (rank order: moxonidine > clonidine > cirazoline > IDX > amiloride).", "entity1": "human subtype-I1 imidazol(in)e receptor", "entity2": "IDX", "span1": [88, 127], "span2": [203, 206]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7586": {"label": 1, "data": {"text": "Specifically, B2-O-CH(2)-CH(2)-N-piperidine and B2-O-CH(2)-CH(2)-N-pyrrolidine revealed a higher affinity towards hERG channels than amiodarone.", "entity1": "hERG", "entity2": "B2-O-CH(2)-CH(2)-N-piperidine", "span1": [114, 118], "span2": [14, 43]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7149": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "GAF-B domain", "entity2": "vardenafil", "span1": [47, 59], "span2": [78, 88]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6567": {"label": 3, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "Y751A", "entity2": "milrinone", "span1": [8, 13], "span2": [60, 69]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8639": {"label": 1, "data": {"text": "Ethanol and melatonin exert opposite effects on E2 and P4, and they differentially regulate the expression of sex steroid receptors in female reproductive tissues.", "entity1": "sex steroid receptors", "entity2": "melatonin", "span1": [110, 131], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2748": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "SRC", "entity2": "BMS-354825", "span1": [87, 90], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1714": {"label": 0, "data": {"text": "Terbinafine resistance was transmitted with the mutated alleles in gene replacement experiments, proving that single amino acid substitutions in the Erg1 protein were sufficient to confer the resistance phenotype.", "entity1": "Erg1", "entity2": "amino acid", "span1": [149, 153], "span2": [117, 127]}, "weak_labels": [0, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11190": {"label": 2, "data": {"text": "In the liver of rats given flutamide as initiating agent at the dose of 500 mg/kg/week for 6 successive weeks, gamma-glutamyltraspeptidase-positive foci were detected only in 3 of 10 rats.", "entity1": "gamma-glutamyltraspeptidase", "entity2": "flutamide", "span1": [111, 138], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15904": {"label": 1, "data": {"text": "Synaptotagmin 1 is required for vesicular Ca(2+) /H(+) -antiport activity.", "entity1": "Synaptotagmin 1", "entity2": "Ca(2+)", "span1": [0, 15], "span2": [42, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8002": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "FXa", "entity2": "IMG", "span1": [195, 198], "span2": [140, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13083": {"label": 1, "data": {"text": "This dual mode of action of sulfonylureas and glinides may open new perspectives for the molecular pharmacology of antidiabetic drugs, because it provides evidence that drugs can be designed that target both the sulfonylurea receptor and PPARgamma.", "entity1": "sulfonylurea receptor", "entity2": "glinides", "span1": [212, 233], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5784": {"label": 3, "data": {"text": "Inhibition of binding of both plasminogen and plasmin to gp330 by benzamidine was similar, although EACA inhibited the binding of plasmin to gp330 slightly more than the binding of plasminogen to gp330.", "entity1": "plasminogen", "entity2": "EACA", "span1": [181, 192], "span2": [100, 104]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5003": {"label": 1, "data": {"text": "Chalcogenopyrylium Dyes as Differential Modulators of Organic Anion Transport by MRP1, MRP2 and MRP4.", "entity1": "MRP2", "entity2": "Chalcogenopyrylium", "span1": [87, 91], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7492": {"label": 3, "data": {"text": "Phenserine, a derivative of physostigmine, was first described as an inhibitor of acetylcholinesterase (AChE) and was shown to improve cognition in various experimental paradigms in rodents and dogs.", "entity1": "AChE", "entity2": "physostigmine", "span1": [104, 108], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14121": {"label": 3, "data": {"text": "These polyphenols, but not GvEx, showed a certain level of inhibition of human-cDNA-expressed CYPs.", "entity1": "CYPs", "entity2": "polyphenols", "span1": [94, 98], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2068": {"label": 3, "data": {"text": "In this study, using a model of gentamicin C (GMC)-induced reduction in SGLT1 activity, we examined whether ligands for megalin protect LLC-PK1 cells from the GMC-induced reduction in SGLT1 activity.", "entity1": "SGLT1", "entity2": "GMC", "span1": [72, 77], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"764": {"label": 0, "data": {"text": "The inhibitor binds at the base of the active site gorge of TcAChE, interacting with both the choline-binding site (Trp-84) and the acyl-binding pocket (Phe-288, Phe-290).", "entity1": "choline-binding site", "entity2": "Trp", "span1": [94, 114], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12621": {"label": 1, "data": {"text": "In addition, three IP ligands, iloprost, carbacyclin and isocarbacyclin, and one TP ligand, STA2, bound to this receptor with Ki values comparable to the Ki values of these compounds for the IP and TP receptors, respectively.", "entity1": "IP", "entity2": "carbacyclin", "span1": [19, 21], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10201": {"label": 3, "data": {"text": "In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2.", "entity1": "Oatp2", "entity2": "rifampicin", "span1": [166, 171], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4856": {"label": 5, "data": {"text": "[6]-gingerol: a novel AT\u2081 antagonist for the treatment of cardiovascular disease.", "entity1": "AT\u2081", "entity2": "[6]-gingerol", "span1": [22, 25], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3643": {"label": 1, "data": {"text": "In the resveratrol+As(2)O(3) group, activities of superoxide dismutase, catalase in serum and GSH/GSSG were significantly increased, histopathological effects were reduced, and arsenic accumulation markedly decreased in the liver, compared with the As(2)O(3)-treated group.", "entity1": "catalase", "entity2": "As(2)O(3)", "span1": [72, 80], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9174": {"label": 1, "data": {"text": "Phenoxybenzamine, an alpha-adrenergic antagonist containing a (chloroethyl)amine group, labels calmodulin in the presence of calcium.", "entity1": "calmodulin", "entity2": "(chloroethyl)amine", "span1": [95, 105], "span2": [62, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14623": {"label": 8, "data": {"text": "All three CDA proteins showed similar K(m) and V(max) for Ara-C and dFdC deamination, except for CDA70Thr, which had a 2.5-fold lower K(m) and 6-fold lower V(max) for Ara-C deamination.", "entity1": "CDA", "entity2": "Ara-C", "span1": [10, 13], "span2": [58, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5861": {"label": 1, "data": {"text": "When delta-receptor binding was determined by using [3H]DPDPE, a 40-50% decrease in binding in the midbrain and cortex, and 25-35% decrease in binding in the striatum were observed after 3 or 4 days of DPDPE treatment.", "entity1": "delta-receptor", "entity2": "[3H]DPDPE", "span1": [5, 19], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8875": {"label": 1, "data": {"text": "The observations suggest that in 5L cells the Igfbp-4 gene may have got under the control of a promoter containing dioxin responsive element(s) leading to the induction of IGFBP-4 by TCDD.", "entity1": "Igfbp-4", "entity2": "TCDD", "span1": [46, 53], "span2": [183, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1357": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "DAT", "entity2": "alkyl", "span1": [317, 320], "span2": [199, 204]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4664": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "p22(phox)", "entity2": "resveratrol", "span1": [145, 154], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11084": {"label": 3, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "Ca2+ channel", "entity2": "felodipine", "span1": [181, 193], "span2": [202, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11755": {"label": 1, "data": {"text": "Around five times as potent as the lead with an IC(50) of 33 \u03bcM for disruption of the Myc-Max heterodimer, JY-3-094 demonstrated excellent selectivity over Max-Max homodimers, with no apparent effect at 100 \u03bcM.", "entity1": "Max", "entity2": "JY-3-094", "span1": [156, 159], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12118": {"label": 1, "data": {"text": "CONCLUSIONS: Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation.", "entity1": "TPA", "entity2": "Argatroban", "span1": [87, 90], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"327": {"label": 1, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "bovine pancreatic ribonuclease A", "entity2": "disulfide", "span1": [63, 95], "span2": [46, 55]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8977": {"label": 9, "data": {"text": "Pretreatment with ceruletide (40 micrograms/100 g b. wt., IP) 3 days or 7 days prior to the injection of SMS 201-995 significantly inhibited the response rate of barrel rotation induced by SMS 201-995, but not that induced by arginine-vasopressin (1 microgram/rat, ICV).", "entity1": "arginine-vasopressin", "entity2": "ceruletide", "span1": [226, 246], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14237": {"label": 2, "data": {"text": "Furthermore, salubrinal, a specific eIF2\u03b1 phosphorylation-inducing agent, increased CHOP and DR5 expression in the presence of VA.", "entity1": "eIF2\u03b1", "entity2": "salubrinal", "span1": [36, 41], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7661": {"label": 3, "data": {"text": "These findings indicate that captopril attenuates the development of monocrotaline-induced right ventricular hypertrophy in association with inhibition of MMP-2 and MMP-9 in rats.", "entity1": "MMP-9", "entity2": "captopril", "span1": [165, 170], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12534": {"label": 1, "data": {"text": "Adenosine analogs in particular the N6-substituted compounds are more potent at A1 receptors than at A2 receptors.", "entity1": "A2 receptors", "entity2": "Adenosine", "span1": [101, 113], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2606": {"label": 3, "data": {"text": "OBJECTIVES: The alkaloid galantamine (GAL), which exhibits a combined anticholinesterase and direct parasympathomimetic mechanism of action, is employed in conjunction with therapeutic interventions in the stimulation of central cholinergic transfer in cognitive diseases.", "entity1": "anticholinesterase", "entity2": "GAL", "span1": [70, 88], "span2": [38, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12730": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "Acetylcholinesterase", "entity2": "ACh", "span1": [0, 20], "span2": [165, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9639": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "PSA", "entity2": "bicalutamide", "span1": [46, 49], "span2": [102, 114]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4776": {"label": 1, "data": {"text": "AOH treatment also induced abnormal Aurora B bridges, suggesting that cytokinesis was interfered within cells undergoing karyokinesis.", "entity1": "Aurora B", "entity2": "AOH", "span1": [36, 44], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"724": {"label": 2, "data": {"text": "Ribonucleotide reductase activity was found to be strongly increased in the gemcitabine-selected line and purine nucleoside phosphorylase was increased in the 2-chlorodeoxyadenosine-selected line.", "entity1": "Ribonucleotide reductase", "entity2": "gemcitabine", "span1": [0, 24], "span2": [76, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3959": {"label": 1, "data": {"text": "Here, we identified Bcl-2 antagonist killer 1 (Bak) as a molecular target of VK2-induced apoptosis.", "entity1": "Bak", "entity2": "VK2", "span1": [47, 50], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4709": {"label": 9, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Dickkopfs", "entity2": "TCDD", "span1": [578, 587], "span2": [655, 659]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15469": {"label": 0, "data": {"text": "An endogenous intracellular domain fragment of p75(NTR) (p75(ICD)) containing these 29 amino acids is produced by regulated proteolysis of the full-length receptor.", "entity1": "p75(NTR)", "entity2": "amino acids", "span1": [47, 55], "span2": [87, 98]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8134": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "PI3K", "entity2": "Sal", "span1": [149, 153], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9253": {"label": 1, "data": {"text": "Ergovaline inhibition of the binding of the D2-specific radioligand, [3H]YM-09151-2, exhibited a KI (inhibition constant) of 6.9 +/- 2.6 nM, whereas dopamine was much less potent (370 +/- 160 nM).", "entity1": "D2", "entity2": "[3H]YM-09151-2", "span1": [44, 46], "span2": [69, 83]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9708": {"label": 3, "data": {"text": "The irreversible MAO-B inhibitors, pargyline (30 mg/kg) and l-deprenyl (3-10 mg/kg) also decreased responding maintained by ethanol reinforcement; these results are consistent with previous findings that both drugs decreased ethanol intake in mice.", "entity1": "MAO-B", "entity2": "l-deprenyl", "span1": [17, 22], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8702": {"label": 3, "data": {"text": "Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: Structure-activity relationships (SAR) of the C3-phenyl moiety.", "entity1": "HIV capsid", "entity2": "1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione", "span1": [72, 82], "span2": [18, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"917": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "propranolol", "span1": [22, 39], "span2": [87, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14666": {"label": 1, "data": {"text": "Inhibition of PKA significantly attenuated the effect of genistein on thrombin-induced EC permeability, MLC phosphorylation, and RhoA membrane translocation in ECs.", "entity1": "thrombin", "entity2": "genistein", "span1": [70, 78], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1749": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "Erk1/2", "entity2": "GW572016", "span1": [121, 127], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2456": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "ABCC2", "entity2": "cisplatin", "span1": [62, 67], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2295": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP2 receptors", "entity2": "AH 6809", "span1": [27, 40], "span2": [249, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6643": {"label": 3, "data": {"text": "To further investigate this positive correlation and its possible therapeutic implications, a selective COX-2 inhibitor, etodolac, was tested on three variants of HT-29 colon cancer cell lines, HT-29/Inv1, HT-29/Inv2 and HT-29/Inv3, with graded increases of in vitro Matrigel invasive potential and COX-2 expression levels.", "entity1": "COX-2", "entity2": "etodolac", "span1": [104, 109], "span2": [121, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5770": {"label": 3, "data": {"text": "NSDA neurons displayed significant axon terminal degeneration (as indexed by decreases in DA, tyrosine hydroxylase (TH) and DA transporter concentrations in the striatum) as well as loss of TH-immunoreactive (IR) neurons in the substantia nigra (SN) following MPTP, whereas TIDA neurons revealed no overt axon terminal pathology or loss of TH-IR cell bodies.", "entity1": "TH", "entity2": "MPTP", "span1": [190, 192], "span2": [260, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14360": {"label": 5, "data": {"text": "Our results showed that bone remodeling was significantly decreased in CCL3(-/-) and CCR1(-/-) mice and in animals treated with Met-RANTES (an antagonist of CCR5 and CCR1).", "entity1": "CCR1", "entity2": "Met", "span1": [166, 170], "span2": [128, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13684": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "porcine TLR7", "entity2": "gardiquimod", "span1": [83, 95], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7845": {"label": 2, "data": {"text": "These data suggest that ribavirin-induced intracellular GTP depletion recruits a super elongation complex containing P-TEFb, AFF4 and ELL3, to F7, and modulates FVII mRNA transcription elongation.", "entity1": "AFF4", "entity2": "ribavirin", "span1": [125, 129], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8129": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "pGSK-3\u03b2", "entity2": "Sal", "span1": [84, 91], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10778": {"label": 3, "data": {"text": "Imatinib mesylate is a tyrosine kinase inhibitor of the ABL, platelet-derived growth factor receptor (PDGFR), and c-kit kinases.", "entity1": "tyrosine kinase", "entity2": "Imatinib mesylate", "span1": [23, 38], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14209": {"label": 3, "data": {"text": "Galantamine is a reversible, competitive acetylcholinesterase (AChE) inhibitor and allosteric potentiating ligand of nicotinic acetylcholine receptors (nAChR-APL) that shares many common structural elements with morphinan-based opioids.", "entity1": "acetylcholinesterase", "entity2": "Galantamine", "span1": [41, 61], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"1208": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "VMAT-2", "entity2": "amphetamines", "span1": [209, 215], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2451": {"label": 3, "data": {"text": "Colonic cyclooxygenase-2 and interkeukin-1beta mRNA and spinal c-FOS mRNA expression were significantly down-regulated by ATB-429, but not by mesalamine.", "entity1": "c-FOS", "entity2": "ATB-429", "span1": [63, 68], "span2": [122, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15543": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "tumor necrosis factor-\u03b1", "entity2": "DMN", "span1": [227, 250], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1189": {"label": 4, "data": {"text": "In conclusion, fenoterol-induced constitutive beta(2)-adrenoceptor activity reduces muscarinic receptor agonist- and histamine-induced contractions of bovine tracheal smooth muscle, which can be reversed by the inverse agonist timolol.", "entity1": "beta(2)-adrenoceptor", "entity2": "timolol", "span1": [46, 66], "span2": [227, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5483": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "norethisterone", "span1": [68, 85], "span2": [160, 174]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9694": {"label": 1, "data": {"text": "Comparison of the novel antipsychotic ziprasidone with clozapine and olanzapine: inhibition of dorsal raphe cell firing and the role of 5-HT1A receptor activation.", "entity1": "5-HT1A receptor", "entity2": "ziprasidone", "span1": [136, 151], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14257": {"label": 8, "data": {"text": "However, SSAT1-deficient mice metabolize TETA at the same rate as the wild-type mice, indicating the existence of another N-acetylase respons 2ible for its metabolism in mice.", "entity1": "N-acetylase", "entity2": "TETA", "span1": [122, 133], "span2": [41, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"742": {"label": 3, "data": {"text": "The kinase activity of EGFR was little inhibited by TT-B in a cell-free system.", "entity1": "kinase", "entity2": "TT-B", "span1": [4, 10], "span2": [52, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"679": {"label": 7, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "TPH", "entity2": "BH4", "span1": [184, 187], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"5793": {"label": 0, "data": {"text": "The amino acid sequence deduced from the nucleotide sequence of the cDNA from porcine liver was identical to that deduced for porcine kidney ACY-1.", "entity1": "porcine kidney ACY-1", "entity2": "nucleotide", "span1": [126, 146], "span2": [41, 51]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3942": {"label": 3, "data": {"text": "Reactivators showed different activity in the reactivation of rat brain AChE after dichlorvos, paraoxon and tabun inhibition.", "entity1": "rat brain AChE", "entity2": "tabun", "span1": [62, 76], "span2": [108, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14827": {"label": 3, "data": {"text": "rivaroxaban and apixaban, are potent, oral direct inhibitors of prothrombinase-bound, clot-associated or free FXa.", "entity1": "FXa", "entity2": "rivaroxaban", "span1": [110, 113], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"61": {"label": 3, "data": {"text": "Enalkiren has been shown to produce dose-related suppression of plasma renin activity (PRA) and angiotensin II when administered intravenously.", "entity1": "angiotensin II", "entity2": "Enalkiren", "span1": [96, 110], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"173": {"label": 5, "data": {"text": "Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists.", "entity1": "cholecystokinin", "entity2": "lorglumide", "span1": [71, 86], "span2": [30, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"596": {"label": 9, "data": {"text": "15d-PGJ2 did not block nuclear translocation or DNA-binding activity of the transcription factor NFkappaB, but it did inhibit the activity of an NFkappaB reporter construct, suggesting that the mechanism of suppression of microglial iNOS by 15d-PGJ2 may involve interference with NFkappaB transcriptional activity in the nucleus.", "entity1": "NFkappaB", "entity2": "15d-PGJ2", "span1": [97, 105], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6552": {"label": 1, "data": {"text": "Identification of interaction sites of cyclic nucleotide phosphodiesterase type 3A with milrinone and cilostazol using molecular modeling and site-directed mutagenesis.", "entity1": "phosphodiesterase type 3A", "entity2": "milrinone", "span1": [57, 82], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3401": {"label": 2, "data": {"text": "We found that PSE inhibits interleukin-2 (IL-2) and tumor necrosis factor (TNF) alpha-gene transcription in stimulated Jurkat cells, a human T-cell leukemia cell line.", "entity1": "tumor necrosis factor (TNF) alpha", "entity2": "PSE", "span1": [52, 85], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11737": {"label": 1, "data": {"text": "These results show that the robust effects of TCDD on the mRNA expression of Snrpn, Peg3 and Igf2r genes in the sperm and of Igf2r in the muscle and liver are unrelated to changes in methylation in their respective genes.", "entity1": "Igf2r", "entity2": "TCDD", "span1": [93, 98], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14938": {"label": 3, "data": {"text": "A novel potent compound, N-benzyl-5-(4-isopropylthiophenol)-2-hydroxyl nicotinamide (12c), which binds Mcl-1 with an IC(50) value of 54 nM was obtained.", "entity1": "Mcl-1", "entity2": "N-benzyl-5-(4-isopropylthiophenol)-2-hydroxyl nicotinamide", "span1": [103, 108], "span2": [25, 83]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14805": {"label": 1, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1) receptor", "entity2": "AM4113", "span1": [155, 169], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5715": {"label": 3, "data": {"text": "Parallel synthetic strategies were used to generate libraries of indomethacin analogues, which exhibit reduced cyclooxygenase inhibitory activity but retain AKR1C3 inhibitory potency and selectivity.", "entity1": "cyclooxygenase", "entity2": "indomethacin", "span1": [111, 125], "span2": [65, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8409": {"label": 3, "data": {"text": "Secondary point mutations in the Fms-like tyrosine kinase 3 (FLT3) tyrosine kinase domain (KD) are common causes of acquired clinical resistance to the FLT3 inhibitors AC220 (quizartinib) and sorafenib.", "entity1": "FLT3", "entity2": "quizartinib", "span1": [152, 156], "span2": [175, 186]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7515": {"label": 2, "data": {"text": "KEY RESULTS: Phenformin, AICAR and metformin increased AMPK (alpha1) activity and decreased I(amiloride).", "entity1": "AMPK (alpha1)", "entity2": "Phenformin", "span1": [55, 68], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13443": {"label": 1, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "COX-2", "entity2": "T0070907", "span1": [74, 79], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15809": {"label": 3, "data": {"text": "Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.", "entity1": "CHK1", "entity2": "imidazo[1,2-a]pyrazine", "span1": [23, 27], "span2": [50, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9207": {"label": 1, "data": {"text": "Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides.", "entity1": "epidermal growth factor", "entity2": "phenothiazines", "span1": [34, 57], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"109": {"label": 5, "data": {"text": "Terfenadine and astemizole are chemically unrelated to histamine H1-receptor antagonists such as diphenhydramine and chlorpheniramine.", "entity1": "histamine H1-receptor", "entity2": "diphenhydramine", "span1": [55, 76], "span2": [97, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"588": {"label": 3, "data": {"text": "These results suggest that the megabase DNA fragmentation is induced as a consequence of inhibition of thymidylate synthase by Tomudex and kilobase DNA fragmentation may correlate with the reduction of p27(kip1) expression and the increase in cyclin E and cdk2 kinase activities.", "entity1": "thymidylate synthase", "entity2": "Tomudex", "span1": [103, 123], "span2": [127, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"643": {"label": 2, "data": {"text": "Sumatriptan and LY 344864 decreased the number of capsaicin-induced c-fos-like immunoreactive cells within trigeminal nucleus caudalis (ID50 = 0.04 and 0.6 mg kg(-1)).", "entity1": "c-fos", "entity2": "capsaicin", "span1": [68, 73], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7636": {"label": 3, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "Panx1", "entity2": "UTP", "span1": [78, 83], "span2": [40, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8277": {"label": 8, "data": {"text": "This investigation tested the hypothesis that CYP2B6 is a prominent CYP isoform responsible for clinical methadone N-demethylation and clearance, using the in vivo mechanism-based CYP2B6 inhibitor ticlopidine, given orally for 4 days.", "entity1": "CYP", "entity2": "methadone", "span1": [68, 71], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12651": {"label": 1, "data": {"text": "This study shows that aspirin and sodium salicylate, its major blood metabolite, reverse contractile actions of endothelin-1 (ET-1) in isolated rat aorta and human mammary arteries.", "entity1": "endothelin-1", "entity2": "aspirin", "span1": [112, 124], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13046": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "retinaldehyde dehydrogenase type 2", "entity2": "retinol", "span1": [177, 211], "span2": [99, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2265": {"label": 1, "data": {"text": "The present results suggest the involvement of astrocytes in the regulation of the glutamatergic activation associated with withdrawal from free-choice ethanol consumption and point to differential adaptations of GS and GFAP to prolonged alcohol drinking in the PLC of P rats.", "entity1": "GS", "entity2": "ethanol", "span1": [213, 215], "span2": [152, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12754": {"label": 2, "data": {"text": "Ang II level in plasma and mesenteric arteries in SHR group was the same or lower than that in WKY group, and was higher in irbesartan group and lower in imidapril group.", "entity1": "Ang II", "entity2": "irbesartan", "span1": [0, 6], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1670": {"label": 1, "data": {"text": "CONCLUSIONS: These results indicate that etomidate acts as an agonist at alpha2-adrenoceptors, which appears in vivo primarily as an alpha2B-receptor-mediated increase in blood pressure.", "entity1": "alpha2B-receptor", "entity2": "etomidate", "span1": [133, 149], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15249": {"label": 8, "data": {"text": "Furthermore, silymarin, silybin A, and silybin B (100 \u00b5M) significantly inhibited OATP-mediated estradiol-17\u03b2-glucuronide and rosuvastatin uptake into human hepatocytes.", "entity1": "OATP", "entity2": "rosuvastatin", "span1": [82, 86], "span2": [126, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1446": {"label": 3, "data": {"text": "The selective norepinephrine (NE) transporter inhibitor atomoxetine (formerly called tomoxetine or LY139603) has been shown to alleviate symptoms in Attention Deficit/Hyperactivity Disorder (ADHD).", "entity1": "norepinephrine (NE) transporter", "entity2": "atomoxetine", "span1": [14, 45], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6117": {"label": 3, "data": {"text": "In addition, another drug that is both a substrate of uptake1 and a MAO inhibitor, debrisoquine, was investigated in the study.", "entity1": "MAO", "entity2": "debrisoquine", "span1": [68, 71], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"3302": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mammalian target of rapamycin", "entity2": "Afinitor((R)) Novartis", "span1": [81, 110], "span2": [20, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"26": {"label": 2, "data": {"text": "On study day 10, the acute effects of candoxatril were similar to those on day 1 (i.e., ANP was further increased, aldosterone was suppressed, and right and left ventricular filling pressures were decreased).", "entity1": "ANP", "entity2": "candoxatril", "span1": [88, 91], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2331": {"label": 2, "data": {"text": "Theophylline exposure resulted in a sustained increase in mRNA expression for CysS and PDE3A, but PDE4D gene expression was unchanged.", "entity1": "PDE3A", "entity2": "Theophylline", "span1": [87, 92], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7869": {"label": 5, "data": {"text": "Neuroprotection was attenuated by pertussis toxin, and inhibited by the selective type-1 S1PR (S1P1R) antagonist, W146, and by inhibitors of the mitogen associated protein kinase (MAPK) and the phosphatidylinositol-3-kinase (PtdIns-3-K) pathways.", "entity1": "type-1 S1PR", "entity2": "W146", "span1": [82, 93], "span2": [114, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10623": {"label": 5, "data": {"text": "Histamine H1-receptor (H1R) antagonists, or antihistamines, often induce sedative side effects when used for the treatment of allergic disorders.", "entity1": "Histamine H1-receptor", "entity2": "antihistamines", "span1": [0, 21], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13953": {"label": 4, "data": {"text": "salmeterol and formoterol, for the beta(2)-adrenoceptor over the beta(1) or beta(3)), while others (e.g. isoprenaline) had little affinity-selectivity.", "entity1": "beta(1)", "entity2": "isoprenaline", "span1": [65, 72], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8485": {"label": 3, "data": {"text": "Furthermore, no impact on cytokine release (i.e., on IL-10, IL-6, IL-12/23p40 and TNF\u03b1 levels) was seen in LPS-stimulated human PBMCs, except with JWH-210 and JWH-122 which caused a decrease of TNF\u03b1 and IL-12/23p40.", "entity1": "TNF\u03b1", "entity2": "JWH-210", "span1": [194, 198], "span2": [147, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15173": {"label": 2, "data": {"text": "DNPKA markedly reduced these GnRH-stimulated FSH\u03b2 responses at both low and high pulse frequencies.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [45, 49], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15973": {"label": 1, "data": {"text": "Mechanistic Aspects of hSOD1 Maturation from the Solution Structure of Cu(I) -Loaded hCCS Domain 1 and Analysis of Disulfide-Free hSOD1 Mutants.", "entity1": "hSOD1", "entity2": "Cu(I)", "span1": [23, 28], "span2": [71, 76]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14284": {"label": 0, "data": {"text": "The mutant Fc domain (AglycoT-Fc1004) contained a total of 5 amino acid substitutions that conferred an activating to inhibitory ratio of 25 (A/I ratio; FcyRIIa-R131:Fc\u03b3RIIb).", "entity1": "Fc domain", "entity2": "amino acid", "span1": [11, 20], "span2": [61, 71]}, "weak_labels": [0, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7978": {"label": 3, "data": {"text": "The mechanism of interaction between JBP485 and 1,25(OH)(2)D(3) could be explained at least in part by inhibitory effect of 1,25(OH)(2)D(3) on expression of Oats in rat kidney.", "entity1": "Oats", "entity2": "1,25(OH)(2)D(3)", "span1": [157, 161], "span2": [124, 139]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3117": {"label": 8, "data": {"text": "First, addition of apolipoprotein A-I (apoA-I), a direct acceptor of the ATP-binding cassette transporter A1 (ABCA1)-secreted lipids, increased alpha-tocopherol secretion in a dose-dependent manner.", "entity1": "apoA-I", "entity2": "alpha-tocopherol", "span1": [39, 45], "span2": [144, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14387": {"label": 3, "data": {"text": "Inhibition of EGF/EGFR activation with naphtho[1,2-b]furan-4,5-dione blocks migration and invasion of MDA-MB-231 cells.", "entity1": "EGF", "entity2": "naphtho[1,2-b]furan-4,5-dione", "span1": [14, 17], "span2": [39, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4604": {"label": 3, "data": {"text": "A new inhibitor of VEGF receptor tyrosine kinases, vegfrecine (1), was isolated from the culture broth of Streptomyces sp.", "entity1": "VEGF receptor tyrosine kinases", "entity2": "vegfrecine", "span1": [19, 49], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8194": {"label": 1, "data": {"text": "Resveratrol improves cardiomyopathy in dystrophin-deficient mice through SIRT1 protein-mediated modulation of p300 protein.", "entity1": "p300", "entity2": "Resveratrol", "span1": [110, 114], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15981": {"label": 5, "data": {"text": "Collectively, these initial findings suggest that design and systematic modification of aminoalkylindoles such as 3 may lead to development of novel cannabinoid ligands with dual CB1R antagonist/CB2R agonist activity with potential for use as treatments of alcohol abuse.", "entity1": "CB1R", "entity2": "aminoalkylindoles", "span1": [179, 183], "span2": [88, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8413": {"label": 9, "data": {"text": "Moreover, since reduced levels of p21CIP1 and Chk2 proteins but no change in p53 levels could be detected in MCF-7 cells after BSC 3g or 3n treatment our results suggest that BSC treated cells die from lethal mitosis.", "entity1": "p53", "entity2": "BSC", "span1": [77, 80], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2943": {"label": 1, "data": {"text": "Vardenafil has higher affinity to phosphodiesterase-5 (PDE5) than sildenafil and lower administered dosage for the treatment of erectile dysfunction.", "entity1": "PDE5", "entity2": "sildenafil", "span1": [55, 59], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1238": {"label": 1, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "dexamethasone", "span1": [277, 280], "span2": [312, 325]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1376": {"label": 3, "data": {"text": "Micromolar Ntp dose-dependently increased the mean open channel probability in ligand-free solution (P(O(max))) and attenuated the ATP inhibition of K(IR)6.2/SUR1, but had no effect on homomeric K(IR)6.2 channels.", "entity1": "K(IR)6.2", "entity2": "ATP", "span1": [149, 157], "span2": [131, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2767": {"label": 3, "data": {"text": "Lumiracoxib is the first example of a marketed COX-2 inhibitor of the arylacetic acid class, and it is reported to be the most selective COXIB in vivo.", "entity1": "COX-2", "entity2": "arylacetic acid", "span1": [47, 52], "span2": [70, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3101": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine", "span1": [354, 357], "span2": [0, 45]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"997": {"label": 8, "data": {"text": "Fumarate reductase (FRD) is the key enzyme in fumarate respiration induced by anaerobic growth of bacteria.", "entity1": "FRD", "entity2": "fumarate", "span1": [20, 23], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1422": {"label": 3, "data": {"text": "To extend structure-activity analyses of binding sites within monoamine transporters and to determine which stereoisomer displayed the best selectivity for PET imaging applications, we tested the HED compounds for their abilities to inhibit [(3)H]neurotransmitter uptake into platelets, transfected cells, and chromaffin vesicles.", "entity1": "monoamine transporters", "entity2": "HED", "span1": [62, 84], "span2": [196, 199]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14781": {"label": 0, "data": {"text": "The CSN/IRF5 interaction occurred on the carboxyl and amino termini of IRF5; a single internal deletion from amino acids 455 to 466 (\u0394455-466) was found to significantly reduce IRF5 protein stability.", "entity1": "IRF5", "entity2": "amino acids", "span1": [177, 181], "span2": [109, 120]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2284": {"label": 3, "data": {"text": "In addition to this evidence (for the involvement of EP2 receptors), evidence for the involvement of EP1 receptors in the PGE1 mediated stimulation of Na,K-ATPase beta subunit gene transcription includes the stimulatory effect of 17-phenyl trinor PGE2, as well as the inhibitory effects of SC-51089.", "entity1": "Na,K-ATPase beta", "entity2": "SC-51089", "span1": [151, 167], "span2": [290, 298]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11436": {"label": 1, "data": {"text": "Due to its central role in the formation and stabilization of a thrombus, the P2Y12 receptor is a well-established target of antithrombotic drugs like ticlopidine or clopidogrel, which have proved efficacy in many clinical trials and experimental models of thrombosis.", "entity1": "P2Y12", "entity2": "ticlopidine", "span1": [78, 83], "span2": [151, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11561": {"label": 3, "data": {"text": "Antitumor activity of sorafenib in FLT3-driven leukemic cells.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [35, 39], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4605": {"label": 3, "data": {"text": "Vegfrecine, an Inhibitor of VEGF Receptor Tyrosine Kinases Isolated from the Culture Broth of Streptomyces sp.", "entity1": "VEGF Receptor Tyrosine Kinases", "entity2": "Vegfrecine", "span1": [28, 58], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9532": {"label": 8, "data": {"text": "These results suggest that Cat3 compensates for the loss of functional Cat1 in cells derived from Cat1 knockout mice and mediates the majority of high affinity arginine transport.", "entity1": "Cat3", "entity2": "arginine", "span1": [27, 31], "span2": [160, 168]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13309": {"label": 3, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "B-RAF", "entity2": "Sorafenib", "span1": [52, 57], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11226": {"label": 1, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "K(ATP) channel", "entity2": "sulfonylureas", "span1": [149, 163], "span2": [44, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3223": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "quercetin", "span1": [262, 280], "span2": [160, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9214": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "EGF", "entity2": "trifluoperazine", "span1": [261, 264], "span2": [142, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14904": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO3", "entity2": "trimethylamine", "span1": [71, 75], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11792": {"label": 1, "data": {"text": "NF-\u03baB-associated mechanisms underlying the response of embryonic cells to Doxorubicin.", "entity1": "NF-\u03baB", "entity2": "Doxorubicin", "span1": [0, 5], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3584": {"label": 1, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "p38", "entity2": "Wogonoside", "span1": [196, 199], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9945": {"label": 3, "data": {"text": "Sulfasalazine inhibited tumor necrosis factor alpha-induced activation of endogenous IKK in Jurkat T cells and SW620 colon cells, as well as the catalytic activity of purified IKK-alpha and IKK-beta in vitro.", "entity1": "IKK", "entity2": "Sulfasalazine", "span1": [85, 88], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6487": {"label": 4, "data": {"text": "The segments were contracted with the alpha(2)-adrenoceptor agonists brimonidine, apraclonidine, and oxymetazoline.", "entity1": "alpha(2)-adrenoceptor", "entity2": "apraclonidine", "span1": [38, 59], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10819": {"label": 9, "data": {"text": "Treatment with valsartan, doxazosin, or N-acetylcysteine did not significantly affect HIF-1alpha and VEGF proteins expression in the banding groups.", "entity1": "VEGF", "entity2": "doxazosin", "span1": [101, 105], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12935": {"label": 3, "data": {"text": "However, in vitro experiments simulating a uremic milieu revealed a marked concentration-dependent inhibition of arginase activity by urea in the tissue lysates.", "entity1": "arginase", "entity2": "urea", "span1": [113, 121], "span2": [134, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11025": {"label": 3, "data": {"text": "It was found that a single intragastric gavage by L-methionine resulted in inhibition of endothelium-dependent relaxation, markedly increased the serum level of malondialdehyde and decreased the activity of PON1 and SOD, similarly decreased the level of NO in the serum; but had no effects on endothelium-independent relaxation and angiotensin-converting enzyme activity compared with the control group.", "entity1": "PON1", "entity2": "L-methionine", "span1": [207, 211], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"8478": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "HTRA1", "entity2": "Gly", "span1": [71, 76], "span2": [254, 257]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15276": {"label": 5, "data": {"text": "The CRF(1) receptor antagonist SSR125543 prevents stress-induced cognitive deficit associated with hippocampal dysfunction: Comparison with paroxetine and D-cycloserine.", "entity1": "CRF(1) receptor", "entity2": "SSR125543", "span1": [4, 19], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9106": {"label": 8, "data": {"text": "Similar concentrations also inhibited the formation of leukotriene C4 (LTC4) by LTC synthetase, a detergent-solubilized cell free particulate enzyme from RBL cells which is capable of coupling LTA4 to glutathione.", "entity1": "LTC synthetase", "entity2": "LTA4", "span1": [80, 94], "span2": [193, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2559": {"label": 3, "data": {"text": "Imatinib was also found to inhibit M-CSF-induced osteoclast survival as well as M-CSF-induced osteoclast bone resorbing activity, but was without effect on interleukin 1alpha (IL-1alpha) and receptor activator of nuclear factor kappa B ligand (RANKL)-induced inhibition of osteoclasts apoptosis, further supporting the hypothesis that imatinib may affect mature osteoclasts through the inhibition of c-FMS.", "entity1": "M-CSF", "entity2": "Imatinib", "span1": [80, 85], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10060": {"label": 8, "data": {"text": "It showed high rat lymphoma growth-inhibitory and lytic activity in vitro (IC50 = 0.16 mM), based specifically on inhibition of x(c)--mediated cystine uptake, in contrast to its colonic metabolites, sulfapyridine and 5-aminosalicylic acid.", "entity1": "x(c)", "entity2": "cystine", "span1": [128, 132], "span2": [143, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8701": {"label": 3, "data": {"text": "Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: Structure-activity relationships (SAR) of the C3-phenyl moiety.", "entity1": "HIV capsid", "entity2": "phenyl", "span1": [72, 82], "span2": [155, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10279": {"label": 2, "data": {"text": "Long-term administration of propargylamines to rats increased the activities of antioxidative enzymes superoxide dismutase (SOD) and catalase in the brain regions containing dopamine neurons.", "entity1": "SOD", "entity2": "propargylamines", "span1": [124, 127], "span2": [28, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14513": {"label": 1, "data": {"text": "Filtering and analysis of data identified three oncogenic pathways interfered by 5-ASA: MAPK/ERK pathway, cell adhesion and \u03b2-catenin/Wnt signaling.", "entity1": "Wnt", "entity2": "5-ASA", "span1": [134, 137], "span2": [81, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15107": {"label": 1, "data": {"text": "Transcripts of GPx4 genes were more highly expressed in most tissues examined in vivo (except blood, head kidney and spleen), whereas those of the GPx1 genes were more responsive to selenium exposure in vitro, especially to the organic form.", "entity1": "GPx1", "entity2": "selenium", "span1": [147, 151], "span2": [182, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4427": {"label": 1, "data": {"text": "The keto and phenolic -OH are major factors that are prominently involved in interaction with COX-2 active site.", "entity1": "COX-2", "entity2": "phenolic", "span1": [94, 99], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1348": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "dopamine transporter", "entity2": "mazindol", "span1": [295, 315], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5997": {"label": 3, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "( Glu1]Pg", "entity2": "Cl-", "span1": [43, 52], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12086": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "3 beta-HSD", "entity2": "androst-5-ene-3 beta, 17 beta-diol", "span1": [74, 84], "span2": [224, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2838": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "lysine", "span1": [83, 99], "span2": [160, 166]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"386": {"label": 9, "data": {"text": "The antagonist SR 141716A has a high specificity for the central CB1 cannabinoid receptor and negligeable affinity for the peripheral CB2 receptor, making it an excellent tool for probing receptor structure-activity relationships.", "entity1": "CB2", "entity2": "SR 141716A", "span1": [134, 137], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14793": {"label": 2, "data": {"text": "In conclusion, this study provides the first evidence implicating that TSA inhibits TGF-\u03b2-induced ROS accumulation and myofibroblast differentiation via enhanced Nrf2-ARE signaling.", "entity1": "Nrf2", "entity2": "TSA", "span1": [162, 166], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8818": {"label": 3, "data": {"text": "Interestingly, SB203580, a selective inhibitor of p38 MAPK, blocked STIM1 phosphorylation and led to sustained STIM1-puncta formation and Ca2+ entry.", "entity1": "MAPK", "entity2": "SB203580", "span1": [54, 58], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8919": {"label": 2, "data": {"text": "The vasopressor response to the calcium channel activator, BAY-K-8644, which is mediated through the opening of voltage dependent calcium channels and the subsequent translocation of extracellular calcium, was significantly inhibited by carvedilol (1 mg/kg, iv), suggesting that carvedilol is also a calcium channel antagonist, consistent with our previous in vitro studies.", "entity1": "calcium channel", "entity2": "BAY-K-8644", "span1": [32, 47], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11760": {"label": 0, "data": {"text": "The protein is formed by an NN-terminal helicase-like domain, a C-terminal DNA polymerase domain, and a large central domain that spans between the two.", "entity1": "N-terminal helicase-like domain", "entity2": "N", "span1": [29, 60], "span2": [28, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11598": {"label": 8, "data": {"text": "In this study, we investigated the presence of H(2)S and the expression of H(2)S synthesizing enzymes, CSE and CBS, in isolated mouse pancreatic acini.", "entity1": "CSE", "entity2": "H(2)S", "span1": [103, 106], "span2": [75, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9109": {"label": 9, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "calmodulin", "entity2": "yohimbine", "span1": [165, 175], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10327": {"label": 2, "data": {"text": "Resiquimod enhances co-stimulatory marker expression, CCR7 expression, and pDC viability.", "entity1": "CCR7", "entity2": "Resiquimod", "span1": [54, 58], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8359": {"label": 3, "data": {"text": "Amino acid derived quinazolines as Rock/PKA inhibitors.", "entity1": "Rock", "entity2": "quinazolines", "span1": [35, 39], "span2": [19, 31]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1553": {"label": 8, "data": {"text": "Even though the activities of MAT and GNMT were elevated, the concentration of liver S-adenosylmethionine was decreased (24%, p<0.001) and S-adenosylhomocysteine increased (113%, p<0.001) in the dwarf mice.", "entity1": "GNMT", "entity2": "S-adenosylmethionine", "span1": [38, 42], "span2": [85, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8431": {"label": 0, "data": {"text": "The endogenous steroid lithocholic acid (LCA) dilates cerebral arteries via BK channel activation, which requires recognition by a BK \u03b21 site that includes Thr169.", "entity1": "BK \u03b21", "entity2": "Thr", "span1": [131, 136], "span2": [156, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3397": {"label": 9, "data": {"text": "To further characterize the inhibitory mechanisms of PSE at the transcriptional level, we examined the transcriptional activities of nuclear factor kappa B (NF-kappaB), nuclear factor of activated T cells (NFAT), and activator protein-1 (AP-1) transcription factors and found that PSE inhibited NF-kappaB-dependent transcriptional activity without affecting either the phosphorylation, the degradation of the cytoplasmic NF-kappaB inhibitory protein, IkappaBalpha or the DNA-binding activity.", "entity1": "NF-kappaB inhibitory protein", "entity2": "PSE", "span1": [421, 449], "span2": [281, 284]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3802": {"label": 3, "data": {"text": "As revealed by glucose oxidase (GOD) and radioimmunoassay (RIA), both dimethyldiguanide (DC, 0.6gkg(-1)d(-1)) and CPS (0.3, 0.6, 1.2gkg(-1)d(-1)) treatments significantly resulted in down-regulation of blood glucose and insulin levels in serum, while the levels of oxidative stress markers were markedly lowered through ELISA assay.", "entity1": "insulin", "entity2": "dimethyldiguanide", "span1": [220, 227], "span2": [70, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8759": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A3", "entity2": "diphenhydramine", "span1": [189, 195], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12404": {"label": 1, "data": {"text": "Moreover, Paeoniflorin promoted the nuclear translocation of nuclear factor erythroid 2 related factor-2 (Nrf-2).", "entity1": "nuclear factor erythroid 2 related factor-2", "entity2": "Paeoniflorin", "span1": [61, 104], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5941": {"label": 3, "data": {"text": "Trilostane, epostane and cyanoketone are potent inhibitors of 3 beta-HSD with Ki values of approximately 50 nM.", "entity1": "3 beta-HSD", "entity2": "epostane", "span1": [62, 72], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8479": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "HTRA1", "entity2": "Gly", "span1": [207, 212], "span2": [254, 257]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10190": {"label": 3, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP-B", "entity2": "Rifampicin", "span1": [102, 108], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3250": {"label": 1, "data": {"text": "The other endogenous steroids, androstenedione (ANE) and dihydrotestosterone (DHT), had considerably lower hAR transport rates.", "entity1": "hAR", "entity2": "steroids", "span1": [107, 110], "span2": [21, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"444": {"label": 1, "data": {"text": "Epinastine (WAL 801CL) is an antihistaminic drug with binding affinity at certain other receptors, including alpha-adrenergic receptors and various serotonin (5-HT) receptor subtypes.", "entity1": "serotonin (5-HT) receptor", "entity2": "WAL 801CL", "span1": [148, 173], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13063": {"label": 3, "data": {"text": "Similar to AMR and AMROH, adriamycin and etoposide (VP-16) are DNA topoisomerase II inhibitors.", "entity1": "DNA topoisomerase II", "entity2": "VP-16", "span1": [63, 83], "span2": [52, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7064": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARalpha", "entity2": "Am80", "span1": [38, 46], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11183": {"label": 3, "data": {"text": "Felbamate block of recombinant N-methyl-D-aspartate receptors: selectivity for the NR2B subunit.", "entity1": "N-methyl-D-aspartate receptors", "entity2": "Felbamate", "span1": [31, 61], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15135": {"label": 0, "data": {"text": "The enzyme (TcCA) has a very high catalytic activity for the CO(2) hydration reaction, being similar kinetically to the human (h) isoform hCA II, although it is devoid of the His64 proton shuttle.", "entity1": "hCA II", "entity2": "His", "span1": [138, 144], "span2": [175, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5923": {"label": 1, "data": {"text": "It is proposed that two molecules of estramustine phosphate interact with each of the three tubulin-binding sites of MAP2 and inhibit the MAP2:tubulin interaction by neutralising two highly conserved basic residues.", "entity1": "MAP2", "entity2": "estramustine phosphate", "span1": [117, 121], "span2": [37, 59]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"936": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "5-trifluorothymidine", "span1": [216, 236], "span2": [60, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10132": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "carprofen", "span1": [34, 37], "span2": [130, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9402": {"label": 1, "data": {"text": "Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).", "entity1": "retinoic acid receptors", "entity2": "tretinoin", "span1": [164, 187], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1355": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "DAT", "entity2": "methoxy", "span1": [317, 320], "span2": [186, 193]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2913": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "ion channel", "entity2": "cibenzoline", "span1": [9, 20], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13262": {"label": 3, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "mucin", "entity2": "ONO-1078", "span1": [114, 119], "span2": [20, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6636": {"label": 5, "data": {"text": "alpha(1A)-Adrenoceptor selective antagonists, 2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane (WB-4101; 0.1-1 mg/kg) and 5-methylurapidil (0.1-1 mg/kg), the alpha(1B)-adrenoceptor selective antagonist, 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765314; 0.3-1 mg/kg), as well as the alpha(1D)-adrenoceptor selective antagonist, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY-7378; 1 mg/kg), were used to delineate the adrenoceptor subtypes involved.", "entity1": "alpha(1A)-Adrenoceptor", "entity2": "2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane", "span1": [0, 22], "span2": [46, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15385": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "activin receptor-like kinase 5", "entity2": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole", "span1": [197, 227], "span2": [0, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5869": {"label": 9, "data": {"text": "By contrast, neither amoxapine nor amitriptyline can be considered as possible ligands of 5-HT1A and 5-HT1B receptors because their affinities for these sites are in the micromolar range (or even worse).", "entity1": "5-HT1A", "entity2": "amitriptyline", "span1": [90, 96], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5016": {"label": 8, "data": {"text": "These five CGPs also inhibited [(3)H]E217\u03b2G uptake by MRP4.", "entity1": "MRP4", "entity2": "[(3)H]E217\u03b2G", "span1": [54, 58], "span2": [31, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1448": {"label": 3, "data": {"text": "The selective norepinephrine (NE) transporter inhibitor atomoxetine (formerly called tomoxetine or LY139603) has been shown to alleviate symptoms in Attention Deficit/Hyperactivity Disorder (ADHD).", "entity1": "norepinephrine (NE) transporter", "entity2": "LY139603", "span1": [14, 45], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10896": {"label": 1, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "PDXK", "entity2": "ATP", "span1": [18, 22], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7023": {"label": 3, "data": {"text": "Competitive radioligand binding assays were performed using cells expressing either the human serotonin (5-HT) transporter (hSERT) or norepinephrine (NE) transporter (hNET) with K(i) values for DVS of 40.2 +/- 1.6 and 558.4 +/- 121.6 nM, respectively.", "entity1": "hNET", "entity2": "DVS", "span1": [167, 171], "span2": [194, 197]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12554": {"label": 1, "data": {"text": "Intracellular protein-bound [57Co]Cbl fractionated with methionine synthase (MS) and methylmalonyl-CoA mutase (MU) activity.", "entity1": "MU", "entity2": "[57Co]Cbl", "span1": [111, 113], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12472": {"label": 9, "data": {"text": "UGT2B10 was inactive in the glucuronidation of desipramine, nortriptyline, carbamazepine and afloqualone.", "entity1": "UGT2B10", "entity2": "desipramine", "span1": [0, 7], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15145": {"label": 9, "data": {"text": "The mRNA level for nestin (Nes, biomarker for stem Leydig cells) was significantly increased in the control testis on day 4 post-EDS, but not in the DEHP treated testes, suggesting that these nestin positive stem cells were differentiated into progenitor Leydig cells in the DEHP-treated testes.", "entity1": "nestin", "entity2": "DEHP", "span1": [19, 25], "span2": [149, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15292": {"label": 3, "data": {"text": "Bicyclic pyrazinone and pyrimidinone amides were designed and synthesized as potent TF-FVIIa inhibitors.", "entity1": "FVIIa", "entity2": "Bicyclic pyrazinone and pyrimidinone amides", "span1": [87, 92], "span2": [0, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7553": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "endothelial nitric oxide synthase", "entity2": "NO", "span1": [123, 156], "span2": [14, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"14135": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "TAK1", "entity2": "Celastrol", "span1": [146, 150], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"557": {"label": 5, "data": {"text": "Both the 5 alpha-reductase inhibitor finasteride and alpha 1-adrenoceptor antagonists (e.g. alfuzosin, doxazosin, prazosin, tamsulosin and terazosin) have been recommended as appropriate treatment options for patients with lower urinary tract symptoms (LUTS) associated with benign prostatic obstruction (BPO), and their efficacy has been proven in several placebo-controlled trials.", "entity1": "alpha 1-adrenoceptor", "entity2": "doxazosin", "span1": [53, 73], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13324": {"label": 3, "data": {"text": "All three salicylates inhibited the diabetes-induced translocation of p50 (a subunit of NF-kappaB) into nuclei of retinal vascular endothelial cells of the isolated retinal vasculature, as well as of p50 and p65 into nuclei of cells in the ganglion cell layer and inner nuclear layer on whole-retinal sections.", "entity1": "NF-kappaB", "entity2": "salicylates", "span1": [88, 97], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12248": {"label": 1, "data": {"text": "For the isolated PKCalpha C2 domain in the presence of physiological Ca2+ levels, the target lipids phosphatidylserine (PS) and phosphatidylinositol-4,5-bisphosphate (PIP2) are together sufficient to recruit the PKCalpha C2 domain to a lipid mixture mimicking the plasma membrane inner leaflet.", "entity1": "PKCalpha C2 domai", "entity2": "PS", "span1": [212, 229], "span2": [120, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15333": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "7-hydroxyflavone", "span1": [287, 296], "span2": [191, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14912": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "estrogen receptor-\u03b1", "entity2": "steroids", "span1": [236, 255], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4661": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "p22(phox)", "entity2": "resveratrol", "span1": [145, 154], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13109": {"label": 2, "data": {"text": "Such organization results in the local activation of PKA subsets through the generation of confined intracellular gradients of cAMP, but the mechanisms responsible for limiting the diffusion of cAMP largely remain to be clarified.", "entity1": "PKA", "entity2": "cAMP", "span1": [53, 56], "span2": [127, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3566": {"label": 1, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u.", "entity1": "IRS-1", "entity2": "MSG", "span1": [42, 47], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6773": {"label": 3, "data": {"text": "Thus, hydralazine activates the HIF pathway through inhibition of PHD activity and initiates a pro-angiogenic phenotype.", "entity1": "PHD", "entity2": "hydralazine", "span1": [66, 69], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6554": {"label": 3, "data": {"text": "In contrast, the mutants T844A, F972A and Q975A showed increased K(i) for cilostazol but no difference for milrinone from the recombinant PDE3A.", "entity1": "T844A", "entity2": "cilostazol", "span1": [25, 30], "span2": [74, 84]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8009": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "thrombin", "entity2": "IMG", "span1": [118, 126], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"372": {"label": 3, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2", "entity2": "DEX", "span1": [189, 193], "span2": [177, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12517": {"label": 9, "data": {"text": "The uncharged estramustine bound to both tubulin and MAPs, but no effects were seen on microtubule assembly, the composition of coassembled MAPs or the microtubule morphology.", "entity1": "MAPs", "entity2": "estramustine", "span1": [140, 144], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8028": {"label": 1, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "human TRPA1", "entity2": "apomorphine", "span1": [21, 32], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9569": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "IL-3", "entity2": "isoproterenol", "span1": [54, 58], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11676": {"label": 1, "data": {"text": "Studies over the past decades suggest that, besides cyclooxygenases, aspirin acetylates other cellular proteins.", "entity1": "cyclooxygenases", "entity2": "aspirin", "span1": [52, 67], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1607": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE1", "entity2": "DMA", "span1": [104, 108], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6627": {"label": 9, "data": {"text": "On the other hand, pranlukast did not modify the eosinophil spontaneous adhesion to the resting or IL-4 plus TNF-alpha-stimulated pulmonary endothelial cells.", "entity1": "IL-4", "entity2": "pranlukast", "span1": [99, 103], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12394": {"label": 1, "data": {"text": "Dexamethasone suppressed IL-11 gene transcription enhanced by PTH(1-34) without affecting \u0394FosB expression or Smad1 phosphorylation, and dexamethasone-GC receptor complex was bound to JunD, which forms heterodimers with \u0394FosB.", "entity1": "GC receptor", "entity2": "dexamethasone", "span1": [151, 162], "span2": [137, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14085": {"label": 3, "data": {"text": "SB203580 (a specific inhibitor of p38 kinase) markedly suppressed the increased expression of collagen type I and \u03b1-SMA in TGF-\u03b21-induced NPDFs.", "entity1": "kinase", "entity2": "SB203580", "span1": [38, 44], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"187": {"label": 1, "data": {"text": "Characterization of rat brain aldosterone receptors reveals high affinity for corticosterone.", "entity1": "rat brain aldosterone receptors", "entity2": "corticosterone", "span1": [20, 51], "span2": [78, 92]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7112": {"label": 3, "data": {"text": "Fulvestrant is a novel ER antagonist that destroys the ER and its signaling pathway and is not associated with tamoxifen-like agonist effects.", "entity1": "ER", "entity2": "Fulvestrant", "span1": [55, 57], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9888": {"label": 1, "data": {"text": "Both radioligands labeled mAch receptors in these brain regions, and the relative regional distributions of the specific binding of 3H-NMPB in vivo paralleled the distribution of mAch receptors.", "entity1": "mAch receptors", "entity2": "3H-NMPB", "span1": [26, 40], "span2": [132, 139]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13279": {"label": 9, "data": {"text": "The imatinib-resistant KIT(D816V) mutant, associated with systemic mastocytosis, was found to be resistant to sorafenib.", "entity1": "D816V", "entity2": "imatinib", "span1": [27, 32], "span2": [4, 12]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10560": {"label": 1, "data": {"text": "Irbesartan is a long-acting angiotensin II antagonist acting specifically at the level of the Type 1-receptor subtype (AT1-receptor).", "entity1": "AT1", "entity2": "Irbesartan", "span1": [119, 122], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5943": {"label": 9, "data": {"text": "Pimozide and thioridazine had no effect on the estradiol binding properties of the MCF-7 ER, nor did pimozide interfere with the induction of progesterone receptors by estradiol.", "entity1": "ER", "entity2": "Pimozide", "span1": [89, 91], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6868": {"label": 1, "data": {"text": "Our results suggest that easing of Fas-triggered fulminant hepatitis by minocycline may involve a mitochondrial apoptotic pathway, probably through preventing cytochrome c release and thereby blocking downstream caspase activation.", "entity1": "Fas", "entity2": "minocycline", "span1": [35, 38], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"578": {"label": 2, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cyclin E", "entity2": "Tomudex", "span1": [129, 137], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15320": {"label": 3, "data": {"text": "(2R)-IKM-159 locks the GluA2 in an open form, consistent with a pharmacological action as competitive antagonist of AMPA receptors.", "entity1": "GluA2", "entity2": "(2R)-IKM-159", "span1": [23, 28], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2886": {"label": 3, "data": {"text": "At PND35, the medial prefrontal cortex (mPFC) of rats given MPH showed 55% greater immunoreactivity (-ir) for the catecholamine marker tyrosine hydroxylase (TH), 60% more Nissl-stained cells, and 40% less norepinephrine transporter (NET)-ir density.", "entity1": "NET", "entity2": "MPH", "span1": [233, 236], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9988": {"label": 1, "data": {"text": "Moreover, it was suggested that promotion of CYP11A1 mRNA expression in Th2 cells was partially involved due to an increase in level of corticosterone in splenic tissue and the breakdown of Th cell responses locally in the splenic tissue, which then affected the maintenance of Th2 cell functions in the microenvironment of tumor-bearing mice.", "entity1": "CYP11A1", "entity2": "corticosterone", "span1": [45, 52], "span2": [136, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4422": {"label": 3, "data": {"text": "We describe here the isolation and biochemical characterization of the marine natural sesquiterpene palinurin as a GSK-3\u03b2 inhibitor.", "entity1": "GSK-3\u03b2", "entity2": "palinurin", "span1": [115, 121], "span2": [100, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14389": {"label": 3, "data": {"text": "These findings suggest that NFD inhibited the EGF-induced invasion and migration of MDA-MB-231 cells via EGFR-dependent PI3K/Akt signaling, leading to the down-regulation of MMP-9 expression.", "entity1": "EGF", "entity2": "NFD", "span1": [46, 49], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5750": {"label": 1, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "p50", "entity2": "vitamin C", "span1": [175, 178], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12232": {"label": 1, "data": {"text": "These data define PFD or PFD-related agents as promising agents for human cancers associated with enhanced TGF-beta activity.", "entity1": "TGF-beta", "entity2": "PFD", "span1": [107, 115], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5893": {"label": 3, "data": {"text": "Mouse ornithine decarboxylase (ODC) was expressed in Escherichia coli and the purified recombinant enzyme used for determination of the binding site for pyridoxal 5'-phosphate and of the residues modified in the inactivation of the enzyme by the enzyme-activated irreversible inhibitor, alpha-difluoromethylornithine (DFMO).", "entity1": "Mouse ornithine decarboxylase", "entity2": "DFMO", "span1": [0, 29], "span2": [318, 322]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5374": {"label": 3, "data": {"text": "Rapamycin inhibits proteinase and selected peptidase activities of the catalytic core proteasome at low micromolar concentrations.", "entity1": "proteinase", "entity2": "Rapamycin", "span1": [19, 29], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11186": {"label": 3, "data": {"text": "We conclude that felbamate exhibits modest selectivity for NMDA receptors composed of NR1a/NR2B subunits.", "entity1": "NR1a", "entity2": "felbamate", "span1": [86, 90], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15774": {"label": 3, "data": {"text": "Both ICI treatments, induced a significant decrease (p<0.01) in uterine estrogen receptor alpha (ER\u03b1) content, had no effect on uterine progesterone receptor (PR) protein expression and caused marked nuclear localization of cyclin D1, in both luminal and glandular uterine epithelium, as compared to vehicle-treated animals.", "entity1": "ER\u03b1", "entity2": "ICI", "span1": [97, 100], "span2": [5, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1115": {"label": 2, "data": {"text": "RESULTS: Indomethacin, in vitro and in vivo. induces an increase in erythorcyte CA I and CA II activity.", "entity1": "CA I", "entity2": "Indomethacin", "span1": [80, 84], "span2": [9, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2620": {"label": 3, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "T700A", "entity2": "foscarnet", "span1": [97, 102], "span2": [149, 158]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13980": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Wnt5a", "entity2": "chlorcyclizine", "span1": [79, 84], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6971": {"label": 1, "data": {"text": "Our data clearly indicate that GPR109A mediates nicotinic acid-induced flushing and that this effect involves release of PGE(2) and PGD(2), most likely from immune cells of the skin.", "entity1": "GPR109A", "entity2": "nicotinic acid", "span1": [31, 38], "span2": [48, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11174": {"label": 1, "data": {"text": "OBJECTIVE: To determine the expression of progesterone receptor (PR) mRNA and PR protein levels in the myometrium and leiomyomata from untreated and mifepristone pretreated women with leiomyoma and to examine the mechanism of mifepristone treatment on uterine leiomyomata.", "entity1": "progesterone receptor", "entity2": "mifepristone", "span1": [42, 63], "span2": [149, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"723": {"label": 8, "data": {"text": "On phosphorylation of Ser40 by protein kinase A, the affinity for H4biopterin increased ([S]0.5 = 11 +/- 2 microM) and the negative cooperativity was amplified (h = 0.27 +/- 0.03).", "entity1": "protein kinase A", "entity2": "Ser40", "span1": [31, 47], "span2": [22, 27]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6780": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-2", "entity2": "NS398", "span1": [257, 262], "span2": [141, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14065": {"label": 3, "data": {"text": "Aspirin and metformin (an activator of AMPK) increased inhibition of mTOR and Akt, as well as autophagy in CRC cells.", "entity1": "Akt", "entity2": "Aspirin", "span1": [78, 81], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"113": {"label": 9, "data": {"text": "Felodipine and the p-chloro analogue inhibited Ca2+/calmodulin-dependent caldesmon kinase with similar potencies (IC50 = 17.4 microM), whereas the oxidized and t-butyl analogues caused no inhibition.", "entity1": "caldesmon kinase", "entity2": "t-butyl", "span1": [73, 89], "span2": [160, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8758": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "diphenhydramine", "span1": [178, 184], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13449": {"label": 2, "data": {"text": "Moreover stimulation of COX-2 promoter activity was increased by those PUFAs or rosiglitazone.", "entity1": "COX-2 promoter", "entity2": "rosiglitazone", "span1": [24, 38], "span2": [80, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5625": {"label": 0, "data": {"text": "Our results suggest that inactivation facilitates cisapride block of HERG channels through affecting the positioning of Phe-656.", "entity1": "HERG", "entity2": "Phe", "span1": [69, 73], "span2": [120, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12612": {"label": 1, "data": {"text": "Likewise, GYKI 52466 (30-100 microM)) shifted the concentration-response curve for the effects of cyclothiazide on AMPA receptor-mediated e.p.s.c.", "entity1": "AMPA receptor", "entity2": "cyclothiazide", "span1": [115, 128], "span2": [98, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7822": {"label": 5, "data": {"text": "Efficacy of the GluK1/AMPA receptor antagonist LY293558 against seizures and neuropathology in a soman-exposure model without pretreatment and its pharmacokinetics after intramuscular administration.", "entity1": "AMPA receptor", "entity2": "LY293558", "span1": [22, 35], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"420": {"label": 1, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "SL 89,0591", "span1": [258, 286], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9204": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "alpha 2-macroglobulin", "entity2": "W-7", "span1": [209, 230], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12161": {"label": 1, "data": {"text": "This represents a novel mechanism of action for hydralazine and presents HIF as a potential target for treatment of ischemic disease.", "entity1": "HIF", "entity2": "hydralazine", "span1": [73, 76], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10847": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Gleevec", "span1": [119, 122], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11548": {"label": 8, "data": {"text": "BACKGROUND: Histamine synthesized by histidine decarboxylase (HDC) from L-histidine is a major chemical mediator in the development of nasal allergy which is characterized by nasal hypersensitivity.", "entity1": "HDC", "entity2": "Histamine", "span1": [62, 65], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"752": {"label": 5, "data": {"text": "The potentiation of the contractile effect induced by 5-HT is only somewhat modified by deendothelialization, but abolished by the thromboxane A2 receptor antagonists GR32191 and ridogrel.", "entity1": "thromboxane A2 receptor", "entity2": "GR32191", "span1": [131, 154], "span2": [167, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2133": {"label": 9, "data": {"text": "Using the nucleoside transporter deficient PK15NTD cells stably expressing ENT1 and ENT2, it was found that troglitazone inhibited ENT1 but had no effect on ENT2.", "entity1": "ENT2", "entity2": "troglitazone", "span1": [157, 161], "span2": [108, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13337": {"label": 1, "data": {"text": "Collectively then, these results indicate that LFA-1 contributes to the regulation of lymphocytic cholinergic activity via CD11a-mediated pathways and suggest that simvastatin exerts its immunosuppressive effects in part via modification of lymphocytic cholinergic activity.", "entity1": "LFA-1", "entity2": "simvastatin", "span1": [47, 52], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11923": {"label": 3, "data": {"text": "The most potent in\u2005vitro DASI discovered is an imidazole derivative with IC50 values against aromatase and steroid sulfatase in a JEG-3 cell preparation of 0.2 and 2.5\u2005nM, respectively.", "entity1": "steroid sulfatase", "entity2": "imidazole", "span1": [107, 124], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15242": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP2B1", "entity2": "silychristin", "span1": [24, 31], "span2": [280, 292]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"5824": {"label": 3, "data": {"text": "After the combined pituitary stimulation test (100 micrograms human CRH, 100 micrograms GnRH, 100 micrograms GH-releasing hormone, and 200 micrograms TRH), the ACTH peak (maximum increase at 30 min) was significantly blunted by loperamide from 9 +/- 1 to 4 +/- 1 pmol/L (P less than 0.001) and the area under the curve of ACTH from 0-120 min was reduced from 35 +/- 5 to 23 +/- 4 pmol/L.2 h (P less than 0.05).", "entity1": "ACTH", "entity2": "loperamide", "span1": [322, 326], "span2": [228, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7392": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "Delta(1)-pyrroline-5-carboxylate dehydrogenase", "entity2": "proline", "span1": [34, 80], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7072": {"label": 3, "data": {"text": "Simvastatin abolished these anti-CD11a mAb-induced increases in lymphocytic cholinergic activity in a manner independent of its cholesterol-lowering activity.", "entity1": "CD11a", "entity2": "Simvastatin", "span1": [33, 38], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10714": {"label": 2, "data": {"text": "The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan.", "entity1": "sigma1 receptor", "entity2": "dextromethorphan", "span1": [79, 94], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12387": {"label": 1, "data": {"text": "Evidence also outlines a role for oxytocin in the prosocial effects of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) in both rodents and humans.", "entity1": "oxytocin", "entity2": "Ecstasy", "span1": [34, 42], "span2": [112, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15483": {"label": 3, "data": {"text": "We developed a computational model of the hypothalamic-pituitary-gonadal (HPG) axis in female fathead minnows to predict dose-response and time-course (DRTC) behaviors for endocrine effects of the aromatase inhibitor, fadrozole (FAD).", "entity1": "aromatase", "entity2": "fadrozole", "span1": [197, 206], "span2": [218, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10055": {"label": 1, "data": {"text": "The x(c)- cystine transporter represents a novel target for sulfasalazine-like drugs with high potential for application in therapy of lymphoblastic and other malignancies dependent on extracellular cyst(e)ine.", "entity1": "x(c)- cystine transporter", "entity2": "sulfasalazine", "span1": [4, 29], "span2": [60, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14980": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "Chk1", "entity2": "ATO", "span1": [46, 50], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6284": {"label": 3, "data": {"text": "Concentration-response curves for the inhibition of monocyte COX-2 and platelet COX-1 were obtained in vitro after the incubation of meloxicam with whole blood samples.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [61, 66], "span2": [133, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10219": {"label": 2, "data": {"text": "The increase in AMPK alpha2 activity was likely due to a change in muscle energy status because ATP and phosphocreatine concentrations were lower after metformin treatment.", "entity1": "AMPK alpha2", "entity2": "metformin", "span1": [16, 27], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14338": {"label": 3, "data": {"text": "Finally, DMF suppressed unilateral ureteral obstruction (UUO)-induced renal fibrosis and alpha-SMA, fibronectin and type 1 collagen expression in the obstructed kidneys from UUO mice, along with increased and decreased expression of Nrf2 and phospho-Smad3, respectively.", "entity1": "phospho-Smad3", "entity2": "DMF", "span1": [242, 255], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9621": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBF2", "entity2": "ATP", "span1": [232, 236], "span2": [174, 177]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10960": {"label": 3, "data": {"text": "Miglustat, an imino sugar that reversibly inhibits glucosylceramide synthase and reduces intracellular substrate burden, is an oral treatment for patients with type 1 GD that was recently approved in the United States for symptomatic patients with mild to moderate clinical manifestations for whom ERT is not an option.", "entity1": "glucosylceramide synthase", "entity2": "Miglustat", "span1": [51, 76], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"4769": {"label": 3, "data": {"text": "Inhibition of angiogenesis and invasion by DMBT is mediated by downregulation of VEGF and MMP-9 through Akt pathway in MDA-MB-231 breast cancer cells.", "entity1": "VEGF", "entity2": "DMBT", "span1": [81, 85], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"562": {"label": 0, "data": {"text": "Several site-specific alterations in the C-terminus of full-length FGFR1IIIc, an isoform that otherwise absolutely rejects FGF-7, resulted in gain of FGF-7 binding.", "entity1": "FGFR1IIIc", "entity2": "C", "span1": [67, 76], "span2": [41, 42]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10087": {"label": 3, "data": {"text": "A series of studies is reviewed that assesses the relationship between cytokines released at the site of tissue injury and NSAID analgesia, and the in vivo selectivity of a selective cyclooxygenase (COX)-2 inhibitor (celecoxib) in comparison to a dual COX-1/COX-2 inhibitor (ketorolac).", "entity1": "COX-1", "entity2": "ketorolac", "span1": [252, 257], "span2": [275, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12703": {"label": 9, "data": {"text": "These two alleles were shown previously to be associated with ivermectin susceptibility (HG1A) and resistance (HG1E), respectively.", "entity1": "HG1E", "entity2": "ivermectin", "span1": [111, 115], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8034": {"label": 1, "data": {"text": "Dietary carbohydrates increase SCD-1 gene expression in liver by sterol response element binding protein (SREBP)-1c-dependent and SREBP-1c -independent pathways.", "entity1": "sterol response element binding protein (SREBP)-1c", "entity2": "carbohydrates", "span1": [65, 115], "span2": [8, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9373": {"label": 1, "data": {"text": "However, recovery from modulation by cyclothiazide was twofold slower for GluR-AiBi than for homomeric GluR-Ai, indicating that the GluR-A and GluR-B subunits are not functionally equivalent in controlling sensitivity to cyclothiazide.", "entity1": "GluR-Ai", "entity2": "cyclothiazide", "span1": [103, 110], "span2": [37, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"115": {"label": 1, "data": {"text": "Finally, the effects of felodipine and the three analogues on two processes which are dependent on myosin phosphorylation were examined, namely the actin-activated Mg2+-ATPase activity of myosin and the assembly of myosin filaments.", "entity1": "Mg2+-ATPase", "entity2": "felodipine", "span1": [164, 175], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11672": {"label": 1, "data": {"text": "The results support a role for rasagiline in protecting dopaminergic cells against free radical mediated damage and apoptosis in the presence of alpha-synuclein over-expression.", "entity1": "alpha-synuclein", "entity2": "rasagiline", "span1": [145, 160], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11288": {"label": 8, "data": {"text": "Firstly, transgenic plants overexpressing formate dehydrogenase (FDH, EC 1.2.1.2) were used to continue our previous studies on the function of FDH in formate metabolism.", "entity1": "formate dehydrogenase", "entity2": "formate", "span1": [42, 63], "span2": [151, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6261": {"label": 1, "data": {"text": "Pharmacological profile of neuroleptics at human monoamine transporters.", "entity1": "human monoamine transporters", "entity2": "neuroleptics", "span1": [43, 71], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4078": {"label": 1, "data": {"text": "Overall, higher alcohol production was reduced by ammonium supplementation, and this can be correlated with a general downregulation of genes encoding decarboxylases and dehydrogenases of the Ehrlich pathway.", "entity1": "Ehrlich pathway", "entity2": "ammonium", "span1": [192, 207], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"16042": {"label": 3, "data": {"text": "Rats intoxicated with Cd for 30 days, significantly increased tissue malondialdehyde (MDA) levels and significantly decreased enzymatic antioxidants superoxide dismutase, glutathione peroxidase and catalase in the frontal cortex tissue.", "entity1": "glutathione peroxidase", "entity2": "Cd", "span1": [171, 193], "span2": [22, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10153": {"label": 1, "data": {"text": "EM-800 and EM-652 are the most potent pure antiestrogens and EM-652 has the highest affinity of all antiestrogens to ER.", "entity1": "ER", "entity2": "EM-800", "span1": [117, 119], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9330": {"label": 1, "data": {"text": "Cell lines stably expressing EAA3a protein formed homomeric ligand-gated ion channels responsive, in order of decreasing affinity to domoate, kainate, L-glutamate and (RS)-alpha-amino-3-hydroxy-5- methylisoxazole-propionate (AMPA).", "entity1": "EAA3a", "entity2": "(RS)-alpha-amino-3-hydroxy-5- methylisoxazole-propionate", "span1": [29, 34], "span2": [167, 223]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12530": {"label": 8, "data": {"text": "Differential lactose/lactulose/L-rhamnose absorption provides a non-invasive and sensitive index of small intestinal integrity of value for the interpretation of prolonged or otherwise complicated enteritis and the distinction of primary secondary intestinal lactase deficiency.", "entity1": "lactase", "entity2": "lactose", "span1": [259, 266], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3582": {"label": 1, "data": {"text": "In conclusion, these results suggested that pioglitazone protected against cisplatin- induced nephrotoxicity through its interaction with PPAR-\u03b3 receptors and antioxidant effects.", "entity1": "PPAR-\u03b3", "entity2": "pioglitazone", "span1": [138, 144], "span2": [44, 56]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13250": {"label": 1, "data": {"text": "Cytokines, lipopolysaccharides and other inflammatory mediators such as prostaglandin and leukotriene are related to the secretion and production of mucin.", "entity1": "mucin", "entity2": "prostaglandin", "span1": [149, 154], "span2": [72, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14537": {"label": 3, "data": {"text": "In addition, our exploration further revealed that the suppressive action of catalpol on inflammation was mediated via inhibiting nuclear factor-\u03baB (NF-\u03baB) activation.", "entity1": "NF-\u03baB", "entity2": "catalpol", "span1": [149, 154], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3428": {"label": 1, "data": {"text": "Notably, the introduction of the F723A mutation greatly enhanced the gefitinib sensitivity of the wild-type EGFR in vivo, supporting our hypothesis that the expansion of the active-site cleft results in enhanced gefitinib sensitivity.", "entity1": "F723A", "entity2": "gefitinib", "span1": [33, 38], "span2": [69, 78]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9430": {"label": 3, "data": {"text": "Here we report that alendronate is a potent inhibitor of the protein-tyrosine-phosphatase-meg1 (PTPmeg1).", "entity1": "PTPmeg1", "entity2": "alendronate", "span1": [96, 103], "span2": [20, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15450": {"label": 8, "data": {"text": "Thus, decreasing liver AOX activity by three quite different procedures gave a corresponding decrease for in vivo reductive metabolites in the liver of IMI-treated mice.", "entity1": "AOX", "entity2": "IMI", "span1": [23, 26], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9914": {"label": 2, "data": {"text": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid (WY-14,643), a specific ligand of the PPAR-alpha subtype, causes the most dramatic increase in UCP-3 mRNA, whereas troglitazone, a specific activator of PPAR-gamma, also significantly increases UCP-3 mRNA abundance in skeletal muscle of lactating mice.", "entity1": "UCP-3", "entity2": "WY-14,643", "span1": [151, 156], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7790": {"label": 3, "data": {"text": "Second, feeding increased both the expression of COX isoforms and PGE(2) level in the duodenum, and the effects were markedly inhibited by pretreatment with cimetidine.", "entity1": "COX", "entity2": "cimetidine", "span1": [49, 52], "span2": [157, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11866": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "malvidin", "span1": [118, 143], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1572": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "acetylcholinesterase", "entity2": "pyrano[2,3-b]quinolines", "span1": [4, 24], "span2": [103, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4356": {"label": 1, "data": {"text": "\u03b2-Lapachone (\u03b2-Lap) is a 1,2-orthonaphthoquinone that selectively induces cell death in human cancer cells through NAD(P)H:quinone oxidoreductase-1 (NQO1).", "entity1": "NAD(P)H:quinone oxidoreductase-1", "entity2": "\u03b2-Lapachone", "span1": [115, 147], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4119": {"label": 1, "data": {"text": "Key marker of diabetes in cells is the insulin dependent glucose transporter-4 (Glut-4) which also responds to exogenous chemicals, and is over expressed up to 5- and 4-fold, by Tinospora cordifolia and palmatine, respectively.", "entity1": "insulin dependent glucose transporter-4", "entity2": "palmatine", "span1": [39, 78], "span2": [203, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15707": {"label": 1, "data": {"text": "Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone.", "entity1": "MMP-9", "entity2": "chalcone", "span1": [108, 113], "span2": [167, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14388": {"label": 3, "data": {"text": "Inhibition of EGF/EGFR activation with naphtho[1,2-b]furan-4,5-dione blocks migration and invasion of MDA-MB-231 cells.", "entity1": "EGFR", "entity2": "naphtho[1,2-b]furan-4,5-dione", "span1": [18, 22], "span2": [39, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13092": {"label": 2, "data": {"text": "The most active of these compounds, gliquidone, is shown to be as potent as pioglitazone at inducing PPARgamma target gene expression.", "entity1": "PPARgamma", "entity2": "pioglitazone", "span1": [101, 110], "span2": [76, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1610": {"label": 8, "data": {"text": "In conclusion, only specific apical NHE3 inhibition increased DBS, whereas prostaglandin synthesis, Na+-HCO3- cotransporter activation, or intracellular HCO3- formation by carbonic anhydrase was not involved.", "entity1": "carbonic anhydrase", "entity2": "HCO3", "span1": [172, 190], "span2": [153, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"13039": {"label": 2, "data": {"text": "ATRA regulates gene expression via the activation of the retinoic acid receptor (RAR)alpha in human DCs, and RARalpha acutely regulates CD1d expression.", "entity1": "CD1d", "entity2": "ATRA", "span1": [136, 140], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1664": {"label": 1, "data": {"text": "Inhibition of binding of the alpha2-receptor antagonist [3H]RX821002 to recombinant alpha2-receptors by etomidate was tested in human embryonic kidney (HEK293) cells in vitro.", "entity1": "alpha2-receptors", "entity2": "etomidate", "span1": [84, 100], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10555": {"label": 1, "data": {"text": "The retention and slow diffusion of DMI and nisoxetine from membranes may contribute to their pharmacological and modulatory action on NET.", "entity1": "NET", "entity2": "DMI", "span1": [135, 138], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4598": {"label": 9, "data": {"text": "A significant decrease in HLA-DR expression was observed in the AP and fractionated procyanidin-treated cells in the presence of ovalbumin (OVA), but no effect on CD86 expression was observed.", "entity1": "CD86", "entity2": "procyanidin", "span1": [163, 167], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2845": {"label": 1, "data": {"text": "BACKGROUND: CYP2C9 polymorphisms are associated with decreased S-warfarin clearance and lower maintenance dosage.", "entity1": "CYP2C9", "entity2": "S-warfarin", "span1": [12, 18], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6738": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "RTKs", "entity2": "phenylaminopyrimidine", "span1": [155, 159], "span2": [77, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7833": {"label": 2, "data": {"text": "Nevertheless, low L-BMAA concentrations (\u2265 0.1mM, 48 h) increased protein ubiquitination, 20S proteasomal and caspase 12 activity, expression of the endoplasmic reticulum (ER) stress marker CHOP, and enhanced phosphorylation of elf2\u03b1 in SH-SY5Y cells.", "entity1": "caspase 12", "entity2": "L-BMAA", "span1": [110, 120], "span2": [18, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6826": {"label": 3, "data": {"text": "These results suggest that pitavastatin efficiently increases apoA-I in the culture medium of HepG2 cells by promoting apoA-I production through inhibition of HMG-CoA reductase and suppression of Rho activity and by protecting apoA-I from catabolism through ABCA1 induction and lipidation of apoA-I.", "entity1": "Rho", "entity2": "pitavastatin", "span1": [196, 199], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4254": {"label": 2, "data": {"text": "Treatment of HDP cells with a c-Jun NH2-terminal kinase (JNK) inhibitor also reduced butein-induced HO-1 expression, and butein treatment led to increased JNK phosphorylation.", "entity1": "HO-1", "entity2": "butein", "span1": [100, 104], "span2": [85, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12744": {"label": 1, "data": {"text": "These studies demonstrate that AMPK activity is subject to regulation by both glucose and metformin in pancreatic islets and clonal beta-cells.", "entity1": "AMPK", "entity2": "metformin", "span1": [31, 35], "span2": [90, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10673": {"label": 1, "data": {"text": "In conclusion, TT-235 may inhibit the uterine response to oxytocin by decreasing oxytocin receptor numbers and oxytocin binding affinity, which might explain the prolonged oxytocin antagonist activity of TT-235.", "entity1": "oxytocin", "entity2": "TT-235", "span1": [111, 119], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8199": {"label": 3, "data": {"text": "We previously reported that caffeoyl-amino acidyl-hydroxamic acid (CA-Xaa-NHOH) acted as both a good antioxidant and tyrosinase inhibitor, in particular when caffeic acid was conjugated with proline or amino acids having aromatic ring like phenylalanine.", "entity1": "tyrosinase", "entity2": "CA-Xaa-NHOH", "span1": [117, 127], "span2": [67, 78]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8004": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "FXa", "entity2": "hyperoside", "span1": [195, 198], "span2": [147, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5815": {"label": 9, "data": {"text": "In four cultured human corticotropic adenomas, loperamide was not able to reduce basal and CRH-induced ACTH secretion.", "entity1": "CRH", "entity2": "loperamide", "span1": [91, 94], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12627": {"label": 1, "data": {"text": "The FP receptor bound PGF2 alpha and fluprostenol with Ki values of 3-4 nM.", "entity1": "FP receptor", "entity2": "PGF2", "span1": [4, 15], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9252": {"label": 1, "data": {"text": "Ergovaline inhibition of the binding of the D2-specific radioligand, [3H]YM-09151-2, exhibited a KI (inhibition constant) of 6.9 +/- 2.6 nM, whereas dopamine was much less potent (370 +/- 160 nM).", "entity1": "D2", "entity2": "Ergovaline", "span1": [44, 46], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8391": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "CAT", "entity2": "Cd", "span1": [154, 157], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7773": {"label": 5, "data": {"text": "GDC-0152 is a small-molecule drug that triggers tumor cell apoptosis by selectively antagonizing IAPs.", "entity1": "IAPs", "entity2": "GDC-0152", "span1": [97, 101], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5394": {"label": 4, "data": {"text": "The experiments were performed on 80 male Wistar rats, 58 of which survived, subdivided into 3 groups: C-control rats, I-EAP group, and II-EAP group treated with the adenosine A3 receptor agonist IB-MECA (1-deoxy-1-6[[(3-iodophenyl) methyl]amino]-9H-purin-9-yl)-N-methyl-B-D-ribofuronamide at a dose of 0.75\u00a0mg/kg b.w.", "entity1": "adenosine A3 receptor", "entity2": "IB-MECA", "span1": [166, 187], "span2": [196, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8272": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "cytochrome P4502B6", "entity2": "N", "span1": [59, 77], "span2": [10, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6727": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "indolinones", "span1": [273, 279], "span2": [129, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3680": {"label": 9, "data": {"text": "8-pCPT-2'-O-Me-cAMP-AM alone (5 \u03bcM) did not stimulate insulin secretion, but did increase intracellular Ca(2+) concentration significantly, and this activity was inhibited by 25 \u03bcM 2-aminoethoxydiphenylborate (2-APB) or the removal of extracellular Ca(2+).", "entity1": "insulin", "entity2": "8-pCPT-2'-O-Me-cAMP-AM", "span1": [54, 61], "span2": [0, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8792": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-Rb", "entity2": "CAPE", "span1": [213, 223], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"900": {"label": 7, "data": {"text": "Our data demonstrate differences in the mechanism of stimulation of phenylalanine hydroxylase and nitric oxide synthase by H(4)biopterin.", "entity1": "nitric oxide synthase", "entity2": "H(4)biopterin", "span1": [98, 119], "span2": [123, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6408": {"label": 3, "data": {"text": "Isoproterenol (50 to 100 nmol/L) was used to mimic an increase in beta-adrenergic tone, d-sotalol (100 micromol/L) to block I(Kr) (LQT2 model), and ATX-II (20 nmol/L) to augment late I(Na) (LQT3 model).", "entity1": "I(Kr)", "entity2": "d-sotalol", "span1": [124, 129], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11080": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "cAMP phosphodiesterase", "entity2": "t-butyl", "span1": [86, 108], "span2": [257, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"0": {"label": 3, "data": {"text": "The failure of the myometrium to respond to ritodrine (desensitization) was associated with significant reductions in agonist-induced cyclic adenosine monophosphate production and beta 2-adrenergic receptor concentration in myometrial tissue collected from these animals compared with the saline solution-treated controls.", "entity1": "beta 2-adrenergic receptor", "entity2": "ritodrine", "span1": [180, 206], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3982": {"label": 1, "data": {"text": "Since DNA methylation is regulated by DNA methyltransferases and methyl cytosine-binding proteins, this study assessed the extent to which developmental Pb exposure might affect expression of these proteins in the hippocampus.", "entity1": "methyl cytosine-binding proteins", "entity2": "Pb", "span1": [65, 97], "span2": [153, 155]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7729": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LHRH", "entity2": "goserelin", "span1": [39, 43], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6047": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "m-CPP", "span1": [63, 69], "span2": [128, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14928": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "methyl", "span1": [257, 260], "span2": [166, 172]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1703": {"label": 8, "data": {"text": "Although a proton-stimulated uptake of cefadroxil was demonstrated in PEPT2(+/+) mice (pH 6.5 versus pH 7.4; p < 0.01), no pH dependence was observed in PEPT2(-/-) mice.", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [70, 75], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10859": {"label": 1, "data": {"text": "Interestingly, we identified 4-methylhistamine as a high-affinity H(4)R ligand (K(i) = 50 nM) that has a >100-fold selectivity for the hH(4)R over the other histamine receptor subtypes.", "entity1": "H(4)R", "entity2": "4-methylhistamine", "span1": [66, 71], "span2": [29, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"482": {"label": 1, "data": {"text": "Extensive inhibitions of TREK-1 activity are observed after activation of protein kinases A and C. TREK-1 currents are sensitive to extracellular K+ and Na+.", "entity1": "TREK-1", "entity2": "Na+", "span1": [99, 105], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11442": {"label": 1, "data": {"text": "We also studied the effects of thalidomide on COX-1, COX-2 or bcl-2 expression, TNFalpha, VEGF, GSH and cytochrome c in these cells.", "entity1": "VEGF", "entity2": "thalidomide", "span1": [90, 94], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7965": {"label": 1, "data": {"text": "The translocator protein (18-kDa) TSPO is an ubiquitous high affinity cholesterol-binding protein reported to be present in the endothelial and smooth muscle cells of the blood vessels; its expression dramatically increased in macrophages found in atherosclerotic plaques.", "entity1": "translocator protein (18-kDa) TSPO", "entity2": "cholesterol", "span1": [4, 38], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15505": {"label": 3, "data": {"text": "Synthesis and in-silico studies of some diaryltriazole derivatives as potential cyclooxygenase inhibitors.", "entity1": "cyclooxygenase", "entity2": "diaryltriazole", "span1": [80, 94], "span2": [40, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13849": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "promegestone", "span1": [252, 261], "span2": [125, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2349": {"label": 5, "data": {"text": "GW9662, a PPARgamma antagonist, prevented (P < 0.01) the lutein-induced iNOS mRNA downregulation in HD11 cells.", "entity1": "PPARgamma", "entity2": "GW9662", "span1": [10, 19], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14509": {"label": 3, "data": {"text": "The MCAO-induced decrease in insulin receptor levels in the liver and skeletal muscle on day 1 was recovered to control levels by orexin-A, and this effect of orexin-A was reversed by the administration of SB334867 as well as by hypothalamic BDNF knockdown.", "entity1": "insulin receptor", "entity2": "SB334867", "span1": [29, 45], "span2": [206, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"906": {"label": 8, "data": {"text": "N(5)-Substituted H(4)biopterin derivatives were not oxidized to products serving as substrates for dihydropteridine reductase and,depending on the substituent, were competitive inhibitors of phenylalanine hydroxylase: N(5)-methyl- and N(5)-hydroxymethyl H(4)biopterin inhibited phenylalanine hydroxylase, whereas N(5)-formyl- and N(5)-acetyl H(4)biopterin had no effect.", "entity1": "dihydropteridine reductase", "entity2": "N(5)-Substituted H(4)biopterin", "span1": [99, 125], "span2": [0, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"8445": {"label": 8, "data": {"text": "Uptake of estrone-3-sulfate (5\u2009nM) by OATP1B1 was reduced by 82%-95%.", "entity1": "OATP1B1", "entity2": "estrone-3-sulfate", "span1": [38, 45], "span2": [10, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13998": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "RET", "entity2": "Cabozantinib", "span1": [239, 242], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12527": {"label": 8, "data": {"text": "The test procedure was verified with respect to intestinal lactose hydrolysis by demonstrating a linear relationship between lactose/lactulose excretion and log jejunal mucosal lactase activity by in vitro assay (R2 = 0.95) in a further group of subjects.", "entity1": "lactase", "entity2": "lactose", "span1": [177, 184], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6562": {"label": 3, "data": {"text": "Molecular models show that the PDE3 inhibitors cilostazol and milrinone share some of common residues but interact with distinct residues at the active site, suggesting that selective inhibitors can be designed with flexible size against PDE3 active site.", "entity1": "PDE3", "entity2": "milrinone", "span1": [31, 35], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"196": {"label": 0, "data": {"text": "Here we report the amino acid sequence of the bovine oxytocin-neurophysin I (OT-NpI) precursor which was derived from sequence analysis of the cloned cDNA.", "entity1": "bovine oxytocin-neurophysin I (OT-NpI) precursor", "entity2": "amino acid", "span1": [46, 94], "span2": [19, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6073": {"label": 0, "data": {"text": "Within the conserved transmembrane domains, the sequences exhibit approximately 52%, 59%, 65%, and 68% amino acid identity with the known rat 5-HT1A, rat 5-HT1B, rat 5-HT1D, and human 5-HT1E receptors, respectively.", "entity1": "rat 5-HT1A", "entity2": "amino acid", "span1": [138, 148], "span2": [103, 113]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15015": {"label": 3, "data": {"text": "In agreement with these data, the exogenous treatment of SAH or inhibition of SAHH by specific siRNA or another type of inhibitor, 3-deazaadenosine (DAZA), similarly resulted in antitumorigenic responses, suppressive activity on Src, the alteration of actin cytoskeleton, and a change of the colocalization pattern between actin and Src.", "entity1": "Src", "entity2": "SAH", "span1": [229, 232], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5264": {"label": 0, "data": {"text": "Interestingly, Nox4 activity is also stimulated by reducing agents that possibly act by reducing the disulfide bridge (Cys226, Cys270) located in the extracellular E-loop of Nox4.", "entity1": "Nox4", "entity2": "Cys", "span1": [174, 178], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13929": {"label": 2, "data": {"text": "Different VDRAs are known to have differential effects on serum calcium (Ca), which may also affect serum PTH levels since serum Ca regulates PTH secretion mediated by the Ca-sensing receptor (CaSR).", "entity1": "PTH", "entity2": "Ca", "span1": [142, 145], "span2": [129, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5066": {"label": 3, "data": {"text": "Rg1 attenuated the A\u03b225-35-associated mitochondrial apoptotic events, accompanied by inhibiting HIF-1\u03b1 expression followed by intracellular reactive nitrogen species generation, and protein nitrotyrosination.", "entity1": "A\u03b225-35", "entity2": "Rg1", "span1": [19, 26], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9353": {"label": 0, "data": {"text": "Single-strand conformational analysis and nucleotide sequencing of the entire coding region of the PC3 gene in 102 Japanese subjects with NIDDM revealed missense mutations in exons 2 (Arg/Gln53) and 14 (Gln/Glu638), neither of which was associated with NIDDM in this population.", "entity1": "Arg/Gln53", "entity2": "nucleotide", "span1": [184, 193], "span2": [42, 52]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10102": {"label": 3, "data": {"text": "The elevation in brain alanine levels could be explained, at least in part, by a time- and dose-dependent inhibitory effect of PLZ on alanine transaminase (ALA-T), although as with GABA the increases are higher than expected from the degree of enzyme inhibition produced.", "entity1": "alanine transaminase", "entity2": "PLZ", "span1": [134, 154], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15538": {"label": 2, "data": {"text": "CK significantly inhibited DMN-induced increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, fibrosis score, and hepatic malondialdehyde and collagen content.", "entity1": "collagen", "entity2": "DMN", "span1": [186, 194], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10148": {"label": 8, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "COX", "entity2": "arachidonic acid", "span1": [93, 96], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12979": {"label": 8, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "DAG kinase", "entity2": "phosphatidic acid", "span1": [120, 130], "span2": [99, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"12184": {"label": 1, "data": {"text": "To probe into the \"logic\" of this enigma, we have started comparative studies among evolutionarily distant organisms, such as mouse and Saccharomyces cerevisiae, and we are now looking for biotin effects on specific genes and proteins, such as HCS and hexokinases, and on their proteomes.", "entity1": "HCS", "entity2": "biotin", "span1": [244, 247], "span2": [189, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13461": {"label": 5, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "PPARgamma", "entity2": "GW9662", "span1": [47, 56], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2374": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "RAF", "entity2": "Nexavar", "span1": [71, 74], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12514": {"label": 1, "data": {"text": "We have named this activity 11 beta HSD2 to distinguish it from the NADP-dependent 11 beta HSD.", "entity1": "11 beta HSD", "entity2": "NADP", "span1": [83, 94], "span2": [68, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14654": {"label": 3, "data": {"text": "Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors.", "entity1": "TNIK", "entity2": "4-phenyl-2-phenylaminopyridine", "span1": [50, 54], "span2": [13, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10936": {"label": 5, "data": {"text": "Losartan (COZAAR) is the prototype of a new class of potent and selective angiotensin II (AII) type 1 (AT(1)) receptor antagonists with the largest published preclinical and clinical data base.", "entity1": "angiotensin II (AII) type 1 (AT(1)) receptor", "entity2": "Losartan", "span1": [74, 118], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11717": {"label": 1, "data": {"text": "Our study aims to explore the potent effects of AC, as a marker component of Aconitum, on CYP3A using the probe buspirone in rats.", "entity1": "CYP3A", "entity2": "buspirone", "span1": [90, 95], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13776": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Lapatinib", "span1": [14, 16], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4446": {"label": 3, "data": {"text": "Inhibition of monoamine oxidase by phthalide analogues.", "entity1": "monoamine oxidase", "entity2": "phthalide", "span1": [14, 31], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3804": {"label": 3, "data": {"text": "These findings demonstrate that cinnamon polyphenols can exert the hypoglycemic and hypolipidemic effects through the mechanisms that may be associated with repairing pancreatic beta cells in diabetic mice and improving its anti-oxidative capacity, as well as attenuating cytotoxicity via inhibition of iNOS, NF-\u03baB activation.", "entity1": "NF-\u03baB", "entity2": "polyphenols", "span1": [309, 314], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7935": {"label": 3, "data": {"text": "Altogether, our results suggest that a high dose of glucosamine may inhibit cell proliferation through apoptosis and disturb cell cycle progression with a halt at G(0)/G(1) phase, and that this occurs, at least in part, by a reduction in Rb phosphorylation together with modulation of p21, p53 and HO-1 expression, and nuclear p21 accumulation.", "entity1": "Rb", "entity2": "glucosamine", "span1": [238, 240], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6348": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "candesartan", "span1": [18, 21], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"488": {"label": 1, "data": {"text": "Conversely, opioid antagonists such as naloxone and naltrexone (which bind to non-selectively opioid receptors) have been shown to decrease alcohol consumption under various experimental conditions.", "entity1": "opioid receptors", "entity2": "naloxone", "span1": [94, 110], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15900": {"label": 1, "data": {"text": "Here, we report that synaptotagmin-1 is necessary for expression of the vesicular Ca(2+) /H(+) -antiport.", "entity1": "synaptotagmin-1", "entity2": "Ca(2+)", "span1": [21, 36], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13759": {"label": 9, "data": {"text": "Although in vivo bosutinib is inactive against ABL T315I, we found this clinically important mutant to be enzymatically inhibited in the mid-nanomolar range.", "entity1": "T315I", "entity2": "bosutinib", "span1": [51, 56], "span2": [17, 26]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11684": {"label": 1, "data": {"text": "Thiazolidinediones (TZDs) are insulin sensitizers used for treatment of diabetes.", "entity1": "insulin", "entity2": "Thiazolidinediones", "span1": [30, 37], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1768": {"label": 1, "data": {"text": "This study demonstrates enhanced cardiostimulation by CGP 12177A (in the presence of propranolol) in rat ventricular myocytes overexpressing beta(1)-adrenoceptors, mediated by a Gs/cAMP signalling pathway.", "entity1": "Gs", "entity2": "propranolol", "span1": [178, 180], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7491": {"label": 3, "data": {"text": "Phenserine is also unique because of differing actions of its enantiomers: (-)-phenserine is the active enantiomer for inhibition of AChE, whereas (+)-phenserine ('posiphen') has weak activity as an AChE inhibitor and can be dosed much higher.", "entity1": "AChE", "entity2": "posiphen", "span1": [199, 203], "span2": [164, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13975": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Bmp4", "entity2": "chlorcyclizine", "span1": [92, 96], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8488": {"label": 3, "data": {"text": "Furthermore, no impact on cytokine release (i.e., on IL-10, IL-6, IL-12/23p40 and TNF\u03b1 levels) was seen in LPS-stimulated human PBMCs, except with JWH-210 and JWH-122 which caused a decrease of TNF\u03b1 and IL-12/23p40.", "entity1": "TNF\u03b1", "entity2": "JWH-122", "span1": [194, 198], "span2": [159, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12095": {"label": 1, "data": {"text": "SB 200646, which demonstrates some selectivity for 5-HT receptors in rat stomach fundus, should provide a useful ligand for confirmation of this view and allow discrimination of 5-HT2B function both in vitro and in vivo.", "entity1": "5-HT2B", "entity2": "SB 200646", "span1": [178, 184], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5198": {"label": 3, "data": {"text": "Inhibition of mTOR by low dose rapamycin decreases HG-induced Nox4 and Nox1, NADPH oxidase activity and podocyte apoptosis.", "entity1": "Nox1", "entity2": "rapamycin", "span1": [71, 75], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3786": {"label": 2, "data": {"text": "Phillyrin attenuates high glucose-induced lipid accumulation in human HepG2 hepatocytes through the activation of LKB1/AMP-activated protein kinase-dependent signalling.", "entity1": "AMP-activated protein kinase", "entity2": "Phillyrin", "span1": [119, 147], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4873": {"label": 3, "data": {"text": "In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAF(V600E) inhibitors.", "entity1": "BRAF", "entity2": "N-(thiophen-2-yl) benzamide", "span1": [142, 146], "span2": [92, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1571": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "butyrylcholinesterase", "entity2": "pyrano[2,3-b]quinolines", "span1": [36, 57], "span2": [103, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12849": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "platelet-derived growth factor (PDGFR)-beta", "entity2": "sorafenib", "span1": [218, 261], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10892": {"label": 1, "data": {"text": "Structural analysis revealed that these three roscovitines bind similarly in the pyridoxal-binding site of PDXK rather than in the anticipated ATP-binding site.", "entity1": "PDXK", "entity2": "pyridoxal", "span1": [107, 111], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4073": {"label": 8, "data": {"text": "During early pregnancy in sheep, the elongating conceptus secretes interferon-\u03c4 (IFNT) and the conceptus as well as endometrial epithelia produce prostaglandins (PG) via PG synthase 2 (PTGS2) and cortisol via hydroxysteroid (11-\u03b2) dehydrogenase 1 (HSD11B1).", "entity1": "PTGS2", "entity2": "prostaglandins", "span1": [185, 190], "span2": [146, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3439": {"label": 2, "data": {"text": "These results showed that WNT6 and Cav1 are upregulated by chemotherapeutics and enhance the resistance of GC cells to anthracycline drugs.", "entity1": "Cav1", "entity2": "anthracycline", "span1": [35, 39], "span2": [119, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12104": {"label": 3, "data": {"text": "HERG/IKr channels are a prime target for the pharmacological management of arrhythmias and are selectively blocked by class III antiarrhythmic methanesulfonanilide drugs, such as dofetilide, E4031, and MK-499, at submicromolar concentrations.", "entity1": "IKr", "entity2": "E4031", "span1": [5, 8], "span2": [191, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9761": {"label": 5, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "hD(2)", "entity2": "yohimbine", "span1": [119, 124], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4824": {"label": 3, "data": {"text": "We previously employed a chemical genomic strategy to identify a novel small molecule, MAC13243, as a likely inhibitor of the bacterial lipoprotein targeting chaperone, LolA.", "entity1": "LolA", "entity2": "MAC13243", "span1": [169, 173], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3757": {"label": 2, "data": {"text": "The results demonstrated that \u03b2-ionone-induced apoptosis in a dose-dependent manner in SGC-7901 cells treated with \u03b2-ionone (25, 50, 100 and 200\u00a0\u03bcmol/L) for 24\u00a0h. \u03b2-ionone was also shown to induce the expression of cleaved-caspase-3 and inhibit bcl-2 expression in SGC-7901 cells in a dose-dependent manner.", "entity1": "caspase-3", "entity2": "\u03b2-ionone", "span1": [223, 232], "span2": [163, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6687": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "Ca(2+)-permeable channel", "entity2": "eucalyptol", "span1": [18, 42], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1060": {"label": 8, "data": {"text": "Humans with FSH beta gene mutations tend to have a more severe phenotype than those with FSHR gene mutations, although infertility and varying degrees of impaired sex steroid production occur in both types of mutations.", "entity1": "FSH beta", "entity2": "steroid", "span1": [12, 20], "span2": [167, 174]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"11877": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [150, 156], "span2": [97, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5159": {"label": 8, "data": {"text": "The intrinsic clearance for both ketamine enantiomers by the high affinity enzyme in HLMs with CYP2B6*1/*1 genotype were at least 2-fold and 6-fold higher, respectively, than those for CYP2B6*1/*6 genotype and CYP2B6*6/*6 genotype.", "entity1": "CYP2B6*1", "entity2": "ketamine", "span1": [95, 103], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1674": {"label": 2, "data": {"text": "In alpha2B-receptor-expressing HEK293 cells, etomidate rapidly increased phosphorylation of the extracellular signal-related kinases ERK1/2.", "entity1": "extracellular signal-related kinases", "entity2": "etomidate", "span1": [96, 132], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6426": {"label": 2, "data": {"text": "Hepatocytes isolated from Sch B pretreated (a daily dose of 1 mmol/kg for 3 days) rats showed a significant increase (25%) in DTD activity.", "entity1": "DTD", "entity2": "Sch B", "span1": [126, 129], "span2": [26, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12272": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1c)", "entity2": "vasopressin", "span1": [221, 226], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12575": {"label": 0, "data": {"text": "This cDNA clone, designated EAA3a, shares a 90% nucleotide identity with the previously reported rat GluR5-2b cDNA splice variant and differed from human GluR5-1d in the amino and carboxy terminal regions.", "entity1": "EAA3a", "entity2": "nucleotide", "span1": [28, 33], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7510": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMPK", "entity2": "AICAR", "span1": [54, 58], "span2": [176, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11124": {"label": 9, "data": {"text": "Prazosin was found to be unselective; 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101), 5-methyl-urapidil, indoramin and (+)-niguldipine were confirmed as selective for the alpha 1A-adrenoceptor, whereas spiperone was weakly alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptor", "entity2": "Prazosin", "span1": [192, 213], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10075": {"label": 1, "data": {"text": "These results indicate that salicylates bind specifically to the polypeptide binding site of BiP in human cells that may interfere with folding and transport of proteins important in inflammation.", "entity1": "BiP", "entity2": "salicylates", "span1": [93, 96], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8801": {"label": 2, "data": {"text": "Although fisetin greatly increases the stability of both Nrf2 and ATF4, only the effect on ATF4 is dependent on protein kinase activity.", "entity1": "Nrf2", "entity2": "fisetin", "span1": [57, 61], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2534": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "human b5R", "entity2": "2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine", "span1": [297, 306], "span2": [158, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14837": {"label": 1, "data": {"text": "The results from monitoring enzyme catalysis in the absence of magnesium suggests that the ALDH1-NADH complex with the shorter fluorescence lifetime is the form initially produced, and the complex with the longer fluorescence lifetime is produced through isomerization.", "entity1": "ALDH1", "entity2": "NADH", "span1": [91, 96], "span2": [97, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"14169": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "COX", "entity2": "chalcones", "span1": [83, 86], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8770": {"label": 1, "data": {"text": "Furthermore, expression of a multivalent but not a monovalent GAG containing syndecan-1 proteoglycan recapitulates the elongation phenotype observed with the bivalent xylosides.", "entity1": "syndecan-1", "entity2": "xylosides", "span1": [77, 87], "span2": [167, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12007": {"label": 2, "data": {"text": "The results showed that administration of AlCl3 resulted in a significant elevation in the levels of AchE activity, CRP, NF-\u03baB, and MCP-1 accompanied with a significant depletion in the Ach level.", "entity1": "NF-\u03baB", "entity2": "AlCl3", "span1": [121, 126], "span2": [42, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4671": {"label": 8, "data": {"text": "To determine whether dysregulation of SIRT1 promotes NADPH oxidase-dependent production of reactive oxygen species (ROS) and impairs endothelial function we assessed the effects of three structurally different inhibitors of SIRT1 (nicotinamide, sirtinol, EX527) in aorta segments isolated from young Wistar rats.", "entity1": "NADPH oxidase", "entity2": "oxygen", "span1": [53, 66], "span2": [100, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14131": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "TGF-\u03b21", "entity2": "Celastrol", "span1": [112, 118], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10788": {"label": 2, "data": {"text": "Simvastatin induces interleukin-18 production in human peripheral blood mononuclear cells.", "entity1": "interleukin-18", "entity2": "Simvastatin", "span1": [20, 34], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7640": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate", "span1": [34, 39], "span2": [172, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15188": {"label": 3, "data": {"text": "While sophocarpine treatment resulted in: significant improvement of steatosis (>50% decrease), decrease of leptin expression (<0.57-fold) and increase of adiponectin expression (>1.48-fold).", "entity1": "leptin", "entity2": "sophocarpine", "span1": [108, 114], "span2": [6, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2667": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE7", "entity2": "BRL-50481", "span1": [300, 304], "span2": [306, 315]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7953": {"label": 2, "data": {"text": "However, mutating putative GR binding sites did not substantially reduce induction of ras-dva promoter activity by corticosterone, suggesting additional DNA elements within the 5'-flanking region are responsible for glucocorticoid regulation.", "entity1": "GR binding sites", "entity2": "corticosterone", "span1": [27, 43], "span2": [115, 129]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1022": {"label": 1, "data": {"text": "Peptidergic neurones accumulate amines via an unusual uptake process, designated Transport-P. [(3)H]-prazosin binds to alpha(1) adrenoceptors on these cells and is displaceable by unlabelled prazosin in concentrations up to 10(-7) M. However, at greater concentrations of prazosin, there is a paradoxical accumulation of [(3)H]-prazosin which we have attributed to Transport-P. Uptake of prazosin via Transport-P is detectable at 10(-10) M prazosin concentration, is linear up to 10(-7) M and at greater concentrations becomes non-linear.", "entity1": "alpha(1) adrenoceptors", "entity2": "prazosin", "span1": [119, 141], "span2": [191, 199]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3191": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "p-hydroxybenzoic acid", "span1": [286, 296], "span2": [64, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"559": {"label": 5, "data": {"text": "Both the 5 alpha-reductase inhibitor finasteride and alpha 1-adrenoceptor antagonists (e.g. alfuzosin, doxazosin, prazosin, tamsulosin and terazosin) have been recommended as appropriate treatment options for patients with lower urinary tract symptoms (LUTS) associated with benign prostatic obstruction (BPO), and their efficacy has been proven in several placebo-controlled trials.", "entity1": "alpha 1-adrenoceptor", "entity2": "tamsulosin", "span1": [53, 73], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7104": {"label": 8, "data": {"text": "To further investigate the molecular basis of POX-induced apoptosis, we utilized the DLD-1.POX cells to show that cells overproducing POX exhibit an L-proline-dependent apoptotic response.", "entity1": "POX", "entity2": "L-proline", "span1": [134, 137], "span2": [149, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12180": {"label": 3, "data": {"text": "Hepatic mRNA expressions of apo B-100 and apo C-III were significantly lower in probucol group than in other groups.", "entity1": "apo B-100", "entity2": "probucol", "span1": [28, 37], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12316": {"label": 8, "data": {"text": "Although acetylcholinesterase (AChE) is primarily a hydrolytic enzyme, metabolising the neurotransmitter acetylcholine in cholinergic synapses, it also has some non-catalytic functions in the brain which are far less well characterised.", "entity1": "AChE", "entity2": "acetylcholine", "span1": [31, 35], "span2": [105, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15480": {"label": 3, "data": {"text": "Glutathione-S-transferase, a phase II enzyme, was inhibited by both arsenic and nicotine but no such inhibition was noted in arsenic-treated animals pre-exposed to nicotine.", "entity1": "Glutathione-S-transferase", "entity2": "arsenic", "span1": [0, 25], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4786": {"label": 3, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP2D", "entity2": "baicalin", "span1": [138, 143], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8475": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "HTRA1", "entity2": "Ala", "span1": [71, 76], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10523": {"label": 1, "data": {"text": "Metformin, but not leptin, regulates AMP-activated protein kinase in pancreatic islets: impact on glucose-stimulated insulin secretion.", "entity1": "AMP-activated protein kinase", "entity2": "Metformin", "span1": [37, 65], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11217": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "tolbutamide", "span1": [4, 11], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1782": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1dAR", "entity2": "Tamsulosin", "span1": [54, 63], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8808": {"label": 0, "data": {"text": "Activation of AMPK using AICAR resulted in STIM1 phosphorylation on serine residues and prevented PAR-1-induced Ca2+ entry.", "entity1": "STIM1", "entity2": "serine", "span1": [43, 48], "span2": [68, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11097": {"label": 1, "data": {"text": "The effects of these metabolites on the expression of uteroglobin (UG) and progesterone receptor (PR) genes, both regulated by progesterone (P4), were evaluated in the uterus of prepubertal female rabbits that were simultaneously treated with P4 (1.0 mg) for 5 consecutive days.", "entity1": "progesterone receptor", "entity2": "progesterone (P4)", "span1": [75, 96], "span2": [127, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4504": {"label": 3, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES1", "entity2": "ibuprofen-\u03b2-d-glucuronide", "span1": [169, 174], "span2": [57, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1426": {"label": 2, "data": {"text": "Culture of HepG2 cells with griseofulvin has now been shown to induce both the formation of intracellular aggregates containing K18 as well as an increase in the abundance of K18 mRNA.", "entity1": "K18", "entity2": "griseofulvin", "span1": [128, 131], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15115": {"label": 2, "data": {"text": "These findings are the first to show that long-term exposure to Mn during a critical period of neurodevelopment causes motor coordination dysfunction with parallel increment in oxidative stress markers, p38(MAPK) phosphorylation and caspase activity in the striatum.", "entity1": "MAPK", "entity2": "Mn", "span1": [207, 211], "span2": [64, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3834": {"label": 3, "data": {"text": "Taken together, the data provide evidence that the synergistic antiproliferative effect of resveratrol and clofarabine is linked to the inhibition of Akt and Sp1 activities, and suggest that this combination may have therapeutic value in treatment of malignant mesothelioma.", "entity1": "Akt", "entity2": "resveratrol", "span1": [150, 153], "span2": [91, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2843": {"label": 7, "data": {"text": "The enzyme requires PLP and divalent cations such as Ca(2+), Mg(2+), or Mn(2+), but not ATP, whereas mammalian serine racemase activity is increased by ATP.", "entity1": "serine racemase", "entity2": "Mn(2+)", "span1": [111, 126], "span2": [72, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15403": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "NPC1L1", "entity2": "7-ketosterols", "span1": [202, 208], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"9671": {"label": 2, "data": {"text": "Inhibition of LTC4 synthesis precedes the global cytotoxic effects of FP as indicated by the simultaneous upregulation of annexin-1 expression.", "entity1": "annexin-1", "entity2": "FP", "span1": [122, 131], "span2": [70, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3264": {"label": 8, "data": {"text": "Gastrointestinal adenocarcinomas and squamous cell uterine carcinomas were often accompanied by high TS expression, indicating activation of pyrimidine synthesis through both the salvage and de novo pathways.", "entity1": "TS", "entity2": "pyrimidine", "span1": [101, 103], "span2": [141, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"832": {"label": 4, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "EP1", "entity2": "17-phenyl-trinor-PGE2", "span1": [92, 95], "span2": [66, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8873": {"label": 9, "data": {"text": "IGFBP-4 was not induced by TCDD in the parental cell line of 5L cells, Fao, and in various closely related rat hepatoma cell lines as well as in other unrelated cell types.", "entity1": "IGFBP-4", "entity2": "TCDD", "span1": [0, 7], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1045": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "doxorubicin", "span1": [110, 114], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10795": {"label": 3, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "CD40", "entity2": "simvastatin", "span1": [78, 82], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2020": {"label": 5, "data": {"text": "Pranlukast, a leukotriene receptor antagonist, inhibits interleukin-5 production via a mechanism distinct from leukotriene receptor antagonism.", "entity1": "leukotriene receptor", "entity2": "Pranlukast", "span1": [14, 34], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12629": {"label": 1, "data": {"text": "The EP1 receptor bound 17-phenyl-PGE2, sulprostone and iloprost in addition to PGE2 and PGE1, with Ki values of 14-36 nM.", "entity1": "EP1", "entity2": "PGE1", "span1": [4, 7], "span2": [88, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4874": {"label": 3, "data": {"text": "In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAF(V600E) inhibitors.", "entity1": "V600E", "entity2": "N-(thiophen-2-yl) benzamide", "span1": [147, 152], "span2": [92, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11117": {"label": 2, "data": {"text": "DEX enhanced the ratio IFN-gamma/IL-4 (mean +/- SEM: control, 28.7 +/- 17.6; with 10-7 M DEX, 55.0 +/- 27.5, P<0.005).", "entity1": "IL-4", "entity2": "DEX", "span1": [33, 37], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13164": {"label": 9, "data": {"text": "Progestin activation of Src/MAPK occurred outside the nucleus with the B isoform of PR that was distributed between the cytoplasm and nucleus, but not with PR-A that was predominantly nuclear.", "entity1": "PR-A", "entity2": "Progestin", "span1": [156, 160], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9948": {"label": 3, "data": {"text": "Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta.", "entity1": "NF-kappaB", "entity2": "sulfasalazine", "span1": [15, 24], "span2": [37, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12585": {"label": 1, "data": {"text": "Coexpression of the flip and flop splice variants of GluR-A, in the absence of GluR-B, revealed that heteromeric AMPA receptors with intermediate sensitivity to cyclothiazide, similar to responses observed for the combinations GluR-AoBi or GluR-AiBo, could be generated independently of the presence of the GluR-B subunit.", "entity1": "GluR-AoBi", "entity2": "cyclothiazide", "span1": [227, 236], "span2": [161, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7118": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "PDE5Delta1-321", "entity2": "N", "span1": [143, 157], "span2": [97, 98]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16011": {"label": 1, "data": {"text": "Chronic exposure to oxyfluorfen provoked then structural changes but also functional changes in the capacity of biofilm CAT activity to respond to a sudden increase in concentration, suggesting a selection of species with higher antioxidant capacity.", "entity1": "CAT", "entity2": "oxyfluorfen", "span1": [120, 123], "span2": [20, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12773": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "LV", "span1": [0, 20], "span2": [108, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4004": {"label": 8, "data": {"text": "In vitro accumulation studies conducted in Madin-Darby canine kidney II cells indicate that dabrafenib is an avid substrate for both P-gp and BCRP.", "entity1": "P-gp", "entity2": "dabrafenib", "span1": [133, 137], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"730": {"label": 9, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "AT1A", "entity2": "cilazapril", "span1": [183, 187], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6350": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "E3174", "span1": [18, 21], "span2": [152, 157]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5188": {"label": 2, "data": {"text": "Treatment of A549 and H1299 cells with dioscin caused a dose-dependent increase in ERK1/2 and JNK1/2 activity, accompanied with a decreased PI3K expression and decreased phosphorylation of Akt and mTOR.", "entity1": "JNK1/2", "entity2": "dioscin", "span1": [94, 100], "span2": [39, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15448": {"label": 8, "data": {"text": "Currently, the most important insecticides are neonicotinoids, which are metabolized in vitro by AOX on reduction of the nitroimino group and by CYPs via oxidation reactions.", "entity1": "CYPs", "entity2": "neonicotinoids", "span1": [145, 149], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12632": {"label": 3, "data": {"text": "Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride.", "entity1": "HERG human cardiac K+ channel", "entity2": "cisapride", "span1": [16, 45], "span2": [87, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8735": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A3", "entity2": "diphenhydramine", "span1": [189, 195], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13226": {"label": 1, "data": {"text": "Furthermore, MG132 prevented glutamate-stimulated reduction in surface amount of GluR2, and knockdown of GRIP1 by RNAi against GRIP1 reduced surface GluR2 in neurons.", "entity1": "GluR2", "entity2": "MG132", "span1": [81, 86], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1036": {"label": 1, "data": {"text": "Pranlukast is a new, orally active, selective inhibitor of CysLt1 leukotrieneleukotriene receptor.", "entity1": "leukotriene receptor", "entity2": "leukotriene", "span1": [77, 97], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"213": {"label": 5, "data": {"text": "Alprenolol and bromoacetylalprenololmenthane are competitive slowly reversible antagonists at the beta 1-adrenoceptors of rat left atria.", "entity1": "beta 1-adrenoceptors", "entity2": "bromoacetylalprenololmenthane", "span1": [98, 118], "span2": [15, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14142": {"label": 1, "data": {"text": "Mianserin and mirtazapine increased ERK1/2 phosphorylation in CHO cells expressing kappa-opioid receptors and C6 cells, and these effects were antagonized by nor-BNI.", "entity1": "kappa-opioid receptors", "entity2": "Mianserin", "span1": [83, 105], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5822": {"label": 3, "data": {"text": "After the combined pituitary stimulation test (100 micrograms human CRH, 100 micrograms GnRH, 100 micrograms GH-releasing hormone, and 200 micrograms TRH), the ACTH peak (maximum increase at 30 min) was significantly blunted by loperamide from 9 +/- 1 to 4 +/- 1 pmol/L (P less than 0.001) and the area under the curve of ACTH from 0-120 min was reduced from 35 +/- 5 to 23 +/- 4 pmol/L.2 h (P less than 0.05).", "entity1": "TRH", "entity2": "loperamide", "span1": [150, 153], "span2": [228, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6106": {"label": 8, "data": {"text": "These events are stimulated by NE and by guanethidine, an hNET substrate, and they are blocked by cocaine and the antidepressant desipramine.", "entity1": "hNET", "entity2": "guanethidine", "span1": [58, 62], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10118": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "COX-2", "entity2": "nimesulide", "span1": [180, 185], "span2": [222, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11213": {"label": 1, "data": {"text": "By theoretical calculations we have determined most probable structure of amiloride/uPAs complexes.", "entity1": "uPAs", "entity2": "amiloride", "span1": [84, 88], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4853": {"label": 3, "data": {"text": "Here we found that the anticancer agent cucurbitacin I, a Jak2 inhibitor, reduced the activation of Rac1 and motility in response to the ErbB3 ligand heregulin in breast cancer cells.", "entity1": "Rac1", "entity2": "cucurbitacin I", "span1": [100, 104], "span2": [40, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7589": {"label": 1, "data": {"text": "Interaction with the hERG channel and cytotoxicity of amiodarone and amiodarone analogues.", "entity1": "hERG", "entity2": "amiodarone", "span1": [21, 25], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3516": {"label": 3, "data": {"text": "TZDs also inhibited alkaline phosphatase activity (58-75%, p<0.046) and osteocalcin production (52-75%, p<0.031).", "entity1": "alkaline phosphatase", "entity2": "TZDs", "span1": [20, 40], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6659": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "COX-2", "entity2": "acetaminophen", "span1": [80, 85], "span2": [178, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11850": {"label": 2, "data": {"text": "Furthermore, the up-regulation of IL-12 and TNF-\u03b1 was found in the procyanidin trimers-treated cells in the presence of OVA.", "entity1": "TNF-\u03b1", "entity2": "procyanidin", "span1": [44, 49], "span2": [67, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8005": {"label": 3, "data": {"text": "In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-\u03b1-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.", "entity1": "PAI-1", "entity2": "IMG", "span1": [101, 106], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1564": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "GTK", "entity2": "glutamine", "span1": [176, 179], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"10015": {"label": 5, "data": {"text": "Other 5-HT3 receptor antagonists also produced such a shift in the following antagonistic-potency order: granisetron> ondansetron=AS-8112>>metoclopramide.", "entity1": "5-HT3 receptor", "entity2": "AS-8112", "span1": [6, 20], "span2": [130, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11196": {"label": 1, "data": {"text": "To further confirm this hypothesis, we investigated the effects of dietary treatment with BH(4) on endothelium-dependent arterial relaxation and vascular oxidative stress in the aortas of insulin-resistant rats.", "entity1": "insulin", "entity2": "BH(4)", "span1": [188, 195], "span2": [90, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11090": {"label": 1, "data": {"text": "Lorglumide is therefore a useful pharmacological tool to study the functions of CCK.", "entity1": "CCK", "entity2": "Lorglumide", "span1": [80, 83], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10333": {"label": 4, "data": {"text": "The immune response modifiers, imiquimod and resiquimod, are TLR7 agonists that induce type I interferon in numerous species, including humans.", "entity1": "TLR7", "entity2": "resiquimod", "span1": [61, 65], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5966": {"label": 4, "data": {"text": "These data suggested that ambenonium had a dual effect on tissue responses to acetylcholine-producing potentiation by blockade of acetylcholinesterase and concomitant antagonism by blockade of muscarinic receptors.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [130, 150], "span2": [78, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10755": {"label": 1, "data": {"text": "An in vitro kinase assay showed that imatinib did not directly affect EGFR kinase activity, suggesting involvement of EGFR-activating molecules.", "entity1": "kinase", "entity2": "imatinib", "span1": [75, 81], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11224": {"label": 1, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "Kir6.2", "entity2": "sulfonylureas", "span1": [97, 103], "span2": [44, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15901": {"label": 1, "data": {"text": "Here, we report that synaptotagmin-1 is necessary for expression of the vesicular Ca(2+) /H(+) -antiport.", "entity1": "synaptotagmin-1", "entity2": "H(+)", "span1": [21, 36], "span2": [90, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12848": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "VEGFR-3", "entity2": "sorafenib", "span1": [209, 216], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9669": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "human recombinant interleukin-5", "entity2": "CB", "span1": [132, 163], "span2": [236, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15972": {"label": 1, "data": {"text": "Together, the information on both hCCS and hSOD1, along with a sequence analysis of eukaryotic CCSD1, allows us to propose important mechanistic aspects regarding the copper-transfer process from hCCS to hSOD1.", "entity1": "hSOD1", "entity2": "copper", "span1": [204, 209], "span2": [167, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13389": {"label": 8, "data": {"text": "In humans, methionine synthase deficiency results in the accumulation of methyltetrahydrofolate at the expense of folate derivatives required for purine and thymidylate biosynthesis.", "entity1": "methionine synthase", "entity2": "methyltetrahydrofolate", "span1": [11, 30], "span2": [73, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10085": {"label": 1, "data": {"text": "Celecoxib selectively suppressed PGE2 but not TxB2 at time points consistent with COX-2 activity, while producing analgesia.", "entity1": "COX-2", "entity2": "TxB2", "span1": [82, 87], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"4451": {"label": 3, "data": {"text": "Guided by the acetylcholinesterase inhibiting activity, the bisindole alkaloid 3'-R/S-hydroxyvoacamine was isolated from a stem extract of Tabernaemontana divaricata, a plant used in Thailand in traditional rejuvenation remedies for improving the memory.", "entity1": "acetylcholinesterase", "entity2": "bisindole alkaloid", "span1": [14, 34], "span2": [60, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7170": {"label": 5, "data": {"text": "However, the expression of AT1R was not suppressed by other AT1R antagonists such as candesartan or olmesartan.", "entity1": "AT1R", "entity2": "olmesartan", "span1": [60, 64], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4110": {"label": 3, "data": {"text": "\u03b2-Amyloid aggregation results showed that all compounds exhibited remarkable A\u03b2 fibril aggregation inhibition activity with a nearly similar potential as the reference compound rifampicin, which makes them promising anti-Alzheimer drug candidates.", "entity1": "A\u03b2", "entity2": "rifampicin", "span1": [77, 79], "span2": [177, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13416": {"label": 9, "data": {"text": "Similarly, the PSS1 enzyme level did not change after ethanol exposure but PSS2 could not be probed with the antibody available currently.", "entity1": "PSS1", "entity2": "ethanol", "span1": [15, 19], "span2": [54, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3237": {"label": 1, "data": {"text": "A comparative autoradiography study of the relationship between the binding pattern of SERT in autoshaping new untrained vs. trained treated (METH, FLX, or both) animals was made.", "entity1": "SERT", "entity2": "METH", "span1": [87, 91], "span2": [142, 146]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15490": {"label": 0, "data": {"text": "We used whole-cell recordings of human embryonic kidney cells heterologously expressing either wild-type TRPA1 or TRPA1 with three serine-substituted cysteines crucial for electrophile activation (C621S, C641S, C665S).", "entity1": "C641S", "entity2": "serine", "span1": [204, 209], "span2": [131, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6496": {"label": 5, "data": {"text": "The following alpha(2)-adrenoceptor antagonists were applied: BRL44408 (alpha(2A)-selective), ARC239 (alpha(2B)- and alpha(2C)-selective), and prazosin (alpha(2B)- and alpha(2C)-selective).", "entity1": "alpha(2B)", "entity2": "ARC239", "span1": [102, 111], "span2": [94, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"610": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "IL-2", "entity2": "BPB", "span1": [193, 197], "span2": [121, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10399": {"label": 0, "data": {"text": "Unlike OFQ II(1-17), high concentrations of its C-terminal extension, OFQ II(1-28), stimulated [35S]-GTPgammaS binding in a mu (mu) opioid receptor-like distribution and the effect was blocked by naloxone.", "entity1": "OFQ II(1-28)", "entity2": "C", "span1": [70, 82], "span2": [48, 49]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13521": {"label": 1, "data": {"text": "The active site coordination of CDO comprises a mononuclear iron ligated by the Nepsilon atoms of three protein-derived histidines, thus representing a new variant on the 2-histidine-1-carboxylate (2H1C) facial triad motif.", "entity1": "CDO", "entity2": "iron", "span1": [32, 35], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8580": {"label": 3, "data": {"text": "These data show that the ATO is a promising new approach to decrease glioblastoma proliferation and recurrence by downregulation of Notch pathway.", "entity1": "Notch", "entity2": "ATO", "span1": [132, 137], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14568": {"label": 2, "data": {"text": "GnRH caused a sustained increase in nuclear \u03b2-catenin levels, which was significantly reduced by c-Jun N-terminal kinase (JNK) inhibition.", "entity1": "\u03b2-catenin", "entity2": "GnRH", "span1": [44, 53], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9650": {"label": 5, "data": {"text": "Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor.", "entity1": "androgen receptor", "entity2": "EMP", "span1": [98, 115], "span2": [56, 59]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5131": {"label": 3, "data": {"text": "In addition, 5HHMF blocked LPS-induced phosphorylation of I\u03baB, resulting in suppression of the nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) subunits, namely p65 and p50, which are important molecules involved in the regulation of iNOS expression.", "entity1": "I\u03baB", "entity2": "5HHMF", "span1": [58, 61], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14225": {"label": 4, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b1", "entity2": "4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol", "span1": [132, 135], "span2": [149, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12111": {"label": 3, "data": {"text": "HERG/IKr channels are a prime target for the pharmacological management of arrhythmias and are selectively blocked by class III antiarrhythmic methanesulfonanilide drugs, such as dofetilide, E4031, and MK-499, at submicromolar concentrations.", "entity1": "HERG", "entity2": "dofetilide", "span1": [0, 4], "span2": [179, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"877": {"label": 1, "data": {"text": "In addition, by comparing the combined administration of (+/-)pindolol with either WAY100635, GR127935 or isamoltane, we have determined that (+/-)pindolol produces much of its acute potentiation of fluoxetine-induced increases in extracellular 5-HT via its action at the 5-HT(1B/D) receptor in addition to any activity it has at the presynaptic 5-HT(1A) receptor.", "entity1": "5-HT(1A)", "entity2": "fluoxetine", "span1": [346, 354], "span2": [199, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"773": {"label": 3, "data": {"text": "Flecainide block of Na(+) current (I(Na)) was investigated in wild-type (WT) or the long QT syndrome 3 (LQT3) sodium channel alpha subunit mutation with three amino acids deleted (DeltaKPQ) stably transfected into human embryonic kidney 293 cells using whole-cell, patch-clamp recordings.", "entity1": "DeltaKPQ", "entity2": "Flecainide", "span1": [180, 188], "span2": [0, 10]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14079": {"label": 3, "data": {"text": "In TGF-\u03b21-induced NPDFs, berberine significantly inhibited the expression of \u03b1-SMA and collagen type I mRNA and reduced \u03b1-SMA and collagen protein levels.", "entity1": "\u03b1-SMA", "entity2": "berberine", "span1": [77, 82], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16048": {"label": 1, "data": {"text": "By contrast, the editing of some sites is completely lost or significantly reduced in other non-green tissues; for instance, the editing of ndhB-149, ndhB-1255, and ndhD-2 is completely lost in roots and in lincomycin-treated seedlings.", "entity1": "ndhB-149", "entity2": "lincomycin", "span1": [140, 148], "span2": [207, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14892": {"label": 1, "data": {"text": "FMO3 expression is induced by dietary bile acids by a mechanism that involves the farnesoid X receptor (FXR), a bile acid-activated nuclear receptor.", "entity1": "FXR", "entity2": "bile acids", "span1": [104, 107], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6033": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "8-hydroxy-2-(di-n-propylamino) tetralin", "span1": [73, 79], "span2": [235, 274]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1983": {"label": 3, "data": {"text": "Mibefradil blocked Nav1.5 in a use/frequency-dependent manner, indicating preferential binding to states visited during depolarization.", "entity1": "Nav1.5", "entity2": "Mibefradil", "span1": [19, 25], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5494": {"label": 3, "data": {"text": "3) The inhibitory effects of the thioureylene drugs, methimazole and carbimazole, on the iodide-dependent catalatic activity were very similar to those reported previously for thyroid peroxidase-catalyzed iodination.", "entity1": "thyroid peroxidase", "entity2": "methimazole", "span1": [176, 194], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"813": {"label": 1, "data": {"text": "The prostaglandin E series modulates high-voltage-activated calcium channels probably through the EP3 receptor in rat paratracheal ganglia.", "entity1": "high-voltage-activated calcium channels", "entity2": "prostaglandin E", "span1": [37, 76], "span2": [4, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2376": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "ERK", "entity2": "Nexavar", "span1": [79, 82], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12722": {"label": 1, "data": {"text": "In human plasma the BrBK half-life values in the absence or in the presence of GW660511X (3.8 microM) or omapatrilat (32 nM) were 38.7 +/- 2.4, 51.2 +/- 4.7 and 114.7 +/- 9.3 min, respectively and BrBK was degraded into BrBK1-8, BrBK1-7, BrBK1-5 and Br-Phe.", "entity1": "BrBK", "entity2": "omapatrilat", "span1": [20, 24], "span2": [105, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12634": {"label": 3, "data": {"text": "We tested the hypothesis that cisapride blocks HERG.", "entity1": "HERG", "entity2": "cisapride", "span1": [47, 51], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1312": {"label": 8, "data": {"text": "Dopamine D(2) receptor-induced COX-2-mediated production of prostaglandin E(2) in D(2)-transfected Chinese hamster ovary cells without simultaneous administration of a Ca(2+)-mobilizing agent.", "entity1": "COX-2", "entity2": "prostaglandin E(2)", "span1": [31, 36], "span2": [60, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13113": {"label": 8, "data": {"text": "We propose a model whereby compartmentalized PDEs, rather than representing an enzymatic barrier to cAMP diffusion, act as a sink to drain the second messenger from discrete locations, resulting in multiple and simultaneous domains with different cAMP concentrations irrespective of their distance from the site of cAMP synthesis.", "entity1": "PDEs", "entity2": "cAMP", "span1": [45, 49], "span2": [315, 319]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8310": {"label": 2, "data": {"text": "Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).", "entity1": "POMC", "entity2": "acylethanolamide", "span1": [119, 123], "span2": [6, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14063": {"label": 3, "data": {"text": "Aspirin induced autophagy, a feature of mTOR inhibition.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [40, 44], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2568": {"label": 3, "data": {"text": "Results showed that neonatal quinpirole treatment induced D2 priming that was eliminated by olanzapine treatment.", "entity1": "D2", "entity2": "olanzapine", "span1": [58, 60], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12166": {"label": 8, "data": {"text": "Of these two enzymes, cystathionine-gamma-lyase (CSE) is believed to be the key enzyme that forms H2S in the cardiovascular system.", "entity1": "cystathionine-gamma-lyase", "entity2": "H2S", "span1": [22, 47], "span2": [98, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"517": {"label": 4, "data": {"text": "Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine.", "entity1": "5HT1B/1D", "entity2": "311C90", "span1": [104, 112], "span2": [59, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13883": {"label": 3, "data": {"text": "A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons.", "entity1": "RhoA", "entity2": "ibuprofen", "span1": [45, 49], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5258": {"label": 3, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "cyclinB1", "entity2": "rofecoxib", "span1": [131, 139], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12766": {"label": 1, "data": {"text": "Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography.", "entity1": "histamine H1-receptor", "entity2": "cetirizine", "span1": [121, 142], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1005": {"label": 1, "data": {"text": "CONCLUSION: 5-HT(4) receptors are involved in the regulation of cisapride stimulated orocaecal transit; SB 207266 tends to modulate colonic transit but not sensory functions or compliance in healthy human subjects.", "entity1": "5-HT(4)", "entity2": "cisapride", "span1": [12, 19], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6984": {"label": 9, "data": {"text": "Although chronic valproic acid produces similar effects on brain arachidonic acid and docosahexaenoic acid turnover, it does not alter phospholipase A(2) activity, suggesting that it targets a different enzyme in the turnover pathway.", "entity1": "phospholipase A(2)", "entity2": "valproic acid", "span1": [135, 153], "span2": [17, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"6390": {"label": 4, "data": {"text": "In alpha(2A)-adrenoceptor transfected cells the rank order of agonist potency was A-54741 (mean pEC(50)=8.96)>dexmedetomidine (8.88)>UK-14304 (8.42)>B-HT 920 (7.05)>noradrenaline (6.92).", "entity1": "alpha(2A)-adrenoceptor", "entity2": "A-54741", "span1": [3, 25], "span2": [82, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6565": {"label": 3, "data": {"text": "We changed the residues to alanine using site-directed mutagenesis technique, expressed the mutants in a baculovirus/Sf9 cell system, and analyzed the kinetic characteristics of inhibition of the mutant enzymes by milrinone and cilostazol, specific inhibitors of PDE3.", "entity1": "PDE3", "entity2": "milrinone", "span1": [263, 267], "span2": [214, 223]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1527": {"label": 0, "data": {"text": "Their deduced amino acid sequences show a high degree of conservation compared with orthologues from other mammalian species, with the notable exception of the N-terminus of ovine M-CPT 1.", "entity1": "ovine M-CPT 1", "entity2": "N", "span1": [174, 187], "span2": [160, 161]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11245": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "DAT", "entity2": "4',7,8-trichloro", "span1": [108, 111], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13591": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "methylphenidate", "span1": [6, 10], "span2": [256, 271]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4541": {"label": 3, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "CYP2D6", "entity2": "harmaline", "span1": [80, 86], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3209": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "ferulic acid", "span1": [286, 296], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2129": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "MCTs", "entity2": "pyruvate", "span1": [30, 34], "span2": [135, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9551": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "IL-3", "entity2": "cAMP", "span1": [70, 74], "span2": [204, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4393": {"label": 3, "data": {"text": "Second, ICRF-187, a Top2 catalytic inhibitor known to deplete Top2\u03b2, specifically sensitized MEFs to CPT.", "entity1": "Top2\u03b2", "entity2": "ICRF-187", "span1": [62, 67], "span2": [8, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1678": {"label": 5, "data": {"text": "Inhibition of binding of the alpha2-receptor antagonist [3H]RX821002 to recombinant alpha2-receptors by etomidate was tested in human embryonic kidney (HEK293) cells in vitro.", "entity1": "alpha2-receptor", "entity2": "[3H]RX821002", "span1": [29, 44], "span2": [56, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9142": {"label": 1, "data": {"text": "The profile of a series of adenosine analogs or of xanthine antagonists can be used to define the nature of adenosine receptors.", "entity1": "adenosine receptors", "entity2": "adenosine", "span1": [108, 127], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15199": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "cyclooxygenase-2", "entity2": "buthanol", "span1": [270, 286], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9145": {"label": 1, "data": {"text": "The subregion of the adenosine receptor that interacts with the N6-substituent is different for A1 and A2 receptors, particularly with respect to phenyl interactions, bulk tolerance and stereoselectivity.", "entity1": "adenosine receptor", "entity2": "phenyl", "span1": [21, 39], "span2": [146, 152]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"390": {"label": 1, "data": {"text": "Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A.", "entity1": "CB1", "entity2": "SR 141716A", "span1": [47, 50], "span2": [115, 125]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2519": {"label": 3, "data": {"text": "This suppression was well correlated with the inhibitory effect of auranofin on the homodimerization of TLR4 induced by an agonist.", "entity1": "TLR4", "entity2": "auranofin", "span1": [104, 108], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1512": {"label": 3, "data": {"text": "Many clinical studies, both pre- and post-marketing, have demonstrated the clinical efficacy and safety of sildenafil (Viagra, Pfizer) - the first approved selective PDE inhibitor for the treatment of ED.", "entity1": "PDE", "entity2": "Viagra", "span1": [166, 169], "span2": [119, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13354": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "PR", "entity2": "MPA", "span1": [115, 117], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15202": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "iNOS", "entity2": "buthanol", "span1": [329, 333], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11966": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "PIP5K1B", "entity2": "phosphatidylinositol 4-phosphate", "span1": [0, 7], "span2": [159, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1061": {"label": 1, "data": {"text": "Triacsin C, a competitive inhibitor of both ACS1 and ACS4, inhibited ACS activity similarly in endoplasmic reticulum, MAM, and mitochondria, suggesting that a hitherto unidentified triacsin-sensitive ACS is present in mitochondria.", "entity1": "ACS", "entity2": "triacsin", "span1": [200, 203], "span2": [181, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14701": {"label": 1, "data": {"text": "Promoter replacements conferring constitutive expression of MSH2 revealed that the transcriptional induction in response to MMS is required to maintain induced levels of Msh2.", "entity1": "MSH2", "entity2": "MMS", "span1": [60, 64], "span2": [124, 127]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15616": {"label": 3, "data": {"text": "Galangin decreased expression of pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-\u03b1, interleukin (IL)-6, IL-1\u03b2, and IL-8.", "entity1": "tumor necrosis factor (TNF)-\u03b1", "entity2": "Galangin", "span1": [69, 98], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4132": {"label": 8, "data": {"text": "Absorption and secretion of fluoride increase at acid pH levels, possibly because of its non-ionized state at these pHs and/or because of participation of a F(-)/H(+) cotransporter or a F(-)/OH(-) antiporter.", "entity1": "F(-)/H(+) cotransporter", "entity2": "fluoride", "span1": [157, 180], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"438": {"label": 1, "data": {"text": "Ka values for rauwolscine and WB-4101, drugs distinguishing the alpha-2D from the alpha-2A adrenoceptor subtype, were significantly higher in blocking relaxation of rat arteries compared with pig arteries, suggesting the alpha-2D adrenoceptor subtype mediates NO-induced relaxation in rat arteries.", "entity1": "alpha-2A adrenoceptor", "entity2": "WB-4101", "span1": [82, 103], "span2": [30, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2100": {"label": 4, "data": {"text": "In contrast, the selective beta2AR antagonists ICI-118,551 and butoxamine inhibited isoproterenol-mediated enhancement with apparent low affinities (K(b) of 222 +/- 61 and 9268 +/- 512 nM, respectively).", "entity1": "beta2AR", "entity2": "isoproterenol", "span1": [27, 34], "span2": [84, 97]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2294": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "AH 6809", "span1": [19, 22], "span2": [249, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13190": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "DAT", "entity2": "mZBrENT", "span1": [278, 281], "span2": [150, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10781": {"label": 3, "data": {"text": "Although, imatinib primarily inhibits tyrosine kinases, it also stimulates the activity of EGFR tyrosine kinase in head and neck squamous tumors.", "entity1": "tyrosine kinases", "entity2": "imatinib", "span1": [38, 54], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13733": {"label": 3, "data": {"text": "Homocysteine release increased during 3T3-L1 differentiation and was reduced when adipose tissue was treated with the NNMT inhibitor 1-methylnicotinamide.", "entity1": "NNMT", "entity2": "1-methylnicotinamide", "span1": [118, 122], "span2": [133, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6947": {"label": 3, "data": {"text": "Vitamin E and probucol significantly suppressed an increase in plasma total-cholesterol (total-C) and low-density lipoprotein cholesterol compared to HC-control group.", "entity1": "low-density lipoprotein", "entity2": "Vitamin E", "span1": [102, 125], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5749": {"label": 1, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "c-Rel", "entity2": "vitamin C", "span1": [169, 174], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2057": {"label": 1, "data": {"text": "This alternate conformation now causes a steric hindrance to the O4 hydroxyl group of the Gal moiety of UDP-Gal, probably causing the dissociation of UDP-Gal and the reduced k(cat) of the Gal-T reaction.", "entity1": "Gal-T", "entity2": "UDP-Gal", "span1": [188, 193], "span2": [104, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3845": {"label": 3, "data": {"text": "Mitochondrial glutathione (GSH) reductase activity and the GSH/glutathione disulfide ratio were decreased by TCDD, ultimately leading to mitochondrial dysfunction, characterized by decreased inner mitochondrial membrane potential and ATP production, and increased production of the reactive oxygen species (ROS), hydrogen peroxide.", "entity1": "glutathione (GSH) reductase", "entity2": "TCDD", "span1": [14, 41], "span2": [109, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4154": {"label": 3, "data": {"text": "The IC50 values for Gli1 mRNA inhibition in the tumor and skin by TAK-441 were estimated to be 0.0457 and 0.113 \u03bcg/ml, respectively.", "entity1": "Gli1", "entity2": "TAK-441", "span1": [20, 24], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7988": {"label": 2, "data": {"text": "ISO significantly inhibited the levels of ERK1/2 kinase and increased the expression of JNK and p38 kinases.", "entity1": "JNK", "entity2": "ISO", "span1": [88, 91], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12710": {"label": 1, "data": {"text": "We demonstrated that the coexpressed HG1 and GAB-1 receptors are GABA-responsive, and provide evidence for the possible involvement of GABA receptors in the mechanism of ivermectin resistance.", "entity1": "GAB-1", "entity2": "GABA", "span1": [45, 50], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4992": {"label": 1, "data": {"text": "Cobalt chloride, a typical HIF activator, induced the gene expression of CAR-target genes, including cyp2b9 and cyp2b10, an accumulation of nuclear CAR and an increase in the PB-responsive enhancer module-mediated transactivation in the mouse liver.", "entity1": "PB-responsive enhancer module", "entity2": "Cobalt chloride", "span1": [175, 204], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2506": {"label": 3, "data": {"text": "Anastrozole and letrozole are both non-steroidal aromatase inhibitors that compete with the substrate for binding to the enzyme active site.", "entity1": "aromatase", "entity2": "Anastrozole", "span1": [49, 58], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8729": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT2B10", "entity2": "imipramine", "span1": [61, 68], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8783": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-Akt", "entity2": "CAPE", "span1": [94, 105], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3961": {"label": 2, "data": {"text": "Although Bak and Bcl-2-associated X protein (Bax), another member of the Bcl-2 family, are generally thought to be functionally redundant, only Bak is necessary and sufficient for VK2-induced cytochrome c (cyt c) release and cell death.", "entity1": "cyt c", "entity2": "VK2", "span1": [206, 211], "span2": [180, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8038": {"label": 1, "data": {"text": "Finally, chronic administration of metformin in diabetic mice restored cardiac autophagy by activating JNK1-Bcl-2 pathways and dissociating Beclin1 and Bcl-2.", "entity1": "Bcl-2", "entity2": "metformin", "span1": [152, 157], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2277": {"label": 3, "data": {"text": "In this article, the action of dasatinib (BMS-354825) is contrasted with that of imatinib, a kinase inhibitor that is currently being used to treat chronic myelogenous leukemia and other disorders.", "entity1": "kinase", "entity2": "imatinib", "span1": [93, 99], "span2": [81, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10404": {"label": 1, "data": {"text": "Orphanin FQ (OFQ) stimulated [35S]-GTPgammaS binding in a pattern similar to that described for [125I]-OFQ at the endogenous opioid receptor-like (ORL1) receptor.", "entity1": "OFQ", "entity2": "[35S]-GTPgammaS", "span1": [13, 16], "span2": [29, 44]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9637": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "AR", "entity2": "estramustine", "span1": [66, 68], "span2": [85, 97]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8103": {"label": 2, "data": {"text": "We found that wogonin can suppress the H2O2-stimulated actin remodeling and albumin uptake of HUVECs, as well as transendothelial cell migration of the human breast carcinoma cell MDA-MB-231.", "entity1": "albumin", "entity2": "H2O2", "span1": [76, 83], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9726": {"label": 0, "data": {"text": "To identify key amino acids involved in factor IX activation, recombinant factor XIa proteins containing alanine substitutions for wild-type sequence were expressed in 293 fibroblasts and tested in a plasma clotting assay.", "entity1": "factor XIa", "entity2": "alanine", "span1": [74, 84], "span2": [105, 112]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4857": {"label": 0, "data": {"text": "Unsaturated FFAs increased DAGs, TAGs and PTP1B expression significantly, but cells remained insulin sensitive as assessed by robust AKt and PTP1B phosphorylation at serine (Ser) 50, Ser 398 and tyrosine 152.", "entity1": "PTP1B", "entity2": "tyrosine", "span1": [141, 146], "span2": [195, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1680": {"label": 5, "data": {"text": "In membranes from HEK293 cells transfected with alpha2-receptors, etomidate inhibited binding of the alpha2-antagonist, [3H]RX821002, with higher potency from alpha2B- and alpha2C-receptors than from alpha2A-receptors (Ki alpha2A 208 microm, alpha2B 26 microm, alpha2C 56 microm).", "entity1": "alpha2-receptors", "entity2": "[3H]RX821002", "span1": [48, 64], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13913": {"label": 3, "data": {"text": "Phenformin reduced the open probability of Kir6.1/SUR2B channels by approximately 90% in inside-out patches.", "entity1": "SUR2B", "entity2": "Phenformin", "span1": [50, 55], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14758": {"label": 2, "data": {"text": "Additional mechanistic studies revealed that jaceosidin treatment resulted in an increase in phosphorylation of Cdc25C and ATM-Chk1/2.", "entity1": "Cdc25C", "entity2": "jaceosidin", "span1": [112, 118], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1453": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "MAO", "entity2": "Rasagiline", "span1": [95, 98], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7166": {"label": 3, "data": {"text": "RESULTS: Telmisartan decreased the expression of AT1R at the mRNA and protein levels in a dose- and time-dependent manner.", "entity1": "AT1R", "entity2": "Telmisartan", "span1": [49, 53], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10309": {"label": 1, "data": {"text": "Study of the nematode putative GABA type-A receptor subunits: evidence for modulation by ivermectin.", "entity1": "GABA type-A receptor", "entity2": "ivermectin", "span1": [31, 51], "span2": [89, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11258": {"label": 0, "data": {"text": "The K(IR) N terminus and the TMD0-L0 segment of SUR1 are known to control the P(O(max)).", "entity1": "K(IR)", "entity2": "N", "span1": [4, 9], "span2": [10, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5927": {"label": 3, "data": {"text": "The concentration of estramustine phosphate required to inhibit the assembly or to induce the disassembly of chick brain MAP2:tubulin microtubules is markedly dependent upon the microtubule protein concentration.", "entity1": "chick brain MAP2", "entity2": "estramustine phosphate", "span1": [109, 125], "span2": [21, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1227": {"label": 3, "data": {"text": "It is not yet clear whether tamoxifen can reduce breast cancer incidence in women with BRCA1 and BRCA2 mutations, although preliminary evidence favors benefit for at least those with a BRCA2 mutation.", "entity1": "BRCA2", "entity2": "tamoxifen", "span1": [185, 190], "span2": [28, 37]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11274": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "glycine decarboxylase complex", "entity2": "glycine", "span1": [80, 109], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14025": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "RANKL", "entity2": "colchicoside", "span1": [101, 106], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8105": {"label": 3, "data": {"text": "We found that wogonin can suppress the H2O2-stimulated actin remodeling and albumin uptake of HUVECs, as well as transendothelial cell migration of the human breast carcinoma cell MDA-MB-231.", "entity1": "albumin", "entity2": "wogonin", "span1": [76, 83], "span2": [14, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2665": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE5", "entity2": "zaprinast", "span1": [258, 262], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15857": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "Human Serum Albumin", "entity2": "amino acid", "span1": [46, 65], "span2": [112, 122]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1454": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "monoamine oxidase", "entity2": "TVP1012", "span1": [76, 93], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10907": {"label": 8, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "Pyridoxal kinase", "entity2": "pyridoxamine", "span1": [0, 16], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15712": {"label": 1, "data": {"text": "3-Hydroxy-5-(2-phenylethyl)pyridine-2(1H)-one exhibited the predicted binding mode and demonstrated high inhibitory activity for human DAAO in enzyme- and cell-based assays.", "entity1": "human DAAO", "entity2": "3-Hydroxy-5-(2-phenylethyl)pyridine-2(1H)-one", "span1": [129, 139], "span2": [0, 45]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7865": {"label": 2, "data": {"text": "Fingolimod (FTY720), a novel drug approved for the treatment of relapsing-remitting multiple sclerosis, activates different sphingosine-1-phosphate receptor (S1PR) subtypes.", "entity1": "sphingosine-1-phosphate receptor", "entity2": "Fingolimod", "span1": [124, 156], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7903": {"label": 2, "data": {"text": "TCDD had no effect on AR activity in PC-3 cells, whereas the shortest AR variant was induced by TCDD in PNT1A cells.", "entity1": "AR", "entity2": "TCDD", "span1": [70, 72], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1062": {"label": 2, "data": {"text": "Re-feeding normal chow or a high sucrose diet for 24 h after a 48-h fast increased both ACS1 and ACS4 protein expression 1.5-2.0-fold, consistent with inhibition studies.", "entity1": "ACS1", "entity2": "sucrose", "span1": [88, 92], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9102": {"label": 8, "data": {"text": "Similar concentrations also inhibited the formation of leukotriene C4 (LTC4) by LTC synthetase, a detergent-solubilized cell free particulate enzyme from RBL cells which is capable of coupling LTA4 to glutathione.", "entity1": "LTC synthetase", "entity2": "leukotriene C4", "span1": [80, 94], "span2": [55, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14728": {"label": 3, "data": {"text": "Inhibitors based on a benzo-fused spirocyclic oxazepine scaffold were discovered for stearoyl-coenzyme A (CoA) desaturase 1 (SCD1) and subsequently optimized to potent compounds with favorable pharmacokinetic profiles and in vivo efficacy in reducing the desaturation index in a mouse model.", "entity1": "SCD1", "entity2": "benzo-fused spirocyclic oxazepine", "span1": [125, 129], "span2": [22, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11339": {"label": 0, "data": {"text": "The expression of the NH2 terminally truncated ErbB2 receptor (p95ErbB2) in breast cancer correlates with metastatic disease progression compared with the expression of full-length p185ErbB2.", "entity1": "p95ErbB2", "entity2": "NH2", "span1": [63, 71], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11502": {"label": 9, "data": {"text": "RNA interference-triggered reversal of ABCC2-dependent cisplatin resistance in human cancer cells.", "entity1": "ABCC2", "entity2": "cisplatin", "span1": [39, 44], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7376": {"label": 1, "data": {"text": "Histamine regulates many functions by binding to four histamine G-coupled receptor proteins (H1R, H2R, H3R and H4R).", "entity1": "H1R", "entity2": "Histamine", "span1": [93, 96], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11910": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "ceramides", "span1": [174, 179], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3530": {"label": 0, "data": {"text": "Phosphorylation of AMPK at Thr172 increased by 1.4-fold within 5 min, and remained elevated throughout a 30-min time course, in response to 2-deoxyglucose.", "entity1": "AMPK", "entity2": "Thr", "span1": [19, 23], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6684": {"label": 2, "data": {"text": "In contrast, menthol- and icilin-activated TRPM8 currents were suppressed by low pH.", "entity1": "TRPM8", "entity2": "menthol", "span1": [43, 48], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9245": {"label": 8, "data": {"text": "Hence, triclosan has the ability to inhibit both the cyclo-oxygenase and lipoxygenase pathways of arachidonic acid metabolism with similar efficacy.", "entity1": "lipoxygenase", "entity2": "arachidonic acid", "span1": [73, 85], "span2": [98, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2318": {"label": 3, "data": {"text": "Glyphosate affects aromatic amino acid biosynthesis by inhibiting 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS).", "entity1": "EPSPS", "entity2": "Glyphosate", "span1": [111, 116], "span2": [0, 10]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8320": {"label": 2, "data": {"text": "Paeoniflorin protects human EA.hy926 endothelial cells against gamma-radiation induced oxidative injury by activating the NF-E2-related factor 2/heme oxygenase-1 pathway.", "entity1": "NF-E2-related factor 2", "entity2": "Paeoniflorin", "span1": [122, 144], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9111": {"label": 9, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c. The irreversible complex between phenoxybenzamine and calmodulin may be useful for inhibiting certain calmodulin-dependent reactions and for studying the various biological functions of calmodulin.", "entity1": "S-100 protein", "entity2": "phenoxybenzamine", "span1": [83, 96], "span2": [13, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2573": {"label": 3, "data": {"text": "Neonatal quinpirole treatment produced a significant decrease in BDNF and ChAT in the frontal cortex that was unaffected by olanzapine treatment.", "entity1": "ChAT", "entity2": "quinpirole", "span1": [74, 78], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7752": {"label": 0, "data": {"text": "By synthesizing and testing a series of alanine point-mutated cyclic peptides, we identified which amino acid was important for the inhibition of the phospholamban function.", "entity1": "cyclic peptides", "entity2": "amino acid", "span1": [62, 77], "span2": [99, 109]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7588": {"label": 1, "data": {"text": "Specifically, B2-O-CH(2)-CH(2)-N-piperidine and B2-O-CH(2)-CH(2)-N-pyrrolidine revealed a higher affinity towards hERG channels than amiodarone.", "entity1": "hERG", "entity2": "amiodarone", "span1": [114, 118], "span2": [133, 143]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3430": {"label": 3, "data": {"text": "They display sensitivity to TK inhibitors, including gefitinib and erlotinib.", "entity1": "TK", "entity2": "erlotinib", "span1": [28, 30], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7458": {"label": 8, "data": {"text": "We found that glycine is released from vesicles when VIAAT is coexpressed with either the neuronal transporter GlyT2 or the glial transporter GlyT1.", "entity1": "VIAAT", "entity2": "glycine", "span1": [53, 58], "span2": [14, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2669": {"label": 3, "data": {"text": "Administration of a concentration (100 microM) of dipyridamole that blocks PDE8 inhibited ecto-phosphodiesterase activity (by 44%).", "entity1": "PDE8", "entity2": "dipyridamole", "span1": [75, 79], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"589": {"label": 3, "data": {"text": "In the long term, orlistat has been shown to be more effective than placebo in reducing body weight and serum total and low-density lipoprotein cholesterol levels.", "entity1": "low-density lipoprotein", "entity2": "orlistat", "span1": [120, 143], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1704": {"label": 8, "data": {"text": "Although a proton-stimulated uptake of cefadroxil was demonstrated in PEPT2(+/+) mice (pH 6.5 versus pH 7.4; p < 0.01), no pH dependence was observed in PEPT2(-/-) mice.", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [153, 158], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15575": {"label": 1, "data": {"text": "Our results revealed an important role of base excision repair (BER) as the ntg1, ntg2, apn1 and apn2 mutants showed pronounced sensitivity to essential oil and nerolidol.", "entity1": "ntg2", "entity2": "nerolidol", "span1": [82, 86], "span2": [161, 170]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6595": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "D(2)", "entity2": "ziprasidone", "span1": [245, 249], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2856": {"label": 2, "data": {"text": "Finally, the amounts of RORalpha and cAspAT mRNAs were similarly increased by TZD treatment of human adipose tissue explants, confirming coordinated regulation.", "entity1": "cAspAT", "entity2": "TZD", "span1": [37, 43], "span2": [78, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1388": {"label": 3, "data": {"text": "Gemfibrozil, a lipid-lowering drug, inhibited cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373MG astroglial cells and primary astrocytes.", "entity1": "iNOS", "entity2": "Gemfibrozil", "span1": [135, 139], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2618": {"label": 3, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "polymerases", "entity2": "foscarnet", "span1": [16, 27], "span2": [149, 158]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15807": {"label": 3, "data": {"text": "Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.", "entity1": "MK2", "entity2": "imidazo[1,2-a]pyrazine", "span1": [32, 35], "span2": [50, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2297": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP2", "entity2": "AH 6809", "span1": [127, 130], "span2": [249, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15899": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "N-glycosyltransferase", "entity2": "benzopyranopyrrole", "span1": [245, 266], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11743": {"label": 0, "data": {"text": "Albumin nanoparticles were surface-coated with bifunctional polyethylene glycol 3500 (PEG) and a nanobody-the single variable domain of an antibody-(Ega1) against the epidermal growth factor receptor (EGFR).", "entity1": "Albumin", "entity2": "PEG", "span1": [0, 7], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1054": {"label": 3, "data": {"text": "doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g. amonafide, batracylin, and menadione) was only slightly (less than 3-fold) affected.", "entity1": "TOP2", "entity2": "batracylin", "span1": [166, 170], "span2": [196, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3036": {"label": 1, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "EP(4)", "entity2": "PGE(2)", "span1": [206, 211], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3315": {"label": 1, "data": {"text": "Mutations in the Ca(2+) sensor, troponin C (TnC), were generated to increase/decrease the Ca(2+) sensitivity of cardiac skinned fibers to create the characteristic effects of DCM, HCM, and RCM.", "entity1": "TnC", "entity2": "Ca(2+)", "span1": [44, 47], "span2": [17, 23]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3965": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "Pin1", "entity2": "pSer", "span1": [66, 70], "span2": [136, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"15020": {"label": 3, "data": {"text": "Through immunoblotting analysis, it was found that AdOx was capable of indirectly diminishing the phosphorylation of oncogenic Src and its kinase activity.", "entity1": "kinase", "entity2": "AdOx", "span1": [139, 145], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7720": {"label": 2, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "gonadotrophin-releasing hormone (GnRH) receptor", "entity2": "leuprorelin", "span1": [140, 187], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3455": {"label": 1, "data": {"text": "RESULTS: (+/-)-, R-, and S-modafinil bind to the DAT and inhibit DA uptake less potently than cocaine, with R-modafinil having approximately threefold higher affinity than its S-enantiomer.", "entity1": "DAT", "entity2": "cocaine", "span1": [49, 52], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7612": {"label": 1, "data": {"text": "In a Phase III trial comparing lapatinib and capecitabine with capecitabine alone in women with HER2-positive, locally advanced breast cancer or MBC that had progressed after treatment with an anthracycline, a taxane, and trastuzumab, the combination of lapatinib and capecitabine was associated with a numeric improvement in response rate compared with capecitabine alone (22% vs 14%, respectively; P = NS) and a significant increase in time to progression (6.2 vs 4.3 months; hazard ratio = 0.57; 95% CI, 0.43-0.77; P < 0.001).", "entity1": "HER2", "entity2": "capecitabine", "span1": [96, 100], "span2": [63, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2637": {"label": 1, "data": {"text": "Exogenous all-trans-retinol, all-trans-13,14-dihydroretinol, or all-trans-7,8-dihydroretinol led to the strong induction of the expression of the retinoic acid-metabolizing enzyme, Cyp26A1, arguing for an active signaling function of dihydroretinoid metabolites in zebrafish.", "entity1": "Cyp26A1", "entity2": "all-trans-retinol", "span1": [181, 188], "span2": [10, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7400": {"label": 1, "data": {"text": "Ca2+ activation targets the PKCalpha C2 domain to the plasma membrane and the cPLA2alpha C2 domain to the internal membranes, with no detectable spatial overlap.", "entity1": "PKCalpha C2 domain", "entity2": "Ca2+", "span1": [28, 46], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9411": {"label": 4, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT4", "entity2": "cinitapride", "span1": [142, 147], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8568": {"label": 3, "data": {"text": "Immunofluorescence staining and western blotting demonstrated that cilostazol treatment reduced GFAP and VEGF expression in the retinas of OLETF rats.", "entity1": "GFAP", "entity2": "cilostazol", "span1": [96, 100], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1684": {"label": 8, "data": {"text": "Cat-1, the transporter for the essential amino acids, arginine and lysine, is one of the up-regulated genes.", "entity1": "Cat-1", "entity2": "lysine", "span1": [0, 5], "span2": [67, 73]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15520": {"label": 1, "data": {"text": "A highly potent inhibition of the peroxidase catalytic reaction by NO/SNO was seen in assays employing the coupled Prx-Trx system.", "entity1": "Trx", "entity2": "NO", "span1": [119, 122], "span2": [67, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"647": {"label": 5, "data": {"text": "The effect of sumatriptan, but not of LY 344864, was prevented by pretreatment with the antagonist SDZ 21-009, which displays high affinity for rat 5-HT1B receptors.", "entity1": "rat 5-HT1B", "entity2": "SDZ 21-009", "span1": [144, 154], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10766": {"label": 2, "data": {"text": "Imatinib stimulated the rapid release of soluble HB-EGF and the subsequent induction of membrane-bound HB-EGF, which correlated with biphasic MAPK activation.", "entity1": "MAPK", "entity2": "Imatinib", "span1": [142, 146], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15851": {"label": 8, "data": {"text": "Because 24(S)-hydroxycholesterol (24-OHC), produced by 24-hydroxylase, induces apoptosis of neuronal cells, it is vital to eliminate it rapidly from cells.", "entity1": "24-hydroxylase", "entity2": "24-OHC", "span1": [55, 69], "span2": [34, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8286": {"label": 4, "data": {"text": "We found that treatment of both differentiated dopaminergic-like SH-SY5Y cells and rat midbrain slices with the dopamine D2 receptor (D2R) agonist, quinpirole, triggered an increase in the expression of GDNF that was temporally preceded by an increase in the levels of zinc-finger protein 268 (Zif268), a DNA-binding transcription factor encoded by an immediate-early gene.", "entity1": "dopamine D2 receptor", "entity2": "quinpirole", "span1": [112, 132], "span2": [148, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1611": {"label": 3, "data": {"text": "In whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala, topiramate at low concentrations (IC50, approximately 0.5 microm) selectively inhibited pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit.", "entity1": "kainate receptors", "entity2": "topiramate", "span1": [251, 268], "span2": [95, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5167": {"label": 8, "data": {"text": "At a substrate concentration of 20\u2009\u00b5M, the most active HFC glucuronidation catalysts were UGT1A10 followed by UGT1A6 >UGT1A7 >UGT2A1, whereas at 300\u2009\u00b5M UGT1A6 was about 10 times better catalyst than the other recombinant UGTs.", "entity1": "UGT2A1", "entity2": "HFC", "span1": [126, 132], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"11942": {"label": 2, "data": {"text": "Results: Our results demonstrate that treatment with LBH589 leads to NIS RNA expression as shown by RT-PCR and luciferase assay, and to protein expression as determined by immunofluorescence in vitro and by immunohistochemistry in xenograft tumors.", "entity1": "NIS", "entity2": "LBH589", "span1": [69, 72], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11645": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "GABA-T", "entity2": "VIG", "span1": [269, 275], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4297": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B3", "entity2": "DHEAS", "span1": [269, 276], "span2": [126, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7486": {"label": 3, "data": {"text": "Phenserine deserves attention for an additional quality of action: in addition to inhibiting AChE, it modulates the amount of beta-amyloid precursor protein (APP) in neuronal cell culture by reducing APP translation.", "entity1": "APP", "entity2": "Phenserine", "span1": [200, 203], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5152": {"label": 1, "data": {"text": "2-Hydroxy-3-methylanthraquinone from Hedyotis diffusa Willd induces apoptosis in human leukemic U937 cells through modulation of MAPK pathways.", "entity1": "MAPK", "entity2": "2-Hydroxy-3-methylanthraquinone", "span1": [129, 133], "span2": [0, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11593": {"label": 8, "data": {"text": "These results suggest that the pro-inflammatory effect of H(2)S may be mediated by SP-NK-1R related pathway in mouse pancreatic acinar cells.", "entity1": "NK-1R", "entity2": "H(2)S", "span1": [86, 91], "span2": [58, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3970": {"label": 1, "data": {"text": "To control for possible interactions between the expression of the estrogen receptor genes and other learning-related steroid receptors, androgen receptors (AR), corticosterone-binding glucocorticoid receptors (GR) and mineralocorticoid receptors (MR) were also measured.", "entity1": "glucocorticoid receptors", "entity2": "corticosterone", "span1": [185, 209], "span2": [162, 176]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8663": {"label": 2, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "kinase", "entity2": "cisplatin", "span1": [107, 113], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14569": {"label": 2, "data": {"text": "Small interfering RNA-mediated knockdown of \u03b2-catenin mRNA demonstrated that induction of FSH\u03b2 mRNA by GnRH depended on \u03b2-catenin and that regulation of FSH\u03b2 by \u03b2-catenin occurred independently of the JNK-c-jun pathway.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [90, 94], "span2": [103, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13453": {"label": 2, "data": {"text": "These findings demonstrate that n-3 and n-6 PUFA increased PPARgamma activity is necessary for the COX-2 induction in HaCaT human keratinocyte cells.", "entity1": "COX-2", "entity2": "n-3 and n-6 PUFA", "span1": [99, 104], "span2": [32, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"646": {"label": 4, "data": {"text": "To establish the relative importance of these subtypes, we compared the effects of sumatriptan with those of a selective 5-HT1F receptor agonist (LY 344864) on c-fos protein expression in the trigeminal nucleus caudalis.", "entity1": "5-HT1F", "entity2": "LY 344864", "span1": [121, 127], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4999": {"label": 2, "data": {"text": "Cobalt chloride, a typical HIF activator, induced the gene expression of CAR-target genes, including cyp2b9 and cyp2b10, an accumulation of nuclear CAR and an increase in the PB-responsive enhancer module-mediated transactivation in the mouse liver.", "entity1": "cyp2b10", "entity2": "Cobalt chloride", "span1": [112, 119], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13879": {"label": 3, "data": {"text": "In addition, another study suggests that ibuprofen reduces generation of amyloid-beta42 peptide via inactivation of RhoA signaling, although it may also regulate amyloid-beta42 formation by direct inhibition of the gamma-secretase complex.", "entity1": "amyloid-beta42", "entity2": "ibuprofen", "span1": [73, 87], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9128": {"label": 1, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "alpha-adrenergic", "entity2": "prazosin", "span1": [81, 97], "span2": [113, 121]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6759": {"label": 2, "data": {"text": "Hydralazine induced rapid and transient expression of HIF-1alpha and downstream targets of HIF (endothelin-1, adrenomedullin, haem oxygenase 1, and vascular endothelial growth factor [VEGF]) in endothelial and smooth muscle cells and induced endothelial cell-specific proliferation.", "entity1": "haem oxygenase 1", "entity2": "Hydralazine", "span1": [126, 142], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3467": {"label": 8, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "human dopamine transporter", "entity2": "DA", "span1": [167, 193], "span2": [125, 127]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6009": {"label": 3, "data": {"text": "The daily administration of low-dose aspirin (40 mg), a selective inhibitor of platelet PGHS-1, caused a cumulative inhibition of urinary 11-dehydro-TXB2 and whole blood TXB2 production that recovered with a timecourse consistent with platelet turnover.", "entity1": "PGHS-1", "entity2": "aspirin", "span1": [88, 94], "span2": [37, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13842": {"label": 8, "data": {"text": "BACKGROUND: Peripheral inflammatory pain is associated with an upregulation of spinal cord COX-2 (cyclooxygenase-2), with a subsequent increase in central prostaglandin E2 (PGE2) levels associated with the development of hyperalgesia.", "entity1": "COX-2", "entity2": "prostaglandin E2", "span1": [91, 96], "span2": [155, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3095": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine", "span1": [354, 357], "span2": [126, 175]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2959": {"label": 1, "data": {"text": "Affinity of V782A for cGMP, vardenafil, sildenafil, tadalafil, or IBMX was reduced 5.5-, 23-, 10-, 3-, and 12-fold, respectively.", "entity1": "V782A", "entity2": "sildenafil", "span1": [12, 17], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16030": {"label": 3, "data": {"text": "This effect was prevented by rapamycin, an inhibitor of the mammalian target of rapamycin complex 1 (mTORC1), or by PF470867, a selective inhibitor of the p70 ribosomal S6 kinase 1 (S6K1).", "entity1": "mammalian target of rapamycin complex 1", "entity2": "rapamycin", "span1": [60, 99], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4150": {"label": 3, "data": {"text": "Local PGE2 administration prevented the increase of airway IL-13 and osteopontin and kept lung plasmacytoid dendritic cell counts close to baseline.", "entity1": "osteopontin", "entity2": "PGE2", "span1": [69, 80], "span2": [6, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"308": {"label": 4, "data": {"text": "In contrast, the D-1997-induced responses were potently and concentration-dependently antagonized by the mixed 5-HT1-like and 5-HT2 receptor antagonist methiothepin (0.01-1 microM).", "entity1": "5-HT2 receptor", "entity2": "D-1997", "span1": [126, 140], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11969": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "PIP5K1B", "entity2": "PI(4)P", "span1": [0, 7], "span2": [193, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15005": {"label": 8, "data": {"text": "In the in vitro model we observed high permeability of imperatorin and isoimperatorin with the P-gp-mediated efflux ratios of 0.53 and 0.06, as well as medium permeability of cnidilin with 0.82.", "entity1": "P-gp", "entity2": "isoimperatorin", "span1": [95, 99], "span2": [71, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7226": {"label": 1, "data": {"text": "GnRH-induced c-Src activation resulted in the phosphorylation of expressed Hic-5 and promoted its association with the human androgen receptor.", "entity1": "Hic-5", "entity2": "GnRH", "span1": [75, 80], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5382": {"label": 2, "data": {"text": "MNU-induced lesions presented markers indicative of an aggressive phenotype: lack of basal cells, rupture of the smooth muscle cell layer, loss of E-cadherin, and high MGMT staining.", "entity1": "MGMT", "entity2": "MNU", "span1": [168, 172], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13463": {"label": 1, "data": {"text": "OBJECTIVE: The aim of this study was to assess the efficacy and tolerability of nebulized arformoterol tartrate (a selective, long-acting beta(2)-adrenergic agonist that is the [R,R] isomer of formoterol) and salmeterol xinafoate versus placebo in patients with chronic obstructive pulmonary disease (COPD).", "entity1": "beta(2)-adrenergic", "entity2": "salmeterol xinafoate", "span1": [138, 156], "span2": [209, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12586": {"label": 1, "data": {"text": "Coexpression of the flip and flop splice variants of GluR-A, in the absence of GluR-B, revealed that heteromeric AMPA receptors with intermediate sensitivity to cyclothiazide, similar to responses observed for the combinations GluR-AoBi or GluR-AiBo, could be generated independently of the presence of the GluR-B subunit.", "entity1": "GluR-AiBo", "entity2": "cyclothiazide", "span1": [240, 249], "span2": [161, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"216": {"label": 1, "data": {"text": "Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.", "entity1": "serotonin receptor", "entity2": "tricyclic", "span1": [34, 52], "span2": [76, 85]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14482": {"label": 8, "data": {"text": "Human liver microsomes of the wild-type CYP2D6 metabolized 5-methoxytryptamine to serotonin more effectively than did the defective CYP2D6*4*4 ones.", "entity1": "CYP2D6", "entity2": "serotonin", "span1": [132, 138], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5050": {"label": 0, "data": {"text": "Intravenous treatment, during coronary artery occlusion, with the melanocortin analogs [Nle(4), D-Phe(7)]\u03b1-melanocyte-stimulating hormone (NDP-\u03b1-MSH) and adrenocorticotropic hormone 1-24 [ACTH-(1-24)], induced a left ventricle up-regulation of pJAK2, pERK1/2 and pTyr-STAT3 (JAK-dependent), and a reduction in pJNK and TNF-\u03b1 levels; these effects of NDP-\u03b1-MSH and ACTH-(1-24) were associated with over-expression of the pro-survival proteins HO-1 and Bcl-XL, and marked decrease of the myocardial infarct size.", "entity1": "\u03b1-melanocyte-stimulating hormone", "entity2": "D-Phe", "span1": [105, 137], "span2": [96, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11505": {"label": 0, "data": {"text": "New data for cattle (Bos taurus) indicates a gene encoding GnRH-II decapeptide possessing arginine (codon: CGG) rather than tryptophan (TGG) at position three in the mature peptide.", "entity1": "GnRH-II", "entity2": "tryptophan", "span1": [59, 66], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9338": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "quisqualate", "span1": [72, 77], "span2": [126, 137]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7202": {"label": 1, "data": {"text": "Estradiol (E2) stimulates BC cells proliferation by binding the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "Estradiol", "span1": [64, 81], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13872": {"label": 1, "data": {"text": "Here, we report that the transcription factor peroxisome proliferator-activated receptor gamma (PPARgamma) is essential for coupling ibuprofen to RhoA inhibition and subsequent neurite growth promotion in neurons.", "entity1": "PPARgamma", "entity2": "ibuprofen", "span1": [96, 105], "span2": [133, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13650": {"label": 0, "data": {"text": "The binding of U46619 to the PGIS protein was demonstrated by 1D NMR titration, and the significant perturbation of the chemical shifts of protons at C-11, H2C, and H20 of U46619 were observed upon U46619 binding to the engineered PGIS in a concentration-dependent manner.", "entity1": "PGIS", "entity2": "U46619", "span1": [29, 33], "span2": [172, 178]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2482": {"label": 1, "data": {"text": "CP-690550, a JAK3 inhibitor is currently in phase II clinical trials.FK778, is a synthetic malononitrilamide that targets the critical enzyme of the de novo pyrimidine synthesis, dihydroorotic acid dehydrogenase, and receptor-associated tyrosine kinases has completed phase II trials.", "entity1": "receptor-associated tyrosine kinases", "entity2": "malononitrilamide", "span1": [217, 253], "span2": [91, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15584": {"label": 1, "data": {"text": "A series of N-substituted lobelane analogues was synthesized and evaluated for their [(3)H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [(3)H]dopamine uptake.", "entity1": "vesicular monoamine transporter", "entity2": "N", "span1": [136, 167], "span2": [12, 13]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11463": {"label": 1, "data": {"text": "In addition, there was a positive correlation between the pre-withdrawal ethanol consumption and the packing density of GS-IR astrocytes.", "entity1": "GS", "entity2": "ethanol", "span1": [120, 122], "span2": [73, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14487": {"label": 8, "data": {"text": "Of the rat CYP isoforms studied, CYP2D isoforms were the most efficient in catalyzing the O-demethylation of 5-methoxytryptamine to serotonin, but they were less effective than the human isoform CYP2D6.", "entity1": "CYP2D", "entity2": "5-methoxytryptamine", "span1": [33, 38], "span2": [109, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1901": {"label": 3, "data": {"text": "PKC isoforms did show different sensitivity and selectivity for down-regulation by I3A and phorbol 12-myristate 13-acetate (PMA) in WEHI-231, HOP-92, and Colo-205 cells.", "entity1": "PKC", "entity2": "phorbol 12-myristate 13-acetate", "span1": [0, 3], "span2": [91, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12314": {"label": 1, "data": {"text": "In an effort to understand the shedding process of AChE, we have used several pharmacological treatments, which showed that it is likely to be mediated in part by an EDTA- and batimastat-sensitive, but GM6001-insensitive metalloprotease, with the possible additional involvement of a thiol isomerase.", "entity1": "AChE", "entity2": "batimastat", "span1": [51, 55], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5225": {"label": 2, "data": {"text": "Also, vinblastine enhances the phosphorylation of Ras homologous protein A, the accumulation of reactive oxygen species, the release of intracellular Ca(2+), as well as the activation of apoptosis signal-regulating kinase 1, c-jun-N-terminal kinase, p38, inhibitor of kappaB\u03b1 (I\u03baB\u03b1) kinase, and inositol requiring enzyme 1\u03b1.", "entity1": "kinase", "entity2": "vinblastine", "span1": [283, 289], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12768": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "5-fluorouracil", "span1": [22, 24], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8889": {"label": 9, "data": {"text": "These effects were not mimicked by oral administration of the beta 2-adrenoceptor agonist salbutamol even at high dose (52 mg/kg diet), and the effects of clenbuterol were not inhibited by addition of DL-propranolol (200 mg/kg diet).", "entity1": "beta 2-adrenoceptor", "entity2": "DL-propranolol", "span1": [62, 81], "span2": [201, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"935": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "FdUrd", "span1": [238, 240], "span2": [49, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"833": {"label": 4, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "EP3", "entity2": "sulprostone", "span1": [135, 138], "span2": [119, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9873": {"label": 3, "data": {"text": "RESULTS: Exposure of in vitro differentiated subcutaneous adipocytes from young normal-weight females to 1 microgram/ml troglitazone for 72 h caused a reduction of both PAI-1 secretion (by 29 +/- 5%; p < 0.01) and PAI-1 mRNA expression (by 26 +/- 3%; p < 0.05).", "entity1": "PAI-1", "entity2": "troglitazone", "span1": [169, 174], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8546": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "histone deacetylase", "entity2": "tert-butylcarbamate", "span1": [159, 178], "span2": [112, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5758": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "parkin", "entity2": "1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine", "span1": [233, 239], "span2": [94, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15081": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "KPCs", "entity2": "ceftazidime", "span1": [237, 241], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15699": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "TRP channels", "entity2": "capsaicin", "span1": [46, 58], "span2": [113, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11072": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "cAMP phosphodiesterase", "entity2": "felodipine", "span1": [86, 108], "span2": [202, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15057": {"label": 8, "data": {"text": "These results underscore a role for TRPML1\u00a0in zinc metabolism.", "entity1": "TRPML1", "entity2": "zinc", "span1": [36, 42], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6144": {"label": 1, "data": {"text": "Treatment using a combination of testosterone and the aromatase inhibitor testolactone may have significantly better effects on sexual function and also seizure frequency than testosterone alone.", "entity1": "aromatase", "entity2": "testosterone", "span1": [54, 63], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3202": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "caffeic acid", "span1": [282, 284], "span2": [104, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15667": {"label": 3, "data": {"text": "Subsequent optimization led to several novel 3HPT-based HDACi that are selective for HDAC 6 and HDAC 8.", "entity1": "HDAC", "entity2": "3HPT", "span1": [56, 60], "span2": [45, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"25": {"label": 2, "data": {"text": "On study day 1, candoxatril acutely increased plasma ANP levels, suppressed aldosterone and decreased right atrial and pulmonary capillary wedge pressures.", "entity1": "ANP", "entity2": "candoxatril", "span1": [53, 56], "span2": [16, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5025": {"label": 8, "data": {"text": "ACTH-stimulated peak cortisol, delta cortisol, and delta DHEA-S levels are decreased during hyperthyroidism, probably due to increased turnover.", "entity1": "ACTH", "entity2": "cortisol", "span1": [0, 4], "span2": [21, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10323": {"label": 2, "data": {"text": "The immune response modifiers, imiquimod and resiquimod, are TLR7 agonists that induce type I interferon in numerous species, including humans.", "entity1": "type I interferon", "entity2": "resiquimod", "span1": [87, 104], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11437": {"label": 1, "data": {"text": "Due to its central role in the formation and stabilization of a thrombus, the P2Y12 receptor is a well-established target of antithrombotic drugs like ticlopidine or clopidogrel, which have proved efficacy in many clinical trials and experimental models of thrombosis.", "entity1": "P2Y12", "entity2": "clopidogrel", "span1": [78, 83], "span2": [166, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12555": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "transcobalamin II", "entity2": "[57Co]cyanocobalamin", "span1": [193, 210], "span2": [154, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13855": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "progestogens", "span1": [252, 261], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4898": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "sulfatase", "entity2": "Cl", "span1": [162, 171], "span2": [102, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3536": {"label": 2, "data": {"text": "2-Deoxyglucose increased phosphorylation of tuberous sclerosis complex 2 (TSC2) on AMPK consensus sites but did not change the amount of TSC1 bound to TSC2.", "entity1": "AMPK", "entity2": "2-Deoxyglucose", "span1": [83, 87], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11185": {"label": 3, "data": {"text": "We conclude that felbamate exhibits modest selectivity for NMDA receptors composed of NR1a/NR2B subunits.", "entity1": "NMDA receptors", "entity2": "felbamate", "span1": [59, 73], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15782": {"label": 8, "data": {"text": "A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone.", "entity1": "OSC", "entity2": "lanosterol", "span1": [123, 126], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11917": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "insulin", "entity2": "DAGs", "span1": [118, 125], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"581": {"label": 3, "data": {"text": "These results suggest that the megabase DNA fragmentation is induced as a consequence of inhibition of thymidylate synthase by Tomudex and kilobase DNA fragmentation may correlate with the reduction of p27(kip1) expression and the increase in cyclin E and cdk2 kinase activities.", "entity1": "p27(kip1)", "entity2": "Tomudex", "span1": [202, 211], "span2": [127, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2862": {"label": 8, "data": {"text": "4-Hydroxynonenal (4-HNE) is a mutagenic alpha,beta-unsaturated aldehyde produced during oxidative injury that is conjugated by several glutathione S-transferase (GST) isoforms.", "entity1": "glutathione S-transferase", "entity2": "4-Hydroxynonenal", "span1": [135, 160], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15771": {"label": 2, "data": {"text": "Agonistic activity of ICI 182 780 on activation of GSK 3\u03b2/AKT pathway in the rat uterus during the estrous cycle.", "entity1": "AKT", "entity2": "ICI 182 780", "span1": [58, 61], "span2": [22, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3391": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "VMAT2", "entity2": "AMPH", "span1": [234, 239], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7036": {"label": 8, "data": {"text": "The tissue RA level is maintained through a cascade of metabolic reactions where retinal dehydrogenases (RALDHs) catalyze the terminal reaction of RA biosynthesis from retinal, a rate-limiting step.", "entity1": "retinal dehydrogenases", "entity2": "RA", "span1": [81, 103], "span2": [147, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10934": {"label": 3, "data": {"text": "Clinical experience in heart failure is growing, and recent data suggest an improved survival with losartan versus captopril, a drug from the angiotensin-converting-enzyme inhibitor class with proven benefit in this population.", "entity1": "angiotensin-converting-enzyme", "entity2": "captopril", "span1": [142, 171], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2257": {"label": 1, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "cytochromes P450", "entity2": "rifampicin", "span1": [119, 135], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10008": {"label": 3, "data": {"text": "In mice, AS-8112 (1.0 - 3.0 mg kg(-1) s.c.) potently inhibited hypothermia induced by the dopamine D3 receptor agonist; R(+)-7-OH-DPAT (R(+)-7-hydroxy-2-(N,N-di-n-propylamino)tetraline) (0.3 mg kg(-1) s.c.).", "entity1": "dopamine D3 receptor", "entity2": "AS-8112", "span1": [90, 110], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14475": {"label": 3, "data": {"text": "Following CdCl\u2082 treatment, ICAM2 was found to be upregulated during restructuring of the seminiferous epithelium, with round spermatids becoming increasingly immunoreactive for ICAM2 by 6-16 h. Interestingly, there was a loss in the binding of ICAM2 to actin during CdCl\u2082-induced germ cell loss, suggesting that a loss of ICAM2-actin interactions might have facilitated junction restructuring.", "entity1": "actin", "entity2": "CdCl\u2082", "span1": [253, 258], "span2": [266, 271]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"486": {"label": 1, "data": {"text": "The atypical neuroleptics remoxipride, clozapine, perlapine, seroquel, and melperone had low affinity for the dopamine D2 receptor (radioligand-independent dissociation constants of 30 to 90 nM).", "entity1": "D2 receptor", "entity2": "seroquel", "span1": [119, 130], "span2": [61, 69]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15059": {"label": 8, "data": {"text": "Furthermore, they suggest that TRPML1 works in concert with ZnT4 to regulate zinc translocation between the cytoplasm and lysosomes.", "entity1": "ZnT4", "entity2": "zinc", "span1": [60, 64], "span2": [77, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4739": {"label": 3, "data": {"text": "In conclusion, we find that sinapic acid exhibits hepatoprotective and antifibrotic effects against DMN-induced liver injury, most likely due to its antioxidant activities of scavenging radicals, its capacity to suppress TGF-\u03b21 and its ability to attenuate activation of hepatic stellate cells.", "entity1": "TGF-\u03b21", "entity2": "sinapic acid", "span1": [221, 227], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5819": {"label": 3, "data": {"text": "After the combined pituitary stimulation test (100 micrograms human CRH, 100 micrograms GnRH, 100 micrograms GH-releasing hormone, and 200 micrograms TRH), the ACTH peak (maximum increase at 30 min) was significantly blunted by loperamide from 9 +/- 1 to 4 +/- 1 pmol/L (P less than 0.001) and the area under the curve of ACTH from 0-120 min was reduced from 35 +/- 5 to 23 +/- 4 pmol/L.2 h (P less than 0.05).", "entity1": "human CRH", "entity2": "loperamide", "span1": [62, 71], "span2": [228, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10543": {"label": 1, "data": {"text": "Within this sequence DNase I footprinting revealed that RA induced binding of a nuclear protein complex to an element containing two GT boxes.", "entity1": "GT boxes", "entity2": "RA", "span1": [133, 141], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2408": {"label": 1, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "L-arginine transporter", "entity2": "Nor-NOHA", "span1": [218, 240], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2633": {"label": 8, "data": {"text": "They all expressed ASS, but not ornithine transcarbamylase (OTC), the enzyme that converts ornithine, the product of degradation of arginine with rhArg, to citrulline, which is converted back to arginine via ASS.", "entity1": "ornithine transcarbamylase", "entity2": "ornithine", "span1": [32, 58], "span2": [91, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, 9]},
	"8236": {"label": 4, "data": {"text": "ICA is a mixed agonist of mutant EAG and EAG/ERG chimera channels that inactivate by a combination of slow and fast mechanisms.", "entity1": "ERG", "entity2": "ICA", "span1": [45, 48], "span2": [0, 3]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6760": {"label": 2, "data": {"text": "Hydralazine induced rapid and transient expression of HIF-1alpha and downstream targets of HIF (endothelin-1, adrenomedullin, haem oxygenase 1, and vascular endothelial growth factor [VEGF]) in endothelial and smooth muscle cells and induced endothelial cell-specific proliferation.", "entity1": "vascular endothelial growth factor", "entity2": "Hydralazine", "span1": [148, 182], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14629": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "cytidine deaminase", "entity2": "Gemcitabine", "span1": [66, 84], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13192": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "SERT", "entity2": "mZIENT", "span1": [272, 276], "span2": [67, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14704": {"label": 3, "data": {"text": "Inhibition of Th1/Th17 responses via suppression of STAT1 and STAT3 activation contributes to the amelioration of murine experimental colitis by a natural flavonoid glucoside icariin.", "entity1": "STAT1", "entity2": "icariin", "span1": [52, 57], "span2": [175, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6685": {"label": 2, "data": {"text": "In contrast, menthol- and icilin-activated TRPM8 currents were suppressed by low pH.", "entity1": "TRPM8", "entity2": "icilin", "span1": [43, 48], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7355": {"label": 2, "data": {"text": "Stimulated P-selectin and integrin alpha(IIb)beta(3) expression were also higher in the upper tertile both before and after aspirin.", "entity1": "P-selectin", "entity2": "aspirin", "span1": [11, 21], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14229": {"label": 5, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b2", "entity2": "PHTPP", "span1": [420, 423], "span2": [435, 440]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3546": {"label": 2, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "NF-\u03baB", "entity2": "LTD4", "span1": [50, 55], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15801": {"label": 2, "data": {"text": "The rate limiting enzyme of beta-oxidation (ACOX1) was significantly over-expressed in the liver with tBHQ treatment.", "entity1": "ACOX1", "entity2": "tBHQ", "span1": [44, 49], "span2": [102, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11753": {"label": 1, "data": {"text": "Around five times as potent as the lead with an IC(50) of 33 \u03bcM for disruption of the Myc-Max heterodimer, JY-3-094 demonstrated excellent selectivity over Max-Max homodimers, with no apparent effect at 100 \u03bcM.", "entity1": "Myc", "entity2": "JY-3-094", "span1": [86, 89], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10078": {"label": 3, "data": {"text": "Aspirin and salicylate bind to immunoglobulin heavy chain binding protein (BiP) and inhibit its ATPase activity in human fibroblasts.", "entity1": "ATPase", "entity2": "Aspirin", "span1": [96, 102], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3267": {"label": 1, "data": {"text": "To examine the interaction of S100A4 with TFP, we determined the 2.3 A crystal structure of human Ca(2+)-S100A4 bound to TFP.", "entity1": "S100A4", "entity2": "TFP", "span1": [105, 111], "span2": [121, 124]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14894": {"label": 2, "data": {"text": "FMO3 expression is induced by dietary bile acids by a mechanism that involves the farnesoid X receptor (FXR), a bile acid-activated nuclear receptor.", "entity1": "FXR", "entity2": "bile acid", "span1": [104, 107], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2900": {"label": 4, "data": {"text": "OBJECTIVES: The aim of this study was to determine whether cocaine's sympathomimetic actions can be reversed by a potent centrally acting alpha2 adrenergic receptor (AR) agonist (dexmedetomidine).", "entity1": "alpha2 adrenergic receptor", "entity2": "dexmedetomidine", "span1": [138, 164], "span2": [179, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15370": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "nuclear receptors", "entity2": "atRA", "span1": [202, 219], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4894": {"label": 3, "data": {"text": "Synthesis and Structure-Activity Relationship Studies of Derivatives of the Dual Aromatase-Sulfatase Inhibitor 4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate.", "entity1": "Sulfatase", "entity2": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate", "span1": [91, 100], "span2": [111, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3137": {"label": 8, "data": {"text": "Moreover, kinetic analysis revealed that inhibition by reserpine, a typical VMAT2 inhibitor, was uncompetitive, decreasing maximum velocity and affinity for dopamine.", "entity1": "VMAT2", "entity2": "dopamine", "span1": [76, 81], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7485": {"label": 3, "data": {"text": "As a consequence, phenserine reduces beta-amyloid peptide (Abeta) formation in vitro and in vivo.", "entity1": "Abeta", "entity2": "phenserine", "span1": [59, 64], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15639": {"label": 3, "data": {"text": "Furthermore, nobiletin could inhibit HGF-induced the membrane localization of phosphorylated c-Met, ERK2, and Akt, but not phosphorylated JNK1/2 and p38.", "entity1": "HGF", "entity2": "nobiletin", "span1": [37, 40], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10528": {"label": 2, "data": {"text": "Metformin, but not leptin, regulates AMP-activated protein kinase in pancreatic islets: impact on glucose-stimulated insulin secretion.", "entity1": "insulin", "entity2": "glucose", "span1": [117, 124], "span2": [98, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14305": {"label": 1, "data": {"text": "Claudin-3 and claudin-4 regulate sensitivity to cisplatin by controlling expression of the copper and cisplatin influx transporter CTR1.", "entity1": "copper and cisplatin influx transporter", "entity2": "cisplatin", "span1": [91, 130], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3792": {"label": 3, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "fatty acid synthase", "entity2": "Phillyrin", "span1": [50, 69], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"234": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D2 receptor", "entity2": "raclopride", "span1": [304, 324], "span2": [336, 346]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10226": {"label": 3, "data": {"text": "Thalidomide has been shown to suppress TNF-alpha production from macrophages.", "entity1": "TNF-alpha", "entity2": "Thalidomide", "span1": [39, 48], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7796": {"label": 2, "data": {"text": "Reversal of inhibition by D2 agonist quinpirole was produced by serotonin (50 \u00b5M) and by neurotensin (5-10 nM).", "entity1": "D2", "entity2": "serotonin", "span1": [26, 28], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8711": {"label": 2, "data": {"text": "The expressions of HSP70 and HO-1 were significantly (P<0.05) increased in the NaAsO2 group and reduced in the combined treatment group.", "entity1": "HSP70", "entity2": "NaAsO2", "span1": [19, 24], "span2": [79, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"120": {"label": 3, "data": {"text": "Similarly, felodipine and the p-chloro analogue blocked myosin filament assembly induced by low concentrations of calmodulin, whereas the oxidized and t-butyl analogues did not.", "entity1": "myosin", "entity2": "felodipine", "span1": [56, 62], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4884": {"label": 3, "data": {"text": "Separate 5-aza-2'-deoxycytidine pretreatment or in combination with trichostatin A reduced (m)CpG and specific small interference RNAs targeting Mecp2 and Creb1 separately or together depleting Mecp2 and/or Creb1 binding of glut3-(m)CpGs reduced glut3 expression in HT22 cells.", "entity1": "Creb1", "entity2": "5-aza-2'-deoxycytidine", "span1": [155, 160], "span2": [9, 31]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15365": {"label": 1, "data": {"text": "Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone.", "entity1": "xenobiotic receptors", "entity2": "oxycodone", "span1": [13, 33], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5980": {"label": 8, "data": {"text": "Tyrosinase usually catalyzes the conversion of monophenols to o-diphenols and oxidation of diphenols to the corresponding quinones.", "entity1": "Tyrosinase", "entity2": "diphenols", "span1": [0, 10], "span2": [91, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"10120": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "COX-2", "entity2": "NS-389", "span1": [180, 185], "span2": [237, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14771": {"label": 1, "data": {"text": "ATP is released from skeletal muscle by contractile activity and can autocrinely signal through purinergic receptors, and we hypothesized it may influence glucose uptake.", "entity1": "purinergic receptors", "entity2": "ATP", "span1": [96, 116], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2086": {"label": 3, "data": {"text": "Am80 inhibited VEGF-induced phosphorylation of VEGF receptor.", "entity1": "VEGF", "entity2": "Am80", "span1": [15, 19], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12700": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "alpha-difluoroalkylthiolate", "span1": [79, 90], "span2": [162, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7789": {"label": 8, "data": {"text": "Here, in expressing cocaine-hydrolyzing mutants of BChE in Nicotiana benthamiana using the MagnICON virus-assisted transient expression system, and in reporting their initial biochemical analysis, we provide proof-of-principle that plants can express engineered BChE proteins with desired properties.", "entity1": "BChE", "entity2": "cocaine", "span1": [51, 55], "span2": [20, 27]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1150": {"label": 3, "data": {"text": "The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.", "entity1": "HER2", "entity2": "Iressa", "span1": [57, 61], "span2": [39, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2849": {"label": 1, "data": {"text": "Cytosolic aspartate aminotransferase, a new partner in adipocyte glyceroneogenesis and an atypical target of thiazolidinedione.", "entity1": "Cytosolic aspartate aminotransferase", "entity2": "thiazolidinedione", "span1": [0, 36], "span2": [109, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10746": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "fluoropyrimidine", "span1": [282, 284], "span2": [57, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13672": {"label": 9, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imiquimod", "span1": [138, 142], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4986": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "CK-MB", "entity2": "vitamin E", "span1": [91, 96], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6475": {"label": 3, "data": {"text": "Nordihydroguaiaretic acid (NDGA) has been shown to inhibit both 5-lipoxygenase and ornithine decarboxylase and is active against several cancer cell lines and at least one mouse tumor model.", "entity1": "ornithine decarboxylase", "entity2": "NDGA", "span1": [83, 106], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15396": {"label": 0, "data": {"text": "p14ARF perturbs the androgen-induced interaction between the N terminus and C terminus of AR.", "entity1": "AR", "entity2": "C", "span1": [90, 92], "span2": [76, 77]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6023": {"label": 3, "data": {"text": "6-Methoxy-2-naphthylacetic acid, the active metabolite of Relafen, inhibits murine PGHS-2 preferentially.", "entity1": "PGHS-2", "entity2": "6-Methoxy-2-naphthylacetic acid", "span1": [83, 89], "span2": [0, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1905": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "5-fluorouracil", "span1": [121, 123], "span2": [71, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13909": {"label": 1, "data": {"text": "These findings suggest that phenformin interacts directly with the pore-forming Kir6.0 subunit however the sulphonylurea receptor is able to significantly modulate the affinity.", "entity1": "Kir6.0", "entity2": "phenformin", "span1": [80, 86], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11235": {"label": 1, "data": {"text": "Taken together, these results reveal several differences between effects of MDMA and previously reported METH on DAT and VMAT-2; differences that may underlie the dissimilar neurotoxic profile of these agents.", "entity1": "VMAT-2", "entity2": "MDMA", "span1": [121, 127], "span2": [76, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"199": {"label": 1, "data": {"text": "BMY 7378 displayed high affinity for cloned human alpha 1D-adrenoceptors (pKi = 8.2 +/- 0.10) and was selective over alpha 1A (pKi = 6.2 +/- 0.10) and alpha 1B subtypes (6.7 +/- 0.11).", "entity1": "human alpha 1D-adrenoceptors", "entity2": "BMY 7378", "span1": [44, 72], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4108": {"label": 2, "data": {"text": "Furthermore, compared with control groups, the plaque endothelium level of p75(NTR) was 3-fold increased and the liver level of p75(NTR) was 17.4-fold increased by SFO-HD.", "entity1": "p75(NTR)", "entity2": "SFO", "span1": [75, 83], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4157": {"label": 3, "data": {"text": "Pharmacokinetic and pharmacodynamic modeling of hedgehog inhibitor TAK-441 for the inhibition of Gli1 messenger RNA expression and antitumor efficacy in xenografted tumor model mice.", "entity1": "hedgehog", "entity2": "TAK-441", "span1": [48, 56], "span2": [67, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7966": {"label": 2, "data": {"text": "The treatment also prevented the high cholesterol diet-induced increase in serum creatine kinase, total and isoforms, markers of neurological, cardiac and muscular damage.", "entity1": "creatine kinase", "entity2": "cholesterol", "span1": [81, 96], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11611": {"label": 1, "data": {"text": "Our data identify cAspAT as a new member of glyceroneogenesis, transcriptionally regulated by TZD via the control of RORalpha expression by PPARgamma in adipocytes.", "entity1": "PPARgamma", "entity2": "TZD", "span1": [140, 149], "span2": [94, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1682": {"label": 8, "data": {"text": "Cat-1, the transporter for the essential amino acids, arginine and lysine, is one of the up-regulated genes.", "entity1": "Cat-1", "entity2": "amino acids", "span1": [0, 5], "span2": [41, 52]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8934": {"label": 0, "data": {"text": "Both these MAPs were found to have two to three binding sites for estramustine phosphate which is compatible with the reported number of basic amino acid repeats of these MAPs, considered to be the ultimate tubulin binding domains.", "entity1": "MAPs", "entity2": "amino acid", "span1": [171, 175], "span2": [143, 153]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7347": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT1", "entity2": "alanine", "span1": [323, 328], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9322": {"label": 3, "data": {"text": "CONCLUSIONS: The chemotactic responses toward C5a were inhibited by nedocromil sodium at higher concentrations than were required in the priming studies (IC50 approximately 10 to 100 nmol/L).", "entity1": "C5a", "entity2": "nedocromil sodium", "span1": [46, 49], "span2": [68, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"357": {"label": 1, "data": {"text": "dSERT1 shows little transport of other monoamines and is Na+ and Cl- dependent.", "entity1": "dSERT1", "entity2": "Na+", "span1": [0, 6], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14906": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO1", "entity2": "TMA", "span1": [62, 66], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1259": {"label": 1, "data": {"text": "The hyperglycemic effect of m-CPBG central administration was blocked by pretreatment with ondansetron, a specific 5-HT3 receptor antagonist, indicating that the effects here obtained with m-CPBG were a result of its interaction with 5-HT3 receptors.", "entity1": "5-HT3", "entity2": "m-CPBG", "span1": [234, 239], "span2": [189, 195]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2707": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "c-kit", "entity2": "parathion", "span1": [30, 35], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3589": {"label": 1, "data": {"text": "Wogonoside induces autophagy in MDA-MB-231 cells by regulating MAPK-mTOR pathway.", "entity1": "mTOR", "entity2": "Wogonoside", "span1": [68, 72], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11591": {"label": 1, "data": {"text": "The acute insulin response to intravenous glucose was augmented (1,300 +/- 110 vs 790 +/- 64 pmol/l; p < 0.001).", "entity1": "insulin", "entity2": "glucose", "span1": [10, 17], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7630": {"label": 3, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "ERK", "entity2": "SB-277011-A", "span1": [102, 105], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5324": {"label": 3, "data": {"text": "Synthesis and biological evaluation of phosphorylated flavonoids as potent and selective inhibitors of cholesterol esterase.", "entity1": "cholesterol esterase", "entity2": "phosphorylated flavonoids", "span1": [103, 123], "span2": [39, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13070": {"label": 8, "data": {"text": "It was, therefore, proposed that H. pylori may in fact, antagonize, aspirin-induced delay of ulcer healing due to suppression of acid secretion by the enhancement in PGE(2) possibly derived from COX-2 expression and activity and to the overexpression of growth factors such as TGF alpha and VEGF.", "entity1": "COX-2", "entity2": "PGE(2)", "span1": [195, 200], "span2": [166, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7099": {"label": 8, "data": {"text": "Proline oxidase (POX), a mitochondrial inner-membrane protein, catalyzes the rate-limiting oxidation of proline to pyrroline- 5-carboxylate (P5C).", "entity1": "POX", "entity2": "P5C", "span1": [17, 20], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4959": {"label": 9, "data": {"text": "Short-term exposure to amprenavir significantly increased plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice.", "entity1": "PXR", "entity2": "amprenavir", "span1": [172, 175], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5237": {"label": 3, "data": {"text": "Treatment of C57 BL/6 mice with bleomycin increased fibroblast viability and collagen production and significantly downregulated Nrf2.", "entity1": "Nrf2", "entity2": "bleomycin", "span1": [129, 133], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15272": {"label": 1, "data": {"text": "The CRF(1) receptor antagonist SSR125543 prevents stress-induced cognitive deficit associated with hippocampal dysfunction: Comparison with paroxetine and D-cycloserine.", "entity1": "CRF(1) receptor", "entity2": "paroxetine", "span1": [4, 19], "span2": [140, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9721": {"label": 3, "data": {"text": "This study confirms the feasibility of using continuous measurement of AChE activity in CSF over prolonged periods, that rivastigmine markedly inhibits CSF AChE after a single oral dose of 3 mg, and that the inhibition of central AChE is substantially greater than that of peripheral AChE or BuChE.", "entity1": "AChE", "entity2": "rivastigmine", "span1": [230, 234], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12678": {"label": 1, "data": {"text": "Rofecoxib has greater selectivity for COX-2 than celecoxib, meloxicam, diclofenac and indomethacin.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [38, 43], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13659": {"label": 1, "data": {"text": "The detailed conformational change and 3D structure of the PGIS-bound U46619 were further demonstrated by 2D 1H NMR experiments using the transferred NOE technique.", "entity1": "PGIS", "entity2": "U46619", "span1": [59, 63], "span2": [70, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11573": {"label": 0, "data": {"text": "That observation, together with previous demonstrations of numerous lipid-synthesizing enzymes in myelin, suggests utilization of acetyl groups liberated by myelin-localized ASPA for lipid synthesis within the myelin sheath.", "entity1": "ASPA", "entity2": "acetyl", "span1": [174, 178], "span2": [130, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12746": {"label": 1, "data": {"text": "The results demonstrate that DMI and nisoxetine are persistently retained in cell membranes, at least partly in association with the NET.", "entity1": "NET", "entity2": "nisoxetine", "span1": [133, 136], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10846": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "BCR", "entity2": "Gleevec", "span1": [115, 118], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6267": {"label": 3, "data": {"text": "OBJECTIVES: This study examined the effect of a small-molecule, direct thrombin inhibitor, argatroban, on reperfusion induced by tissue plasminogen activator (TPA) in patients with acute myocardial infarction (AMI).", "entity1": "thrombin", "entity2": "argatroban", "span1": [71, 79], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14958": {"label": 2, "data": {"text": "Bile acids are signaling molecules that activate nuclear receptors, such as farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, and vitamin D receptor, and play a critical role in the regulation of lipid, glucose, energy, and drug metabolism.", "entity1": "farnesoid X receptor", "entity2": "Bile acids", "span1": [76, 96], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7611": {"label": 1, "data": {"text": "In a Phase III trial comparing lapatinib and capecitabine with capecitabine alone in women with HER2-positive, locally advanced breast cancer or MBC that had progressed after treatment with an anthracycline, a taxane, and trastuzumab, the combination of lapatinib and capecitabine was associated with a numeric improvement in response rate compared with capecitabine alone (22% vs 14%, respectively; P = NS) and a significant increase in time to progression (6.2 vs 4.3 months; hazard ratio = 0.57; 95% CI, 0.43-0.77; P < 0.001).", "entity1": "HER2", "entity2": "capecitabine", "span1": [96, 100], "span2": [45, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4392": {"label": 3, "data": {"text": "Second, ICRF-187, a Top2 catalytic inhibitor known to deplete Top2\u03b2, specifically sensitized MEFs to CPT.", "entity1": "Top2", "entity2": "ICRF-187", "span1": [20, 24], "span2": [8, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4074": {"label": 8, "data": {"text": "During early pregnancy in sheep, the elongating conceptus secretes interferon-\u03c4 (IFNT) and the conceptus as well as endometrial epithelia produce prostaglandins (PG) via PG synthase 2 (PTGS2) and cortisol via hydroxysteroid (11-\u03b2) dehydrogenase 1 (HSD11B1).", "entity1": "hydroxysteroid (11-\u03b2) dehydrogenase 1", "entity2": "cortisol", "span1": [209, 246], "span2": [196, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5460": {"label": 3, "data": {"text": "Considerable attention has focused on the antitumor effect of histone deacetylase inhibitor (Trichostatin A, TSA) as well as the coding gene expression-induced apoptosis of cancer cells.", "entity1": "histone deacetylase", "entity2": "TSA", "span1": [62, 81], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2876": {"label": 3, "data": {"text": "AIM: To assess the efficacy and safety of a 24-week treatment with sitagliptin, a highly selective once-daily oral dipeptidyl peptidase-4 (DPP-4) inhibitor, in patients with type 2 diabetes who had inadequate glycaemic control [glycosylated haemoglobin (HbA(1c)) >or=7.5% and <or=10.5%] while on glimepiride alone or in combination with metformin.", "entity1": "dipeptidyl peptidase-4", "entity2": "sitagliptin", "span1": [115, 137], "span2": [67, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9729": {"label": 0, "data": {"text": "Identification of amino acids in the factor XI apple 3 domain required for activation of factor IX.", "entity1": "factor XI apple 3 domain", "entity2": "amino acids", "span1": [37, 61], "span2": [18, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9000": {"label": 4, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "N6-(S-phenylisopropyl)adenosine", "span1": [0, 9], "span2": [61, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4902": {"label": 3, "data": {"text": "A series of pyrido-quinazolines have been synthesised, characterised and tested for their in vitro EGFR tyrosine kinase inhibitory activity.", "entity1": "tyrosine kinase", "entity2": "pyrido-quinazolines", "span1": [104, 119], "span2": [12, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12083": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase", "entity2": "dehydroepiandrosterone", "span1": [0, 72], "span2": [197, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9594": {"label": 3, "data": {"text": "Crystallographic analysis of the human phenylalanine hydroxylase catalytic domain with bound catechol inhibitors at 2.0 A resolution.", "entity1": "human phenylalanine hydroxylase catalytic domain", "entity2": "catechol", "span1": [33, 81], "span2": [93, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2420": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "constitutive nitric-oxide synthase", "entity2": "NO", "span1": [164, 198], "span2": [35, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9825": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "Lck", "entity2": "geldanamycin", "span1": [67, 70], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14151": {"label": 3, "data": {"text": "The agonist activity was antagonized by the selective kappa-opioid blocker nor-binaltorphimine (nor-BNI).", "entity1": "kappa-opioid", "entity2": "nor-binaltorphimine", "span1": [54, 66], "span2": [75, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1539": {"label": 9, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "PAOh1", "entity2": "spermidine", "span1": [9, 14], "span2": [123, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11920": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "ceramides", "span1": [174, 179], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10601": {"label": 3, "data": {"text": "Furthermore, gallium also seems to affect intracellular availability of iron already taken up via this pathway, probably due to its inhibitory activity on vacuolar-type H(+)-ATPases.", "entity1": "vacuolar-type H(+)-ATPases", "entity2": "gallium", "span1": [155, 181], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4725": {"label": 3, "data": {"text": "This study focuses on determining whether treatment of TCDD-exposed UGS organ cultures with RSPO2 and/or RSPO3 is capable of rescuing the inhibitory effects of TCDD on canonical Wnt signaling and prostatic bud formation.", "entity1": "Wnt", "entity2": "TCDD", "span1": [178, 181], "span2": [160, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9189": {"label": 2, "data": {"text": "This agent acts synergistically with many penicillins, such as ampicillin, carbenicillin, and the like, and with cephalosporins, cefazolin, cefamandole, or cefoxitin to inhibit gram-negative bacilli, probably on the basis of binding to different proteins needed for the production of the peptidoglycan of the bacterial cell wall.", "entity1": "peptidoglycan", "entity2": "carbenicillin", "span1": [288, 301], "span2": [75, 88]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10460": {"label": 3, "data": {"text": "Blocking EGFR signaling with the EGFR/HER-2 kinase inhibitor (KI) GW572016 decreased the postradiation survival of irradiated Ras-transformed cells and normal cells but had no effect on the survival of unirradiated cells.", "entity1": "Ras", "entity2": "GW572016", "span1": [126, 129], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9202": {"label": 1, "data": {"text": "Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides.", "entity1": "epidermal growth factor", "entity2": "naphthalene sulfonamides", "span1": [34, 57], "span2": [104, 128]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5316": {"label": 3, "data": {"text": "A series of phosphorylated flavonoids were synthesized and investigated in\u00a0vitro as inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE).", "entity1": "acetylcholinesterase", "entity2": "phosphorylated flavonoids", "span1": [142, 162], "span2": [12, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4256": {"label": 2, "data": {"text": "Repression of farnesyltransferase (FNTA) by siRNA and the enzyme inhibitor manumycin A caused elevation of ApoA-I secretion from hepatocytes and from transgenic mice expressing hApoA-I and cholesterol ester transfer protein transgenes.", "entity1": "ApoA-I", "entity2": "manumycin A", "span1": [107, 113], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4053": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "ASK-1", "entity2": "neoechinulin A", "span1": [187, 192], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12961": {"label": 3, "data": {"text": "Reduction of cerebral infarct size by the AT1-receptor blocker candesartan, the HMG-CoA reductase inhibitor rosuvastatin and their combination.", "entity1": "HMG-CoA reductase", "entity2": "rosuvastatin", "span1": [80, 97], "span2": [108, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5070": {"label": 5, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "GR", "entity2": "RU486", "span1": [68, 70], "span2": [83, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8420": {"label": 3, "data": {"text": "These compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity and 5-amino-2,7-bis(4-methoxyphenyl)-2,3-dihydrobenzo[b]thiophene-4,6-dicarbonitrile was found to be the most potent against AChE with IC50 4.16 \u03bcmol/L.", "entity1": "AChE", "entity2": "5-amino-2,7-bis(4-methoxyphenyl)-2,3-dihydrobenzo[b]thiophene-4,6-dicarbonitrile", "span1": [214, 218], "span2": [93, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11516": {"label": 3, "data": {"text": "The beneficial role of 17beta-estradiol on blood pressure, cardiac hypertrophy, vascular osteopontin expression, perivascular fibrosis, and impaired NO-dependent relaxation of isolated aortic rings was completely abrogated by coadministration of medroxyprogesterone acetate.", "entity1": "osteopontin", "entity2": "medroxyprogesterone acetate", "span1": [89, 100], "span2": [246, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7723": {"label": 3, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LH", "entity2": "goserelin", "span1": [260, 262], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14261": {"label": 8, "data": {"text": "By contrast, 1,12-diamino-3,6,9-triazadodecane(SpmTrien), a charge-deficient spermine analog, was an extremely poor substrate of human recombinant SSAT2 and was metabolized by SSAT1 in HEPG2 cells and in wild-type primary hepatocytes.", "entity1": "SSAT1", "entity2": "SpmTrien", "span1": [176, 181], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6121": {"label": 8, "data": {"text": "The results when considered with previous reports in the literature show that amezinium is about 1000 times more potent and debrisoquine is about 20 times more potent for MAO inhibition in rat lungs than in tissue homogenates, and the reason for their high potencies in the intact lungs is transport and accumulation of the drugs in the pulmonary endothelial cells by uptake1.", "entity1": "uptake1", "entity2": "amezinium", "span1": [368, 375], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13319": {"label": 3, "data": {"text": "All three salicylates inhibited the diabetes-induced translocation of p50 (a subunit of NF-kappaB) into nuclei of retinal vascular endothelial cells of the isolated retinal vasculature, as well as of p50 and p65 into nuclei of cells in the ganglion cell layer and inner nuclear layer on whole-retinal sections.", "entity1": "p50", "entity2": "salicylates", "span1": [70, 73], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11884": {"label": 1, "data": {"text": "The objective of the current study was to investigate the effect of vanadium (V(5+)) on Cyp1 expression and activity in C57BL/6 mice liver and isolated hepatocytes.", "entity1": "Cyp1", "entity2": "V(5+)", "span1": [88, 92], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5829": {"label": 3, "data": {"text": "The compounds identified as 5-LO inhibitors can be divided into antioxidants, substrate-analogous, and a large miscellaneous group of inhibitors, where hydroxamic acids are potent and more selective inhibitors of 5-LO.", "entity1": "5-LO", "entity2": "hydroxamic acids", "span1": [213, 217], "span2": [152, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"797": {"label": 1, "data": {"text": "Lithium modulates desensitization of the glutamate receptor subtype gluR3 in Xenopus oocytes.", "entity1": "glutamate receptor", "entity2": "Lithium", "span1": [41, 59], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"883": {"label": 3, "data": {"text": "Orlistat, a new lipase inhibitor for the management of obesity.", "entity1": "lipase", "entity2": "Orlistat", "span1": [16, 22], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6265": {"label": 1, "data": {"text": "A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study.", "entity1": "tissue plasminogen activator", "entity2": "argatroban", "span1": [75, 103], "span2": [35, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14733": {"label": 1, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "StAR", "entity2": "raisanberine", "span1": [74, 78], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6751": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "RTKs", "entity2": "Imatinib", "span1": [155, 159], "span2": [116, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"100": {"label": 1, "data": {"text": "These results suggest that the beneficial effect of minaprine on cycloheximide-induced amnesia may be related not only to cholinergic but also serotonergic neuronal systems (5-HT2 receptors).", "entity1": "5-HT2 receptors", "entity2": "cycloheximide", "span1": [174, 189], "span2": [65, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6791": {"label": 3, "data": {"text": "CONCLUSIONS AND CLINICAL RELEVANCE: Canine COX-2 was selectively inhibited by etodolac, nimesulide, and NS398; tolfenamic acid and carprofen also appeared to be preferential COX-2 inhibitors in dogs.", "entity1": "Canine COX-2", "entity2": "nimesulide", "span1": [36, 48], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16039": {"label": 3, "data": {"text": "Resulting from this study, a structurally novel class of submicromolar fibrinogen GPIIb/IIIa binding inhibitor bearing 1,2,4-oxadiazol-5(4H)-one moiety is also described.", "entity1": "GPIIb/IIIa", "entity2": "1,2,4-oxadiazol-5(4H)-one", "span1": [82, 92], "span2": [119, 144]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2873": {"label": 1, "data": {"text": "FINDINGS: Compared with other ARBs, candesartan demonstrates the strongest binding affinity to the angiotensin II type 1 receptor.", "entity1": "angiotensin II type 1 receptor", "entity2": "candesartan", "span1": [99, 129], "span2": [36, 47]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"75": {"label": 3, "data": {"text": "Aspirin (ASA) and other non-steroidal anti-inflammatory drugs, which are cyclooxygenase (COX) inhibitors, precipitate asthmatic attacks in ASA-intolerant patients, while sodium salicylate, hardly active on COX by itself, is well tolerated by these patients.", "entity1": "cyclooxygenase", "entity2": "Aspirin", "span1": [73, 87], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12072": {"label": 0, "data": {"text": "Cysteine 360, which was the major adduct accounting for about 90% of the total labeling, is contained within the sequence -WGPTCDGL(I)D-, which is present in all known eukaryote ODCs.", "entity1": "eukaryote ODCs", "entity2": "Cysteine", "span1": [168, 182], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8065": {"label": 3, "data": {"text": "Furthermore, metformin was able to not only decrease the paclitaxel-induced p38 MAPK-mediated ERCC1 expression, but also augment the cytotoxic effect induced by paclitaxel.", "entity1": "p38", "entity2": "metformin", "span1": [76, 79], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1548": {"label": 8, "data": {"text": "The purified human enzyme also does not oxidize eight representative antitumor polyamine analogues; however, specific oligamine analogues were found to be potent inhibitors of the oxidation of spermine by PAOh1/SMO.", "entity1": "SMO", "entity2": "spermine", "span1": [211, 214], "span2": [193, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11863": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "delphinidin", "span1": [118, 143], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13764": {"label": 3, "data": {"text": "Finally, bosutinib is the first kinase inhibitor shown to target CAMK2G, recently implicated in myeloid leukemia cell proliferation.", "entity1": "CAMK2G", "entity2": "bosutinib", "span1": [65, 71], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5319": {"label": 3, "data": {"text": "Furthermore, these phosphorylated flavonoids demonstrated good to high selectivity for CEase over AChE, which only showed micromolar potency inhibition of AChE.", "entity1": "AChE", "entity2": "phosphorylated flavonoids", "span1": [98, 102], "span2": [19, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9002": {"label": 5, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "theophylline", "span1": [0, 9], "span2": [148, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13526": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "CDO", "entity2": "O2", "span1": [22, 25], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12659": {"label": 1, "data": {"text": "This finding, together with the more favorable accumulation of 3H-NMPB in cerebral cortex, hippocampus, and striatum, leads us to conclude that 3H-NMPB, or its positron emitting counterpart, should be the more favorable radiotracer for the estimation of mAch receptor occupancy by cholinergic drugs in the brain.", "entity1": "mAch receptor", "entity2": "3H-NMPB", "span1": [254, 267], "span2": [144, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10040": {"label": 2, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "enoyl-CoA hydratase", "entity2": "GW2331", "span1": [79, 98], "span2": [16, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13895": {"label": 3, "data": {"text": "We determined whether an angiotensin-converting enzyme (ACE) inhibitor, captopril, inhibits MMP-2 activity in peritoneal effluents from patients on CAPD, and simulated molecular models of the MMP-2-captopril complex.", "entity1": "angiotensin-converting enzyme", "entity2": "captopril", "span1": [25, 54], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3901": {"label": 3, "data": {"text": "Ozone plus PM(2.5) exposure, however, induced CRP, IL-6, CK, LDH and MDA increase, SOD and HRV decrease significantly in a dose-response way.", "entity1": "SOD", "entity2": "Ozone", "span1": [83, 86], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15291": {"label": 3, "data": {"text": "Repeated Low Dose Administration of the Monoacylglycerol Lipase Inhibitor JZL184 Retains CB1 Receptor Mediated Antinociceptive and Gastroprotective Effects.", "entity1": "Monoacylglycerol Lipase", "entity2": "JZL184", "span1": [40, 63], "span2": [74, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9801": {"label": 3, "data": {"text": "Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid.", "entity1": "human and rat dihydroorotate dehydrogenase", "entity2": "polyporic acid", "span1": [26, 68], "span2": [126, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11353": {"label": 8, "data": {"text": "Block of human NaV1.5 sodiumsodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin.", "entity1": "sodium channels", "entity2": "sodium", "span1": [28, 43], "span2": [22, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14893": {"label": 2, "data": {"text": "FMO3 expression is induced by dietary bile acids by a mechanism that involves the farnesoid X receptor (FXR), a bile acid-activated nuclear receptor.", "entity1": "farnesoid X receptor", "entity2": "bile acid", "span1": [82, 102], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3104": {"label": 3, "data": {"text": "Clinical utility of acarbose, an alpha-glucosidase inhibitor in cardiometabolic disorders.", "entity1": "alpha-glucosidase", "entity2": "acarbose", "span1": [33, 50], "span2": [20, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15877": {"label": 4, "data": {"text": "In the presence of this inhibitor, the selective D3 agonist PD 128,907 reduced the ED50 for the D1 agonist SKF 38393 from 56 to 4\u00a0nM.", "entity1": "D1", "entity2": "SKF 38393", "span1": [96, 98], "span2": [107, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3696": {"label": 3, "data": {"text": "Tolbutamide and gliclazide block the K(ATP) channel K(ir)6.2/Sur1, causing membrane depolarization and stimulating insulin secretion in pancreatic beta cells.", "entity1": "K(ATP) channel", "entity2": "Tolbutamide", "span1": [37, 51], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4466": {"label": 3, "data": {"text": "Catalpol reduced the expression of pro-inflammatory mediates, such as monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-\u03b1 (TNF-\u03b1), inducible NO synthase (iNOS), and receptor for AGE (RAGE).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "Catalpol", "span1": [110, 133], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13086": {"label": 1, "data": {"text": "Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach.", "entity1": "peroxisome proliferator-activated receptor gamma", "entity2": "glinides", "span1": [35, 83], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6299": {"label": 2, "data": {"text": "5-hydroxytryptamine evokes endothelial nitric oxide synthase activation in bovine aortic endothelial cell cultures.", "entity1": "endothelial nitric oxide synthase", "entity2": "5-hydroxytryptamine", "span1": [27, 60], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15553": {"label": 2, "data": {"text": "Our findings reveal that CdTe-QDs cause oxidative stress, interfere with antioxidant defenses and activate protein kinases, leading to apoptosis via both extrinsic and intrinsic pathways.", "entity1": "kinases", "entity2": "CdTe", "span1": [115, 122], "span2": [25, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"955": {"label": 3, "data": {"text": "Human atrial appendages and rabbit pulmonary arteries were used to determine the potencies of alpha(2)-adrenoceptor agonists in inhibiting the electrically (2 Hz) evoked [(3)H]norepinephrine release and of antagonists in counteracting the alpha(2)-adrenoceptor-mediated inhibition induced by moxonidine.", "entity1": "alpha(2)-adrenoceptor", "entity2": "moxonidine", "span1": [239, 260], "span2": [292, 302]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12682": {"label": 1, "data": {"text": "Different forms of therapy, potassium and magnesium substitution, spironolactone and indomethacin failed to fully correct hypokalemia and hypomagnesemia, but markedly improved growth velocity and normalized IGF-I levels in the three patients with short stature.", "entity1": "IGF-I", "entity2": "potassium", "span1": [207, 212], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15017": {"label": 3, "data": {"text": "Interestingly, AdOx disrupted actin cytoskeleton structures, leading to morphological changes, and suppressed the formation of a signaling complex composed of Src and p85/PI3K, which is linked to various tumorigenic responses.", "entity1": "Src", "entity2": "AdOx", "span1": [159, 162], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9359": {"label": 1, "data": {"text": "Desipramine administration in the olfactory bulbectomized rat: changes in brain beta-adrenoceptor and 5-HT2A binding sites and their relationship to behaviour.", "entity1": "beta-adrenoceptor", "entity2": "Desipramine", "span1": [80, 97], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7619": {"label": 3, "data": {"text": "BACKGROUND: Lapatinib, the first dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases, was approved by the US Food and Drug Administration (FDA) in 2007.", "entity1": "HER2", "entity2": "Lapatinib", "span1": [137, 141], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15839": {"label": 1, "data": {"text": "When the expression of ABCA1 and ABCG1 was induced, 24-OHC efflux was stimulated in the presence of high density lipoprotein (HDL), whereas apolipoprotein A-I was not an efficient acceptor.", "entity1": "high density lipoprotein", "entity2": "24-OHC", "span1": [100, 124], "span2": [52, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4478": {"label": 3, "data": {"text": "In this study, we assessed the effects of clopidogrel and clarithromycin, known CYP2B6 and CYP3A inhibitors, respectively, on the enantioselective disposition of racemic sibutramine in conjunction with CYP2B6 polymorphisms in humans.", "entity1": "CYP2B6", "entity2": "clopidogrel", "span1": [202, 208], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4472": {"label": 3, "data": {"text": "Promoter and electromobility shift assays showed that transcriptional activation of NF-\u03baB was significantly reduced by catalpol treatment, while AP-1 was not.", "entity1": "NF-\u03baB", "entity2": "catalpol", "span1": [84, 89], "span2": [119, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6099": {"label": 3, "data": {"text": "bolus); finally, 8 rabbits received aurintrycarboxilic acid (ATA), an inhibitor of platelet glycoprotein Ib/von Willebrand factor interaction (10 mg/kg i.v.", "entity1": "von Willebrand factor", "entity2": "aurintrycarboxilic acid", "span1": [108, 129], "span2": [36, 59]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12155": {"label": 1, "data": {"text": "Beta 1-adrenergic receptor polymorphisms and antihypertensive response to metoprolol.", "entity1": "Beta 1-adrenergic receptor", "entity2": "metoprolol", "span1": [0, 26], "span2": [74, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1762": {"label": 9, "data": {"text": "CGP 12177A but not isoprenaline initiated arrhythmias at lower concentrations following beta(1)-adrenoceptor overexpression.", "entity1": "beta(1)-adrenoceptor", "entity2": "isoprenaline", "span1": [88, 108], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6847": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "A1298C", "entity2": "Hcy", "span1": [136, 142], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8408": {"label": 3, "data": {"text": "Secondary point mutations in the Fms-like tyrosine kinase 3 (FLT3) tyrosine kinase domain (KD) are common causes of acquired clinical resistance to the FLT3 inhibitors AC220 (quizartinib) and sorafenib.", "entity1": "FLT3", "entity2": "AC220", "span1": [152, 156], "span2": [168, 173]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"783": {"label": 3, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "COX-2", "entity2": "sulindac sulfide", "span1": [92, 97], "span2": [62, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13495": {"label": 2, "data": {"text": "The sibutramine group showed significant retardation in gastric emptying of solids (P = .03), reduced maximum tolerated volume (P = .03), and increased postprandial peptide YY compared with the placebo group.", "entity1": "peptide YY", "entity2": "sibutramine", "span1": [165, 175], "span2": [4, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12313": {"label": 1, "data": {"text": "In an effort to understand the shedding process of AChE, we have used several pharmacological treatments, which showed that it is likely to be mediated in part by an EDTA- and batimastat-sensitive, but GM6001-insensitive metalloprotease, with the possible additional involvement of a thiol isomerase.", "entity1": "AChE", "entity2": "EDTA", "span1": [51, 55], "span2": [166, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2915": {"label": 3, "data": {"text": "The pharmacology of NCX inhibitors has been studied extensively since the development of KB-R7943, a prototype benzyloxyphenyl NCX inhibitor, in 1996.", "entity1": "NCX", "entity2": "KB-R7943", "span1": [127, 130], "span2": [89, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13530": {"label": 1, "data": {"text": "Characterization of the nitrosyl adduct of substrate-bound mouse cysteine dioxygenase by electron paramagnetic resonance: electronic structure of the active site and mechanistic implications.", "entity1": "mouse cysteine dioxygenase", "entity2": "nitrosyl", "span1": [59, 85], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3507": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "AKRs", "entity2": "oxygen", "span1": [22, 26], "span2": [167, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8274": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "CYP3A4", "entity2": "N", "span1": [91, 97], "span2": [10, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4028": {"label": 3, "data": {"text": "Several inhibitors of Lp-PLA(2) have been described, including darapladib, which is currently in phase 3 clinical development for the treatment of atherosclerosis.", "entity1": "Lp-PLA(2)", "entity2": "darapladib", "span1": [22, 31], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7244": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "TYR", "span1": [192, 229], "span2": [76, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3538": {"label": 2, "data": {"text": "Exposure to Cu NPs decreased cell viability to 73% (p<0.01) and significantly (p<0.05) elevated levels of lactate dehydrogenase, intracellular reactive oxygen species and interleukin-8 that mirrored our findings from subacute in vivo inhalation studies in mice.", "entity1": "lactate dehydrogenase", "entity2": "Cu", "span1": [106, 127], "span2": [12, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"119": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited the actin-activated Mg2+-ATPase activity of smooth muscle myosin (IC50 = 25.1 microM).", "entity1": "myosin", "entity2": "p-chloro", "span1": [105, 111], "span2": [19, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8935": {"label": 0, "data": {"text": "Both these MAPs were found to have two to three binding sites for estramustine phosphate which is compatible with the reported number of basic amino acid repeats of these MAPs, considered to be the ultimate tubulin binding domains.", "entity1": "tubulin", "entity2": "amino acid", "span1": [207, 214], "span2": [143, 153]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7030": {"label": 1, "data": {"text": "Further, cholesterol metabolites, predominantly the oxysterols, the natural ligands for liver X receptor (LXR), induced these genes via upregulation of sterol regulatory element binding protein-1c (SREBP-1c) that bound to the regulatory regions of these genes.", "entity1": "liver X receptor", "entity2": "oxysterols", "span1": [88, 104], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14273": {"label": 8, "data": {"text": "We recently showed that TETA is metabolized in vitro by polyamine catabolic enzyme spermidine/spermine-N(1)-acetyltransferase (SSAT1) and by thialysine acetyltransferase (SSAT2) to its monoacetylated derivative (MAT).", "entity1": "thialysine acetyltransferase", "entity2": "TETA", "span1": [141, 169], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9440": {"label": 8, "data": {"text": "The hydrolysis of fluorescein diphosphate by PTP epsilon and PTPmeg1 was sensitive to alendronate, with IC50 values of less than 1 microM; PTPsigma, however, under the same conditions, was inhibited by only 50% with 141 microM alendronate.", "entity1": "PTP epsilon", "entity2": "diphosphate", "span1": [45, 56], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4337": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "c-Src", "entity2": "Pinosylvin", "span1": [106, 111], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10582": {"label": 3, "data": {"text": "CONCLUSION: Imidapril and irbesartan can not only control blood pressure but also inhibit mesenteric arteries remodeling and mRNA expression of TGF-beta1, c-Jun in SHR.", "entity1": "c-Jun", "entity2": "Imidapril", "span1": [155, 160], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"310": {"label": 5, "data": {"text": "In contrast, the D-1997-induced responses were potently and concentration-dependently antagonized by the mixed 5-HT1-like and 5-HT2 receptor antagonist methiothepin (0.01-1 microM).", "entity1": "5-HT2 receptor", "entity2": "methiothepin", "span1": [126, 140], "span2": [152, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1608": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE2", "entity2": "DMA", "span1": [113, 117], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7385": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "PRODH", "entity2": "glutamate", "span1": [23, 28], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3395": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "VMAT2", "entity2": "COC", "span1": [234, 239], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6794": {"label": 3, "data": {"text": "CONCLUSIONS AND CLINICAL RELEVANCE: Canine COX-2 was selectively inhibited by etodolac, nimesulide, and NS398; tolfenamic acid and carprofen also appeared to be preferential COX-2 inhibitors in dogs.", "entity1": "COX-2", "entity2": "carprofen", "span1": [174, 179], "span2": [131, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12680": {"label": 1, "data": {"text": "Rofecoxib has greater selectivity for COX-2 than celecoxib, meloxicam, diclofenac and indomethacin.", "entity1": "COX-2", "entity2": "indomethacin", "span1": [38, 43], "span2": [86, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5257": {"label": 2, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "CIP1", "entity2": "rofecoxib", "span1": [105, 109], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5366": {"label": 1, "data": {"text": "Potent and selective: The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity.", "entity1": "Pim", "entity2": "ATP", "span1": [79, 82], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"939": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "F3(d)Thd", "span1": [238, 240], "span2": [82, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2807": {"label": 8, "data": {"text": "In addition, cells pre-treated with DL-propargylglycine (PAG, 3 mM), a CSE inhibitor, reduced the formation of H(2)S in caerulein treated cells, suggesting that CSE may be the main enzyme involved in H(2)S formation in mouse acinar cells.", "entity1": "CSE", "entity2": "H(2)S", "span1": [161, 164], "span2": [200, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4932": {"label": 2, "data": {"text": "Little is known in terms of multi-matrix cytochrome P450 activity induction under repeated oral exposure to planar halogenated and polycyclic aromatic hydrocarbons (PHH, PAH).", "entity1": "cytochrome P450", "entity2": "PAH", "span1": [41, 56], "span2": [170, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11621": {"label": 8, "data": {"text": "We isolated partial cDNAs that codified for enzymes implicated in the anthocyanin biosynthesis such as l-phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS), and an antioxidant enzyme such as ascorbate peroxidase (APX).", "entity1": "CHS", "entity2": "anthocyanin", "span1": [162, 165], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12349": {"label": 8, "data": {"text": "In contrast, flunisolide was only metabolized via CYP3A4, with no significant turnover by CYP3A5 or CYP3A7.", "entity1": "CYP3A4", "entity2": "flunisolide", "span1": [50, 56], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1021": {"label": 1, "data": {"text": "In COS cells transfected with alpha(1b) adrenoceptor cDNA and in DDT(1) MF-2 cells which express native alpha(1B) adrenoceptors, [(3)H]-prazosin was displaced by unlabelled prazosin in a normal equilibrium process, with no prazosin paradox in concentrations up to 10(-6) M. In DDT(1) MF-2 cells, [(3)H]-prazosin was displaced likewise by a series of alpha(1) adrenergic agonists, none of which increased the binding of [(3)H]-prazosin.", "entity1": "alpha(1)", "entity2": "[(3)H]-prazosin", "span1": [350, 358], "span2": [419, 434]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15183": {"label": 2, "data": {"text": "Moreover, compared with the model group, sophocarpine could significantly increase P-AMPK\u03b1 (>5.82-fold), AMPK\u03b1 (>1.29-fold) and ACC (>3.27-fold) protein expressions, and reduce P-ACC (<0.30-fold) and HNF-4\u03b1 (<0.20-fold) protein expression.", "entity1": "P-AMPK\u03b1", "entity2": "sophocarpine", "span1": [83, 90], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9417": {"label": 5, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT2", "entity2": "cinitapride", "span1": [172, 177], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11257": {"label": 0, "data": {"text": "Ntp and Ctp, synthetic peptides based on the N- and C-terminal sequences of K(IR)6.0, respectively, were used to probe gating of K(IR)6.0/SUR K(ATP) channels.", "entity1": "K(IR)6.0", "entity2": "C", "span1": [76, 84], "span2": [52, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5051": {"label": 0, "data": {"text": "Intravenous treatment, during coronary artery occlusion, with the melanocortin analogs [Nle(4), D-Phe(7)]\u03b1-melanocyte-stimulating hormone (NDP-\u03b1-MSH) and adrenocorticotropic hormone 1-24 [ACTH-(1-24)], induced a left ventricle up-regulation of pJAK2, pERK1/2 and pTyr-STAT3 (JAK-dependent), and a reduction in pJNK and TNF-\u03b1 levels; these effects of NDP-\u03b1-MSH and ACTH-(1-24) were associated with over-expression of the pro-survival proteins HO-1 and Bcl-XL, and marked decrease of the myocardial infarct size.", "entity1": "\u03b1-MSH", "entity2": "D-Phe", "span1": [143, 148], "span2": [96, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7823": {"label": 2, "data": {"text": "Cellular release of AChE by SH-SY5Y is significantly enhanced by the muscarinic acetylcholine receptor (mAChR) agonists carbachol or muscarine, with the effect of carbachol blocked by the mAChR antagonist atropine.", "entity1": "AChE", "entity2": "carbachol", "span1": [20, 24], "span2": [120, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3935": {"label": 2, "data": {"text": "The reactivation of brain AChE inhibited with tabun demonstrated better activity of new compound BT-07-4M, TMB-4 and obidoxime from symmetric oximes, and BT-05 and BT-03 possessing asymmetric structure.", "entity1": "AChE", "entity2": "oximes", "span1": [26, 30], "span2": [142, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5714": {"label": 3, "data": {"text": "Indomethacin, used to inhibit cyclooxygenase, also inhibits AKR1C3 and displays selectivity over AKR1C1/AKR1C2.", "entity1": "AKR1C3", "entity2": "Indomethacin", "span1": [60, 66], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14765": {"label": 3, "data": {"text": "These data suggest that jaceosidin, isolated from Japanese mugwort, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells.", "entity1": "cyclin B1", "entity2": "jaceosidin", "span1": [142, 151], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2962": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "Y612F", "entity2": "cGMP", "span1": [64, 69], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3964": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "peptidyl-prolyl cis/trans-isomerase A1", "entity2": "pSer", "span1": [26, 64], "span2": [136, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"13739": {"label": 8, "data": {"text": "Nicotinamide N-methyltransferase (NNMT) catalyses the conversion of nicotinamide to 1-methylnicotinamide and plays an important role in hepatic detoxification reactions.", "entity1": "NNMT", "entity2": "nicotinamide", "span1": [34, 38], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"2489": {"label": 3, "data": {"text": "Moreover, licofelone inhibited COX-2 and 5-LOX protein expression in vascular lesions.", "entity1": "COX-2", "entity2": "licofelone", "span1": [31, 36], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7463": {"label": 8, "data": {"text": "The mechanisms that specify the vesicular phenotype of inhibitory interneurons in vertebrates are poorly understood because the two main inhibitory transmitters, glycine and GABA, share the same vesicular inhibitory amino acid transporter (VIAAT) and are both present in neurons during postnatal development.", "entity1": "VIAAT", "entity2": "glycine", "span1": [240, 245], "span2": [162, 169]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"4791": {"label": 8, "data": {"text": "Concentration-dependent inhibitory effects of baicalin on the metabolism of dextromethorphan, a dual probe of CYP2D and CYP3A, in rats.", "entity1": "CYP3A", "entity2": "dextromethorphan", "span1": [120, 125], "span2": [76, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1576": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "butyrylcholinesterase", "entity2": "[1,8]naphthyridines", "span1": [36, 57], "span2": [135, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6338": {"label": 1, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "candesartan cilexetil", "span1": [18, 21], "span2": [257, 278]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3795": {"label": 3, "data": {"text": "Moreover, use of the pharmacological AMP-activated protein kinase (AMPK) inhibitor compound C revealed that AMPK is essential for suppressing SREBP-1c expression in phillyrin-treated cells.", "entity1": "AMPK", "entity2": "compound C", "span1": [67, 71], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9740": {"label": 1, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "h5-HT(1A)", "entity2": "(35)S", "span1": [163, 172], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4654": {"label": 3, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [204, 210], "span2": [163, 175]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4212": {"label": 3, "data": {"text": "In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OST\u03b2, and a down-regulation of CYP27A1.", "entity1": "CYP27A1", "entity2": "GW4064", "span1": [136, 143], "span2": [66, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12813": {"label": 3, "data": {"text": "Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values.", "entity1": "HIF-1alpha", "entity2": "carvedilol", "span1": [60, 70], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4768": {"label": 3, "data": {"text": "Furthermore, BRN-250 inhibited the VEGF-induced phosphorylation and intracellular tyrosine kinase activity of VEGF receptor 2 (VEGFR2) and the activation of its downstream AKT pathway.", "entity1": "AKT", "entity2": "BRN-250", "span1": [172, 175], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10019": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Arg", "span1": [126, 138], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7543": {"label": 3, "data": {"text": "To determine whether a metabolite formed by the action of MAO on PLZ may be responsible for the elevation in brain ORN observed, animals were pretreated with vehicle or the MAO inhibitor tranylcypromine (TCP) before vehicle or PLZ (15 mg/kg), and brains collected 3 h later.", "entity1": "MAO", "entity2": "TCP", "span1": [173, 176], "span2": [204, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12266": {"label": 0, "data": {"text": "Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function.", "entity1": "amylin receptor", "entity2": "N", "span1": [141, 156], "span2": [18, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14038": {"label": 4, "data": {"text": "Unexpectedly, both the mGluR(5)specific agonist, CHPG, and the group II mGluR (mGlu(2/3)) agonist, LY379268 (LY), induced a TTX-insensitive outward current/hyperpolarization.", "entity1": "mGluR(5)", "entity2": "CHPG", "span1": [23, 31], "span2": [49, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12523": {"label": 1, "data": {"text": "However, 5'-(N-cyclopropyl)-carboxamidoadenosine data indicate complexity of the mechanism(s) and point toward an additional involvement of a yet unknown subtype of adenosine A2.", "entity1": "adenosine A2", "entity2": "5'-(N-cyclopropyl)-carboxamidoadenosine", "span1": [165, 177], "span2": [9, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8898": {"label": 4, "data": {"text": "The preferential alpha 2A-adrenoceptor partial agonist, guanfacine, partially inhibited UK 14,304-induced antinociception.", "entity1": "alpha 2A-adrenoceptor", "entity2": "UK 14,304", "span1": [17, 38], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3688": {"label": 2, "data": {"text": "Insulin secretion stimulated by both 200 \u03bcM tolbutamide and 20 \u03bcM gliclazide, concentrations that had equivalent effects on membrane potential, was inhibited by thapsigargin (1 \u03bcM) or the L-type Ca(2+) channel blocker nicardipine (2 \u03bcM) and was potentiated by 8-pCPT-2'-O-Me-cAMP-AM at concentrations \u22652 \u03bcM in INS-1 cells.", "entity1": "Insulin", "entity2": "gliclazide", "span1": [0, 7], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10883": {"label": 9, "data": {"text": "To understand this interaction, we determined the crystal structure of PDXK in complex with (R)-roscovitine, N6-methyl-(R)-roscovitine, and O6-(R)-roscovitine, the two latter derivatives being designed to bind to PDXK but not to CDKs.", "entity1": "CDKs", "entity2": "N6-methyl-(R)-roscovitine", "span1": [229, 233], "span2": [109, 134]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11943": {"label": 1, "data": {"text": "Finally, molecular modeling and (1)H- and (13)C-NMR studies performed on compounds 6c,d, 9c, and 10b allowed the right conformation of nitrooxyalkyl ester and ether side chain of these molecules within the COX-2 active site to be assessed.", "entity1": "COX-2", "entity2": "nitrooxyalkyl ester and ether", "span1": [206, 211], "span2": [135, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14520": {"label": 3, "data": {"text": "PAK1 expression was elevated in APC(min) polyps and 5-ASA treatment reduced its expression.", "entity1": "PAK1", "entity2": "5-ASA", "span1": [0, 4], "span2": [52, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5621": {"label": 8, "data": {"text": "Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M.", "entity1": "HERG", "entity2": "K+", "span1": [36, 40], "span2": [41, 43]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2968": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "L765A", "entity2": "vardenafil", "span1": [78, 83], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2443": {"label": 9, "data": {"text": "In healthy rats, ATB-429 dose dependently (25, 50, or 100 mg/kg) attenuated CRD-induced hypersensitivity and significantly inhibited CRD-induced overexpression of spinal c-FOS mRNA, whereas mesalamine had no effect.", "entity1": "c-FOS", "entity2": "mesalamine", "span1": [170, 175], "span2": [190, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6200": {"label": 5, "data": {"text": "administration of the non-selective muscarinic receptor antagonist atropine (ID50 = 1.45 microg), the muscarinic M1 receptor antagonist pirenzepine (ID50 = 4.33 microg), the muscarinic M2 receptor antagonist methoctramine (ID50 = 1.39 microg) and the muscarinic M3 receptor antagonist para-fluoro-hexahydro-sila-difenidol (ID50 = 31.19 microg).", "entity1": "muscarinic M2 receptor", "entity2": "methoctramine", "span1": [174, 196], "span2": [208, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2050": {"label": 0, "data": {"text": "The kinetic parameters indicate that the main effect of the mutation of Arg228 to lysine is on the k(cat) of Glc-T, which increases 3-4-fold, both in the absence and in the presence of LA; simultaneously, the k(cat) for the Gal-T reaction is reduced 30-fold.", "entity1": "Glc-T", "entity2": "lysine", "span1": [109, 114], "span2": [82, 88]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3736": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates (N-BPs) induce apoptosis in tumor cells by inhibiting the prenylation of small G-proteins.", "entity1": "G-proteins", "entity2": "Nitrogen", "span1": [115, 125], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4729": {"label": 1, "data": {"text": "In lymphoblastoid cells induced to undergo endoplasmic reticulum (ER) stress by treatment of tunicamycin, higher fold change of TCF7L2 and VEGFA mRNA levels were observed in rs7903146-TT cells than that in rs7903146-CC cells (P = 0.02 for TCF7L2; P = 0.004 for VEGFA), suggesting ER stress plays a role in PDR pathogenesis.", "entity1": "VEGFA", "entity2": "tunicamycin", "span1": [139, 144], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1739": {"label": 3, "data": {"text": "On the other hand, in patients with a mean serum carvedilol level (Cmin) of less than 2.5 nmol/l up to 2 weeks after the start ofcarvedilol therapy, the degree of reduction in the BNP value after the 3rd month was significantly larger, relative to the patient group with Cmin over 2.5 nmol/l.", "entity1": "BNP", "entity2": "carvedilol", "span1": [180, 183], "span2": [129, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15460": {"label": 3, "data": {"text": "Benzenesulfonamides: a unique class of chemokine receptor type 4 inhibitors.", "entity1": "chemokine receptor type 4", "entity2": "Benzenesulfonamides", "span1": [39, 64], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8825": {"label": 3, "data": {"text": "Exhibiting unique properties over other MMPIs (e.g., hydroxamates), these newly reported compounds are capable of modulating activities of several MMPs in the low nanomolar range, including MMP-2 (~2 to 50 nM), MMP-13 (~2 to 50 nM), and MMP-14 (~4 to 60 nM).", "entity1": "MMP-13", "entity2": "hydroxamates", "span1": [211, 217], "span2": [53, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6664": {"label": 2, "data": {"text": "RESULTS: Eprosartan tended to lower mean AP, it slightly increased heart rate (HR) (p<0.05), and markedly increased circulating Ang-II levels (p<0.01).", "entity1": "Ang-II", "entity2": "Eprosartan", "span1": [128, 134], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4499": {"label": 9, "data": {"text": "Time-dependent inactivation of hCES1 by diclofenac-\u03b2-d-glucuronide was not observed.", "entity1": "hCES1", "entity2": "diclofenac-\u03b2-d-glucuronide", "span1": [31, 36], "span2": [40, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3523": {"label": 8, "data": {"text": "Multidrug resistance-associated proteins are involved in the transport of the glutathione conjugates of the ultimate carcinogen of benzo[a]pyrene in human Caco-2 cells.", "entity1": "Multidrug resistance-associated proteins", "entity2": "glutathione", "span1": [0, 40], "span2": [78, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6342": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "valsartan", "span1": [25, 28], "span2": [222, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8144": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "cytochrome-C-oxidase", "entity2": "Isoproterenol", "span1": [387, 407], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4163": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "NF-\u03baB", "entity2": "rocaglate", "span1": [173, 178], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12102": {"label": 1, "data": {"text": "By contrast, the closely related bovine ether-a-go-go channel (BEAG) is 100-fold less sensitive to dofetilide.", "entity1": "BEAG", "entity2": "dofetilide", "span1": [63, 67], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3597": {"label": 0, "data": {"text": "Interestingly, recent crystallographic evidence identified that ifenprodil, unlike zinc, binds at the interface of the GluN1/GluN2B amino terminal domain dimer by an induced-fit mechanism.", "entity1": "GluN2B", "entity2": "amino", "span1": [125, 131], "span2": [132, 137]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15687": {"label": 3, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Cdc25c", "entity2": "EVn-50", "span1": [284, 290], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15304": {"label": 9, "data": {"text": "Catalase, glutathione-S-transferase and xanthine oxidase activities were not altered by atorvastatin treatment or withdrawal, as well as protein carbonyl and 4-hydroxy-2-nonenal immunoreactivity.", "entity1": "Catalase", "entity2": "atorvastatin", "span1": [0, 8], "span2": [88, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"974": {"label": 3, "data": {"text": "These results indicate that U50,488H-induced down-regulation of the hkor involves GRK-, arrestin-2-, dynamin-, rab5-, and rab7-dependent mechanisms and receptors seem to be trafficked to lysosomes and proteasomes for degradation.", "entity1": "hkor", "entity2": "U50,488H", "span1": [68, 72], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11562": {"label": 3, "data": {"text": "In HEK293 cells stably transfected with FLT3-WT or FLT3-ITD, sorafenib blocked basal and ligand dependent FLT3-mediated tyrosine autophosphorylation as well as extracellular signal-regulated kinase1/2 and Stat5 phosphorylation.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [106, 110], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11809": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "c-jun", "entity2": "PhIP", "span1": [131, 136], "span2": [63, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6319": {"label": 3, "data": {"text": "Inhibition of ATM provides a molecular explanation of the attenuation of DNA-damage checkpoint responses and for the increased radiosensitivity of caffeine-treated cells [6] [7] [8].", "entity1": "ATM", "entity2": "caffeine", "span1": [14, 17], "span2": [147, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7262": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "dichlorophenamide", "span1": [218, 224], "span2": [85, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3235": {"label": 1, "data": {"text": "Serotonin transporter (SERT) has been associated with drugs of abuse like d-methamphetamine (METH).", "entity1": "Serotonin transporter", "entity2": "d-methamphetamine", "span1": [0, 21], "span2": [74, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3994": {"label": 8, "data": {"text": "Aldose reductase (AR) catalyzes the reduction of toxic lipid aldehydes to their alcohol products and mediates inflammatory signals triggered by lipopolysaccharide (LPS).", "entity1": "Aldose reductase", "entity2": "alcohol", "span1": [0, 16], "span2": [80, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"14617": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala70Thr", "entity2": "2',2'-difluorodeoxyuridine", "span1": [52, 60], "span2": [255, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15841": {"label": 1, "data": {"text": "To confirm the role of each transporter, we analyzed HEK293 cells stably expressing human ABCA1 or ABCG1; we clearly observed 24-OHC efflux in the presence of HDL, whereas efflux in the presence of apolipoprotein A-I was marginal.", "entity1": "HDL", "entity2": "24-OHC", "span1": [159, 162], "span2": [126, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8347": {"label": 8, "data": {"text": "Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine.", "entity1": "HDC", "entity2": "histamine", "span1": [25, 28], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3486": {"label": 2, "data": {"text": "On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-\u03b3, GLUT-4 and adiponectin.", "entity1": "GLUT-4", "entity2": "gentianine", "span1": [166, 172], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14022": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "NF-kappaBalpha", "entity2": "colchicoside", "span1": [200, 214], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3378": {"label": 5, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "L-VGCC", "entity2": "dihydropyridine", "span1": [123, 129], "span2": [101, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1934": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "CrAT", "entity2": "myristoyl-CoA", "span1": [155, 159], "span2": [93, 106]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9578": {"label": 5, "data": {"text": "The selective beta1AR antagonist atenolol (0.3 x 10(-6) M) did not have any effect.", "entity1": "beta1AR", "entity2": "atenolol", "span1": [14, 21], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5738": {"label": 1, "data": {"text": "These data provided a novel insight to the mechanisms of Rg1protective effects on A\u03b225-35-induced endothelial cells apoptosis, suggesting that GR-ERK signaling pathway might play an important role in it.", "entity1": "GR", "entity2": "Rg1", "span1": [143, 145], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15339": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "2-ethynylnaphthalene", "span1": [39, 48], "span2": [109, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1329": {"label": 1, "data": {"text": "Eprosartan acts not only at vascular AT1 receptors but also at presynaptic AT1 receptors, causing inhibition of sympathetically stimulated noradrenaline release.", "entity1": "AT1", "entity2": "Eprosartan", "span1": [37, 40], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4864": {"label": 2, "data": {"text": "Saturated palmitic and stearic acids increased ceramides, up-regulated PTP1B, and had AKt and PTP1B phosphorylation at Ser 50 impaired.", "entity1": "AKt", "entity2": "palmitic and stearic acids", "span1": [86, 89], "span2": [10, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15555": {"label": 1, "data": {"text": "A low molecular weight polyethyleneimine modified with deoxycholic acid (PEI1.8-DA)-based delivery strategy was suggested for the cardiac application of SHP-1 siRNA to overcome the poor gene delivery efficiency to myocardium due to the highly charged structures of the compact cardiac muscles.", "entity1": "SHP-1", "entity2": "polyethyleneimine", "span1": [153, 158], "span2": [23, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11361": {"label": 1, "data": {"text": "The estimated plasma ziprasidone concentration associated with 50% maximal 5-HT(2) receptor occupancy was almost four times lower than that for D(2) receptor occupancy.", "entity1": "D(2) receptor", "entity2": "ziprasidone", "span1": [144, 157], "span2": [21, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13026": {"label": 1, "data": {"text": "11Beta-HSD1 activates cortisone to cortisol to facilitate glucocorticoid receptor (GR)-mediated action.", "entity1": "glucocorticoid receptor", "entity2": "cortisol", "span1": [58, 81], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3559": {"label": 3, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "p65", "entity2": "pranlukast", "span1": [56, 59], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4189": {"label": 2, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "Bax", "entity2": "PTE", "span1": [200, 203], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4699": {"label": 2, "data": {"text": "V(5+) also increased serum hemoglobin (Hb) levels in animals treated for 24\u00a0h. Upon treatment of isolated hepatocytes with Hb alone or in the presence of TCDD, there was an increase in the AhR-dependent luciferase activity.", "entity1": "serum hemoglobin", "entity2": "V(5+)", "span1": [21, 37], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15866": {"label": 1, "data": {"text": "These experiments show that in striatonigral projections, CaMKII\u03b1 inhibits the action of D3 receptors in a Ca(2+) dependent manner blocking their modulatory effects on GABA release.", "entity1": "D3 receptors", "entity2": "Ca(2+)", "span1": [89, 101], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9051": {"label": 1, "data": {"text": "Chlorpromazine, levomepromazine, and their metabolites had 5-30 times higher binding affinities for muscarinic cholinergic receptors than fluphenazine, perphenazine and their metabolites.", "entity1": "muscarinic cholinergic receptors", "entity2": "fluphenazine", "span1": [100, 132], "span2": [138, 150]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14584": {"label": 3, "data": {"text": "P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL.", "entity1": "SYK", "entity2": "P505-15", "span1": [31, 34], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7692": {"label": 1, "data": {"text": "A PKC or MAP kinase inhibitor blocked the inhibitory effect of fenoldopam on insulin receptor expression, indicating that PKC and MAP kinase were involved in the signaling pathway.", "entity1": "MAP kinase", "entity2": "fenoldopam", "span1": [130, 140], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13990": {"label": 3, "data": {"text": "Importantly, treatment with cabozantinib did not increase lung tumor burden in an experimental model of metastasis, which has been observed with inhibitors of VEGF signaling that do not target MET.", "entity1": "VEGF", "entity2": "cabozantinib", "span1": [159, 163], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5768": {"label": 3, "data": {"text": "NSDA neurons displayed significant axon terminal degeneration (as indexed by decreases in DA, tyrosine hydroxylase (TH) and DA transporter concentrations in the striatum) as well as loss of TH-immunoreactive (IR) neurons in the substantia nigra (SN) following MPTP, whereas TIDA neurons revealed no overt axon terminal pathology or loss of TH-IR cell bodies.", "entity1": "TH", "entity2": "MPTP", "span1": [116, 118], "span2": [260, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2370": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "ERK", "entity2": "BAY 43-9006", "span1": [79, 82], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7511": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMP-activated protein kinase", "entity2": "metformin", "span1": [24, 52], "span2": [76, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15228": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "TNF- \u03b1", "entity2": "CLS", "span1": [365, 371], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9205": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "epidermal growth factor", "entity2": "W-7", "span1": [236, 259], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16008": {"label": 1, "data": {"text": "The preventive effect of uncarboxylated osteocalcin against free fatty acid-induced endothelial apoptosis through the activation of phosphatidylinositol 3-kinase/Akt signaling pathway: Uncarboxylated osteocalcin and endothelial apoptosis.", "entity1": "Akt", "entity2": "free fatty acid", "span1": [162, 165], "span2": [60, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8945": {"label": 9, "data": {"text": "Unlike bacterial 3-keto-5-ene-steroid isomerase, the human isomerase reaction is stimulated by diphosphopyridine nucleotides (NADH, NAD+).", "entity1": "3-keto-5-ene-steroid isomerase", "entity2": "NADH", "span1": [17, 47], "span2": [126, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10865": {"label": 4, "data": {"text": "Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.", "entity1": "H4 receptor", "entity2": "4-methylhistamine", "span1": [164, 175], "span2": [112, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11266": {"label": 3, "data": {"text": "and cantharidin (1 microg/mouse, i.c.v. ), which also block PP1, and calyculin-A (0.1 fg/mouse-1 ng/mouse, i.c.v.", "entity1": "PP1", "entity2": "cantharidin", "span1": [60, 63], "span2": [4, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12361": {"label": 8, "data": {"text": "Regulation of multiple adenylyl cyclases (AC) provides unique inputs to mediate the synthesis of cAMP, a ubiquitous second messenger that controls many aspects of cellular function.", "entity1": "AC", "entity2": "cAMP", "span1": [42, 44], "span2": [97, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15595": {"label": 3, "data": {"text": "Biological evaluation revealed that most tested compounds were potent dipeptidyl peptidase 4 (DPP-4) inhibitors, among them, the cyclopropyl-substituted phenylalanine derivative 11h displayed the most potent DPP-4 inhibitory activity with an IC50 value of 0.247 \u03bcM.", "entity1": "DPP-4", "entity2": "cyclopropyl-substituted phenylalanine", "span1": [208, 213], "span2": [129, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13479": {"label": 1, "data": {"text": "It has been claimed that partial agonism of the dopamine D(2) and 5-HT(1A) receptors and antagonism of the 5-HT(2) receptor contribute to the clinical profile of aripiprazole, a so-called dopamine- and 5-HT stabiliser.", "entity1": "5-HT(2)", "entity2": "aripiprazole", "span1": [107, 114], "span2": [162, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13047": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "RALDH2", "entity2": "retinol", "span1": [213, 219], "span2": [99, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4815": {"label": 1, "data": {"text": "Taken together, we conclude that the thiourea series of compounds share a similar cellular mechanism that includes interaction with LolA in addition to the well-characterized target MreB.", "entity1": "LolA", "entity2": "thiourea", "span1": [132, 136], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4396": {"label": 0, "data": {"text": "The M6P (mannose 6-phosphate)/IGF2R (insulin-like growth factor II receptor) interacts with a variety of factors that impinge on tumour invasion and metastasis.", "entity1": "IGF2R", "entity2": "mannose 6-phosphate", "span1": [30, 35], "span2": [9, 28]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"529": {"label": 2, "data": {"text": "In a further study to analyse the downstream mediator of Rac in the ceramide-signalling pathway, we observed that either pretreatment with mepacrine, a potent and specific inhibitor of phospholipase A2, or co-transfection with antisense cytosolic phospholipase A2 (cPLA2) oligonucleotide repressed the C2-ceramide-induced SRE activation selectively, implying a critical role of cPLA2 in C2-ceramide-induced signalling to nucleus.", "entity1": "SRE", "entity2": "C2-ceramide", "span1": [322, 325], "span2": [302, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9019": {"label": 1, "data": {"text": "The mitogenic effect of DHT on bone cells was inhibited by antiandrogens (hydroxyflutamide and cyproterone acetate) which compete for binding to the androgen receptor.", "entity1": "androgen receptor", "entity2": "DHT", "span1": [149, 166], "span2": [24, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8440": {"label": 2, "data": {"text": "HENA activated the BK (cbv1 + \u03b21) channels cloned from rat cerebral artery myocytes with a potency (EC50 = 53 \u03bcM) similar to and an efficacy (\u00d72.5 potentiation) significantly greater than that of LCA.", "entity1": "BK (cbv1 + \u03b21) channels", "entity2": "LCA", "span1": [19, 42], "span2": [196, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1917": {"label": 0, "data": {"text": "We show for the first time that a single amino acid is able to determine the substrate specificity of CrAT and COT.", "entity1": "COT", "entity2": "amino acid", "span1": [111, 114], "span2": [41, 51]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8253": {"label": 1, "data": {"text": "Results indicate that 5-HT2C receptor agonists and antagonists attenuate the DOI-elicited-HTR in C57Bl/6J mice, and suggest that structurally diverse 5-HT2C ligands result in different 5-HT2C receptor signaling outcomes compared to DOI.", "entity1": "5-HT2C", "entity2": "DOI", "span1": [150, 156], "span2": [232, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1787": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1bAR", "entity2": "terazosin", "span1": [85, 94], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2796": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "SP", "entity2": "caerulein", "span1": [75, 77], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4388": {"label": 1, "data": {"text": "In this study, we have identified topoisomerase II\u03b2 (Top2\u03b2) as a specific determinant for CPT sensitivity, but not for many other cytotoxic agents, in non-S-phase cells.", "entity1": "topoisomerase II\u03b2", "entity2": "CPT", "span1": [34, 51], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5611": {"label": 1, "data": {"text": "Modulation of HERG inactivation was achieved by either changing extracellular K+ or Cs+ concentrations or by mutations of the channel.", "entity1": "HERG", "entity2": "Cs+", "span1": [14, 18], "span2": [84, 87]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13664": {"label": 1, "data": {"text": "The bound conformation of U46619 fits the crystal structure of the PGIS substrate binding pocket considerably better than that of the unbound U46619.", "entity1": "PGIS", "entity2": "U46619", "span1": [67, 71], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12274": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1b)", "entity2": "AVP", "span1": [154, 159], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8324": {"label": 2, "data": {"text": "Our findings confirmed that Paeoniflorin protected EA.hy926 cells against radiation-induced injury through the Nrf2/HO-1 pathway.", "entity1": "HO-1", "entity2": "Paeoniflorin", "span1": [116, 120], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4089": {"label": 2, "data": {"text": "Activation of an apoptotic signal transduction pathway involved in the upregulation of calpain and apoptosis-inducing factor in aldosterone-induced primary cultured cardiomyocytes.", "entity1": "calpain", "entity2": "aldosterone", "span1": [87, 94], "span2": [128, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6740": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "c-Kit", "entity2": "phenylaminopyrimidine", "span1": [208, 213], "span2": [77, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7307": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT1", "entity2": "alanine", "span1": [224, 229], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13621": {"label": 2, "data": {"text": "One is that the binding of retinoids to nuclear retinoic acid receptors (RARs) does not match their therapeutic efficacy: acitretin activates the three receptor subtypes, RAR-alpha, -beta and -gamma, without measurable receptor binding, whereas tazarotene preferentially binds to and activates RAR-beta and -gamma in preference to RAR-alpha.", "entity1": "RAR-alpha", "entity2": "tazarotene", "span1": [331, 340], "span2": [245, 255]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6237": {"label": 1, "data": {"text": "Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.", "entity1": "human 5-HT1B", "entity2": "[3H]eletriptan", "span1": [110, 122], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2182": {"label": 2, "data": {"text": "Furthermore, tPA induced rapid tyrosine phosphorylation on the beta subunit of LRP-1, which was followed by the activation of Mek1 and its downstream Erk-1 and -2.", "entity1": "Mek1", "entity2": "tyrosine", "span1": [126, 130], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2649": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "milrinone", "span1": [397, 414], "span2": [138, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10875": {"label": 2, "data": {"text": "CPT-11 and SN-38 may also stimulate the production of pro-inflammatory cytokines and prostaglandins (PGs), thus inducing the secretion of Na(+) and Cl(-).", "entity1": "cytokines", "entity2": "SN-38", "span1": [71, 80], "span2": [11, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7180": {"label": 1, "data": {"text": "Administration of m-chlorophenylpiperazine and fenfluramine, both of which induce anorexic effects via 5-HT2C receptors and/or 5-HT1B receptors, suppressed food intake in 5- and 8-wk-old Ay mice, whereas the anorexic effects were attenuated in food-restricted Ay mice.", "entity1": "5-HT2C", "entity2": "m-chlorophenylpiperazine", "span1": [103, 109], "span2": [18, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15947": {"label": 1, "data": {"text": "Vildagliptin, in addition to metformin, proved to be effective in improving \u03b2-cell function and in reducing insulin resistance measurements.", "entity1": "insulin", "entity2": "metformin", "span1": [108, 115], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14136": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "RELA", "entity2": "Celastrol", "span1": [155, 159], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8902": {"label": 3, "data": {"text": "The identity of the lung beta-ADHs was further demonstrated by their characteristic pH-activity profiles for ethanol oxidation, Km values for NAD and ethanol, and inhibition by 4-methylpyrazole or 1,10-phenanthroline.", "entity1": "beta-ADHs", "entity2": "4-methylpyrazole", "span1": [25, 34], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14775": {"label": 3, "data": {"text": "Electrical stimulation transiently elevated extracellular ATP and caused Akt phosphorylation that was additive to insulin and inhibited by suramin.", "entity1": "Akt", "entity2": "suramin", "span1": [73, 76], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"237": {"label": 1, "data": {"text": "In all cases at both the 5-HT2A and 5-HT2C receptors, the affinities of the isomers of MDMA and MDA were at least 2-3 orders of magnitude less than 5-HT.", "entity1": "5-HT2A", "entity2": "MDA", "span1": [25, 31], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10979": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "protein kinase C", "entity2": "phorbol 12-myristate 13-acetate", "span1": [35, 51], "span2": [68, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15760": {"label": 3, "data": {"text": "Ethanol-stimulated (100mM) CYP2E1 upregulation was suppressed by quercetin but further enhanced by HO-1 inhibition with resultant heme accumulation.", "entity1": "HO-1", "entity2": "Ethanol", "span1": [99, 103], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"74": {"label": 3, "data": {"text": "However, salicylate moiety appears to interfere with aspirin inhibitory action on platelets and vascular COX.", "entity1": "COX", "entity2": "aspirin", "span1": [105, 108], "span2": [53, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6086": {"label": 2, "data": {"text": "Pretreatment with the dopamine D1 receptor antagonist, SCH23390, and the NMDA receptor antagonist, MK-801, blocked amantadine induction of Fos in the striatum.", "entity1": "Fos", "entity2": "amantadine", "span1": [139, 142], "span2": [115, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9380": {"label": 1, "data": {"text": "Striatal DAT protein (-25 to -46%) and VMAT2 (-17 to -22%) were reduced, whereas DAT determined by [3H]WIN 35,428 binding was normal.", "entity1": "DAT", "entity2": "[3H]WIN 35,428", "span1": [81, 84], "span2": [99, 113]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9371": {"label": 3, "data": {"text": "The immunomodulatory activity of thalidomide has been ascribed to the selective inhibition of tumor necrosis factor alpha from monocytes.", "entity1": "tumor necrosis factor alpha", "entity2": "thalidomide", "span1": [94, 121], "span2": [33, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12331": {"label": 0, "data": {"text": "Using site-directed mutagenesis, we identified three serines (Ser833, Ser836, and Ser840) within the membrane proximal region of the GluK5 C-terminal domain that, in combination, are required for mGlu1-mediated potentiation of KARs.", "entity1": "GluK5", "entity2": "Ser", "span1": [133, 138], "span2": [62, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3165": {"label": 1, "data": {"text": "A few compounds, 17alpha-methyltestosterone (17alpha-MT), vinclozolin and linuron, were studied using a real world scenario, i.e., assuming that their interaction with the AR was not known: A prescreening for agonism and true, competitive antagonism was used to select conditions such as the appropriate mode of action, and the working range excluding cytotoxicity for the final screening.", "entity1": "AR", "entity2": "17alpha-methyltestosterone", "span1": [172, 174], "span2": [17, 43]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14118": {"label": 3, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "Lenalidomide", "span1": [135, 139], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"699": {"label": 1, "data": {"text": "In summary, data obtained in our experiments in rat SMA indicate that the alpha 1-adrenoceptor mediating noradrenaline-induced contraction displays a distinct alpha 1L-adrenoceptor pharmacology.", "entity1": "alpha 1L-adrenoceptor", "entity2": "noradrenaline", "span1": [159, 180], "span2": [105, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10027": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Arg", "span1": [126, 138], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6880": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "CSE", "entity2": "L-cysteine", "span1": [27, 30], "span2": [78, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2728": {"label": 3, "data": {"text": "Indomethacin and SC-236, a selective cyclooxygenase-2 (COX-2) inhibitor, exerted a similar effect as sulindac.", "entity1": "COX-2", "entity2": "Indomethacin", "span1": [55, 60], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11060": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "CsA", "span1": [89, 95], "span2": [217, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11249": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "DAT", "entity2": "4',7,8-trichloro", "span1": [151, 154], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6340": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "zolasartan", "span1": [25, 28], "span2": [198, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7469": {"label": 1, "data": {"text": "Additionally, Na+ and Cl- ions coactivate GluR6 receptors by establishing a dipole, accounting for their common effect on KARs.", "entity1": "KARs", "entity2": "Cl-", "span1": [122, 126], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11511": {"label": 8, "data": {"text": "Choline dehydrogenase (CHDH) and betaine-homocysteine methyltransferase (BHMT) are 2 enzymes involved in choline oxidation.", "entity1": "betaine-homocysteine methyltransferase", "entity2": "choline", "span1": [33, 71], "span2": [105, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9558": {"label": 1, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "Con A", "entity2": "fenoterol", "span1": [16, 21], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7847": {"label": 2, "data": {"text": "These data suggest that ribavirin-induced intracellular GTP depletion recruits a super elongation complex containing P-TEFb, AFF4 and ELL3, to F7, and modulates FVII mRNA transcription elongation.", "entity1": "F7", "entity2": "ribavirin", "span1": [143, 145], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15758": {"label": 3, "data": {"text": "CO donor dose-dependently inactivated CYP2E1 of ethanol-incubated microsome, which was mimicked by HO-1 substrate but abolished by CO scavenger.", "entity1": "CYP2E1", "entity2": "CO", "span1": [38, 44], "span2": [131, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8369": {"label": 1, "data": {"text": "The crystal structure of HSA complexed with fatty acid and acetyldiflunisal revealed that acetyldiflunisal binds to the IIA subdomain and that upon binding, it acetylates lysine 199.", "entity1": "IIA subdomain", "entity2": "acetyldiflunisal", "span1": [120, 133], "span2": [90, 106]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7208": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "Akt", "entity2": "Cd", "span1": [100, 103], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5671": {"label": 2, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "FAS", "entity2": "farnesylpyrophosphate", "span1": [32, 35], "span2": [213, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2832": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "PLP", "span1": [83, 99], "span2": [171, 174]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15125": {"label": 3, "data": {"text": "Notably, the antioxidant Trolox\u2122 reversed the Mn (20\u00a0mg/kg)-dependent augmentation in p38(MAPK) phosphorylation and reduced the Mn (20\u00a0mg/kg)-induced caspase activity and F(2)-isoprostane production.", "entity1": "p38", "entity2": "Trolox", "span1": [86, 89], "span2": [25, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8512": {"label": 1, "data": {"text": "To overcome this limitation, we de novo synthesized a conjugate that covalently combines a Gd-based MRI contrast agent, encaged with a chelating agent (DOTA), with pantoprazole, which is a widely used proton pump inhibitor that binds to proton pumps in the stomach and colon.", "entity1": "proton pumps", "entity2": "pantoprazole", "span1": [237, 249], "span2": [164, 176]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8647": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b2", "entity2": "melatonin", "span1": [14, 18], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15977": {"label": 4, "data": {"text": "Collectively, these initial findings suggest that design and systematic modification of aminoalkylindoles such as 3 may lead to development of novel cannabinoid ligands with dual CB1R antagonist/CB2R agonist activity with potential for use as treatments of alcohol abuse.", "entity1": "CB2R", "entity2": "aminoalkylindoles", "span1": [195, 199], "span2": [88, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12344": {"label": 8, "data": {"text": "In this work, the metabolism of four frequently prescribed inhaled GCs, triamcinolone acetonide, flunisolide, budesonide, and fluticasone propionate, by the CYP3A family of enzymes was studied to identify differences in their rates of clearance and to identify their metabolites.", "entity1": "CYP3A", "entity2": "budesonide", "span1": [157, 162], "span2": [110, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9188": {"label": 2, "data": {"text": "This agent acts synergistically with many penicillins, such as ampicillin, carbenicillin, and the like, and with cephalosporins, cefazolin, cefamandole, or cefoxitin to inhibit gram-negative bacilli, probably on the basis of binding to different proteins needed for the production of the peptidoglycan of the bacterial cell wall.", "entity1": "peptidoglycan", "entity2": "ampicillin", "span1": [288, 301], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3669": {"label": 3, "data": {"text": "Additionally, the mRNA levels of melanogenesis-related genes (c-KIT, stem cell factor (SCF), and macrophage migration inhibitory factor (MIF)) were down-regulated by artemisinic acid.", "entity1": "SCF", "entity2": "artemisinic acid", "span1": [87, 90], "span2": [166, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2820": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "iNOS", "entity2": "Dexamethasone", "span1": [66, 70], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10786": {"label": 2, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "TNF-alpha", "entity2": "simvastatin", "span1": [119, 128], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2636": {"label": 8, "data": {"text": "They all expressed ASS, but not ornithine transcarbamylase (OTC), the enzyme that converts ornithine, the product of degradation of arginine with rhArg, to citrulline, which is converted back to arginine via ASS.", "entity1": "ASS", "entity2": "arginine", "span1": [208, 211], "span2": [195, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, 9]},
	"8467": {"label": 3, "data": {"text": "In conclusion, hinokitiol may inhibit platelet activation by inhibiting the PLC\u03b32-PKC cascade and hydroxyl radical formation, followed by suppressing the activation of MAPKs and Akt.", "entity1": "Akt", "entity2": "hinokitiol", "span1": [178, 181], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4168": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "p65", "entity2": "2-oxaisodauc-5-en-12-al", "span1": [180, 183], "span2": [124, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13750": {"label": 1, "data": {"text": "(+)-[(3)H]isradipine binding to Ca(v)1.2DHP(-/-) and Ca(v)-DM brains was reduced to 15.1 and 4.4% of wild type, respectively, indicating that Ca(v)1.3 accounts for 10.7% of brain LTCCs.", "entity1": "LTCCs", "entity2": "(+)-[(3)H]isradipine", "span1": [179, 184], "span2": [0, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"760": {"label": 3, "data": {"text": "This hypothesis was tested by investigating whether, in subjects with essential hypertension, the natriuretic response to specific renin-angiotensin-aldosterone system (RAAS) blockade by renin-inhibitor remikiren could be predicted from pretreatment renal vascular tone.", "entity1": "renin", "entity2": "remikiren", "span1": [131, 136], "span2": [203, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12884": {"label": 8, "data": {"text": "However, N-methyl-phosphatidylserine, which is transported by the plasma membrane flippase at a rate equivalent to PS, is incapable of activating Atp8a1 activity.", "entity1": "flippase", "entity2": "N-methyl-phosphatidylserine", "span1": [82, 90], "span2": [9, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14561": {"label": 5, "data": {"text": "On the other hand, peptides modified with (2S,4R)-4-(naphthalene-2-ylmethyl)pyrrolidine-2-carboxylic acid, apart from their moderate antioxytocic activity, turned out to be weak antagonists of the pressor response to arginine vasopressin.", "entity1": "arginine vasopressin", "entity2": "(2S,4R)-4-(naphthalene-2-ylmethyl)pyrrolidine-2-carboxylic acid", "span1": [217, 237], "span2": [42, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10342": {"label": 2, "data": {"text": "The results show that transient arsenite pre-treatment induces Hsp72, HO-1 and, to a lesser extent, Hsp27; it reduces H2O2-induced astrocyte death; and it causes selective activation of Akt following H2O2.", "entity1": "HO-1", "entity2": "arsenite", "span1": [70, 74], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13255": {"label": 2, "data": {"text": "The inhibitory effect of the leukotriene receptor antagonist on leukotriene D4-induced MUC2/5AC gene expression and mucin secretion in human airway epithelial cells.", "entity1": "mucin", "entity2": "leukotriene D4", "span1": [116, 121], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14634": {"label": 8, "data": {"text": "In conclusion, the Lys27Gln substitution does not significantly modulate CDA activity toward dFdC, and therefore would not contribute to interindividual variability in response to gemcitabine.", "entity1": "CDA", "entity2": "dFdC", "span1": [73, 76], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10339": {"label": 2, "data": {"text": "Induction of heat shock proteins (HSPs) by sodium arsenite in cultured astrocytes and reduction of hydrogen peroxide-induced cell death.", "entity1": "heat shock proteins", "entity2": "sodium arsenite", "span1": [13, 32], "span2": [43, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9654": {"label": 3, "data": {"text": "RESULTS: Administration of SC-236 to cirrhotic animals did not produce significant renal effects, whereas administration of the nonselective COX-1/COX-2 inhibitor, ketorolac, resulted in a marked reduction in urine volume, urinary excretion of prostaglandins, and glomerular filtration rate and in a significant impairment in renal water metabolism.", "entity1": "COX-2", "entity2": "ketorolac", "span1": [147, 152], "span2": [164, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"13195": {"label": 8, "data": {"text": "MicroPET imaging in nonhuman primates with [11C]1 and [11C]2 demonstrated that both tracers behave similarly in vivo with high uptake being observed in the SERT-rich brain regions and peak uptake being achieved in about 55 min postinjection.", "entity1": "SERT", "entity2": "11C", "span1": [156, 160], "span2": [44, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5832": {"label": 8, "data": {"text": "The unique role of the enzyme 5-lipoxygenase (5-LO) in the production of leukotrienes (LTs) makes it a likely target for biochemical manipulation.", "entity1": "5-lipoxygenase", "entity2": "leukotrienes", "span1": [30, 44], "span2": [73, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4544": {"label": 8, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "MAO-A", "entity2": "5-MeO-DMT", "span1": [69, 74], "span2": [174, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14840": {"label": 1, "data": {"text": "From the resolved free and bound NADH fluorescence signatures, the KD values for both NADH conformations in ALDH1A1 ranged from about 24 \u03bcM to 1 \u03bcM for Mg(2+) ion concentrations of 0-6000 \u03bcM, respectively.", "entity1": "ALDH1A1", "entity2": "Mg(2+)", "span1": [108, 115], "span2": [152, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3595": {"label": 3, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "mTOR", "entity2": "Wogonoside", "span1": [76, 80], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14695": {"label": 3, "data": {"text": "In vitro experiments assessed the inhibition of transporters and CYP enzymes by GSK1292263, and a clinical drug interaction study investigated the effect of GSK1292263 (300\u2009mg BID) on the pharmacokinetic profile of simvastatin (40\u2009mg single dose) and rosuvastatin (10\u2009mg single dose).", "entity1": "CYP", "entity2": "GSK1292263", "span1": [65, 68], "span2": [80, 90]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8212": {"label": 2, "data": {"text": "TAA increased the number and area of glutathione S-transferase placental form (GST-P)(+) liver cell foci and the numbers of proliferating and apoptotic cells in randomly selected areas in liver sections.", "entity1": "GST-P", "entity2": "TAA", "span1": [79, 84], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10099": {"label": 1, "data": {"text": "[3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen.", "entity1": "HERG", "entity2": "[3H]dofetilide", "span1": [26, 30], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9474": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "TP", "entity2": "GR 32191", "span1": [248, 250], "span2": [235, 243]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11839": {"label": 1, "data": {"text": "These results suggest that the enantioselective disposition of sibutramine and its active metabolites are influenced by the altered genetic and environmental factors of CYP2B6 and CYP3A activity in vivo.", "entity1": "CYP2B6", "entity2": "sibutramine", "span1": [169, 175], "span2": [63, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4938": {"label": 3, "data": {"text": "Moreover, protein and mRNA levels of DSS-induced proinflammatory cytokines in colon, including TNF-\u03b1, IL-1\u03b2, IL-18, IL-17A and IFN-\u03b3, were markedly suppressed by Fc11a-2.", "entity1": "cytokines", "entity2": "Fc11a-2", "span1": [65, 74], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11725": {"label": 2, "data": {"text": "The concentration response to levcromakalim (LEVC), a K(ATP) channel opener, was significantly shifted to the left in the inflamed smooth-muscle cells.", "entity1": "K(ATP) channel", "entity2": "LEVC", "span1": [54, 68], "span2": [45, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7507": {"label": 2, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "AMPK", "entity2": "phenformin", "span1": [256, 260], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1580": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "butyrylcholinesterase", "entity2": "4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines", "span1": [36, 57], "span2": [163, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15029": {"label": 8, "data": {"text": "Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner.", "entity1": "SAHH", "entity2": "SAH", "span1": [127, 131], "span2": [156, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2792": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "NK1-R", "entity2": "NaHS", "span1": [258, 263], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6824": {"label": 3, "data": {"text": "Further study revealed that pitavastatin increased ABCA1 mRNA in HMG-CoA reductase-dependent manner and that Rho and Rho kinase inhibitor (C3T and Y27632) increased apoA-I production in the HepG2 cells.", "entity1": "Rho kinase", "entity2": "Y27632", "span1": [117, 127], "span2": [147, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13377": {"label": 8, "data": {"text": "The expression of key genes important in methionine metabolism, such as methionine adenosyltransferase-1a, betaine-homocysteine methyltransferase and thioether S-methyltransferase, were suppressed.", "entity1": "methionine adenosyltransferase-1a", "entity2": "methionine", "span1": [72, 105], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11854": {"label": 8, "data": {"text": "The calcium homeostasis proteins sarcoendoplasmic reticulum ATPase 2a (SERCA2a), sodium calcium exchanger-1, phospholamban (PLB), phospho-PLB, and calsequestrin 2 are important for contraction and relaxation.", "entity1": "phospho-PLB", "entity2": "calcium", "span1": [130, 141], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"659": {"label": 3, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "angiotensin-converting enzyme", "entity2": "captopril", "span1": [109, 138], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"6988": {"label": 3, "data": {"text": "MATERIALS AND METHODS/RESULTS: By isolating rat brain microsomal long-chain fatty acyl-CoA synthetases (Acsl), we show in vitro that valproic acid is a non-competitive inhibitor of Acsl, as it reduces the maximal velocity of the reaction without changing the affinity of the substrate for the enzyme.", "entity1": "Acsl", "entity2": "valproic acid", "span1": [181, 185], "span2": [133, 146]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7524": {"label": 3, "data": {"text": "Neuroprotective effect of nimesulide, a preferential COX-2 inhibitor, against pentylenetetrazol (PTZ)-induced chemical kindling and associated biochemical parameters in mice.", "entity1": "COX-2", "entity2": "nimesulide", "span1": [53, 58], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14464": {"label": 1, "data": {"text": "This suggests that for the mutant receptors, ECII plays a critical role in linking the agonist bound receptor conformation to the G protein nucleotide bound state.", "entity1": "G protein", "entity2": "nucleotide", "span1": [130, 139], "span2": [140, 150]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12231": {"label": 1, "data": {"text": "These data define PFD or PFD-related agents as promising agents for human cancers associated with enhanced TGF-beta activity.", "entity1": "TGF-beta", "entity2": "PFD", "span1": [107, 115], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7727": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LHRH", "entity2": "buserelin", "span1": [39, 43], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15827": {"label": 8, "data": {"text": "In terms of the mechanisms, we found that fatty acid amide hydrolase (FAAH) which degrades anandamide, was upregulated after nerve injury at both ages, so that this upregulation likely did not account for the age-dependent differences.", "entity1": "fatty acid amide hydrolase", "entity2": "anandamide", "span1": [42, 68], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3609": {"label": 1, "data": {"text": "SB365, Pulsatilla saponin D suppresses the proliferation of human colon cancer cells and induces apoptosis by modulating the AKT/mTOR signalling pathway.", "entity1": "AKT", "entity2": "SB365", "span1": [125, 128], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3200": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "caffeic acid", "span1": [248, 261], "span2": [104, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7164": {"label": 3, "data": {"text": "The deletion and mutation analysis of the AT1R gene promoter indicated that a GC box located in the proximal promoter region is responsible for the telmisartan-induced downregulation.", "entity1": "GC box", "entity2": "telmisartan", "span1": [78, 84], "span2": [148, 159]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13342": {"label": 2, "data": {"text": "In addition, activation of protein kinase C and increases in intracellular cAMP also enhance cholinergic activity in T cells, and lymphocyte function associated antigen-1 (LFA-1; CD11a/CD18) is an important mediator of leukocyte migration and T cell activation.", "entity1": "CD18", "entity2": "cAMP", "span1": [185, 189], "span2": [75, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5223": {"label": 2, "data": {"text": "Also, vinblastine enhances the phosphorylation of Ras homologous protein A, the accumulation of reactive oxygen species, the release of intracellular Ca(2+), as well as the activation of apoptosis signal-regulating kinase 1, c-jun-N-terminal kinase, p38, inhibitor of kappaB\u03b1 (I\u03baB\u03b1) kinase, and inositol requiring enzyme 1\u03b1.", "entity1": "inhibitor of kappaB\u03b1", "entity2": "vinblastine", "span1": [255, 275], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11208": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel.", "entity1": "human brain K(+) channel", "entity2": "pimozide", "span1": [62, 86], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10361": {"label": 2, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK1-8", "entity2": "omapatrilat", "span1": [59, 66], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12660": {"label": 1, "data": {"text": "However, inter-helical distances calculated and determined by EPR for PGHS-2 complexed with arachidonic acid, flurbiprofen, and SC-58125 were in close agreement with those obtained from the cognate crystal structures.", "entity1": "PGHS-2", "entity2": "arachidonic acid", "span1": [70, 76], "span2": [92, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11103": {"label": 8, "data": {"text": "of 1500 nmol of O2/nmol of enzyme, whereas hCOX-2 had a specific activity of 12.2 mumol of O2/mg with a Km of 8.7 microM for arachidonate and a Vmax.", "entity1": "hCOX-2", "entity2": "arachidonate", "span1": [43, 49], "span2": [125, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13851": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "nomegestrol acetate", "span1": [252, 261], "span2": [139, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12808": {"label": 3, "data": {"text": "However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50.", "entity1": "COX-2", "entity2": "phenylbutazone", "span1": [76, 81], "span2": [17, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9905": {"label": 1, "data": {"text": "The impaired expression of the UCP-3 gene is consistent with the involvement of UCP-3 gene regulation in the reduction of the use of fatty acids as fuel by the skeletal muscle and in impaired adaptative thermogenesis, both of which are major metabolic adaptations that occur during lactation.", "entity1": "UCP-3", "entity2": "fatty acids", "span1": [31, 36], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1536": {"label": 3, "data": {"text": "However, topiramate at low concentrations causes slow inhibition of GluR5 kainate receptor-mediated synaptic currents in the basolateral amygdala, indicating that it may protect against seizures, at least in part, through suppression of GluR5 kainate receptor responses.", "entity1": "kainate receptor", "entity2": "topiramate", "span1": [243, 259], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5598": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "olanzapine", "span1": [171, 177], "span2": [139, 149]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"731": {"label": 2, "data": {"text": "Endothelial NO synthase expression was increased by cilazapril but not by losartan.", "entity1": "Endothelial NO synthase", "entity2": "cilazapril", "span1": [0, 23], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4747": {"label": 8, "data": {"text": "We have shown that COX-2 mediates acid-induced PGE2 production.", "entity1": "COX-2", "entity2": "PGE2", "span1": [19, 24], "span2": [47, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13054": {"label": 3, "data": {"text": "Late INa induced by the VGSC long QT mutant R1623Q was reduced by resveratrol and quercetin.", "entity1": "R1623Q", "entity2": "resveratrol", "span1": [44, 50], "span2": [66, 77]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12971": {"label": 1, "data": {"text": "gammaPKC directly associated with DGKgamma through its accessory domain (AD), depending on Ca2+ as well as phosphatidylserine/diolein in vitro.", "entity1": "gammaPKC", "entity2": "phosphatidylserine", "span1": [0, 8], "span2": [107, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5551": {"label": 2, "data": {"text": "Immunohistochemical studies show that alpha(2A)-AR increased in the dentate gyrus area of the hippocampus 24 h after five repeated administrations of METH.", "entity1": "alpha(2A)-AR", "entity2": "METH", "span1": [38, 50], "span2": [150, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1987": {"label": 3, "data": {"text": "When selectively applied to channels after inducing slow inactivation with a 60-s pulse to -10 mV, mibefradil (1 microM) produced 45% fractional block in Nav1.5 and greater block (88%) in an isoform (Nav1.4) that slow-inactivates more completely.", "entity1": "Nav1.5", "entity2": "mibefradil", "span1": [154, 160], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2152": {"label": 3, "data": {"text": "(R)-Ketoprofen (1) was previously reported to be a potent and specific noncompetitive inhibitor of CXCL8-induced human PMNs chemotaxis.", "entity1": "CXCL8", "entity2": "(R)-Ketoprofen", "span1": [99, 104], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10608": {"label": 1, "data": {"text": "These experimental results suggest that SV2A is the binding site of LEV in the brain and that LEV acts by modulating the function of SV2A, supporting previous indications that LEV possesses a mechanism of action distinct from that of other antiepileptic drugs.", "entity1": "SV2A", "entity2": "LEV", "span1": [133, 137], "span2": [94, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"287": {"label": 0, "data": {"text": "The two NH2-terminal truncated vectors deleted, respectively, 1) the 29-amino acid putative targeting sequence and 2) 51 amino acids, yielding a protein equivalent to a carbonic anhydrase (CA) V isolated from mouse liver mitochondria; and both vectors produced homogeneous protein fractions.", "entity1": "carbonic anhydrase (CA) V", "entity2": "amino acid", "span1": [169, 194], "span2": [72, 82]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15024": {"label": 3, "data": {"text": "Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner.", "entity1": "adenosylhomocysteine (SAH) hydrolase", "entity2": "adenosine dialdehyde", "span1": [89, 125], "span2": [15, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10640": {"label": 8, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "bile salt export pump", "entity2": "taurocholate", "span1": [53, 74], "span2": [99, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12690": {"label": 1, "data": {"text": "Corticosteroids act, at least in part, by recruitment of histone deacetylases (HDACs) to the site of active inflammatory gene transcription.", "entity1": "histone deacetylases", "entity2": "Corticosteroids", "span1": [57, 77], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14052": {"label": 3, "data": {"text": "Aspirin inhibits mTOR signaling, activates AMP-activated protein kinase, and induces autophagy in colorectal cancer cells.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [17, 21], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13364": {"label": 1, "data": {"text": "Several genes involved with steroid metabolism also showed remarkable expression changes, including increased expression of 17beta-hydroxysteroid dehydrogenase-7 (HSD17beta7; involved in estradiol production) and decreased expression of HSD17beta5 (involved in testosterone production).", "entity1": "HSD17beta5", "entity2": "steroid", "span1": [237, 247], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4917": {"label": 3, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "SOD", "entity2": "kinsenoside", "span1": [183, 186], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2830": {"label": 3, "data": {"text": "Pharmacological treatment has been studied and it could be demonstrated, that some mutant currents may be insufficiently suppressed by drugs targeted to block the specific current such as, e.g., sotalol or ibutilide in patients with a mutation in the IKr-coding gene KCNH2 (HERG).", "entity1": "KCNH2", "entity2": "ibutilide", "span1": [267, 272], "span2": [206, 215]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15910": {"label": 1, "data": {"text": "Synaptotagmin-1, a vesicular protein interacting with membranes upon low-affinity Ca(2+) -binding, plays a major role in excitation-release coupling, by synchronizing calcium entry with fast neurotransmitter release.", "entity1": "Synaptotagmin-1", "entity2": "calcium", "span1": [0, 15], "span2": [167, 174]}, "weak_labels": [-1, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10856": {"label": 1, "data": {"text": "Almost all of the tested H(1)R and H(2)R antagonists, including several important therapeutics, displaced less than 30% of specific [(3)H]histamine binding to the hH(4)R at concentrations up to 10 microM.", "entity1": "hH(4)R", "entity2": "[(3)H]histamine", "span1": [163, 169], "span2": [132, 147]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1514": {"label": 3, "data": {"text": "Sildenafil is inhibitory of PDE5 at a rate tenfold higher than for the next PDE (PDE6), which produces visual changes through the retinal rods.", "entity1": "PDE", "entity2": "Sildenafil", "span1": [76, 79], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6375": {"label": 5, "data": {"text": "The kappa(1)+kappa(3)-opioid receptor agonist/mu-opioid receptor antagonist naloxone benzoylhydrazone was a pure antagonist at both rat brain and human ORL1 receptors.", "entity1": "mu-opioid receptor", "entity2": "naloxone benzoylhydrazone", "span1": [46, 64], "span2": [76, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15609": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "N-terminal kinases", "entity2": "galangin", "span1": [94, 112], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12611": {"label": 1, "data": {"text": "Likewise, GYKI 52466 (30-100 microM)) shifted the concentration-response curve for the effects of cyclothiazide on AMPA receptor-mediated e.p.s.c.", "entity1": "AMPA receptor", "entity2": "GYKI 52466", "span1": [115, 128], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5495": {"label": 3, "data": {"text": "3) The inhibitory effects of the thioureylene drugs, methimazole and carbimazole, on the iodide-dependent catalatic activity were very similar to those reported previously for thyroid peroxidase-catalyzed iodination.", "entity1": "thyroid peroxidase", "entity2": "carbimazole", "span1": [176, 194], "span2": [69, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12701": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "TFEC", "span1": [79, 90], "span2": [196, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11895": {"label": 8, "data": {"text": "Cytochrome P450 epoxygenase 2J2 (CYP2J2) metabolizes arachidonic acids to form epoxyeicosatrienoic acids (EETs), which possess various beneficial effects on the cardiovascular system.", "entity1": "Cytochrome P450 epoxygenase 2J2", "entity2": "EETs", "span1": [0, 31], "span2": [106, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15630": {"label": 3, "data": {"text": "Nobiletin attenuates metastasis via both ERK and PI3K/Akt pathways in HGF-treated liver cancer HepG2 cells.", "entity1": "ERK", "entity2": "Nobiletin", "span1": [41, 44], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2715": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "p53", "entity2": "parathion", "span1": [110, 113], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6156": {"label": 1, "data": {"text": "For example, it is clear that the closed conformation of the regulatory N-terminal domain in Ca2+-bound cardiac troponin C (cTnC) presents a much different binding surface for Ca2+-sensitizing compounds than previously thought.", "entity1": "cTnC", "entity2": "Ca2+", "span1": [124, 128], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9544": {"label": 5, "data": {"text": "Effect of lintitript, a new CCK-A receptor antagonist, on gastric emptying of a solid-liquid meal in humans.", "entity1": "CCK-A receptor", "entity2": "lintitript", "span1": [28, 42], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3908": {"label": 3, "data": {"text": "Importantly, pre-treatment with buthionine sulfoximine (BSO), an inhibitor of \u03b3-GCS, prevented \u03b1-MeDA induced increase in GSH levels, but did not augment this metabolite cytotoxicity.", "entity1": "\u03b3-GCS", "entity2": "BSO", "span1": [78, 83], "span2": [56, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3772": {"label": 4, "data": {"text": "Antiarrhythmic effects of (-)-epicatechin-3-gallate, a novel sodium channel agonist in cultured neonatal rat ventricular myocytes.", "entity1": "sodium channel", "entity2": "(-)-epicatechin-3-gallate", "span1": [61, 75], "span2": [26, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11601": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "cystathionine-beta-synthase", "entity2": "Hydrogen sulphide", "span1": [111, 138], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6288": {"label": 1, "data": {"text": "In conclusion, (-)-pindolol modulates, both alone and together with 5-HT reuptake inhibitors, dopaminergic, adrenergic, and serotonergic transmission in the FCX via a complex pattern of actions at beta 1/2-ARs, 5-HT1A, and 5-HT1B receptors.", "entity1": "5-HT1B", "entity2": "(-)-pindolol", "span1": [223, 229], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3193": {"label": 3, "data": {"text": "Phenols like the ones investigated here possess a CA inhibition mechanism distinct of that of the sulfonamides/sulfamates used clinically or the coumarins.", "entity1": "CA", "entity2": "sulfonamides", "span1": [50, 52], "span2": [98, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14738": {"label": 3, "data": {"text": "APO and RS at least partially normalize hypoxia caused male hypogonadism by suppressing ER stress, and p66Shc in testes.", "entity1": "p66Shc", "entity2": "APO", "span1": [103, 109], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13792": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Leflunomide", "span1": [14, 16], "span2": [254, 265]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11586": {"label": 1, "data": {"text": "Overexpression of PPARdelta by adenoviral transfer rescued 14-3-3epsilon proteins from elimination by sulindac or indomethacin.", "entity1": "14-3-3epsilon", "entity2": "sulindac", "span1": [59, 72], "span2": [102, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8299": {"label": 3, "data": {"text": "The pharmacological inhibitors SB203580 (p38 inhibitor) and SP600125 (a JNK inhibitor) protected primary cultures of rat CGCs from LY294002-induced apoptosis.", "entity1": "JNK", "entity2": "SP600125", "span1": [72, 75], "span2": [60, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8796": {"label": 1, "data": {"text": "Using siRNA we found that ATF4, but not Nrf2, is important for fisetin's ability to increase GSH levels under basal conditions whereas both ATF4 and Nrf2 appear to cooperate to increase GSH levels under oxidative stress conditions.", "entity1": "ATF4", "entity2": "fisetin", "span1": [26, 30], "span2": [63, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6395": {"label": 2, "data": {"text": "Glucocorticoid receptors were activated by dexamethasone as assessed using a glucocorticoid-responsive reporter plasmid, pTAT3-CAT.", "entity1": "Glucocorticoid receptors", "entity2": "dexamethasone", "span1": [0, 24], "span2": [43, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2826": {"label": 3, "data": {"text": "Pharmacological treatment has been studied and it could be demonstrated, that some mutant currents may be insufficiently suppressed by drugs targeted to block the specific current such as, e.g., sotalol or ibutilide in patients with a mutation in the IKr-coding gene KCNH2 (HERG).", "entity1": "IKr", "entity2": "sotalol", "span1": [251, 254], "span2": [195, 202]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12953": {"label": 0, "data": {"text": "METHODS: We identified seven SNP(single nucleotide polymorphism) (-141Cins>del, TaqIB, TaqID, Ser311Cys, rs6275, rs6277 and TaqIA) in the DRD2 gene in 146 schizophrenic inpatients (59 with EPS and 87 without EPS according to the Simpson-Angus Scale) treated with chlorpromazine after 8 weeks.", "entity1": "Ser311Cys", "entity2": "nucleotide", "span1": [94, 103], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11909": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "DAGs", "span1": [174, 179], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8115": {"label": 1, "data": {"text": "The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.", "entity1": "gamma secretase", "entity2": "oxadiazepines", "span1": [40, 55], "span2": [23, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15345": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "naphthalene", "span1": [39, 48], "span2": [213, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7350": {"label": 1, "data": {"text": "Reticulated platelets and uninhibited COX-1 and COX-2 decrease the antiplatelet effects of aspirin.", "entity1": "COX-1", "entity2": "aspirin", "span1": [38, 43], "span2": [91, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5007": {"label": 1, "data": {"text": "This study is the first to identify Class V CGPs with their distinctive methine or trimethine linkage between two disubstituted pyrylium moieties as a particularly potent class of MRP modulators and also show that within this core structure, differences in the electronegativity associated with a chalcogen atom can be the sole determinant of whether a compound will stimulate or inhibit MRP2.", "entity1": "MRP", "entity2": "pyrylium", "span1": [180, 183], "span2": [128, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15906": {"label": 1, "data": {"text": "Therefore, in addition to its previously described functions, synaptotagmin-1 is involved in a rapid vesicular Ca(2+) sequestration through a Ca(2+) /H(+) antiport.", "entity1": "synaptotagmin-1", "entity2": "Ca(2+)", "span1": [62, 77], "span2": [111, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13275": {"label": 8, "data": {"text": "[H]-Cholesterol-labeled J774 macrophage cells, with and without ABCA1 up-regulation, were incubated with the samples, and ABCA1-dependent cholesterol efflux and serum lipid and lipoprotein levels were assessed.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [122, 127], "span2": [138, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6811": {"label": 2, "data": {"text": "Based on HMG-CoA reductase inhibition, pitavastatin-induced apoA-I more efficiently than simvastatin and atorvastatin.", "entity1": "apoA-I", "entity2": "atorvastatin", "span1": [60, 66], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15312": {"label": 1, "data": {"text": "The serum or dexamethasone-induced oscillation in the expression of DRD3 in cells was abrogated by the downregulation or overexpression of REV-ERB\u03b1, suggesting that REV-ERB\u03b1 functions as a regulator of DRD3 oscillations in the cellular autonomous clock.", "entity1": "DRD3", "entity2": "dexamethasone", "span1": [68, 72], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12508": {"label": 1, "data": {"text": "Among all the organophosphates tested, the combination of a methyl group and a negatively charged oxygen attached to the P atom, CH3P(O)(O-)-AChE, conferred the greatest protection to the active site of aged or nonaged organophosphoryl conjugates of acetylcholinesterase.", "entity1": "AChE", "entity2": "CH3P(O)(O-)", "span1": [141, 145], "span2": [129, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2342": {"label": 1, "data": {"text": "We conclude that lutein and EPA interact through the PPARgamma and RXR pathways to modulate iNOS mRNA.", "entity1": "PPARgamma", "entity2": "EPA", "span1": [53, 62], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1720": {"label": 2, "data": {"text": "Ginsenosides Rb2, Rd and Rg1 significantly decreased norepinephrine and/or epinephrine-induced increase of IL-6 level in macrophage cell line (RAW 264.7).", "entity1": "IL-6", "entity2": "norepinephrine", "span1": [107, 111], "span2": [53, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14585": {"label": 1, "data": {"text": "Alleles of RPB1 (RPO21) with elevated slippage rates were identified among 6-azauracil-sensitive mutants and were also isolated using a slippage-dependent reporter gene.", "entity1": "RPB1", "entity2": "6-azauracil", "span1": [11, 15], "span2": [75, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1544": {"label": 8, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "SMO", "entity2": "spermine", "span1": [15, 18], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14583": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "PRT062607", "span1": [147, 150], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1640": {"label": 1, "data": {"text": "2-Amino-3-[3-hydroxy-5-(2-thiazolyl)-4-isoxazolyl]propionic acid (1) is a potent AMPA receptor agonist with moderate affinity for native kainic acid (KA) receptors, whereas (S)-E-4-(2,2-dimethylpropylidene)glutamic acid (3) show high affinity for the GluR5 subtype of KA receptors and much lower affinity for the GluR2 subtype of AMPA receptors.", "entity1": "GluR5", "entity2": "(S)-E-4-(2,2-dimethylpropylidene)glutamic acid", "span1": [251, 256], "span2": [173, 219]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2773": {"label": 3, "data": {"text": "Mutation of Ser-530 to Ala or Val-349 to Ala or Leu abolished the potent inhibition observed with wild-type human COX-2 and key lumiracoxib analogs.", "entity1": "human COX-2", "entity2": "lumiracoxib", "span1": [108, 119], "span2": [128, 139]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5940": {"label": 3, "data": {"text": "Trilostane, epostane and cyanoketone are potent inhibitors of 3 beta-HSD with Ki values of approximately 50 nM.", "entity1": "3 beta-HSD", "entity2": "Trilostane", "span1": [62, 72], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13137": {"label": 2, "data": {"text": "In the present study, glucose-stimulated insulin secretion was significantly increased in GalN-treated rats compared to controls.", "entity1": "insulin", "entity2": "glucose", "span1": [41, 48], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3257": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "MET", "span1": [13, 16], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15445": {"label": 8, "data": {"text": "Possible AOX involvement in IMI metabolism in insects was evaluated using AOX-expressing and AOX-deficient Drosophila, but no differences were found in IMI nitroreduction or sensitivity between the two strains.", "entity1": "AOX", "entity2": "IMI", "span1": [74, 77], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8109": {"label": 3, "data": {"text": "Moreover, wogonin repressed anisomycin-induced phosphorylation of p38, cav-1 and vascular permeability.", "entity1": "cav-1", "entity2": "wogonin", "span1": [71, 76], "span2": [10, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7576": {"label": 4, "data": {"text": "Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist.", "entity1": "M3 muscarinic receptor", "entity2": "cevimeline", "span1": [124, 146], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1661": {"label": 4, "data": {"text": "P2Y(2) receptor agonist INS37217 enhances functional recovery after detachment caused by subretinal injection in normal and rds mice.", "entity1": "P2Y(2) receptor", "entity2": "INS37217", "span1": [0, 15], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8142": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "glutathione reductase", "entity2": "Isoproterenol", "span1": [271, 292], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"507": {"label": 3, "data": {"text": "The results suggest that the 63-kDa (PDE 1B1) and 60-kDa (PDE 1A2) CaMPDE isozymes are inhibited by felodipine and nicardipine by partial competitive inhibition and that these two Ca2+ antagonists appear to counteract each other.", "entity1": "PDE 1A2", "entity2": "nicardipine", "span1": [58, 65], "span2": [115, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"39": {"label": 1, "data": {"text": "These G-proteins are likely to be involved in the adrenaline-induced inhibition of dihydropyridine-sensitive Ca2+ currents and in other signal transduction pathways contributing to the adrenaline-induced inhibition of insulin secretion.", "entity1": "G-proteins", "entity2": "adrenaline", "span1": [6, 16], "span2": [50, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1671": {"label": 1, "data": {"text": "The current study was performed to elucidate the possible interaction of etomidate with alpha2-adrenoceptors in mice lacking individual alpha2-adrenoceptor subtypes (alpha2-KO).", "entity1": "alpha2-adrenoceptors", "entity2": "etomidate", "span1": [88, 108], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3727": {"label": 3, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "Ras", "entity2": "N", "span1": [240, 243], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16047": {"label": 1, "data": {"text": "In addition, the expression of nucleus-encoded RNA polymerase dependent transcripts is specifically induced by lincomycin, and the splicing of ndhB transcripts is significantly reduced in the albino mutants and inhibitor-treated seedlings.", "entity1": "ndhB", "entity2": "lincomycin", "span1": [143, 147], "span2": [111, 121]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9648": {"label": 5, "data": {"text": "Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor.", "entity1": "androgen receptor", "entity2": "Androgen", "span1": [98, 115], "span2": [0, 8]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8635": {"label": 2, "data": {"text": "In contrast, activation of Nrf2 by sulforaphane and tert-butylhydroquinone depend upon Keap1-C151 and not p62 (the canonical mechanism).", "entity1": "Nrf2", "entity2": "tert-butylhydroquinone", "span1": [27, 31], "span2": [52, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11021": {"label": 3, "data": {"text": "We compared the effects of Captopril (an ACE inhibitor with -SH group), enalapril (an ACE-inhibitor without -SH group), N-acetylcysteine (only -SH group not ACE inhibitor) on endothelial dysfunction injured by methionine-induced hyperhomocysteinemia (HHcy) in rats.", "entity1": "ACE", "entity2": "enalapril", "span1": [86, 89], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5713": {"label": 3, "data": {"text": "Indomethacin, used to inhibit cyclooxygenase, also inhibits AKR1C3 and displays selectivity over AKR1C1/AKR1C2.", "entity1": "cyclooxygenase", "entity2": "Indomethacin", "span1": [30, 44], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13701": {"label": 1, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.4", "entity2": "4-iodopropofol", "span1": [150, 158], "span2": [94, 108]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7445": {"label": 9, "data": {"text": "Reducing GSH levels in female mice CNS by pretreatment with diethyl maleate or L-propargyl glycine did not result in inhibition of complex I activity, unlike male mice.", "entity1": "complex I", "entity2": "diethyl maleate", "span1": [131, 140], "span2": [60, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3835": {"label": 3, "data": {"text": "Taken together, the data provide evidence that the synergistic antiproliferative effect of resveratrol and clofarabine is linked to the inhibition of Akt and Sp1 activities, and suggest that this combination may have therapeutic value in treatment of malignant mesothelioma.", "entity1": "Sp1", "entity2": "resveratrol", "span1": [158, 161], "span2": [91, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"65": {"label": 1, "data": {"text": "Histamine and asthma: an appraisal based on specific H1-receptor antagonism.", "entity1": "H1-receptor", "entity2": "Histamine", "span1": [53, 64], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"719": {"label": 1, "data": {"text": "Infrared spectroscopic studies revealed a reduced thermal stability both of the apo-and the holo-hTH1 on binding of H4biopterin and Lerythro-dihydrobiopterin (H2biopterin).", "entity1": "hTH1", "entity2": "H4biopterin", "span1": [97, 101], "span2": [116, 127]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15001": {"label": 3, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "cytokine", "entity2": "fatty acids", "span1": [123, 131], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8732": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "imipramine", "span1": [225, 231], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15186": {"label": 3, "data": {"text": "Moreover, compared with the model group, sophocarpine could significantly increase P-AMPK\u03b1 (>5.82-fold), AMPK\u03b1 (>1.29-fold) and ACC (>3.27-fold) protein expressions, and reduce P-ACC (<0.30-fold) and HNF-4\u03b1 (<0.20-fold) protein expression.", "entity1": "P-ACC", "entity2": "sophocarpine", "span1": [177, 182], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3375": {"label": 3, "data": {"text": "All GABA(A)R modulators induced a negative shift in the steady-state inactivation curve of Ca(v)1.3 channels, but only BDZs and pentobarbital induced a negative shift in Ca(v)1.2 channel inactivation.", "entity1": "Ca(v)1.2", "entity2": "pentobarbital", "span1": [170, 178], "span2": [128, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11885": {"label": 8, "data": {"text": "Ferredoxin 1 (FDX1; adrenodoxin) is an iron-sulfur protein that is involved in various metabolic processes, including steroid hormone synthesis in mammalian tissues.", "entity1": "FDX1", "entity2": "steroid", "span1": [14, 18], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3549": {"label": 2, "data": {"text": "The results demonstrated that intracerebral infusions of LTD4 (1 ng/mouse) produced memory impairment as determined by Morris water maze test and Y-maze test in mice, and caused the accumulation of A\u03b21-40 and A\u03b21-42 in the hippocampus and cortex through increased activity of \u03b2- and \u03b3-secretases accompanied with increased expression of amyloid precursor protein (APP).", "entity1": "A\u03b21-40", "entity2": "LTD4", "span1": [198, 204], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10495": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "SR 59230A", "span1": [392, 423], "span2": [333, 342]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10304": {"label": 3, "data": {"text": "As free sildenafil plasma concentrations approach concentrations sufficient to inhibit retinal PDE6, usually at higher therapeutic doses, transient, reversible visual adverse events can occur, albeit infrequently.", "entity1": "PDE6", "entity2": "sildenafil", "span1": [95, 99], "span2": [8, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11817": {"label": 8, "data": {"text": "Cytotoxicity assays demonstrated that epigallocatechin 3-O-gallate (EGCG) and most of compounds 1-6 killed preferentially OATP-expressing CHO cells.", "entity1": "OATP", "entity2": "epigallocatechin 3-O-gallate", "span1": [122, 126], "span2": [38, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15903": {"label": 1, "data": {"text": "The results were congruent and highly significant: Ca(2+) /H(+) -antiport activity is detectable only in acidic organelles expressing functional synaptotagmin-1.", "entity1": "synaptotagmin-1", "entity2": "H(+)", "span1": [145, 160], "span2": [59, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1359": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "DAT", "entity2": "hydroxyl", "span1": [317, 320], "span2": [226, 234]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4514": {"label": 8, "data": {"text": "Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also interact with carboxylesterases.", "entity1": "Uridine 5'-diphosphate- glucuronosyltransferases", "entity2": "acyl glucuronides", "span1": [0, 48], "span2": [153, 170]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11762": {"label": 1, "data": {"text": "The purpose of this study is to determine the effects on insulin sensitivity of a carbohydrate-rich diet (CARB; similar to the Dietary Approaches to Stop Hypertension [DASH] diet), a protein-rich diet (PROT; protein predominantly from plant sources), and an unsaturated fat-rich diet (UNSAT; predominantly monounsaturated).", "entity1": "insulin", "entity2": "carbohydrate", "span1": [57, 64], "span2": [82, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14853": {"label": 2, "data": {"text": "Interestingly, Acrolein increased proteins' levels of amyloid precursor protein (APP), \u03b2-secretase (BACE-1) and the amyloid \u03b2-peptide transporter receptor for advanced glycation end products, and decreased A-disintegrin and metalloprotease (ADAM) 10 levels.", "entity1": "amyloid \u03b2-peptide transporter", "entity2": "Acrolein", "span1": [116, 145], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"7813": {"label": 8, "data": {"text": "Compared with active peptides containing F or W, peptides containing E in either of these two positions were more than 10-fold less effective in effluxing cholesterol by the ABCA1 transporter.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [174, 179], "span2": [155, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15582": {"label": 1, "data": {"text": "We rescued cells lethally depleted of endogenous Cdk1 with an exogenous Cdk1 conferring sensitivity to one ATP analogue inhibitor (1NMPP1) and resistance to another (RO3306).", "entity1": "Cdk1", "entity2": "1NMPP1", "span1": [72, 76], "span2": [131, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10222": {"label": 8, "data": {"text": "AMP-activated protein kinase (AMPK) activity increases in response to depletion of cellular energy stores, and this enzyme has been implicated in the stimulation of glucose uptake into skeletal muscle and the inhibition of liver gluconeogenesis.", "entity1": "AMP-activated protein kinase", "entity2": "glucose", "span1": [0, 28], "span2": [165, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11239": {"label": 1, "data": {"text": "MCP-1 and MIP-2 was tested after 1, 10, 20, 30, and 40 days post inoculation, before and after mimosine treatment.", "entity1": "MCP-1", "entity2": "mimosine", "span1": [0, 5], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7558": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "eNOS", "entity2": "L-citrulline", "span1": [158, 162], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"972": {"label": 3, "data": {"text": "Expression of the dominant negative mutants rab5A-N133I or rab7-N125I blunted U50,488H-induced down-regulation.", "entity1": "rab7", "entity2": "U50,488H", "span1": [59, 63], "span2": [78, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11259": {"label": 8, "data": {"text": "The COX pathway generates inflammatory prostaglandins, while the 5-LOX pathway generates inflammatory leukotrienes.", "entity1": "COX", "entity2": "prostaglandins", "span1": [4, 7], "span2": [39, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13053": {"label": 3, "data": {"text": "Late INa induced by the VGSC long QT mutant R1623Q was reduced by resveratrol and quercetin.", "entity1": "VGSC", "entity2": "resveratrol", "span1": [24, 28], "span2": [66, 77]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3051": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "stromal cell-derived factor-1", "entity2": "Plerixafor", "span1": [111, 140], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5021": {"label": 0, "data": {"text": "Little is known regarding the transport activity and regulation of OATP2B1 variants with N-terminus truncation.", "entity1": "OATP2B1", "entity2": "N", "span1": [67, 74], "span2": [89, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6623": {"label": 0, "data": {"text": "In arginase, two cysteines at the C terminus of the protein are crucial for its epiarginase function but not for its catalytic activity and trimeric structure.", "entity1": "arginase", "entity2": "C", "span1": [3, 11], "span2": [34, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13888": {"label": 3, "data": {"text": "In addition, another study suggests that ibuprofen reduces generation of amyloid-beta42 peptide via inactivation of RhoA signaling, although it may also regulate amyloid-beta42 formation by direct inhibition of the gamma-secretase complex.", "entity1": "gamma-secretase complex", "entity2": "ibuprofen", "span1": [215, 238], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10526": {"label": 2, "data": {"text": "Metformin, a drug widely used in the treatment of type 2 diabetes, has recently been shown to act on skeletal muscle and liver in part through the activation of AMP-activated protein kinase (AMPK).", "entity1": "AMPK", "entity2": "Metformin", "span1": [191, 195], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9389": {"label": 1, "data": {"text": "Interactions of 2,3-benzodiazepines and cyclothiazide at AMPA receptors: patch clamp recordings in cultured neurones and area CA1 in hippocampal slices.", "entity1": "AMPA receptors", "entity2": "cyclothiazide", "span1": [57, 71], "span2": [40, 53]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2646": {"label": 8, "data": {"text": "The latter reaction, catalyzed by aspartoacylase (ASPA), produces acetyl groups plus aspartate and has been proposed to occur in both soluble and membranous subfractions of white matter.", "entity1": "ASPA", "entity2": "aspartate", "span1": [50, 54], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"11858": {"label": 8, "data": {"text": "The calcium homeostasis proteins sarcoendoplasmic reticulum ATPase 2a (SERCA2a), sodium calcium exchanger-1, phospholamban (PLB), phospho-PLB, and calsequestrin 2 are important for contraction and relaxation.", "entity1": "sodium calcium exchanger-1", "entity2": "calcium", "span1": [81, 107], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2449": {"label": 3, "data": {"text": "Colonic cyclooxygenase-2 and interkeukin-1beta mRNA and spinal c-FOS mRNA expression were significantly down-regulated by ATB-429, but not by mesalamine.", "entity1": "cyclooxygenase-2", "entity2": "ATB-429", "span1": [8, 24], "span2": [122, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6804": {"label": 9, "data": {"text": "Although celecoxib inhibits PG biosynthesis, most do not affect the peroxidase activity of COX, which can generate proximate carcinogens.", "entity1": "COX", "entity2": "celecoxib", "span1": [91, 94], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1154": {"label": 8, "data": {"text": "Growth inhibition of these tumor cell lines was associated with the dephosphorylation of EGFR, HER2, and HER3, accompanied by the loss of association of HER3 with phosphatidylinositolphosphatidylinositol 3-kinase, and down-regulation of Akt activity.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "phosphatidylinositol", "span1": [183, 212], "span2": [163, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2784": {"label": 1, "data": {"text": "The early insulin response to oral glucose was reduced in mice on HFD + GRA (1,890 +/- 160 vs 3,040 +/- 420 pmol/l; p = 0.012), but glucose excursions were improved.", "entity1": "insulin", "entity2": "glucose", "span1": [10, 17], "span2": [35, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2327": {"label": 1, "data": {"text": "Reboxetine, a selective norepinephrine reuptake inhibitor, exhibits high affinity and selectivity for the human norepinephrine transporter.", "entity1": "human norepinephrine transporter", "entity2": "Reboxetine", "span1": [106, 138], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12861": {"label": 9, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "phosphoserine", "span1": [236, 242], "span2": [146, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"5462": {"label": 3, "data": {"text": "Compared with aripiprazole, which significantly inhibited the firing activity of VTA DA neurons, brexpiprazole displayed less efficacy at D2 receptors.", "entity1": "D2 receptors", "entity2": "brexpiprazole", "span1": [138, 150], "span2": [97, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5978": {"label": 8, "data": {"text": "Present studies demonstrate that mushroom tyrosinase will also catalyze quinone methide production with the same active site copper if a suitable substrate such as 3,4-dihydroxymandelic acid is provided.", "entity1": "mushroom tyrosinase", "entity2": "3,4-dihydroxymandelic acid", "span1": [33, 52], "span2": [164, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, 8, -1, -1]},
	"6852": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "MTRR", "entity2": "Hcy", "span1": [208, 212], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13996": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "VEGFR2", "entity2": "Cabozantinib", "span1": [111, 117], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13483": {"label": 1, "data": {"text": "Autoradiography studies with [(3)H](-)-CP 55,940 show that chronic treatment with SR 141716A for 15 days twice daily (1 mg/kg i.p.) significantly increases the density of CB1 receptors in the PVN.", "entity1": "CB1 receptors", "entity2": "SR 141716A", "span1": [171, 184], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13069": {"label": 2, "data": {"text": "It was, therefore, proposed that H. pylori may in fact, antagonize, aspirin-induced delay of ulcer healing due to suppression of acid secretion by the enhancement in PGE(2) possibly derived from COX-2 expression and activity and to the overexpression of growth factors such as TGF alpha and VEGF.", "entity1": "COX-2", "entity2": "aspirin", "span1": [195, 200], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8623": {"label": 9, "data": {"text": "In contrast, activation of Nrf2 by sulforaphane and tert-butylhydroquinone depend upon Keap1-C151 and not p62 (the canonical mechanism).", "entity1": "p62", "entity2": "tert-butylhydroquinone", "span1": [106, 109], "span2": [52, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13506": {"label": 6, "data": {"text": "These data indicate that vecuronium, gallamine and pancuronium interact with an allosteric site on the muscarinic M2 receptor (located on the heart) and this may explain some of their cardiac side effects.", "entity1": "muscarinic M2 receptor", "entity2": "gallamine", "span1": [103, 125], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"4032": {"label": 3, "data": {"text": "This paper describes the identification and synthesis of substituted benzofurans as LTH(4)H inhibitors.", "entity1": "LTH(4)H", "entity2": "benzofurans", "span1": [84, 91], "span2": [69, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5154": {"label": 2, "data": {"text": "Our results showed that 2-hydroxy-3-methylanthraquinone decreased phosphorylation-ERK1/2 (p-ERK1/2), and increased p-p38MAPK, but did not affect expressions of p-JNK1/2 in U937 cells.", "entity1": "p-p38MAPK", "entity2": "2-hydroxy-3-methylanthraquinone", "span1": [115, 124], "span2": [24, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1855": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "CA I", "entity2": "acetazolamide", "span1": [134, 138], "span2": [211, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6786": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-2", "entity2": "nimesulide", "span1": [257, 262], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8786": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "FOXO3a", "entity2": "CAPE", "span1": [129, 135], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"830": {"label": 3, "data": {"text": "The inhibitory effect of PGE1 or sulprostone was prevented by pretreatment with pertussis toxin [islet activating protein (IAP)] or phorbol-12-myristate-13-acetate (PMA), and the protein kinase C (PKC) inhibitor chelerythrine blocked the action of PMA.", "entity1": "protein kinase C", "entity2": "chelerythrine", "span1": [179, 195], "span2": [212, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10642": {"label": 1, "data": {"text": "Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib).", "entity1": "COX-2", "entity2": "valdecoxib", "span1": [47, 52], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4310": {"label": 2, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "p38", "entity2": "AuF", "span1": [72, 75], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1946": {"label": 9, "data": {"text": "Several purinergic receptors have been described on platelets; P2X (1), a calcium channel, and P2Y1 a Gq-coupled seven-transmembrane domain receptor, have been found not to be antagonized by clopidogrel.", "entity1": "P2Y1", "entity2": "clopidogrel", "span1": [95, 99], "span2": [191, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8681": {"label": 3, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "TAp63", "entity2": "cisplatin", "span1": [232, 237], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12481": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO5", "entity2": "benzydamine", "span1": [33, 37], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4515": {"label": 8, "data": {"text": "Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also interact with carboxylesterases.", "entity1": "carboxylesterases", "entity2": "acyl glucuronides", "span1": [70, 87], "span2": [153, 170]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13146": {"label": 2, "data": {"text": "CONCLUSION: CysLT1 receptor expression in neurons is upregulated after NMDA injection, and NMDA-induced responses are inhibited by CysLT1 receptor antagonists, indicating that the increased CysLT1 receptor is involved in NMDA excitotoxicity.", "entity1": "CysLT1 receptor", "entity2": "NMDA", "span1": [12, 27], "span2": [71, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1865": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "kushenol K", "span1": [221, 251], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15342": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "acenaphthene", "span1": [39, 48], "span2": [183, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9003": {"label": 5, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "8-p-(sulfophenyl)theophylline", "span1": [0, 9], "span2": [165, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7273": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "benzolamide", "span1": [218, 224], "span2": [188, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14993": {"label": 9, "data": {"text": "In monocytes, both EPA and DHA increased interleukin (IL)-10 without affecting tumor necrosis factor (TNF)-\u03b1 and IL-6.", "entity1": "IL-6", "entity2": "EPA", "span1": [113, 117], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8280": {"label": 2, "data": {"text": "We found that treatment of both differentiated dopaminergic-like SH-SY5Y cells and rat midbrain slices with the dopamine D2 receptor (D2R) agonist, quinpirole, triggered an increase in the expression of GDNF that was temporally preceded by an increase in the levels of zinc-finger protein 268 (Zif268), a DNA-binding transcription factor encoded by an immediate-early gene.", "entity1": "GDNF", "entity2": "quinpirole", "span1": [203, 207], "span2": [148, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14386": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "Akt", "entity2": "AG1478", "span1": [142, 145], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11177": {"label": 1, "data": {"text": "METHODS: Expression of PR mRNA and PR protein were determined by Northern blot and HAP of single-dose saturated analysis in myometrium and leiomyomata (center and marginal area) from 27 untreated and 6 mifepristone pretreated women with leiomyomata.", "entity1": "PR mRNA", "entity2": "mifepristone", "span1": [23, 30], "span2": [202, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8842": {"label": 2, "data": {"text": "In the presence of H2O2, calycopterin inhibited decrease in GSH level and SOD activity.", "entity1": "SOD", "entity2": "calycopterin", "span1": [74, 77], "span2": [25, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6888": {"label": 1, "data": {"text": "Sterol transporters: targets of natural sterols and new lipid lowering drugs.", "entity1": "Sterol transporters", "entity2": "sterols", "span1": [0, 19], "span2": [40, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"573": {"label": 2, "data": {"text": "These results suggest that the megabase DNA fragmentation is induced as a consequence of inhibition of thymidylate synthase by Tomudex and kilobase DNA fragmentation may correlate with the reduction of p27(kip1) expression and the increase in cyclin E and cdk2 kinase activities.", "entity1": "kinase", "entity2": "Tomudex", "span1": [261, 267], "span2": [127, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15878": {"label": 2, "data": {"text": "Additionally, treatment with glucose/iron showed a higher HO activity.", "entity1": "HO", "entity2": "glucose", "span1": [58, 60], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11680": {"label": 0, "data": {"text": "The C-terminal antibodies detected both proteins in extracts of mouse medulla/pons, cortex, hypothalamus, and cerebellum but only the 73 kD protein and higher molecular weight immunoreactive proteins in mouse adrenal and rat PC12 cells, which are positive controls for rodent VMAT-1.", "entity1": "rodent VMAT-1", "entity2": "C", "span1": [269, 282], "span2": [4, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11212": {"label": 6, "data": {"text": "In addition to studies focused on the mechanisms of nuclear receptor function, additional work has illuminated the mechanism by which androgens are metabolized in selected tissues.", "entity1": "nuclear receptor", "entity2": "androgens", "span1": [52, 68], "span2": [134, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3505": {"label": 2, "data": {"text": "Exposure to PAHs, their metabolites, and ROS further increase AKRs isoform expression that may amplify oxidative damage.", "entity1": "AKRs", "entity2": "PAHs", "span1": [62, 66], "span2": [12, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6275": {"label": 3, "data": {"text": "The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro.", "entity1": "angiotensin II type 1 receptor", "entity2": "losartan", "span1": [49, 79], "span2": [124, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4795": {"label": 8, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP3A", "entity2": "dextromethorphan", "span1": [148, 153], "span2": [88, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15692": {"label": 1, "data": {"text": "Conclusion The results of this work contribute information regarding the antinociceptive properties of CAT on acute pain and show that, at least in part, TRPV1, TRPM8, ASIC, glutamate receptors, PKC and PKA participate in CAT's antinociceptive mechanism.", "entity1": "TRPM8", "entity2": "CAT", "span1": [161, 166], "span2": [222, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"922": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "timolol", "span1": [22, 39], "span2": [175, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9697": {"label": 4, "data": {"text": "These profiles suggest a mechanism of action for each agent, 5-HT1A agonism for ziprasidone and alpha 1 antagonism for clozapine and olanzapine.", "entity1": "5-HT1A", "entity2": "ziprasidone", "span1": [61, 67], "span2": [80, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7041": {"label": 5, "data": {"text": "Thus, severe LV dysfunction and accompanying abnormal myocardial bioenergetic phenotype were prevented by the AT1 antagonist olmesartan medoxomil.", "entity1": "AT1", "entity2": "olmesartan medoxomil", "span1": [110, 113], "span2": [125, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14068": {"label": 1, "data": {"text": "Exogenous stimulation of PKA activity, achieved by forskolin treatment, protected K-ras-transformed cells from apoptosis induced by glucose deprivation, enhanced complex I activity, intracellular adenosine triphosphate (ATP) levels, mitochondrial fusion and decreased intracellular reactive oxygen species (ROS) levels.", "entity1": "K-ras", "entity2": "forskolin", "span1": [82, 87], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4634": {"label": 1, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [128, 131], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"247": {"label": 3, "data": {"text": "Indomethacin inhibited both hCOX-1 and hCOX-2, whereas NS-398 and Dup-697 selectively inhibited hCOX-2.", "entity1": "hCOX-2", "entity2": "NS-398", "span1": [96, 102], "span2": [55, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7317": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SLC1", "entity2": "amino acids", "span1": [190, 194], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4368": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "dexamethasone 21-phosphate", "span1": [171, 176], "span2": [192, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12614": {"label": 1, "data": {"text": "The nuclear gene transcription factors RAR beta and RAR gamma mediate the retinoid activity of adapalene.", "entity1": "nuclear gene transcription factors", "entity2": "adapalene", "span1": [4, 38], "span2": [95, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16053": {"label": 3, "data": {"text": "The HCV-PIs boceprevir and telaprevir are both, to different extents, inhibitors of CYP3A.", "entity1": "CYP3A", "entity2": "boceprevir", "span1": [84, 89], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3528": {"label": 0, "data": {"text": "While DNA damage does not affect phosphorylation at the PDK-1 site Thr350/Thr308 of AKT-1, it increased phosphorylation at Ser517/Ser473.", "entity1": "AKT-1", "entity2": "Ser", "span1": [84, 89], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"416": {"label": 1, "data": {"text": "The quinazoline antagonists, prazosin, doxazosin and alfuzosin displayed high affinity but were non selective for the three cloned human alpha 1 adrenoceptors.", "entity1": "human alpha 1 adrenoceptors", "entity2": "alfuzosin", "span1": [131, 158], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13598": {"label": 5, "data": {"text": "Desvenlafaxine succinate (DVS) is a recently introduced antagonist of the human norepinephrine and serotonin transporters (hNET and hSERT, respectively), currently in clinical development for use in the treatment of major depressive disorder and vasomotor symptoms associated with menopause.", "entity1": "hSERT", "entity2": "Desvenlafaxine succinate", "span1": [132, 137], "span2": [0, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13700": {"label": 3, "data": {"text": "Moreover, activation of transfected cells and porcine PBMC by TLR7 ligands was inhibited by bafilomycin A(1) indicating the requirement of endosomal/lysosomal acidification for activation of the receptors.", "entity1": "TLR7", "entity2": "bafilomycin A(1)", "span1": [62, 66], "span2": [92, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11230": {"label": 1, "data": {"text": "The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide.", "entity1": "insulin", "entity2": "mitiglinide", "span1": [98, 105], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11668": {"label": 1, "data": {"text": "Within each pentamer most of the contacts between S100A4 dimers occurs through the TFP moieties.", "entity1": "S100A4", "entity2": "TFP", "span1": [50, 56], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10645": {"label": 1, "data": {"text": "The overall saturation binding affinity for COX-2 of valdecoxib is 2.6 nM (compared with 1.6 nM for celecoxib, 51 nM for rofecoxib, and 260 nM for etoricoxib), with a slow off-rate (t(1/2) approximately 98 min).", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [44, 49], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5531": {"label": 2, "data": {"text": "In direct adenylyl cyclase activation, in effects on adenylyl cyclase after pretreatment of intact cells, and in guinea pig tracheal relaxation assays, IAS and the parent drug salmeterol behave essentially the same.", "entity1": "adenylyl cyclase", "entity2": "salmeterol", "span1": [10, 26], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8281": {"label": 2, "data": {"text": "We found that treatment of both differentiated dopaminergic-like SH-SY5Y cells and rat midbrain slices with the dopamine D2 receptor (D2R) agonist, quinpirole, triggered an increase in the expression of GDNF that was temporally preceded by an increase in the levels of zinc-finger protein 268 (Zif268), a DNA-binding transcription factor encoded by an immediate-early gene.", "entity1": "zinc-finger protein 268", "entity2": "quinpirole", "span1": [269, 292], "span2": [148, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4800": {"label": 1, "data": {"text": "The neurotrophic factors pleiotrophin (PTN) and midkine (MK) have been shown to modulate amphetamine-induced neurotoxicity.", "entity1": "midkine", "entity2": "amphetamine", "span1": [48, 55], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9762": {"label": 5, "data": {"text": "Herein, we evaluate the interaction of the alpha(2)-AR antagonist, yohimbine, as compared to fluparoxan, at multiple monoaminergic receptors and examine their roles in the modulation of adrenergic, dopaminergic and serotonergic transmission in freely-moving rats.", "entity1": "alpha(2)-AR antagonist", "entity2": "yohimbine", "span1": [43, 65], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"264": {"label": 0, "data": {"text": "Cyclodiene resistance in D. melanogaster has been attributed to a mutation resulting in an Ala302-->Ser replacement in the Rdl GABA receptor subunit and in D. simulans to an homologous Ala-->Ser or Gly replacement.", "entity1": "Rdl GABA receptor", "entity2": "Ala", "span1": [123, 140], "span2": [185, 188]}, "weak_labels": [-1, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12696": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "pyruvate", "span1": [79, 90], "span2": [94, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5212": {"label": 1, "data": {"text": "In the present study, the exposure of melanoma cells to vinblastine was found to trigger apoptosis as evidenced by the loss of mitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activation of caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase.", "entity1": "Poly (ADP-ribose)-Polymerase", "entity2": "vinblastine", "span1": [272, 300], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12891": {"label": 1, "data": {"text": "Hydrogen sulfide inhibits nitric oxide production and nuclear factor-kappaB via heme oxygenase-1 expression in RAW264.7 macrophages stimulated with lipopolysaccharide.", "entity1": "heme oxygenase-1", "entity2": "Hydrogen sulfide", "span1": [80, 96], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"281": {"label": 4, "data": {"text": "Cardiac effects of the beta 3-adrenoceptor agonist BRL35135 in man.", "entity1": "beta 3-adrenoceptor", "entity2": "BRL35135", "span1": [23, 42], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11747": {"label": 0, "data": {"text": "Moreover, the observed insertion of proline into the lid domain of the Ves a 1 structure is rare.", "entity1": "Ves a 1", "entity2": "proline", "span1": [71, 78], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8230": {"label": 2, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "EAG", "entity2": "ICA-105574", "span1": [101, 104], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3147": {"label": 1, "data": {"text": "Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization.", "entity1": "TrkA", "entity2": "Amitriptyline", "span1": [80, 84], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5360": {"label": 3, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "I-\u03baB\u03b5", "entity2": "vitamin C", "span1": [134, 139], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1035": {"label": 1, "data": {"text": "Pranlukast is a new, orally active, selective inhibitor of CysLt1 leukotriene receptor.", "entity1": "CysLt1", "entity2": "leukotriene", "span1": [59, 65], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13061": {"label": 3, "data": {"text": "Similar to AMR and AMROH, adriamycin and etoposide (VP-16) are DNA topoisomerase II inhibitors.", "entity1": "DNA topoisomerase II", "entity2": "adriamycin", "span1": [63, 83], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2472": {"label": 2, "data": {"text": "Independent of dietary choline, supplemental Met increased hepatic BHMT activity approximately 30%.", "entity1": "BHMT", "entity2": "Met", "span1": [67, 71], "span2": [45, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15134": {"label": 8, "data": {"text": "BCRP appeared to play a more important role for absorption and intestinal and renal elimination of apixaban than P-gp in transporter-KO rats after oral and i.v.", "entity1": "P-gp", "entity2": "apixaban", "span1": [113, 117], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7959": {"label": 5, "data": {"text": "Here, we compared the effects of a dimeric PSD-95 inhibitor, UCCB01-125, and the NMDAR antagonist, MK-801, on mechanical hypersensitivity in the complete Freund's adjuvant (CFA) model of inflammatory pain.", "entity1": "NMDAR", "entity2": "MK-801", "span1": [81, 86], "span2": [99, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15966": {"label": 1, "data": {"text": "We recently showed that the first domain of human CCS (hCCSD1) is responsible for copper transfer to its protein partner, human SOD1 (hSOD1).", "entity1": "human CCS", "entity2": "copper", "span1": [44, 53], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14881": {"label": 3, "data": {"text": "In cultured primary microglia and astrocytes, EHT had a direct anti-inflammatory effect demonstrated by repression of lipopolysaccharide-induced NF\u03baB activation, iNOS induction, and nitric oxide production.", "entity1": "iNOS", "entity2": "EHT", "span1": [162, 166], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4217": {"label": 1, "data": {"text": "Although dopaminergic neurons within the nigrostriatal pathway appear intact, Mn-induced irregularities in DA transmission have been observed including decreased amphetamine-induced DA release and loss of the dopamine transporter (DAT).", "entity1": "DAT", "entity2": "Mn", "span1": [231, 234], "span2": [78, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2017": {"label": 3, "data": {"text": "The aim of this study was to determine the mechanism of pranlukast-induced interleukin-5 (IL-5) inhibition in allergic inflammation.", "entity1": "interleukin-5", "entity2": "pranlukast", "span1": [75, 88], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8033": {"label": 9, "data": {"text": "Dietary carbohydrates increase SCD-1 gene expression in liver by sterol response element binding protein (SREBP)-1c-dependent and SREBP-1c -independent pathways.", "entity1": "SREBP-1c", "entity2": "carbohydrates", "span1": [130, 138], "span2": [8, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2981": {"label": 1, "data": {"text": "The results quantify the role of PDE5 catalytic-site residues for cGMP and inhibitors, indicate that Tyr-612, Gln-817, and Phe-820 are the most important cGMP or inhibitor contacts studied, and identify residues that contribute to selectivity among different classes of inhibitors.", "entity1": "PDE5", "entity2": "cGMP", "span1": [33, 37], "span2": [154, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5187": {"label": 1, "data": {"text": "Dioscin-induced autophagy via ERK1/2 and JNK1/2 pathways may provide a protective mechanism for cell survival against dioscin-induced apoptosis to act as a cytoprotective reaction.", "entity1": "JNK1/2", "entity2": "dioscin", "span1": [41, 47], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7479": {"label": 2, "data": {"text": "Additionally, Na+ and Cl- ions coactivate GluR6 receptors by establishing a dipole, accounting for their common effect on KARs.", "entity1": "GluR6", "entity2": "Cl-", "span1": [42, 47], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7": {"label": 5, "data": {"text": "It is concluded that labetalol and dilevalol are beta 1-adrenoceptor selective antagonists.", "entity1": "beta 1-adrenoceptor", "entity2": "labetalol", "span1": [49, 68], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12658": {"label": 8, "data": {"text": "These data directly demonstrate that NKCC1 is the major Cl(-) uptake mechanism across the basolateral membrane of acinar cells and is critical for driving saliva secretion in vivo.", "entity1": "NKCC1", "entity2": "Cl(-)", "span1": [37, 42], "span2": [56, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6422": {"label": 2, "data": {"text": "Thus, bezafibrate treatment resulted in an 8-fold induction in UCP-3 mRNA levels in preadipocytes compared with the 3.5-fold induction observed in adipocytes.", "entity1": "UCP-3", "entity2": "bezafibrate", "span1": [63, 68], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5255": {"label": 2, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "p21", "entity2": "rofecoxib", "span1": [96, 99], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10335": {"label": 2, "data": {"text": "Pre-treatment with arsenite increased protein kinase B (Akt) and extracellular signal regulated kinase 1/2 (ERK1/2) phosphorylation after H2O2.", "entity1": "protein kinase B", "entity2": "H2O2", "span1": [38, 54], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4774": {"label": 3, "data": {"text": "Inhibition of angiogenesis and invasion by DMBT is mediated by downregulation of VEGF and MMP-9 through Akt pathway in MDA-MB-231 breast cancer cells.", "entity1": "Akt", "entity2": "DMBT", "span1": [104, 107], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2071": {"label": 8, "data": {"text": "Apolipoprotein E3 (apoE3) safeguards pig proximal tubular LLC-PK1 cells against reduction in SGLT1 activity induced by gentamicin C.\tMegalin, a family of endocytic receptors related to the low-density lipoprotein (LDL) receptor, is a major pathway for proximal tubular aminoglycoside accumulation.", "entity1": "endocytic receptors", "entity2": "aminoglycoside", "span1": [154, 173], "span2": [269, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11441": {"label": 1, "data": {"text": "We also studied the effects of thalidomide on COX-1, COX-2 or bcl-2 expression, TNFalpha, VEGF, GSH and cytochrome c in these cells.", "entity1": "TNFalpha", "entity2": "thalidomide", "span1": [80, 88], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1368": {"label": 0, "data": {"text": "The L0 linker has been reported to be required for glibenclamide binding, and DeltaNK(IR)6.2/SUR1 channels exhibit reduced labeling of K(IR) with (125)I-azidoglibenclamide, implying that the K(IR) N terminus and L0 of SUR1 are in proximity.", "entity1": "K(IR)", "entity2": "N", "span1": [191, 196], "span2": [197, 198]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10221": {"label": 3, "data": {"text": "Metformin treatment for 10 weeks significantly increased AMPK alpha2 activity in the skeletal muscle, and this was associated with increased phosphorylation of AMPK on Thr172 and decreased acetyl-CoA carboxylase-2 activity.", "entity1": "acetyl-CoA carboxylase-2", "entity2": "Metformin", "span1": [189, 213], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13560": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase (DDAH) metabolizes asymmetric dimethylarginine to generate L-citrulline and is present in large quantities in the kidney.", "entity1": "Dimethylarginine dimethylaminohydrolase", "entity2": "L-citrulline", "span1": [0, 39], "span2": [99, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2840": {"label": 7, "data": {"text": "The enzyme requires PLP and divalent cations such as Ca(2+), Mg(2+), or Mn(2+), but not ATP, whereas mammalian serine racemase activity is increased by ATP.", "entity1": "serine racemase", "entity2": "PLP", "span1": [111, 126], "span2": [20, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8468": {"label": 3, "data": {"text": "Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.", "entity1": "c-Met", "entity2": "5-(benzyloxy)pyridin-2(1H)-one", "span1": [59, 64], "span2": [6, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8113": {"label": 3, "data": {"text": "The mechanism revealed that wogonin inhibited H2O2-induced phosphorylation of caveolin-1 (cav-1) associating with the suppression of stabilization of VE-cadherin and \u03b2-catenin.", "entity1": "cav-1", "entity2": "wogonin", "span1": [90, 95], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"913": {"label": 1, "data": {"text": "None of the drugs caused a significant inhibition of [(3)H]-saxitoxin binding to neurotoxin receptor site 1, even at concentrations as high as 250 microM.", "entity1": "neurotoxin receptor site 1", "entity2": "[(3)H]-saxitoxin", "span1": [81, 107], "span2": [53, 69]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15955": {"label": 1, "data": {"text": "Furthermore, OHT-stimulated cleavage of cyclin E and migration were tremendously attenuated by G15, a GPR30 antagonist, or siRNA against GPR30.", "entity1": "cyclin E", "entity2": "OHT", "span1": [40, 48], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7537": {"label": 8, "data": {"text": "10), is an 18-kDa integral nuclear membrane protein that belongs to a superfamily of membrane-associated proteins in eicosanoid and glutathione metabolism that includes 5-lipoxygenase-activating protein, microsomal glutathione S-transferases (MGSTs), and microsomal prostaglandin E synthase 1 (ref.", "entity1": "microsomal prostaglandin E synthase 1", "entity2": "glutathione", "span1": [255, 292], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"771": {"label": 0, "data": {"text": "Flecainide block of Na(+) current (I(Na)) was investigated in wild-type (WT) or the long QT syndrome 3 (LQT3) sodium channel alpha subunit mutation with three amino acids deleted (DeltaKPQ) stably transfected into human embryonic kidney 293 cells using whole-cell, patch-clamp recordings.", "entity1": "DeltaKPQ", "entity2": "amino acids", "span1": [180, 188], "span2": [159, 170]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1948": {"label": 1, "data": {"text": "These results demonstrate that this receptor corresponds to the previously called \"P2t\" platelet receptor and show that the active metabolite of clopidogrel binds in a covalent manner to this receptor, thus explaining how it blocks the aggregating effect of ADP on platelets.", "entity1": "P2t", "entity2": "clopidogrel", "span1": [83, 86], "span2": [145, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7733": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LHRH", "entity2": "triptorelin", "span1": [39, 43], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5444": {"label": 3, "data": {"text": "Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae \u03b2-carbonic anhydrase.", "entity1": "Saccharomyces cerevisiae \u03b2-carbonic anhydrase", "entity2": "cyanoacrylamide", "span1": [76, 121], "span2": [34, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15016": {"label": 3, "data": {"text": "Through immunoblotting analysis, it was found that AdOx was capable of indirectly diminishing the phosphorylation of oncogenic Src and its kinase activity.", "entity1": "Src", "entity2": "AdOx", "span1": [127, 130], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6577": {"label": 8, "data": {"text": "The bacterial enzyme maltodextrin phosphorylase (MalP) catalyses the phosphorolysis of an alpha-1,4-glycosidic bond in maltodextrins, removing the non-reducing glucosyl residues of linear oligosaccharides as glucose-1-phosphate (Glc1P).", "entity1": "maltodextrin phosphorylase", "entity2": "glucose-1-phosphate", "span1": [21, 47], "span2": [208, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15495": {"label": 0, "data": {"text": "We used whole-cell recordings of human embryonic kidney cells heterologously expressing either wild-type TRPA1 or TRPA1 with three serine-substituted cysteines crucial for electrophile activation (C621S, C641S, C665S).", "entity1": "C665S", "entity2": "cysteines", "span1": [211, 216], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3489": {"label": 2, "data": {"text": "In the CCl4 hepatotoxicity model, pre-treatment with PSM or silymarin resulted in significantly increased activities of ethylmorphine-N-demethylase and aniline 4-hydroxylase activity and cytochrome P450, compared to the CCl4 only group.", "entity1": "aniline 4-hydroxylase", "entity2": "silymarin", "span1": [152, 173], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6525": {"label": 9, "data": {"text": "Almost all patients with SUR1 (38/41) or KIR6.2 (5/7) mutations were resistant to diazoxide.", "entity1": "SUR1", "entity2": "diazoxide", "span1": [25, 29], "span2": [82, 91]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6470": {"label": 8, "data": {"text": "Diacylglycerol kinase (DGK) catalyzes the conversion of diacylglycerol to phosphatidic acid, making it an attractive candidate for a signal transduction component.", "entity1": "DGK", "entity2": "phosphatidic acid", "span1": [23, 26], "span2": [74, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"12477": {"label": 8, "data": {"text": "This group of drugs contains secondary or primary amines, and these results suggest that UGT2B10 preferably conjugates tertiary amines.", "entity1": "UGT2B10", "entity2": "tertiary amines", "span1": [89, 96], "span2": [119, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15509": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "Prx1", "entity2": "Cys", "span1": [163, 167], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4161": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "NF-\u03baB", "entity2": "perviridicin B", "span1": [173, 178], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12837": {"label": 9, "data": {"text": "When expressed heterologously in a mammalian cell line, rabbit PAT1 mediates pH-dependent, Na(+)-independent uptake of proline, glycine, l-alanine and alpha-(methylamino)isobutyric acid.", "entity1": "rabbit PAT1", "entity2": "Na(+)", "span1": [56, 67], "span2": [91, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4518": {"label": 8, "data": {"text": "Carboxylesterases hydrolyze esters, amides, and thioesters to produce carboxylic acids and resulting alcohols, amines, and thiols, respectively.", "entity1": "Carboxylesterases", "entity2": "amines", "span1": [0, 17], "span2": [111, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11853": {"label": 8, "data": {"text": "The calcium homeostasis proteins sarcoendoplasmic reticulum ATPase 2a (SERCA2a), sodium calcium exchanger-1, phospholamban (PLB), phospho-PLB, and calsequestrin 2 are important for contraction and relaxation.", "entity1": "PLB", "entity2": "calcium", "span1": [124, 127], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7078": {"label": 2, "data": {"text": "Menthol, popularly known for its cooling effect, activates TRPM8--a cold-activated thermoTRP ion channel.", "entity1": "thermoTRP ion channel", "entity2": "Menthol", "span1": [83, 104], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12354": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPV3", "entity2": "apomorphine", "span1": [35, 41], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14481": {"label": 8, "data": {"text": "Human liver microsomes of the wild-type CYP2D6 metabolized 5-methoxytryptamine to serotonin more effectively than did the defective CYP2D6*4*4 ones.", "entity1": "CYP2D6", "entity2": "serotonin", "span1": [40, 46], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13100": {"label": 4, "data": {"text": "Glinides, sulfonylureas, and other acidified sulfonamides may be promising leads in the development of new PPARgamma agonists.", "entity1": "PPARgamma", "entity2": "Glinides", "span1": [107, 116], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10256": {"label": 9, "data": {"text": "No trans-stimulation of [3H]-MPP+ outflow was observed by the OCTN1 and OCTN2 substrate carnitine at 100 microM.", "entity1": "OCTN1", "entity2": "[3H]-MPP+", "span1": [62, 67], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7527": {"label": 8, "data": {"text": "Brain cyclooxygenases (COX), the rate-limiting enzyme in prostaglandin synthesis, is rapidly and transiently induced by convulsions in hippocampal and cortical neurons.", "entity1": "COX", "entity2": "prostaglandin", "span1": [23, 26], "span2": [57, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5502": {"label": 1, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "dezocine", "span1": [108, 126], "span2": [45, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11650": {"label": 1, "data": {"text": "To confirm molecular recognition of tinzaparin by VLA-4, a surface acoustic wave-biosensor was applied.", "entity1": "VLA-4", "entity2": "tinzaparin", "span1": [50, 55], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3742": {"label": 1, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "AhR", "entity2": "TCDD", "span1": [61, 64], "span2": [110, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15251": {"label": 1, "data": {"text": "Selective oxidation of \u03c9-tertiary amine self-assembled thiol monolayers to tertiary amine N-oxides is shown to transform the adhesion of model proteins lysozyme and fibrinogen upon them.", "entity1": "fibrinogen", "entity2": "tertiary amine N-oxides", "span1": [165, 175], "span2": [75, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7322": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "sodium-coupled neutral amino acid transporter 1", "entity2": "amino acids", "span1": [274, 321], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13853": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "norelgestromin", "span1": [252, 261], "span2": [163, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13020": {"label": 8, "data": {"text": "It has been known for decades that lithium chloride (LiCl) leads to D-myo-inositol 1-phosphate accumulation on GPCR activation by inhibiting inositol monophosphatase, the final enzyme of the IP3 metabolic cascade.", "entity1": "inositol monophosphatase", "entity2": "D-myo-inositol 1-phosphate", "span1": [141, 165], "span2": [68, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"141": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited the actin-activated Mg2+-ATPase activity of smooth muscle myosin (IC50 = 25.1 microM).", "entity1": "Mg2+-ATPase", "entity2": "Felodipine", "span1": [67, 78], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14780": {"label": 0, "data": {"text": "The CSN/IRF5 interaction occurred on the carboxyl and amino termini of IRF5; a single internal deletion from amino acids 455 to 466 (\u0394455-466) was found to significantly reduce IRF5 protein stability.", "entity1": "IRF5", "entity2": "amino", "span1": [71, 75], "span2": [54, 59]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5036": {"label": 3, "data": {"text": "Nitrooxy derivatives showed NO-dependent vasorelaxing properties, while most of the compounds proved to be very potent and selective COX-2 inhibitors in in vitro experimental models.", "entity1": "COX-2", "entity2": "Nitrooxy", "span1": [133, 138], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2719": {"label": 2, "data": {"text": "Indomethacin treatment led to an increase in lipid peroxidation, glutathione peroxidase and glucose-6-phosphate dehydrogenase activities and to a decrease in catalase activity and glutathione levels in gastric mucosa.", "entity1": "glucose-6-phosphate dehydrogenase", "entity2": "Indomethacin", "span1": [92, 125], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12074": {"label": 1, "data": {"text": "Nicotinic acid and acipimox interfere with the biosynthesis of LDL and can also improve the clearance of VLDL/LDL.", "entity1": "LDL", "entity2": "Nicotinic acid", "span1": [63, 66], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13622": {"label": 9, "data": {"text": "In experimental models, rasagiline has been found to have neuroprotective properties that may be independent of MAO-B inhibition.", "entity1": "MAO-B", "entity2": "rasagiline", "span1": [112, 117], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8154": {"label": 3, "data": {"text": "Additionally, DPEP suppressed the production of inflammatory cytokines, including tumor necrosis factor-\u03b1 (TNF-\u03b1), interleukin (IL)-1\u03b2, and IL-6.", "entity1": "cytokines", "entity2": "DPEP", "span1": [61, 70], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8737": {"label": 1, "data": {"text": "In conclusion, this study expands the understanding of the substrate specificity of UGT2B10, highlighting its preference for tertiary amines with higher affinities and clearance values than those of UGT1A4 and UGT1A3.", "entity1": "UGT2B10", "entity2": "tertiary amines", "span1": [84, 91], "span2": [125, 140]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15917": {"label": 4, "data": {"text": "The current study examined the bioactivation potential of ghrelin receptor inverse agonists, 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(imidazo[2,1-b]thiazol-6-yl)ethanone (1) and 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone (2), containing a fused imidazo[2,1-b]thiazole motif in the core structure.", "entity1": "ghrelin receptor", "entity2": "imidazo[2,1-b]thiazole", "span1": [58, 74], "span2": [369, 391]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8905": {"label": 8, "data": {"text": "The identity of the lung beta-ADHs was further demonstrated by their characteristic pH-activity profiles for ethanol oxidation, Km values for NAD and ethanol, and inhibition by 4-methylpyrazole or 1,10-phenanthroline.", "entity1": "beta-ADHs", "entity2": "ethanol", "span1": [25, 34], "span2": [150, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"959": {"label": 5, "data": {"text": "In the rabbit pulmonary artery, rilmenidine and oxymetazoline are potent full agonists, whereas in the human atrial appendages they are antagonists at the alpha(2)-autoreceptors, sharing this property with rauwolscine, phentolamine, and idazoxan.", "entity1": "alpha(2)-autoreceptors", "entity2": "rauwolscine", "span1": [155, 177], "span2": [206, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8282": {"label": 2, "data": {"text": "We found that treatment of both differentiated dopaminergic-like SH-SY5Y cells and rat midbrain slices with the dopamine D2 receptor (D2R) agonist, quinpirole, triggered an increase in the expression of GDNF that was temporally preceded by an increase in the levels of zinc-finger protein 268 (Zif268), a DNA-binding transcription factor encoded by an immediate-early gene.", "entity1": "Zif268", "entity2": "quinpirole", "span1": [294, 300], "span2": [148, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10426": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "RARgamma", "entity2": "Tazarotene", "span1": [144, 152], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11299": {"label": 8, "data": {"text": "The protein exhibited modest H(2)O(2)-dependent peroxidase activities with guaiacol, potassium iodide, and 2,2(')-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS).", "entity1": "peroxidase", "entity2": "potassium iodide", "span1": [48, 58], "span2": [85, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11051": {"label": 3, "data": {"text": "For some, pharmacologic inhibitors are available, including sorafenib for BRAF, farnesyltransferase inhibitors for NRAS, PD-0325901 for mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, rapamycin analogues for mammalian target of rapamycin, and agents that inhibit either vascular endothelial growth factor or its receptors.", "entity1": "extracellular signal-regulated kinase kinase", "entity2": "PD-0325901", "span1": [169, 213], "span2": [121, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5140": {"label": 1, "data": {"text": "An intermediate GTX2,3-aldehyde was first synthesized by activating the NH2 group of the 2nd and 8th amino acid residues with three different aldehydes and two artificial complete antigens GTX2,3-aldehyde-bovine serum albumin (BSA) and GTX2,3-aldehyde- keyhole limpet hemocyanin (KLH) were then prepared by cross-linking the intermediate with BSA or KLH.", "entity1": "bovine serum albumin", "entity2": "GTX2,3-aldehyde", "span1": [205, 225], "span2": [189, 204]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2263": {"label": 1, "data": {"text": "Ethanol withdrawal significantly increased the packing density of GS- and GFAP-IR astrocytes in the PLC of P rats as compared with P rats with continuous access to ethanol.", "entity1": "GS", "entity2": "Ethanol", "span1": [66, 68], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10735": {"label": 5, "data": {"text": "For the vasopressin V1A/oxytocin receptor antagonist atosiban, none of the receptor constructs were able to provide a binding with higher affinity than the starting vasopressin V2 receptor.", "entity1": "vasopressin V1A/oxytocin receptor", "entity2": "atosiban", "span1": [8, 41], "span2": [53, 61]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3071": {"label": 3, "data": {"text": "PURPOSE: To compare phenelzine (PLZ), an antidepressant drug with anxiolytic properties which inhibits monoamine oxidase (MAO) but also elevates rat brain levels of the amino acids ?-aminobutyric acid (GABA) and alanine (ALA), with vigabatrin (VIG), an anticonvulsant which elevates brain GABA by inhibition of GABA transaminase (GABA-T), with regard to their actions on brain levels of GABA and ALA and on activities of MAO, GABA-T and ALA transaminase (ALA-T).", "entity1": "MAO", "entity2": "phenelzine", "span1": [122, 125], "span2": [20, 30]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10589": {"label": 3, "data": {"text": "Auranofin, an antirheumatic gold compound, is an inhibitor of selenocysteine enzymes, such as thioredoxin reductase and glutathione peroxidase.", "entity1": "glutathione peroxidase", "entity2": "Auranofin", "span1": [120, 142], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1918": {"label": 8, "data": {"text": "Carnitine acetyltransferases (CrAT) catalyze the reversible conversion of acetyl-CoA and carnitine to acetylcarnitine and free CoA.", "entity1": "CrAT", "entity2": "acetylcarnitine", "span1": [30, 34], "span2": [102, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"9227": {"label": 3, "data": {"text": "The histamine H2 receptor antagonist cimetidine blocked the FHA-HIS binding on 14-37% of the platelets.", "entity1": "FHA", "entity2": "cimetidine", "span1": [60, 63], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8549": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "HDAC", "entity2": "pyrrole", "span1": [180, 184], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12874": {"label": 2, "data": {"text": "These results indicate that the ATPase activity of the secretory granule Atp8a1 is activated by phospholipids binding to a specific site whose properties (PS selectivity, dependence upon glycerol but not serine, stereochemistry, and vanadate sensitivity) are similar to, but distinct from, the properties of the substrate binding site of the plasma membrane flippase.", "entity1": "ATPase", "entity2": "PS", "span1": [32, 38], "span2": [155, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"10622": {"label": 1, "data": {"text": "Cerebral histamine H1 receptor (H(1)R) binding was measured in 10 patients with major depression and in 10 normal age-matched subjects using PET and [(11)C]-doxepin.", "entity1": "H(1)R", "entity2": "[(11)C]-doxepin", "span1": [32, 37], "span2": [149, 164]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9279": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "risperidone", "span1": [166, 186], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2834": {"label": 0, "data": {"text": "In this study, we cloned and sequenced a cDNA encoding a serine racemase from barley which contained an open reading frame encoding 337 amino acid residues.", "entity1": "serine racemase", "entity2": "amino acid", "span1": [57, 72], "span2": [136, 146]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10180": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "SLC21A8", "entity2": "rifamycin SV", "span1": [219, 226], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1677": {"label": 4, "data": {"text": "CONCLUSIONS: These results indicate that etomidate acts as an agonist at alpha2-adrenoceptors, which appears in vivo primarily as an alpha2B-receptor-mediated increase in blood pressure.", "entity1": "alpha2-adrenoceptors", "entity2": "etomidate", "span1": [73, 93], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6311": {"label": 8, "data": {"text": "Activation of endothelial nitric oxide synthase (eNOS) results in the production of nitric oxide (NO) that mediates the vasorelaxing properties of endothelial cells.", "entity1": "endothelial nitric oxide synthase", "entity2": "nitric oxide", "span1": [14, 47], "span2": [84, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3508": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "Aldo-keto reductases", "entity2": "polycyclic aromatic hydrocarbons", "span1": [0, 20], "span2": [77, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10728": {"label": 4, "data": {"text": "We have analyzed binding domains of the oxytocin receptor for barusiban, a highly selective oxytocin receptor antagonist, in comparison to the combined vasopressin V1A/oxytocin receptor antagonist atosiban and the agonists oxytocin and carbetocin.", "entity1": "vasopressin V1A/oxytocin receptor", "entity2": "carbetocin", "span1": [152, 185], "span2": [236, 246]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11719": {"label": 1, "data": {"text": "Apoptosis initiation of \u03b2-ionone in SGC-7901 gastric carcinoma cancer cells via a PI3K-AKT pathway.", "entity1": "PI3K", "entity2": "\u03b2-ionone", "span1": [82, 86], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5252": {"label": 3, "data": {"text": "Here we studied the effects of the recently developed monoacylglycerol lipase inhibitor JZL184 on basal and stress-induced corticosterone levels in male CD1 mice, and found that this compound dramatically increased basal levels without affecting stress responses.", "entity1": "monoacylglycerol lipase", "entity2": "JZL184", "span1": [54, 77], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6007": {"label": 3, "data": {"text": "BACKGROUND: The active metabolite of the anti-inflammatory drug nabumetone has been characterized as a selective inhibitor of the inducible prostaglandin H synthase (PGHS).", "entity1": "prostaglandin H synthase", "entity2": "nabumetone", "span1": [140, 164], "span2": [64, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4818": {"label": 1, "data": {"text": "We provide STD NMR data which confirms a physical interaction between LolA and the thiourea degradation product of MAC13243, with a Kd of ~150 \u03bcM.", "entity1": "LolA", "entity2": "MAC13243", "span1": [70, 74], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2128": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "Monocarboxylate transporters", "entity2": "pyruvate", "span1": [0, 28], "span2": [135, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"133": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited the basal (Ca2+/calmodulin-independent) activity of cAMP phosphodiesterase as well as the calmodulin-stimulated activity.", "entity1": "cAMP phosphodiesterase", "entity2": "p-chloro", "span1": [99, 121], "span2": [19, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14862": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "ER\u03b1", "entity2": "ICI 182,780", "span1": [13, 16], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14473": {"label": 1, "data": {"text": "Following CdCl\u2082 treatment, ICAM2 was found to be upregulated during restructuring of the seminiferous epithelium, with round spermatids becoming increasingly immunoreactive for ICAM2 by 6-16 h. Interestingly, there was a loss in the binding of ICAM2 to actin during CdCl\u2082-induced germ cell loss, suggesting that a loss of ICAM2-actin interactions might have facilitated junction restructuring.", "entity1": "ICAM2", "entity2": "CdCl\u2082", "span1": [244, 249], "span2": [266, 271]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1353": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "DAT", "entity2": "benzo", "span1": [317, 320], "span2": [158, 163]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13854": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "17beta-hydroxysteroid-dehydrogenase type 1", "entity2": "norelgestromin", "span1": [266, 308], "span2": [163, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3372": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.3", "entity2": "DHP", "span1": [0, 8], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8967": {"label": 5, "data": {"text": "The Schild plots for the competitive antagonists WB4101 and 5-methyl-urapidil against alpha 1a-adrenoceptor-selective agonist methoxamine-induced contraction were linear and had slopes not significantly different from unity, with a pA2 of 9.07 +/- 0.07 (n = 5) for WB4101 and 9.09 +/- 0.05 (n = 3) for 5-methyl-urapidil.", "entity1": "alpha 1a-adrenoceptor", "entity2": "5-methyl-urapidil", "span1": [86, 107], "span2": [302, 319]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9392": {"label": 1, "data": {"text": "To identify selective compounds for nonadrenergic I1-imidazoline receptors (I1), the affinities of 22 ligands for [125I]p-iodoclonidine binding have been compared at human platelet I1-imidazoline binding sites (analyzed under norepinephrine mask of alpha-2 AR) and at human alpha-2A, alpha-2B and alpha-2C adrenoceptors stably expressed on transfected Chinese hamster ovary cells.", "entity1": "human platelet I1-imidazoline binding sites", "entity2": "[125I]p-iodoclonidine", "span1": [166, 209], "span2": [114, 135]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1087": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "desoxypeganine", "span1": [242, 262], "span2": [160, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3914": {"label": 1, "data": {"text": "To clarify the cause of age differences on selenite cataract formation in rats, mRNA expression of GPx1, MsrA and MsrB1, as well as GPx activity in Wistar rat lens at different ages were assayed, level of lipid peroxidation, extent of lens damage induced by sodium selenite and barricade function of blood-retinal barrier (BRB) were investigated.", "entity1": "GPx", "entity2": "sodium selenite", "span1": [132, 135], "span2": [258, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15149": {"label": 1, "data": {"text": "However, there were detectable concentrations of Lhcgr, Cyp11a1 and Cyp17a1 mRNAs but undetectable concentrations of Insl3, Hsd17b3 and Hsd11b1 in the DEHP-treated testes, indicating that these 3\u03b2-HSD(pos) cells were newly formed progenitor Leydig cells.", "entity1": "Cyp17a1", "entity2": "DEHP", "span1": [68, 75], "span2": [151, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5996": {"label": 3, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "human [Glu1]plasminogen", "entity2": "Cl-", "span1": [18, 41], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7685": {"label": 3, "data": {"text": "We discovered sergliflozin etabonate, a novel selective SGLT2 inhibitor, and found that selective inhibition of SGLT2 increased urinary glucose excretion and consequently decreased plasma glucose levels.", "entity1": "SGLT2", "entity2": "sergliflozin etabonate", "span1": [56, 61], "span2": [14, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1981": {"label": 3, "data": {"text": "As opposed to the rat and flounder orthologs, hNaDC-3 was hardly inhibited by lithium concentrations up to 5 mM.", "entity1": "hNaDC-3", "entity2": "lithium", "span1": [46, 53], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5281": {"label": 2, "data": {"text": "Thus, the NF-\u03baB signaling pathway can be activated after TCDD treatment.", "entity1": "NF-\u03baB", "entity2": "TCDD", "span1": [10, 15], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15308": {"label": 8, "data": {"text": "Statins are inhibitors of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase, the rate-limiting step in cholesterol biosynthesis.", "entity1": "3-hydroxy-3-methylglutaryl coenzyme A reductase", "entity2": "cholesterol", "span1": [37, 84], "span2": [112, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1011": {"label": 0, "data": {"text": "Insulin-like growth factor (IGF)-binding protein (IGFBP)-related proteins (IGFBP-rPs) are newly described cysteine-rich proteins that share significant aminoterminal structural similarity with the conventional IGFBPs and are involved in a diversity of biological functions, including growth regulation.", "entity1": "Insulin-like growth factor (IGF)-binding protein (IGFBP)-related proteins", "entity2": "cysteine", "span1": [0, 73], "span2": [106, 114]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13490": {"label": 3, "data": {"text": "Modulation of the function of CD36 (CD36-/- mice), p38(MAPK) (SB203580), COX-1 (indomethacin), and glycoprotein Ib alpha (Nk-protease, 6D1 antibody) induced approximately 50% inhibition.", "entity1": "COX-1", "entity2": "indomethacin", "span1": [73, 78], "span2": [80, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6158": {"label": 1, "data": {"text": "We report here the use of Met methyl groups as site-specific structural markers to identify drug binding sites for trifluoperazine and bepridil on cTnC.", "entity1": "cTnC", "entity2": "bepridil", "span1": [147, 151], "span2": [135, 143]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11499": {"label": 8, "data": {"text": "Density functional theory calculations using the hybrid functional B3LYP have been performed to study the methyl transfer step in glycine N-methyltransferase (GNMT).", "entity1": "glycine N-methyltransferase", "entity2": "methyl", "span1": [130, 157], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14905": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "flavin mono-oxygenase", "entity2": "TMA", "span1": [24, 45], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2857": {"label": 9, "data": {"text": "As expected, the hGSTA4 cells showed resistance to 4-HNE stimulated lipid peroxidation at all 4-HNE doses.", "entity1": "hGSTA4", "entity2": "4-HNE", "span1": [17, 23], "span2": [51, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2124": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "Monocarboxylate transporters", "entity2": "monocarboxylates", "span1": [0, 28], "span2": [101, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6940": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "flurbiprofen", "span1": [81, 86], "span2": [24, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2632": {"label": 8, "data": {"text": "They all expressed ASS, but not ornithine transcarbamylase (OTC), the enzyme that converts ornithine, the product of degradation of arginine with rhArg, to citrulline, which is converted back to arginine via ASS.", "entity1": "rhArg", "entity2": "citrulline", "span1": [146, 151], "span2": [156, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, 9]},
	"14346": {"label": 3, "data": {"text": "The expression of the osteoblast markers runt-related transcription factor 2 (RUNX2) and periostin was decreased, while osteocalcin (OCN) was augmented in CCL3(-/-) and Met-RANTES-treated mice.", "entity1": "periostin", "entity2": "Met", "span1": [89, 98], "span2": [169, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15259": {"label": 1, "data": {"text": "Oxidation with hydrogen peroxide was similarly assessed, and adhesion of lysozyme and fibrinogen from phosphate buffered saline was then assayed by QCM and imaged by AFM.", "entity1": "fibrinogen", "entity2": "hydrogen peroxide", "span1": [86, 96], "span2": [15, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4319": {"label": 2, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "WAF1", "entity2": "Pinosylvin", "span1": [286, 290], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4017": {"label": 3, "data": {"text": "This study explored whether curcumin improves colonic inflammation in a rat colitis model through inhibition of the TLR4/NF-\u03baB signaling pathway and IL-27 expression.", "entity1": "TLR4", "entity2": "curcumin", "span1": [116, 120], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9877": {"label": 5, "data": {"text": "In these tissues, JTH-601, prazosin (a non-selective alpha(1)-adrenoceptor antagonist), and tamsulosin (an alpha(1A)-adrenoceptor antagonist) competitively antagonized contraction in a concentration-dependent manner.", "entity1": "alpha(1)-adrenoceptor", "entity2": "prazosin", "span1": [53, 74], "span2": [27, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"268": {"label": 0, "data": {"text": "Drosophila GABA-gated chloride channel: modified [3H]EBOB binding site associated with Ala-->Ser or Gly mutants of Rdl subunit.", "entity1": "Rdl", "entity2": "Ala", "span1": [115, 118], "span2": [87, 90]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12191": {"label": 3, "data": {"text": "Low TS expression levels, cytoplasmic expression pattern and C SNP arose as variables associated to longer progression-free survival (PFS) in patients treated with 5FU.", "entity1": "TS", "entity2": "5FU", "span1": [4, 6], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2536": {"label": 8, "data": {"text": "Reductive detoxification of arylhydroxylamine carcinogens by human NADH cytochrome b5 reductase and cytochrome b5.", "entity1": "cytochrome b5", "entity2": "arylhydroxylamine", "span1": [100, 113], "span2": [28, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13355": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "estrogen receptor", "entity2": "MPA", "span1": [56, 73], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8525": {"label": 8, "data": {"text": "CYP3A4 and CYP3A5 metabolized BDP via hydroxylation ([M4] and [M6]) and dehydrogenation ([M5]) at similar rates; CYP3A7 did not metabolize BDP.", "entity1": "CYP3A4", "entity2": "BDP", "span1": [0, 6], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5186": {"label": 1, "data": {"text": "Dioscin-induced autophagy via ERK1/2 and JNK1/2 pathways may provide a protective mechanism for cell survival against dioscin-induced apoptosis to act as a cytoprotective reaction.", "entity1": "ERK1/2", "entity2": "dioscin", "span1": [30, 36], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2169": {"label": 0, "data": {"text": "Binding sites for hERG blockers have been mapped within the inner cavity of the channel and include aromatic residues in the S6 helix (Tyr-652, Phe-656) and residues in the pore helix (Thr-623, Ser-624, Val-625).", "entity1": "hERG", "entity2": "Tyr", "span1": [18, 22], "span2": [135, 138]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2821": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "CXCL-8", "entity2": "DXM", "span1": [48, 54], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2356": {"label": 3, "data": {"text": "Thus, sorafenib may inhibit tumor growth by a dual mechanism, acting either directly on the tumor (through inhibition of Raf and Kit signaling) and/or on tumor angiogenesis (through inhibition of VEGFR and PDGFR signaling).", "entity1": "Kit", "entity2": "sorafenib", "span1": [129, 132], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"474": {"label": 1, "data": {"text": "However, at guinea-pig and mouse splenic alpha 1B-adrenoceptors, the affinity values of risperidone were 10-fold lower than those of prazosin.", "entity1": "guinea-pig and mouse splenic alpha 1B-adrenoceptors", "entity2": "prazosin", "span1": [12, 63], "span2": [133, 141]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2165": {"label": 3, "data": {"text": "In conclusion, of the seven NSAIDs investigated, niflumic acid was the most potent inhibitor of recombinant UGT1A9 via 4-MUG in a competitive manner.", "entity1": "UGT1A9", "entity2": "niflumic acid", "span1": [108, 114], "span2": [49, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4716": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "RSPO receptor", "entity2": "TCDD", "span1": [490, 503], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14843": {"label": 3, "data": {"text": "Physiologic levels of Mg(2+) ions decrease ALDH1 activity in part by increasing NADH binding affinity to the enzyme.", "entity1": "ALDH1", "entity2": "Mg(2+)", "span1": [43, 48], "span2": [22, 28]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5753": {"label": 1, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.", "entity1": "c-Rel", "entity2": "vitamin C", "span1": [115, 120], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9897": {"label": 9, "data": {"text": "However, in virgin mice, bezafibrate and WY-14,643 do not significantly affect UCP-3 mRNA expression, whereas troglitazone is at least as effective as it is in lactating dams.", "entity1": "UCP-3", "entity2": "WY-14,643", "span1": [79, 84], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13801": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "kinase", "entity2": "Gleevec", "span1": [31, 37], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14679": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "CYP1A2", "entity2": "GSK1292263", "span1": [92, 98], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7746": {"label": 3, "data": {"text": "Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer.", "entity1": "tyrosine kinase", "entity2": "XL184", "span1": [42, 57], "span2": [12, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9667": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "human recombinant interleukin-5", "entity2": "cytochalasin B", "span1": [132, 163], "span2": [220, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14049": {"label": 2, "data": {"text": "Aspirin changed nucleotide ratios and activated AMPK in CRC cells.", "entity1": "AMPK", "entity2": "Aspirin", "span1": [48, 52], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1267": {"label": 3, "data": {"text": "Increased IL-5 activity in the serum was inhibited by both pranlukast and MCI-826 by over 90%.", "entity1": "IL-5", "entity2": "MCI-826", "span1": [10, 14], "span2": [74, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2597": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "dopamine D(2)", "entity2": "risperidone", "span1": [42, 55], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4545": {"label": 8, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "CYP2D6", "entity2": "5-MeO-DMT", "span1": [80, 86], "span2": [174, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10649": {"label": 3, "data": {"text": "Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib).", "entity1": "COX-2", "entity2": "valdecoxib", "span1": [99, 104], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9385": {"label": 1, "data": {"text": "In conclusion, cyclothiazide and the 2,3-benzodiazepines seem to bind to different sites on AMPA receptors but exert strong allosteric interactions with one another and with other domains such as the agonist recognition site.", "entity1": "AMPA receptors", "entity2": "2,3-benzodiazepines", "span1": [92, 106], "span2": [37, 56]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, 6, -1, -1, -1, -1, -1, -1, 9]},
	"12592": {"label": 1, "data": {"text": "AMPA receptor heterogeneity in rat hippocampal neurons revealed by differential sensitivity to cyclothiazide.", "entity1": "AMPA receptor", "entity2": "cyclothiazide", "span1": [0, 13], "span2": [95, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13348": {"label": 1, "data": {"text": "In addition, BALB/c and C57BL/6 females were treated with progesterone or MPA for 1 or 2 months, and mammary glands were excised for histologic studies and for immunohistochemical and Western blot evaluation of ER and PR.", "entity1": "ER", "entity2": "progesterone", "span1": [211, 213], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6082": {"label": 3, "data": {"text": "Edrophonium (10 mg i.v. ), a cholinesterase inhibitor that potentiates the effects of acetylcholine at the muscarinic cholinergic receptor, terminated VT in four of four patients, an effect that was reversed by atropine.", "entity1": "cholinesterase", "entity2": "Edrophonium", "span1": [29, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9199": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "alpha 2-macroglobulin", "entity2": "N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide", "span1": [209, 230], "span2": [58, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12899": {"label": 3, "data": {"text": "Here, we show that at noncytotoxic concentrations, H(2)S was able to inhibit NO production and inducible NO synthase (iNOS) expression via heme oxygenase (HO-1) expression in RAW264.7 macrophages stimulated with lipopolysaccharide (LPS).", "entity1": "iNOS", "entity2": "H(2)S", "span1": [118, 122], "span2": [51, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7913": {"label": 8, "data": {"text": "In conclusion, rCtr1 can transport copper and platinum drugs, and sensitizes cells to their cytotoxicities.", "entity1": "rCtr1", "entity2": "platinum", "span1": [15, 20], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3392": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "DAT", "entity2": "cocaine", "span1": [178, 181], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1940": {"label": 3, "data": {"text": "The aim of this study was to evaluate the influence of hepatic impairment on the pharmacokinetics (PK) of the novel cyclooxygenase-2 (COX-2) selective inhibitor lumiracoxib (Prexige), so that dose recommendations for clinical use can be provided.", "entity1": "COX-2", "entity2": "lumiracoxib", "span1": [134, 139], "span2": [161, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9908": {"label": 2, "data": {"text": "Treatment of lactating mice with a single injection of bezafibrate, an activator of the peroxisome proliferator-activated receptor (PPAR), raises UCP-3 mRNA in skeletal muscle to levels similar to those in virgin mice.", "entity1": "PPAR", "entity2": "bezafibrate", "span1": [132, 136], "span2": [55, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11905": {"label": 0, "data": {"text": "A clear relationship between PTP1B phosphorylation levels at Ser 50 and its negative effect on insulin signaling is shown.", "entity1": "PTP1B", "entity2": "Ser", "span1": [29, 34], "span2": [61, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"178": {"label": 5, "data": {"text": "The most potent compound, D,L-4-(3,4-dichlorobenzoylamino)-5-(dipentylamino)-5-oxo-pen tanoic acid (lorglumide, CR 1409), has a great affinity for the pancreatic CCK receptors and is a competitive, specific and potent CCK antagonist on the smooth muscles of the gall bladder and ileum of the guinea pig and on the CCK-induced amylase secretion of isolated pancreatic acini.", "entity1": "CCK", "entity2": "CR 1409", "span1": [218, 221], "span2": [112, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7678": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "EC 4.2.1.1", "entity2": "methazolamide", "span1": [117, 127], "span2": [219, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2082": {"label": 8, "data": {"text": "Phenytoin is principally metabolized by CYP2C9, and both are probable substrates of the drug transporter P-glycoprotein.", "entity1": "CYP2C9", "entity2": "Phenytoin", "span1": [40, 46], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"2686": {"label": 1, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "AXL", "entity2": "MP470", "span1": [68, 71], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"996": {"label": 3, "data": {"text": "Given that FRD, present in all H. pylori strains, is immunogenic in H. pylori -infected patients and H. pylori growth in vitro can be inhibited by three anthelmintics (morantel, oxantel and thiabendazole), this enzyme could potentially be used both as a novel drug target as well as in the development of vaccines for H. pylori prevention and eradication.", "entity1": "FRD", "entity2": "thiabendazole", "span1": [11, 14], "span2": [190, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5035": {"label": 5, "data": {"text": "Ifenprodil, known as the GluNR2B antagonist of reference, was chosen as the template for the elaboration of probes.", "entity1": "GluNR2B", "entity2": "Ifenprodil", "span1": [25, 32], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11254": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "NET", "entity2": "mazindol", "span1": [147, 150], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7866": {"label": 2, "data": {"text": "Fingolimod (FTY720), a novel drug approved for the treatment of relapsing-remitting multiple sclerosis, activates different sphingosine-1-phosphate receptor (S1PR) subtypes.", "entity1": "S1PR", "entity2": "Fingolimod", "span1": [158, 162], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12480": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO3", "entity2": "benzydamine", "span1": [23, 27], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4590": {"label": 3, "data": {"text": "Our previous work, built on the early pioneering multikinase inhibitor LY294002, resulted in the only PI3K vascular-targeted PI3K inhibitor prodrug, SF1126, which has now completed Phase I clinical trials.", "entity1": "PI3K", "entity2": "LY294002", "span1": [125, 129], "span2": [71, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15211": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "cyclooxygenase-2", "entity2": "methanol", "span1": [270, 286], "span2": [59, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14394": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "NFD", "span1": [69, 98], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6553": {"label": 3, "data": {"text": "In contrast, the mutants T844A, F972A and Q975A showed increased K(i) for cilostazol but no difference for milrinone from the recombinant PDE3A.", "entity1": "PDE3A", "entity2": "cilostazol", "span1": [138, 143], "span2": [74, 84]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5900": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "VLDL", "entity2": "fibric acids", "span1": [133, 137], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8831": {"label": 3, "data": {"text": "RESULTS: By Western blot analysis of spinal cord tissues, we have demonstrated that treatment with bioactive RS -GRA significantly decreased nuclear factor (NF)-kB translocation, pro-inflammatory cytokine production such as interleukin-1\u03b2 (IL-1\u03b2), and apoptosis (Bax and caspase 3 expression).", "entity1": "interleukin-1\u03b2", "entity2": "RS -GRA", "span1": [224, 238], "span2": [109, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14527": {"label": 3, "data": {"text": "In contrast, EGCG markedly downregulated major bile acid transporters (Asbt and Ost\u03b1) and regulatory molecules (Shp and Fgf15) in the ileum.", "entity1": "Ost\u03b1", "entity2": "EGCG", "span1": [80, 84], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7597": {"label": 1, "data": {"text": "Interaction of human alpha-lactalbumin with fatty acids: determination of binding parameters.", "entity1": "human alpha-lactalbumin", "entity2": "fatty acids", "span1": [15, 38], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"238": {"label": 1, "data": {"text": "In all cases at both the 5-HT2A and 5-HT2C receptors, the affinities of the isomers of MDMA and MDA were at least 2-3 orders of magnitude less than 5-HT.", "entity1": "5-HT2C", "entity2": "MDA", "span1": [36, 42], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12150": {"label": 0, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "Lys", "span1": [150, 156], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9126": {"label": 1, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c. The irreversible complex between phenoxybenzamine and calmodulin may be useful for inhibiting certain calmodulin-dependent reactions and for studying the various biological functions of calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [190, 200], "span2": [169, 185]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10557": {"label": 1, "data": {"text": "[3H]DMI trapped in membranes was displaceable by the structurally unrelated NET inhibitor, nisoxetine, in a concentration-dependent manner, implying interaction of retained [3H]DMI with the NET.", "entity1": "NET", "entity2": "[3H]DMI", "span1": [76, 79], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6134": {"label": 5, "data": {"text": "We have investigated the effects of CP-99,994 [(+)-(2s,3s)-3-(2-methoxybenzylamino)-2-phenylpiperidine], a tachykinin NK1 receptor antagonist, HOE 140 (D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin), a bradykinin B2 receptor antagonist, and ketotifen (4-(1-methyl-4-piperidylidene)4 H-benzo[4,5]cycloheptal[1,2-b]thiophen-10(9H)-one hydrogen fumarate), a histamine H1 receptor antagonist with mast cell-stabilizing properties, on microvascular leakage induced by gaseous formaldehyde.", "entity1": "histamine H1 receptor", "entity2": "(4-(1-methyl-4-piperidylidene)4 H-benzo[4,5]cycloheptal[1,2-b]thiophen-10(9H)-one hydrogen fumarate)", "span1": [348, 369], "span2": [244, 344]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12141": {"label": 1, "data": {"text": "Because rhoA requires GGPP for its function, this links the microarray and biochemical data and identifies rhoA as a potential mediator of the anticancer properties of lovastatin.", "entity1": "rhoA", "entity2": "GGPP", "span1": [8, 12], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"341": {"label": 3, "data": {"text": "The anti-inflammatory drugs sodium salicylate and aspirin inhibited the activation of NF-kappa B, which further explains the mechanism of action of these drugs.", "entity1": "NF-kappa B", "entity2": "aspirin", "span1": [86, 96], "span2": [50, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6083": {"label": 5, "data": {"text": "VT recurred with the addition of aminophylline, a competitive adenosine A1-receptor antagonist.", "entity1": "adenosine A1-receptor", "entity2": "aminophylline", "span1": [62, 83], "span2": [33, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4537": {"label": 3, "data": {"text": "Our data revealed that inhibition of MAO-A-mediated metabolic elimination by harmaline (2, 5, and 15 mg/kg) led to a sharp increase in systemic and cerebral exposure to 5-MeO-DMT (2 and 10 mg/kg) at all dose combinations.", "entity1": "MAO-A", "entity2": "harmaline", "span1": [37, 42], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7912": {"label": 2, "data": {"text": "We found that helenalin markedly induced endoplasmic reticulum (ER) stress-related genes, such as regulated in development and DNA damage responses (REDD) 1, activating transcription factor-4 (ATF4) and/or the CCAAT enhancer-binding protein-homologous protein (CHOP).", "entity1": "CHOP", "entity2": "helenalin", "span1": [261, 265], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14080": {"label": 3, "data": {"text": "In TGF-\u03b21-induced NPDFs, berberine significantly inhibited the expression of \u03b1-SMA and collagen type I mRNA and reduced \u03b1-SMA and collagen protein levels.", "entity1": "collagen type I", "entity2": "berberine", "span1": [87, 102], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10860": {"label": 1, "data": {"text": "Interestingly, we identified 4-methylhistamine as a high-affinity H(4)R ligand (K(i) = 50 nM) that has a >100-fold selectivity for the hH(4)R over the other histamine receptor subtypes.", "entity1": "hH(4)R", "entity2": "4-methylhistamine", "span1": [135, 141], "span2": [29, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11570": {"label": 8, "data": {"text": "Specifically, all-trans-13,14-dihydroretinol is transiently oxidized to all-trans-13,14-dihydroretinoic acid before being oxidized further by Cyp26 enzymes.", "entity1": "Cyp26", "entity2": "all-trans-13,14-dihydroretinol", "span1": [142, 147], "span2": [14, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13111": {"label": 8, "data": {"text": "By using pharmacological and genetic manipulation of phosphodiesterases (PDEs), we demonstrate that compartmentalized PDE4B and PDE4D are responsible for selectively modulating the concentration of cAMP in individual subcellular compartments.", "entity1": "PDE4D", "entity2": "cAMP", "span1": [128, 133], "span2": [198, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4046": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "p65", "entity2": "neoechinulin A", "span1": [249, 252], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12359": {"label": 0, "data": {"text": "Exchange of domains between the two isoforms indicates that the C1b domain and the N-terminus of the C1a domain are important for directing selective regulation of AC7 by the G(13) pathway.", "entity1": "C1a domain", "entity2": "N", "span1": [101, 111], "span2": [83, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10541": {"label": 1, "data": {"text": "A transcription factor-transcription factor binding array analysis of nuclear lysate from RA-treated cells indicated several prominent RARalpha binding partners; among these, Oct1, NFATc3, and CREB2 were identified by competition EMSA and supershift and chromatin immunoprecipitation assays as components of the complex.", "entity1": "CREB2", "entity2": "RA", "span1": [193, 198], "span2": [90, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14942": {"label": 2, "data": {"text": "Peginesatide, a polyethylene glycol (PEG)ylated peptide-based erythropoiesis-stimulating agent, stimulates the erythropoietin receptor dimer that governs erythropoiesis.", "entity1": "erythropoietin receptor", "entity2": "polyethylene glycol", "span1": [111, 134], "span2": [16, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1570": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "AChE", "entity2": "pyrano[2,3-b]quinolines", "span1": [26, 30], "span2": [103, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13284": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "platelet-derived growth factor receptor", "entity2": "Sorafenib", "span1": [203, 242], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13589": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol", "span1": [6, 10], "span2": [170, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3986": {"label": 8, "data": {"text": "Mammalian ALDH1B1, another mitochondrial enzyme sharing 72% identity with ALDH2, is also capable of metabolizing acetaldehyde but has a tissue distribution and pattern of activity distinct from that of ALDH2.", "entity1": "ALDH2", "entity2": "acetaldehyde", "span1": [74, 79], "span2": [113, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14582": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "PRT062607", "span1": [118, 121], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6196": {"label": 5, "data": {"text": "The alpha1-adrenoceptor antagonist prazosin or the vasopressin V1 receptor antagonist, [beta-mercapto-beta,beta-cyclopenta-methylenepropionyl1, O-Me-Tyr2, Arg8] vasopressin partially but significantly reduced tacrine pressor effect and mostly abolished it when administered concomitantly.", "entity1": "alpha1-adrenoceptor", "entity2": "prazosin", "span1": [4, 23], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2545": {"label": 9, "data": {"text": "Imatinib was also found to inhibit M-CSF-induced osteoclast survival as well as M-CSF-induced osteoclast bone resorbing activity, but was without effect on interleukin 1alpha (IL-1alpha) and receptor activator of nuclear factor kappa B ligand (RANKL)-induced inhibition of osteoclasts apoptosis, further supporting the hypothesis that imatinib may affect mature osteoclasts through the inhibition of c-FMS.", "entity1": "IL-1alpha", "entity2": "Imatinib", "span1": [176, 185], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13126": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "TOP2A", "entity2": "VP-16", "span1": [64, 69], "span2": [109, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12010": {"label": 9, "data": {"text": "Cosinor analysis indicated no diurnal rhythm of Ppar\u03b3 expression in the livers of diabetic STZ or Iddm rats or in those of insulin-substituted Iddm rats.", "entity1": "Ppar\u03b3", "entity2": "STZ", "span1": [48, 53], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10232": {"label": 9, "data": {"text": "Substrate specificity using lysates of oxidase-transfected HEK-293 cells revealed that the newly identified oxidase strongly favoured spermine over N (1)-acetylspermine and that it failed to act on N (1)-acetylspermidine, spermidine or the preferred PAO substrate, N (1), N (12)-diacetylspermine.", "entity1": "oxidase", "entity2": "spermidine", "span1": [108, 115], "span2": [222, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9913": {"label": 2, "data": {"text": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid (WY-14,643), a specific ligand of the PPAR-alpha subtype, causes the most dramatic increase in UCP-3 mRNA, whereas troglitazone, a specific activator of PPAR-gamma, also significantly increases UCP-3 mRNA abundance in skeletal muscle of lactating mice.", "entity1": "UCP-3", "entity2": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid", "span1": [151, 156], "span2": [0, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15375": {"label": 3, "data": {"text": "Interestingly, miR-21 expression positively correlated with urine albumin creatine ratio (ACR), TIMP1, collagen IV (ColIV), and fibronectin (FN); while negatively correlated with creatine clearance ratio (Ccr) and MMP-9 protein.", "entity1": "miR-21", "entity2": "creatine", "span1": [15, 21], "span2": [179, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3288": {"label": 1, "data": {"text": "We have investigated in normal human male subjects the importance, site of action, and receptor-mediated processes involved in rapid basal corticosteroid feedback and its interaction with corticotrophin releasing hormone (CRH) drive.", "entity1": "corticotrophin releasing hormone", "entity2": "corticosteroid", "span1": [188, 220], "span2": [139, 153]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1192": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "aminopeptidase B", "entity2": "L-arginine", "span1": [369, 385], "span2": [354, 364]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13175": {"label": 2, "data": {"text": "Progestin activation of Src/MAPK occurred outside the nucleus with the B isoform of PR that was distributed between the cytoplasm and nucleus, but not with PR-A that was predominantly nuclear.", "entity1": "MAPK", "entity2": "Progestin", "span1": [28, 32], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7509": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMP-activated protein kinase", "entity2": "AICAR", "span1": [24, 52], "span2": [176, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10255": {"label": 9, "data": {"text": "However, desipramine at a low concentration essentially blocked the radioactive outflow induced by all of these substances with the exception of MPP+, indicating the NAT and not an OCT as their primary site of action.", "entity1": "OCT", "entity2": "MPP+", "span1": [181, 184], "span2": [145, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7883": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "protease", "entity2": "RTV", "span1": [15, 23], "span2": [66, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5373": {"label": 1, "data": {"text": "Interestingly, we showed that rapamycin shares all the proteasome targeting properties not only with other two-domain, closed-ring analogs (rapalogs), but also with its single domain mimics, and with seco-rapamycin.", "entity1": "proteasome", "entity2": "rapamycin", "span1": [55, 65], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6088": {"label": 2, "data": {"text": "These results suggest that amantadine induction of Fos in the rat striatum is related to dopamine D1 and NMDA receptors.", "entity1": "Fos", "entity2": "amantadine", "span1": [51, 54], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12382": {"label": 0, "data": {"text": "Similarly, mature BMP-2 was also cleaved to a truncated peptide within its N-terminal region (Arg(289)\u2193Lys(290)).", "entity1": "BMP-2", "entity2": "N", "span1": [18, 23], "span2": [75, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11557": {"label": 1, "data": {"text": "Warfarin dose and the pharmacogenomics of CYP2C9 and VKORC1 - rationale and perspectives.", "entity1": "CYP2C9", "entity2": "Warfarin", "span1": [42, 48], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1944": {"label": 9, "data": {"text": "Several purinergic receptors have been described on platelets; P2X (1), a calcium channel, and P2Y1 a Gq-coupled seven-transmembrane domain receptor, have been found not to be antagonized by clopidogrel.", "entity1": "P2X (1)", "entity2": "clopidogrel", "span1": [63, 70], "span2": [191, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14983": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "p21", "entity2": "ATO", "span1": [67, 70], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5356": {"label": 1, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [74, 79], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6461": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "thymidylate synthase", "entity2": "Pemetrexed disodium", "span1": [90, 110], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7475": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "GluRs", "entity2": "Na+", "span1": [50, 55], "span2": [74, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15141": {"label": 8, "data": {"text": "The enzyme (TcCA) has a very high catalytic activity for the CO(2) hydration reaction, being similar kinetically to the human (h) isoform hCA II, although it is devoid of the His64 proton shuttle.", "entity1": "TcCA", "entity2": "CO(2)", "span1": [12, 16], "span2": [61, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13543": {"label": 2, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha2", "entity2": "5,8,11,14-eicosatetraynoic acid", "span1": [188, 198], "span2": [100, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5377": {"label": 6, "data": {"text": "We hypothesize that the rapamycin and related compounds bind to the \u03b1 face and allosterically impact the proteasome function.", "entity1": "proteasome", "entity2": "rapamycin", "span1": [105, 115], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"5499": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D1 receptor", "entity2": "SCH 39166", "span1": [153, 173], "span2": [185, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8660": {"label": 2, "data": {"text": "The expression kinetics of TAp63, c-Abl and TAp73 suggest that cisplatin activates TAp63-dependent expression of c-Abl and TAp73 and, in turn, the activation of TAp73 by c-Abl-induced BAX expression.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [170, 175], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4735": {"label": 3, "data": {"text": "Furthermore, sinapic acid reduced hepatic hydroxyproline content, which correlated with a reduction in the expression of type I collagen mRNA and histological analysis of collagen in liver tissue.", "entity1": "type I collagen", "entity2": "sinapic acid", "span1": [121, 136], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9752": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "5-HT(1D)", "entity2": "yohimbine", "span1": [142, 150], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10924": {"label": 3, "data": {"text": "The inhibition of ERK, moreover, did not cause attenuation in mucin secretion in response to cAMP and forskolin.", "entity1": "ERK", "entity2": "cAMP", "span1": [18, 21], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9515": {"label": 5, "data": {"text": "Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.", "entity1": "neurotensin receptor", "entity2": "[3H]SR 142948A", "span1": [43, 63], "span2": [76, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15607": {"label": 2, "data": {"text": "TCPOBOP, a CAR ligand, modestly induced mdr1a.fLUC in pxr(+/+) and pxr(-/-) strains, consistent with CAR's minor role in mdr1a regulation.", "entity1": "mdr1a", "entity2": "TCPOBOP", "span1": [40, 45], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14361": {"label": 3, "data": {"text": "The quinolizidine alkaloids (natural products) such as oxymatrine, sophoridine, sophocarpine and matrine carry the common molecular structure of O=C=N-C-C-C-N that possessed positive ionotropic effect and hERG blocking activity.", "entity1": "hERG", "entity2": "matrine", "span1": [205, 209], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"1521": {"label": 9, "data": {"text": "Neither okadaic acid nor cantharidin (1-10000 nM) displaced [3H]naloxone from its specific binding sites, which indicates that they do not interact at the opioid receptor level.", "entity1": "opioid receptor", "entity2": "[3H]naloxone", "span1": [155, 170], "span2": [60, 72]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6802": {"label": 1, "data": {"text": "Psychopharmacology of anticonvulsants: levetiracetam as a synaptic vesicle protein modulator.", "entity1": "synaptic vesicle protein", "entity2": "levetiracetam", "span1": [58, 82], "span2": [39, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11879": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "AhR", "entity2": "anthocyanidins", "span1": [145, 148], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4159": {"label": 1, "data": {"text": "CNTs with linear poly(ethylene glycol) amphiphiles trigger the lectin pathway of the complement through both L-ficolin and mannan-binding lectin recognition.", "entity1": "lectin", "entity2": "poly(ethylene glycol)", "span1": [63, 69], "span2": [17, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11925": {"label": 1, "data": {"text": "Oxysterols interfere with ERK, hedgehog and wnt pathways of proliferation and differentiation.", "entity1": "hedgehog", "entity2": "Oxysterols", "span1": [31, 39], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12485": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO1", "entity2": "trimethylamine", "span1": [67, 71], "span2": [119, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9141": {"label": 1, "data": {"text": "Certain analogs of caffeine in which the methyl group at the 1- or 7-position is replaced with a propargyl or propyl group display selectivity for A2 receptors.", "entity1": "A2 receptors", "entity2": "propyl", "span1": [147, 159], "span2": [110, 116]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13163": {"label": 9, "data": {"text": "Progestin induction of cell cycle progression was also abrogated in cells expressing PR-BDeltaSH3, and no effect of progestin on cyclin D1 expression and cell cycle was observed in the presence of PR-A.", "entity1": "cyclin D1", "entity2": "progestin", "span1": [129, 138], "span2": [116, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4905": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "tissue inhibitors of matrix metalloproteinases", "entity2": "kinsenoside", "span1": [382, 428], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15293": {"label": 3, "data": {"text": "Bicyclic pyrazinone and pyrimidinone amides were designed and synthesized as potent TF-FVIIa inhibitors.", "entity1": "TF", "entity2": "Bicyclic pyrazinone and pyrimidinone amides", "span1": [84, 86], "span2": [0, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11160": {"label": 8, "data": {"text": "Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A).", "entity1": "human phosphodiesterase", "entity2": "cGMP", "span1": [40, 63], "span2": [94, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3025": {"label": 3, "data": {"text": "Flavopiridol inhibits CDK with an IC50 value of 0.4 mM [285707].", "entity1": "CDK", "entity2": "Flavopiridol", "span1": [22, 25], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14256": {"label": 8, "data": {"text": "The acetylation of TETA is increased in SSAT1-overexpressing mice compared with wild-type mice.", "entity1": "SSAT1", "entity2": "TETA", "span1": [40, 45], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4695": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "V(5+)", "span1": [123, 129], "span2": [36, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9347": {"label": 3, "data": {"text": "One group of experimental animals was treated with 5-lipoxygenase (5-LO) inhibitor, diethylcarbamazine (DEC, Sigma, St. Louis, Missouri) (50 mg/kg, i.v.", "entity1": "5-LO", "entity2": "diethylcarbamazine", "span1": [67, 71], "span2": [84, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12247": {"label": 1, "data": {"text": "For the isolated PKCalpha C2 domain in the presence of physiological Ca2+ levels, the target lipids phosphatidylserine (PS) and phosphatidylinositol-4,5-bisphosphate (PIP2) are together sufficient to recruit the PKCalpha C2 domain to a lipid mixture mimicking the plasma membrane inner leaflet.", "entity1": "PKCalpha C2 domai", "entity2": "phosphatidylserine", "span1": [212, 229], "span2": [100, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4067": {"label": 2, "data": {"text": "Cortisol and IFNT stimulated endometrial HSD11B1 expression and activity, increased endometrial PTGS2 activity and the amount of PG in the uterine lumen, and up-regulated many conceptus elongation-related genes in the endometrium.", "entity1": "HSD11B1", "entity2": "Cortisol", "span1": [41, 48], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8211": {"label": 2, "data": {"text": "TAA increased the number and area of glutathione S-transferase placental form (GST-P)(+) liver cell foci and the numbers of proliferating and apoptotic cells in randomly selected areas in liver sections.", "entity1": "glutathione S-transferase placental form", "entity2": "TAA", "span1": [37, 77], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8757": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT2B10", "entity2": "diphenhydramine", "span1": [61, 68], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5926": {"label": 2, "data": {"text": "The concentration of estramustine phosphate required to inhibit the assembly or to induce the disassembly of chick brain MAP2:tubulin microtubules is markedly dependent upon the microtubule protein concentration.", "entity1": "tubulin", "entity2": "estramustine phosphate", "span1": [126, 133], "span2": [21, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2539": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "PhIP", "span1": [311, 317], "span2": [209, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3575": {"label": 3, "data": {"text": "); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [50, 53], "span2": [106, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2093": {"label": 3, "data": {"text": "Effects of inhibition of urokinase-type plasminogen activator (u-PA) by amiloride in the cornea and tear fluid of eyes irradiated with UVB.", "entity1": "urokinase-type plasminogen activator", "entity2": "amiloride", "span1": [25, 61], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8354": {"label": 3, "data": {"text": "This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.", "entity1": "PKA", "entity2": "quinazolinones", "span1": [117, 120], "span2": [70, 84]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15596": {"label": 3, "data": {"text": "Design, Synthesis, Biological Evaluation, and Docking Studies of (S)-Phenylalanine Derivatives with a 2-Cyanopyrrolidine Moiety as Potent Dipeptidyl Peptidase 4 Inhibitors.", "entity1": "Dipeptidyl Peptidase 4", "entity2": "2-Cyanopyrrolidine", "span1": [138, 160], "span2": [102, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9460": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "PGE1", "span1": [4, 7], "span2": [177, 181]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9232": {"label": 8, "data": {"text": "Alanine:glyoxylate aminotransferase (AGT) in the liver catalyzes most of the glyoxylate transamination in mammalian tissues (E. V. Rowsell, K. Snell, J.", "entity1": "AGT", "entity2": "glyoxylate", "span1": [37, 40], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"11045": {"label": 3, "data": {"text": "Novel highly affine histamine H3 receptor ligands with additional inhibitory effects on the main histamine metabolizing enzyme in the brain, N-methyltransferase, chemically show structural elements of the acetylcholinesterase inhibitor tacrine.", "entity1": "acetylcholinesterase", "entity2": "tacrine", "span1": [205, 225], "span2": [236, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14776": {"label": 3, "data": {"text": "ATP-dependent 2-NBDG uptake was also inhibited by the G protein \u03b2\u03b3 subunit-interacting peptide \u03b2ark-ct and by the phosphatidylinositol 3-kinase-\u03b3 (PI3K\u03b3) inhibitor AS605240.", "entity1": "phosphatidylinositol 3-kinase-\u03b3", "entity2": "AS605240", "span1": [114, 145], "span2": [164, 172]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10571": {"label": 4, "data": {"text": "To verify the hypothesis that the non-conventional partial agonist (-)-CGP12177 binds at two beta(1)-adrenoceptor sites, human beta(1)-adrenoceptors, expressed in CHO cells, were labelled with (-)-[(3)H]-CGP12177.", "entity1": "beta(1)-adrenoceptor", "entity2": "(-)-CGP12177", "span1": [93, 113], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2194": {"label": 1, "data": {"text": "Crystal structures of protein phosphatase-1 bound to motuporin and dihydromicrocystin-LA: elucidation of the mechanism of enzyme inhibition by cyanobacterial toxins.", "entity1": "protein phosphatase-1", "entity2": "dihydromicrocystin-LA", "span1": [22, 43], "span2": [67, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13225": {"label": 1, "data": {"text": "Our results suggest that glutamate induces GRIP1 degradation by proteasome through an NMDA receptor-Ca2+ pathway and that GRIP1 degradation may play an important role in regulating GluR2 surface expression.", "entity1": "GluR2", "entity2": "glutamate", "span1": [181, 186], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3748": {"label": 3, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "Cx43", "entity2": "TCDD", "span1": [189, 193], "span2": [110, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2844": {"label": 1, "data": {"text": "Decreased expression of VKORC1 resulting from the -1639G>A substitution has also been implicated in lower warfarin dose requirements.", "entity1": "VKORC1", "entity2": "warfarin", "span1": [24, 30], "span2": [106, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11990": {"label": 2, "data": {"text": "In this study, using reverse transcriptase PCR (RT-PCR) and ELISA, we showed that TCDD up-regulated the expression and secretion of tumor necrosis factor-alpha (TNF-\u03b1) in a time-dependent manner in cultured HAPI microglial cells.", "entity1": "tumor necrosis factor-alpha", "entity2": "TCDD", "span1": [132, 159], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10314": {"label": 1, "data": {"text": "Plasmacytoid dendritic cells produce cytokines and mature in response to the TLR7 agonists, imiquimod and resiquimod.", "entity1": "cytokines", "entity2": "resiquimod", "span1": [37, 46], "span2": [106, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15868": {"label": 1, "data": {"text": "Immunoblot studies showed that K(+)-depolarization increased CaMKII\u03b1 phosphorylation in a KN-62 sensitive manner and promoted CaMKII\u03b1 binding to D3 receptors.", "entity1": "D3 receptors", "entity2": "KN-62", "span1": [145, 157], "span2": [90, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12510": {"label": 1, "data": {"text": "Among all the organophosphates tested, the combination of a methyl group and a negatively charged oxygen attached to the P atom, CH3P(O)(O-)-AChE, conferred the greatest protection to the active site of aged or nonaged organophosphoryl conjugates of acetylcholinesterase.", "entity1": "AChE", "entity2": "organophosphates", "span1": [141, 145], "span2": [14, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5112": {"label": 2, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "HO-1", "entity2": "5HHMF", "span1": [192, 196], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5800": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "N", "span1": [125, 145], "span2": [43, 44]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14428": {"label": 3, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C. Furthermore, the AMPK activator 5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) significantly inhibited ghrelin secretion.", "entity1": "ghrelin", "entity2": "Metformin", "span1": [32, 39], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9412": {"label": 4, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT1", "entity2": "cinitapride", "span1": [152, 157], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13695": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "porcine TLR7", "entity2": "gardiquimod", "span1": [83, 95], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13545": {"label": 2, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha2", "entity2": "ETYA", "span1": [188, 198], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8707": {"label": 2, "data": {"text": "To delineate the pathogenesis, we examined changes in the mRNA levels of 2 angiotensin II Type I receptor (AT1R) subtypes, AT1AR and AT1BR, in a mouse aortic endothelial cell line, END-D. Quantitative real-time PCR analysis revealed significant increases in the mRNA levels of 2 AT1R subtypes, AT1AR and AT1BR following sodium arsenite (SA) treatment.", "entity1": "AT1AR", "entity2": "sodium arsenite", "span1": [294, 299], "span2": [320, 335]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13068": {"label": 2, "data": {"text": "It was, therefore, proposed that H. pylori may in fact, antagonize, aspirin-induced delay of ulcer healing due to suppression of acid secretion by the enhancement in PGE(2) possibly derived from COX-2 expression and activity and to the overexpression of growth factors such as TGF alpha and VEGF.", "entity1": "VEGF", "entity2": "aspirin", "span1": [291, 295], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6423": {"label": 8, "data": {"text": "Uncoupling proteins (UCPs) are inner mitochondrial membrane transporters which act as pores for H(+) ions, dissipating the electrochemical gradient that develops during mitochondrial respiration at the expense of ATP synthesis.", "entity1": "Uncoupling proteins", "entity2": "H(+)", "span1": [0, 19], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11847": {"label": 9, "data": {"text": "We conclude that there are prejunctional A1Rs in arteries and both pre- and postjunctional A1Rs in veins; thus, adenosine selectively constricts the veins.", "entity1": "A1Rs", "entity2": "adenosine", "span1": [41, 45], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3352": {"label": 1, "data": {"text": "The Ca(2+) dependent interaction between troponin I (cTnI) and troponin C (cTnC) triggers contraction in heart muscle.", "entity1": "troponin I", "entity2": "Ca(2+)", "span1": [41, 51], "span2": [4, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7084": {"label": 2, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "TRPV3", "entity2": "cinnamaldehyde", "span1": [101, 106], "span2": [37, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"58": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "human renin", "entity2": "A-64662", "span1": [93, 104], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6921": {"label": 9, "data": {"text": "Our results provided direct evidence indicating that HM74A, but not HM74, was sufficient to mediate anti-lipolytic effect of niacin in adipose tissue.", "entity1": "HM74", "entity2": "niacin", "span1": [68, 72], "span2": [125, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12800": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "c-kit", "entity2": "STI 571", "span1": [120, 125], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10768": {"label": 2, "data": {"text": "Although, imatinib primarily inhibits tyrosine kinases, it also stimulates the activity of EGFR tyrosine kinase in head and neck squamous tumors.", "entity1": "tyrosine kinase", "entity2": "imatinib", "span1": [96, 111], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8553": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "HDAC", "entity2": "hydroxamates", "span1": [180, 184], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6021": {"label": 3, "data": {"text": "Indomethacin, piroxicam, and sulindac sulfide were found to preferentially inhibit PGHS-1.", "entity1": "PGHS-1", "entity2": "piroxicam", "span1": [83, 89], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"629": {"label": 3, "data": {"text": "Likewise, IL-2 steady-state mRNA expression was inhibited by both PLA2 inhibitors in a concentration-dependent fashion with > 90% inhibition at 1 microM BPB and 20 microM AACOCF3.", "entity1": "PLA2", "entity2": "BPB", "span1": [66, 70], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10494": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "CGP 20712", "span1": [392, 423], "span2": [322, 331]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5243": {"label": 1, "data": {"text": "Sodium fluoride induces apoptosis in odontoblasts via a JNK-dependent mechanism.", "entity1": "JNK", "entity2": "Sodium fluoride", "span1": [56, 59], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7772": {"label": 2, "data": {"text": "GDC-0152 induces NF-\u03baB transcriptional activity leading to expression of several chemokines and cytokines, of which tumor necrosis factor alpha (TNF-\u03b1) is the most important for single-agent tumor activity.", "entity1": "NF-\u03baB", "entity2": "GDC-0152", "span1": [17, 22], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2575": {"label": 2, "data": {"text": "Histamine content, HDC activity and HDC mRNA expression in nasal mucosa were also significantly increased after TDI provocation.", "entity1": "HDC", "entity2": "TDI", "span1": [19, 22], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15761": {"label": 3, "data": {"text": "Depleted heme pool and CO releasing limited protein synthesis and inhibited enzymatic activity of CYP2E1, respectively.", "entity1": "CYP2E1", "entity2": "CO", "span1": [98, 104], "span2": [23, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6977": {"label": 1, "data": {"text": "Bisoprolol reduced dobutamine-induced heart rate and contractility increases and diastolic blood pressure decreases more potently in Arg389- versus Gly389-beta1AR subjects.", "entity1": "beta1AR", "entity2": "Bisoprolol", "span1": [155, 162], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2016": {"label": 3, "data": {"text": "CONCLUSION: Our results indicate that pranlukast inhibits IL-5 synthesis via a mechanism distinct from CysLTR1 antagonism.", "entity1": "IL-5", "entity2": "pranlukast", "span1": [58, 62], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10442": {"label": 7, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "EC 4.3.1.17", "entity2": "pyridoxal 5'-phosphate", "span1": [27, 38], "span2": [54, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6904": {"label": 2, "data": {"text": "In vitro studies demonstrated that the retinoid X receptor (RXR) retinoid, bexarotene, at biologically relevant concentrations of 10(-6) M to 10(-8) M, upregulated both the p55 and p75 subunits of the IL-2R and enhanced 5- to 10-fold the susceptibility of T-cell leukemia cells to denileukin diftitox.", "entity1": "IL-2R", "entity2": "bexarotene", "span1": [201, 206], "span2": [75, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15157": {"label": 2, "data": {"text": "A dominant negative PKA (DNPKA) reduced GnRH-stimulated pCREB and markedly decreased GnRH stimulation of FSH\u03b2 mRNA and FSH\u03b2LUC activity, but had little effect on LH\u03b2LUC activity, indicating relative specificity of this pathway.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [119, 123], "span2": [85, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5805": {"label": 8, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "EC 3.5.1.14", "entity2": "N-acylated L-amino acids", "span1": [109, 120], "span2": [216, 240]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14126": {"label": 3, "data": {"text": "Crizotinib is an oral tyrosine kinase inhibitor (TKI), which silences the protein product of the ALK fusion gene and has recently been approved for the treatment of NSCLC aberrantly expressing ALK.", "entity1": "ALK", "entity2": "Crizotinib", "span1": [97, 100], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13742": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "Ca(v)1.2", "entity2": "DHP", "span1": [43, 51], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"992": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "eNOS", "entity2": "BH(4)", "span1": [180, 184], "span2": [59, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"8828": {"label": 3, "data": {"text": "New series of pyrrolidine mercaptosulfide, 2-mercaptocyclopentane arylsulfonamide, and 3-mercapto-4-arylsulfonamido pyrrolidine matrix metalloproteinase inhibitors (MMPIs) were designed, synthesized, and evaluated.", "entity1": "matrix metalloproteinase", "entity2": "3-mercapto-4-arylsulfonamido pyrrolidine", "span1": [128, 152], "span2": [87, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5845": {"label": 3, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT3", "entity2": "benzamide", "span1": [96, 101], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13555": {"label": 9, "data": {"text": "Arginase or nitric oxide synthase isoenzymes were not found to influence L-citrulline production.", "entity1": "Arginase", "entity2": "L-citrulline", "span1": [0, 8], "span2": [73, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"4311": {"label": 2, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "MAPK", "entity2": "AuF", "span1": [76, 80], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15526": {"label": 1, "data": {"text": "Our findings that NO/SNO target both Prx and Trx reductase may have implications for understanding the impact of nitrosylation on cellular redox homeostasis.", "entity1": "Trx reductase", "entity2": "NO", "span1": [45, 58], "span2": [18, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8951": {"label": 3, "data": {"text": "The affinity labeling nucleotide analog, 5'-[p-(fluorosulfonyl)benzoyl]adenosine (FSA), inactivates the dehydrogenase and isomerase activities at similar rates in an irreversible manner which follows first order kinetics with respect to both time and alkylator concentration (0.2-0.6 mM).", "entity1": "dehydrogenase", "entity2": "nucleotide", "span1": [104, 117], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12733": {"label": 3, "data": {"text": "Agents which have recently been shown to block cyclin D1 translation by regulating calcium levels are the unsaturated essential fatty acid, eicosapentaenoic acid (EPA), the antidiabetic thiazolidinediones, and the antifungal agent, clotrimazole.", "entity1": "cyclin D1", "entity2": "eicosapentaenoic acid", "span1": [47, 56], "span2": [140, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4091": {"label": 2, "data": {"text": "The upregulation of calpain, tBid and caspase-3 activity were further inhibited by treatment with EGTA in the presence of ALD.", "entity1": "calpain", "entity2": "ALD", "span1": [20, 27], "span2": [122, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13988": {"label": 8, "data": {"text": "An essential control in experiments using Gy mice is to demonstrate that the abnormal phenotypes exhibited by these mice are abolished by providing replacement spermine and this can be accomplished by breeding with CAG-SMS mice that express SpmS from a ubiquitous promoter.", "entity1": "SpmS", "entity2": "spermine", "span1": [241, 245], "span2": [160, 168]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12833": {"label": 3, "data": {"text": "This effect was reverted in the presence of atropine (ATR; 0.1 microM), which blocks the pre-synaptic muscarinic M2 receptor.", "entity1": "muscarinic M2 receptor", "entity2": "atropine", "span1": [102, 124], "span2": [44, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3839": {"label": 3, "data": {"text": "Emodin-6-O-\u03b2-D-glucoside inhibits HMGB1-induced inflammatory responses in vitro and in vivo.", "entity1": "HMGB1", "entity2": "Emodin-6-O-\u03b2-D-glucoside", "span1": [34, 39], "span2": [0, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5126": {"label": 3, "data": {"text": "Pyrrolidine dithiocarbamate (PDTC), a specific NF-\u03baB inhibitor, along with 20S proteasome inhibitor (PSI) significantly inhibited LPS-induced iNOS expression, which indirectly suggested that 5HHMF downregulated iNOS expression by suppressing NF-\u03baB activity.", "entity1": "iNOS", "entity2": "Pyrrolidine dithiocarbamate", "span1": [142, 146], "span2": [0, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1092": {"label": 3, "data": {"text": "The capacity of acetylcholinesterase inhibitors, with the exception of tacrine and ambenonium, to displace bound [3H]-oxotremorine-M in preference to [3H]quinuclinidyl benzilate predicts that the former compounds could act as potential agonists at muscarinic receptors.", "entity1": "acetylcholinesterase", "entity2": "tacrine", "span1": [16, 36], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9575": {"label": 4, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "beta2AR", "entity2": "fenoterol", "span1": [166, 173], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4247": {"label": 2, "data": {"text": "Treatment of HDP cells with a c-Jun NH2-terminal kinase (JNK) inhibitor also reduced butein-induced HO-1 expression, and butein treatment led to increased JNK phosphorylation.", "entity1": "JNK", "entity2": "butein", "span1": [155, 158], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5446": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "androgen receptor", "entity2": "juglone", "span1": [81, 98], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11977": {"label": 0, "data": {"text": "Saccharomyces cerevisiae \u03c455, a subunit of the RNA polymerase III-specific general transcription factor TFIIIC, comprises an N-terminal histidine phosphatase domain (\u03c455-HPD) whose catalytic activity and cellular function is poorly understood.", "entity1": "Saccharomyces cerevisiae \u03c455", "entity2": "histidine", "span1": [0, 28], "span2": [136, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8718": {"label": 3, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "GPx", "entity2": "NaAsO2", "span1": [30, 33], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2158": {"label": 3, "data": {"text": "Thalidomide reduced COX-2 expression accompanied by a decrease of bcl-2 protein, TNFalpha, VEGF, GSH and an increased cytochrome c, but had no effect on that of COX-1, in MCF-7 and HL-60.", "entity1": "TNFalpha", "entity2": "Thalidomide", "span1": [81, 89], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4148": {"label": 2, "data": {"text": "All-trans retinoic acid protects hepatocellular carcinoma cells against serum-starvation-induced cell death by upregulating collagen 8A2.", "entity1": "collagen 8A2", "entity2": "All-trans retinoic acid", "span1": [124, 136], "span2": [0, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5618": {"label": 8, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "K+", "span1": [131, 135], "span2": [76, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"27": {"label": 3, "data": {"text": "Candoxatril is a novel, orally active inhibitor of neutral endopeptidase EC 3.4.24.11, the enzyme that degrades atrial natriuretic peptide (ANP).", "entity1": "neutral endopeptidase", "entity2": "Candoxatril", "span1": [51, 72], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"577": {"label": 2, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cdk2", "entity2": "Tomudex", "span1": [44, 48], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7938": {"label": 9, "data": {"text": "Structure-activity relationship analysis of highly potent subtype-selective ligands (MT(2) EC(50) 10-90 pM) revealed that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT(2) potency and at the same time decreased MT(1) potency.", "entity1": "MT(1)", "entity2": "3-methoxyphenyl", "span1": [274, 279], "span2": [182, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2185": {"label": 1, "data": {"text": "showed that when AdoCbl is bound to the MMCM active site, no enzymatic perturbation of the Co3+ Cbl electronic structure occurs, even in the presence of substrate (analogues).", "entity1": "MMCM", "entity2": "AdoCbl", "span1": [40, 44], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11995": {"label": 3, "data": {"text": "The results showed that most of the synthesized compounds exhibited nanomolar potency against CEase, much better than the parent flavonoids.", "entity1": "CEase", "entity2": "flavonoids", "span1": [94, 99], "span2": [129, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5197": {"label": 3, "data": {"text": "Inhibition of mTOR by low dose rapamycin decreases HG-induced Nox4 and Nox1, NADPH oxidase activity and podocyte apoptosis.", "entity1": "Nox4", "entity2": "rapamycin", "span1": [62, 66], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13625": {"label": 3, "data": {"text": "Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease.", "entity1": "monoamine oxidase", "entity2": "rasagiline", "span1": [56, 73], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4568": {"label": 4, "data": {"text": "Adenosine and N(6)-cyclopentyl-adenosine (CPA, A1R agonist) constricted MVs but not MAs.", "entity1": "A1R", "entity2": "N(6)-cyclopentyl-adenosine", "span1": [47, 50], "span2": [14, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11317": {"label": 3, "data": {"text": "Ten IU/mL urokinase was also incubated with pooled plasma of stroke patients, that was previously oxidized with the singlet oxygen (1O2) donor chloramine T (CT), to destroy plasmatic PAI-1 and alpha2-antiplasmin.", "entity1": "plasmin", "entity2": "CT", "span1": [204, 211], "span2": [157, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14445": {"label": 4, "data": {"text": "As these regulatory motifs mediate regulation of target genes by AhR agonists including TCDD and prochloraz, we have systematically investigated the effect of both contaminants on functional ABCG2 transport activity in primary bovine mammary epithelial cells.", "entity1": "AhR", "entity2": "TCDD", "span1": [65, 68], "span2": [88, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15412": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "ABCG5/8", "entity2": "stigmasterol", "span1": [210, 217], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"2412": {"label": 3, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "arginase", "entity2": "Nor-NOHA", "span1": [117, 125], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13247": {"label": 5, "data": {"text": "The GRIP1 reduction was inhibited by MK-801, an N-methyl-d-aspartate (NMDA) receptor antagonist, but not by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an AMPA receptor antagonist.", "entity1": "N-methyl-d-aspartate (NMDA) receptor", "entity2": "MK-801", "span1": [48, 84], "span2": [37, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11708": {"label": 2, "data": {"text": "DBDCT also caused the phosphorylation of JNK and p38(MAPK).", "entity1": "p38", "entity2": "DBDCT", "span1": [49, 52], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2924": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "ion channel", "entity2": "aprindine", "span1": [9, 20], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6040": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "Ru 24969", "span1": [73, 79], "span2": [136, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4252": {"label": 2, "data": {"text": "Furthermore, butein treatment caused nuclear accumulation of nuclear factor-E2-related factor 2 (Nrf2) and increased the promoter activity of antioxidant response elements (AREs).", "entity1": "nuclear factor-E2-related factor 2", "entity2": "butein", "span1": [61, 95], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2762": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "human COX-2", "entity2": "lumiracoxib", "span1": [75, 86], "span2": [186, 197]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5801": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "C", "span1": [125, 145], "span2": [50, 51]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15192": {"label": 8, "data": {"text": "Involvement of P450 mediated metabolism in the absorption of darunavir could not be demonstrated in this rat model.", "entity1": "P450", "entity2": "darunavir", "span1": [15, 19], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"483": {"label": 1, "data": {"text": "The atypical neuroleptics remoxipride, clozapine, perlapine, seroquel, and melperone had low affinity for the dopamine D2 receptor (radioligand-independent dissociation constants of 30 to 90 nM).", "entity1": "D2 receptor", "entity2": "remoxipride", "span1": [119, 130], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3376": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-type voltage-gated calcium channels", "entity2": "BDZs", "span1": [114, 151], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10850": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "KIT", "entity2": "Glivec", "span1": [105, 108], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14841": {"label": 3, "data": {"text": "This shift in conformational population at higher Mg(2+) ion concentrations and to lower enzyme activity may be due to longer residence time of the NADH in the ALDH1 pocket.", "entity1": "ALDH1", "entity2": "Mg(2+)", "span1": [160, 165], "span2": [50, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2745": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "BCR", "entity2": "BMS-354825", "span1": [142, 145], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9459": {"label": 1, "data": {"text": "The EP3 receptor showed the broadest binding profile, and bound sulprostone, M&B-28767, GR63799X, 11-deoxy-PGE1, 16,16-dimethyl-PGE2 and 17-phenyl-PGE2, in addition to PGE2 and PGE1, with Ki values of 0.6-3.7 nM.", "entity1": "EP3", "entity2": "PGE2", "span1": [4, 7], "span2": [168, 172]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8449": {"label": 2, "data": {"text": "The objective of the present investigation was to evaluate l-glutamine increases glucagon like peptide-1 (GLP-1) (7-36) amide secretion in streptozotocin-nicotinamide (STZ-NTM) induced diabetic Sprague Dawley rats.", "entity1": "glucagon like peptide-1", "entity2": "l-glutamine", "span1": [81, 104], "span2": [59, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14395": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "PI3K", "entity2": "NFD", "span1": [100, 104], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5796": {"label": 0, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "ACY-1", "entity2": "amino acid", "span1": [101, 106], "span2": [29, 39]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10128": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "meclofenamic acid", "span1": [34, 37], "span2": [181, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9689": {"label": 1, "data": {"text": "Ziprasidone is a novel antipsychotic agent which binds with high affinity to 5-HT1A receptors (Ki = 3.4 nM), in addition to 5-HT1D, 5-HT2, and D2 sites.", "entity1": "5-HT1A receptors", "entity2": "Ziprasidone", "span1": [77, 93], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2116": {"label": 1, "data": {"text": "Pre-treatment of animals with dexamethasone or indomethacin reduced DEC's efficacy by almost 90% or 56%, respectively, supporting a role for the arachidonic acid and cyclooxygenase pathways in vivo.", "entity1": "cyclooxygenase", "entity2": "dexamethasone", "span1": [166, 180], "span2": [30, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7587": {"label": 1, "data": {"text": "Specifically, B2-O-CH(2)-CH(2)-N-piperidine and B2-O-CH(2)-CH(2)-N-pyrrolidine revealed a higher affinity towards hERG channels than amiodarone.", "entity1": "hERG", "entity2": "B2-O-CH(2)-CH(2)-N-pyrrolidine", "span1": [114, 118], "span2": [48, 78]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9486": {"label": 1, "data": {"text": "NMDA receptors in postmortem human spinal cord were analyzed using [3H]MK-801 ligand binding and immunoblotting with NMDA receptor subunit-specific antibodies.", "entity1": "NMDA receptors", "entity2": "[3H]MK-801", "span1": [0, 14], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7125": {"label": 0, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "amino acid", "span1": [27, 46], "span2": [5, 15]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10963": {"label": 1, "data": {"text": "Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors.", "entity1": "Nicotinic-receptor", "entity2": "galantamine", "span1": [0, 18], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7732": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "Luteinizing hormone-releasing hormone", "entity2": "triptorelin", "span1": [0, 37], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4674": {"label": 1, "data": {"text": "Using cultured human keratinocytes and diabetic rat model, the current study showed that high-glucose environment enhanced IL-8 production via epidermal growth factor receptor (EGFR) -extracelluar signal-regulated kinase (ERK) pathway in a reactive oxygen species (ROS)-dependent manner in keratinocytes.", "entity1": "extracelluar signal-regulated kinase", "entity2": "glucose", "span1": [184, 220], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10986": {"label": 3, "data": {"text": "Moreover, the specific PKC-inhibitor 2-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl) maleimide (GF 109203X) markedly increased the potency and E(max) of isoprenaline for all conditions used, including control conditions, and the synergistic effects of PMA and fenoterol were completely prevented.", "entity1": "PKC", "entity2": "GF 109203X", "span1": [23, 26], "span2": [110, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15988": {"label": 8, "data": {"text": "Protein levels of the glucose transporter (GLUT4) involved in glucose transport via these two pathways were also increased.", "entity1": "GLUT4", "entity2": "glucose", "span1": [43, 48], "span2": [62, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11291": {"label": 8, "data": {"text": "Firstly, transgenic plants overexpressing formate dehydrogenase (FDH, EC 1.2.1.2) were used to continue our previous studies on the function of FDH in formate metabolism.", "entity1": "FDH", "entity2": "formate", "span1": [144, 147], "span2": [151, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1810": {"label": 3, "data": {"text": "In this study, we have synthesized novel alpha-hydroxyphenylamide analogues of diphenylhydantoin and examined their ability to inhibit human Na(V)1.5 sodium channels expressed in Chinese Hamster Ovary (CHO-K1) cells.", "entity1": "human Na(V)1.5", "entity2": "diphenylhydantoin", "span1": [135, 149], "span2": [79, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12797": {"label": 8, "data": {"text": "As thiamine metabolism deficiencies have been seen in placental infarcts previously, these indicate that PP20/hTPK may have a role in placental diseases.", "entity1": "PP20", "entity2": "thiamine", "span1": [105, 109], "span2": [3, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13103": {"label": 4, "data": {"text": "Our work shows that sulfonylureas and glinides additionally bind to PPARgamma and exhibit PPARgamma agonistic activity.", "entity1": "PPARgamma", "entity2": "sulfonylureas", "span1": [90, 99], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4867": {"label": 3, "data": {"text": "Only FFAs that increased ceramides caused impairment of AKt and PTP1B phosphorylation at Ser 50.", "entity1": "AKt", "entity2": "ceramides", "span1": [56, 59], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13382": {"label": 0, "data": {"text": "Our structural studies provide a view of a synthetic inhibitory compound in a sirtuin active site revealing that suramin binds into the NAD(+), the product, and the substrate-binding site.", "entity1": "sirtuin", "entity2": "NAD(+)", "span1": [78, 85], "span2": [136, 142]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, -1]},
	"1702": {"label": 8, "data": {"text": "Glycylsarcosine coadministration could inhibit the uptake of cefadroxil in PEPT2(+/+) mice (p < 0.01) but not PEPT2(-/-) mice.", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [110, 115], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2466": {"label": 9, "data": {"text": "Liver choline dehydrogenase and kidney betaine-homocysteine methyltransferase expression are not affected by methionine or choline intake in growing rats.", "entity1": "betaine-homocysteine methyltransferase", "entity2": "methionine", "span1": [39, 77], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7058": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARgamma", "entity2": "retinoid", "span1": [74, 82], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12198": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "linoleic acid", "span1": [282, 285], "span2": [205, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4318": {"label": 2, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "p21", "entity2": "Pinosylvin", "span1": [282, 285], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1270": {"label": 3, "data": {"text": "Minocycline-mediated inhibition of cytochrome c release is demonstrated in vivo, in cells, and in isolated mitochondria.", "entity1": "cytochrome c", "entity2": "Minocycline", "span1": [35, 47], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5344": {"label": 2, "data": {"text": "These findings suggest that S1P activates the PI3K/Akt signaling pathway leading to the promotion of nuclear translocation of \u03b2-catenin in osteoblast-like cells, resulting in the upregulation of osteoptotegerin and osteoblast differentiation markers including alkaline phosphatase, probably relating to the inhibition of osteoclast formation and the mineralization, respectively.", "entity1": "Akt", "entity2": "S1P", "span1": [51, 54], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5353": {"label": 3, "data": {"text": "S1P activated phosphatidylinositol 3-kinase (PI3K)/Akt signaling, leading to the inhibition of glycogen synthase kinase-3\u03b2 and the nuclear translocation of \u03b2-catenin, followed by the increase of the transcriptional activity by \u03b2-catenin/T-cell factor complex formation in both SaOS-2 cells and MC3T3-E1 cells.", "entity1": "glycogen synthase kinase-3\u03b2", "entity2": "S1P", "span1": [95, 122], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2046": {"label": 1, "data": {"text": "Carvedilol modulates the expression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in a rat model of volume-overload heart failure.", "entity1": "vascular endothelial growth factor", "entity2": "Carvedilol", "span1": [75, 109], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15171": {"label": 2, "data": {"text": "In perifusion studies, FSH\u03b2 mRNA levels and FSH\u03b2LUC activities were increased by pulsatile GnRH, with significantly greater increases at low compared with high pulse frequencies.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [23, 27], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10943": {"label": 1, "data": {"text": "These results provide biochemical evidence of a H(+)-coupled and saturable transport system, presumed to be a low-affinity monocarboxylate transporter MCT4 or other unknown H(+)-coupled monocarboxylate transport system, for nicotinate in rat cerebrocortical astrocytes.", "entity1": "low-affinity monocarboxylate transporter", "entity2": "H(+)", "span1": [110, 150], "span2": [48, 52]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8266": {"label": 3, "data": {"text": "This investigation tested the hypothesis that CYP2B6 is a prominent CYP isoform responsible for clinical methadone N-demethylation and clearance, using the in vivo mechanism-based CYP2B6 inhibitor ticlopidine, given orally for 4 days.", "entity1": "CYP2B6", "entity2": "ticlopidine", "span1": [180, 186], "span2": [197, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10394": {"label": 3, "data": {"text": "We investigated the effect of AT1 receptor blockade in the NTS on the response to stimulation of HDA in anaesthetised rats treated with the neuromuscular blocking agent pancuronium bromide.", "entity1": "AT1 receptor", "entity2": "pancuronium bromide", "span1": [30, 42], "span2": [169, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"533": {"label": 1, "data": {"text": "We propose that Cu(I) binds the type-1 copper ion-binding site in the A1 domain and provides the essential requirement for a stable interaction between the heavy and light chains.", "entity1": "type-1 copper ion-binding site", "entity2": "Cu(I)", "span1": [32, 62], "span2": [16, 21]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1430": {"label": 3, "data": {"text": "They included the COX-1 inhibitor indomethacin; the COX-2 inhibitor NS-398; the mixed COX-1/COX-2 inhibitor ibuprofen; the nitric oxide (NO) derivatives of indomethacin, ibuprofen and flurbiprofen; the 5-LOX inhibitor REV 5901; and the 5-LOX activating protein (FLAP) inhibitor MK-886.", "entity1": "FLAP", "entity2": "MK-886", "span1": [262, 266], "span2": [278, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9604": {"label": 9, "data": {"text": "Mutation in the Walker A and B motifs of NBF2 of SUR1 abolished this stabilizing effect of MgADP.", "entity1": "Walker A and B motifs", "entity2": "MgADP", "span1": [16, 37], "span2": [91, 96]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11993": {"label": 2, "data": {"text": "This initial action was accompanied by up-regulation of cyclooxygenase-2 (COX-2), an important inflammation marker within 1h after TCDD treatment.", "entity1": "COX-2", "entity2": "TCDD", "span1": [74, 79], "span2": [131, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8067": {"label": 3, "data": {"text": "Overall, our results suggest that inhibition of the p38 MAPK signaling by metformin coupled with paclitaxel therapy in human NSCLC cells may be a clinically useful combination, which however will require further validation.", "entity1": "p38", "entity2": "metformin", "span1": [52, 55], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5607": {"label": 1, "data": {"text": "Intracellular K+ is required for the inactivation-induced high-affinity binding of cisapride to HERG channels.", "entity1": "HERG", "entity2": "cisapride", "span1": [96, 100], "span2": [83, 92]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7735": {"label": 5, "data": {"text": "Two pure GnRH antagonists have been developed, abarelix and degarelix, that are devoid of any agonist effect on the GnRH receptor and consequently do not result in testosterone flare.", "entity1": "GnRH", "entity2": "degarelix", "span1": [9, 13], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5764": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "UCHL- 1", "entity2": "1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine", "span1": [286, 293], "span2": [94, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3931": {"label": 3, "data": {"text": "OMT showed partial protection in the cortical neurons via down-regulation of NR2B containing NMDA receptors and up-regulation of Bcl-2 family.", "entity1": "NR2B", "entity2": "OMT", "span1": [77, 81], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9154": {"label": 3, "data": {"text": "Gossypol acetic acid (0-100 mumol/l) inhibited LDH-X prepared from the testes of the mouse greater than rabbit greater than human greater than rat greater than hamster.", "entity1": "LDH-X", "entity2": "Gossypol acetic acid", "span1": [47, 52], "span2": [0, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8646": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b1", "entity2": "melatonin", "span1": [8, 12], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4996": {"label": 2, "data": {"text": "Phenobarbital (PB), a typical CAR activator, increased the gene expression of HIF-target genes in the livers of mice, including erythropoietin, heme oxygenase-1 and vascular endothelial growth factor-a.", "entity1": "heme oxygenase-1", "entity2": "Phenobarbital", "span1": [144, 160], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15682": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Cdk1", "entity2": "EVn-50", "span1": [216, 220], "span2": [15, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15284": {"label": 1, "data": {"text": "Mice given daily injections of high dose JZL184 (\u226516 mg/kg) for six days displayed decreased CB(1) receptor density and function in brain, as assessed in [(3)H]SR141716A binding and CP55,940-stimulated [(35)S]GTP\u03b3S binding assays, respectively.", "entity1": "CB(1)", "entity2": "(35)S", "span1": [93, 98], "span2": [203, 208]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1243": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "dexamethasone", "span1": [115, 118], "span2": [59, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"103": {"label": 5, "data": {"text": "The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed.", "entity1": "histamine H1-receptor", "entity2": "terfenadine", "span1": [114, 135], "span2": [148, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14270": {"label": 8, "data": {"text": "Thus, despite the similar structures of TETA and SpmTrien, SSAT2 is the main acetylator of TETA, whereas SpmTrien is primarily acetylated by SSAT1.", "entity1": "SSAT1", "entity2": "SpmTrien", "span1": [141, 146], "span2": [105, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12673": {"label": 1, "data": {"text": "The anti-emetic and pharmacological profile of AS-8112 ((R)-5-bromo-N-(1-ethyl-4-methylhexahydro-1H-1,4-diazepin-6-yl)-2-methoxy-6-methy lamino-3-pyridinecarboxamide.2 fumarate), a novel and potent dopamine D2, D3 and 5-hydroxytryptamine-3 (5-HT3) receptors ligand, was investigated in the present study.", "entity1": "5-hydroxytryptamine-3 (5-HT3) receptors", "entity2": "AS-8112", "span1": [218, 257], "span2": [47, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11648": {"label": 8, "data": {"text": "Third, ABCA1-RNAi suppressed hepatic alpha-tocopherol secretion.", "entity1": "ABCA1", "entity2": "alpha-tocopherol", "span1": [7, 12], "span2": [37, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5044": {"label": 3, "data": {"text": "Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 2.", "entity1": "acyl-CoA:cholesterol acyltransferase 2", "entity2": "pyripyropene A", "span1": [100, 138], "span2": [49, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13289": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "platelet-derived growth factor receptor", "entity2": "BAY43-9006", "span1": [203, 242], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2436": {"label": 3, "data": {"text": "Epididymal tissue from wild-type mice responded in vitro to noradrenaline and isoprenaline with increased glycerol release, reduced IL-6 release, and increased cAMP accumulation.", "entity1": "IL-6", "entity2": "isoprenaline", "span1": [132, 136], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"231": {"label": 3, "data": {"text": "The inhibition of UG synthesis and PR down-regulation by 5 alpha-NET and 3 beta,5 alpha-NET indicates that these NET metabolites possess antiprogestational properties.", "entity1": "PR", "entity2": "NET", "span1": [35, 37], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4336": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "FAK", "entity2": "Pinosylvin", "span1": [101, 104], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9876": {"label": 5, "data": {"text": "In these tissues, JTH-601, prazosin (a non-selective alpha(1)-adrenoceptor antagonist), and tamsulosin (an alpha(1A)-adrenoceptor antagonist) competitively antagonized contraction in a concentration-dependent manner.", "entity1": "alpha(1)-adrenoceptor", "entity2": "JTH-601", "span1": [53, 74], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3229": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "ellagic acid", "span1": [286, 296], "span2": [175, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11352": {"label": 8, "data": {"text": "Voltage-gated sodium (Na) channelsNa) channels are a critical component of electrically excitable cells.", "entity1": "Voltage-gated sodium (Na) channels", "entity2": "Na", "span1": [0, 34], "span2": [34, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5304": {"label": 3, "data": {"text": "Promoter assay revealed that prunetin inhibits LPS-induced nitric oxide and prostaglandin E2 production through the suppression of iNOS and COX-2 at the transcriptional level.", "entity1": "COX-2", "entity2": "prunetin", "span1": [140, 145], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1936": {"label": 8, "data": {"text": "Carnitine acetyltransferases (CrAT) catalyze the reversible conversion of acetyl-CoA and carnitine to acetylcarnitine and free CoA.", "entity1": "Carnitine acetyltransferases", "entity2": "carnitine", "span1": [0, 28], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"4608": {"label": 3, "data": {"text": "Although thioredoxin reductase (TRR) inhibitors (aurothioglucose and Sb(III)) inhibited cytosolic DMAs(V) reduction, recombinant rat TRR plus NADPH, alone or when added to the cytosol, failed to support DMAs(V) reduction.", "entity1": "thioredoxin reductase", "entity2": "Sb(III)", "span1": [9, 30], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4745": {"label": 3, "data": {"text": "Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects.", "entity1": "MLCK", "entity2": "genistin", "span1": [249, 253], "span2": [283, 291]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5001": {"label": 1, "data": {"text": "Five classes of chalcogenopyrylium dyes (CGPs) were examined for their ability to modulate transport of [(3)H]estradiol glucuronide (E217\u03b2G) (a prototypical MRP substrate) into MRP-enriched inside-out membrane vesicles.", "entity1": "MRP", "entity2": "CGPs", "span1": [157, 160], "span2": [41, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, 8, 8, -1, -1, -1, -1]},
	"9814": {"label": 3, "data": {"text": "Mibefradil (Ro 40-5967) belongs to a new chemical class of these molecules which differs from other Ca2+ antagonists by its ability to potently block T-type Ca2+ channels.", "entity1": "T-type Ca2+ channels", "entity2": "Mibefradil", "span1": [150, 170], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2854": {"label": 2, "data": {"text": "RORalpha ectopic expression activated the cAspAT gene transcription in absence of rosiglitazone, and its protein amount in nuclear extracts is 1.8-fold increased by rosiglitazone treatment of adipocytes.", "entity1": "cAspAT", "entity2": "rosiglitazone", "span1": [42, 48], "span2": [165, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6962": {"label": 5, "data": {"text": "The aim of this study was to determine if macaque represents a suitable species for the pre-clinical evaluation of novel CCR5 antagonists, such as maraviroc (UK-427,857).", "entity1": "CCR5", "entity2": "UK-427,857", "span1": [121, 125], "span2": [158, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15070": {"label": 2, "data": {"text": "Importantly, expression of the acute-phase reactant serum amyloid A (SAA) significantly increased after ritodrine injection, with values indicating the largest fold-change.", "entity1": "serum amyloid A", "entity2": "ritodrine", "span1": [52, 67], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12013": {"label": 1, "data": {"text": "We investigated the diurnal expression of clock genes and clock-controlled genes (CCGs) in 3-hour intervals for a 24-h period in the livers of male streptozotocin (STZ)-treated rats, male spontaneous type 1 diabetic LEW.1AR1-iddm (Iddm) rats, and Iddm rats treated for 10 days with insulin.", "entity1": "CCGs", "entity2": "streptozotocin", "span1": [82, 86], "span2": [148, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2514": {"label": 3, "data": {"text": "Furthermore, auranofin inhibited NF-kappaB activation induced by MyD88-dependent downstream signaling components of TLR4, MyD88, IKKbeta, and p65.", "entity1": "NF-kappaB", "entity2": "auranofin", "span1": [33, 42], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2882": {"label": 2, "data": {"text": "In hippocampal dentate gyrus, MPH-receiving rats showed a 51% decrease in NET-ir density and a 61% expanded distribution of the new-cell marker PSA-NCAM (polysialylated form of neural cell adhesion molecule).", "entity1": "neural cell adhesion molecule", "entity2": "MPH", "span1": [177, 206], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11029": {"label": 3, "data": {"text": "Sorafenib, which belongs chemically to a class that can be described as bis-aryl ureas, was selected for further pharmacologic characterization based on potent inhibition of Raf-1 and its favorable kinase selectivity profile.", "entity1": "Raf-1", "entity2": "Sorafenib", "span1": [174, 179], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8615": {"label": 2, "data": {"text": "Conversely, cell pre-treatment with Vermentino white wine extract with smaller phenolic fraction showed only a partial NOX1 down-regulation and was ineffective in interleukin synthesis induced by dietary oxysterols.", "entity1": "NOX1", "entity2": "oxysterols", "span1": [119, 123], "span2": [204, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14444": {"label": 3, "data": {"text": "This effect was almost completely reversed by specific ABCG2 inhibitor Ko143.", "entity1": "ABCG2", "entity2": "Ko143", "span1": [55, 60], "span2": [71, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3227": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "ellagic acid", "span1": [262, 280], "span2": [175, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10550": {"label": 2, "data": {"text": "RA is known to induce expression of the Burkitt's lymphoma receptor 1 (BLR1) gene which propels RA-induced cell cycle arrest and differentiation of HL-60 human myeloblastic leukemia cells, motivating the present analysis of transcriptional regulation of blr1 expression by RA.", "entity1": "Burkitt's lymphoma receptor 1", "entity2": "RA", "span1": [40, 69], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6729": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "SU5416", "span1": [273, 279], "span2": [141, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14342": {"label": 3, "data": {"text": "Additionally, DMF and Ad-Nrf2 repressed TGF-beta-stimulated Smad3 activity by inhibiting Smad3 phosphorylation, which was restored by siRNA-mediated knockdown of Nrf2 expression.", "entity1": "Smad3", "entity2": "DMF", "span1": [89, 94], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9900": {"label": 1, "data": {"text": "Changes in UCP-3 mRNA occur in parallel with modifications in the levels of free fatty acids, which are reduced in lactation and are upregulated due to weaning or fasting.", "entity1": "UCP-3", "entity2": "fatty acids", "span1": [11, 16], "span2": [81, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2025": {"label": 1, "data": {"text": "CONCLUSION: Oral quinidine is effective in suppressing the gain of function in IKr responsible for some cases of short QT syndrome with a mutation in HERG and thus restoring normal rate dependence of the QT interval and rendering ventricular tachycardia/ventricular fibrillation noninducible.", "entity1": "HERG", "entity2": "quinidine", "span1": [150, 154], "span2": [17, 26]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1541": {"label": 9, "data": {"text": "The purified human enzyme also does not oxidize eight representative antitumor polyamine analogues; however, specific oligamine analogues were found to be potent inhibitors of the oxidation of spermine by PAOh1/SMO.", "entity1": "PAOh1", "entity2": "polyamine", "span1": [205, 210], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12663": {"label": 1, "data": {"text": "Various drugs used in the treatment of IBD, such as glucocorticoids, 5-aminosalicylic acid, and sulfasalazine, interfere with NF-kappaB/Rel signaling.", "entity1": "NF-kappaB", "entity2": "5-aminosalicylic acid", "span1": [126, 135], "span2": [69, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13995": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "VEGF receptor 2", "entity2": "Cabozantinib", "span1": [94, 109], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8608": {"label": 3, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "AST", "entity2": "NAC", "span1": [31, 34], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14917": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "\u0394(5)-androstenediol", "span1": [266, 269], "span2": [35, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3424": {"label": 0, "data": {"text": "In the L858R mutant structure, the active-site cleft is expanded by the repositioning of Phe723 within the P-loop.", "entity1": "L858R", "entity2": "Phe", "span1": [7, 12], "span2": [89, 92]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11240": {"label": 1, "data": {"text": "MCP-1 and MIP-2 was tested after 1, 10, 20, 30, and 40 days post inoculation, before and after mimosine treatment.", "entity1": "MIP-2", "entity2": "mimosine", "span1": [10, 15], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9591": {"label": 5, "data": {"text": "These results indicate that carbetocin is a partial agonist/antagonist to the oxytocin receptor while the two metabolites carbetocin metabolite I and carbetocin metabolite II are pure antagonists.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [78, 95], "span2": [150, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6736": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "CEP-701", "span1": [268, 272], "span2": [193, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4109": {"label": 2, "data": {"text": "Furthermore, compared with control groups, the plaque endothelium level of p75(NTR) was 3-fold increased and the liver level of p75(NTR) was 17.4-fold increased by SFO-HD.", "entity1": "p75(NTR)", "entity2": "SFO", "span1": [128, 136], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5579": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "CA II", "entity2": "methazolamide", "span1": [144, 149], "span2": [229, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15599": {"label": 1, "data": {"text": "In the current study, we crossed mdr1a.fLUC mice into the pxr knockout (pxr(-/-)) genetic background and injected mice with pregnenolone-16\u03b1-carbonitrile (PCN), a strong PXR ligand, and two therapeutically relevant taxanes, paclitaxel and docetaxel.", "entity1": "PXR", "entity2": "pregnenolone-16\u03b1-carbonitrile", "span1": [170, 173], "span2": [124, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12462": {"label": 1, "data": {"text": "In the African-American cohort, after excluding Y186C carriers, homozygous carriers of C29R showed 27% higher DPD activity as compared with noncarriers (609\u2009\u00b1\u2009152 and 480\u2009\u00b1\u2009152 pmol 5-FU min(-1) mg(-1), respectively; P = 0.013).Clinical Pharmacology & Therapeutics (2013); advance online publication 1 May 2013. doi:10.1038/clpt.2013.69.", "entity1": "DPD", "entity2": "5-FU", "span1": [110, 113], "span2": [182, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9262": {"label": 3, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "ergotamine", "span1": [50, 53], "span2": [153, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8666": {"label": 2, "data": {"text": "We found that, before apoptosis, cisplatin induces c-Abl and TAp73 expression in the oocyte.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [51, 56], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2542": {"label": 8, "data": {"text": "Polyclonal antisera to either b5R or cyt b5 significantly inhibited N-hydroxy-4-aminobiphenyl (NHOH-4-ABP) reduction by 95 and 89%, respectively, and immunoreactive cyt b5 protein content in individual HLM was significantly correlated with individual reduction of both NHOH-4-ABP and N-hydroxy-PhIP (NHOH-PhIP).", "entity1": "b5R", "entity2": "NHOH-4-ABP", "span1": [30, 33], "span2": [95, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12926": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CSE", "entity2": "L-cysteine", "span1": [119, 122], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8664": {"label": 2, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "TAp73", "entity2": "cisplatin", "span1": [146, 151], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"499": {"label": 1, "data": {"text": "Using biotinylated FGF-2 and FGF-7 (KGF) as probes, we have identified specific interactions between FGFs and heparan sulfates in human tissues.", "entity1": "FGFs", "entity2": "sulfates", "span1": [101, 105], "span2": [118, 126]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6557": {"label": 3, "data": {"text": "In contrast, the mutants T844A, F972A and Q975A showed increased K(i) for cilostazol but no difference for milrinone from the recombinant PDE3A.", "entity1": "PDE3A", "entity2": "milrinone", "span1": [138, 143], "span2": [107, 116]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4059": {"label": 9, "data": {"text": "Jaspamide also inhibited other channels including Cav1.2, Cav3.2, and HCN2; however, the Kv11.1 (hERG) channel was minimally affected.", "entity1": "Kv11.1", "entity2": "Jaspamide", "span1": [89, 95], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6202": {"label": 3, "data": {"text": "Cocaine block of hH1 channels was greater than block of mu1 channels at voltages between -120 mV and -90 mV, suggesting that greater steady-state inactivation of hH1 channels in this voltage range makes them more susceptible to cocaine block.", "entity1": "hH1 channels", "entity2": "Cocaine", "span1": [17, 29], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1419": {"label": 3, "data": {"text": "We hypothesized that the HED compounds would be most potent at the norepinephrine transporter (NET) compared to the serotonin or dopamine transporters and that the 1R diastereomers would be more effective than 1S diastereomers.", "entity1": "norepinephrine transporter", "entity2": "HED", "span1": [67, 93], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"16072": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "Bruton's tyrosine kinase", "entity2": "Ibrutinib", "span1": [97, 121], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5214": {"label": 1, "data": {"text": "Vinblastine-induced apoptosis of melanoma cells is mediated by Ras homologous A protein (Rho A) via mitochondrial and non-mitochondrial-dependent mechanisms.", "entity1": "Rho A", "entity2": "Vinblastine", "span1": [89, 94], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"206": {"label": 2, "data": {"text": "The results of this study suggest that noradrenaline predominantly, but not exclusively, mediates contraction of rat aorta through the activation of an alphalD-adrenoceptor.", "entity1": "alphalD-adrenoceptor", "entity2": "noradrenaline", "span1": [152, 172], "span2": [39, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4868": {"label": 3, "data": {"text": "Cells were also evaluated in the presence of wortmannin, an inhibitor of phosphatidylinositol 3-kinases and thus AKt (0-100 nM).", "entity1": "phosphatidylinositol 3-kinases", "entity2": "wortmannin", "span1": [73, 103], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12732": {"label": 3, "data": {"text": "Agents which have recently been shown to block cyclin D1 translation by regulating calcium levels are the unsaturated essential fatty acid, eicosapentaenoic acid (EPA), the antidiabetic thiazolidinediones, and the antifungal agent, clotrimazole.", "entity1": "cyclin D1", "entity2": "unsaturated essential fatty acid", "span1": [47, 56], "span2": [106, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1185": {"label": 2, "data": {"text": "In conclusion, fenoterol-induced constitutive beta(2)-adrenoceptor activity reduces muscarinic receptor agonist- and histamine-induced contractions of bovine tracheal smooth muscle, which can be reversed by the inverse agonist timolol.", "entity1": "beta(2)-adrenoceptor", "entity2": "fenoterol", "span1": [46, 66], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15287": {"label": 1, "data": {"text": "In contrast, normal CB(1) receptor expression and function were maintained following repeated administration of low dose JZL184 (\u22648 mg/kg).", "entity1": "CB(1)", "entity2": "JZL184", "span1": [20, 25], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8379": {"label": 3, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "IR", "entity2": "BPA", "span1": [173, 175], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13926": {"label": 1, "data": {"text": "Different VDRAs are known to have differential effects on serum calcium (Ca), which may also affect serum PTH levels since serum Ca regulates PTH secretion mediated by the Ca-sensing receptor (CaSR).", "entity1": "Ca-sensing receptor", "entity2": "Ca", "span1": [172, 191], "span2": [129, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13571": {"label": 1, "data": {"text": "A humanized antibody to HER2/neu, trastuzumab, is now FDA approved for the treatment of early stage, HER2/neu overexpressing breast cancer sequenced with chemotherapy including doxorubicin, cyclophosphamide, and paclitaxel.", "entity1": "HER2", "entity2": "paclitaxel", "span1": [101, 105], "span2": [212, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7858": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "mGlu1", "entity2": "BAPTA", "span1": [40, 45], "span2": [207, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6234": {"label": 1, "data": {"text": "However, [3H]eletriptan had over 6-fold higher affinity than [3H]sumatriptan at the 5-HT1D receptor (K(D)): 0.92 and 6.58 nM, respectively) and over 3-fold higher affinity than [3H]sumatriptan at the 5-HT1B receptor (K(D): 3.14 and 11.07 nM, respectively).", "entity1": "5-HT1B", "entity2": "[3H]sumatriptan", "span1": [200, 206], "span2": [61, 76]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9707": {"label": 3, "data": {"text": "The reversible MAO-A inhibitor, befloxatone (0.3-3 mg/kg), and the irreversible MAO-A inhibitor, clorgyline (10-30 mg/kg), also reduced ethanol self-administration.", "entity1": "MAO-A", "entity2": "clorgyline", "span1": [80, 85], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7391": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "PRODH", "entity2": "proline", "span1": [23, 28], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3014": {"label": 3, "data": {"text": "Inhibitors of PDE4 (rolipram; 0.1-10 microM) and PDE3 (cilostazol; 0.1-10 microM) delayed spontaneous eosinophil apoptosis maximally by 25% and 15%, respectively.", "entity1": "PDE4", "entity2": "rolipram", "span1": [14, 18], "span2": [20, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13210": {"label": 9, "data": {"text": "Triflusal (30 mg/kg) or aspirin treatment (30 mg/kg) did not reduce the levels of GFAP or Hsp27 immunostaining.", "entity1": "Hsp27", "entity2": "Triflusal", "span1": [90, 95], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6703": {"label": 1, "data": {"text": "Inhibitory effects of the monoamine oxidase inhibitor tranylcypromine on the cytochrome P450 enzymes CYP2C19, CYP2C9, and CYP2D6.", "entity1": "CYP2C9", "entity2": "tranylcypromine", "span1": [110, 116], "span2": [54, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7642": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "indanyloxyacetic acid 94", "span1": [34, 39], "span2": [296, 320]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14027": {"label": 3, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Together, these data suggest that thiocolchicoside significantly suppressed osteoclastogenesis induced by RANKL and tumour cells via the NF-kappaB signalling pathway.", "entity1": "NF-kappaB", "entity2": "thiocolchicoside", "span1": [167, 176], "span2": [64, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11506": {"label": 0, "data": {"text": "New data for cattle (Bos taurus) indicates a gene encoding GnRH-II decapeptide possessing arginine (codon: CGG) rather than tryptophan (TGG) at position three in the mature peptide.", "entity1": "GnRH-II", "entity2": "TGG", "span1": [59, 66], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8244": {"label": 1, "data": {"text": "PURPOSE: To characterise further the previously observed cytochrome P450 3A4 (CYP3A4) interaction of the dual orexin receptor antagonist almorexant.", "entity1": "cytochrome P450 3A4", "entity2": "almorexant", "span1": [57, 76], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8982": {"label": 5, "data": {"text": "The suppressive effect of ceruletide on barrel rotation could be partially countered by MK-329, a selective peripheral CCK (CCK-A) receptor antagonist.", "entity1": "(CCK-A) receptor", "entity2": "MK-329", "span1": [123, 139], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14727": {"label": 4, "data": {"text": "Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.", "entity1": "Toll-like receptor 7", "entity2": "8-oxoadenine", "span1": [63, 83], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11017": {"label": 2, "data": {"text": "These results suggested that Captopril can protect the vascular endothelium against the damages induced by L-methionine in rats, and the beneficial effects of Captopril may be related to attenuating the decrease in PON1 activity and NO levels.", "entity1": "PON1", "entity2": "Captopril", "span1": [215, 219], "span2": [159, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3955": {"label": 1, "data": {"text": "Vitamin K2 covalently binds to Bak and induces Bak-mediated apoptosis.", "entity1": "Bak", "entity2": "Vitamin K2", "span1": [47, 50], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6138": {"label": 1, "data": {"text": "Thus, our results indicate that important determinants of dofetilide binding are localized to the pore region of HERG.", "entity1": "HERG", "entity2": "dofetilide", "span1": [113, 117], "span2": [58, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2039": {"label": 8, "data": {"text": "L-serine dehydratase (SDH), a member of the beta-family of pyridoxal phosphate-dependent (PLP) enzymes, catalyzes the deamination of L-serine and L-threonine to yield pyruvate or 2-oxobutyrate.", "entity1": "L-serine dehydratase", "entity2": "L-serine", "span1": [0, 20], "span2": [133, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3457": {"label": 1, "data": {"text": "R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less.", "entity1": "DAT", "entity2": "S-modafinil", "span1": [49, 52], "span2": [103, 114]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9201": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "EGF", "entity2": "N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide", "span1": [261, 264], "span2": [58, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8715": {"label": 2, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "GPx", "entity2": "Na2SeO3", "span1": [30, 33], "span2": [99, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1126": {"label": 3, "data": {"text": "Our data also prove that indomethacin is not only an activator of CA but also antagonizes the effect of acetazolamide, a specific inhibitor of this enzyme.", "entity1": "CA", "entity2": "acetazolamide", "span1": [66, 68], "span2": [104, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"85": {"label": 1, "data": {"text": "The high-affinity of catecholamines to phenylalanine hydroxylase is a valuable probe to study the active site of this enzyme and is also relevant for the homologous enzyme tyrosine hydroxylase, which is purified as a stable catecholamine-Fe(III) complex.", "entity1": "phenylalanine hydroxylase", "entity2": "catecholamines", "span1": [39, 64], "span2": [21, 35]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9362": {"label": 3, "data": {"text": "DMI administration for up to 21 days produced a progressive reduction in the number of 5-HT2A receptors in frontal cortex, without significant alterations in occipital cortex.", "entity1": "5-HT2A", "entity2": "DMI", "span1": [87, 93], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1549": {"label": 8, "data": {"text": "The discovery of an inducible oxidase whose apparent substrate preference is spermine indicates that polyamine catabolism is more complex than that originally proposed.", "entity1": "oxidase", "entity2": "spermine", "span1": [30, 37], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11155": {"label": 1, "data": {"text": "LY 344864 appears to attenuate c-fos-like immunoreactivity via 5-HT1F receptors, while sumatriptan acts via 5-HT1B receptors.", "entity1": "5-HT1F", "entity2": "LY 344864", "span1": [63, 69], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14761": {"label": 3, "data": {"text": "Jaceosidin, isolated from dietary mugwort (Artemisia princeps), induces G2/M cell cycle arrest by inactivating cdc25C-cdc2 via ATM-Chk1/2 activation.", "entity1": "cdc25C", "entity2": "Jaceosidin", "span1": [111, 117], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11714": {"label": 1, "data": {"text": "F344 gpt delta rats were subjected to repeated oral administration of MEG at dosages of 0, 10, 30, or 100mg/kg (a carcinogenic dose) for 13 weeks.", "entity1": "gpt", "entity2": "MEG", "span1": [5, 8], "span2": [70, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10940": {"label": 3, "data": {"text": "Therefore, decreases of PLK and PNPO in the hippocampal CA1 region of aged brains may be involved in aging processes related with gamma-aminobutyric acid (GABA) function.", "entity1": "PLK", "entity2": "GABA", "span1": [24, 27], "span2": [155, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12190": {"label": 1, "data": {"text": "Several variables associated to thymidylate synthase (TS), the biological target of 5-fluorouracil (5FU) have been studied for their possible role as predictors of the clinical outcome and response to chemotherapy in colorectal cancer (CRC) patients.", "entity1": "TS", "entity2": "5-fluorouracil", "span1": [54, 56], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2272": {"label": 8, "data": {"text": "CONCLUSIONS: Total vitamin B6 is abnormally high in autism, consistent with previous reports of an impaired pyridoxal kinase for the conversion of pyridoxine and pyridoxal to PLP.", "entity1": "pyridoxal kinase", "entity2": "PLP", "span1": [108, 124], "span2": [175, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14042": {"label": 3, "data": {"text": "We have examined the effectiveness of two novel Chk1 selective inhibitors, AR323 and AR678, in a panel of melanoma cell lines and normal cell types.", "entity1": "Chk1", "entity2": "AR323", "span1": [48, 52], "span2": [75, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11752": {"label": 3, "data": {"text": "Three different 3D-QSAR models were built and validated by using a set of 66 pyrazole (Model\u2005I) and furanopyrimidine (Model\u2005II) compounds with IC(50) values toward Aurora kinase\u2005A ranging from 33\u2005nM to 10.5\u2005\u03bcM.", "entity1": "Aurora kinase\u2005A", "entity2": "furanopyrimidine", "span1": [164, 179], "span2": [100, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6777": {"label": 1, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX", "entity2": "Aspirin", "span1": [119, 122], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13524": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "CDO", "entity2": "NO", "span1": [22, 25], "span2": [77, 79]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9675": {"label": 8, "data": {"text": "We find that FP causes a decrease in stimulated eosinophil secretion of LTC4 that is regulated by phospholipase A2 (PLA2).", "entity1": "phospholipase A2", "entity2": "LTC4", "span1": [98, 114], "span2": [72, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3295": {"label": 3, "data": {"text": "A phase III randomized placebo-controlled trial has examined the impact of everolimus in patients with clear cell renal cancers and progressive disease on or within 6 months of the VEGFR tyrosine kinase inhibitors sunitinib and/or sorafenib.", "entity1": "VEGFR", "entity2": "sorafenib", "span1": [181, 186], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11287": {"label": 8, "data": {"text": "An alternative THF-dependent pathway involves the C1-THF synthase/SHMT activities with formate as 1-C source.", "entity1": "SHMT", "entity2": "formate", "span1": [66, 70], "span2": [87, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7747": {"label": 3, "data": {"text": "Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer.", "entity1": "tyrosine kinase", "entity2": "Cabozantinib", "span1": [42, 57], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6650": {"label": 1, "data": {"text": "A comparison of the results with previous data for desipramine and cocaine inhibition of norepinephrine uptake by the mutant hNETs reveals that MrIA binding to hNET occurs at a site that is distinct from but overlaps with the binding sites for tricyclic antidepressants and cocaine.", "entity1": "hNET", "entity2": "tricyclic", "span1": [160, 164], "span2": [244, 253]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5698": {"label": 1, "data": {"text": "In addition, we provide evidence that apomorphine also acts on endogenous TRPA1 in cultured dorsal root ganglion neurons from rats and in the enterochromaffin model cell line QGP-1, from which serotonin is released upon activation of TRPA1.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [74, 79], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7121": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "PDE5Delta1-465", "entity2": "N", "span1": [276, 290], "span2": [97, 98]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13654": {"label": 0, "data": {"text": "The distances between the protons H20 and H2, H18 and H2, and H18 and H4 are shorter following their binding to the PGIS in solution-down to within 5 A.", "entity1": "PGIS", "entity2": "H2", "span1": [116, 120], "span2": [54, 56]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5865": {"label": 1, "data": {"text": "To our surprise, when mu-receptor binding was determined by using [3H]Tyr-D-Ala-Gly-MePhe-Gly-ol (DAMGO), a 10-15% decrease in binding was also observed in the midbrain and cortex after 4 days of DPDPE treatment.", "entity1": "mu-receptor", "entity2": "DPDPE", "span1": [22, 33], "span2": [196, 201]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10220": {"label": 2, "data": {"text": "Metformin-induced increases in AMPK activity were associated with higher rates of glucose disposal and muscle glycogen concentrations.", "entity1": "AMPK", "entity2": "Metformin", "span1": [31, 35], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11178": {"label": 1, "data": {"text": "METHODS: Expression of PR mRNA and PR protein were determined by Northern blot and HAP of single-dose saturated analysis in myometrium and leiomyomata (center and marginal area) from 27 untreated and 6 mifepristone pretreated women with leiomyomata.", "entity1": "PR protein", "entity2": "mifepristone", "span1": [35, 45], "span2": [202, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2756": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "human COX-2", "entity2": "2,6-dichloro", "span1": [75, 86], "span2": [92, 104]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3500": {"label": 1, "data": {"text": "Effects of fenofibrate, a PPAR-\u03b1 ligand, on the haemodynamics of glycerol-induced renal failure in rats.", "entity1": "PPAR-\u03b1", "entity2": "fenofibrate", "span1": [26, 32], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3183": {"label": 2, "data": {"text": "The maximum stimulation of Cdx2 and MUC2 mRNA induced by CDCA was observed at 3 h and by 6 h, respectively.", "entity1": "Cdx2", "entity2": "CDCA", "span1": [27, 31], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5767": {"label": 3, "data": {"text": "NSDA neurons displayed significant axon terminal degeneration (as indexed by decreases in DA, tyrosine hydroxylase (TH) and DA transporter concentrations in the striatum) as well as loss of TH-immunoreactive (IR) neurons in the substantia nigra (SN) following MPTP, whereas TIDA neurons revealed no overt axon terminal pathology or loss of TH-IR cell bodies.", "entity1": "tyrosine hydroxylase", "entity2": "MPTP", "span1": [94, 114], "span2": [260, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10604": {"label": 1, "data": {"text": "Here, we show that the synaptic vesicle protein SV2A is the brain binding site of levetiracetam (LEV), a new antiepileptic drug with a unique activity profile in animal models of seizure and epilepsy.", "entity1": "synaptic vesicle protein SV2A", "entity2": "levetiracetam", "span1": [23, 52], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13239": {"label": 3, "data": {"text": "Our results suggest that glutamate induces GRIP1 degradation by proteasome through an NMDA receptor-Ca2+ pathway and that GRIP1 degradation may play an important role in regulating GluR2 surface expression.", "entity1": "GRIP1", "entity2": "glutamate", "span1": [122, 127], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12875": {"label": 2, "data": {"text": "These results indicate that the ATPase activity of the secretory granule Atp8a1 is activated by phospholipids binding to a specific site whose properties (PS selectivity, dependence upon glycerol but not serine, stereochemistry, and vanadate sensitivity) are similar to, but distinct from, the properties of the substrate binding site of the plasma membrane flippase.", "entity1": "Atp8a1", "entity2": "PS", "span1": [73, 79], "span2": [155, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"11709": {"label": 2, "data": {"text": "DBDCT also caused the phosphorylation of JNK and p38(MAPK).", "entity1": "MAPK", "entity2": "DBDCT", "span1": [53, 57], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13973": {"label": 3, "data": {"text": "BACKGROUND: Recent epidemiologic and laboratory studies have suggested that non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the risk of breast cancer through inhibition of cyclooxygenase-2 (COX-2).", "entity1": "COX-2", "entity2": "steroidal", "span1": [200, 205], "span2": [80, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13730": {"label": 1, "data": {"text": "These data support the concept that adipose tissue NNMT contributes to the increased plasma homocysteine levels in patients treated with NA.", "entity1": "NNMT", "entity2": "NA", "span1": [51, 55], "span2": [137, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14048": {"label": 2, "data": {"text": "Aspirin inhibits mTOR signaling, activates AMP-activated protein kinase, and induces autophagy in colorectal cancer cells.", "entity1": "AMP-activated protein kinase", "entity2": "Aspirin", "span1": [43, 71], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9787": {"label": 5, "data": {"text": "In contrast, combined pretreatment with beta-funaltrexamine (mu-receptor antagonist; 20 mg/kg, s.c.) and norbinaltorphimine (kappa-receptor antagonist; 20 mg/kg, s.c.), at doses that inhibited the antitussive activity of mu- and kappa-receptor agonists, respectively, was without effect on the antitussive response of SB 227122 (20 mg/kg, i.p.).", "entity1": "mu-receptor", "entity2": "beta-funaltrexamine", "span1": [61, 72], "span2": [40, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11800": {"label": 1, "data": {"text": "In this study, we assessed the antitumor activity of PTE against human osteosarcoma cells and explored the role of JAK2/STAT3 and apoptosis-related signaling pathways on the activity of PTE.", "entity1": "JAK2", "entity2": "PTE", "span1": [115, 119], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7177": {"label": 3, "data": {"text": "In order to produce potent new leads for anticancer drugs, a new series of quinazoline analogs was designed to resemble methotrexate (MTX, 1) structure features and fitted with functional groups believed to enhance inhibition of mammalian DHFR activity.", "entity1": "mammalian DHFR", "entity2": "MTX", "span1": [229, 243], "span2": [134, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9657": {"label": 8, "data": {"text": "RESULTS: Administration of SC-236 to cirrhotic animals did not produce significant renal effects, whereas administration of the nonselective COX-1/COX-2 inhibitor, ketorolac, resulted in a marked reduction in urine volume, urinary excretion of prostaglandins, and glomerular filtration rate and in a significant impairment in renal water metabolism.", "entity1": "COX-2", "entity2": "prostaglandins", "span1": [147, 152], "span2": [244, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8396": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "glutathione-S-transferase", "entity2": "Cd", "span1": [244, 269], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"401": {"label": 3, "data": {"text": "Association of PGE2 or acetazolamide to NSAIDs reduced NSAID-induced activation of CA I and CA II.", "entity1": "CA I", "entity2": "acetazolamide", "span1": [83, 87], "span2": [23, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9391": {"label": 1, "data": {"text": "Naphazoline was the most selective compound for the high affinity state of the alpha-2A adrenoceptor, displaying 7-, 23- and 9-fold higher affinity than alpha-2B, alpha-2C and platelet I1-midazoline binding sites, respectively.", "entity1": "alpha-2A adrenoceptor", "entity2": "Naphazoline", "span1": [79, 100], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11406": {"label": 1, "data": {"text": "Comparison with the rSDH-(PLP-OMS) holo-enzyme reveals a large structural difference in active sites caused by the artifical O-methylserine.", "entity1": "rSDH", "entity2": "O-methylserine", "span1": [20, 24], "span2": [125, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1729": {"label": 1, "data": {"text": "The [3H]DHA binding was to a single receptor population with a dissociation constant of 0.42 nM, as would be expected for wild-type beta2AR.", "entity1": "beta2AR", "entity2": "[3H]DHA", "span1": [132, 139], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14110": {"label": 2, "data": {"text": "CRBN mediated antiproliferative activities of lenalidomide and pomalidomide in myeloma cells, as well as lenalidomide- and pomalidomide-induced cytokine production in T cells.", "entity1": "cytokine", "entity2": "lenalidomide", "span1": [144, 152], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7933": {"label": 3, "data": {"text": "In addition, glucosamine attenuated p21 protein stability via the proteasomal proteolytic pathway, as well as inducing p21 nuclear accumulation.", "entity1": "p21", "entity2": "glucosamine", "span1": [36, 39], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13015": {"label": 7, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "Phospholipase C beta", "entity2": "Ca2+", "span1": [0, 20], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6607": {"label": 3, "data": {"text": "The effects of histamine H1-receptor antagonists, promethazine and homochlorcyclizine, both of which are inhibitors of CYP2D6, on the steady-state plasma concentrations (Css) of haloperidol and reduced haloperidol were studied in 23 schizophrenic inpatients receiving haloperidol, 12 to 36 mg/d, for 2 to 29 weeks.", "entity1": "CYP2D6", "entity2": "promethazine", "span1": [119, 125], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13965": {"label": 1, "data": {"text": "However, a glutathione-S-transferase pull-down assay showed reduced binding of R316C with NCoR in the absence of T3 and impaired release in the presence of T3.", "entity1": "NCoR", "entity2": "T3", "span1": [90, 94], "span2": [156, 158]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13358": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "estrogen receptor", "entity2": "Medroxyprogesterone acetate", "span1": [56, 73], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7433": {"label": 1, "data": {"text": "Potential binding conformations of D1 and D2 receptors were obtained, and the D1-SPD and D2-SPD complexes were generated, which are in good agreement with most of experimental data.", "entity1": "D2", "entity2": "SPD", "span1": [89, 91], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5877": {"label": 1, "data": {"text": "In vitro binding studies showed that both amoxapine and amitriptyline interact in the nanomolar range with 5-HT2 receptors labelled by [3H]ketanserin in cortical membranes.", "entity1": "5-HT2", "entity2": "[3H]ketanserin", "span1": [107, 112], "span2": [135, 149]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1118": {"label": 3, "data": {"text": "Acetazolamide, a specific inhibitor of CA, reduces the activity of CA I and CA II from red cells.", "entity1": "CA I", "entity2": "Acetazolamide", "span1": [67, 71], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14768": {"label": 1, "data": {"text": "Electrical Stimuli Release ATP to Increase GLUT4 Translocation and Glucose Uptake via PI3K\u03b3-Akt-AS160 in Skeletal Muscle Cells.", "entity1": "Akt", "entity2": "ATP", "span1": [92, 95], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1794": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "kinase", "entity2": "GW572016", "span1": [175, 181], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12113": {"label": 3, "data": {"text": "Cocaine block of human cardiac (hH1) and rat skeletal (mu1) muscle sodium channels was examined under whole-cell voltage clamp in transiently transfected HEK293t cells.", "entity1": "human cardiac (hH1)", "entity2": "Cocaine", "span1": [17, 36], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9068": {"label": 1, "data": {"text": "The present study reports the in vitro binding affinities of the same compounds for muscarinic cholinergic receptors and for histamine H1 receptors in rat brain, using 3H-quinuclidinyl benzilate and 3H-mepyramine as radioligands.", "entity1": "histamine H1 receptors", "entity2": "3H-quinuclidinyl benzilate", "span1": [125, 147], "span2": [168, 194]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8427": {"label": 3, "data": {"text": "Compared with normally-fed counterparts, PM-CP rats exhibited higher glutathione S-transferase, aminopeptidase N and cysteine S-conjugate beta-lyase (CCBL) and lower gamma-glutamyltransferase activities, PM-FU rats exhibited decreased dihydropyrimidine dehydrogenase and cytochrome P450 1A1/2 activities and PM-MMC rats showed higher quinone reductase and depleted xanthine oxidase activities.", "entity1": "xanthine oxidase", "entity2": "MMC", "span1": [365, 381], "span2": [311, 314]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9282": {"label": 1, "data": {"text": "Mediation of noradrenaline-induced contractions of rat aorta by the alpha 1B-adrenoceptor subtype.", "entity1": "alpha 1B-adrenoceptor", "entity2": "noradrenaline", "span1": [68, 89], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8205": {"label": 3, "data": {"text": "Ruxolitinib is a small-molecule inhibitor\u00a0of JAK1 and JAK2 and recently became the first drug approved by the United States Food and Drug Administration for the treatment of symptomatic intermediate- or high-risk myelofibrosis.", "entity1": "JAK1", "entity2": "Ruxolitinib", "span1": [45, 49], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10798": {"label": 3, "data": {"text": "Simvastatin, an HMG-CoA reductase inhibitor with mild inhibition of LFA-1, induced the production of interleukin (IL)-18, tumor necrosis factor (TNF)-alpha and interferon (IFN)-gamma in human peripheral blood mononuclear cells (PBMC).", "entity1": "LFA-1", "entity2": "Simvastatin", "span1": [68, 73], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9617": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBFs", "entity2": "nucleotide", "span1": [93, 97], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10584": {"label": 3, "data": {"text": "CONCLUSION: Imidapril and irbesartan can not only control blood pressure but also inhibit mesenteric arteries remodeling and mRNA expression of TGF-beta1, c-Jun in SHR.", "entity1": "c-Jun", "entity2": "irbesartan", "span1": [155, 160], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8949": {"label": 1, "data": {"text": "Analysis of coenzyme binding by human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase and steroid 5----4-ene-isomerase using 5'-[p-(fluorosulfonyl)benzoyl]adenosine, an affinity labeling cofactor analog.", "entity1": "human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase", "entity2": "5'-[p-(fluorosulfonyl)benzoyl]adenosine", "span1": [32, 90], "span2": [130, 169]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"1932": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "M564G", "entity2": "myristoyl-CoA", "span1": [4, 9], "span2": [93, 106]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15971": {"label": 1, "data": {"text": "Together, the information on both hCCS and hSOD1, along with a sequence analysis of eukaryotic CCSD1, allows us to propose important mechanistic aspects regarding the copper-transfer process from hCCS to hSOD1.", "entity1": "hCCS", "entity2": "copper", "span1": [196, 200], "span2": [167, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13464": {"label": 4, "data": {"text": "OBJECTIVE: The aim of this study was to assess the efficacy and tolerability of nebulized arformoterol tartrate (a selective, long-acting beta(2)-adrenergic agonist that is the [R,R] isomer of formoterol) and salmeterol xinafoate versus placebo in patients with chronic obstructive pulmonary disease (COPD).", "entity1": "beta(2)-adrenergic", "entity2": "[R,R] isomer of formoterol", "span1": [138, 156], "span2": [177, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9442": {"label": 9, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP4", "entity2": "butaprost", "span1": [118, 121], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11908": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "diglycerides", "span1": [174, 179], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11176": {"label": 1, "data": {"text": "OBJECTIVE: To determine the expression of progesterone receptor (PR) mRNA and PR protein levels in the myometrium and leiomyomata from untreated and mifepristone pretreated women with leiomyoma and to examine the mechanism of mifepristone treatment on uterine leiomyomata.", "entity1": "PR protein", "entity2": "mifepristone", "span1": [78, 88], "span2": [149, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3265": {"label": 8, "data": {"text": "TAS-102 is a novel drug containing trifluorothymidine, which is phosphorylated by TK-1 to its active monophosphated form, that in turn can inhibit TS.", "entity1": "TK-1", "entity2": "TAS-102", "span1": [82, 86], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8340": {"label": 3, "data": {"text": "Aqueous ethanol (80%) extract of lentil hulls exhibited high antioxidant and anti-inflammatory activities preferentially inhibiting 15-LOX (IC(50), 55 \u03bcg/ml), with moderate COX-1 (IC(50), 66 \u03bcg/ml) and COX-2 (IC(50), 119 \u03bcg/ml) inhibitory effects on the COX pathway, whereas faba bean hull extracts exerted relatively mild LOX inhibitory activity.", "entity1": "COX-2", "entity2": "ethanol", "span1": [202, 207], "span2": [8, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11946": {"label": 8, "data": {"text": "Ketamine is primarily metabolized to norketamine by hepatic cytochrome P450 (CYP) 2B6 and CYP3A4-mediated N-demethylation.", "entity1": "cytochrome P450 (CYP) 2B6", "entity2": "Ketamine", "span1": [60, 85], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"779": {"label": 8, "data": {"text": "Flecainide block of Na(+) current (I(Na)) was investigated in wild-type (WT) or the long QT syndrome 3 (LQT3) sodium channel alphasodium channel alpha subunit mutation with three amino acids deleted (DeltaKPQ) stably transfected into human embryonic kidney 293 cells using whole-cell, patch-clamp recordings.", "entity1": "long QT syndrome 3 (LQT3) sodium channel alpha", "entity2": "sodium", "span1": [84, 130], "span2": [130, 136]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"209": {"label": 4, "data": {"text": "Alprenolol and BAAM also caused surmountable antagonism of isoprenaline responses, and this beta 1-adrenoceptor antagonism was slowly reversible.", "entity1": "beta 1-adrenoceptor", "entity2": "isoprenaline", "span1": [92, 111], "span2": [59, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6359": {"label": 3, "data": {"text": "The mNQO activity was insensitive to dicoumarol, a potent inhibitor of cytosolic NQO1.", "entity1": "NQO1", "entity2": "dicoumarol", "span1": [81, 85], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8616": {"label": 3, "data": {"text": "Oxysterol-dependent NOX1 activation, as well as interleukin synthesis, were completely prevented by Cannonau red wine extract that contains an abundant phenolic fraction, in particular phenolic acids and flavonoids.", "entity1": "interleukin", "entity2": "phenolic acids", "span1": [48, 59], "span2": [185, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7904": {"label": 2, "data": {"text": "The AhR target gene CYP1A1 mRNA expression was induced by TCDD, but was not affected by the AR CAG length.", "entity1": "CYP1A1", "entity2": "TCDD", "span1": [20, 26], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8637": {"label": 9, "data": {"text": "Ovarian AR was not influenced by either treatment, and oviduct AR was reduced after ethanol-melatonin combination.", "entity1": "AR", "entity2": "melatonin", "span1": [8, 10], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11238": {"label": 6, "data": {"text": "A number of agents are being developed that target molecular abnormalities in IEN, have fewer or different side effects than tamoxifen, and may be effective in ER-negative or tamoxifen-resistant disease.", "entity1": "ER", "entity2": "tamoxifen", "span1": [160, 162], "span2": [125, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1469": {"label": 8, "data": {"text": "L-proline accumulation and freeze tolerance of Saccharomyces cerevisiae are caused by a mutation in the PRO1 gene encoding gamma-glutamyl kinase.", "entity1": "gamma-glutamyl kinase", "entity2": "L-proline", "span1": [123, 144], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5879": {"label": 9, "data": {"text": "Labetalol and the enantiomers lacked affinity at alpha 2-adrenoceptors while at alpha 1-adrenoceptors the order of potency was prazosin much greater than RR-SR greater than labetalol.", "entity1": "alpha 2-adrenoceptors", "entity2": "Labetalol", "span1": [49, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3256": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "methyltrienelone", "span1": [13, 16], "span2": [54, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6183": {"label": 3, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "K+ channels", "entity2": "salicylic acid", "span1": [232, 243], "span2": [66, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10296": {"label": 5, "data": {"text": "Pentosan polysulfate sodium (PPS) has been shown to exert antitumor activity by antagonizing the binding of bFGF to cell surface receptors.", "entity1": "bFGF", "entity2": "sodium", "span1": [108, 112], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13159": {"label": 2, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "JNK", "entity2": "paclitaxel", "span1": [315, 318], "span2": [378, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4834": {"label": 2, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "caspase-3", "entity2": "7\u03b2OHC", "span1": [258, 267], "span2": [67, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"938": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "F3(d)Thd", "span1": [216, 236], "span2": [82, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11740": {"label": 1, "data": {"text": "GABA type A receptors (GABA(A)-R) are important for ethanol actions and it is of interest to link individual subunits with specific ethanol behaviors.", "entity1": "GABA(A)-R", "entity2": "ethanol", "span1": [23, 32], "span2": [52, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8565": {"label": 2, "data": {"text": "Under NaCl and sorbitol stresses, catalase (CAT) activity in wnk8 mutant was 1.92- and 3.7-times of that in Col-0, respectively.", "entity1": "catalase", "entity2": "sorbitol", "span1": [34, 42], "span2": [15, 23]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12225": {"label": 2, "data": {"text": "EC50 values for S-(+)-METH were 0.89, 0.92, and 4.44 microM for rTAAR1, mTAAR1, and h-rChTAAR1, respectively.", "entity1": "rTAAR1", "entity2": "S-(+)-METH", "span1": [64, 70], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12100": {"label": 3, "data": {"text": "The results also confirmed previous reports that amezinium is highly selective for MAO-A.", "entity1": "MAO-A", "entity2": "amezinium", "span1": [83, 88], "span2": [49, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12283": {"label": 9, "data": {"text": "These data indicate that sergliflozin etabonate could improve glycemic control without its use resulting in insulin secretion, hypoglycemia, and body weight gain, and may provide a unique approach to the treatment of diabetes.", "entity1": "insulin", "entity2": "sergliflozin etabonate", "span1": [108, 115], "span2": [25, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14522": {"label": 3, "data": {"text": "Mesalamine modulates intercellular adhesion through inhibition of p-21 activated kinase-1.", "entity1": "p-21 activated kinase-1", "entity2": "Mesalamine", "span1": [66, 89], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9055": {"label": 1, "data": {"text": "Levomepromazine was the most potent and fluphenazine the least potent of the four drugs in histamine H1 receptor binding.", "entity1": "histamine H1 receptor", "entity2": "fluphenazine", "span1": [91, 112], "span2": [40, 52]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11081": {"label": 1, "data": {"text": "These observations suggest that felodipine may act directly on the phosphodiesterase as well as through calmodulin.", "entity1": "phosphodiesterase", "entity2": "felodipine", "span1": [67, 84], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2192": {"label": 1, "data": {"text": "We have elucidated the crystal structures of the cyanotoxins, motuporin (nodularin-V) and dihydromicrocystin-LA bound to human protein phosphatase-1c (gamma isoform).", "entity1": "human protein phosphatase-1c (gamma isoform)", "entity2": "dihydromicrocystin-LA", "span1": [121, 165], "span2": [90, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5402": {"label": 2, "data": {"text": "The data show that CP[c]Ph is less potent at inducing CYP1A gene expression in rainbow trout than benzo[a]pyrene (B[a]P), a well-known Ah-receptor agonist.", "entity1": "CYP1A", "entity2": "CP[c]Ph", "span1": [54, 59], "span2": [19, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6229": {"label": 1, "data": {"text": "Kinetic studies comparing the binding of [3H]eletriptan and [3H]sumatriptan to the human recombinant 5-HT1B and 5-HT1D receptors expressed in HeLa cells revealed that both radioligands bound with high specificity (>90%) and reached equilibrium within 10-15 min.", "entity1": "human recombinant 5-HT1B", "entity2": "[3H]sumatriptan", "span1": [83, 107], "span2": [60, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13200": {"label": 1, "data": {"text": "CONCLUSION: Cromolyn binds S100P, prevents activation of RAGE, inhibits tumor growth, and increases the effectiveness of gemcitabine in experimental models.", "entity1": "S100P", "entity2": "gemcitabine", "span1": [27, 32], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11664": {"label": 8, "data": {"text": "Thymidine kinase-1 (TK-1) and thymidylate synthase (TS) are key enzymes for salvage and de novo pyrimidine synthesis, respectively.", "entity1": "thymidylate synthase", "entity2": "pyrimidine", "span1": [30, 50], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15113": {"label": 2, "data": {"text": "Interestingly, GPx1a was the most sensitive to selenium availability in non stressful conditions, whereas GPx1b1 and GPx1b2 were highly induced by exposure to selenium levels that had some toxic effects on the cells.", "entity1": "GPx1b2", "entity2": "selenium", "span1": [117, 123], "span2": [159, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9772": {"label": 5, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "alpha(2)-adrenergic receptors", "entity2": "yohimbine", "span1": [73, 102], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8156": {"label": 3, "data": {"text": "Additionally, DPEP suppressed the production of inflammatory cytokines, including tumor necrosis factor-\u03b1 (TNF-\u03b1), interleukin (IL)-1\u03b2, and IL-6.", "entity1": "TNF-\u03b1", "entity2": "DPEP", "span1": [107, 112], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12500": {"label": 8, "data": {"text": "The results suggest that individuals with high Vmax beta 2-ADH and deficient in low-Km mitochondrial ALDH2, accounting for approximately 45% of the Chinese population, may end up with acetaldehyde accumulation during alcohol consumption, rendering them vulnerable to tissue injury caused by this highly reactive and toxic metabolite.", "entity1": "beta 2-ADH", "entity2": "acetaldehyde", "span1": [52, 62], "span2": [184, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12426": {"label": 1, "data": {"text": "Here, we report the first crystal structure of KIF4 complexed with the non-hydrolyzable ATP analog, AMPPNP (adenylyl imidodiphosphate), at 1.7\u00c5 resolution.", "entity1": "KIF4", "entity2": "adenylyl imidodiphosphate", "span1": [47, 51], "span2": [108, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11798": {"label": 3, "data": {"text": "Fisetin treatment showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), NF-kB p65 unit (in pancreas) and IL-1\u03b2 (plasma), serum nitric oxide (NO) with an elevation in plasma insulin.", "entity1": "IL-1\u03b2", "entity2": "Fisetin", "span1": [145, 150], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14429": {"label": 3, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C. Furthermore, the AMPK activator 5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) significantly inhibited ghrelin secretion.", "entity1": "proghrelin", "entity2": "Metformin", "span1": [54, 64], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10328": {"label": 4, "data": {"text": "Plasmacytoid dendritic cells produce cytokines and mature in response to the TLR7 agonists, imiquimod and resiquimod.", "entity1": "TLR7", "entity2": "resiquimod", "span1": [77, 81], "span2": [106, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13587": {"label": 1, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "[(3)H]NIS", "span1": [6, 10], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4387": {"label": 1, "data": {"text": "Camptothecin (CPT), a topoisomerase (Top) I-targeting drug that stabilizes Top1-DNA covalent adducts, can induce S-phase-specific cytotoxicity due to the arrest of progressing replication forks.", "entity1": "Top1", "entity2": "CPT", "span1": [75, 79], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15065": {"label": 9, "data": {"text": "The increase in SAA expression is specific to ritodrine-induced liver damage, because SAA expression was not induced by other hepatotoxic drugs such as acetaminophen, valproic acid, or metformin.", "entity1": "SAA", "entity2": "valproic acid", "span1": [86, 89], "span2": [167, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11883": {"label": 1, "data": {"text": "The objective of the current study was to investigate the effect of vanadium (V(5+)) on Cyp1 expression and activity in C57BL/6 mice liver and isolated hepatocytes.", "entity1": "Cyp1", "entity2": "vanadium", "span1": [88, 92], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1573": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "pyrano[2,3-b]quinolines", "span1": [59, 64], "span2": [103, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8147": {"label": 2, "data": {"text": "Increased urinary excretion of albumin, hemopexin, transferrin and VDBP correlates with chronic sensitization to gentamicin nephrotoxicity in rats.", "entity1": "transferrin", "entity2": "gentamicin", "span1": [51, 62], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14745": {"label": 1, "data": {"text": "Arsenic suppresses cell survival via Pirh2-mediated proteasomal degradation of \u0394Np63 protein.", "entity1": "Pirh2", "entity2": "Arsenic", "span1": [37, 42], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11308": {"label": 9, "data": {"text": "Administration of zuclopenthixol (0.7 and 1.4 mg/kg i.p.) neither affected dopamine (DA) level nor AChE activity in rat cortex and hippocampus.", "entity1": "AChE", "entity2": "zuclopenthixol", "span1": [99, 103], "span2": [18, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10395": {"label": 5, "data": {"text": "Angiotensin AT1 receptor antagonist losartan and the defence reaction in the anaesthetised rat.", "entity1": "Angiotensin AT1 receptor", "entity2": "losartan", "span1": [0, 24], "span2": [36, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15018": {"label": 3, "data": {"text": "Interestingly, AdOx disrupted actin cytoskeleton structures, leading to morphological changes, and suppressed the formation of a signaling complex composed of Src and p85/PI3K, which is linked to various tumorigenic responses.", "entity1": "p85", "entity2": "AdOx", "span1": [167, 170], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13755": {"label": 1, "data": {"text": "Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms.", "entity1": "L-type calcium channel", "entity2": "1,4-dihydropyridine", "span1": [63, 85], "span2": [15, 34]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14694": {"label": 3, "data": {"text": "In vitro experiments assessed the inhibition of transporters and CYP enzymes by GSK1292263, and a clinical drug interaction study investigated the effect of GSK1292263 (300\u2009mg BID) on the pharmacokinetic profile of simvastatin (40\u2009mg single dose) and rosuvastatin (10\u2009mg single dose).", "entity1": "transporters", "entity2": "GSK1292263", "span1": [48, 60], "span2": [80, 90]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8749": {"label": 8, "data": {"text": "Recent observations revealed that human UDP-glucuronosyltransferase (UGT) 2B10 catalyzes N-glucuronidation of amine-containing compounds.", "entity1": "human UDP-glucuronosyltransferase (UGT) 2B10", "entity2": "amine", "span1": [34, 78], "span2": [110, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1224": {"label": 9, "data": {"text": "Tamoxifen does not reduce the incidence of ER-negative cancers, nor does it appear to be effective in preventing the appearance of one third of ER-positive cancers.", "entity1": "ER", "entity2": "Tamoxifen", "span1": [144, 146], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12513": {"label": 3, "data": {"text": "Thus, carvedilol blocks both beta 1 and beta 2 adrenoceptors at antihypertensive doses, with modest selectivity being observed for the beta 1 adrenoceptor subtype.", "entity1": "beta 1 adrenoceptor", "entity2": "carvedilol", "span1": [135, 154], "span2": [6, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10048": {"label": 0, "data": {"text": "We have previously isolated from human hemofiltrate an N-terminally truncated form of the hemofiltrate CC chemokine 1 (HCC-1), and characterized HCC-1[9-74] as a strong agonist of CCR1, CCR5, and to a lower extent CCR3.", "entity1": "hemofiltrate CC chemokine 1", "entity2": "N", "span1": [90, 117], "span2": [55, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6115": {"label": 3, "data": {"text": "Previous studies have resulted in the classification of amezinium as a selective inhibitor of neuronal monoamine oxidase (MAO), because it is a much more potent MAO inhibitor in intact tissues, in which it is accumulated in noradrenergic neurones by uptake1, than in tissue homogenates.", "entity1": "MAO", "entity2": "amezinium", "span1": [122, 125], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8931": {"label": 8, "data": {"text": "The vasopressor response to the calcium channel activator, BAY-K-8644, which is mediated through the opening of voltage dependent calcium channels and the subsequent translocation of extracellular calcium, was significantly inhibited by carvedilol (1 mg/kg, iv), suggesting that carvedilol is also a calcium channel antagonist, consistent with our previous in vitro studies.", "entity1": "voltage dependent calcium channels", "entity2": "calcium", "span1": [112, 146], "span2": [197, 204]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1616": {"label": 5, "data": {"text": "Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topiramate in rat basolateral amygdala neurons.", "entity1": "kainate-receptor", "entity2": "topiramate", "span1": [30, 46], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11338": {"label": 0, "data": {"text": "The expression of the NH2 terminally truncated ErbB2 receptor (p95ErbB2) in breast cancer correlates with metastatic disease progression compared with the expression of full-length p185ErbB2.", "entity1": "ErbB2", "entity2": "NH2", "span1": [47, 52], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4885": {"label": 3, "data": {"text": "Separate 5-aza-2'-deoxycytidine pretreatment or in combination with trichostatin A reduced (m)CpG and specific small interference RNAs targeting Mecp2 and Creb1 separately or together depleting Mecp2 and/or Creb1 binding of glut3-(m)CpGs reduced glut3 expression in HT22 cells.", "entity1": "Mecp2", "entity2": "trichostatin A", "span1": [145, 150], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1501": {"label": 2, "data": {"text": "db/db mice treated with DRF 2655 showed 5- and 3.6-fold inhibition in phosphoenolpyruvate carboxykinase and glucose 6-phosphatase activity and 651% and 77% increases in the beta-oxidation enzymes carnitine palmitoyltransferase and carnitine acetyltransferase, respectively.", "entity1": "carnitine palmitoyltransferase", "entity2": "DRF 2655", "span1": [196, 226], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"686": {"label": 3, "data": {"text": "We evaluated the effects of angiotensin II and an angiotensin-converting enzyme inhibitor (cilazapril) on nerve blood flow (NBF) and electrophysiology in control and diabetic rats.", "entity1": "angiotensin-converting enzyme", "entity2": "cilazapril", "span1": [50, 79], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"6592": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "5-HT(2A)", "entity2": "clozapine", "span1": [232, 240], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8827": {"label": 3, "data": {"text": "New series of pyrrolidine mercaptosulfide, 2-mercaptocyclopentane arylsulfonamide, and 3-mercapto-4-arylsulfonamido pyrrolidine matrix metalloproteinase inhibitors (MMPIs) were designed, synthesized, and evaluated.", "entity1": "matrix metalloproteinase", "entity2": "2-mercaptocyclopentane arylsulfonamide", "span1": [128, 152], "span2": [43, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3000": {"label": 1, "data": {"text": "The molecular bases for phosphodiesterase 5 (PDE5) catalytic-site affinity for cyclic guanosine monophosphate (cGMP) and potency of inhibitors are poorly understood.", "entity1": "PDE5", "entity2": "cyclic guanosine monophosphate", "span1": [45, 49], "span2": [79, 109]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11086": {"label": 3, "data": {"text": "Effects of felodipine (a dihydropyridine calcium channel blocker) and analogues on calmodulin-dependent enzymes.", "entity1": "calcium channel", "entity2": "dihydropyridine", "span1": [41, 56], "span2": [25, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"106": {"label": 5, "data": {"text": "The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed.", "entity1": "histamine H1-receptor", "entity2": "acrivastine", "span1": [114, 135], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1214": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DAT", "entity2": "MDMA", "span1": [165, 168], "span2": [123, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2798": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "PPT-A", "entity2": "caerulein", "span1": [104, 109], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9647": {"label": 5, "data": {"text": "Our data indicate that estramustine phosphate metabolites perform as androgen antagonists of AR, an additional mechanism involved in the therapeutic effect of estramustine phosphate in patients with prostate cancer.", "entity1": "AR", "entity2": "androgen", "span1": [93, 95], "span2": [69, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13106": {"label": 1, "data": {"text": "There is a growing appreciation that the cyclic adenosine monophosphate (cAMP)-protein kinase A (PKA) signaling pathway is organized to form transduction units that function to deliver specific messages.", "entity1": "PKA", "entity2": "cyclic adenosine monophosphate", "span1": [97, 100], "span2": [41, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15717": {"label": 8, "data": {"text": "d-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor.", "entity1": "d-Amino acid oxidase", "entity2": "d-serine", "span1": [0, 20], "span2": [79, 87]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7326": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "ASCT2", "entity2": "MNI", "span1": [217, 222], "span2": [123, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3870": {"label": 1, "data": {"text": "The glycogen synthase kinase-3\u03b2/nuclear factor-kappa B pathway is involved in cinobufagin-induced apoptosis in cultured osteosarcoma cells.", "entity1": "nuclear factor-kappa B", "entity2": "cinobufagin", "span1": [32, 54], "span2": [78, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"232": {"label": 5, "data": {"text": "Doses of dimethocaine (1.7 mg/kg) and cocaine (0.3 mg/kg) which produced full (> 80%) substitution for cocaine were administered in combination with the dopamine D1 receptor antagonist SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H -benzo [d]naphtho-(2,1-b)azepine) and the dopamine D2 receptor antagonist raclopride (both at 0.003-0.03 mg/kg).", "entity1": "dopamine D1 receptor", "entity2": "SCH 39166", "span1": [153, 173], "span2": [185, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10803": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-1", "entity2": "phenylbutazone", "span1": [0, 5], "span2": [45, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10547": {"label": 2, "data": {"text": "A 5'-flanking region capable of supporting RA-induced blr1 activation in HL-60 cells was found to contain a 205-bp sequence in the distal portion that was necessary for transcriptional activation by RA.", "entity1": "blr1", "entity2": "RA", "span1": [54, 58], "span2": [43, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15799": {"label": 8, "data": {"text": "Opening of Panx1 HCs during repetitive activation allows efflux of ATP, influx of glucose and possibly Ca(2+) too, which are required for potentiation of contraction.", "entity1": "Panx1", "entity2": "glucose", "span1": [11, 16], "span2": [82, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10189": {"label": 3, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP-C", "entity2": "Rifampicin", "span1": [93, 99], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4007": {"label": 3, "data": {"text": "This study explored whether curcumin improves colonic inflammation in a rat colitis model through inhibition of the TLR4/NF-\u03baB signaling pathway and IL-27 expression.", "entity1": "IL-27", "entity2": "curcumin", "span1": [149, 154], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4998": {"label": 2, "data": {"text": "Cobalt chloride, a typical HIF activator, induced the gene expression of CAR-target genes, including cyp2b9 and cyp2b10, an accumulation of nuclear CAR and an increase in the PB-responsive enhancer module-mediated transactivation in the mouse liver.", "entity1": "cyp2b9", "entity2": "Cobalt chloride", "span1": [101, 107], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6563": {"label": 3, "data": {"text": "Our study implies that highly conserved residuals Y751, D950 and F1004 in the PDE families are key residues for binding of both substrate and inhibitors, and nonconserved T844 may be responsible for the cilostazol selectivity of PDE3A.", "entity1": "PDE", "entity2": "cilostazol", "span1": [78, 81], "span2": [203, 213]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10583": {"label": 3, "data": {"text": "CONCLUSION: Imidapril and irbesartan can not only control blood pressure but also inhibit mesenteric arteries remodeling and mRNA expression of TGF-beta1, c-Jun in SHR.", "entity1": "TGF-beta1", "entity2": "irbesartan", "span1": [144, 153], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12567": {"label": 9, "data": {"text": "Glutathione-independent prostaglandin D synthase [prostaglandin-H2 D-isomerase; (5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase, EC 5.3.99.2] is an enzyme responsible for biosynthesis of prostaglandin D2 in the central nervous system.", "entity1": "prostaglandin-H2 D-isomerase", "entity2": "Glutathione", "span1": [50, 78], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4835": {"label": 1, "data": {"text": "Lastly, the results add to the growing literature on H3R modulation in the pharmacotherapy of EtOH addiction.", "entity1": "H3R", "entity2": "EtOH", "span1": [53, 56], "span2": [94, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6435": {"label": 3, "data": {"text": "RESULT(S): Buserelin acetate, a GnRH agonist (0.1-10 ng/mL), had no significant effect on MCP-1 expression, whereas danazol (10(-7)-10(-5) M), a testosterone analog, and dexamethasone, an anti-inflammatory glucocorticoid hormone (10(-12)-10(-6)M), showed a direct and a dose-dependent inhibitory effect on MCP-1 expression.", "entity1": "MCP-1", "entity2": "danazol", "span1": [306, 311], "span2": [116, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10390": {"label": 3, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "BuChE", "entity2": "rivastigmine", "span1": [152, 157], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10581": {"label": 3, "data": {"text": "CONCLUSION: Imidapril and irbesartan can not only control blood pressure but also inhibit mesenteric arteries remodeling and mRNA expression of TGF-beta1, c-Jun in SHR.", "entity1": "TGF-beta1", "entity2": "Imidapril", "span1": [144, 153], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15569": {"label": 3, "data": {"text": "In addition to the effect on ROS, puerarin ameliorated MPTP-reduced lysosome-associated membrane protein type 2A (Lamp 2A) expression.", "entity1": "Lamp 2A", "entity2": "MPTP", "span1": [114, 121], "span2": [55, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4860": {"label": 0, "data": {"text": "Unsaturated FFAs increased DAGs, TAGs and PTP1B expression significantly, but cells remained insulin sensitive as assessed by robust AKt and PTP1B phosphorylation at serine (Ser) 50, Ser 398 and tyrosine 152.", "entity1": "PTP1B", "entity2": "Ser", "span1": [141, 146], "span2": [183, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12356": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "hTRPM8", "entity2": "apomorphine", "span1": [66, 72], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"767": {"label": 0, "data": {"text": "The inhibitor binds at the base of the active site gorge of TcAChE, interacting with both the choline-binding site (Trp-84) and the acyl-binding pocket (Phe-288, Phe-290).", "entity1": "TcAChE", "entity2": "Phe", "span1": [60, 66], "span2": [162, 165]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9709": {"label": 3, "data": {"text": "Dicumarol, a potent inhibitor of quinone oxidoreductase, at high concentration (500 microm ) caused only a 72% decrease in the utilization of resorufin.", "entity1": "quinone oxidoreductase", "entity2": "Dicumarol", "span1": [33, 55], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14531": {"label": 0, "data": {"text": "The serotonin (5-HT) receptors of type 6 (5-HT6) are quite different from all other 5-HT receptors, as they include a short third cytoplasmatic loop and a long C-terminal tail, and one intron located in the middle of the third cytoplasmatic loop.", "entity1": "serotonin (5-HT) receptors", "entity2": "C", "span1": [4, 30], "span2": [160, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13376": {"label": 8, "data": {"text": "Several genes involved with steroid metabolism also showed remarkable expression changes, including increased expression of 17beta-hydroxysteroid dehydrogenase-7 (HSD17beta7; involved in estradiol production) and decreased expression of HSD17beta5 (involved in testosterone production).", "entity1": "HSD17beta5", "entity2": "testosterone", "span1": [237, 247], "span2": [261, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1824": {"label": 3, "data": {"text": "Our studies shed light on the possible in vivo potency of the quinolines and provide a foundation for future studies aimed at creating more potent QR2 inhibitors and at understanding the physiological significance of QR2.", "entity1": "QR2", "entity2": "quinolines", "span1": [147, 150], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14409": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "ESI-09", "span1": [320, 324], "span2": [145, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8176": {"label": 1, "data": {"text": "These results demonstrate that the incoming nucleotide is unable to induce a syn-8-oxoG conformation without minor groove DNA polymerase interactions that influence templating (anti-/syn-equilibrium) of 8-oxoG while modulating fidelity.", "entity1": "DNA polymerase", "entity2": "syn-8-oxoG", "span1": [122, 136], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12143": {"label": 8, "data": {"text": "Cilostazol undergoes intensive and finally complete hepatic metabolism via the cytochrome P450 systems.", "entity1": "cytochrome P450", "entity2": "Cilostazol", "span1": [79, 94], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14485": {"label": 8, "data": {"text": "Of the rat CYP isoforms studied, CYP2D isoforms were the most efficient in catalyzing the O-demethylation of 5-methoxytryptamine to serotonin, but they were less effective than the human isoform CYP2D6.", "entity1": "CYP2D", "entity2": "O", "span1": [33, 38], "span2": [90, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2362": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "RAF", "entity2": "Sorafenib", "span1": [71, 74], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2239": {"label": 3, "data": {"text": "Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.", "entity1": "D816V", "entity2": "BMS-354825", "span1": [35, 40], "span2": [11, 21]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7100": {"label": 8, "data": {"text": "Overexpression of proline oxidase induces proline-dependent and mitochondria-mediated apoptosis.", "entity1": "proline oxidase", "entity2": "proline", "span1": [18, 33], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4638": {"label": 2, "data": {"text": "Pelargonidin activates the AhR and induces CYP1A1 in primary human hepatocytes and human cancer cell lines HepG2 and LS174T.", "entity1": "AhR", "entity2": "Pelargonidin", "span1": [27, 30], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9185": {"label": 1, "data": {"text": "Amdinocillin is a beta-amidino penicillanic acid derivative that binds specifically to penicillin-binding protein 2.", "entity1": "penicillin-binding protein 2", "entity2": "beta-amidino penicillanic acid", "span1": [87, 115], "span2": [18, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2640": {"label": 8, "data": {"text": "Unlike mouse RetSat (mRetSat), zRetSat A had an altered bond specificity saturating either the 13-14 or 7-8 double bonds of all-trans-retinol to produce either all-trans-13,14-dihydroretinol or all-trans-7,8-dihydroretinol, respectively.", "entity1": "zRetSat A", "entity2": "all-trans-13,14-dihydroretinol", "span1": [31, 40], "span2": [160, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4130": {"label": 1, "data": {"text": "Zinc drives a tertiary fold in the prion protein with familial disease mutation sites at the interface.", "entity1": "prion protein", "entity2": "Zinc", "span1": [35, 48], "span2": [0, 4]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13897": {"label": 3, "data": {"text": "METHODS: The inhibitory effect of captopril on MMP-2 activity was measured in peritoneal effluents from 17 patients on CAPD.", "entity1": "MMP-2", "entity2": "captopril", "span1": [47, 52], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6142": {"label": 1, "data": {"text": "Moreover, the reverse mutation BEAG T432S increased the affinity of BEAG K+ channels for dofetilide, whereas C-type inactivation could not be recovered.", "entity1": "K+ channels", "entity2": "dofetilide", "span1": [73, 84], "span2": [89, 99]}, "weak_labels": [-1, -1, 0, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7815": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "GluK1", "entity2": "(3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid", "span1": [176, 181], "span2": [270, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6941": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "ketoprofen", "span1": [81, 86], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3493": {"label": 2, "data": {"text": "In the CCl4 hepatotoxicity model, pre-treatment with PSM or silymarin resulted in significantly increased activities of ethylmorphine-N-demethylase and aniline 4-hydroxylase activity and cytochrome P450, compared to the CCl4 only group.", "entity1": "cytochrome P450", "entity2": "CCl4", "span1": [187, 202], "span2": [220, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10160": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "Faslodex", "span1": [110, 127], "span2": [27, 35]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7555": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "endothelial nitric oxide synthase", "entity2": "Nitric oxide", "span1": [123, 156], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"13958": {"label": 3, "data": {"text": "Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug.", "entity1": "monoamine oxidase (MAO)-B", "entity2": "N-propargyl-1-(R)-aminoindan", "span1": [81, 106], "span2": [12, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10849": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "PDGFRB,", "entity2": "Gleevec", "span1": [136, 143], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13029": {"label": 2, "data": {"text": "inactivation of cortisol to cortisone) to prevent activation of the mineralocorticoid receptor (MR) by cortisol.", "entity1": "mineralocorticoid receptor", "entity2": "cortisol", "span1": [68, 94], "span2": [103, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6624": {"label": 0, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "Asp", "span1": [3, 9], "span2": [61, 64]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6081": {"label": 3, "data": {"text": "), a cholinesterase inhibitor that potentiates the effects of acetylcholine at the muscarinic cholinergic receptor, terminated VT in four of four patients, an effect that was reversed by atropine.", "entity1": "muscarinic cholinergic receptor", "entity2": "atropine", "span1": [83, 114], "span2": [187, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11550": {"label": 8, "data": {"text": "BACKGROUND: Histamine synthesized by histidine decarboxylase (HDC) from L-histidine is a major chemical mediator in the development of nasal allergy which is characterized by nasal hypersensitivity.", "entity1": "HDC", "entity2": "L-histidine", "span1": [62, 65], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7429": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "Delta 6 desaturase", "entity2": "ALA", "span1": [11, 29], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10799": {"label": 8, "data": {"text": "The effects of simvastatin were abolished by the addition of the product of the HMG-CoA reductase, mevalonate, indicating the involvement of HMG-CoA reductase in the action of simvastatin.", "entity1": "HMG-CoA reductase", "entity2": "mevalonate", "span1": [80, 97], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14242": {"label": 2, "data": {"text": "Verrucarin A sensitizes TRAIL-induced apoptosis via the upregulation of DR5 in an eIF2\u03b1/CHOP-dependent manner.", "entity1": "CHOP", "entity2": "Verrucarin A", "span1": [88, 92], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4029": {"label": 3, "data": {"text": "We show that both darapladib and a novel class of structurally distinct carbamate inhibitors inactivate Lp-PLA(2) in mouse tissues and human cell lines with high selectivity.", "entity1": "Lp-PLA(2)", "entity2": "darapladib", "span1": [104, 113], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8406": {"label": 1, "data": {"text": "Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD.", "entity1": "FLT3", "entity2": "ponatinib", "span1": [91, 95], "span2": [12, 21]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7471": {"label": 2, "data": {"text": "Na+/Cl- dipole couples agonist binding to kainate receptor activation.", "entity1": "kainate receptor", "entity2": "Cl-", "span1": [42, 58], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7428": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "D6D", "entity2": "alpha-linolenic acid", "span1": [31, 34], "span2": [63, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15548": {"label": 2, "data": {"text": "DMN-induced cyclooxygenase-2 (COX-2) expression and nuclear factor-kappa B (NF-\u03baB) activation was reduced by CK treatment.", "entity1": "COX-2", "entity2": "DMN", "span1": [30, 35], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14726": {"label": 4, "data": {"text": "We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenine moiety.", "entity1": "TLR7", "entity2": "8-oxoadenines", "span1": [57, 61], "span2": [80, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10903": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "cyclin-dependent kinases", "entity2": "Seliciclib", "span1": [76, 100], "span2": [25, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1537": {"label": 5, "data": {"text": "The selective GluR5 kainate receptor agonist ATPA induces spontaneous epileptiform bursting that is sensitive to the GluR5 kainate receptor antagonist LY293558.", "entity1": "GluR5", "entity2": "LY293558", "span1": [117, 122], "span2": [151, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7097": {"label": 8, "data": {"text": "Proline oxidase (POX), a mitochondrial inner-membrane protein, catalyzes the rate-limiting oxidation of proline to pyrroline- 5-carboxylate (P5C).", "entity1": "POX", "entity2": "pyrroline- 5-carboxylate", "span1": [17, 20], "span2": [115, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15723": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b1", "entity2": "heptylparaben", "span1": [142, 145], "span2": [77, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9821": {"label": 5, "data": {"text": "Iontophoresis of +/- propranolol, whose serotonergic actions include antagonism and partial agonism at 5-HT1 receptors, also increased serotonin and decreased firing (n=4).", "entity1": "5-HT1", "entity2": "+/- propranolol", "span1": [103, 108], "span2": [17, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6064": {"label": 3, "data": {"text": "The mechanism by which norepinephrine (NE) down-regulates alpha 1B-adrenergic receptor (alpha-AR) mRNA was studied in rabbit aortic smooth muscle cells.", "entity1": "alpha-AR", "entity2": "norepinephrine", "span1": [88, 96], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10083": {"label": 8, "data": {"text": "The specific activity of only ornithine aminotransferase (OAT), the rate-limiting enzyme in the conversion of ornithine to proline, increased in 2 weeks of hypertrophy.", "entity1": "OAT", "entity2": "ornithine", "span1": [58, 61], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"2106": {"label": 5, "data": {"text": "The selective beta1AR antagonists atenolol and metoprolol blocked isoproterenol-induced enhancement, with apparent K(b) values of 85 +/- 36 and 3.9 +/- 1.7 nM, respectively.", "entity1": "beta1AR", "entity2": "metoprolol", "span1": [14, 21], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5379": {"label": 6, "data": {"text": "Rapamycin allosterically inhibits the proteasome.", "entity1": "proteasome", "entity2": "Rapamycin", "span1": [38, 48], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"4943": {"label": 3, "data": {"text": "Moreover, protein and mRNA levels of DSS-induced proinflammatory cytokines in colon, including TNF-\u03b1, IL-1\u03b2, IL-18, IL-17A and IFN-\u03b3, were markedly suppressed by Fc11a-2.", "entity1": "IFN-\u03b3", "entity2": "Fc11a-2", "span1": [127, 132], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15037": {"label": 1, "data": {"text": "It had higher levels of oleocanthal (p-HPEA-EDA), a nutraceutical compound exerting actions against COX1 and COX2 (cycloxygenases).", "entity1": "COX1", "entity2": "oleocanthal", "span1": [100, 104], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12646": {"label": 1, "data": {"text": "Salicylic acid promotes dissociation of (125)I-ET-1 ETA receptor complexes both in the absence and the presence of unlabeled ET-1.", "entity1": "ETA receptor", "entity2": "Salicylic acid", "span1": [52, 64], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9870": {"label": 3, "data": {"text": "In cultures from severely obese subjects, troglitazone induced a decrease of PAI-1 antigen secretion from newly differentiated omental adipocytes by 49 +/- 8% (p < 0.01) and from subcutaneous adipocytes by 30 +/- 7% (p < 0.05).", "entity1": "PAI-1", "entity2": "troglitazone", "span1": [77, 82], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4792": {"label": 8, "data": {"text": "Taken together, these data demonstrate that baicalin inhibits the metabolism of DXM in a concentration-dependent manner in rats, possibly through inhibiting hepatic CYP2D and CYP3A activities.", "entity1": "CYP2D", "entity2": "DXM", "span1": [165, 170], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"977": {"label": 3, "data": {"text": "Previously, we showed that the human kappa-opioid receptor (hkor) stably expressed in Chinese hamster ovary (CHO) cells underwent down-regulation after prolonged U50,488H treatment.", "entity1": "hkor", "entity2": "U50,488H", "span1": [60, 64], "span2": [162, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2440": {"label": 3, "data": {"text": "Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium.", "entity1": "cyclooxygenase", "entity2": "ketorolac tromethamine", "span1": [14, 28], "span2": [89, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13022": {"label": 8, "data": {"text": "Once formed, the molecule can be converted to glycine by alanine-glyoxylate aminotransferase (AGAT).", "entity1": "alanine-glyoxylate aminotransferase", "entity2": "glycine", "span1": [57, 92], "span2": [46, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"306": {"label": 4, "data": {"text": "2-(2-Aminoethyl)-quinoline (D-1997): a novel agonist at 5-hydroxytryptamine1-like receptors in the canine basilar artery.", "entity1": "5-hydroxytryptamine1-like receptors", "entity2": "D-1997", "span1": [56, 91], "span2": [28, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10325": {"label": 2, "data": {"text": "Resiquimod-stimulated pDC also produce a number of other cytokines including TNF-alpha and IP-10.", "entity1": "TNF-alpha", "entity2": "Resiquimod", "span1": [77, 86], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14937": {"label": 1, "data": {"text": "A novel potent compound, N-benzyl-5-(4-isopropylthiophenol)-2-hydroxyl nicotinamide (12c), which binds Mcl-1 with an IC(50) value of 54 nM was obtained.", "entity1": "Mcl-1", "entity2": "N-benzyl-5-(4-isopropylthiophenol)-2-hydroxyl nicotinamide", "span1": [103, 108], "span2": [25, 83]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12761": {"label": 1, "data": {"text": "Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography.", "entity1": "histamine H1-receptor", "entity2": "11C-doxepin", "span1": [121, 142], "span2": [159, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4690": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "V(5+)", "span1": [103, 109], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9581": {"label": 1, "data": {"text": "Both carbetocin, carbetocin metabolite I and carbetocin metabolite II displayed binding affinities to the myometrial oxytocin receptor of a similar magnitude as oxytocin.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [117, 134], "span2": [17, 27]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9880": {"label": 5, "data": {"text": "We examined the effect of JTH-601 (3- inverted question markN-[2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethyl]-N-methylaminom ethyl inverted question mark-4-methoxy-2,5,6-trimethylphenol hemifumarate), a new alpha(1L)-adrenoceptor antagonist, on prostatic function in isolated canine prostate and in anesthetized dogs.", "entity1": "alpha(1L)-adrenoceptor", "entity2": "ethyl", "span1": [208, 230], "span2": [126, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6148": {"label": 0, "data": {"text": "For example, it is clear that the closed conformation of the regulatory N-terminal domain in Ca2+-bound cardiac troponin C (cTnC) presents a much different binding surface for Ca2+-sensitizing compounds than previously thought.", "entity1": "cardiac troponin C", "entity2": "N", "span1": [104, 122], "span2": [72, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11660": {"label": 1, "data": {"text": "These results led us to consider that TAS-102 may also be effective for esophageal and uterine squamous cell carcinomas, as well as for gastrointestinal adenocarcinomas, even in fluoropyrimidine-resistant cases with high TS expression.", "entity1": "TS", "entity2": "fluoropyrimidine", "span1": [221, 223], "span2": [178, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10531": {"label": 3, "data": {"text": "Increases in glucose concentration from 0 to 3 and from 3 to 17 mM inhibited AMPK activity in primary islets from mouse, rat, and human, confirming previous findings in insulinoma cells.", "entity1": "AMPK", "entity2": "glucose", "span1": [77, 81], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7216": {"label": 2, "data": {"text": "Cd rapidly increased c-jun, c-fos and PDGFA expression.", "entity1": "c-jun", "entity2": "Cd", "span1": [21, 26], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11772": {"label": 1, "data": {"text": "Recent studies indicate that Pin1 is an important molecular target for the chemopreventive effects of green tea polyphenols.", "entity1": "Pin1", "entity2": "polyphenols", "span1": [29, 33], "span2": [112, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3779": {"label": 5, "data": {"text": "Both 5'-AMN and 5'-MABN had high affinity for \u03ba-receptors (K (i) 1.36 \u00b1 0.98 and 0.27 \u00b1 0.08, respectively) and were revealed as potent \u03ba-antagonists (pA(2) 7.43 and 8.18, respectively) and \u03bc-receptor antagonists (pA(2) 7.62 and 7.85, respectively) in the ileum.", "entity1": "\u03bc-receptor", "entity2": "5'-MABN", "span1": [190, 200], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13152": {"label": 0, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "Fas-associated death domain-containing protein", "entity2": "serine", "span1": [56, 102], "span2": [117, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3289": {"label": 1, "data": {"text": "We have investigated in normal human male subjects the importance, site of action, and receptor-mediated processes involved in rapid basal corticosteroid feedback and its interaction with corticotrophin releasing hormone (CRH) drive.", "entity1": "CRH", "entity2": "corticosteroid", "span1": [222, 225], "span2": [139, 153]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15613": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "caspase-1", "entity2": "galangin", "span1": [179, 188], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"816": {"label": 1, "data": {"text": "The prostaglandin E series modulates high-voltage-activated calcium channels probably through the EP3 receptor in rat paratracheal ganglia.", "entity1": "EP3 receptor", "entity2": "prostaglandin E", "span1": [98, 110], "span2": [4, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10497": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "ICI 118551", "span1": [392, 423], "span2": [355, 365]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10454": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "EC 4.3.1.17", "entity2": "ammonia", "span1": [27, 38], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11928": {"label": 1, "data": {"text": "This paper aims to review briefly the literature on the 5-HT hypothesis of depression with a major focus on the possible role of SERT in this disorder, while highlighting how recent data are more oriented on dimensional rather than nosological involvement of this structure in different conditions spanning from normality to pathology.", "entity1": "SERT", "entity2": "5-HT", "span1": [129, 133], "span2": [56, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8443": {"label": 5, "data": {"text": "Assessment of the abuse liability of ABT-288, a novel histamine H3 receptor antagonist.", "entity1": "histamine H3 receptor", "entity2": "ABT-288", "span1": [54, 75], "span2": [37, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6834": {"label": 9, "data": {"text": "In addition, both drugs significantly reduced PGE2 levels (P<0.05) 6-h following LPS injection, whereas the probable COX-1 prostanoid TXB2 was significantly reduced by phenylbutazone (P<0.05), but not etodolac.", "entity1": "COX-1", "entity2": "etodolac", "span1": [117, 122], "span2": [201, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4680": {"label": 2, "data": {"text": "High-glucose environment enhanced oxidative stress and increased interleukin-8 secretion from keratinocytes: New insights on impaired diabetic wound healing.", "entity1": "interleukin-8", "entity2": "glucose", "span1": [65, 78], "span2": [5, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10371": {"label": 3, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "BrBK1-7", "entity2": "omapatrilat", "span1": [70, 77], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4418": {"label": 3, "data": {"text": "We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies.", "entity1": "Syk", "entity2": "pyrrolopyrazines", "span1": [78, 81], "span2": [37, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15908": {"label": 1, "data": {"text": "Therefore, in addition to its previously described functions, synaptotagmin-1 is involved in a rapid vesicular Ca(2+) sequestration through a Ca(2+) /H(+) antiport.", "entity1": "synaptotagmin-1", "entity2": "H(+)", "span1": [62, 77], "span2": [150, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"54": {"label": 3, "data": {"text": "Clinical pharmacology of enalkiren, a novel, dipeptide renin inhibitor.", "entity1": "renin", "entity2": "dipeptide", "span1": [55, 60], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8326": {"label": 2, "data": {"text": "In particular, we showed that Paeoniflorin significantly reduced the formation of intracellular reactive oxygen species (ROS), the level of malondialdehyde (MDA) and lactate dehydrogenase (LDH) leakage, and enhanced production of the endogenous antioxidants, glutathione (GSH) and superoxide dismutase (SOD) in EA.hy926 cells.", "entity1": "SOD", "entity2": "Paeoniflorin", "span1": [303, 306], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3598": {"label": 1, "data": {"text": "Interestingly, recent crystallographic evidence identified that ifenprodil, unlike zinc, binds at the interface of the GluN1/GluN2B amino terminal domain dimer by an induced-fit mechanism.", "entity1": "GluN1", "entity2": "ifenprodil,", "span1": [119, 124], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9028": {"label": 9, "data": {"text": "Alprenolol treatment (4 X 100 mg/day) led to a rapid fall in PRA, but did not significantly affect beta 2-adrenoceptor density.", "entity1": "beta 2-adrenoceptor", "entity2": "Alprenolol", "span1": [99, 118], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12181": {"label": 3, "data": {"text": "Hepatic mRNA expressions of apo B-100 and apo C-III were significantly lower in probucol group than in other groups.", "entity1": "apo C-III", "entity2": "probucol", "span1": [42, 51], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"186": {"label": 1, "data": {"text": "However, due to the very high affinity of CBG for corticosterone at 4 C, this slight contamination resulted in significant alterations in the apparent affinity of steroids competing for aldosterone-binding sites.", "entity1": "CBG", "entity2": "corticosterone", "span1": [42, 45], "span2": [50, 64]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6950": {"label": 3, "data": {"text": "Hepatic ACAT activity was significantly lower in both vitamin E and probucol groups than in HC-control group, while HMG-CoA reductase activity was the highest only in the probucol group.", "entity1": "ACAT", "entity2": "vitamin E", "span1": [8, 12], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14240": {"label": 2, "data": {"text": "Verrucarin A sensitizes TRAIL-induced apoptosis via the upregulation of DR5 in an eIF2\u03b1/CHOP-dependent manner.", "entity1": "DR5", "entity2": "Verrucarin A", "span1": [72, 75], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4935": {"label": 3, "data": {"text": "The mechanism of action of Fc11a-2 was related to the inhibition of the cleavage of pro-caspase-1, pro-IL-1\u03b2 and pro-IL-18 which in turn suppressed the activation of NLRP3 inflammasome.", "entity1": "pro-caspase-1", "entity2": "Fc11a-2", "span1": [84, 97], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12890": {"label": 1, "data": {"text": "Here, we show that at noncytotoxic concentrations, H(2)S was able to inhibit NO production and inducible NO synthase (iNOS) expression via heme oxygenase (HO-1) expression in RAW264.7 macrophages stimulated with lipopolysaccharide (LPS).", "entity1": "HO-1", "entity2": "H(2)S", "span1": [155, 159], "span2": [51, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12293": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Pon1", "entity2": "Quercetin", "span1": [113, 117], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6110": {"label": 5, "data": {"text": "In extending these initial findings, we have shown that cardiac fibrosis (i) is not reversed by correction of mineralocorticoid-induced hypokalemia; (ii) appears not to involve the plasma or tissue renin-angiotensin systems, as fibrosis is largely unaffected by concurrent administration of Losartan or Perindopril; (iii) is independent of cardiac hypertrophy, in that it is equally seen in right and left ventricles, and in rats rendered hypertensive without cardiac hypertrophy by the administration of 9 alpha-fluorocortisol; (iv) is independent of elevated blood pressure, in that it is found in normotensive animals infused peripherally with aldosterone and intracerebroventricularly with the mineralocorticoid receptor (MR) antagonist RU28318; (v) is via classical MR, in that it is blocked by concurrent administration of the MR antagonist potassium canrenoate; and (vi) may or may not be a direct cardiac effect, inasmuch as data for in vivo effects on collagen formation by cardiac fibroblasts are conflicting.", "entity1": "MR", "entity2": "potassium canrenoate", "span1": [833, 835], "span2": [847, 867]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14313": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "glutathione S-transferase", "entity2": "DMF", "span1": [114, 139], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"503": {"label": 3, "data": {"text": "The results suggest that the 63-kDa (PDE 1B1) and 60-kDa (PDE 1A2) CaMPDE isozymes are inhibited by felodipine and nicardipine by partial competitive inhibition and that these two Ca2+ antagonists appear to counteract each other.", "entity1": "PDE 1B1", "entity2": "felodipine", "span1": [37, 44], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4842": {"label": 2, "data": {"text": "Subsequent analysis revealed that cucurbitacin I strongly activates RhoA and the Rho effector Rho kinase (ROCK) in breast cancer cells and induces the formation of stress fibers.", "entity1": "RhoA", "entity2": "cucurbitacin I", "span1": [68, 72], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12020": {"label": 1, "data": {"text": "Using electrophysiologic techniques, the present study assessed the in vivo action of brexpiprazole on serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, and 5-HT2A; dopamine (DA) D2 autoreceptors, and alpha1- and alpha2-adrenergic receptors.", "entity1": "5-HT1A", "entity2": "brexpiprazole", "span1": [138, 144], "span2": [86, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8906": {"label": 2, "data": {"text": "Abrupt removal of amrinone or pentoxifylline from the culture medium prior to LPS stimulation, however, caused significantly augmented TNF production.", "entity1": "TNF", "entity2": "amrinone", "span1": [135, 138], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10230": {"label": 3, "data": {"text": "Moreover, thalidomide reduced the LPS-induced TNF-alpha production by KCs by decreasing TNF-alpha messenger RNA.", "entity1": "TNF-alpha", "entity2": "thalidomide", "span1": [88, 97], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8682": {"label": 3, "data": {"text": "Recently, the c-Abl kinase inhibitor imatinib mesylate (imatinib) has become the focus of research as a fertoprotective drug against cisplatin.", "entity1": "c-Abl", "entity2": "imatinib mesylate", "span1": [14, 19], "span2": [37, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6066": {"label": 3, "data": {"text": "The mechanism by which norepinephrine (NE) down-regulates alpha 1B-adrenergic receptor (alpha-AR) mRNA was studied in rabbit aortic smooth muscle cells.", "entity1": "alpha-AR", "entity2": "NE", "span1": [88, 96], "span2": [39, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14467": {"label": 1, "data": {"text": "Seven point mutations were introduced into the conserved motif in the second extracellular loop (ECII) of EP3, resulting in acquisition of GTP-sensitive agonist binding.", "entity1": "second extracellular loop", "entity2": "GTP", "span1": [70, 95], "span2": [139, 142]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12216": {"label": 1, "data": {"text": "This mechanism involves the calcium-dependent tyrosine kinase Pyk2, the non-receptor tyrosine kinase c-Src and the focal adhesion protein/steroid receptor co-factor, Hic-5.", "entity1": "non-receptor tyrosine kinase", "entity2": "calcium", "span1": [72, 100], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1842": {"label": 3, "data": {"text": "Here, we show that one BLT, [1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea] (BLT-4), blocked ABCA1-mediated cholesterol efflux to lipid-poor apoA-I at a potency similar to that for its inhibition of SR-BI (IC(50) approximately 55-60 microM).", "entity1": "ABCA1", "entity2": "1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea", "span1": [91, 96], "span2": [29, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12440": {"label": 6, "data": {"text": "This Letter describes the further chemical optimization of the M5 PAM MLPCN probes ML129 and ML172.", "entity1": "M5", "entity2": "ML172", "span1": [63, 65], "span2": [93, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10724": {"label": 1, "data": {"text": "We have analyzed binding domains of the oxytocin receptor for barusiban, a highly selective oxytocin receptor antagonist, in comparison to the combined vasopressin V1A/oxytocin receptor antagonist atosiban and the agonists oxytocin and carbetocin.", "entity1": "oxytocin receptor", "entity2": "barusiban", "span1": [40, 57], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9012": {"label": 1, "data": {"text": "The limitation of SRF by diazepam was not prevented by inverse or partial agonists at the BDZ receptor, including Ro 15-1788 and the beta CCs.", "entity1": "BDZ receptor", "entity2": "diazepam", "span1": [90, 102], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8628": {"label": 2, "data": {"text": "Arsenic inhibits autophagic flux activating the Nrf2-Keap1 pathway in a p62-dependent manner.", "entity1": "Nrf2", "entity2": "Arsenic", "span1": [48, 52], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8235": {"label": 4, "data": {"text": "ICA is a mixed agonist of mutant EAG and EAG/ERG chimera channels that inactivate by a combination of slow and fast mechanisms.", "entity1": "EAG", "entity2": "ICA", "span1": [41, 44], "span2": [0, 3]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5905": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "low-density lipoproteins", "entity2": "nicotinic acid", "span1": [146, 170], "span2": [32, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3151": {"label": 4, "data": {"text": "Thus, amitriptyline acts as a TrkA and TrkB agonist and possesses marked neurotrophic activity.", "entity1": "TrkB", "entity2": "amitriptyline", "span1": [39, 43], "span2": [6, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1707": {"label": 8, "data": {"text": "At normal pH (7.4) and temperature (37 degrees C), the uptake of 1 microM cefadroxil was reduced by 83% in PEPT2(-/-) mice as compared with PEPT2(+/+) mice (p < 0.001).", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [140, 145], "span2": [74, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1442": {"label": 1, "data": {"text": "We investigated the mechanism of action of atomoxetine in ADHD by evaluating the interaction of atomoxetine with monoamine transporters, the effects on extracellular levels of monoamines, and the expression of the neuronal activity marker Fos in brain regions.", "entity1": "monoamine transporters", "entity2": "atomoxetine", "span1": [113, 135], "span2": [96, 107]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15476": {"label": 2, "data": {"text": "Upon nicotine pre-exposure, brain acetylcholinesterase increased, while monoamine oxidase (MAO) decreased.", "entity1": "acetylcholinesterase", "entity2": "nicotine", "span1": [34, 54], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15577": {"label": 1, "data": {"text": "Our results revealed an important role of base excision repair (BER) as the ntg1, ntg2, apn1 and apn2 mutants showed pronounced sensitivity to essential oil and nerolidol.", "entity1": "apn2", "entity2": "nerolidol", "span1": [97, 101], "span2": [161, 170]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10947": {"label": 3, "data": {"text": "This process was reduced by a protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, and a typical monocarboxylate transporter (MCT) inhibitor, alpha-cyano-4-hydroxycinnamic acid, suggesting that nicotinate uptake by rat astrocytes is mediated by H(+)-coupled monocarboxylate transport system.", "entity1": "MCT", "entity2": "alpha-cyano-4-hydroxycinnamic acid", "span1": [138, 141], "span2": [154, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"326": {"label": 1, "data": {"text": "Folding pathway of guanidine-denatured disulfide-intact wild-type and mutant bovine pancreatic ribonuclease A.", "entity1": "bovine pancreatic ribonuclease A", "entity2": "disulfide", "span1": [77, 109], "span2": [39, 48]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11838": {"label": 1, "data": {"text": "There was a significant overlap (42 genes) between the 3 and 30 ppb differentially expressed gene lists, with two of these genes (CYP17A1 and SAMHD1) present in all three atrazine treatments.", "entity1": "SAMHD1", "entity2": "atrazine", "span1": [142, 148], "span2": [171, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10312": {"label": 5, "data": {"text": "Yohimbine is a potent and selective alpha2- versus alpha1-adrenoceptor antagonist.", "entity1": "alpha2- versus alpha1-adrenoceptor", "entity2": "Yohimbine", "span1": [36, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3201": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "caffeic acid", "span1": [262, 280], "span2": [104, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7109": {"label": 1, "data": {"text": "Tamoxifen blocks the action of estrogen by binding to the ER, and possesses both ER-agonist and antagonist properties.", "entity1": "ER", "entity2": "Tamoxifen", "span1": [58, 60], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12271": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(2)", "entity2": "vasopressin", "span1": [173, 177], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2250": {"label": 8, "data": {"text": "BACKGROUND: Since the introduction of the first cholinesterase inhibitor (ChEI) in 1997, most clinicians and probably most patients would consider the cholinergic drugs, donepezil, galantamine and rivastigmine, to be the first line pharmacotherapy for mild to moderate Alzheimer's disease.The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [492, 512], "span2": [400, 413]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2461": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "MRP2", "entity2": "paclitaxel", "span1": [69, 73], "span2": [161, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9251": {"label": 1, "data": {"text": "Ergovaline binding and activation of D2 dopamine receptors in GH4ZR7 cells.", "entity1": "D2 dopamine receptors", "entity2": "Ergovaline", "span1": [37, 58], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3290": {"label": 3, "data": {"text": "Prednisolone also inhibited ACTH and cortisol secretion in response to exogenous CRH stimulation, inferring rapid feedback inhibition at the anterior pituitary.", "entity1": "CRH", "entity2": "Prednisolone", "span1": [81, 84], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15804": {"label": 2, "data": {"text": "When dual angiogenic growth factors (GFs), such as platelet-derived GF (PDGF) and vascular endothelial GF (VEGF), are encapsulated separately in the core and shell domains, respectively, the VEGF release rate is much greater than that of PDGF, and the difference of the cumulative release percentage between the two GFs is about 30% on day 7 with LMW core PLGA and more than 45% with HMW core PLGA.", "entity1": "PDGF", "entity2": "PLGA", "span1": [238, 242], "span2": [356, 360]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"920": {"label": 5, "data": {"text": "Comparison of all the beta-adrenoceptor antagonists tested revealed a potency order of propranolol>betaxolol approximately levobetaxolol>levobunolol approximately carteolol>/=timolol>atenolol.", "entity1": "beta-adrenoceptor", "entity2": "levobunolol", "span1": [22, 39], "span2": [137, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14752": {"label": 3, "data": {"text": "In addition, we found that arsenic trioxide decreases the stability of \u0394Np63 protein via a proteasome-dependent pathway but has little effect on the level of \u0394Np63 transcript.", "entity1": "\u0394Np63", "entity2": "arsenic trioxide", "span1": [71, 76], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2312": {"label": 3, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "beta-catenin", "entity2": "YC-1", "span1": [167, 179], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6976": {"label": 2, "data": {"text": "Its special profile of actions, especially the rise in HDL-cholesterol levels induced by nicotinic acid, is unique among the currently available pharmacological tools to treat lipid disorders.", "entity1": "HDL", "entity2": "nicotinic acid", "span1": [55, 58], "span2": [89, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2268": {"label": 8, "data": {"text": "Astrocytes may play a role in these manifestations because astrocytes are essential in the regulation of released glutamate and its conversion to glutamine through the enzyme glutamine synthetase (GS).", "entity1": "glutamine synthetase", "entity2": "glutamine", "span1": [175, 195], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14318": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "ARE", "entity2": "DMF", "span1": [293, 296], "span2": [335, 338]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"263": {"label": 0, "data": {"text": "Cyclodiene resistance in D. melanogaster has been attributed to a mutation resulting in an Ala302-->Ser replacement in the Rdl GABA receptor subunit and in D. simulans to an homologous Ala-->Ser or Gly replacement.", "entity1": "Rdl GABA receptor", "entity2": "Ser", "span1": [123, 140], "span2": [100, 103]}, "weak_labels": [-1, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10832": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "KIT", "entity2": "Imatinib", "span1": [105, 108], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4977": {"label": 2, "data": {"text": "RESULTS: DZN induced histophatological damages and elevated the level of cardiac marker CK-MB.", "entity1": "CK-MB", "entity2": "DZN", "span1": [88, 93], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7646": {"label": 3, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "Panx1", "entity2": "Triphosphate nucleotides", "span1": [78, 83], "span2": [0, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7335": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SLC38", "entity2": "glutamine", "span1": [258, 263], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11435": {"label": 3, "data": {"text": "Experimental as well as clinical reports support the hypothesis that calcium channel blockers such as verapamil may be an appropriate therapeutic approach in LQTS.", "entity1": "calcium channel", "entity2": "verapamil", "span1": [69, 84], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11111": {"label": 1, "data": {"text": "Two migraine patients were studied by in vivo SPECT using the dopamine D2-receptor specific radioligand 123I-3-iodo-6-methoxybenzamide (123I-IBZM) during ergotamine abuse and after withdrawal.", "entity1": "dopamine D2-receptor", "entity2": "ergotamine", "span1": [62, 82], "span2": [154, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11401": {"label": 1, "data": {"text": "Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties.", "entity1": "KCNQ2/Q3", "entity2": "diclofenac", "span1": [53, 61], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14259": {"label": 8, "data": {"text": "By contrast, 1,12-diamino-3,6,9-triazadodecane(SpmTrien), a charge-deficient spermine analog, was an extremely poor substrate of human recombinant SSAT2 and was metabolized by SSAT1 in HEPG2 cells and in wild-type primary hepatocytes.", "entity1": "SSAT1", "entity2": "1,12-diamino-3,6,9-triazadodecane", "span1": [176, 181], "span2": [13, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11688": {"label": 8, "data": {"text": "Stable ABCC1, ABCC2 and ABCC3 knockdown cell lines were generated, thus making it possible to demonstrate that ABCC1 mediates the basolateral and ABCC2 the apical excretion of BPDE glutathione conjugates.", "entity1": "ABCC2", "entity2": "BPDE glutathione", "span1": [14, 19], "span2": [176, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14302": {"label": 8, "data": {"text": "Human serum butyrylcholinesterase (HuBChE) is currently the most suitable bioscavenger for the prophylaxis of highly toxic organophosphate (OP) nerve agents.", "entity1": "HuBChE", "entity2": "organophosphate", "span1": [35, 41], "span2": [123, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8025": {"label": 1, "data": {"text": "On the contrary, human TRPA1 could be concentration-dependently modulated by apomorphine.", "entity1": "human TRPA1", "entity2": "apomorphine", "span1": [17, 28], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8053": {"label": 2, "data": {"text": "Furthermore, metformin was able to not only decrease the paclitaxel-induced p38 MAPK-mediated ERCC1 expression, but also augment the cytotoxic effect induced by paclitaxel.", "entity1": "MAPK", "entity2": "paclitaxel", "span1": [80, 84], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3425": {"label": 1, "data": {"text": "The G719S/T790M double mutant has enhanced activity and retains high gefitinib-binding affinity.", "entity1": "G719S", "entity2": "gefitinib", "span1": [4, 9], "span2": [69, 78]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11293": {"label": 8, "data": {"text": "BACKGROUND & AIMS: Of the 2 genes (MAT1A, MAT2A) encoding methionine adenosyltransferase, the enzyme that synthesizes S-adenosylmethionine, MAT1A, is expressed in liver, whereas MAT2A is expressed in extrahepatic tissues.", "entity1": "MAT1A", "entity2": "S-adenosylmethionine", "span1": [140, 145], "span2": [118, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10674": {"label": 3, "data": {"text": "In Experiment 2, TT-235 induced a significant decrease (p<0.05) in oxytocin receptor number and binding affinity at both 0.5 and 4 hours compared with controls.", "entity1": "oxytocin receptor", "entity2": "TT-235", "span1": [67, 84], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7489": {"label": 3, "data": {"text": "Phenserine is also unique because of differing actions of its enantiomers: (-)-phenserine is the active enantiomer for inhibition of AChE, whereas (+)-phenserine ('posiphen') has weak activity as an AChE inhibitor and can be dosed much higher.", "entity1": "AChE", "entity2": "(-)-phenserine", "span1": [133, 137], "span2": [75, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1265": {"label": 2, "data": {"text": "CONCLUSIONS: CysLTs produced after antigen provocation sequentially induced IL-5 production from some immune component cells via CysLT1 receptor activation.", "entity1": "CysLT1", "entity2": "CysLTs", "span1": [129, 135], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12332": {"label": 1, "data": {"text": "However, recent evidence suggests that the action of FTY720 involves S1PRs expressed by cells resident in the CNS, including neurons.", "entity1": "S1PRs", "entity2": "FTY720", "span1": [69, 74], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2928": {"label": 5, "data": {"text": "Conivaptan is a nonpeptide dual V1a/V2 AVP receptor antagonist.", "entity1": "V1a/V2 AVP receptor", "entity2": "Conivaptan", "span1": [32, 51], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5995": {"label": 3, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "t-PA", "entity2": "Cl-", "span1": [121, 125], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10684": {"label": 9, "data": {"text": "In cellular assays, lumiracoxib had an IC(50) of 0.14 microM in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 microM (HEK 293 cells transfected with human COX-1).", "entity1": "COX-1", "entity2": "lumiracoxib", "span1": [129, 134], "span2": [20, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8423": {"label": 8, "data": {"text": "Furthermore, knockdown of OPN enhanced cell death caused by other drugs, including paclitaxel, doxorubicin, actinomycin-D, and rapamycin, which are also P-gp substrates.", "entity1": "P-gp", "entity2": "doxorubicin", "span1": [153, 157], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10139": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "rofecoxib", "span1": [34, 37], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6037": {"label": 1, "data": {"text": "We conclude that despite small differences concerning the enantiomeric selectivity and affinity of rauwolscine and yohimbine, the close pharmacological identity of 5-HT receptors in rat stomach fundus and the recently cloned 5-HT2B receptor is maintained.", "entity1": "5-HT receptors", "entity2": "yohimbine", "span1": [164, 178], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14619": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ile24Val", "entity2": "2',2'-difluorodeoxyuridine", "span1": [71, 79], "span2": [255, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9597": {"label": 3, "data": {"text": "Here we present the crystal structure of the dimeric catalytic domain (residues 117-424) of human phenylalanine hydroxylase (hPheOH), cocrystallized with various potent and well-known catechol inhibitors and refined at a resolution of 2.0 A.", "entity1": "human phenylalanine hydroxylase", "entity2": "catechol", "span1": [92, 123], "span2": [184, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3169": {"label": 1, "data": {"text": "A VLA-4 containing membrane preparation of MV3 cells was immobilised at the sensors to allow for detection of kinetic binding constants of tinzaparin compared to VCAM-1.", "entity1": "VLA-4", "entity2": "tinzaparin", "span1": [2, 7], "span2": [139, 149]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10152": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "ER", "entity2": "estrogen", "span1": [129, 131], "span2": [83, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9332": {"label": 1, "data": {"text": "Ligand binding studies with the recombinant EAA3a receptor expressed in mammalian cells indicated a high affinity kainate binding site (Kd = 120 +/- 15.0 nM).", "entity1": "EAA3a", "entity2": "kainate", "span1": [44, 49], "span2": [114, 121]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9609": {"label": 1, "data": {"text": "The KATP channel is a heterooligomeric complex of SUR1 subunits of the ATP-binding-cassette superfamily with two nucleotide-binding folds (NBF1 and NBF2) and the pore-forming Kir6.2 subunits.", "entity1": "NBF2", "entity2": "ATP", "span1": [148, 152], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"688": {"label": 3, "data": {"text": "We topically applied the nitric oxide synthase (NOS) inhibitor, NG-nitro-L-arginine, on sciatic nerve and observed reduced inhibition of NBF in EDN, which was correctable with a cilazapril diet.", "entity1": "nitric oxide synthase", "entity2": "NG-nitro-L-arginine", "span1": [25, 46], "span2": [64, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12257": {"label": 8, "data": {"text": "However, GlyT2 was more effective than GlyT1, probably because GlyT2 is unable to operate in the reverse mode, which gives it an advantage in maintaining the high cytosolic glycine concentration required for efficient vesicular loading by VIAAT.", "entity1": "VIAAT", "entity2": "glycine", "span1": [239, 244], "span2": [173, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2148": {"label": 3, "data": {"text": "Pharmacologically, troglitazone is a novel inhibitor of ENT1.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [56, 60], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9992": {"label": 9, "data": {"text": "Fibroblast cultures from the patient exhibited severe reduction of the rotenone-sensitive NADH-->UQ oxidoreductase activity of complex I, which was insensitive to cAMP stimulation.", "entity1": "complex I", "entity2": "cAMP", "span1": [127, 136], "span2": [163, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7709": {"label": 3, "data": {"text": "The mechanism of OP poisoning involves inhibition of acetylcholinesterase (AChE) leading to inactivation of the enzyme which has an important role in neurotransmission.", "entity1": "AChE", "entity2": "OP", "span1": [75, 79], "span2": [17, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6548": {"label": 0, "data": {"text": "To identify amino acid residues involved in PDE3-selective inhibitor binding, we selected eight presumed interacting residues in the substrate-binding pocket of PDE3A using a model created on basis of homology to the PDE4B crystal structure.", "entity1": "PDE3A", "entity2": "amino acid", "span1": [161, 166], "span2": [12, 22]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9203": {"label": 1, "data": {"text": "Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides.", "entity1": "alpha 2-macroglobulin", "entity2": "naphthalene sulfonamides", "span1": [8, 29], "span2": [104, 128]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1679": {"label": 5, "data": {"text": "Inhibition of binding of the alpha2-receptor antagonist [3H]RX821002 to recombinant alpha2-receptors by etomidate was tested in human embryonic kidney (HEK293) cells in vitro.", "entity1": "alpha2-receptors", "entity2": "[3H]RX821002", "span1": [84, 100], "span2": [56, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15161": {"label": 2, "data": {"text": "Correlating with FSH\u03b2 activation, both PKA activity and levels of pCREB were increased to a greater extent by low compared with high GnRH pulse frequencies, and the induction of pCREB was also attenuated by overexpression of DNPKA at both low and high pulse frequencies.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [17, 21], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3206": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "ferulic acid", "span1": [248, 261], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10741": {"label": 3, "data": {"text": "The compounds 5'-azacytidine (AZC) and procainamide (PCA) belong to inhibitors of DNMT1, whose low activity correlates with increase in transcription of various genes.", "entity1": "DNMT1", "entity2": "AZC", "span1": [82, 87], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3144": {"label": 1, "data": {"text": "Truncation of amitriptyline binding motif on TrkA abrogates the receptor dimerization by amitriptyline.", "entity1": "TrkA", "entity2": "amitriptyline", "span1": [45, 49], "span2": [14, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"880": {"label": 5, "data": {"text": "In the present study, we compared the pharmacology of (+/-)pindolol, WAY-100635 (a 5-HT(1A) antagonist), GR127935 (a 5-HT(1B/1D) antagonist), and isamoltane (a 5-HT(1B) antagonist), when given acutely in combination with fluoxetine, using in vivo microdialysis in the frontal cortex of the freely moving rat.", "entity1": "5-HT(1A)", "entity2": "(+/-)pindolol", "span1": [83, 91], "span2": [54, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5678": {"label": 3, "data": {"text": "We demonstrate that HZ mice are significantly more sensitive to local AChE inhibition (BW284c51), but remain insensitive to butyrylcholinesterase (BuChE) inhibition (bambuterol).", "entity1": "AChE", "entity2": "BW284c51", "span1": [70, 74], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8667": {"label": 2, "data": {"text": "We found that, before apoptosis, cisplatin induces c-Abl and TAp73 expression in the oocyte.", "entity1": "TAp73", "entity2": "cisplatin", "span1": [61, 66], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9891": {"label": 1, "data": {"text": "A similar discrepancy in sensitivity to competitors between 3H-NMPB and 3H-QNB was also observed when biperiden was used as a competitor, indicating that binding to different subtypes of the mAch receptor could not account for the observed differences in sensitivity to competition.", "entity1": "mAch receptor", "entity2": "3H-QNB", "span1": [191, 204], "span2": [72, 78]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4953": {"label": 3, "data": {"text": "Fisetin treatment inhibited adipocyte differentiation, consistent with the negative effect of fisetin on mTOR.", "entity1": "mTOR", "entity2": "fisetin", "span1": [105, 109], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4105": {"label": 1, "data": {"text": "In this study, we investigated SFO-induced atherosclerotic plaque vulnerability (possibility of rupture) in apolipoprotein E-knockout (apoE(-/-)) mice.", "entity1": "apoE", "entity2": "SFO", "span1": [135, 139], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3222": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "quercetin", "span1": [248, 261], "span2": [160, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7015": {"label": 3, "data": {"text": "Sorafenib has the added advantage of inhibiting multiple different Raf isoforms, which enables it to target TGF-alpha/EGFR signaling and may also enhance its inhibition of VEGFR and PDGFR-beta.", "entity1": "VEGFR", "entity2": "Sorafenib", "span1": [172, 177], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8913": {"label": 3, "data": {"text": "Monoclonal antibody 25B1 generated against diisopropyl phosphorofluoridate inhibited fetal bovine serum acetylcholinesterase has been extensively characterized with respect to its anticholinesterase properties.", "entity1": "bovine serum acetylcholinesterase", "entity2": "diisopropyl phosphorofluoridate", "span1": [91, 124], "span2": [43, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12": {"label": 1, "data": {"text": "An orally active analogue, cicaprost, was equally effective against endotoxin-induced tissue factor expression.", "entity1": "tissue factor", "entity2": "cicaprost", "span1": [86, 99], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8691": {"label": 8, "data": {"text": "These results suggest that ZIP8 plays a pivotal role in the transport and toxicity of Cd(2+) and Mn(2+) in RBL-2H3 cells.", "entity1": "ZIP8", "entity2": "Cd(2+)", "span1": [27, 31], "span2": [86, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"16029": {"label": 2, "data": {"text": "These results show that haloperidol promotes mTORC1- and S6K1-dependent phosphorylation of rpS6 at Ser240/244, in a subpopulation of striatal MSNs expressing D2Rs.", "entity1": "rpS6", "entity2": "haloperidol", "span1": [91, 95], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13703": {"label": 1, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.4", "entity2": "4-chloropropofol", "span1": [150, 158], "span2": [130, 146]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11547": {"label": 8, "data": {"text": "BACKGROUND: Histamine synthesized by histidine decarboxylase (HDC) from L-histidine is a major chemical mediator in the development of nasal allergy which is characterized by nasal hypersensitivity.", "entity1": "histidine decarboxylase", "entity2": "Histamine", "span1": [37, 60], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14152": {"label": 3, "data": {"text": "The agonist activity was antagonized by the selective kappa-opioid blocker nor-binaltorphimine (nor-BNI).", "entity1": "kappa-opioid", "entity2": "nor-BNI", "span1": [54, 66], "span2": [96, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12818": {"label": 3, "data": {"text": "Treatment with carvedilol is associated with a reversal of abnormal regulation of HIF-1alpha, VEGF, BNP, and NGF-beta in the hypertrophic myocardium.", "entity1": "BNP", "entity2": "carvedilol", "span1": [100, 103], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9574": {"label": 4, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "betaAR", "entity2": "isoproterenol", "span1": [116, 122], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4954": {"label": 3, "data": {"text": "Collectively, these results suggest that inhibition of mTORC1 signaling by fisetin prevents adipocyte differentiation of 3T3-L1 preadipocytes and obesity in HFD-fed mice.", "entity1": "mTORC1", "entity2": "fisetin", "span1": [55, 61], "span2": [75, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5080": {"label": 2, "data": {"text": "In addition to CYP2B6, anisomycin co-treatment potentiated an increase in CYP2A7 and CYP2C9 mRNAs but not CYP3A4 or UDP-glucuronosyltransferase 1A1 mRNAs.", "entity1": "CYP2C9", "entity2": "anisomycin", "span1": [85, 91], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7592": {"label": 3, "data": {"text": "The principal aim of the study was to find amiodarone analogues that retained human ether-a-go-go-related protein (hERG) channel inhibition but with reduced cytotoxicity.", "entity1": "human ether-a-go-go-related protein (hERG) channel", "entity2": "amiodarone", "span1": [78, 128], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7048": {"label": 3, "data": {"text": "RESULTS: Imatinib inhibited RET Y1062 phosphorylation in a dose-dependent manner after 1.5 hours of exposure.", "entity1": "RET", "entity2": "Imatinib", "span1": [28, 31], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8232": {"label": 2, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "potassium channels", "entity2": "ICA-105574", "span1": [113, 131], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12031": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "EO", "entity2": "hypoiodite", "span1": [75, 77], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12606": {"label": 0, "data": {"text": "Thus, PHBP was a heterodimer composed of 50-kDa and 17-kDa subunits, bridged by a disulfide linkage.", "entity1": "PHBP", "entity2": "disulfide", "span1": [6, 10], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9397": {"label": 0, "data": {"text": "In Drosophila, glutamyl-prolyl-tRNA synthetase is a multifunctional synthetase encoded by a unique gene and composed of three domains: the amino- and carboxy-terminal domains catalyze the aminoacylation of glutamic acid and proline tRNA species, respectively, and the central domain is made of 75 amino acids repeated six times amongst which 46 are highly conserved and constitute the repeated motifs [Cerini, C., Kerjan, P., Astier, M., Gratecos, D., Mirande, M. & Semeriva, M. (1991) EMBO J.", "entity1": "glutamyl-prolyl-tRNA synthetase", "entity2": "amino", "span1": [15, 46], "span2": [139, 144]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5689": {"label": 5, "data": {"text": "In a neuronal cell line, we found that selective CB(2) receptor agonists upregulate \u03b2-Arrestin 2, an effect that was prevented by selective CB(2) receptor antagonist JTE-907 and CB(2) shRNA lentiviral particles.", "entity1": "CB(2)", "entity2": "JTE-907", "span1": [140, 145], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"370": {"label": 3, "data": {"text": "GCS therapy results in reduced mRNA expression of interleukin-4 (IL-4) and IL-5 in cells from bronchoalveolar lavage (BAL) but not of IFN-gamma.", "entity1": "IL-4", "entity2": "GCS", "span1": [65, 69], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14341": {"label": 3, "data": {"text": "Additionally, DMF and Ad-Nrf2 repressed TGF-beta-stimulated Smad3 activity by inhibiting Smad3 phosphorylation, which was restored by siRNA-mediated knockdown of Nrf2 expression.", "entity1": "Smad3", "entity2": "DMF", "span1": [60, 65], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8503": {"label": 3, "data": {"text": "Our study demonstrated that curcumin inhibited OVA-induced increases in eosinophil count; interleukin (IL)-17A level were recovered in bronchoalveolar lavage fluid increased IL-10 level in bronchoalveolar lavage fluid.", "entity1": "interleukin (IL)-17A", "entity2": "curcumin", "span1": [90, 110], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"484": {"label": 1, "data": {"text": "The atypical neuroleptics remoxipride, clozapine, perlapine, seroquel, and melperone had low affinity for the dopamine D2 receptor (radioligand-independent dissociation constants of 30 to 90 nM).", "entity1": "D2 receptor", "entity2": "clozapine", "span1": [119, 130], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11236": {"label": 1, "data": {"text": "Taken together, these results reveal several differences between effects of MDMA and previously reported METH on DAT and VMAT-2; differences that may underlie the dissimilar neurotoxic profile of these agents.", "entity1": "DAT", "entity2": "METH", "span1": [113, 116], "span2": [105, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11902": {"label": 3, "data": {"text": "Western blotting demonstrated that DMBT effectively suppressed the expression of VEGF, p-VEGFR-2, p-EGFR, and p-Akt.", "entity1": "p-VEGFR-2", "entity2": "DMBT", "span1": [87, 96], "span2": [35, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12859": {"label": 0, "data": {"text": "Removal of Pro128 from the hepatic SDH consisting of 328 residues, which is missing in the corresponding position of the isoform consisting of 329 residues, significantly changed the Michaelis constants and Kd value for pyridoxal 5'-phosphate, whereas addition of a proline residue to the isoform was without effect.", "entity1": "SDH", "entity2": "proline", "span1": [35, 38], "span2": [266, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9649": {"label": 5, "data": {"text": "Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor.", "entity1": "androgen receptor", "entity2": "estramustine phosphate", "span1": [98, 115], "span2": [32, 54]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15527": {"label": 3, "data": {"text": "A highly potent inhibition of the peroxidase catalytic reaction by NO/SNO was seen in assays employing the coupled Prx-Trx system.", "entity1": "peroxidase", "entity2": "NO", "span1": [34, 44], "span2": [67, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14493": {"label": 1, "data": {"text": "In breast cancer (BC) epithelial cells, the mitogenic action of estradiol is transduced through binding to two receptors, ER\u03b1 and ER\u03b2, which act as transcription factors.", "entity1": "ER\u03b1", "entity2": "estradiol", "span1": [122, 125], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"380": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "IFN-gamma", "entity2": "Dexamethasone", "span1": [80, 89], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9950": {"label": 9, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-1", "entity2": "meloxicam", "span1": [180, 185], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10485": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "terbutalin", "span1": [392, 423], "span2": [177, 187]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"640": {"label": 1, "data": {"text": "To establish the relative importance of these subtypes, we compared the effects of sumatriptan with those of a selective 5-HT1F receptor agonist (LY 344864) on c-fos protein expression in the trigeminal nucleus caudalis.", "entity1": "c-fos", "entity2": "LY 344864", "span1": [160, 165], "span2": [146, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6154": {"label": 1, "data": {"text": "Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C.", "entity1": "cardiac troponin C", "entity2": "trifluoperazine", "span1": [68, 86], "span2": [49, 64]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10626": {"label": 3, "data": {"text": "While fluoropyrimidine antimetabolites have other sites of action, antifolates ZD1694 (raltitrexed, Tomudex) and AG337 (Thymitag) are more specific and potent TS inhibitors.", "entity1": "TS", "entity2": "ZD1694", "span1": [159, 161], "span2": [79, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14437": {"label": 1, "data": {"text": "Fungicide prochloraz and environmental pollutant dioxin induce the ABCG2 transporter in bovine mammary epithelial cells by the arylhydrocarbon receptor signaling pathway.", "entity1": "arylhydrocarbon receptor", "entity2": "dioxin", "span1": [127, 151], "span2": [49, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14021": {"label": 3, "data": {"text": "Inhibition of the NF-kappaB pathway was responsible for this effect since the colchicoside inhibited RANKL-induced NF-kappaB activation, activation of IkappaB kinase (IKK) and suppressed inhibitor of NF-kappaBalpha (IkappaBalpha) phosphorylation and degradation, an inhibitor of NF-kappaB.", "entity1": "IKK", "entity2": "colchicoside", "span1": [167, 170], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3319": {"label": 1, "data": {"text": "VP-16 induced the release of IL-8, and addition of MXF reduced enhanced release and the spontaneous release of VEGF from the cells.", "entity1": "IL-8", "entity2": "VP-16", "span1": [29, 33], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2906": {"label": 3, "data": {"text": "Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man.", "entity1": "cyclooxygenase-2", "entity2": "paracetamol", "span1": [43, 59], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4039": {"label": 3, "data": {"text": "In addition, we found that neoechinulin A significantly suppressed the production of neurotoxic inflammatory mediator tumour necrosis factor-\u03b1 (TNF-\u03b1), interleukin-1\u03b2 (IL-1\u03b2), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) in activated BV-2 cells.", "entity1": "TNF-\u03b1", "entity2": "neoechinulin A", "span1": [144, 149], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3475": {"label": 4, "data": {"text": "Previous studies demonstrated that the Group III mGlu receptor-selective orthosteric agonist, LSP1-2111 produced anxiolytic- but not antidepressant-like effects upon peripheral administration.", "entity1": "Group III mGlu receptor", "entity2": "LSP1-2111", "span1": [39, 62], "span2": [94, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"4493": {"label": 9, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES2", "entity2": "clopidogrel-\u03b2-d-glucuronide", "span1": [300, 305], "span2": [28, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7814": {"label": 8, "data": {"text": "Hydrophobic amino acids in the hinge region of the 5A apolipoprotein mimetic peptide are essential for promoting cholesterol efflux by the ABCA1 transporter.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [139, 144], "span2": [113, 124]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10949": {"label": 8, "data": {"text": "Because l-lactate reduced to 67% of the nicotinate uptake even at 10mM, it is unlikely that nicotinate uptake in rat astrocytes is mediated by MCT1 and/or MCT2.", "entity1": "MCT1", "entity2": "nicotinate", "span1": [143, 147], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12946": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "YM-087", "span1": [39, 59], "span2": [132, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14175": {"label": 8, "data": {"text": "Defects resulting in slowed release of cholesterol from late endosomes and lysosomes or reduction in sterol-27-hydroxylase activity lead to specific blocks in oxysterol production and impaired LXR-dependent gene activation.", "entity1": "sterol-27-hydroxylase", "entity2": "oxysterol", "span1": [101, 122], "span2": [159, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12743": {"label": 1, "data": {"text": "These studies demonstrate that AMPK activity is subject to regulation by both glucose and metformin in pancreatic islets and clonal beta-cells.", "entity1": "AMPK", "entity2": "glucose", "span1": [31, 35], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12062": {"label": 9, "data": {"text": "In the insulin-hypoglycemia test (0.15 IU/kg BW), neither the ACTH peak nor the area under the curve of ACTH was affected by loperamide.", "entity1": "ACTH", "entity2": "loperamide", "span1": [104, 108], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9325": {"label": 3, "data": {"text": "RESULTS: Nedocromil sodium inhibited the chemotactic response toward FMLP and NAF/IL-8 of GM-CSF primed eosinophils approximately 60% (inhibitory concentration of 50% [IC50] approximately 1 to 10 nmol/L), whereas these responses of IL-3 primed eosinophils was completely inhibited (IC50 approximately 1 nmol/L).", "entity1": "IL-8", "entity2": "Nedocromil sodium", "span1": [82, 86], "span2": [9, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10289": {"label": 1, "data": {"text": "These differences from the horse might be the result of: (a) the presence in equine biological fluids of higher concentrations than in calves of the active PBZ metabolite, OPBZ; (b) a greater degree of binding of PBZ to plasma protein in calves; (c) species differences in the sensitivity to PBZ of the cyclo-oxygenase (COX) isoenzymes, COX-1 and COX-2 or; (d) a combination of these factors.", "entity1": "cyclo-oxygenase", "entity2": "PBZ", "span1": [303, 318], "span2": [292, 295]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11130": {"label": 1, "data": {"text": "Prazosin was found to be unselective; 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101), 5-methyl-urapidil, indoramin and (+)-niguldipine were confirmed as selective for the alpha 1A-adrenoceptor, whereas spiperone was weakly alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptor", "entity2": "(+)-niguldipine", "span1": [192, 213], "span2": [140, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10738": {"label": 3, "data": {"text": "However, the flowcytometric analysis revealed that AZC and PCA decreased intracellular contents of CD3-zeta chain in these cells in dose dependent manner.", "entity1": "CD3-zeta chain", "entity2": "AZC", "span1": [99, 113], "span2": [51, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4611": {"label": 8, "data": {"text": "Although glutathione S-transferase omega 1 (GSTO1) and arsenic methyltransferase have been shown or thought to catalyze DMAs(V) reduction, their role in DMAs(V) reduction in vivo, or in cell extracts is uncertain.", "entity1": "glutathione S-transferase omega 1", "entity2": "DMAs(V)", "span1": [9, 42], "span2": [120, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13227": {"label": 1, "data": {"text": "Glutamate stimulates glutamate receptor interacting protein 1 degradation by ubiquitin-proteasome system to regulate surface expression of GluR2.", "entity1": "GluR2", "entity2": "Glutamate", "span1": [139, 144], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"660": {"label": 3, "data": {"text": "Thus our data suggest that the COX-2 preference of meloxicam observed in vitro may not result in clinical advantages when the higher dose of 15 mg is needed.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [31, 36], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4335": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "ocal adhesion kinase", "entity2": "Pinosylvin", "span1": [79, 99], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15783": {"label": 8, "data": {"text": "A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone.", "entity1": "oxidosqualene cyclase(1)", "entity2": "lanosterol", "span1": [97, 121], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9903": {"label": 1, "data": {"text": "However, in virgin mice, bezafibrate and WY-14,643 do not significantly affect UCP-3 mRNA expression, whereas troglitazone is at least as effective as it is in lactating dams.", "entity1": "UCP-3", "entity2": "troglitazone", "span1": [79, 84], "span2": [110, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9285": {"label": 9, "data": {"text": "Beta 2- but not beta 1-adrenoceptors are involved in desipramine enhancement of aggressive behavior in long-term isolated mice.", "entity1": "beta 1-adrenoceptors", "entity2": "desipramine", "span1": [16, 36], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"547": {"label": 1, "data": {"text": "The selective 5-HT reuptake inhibitors paroxetine, indalpine and fluvoxamine displayed a high affinity for the 5-HT transporter, whereas the norepinephrine reuptake inhibitor desipramine had a high affinity for the norepinephrine transporter.", "entity1": "5-HT transporter", "entity2": "fluvoxamine", "span1": [111, 127], "span2": [65, 76]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12751": {"label": 2, "data": {"text": "The c-Jun absorbed light value/GAPDH absorbed light value of mesenteric arteries in the SHR group was 0.850+/-0.015, which was significantly higher than that in the WKY, imidapril, and irbesartan groups (0.582+/-0.013, 0.743+/-0.012, and 0.789+/-0.013, respectively, P<0.01), and was significantly lower in imidapril group than in irbesartan group (P<0.05).", "entity1": "GAPDH", "entity2": "imidapril", "span1": [31, 36], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"362": {"label": 1, "data": {"text": "Interestingly, two categories of clones were distinguished based on the effects of GCS on IL-2 production and IL-2R alpha expression and proliferation; 1) In low IL-2 producers DEX blocked IL-2 production and decreased IL-2R alpha expression and proliferation; 2) In high IL-2 producers DEX inhibited IL-2 production partially and enhanced IL-2R alpha expression and proliferation.", "entity1": "IL-2", "entity2": "GCS", "span1": [90, 94], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8830": {"label": 1, "data": {"text": "A Structural Snapshot of Cytochrome P450 2B4 in Complex with Paroxetine Provides Insights into Ligand Binding and Clusters of Conformational States.", "entity1": "Cytochrome P450 2B4", "entity2": "Paroxetine", "span1": [25, 44], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10537": {"label": 1, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "CREB", "entity2": "RA", "span1": [353, 357], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14066": {"label": 1, "data": {"text": "Oncogenic K-ras expression is associated with derangement of the cAMP/PKA pathway and forskolin-reversible alterations of mitochondrial dynamics and respiration.", "entity1": "K-ras", "entity2": "forskolin", "span1": [10, 15], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2774": {"label": 2, "data": {"text": "In conclusion, immortalized SHR and WKY PTE cells take up l-alanine mainly through a high-affinity Na(+)-dependent amino acid transporter, with functional features of ASCT2 transport.", "entity1": "ASCT2", "entity2": "Na(+)", "span1": [167, 172], "span2": [99, 104]}, "weak_labels": [0, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6046": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "1-m-chlorophenylpiperazine", "span1": [73, 79], "span2": [100, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11656": {"label": 3, "data": {"text": "The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone.", "entity1": "MUC2", "entity2": "guggulsterone", "span1": [57, 61], "span2": [80, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1491": {"label": 3, "data": {"text": "EGF-stimulated phosphorylation of ERK and Bad is blocked by pretreatment with U0126, a selective MAP kinase kinase (MKK)1/2 inhibitor.", "entity1": "MAP kinase kinase (MKK)1/2", "entity2": "U0126", "span1": [97, 123], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15109": {"label": 1, "data": {"text": "Our results lead us to conclude that trout GPx1 transcripts expression level may represent a sensitive biomarker for selenium intake, helping to evaluate if selenium concentration and chemical speciation impact on cell homeostasis.", "entity1": "GPx1", "entity2": "selenium", "span1": [43, 47], "span2": [117, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2884": {"label": 2, "data": {"text": "In medial striatum, TH-ir decreased by 21%, and in hypothalamus neuropeptide Y-ir increased by 10% in MPH-exposed rats.", "entity1": "neuropeptide Y", "entity2": "MPH", "span1": [64, 78], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15400": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-8", "entity2": "7-ketosterols", "span1": [71, 75], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"14659": {"label": 0, "data": {"text": "Genistein also reduced the formation of stress fibers by thrombin and suppressed thrombin-induced phosphorylation of myosin light chain (MLC) on Ser(19)/Thr(18) in endothelial cells (ECs).", "entity1": "myosin light chain", "entity2": "Ser", "span1": [117, 135], "span2": [145, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13259": {"label": 3, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "MUC2/5AC", "entity2": "Pranlukast hydrate", "span1": [85, 93], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6294": {"label": 5, "data": {"text": "The selective 5-HT1A receptor antagonist, WAY100,635, slightly attenuated the (-)-pindolol-induced increase in DA and NAD levels, while the selective 5-HT1B antagonist, SB224,289, was ineffective.", "entity1": "5-HT1A", "entity2": "WAY100,635", "span1": [14, 20], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3756": {"label": 1, "data": {"text": "Thus, the apoptosis induction in SGC-7901 cells by \u03b2-ionone may be regulated through a PI3K-AKT pathway.", "entity1": "AKT", "entity2": "\u03b2-ionone", "span1": [92, 95], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11687": {"label": 8, "data": {"text": "Stable ABCC1, ABCC2 and ABCC3 knockdown cell lines were generated, thus making it possible to demonstrate that ABCC1 mediates the basolateral and ABCC2 the apical excretion of BPDE glutathione conjugates.", "entity1": "ABCC1", "entity2": "BPDE glutathione", "span1": [7, 12], "span2": [176, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5577": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "human CA", "entity2": "methazolamide", "span1": [69, 77], "span2": [229, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1596": {"label": 3, "data": {"text": "Nevertheless, 3 mM DMA, a higher concentration that inhibits NHE1, NHE2, and NHE3, significantly increased DBS.", "entity1": "NHE2", "entity2": "DMA", "span1": [67, 71], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11616": {"label": 8, "data": {"text": "The alpha class human GSTA4-4 enzyme (hGSTA4-4) has a particularly high catalytic efficiency toward 4-HNE conjugation.", "entity1": "hGSTA4-4", "entity2": "4-HNE", "span1": [38, 46], "span2": [100, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6574": {"label": 1, "data": {"text": "The comparison between MalP structures shows that His377, through a hydrogen bond with the 6-hydroxyl group of Glc1P substrate, triggers a conformational change of the 380s loop.", "entity1": "MalP", "entity2": "Glc1P", "span1": [23, 27], "span2": [111, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6800": {"label": 1, "data": {"text": "Levetiracetam binds selectively and with high affinity to a synaptic vesicle protein known as SV2A, thought to be involved with synaptic vesicle exocytosis and presynaptic neurotransmitter release.", "entity1": "synaptic vesicle protein", "entity2": "Levetiracetam", "span1": [60, 84], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5911": {"label": 3, "data": {"text": "Fibric acids, in particular, act by stimulating the catabolism of VLDL and also, as a consequence, improving LDL delipidation, thus favoring receptor uptake.", "entity1": "VLDL", "entity2": "Fibric acids", "span1": [66, 70], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2958": {"label": 1, "data": {"text": "Affinity of V782A for cGMP, vardenafil, sildenafil, tadalafil, or IBMX was reduced 5.5-, 23-, 10-, 3-, and 12-fold, respectively.", "entity1": "V782A", "entity2": "vardenafil", "span1": [12, 17], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8020": {"label": 3, "data": {"text": "Optimization of 5-hydroxytryptamines as dual function inhibitors targeting phospholipase A2 and leukotriene A4 hydrolase.", "entity1": "leukotriene A4 hydrolase", "entity2": "5-hydroxytryptamines", "span1": [96, 120], "span2": [16, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11335": {"label": 3, "data": {"text": "In the present study, we measured the enzyme activity of thymidine kinase (TK), thymidine phosphorylase (TP) and thymidilate synthase (TS) in human cancer xenografts to investigate the contribution of these enzymes to the sensitivity of TAS-102.", "entity1": "thymidilate synthase", "entity2": "TAS-102", "span1": [113, 133], "span2": [237, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10726": {"label": 1, "data": {"text": "For the vasopressin V1A/oxytocin receptor antagonist atosiban, none of the receptor constructs were able to provide a binding with higher affinity than the starting vasopressin V2 receptor.", "entity1": "vasopressin V2 receptor", "entity2": "atosiban", "span1": [165, 188], "span2": [53, 61]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8839": {"label": 1, "data": {"text": "CONCLUSION: We provided documentation of neuroprotective effect of a natural flavone, calycopterin, against H2O2-induced oxidative stress in differentiated PC12 cells by modulating the level of CREB phosphorylation and Nrf2 pathway.", "entity1": "Nrf2", "entity2": "calycopterin", "span1": [219, 223], "span2": [86, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9996": {"label": 3, "data": {"text": "We report here that a human degradation-resistant GLP-2 analogue, h[Gly2]-GLP-2 significantly improves survival, reduces bacteremia, attenuates epithelial injury, and inhibits crypt apoptosis in the murine gastrointestinal tract after administration of topoisomerase I inhibitor irinotecan hydrochloride or the antimetabolite 5-fluorouracil.", "entity1": "topoisomerase I", "entity2": "irinotecan hydrochloride", "span1": [253, 268], "span2": [279, 303]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12788": {"label": 3, "data": {"text": "Valdecoxib showed similar activity in the human whole-blood COX assay (COX-2 IC(50) = 0.24 microM; COX-1 IC(50) = 21.9 microM).", "entity1": "COX-2", "entity2": "Valdecoxib", "span1": [71, 76], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5417": {"label": 1, "data": {"text": "Clock Gene Expression in the Liver of Streptozotocin-induced and Spontaneous Type 1 Diabetic Rats.", "entity1": "Clock", "entity2": "Streptozotocin", "span1": [0, 5], "span2": [38, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4277": {"label": 2, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "AEG-1", "entity2": "ursolic acid", "span1": [118, 123], "span2": [135, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3416": {"label": 3, "data": {"text": "Because clinical studies investigating interactions between garlic and human immunodeficiency virus protease inhibitors saquinavir and ritonavir have already been performed, we used these in vivo data to evaluate the in vitro results and the reliability of the models employed as screening tools for forecasting the potential of first-pass intestinal metabolism changes.", "entity1": "human immunodeficiency virus protease", "entity2": "ritonavir", "span1": [71, 108], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9794": {"label": 3, "data": {"text": "Dichloroally]-lawsone was found to be a time-dependent inhibitor of the rat enzyme, with the lowest inhibition constant (Ki* = 0.77 nM) determined so far for mammalian dihydroorotate dehydrogenases.", "entity1": "mammalian dihydroorotate dehydrogenases", "entity2": "Dichloroally]-lawsone", "span1": [158, 197], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"627": {"label": 3, "data": {"text": "Inhibition > 90% of IL-2 secretion was observed at 1 microM BPB and 10 microM AACOCF3 compared to the respective vehicle control.", "entity1": "IL-2", "entity2": "BPB", "span1": [20, 24], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1043": {"label": 2, "data": {"text": "In addition, ADP was shown to strongly antagonize TOP2-mediated DNA cleavage induced by ATP-sensitive but not ATP-insensitive TOP2 poisons.", "entity1": "TOP2", "entity2": "ATP", "span1": [50, 54], "span2": [88, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12342": {"label": 8, "data": {"text": "In this work, the metabolism of four frequently prescribed inhaled GCs, triamcinolone acetonide, flunisolide, budesonide, and fluticasone propionate, by the CYP3A family of enzymes was studied to identify differences in their rates of clearance and to identify their metabolites.", "entity1": "CYP3A", "entity2": "triamcinolone acetonide", "span1": [157, 162], "span2": [72, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15815": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFbeta receptor", "entity2": "Tyr", "span1": [70, 87], "span2": [157, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"394": {"label": 1, "data": {"text": "The antagonist SR 141716A has a high specificity for the central CB1 cannabinoid receptor and negligeable affinity for the peripheral CB2 receptor, making it an excellent tool for probing receptor structure-activity relationships.", "entity1": "cannabinoid receptor", "entity2": "SR 141716A", "span1": [69, 89], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8603": {"label": 2, "data": {"text": "Serum markers of liver damage (AST, ALT, ALP and Bilirubin) were increased by CCl4 and TAA intoxication (p<0.001), whereas co-treatment with NAC reversed such changes (p<0.001).", "entity1": "ALT", "entity2": "CCl4", "span1": [36, 39], "span2": [78, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9971": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-1", "entity2": "aspirin", "span1": [214, 219], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5648": {"label": 2, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "hERG", "entity2": "oxymatrine", "span1": [25, 29], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8306": {"label": 2, "data": {"text": "Cellular responses to DNA damage induced by etoposide or doxorubicin include down-regulation of endogenous supervillin coincident with increases in p53.", "entity1": "p53", "entity2": "etoposide", "span1": [148, 151], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"409": {"label": 1, "data": {"text": "The affinity estimate for prazosin on human prostate was lower than the corresponding binding affinity determined at alpha 1A adrenoceptors and RS 17053 was a very weak antagonist on human prostate (pA2 = 6.0) relative to the high affinity (pKi = 8.6) determined at cloned human alpha 1A adrenoceptors.", "entity1": "alpha 1A adrenoceptors", "entity2": "prazosin", "span1": [117, 139], "span2": [26, 34]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14600": {"label": 9, "data": {"text": "In conclusion, the Lys27Gln substitution does not significantly modulate CDA activity toward dFdC, and therefore would not contribute to interindividual variability in response to gemcitabine.", "entity1": "CDA", "entity2": "gemcitabine", "span1": [73, 76], "span2": [180, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"636": {"label": 3, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "PLA2", "entity2": "arachidonyl trifluoromethyl ketone", "span1": [80, 84], "span2": [130, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8542": {"label": 3, "data": {"text": "In DU-PM cells with acquired resistance to elisidepsin, ErbB3 expression was decreased, while Bcl2 was increased.", "entity1": "ErbB3", "entity2": "elisidepsin", "span1": [56, 61], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12987": {"label": 1, "data": {"text": "The C677T polymorphism of the methylene-tetrahydrofolate reductase (MTHFR) gene is associated with a reduction of catalytic activity and is suggested to modify cancer risk differently depending on folate status.", "entity1": "methylene-tetrahydrofolate reductase", "entity2": "folate", "span1": [30, 66], "span2": [197, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14778": {"label": 8, "data": {"text": "Electrical Stimuli Release ATP to Increase GLUT4 Translocation and Glucose Uptake via PI3K\u03b3-Akt-AS160 in Skeletal Muscle Cells.", "entity1": "GLUT4", "entity2": "Glucose", "span1": [43, 48], "span2": [67, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2216": {"label": 3, "data": {"text": "A dose of 25 microg kg(-1) day(-1) of formoterol elicited greater EDL and soleus hypertrophy than salmeterol, but resulted in similar beta-adrenoceptor downregulation.", "entity1": "beta-adrenoceptor", "entity2": "salmeterol", "span1": [134, 151], "span2": [98, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12600": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "fibronectin type II domain", "entity2": "N", "span1": [172, 198], "span2": [316, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6188": {"label": 5, "data": {"text": "These data indicate that mixed 5-HT1/5-HT2 receptor antagonists such as pizotifen and methysergide, and mixed 5-HT and catecholamine antagonists such as mianserin and mirtazapine are more potent antagonists of mCPP-induced behavioural inhibition in rats than the more selective 5-HT2A/5-HT2C antagonist ritanserin.", "entity1": "5-HT1", "entity2": "pizotifen", "span1": [31, 36], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11373": {"label": 1, "data": {"text": "Here, we report the initial characterization of I3A as a protein kinase C (PKC) ligand.", "entity1": "PKC", "entity2": "I3A", "span1": [75, 78], "span2": [48, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4273": {"label": 2, "data": {"text": "Overall, our findings suggest that ursolic acid induced apoptosis in HepG2 cells via AMPK activation and GSK3\u03b2 phosphorylation as a potent chemopreventive agent.", "entity1": "GSK3\u03b2", "entity2": "ursolic acid", "span1": [105, 110], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10524": {"label": 2, "data": {"text": "Incubation with metformin (0.2-1 mM) activated AMPK in both human islets and MIN6 beta-cells in parallel with an inhibition of insulin secretion, whereas leptin (10-100 nM) was without effect in MIN6 cells.", "entity1": "AMPK", "entity2": "metformin", "span1": [47, 51], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12970": {"label": 1, "data": {"text": "gammaPKC directly associated with DGKgamma through its accessory domain (AD), depending on Ca2+ as well as phosphatidylserine/diolein in vitro.", "entity1": "DGKgamma", "entity2": "Ca2+", "span1": [34, 42], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8925": {"label": 5, "data": {"text": "The vasopressor response to the calcium channel activator, BAY-K-8644, which is mediated through the opening of voltage dependent calcium channels and the subsequent translocation of extracellular calcium, was significantly inhibited by carvedilol (1 mg/kg, iv), suggesting that carvedilol is also a calcium channel antagonist, consistent with our previous in vitro studies.", "entity1": "calcium channel", "entity2": "carvedilol", "span1": [300, 315], "span2": [279, 289]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4245": {"label": 1, "data": {"text": "Butein protects human dental pulp cells from hydrogen peroxide-induced oxidative toxicity via Nrf2 pathway-dependent heme oxygenase-1 expressions.", "entity1": "heme oxygenase-1", "entity2": "Butein", "span1": [117, 133], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3717": {"label": 3, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "ERK", "entity2": "N", "span1": [97, 100], "span2": [13, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2313": {"label": 3, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "beta-catenin", "entity2": "sulindac", "span1": [167, 179], "span2": [128, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16068": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "B-cell antigen receptor", "entity2": "Ibrutinib", "span1": [142, 165], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11033": {"label": 1, "data": {"text": "In vivo angiogenesis assay utilising gelfoam sponges, bexarotene reduced angiogenesis in sponges containing vascular endothelial growth factor, epidermal growth factor and basic fibroblast growth factor to various extent.", "entity1": "vascular endothelial growth factor", "entity2": "bexarotene", "span1": [108, 142], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10484": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "salmeterol", "span1": [392, 423], "span2": [165, 175]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10191": {"label": 3, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP-A", "entity2": "Rifampicin", "span1": [115, 121], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9197": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "EGF", "entity2": "naphthalenesulfonamides", "span1": [261, 264], "span2": [27, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11310": {"label": 1, "data": {"text": "This study also investigated the effect of zuclopenthixol on cortical and hippocampal monoaminergic neurotransmitters' levels together with acetylcholinesterase enzyme (AChE) activity, both of which are known to be important in control of cognitive function.", "entity1": "AChE", "entity2": "zuclopenthixol", "span1": [169, 173], "span2": [43, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11342": {"label": 8, "data": {"text": "Phosphatidylserine (PtdSer) is made in mammalian cells by two PtdSer synthases, PSS1 and PSS2.", "entity1": "PSS1", "entity2": "Phosphatidylserine", "span1": [80, 84], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14159": {"label": 4, "data": {"text": "The atypical antidepressant mianserin exhibits agonist activity at kappa-opioid receptors.", "entity1": "kappa-opioid receptors", "entity2": "mianserin", "span1": [67, 89], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8539": {"label": 1, "data": {"text": "In addition, high ErbB3 and Muc1 expression was correlated with sensitivity to elisidepsin, whereas the presence of KRAS activating mutations was associated with resistance.", "entity1": "ErbB3", "entity2": "elisidepsin", "span1": [18, 23], "span2": [79, 90]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1581": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "acetylcholinesterase", "entity2": "4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines", "span1": [4, 24], "span2": [163, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7940": {"label": 1, "data": {"text": "Structure-activity relationship analysis of highly potent subtype-selective ligands (MT(2) EC(50) 10-90 pM) revealed that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT(2) potency and at the same time decreased MT(1) potency.", "entity1": "MT(2)", "entity2": "3-methoxyphenyl", "span1": [229, 234], "span2": [182, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10818": {"label": 9, "data": {"text": "Treatment with valsartan, doxazosin, or N-acetylcysteine did not significantly affect HIF-1alpha and VEGF proteins expression in the banding groups.", "entity1": "HIF-1alpha", "entity2": "doxazosin", "span1": [86, 96], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15620": {"label": 3, "data": {"text": "Galangin decreased expression of pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-\u03b1, interleukin (IL)-6, IL-1\u03b2, and IL-8.", "entity1": "IL-8", "entity2": "Galangin", "span1": [131, 135], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5295": {"label": 3, "data": {"text": "Chelation of calcium ions by BAPTA-AM or blockade of ERK1/2 activation by UO126 also prevented the NMDA effects.", "entity1": "ERK1/2", "entity2": "UO126", "span1": [53, 59], "span2": [74, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13933": {"label": 3, "data": {"text": "Both drugs at the tested doses (0.042-0.33 mug/kg) suppressed PTH mRNA expression and serum PTH effectively in the 5/6 NX rats, but paricalcitol was less potent in raising serum Ca than doxercalciferol.", "entity1": "PTH", "entity2": "doxercalciferol", "span1": [62, 65], "span2": [186, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11452": {"label": 1, "data": {"text": "The present study examined the reinforcing and DAT effects of the local anesthetics dimethocaine, procaine and cocaine using in vivo techniques.", "entity1": "DAT", "entity2": "cocaine", "span1": [47, 50], "span2": [111, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7956": {"label": 4, "data": {"text": "To investigate the role of mGluR8 in modulating the synaptic responses of retinal ganglion cells, we used a recently identified positive allosteric modulator of mGluR8, AZ12216052 (AZ) and the mGluR8-specific orthosteric agonist (S)-3,4-dicarboxyphenylglycine (DCPG).", "entity1": "mGluR8", "entity2": "DCPG", "span1": [193, 199], "span2": [261, 265]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"1037": {"label": 3, "data": {"text": "Pranlukast is a new, orally active, selective inhibitor of CysLt1 leukotriene receptor.", "entity1": "CysLt1", "entity2": "Pranlukast", "span1": [59, 65], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9929": {"label": 1, "data": {"text": "Arachidonic acid and nonsteroidal anti-inflammatory drugs induce conformational changes in the human prostaglandin endoperoxide H2 synthase-2 (cyclooxygenase-2).", "entity1": "human prostaglandin endoperoxide H2 synthase-2", "entity2": "Arachidonic acid", "span1": [95, 141], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6451": {"label": 1, "data": {"text": "CONCLUSIONS: After the initial bleach, halothane impeded photon absorption by rhodopsin by inhibiting metabolic rhodopsin regeneration.", "entity1": "rhodopsin", "entity2": "halothane", "span1": [78, 87], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9081": {"label": 2, "data": {"text": "The order of effect was 4HPR greater than ROAc greater than 13cisRA, with increases in prothrombin times correlating with increases in hemorrhagic deaths.", "entity1": "prothrombin", "entity2": "ROAc", "span1": [87, 98], "span2": [42, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14885": {"label": 9, "data": {"text": "The induction of HO-1 by EIH was inhibited by SB203580 but not by SP600125, PD98059, nor LY294002.", "entity1": "HO-1", "entity2": "PD98059", "span1": [17, 21], "span2": [76, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10701": {"label": 4, "data": {"text": "Safety and tolerability of denufosol tetrasodium inhalation solution, a novel P2Y2 receptor agonist: results of a phase 1/phase 2 multicenter study in mild to moderate cystic fibrosis.", "entity1": "P2Y2 receptor", "entity2": "denufosol tetrasodium", "span1": [78, 91], "span2": [27, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13706": {"label": 3, "data": {"text": "The IC(50) for block of resting channels at -150 mV was 2.3, 3.9 and 11.3 microM in Na(V)1.4, respectively, and 29.2 microM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.2", "entity2": "4-chloropropofol", "span1": [148, 156], "span2": [128, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10254": {"label": 8, "data": {"text": "The juvenile visceral steatosis (jvs) mouse, having a mutation in the carnitine transporter gene Octn2, is a model of primary systemic carnitine deficiency in humans (SCD, OMIM 212140).", "entity1": "Octn2", "entity2": "carnitine", "span1": [97, 102], "span2": [70, 79]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2561": {"label": 1, "data": {"text": "In randomized controlled trials, bisphosphonates (pamidronate and zoledronic acid) and selective estrogen receptor modulators (raloxifene and toremifene) increased bone mineral density in GnRH agonist-treated men.", "entity1": "estrogen receptor", "entity2": "raloxifene", "span1": [97, 114], "span2": [127, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1384": {"label": 2, "data": {"text": "Gemfibrozil induced peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which was inhibited by the expression of DeltahPPAR-alpha, the dominant-negative mutant of human PPAR-alpha.", "entity1": "peroxisome proliferator-responsive element", "entity2": "Gemfibrozil", "span1": [20, 62], "span2": [0, 11]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4840": {"label": 9, "data": {"text": "Cucurbitacin I inhibits rac1 activation in breast cancer cells by a reactive oxygen species-mediated mechanism and independently of janus tyrosine kinase 2 and p-rex1.", "entity1": "janus tyrosine kinase 2", "entity2": "Cucurbitacin I", "span1": [132, 155], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8490": {"label": 3, "data": {"text": "Furthermore, no impact on cytokine release (i.e., on IL-10, IL-6, IL-12/23p40 and TNF\u03b1 levels) was seen in LPS-stimulated human PBMCs, except with JWH-210 and JWH-122 which caused a decrease of TNF\u03b1 and IL-12/23p40.", "entity1": "23p40", "entity2": "JWH-122", "span1": [209, 214], "span2": [159, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2213": {"label": 1, "data": {"text": "Two beta(2)-agonists, formoterol and salmeterol, are approved for treating asthma and have an extended duration of action and increased safety, associated with greater beta(2)-adrenoceptor selectivity.", "entity1": "beta(2)-adrenoceptor", "entity2": "formoterol", "span1": [168, 188], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6457": {"label": 4, "data": {"text": "METHODS: Different classes of antidepressants [imipramine (tricyclic), maprotiline (noradrenline reuptake inhibitor), venlafaxine (mixed serotonin and noradrenaline reuptake inhibitors), fluvoxamine and sertraline (selective serotonin reuptake inhibitor)] were tested in the same randomised experimental session, alone and in combination with 5-HT1A and 5-HT1B receptor agonists [buspirone (partial 5-HT1A agonist), anpirtoline (5-HT1B agonist)] in the mouse forced swimming test.", "entity1": "5-HT1A", "entity2": "buspirone", "span1": [399, 405], "span2": [380, 389]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5210": {"label": 1, "data": {"text": "In the present study, the exposure of melanoma cells to vinblastine was found to trigger apoptosis as evidenced by the loss of mitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activation of caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase.", "entity1": "cytochrome c", "entity2": "vinblastine", "span1": [181, 193], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10469": {"label": 4, "data": {"text": "(-)-Isoprenaline and a nonconventional beta(3)-adrenoceptor agonist, (+/-)-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimida zol-2-one] hydrochloride ((+/-)-CGP12177A), induced concentration-dependent relaxation of (-)-phenylephrine (0.3 microM) preconstricted spiral preparations.", "entity1": "beta(3)-adrenoceptor", "entity2": "(+/-)-CGP12177A", "span1": [39, 59], "span2": [177, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11475": {"label": 0, "data": {"text": "Functional divergence of a unique C-terminal domain of leucyl-tRNA synthetase to accommodate its splicing and aminoacylation roles.", "entity1": "leucyl-tRNA synthetase", "entity2": "C", "span1": [55, 77], "span2": [34, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"800": {"label": 1, "data": {"text": "Analysis of splice variants and site-directed mutants of the AMPA receptor GluR3 expressed in Xenopus oocytes has shown that lithium produces a large potentiation of the GluR3 flop splice variant and suggested that lithium might inhibit rapid desensitization, which is characteristic of this receptor (Karkanias, N. and Papke, R., Subtype-specific effects of lithium on glutamate receptor function.", "entity1": "glutamate receptor", "entity2": "lithium", "span1": [370, 388], "span2": [359, 366]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10205": {"label": 8, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP-A", "entity2": "BSP", "span1": [115, 121], "span2": [131, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1913": {"label": 1, "data": {"text": "SL-11158 inhibited SSAT activity with a mixed type of inhibition in which the analogue had a 70-fold higher affinity for the enzyme than the natural substrate, spermine.", "entity1": "SSAT", "entity2": "spermine", "span1": [19, 23], "span2": [160, 168]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5567": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase 1 (DDAH1) is an enzyme that metabolizes methylated arginine to citrulline and methylamine, thus working to produce nitric oxide (NO).", "entity1": "DDAH1", "entity2": "methylated arginine", "span1": [43, 48], "span2": [80, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11273": {"label": 8, "data": {"text": "The ratio between the GDC/SHMT and C1-THF synthase/SHMT pathways of Ser synthesis from [alpha-(13)C]Gly and [(13)C]formate, respectively, in Arabidopsis shoots was 21 : 1; in roots, 9 : 1.", "entity1": "C1-THF synthase", "entity2": "[(13)C]formate", "span1": [35, 50], "span2": [108, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14782": {"label": 1, "data": {"text": "A series of anthra[1,2-d]imidazole-6,11-dione derivatives were synthesized and evaluated for telomerase inhibition, hTERT expression and suppression of cancer cell growth in vitro.", "entity1": "hTERT", "entity2": "anthra[1,2-d]imidazole-6,11-dione", "span1": [116, 121], "span2": [12, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7561": {"label": 1, "data": {"text": "It is more potent and selective than citalopram in inhibiting serotonin re-uptake in the CNS, and less potent than various other selective serotonin re-uptake inhibitors in relation to other transporter proteins and receptors: in particular, it is six times less potent than citalopram in binding to the histamine H1 and muscarinic receptors.", "entity1": "histamine H1", "entity2": "citalopram", "span1": [304, 316], "span2": [275, 285]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8797": {"label": 2, "data": {"text": "Here we show that fisetin rapidly increases the levels of both Nrf2 and ATF4 as well as Nrf2- and ATF4-dependent gene transcription via distinct mechanisms.", "entity1": "Nrf2", "entity2": "fisetin", "span1": [63, 67], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3242": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "NAN", "span1": [13, 16], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8125": {"label": 3, "data": {"text": "We used nutlin-3, a well-known disruptor of p53-Mdm2 interaction, to validate the specificity of the assay.", "entity1": "p53", "entity2": "nutlin-3", "span1": [44, 47], "span2": [8, 16]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4081": {"label": 3, "data": {"text": "An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective \u03b3-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease.", "entity1": "PS1", "entity2": "SCH 900229", "span1": [145, 148], "span2": [122, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11077": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "caldesmon kinase", "entity2": "t-butyl", "span1": [110, 126], "span2": [257, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1925": {"label": 8, "data": {"text": "In the reverse case, mutation of the orthologous glycine (Gly553) to methionine in carnitine octanoyltransferase (COT) decreased activity toward its natural substrates, medium- and long-chain acyl-CoAs, and increased activity toward short-chain acyl-CoAs.", "entity1": "carnitine octanoyltransferase", "entity2": "acyl-CoAs", "span1": [83, 112], "span2": [245, 254]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10520": {"label": 3, "data": {"text": "To gauge the potential clinical utility of targeting both EGFR and HER2 to control growth and radiosensitize human breast cancers, we examined the effect of a dual EGFR/HER2 inhibitor, GW572016, on the proliferation and radiation response of either EGFR- or HER2-overexpressing human breast cancer cell lines.", "entity1": "HER2", "entity2": "GW572016", "span1": [169, 173], "span2": [185, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4907": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "TIM", "entity2": "kinsenoside", "span1": [434, 437], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3524": {"label": 8, "data": {"text": "Inhibition studies revealed that the multidrug resistance-associated proteins (ABCCs) are involved in the transport of BPDE glutathione conjugates.", "entity1": "multidrug resistance-associated proteins", "entity2": "BPDE glutathione", "span1": [37, 77], "span2": [119, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11271": {"label": 8, "data": {"text": "We concluded that FDH has no direct role in the regulation of the above two pathways of Ser synthesis; the breakdown of formate to CO(2) by the FDH reaction is the primary and preferred fate of the organic acid in Arabidopsis.", "entity1": "FDH", "entity2": "CO(2)", "span1": [144, 147], "span2": [131, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5247": {"label": 2, "data": {"text": "Fluoride treatment also increased phosphorylation of JNK and ERK, but not p38, and apoptosis induced by fluoride was notably or partly suppressed by treatment with JNK or ERK inhibitors, respectively.", "entity1": "ERK", "entity2": "Fluoride", "span1": [61, 64], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5242": {"label": 1, "data": {"text": "Exposure of cells to 4mM NaF for 24h induced caspase-3 activation, ultrastructural alterations, and resulted in the translocation of Bax to the mitochondria and the release of cytochrome c from the mitochondrial inter-membrane space into the cytosol, indicating that fluoride-mediated apoptosis is mitochondria-dependent.", "entity1": "cytochrome c", "entity2": "NaF", "span1": [176, 188], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13297": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "VEGFR", "entity2": "Nexavar", "span1": [300, 305], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4633": {"label": 1, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [120, 123], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8700": {"label": 3, "data": {"text": "Detailed structure-activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione inhibitors of HIV capsid (CA) assembly are described.", "entity1": "CA", "entity2": "1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione", "span1": [204, 206], "span2": [134, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8619": {"label": 3, "data": {"text": "Oxysterol-dependent NOX1 activation, as well as interleukin synthesis, were completely prevented by Cannonau red wine extract that contains an abundant phenolic fraction, in particular phenolic acids and flavonoids.", "entity1": "NOX1", "entity2": "flavonoids", "span1": [20, 24], "span2": [204, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12777": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "capecitabine", "span1": [0, 20], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14465": {"label": 1, "data": {"text": "Extracellular loop II modulates GTP sensitivity of the prostaglandin EP3 receptor.", "entity1": "Extracellular loop II", "entity2": "GTP", "span1": [0, 21], "span2": [32, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3355": {"label": 1, "data": {"text": "The Ca(2+) dependent interaction between troponin I (cTnI) and troponin C (cTnC) triggers contraction in heart muscle.", "entity1": "cTnC", "entity2": "Ca(2+)", "span1": [75, 79], "span2": [4, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11726": {"label": 1, "data": {"text": "In vivo and in vitro characterization of naltrindole-derived ligands at the \u03ba-opioid receptor.", "entity1": "\u03ba-opioid receptor", "entity2": "naltrindole", "span1": [76, 93], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10694": {"label": 3, "data": {"text": "Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety.", "entity1": "COX-2", "entity2": "diclofenac", "span1": [34, 39], "span2": [127, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11563": {"label": 3, "data": {"text": "In HEK293 cells stably transfected with FLT3-WT or FLT3-ITD, sorafenib blocked basal and ligand dependent FLT3-mediated tyrosine autophosphorylation as well as extracellular signal-regulated kinase1/2 and Stat5 phosphorylation.", "entity1": "extracellular signal-regulated kinase1/2", "entity2": "sorafenib", "span1": [160, 200], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8527": {"label": 1, "data": {"text": "Effect of the Potent Antiviral 1-Cinnamoyl-3,11-Dihydroxymeliacarpin on Cytokine Production by Murine Macrophages Stimulated with HSV-2.", "entity1": "Cytokine", "entity2": "1-Cinnamoyl-3,11-Dihydroxymeliacarpin", "span1": [72, 80], "span2": [31, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6197": {"label": 5, "data": {"text": "The alpha1-adrenoceptor antagonist prazosin or the vasopressin V1 receptor antagonist, [beta-mercapto-beta,beta-cyclopenta-methylenepropionyl1, O-Me-Tyr2, Arg8] vasopressin partially but significantly reduced tacrine pressor effect and mostly abolished it when administered concomitantly.", "entity1": "vasopressin V1 receptor", "entity2": "[beta-mercapto-beta,beta-cyclopenta-methylenepropionyl1, O-Me-Tyr2, Arg8] vasopressin", "span1": [51, 74], "span2": [87, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13547": {"label": 2, "data": {"text": "Furthermore, the activities of the two torafugu PPARalphas were enhanced 4.3- and 7.6-fold by arachidonic acid, 4.4- and 5.2-fold by docosahexaenoic acid, and 6.7- and 8.0-fold by eicosapentaenoic acid each at 50 microM, respectively.", "entity1": "torafugu PPARalphas", "entity2": "docosahexaenoic acid", "span1": [39, 58], "span2": [133, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"623": {"label": 3, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "arachidonyl trifluoromethyl ketone", "span1": [102, 115], "span2": [56, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14791": {"label": 2, "data": {"text": "Human immortalized corneal fibroblasts were treated with TGF-\u03b2 in the presence of TSA, the NAD(P)H oxidase inhibitor diphenyleneiodonium (DPI), the antioxidant N-acetyl-cysteine (NAC), the NF-E2-related factor 2-antioxidant response element (Nrf2-ARE) activator sulforaphane, or small interfering RNA.", "entity1": "Nrf2", "entity2": "sulforaphane", "span1": [242, 246], "span2": [262, 274]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5690": {"label": 5, "data": {"text": "In a neuronal cell line, we found that selective CB(2) receptor agonists upregulate \u03b2-Arrestin 2, an effect that was prevented by selective CB(2) receptor antagonist JTE-907 and CB(2) shRNA lentiviral particles.", "entity1": "CB(2)", "entity2": "JTE-907", "span1": [49, 54], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14078": {"label": 3, "data": {"text": "In TGF-\u03b21-induced NPDFs, berberine significantly inhibited the expression of \u03b1-SMA and collagen type I mRNA and reduced \u03b1-SMA and collagen protein levels.", "entity1": "TGF-\u03b21", "entity2": "berberine", "span1": [3, 9], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9277": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "thioridazine", "span1": [166, 186], "span2": [103, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6677": {"label": 1, "data": {"text": "Rats received a concomitant treatment with the selective beta(1)-adrenoceptor antagonist, bisoprolol (50 mg/kg/day p.o.) or were chronically pretreated with the selective beta(2)-adrenoceptor agonist salbutamol (40 microg/kg/h) for 1 week to induce beta(2)-adrenoceptor desensitization.", "entity1": "beta(2)-adrenoceptor", "entity2": "bisoprolol", "span1": [249, 269], "span2": [90, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10434": {"label": 0, "data": {"text": "The phosphate group of PLP is surrounded by a characteristic G-rich sequence ((168)GGGGL(172)) and forms hydrogen bonds with the amide groups of those amino acid residues, suggesting that the phosphate group can be protonated.", "entity1": "G-rich sequence", "entity2": "GGGGL", "span1": [61, 76], "span2": [83, 88]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7059": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RXRs", "entity2": "retinoid", "span1": [88, 92], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"31": {"label": 0, "data": {"text": "A major part of this processing requires endoproteolytic cleavage at specific pairs of basic amino acid residues, an event necessary for the maturation of a variety of important biologically active proteins, such as insulin and nerve growth factor.", "entity1": "nerve growth factor", "entity2": "amino acid", "span1": [228, 247], "span2": [93, 103]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"160": {"label": 2, "data": {"text": "Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex.", "entity1": "AChE", "entity2": "oximes", "span1": [22, 26], "span2": [162, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9997": {"label": 8, "data": {"text": "OBJECTIVES: The hypothesis of the present study was that differences among dopamine transporter (DAT) ligands in potency and effectiveness as a positive reinforcers were related to potency and effectiveness as DA uptake inhibitors.", "entity1": "dopamine transporter", "entity2": "DA", "span1": [75, 95], "span2": [210, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7778": {"label": 1, "data": {"text": "Accordingly, in transfection experiments performed in TPC1 cells, treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence.", "entity1": "PARP-1", "entity2": "PJ34", "span1": [136, 142], "span2": [81, 85]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12770": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "TS", "entity2": "5-FU", "span1": [22, 24], "span2": [80, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11109": {"label": 1, "data": {"text": "Two migraine patients were studied by in vivo SPECT using the dopamine D2-receptor specific radioligand 123I-3-iodo-6-methoxybenzamide (123I-IBZM) during ergotamine abuse and after withdrawal.", "entity1": "dopamine D2-receptor", "entity2": "123I-IBZM", "span1": [62, 82], "span2": [136, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5774": {"label": 9, "data": {"text": "This binding was not significantly inhibited by the lysine analogue epsilon-amino caproic acid (EACA), indicating that plasminogen binding was not just through lysine binding sites as suggested for other plasminogen binding sites.", "entity1": "plasminogen", "entity2": "lysine", "span1": [119, 130], "span2": [52, 58]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14448": {"label": 8, "data": {"text": "TCDD or prochloraz doubled ABCG2-mediated Hoechst H33342 secretion.", "entity1": "ABCG2", "entity2": "Hoechst H33342", "span1": [27, 32], "span2": [42, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3570": {"label": 1, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "IR", "entity2": "MSG", "span1": [24, 26], "span2": [199, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4972": {"label": 3, "data": {"text": "Coupling this computational technique with a high-quality low-throughput screen identified 5-(4-piperidyl)-3-isoxazolol (4-PIOL) as a potent plasminogen binding inhibitor with the potential for the treatment of various bleeding disorders.", "entity1": "plasminogen", "entity2": "5-(4-piperidyl)-3-isoxazolol", "span1": [141, 152], "span2": [91, 119]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11324": {"label": 4, "data": {"text": "METHODS: Sedative and cardiovascular responses to etomidate and the alpha2-agonist, dexmedetomidine, were determined in mice deficient in alpha2-receptor subtypes.", "entity1": "alpha2-receptor", "entity2": "dexmedetomidine", "span1": [138, 153], "span2": [84, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13542": {"label": 2, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha1", "entity2": "5,8,11,14-eicosatetraynoic acid", "span1": [41, 51], "span2": [100, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4171": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "sulforaphane", "span1": [151, 155], "span2": [166, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7918": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "oxaliplatin", "span1": [27, 32], "span2": [116, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7198": {"label": 2, "data": {"text": "ADP initiates platelet aggregation by 'simultaneous activation of two G protein-coupled receptors, P2Y1 and P2Y12.", "entity1": "P2Y12", "entity2": "ADP", "span1": [108, 113], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15820": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFRbeta", "entity2": "Tyr", "span1": [89, 98], "span2": [176, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12110": {"label": 3, "data": {"text": "HERG/IKr channels are a prime target for the pharmacological management of arrhythmias and are selectively blocked by class III antiarrhythmic methanesulfonanilide drugs, such as dofetilide, E4031, and MK-499, at submicromolar concentrations.", "entity1": "IKr", "entity2": "methanesulfonanilide", "span1": [5, 8], "span2": [143, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1779": {"label": 2, "data": {"text": "CGP 12177A mediates cardiostimulation by activation of the 'putative' beta(4)-adrenoceptor; however, it has recently been reported that disruption of the beta(1)-adrenoceptor gene abolishes this effect.", "entity1": "beta(1)-adrenoceptor", "entity2": "CGP 12177A", "span1": [154, 174], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15864": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "HSA", "entity2": "Lys", "span1": [67, 70], "span2": [151, 154]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13095": {"label": 4, "data": {"text": "Among the measured compounds, gliquidone and glipizide (two sulfonylureas), as well as nateglinide (a glinide), exhibit PPARgamma agonistic activity at concentrations comparable with those reached under pharmacological treatment.", "entity1": "PPARgamma", "entity2": "gliquidone", "span1": [120, 129], "span2": [30, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15887": {"label": 8, "data": {"text": "Targeted disruption of the gene encoding the N-glycosyltransferase, prlH, abolished pyralomicin production, and recombinant expression of PrlA confirms the activity of this enzyme as a sugar phosphate cyclase involved in the formation of the C7-cyclitol moiety.", "entity1": "N-glycosyltransferase", "entity2": "pyralomicin", "span1": [45, 66], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12327": {"label": 0, "data": {"text": "Using site-directed mutagenesis, we identified three serines (Ser833, Ser836, and Ser840) within the membrane proximal region of the GluK5 C-terminal domain that, in combination, are required for mGlu1-mediated potentiation of KARs.", "entity1": "GluK5", "entity2": "Ser", "span1": [133, 138], "span2": [70, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13270": {"label": 2, "data": {"text": "However, as a novel finding, isoflavone treatment increased a subclass of high-density lipoprotein, the pre-beta high-density lipoprotein levels by 18% without affecting any other serum lipid concentrations.", "entity1": "high-density lipoprotein", "entity2": "isoflavone", "span1": [74, 98], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6075": {"label": 0, "data": {"text": "Within the conserved transmembrane domains, the sequences exhibit approximately 52%, 59%, 65%, and 68% amino acid identity with the known rat 5-HT1A, rat 5-HT1B, rat 5-HT1D, and human 5-HT1E receptors, respectively.", "entity1": "rat 5-HT1D", "entity2": "amino acid", "span1": [162, 172], "span2": [103, 113]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14515": {"label": 1, "data": {"text": "Filtering and analysis of data identified three oncogenic pathways interfered by 5-ASA: MAPK/ERK pathway, cell adhesion and \u03b2-catenin/Wnt signaling.", "entity1": "ERK", "entity2": "5-ASA", "span1": [93, 96], "span2": [81, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5256": {"label": 2, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "WAF1", "entity2": "rofecoxib", "span1": [100, 104], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10329": {"label": 4, "data": {"text": "Plasmacytoid dendritic cells produce cytokines and mature in response to the TLR7 agonists, imiquimod and resiquimod.", "entity1": "TLR7", "entity2": "imiquimod", "span1": [77, 81], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15755": {"label": 3, "data": {"text": "CO scavenging blocked the suppression of quercetin only on CYP2E1 activity.", "entity1": "CYP2E1", "entity2": "CO", "span1": [59, 65], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5521": {"label": 1, "data": {"text": "Probing the salmeterol binding site on the beta 2-adrenergic receptor using a novel photoaffinity ligand, [(125)I]iodoazidosalmeterol.", "entity1": "beta 2-adrenergic receptor", "entity2": "[(125)I]iodoazidosalmeterol", "span1": [43, 69], "span2": [106, 133]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2372": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "VEGFR", "entity2": "Nexavar", "span1": [127, 132], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13027": {"label": 1, "data": {"text": "11Beta-HSD1 activates cortisone to cortisol to facilitate glucocorticoid receptor (GR)-mediated action.", "entity1": "GR", "entity2": "cortisol", "span1": [83, 85], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3873": {"label": 1, "data": {"text": "These studies are the first to reveal the involvement of the GSK-3\u03b2/NF-\u03baB pathway in cinobufagin-induced apoptosis.", "entity1": "NF-\u03baB", "entity2": "cinobufagin", "span1": [68, 73], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13912": {"label": 3, "data": {"text": "Phenformin reduced the open probability of Kir6.1/SUR2B channels by approximately 90% in inside-out patches.", "entity1": "Kir6.1", "entity2": "Phenformin", "span1": [43, 49], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15386": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "ALK5", "entity2": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole", "span1": [231, 235], "span2": [0, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8062": {"label": 3, "data": {"text": "Moreover, paclitaxel-induced ERCC1 protein and mRNA levels significantly decreased via the downregulation of p38 activity by either a p38 MAPK inhibitor SB202190 or p38 knockdown with specific small interfering RNA (siRNA).", "entity1": "p38", "entity2": "SB202190", "span1": [109, 112], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"94": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "EC 1.14.16.1", "entity2": "dopamine", "span1": [139, 151], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9299": {"label": 1, "data": {"text": "The present study utilized blood from normal volunteers and 125I-fibrinogen in a dilute whole blood clot assay to determine the relative concentrations of lysine analogues required for inhibition of clot lysis induced by exogenous t-PA. AMCA (0.06 mM) and EACA (0.6 mM) were effective in prolonging clot lysis if (1) whole blood clots were formed and then exposed to a lysine analogue and exogenous t-PA or if (2) whole blood clots were formed in the presence of exogenous t-PA and a lysine analogue.", "entity1": "fibrinogen", "entity2": "125I", "span1": [65, 75], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7854": {"label": 2, "data": {"text": "Protein kinase C (PKC) inhibition reduced the potentiation by mGlu1 of GluK2/GluK5, and conversely, direct activation of PKC by phorbol 12-myristate,13-acetate potentiated GluK2/GluK5.", "entity1": "GluK5", "entity2": "phorbol 12-myristate,13-acetate", "span1": [178, 183], "span2": [128, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"868": {"label": 3, "data": {"text": "Inhibition of S-adenosylmethionine decarboxylase by a specific inhibitor [diethylglyoxal bis-(guanylhydrazone); DEGBG] led to depletion of spermidine and spermine with a significant accumulation of putrescine and induction of ODC.", "entity1": "S-adenosylmethionine decarboxylase", "entity2": "DEGBG", "span1": [14, 48], "span2": [112, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"511": {"label": 1, "data": {"text": "Consistent with its selectivity for 5HT1B/1D receptors, zolmitriptan produces constriction of various isolated blood vessels, most notably cranial arteries.", "entity1": "5HT1B/1D", "entity2": "zolmitriptan", "span1": [36, 44], "span2": [56, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8988": {"label": 3, "data": {"text": "Removing medium Ca2+, blocking Ca2+ channels with 50 mumol/l verapamil, or inhibiting calmodulin activation with 20 mumol/l trifluoperazine, 10 mumol/l chlorpromazine or 10 mumol/l pimozide almost completely blocked hyposmolarity-induced secretion.", "entity1": "calmodulin", "entity2": "trifluoperazine", "span1": [86, 96], "span2": [124, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6665": {"label": 5, "data": {"text": "AT1 antagonism by eprosartan lowers heart rate variability and baroreflex gain.", "entity1": "AT1", "entity2": "eprosartan", "span1": [0, 3], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12401": {"label": 2, "data": {"text": "Number and area of preneoplastic foci positive for glutathione S-transferase placental form (GST-P) were consistently higher in these groups than the sum of individual values in the groups treated with HEP or HCB alone.", "entity1": "GST-P", "entity2": "HCB", "span1": [93, 98], "span2": [209, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11842": {"label": 1, "data": {"text": "The baseline HbA1c and glycated albumin levels were identified as factors that predicted the response to add-on therapy with sitagliptin.", "entity1": "HbA1c", "entity2": "sitagliptin", "span1": [13, 18], "span2": [125, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1803": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "cetuximab", "span1": [0, 32], "span2": [204, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3517": {"label": 3, "data": {"text": "TZDs also inhibited alkaline phosphatase activity (58-75%, p<0.046) and osteocalcin production (52-75%, p<0.031).", "entity1": "osteocalcin", "entity2": "TZDs", "span1": [72, 83], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6648": {"label": 5, "data": {"text": "However, other alpha(1)-adrenoceptor antagonists (tamsulosin, WB4101 and corynanthine) did not inhibit the binding at a range of concentrations that generally exhibit alpha(1)-adrenoceptor antagonism, and noradrenaline, rauwolscine and propranolol were without effect on the [(3)H]prazosin binding.", "entity1": "alpha(1)-adrenoceptor", "entity2": "corynanthine", "span1": [15, 36], "span2": [73, 85]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13536": {"label": 8, "data": {"text": "Mammalian cysteine dioxygenase (CDO) is a non-heme iron metalloenzyme that catalyzes the first committed step in oxidative cysteine catabolism.", "entity1": "CDO", "entity2": "cysteine", "span1": [32, 35], "span2": [123, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10065": {"label": 3, "data": {"text": "Advances in antihypertensive combination therapy: benefits of low-dose thiazide diuretics in conjunction with omapatrilat, a vasopeptidase inhibitor.", "entity1": "vasopeptidase", "entity2": "omapatrilat", "span1": [125, 138], "span2": [110, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7806": {"label": 2, "data": {"text": "RSV targets and activates the NAD(+)-dependent protein deacetylase SIRT1; in turn, SIRT1 induces an intracellular antioxidative mechanism by inducing mitochondrial superoxide dismutase (SOD2).", "entity1": "SIRT1", "entity2": "RSV", "span1": [83, 88], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12895": {"label": 2, "data": {"text": "Both H(2)S solution prepared by bubbling pure H(2)S gas and NaSH, a H(2)S donor, dose dependently induced HO-1 expression through the activation of the extracellular signal-regulated kinase (ERK).", "entity1": "ERK", "entity2": "H(2)S", "span1": [191, 194], "span2": [5, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14": {"label": 3, "data": {"text": "These results suggest that prostacyclin may play a role in downregulating tissue factor expression in monocytes, at least in part via elevation of intracellular levels of cyclic AMP.", "entity1": "tissue factor", "entity2": "cyclic AMP", "span1": [74, 87], "span2": [171, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"745": {"label": 3, "data": {"text": "We report here that lovastatin, a drug clinically used for lowering cholesterol levels, inhibits the interaction of human LFA-1 with its counter-receptor intercellular adhesion molecule-1.", "entity1": "human LFA-1", "entity2": "lovastatin", "span1": [116, 127], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10970": {"label": 1, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "nuclear receptors", "entity2": "retinoic acid", "span1": [55, 72], "span2": [77, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10231": {"label": 9, "data": {"text": "Substrate specificity using lysates of oxidase-transfected HEK-293 cells revealed that the newly identified oxidase strongly favoured spermine over N (1)-acetylspermine and that it failed to act on N (1)-acetylspermidine, spermidine or the preferred PAO substrate, N (1), N (12)-diacetylspermine.", "entity1": "oxidase", "entity2": "N (1)-acetylspermidine", "span1": [108, 115], "span2": [198, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8433": {"label": 1, "data": {"text": "The endogenous steroid lithocholic acid (LCA) dilates cerebral arteries via BK channel activation, which requires recognition by a BK \u03b21 site that includes Thr169.", "entity1": "BK \u03b21", "entity2": "LCA", "span1": [131, 136], "span2": [41, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8031": {"label": 2, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [95, 100], "span2": [219, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"295": {"label": 3, "data": {"text": "In catalytic properties, mouse CA V is closest to CA I; however, in inhibition by acetazolamide, ethoxzolamide, and cyanate, CA V is very similar to CA II.", "entity1": "CA V", "entity2": "ethoxzolamide", "span1": [125, 129], "span2": [97, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4981": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "cytochrome c", "entity2": "Crocin", "span1": [206, 218], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5251": {"label": 3, "data": {"text": "Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38\u03b1 inhibitor.", "entity1": "p38\u03b1", "entity2": "BMS-582949", "span1": [89, 93], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8121": {"label": 3, "data": {"text": "Both CE and E(2) alone increased DNA synthesis and reduced apoptosis with activation of MAPK, Akt, and p70S6K and up-regulation of antiapoptotic factors survivin, Bcl-2, and X-linked inhibitor of apoptosis protein, These effects could be completely blocked by BZA.", "entity1": "Akt", "entity2": "BZA", "span1": [94, 97], "span2": [260, 263]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4293": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B3", "entity2": "estrone 3-sulfate", "span1": [269, 276], "span2": [71, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6025": {"label": 3, "data": {"text": "Aspirin irreversibly inhibits PGHS-1, preventing this isozyme from forming PGH2 or any other oxygenated product; in contrast, aspirin treatment of PGHS-2 causes this enzyme to form 15-hydroxy-5c,8c,11c,13t-eicosatetraenoic acid (15-HETE) instead of PGH2.", "entity1": "PGHS-1", "entity2": "Aspirin", "span1": [30, 36], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4900": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "sulfatase", "entity2": "Br", "span1": [162, 171], "span2": [106, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12724": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "butyrylcholinesterase", "entity2": "acetylcholine", "span1": [68, 89], "span2": [150, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14618": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "DCK", "entity2": "2',2'-difluorodeoxyuridine", "span1": [66, 69], "span2": [255, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5814": {"label": 9, "data": {"text": "In six patients with Cushing's disease and one patient with secondary adrenal insufficiency due to hypothalamic failure, neither basal ACTH and cortisol levels nor CRH-stimulated levels were influenced by loperamide.", "entity1": "CRH", "entity2": "loperamide", "span1": [164, 167], "span2": [205, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10827": {"label": 9, "data": {"text": "The reported mechanism of imatinib resistance in GISTs involves missense mutation in the kinase domain of KIT, including Thr670Ile, Tyr823Asp, and Val654Ala.", "entity1": "kinase domain", "entity2": "imatinib", "span1": [89, 102], "span2": [26, 34]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6453": {"label": 3, "data": {"text": "CONCLUSIONS: After the initial bleach, halothane impeded photon absorption by rhodopsin by inhibiting metabolic rhodopsin regeneration.", "entity1": "rhodopsin", "entity2": "halothane", "span1": [112, 121], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6819": {"label": 2, "data": {"text": "Each statin induced apoA-I expression (mRNA and protein) dose-dependently: the rank order of the apoA-I induction pitavastatin (3 microM)>simvastatin (10 microM)>atorvastatin (30 microM).", "entity1": "apoA-I", "entity2": "simvastatin", "span1": [97, 103], "span2": [138, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12991": {"label": 1, "data": {"text": "The main molecular target of azole antifungals is the cytochrome P-450 protein Erg11p/Cyp51p.", "entity1": "Cyp51p", "entity2": "azole", "span1": [86, 92], "span2": [29, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11453": {"label": 1, "data": {"text": "In contrast, analogs with different para-substituents on the phenyl ring had significantly different potencies for wild-type hERG block.", "entity1": "hERG", "entity2": "phenyl", "span1": [125, 129], "span2": [61, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3492": {"label": 2, "data": {"text": "In the CCl4 hepatotoxicity model, pre-treatment with PSM or silymarin resulted in significantly increased activities of ethylmorphine-N-demethylase and aniline 4-hydroxylase activity and cytochrome P450, compared to the CCl4 only group.", "entity1": "aniline 4-hydroxylase", "entity2": "CCl4", "span1": [152, 173], "span2": [220, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9309": {"label": 4, "data": {"text": "The enhancement of the depolarizing afterpotential by histamine was mimicked by the histamine H1-receptor agonist 2-thiazolylethylamine and was reduced or blocked by the H1-receptor antagonist promethazine, but was not blocked or reduced in the presence of the histamine H2-receptor antagonist, cimetidine.", "entity1": "histamine H1-receptor", "entity2": "2-thiazolylethylamine", "span1": [84, 105], "span2": [114, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4092": {"label": 2, "data": {"text": "The upregulation of calpain, tBid and caspase-3 activity were further inhibited by treatment with EGTA in the presence of ALD.", "entity1": "tBid", "entity2": "ALD", "span1": [29, 33], "span2": [122, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9640": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "AR", "entity2": "bicalutamide", "span1": [66, 68], "span2": [102, 114]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13802": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "Bcr", "entity2": "Gleevec", "span1": [114, 117], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2999": {"label": 1, "data": {"text": "The molecular bases for phosphodiesterase 5 (PDE5) catalytic-site affinity for cyclic guanosine monophosphate (cGMP) and potency of inhibitors are poorly understood.", "entity1": "phosphodiesterase 5", "entity2": "cyclic guanosine monophosphate", "span1": [24, 43], "span2": [79, 109]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"220": {"label": 1, "data": {"text": "Norethisterone metabolites modulate the uteroglobin and progesterone receptor gene expression in prepubertal rabbits.", "entity1": "progesterone receptor", "entity2": "Norethisterone", "span1": [56, 77], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11704": {"label": 2, "data": {"text": "The results showed that wogonoside promotes the expression of LC3-II and Beclin-1.", "entity1": "Beclin-1", "entity2": "wogonoside", "span1": [73, 81], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9828": {"label": 3, "data": {"text": "Through demonstrating the selective inhibition of kinase-related T-lymphocyte responses by geldanamycin, our results emphasize the substantial role of Hsp90-kinase complexes in T-cell activation.", "entity1": "kinase", "entity2": "geldanamycin", "span1": [50, 56], "span2": [91, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13075": {"label": 8, "data": {"text": "Methylthioadenosine phosphorylase (MTAP) salvages purines by releasing adenine from methylthioadenosine and is often deleted in mesothelioma.", "entity1": "Methylthioadenosine phosphorylase", "entity2": "adenine", "span1": [0, 33], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10552": {"label": 2, "data": {"text": "In sum the results of the present study indicate that RA-induced expression of blr1 expression depends on a novel RA response element.", "entity1": "blr1", "entity2": "RA", "span1": [79, 83], "span2": [54, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11289": {"label": 8, "data": {"text": "Firstly, transgenic plants overexpressing formate dehydrogenase (FDH, EC 1.2.1.2) were used to continue our previous studies on the function of FDH in formate metabolism.", "entity1": "FDH", "entity2": "formate", "span1": [65, 68], "span2": [151, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6272": {"label": 3, "data": {"text": "In addition, when candesartan was given to conscious rats, the inhibitory effect on Ang II-induced blood pressure responses persisted during the 24-hour period despite nondetectable plasma concentrations of candesartan at 24 hours.", "entity1": "Ang II", "entity2": "candesartan", "span1": [84, 90], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"252": {"label": 3, "data": {"text": "The competitive inhibitor of hCOX-1, mefenamic acid, also displayed competitive inhibition of hCOX-2.", "entity1": "hCOX-1", "entity2": "mefenamic acid", "span1": [29, 35], "span2": [37, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8133": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "BDNF", "entity2": "Sal", "span1": [123, 127], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13288": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "receptor tyrosine kinases", "entity2": "BAY43-9006", "span1": [168, 193], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5144": {"label": 9, "data": {"text": "However, we show that hCTR1 is not the major entry route of platinum-drugs and that the copper transporter is not internalized in response to extracellular drug.", "entity1": "hCTR1", "entity2": "platinum", "span1": [22, 27], "span2": [60, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"3846": {"label": 1, "data": {"text": "Using the viral mimic polyinosinic:polycytidylic acid and the IFN\u03b1/\u03b2 antagonist B18R we furthermore demonstrate the capability of endogenous IFN to promote IL-22-induced STAT1 activation and expression of CXCL10.", "entity1": "IFN", "entity2": "polyinosinic:polycytidylic acid", "span1": [141, 144], "span2": [22, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9414": {"label": 4, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT1", "entity2": "benzamide", "span1": [152, 157], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"16071": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "BTK", "entity2": "Ibrutinib", "span1": [191, 194], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3331": {"label": 3, "data": {"text": "MXF or VP-16 slightly affected cellular topo II activity in nuclear extracts derived from drug-treated cells while the combination enhanced inhibitory activity and the reduction in band depletion of topo II.", "entity1": "topo II", "entity2": "MXF", "span1": [199, 206], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"514": {"label": 4, "data": {"text": "Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine.", "entity1": "5HT1B/1D", "entity2": "zolmitriptan", "span1": [104, 112], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13381": {"label": 2, "data": {"text": "Monosodium urate crystals stimulate monocytes and macrophages to release IL-1beta through the NALP3 component of the inflammasome.", "entity1": "IL-1beta", "entity2": "Monosodium urate", "span1": [73, 81], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6256": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "norepinephrine transporter", "entity2": "chlorprothixene", "span1": [182, 208], "span2": [236, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8421": {"label": 3, "data": {"text": "A one-pot domino synthesis and discovery of highly functionalized dihydrobenzo[b]thiophenes as AChE inhibitors.", "entity1": "AChE", "entity2": "dihydrobenzo[b]thiophenes", "span1": [95, 99], "span2": [66, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1161": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "mitiglinide", "span1": [161, 165], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2484": {"label": 9, "data": {"text": "To address this issue and taking into account that effects of synthetic progestins are not only referable to action through the progesterone receptor but may also be mediated by other steroid receptors, we characterized cardiovascular function and inflammatory gene expression in aldosterone salt-treated rats on long-term administration of 17beta-estradiol, medroxyprogesterone acetate, and drospirenone, a new progestogen exhibiting antimineralocorticoid activity.", "entity1": "progesterone receptor", "entity2": "progestins", "span1": [128, 149], "span2": [72, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12085": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase", "entity2": "androst-5-ene-3 beta, 17 beta-diol", "span1": [0, 72], "span2": [224, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"185": {"label": 5, "data": {"text": "Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels.", "entity1": "histamine H1-receptor", "entity2": "Astemizole", "span1": [21, 42], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10291": {"label": 1, "data": {"text": "These differences from the horse might be the result of: (a) the presence in equine biological fluids of higher concentrations than in calves of the active PBZ metabolite, OPBZ; (b) a greater degree of binding of PBZ to plasma protein in calves; (c) species differences in the sensitivity to PBZ of the cyclo-oxygenase (COX) isoenzymes, COX-1 and COX-2 or; (d) a combination of these factors.", "entity1": "COX-1", "entity2": "PBZ", "span1": [337, 342], "span2": [292, 295]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12103": {"label": 3, "data": {"text": "HERG/IKr channels are a prime target for the pharmacological management of arrhythmias and are selectively blocked by class III antiarrhythmic methanesulfonanilide drugs, such as dofetilide, E4031, and MK-499, at submicromolar concentrations.", "entity1": "HERG", "entity2": "E4031", "span1": [0, 4], "span2": [191, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7494": {"label": 3, "data": {"text": "Phenserine deserves attention for an additional quality of action: in addition to inhibiting AChE, it modulates the amount of beta-amyloid precursor protein (APP) in neuronal cell culture by reducing APP translation.", "entity1": "AChE", "entity2": "Phenserine", "span1": [93, 97], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12864": {"label": 9, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "phosphatidic acid", "span1": [13, 19], "span2": [101, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10080": {"label": 8, "data": {"text": "The specific activity of only ornithine aminotransferase (OAT), the rate-limiting enzyme in the conversion of ornithine to proline, increased in 2 weeks of hypertrophy.", "entity1": "ornithine aminotransferase", "entity2": "proline", "span1": [30, 56], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"999": {"label": 8, "data": {"text": "The frdA gene coding for subunit A of FRD, and two control genes, copA and copP associated with the export of copper out of H. pylori, were inactivated by insertion of the chloramphenicol acetyltransferase cassette into these individual genes.", "entity1": "copA", "entity2": "copper", "span1": [66, 70], "span2": [110, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12533": {"label": 1, "data": {"text": "Adenosine analogs in particular the N6-substituted compounds are more potent at A1 receptors than at A2 receptors.", "entity1": "A1 receptors", "entity2": "Adenosine", "span1": [80, 92], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8012": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "FXa", "entity2": "hyperoside", "span1": [131, 134], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9112": {"label": 9, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c. The irreversible complex between phenoxybenzamine and calmodulin may be useful for inhibiting certain calmodulin-dependent reactions and for studying the various biological functions of calmodulin.", "entity1": "bovine serum albumin", "entity2": "phenoxybenzamine", "span1": [98, 118], "span2": [13, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15295": {"label": 3, "data": {"text": "Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.", "entity1": "FVIIa", "entity2": "bicyclic pyrazinone and pyrimidinone amides", "span1": [81, 86], "span2": [24, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7449": {"label": 1, "data": {"text": "Female mice express higher levels of glutaredoxin in certain CNS regions and downregulation of glutaredoxin using antisense oligonucleotides sensitizes them to L-BOAA toxicity seen as mitochondrial complex I loss.", "entity1": "glutaredoxin", "entity2": "L-BOAA", "span1": [95, 107], "span2": [160, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12552": {"label": 1, "data": {"text": "Intracellular protein-bound [57Co]Cbl fractionated with methionine synthase (MS) and methylmalonyl-CoA mutase (MU) activity.", "entity1": "MS", "entity2": "[57Co]Cbl", "span1": [77, 79], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"751": {"label": 5, "data": {"text": "The inhibitory effect of endothelin-1 on the contraction induced by 5-HT is abolished by deendothelialization, by the endothelin ET(B) receptor antagonist RES 701-1, by indomethacin, or by glibenclamide.", "entity1": "endothelin ET(B) receptor", "entity2": "RES 701-1", "span1": [118, 143], "span2": [155, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12469": {"label": 3, "data": {"text": "Arsenic deregulates the autophagic pathway through blockage of autophagic flux, resulting in accumulation of autophagosomes and sequestration of p62, Keap1, and LC3.", "entity1": "p62", "entity2": "Arsenic", "span1": [145, 148], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10316": {"label": 1, "data": {"text": "Results indicate that imiquimod and resiquimod induce IFN-alpha and IFN-omega from purified pDC, and pDC are the principle IFN-producing cells in the blood.", "entity1": "IFN", "entity2": "imiquimod", "span1": [123, 126], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6207": {"label": 1, "data": {"text": "Furthermore, since they have equipotent anticonvulsant effects and similar binding affinities to sigma-1 receptors, the very low affinity of DF at PCP sites may suggest that acting on the PCP sites may not be the requisite for mediating the anticonvulsant activity of these DM analogs.", "entity1": "sigma-1 receptors", "entity2": "PCP", "span1": [97, 114], "span2": [147, 150]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11108": {"label": 1, "data": {"text": "Two migraine patients were studied by in vivo SPECT using the dopamine D2-receptor specific radioligand 123I-3-iodo-6-methoxybenzamide (123I-IBZM) during ergotamine abuse and after withdrawal.", "entity1": "dopamine D2-receptor", "entity2": "123I-3-iodo-6-methoxybenzamide", "span1": [62, 82], "span2": [104, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12708": {"label": 1, "data": {"text": "However, when coapplied with 10 micro m GABA, ivermectin potentiated the GABA-evoked current of the GAB-1/HG1A receptor, but attenuated the GABA response of the GAB-1/HG1E receptor.", "entity1": "HG1E", "entity2": "GABA", "span1": [167, 171], "span2": [140, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3478": {"label": 6, "data": {"text": "Herein, we report the pharmacological actions of Lu AF21934, a novel, selective, and brain-penetrant positive allosteric modulator (PAM) of the mGlu(4) receptor in the stress-induced hyperthermia (SIH), four-plate, marble-burying and Vogel's conflict tests.", "entity1": "mGlu(4)", "entity2": "Lu AF21934", "span1": [144, 151], "span2": [49, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"2288": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "17-phenyl trinor PGE2", "span1": [74, 77], "span2": [96, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8051": {"label": 2, "data": {"text": "In this current study, paclitaxel was found to increase phosphorylation of mitogen-activated protein kinase (MAPK) kinase 3/6 (MKK3/6)-p38 MAPK as well as protein and mRNA levels of ERCC1 in H1650 and H1703 cells.", "entity1": "MAPK", "entity2": "paclitaxel", "span1": [139, 143], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9451": {"label": 1, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP2", "entity2": "AH-6809", "span1": [90, 93], "span2": [64, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8373": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "Akt", "entity2": "BPA", "span1": [69, 72], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12466": {"label": 1, "data": {"text": "The DPYD-Y186C variant was unique to individuals of African ancestry, and DPD activity was 46% lower in carriers as compared with noncarriers (279\u2009\u00b1\u200935 vs. 514\u2009\u00b1\u2009168 pmol 5-FU min(-1) mg(-1); P = 0.00029).", "entity1": "DPYD", "entity2": "5-FU", "span1": [4, 8], "span2": [171, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6452": {"label": 1, "data": {"text": "Consequently, photoreceptors of mice and rats anesthetized with halothane were completely protected against degeneration induced by white light.", "entity1": "photoreceptors", "entity2": "halothane", "span1": [14, 28], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3604": {"label": 3, "data": {"text": "At a low pH (pH 7.4), but not pH 7.9, ifenprodil reduces the mean open time of GluN1/GluN2B receptors, which may be responsible for its usefulness as a context-dependent inhibitor in conditions like ischemia and stroke, when the pH of the extracellular milieu becomes acidic.", "entity1": "GluN1", "entity2": "ifenprodil", "span1": [79, 84], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12427": {"label": 0, "data": {"text": "Studies mainly in osteoporosis rodent models and limited data in postmenopausal women suggest that N-terminal PTHrP peptides might be considered a promising bone anabolic therapy.", "entity1": "PTHrP", "entity2": "N", "span1": [110, 115], "span2": [99, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2716": {"label": 3, "data": {"text": "Parathion is a cholinesterase inhibitor that induces the hydrolysis of body choline esters, including acetylcholine at cholinergic synapses.", "entity1": "cholinesterase", "entity2": "Parathion", "span1": [15, 29], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9859": {"label": 6, "data": {"text": "It is concluded that salicylates are allosteric inhibitors of ETA receptors.", "entity1": "ETA receptors", "entity2": "salicylates", "span1": [62, 75], "span2": [21, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"15728": {"label": 4, "data": {"text": "Most parabens showing estrogenic activity exhibited ER\u03b2-agonistic activity at lower concentrations than those inducing ER\u03b1-agonistic activity.", "entity1": "ER\u03b1", "entity2": "parabens", "span1": [119, 122], "span2": [5, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8197": {"label": 3, "data": {"text": "The pro-hypertrophic co-activator p300 protein but not p300 mRNA was up-regulated in the mdx heart, and resveratrol administration down-regulated the p300 protein level.", "entity1": "p300", "entity2": "resveratrol", "span1": [150, 154], "span2": [104, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2934": {"label": 7, "data": {"text": "Adenylosuccinate synthetase (AdSS) catalyzes the Mg2+ dependent condensation of a molecule of IMP with aspartate to form adenylosuccinate, in a reaction driven by the hydrolysis of GTP to GDP.", "entity1": "Adenylosuccinate synthetase", "entity2": "Mg2+", "span1": [0, 27], "span2": [49, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15019": {"label": 3, "data": {"text": "Interestingly, AdOx disrupted actin cytoskeleton structures, leading to morphological changes, and suppressed the formation of a signaling complex composed of Src and p85/PI3K, which is linked to various tumorigenic responses.", "entity1": "PI3K", "entity2": "AdOx", "span1": [171, 175], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12203": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D5D", "entity2": "alpha-linolenic acid", "span1": [290, 293], "span2": [228, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13330": {"label": 3, "data": {"text": "Salicylates, in doses administrated in our experiments, inhibited NF-kappaB and perhaps other transcription factors in the retina, were well tolerated, and offered new tools to investigate and inhibit the development of diabetic retinopathy.", "entity1": "NF-kappa", "entity2": "Salicylates", "span1": [66, 74], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5315": {"label": 3, "data": {"text": "A series of phosphorylated flavonoids were synthesized and investigated in\u00a0vitro as inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE).", "entity1": "CEase", "entity2": "phosphorylated flavonoids", "span1": [131, 136], "span2": [12, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"284": {"label": 4, "data": {"text": "Eight normal males received single oral doses of BRL35135 8 mg (BRL) or the selective beta 2-adrenoceptor agonist salbutamol 8 mg (SAL), after pretreatment with either placebo (PL), bisoprolol 5 mg (B5) as a selective beta 1-adrenoceptor antagonist, or nadolol 20 mg (N20) to block beta 1- and beta 2- but not beta 3-receptors.", "entity1": "beta 2-adrenoceptor", "entity2": "SAL", "span1": [86, 105], "span2": [131, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2426": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "constitutive nitric-oxide synthase", "entity2": "L-arginine", "span1": [164, 198], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9829": {"label": 3, "data": {"text": "Improper function of these proteins can be induced by selective disruption of their complexes with Hsp90 using the benzoquinonoid ansamycin geldanamycin.", "entity1": "Hsp90", "entity2": "benzoquinonoid ansamycin", "span1": [99, 104], "span2": [115, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6500": {"label": 3, "data": {"text": "Pemetrexed disodium (ALIMTA) is a novel antimetabolite that inhibits at least three folate-dependent enzymes, thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase.", "entity1": "thymidylate synthase", "entity2": "Pemetrexed disodium", "span1": [110, 130], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4594": {"label": 3, "data": {"text": "This work resulted in the discovery of the 5-morpholino-7H-thieno[3,2-b]pyran-7-one system as the foundation of a new compound class of potential PI3K inhibitors having improved potency toward PI3K.", "entity1": "PI3K", "entity2": "5-morpholino-7H-thieno[3,2-b]pyran-7-one", "span1": [193, 197], "span2": [43, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2188": {"label": 7, "data": {"text": "In this work, we utilized magnetic circular dichroism spectroscopy to explore how the electronic structure of the reduced B12 cofactor (i.e., the post-homolysis product Co2+ Cbl) is modulated by the enzyme methylmalonyl-CoA mutase.", "entity1": "methylmalonyl-CoA mutase", "entity2": "Co2+ Cbl", "span1": [206, 230], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, 7, -1, -1, -1, 8, -1, -1]},
	"6987": {"label": 3, "data": {"text": "RATIONALE: Several drugs used to treat bipolar disorder (lithium and carbamazepine), when administered chronically to rats, reduce the turnover of arachidonic acid, but not docosahexaenoic acid, in brain phospholipids by decreasing the activity of an arachidonic acid-selective phospholipase A(2).", "entity1": "phospholipase A(2)", "entity2": "lithium", "span1": [278, 296], "span2": [57, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6044": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2C", "entity2": "SCH 23390", "span1": [73, 79], "span2": [157, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8983": {"label": 1, "data": {"text": "The smooth muscle relaxant, W-7, which is believed relatively specific in inhibiting the Ca2(+)-calmodulin interaction, depressed hyposmolarity-induced PRL secretion in a dose-dependent manner (r = -0.991, p less than 0.01).", "entity1": "calmodulin", "entity2": "Ca2(+)", "span1": [96, 106], "span2": [89, 95]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5841": {"label": 9, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT3", "entity2": "ondansetron", "span1": [5, 10], "span2": [120, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13567": {"label": 1, "data": {"text": "A humanized antibody to HER2/neu, trastuzumab, is now FDA approved for the treatment of early stage, HER2/neu overexpressing breast cancer sequenced with chemotherapy including doxorubicin, cyclophosphamide, and paclitaxel.", "entity1": "HER2", "entity2": "doxorubicin", "span1": [101, 105], "span2": [177, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4700": {"label": 2, "data": {"text": "V(5+) also increased serum hemoglobin (Hb) levels in animals treated for 24\u00a0h. Upon treatment of isolated hepatocytes with Hb alone or in the presence of TCDD, there was an increase in the AhR-dependent luciferase activity.", "entity1": "Hb", "entity2": "V(5+)", "span1": [39, 41], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11924": {"label": 1, "data": {"text": "Oxysterols interfere with ERK, hedgehog and wnt pathways of proliferation and differentiation.", "entity1": "ERK", "entity2": "Oxysterols", "span1": [26, 29], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4782": {"label": 3, "data": {"text": "Concentration-dependent inhibitory effects of baicalin on the metabolism of dextromethorphan, a dual probe of CYP2D and CYP3A, in rats.", "entity1": "CYP3A", "entity2": "baicalin", "span1": [120, 125], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"947": {"label": 3, "data": {"text": "Endogenously produced asymmetrically methylated arginine residues are competitive inhibitors of all three isoforms of nitric oxide synthase (NOS).", "entity1": "NOS", "entity2": "arginine", "span1": [141, 144], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8595": {"label": 2, "data": {"text": "Further, both the flavonoids were also found to increase the expression of some of the prominent markers for differentiation of osteoblast like osteopontin, osterix, RunX2, osteoprotegerin and osteocalcin.", "entity1": "osterix", "entity2": "flavonoids", "span1": [157, 164], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8903": {"label": 3, "data": {"text": "The identity of the lung beta-ADHs was further demonstrated by their characteristic pH-activity profiles for ethanol oxidation, Km values for NAD and ethanol, and inhibition by 4-methylpyrazole or 1,10-phenanthroline.", "entity1": "beta-ADHs", "entity2": "1,10-phenanthroline", "span1": [25, 34], "span2": [197, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6039": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "Ru 24969", "span1": [63, 69], "span2": [136, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5588": {"label": 3, "data": {"text": "5-FU interferes with DNA synthesis by blocking thymidylate synthase (TS) but is inactivated by dihydropyrimidine dehydrogenase (DPD).", "entity1": "thymidylate synthase", "entity2": "5-FU", "span1": [47, 67], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3708": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "caspase-9", "entity2": "BPs", "span1": [144, 153], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2503": {"label": 3, "data": {"text": "Chronic insulin (24 h) activates NHE3 through the classic phosphatidylinositol 3-kinase-serum- and glucocorticoid-dependent kinase 1 (PI3K-SGK1) pathway as insulin stimulates SGK1 phosphorylation and the insulin effect can be blocked by the PI3K inhibitor wortmannin or a dominant-negative SGK1.", "entity1": "PI3K", "entity2": "wortmannin", "span1": [134, 138], "span2": [256, 266]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4006": {"label": 1, "data": {"text": "Here, we leveraged protein engineering to modify the PK characteristics of the native molecule by fusing FST315 to a murine IgG(1) Fc and removing the intrinsic heparan sulfate-binding activity of follistatin.", "entity1": "follistatin", "entity2": "sulfate", "span1": [197, 208], "span2": [169, 176]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12684": {"label": 1, "data": {"text": "Different forms of therapy, potassium and magnesium substitution, spironolactone and indomethacin failed to fully correct hypokalemia and hypomagnesemia, but markedly improved growth velocity and normalized IGF-I levels in the three patients with short stature.", "entity1": "IGF-I", "entity2": "spironolactone", "span1": [207, 212], "span2": [66, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1242": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "beclomethasone", "span1": [115, 118], "span2": [43, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15742": {"label": 1, "data": {"text": "E-cadherin is a transmembrane glycoprotein that mediates calcium-dependent interactions between adjacent epithelial cells.", "entity1": "E-cadherin", "entity2": "calcium", "span1": [0, 10], "span2": [57, 64]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5681": {"label": 3, "data": {"text": "HZ mice are also more sensitive to the peripheral application of the selective AChE inhibitor donepezil or the mixed inhibitor physostigmine; extracellular ACh levels rise significantly after administration of both drugs; also glucose levels are moderately increased indicating potentially non-cholinergic effects of donepezil.", "entity1": "AChE", "entity2": "donepezil", "span1": [79, 83], "span2": [94, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12540": {"label": 1, "data": {"text": "Adducts of calmodulin and phenoxybenzamine were separated by high-performance liquid chromatography into four major fractions: two containing 0.6 and 1.2 mol of drug per mol of protein and two different fractions each containing 2.0 mol/mol.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [11, 21], "span2": [26, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6839": {"label": 1, "data": {"text": "However, MS A2756G was significantly associated with cobalamin levels (AA genotype: 290 +/- 122 pmol/l; AG: 381 +/- 151 pmol/l and GG: 415 +/- 100 pmol/l), as was MTRR A66G (AA: 478 +/- 219 pmol/l, AG: 306 +/- 124 pmol/l and GG: 306 +/- 123 pmol/l).", "entity1": "A2756G", "entity2": "cobalamin", "span1": [12, 18], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2587": {"label": 8, "data": {"text": "Methionine synthase reductase (MTRR) is an enzyme involved in the conversion of Hcy to methionine.", "entity1": "Methionine synthase reductase", "entity2": "Hcy", "span1": [0, 29], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12718": {"label": 1, "data": {"text": "Yohimbine dimers exhibiting selectivity for the human alpha 2C-adrenoceptor subtype.", "entity1": "human alpha 2C-adrenoceptor", "entity2": "Yohimbine", "span1": [48, 75], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7098": {"label": 8, "data": {"text": "Proline oxidase (POX), a mitochondrial inner-membrane protein, catalyzes the rate-limiting oxidation of proline to pyrroline- 5-carboxylate (P5C).", "entity1": "Proline oxidase", "entity2": "P5C", "span1": [0, 15], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13406": {"label": 3, "data": {"text": "Histamine H(1) blockade is one of the more prominent actions of the multi-receptor acting antipsychotic clozapine.", "entity1": "Histamine H(1)", "entity2": "clozapine", "span1": [0, 14], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8751": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "amitriptyline", "span1": [178, 184], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7111": {"label": 1, "data": {"text": "The selective ER modulator (SERM) tamoxifen has been in use for the treatment of advanced breast cancer for more than 30 years and is currently a treatment option for all stages of ER-positive disease.", "entity1": "ER", "entity2": "tamoxifen", "span1": [14, 16], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6493": {"label": 5, "data": {"text": "Schild analyses for the antagonists against brimonidine yielded regression lines with slopes of unity and functional antagonist potencies (pK(B)) for BRL44408 (7.8), ARC 239 (5.8) and for prazosin (6.0) suggesting the presence of functional alpha(2A)-adrenoceptors.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "ARC 239", "span1": [241, 264], "span2": [166, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6484": {"label": 4, "data": {"text": "CONCLUSIONS: The alpha(2)-adrenoceptor agonists brimonidine, apraclonidine, and oxymetazoline are potent vasoconstrictors in the porcine ciliary artery.", "entity1": "alpha(2)-adrenoceptor", "entity2": "apraclonidine", "span1": [17, 38], "span2": [61, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3141": {"label": 1, "data": {"text": "We report here that amitriptyline, an antidepressant drug, directly binds TrkA and TrkB and triggers their dimerization and activation.", "entity1": "TrkB", "entity2": "amitriptyline", "span1": [83, 87], "span2": [20, 33]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6122": {"label": 8, "data": {"text": "The results when considered with previous reports in the literature show that amezinium is about 1000 times more potent and debrisoquine is about 20 times more potent for MAO inhibition in rat lungs than in tissue homogenates, and the reason for their high potencies in the intact lungs is transport and accumulation of the drugs in the pulmonary endothelial cells by uptake1.", "entity1": "uptake1", "entity2": "debrisoquine", "span1": [368, 375], "span2": [124, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2215": {"label": 3, "data": {"text": "A dose of 25 microg kg(-1) day(-1) of formoterol elicited greater EDL and soleus hypertrophy than salmeterol, but resulted in similar beta-adrenoceptor downregulation.", "entity1": "beta-adrenoceptor", "entity2": "formoterol", "span1": [134, 151], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2161": {"label": 3, "data": {"text": "These results demonstrated that thalidomide might inhibit growth of tumors through COX-2 degradation independent of antiangiogenesis.", "entity1": "COX-2", "entity2": "thalidomide", "span1": [83, 88], "span2": [32, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15392": {"label": 3, "data": {"text": "Discovery of 7-methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole (TASP0382088): a potent and selective transforming growth factor-\u03b2 type I receptor inhibitor as a topical drug for alopecia.", "entity1": "transforming growth factor-\u03b2 type I receptor", "entity2": "TASP0382088", "span1": [130, 174], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6641": {"label": 5, "data": {"text": "alpha(1A)-Adrenoceptor selective antagonists, 2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane (WB-4101; 0.1-1 mg/kg) and 5-methylurapidil (0.1-1 mg/kg), the alpha(1B)-adrenoceptor selective antagonist, 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765314; 0.3-1 mg/kg), as well as the alpha(1D)-adrenoceptor selective antagonist, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY-7378; 1 mg/kg), were used to delineate the adrenoceptor subtypes involved.", "entity1": "alpha(1D)-adrenoceptor", "entity2": "8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione", "span1": [371, 393], "span2": [416, 494]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"575": {"label": 2, "data": {"text": "Tomudex treatment resulted in the decrease in p27(kip1) expression, with an increase in cyclin E and cdk2 protein expression and kinase activities 24 h after a 2-h exposure.", "entity1": "cdk2", "entity2": "Tomudex", "span1": [101, 105], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1488": {"label": 3, "data": {"text": "Sulindac metabolites and other nonsteroidal anti-inflammatory drugs selectively inhibit ERK1/2 phosphorylation in human colon cancer cells.", "entity1": "ERK1/2", "entity2": "Sulindac", "span1": [88, 94], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7130": {"label": 1, "data": {"text": "GAF-B contributes to dimerization of PDE5, inhibition of cGMP binding to GAF-A, and sequestration of the phosphorylation site.", "entity1": "GAF-A", "entity2": "cGMP", "span1": [73, 78], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9952": {"label": 9, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-1", "entity2": "SC-58635", "span1": [180, 185], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11377": {"label": 8, "data": {"text": "Favorable enzyme profiles (high TP and low DPD) generate high intratumor levels of 5-FU that are effective against many tumors, especially those with low TS.", "entity1": "DPD", "entity2": "5-FU", "span1": [43, 46], "span2": [83, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2453": {"label": 1, "data": {"text": "CONCLUSION: The peptide sequences containing Tyr, Phe conservative residues identified in this study can bind to cell surface IL-2Ralpha.", "entity1": "IL-2Ralpha", "entity2": "Tyr", "span1": [126, 136], "span2": [45, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9": {"label": 9, "data": {"text": "The inhibitory effects of iloprost on tissue factor expression were also potentiated by isobutylmethylxanthine and mimicked by forskolin and dibutyryl cyclic AMP but not dibutyryl cyclic GMP.", "entity1": "tissue factor", "entity2": "dibutyryl cyclic GMP", "span1": [38, 51], "span2": [170, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1756": {"label": 3, "data": {"text": "GW572016, a reversible small molecule inhibitor of EGFR and ErbB2 tyrosine kinases, inhibits baseline p95ErbB2 phosphorylation in BT474 cells and tumor xenografts.", "entity1": "tyrosine kinases", "entity2": "GW572016", "span1": [66, 82], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10504": {"label": 3, "data": {"text": "Manipulation of kinetic profiles in 2-aryl propionic acid cyclooxygenase inhibitors.", "entity1": "cyclooxygenase", "entity2": "2-aryl propionic acid", "span1": [58, 72], "span2": [36, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2322": {"label": 1, "data": {"text": "Autoradiographic studies showed decreased binding of the beta-adrenergic ligand [3H]CGP12177 in the cerebral cortex of NET-/- mice, indicating the changes at the level of beta-adrenergic receptors similar to those obtained with ADs treatment.", "entity1": "beta-adrenergic receptors", "entity2": "[3H]CGP12177", "span1": [171, 196], "span2": [80, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8975": {"label": 5, "data": {"text": "The Schild plots for the competitive antagonists WB4101 and 5-methyl-urapidil against alpha 1a-adrenoceptor-selective agonist methoxamine-induced contraction were linear and had slopes not significantly different from unity, with a pA2 of 9.07 +/- 0.07 (n = 5) for WB4101 and 9.09 +/- 0.05 (n = 3) for 5-methyl-urapidil.", "entity1": "alpha 1a-adrenoceptor", "entity2": "WB4101", "span1": [86, 107], "span2": [49, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2350": {"label": 4, "data": {"text": "Effect of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide (ramelteon, TAK-375), a selective MT1/MT2 receptor agonist, on motor coordination was studied using rota-rod performance in mice.", "entity1": "MT1/MT2 receptor", "entity2": "ramelteon", "span1": [120, 136], "span2": [87, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6026": {"label": 8, "data": {"text": "Aspirin irreversibly inhibits PGHS-1, preventing this isozyme from forming PGH2 or any other oxygenated product; in contrast, aspirin treatment of PGHS-2 causes this enzyme to form 15-hydroxy-5c,8c,11c,13t-eicosatetraenoic acid (15-HETE) instead of PGH2.", "entity1": "PGHS-2", "entity2": "15-HETE", "span1": [147, 153], "span2": [229, 236]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2354": {"label": 4, "data": {"text": "Effect of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide (ramelteon, TAK-375), a selective MT1/MT2 receptor agonist, on motor coordination was studied using rota-rod performance in mice.", "entity1": "MT1/MT2 receptor", "entity2": "(S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide", "span1": [120, 136], "span2": [10, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10588": {"label": 8, "data": {"text": "BACKGROUND: To assess the sensitivity of biochemical, physiological, and pharmacological markers of peripheral norepinephrine (NE) transporter (NET) function, we chronically antagonized NET by a range of doses of duloxetine [(+)-N-methyl-3-(1-naphthalenyloxy)-2 thiophenepropanamine], which blocks the NE reuptake process.", "entity1": "NET", "entity2": "NE", "span1": [186, 189], "span2": [302, 304]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15098": {"label": 3, "data": {"text": "The addition of avibactam greatly (4-1024-fold minimum inhibitory concentration [MIC] reduction) improves the activity of ceftazidime versus most species of Enterobacteriaceae depending on the presence or absence of \u03b2-lactamase enzyme(s).", "entity1": "\u03b2-lactamase", "entity2": "avibactam", "span1": [216, 227], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15492": {"label": 0, "data": {"text": "We used whole-cell recordings of human embryonic kidney cells heterologously expressing either wild-type TRPA1 or TRPA1 with three serine-substituted cysteines crucial for electrophile activation (C621S, C641S, C665S).", "entity1": "TRPA1", "entity2": "cysteines", "span1": [114, 119], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1460": {"label": 3, "data": {"text": "), did not induce the behavioural hyperactivity syndrome which is seen following inhibition of both MAO-A and MAO-B by tranylcypromine together with the monoamine precursors.", "entity1": "MAO-A", "entity2": "monoamine", "span1": [100, 105], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1593": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "acetylcholinesterase", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine", "span1": [4, 24], "span2": [381, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15003": {"label": 3, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "cytokine", "entity2": "EPA", "span1": [123, 131], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11031": {"label": 3, "data": {"text": "Sorafenib, which belongs chemically to a class that can be described as bis-aryl ureas, was selected for further pharmacologic characterization based on potent inhibition of Raf-1 and its favorable kinase selectivity profile.", "entity1": "Raf-1", "entity2": "bis-aryl ureas", "span1": [174, 179], "span2": [72, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1207": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "vesicular monoamine transporter-2", "entity2": "amphetamines", "span1": [174, 207], "span2": [58, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7065": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARbeta", "entity2": "Am80", "span1": [52, 59], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8247": {"label": 0, "data": {"text": "N-terminal sequencing indicated that pro-BMP-2 was cleaved by FSAP at the canonical PC cleavage site, giving rise to mature BMP-2 (Arg(282)\u2193Gln(283)), as well as in the N-terminal heparin binding region of mature BMP-2, generating a truncated mature BMP-2 peptide (Arg(289)\u2193Lys(290)).", "entity1": "BMP-2", "entity2": "Arg", "span1": [250, 255], "span2": [265, 268]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14504": {"label": 2, "data": {"text": "Administration of low, but not high, doses of oral nicotine in DSS-treated mice resulted in a significant decrease in disease severity, histologic damage scores, as well as colonic level of tumor necrosis factor-\u03b1.", "entity1": "tumor necrosis factor-\u03b1", "entity2": "nicotine", "span1": [190, 213], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9084": {"label": 3, "data": {"text": "13cisRA and ROAc, but not 4HPR, caused a dose-dependent reduction in plasma osteocalcin, an effect that correlated with retinoid-induced bone effects.", "entity1": "osteocalcin", "entity2": "ROAc", "span1": [76, 87], "span2": [12, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13812": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "Erlotinib", "span1": [233, 246], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10901": {"label": 3, "data": {"text": "(R)-Roscovitine (CYC202, Seliciclib) is a relatively selective inhibitor of cyclin-dependent kinases (CDKs), currently evaluated for the treatment of cancers, neurodegenerative disorders, renal diseases, and several viral infections.", "entity1": "cyclin-dependent kinases", "entity2": "CYC202", "span1": [76, 100], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4285": {"label": 3, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "AMPK", "entity2": "MG132", "span1": [52, 56], "span2": [35, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12964": {"label": 0, "data": {"text": "The phosphorylation by gammaPKC resulted in activation of DGKgamma because a DGKgamma mutant in which Ser-776 and Ser-779 were substituted with glutamic acid to mimic phosphorylation exhibited significantly higher activity compared with wild type DGKgamma and an unphosphorylatable DGKgamma mutant.", "entity1": "DGKgamma", "entity2": "glutamic acid", "span1": [77, 85], "span2": [144, 157]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"71": {"label": 4, "data": {"text": "The recent development of H1-receptor antagonists devoid of clinical sedative effects has enabled the administration of doses of H1-antihistamines which achieve a greater degree of H1-receptor blockade within the airways, thus permitting a better appraisal of the role of histamine in this condition.", "entity1": "H1-receptor", "entity2": "histamine", "span1": [181, 192], "span2": [272, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1041": {"label": 1, "data": {"text": "Third, using ciprofloxacin competition assay, TOP2-mediated DNA cleavage induced by ATP-sensitive but not ATP-insensitive poisons was shown to be antagonized by ciprofloxacin.", "entity1": "TOP2", "entity2": "ciprofloxacin", "span1": [46, 50], "span2": [161, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15007": {"label": 1, "data": {"text": "In agreement with these data, the exogenous treatment of SAH or inhibition of SAHH by specific siRNA or another type of inhibitor, 3-deazaadenosine (DAZA), similarly resulted in antitumorigenic responses, suppressive activity on Src, the alteration of actin cytoskeleton, and a change of the colocalization pattern between actin and Src.", "entity1": "actin", "entity2": "SAH", "span1": [252, 257], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12507": {"label": 1, "data": {"text": "Among all the organophosphates tested, the combination of a methyl group and a negatively charged oxygen attached to the P atom, CH3P(O)(O-)-AChE, conferred the greatest protection to the active site of aged or nonaged organophosphoryl conjugates of acetylcholinesterase.", "entity1": "AChE", "entity2": "P", "span1": [141, 145], "span2": [121, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8534": {"label": 2, "data": {"text": "Besides, CDM not only synergized TNF-\u03b1 production combined with IFN-\u03b3, but also prolonged its expression in time.", "entity1": "IFN-\u03b3", "entity2": "CDM", "span1": [64, 69], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"318": {"label": 0, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "bovine pancreatic ribonuclease A", "entity2": "proline", "span1": [63, 95], "span2": [114, 121]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12636": {"label": 1, "data": {"text": "The sulfonylurea glibenclamide caused release of prebound 8-azido-[alpha-32P]ATP from SUR1 in the presence of MgADP or MgATP in a concentration-dependent manner.", "entity1": "SUR1", "entity2": "sulfonylurea glibenclamide", "span1": [86, 90], "span2": [4, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1643": {"label": 1, "data": {"text": "2-Amino-3-[3-hydroxy-5-(2-thiazolyl)-4-isoxazolyl]propionic acid (1) is a potent AMPA receptor agonist with moderate affinity for native kainic acid (KA) receptors, whereas (S)-E-4-(2,2-dimethylpropylidene)glutamic acid (3) show high affinity for the GluR5 subtype of KA receptors and much lower affinity for the GluR2 subtype of AMPA receptors.", "entity1": "AMPA receptors", "entity2": "(S)-E-4-(2,2-dimethylpropylidene)glutamic acid", "span1": [330, 344], "span2": [173, 219]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"743": {"label": 3, "data": {"text": "The kinase activity of EGFR was little inhibited by TT-B in a cell-free system.", "entity1": "EGFR", "entity2": "TT-B", "span1": [23, 27], "span2": [52, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8719": {"label": 3, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "Txnrd1", "entity2": "NaAsO2", "span1": [38, 44], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12449": {"label": 1, "data": {"text": "Meanwhile, the alterations of cyclin A and B1, p-CDK1 and p-cdc25c levels were also observed in response to DICO treatment.", "entity1": "p-CDK1", "entity2": "DICO", "span1": [47, 53], "span2": [108, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9230": {"label": 5, "data": {"text": "The histamine H2 receptor antagonist cimetidine blocked the FHA-HIS binding on 14-37% of the platelets.", "entity1": "histamine H2 receptor", "entity2": "cimetidine", "span1": [4, 25], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12393": {"label": 1, "data": {"text": "Androgen action is exerted through the androgen receptor.", "entity1": "androgen receptor", "entity2": "Androgen", "span1": [39, 56], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13579": {"label": 5, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "NMDA receptor", "entity2": "(5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine", "span1": [188, 201], "span2": [35, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"650": {"label": 1, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "metalloproteinase", "entity2": "captopril", "span1": [164, 181], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5397": {"label": 4, "data": {"text": "The use of A3 receptor agonist IB-MECA attenuates EAP.", "entity1": "A3 receptor", "entity2": "IB-MECA", "span1": [11, 22], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6851": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "methionine synthase reductase", "entity2": "Hcy", "span1": [177, 206], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3010": {"label": 1, "data": {"text": "Eprosartan acts at vascular AT1 receptors (postsynaptically) and at presynaptic AT1 receptors, where it inhibits noradrenaline release.", "entity1": "AT1 receptors", "entity2": "Eprosartan", "span1": [80, 93], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14028": {"label": 1, "data": {"text": "Our findings show evidence that eNOS polymorphisms affect the responses of PED and clinical ED patients to sildenafil.", "entity1": "eNOS", "entity2": "sildenafil", "span1": [32, 36], "span2": [107, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9349": {"label": 3, "data": {"text": "One group of experimental animals was treated with 5-lipoxygenase (5-LO) inhibitor, diethylcarbamazine (DEC, Sigma, St. Louis, Missouri) (50 mg/kg, i.v.", "entity1": "5-LO", "entity2": "DEC", "span1": [67, 71], "span2": [104, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12941": {"label": 8, "data": {"text": "L-arg is converted to urea by arginase I in the liver and arginase II in the kidney.", "entity1": "arginase I", "entity2": "L-arg", "span1": [30, 40], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5907": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "plasma very-low-density lipoproteins", "entity2": "probucol", "span1": [95, 131], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13595": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "NIS", "span1": [379, 383], "span2": [405, 408]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4582": {"label": 3, "data": {"text": "Moreover, co-treatment with antofine and a specific PKC\u03b2 inhibitor prevented endocytosis of gap junctions, downregulation of Cx43, and inhibition of GJIC.", "entity1": "Cx43", "entity2": "antofine", "span1": [125, 129], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2926": {"label": 8, "data": {"text": "The Na(+)/Ca(2+) exchanger (NCX) is a bidirectional transporter that normally extrudes Ca(2+) from the cell (forward mode), but also brings Ca(2+) into the cell (reverse mode) under special conditions such as intracellular Na(+) (Na(+)(i)) accumulation or membrane depolarization.", "entity1": "Na(+)/Ca(2+) exchanger", "entity2": "Ca(2+)", "span1": [4, 26], "span2": [140, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7358": {"label": 1, "data": {"text": "Moreover, ERalpha mediated the protection afforded by estrogen since only the ERalpha agonist, HPTE, but not the ERbeta agonist, DPN, protected against dopamine cell loss.", "entity1": "ERalpha", "entity2": "estrogen", "span1": [10, 17], "span2": [54, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1046": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "doxorubicin", "span1": [162, 166], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3555": {"label": 2, "data": {"text": "LTD4 also induced expression of cysteinyl leukotriene receptor 1 (CysLT(1)R) and NF-\u03baB p65 in the hippocampus and cortex.", "entity1": "NF-\u03baB", "entity2": "LTD4", "span1": [81, 86], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10718": {"label": 3, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "c-jun", "entity2": "Dimemorfan", "span1": [75, 80], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7336": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "sodium-coupled neutral amino acid transporter 1", "entity2": "glutamine", "span1": [274, 321], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1333": {"label": 1, "data": {"text": "Species-specific differences in the glucocorticoid receptor transactivation function upon binding with betamethasone-esters.", "entity1": "glucocorticoid receptor", "entity2": "betamethasone-esters", "span1": [36, 59], "span2": [103, 123]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12452": {"label": 0, "data": {"text": "C47 of GSTP1-1 is S-nitrosated in two steps, with the chemical step limited by a pre-equilibrium between the open and closed conformations of helix \u03b12 at the active site.", "entity1": "GSTP1-1", "entity2": "S", "span1": [7, 14], "span2": [18, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2944": {"label": 1, "data": {"text": "It is noteworthy that the binding of vardenafil causes loss of the divalent metal ions that have been observed in all the previously published PDE structures.", "entity1": "PDE", "entity2": "vardenafil", "span1": [143, 146], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4692": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "V(5+)", "span1": [123, 129], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7185": {"label": 2, "data": {"text": "CONCLUSION: Intake of high SFAs and MUFAs appears to increase expression of PBMC D6D and D5D genes, whilst high EFAs intake appears to decrease expression of PBMC D6D and D5D genes.", "entity1": "D5D", "entity2": "SFAs", "span1": [89, 92], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9546": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "GM-CSF", "entity2": "cyclic adenosine monophosphate", "span1": [58, 64], "span2": [172, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9097": {"label": 3, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "5-lipoxygenase", "entity2": "U-60,257", "span1": [194, 208], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4126": {"label": 0, "data": {"text": "The cellular prion protein PrP(C) consists of two domains--a flexible N-terminal domain, which participates in copper and zinc regulation, and a largely helical C-terminal domain that converts to \u03b2 sheet in the course of prion disease.", "entity1": "prion protein PrP(C)", "entity2": "N", "span1": [13, 33], "span2": [70, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15740": {"label": 3, "data": {"text": "Wattakaka volubilis steroidal glycoside mixture (WVSM) and PPG (1-50\u03bcM) significantly inhibited the COX-2 and iNOS enzymes resulting in low levels of PGE2 and NO in LPS-induced RAW 264.7 macrophage cells.", "entity1": "COX-2", "entity2": "PPG", "span1": [100, 105], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11805": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "c-fos", "entity2": "2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine", "span1": [124, 129], "span2": [11, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15938": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "glucagon", "entity2": "metformin", "span1": [126, 134], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1085": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "galanthamine", "span1": [242, 262], "span2": [146, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4266": {"label": 2, "data": {"text": "Interestingly, ursolic acid increased the phosphorylation of AMPK and coenzyme A carboxylase and also enhanced phosphorylation of GSK3\u03b2 at inactive form serine 9, whereas ursolic acid attenuated the phosphorylation of AKT and mTOR in HepG2 cells.", "entity1": "coenzyme A carboxylase", "entity2": "ursolic acid", "span1": [70, 92], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9031": {"label": 3, "data": {"text": "Mepindolol treatment (2 X 5 mg/day) caused a 30% decrease of beta 2-adrenoceptor density and PRA after 2 days; both parameters remained reduced during treatment.", "entity1": "beta 2-adrenoceptor", "entity2": "Mepindolol", "span1": [61, 80], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2929": {"label": 5, "data": {"text": "Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected].", "entity1": "vasopressin receptor v1a/v2", "entity2": "Conivaptan", "span1": [19, 46], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7690": {"label": 8, "data": {"text": "The low-affinity sodium glucose cotransporter (SGLT2) is responsible for most of the glucose reabsorption in the kidney and has been highlighted as a novel therapeutic target for the treatment of diabetes.", "entity1": "SGLT2", "entity2": "glucose", "span1": [47, 52], "span2": [85, 92]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7684": {"label": 3, "data": {"text": "Chronic treatment with sergliflozin etabonate reduced the levels of glycated hemoglobin and fasting plasma glucose, and improved the glycemic response after glucose loading in Zucker fatty rats.", "entity1": "glycated hemoglobin", "entity2": "sergliflozin etabonate", "span1": [68, 87], "span2": [23, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6002": {"label": 3, "data": {"text": "Sodium-dependent norepinephrine-induced currents in norepinephrine-transporter-transfected HEK-293 cells blocked by cocaine and antidepressants.", "entity1": "norepinephrine-transporter", "entity2": "cocaine", "span1": [52, 78], "span2": [116, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4022": {"label": 3, "data": {"text": "The anti-inflammatory actions of curcumin on colitis may involve inhibition of the TLR4/NF-\u03baB signaling pathway and of IL-27 expression.", "entity1": "TLR4", "entity2": "curcumin", "span1": [83, 87], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13602": {"label": 5, "data": {"text": "Desvenlafaxine succinate (DVS) is a recently introduced antagonist of the human norepinephrine and serotonin transporters (hNET and hSERT, respectively), currently in clinical development for use in the treatment of major depressive disorder and vasomotor symptoms associated with menopause.", "entity1": "hNET", "entity2": "DVS", "span1": [123, 127], "span2": [26, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6658": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "cyclooxygenase-2", "entity2": "acetaminophen", "span1": [62, 78], "span2": [178, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4926": {"label": 2, "data": {"text": "This study assessed changes in myocardial ALDH2 expression in the diabetic rat, in particular the diabetic rat pretreated with ALDH2 activator ethanol (EtOH).", "entity1": "ALDH2", "entity2": "EtOH", "span1": [127, 132], "span2": [152, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5431": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "EC 4.2.1.1", "entity2": "benzenesulfonamides", "span1": [153, 163], "span2": [12, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12850": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "Flt-3", "entity2": "sorafenib", "span1": [262, 267], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7928": {"label": 1, "data": {"text": "Altogether, our results suggest that a high dose of glucosamine may inhibit cell proliferation through apoptosis and disturb cell cycle progression with a halt at G(0)/G(1) phase, and that this occurs, at least in part, by a reduction in Rb phosphorylation together with modulation of p21, p53 and HO-1 expression, and nuclear p21 accumulation.", "entity1": "HO-1", "entity2": "glucosamine", "span1": [298, 302], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9842": {"label": 1, "data": {"text": "gamma-Butyrobetaine hydroxylase catalyse the last step in carnitine biosynthesis, the formation of L-carnitine from gamma-butyrobetaine, a reaction dependent on Fe2+, alpha-ketoglutarate, ascorbate and oxygen.", "entity1": "gamma-Butyrobetaine hydroxylase", "entity2": "alpha-ketoglutarate", "span1": [0, 31], "span2": [167, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"246": {"label": 3, "data": {"text": "Indomethacin inhibited both hCOX-1 and hCOX-2, whereas NS-398 and Dup-697 selectively inhibited hCOX-2.", "entity1": "hCOX-2", "entity2": "Indomethacin", "span1": [39, 45], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13804": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "kinase", "entity2": "STI571", "span1": [31, 37], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11594": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "CSE", "entity2": "H(2)S", "span1": [102, 105], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4624": {"label": 2, "data": {"text": "DNA methyltransferase 3a expression was increased in all BPA males and BPA 0.5 females and reduced in BPA 200 females.", "entity1": "DNA methyltransferase 3a", "entity2": "BPA", "span1": [0, 24], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12759": {"label": 3, "data": {"text": "Ang II level in plasma and mesenteric arteries in imidapril group was significantly lower than that in irbesartan group (P<0.05).", "entity1": "Ang II", "entity2": "imidapril", "span1": [0, 6], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13456": {"label": 2, "data": {"text": "We demonstrate that only treatment of HaCaT with GLA and EPA or a PPARgamma ligand (roziglitazone), induced COX-2 expression (protein and mRNA).", "entity1": "COX-2", "entity2": "EPA", "span1": [108, 113], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14053": {"label": 3, "data": {"text": "Aspirin and metformin (an activator of AMPK) increased inhibition of mTOR and Akt, as well as autophagy in CRC cells.", "entity1": "mTOR", "entity2": "metformin", "span1": [69, 73], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10697": {"label": 8, "data": {"text": "Ex vivo, lumiracoxib inhibited COX-1-derived thromboxane B(2) (TxB(2)) generation with an ID(50) of 33 mg kg(-1), whereas COX-2-derived production of prostaglandin E(2) (PGE(2)) in the lipopolysaccharide-stimulated rat air pouch was inhibited with an ID(50) value of 0.24 mg kg(-1).", "entity1": "COX-1", "entity2": "TxB(2)", "span1": [31, 36], "span2": [63, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9871": {"label": 3, "data": {"text": "Exposure of freshly isolated subcutaneous and omental adipocytes in suspension culture to troglitazone induced a similar reduction of PAI-1 concentration in the culture medium (by 35 +/- 11%, p < 0.05, and 33 +/- 8%, p < 0.05 compared with control, respectively).", "entity1": "PAI-1", "entity2": "troglitazone", "span1": [134, 139], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16003": {"label": 2, "data": {"text": "Puerarin promotes proliferation by altering cell cycle distribution whereas puerarin-mediated survival may be associated with up-regulation of Bcl-xL expression.", "entity1": "Bcl-xL", "entity2": "puerarin", "span1": [143, 149], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6439": {"label": 9, "data": {"text": "Clenbuterol was without effect on NGF mRNA levels in L929 cells, whereas CB1093 caused significant increases in both NGF mRNA and protein levels in both 3T3 and L929 cells.", "entity1": "NGF", "entity2": "Clenbuterol", "span1": [34, 37], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7728": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "Luteinizing hormone-releasing hormone", "entity2": "goserelin", "span1": [0, 37], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4928": {"label": 2, "data": {"text": "Compared with DM8W group, SOD and ALDH2 in EtOH+DM8W group was increased, MDA was decreased.", "entity1": "ALDH2", "entity2": "EtOH", "span1": [34, 39], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10052": {"label": 1, "data": {"text": "Cembranoid and long-chain alkanol sites on the nicotinic acetylcholine receptor and their allosteric interaction.", "entity1": "nicotinic acetylcholine receptor", "entity2": "long-chain alkanol", "span1": [47, 79], "span2": [15, 33]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"2677": {"label": 8, "data": {"text": "In kidneys, stimulation of adenylyl cyclase causes egress of cAMP, conversion of cAMP to AMP by ecto-phosphodiesterase, and metabolism of AMP to adenosine by ecto-5'-nucleotidase.", "entity1": "ecto-5'-nucleotidase", "entity2": "AMP", "span1": [158, 178], "span2": [138, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4054": {"label": 3, "data": {"text": "In this study, focus was given to evaluate the ability of neoechinulin A, an indole alkaloid isolated from marine-derived Microsporum sp., to attenuate microglial activation by oligomeric amyloid-\u03b2 1-42 (A\u03b242).", "entity1": "amyloid-\u03b2 1-42", "entity2": "neoechinulin A", "span1": [188, 202], "span2": [58, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8645": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b2", "entity2": "ethanol", "span1": [31, 35], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7399": {"label": 1, "data": {"text": "The C2 domains studied here both utilize the TAMA mechanism, in which the C2 domain Ca2+ affinity is too low to be activated by physiological Ca2+ signals in most regions of the cell.", "entity1": "C2 domain", "entity2": "Ca2+", "span1": [74, 83], "span2": [84, 88]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12738": {"label": 3, "data": {"text": "The observation that Ras-transformed cells can be sensitized to killing by ionizing radiation with GW572016 demonstrates that EGFR KIs could potentially be used to radiosensitize tumors in which radioresistance is dependent on Ras-driven autocrine signaling through EGFR.", "entity1": "EGFR", "entity2": "GW572016", "span1": [126, 130], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15462": {"label": 8, "data": {"text": "Measurement of Transport Activities of 3\u03b2-Hydroxy-\u0394(5)-bile Acids in Bile Salt Export Pump and Multidrug Resistance-Associated Proteins Using LC-MS/MS.", "entity1": "Multidrug Resistance-Associated Proteins", "entity2": "3\u03b2-Hydroxy-\u0394(5)-bile Acids", "span1": [95, 135], "span2": [39, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1307": {"label": 3, "data": {"text": "It was also antagonized by the non-specific cyclooxygenase (COX) inhibitor, indomethacin, and by the selective COX-2 inhibitor, NS-398, but not by the specific COX-1 inhibitor, valeryl salicylate.", "entity1": "COX", "entity2": "indomethacin", "span1": [60, 63], "span2": [76, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7047": {"label": 3, "data": {"text": "CONCLUSIONS: Imatinib inhibits RET-mediated MTC cell growth affecting RET protein levels in vitro in a dose-dependent manner.", "entity1": "RET", "entity2": "Imatinib", "span1": [70, 73], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5798": {"label": 0, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "aminoacylase 1", "entity2": "amino acid", "span1": [52, 66], "span2": [29, 39]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10630": {"label": 3, "data": {"text": "While fluoropyrimidine antimetabolites have other sites of action, antifolates ZD1694 (raltitrexed, Tomudex) and AG337 (Thymitag) are more specific and potent TS inhibitors.", "entity1": "TS", "entity2": "Thymitag", "span1": [159, 161], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15166": {"label": 2, "data": {"text": "cAMP response element-binding protein (CREB) has been implicated in the regulation of FSH\u03b2 gene expression, but the molecular mechanisms by which pulsatile GnRH regulates CREB activation remain poorly understood.", "entity1": "CREB", "entity2": "GnRH", "span1": [171, 175], "span2": [156, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12363": {"label": 1, "data": {"text": "Structural studies with R283K pol \u03b2 show that the binary DNA complex has 8-oxoG in equilibrium between anti- and syn-forms.", "entity1": "R283K", "entity2": "8-oxoG", "span1": [24, 29], "span2": [73, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10167": {"label": 1, "data": {"text": "Considerable evidence indicates that serotonergic mechanisms, particularly the serotonin transporter (5HTT), may mediate central effects of cocaine and may also be involved in impulsive and aggressive behavior.", "entity1": "serotonin transporter", "entity2": "cocaine", "span1": [79, 100], "span2": [140, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10591": {"label": 3, "data": {"text": "Auranofin, an antirheumatic gold compound, is an inhibitor of selenocysteine enzymes, such as thioredoxin reductase and glutathione peroxidase.", "entity1": "thioredoxin reductase", "entity2": "Auranofin", "span1": [94, 115], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6380": {"label": 3, "data": {"text": "Thirty-week administration of UFT with or without leucovorin markedly suppressed both colorectal carcinogenesis and tumor growth, resulted in the increase of thymidylate synthase inhibition and the decrease of thymidine kinase activity in the tumor cells.", "entity1": "thymidine kinase", "entity2": "leucovorin", "span1": [210, 226], "span2": [50, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14946": {"label": 1, "data": {"text": "LPA1-induced cytoskeleton reorganization therefore makes a previously unrecognized but critically important contribution to the profibrotic activities of LPA by driving MRTF-dependent CTGF expression, which, in turn, drives fibroblast proliferation.-Sakai, N., Chun, J., Duffield, J. S., Wada, T., Luster, A. D., Tager, A. M. LPA1-induced cytoskeleton reorganization drives fibrosis through CTGF-dependent fibroblast proliferation.", "entity1": "MRTF", "entity2": "LPA", "span1": [169, 173], "span2": [154, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11823": {"label": 2, "data": {"text": "Moreover, curcumin alleviated Sim2 expression, and reversely raised Drebrin expression in neurons treated with hyperglycaemia.", "entity1": "Drebrin", "entity2": "curcumin", "span1": [68, 75], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4362": {"label": 5, "data": {"text": "However, recent clinical studies have shown that a single low-dose injection of ketamine, an N-methyl d-aspartate receptor (NMDAR) antagonist, has rapid antidepressant effects that are observed within hours and are long lasting.", "entity1": "N-methyl d-aspartate receptor", "entity2": "ketamine", "span1": [93, 122], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11485": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "cyclooxygenase", "entity2": "bromfenac", "span1": [26, 40], "span2": [196, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6871": {"label": 1, "data": {"text": "Also, prophylactic, as well as therapeutic, treatment with the CSE inhibitor, DL-propargylglycine (PAG), significantly reduced the severity of caerulein-induced pancreatitis and associated lung injury, as determined by 1) hyperamylasemia [plasma amylase (U/L) (control, 1204+/-59); prophylactic treatment: placebo, 10635+/-305; PAG, 7904+/-495; therapeutic treatment: placebo, 10427+/-470; PAG, 7811+/-428; P<0.05 PAG c.f.", "entity1": "amylase", "entity2": "PAG", "span1": [246, 253], "span2": [328, 331]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6050": {"label": 9, "data": {"text": "Only strains of P. aeruginosa producing large amounts of beta-lactamase may be resistant to both ceftazidime and cefepime.", "entity1": "beta-lactamase", "entity2": "cefepime", "span1": [57, 71], "span2": [113, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7949": {"label": 2, "data": {"text": "Moreover, activation of the ERK and CREB signaling pathway in the hippocampus might be involved in METH-induced spatial memory changes.", "entity1": "CREB", "entity2": "METH", "span1": [36, 40], "span2": [99, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1804": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "IMC-225", "span1": [0, 32], "span2": [215, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7183": {"label": 1, "data": {"text": "Administration of m-chlorophenylpiperazine and fenfluramine, both of which induce anorexic effects via 5-HT2C receptors and/or 5-HT1B receptors, suppressed food intake in 5- and 8-wk-old Ay mice, whereas the anorexic effects were attenuated in food-restricted Ay mice.", "entity1": "5-HT1B", "entity2": "fenfluramine", "span1": [127, 133], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8258": {"label": 4, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2C", "entity2": "Ro 60-0175", "span1": [23, 29], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14797": {"label": 2, "data": {"text": "In addition, TSA induced Nrf2 nuclear translocation and up-regulated the expression of Nrf2-ARE downstream antioxidant genes, whereas Nrf2 knockdown by RNA interference blocked the inhibition of TSA on myofibroblast differentiation.", "entity1": "Nrf2", "entity2": "TSA", "span1": [87, 91], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"69": {"label": 4, "data": {"text": "H1-receptor antagonists have been utilized, following their initial chemical synthesis in 1933, both in the treatment of conditions in which histamine is considered to be of pathogenic importance and conversely to help elucidate the role of histamine in disease, through an evaluation of their influence on disease expression.", "entity1": "H1-receptor", "entity2": "histamine", "span1": [0, 11], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3218": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "syringic acid", "span1": [248, 261], "span2": [145, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12207": {"label": 8, "data": {"text": "During embryogenesis, lratb is expressed in mostly non-overlapping domains opposite to retinal dehydrogenase 2 (raldh2), the key enzyme for retinoic acid synthesis.", "entity1": "retinal dehydrogenase 2", "entity2": "retinoic acid", "span1": [87, 110], "span2": [140, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13442": {"label": 1, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "COX-2 promoter", "entity2": "GW9662", "span1": [113, 127], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7133": {"label": 1, "data": {"text": "All PDE5 constructs had similar affinities for 3-isobutyl-1-methylxanthine, sildenafil, tadalafil, and UK-122764, but mutants containing a complete GAF-B had 7- to 18-fold higher affinity for vardenafil-based compounds compared with those lacking a complete GAF-B.", "entity1": "PDE5", "entity2": "sildenafil", "span1": [4, 8], "span2": [76, 86]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7560": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "eNOS", "entity2": "L-arginine", "span1": [158, 162], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"5988": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "( Glu1]Pg", "entity2": "epsilon-aminocaproic acid", "span1": [43, 52], "span2": [199, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13920": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR1", "entity2": "Phenformin", "span1": [231, 235], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3818": {"label": 1, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "D281A", "entity2": "Ile", "span1": [109, 114], "span2": [58, 61]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11936": {"label": 1, "data": {"text": "To further our understanding of how fisetin negatively regulates mTORC1 signaling, we analyzed the phosphorylation of S6K1, mTOR and Akt in fisetin-treated TSC2-knockdown cells.", "entity1": "Akt", "entity2": "fisetin", "span1": [133, 136], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9746": {"label": 4, "data": {"text": "In guinea pigs, antagonist actions of yohimbine at 5-HT(1B) receptors are revealed by blockade of hypothermia evoked by the 5-HT(1B) agonist, GR46,611.", "entity1": "5-HT(1B)", "entity2": "GR46,611", "span1": [124, 132], "span2": [142, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8233": {"label": 3, "data": {"text": "Although ICA greatly attenuates ERG inactivation by shifting its voltage dependence to more positive potentials, it enhances the rate and extent of EAG inactivation without altering its voltage dependence.", "entity1": "EAG", "entity2": "ICA", "span1": [148, 151], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5987": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "human [Glu1]plasminogen", "entity2": "epsilon-aminocaproic acid", "span1": [18, 41], "span2": [199, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8487": {"label": 3, "data": {"text": "Furthermore, no impact on cytokine release (i.e., on IL-10, IL-6, IL-12/23p40 and TNF\u03b1 levels) was seen in LPS-stimulated human PBMCs, except with JWH-210 and JWH-122 which caused a decrease of TNF\u03b1 and IL-12/23p40.", "entity1": "23p40", "entity2": "JWH-210", "span1": [209, 214], "span2": [147, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12395": {"label": 1, "data": {"text": "Dexamethasone suppressed IL-11 gene transcription enhanced by PTH(1-34) without affecting \u0394FosB expression or Smad1 phosphorylation, and dexamethasone-GC receptor complex was bound to JunD, which forms heterodimers with \u0394FosB.", "entity1": "JunD", "entity2": "dexamethasone", "span1": [184, 188], "span2": [137, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6419": {"label": 2, "data": {"text": "The induction in UCP-3 expression was not accompanied by changes in the mitochondrial membrane potential of rat primary preadipocytes after bezafibrate or Wy-14,643 treatment.", "entity1": "UCP-3", "entity2": "Wy-14,643", "span1": [17, 22], "span2": [155, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14599": {"label": 9, "data": {"text": "In conclusion, the Lys27Gln substitution does not significantly modulate CDA activity toward dFdC, and therefore would not contribute to interindividual variability in response to gemcitabine.", "entity1": "Lys27Gln", "entity2": "gemcitabine", "span1": [19, 27], "span2": [180, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2885": {"label": 3, "data": {"text": "At PND35, the medial prefrontal cortex (mPFC) of rats given MPH showed 55% greater immunoreactivity (-ir) for the catecholamine marker tyrosine hydroxylase (TH), 60% more Nissl-stained cells, and 40% less norepinephrine transporter (NET)-ir density.", "entity1": "norepinephrine transporter", "entity2": "MPH", "span1": [205, 231], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5544": {"label": 9, "data": {"text": "However, the neutrophils and the endogenous NO generated by them failed to modify P-selectin expression in ADP-activated platelets.", "entity1": "P-selectin", "entity2": "NO", "span1": [82, 92], "span2": [44, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10044": {"label": 3, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "apolipoprotein C-III", "entity2": "Fenofibrate", "span1": [111, 131], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15536": {"label": 2, "data": {"text": "DMN-induced cyclooxygenase-2 (COX-2) expression and nuclear factor-kappa B (NF-\u03baB) activation was reduced by CK treatment.", "entity1": "nuclear factor-kappa B", "entity2": "DMN", "span1": [52, 74], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1004": {"label": 1, "data": {"text": "Effects of a serotoninserotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans.", "entity1": "serotonin 5-HT(4) receptor", "entity2": "serotonin", "span1": [22, 48], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3526": {"label": 3, "data": {"text": "\u03b1-Amino-\u03b1\u00b4-Halomethylketones: Synthetic Methodologies and Pharmaceutical Applications as Serine and Cysteine Protease Inhibitors.", "entity1": "Serine and Cysteine Protease", "entity2": "\u03b1-Amino-\u03b1\u00b4-Halomethylketones", "span1": [89, 117], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10023": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Lys", "span1": [126, 138], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16033": {"label": 3, "data": {"text": "This effect was prevented by rapamycin, an inhibitor of the mammalian target of rapamycin complex 1 (mTORC1), or by PF470867, a selective inhibitor of the p70 ribosomal S6 kinase 1 (S6K1).", "entity1": "S6K1", "entity2": "PF470867", "span1": [182, 186], "span2": [116, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6894": {"label": 8, "data": {"text": "NPC1L1 could recently be identified as a major sterol transporter for the intestinal uptake of cholesterol as well as plant sterols.", "entity1": "sterol transporter", "entity2": "sterols", "span1": [47, 65], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13286": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "vascular endothelial growth factor receptor", "entity2": "Sorafenib", "span1": [255, 298], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11694": {"label": 2, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "nuclear factor kappa B", "entity2": "pioglitazone", "span1": [161, 183], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4385": {"label": 1, "data": {"text": "Camptothecin (CPT), a topoisomerase (Top) I-targeting drug that stabilizes Top1-DNA covalent adducts, can induce S-phase-specific cytotoxicity due to the arrest of progressing replication forks.", "entity1": "Top1", "entity2": "Camptothecin", "span1": [75, 79], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12597": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "kringle domain", "entity2": "N", "span1": [86, 100], "span2": [140, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9852": {"label": 1, "data": {"text": "Salicylates inhibit (125)I-ET-1 binding to recombinant rat ETA receptors.", "entity1": "ET-1", "entity2": "Salicylates", "span1": [27, 31], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4152": {"label": 1, "data": {"text": "6-Ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide (TAK-441) is a potent, selective hedgehog signaling pathway inhibitor that binds to Smo and is being developed for the treatment of cancer.", "entity1": "Smo", "entity2": "TAK-441", "span1": [245, 248], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6784": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-2", "entity2": "tolfenamic acid", "span1": [257, 262], "span2": [159, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8407": {"label": 1, "data": {"text": "Ponatinib has demonstrated early clinical efficacy in chemotherapy-resistant acute myeloid leukemia (AML) patients with internal tandem duplication (ITD) mutations in FLT3.", "entity1": "FLT3", "entity2": "Ponatinib", "span1": [167, 171], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6297": {"label": 3, "data": {"text": "UNLABELLED: Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor.", "entity1": "COMT", "entity2": "Entacapone", "span1": [89, 93], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13041": {"label": 2, "data": {"text": "Furthermore, in vivo relevant lipids such as oxidized low-density lipoprotein can also elicit retinoid signaling leading to CD1d up-regulation.", "entity1": "CD1d", "entity2": "retinoid", "span1": [124, 128], "span2": [94, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12625": {"label": 1, "data": {"text": "The EP1 receptor bound 17-phenyl-PGE2, sulprostone and iloprost in addition to PGE2 and PGE1, with Ki values of 14-36 nM.", "entity1": "EP1", "entity2": "iloprost", "span1": [4, 7], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15209": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "ethylacetate", "span1": [340, 363], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5594": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "risperidone", "span1": [111, 117], "span2": [151, 162]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11614": {"label": 8, "data": {"text": "In summary, our data indicates that over-expression of hGSTA4 at levels conferring high GST-4-HNE conjugating activity confers a partial growth advantage to HepG2 cells and protects against 4-HNE oxidative injury.", "entity1": "GST", "entity2": "4-HNE", "span1": [88, 91], "span2": [92, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12938": {"label": 8, "data": {"text": "L-arg is converted to urea by arginase I in the liver and arginase II in the kidney.", "entity1": "arginase II", "entity2": "urea", "span1": [58, 69], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12699": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "DCVC", "span1": [79, 90], "span2": [150, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11970": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I", "entity2": "PI(4)P", "span1": [16, 66], "span2": [193, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12541": {"label": 1, "data": {"text": "In plasma membranes prepared from these isolated brown fat cells by borate extraction there was a similar enrichment of activity of SSAO and of the plasma membrane marker enzyme, phosphodiesterase I.", "entity1": "phosphodiesterase I", "entity2": "borate", "span1": [179, 198], "span2": [68, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2494": {"label": 3, "data": {"text": "Licofelone, a dual anti-inflammatory drug that inhibits 5-lipoxygenase (LOX) and cyclooxygenase (COX) enzymes, may have a better cardiovascular profile that cycloxygenase-2 inhibitors due to cycloxygenase-1 blockade-mediated antithrombotic effect and a better gastrointestinal tolerability.", "entity1": "cycloxygenase-1", "entity2": "Licofelone", "span1": [191, 206], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11827": {"label": 1, "data": {"text": "In preclinical studies, the mammalian target of rapamycin (mTOR) in the medial prefrontal cortex and the eukaryotic elongation factor (eEF2) in the hippocampus have been proposed as critical mediators of ketamine's rapid antidepressant actions.", "entity1": "eEF2", "entity2": "ketamine", "span1": [135, 139], "span2": [204, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9386": {"label": 1, "data": {"text": "The interactions of GYKI 52466 and cyclothiazide on AMPA receptor-mediated e.p.s.cs in area CA1 of hippocampal slices provide evidence that the decay time constant of these synaptic events are not governed by desensitization.", "entity1": "AMPA receptor", "entity2": "GYKI 52466", "span1": [52, 65], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"634": {"label": 3, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "PLA2", "entity2": "p-bromophenacyl bromide", "span1": [80, 84], "span2": [96, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1472": {"label": 8, "data": {"text": "These results suggest that the altered gamma-glutamyl kinase results in stabilization of the complex or has an indirect effect on gamma-glutamyl phosphate reductase activity, which leads to an increase in L-proline production in Saccharomyces cerevisiae.", "entity1": "gamma-glutamyl phosphate reductase", "entity2": "L-proline", "span1": [130, 164], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2952": {"label": 0, "data": {"text": "Cocrystal structures of PDE5 catalytic (C) domain with inhibitors reveal a hydrogen bond and hydrophobic interactions with Tyr-612, hydrogen bonds with Gln-817, a hydrophobic clamp formed by Phe-820 and Val-782, and contacts with His-613, Leu-765, and Phe-786 [Sung et al.", "entity1": "PDE5 catalytic (C) domain", "entity2": "Phe", "span1": [24, 49], "span2": [191, 194]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10456": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "SDH", "entity2": "L-serine", "span1": [0, 3], "span2": [108, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12802": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "c-kit", "entity2": "imatinib mesylate", "span1": [120, 125], "span2": [9, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8733": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT2B10", "entity2": "diphenhydramine", "span1": [61, 68], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4679": {"label": 2, "data": {"text": "Using cultured human keratinocytes and diabetic rat model, the current study showed that high-glucose environment enhanced IL-8 production via epidermal growth factor receptor (EGFR) -extracelluar signal-regulated kinase (ERK) pathway in a reactive oxygen species (ROS)-dependent manner in keratinocytes.", "entity1": "IL-8", "entity2": "glucose", "span1": [123, 127], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13694": {"label": 2, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "human TLR7", "entity2": "imiquimod", "span1": [118, 128], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10416": {"label": 3, "data": {"text": "Inhibition corresponded to increased cAMP production caused by rolipram alone or rolipram plus salmeterol and blocked proportionately the phosphorylation and activation of gIV-PLA(2) in FMLP/B-activated eosinophils.", "entity1": "gIV-PLA(2)", "entity2": "rolipram", "span1": [172, 182], "span2": [81, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"16049": {"label": 1, "data": {"text": "By contrast, the editing of some sites is completely lost or significantly reduced in other non-green tissues; for instance, the editing of ndhB-149, ndhB-1255, and ndhD-2 is completely lost in roots and in lincomycin-treated seedlings.", "entity1": "ndhB-1255", "entity2": "lincomycin", "span1": [150, 159], "span2": [207, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6437": {"label": 3, "data": {"text": "RESULT(S): Buserelin acetate, a GnRH agonist (0.1-10 ng/mL), had no significant effect on MCP-1 expression, whereas danazol (10(-7)-10(-5) M), a testosterone analog, and dexamethasone, an anti-inflammatory glucocorticoid hormone (10(-12)-10(-6)M), showed a direct and a dose-dependent inhibitory effect on MCP-1 expression.", "entity1": "MCP-1", "entity2": "dexamethasone", "span1": [306, 311], "span2": [170, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7839": {"label": 2, "data": {"text": "We found that intracellular GTP depletion by ribavirin as well as other IMPDH (inosine-5'-monophosphate dehydrogenase) inhibitors, such as mycophenolic acid and 6-mercaptopurine, up-regulated F7 expression.", "entity1": "F7", "entity2": "6-mercaptopurine", "span1": [192, 194], "span2": [161, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13438": {"label": 8, "data": {"text": "TGF-beta1 and high D-glucose increased hCAT-1 mRNA expression ( approximately 8-fold) and maximal transport velocity (V(max)), L-[(3)H]citrulline formation from L-[(3)H]arginine (index of NO synthesis) and endothelial NO synthase (eNOS) protein abundance, but did not alter eNOS phosphorylation.", "entity1": "endothelial NO synthase", "entity2": "NO", "span1": [206, 229], "span2": [188, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"7344": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT1", "entity2": "alanine", "span1": [235, 240], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2801": {"label": 3, "data": {"text": "Caerulein increased the levels of H(2)S and CSE mRNA expression while CBS mRNA expression was decreased.", "entity1": "CBS", "entity2": "Caerulein", "span1": [70, 73], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5493": {"label": 3, "data": {"text": "3) The inhibitory effects of the thioureylene drugs, methimazole and carbimazole, on the iodide-dependent catalatic activity were very similar to those reported previously for thyroid peroxidase-catalyzed iodination.", "entity1": "thyroid peroxidase", "entity2": "thioureylene", "span1": [176, 194], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8081": {"label": 9, "data": {"text": "E235-mediated induction of senescence was not dependent on p21 or p53; however, p21 conferred protection against the growth inhibitory effects of E235.", "entity1": "p21", "entity2": "E235", "span1": [59, 62], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2474": {"label": 4, "data": {"text": "The beta(2)-adrenoceptor (beta(2)-AR) agonists clenbuterol and fenoterol have similar beneficial effects in animal models of heart failure.", "entity1": "beta(2)-AR", "entity2": "clenbuterol", "span1": [26, 36], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5919": {"label": 3, "data": {"text": "Phenelzine is a more potent monoamine oxidase inhibitor than is N2-acetylphenelzine.", "entity1": "monoamine oxidase", "entity2": "Phenelzine", "span1": [28, 45], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10562": {"label": 3, "data": {"text": "Irbesartan may have antiatherosclerotic properties beyond those expected from blood pressure lowering per se: this AT1-blocker decreases the vascular oxidative stress and prevents the procoagulant as well as the pro-inflammatory effects of angiotensin II.", "entity1": "AT1", "entity2": "Irbesartan", "span1": [115, 118], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11819": {"label": 8, "data": {"text": "EGCG, 1, and 3 were the most potent cytotoxic compounds, with EGCG and 3 selectively killing OATP1B3-expressing cells.", "entity1": "OATP1B3", "entity2": "EGCG", "span1": [93, 100], "span2": [62, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9018": {"label": 4, "data": {"text": "The limitation of SRF by diazepam was not prevented by inverse or partial agonists at the BDZ receptor, including Ro 15-1788 and the beta CCs.", "entity1": "BDZ receptor", "entity2": "beta CCs", "span1": [90, 102], "span2": [133, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14064": {"label": 3, "data": {"text": "Aspirin and metformin (an activator of AMPK) increased inhibition of mTOR and Akt, as well as autophagy in CRC cells.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [69, 73], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2693": {"label": 4, "data": {"text": "Combining in vivo and in vitro findings, we identified nine AhR agonists, six of which are marketed therapeutics and have been approved by the U.S. Food and Drug Administration, including leflunomide, flutamide, and nimodipine.", "entity1": "AhR", "entity2": "flutamide", "span1": [60, 63], "span2": [201, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7999": {"label": 3, "data": {"text": "While SP600125 (a JNK inhibitor) and SB203580 (a p38 inhibitor) markedly prevented the expression of these proteins induced by ISO.", "entity1": "JNK", "entity2": "SP600125", "span1": [18, 21], "span2": [6, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9013": {"label": 2, "data": {"text": "These findings suggest that limitation of SRF was produced by binding of BDZs, but not beta CCs, to voltage-dependent sodium channels and not to high affinity central BDZ receptors, and that BDZs limit SRF by slowing recovery of sodium channels from inactivation.", "entity1": "sodium channels", "entity2": "BDZs", "span1": [229, 244], "span2": [191, 195]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8583": {"label": 3, "data": {"text": "The high fat diet significantly increased hepatic mRNA expressions of PPAR\u03b3, SREBP1C and SCD-1 genes in comparison to the control diet, which was subsequently reversed by supplementation with fisetin.", "entity1": "PPAR\u03b3", "entity2": "fisetin", "span1": [70, 75], "span2": [192, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15528": {"label": 3, "data": {"text": "A highly potent inhibition of the peroxidase catalytic reaction by NO/SNO was seen in assays employing the coupled Prx-Trx system.", "entity1": "peroxidase", "entity2": "SNO", "span1": [34, 44], "span2": [70, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7092": {"label": 5, "data": {"text": "Focal application of the transporter substrate D-aspartate elicited inward currents in IPCs, which were larger in the presence of anions that permeate the transporter-associated anion channel and blocked by the transporter antagonist D,L-threo-beta-benzyloxyaspartate.", "entity1": "anion channel", "entity2": "D,L-threo-beta-benzyloxyaspartate", "span1": [178, 191], "span2": [234, 267]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"2848": {"label": 1, "data": {"text": "The cAspAT TZD-responsive site was restricted to a single AGGACA hexanucleotide located at -381 to -376 bp whose mutation impaired the specific RORalpha binding.", "entity1": "cAspAT", "entity2": "TZD", "span1": [4, 10], "span2": [11, 14]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1314": {"label": 3, "data": {"text": "Minocycline treatment prevents the formation of activated caspase-3, a known effector of apoptosis, as well as the appearance of a calpain cleaved substrate, a marker of excitotoxic/necrotic cell death.", "entity1": "caspase-3", "entity2": "Minocycline", "span1": [58, 67], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10315": {"label": 1, "data": {"text": "Plasmacytoid dendritic cells produce cytokines and mature in response to the TLR7 agonists, imiquimod and resiquimod.", "entity1": "cytokines", "entity2": "imiquimod", "span1": [37, 46], "span2": [92, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11326": {"label": 8, "data": {"text": "Mechanisms of cefadroxil uptake in the choroid plexus: studies in wild-type and PEPT2 knockout mice.", "entity1": "PEPT2", "entity2": "cefadroxil", "span1": [80, 85], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13282": {"label": 1, "data": {"text": "The direct effect of sorafenib on the activity of these kinases and their downstream signaling was tested using phospho-specific antibodies.", "entity1": "kinases", "entity2": "sorafenib", "span1": [56, 63], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9133": {"label": 3, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c. The irreversible complex between phenoxybenzamine and calmodulin may be useful for inhibiting certain calmodulin-dependent reactions and for studying the various biological functions of calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [238, 248], "span2": [169, 185]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9840": {"label": 3, "data": {"text": "The Hsp90-specific inhibitor geldanamycin selectively disrupts kinase-mediated signaling events of T-lymphocyte activation.", "entity1": "kinase", "entity2": "geldanamycin", "span1": [63, 69], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9118": {"label": 1, "data": {"text": "The site at which phenoxybenzamine bound to calmodulin appears to be similar to that at which certain antipsychotic agents bind, since several of them, including penfluridol, pimozide and spiroperidol, prevented the binding of phenoxybenzamine to calmodulin.", "entity1": "calmodulin", "entity2": "spiroperidol", "span1": [247, 257], "span2": [188, 200]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3641": {"label": 1, "data": {"text": "In the resveratrol+As(2)O(3) group, activities of superoxide dismutase, catalase in serum and GSH/GSSG were significantly increased, histopathological effects were reduced, and arsenic accumulation markedly decreased in the liver, compared with the As(2)O(3)-treated group.", "entity1": "catalase", "entity2": "resveratrol", "span1": [72, 80], "span2": [7, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1939": {"label": 3, "data": {"text": "The aim of this study was to evaluate the influence of hepatic impairment on the pharmacokinetics (PK) of the novel cyclooxygenase-2 (COX-2) selective inhibitor lumiracoxib (Prexige), so that dose recommendations for clinical use can be provided.", "entity1": "cyclooxygenase-2", "entity2": "lumiracoxib", "span1": [116, 132], "span2": [161, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10948": {"label": 8, "data": {"text": "This process was reduced by a protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, and a typical monocarboxylate transporter (MCT) inhibitor, alpha-cyano-4-hydroxycinnamic acid, suggesting that nicotinate uptake by rat astrocytes is mediated by H(+)-coupled monocarboxylate transport system.", "entity1": "monocarboxylate transport system", "entity2": "nicotinate", "span1": [270, 302], "span2": [206, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1513": {"label": 3, "data": {"text": "Sildenafil is inhibitory of PDE5 at a rate tenfold higher than for the next PDE (PDE6), which produces visual changes through the retinal rods.", "entity1": "PDE5", "entity2": "Sildenafil", "span1": [28, 32], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1393": {"label": 3, "data": {"text": "Since gemfibrozil is known to activate peroxisome proliferator-activated receptor-alpha (PPAR-alpha), we investigated the role of PPAR-alpha in gemfibrozil-mediated inhibition of iNOS.", "entity1": "iNOS", "entity2": "gemfibrozil", "span1": [179, 183], "span2": [144, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7849": {"label": 2, "data": {"text": "In the present study, we investigated the molecular mechanism of ribavirin-induced up-regulation of F7 expression in HepG2 (human hepatoma cell line).", "entity1": "F7", "entity2": "ribavirin", "span1": [100, 102], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11493": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "cyclooxygenase", "entity2": "ketorolac", "span1": [26, 40], "span2": [163, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14034": {"label": 2, "data": {"text": "Here, we report biochemical evidence that mercury alone induces NF-\u03baB activation, resulting in the induced expression of COX-2 and iNOS.", "entity1": "COX-2", "entity2": "mercury", "span1": [121, 126], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1026": {"label": 2, "data": {"text": "Activation of endogenous somatostatin receptor subtype 2 (sst2) by somatostatin-14 or activation of transiently transfected rat D2 dopamine receptors (rD2(long)) by quinpirole had no effect.", "entity1": "rD2", "entity2": "quinpirole", "span1": [151, 154], "span2": [165, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8774": {"label": 0, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-Rb", "entity2": "Ser", "span1": [213, 223], "span2": [224, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11526": {"label": 8, "data": {"text": "Estrogens are biosynthesised from androgens by the CYP450 enzyme complex called aromatase.", "entity1": "aromatase", "entity2": "Estrogens", "span1": [80, 89], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14857": {"label": 2, "data": {"text": "Regulation of sexual reproduction by estradiol involves the activation of estrogen receptors (ERs) in the hypothalamus.", "entity1": "estrogen receptors", "entity2": "estradiol", "span1": [74, 92], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11574": {"label": 8, "data": {"text": "OBJECTIVE: The aim was to test whether the common deletion [T/-] in the promoter of FADS2 affects the PUFA biosynthetic pathway and consequently modifies the effect of alpha-linolenic acid (ALA) on myocardial infarction (MI).", "entity1": "FADS2", "entity2": "PUFA", "span1": [84, 89], "span2": [102, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9089": {"label": 9, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "leukotriene synthetase", "entity2": "piriprost", "span1": [251, 273], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4531": {"label": 3, "data": {"text": "The in vivo inhibitory effect of harmaline on CYP2D6-catalyzed bufotenine formation was confirmed by in vitro study using purified CYP2D6.", "entity1": "CYP2D6", "entity2": "harmaline", "span1": [131, 137], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5330": {"label": 1, "data": {"text": "Few targets like epidermal growth factor receptor (EGFR) mutations and anaplastic lymphoma kinase (ALK) gene rearrangements have successfully been targeted with EGFR tyrosine kinase inhibitors (TKIs) and crizotinib, respectively.", "entity1": "anaplastic lymphoma kinase", "entity2": "crizotinib", "span1": [71, 97], "span2": [204, 214]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7809": {"label": 2, "data": {"text": "RSV targets and activates the NAD(+)-dependent protein deacetylase SIRT1; in turn, SIRT1 induces an intracellular antioxidative mechanism by inducing mitochondrial superoxide dismutase (SOD2).", "entity1": "SOD2", "entity2": "RSV", "span1": [186, 190], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12348": {"label": 8, "data": {"text": "CYP3A5, which is particularly relevant to GC metabolism in the lungs, was also shown to efficiently metabolize triamcinolone acetonide, budesonide, and fluticasone propionate.", "entity1": "CYP3A5", "entity2": "fluticasone propionate", "span1": [0, 6], "span2": [152, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15537": {"label": 2, "data": {"text": "DMN-induced cyclooxygenase-2 (COX-2) expression and nuclear factor-kappa B (NF-\u03baB) activation was reduced by CK treatment.", "entity1": "NF-\u03baB", "entity2": "DMN", "span1": [76, 81], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6177": {"label": 3, "data": {"text": "Similarly, salicylic acid (3 mM) reduced CFTR Cl- current by 50+/-8% with an apparent reduction in single channel amplitude from 1.08+/-0.03 pA to 0.48+/-0.06 pA (n = 4).", "entity1": "CFTR", "entity2": "salicylic acid", "span1": [41, 45], "span2": [11, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3487": {"label": 2, "data": {"text": "On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-\u03b3, GLUT-4 and adiponectin.", "entity1": "adiponectin", "entity2": "gentianine", "span1": [177, 188], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7496": {"label": 9, "data": {"text": "The AMPK inhibitor Compound C prevented the action of metformin and AICAR but not phenformin.", "entity1": "AMPK", "entity2": "AICAR", "span1": [4, 8], "span2": [68, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11456": {"label": 1, "data": {"text": "At the enzymatic activity level, doxycycline started to suppress MMP-9 activity at 5 mg/kg/day (P<0.001), while minocycline had an effect at a lower dose, 1 mg/kg/day (P<0.02).", "entity1": "MMP-9", "entity2": "minocycline", "span1": [65, 70], "span2": [112, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13151": {"label": 5, "data": {"text": "The changes in CysLT1 receptor expression 24 h after NMDA injection and the effects of a CysLT1 receptor antagonist, pranlukast (0.01 and 0.1 mg/kg), an NMDA receptor antagonist, ketamine (30 mg/kg), and an antioxidant, edaravone (9 mg/kg) were observed.", "entity1": "NMDA receptor", "entity2": "ketamine", "span1": [153, 166], "span2": [179, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15876": {"label": 4, "data": {"text": "In the presence of this inhibitor, the selective D3 agonist PD 128,907 reduced the ED50 for the D1 agonist SKF 38393 from 56 to 4\u00a0nM.", "entity1": "D3", "entity2": "PD 128,907", "span1": [49, 51], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1219": {"label": 3, "data": {"text": "Also in contrast to effects of multiple METH injections, 1) MDMA caused little or no decrease in binding of the DAT ligand WIN35428, and 2) neither prevention of hyperthermia nor prior depletion of DA prevented the MDMA-induced reduction in plasmalemmal DA transport.", "entity1": "DAT", "entity2": "MDMA", "span1": [112, 115], "span2": [215, 219]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8000": {"label": 3, "data": {"text": "While SP600125 (a JNK inhibitor) and SB203580 (a p38 inhibitor) markedly prevented the expression of these proteins induced by ISO.", "entity1": "p38", "entity2": "SB203580", "span1": [49, 52], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1158": {"label": 9, "data": {"text": "Patch-clamp analysis using inside-out recording configuration showed that mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 microM).", "entity1": "Kir6.2", "entity2": "mitiglinide", "span1": [234, 240], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10801": {"label": 3, "data": {"text": "We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays.", "entity1": "cyclooxygenases", "entity2": "phenylbutazone", "span1": [111, 126], "span2": [73, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8075": {"label": 3, "data": {"text": "This study was designed to test the hypothesis that orlistat inhibits CESs with higher potency toward CES1 than CES2, a carboxylesterase with little lipase activity.", "entity1": "CESs", "entity2": "orlistat", "span1": [70, 74], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14208": {"label": 1, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "AChE", "entity2": "galantamine", "span1": [135, 139], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8352": {"label": 3, "data": {"text": "This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.", "entity1": "PKA", "entity2": "amino acid", "span1": [117, 120], "span2": [51, 61]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8514": {"label": 3, "data": {"text": "To overcome this limitation, we de novo synthesized a conjugate that covalently combines a Gd-based MRI contrast agent, encaged with a chelating agent (DOTA), with pantoprazole, which is a widely used proton pump inhibitor that binds to proton pumps in the stomach and colon.", "entity1": "proton pump", "entity2": "DOTA", "span1": [201, 212], "span2": [152, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3332": {"label": 3, "data": {"text": "MXF or VP-16 slightly affected cellular topo II activity in nuclear extracts derived from drug-treated cells while the combination enhanced inhibitory activity and the reduction in band depletion of topo II.", "entity1": "topo II", "entity2": "VP-16", "span1": [199, 206], "span2": [7, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"80": {"label": 3, "data": {"text": "Although the precise mechanism of the protective action of trilisate is unknown, our data support the possibility of interaction between salicylate and ASA on cyclo-oxygenase locus in the respiratory tract in ASA-intolerant patients.", "entity1": "cyclo-oxygenase", "entity2": "ASA", "span1": [159, 174], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12972": {"label": 1, "data": {"text": "gammaPKC directly associated with DGKgamma through its accessory domain (AD), depending on Ca2+ as well as phosphatidylserine/diolein in vitro.", "entity1": "DGKgamma", "entity2": "phosphatidylserine", "span1": [34, 42], "span2": [107, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10887": {"label": 1, "data": {"text": "To understand this interaction, we determined the crystal structure of PDXK in complex with (R)-roscovitine, N6-methyl-(R)-roscovitine, and O6-(R)-roscovitine, the two latter derivatives being designed to bind to PDXK but not to CDKs.", "entity1": "PDXK", "entity2": "N6-methyl-(R)-roscovitine", "span1": [71, 75], "span2": [109, 134]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5019": {"label": 0, "data": {"text": "These variants are expected to encode either a full length (OATP2B1-FL) or shortened protein lacking 22 N-terminus amino acids (OATP2B-Short).", "entity1": "OATP2B-Short", "entity2": "N", "span1": [128, 140], "span2": [104, 105]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2001": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "rat GnRHR", "entity2": "Pro", "span1": [158, 167], "span2": [136, 139]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1165": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "repaglinide", "span1": [161, 165], "span2": [53, 64]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12872": {"label": 2, "data": {"text": "Weakly translocated lipids (PE, phosphatidylhydroxypropionate, and phosphatidylhomoserine) are also weak Atp8a1 activators.", "entity1": "Atp8a1", "entity2": "phosphatidylhydroxypropionate", "span1": [105, 111], "span2": [32, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6060": {"label": 3, "data": {"text": "In NE-desensitized cells, phorbol esters and bradykinin each caused the expected down-regulation of alpha-AR mRNA.", "entity1": "alpha-AR", "entity2": "phorbol esters", "span1": [100, 108], "span2": [26, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4409": {"label": 6, "data": {"text": "However, one mGlu5 PAM, CPPHA (N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide), interacts with a separate allosteric site on mGlu5.", "entity1": "mGlu5", "entity2": "CPPHA", "span1": [13, 18], "span2": [24, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"2431": {"label": 1, "data": {"text": "SSTR2 and SSTR5 are usually expressed in GH-secreting pituitary tumors, and both octreotide and lanreotide bind preferentially to SSTR2 and, to a lesser extent, to SSTR5.", "entity1": "SSTR5", "entity2": "octreotide", "span1": [164, 169], "span2": [81, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13136": {"label": 2, "data": {"text": "The cytosolic fraction obtained from pancreatic islets obtained from GalN-treated rats had an increased PTB level compared to the levels obtained from the pancreatic islets of control rats.", "entity1": "PTB", "entity2": "GalN", "span1": [104, 107], "span2": [69, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7302": {"label": 8, "data": {"text": "The absence or presence of a cytosolic pool of BAAT has important implications for the intracellular transport of unconjugated/deconjugated bile salts.", "entity1": "BAAT", "entity2": "bile salts", "span1": [47, 51], "span2": [140, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11673": {"label": 1, "data": {"text": "In the absence of cTnI, docking localized dfbp-o to the same position in the hydrophobic groove of cTnC.", "entity1": "cTnC", "entity2": "dfbp-o", "span1": [99, 103], "span2": [42, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11889": {"label": 8, "data": {"text": "Ferredoxin 1 (FDX1; adrenodoxin) is an iron-sulfur protein that is involved in various metabolic processes, including steroid hormone synthesis in mammalian tissues.", "entity1": "adrenodoxin", "entity2": "steroid hormone", "span1": [20, 31], "span2": [118, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13762": {"label": 3, "data": {"text": "Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.", "entity1": "kinase", "entity2": "bosutinib", "span1": [29, 35], "span2": [46, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10878": {"label": 3, "data": {"text": "Early-onset diarrhea is observed immediately after CPT-11 infusion and probably due to the inhibition of acetylcholinesterase activity, which can be eliminated by administration of atropine.", "entity1": "acetylcholinesterase", "entity2": "CPT-11", "span1": [105, 125], "span2": [51, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9022": {"label": 1, "data": {"text": "We conclude that androgens can stimulate human and murine osteoblastic cell proliferation in vitro, and induce expression of the osteoblast-line differentiation marker ALP, presumably by an androgen receptor mediated mechanism.", "entity1": "androgen receptor", "entity2": "androgens", "span1": [190, 207], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3715": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "Bim", "entity2": "BPs", "span1": [183, 186], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10690": {"label": 3, "data": {"text": "Lumiracoxib inhibited purified COX-1 and COX-2 with K(i) values of 3 and 0.06 microM, respectively.", "entity1": "COX-1", "entity2": "Lumiracoxib", "span1": [31, 36], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3635": {"label": 9, "data": {"text": "NaAsO(2) increased the mRNA levels of the light and medium subunits of neurofilament and decreased the mRNA levels of tau and tubulin in a dose-dependent manner; no significant effect was found in the mRNA levels of the heavy subunit of neurofilament, microtubule-associated protein 2, or actin.", "entity1": "actin", "entity2": "NaAsO(2)", "span1": [289, 294], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14957": {"label": 2, "data": {"text": "Bile acids are signaling molecules that activate nuclear receptors, such as farnesoid X receptor, pregnane X receptor, constitutive androstane receptor, and vitamin D receptor, and play a critical role in the regulation of lipid, glucose, energy, and drug metabolism.", "entity1": "nuclear receptors", "entity2": "Bile acids", "span1": [49, 66], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6723": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "bis(1H-2-indolyl)-1-methanone", "span1": [273, 279], "span2": [86, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14336": {"label": 3, "data": {"text": "Finally, DMF suppressed unilateral ureteral obstruction (UUO)-induced renal fibrosis and alpha-SMA, fibronectin and type 1 collagen expression in the obstructed kidneys from UUO mice, along with increased and decreased expression of Nrf2 and phospho-Smad3, respectively.", "entity1": "fibronectin", "entity2": "DMF", "span1": [100, 111], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10835": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Imatinib", "span1": [119, 122], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10086": {"label": 3, "data": {"text": "A series of studies is reviewed that assesses the relationship between cytokines released at the site of tissue injury and NSAID analgesia, and the in vivo selectivity of a selective cyclooxygenase (COX)-2 inhibitor (celecoxib) in comparison to a dual COX-1/COX-2 inhibitor (ketorolac).", "entity1": "cyclooxygenase (COX)-2", "entity2": "celecoxib", "span1": [183, 205], "span2": [217, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2477": {"label": 4, "data": {"text": "The beta(2)-adrenoceptor (beta(2)-AR) agonists clenbuterol and fenoterol have similar beneficial effects in animal models of heart failure.", "entity1": "beta(2)-adrenoceptor", "entity2": "fenoterol", "span1": [4, 24], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8599": {"label": 0, "data": {"text": "Despite the presence of a GSNO binding site at the active site of GSTP1-1, isothermal titration calorimetry as well as nitrosation experiments using CysNO demonstrate that GSNO binding does not precede S-nitrosation of GSTP1-1.", "entity1": "GSTP1-1", "entity2": "S", "span1": [219, 226], "span2": [202, 203]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6948": {"label": 3, "data": {"text": "Vitamin E and probucol significantly suppressed an increase in plasma total-cholesterol (total-C) and low-density lipoprotein cholesterol compared to HC-control group.", "entity1": "low-density lipoprotein", "entity2": "probucol", "span1": [102, 125], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3459": {"label": 1, "data": {"text": "R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less.", "entity1": "DAT", "entity2": "S-modafinil", "span1": [90, 93], "span2": [103, 114]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7574": {"label": 2, "data": {"text": "Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist.", "entity1": "AQP5", "entity2": "cevimeline", "span1": [35, 39], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8387": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "GST", "entity2": "Cd", "span1": [271, 274], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10836": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "PDGFRA", "entity2": "Imatinib", "span1": [124, 130], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4625": {"label": 3, "data": {"text": "DNA methyltransferase 3a expression was increased in all BPA males and BPA 0.5 females and reduced in BPA 200 females.", "entity1": "DNA methyltransferase 3a", "entity2": "BPA", "span1": [0, 24], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5844": {"label": 9, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT4", "entity2": "granisetron", "span1": [28, 33], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10602": {"label": 3, "data": {"text": "However, some experimental findings raise the question whether these effects resulting from the iron-mimicking properties of gallium are solely responsible for its antineoplastic activity or whether additional mechanisms are involved, such as antimitotic effects which result from its capability of inhibiting tubulin polymerization.", "entity1": "tubulin", "entity2": "iron", "span1": [310, 317], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14195": {"label": 1, "data": {"text": "CCAAT/Enhancer-binding protein-homologous protein sensitizes to SU5416 by modulating p21 and PI3K/Akt signal pathway in FRO anaplastic thyroid carcinoma cells.", "entity1": "Akt", "entity2": "SU5416", "span1": [98, 101], "span2": [64, 70]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10319": {"label": 2, "data": {"text": "These results demonstrate that imidazoquinoline molecules directly induce pDC maturation as determined by cytokine induction, CCR7 and co-stimulatory marker expression and prolonging viability.", "entity1": "cytokine", "entity2": "imidazoquinoline", "span1": [106, 114], "span2": [31, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2522": {"label": 8, "data": {"text": "On the basis of our findings with structurally similar arylhydroxylamine metabolites of therapeutic drugs, we hypothesized that the reductive detoxification of arylhydroxylamine carcinogens was catalyzed by NADH cytochrome b5 reductase (b5R) and cytochrome b5 (cyt b5).", "entity1": "cytochrome b5", "entity2": "arylhydroxylamine", "span1": [246, 259], "span2": [160, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8559": {"label": 3, "data": {"text": "As a potent synthetic APN inhibitor (IC50=850nM, versus bestatin of 8.1\u03bcM), LB-4b was determined to have more significant block effects to cancer cell invasion and angiogenesis than bestatin.", "entity1": "APN", "entity2": "bestatin", "span1": [22, 25], "span2": [182, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"980": {"label": 1, "data": {"text": "These results indicate that BH(4) augmentation is essential for the restoration of eNOS function and the reduction of vascular oxidative stress in insulin-resistant rats.", "entity1": "eNOS", "entity2": "BH(4)", "span1": [83, 87], "span2": [28, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3967": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "Pin1", "entity2": "pThr", "span1": [66, 70], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"7763": {"label": 4, "data": {"text": "Rescue of both impaired extinction acquisition and deficient extinction consolidation/retrieval was achieved with prior extinction training administration of valproic acid (a GABAergic enhancer and HDAC inhibitor) or AMN082 [metabotropic glutamate receptor 7 (mGlu7) agonist], while MS-275 or PEPA (AMPA receptor potentiator) failed to affect extinction acquisition in S1 mice.", "entity1": "mGlu7", "entity2": "AMN082", "span1": [260, 265], "span2": [217, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12822": {"label": 3, "data": {"text": "The current comprehensive losartan clinical end-point programme (4 large scale morbidity/mortality trials) should provide evidence regarding the efficacy of direct blockade of the AT(1) receptor with losartan compared to standard therapy: 1) The Losartan Heart Failure Survival Study - ELITE II, 2) The Losartan Post-Myocardial Infarction Survival Study - OPTIMAAL, 3) The Losartan Hypertension Survival Study - LIFE and 4) The Losartan Renal Protection Study - RENAAL.", "entity1": "AT(1) receptor", "entity2": "losartan", "span1": [180, 194], "span2": [200, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4548": {"label": 8, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "MAO-A", "entity2": "5-MeO-DMT", "span1": [69, 74], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8567": {"label": 3, "data": {"text": "Immunofluorescence staining and western blotting demonstrated that cilostazol treatment reduced GFAP and VEGF expression in the retinas of OLETF rats.", "entity1": "VEGF", "entity2": "cilostazol", "span1": [105, 109], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5675": {"label": 1, "data": {"text": "Data suggest that bisphosphonates via modulation of the activity of small-GTPases induce apoptosis in neoplastic cells by DNA-CpG-demethylation and stimulation of FAS-expression.", "entity1": "GTPases", "entity2": "bisphosphonates", "span1": [74, 81], "span2": [18, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9830": {"label": 3, "data": {"text": "Improper function of these proteins can be induced by selective disruption of their complexes with Hsp90 using the benzoquinonoid ansamycin geldanamycin.", "entity1": "Hsp90", "entity2": "geldanamycin", "span1": [99, 104], "span2": [140, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6699": {"label": 5, "data": {"text": "Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively).", "entity1": "VR1", "entity2": "BCTC", "span1": [6, 9], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11343": {"label": 8, "data": {"text": "Phosphatidylserine (PtdSer) is made in mammalian cells by two PtdSer synthases, PSS1 and PSS2.", "entity1": "PSS2", "entity2": "Phosphatidylserine", "span1": [89, 93], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5398": {"label": 9, "data": {"text": "Furthermore, estrogen responsive genes in fish liver, ER\u03b1 and VTG, are not induced by CP[c]Ph, suggesting that the compound has no endocrine disrupting potential.", "entity1": "ER\u03b1", "entity2": "CP[c]Ph", "span1": [54, 57], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1751": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "cyclin D", "entity2": "GW572016", "span1": [146, 154], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"534": {"label": 1, "data": {"text": "We propose that Cu(I) binds the type-1 copper ion-binding site in the A1 domain and provides the essential requirement for a stable interaction between the heavy and light chains.", "entity1": "A1 domain", "entity2": "Cu(I)", "span1": [70, 79], "span2": [16, 21]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3122": {"label": 8, "data": {"text": "alpha-Tocopherol transfer protein (alpha-TTP), the product of the gene responsible for familial isolated vitamin E deficiency, plays an important role in maintaining the plasma alpha-tocopherol level by mediating the secretion of alpha-tocopherol by the liver.", "entity1": "alpha-Tocopherol transfer protein", "entity2": "alpha-tocopherol", "span1": [0, 33], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12406": {"label": 3, "data": {"text": "In conclusion, BPA has adverse effects on phosphorylation of Akt, GLUT4 translocation and (14)C-glucose oxidation.", "entity1": "GLUT4", "entity2": "BPA", "span1": [66, 71], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12905": {"label": 3, "data": {"text": "Moreover, NO production in LPS-stimulated macrophages that are expressing CSE mRNA was significantly reduced by the addition of L-Cys, a substrate for H(2)S, but enhanced by the selective CSE inhibitor beta-cyano-L-alanine but not by the CBS inhibitor aminooxyacetic acid.", "entity1": "CSE", "entity2": "beta-cyano-L-alanine", "span1": [188, 191], "span2": [202, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"10574": {"label": 2, "data": {"text": "Imiquimod (IMQ), an activator of Toll-like receptor-7 (TLR-7), induces by several routes a profound anti-viral and anti-tumor effect in vivo.", "entity1": "TLR-7", "entity2": "Imiquimod", "span1": [55, 60], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8864": {"label": 2, "data": {"text": "In the present study, using in vitro Th17 differentiation model, we examined effects of AhR activation by indoxyl 3-sulfate (I3S), a uremic toxin, on Th17 differentiation and investigated underlying mechanisms.", "entity1": "AhR", "entity2": "indoxyl 3-sulfate", "span1": [88, 91], "span2": [106, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5585": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "5-FU", "span1": [96, 119], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"9063": {"label": 1, "data": {"text": "Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites.", "entity1": "histamine H1 receptor", "entity2": "phenothiazine", "span1": [27, 48], "span2": [60, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11443": {"label": 1, "data": {"text": "We also studied the effects of thalidomide on COX-1, COX-2 or bcl-2 expression, TNFalpha, VEGF, GSH and cytochrome c in these cells.", "entity1": "cytochrome c", "entity2": "thalidomide", "span1": [104, 116], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2365": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "tyrosine kinases", "entity2": "BAY 43-9006", "span1": [110, 126], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5400": {"label": 1, "data": {"text": "Furthermore, estrogen responsive genes in fish liver, ER\u03b1 and VTG, are not induced by CP[c]Ph, suggesting that the compound has no endocrine disrupting potential.", "entity1": "ER\u03b1", "entity2": "estrogen", "span1": [54, 57], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4170": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "sulforaphane", "span1": [118, 122], "span2": [166, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12154": {"label": 1, "data": {"text": "CONCLUSIONS: Our data suggest that beta(1)-adrenergic receptor polymorphisms are important determinants of antihypertensive response to metoprolol.", "entity1": "beta(1)-adrenergic receptor", "entity2": "metoprolol", "span1": [35, 62], "span2": [136, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5181": {"label": 1, "data": {"text": "Dioscin-induced autophagy mitigates cell apoptosis through modulation of PI3K/Akt and ERK and JNK signaling pathways in human lung cancer cell lines.", "entity1": "Akt", "entity2": "Dioscin", "span1": [78, 81], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9855": {"label": 1, "data": {"text": "The results also suggest that: 1) irreversible ET-1 binding probably limits actions of receptor antagonists in vivo, and 2) an association of salicylates and ETA receptor antagonists should be used to evaluate the physiopathological role of ET-1 and may be of therapeutic interest in the treatment of ischemic heart disease.", "entity1": "ET-1", "entity2": "salicylates", "span1": [241, 245], "span2": [142, 153]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2276": {"label": 3, "data": {"text": "In this article, the action of dasatinib (BMS-354825) is contrasted with that of imatinib, a kinase inhibitor that is currently being used to treat chronic myelogenous leukemia and other disorders.", "entity1": "kinase", "entity2": "BMS-354825", "span1": [93, 99], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3806": {"label": 4, "data": {"text": "One of the CB2 agonists, N-cyclopentyl-4-ethoxy-6-(4-methylpiperidin-1-yl)-1,3,5-triazin-2-amine (19, -logEC(50)=7.5, E(max)=255%) was selected for further development.", "entity1": "CB2", "entity2": "N-cyclopentyl-4-ethoxy-6-(4-methylpiperidin-1-yl)-1,3,5-triazin-2-amine", "span1": [11, 14], "span2": [25, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1299": {"label": 3, "data": {"text": "This study was conducted in order to understand the association between acute renal failure and the two COX-2 inhibitors celecoxib and rofecoxib.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [104, 109], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14350": {"label": 3, "data": {"text": "mRNA levels of receptor activator of nuclear factor kappa-B (RANK), its ligand RANKL, tumor necrosis factor alpha (TNF-\u03b1) and RANKL/osteoprotegerin (OPG) ratio were diminished in the periodontium of CCL3(-/-) mice and in the group treated with Met-RANTES.", "entity1": "RANKL", "entity2": "Met", "span1": [79, 84], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2613": {"label": 4, "data": {"text": "The identification of the succinate receptor SUCNR1 in platelets is of particular interest, because physiologically relevant concentrations of succinate were shown to potentiate the effect of low doses of a variety of platelet agonists.", "entity1": "succinate receptor", "entity2": "succinate", "span1": [26, 44], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9360": {"label": 3, "data": {"text": "The present results suggest that the action of DMI in this animal model is unlikely to be directly related to a reduction in beta-adrenoceptors but may be related to a reduction in frontal cortical 5-HT2A receptors.", "entity1": "beta-adrenoceptors", "entity2": "DMI", "span1": [125, 143], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12845": {"label": 1, "data": {"text": "However, there were some significant differences among Captopril (30 mg/kg or 45 mg/kg), enalapril (20 mg/kg), and N-acetylcysteine particular in the activity of PON1 and ACE.", "entity1": "ACE", "entity2": "enalapril", "span1": [171, 174], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10030": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Arg", "span1": [199, 208], "span2": [54, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7656": {"label": 3, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-2", "entity2": "captopril", "span1": [0, 5], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7115": {"label": 5, "data": {"text": "Fulvestrant is a novel ER antagonist that destroys the ER and its signaling pathway and is not associated with tamoxifen-like agonist effects.", "entity1": "ER", "entity2": "Fulvestrant", "span1": [23, 25], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13486": {"label": 5, "data": {"text": "[N-(piperidin-1-yl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxyamide] (SR 141716A), a selective cannabinoid CB1 receptor antagonist, injected into the paraventricular nucleus of the hypothalamus (PVN) of male rats, induces penile erection.", "entity1": "cannabinoid CB1 receptor", "entity2": "N-(piperidin-1-yl)-5-(4-chlorophenyl)-4-methyl-1H-pyrazole-3-carboxyamide", "span1": [102, 126], "span2": [1, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7332": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "alanine serine cysteine transporter 1", "entity2": "glutamine", "span1": [196, 233], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12468": {"label": 1, "data": {"text": "The DPYD-Y186C variant was unique to individuals of African ancestry, and DPD activity was 46% lower in carriers as compared with noncarriers (279\u2009\u00b1\u200935 vs. 514\u2009\u00b1\u2009168 pmol 5-FU min(-1) mg(-1); P = 0.00029).", "entity1": "DPD", "entity2": "5-FU", "span1": [74, 77], "span2": [171, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4509": {"label": 3, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "hCES1", "entity2": "acyl glucuronides", "span1": [129, 134], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4704": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "TCDD", "span1": [103, 109], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4191": {"label": 2, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "Cytochrome c", "entity2": "PTE", "span1": [220, 232], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11329": {"label": 1, "data": {"text": "The degree of improvement in heart failure was assessed from the ratio of change in the plasma BNP concentration, 2 weeks, 1 month and 3 months after the commencement of carvedilol administration.", "entity1": "BNP", "entity2": "carvedilol", "span1": [95, 98], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1974": {"label": 3, "data": {"text": "We demonstrate that among the three nitrates, only SNP inhibits HIF-1 activation in response to hypoxia.", "entity1": "HIF-1", "entity2": "SNP", "span1": [64, 69], "span2": [51, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6231": {"label": 1, "data": {"text": "However, [3H]eletriptan had over 6-fold higher affinity than [3H]sumatriptan at the 5-HT1D receptor (K(D)): 0.92 and 6.58 nM, respectively) and over 3-fold higher affinity than [3H]sumatriptan at the 5-HT1B receptor (K(D): 3.14 and 11.07 nM, respectively).", "entity1": "5-HT1D", "entity2": "[3H]eletriptan", "span1": [84, 90], "span2": [9, 23]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2824": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "iNOS", "entity2": "1400W dihydrochloride", "span1": [152, 156], "span2": [96, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2455": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "adenosine triphosphate binding cassette (ABC)-transporter", "entity2": "cisplatin", "span1": [4, 61], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9448": {"label": 9, "data": {"text": "16,16-dimethyl-PGE2 and two putative EP1 antagonists, AH6809 and SC-19220, did not show any significant binding to this receptor.", "entity1": "EP1", "entity2": "SC-19220", "span1": [37, 40], "span2": [65, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"468": {"label": 5, "data": {"text": "These results indicate that the positive inotropic effect, mediated via (+/-)-tamsulosin- and oxymetazoline-sensitive subtype of alpha 1-adrenoceptors, is exerted by a subcellular mechanism that is independent of the accumulation of inositol phosphates.", "entity1": "alpha 1-adrenoceptors", "entity2": "(+/-)-tamsulosin", "span1": [129, 150], "span2": [72, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3186": {"label": 4, "data": {"text": "RGM-1 cells were treated with CDCA or GW4064, an FXR agonist, in the presence or absence of guggulsterone, an FXR antagonist.", "entity1": "FXR", "entity2": "GW4064", "span1": [49, 52], "span2": [38, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14966": {"label": 3, "data": {"text": "Results confirmed that YR-11 peptide inhibited pro-inflammatory cytokines in the sera and hind paw tissues of AIA rats through its suppressive effect on RANKL induced nuclear translocation of NF-\u03baB.", "entity1": "NF-\u03baB", "entity2": "YR-11", "span1": [192, 197], "span2": [23, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6682": {"label": 2, "data": {"text": "Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively).", "entity1": "TRPM8", "entity2": "menthol", "span1": [96, 101], "span2": [105, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13917": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "Kir6.2", "entity2": "Phenformin", "span1": [183, 189], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9549": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "IFN-gamma", "entity2": "cAMP", "span1": [47, 56], "span2": [204, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5791": {"label": 0, "data": {"text": "From sequence analysis of the cDNA and the N- and C-terminal amino acid analyses of the purified protein, it is deduced that porcine kidney ACY-1 consists of two identical subunits (M(r) 45,260), each of which consists of a single chain of 406 amino acids with acetylalanine at the N-terminus.", "entity1": "porcine kidney ACY-1", "entity2": "N", "span1": [125, 145], "span2": [282, 283]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4479": {"label": 3, "data": {"text": "In this study, we assessed the effects of clopidogrel and clarithromycin, known CYP2B6 and CYP3A inhibitors, respectively, on the enantioselective disposition of racemic sibutramine in conjunction with CYP2B6 polymorphisms in humans.", "entity1": "CYP2B6", "entity2": "clopidogrel", "span1": [80, 86], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1752": {"label": 3, "data": {"text": "Increased phosphorylation of p95ErbB2 and AKT in response to HRG was abrogated to varying degrees by GW572016.", "entity1": "p95ErbB2", "entity2": "GW572016", "span1": [29, 37], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"128": {"label": 3, "data": {"text": "These observations suggest that some of the pharmacological actions of felodipine on smooth muscle may involve inhibition of calmodulin-dependent enzymes which are functionally involved in the regulation of smooth muscle contraction.", "entity1": "calmodulin-dependent enzymes", "entity2": "felodipine", "span1": [125, 153], "span2": [71, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11543": {"label": 3, "data": {"text": "Dexamethasone suppresses histamine synthesis by repressing both transcription and activity of HDC in allergic rats.", "entity1": "HDC", "entity2": "Dexamethasone", "span1": [94, 97], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9711": {"label": 1, "data": {"text": "A novel missense mutation, G663A, in exon 5 of the erythroid-specific delta-aminolevulinate synthase gene (ALAS2) was identified in a Japanese male with pyridoxine-responsive sideroblastic anemia.", "entity1": "erythroid-specific delta-aminolevulinate synthase", "entity2": "pyridoxine", "span1": [51, 100], "span2": [153, 163]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10783": {"label": 1, "data": {"text": "The effects of simvastatin were abolished by the addition of the product of the HMG-CoA reductase, mevalonate, indicating the involvement of HMG-CoA reductase in the action of simvastatin.", "entity1": "HMG-CoA reductase", "entity2": "simvastatin", "span1": [141, 158], "span2": [176, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6035": {"label": 1, "data": {"text": "We conclude that despite small differences concerning the enantiomeric selectivity and affinity of rauwolscine and yohimbine, the close pharmacological identity of 5-HT receptors in rat stomach fundus and the recently cloned 5-HT2B receptor is maintained.", "entity1": "5-HT receptors", "entity2": "rauwolscine", "span1": [164, 178], "span2": [99, 110]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12368": {"label": 3, "data": {"text": "Tamoxifen represses miR-200 microRNAs and promotes epithelial-to-mesenchymal transition by up-regulating c-Myc in endometrial carcinoma cell lines.", "entity1": "miR-200", "entity2": "Tamoxifen", "span1": [20, 27], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4033": {"label": 3, "data": {"text": "Benzofuran 28 showed dose responsive target engagement and provides a useful tool to explore a LTA(4)H inhibitor for the treatment of inflammatory diseases, such as asthma and inflammatory bowel disease (IBD).", "entity1": "LTA(4)H", "entity2": "Benzofuran", "span1": [95, 102], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10923": {"label": 3, "data": {"text": "The gastric mucin secretory responses to isoproterenol, furthermore, were inhibited by PP2, a selective inhibitor of tyrosine kinase Src responsible for ligand-independent EGFR autophosphorylation, but not by ERK inhibitor, PD98059.", "entity1": "ERK", "entity2": "PD98059", "span1": [209, 212], "span2": [224, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7987": {"label": 2, "data": {"text": "These results demonstrated for the first time that ISO induces apoptosis in HepG2 cells through inactivating ERK1/2 kinase and activating JNK and p38 kinases, and ROS stimulated by ISO is able to activate the MAPK singaling pathway as the upstream signaling molecules.", "entity1": "MAPK", "entity2": "ISO", "span1": [209, 213], "span2": [181, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10525": {"label": 2, "data": {"text": "Metformin, a drug widely used in the treatment of type 2 diabetes, has recently been shown to act on skeletal muscle and liver in part through the activation of AMP-activated protein kinase (AMPK).", "entity1": "AMP-activated protein kinase", "entity2": "Metformin", "span1": [161, 189], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13306": {"label": 3, "data": {"text": "RESULTS: We show that sorafenib is a potent inhibitor of ETV6-PDGFRbeta and FLT3 mutants, including some of the mutants that confer resistance to PKC412 and other FLT3 inhibitors.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [76, 80], "span2": [22, 31]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2842": {"label": 7, "data": {"text": "The enzyme requires PLP and divalent cations such as Ca(2+), Mg(2+), or Mn(2+), but not ATP, whereas mammalian serine racemase activity is increased by ATP.", "entity1": "serine racemase", "entity2": "Mg(2+)", "span1": [111, 126], "span2": [61, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10242": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "SSAT", "entity2": "spermidine", "span1": [121, 125], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12909": {"label": 3, "data": {"text": "While either blockage of HO activity by the HO inhibitor, tin protoporphyrin IX, or down-regulation of HO-1 expression by HO-1 small interfering RNA (siRNA) reversed the inhibitory effects of H(2)S on iNOS expression and NO production, HO-1 overexpression produced the same inhibitory effects of H(2)S. In addition, LPS-induced nuclear factor (NF)-kappaB activation was diminished in RAW264.7 macrophages preincubated with H(2)S. Interestingly, the inhibitory effect of H(2)S on NF-kappaB activation was reversed by the transient transfection with HO-1 siRNA, but was mimicked by either HO-1 gene transfection or treatment with carbon monoxide (CO), an end product of HO-1.", "entity1": "NF-kappaB", "entity2": "H(2)S", "span1": [479, 488], "span2": [470, 475]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5260": {"label": 8, "data": {"text": "Platelet-induced COX-2-dependent PGE2 synthesis in HT29 cells was involved in downregulation of p21(WAF1/CIP1) and upregulation of cyclinB1, since these effects were prevented by rofecoxib(a selective COX-2 inhibitor) and rescued by exogenous PGE2.", "entity1": "COX-2", "entity2": "PGE2", "span1": [17, 22], "span2": [33, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10071": {"label": 9, "data": {"text": "Salicylates inhibited ATPase activity stimulated by this specific heptapeptide but did not block ATP binding or induce BiP expression.", "entity1": "BiP", "entity2": "Salicylates", "span1": [119, 122], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6502": {"label": 3, "data": {"text": "Pemetrexed disodium (ALIMTA) is a novel antimetabolite that inhibits at least three folate-dependent enzymes, thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase.", "entity1": "glycinamide ribonucleotide formyltransferase", "entity2": "Pemetrexed disodium", "span1": [161, 205], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7120": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "PDE5Delta1-419", "entity2": "N", "span1": [231, 245], "span2": [97, 98]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13466": {"label": 1, "data": {"text": "The cytosolic ACC1 is expressed primarily in liver and adipose tissue, and uses malonyl-coenzyme A as a key building block in fatty acid biosynthesis.", "entity1": "ACC1", "entity2": "malonyl-coenzyme A", "span1": [14, 18], "span2": [80, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8570": {"label": 4, "data": {"text": "Other dams received 1.8ng/kg/day of a mixture of aryl hydrocarbon receptor (AhR) agonists (non-ortho PCBs, PC-dibenzodioxins and PC-dibenzofurans) without or with 0.5M (0.5MAhR).", "entity1": "aryl hydrocarbon receptor", "entity2": "non-ortho PCB", "span1": [49, 74], "span2": [91, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"337": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "bovine pancreatic ribonuclease A", "entity2": "2'CMP", "span1": [63, 95], "span2": [233, 238]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5983": {"label": 1, "data": {"text": "Analysis of the results of this paper reveals that normal plasma components, Cl- and fibrinogen, exert major regulatory roles on the ability of [Glu1]Pg to be activated by two-chain rec-t-PA, in in vitro systems.", "entity1": "[Glu1]Pg", "entity2": "Cl-", "span1": [144, 152], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2251": {"label": 0, "data": {"text": "SSAT was found to self-acetylate lysine-26 in the presence of AcCoA and absence of substrate, a reaction apparently catalzyed by AcCoA bound in the second channel of the asymmetric dimer.", "entity1": "SSAT", "entity2": "lysine", "span1": [0, 4], "span2": [33, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6516": {"label": 3, "data": {"text": "Aliskiren has the potential to become the first orally active renin inhibitor that provides a true alternative to ACE-inhibitors and Ang II receptor antagonists in therapy for hypertension and other cardiovascular and renal diseases.", "entity1": "renin", "entity2": "Aliskiren", "span1": [62, 67], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5317": {"label": 3, "data": {"text": "A series of phosphorylated flavonoids were synthesized and investigated in\u00a0vitro as inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE).", "entity1": "AChE", "entity2": "phosphorylated flavonoids", "span1": [164, 168], "span2": [12, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14310": {"label": 3, "data": {"text": "Protein expression of Ugt1a6 also decreased and corresponded with reduced in vitro glucuronidation of bisphenol A in S9 fractions from livers of pregnant mice.", "entity1": "Ugt1a6", "entity2": "bisphenol A", "span1": [22, 28], "span2": [102, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12463": {"label": 1, "data": {"text": "The responses to 5-FU, with respect to both toxicity and efficacy, vary among racial groups, potentially because of variability in the activity levels of the enzyme dihydropyrimidine dehydrogenase (DPD, encoded by the DPYD gene).", "entity1": "dihydropyrimidine dehydrogenase", "entity2": "5-FU", "span1": [165, 196], "span2": [17, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2605": {"label": 3, "data": {"text": "OBJECTIVES: The alkaloid galantamine (GAL), which exhibits a combined anticholinesterase and direct parasympathomimetic mechanism of action, is employed in conjunction with therapeutic interventions in the stimulation of central cholinergic transfer in cognitive diseases.", "entity1": "anticholinesterase", "entity2": "galantamine", "span1": [70, 88], "span2": [25, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7235": {"label": 5, "data": {"text": "Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5.", "entity1": "human androgen receptor", "entity2": "Gonadotropin-releasing hormone", "span1": [87, 110], "span2": [0, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11147": {"label": 8, "data": {"text": "Levodopa is absorbed in the small bowel and is rapidly catabolized by aromatic-L-amino-acid decarboxylase (AADC) and catechol-O-methyltransferase (COMT).", "entity1": "AADC", "entity2": "Levodopa", "span1": [107, 111], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14551": {"label": 3, "data": {"text": "Neurodegeneration was related with decreased [(3)H]glutamate uptake and decreased Akt immunoreactivity, however phospho-GSK-3-\u03b2 (Ser9) was not altered in (PhTe)(2) injected rat.", "entity1": "Akt", "entity2": "(PhTe)(2)", "span1": [82, 85], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6052": {"label": 2, "data": {"text": "Neither ryanodine nor EGTA inhibited down-regulation of alpha-AR mRNA by NE.", "entity1": "alpha-AR", "entity2": "EGTA", "span1": [56, 64], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12620": {"label": 1, "data": {"text": "In addition, three IP ligands, iloprost, carbacyclin and isocarbacyclin, and one TP ligand, STA2, bound to this receptor with Ki values comparable to the Ki values of these compounds for the IP and TP receptors, respectively.", "entity1": "IP", "entity2": "iloprost", "span1": [19, 21], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7551": {"label": 3, "data": {"text": "As further support, alpha-methyl-DL-aspartate, an inhibitor of argininosuccinate synthase (AS), a component of the citrulline-NO cycle, inhibited NO production in a dose-dependent manner.", "entity1": "argininosuccinate synthase", "entity2": "alpha-methyl-DL-aspartate", "span1": [63, 89], "span2": [20, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11426": {"label": 1, "data": {"text": "We also show that an intronic polymorphism in the SCN1A gene shows significant association with maximum doses in regular usage of both carbamazepine and phenytoin (P = 0.0051 and P = 0.014, respectively).", "entity1": "SCN1A", "entity2": "phenytoin", "span1": [50, 55], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16064": {"label": 3, "data": {"text": "The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described.", "entity1": "anaplastic lymphoma kinase", "entity2": "LDK378", "span1": [108, 134], "span2": [150, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13741": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "L-type calcium channel", "entity2": "DHP", "span1": [4, 26], "span2": [102, 105]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11120": {"label": 1, "data": {"text": "Rec 15/2739, WB 4101, SL 89,0591, (+)- and (-)- tamsulosin showed selectivity for alpha 1A and alpha 1D adrenoceptors relative to the alpha 1B subtype.", "entity1": "alpha 1B subtype", "entity2": "Rec 15/2739", "span1": [134, 150], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10051": {"label": 1, "data": {"text": "Cembranoid and long-chain alkanol sites on the nicotinic acetylcholine receptor and their allosteric interaction.", "entity1": "nicotinic acetylcholine receptor", "entity2": "Cembranoid", "span1": [47, 79], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"4063": {"label": 3, "data": {"text": "Jaspamide also inhibited other channels including Cav1.2, Cav3.2, and HCN2; however, the Kv11.1 (hERG) channel was minimally affected.", "entity1": "HCN2", "entity2": "Jaspamide", "span1": [70, 74], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8671": {"label": 2, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "TAp73", "entity2": "cisplatin", "span1": [189, 194], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9229": {"label": 5, "data": {"text": "The binding of FHA-HIS was inhibited on 35-79% of the platelets by the histamine H1 receptor antagonists diphenhydramine and clemastine.", "entity1": "histamine H1 receptor", "entity2": "clemastine", "span1": [71, 92], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1979": {"label": 1, "data": {"text": "Thus far, PHA1 has been attributed to mutations affecting the mineralocorticoid receptor or any of the three subunits assembling the amiloride-sensitive epithelial sodium channel (ENaC).", "entity1": "ENaC", "entity2": "amiloride", "span1": [180, 184], "span2": [133, 142]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14194": {"label": 1, "data": {"text": "CCAAT/Enhancer-binding protein-homologous protein sensitizes to SU5416 by modulating p21 and PI3K/Akt signal pathway in FRO anaplastic thyroid carcinoma cells.", "entity1": "PI3K", "entity2": "SU5416", "span1": [93, 97], "span2": [64, 70]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7856": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "mGlu1", "entity2": "1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid", "span1": [40, 45], "span2": [149, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1938": {"label": 3, "data": {"text": "No influence of moderate hepatic impairment on the pharmacokinetics of lumiracoxib, an oral COX-2 selective inhibitor.", "entity1": "COX-2", "entity2": "lumiracoxib", "span1": [92, 97], "span2": [71, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7739": {"label": 3, "data": {"text": "PURPOSE: XL184 (cabozantinib) is a potent inhibitor of MET, vascular endothelial growth factor receptor 2 (VEGFR2), and RET, with robust antiangiogenic, antitumor, and anti-invasive effects in preclinical models.", "entity1": "RET", "entity2": "cabozantinib", "span1": [120, 123], "span2": [16, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9363": {"label": 3, "data": {"text": "The time course of the reduction in the number of 5-HT2A receptors was similar to that of the DMI-induced behavioural changes whereas that for the reduction in beta-adrenoceptors was clearly different.", "entity1": "5-HT2A", "entity2": "DMI", "span1": [50, 56], "span2": [94, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1001": {"label": 0, "data": {"text": "For MICA3, a surface loop containing the sequence PEVKEK and two adjacent exposed helixes were identified in the PLP binding domain as well as a region of the C terminus of GAD65 that has previously been identified as critical for MICA3 binding.", "entity1": "GAD65", "entity2": "C", "span1": [173, 178], "span2": [159, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6218": {"label": 3, "data": {"text": "This study thus demonstrates that the first administration of the recommended starting dose of irbesartan induces a greater and longer lasting Ang II receptor blockade than that of valsartan and losartan in normotensive subjects.", "entity1": "Ang II receptor", "entity2": "irbesartan", "span1": [143, 158], "span2": [95, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13784": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Vatalanib", "span1": [14, 16], "span2": [186, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10007": {"label": 1, "data": {"text": "Domperidone and haloperidol, which have affinity for dopamine D3 receptor, also inhibited R(+)-7-OH-DPAT-induced hypothermia.", "entity1": "dopamine D3 receptor", "entity2": "R(+)-7-OH-DPAT", "span1": [53, 73], "span2": [90, 104]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1027": {"label": 3, "data": {"text": "In contrast, in the same system, N-type currents, formed from transiently transfected alpha(1B)/alpha(2)delta-1/beta(3), showed strong G-protein-mediated inhibition.", "entity1": "G-protein", "entity2": "N", "span1": [135, 144], "span2": [33, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12548": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "transcobalamin II", "entity2": "CN-Cbl", "span1": [193, 210], "span2": [176, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1962": {"label": 1, "data": {"text": "A receptor binding assay using rat forebrain and spinal cord membrane preparations demonstrated that [3H]CP-101,606 bound to the brain NR2B receptor with a greater extent compared to the spinal cord one.", "entity1": "NR2B", "entity2": "[3H]CP-101,606", "span1": [135, 139], "span2": [101, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3665": {"label": 3, "data": {"text": "The mRNA levels of microphthalmia-associated transcription factor (MITF) and its downstream genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 were reduced by artemisinic acid treatment.", "entity1": "tyrosinase-related protein (TRP)-1", "entity2": "artemisinic acid", "span1": [110, 144], "span2": [172, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4192": {"label": 2, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "Caspase3", "entity2": "PTE", "span1": [246, 254], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12196": {"label": 1, "data": {"text": "A follow-up study of the expression of D6D and D5D genes in Chinese who live in European countries with high SFA and MUFA diets would be of interest.", "entity1": "D6D", "entity2": "MUFA", "span1": [39, 42], "span2": [117, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5238": {"label": 3, "data": {"text": "In a cell-based model, bleomycin suppressed Nrf2 activation via extracellular signal-related kinase phosphorylation, enhancing intracellular reactive oxygen species in lung fibroblasts and stimulating abnormal cell proliferation and collagen secretion.", "entity1": "Nrf2", "entity2": "bleomycin", "span1": [44, 48], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14916": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "\u0394(5)-androstenediol", "span1": [257, 260], "span2": [35, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12197": {"label": 1, "data": {"text": "A follow-up study of the expression of D6D and D5D genes in Chinese who live in European countries with high SFA and MUFA diets would be of interest.", "entity1": "D5D", "entity2": "MUFA", "span1": [47, 50], "span2": [117, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5286": {"label": 2, "data": {"text": "TCDD also caused a fast (within 30min as judged by the increase in its mRNA level) activation of cytosolic phospholipase A2 (cPLA2).", "entity1": "cPLA2", "entity2": "TCDD", "span1": [125, 130], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15984": {"label": 3, "data": {"text": "The improved survival rates for obese mice chronically treated with vildagliptin suggest that chronic DPP4 inhibition potentially results in additional quality-adjusted life-years for individuals with type 2 diabetes, which is the primary goal of any diabetes therapy.", "entity1": "DPP4", "entity2": "vildagliptin", "span1": [102, 106], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15532": {"label": 2, "data": {"text": "CK significantly inhibited DMN-induced increases in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, fibrosis score, and hepatic malondialdehyde and collagen content.", "entity1": "alanine aminotransferase", "entity2": "DMN", "span1": [58, 82], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7286": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "TGF-beta2", "entity2": "PFD", "span1": [68, 77], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"988": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "eNOS", "entity2": "tetrahydrobiopterin", "span1": [114, 118], "span2": [38, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"5913": {"label": 8, "data": {"text": "accelerating reverse transport of cholesteryl esters from high-density lipoproteins to lower-density lipoproteins.", "entity1": "lower-density lipoproteins", "entity2": "cholesteryl esters", "span1": [87, 113], "span2": [34, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7017": {"label": 1, "data": {"text": "DVS showed weak binding affinity (62% inhibition at 100 microM) at the human dopamine (DA) transporter.", "entity1": "human dopamine (DA) transporter", "entity2": "DVS", "span1": [71, 102], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14130": {"label": 2, "data": {"text": "Celastrol also inhibited cell proliferation, while increasing sub-G0 DNA fragmentation and Annexin V markers of apoptosis.", "entity1": "Annexin V", "entity2": "Celastrol", "span1": [91, 100], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3280": {"label": 3, "data": {"text": "Assays examining the ability of TFP to block S100A4-mediated disassembly of myosin-IIA filaments demonstrate that significant inhibition of S100A4 function occurs only at TFP concentrations that promote S100A4 oligomerization.", "entity1": "myosin-IIA", "entity2": "TFP", "span1": [76, 86], "span2": [32, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6477": {"label": 8, "data": {"text": "Carbonic anhydrase (CA) is a zinc enzyme that catalyses the reversible hydration reaction of CO2 and plays a major role in the acid-base balance.", "entity1": "Carbonic anhydrase", "entity2": "CO2", "span1": [0, 18], "span2": [93, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9176": {"label": 3, "data": {"text": "Staining was largely absent when substrate was omitted or after pretreatment with the irreversible SSAO inhibitor, hydralazine and the slowly reversible inhibitor, semicarbazide.", "entity1": "SSAO", "entity2": "hydralazine", "span1": [99, 103], "span2": [115, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15355": {"label": 8, "data": {"text": "Additionally, there was a significant difference in plasma concentrations of (R)-5-hydroxyomeprazole among CYP2C19 genotype groups, whereas no significant differences were observed in that of (S)-5-hydroxyomeprazole.", "entity1": "CYP2C19", "entity2": "(R)-5-hydroxyomeprazole", "span1": [107, 114], "span2": [77, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12033": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "peroxidases", "entity2": "hypoiodite", "span1": [18, 29], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3285": {"label": 9, "data": {"text": "Prednisolone fast feedback was only reduced by glucocorticoid receptor antagonist pretreatment and not by mineralocorticoid receptor antagonism, suggesting a glucocorticoid receptor-mediated pathway.", "entity1": "mineralocorticoid receptor", "entity2": "Prednisolone", "span1": [106, 132], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5199": {"label": 3, "data": {"text": "Pharmacological doses of the mTOR inhibitor rapamycin reduce albuminura in diabetes.", "entity1": "mTOR", "entity2": "rapamycin", "span1": [29, 33], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3173": {"label": 4, "data": {"text": "Terbutaline (Bricanyl) and its prodrug Bambuterol (Bambec) are highly potent beta(2)-adrenoceptor agonists often used in asthma patients.", "entity1": "beta(2)-adrenoceptor", "entity2": "Terbutaline", "span1": [77, 97], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6210": {"label": 1, "data": {"text": "This study therefore characterized the binding of DF to the sigma receptors and NMDA-linked PCP sites and examined the anticonvulsant as well as locomotor effects of DF in mice in comparison with those of DM and DR. We found that DF, DM, and DR were relative high-affinity ligands at sigma-1 receptors (Ki=151, 205, 144 nM, respectively) while all of them were with low affinity at sigma-2 receptors (Ki=4-11 microM).", "entity1": "sigma-1 receptors", "entity2": "DF", "span1": [284, 301], "span2": [230, 232]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8130": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "Bcl-2", "entity2": "Sal", "span1": [93, 98], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"607": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "p-bromophenacyl bromide", "span1": [178, 191], "span2": [96, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10084": {"label": 1, "data": {"text": "Three replicate studies in the oral surgery model of acute pain used submucosal microdialysis sample collection for the measurement of prostaglandin E2 (PGE2; a product of both COX-1 and COX-2) and thromboxane B2 (as a biomarker for COX-1 activity) with parallel assessments of pain.", "entity1": "COX-1", "entity2": "thromboxane B2", "span1": [233, 238], "span2": [198, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14073": {"label": 1, "data": {"text": "Berberine exerts suppressive effects on phenotype changes and ECM production in NPDFs via p38 signaling pathway interference.", "entity1": "p38", "entity2": "Berberine", "span1": [90, 93], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"15519": {"label": 1, "data": {"text": "A highly potent inhibition of the peroxidase catalytic reaction by NO/SNO was seen in assays employing the coupled Prx-Trx system.", "entity1": "Prx", "entity2": "NO", "span1": [115, 118], "span2": [67, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10265": {"label": 8, "data": {"text": "Reuptake of extracellular noradrenaline (NA) into superior cervical ganglion (SCG) neurones is mediated by means of the noradrenaline transporter (NAT, uptake 1).", "entity1": "NAT", "entity2": "noradrenaline", "span1": [147, 150], "span2": [26, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6953": {"label": 1, "data": {"text": "[3H]-maraviroc bound with high affinity to CCR5 from macaque (K(d) = 1.36+/-0.07 nM) and human (K(d) = 0.86 +/- 0.08 nM), but was found to dissociate approximately 10-fold more quickly from macaque CCR5.", "entity1": "macaque CCR5", "entity2": "[3H]-maraviroc", "span1": [190, 202], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13123": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "topoisomerase IIalpha", "entity2": "etopoxide", "span1": [41, 62], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4816": {"label": 1, "data": {"text": "Taken together, we conclude that the thiourea series of compounds share a similar cellular mechanism that includes interaction with LolA in addition to the well-characterized target MreB.", "entity1": "MreB", "entity2": "thiourea", "span1": [182, 186], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12289": {"label": 1, "data": {"text": "Cabozantinib may provide clinical benefit by simultaneously targeting multiple pathways of importance in MTC, including MET, VEGFR2, and RET.", "entity1": "MET", "entity2": "Cabozantinib", "span1": [120, 123], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6258": {"label": 1, "data": {"text": "At the human dopamine transporter, only pimozide (K(D) = 69+/-3) ziprasidone (K(D) = 76+/-5) had notable potency.", "entity1": "human dopamine transporter", "entity2": "pimozide", "span1": [7, 33], "span2": [40, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"3969": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "Pin1", "entity2": "Pro", "span1": [66, 70], "span2": [146, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"12315": {"label": 1, "data": {"text": "In an effort to understand the shedding process of AChE, we have used several pharmacological treatments, which showed that it is likely to be mediated in part by an EDTA- and batimastat-sensitive, but GM6001-insensitive metalloprotease, with the possible additional involvement of a thiol isomerase.", "entity1": "metalloprotease", "entity2": "batimastat", "span1": [221, 236], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1378": {"label": 3, "data": {"text": "These effects resemble those seen with N-terminal deletions (DeltaN) of K(IR)6.0, and application of Ntp to DeltaNK(ATP) channels decreased their P(O(max)) and apparent IC(50) for ATP in the absence of Mg(2+).", "entity1": "DeltaNK(ATP) channels", "entity2": "ATP", "span1": [108, 129], "span2": [180, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7670": {"label": 3, "data": {"text": "Some of these structurally related compounds have a very different behavior against the widespread isozyme CA II, with chlorthalidone, trichloromethiazide, and furosemide being efficient inhibitors against CA II (K(I)s of 65-138 nM), whereas indapamide is a much weaker one (K(I) of 2520 nM).", "entity1": "CA II", "entity2": "indapamide", "span1": [206, 211], "span2": [242, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7128": {"label": 1, "data": {"text": "Binding of cGMP to GAF-A increases cNPK phosphorylation of PDE5 and improves catalytic site affinity for cGMP or inhibitors.", "entity1": "GAF-A", "entity2": "cGMP", "span1": [19, 24], "span2": [11, 15]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4431": {"label": 8, "data": {"text": "Type 2 11\u03b2-hydroxysteroid dehydrogenase encoded by the HSD11B2 gene converts cortisol to inactive cortisone, and alteration in this enzymatic activity might affect glucose homeostasis by affecting circulating levels or tissue availability of glucocorticoids.", "entity1": "Type 2 11\u03b2-hydroxysteroid dehydrogenase", "entity2": "cortisone", "span1": [0, 39], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15825": {"label": 1, "data": {"text": "An increase in the energy required to remove the same anion from the tridentate receptor when compared to the bidentate and monodentate receptors is explained as being due to the increase in halogen bonding interactions.", "entity1": "tridentate receptor", "entity2": "halogen", "span1": [69, 88], "span2": [191, 198]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6326": {"label": 1, "data": {"text": "Following 6 h of in vivo intracerebroventricular injections of 100 nmol of RTI-76, there was a dose- and time-dependent reduction (- 60%) of SERT binding in hippocampus and striatum, without a change in the Kd.", "entity1": "SERT", "entity2": "RTI-76", "span1": [141, 145], "span2": [75, 81]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13769": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "kinase", "entity2": "SU 11248", "span1": [247, 253], "span2": [202, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8930": {"label": 5, "data": {"text": "Carvedilol produced significant inhibition of the alpha 1 adrenoceptor mediated pressor response to cirazoline in the pithed rat, but had no effect on the alpha 2 adrenoceptor mediated pressor response to B-HT 933, suggesting that carvedilol is also an alpha 1 adrenoceptor antagonist at antihypertensive doses.", "entity1": "alpha 1 adrenoceptor", "entity2": "carvedilol", "span1": [253, 273], "span2": [231, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3556": {"label": 2, "data": {"text": "LTD4 also induced expression of cysteinyl leukotriene receptor 1 (CysLT(1)R) and NF-\u03baB p65 in the hippocampus and cortex.", "entity1": "p65", "entity2": "LTD4", "span1": [87, 90], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4260": {"label": 0, "data": {"text": "Interestingly, ursolic acid increased the phosphorylation of AMPK and coenzyme A carboxylase and also enhanced phosphorylation of GSK3\u03b2 at inactive form serine 9, whereas ursolic acid attenuated the phosphorylation of AKT and mTOR in HepG2 cells.", "entity1": "GSK3\u03b2", "entity2": "serine", "span1": [130, 135], "span2": [153, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2903": {"label": 3, "data": {"text": "In vitro, acetaminophen elicited a 4.4-fold selectivity toward COX-2 inhibition (IC(50)=113.7 micromol/L for COX-1; IC(50)=25.8 micromol/L for COX-2).", "entity1": "COX-1", "entity2": "acetaminophen", "span1": [109, 114], "span2": [10, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2976": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "L765A", "entity2": "IBMX", "span1": [78, 83], "span2": [56, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13150": {"label": 5, "data": {"text": "The changes in CysLT1 receptor expression 24 h after NMDA injection and the effects of a CysLT1 receptor antagonist, pranlukast (0.01 and 0.1 mg/kg), an NMDA receptor antagonist, ketamine (30 mg/kg), and an antioxidant, edaravone (9 mg/kg) were observed.", "entity1": "CysLT1 receptor", "entity2": "pranlukast", "span1": [89, 104], "span2": [117, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2034": {"label": 8, "data": {"text": "Firstly, the V(max) of GAD was increased when ApoCaM was present whereas the affinity for the substrate, glutamate, was not affected.", "entity1": "GAD", "entity2": "glutamate", "span1": [23, 26], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"4562": {"label": 3, "data": {"text": "In addition, ethanol induced degradation of DNA methyltransferases (DNMT-1, DNMT-3a, and DNMT-3b), as well as the methyl CpG-binding proteins (MeCP-2, MBD-2 and MBD-3), in MEF cells by the proteasomal pathway.", "entity1": "MBD-2", "entity2": "ethanol", "span1": [151, 156], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"382": {"label": 3, "data": {"text": "In vitro studies with blood-derived T cells, however, show inhibition of all three cytokines by GCS.", "entity1": "cytokines", "entity2": "GCS", "span1": [83, 92], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4160": {"label": 2, "data": {"text": "An amphiphile with branched poly(ethylene glycol) architecture also activated the lectin pathway but only through L-ficolin recognition.", "entity1": "lectin", "entity2": "poly(ethylene glycol)", "span1": [82, 88], "span2": [28, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12159": {"label": 2, "data": {"text": "CONCLUSION: Nandrolone phenylpropionate up-regulated the density of AR in liver tissue, whereas it had no significant effects on the density of AR in testis and ovary tissues.", "entity1": "AR", "entity2": "Nandrolone phenylpropionate", "span1": [68, 70], "span2": [12, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4513": {"label": 8, "data": {"text": "Carboxylesterases hydrolyze esters, amides, and thioesters to produce carboxylic acids and resulting alcohols, amines, and thiols, respectively.", "entity1": "Carboxylesterases", "entity2": "alcohols", "span1": [0, 17], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15214": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "iNOS", "entity2": "methanol", "span1": [329, 333], "span2": [59, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10954": {"label": 1, "data": {"text": "The marked antihypertensive efficacy of olmesartan medoxomil may result from a unique pharmacological interaction of the drug with the AT1 receptor, resulting in a potent, long-lasting, dose-dependent blockade of A-II.", "entity1": "AT1", "entity2": "olmesartan medoxomil", "span1": [135, 138], "span2": [40, 60]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4629": {"label": 4, "data": {"text": "The results suggested that both the EtOAc extract and berberine were able to activate PPAR\u03b1/\u03b2/\u03b3, and Rhizoma Coptis contains potential natural agonists of PPARs besides berberine.", "entity1": "PPARs", "entity2": "berberine", "span1": [155, 160], "span2": [169, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7184": {"label": 2, "data": {"text": "CONCLUSION: Intake of high SFAs and MUFAs appears to increase expression of PBMC D6D and D5D genes, whilst high EFAs intake appears to decrease expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "SFAs", "span1": [81, 84], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2692": {"label": 4, "data": {"text": "Combining in vivo and in vitro findings, we identified nine AhR agonists, six of which are marketed therapeutics and have been approved by the U.S. Food and Drug Administration, including leflunomide, flutamide, and nimodipine.", "entity1": "AhR", "entity2": "leflunomide", "span1": [60, 63], "span2": [188, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3076": {"label": 3, "data": {"text": "PURPOSE: To compare phenelzine (PLZ), an antidepressant drug with anxiolytic properties which inhibits monoamine oxidase (MAO) but also elevates rat brain levels of the amino acids ?-aminobutyric acid (GABA) and alanine (ALA), with vigabatrin (VIG), an anticonvulsant which elevates brain GABA by inhibition of GABA transaminase (GABA-T), with regard to their actions on brain levels of GABA and ALA and on activities of MAO, GABA-T and ALA transaminase (ALA-T).", "entity1": "monoamine oxidase", "entity2": "PLZ", "span1": [103, 120], "span2": [32, 35]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14657": {"label": 3, "data": {"text": "Boron-based inhibitors of acyl protein thioesterases 1 and 2.", "entity1": "acyl protein thioesterases 1 and 2", "entity2": "Boron", "span1": [26, 60], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13604": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "DVS", "span1": [6, 10], "span2": [150, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2697": {"label": 0, "data": {"text": "Mutation analysis of KYNU encoding kynureninase of the index case revealed homozygosity for a c.593 A > G substitution leading to a threonine-to-alanine (T198A) shift.", "entity1": "kynureninase", "entity2": "threonine", "span1": [35, 47], "span2": [132, 141]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"334": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "RNase A", "entity2": "2'-cytidine monophosphate", "span1": [97, 104], "span2": [206, 231]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1774": {"label": 2, "data": {"text": "CGP 12177A mediates cardiostimulation by activation of the 'putative' beta(4)-adrenoceptor; however, it has recently been reported that disruption of the beta(1)-adrenoceptor gene abolishes this effect.", "entity1": "beta(4)-adrenoceptor", "entity2": "CGP 12177A", "span1": [70, 90], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1330": {"label": 1, "data": {"text": "Eprosartan acts not only at vascular AT1 receptors but also at presynaptic AT1 receptors, causing inhibition of sympathetically stimulated noradrenaline release.", "entity1": "AT1", "entity2": "Eprosartan", "span1": [75, 78], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1597": {"label": 3, "data": {"text": "Nevertheless, 3 mM DMA, a higher concentration that inhibits NHE1, NHE2, and NHE3, significantly increased DBS.", "entity1": "NHE3", "entity2": "DMA", "span1": [77, 81], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"845": {"label": 5, "data": {"text": "The anticonvulsant felbamate blocks N-methyl-D-asparate (NMDA) receptors but fails to exhibit the neurobehavioral toxicity characteristic of other NMDA receptor antagonists.", "entity1": "NMDA receptor", "entity2": "felbamate", "span1": [147, 160], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4797": {"label": 8, "data": {"text": "In the current study, we reveal the inhibitory effects of baicalin on the metabolism of dextromethorphan (DXM), a dual probe substrate of CYP2D and CYP3A, in rats.", "entity1": "CYP3A", "entity2": "DXM", "span1": [148, 153], "span2": [106, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14767": {"label": 1, "data": {"text": "Electrical Stimuli Release ATP to Increase GLUT4 Translocation and Glucose Uptake via PI3K\u03b3-Akt-AS160 in Skeletal Muscle Cells.", "entity1": "PI3K\u03b3", "entity2": "ATP", "span1": [86, 91], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8136": {"label": 3, "data": {"text": "This was confirmed on adding LY294002 the PI3K inhibitor which abolished the protection.", "entity1": "PI3K", "entity2": "LY294002", "span1": [42, 46], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2724": {"label": 3, "data": {"text": "Sulindac sulfide inhibited PPARdelta protein expression and PPARdelta transcriptional activity.", "entity1": "PPARdelta", "entity2": "Sulindac sulfide", "span1": [27, 36], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15347": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "3-ethynylphenanthrene", "span1": [39, 48], "span2": [262, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1895": {"label": 2, "data": {"text": "The in vitro kinase activity of PKC-alpha induced by I3A was lower than that induced by PMA.", "entity1": "PKC-alpha", "entity2": "PMA", "span1": [32, 41], "span2": [88, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9137": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "xanthines", "span1": [124, 136], "span2": [93, 102]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11987": {"label": 8, "data": {"text": "6-DHSG was metabolised by GSH to form a GSH conjugate (GS-6-DHSG) in RAW 264.7 cells, via a potential mechanism involving the catalytic activity of glutathione-S-transferase (GST).", "entity1": "GST", "entity2": "6-DHSG", "span1": [175, 178], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"834": {"label": 5, "data": {"text": "SC-51089 (10(-5) M), a selective EP1-receptor antagonist, showed no effect on the PGE1- or PGE2-induced inhibition of the HVA ICa, thereby indicating that PGE1- and PGE2-induced inhibition of the HVA Ca2+ channels is possibly mediated by the EP3 receptor.", "entity1": "EP1-receptor", "entity2": "SC-51089", "span1": [33, 45], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"885": {"label": 9, "data": {"text": "N(5)-Substituted H(4)biopterin derivatives were not oxidized to products serving as substrates for dihydropteridine reductase and,depending on the substituent, were competitive inhibitors of phenylalanine hydroxylase: N(5)-methyl- and N(5)-hydroxymethyl H(4)biopterin inhibited phenylalanine hydroxylase, whereas N(5)-formyl- and N(5)-acetyl H(4)biopterin had no effect.", "entity1": "phenylalanine hydroxylase", "entity2": "N(5)-formyl", "span1": [278, 303], "span2": [313, 324]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"11796": {"label": 3, "data": {"text": "Fisetin treatment showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), NF-kB p65 unit (in pancreas) and IL-1\u03b2 (plasma), serum nitric oxide (NO) with an elevation in plasma insulin.", "entity1": "NF-kB", "entity2": "Fisetin", "span1": [112, 117], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14344": {"label": 2, "data": {"text": "The expression of the osteoblast markers runt-related transcription factor 2 (RUNX2) and periostin was decreased, while osteocalcin (OCN) was augmented in CCL3(-/-) and Met-RANTES-treated mice.", "entity1": "OCN", "entity2": "Met", "span1": [133, 136], "span2": [169, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9831": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "Lck", "entity2": "geldanamycin", "span1": [67, 70], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7173": {"label": 5, "data": {"text": "Since the suppression of AT1R expression was prevented by pretreatment with GW9662, a PPARgamma antagonist, PPARgamma should have participated in the process.", "entity1": "PPARgamma", "entity2": "GW9662", "span1": [86, 95], "span2": [76, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9364": {"label": 3, "data": {"text": "The time course of the reduction in the number of 5-HT2A receptors was similar to that of the DMI-induced behavioural changes whereas that for the reduction in beta-adrenoceptors was clearly different.", "entity1": "beta-adrenoceptors", "entity2": "DMI", "span1": [160, 178], "span2": [94, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"121": {"label": 3, "data": {"text": "Similarly, felodipine and the p-chloro analogue blocked myosin filament assembly induced by low concentrations of calmodulin, whereas the oxidized and t-butyl analogues did not.", "entity1": "myosin", "entity2": "p-chloro", "span1": [56, 62], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14132": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "TGF-\u03b21", "entity2": "Celastrol", "span1": [183, 189], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2580": {"label": 3, "data": {"text": "Pretreatment with dexamethasone significantly suppressed nasal allergy-like behaviors, up-regulation of histamine content, HDC activity and HDC mRNA induced by TDI in TDI-sensitized rats.", "entity1": "HDC", "entity2": "dexamethasone", "span1": [140, 143], "span2": [18, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4419": {"label": 3, "data": {"text": "Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors.", "entity1": "Spleen Tyrosine Kinase", "entity2": "Pyrrolopyrazines", "span1": [30, 52], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"985": {"label": 2, "data": {"text": "Moreover, BH(4) treatment of the fructose-fed rats markedly reduced the lipid peroxide content of both aortic and cardiac tissues and inhibited the activation of 2 redox-sensitive transcription factors, nuclear factor-kappaB and activating protein-1, which were increased in fructose-fed rats.", "entity1": "activating protein-1", "entity2": "fructose", "span1": [229, 249], "span2": [275, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12267": {"label": 0, "data": {"text": "Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function.", "entity1": "calcitonin gene-related peptide", "entity2": "N", "span1": [88, 119], "span2": [18, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14684": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "Pgp", "entity2": "GSK1292263", "span1": [122, 125], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5437": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "\u03b2-carbonic anhydrase", "entity2": "cyanoacrylamide", "span1": [127, 147], "span2": [46, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13861": {"label": 8, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "estradiol", "span1": [252, 261], "span2": [213, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8868": {"label": 2, "data": {"text": "Finally, we found that I3S worsened experimental autoimmune encephalomyelitis (EAE), which is primarily mediated by Th17 cells, enhancing the frequency of IL-17-producing cells in draining lymph nodes.", "entity1": "IL-17", "entity2": "I3S", "span1": [155, 160], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11652": {"label": 1, "data": {"text": "The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone.", "entity1": "MUC2", "entity2": "CDCA", "span1": [57, 61], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12630": {"label": 0, "data": {"text": "Thymidine kinase from Herpes simplex virus type 1 (TK) was crystallized in an N-terminally truncated but fully active form.", "entity1": "TK", "entity2": "N", "span1": [51, 53], "span2": [78, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7541": {"label": 3, "data": {"text": "Phenelzine (PLZ), a nonselective irreversible inhibitor of monoamine oxidase (MAO), also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels.", "entity1": "GABA-transaminase", "entity2": "Phenelzine", "span1": [98, 115], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7126": {"label": 0, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "GAF-B domain", "entity2": "amino acid", "span1": [47, 59], "span2": [5, 15]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1759": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "p185ErbB2", "entity2": "GW572016", "span1": [24, 33], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8531": {"label": 2, "data": {"text": "In macrophages, levels of TNF-\u03b1, IFN-\u03b3, NO, IL-6 and IL-10 were increased by CDM used alone or in combination with HSV-2.", "entity1": "IL-6", "entity2": "CDM", "span1": [44, 48], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6178": {"label": 3, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "CFTR", "entity2": "ibuprofen", "span1": [182, 186], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"191": {"label": 3, "data": {"text": "Selective precipitation of cytosol receptors with 36% (NH4)2SO4 reduced CBG concentrations to negligible levels.", "entity1": "CBG", "entity2": "(NH4)2SO4", "span1": [72, 75], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9916": {"label": 2, "data": {"text": "Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.", "entity1": "potassium channels", "entity2": "Retigabine", "span1": [69, 87], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6450": {"label": 4, "data": {"text": "The present studies were undertaken to compare two compounds, a vitamin D(3) analogue (CB1093) with minimal calcaemic effects, and clenbuterol, a long-acting beta(2)-adrenoceptor agonist, both of which induce NGF synthesis in vivo.", "entity1": "beta(2)-adrenoceptor", "entity2": "clenbuterol", "span1": [158, 178], "span2": [131, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14770": {"label": 1, "data": {"text": "ATP caused translocation of GLUT4myc-eGFP to the cell surface, mechanistically mediated by increased exocytosis involving AS160/Rab8A reduced by dominant-negative Akt or PI3K\u03b3 kinase-dead mutants, and potentiated by myristoylated PI3K\u03b3.", "entity1": "GLUT4", "entity2": "ATP", "span1": [28, 33], "span2": [0, 3]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7423": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "Delta 6 desaturase", "entity2": "DHA", "span1": [11, 29], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12572": {"label": 8, "data": {"text": "Glutathione-independent prostaglandin D synthase [prostaglandin-H2 D-isomerase; (5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase, EC 5.3.99.2] is an enzyme responsible for biosynthesis of prostaglandin D2 in the central nervous system.", "entity1": "(5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase", "entity2": "prostaglandin D2", "span1": [80, 163], "span2": [223, 239]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12745": {"label": 1, "data": {"text": "The results demonstrate that DMI and nisoxetine are persistently retained in cell membranes, at least partly in association with the NET.", "entity1": "NET", "entity2": "DMI", "span1": [133, 136], "span2": [29, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3001": {"label": 1, "data": {"text": "The molecular bases for phosphodiesterase 5 (PDE5) catalytic-site affinity for cyclic guanosine monophosphate (cGMP) and potency of inhibitors are poorly understood.", "entity1": "phosphodiesterase 5", "entity2": "cGMP", "span1": [24, 43], "span2": [111, 115]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5272": {"label": 2, "data": {"text": "In fact, we demonstrated a significant stimulation of Nox4 activity by 4 quinone derivatives (AA-861, tBuBHQ, tBuBQ, and duroquinone) observed in 3 different cellular models, HEK293E, T-REx\u2122, and chondrocyte cell lines.", "entity1": "Nox4", "entity2": "tBuBQ", "span1": [54, 58], "span2": [110, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7141": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "sildenafil", "span1": [146, 165], "span2": [102, 112]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6792": {"label": 3, "data": {"text": "CONCLUSIONS AND CLINICAL RELEVANCE: Canine COX-2 was selectively inhibited by etodolac, nimesulide, and NS398; tolfenamic acid and carprofen also appeared to be preferential COX-2 inhibitors in dogs.", "entity1": "Canine COX-2", "entity2": "NS398", "span1": [36, 48], "span2": [104, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14291": {"label": 3, "data": {"text": "The signaling of both Sox9 and Runx2, key regulators of chondrogenesis, was downregulated by VPA.", "entity1": "Sox9", "entity2": "VPA", "span1": [22, 26], "span2": [93, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10240": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "spermidine/spermine N(1)-acetyltransferase", "entity2": "spermine", "span1": [77, 119], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15501": {"label": 2, "data": {"text": "We found that pBQN activates TRPA1 starting at 10 nM and peaking at 300 nM; higher concentrations caused rapid activation followed by a fast decline.", "entity1": "TRPA1", "entity2": "pBQN", "span1": [29, 34], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7260": {"label": 9, "data": {"text": "Simple benzenesulfonamides were rather ineffective hCA VI inhibitors, with inhibition constants in the range of 1090-6680 nM.", "entity1": "hCA VI", "entity2": "benzenesulfonamides", "span1": [51, 57], "span2": [7, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8395": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "GR", "entity2": "Cd", "span1": [216, 218], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15402": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "TNF\u03b1", "entity2": "7-ketosterols", "span1": [84, 88], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"792": {"label": 1, "data": {"text": "Additionally, experiments with the non-desensitizing site-directed mutant GluR3(L507Y) (Stern-Bach, Y., Russo, S., Neuman, M. and Rosenmund, C., A point mutation in the glutamate binding site blocks desensitization of AMPA receptors.", "entity1": "AMPA receptors", "entity2": "glutamate", "span1": [218, 232], "span2": [169, 178]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15583": {"label": 1, "data": {"text": "At no 1NMPP1 concentration was mitosis in rescued clones prevented without also inducing endoreduplication, suggesting that these two key roles for Cdk1 are not simply controlled by different Cdk1 activity thresholds.", "entity1": "Cdk1", "entity2": "1NMPP1", "span1": [148, 152], "span2": [6, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9548": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "GM-CSF", "entity2": "cyclic adenosine monophosphate", "span1": [97, 103], "span2": [172, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3364": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-type voltage-gated calcium channels", "entity2": "ethanol", "span1": [114, 151], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9833": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "kinases", "entity2": "geldanamycin", "span1": [81, 88], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6755": {"label": 1, "data": {"text": "Hydralazine dose-dependently inhibited PHD activity and induced nonhydroxylated HIF-1alpha, evidence for HIF stabilization specifically by inhibition of PHD enzyme activity.", "entity1": "HIF", "entity2": "Hydralazine", "span1": [105, 108], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12082": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "3 beta-HSD", "entity2": "17 alpha-hydroxy pregnenolone", "span1": [74, 84], "span2": [149, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12128": {"label": 1, "data": {"text": "The selective alpha(1)-adrenoceptor ligands prazosin and doxazosin (each 3 microM) had no effect on noradrenaline responses.", "entity1": "alpha(1)-adrenoceptor", "entity2": "prazosin", "span1": [14, 35], "span2": [44, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8790": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-NF-\u03baB", "entity2": "CAPE", "span1": [187, 200], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"670": {"label": 3, "data": {"text": "OBJECTIVE: To evaluate the extent of human cyclooxygenase-1 (COX-1) inhibition by meloxicam, which has been reported to preferentially inhibit cyclooxygenase-2 (COX-2).", "entity1": "COX-1", "entity2": "meloxicam", "span1": [61, 66], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3230": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "phenol", "span1": [248, 261], "span2": [31, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6965": {"label": 1, "data": {"text": "As CRABPI was elevated far more than any other genes, we observed that the retinoids, all-trans retinoic acid and 9-cis retinoic acid, that bind CRABPI, promoted nitroblue tetrazolium-associated functional cell differentiation in p75NTR PC-3 cells, but not in neo control PC-3 cells.", "entity1": "CRABPI", "entity2": "all-trans retinoic acid", "span1": [145, 151], "span2": [86, 109]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1942": {"label": 3, "data": {"text": "The aim of this study was to evaluate the influence of hepatic impairment on the pharmacokinetics (PK) of the novel cyclooxygenase-2 (COX-2) selective inhibitor lumiracoxib (Prexige), so that dose recommendations for clinical use can be provided.", "entity1": "COX-2", "entity2": "Prexige", "span1": [134, 139], "span2": [174, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6749": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "PDGFbeta-receptor", "entity2": "Gleevec", "span1": [187, 204], "span2": [107, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10251": {"label": 9, "data": {"text": "A moderate (twofold) stimulation of CD62P expression by abciximab but not by tirofiban or eptifibatide was observed in one patient.", "entity1": "CD62P", "entity2": "eptifibatide", "span1": [36, 41], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4631": {"label": 9, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "CYP1A1", "entity2": "anthocyanidins", "span1": [60, 66], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3244": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "OXA", "span1": [13, 16], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2209": {"label": 2, "data": {"text": "Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures.", "entity1": "cyclic AMP regulatory element-binding protein", "entity2": "morphine", "span1": [19, 64], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13863": {"label": 1, "data": {"text": "OBJECTIVE: Mitiglinide, a rapid- and short-acting insulinotropic sulfonylurea receptor ligand, exhibits hypoglycemic action unlike other sulfonylureas.", "entity1": "sulfonylurea receptor", "entity2": "Mitiglinide", "span1": [65, 86], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"849": {"label": 3, "data": {"text": "Troglitazone inhibited the antigen-induced production of LTB(4), C(4) and E(4) and the potency of the inhibition was comparable to that of zileuton, a specific inhibitor of 5-lipoxygenase (5-LOX) and a clinically used anti-asthmatic drug.", "entity1": "5-lipoxygenase", "entity2": "zileuton", "span1": [173, 187], "span2": [139, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14603": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala70Thr", "entity2": "Ara-C", "span1": [52, 60], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11315": {"label": 3, "data": {"text": "Ten IU/mL urokinase was also incubated with pooled plasma of stroke patients, that was previously oxidized with the singlet oxygen (1O2) donor chloramine T (CT), to destroy plasmatic PAI-1 and alpha2-antiplasmin.", "entity1": "plasmin", "entity2": "chloramine T", "span1": [204, 211], "span2": [143, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11368": {"label": 1, "data": {"text": "In intact CHO-K1 cells, I3A was able to translocate different green fluorescent protein-tagged PKC isoforms, visualized by confocal microscopy, with equal or higher potency than PMA.", "entity1": "PKC", "entity2": "I3A", "span1": [95, 98], "span2": [24, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5292": {"label": 3, "data": {"text": "Vandetanib (Caprelsa(\u00ae), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60\u00a0% of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors.", "entity1": "epidermal growth-factor receptors", "entity2": "Caprelsa", "span1": [291, 324], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9177": {"label": 3, "data": {"text": "Staining was largely absent when substrate was omitted or after pretreatment with the irreversible SSAO inhibitor, hydralazine and the slowly reversible inhibitor, semicarbazide.", "entity1": "SSAO", "entity2": "semicarbazide", "span1": [99, 103], "span2": [164, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14559": {"label": 8, "data": {"text": "The objective of this article is to examine the effects of single and repeated administrations of silymarin on pharmacokinetics of a P-gp substrate, risperidone, and its major metabolite, 9-hydroxyrisperidone, in rats.", "entity1": "P-gp", "entity2": "9-hydroxyrisperidone", "span1": [133, 137], "span2": [188, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9661": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "human recombinant interleukin-5", "entity2": "FP", "span1": [132, 163], "span2": [101, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6827": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "receptor tyrosine kinase", "entity2": "imatinib", "span1": [120, 144], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9556": {"label": 1, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "Con A", "entity2": "isoproterenol", "span1": [16, 21], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7846": {"label": 2, "data": {"text": "These data suggest that ribavirin-induced intracellular GTP depletion recruits a super elongation complex containing P-TEFb, AFF4 and ELL3, to F7, and modulates FVII mRNA transcription elongation.", "entity1": "ELL3", "entity2": "ribavirin", "span1": [134, 138], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1468": {"label": 8, "data": {"text": "Interestingly, the allele of PRO1 was shown to enhance the activities of gamma-glutamyl kinase and gamma-glutamyl phosphate reductase, both of which catalyze the first two steps of L-proline synthesis from L-glutamate and which together may form a complex in vivo.", "entity1": "gamma-glutamyl phosphate reductase", "entity2": "L-proline", "span1": [99, 133], "span2": [181, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4259": {"label": 3, "data": {"text": "Repression of farnesyltransferase (FNTA) by siRNA and the enzyme inhibitor manumycin A caused elevation of ApoA-I secretion from hepatocytes and from transgenic mice expressing hApoA-I and cholesterol ester transfer protein transgenes.", "entity1": "FNTA", "entity2": "manumycin A", "span1": [35, 39], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12153": {"label": 3, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "ornithine", "span1": [150, 156], "span2": [160, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4636": {"label": 2, "data": {"text": "Similarly, pelargonidin induced the expression of CYP1A1 mRNA up to 5-fold in HepG2 and LS174T cells relative to the induction by 5 nM 2,3,7,8-tetrachlorodibenzodioxin (TCDD), the most potent activator of AhR.", "entity1": "AhR", "entity2": "2,3,7,8-tetrachlorodibenzodioxin", "span1": [205, 208], "span2": [135, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14884": {"label": 9, "data": {"text": "The induction of HO-1 by EIH was inhibited by SB203580 but not by SP600125, PD98059, nor LY294002.", "entity1": "HO-1", "entity2": "SP600125", "span1": [17, 21], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5396": {"label": 4, "data": {"text": "The effects of the adenosine A3 receptor agonist IB-MECA on sodium taurocholate-induced experimental acute pancreatitis.", "entity1": "adenosine A3 receptor", "entity2": "IB-MECA", "span1": [19, 40], "span2": [49, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3966": {"label": 8, "data": {"text": "Here, we demonstrate that peptidyl-prolyl cis/trans-isomerase A1 (Pin1), an enzyme that catalyzes the conversion of the peptide bond of pSer/pThr-Pro moieties in signaling proteins from cis to trans, is highly susceptible to HNE modification.", "entity1": "peptidyl-prolyl cis/trans-isomerase A1", "entity2": "pThr", "span1": [26, 64], "span2": [141, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"5871": {"label": 9, "data": {"text": "By contrast, neither amoxapine nor amitriptyline can be considered as possible ligands of 5-HT1A and 5-HT1B receptors because their affinities for these sites are in the micromolar range (or even worse).", "entity1": "5-HT1A", "entity2": "amoxapine", "span1": [90, 96], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11876": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [145, 148], "span2": [97, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2621": {"label": 3, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "N495K", "entity2": "foscarnet", "span1": [107, 112], "span2": [149, 158]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5651": {"label": 3, "data": {"text": "Arsenic trioxide (As(2)O(3)), which is used to treat acute promyelocytic leukemia, can cause LQTS type 2 (LQT2) by reducing the hERG current through the diversion of hERG trafficking to the cytoplasmic membrane.", "entity1": "hERG", "entity2": "Arsenic trioxide", "span1": [166, 170], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9268": {"label": 8, "data": {"text": "Ergovaline inhibition of radioligand binding to the D2 dopamine receptor and ergot alkaloid inhibition of vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production in GH4ZR7 cells, stably transfected with a rat D2 dopamine receptor, were evaluated.", "entity1": "vasoactive intestinal peptide", "entity2": "cyclic AMP", "span1": [106, 135], "span2": [153, 163]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9630": {"label": 1, "data": {"text": "Binding of hydroxyflutamide to m-AR in LNCaP cells resulted in a concentration-dependent stimulation of PSA expression, suggesting that hydroxyflutamide acted as an agonist of the m-AR.", "entity1": "AR", "entity2": "hydroxyflutamide", "span1": [33, 35], "span2": [11, 27]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5569": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase 1 (DDAH1) is an enzyme that metabolizes methylated arginine to citrulline and methylamine, thus working to produce nitric oxide (NO).", "entity1": "Dimethylarginine dimethylaminohydrolase 1", "entity2": "citrulline", "span1": [0, 41], "span2": [103, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"561": {"label": 0, "data": {"text": "Addition of a specific number of FGFR sequences to the C-terminus of Ig module II resulted in a gain in affinity for FGF-7.", "entity1": "Ig module II", "entity2": "C", "span1": [69, 81], "span2": [55, 56]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15080": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "Klebsiella pneumoniae carbapenemases", "entity2": "ceftazidime", "span1": [199, 235], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15455": {"label": 3, "data": {"text": "Of the compounds active in the present assay system, the most potent compound 7, platyphyllonol-5-O-\u03b2-d-xylopyranoside, significantly suppressed the induction of peroxisome proliferator activated receptor \u03b3 (PPAR\u03b3 and CCAAT/enhancer binding protein \u03b1 (C/EBP\u03b1) protein expression, and inhibited adipocyte differentiation induced by troglitazone, a PPAR\u03b3 agonist.", "entity1": "PPAR\u03b3", "entity2": "platyphyllonol-5-O-\u03b2-d-xylopyranoside", "span1": [208, 213], "span2": [81, 118]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15909": {"label": 1, "data": {"text": "Synaptotagmin-1, a vesicular protein interacting with membranes upon low-affinity Ca(2+) -binding, plays a major role in excitation-release coupling, by synchronizing calcium entry with fast neurotransmitter release.", "entity1": "Synaptotagmin-1", "entity2": "Ca(2+)", "span1": [0, 15], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11690": {"label": 8, "data": {"text": "Stable ABCC1, ABCC2 and ABCC3 knockdown cell lines were generated, thus making it possible to demonstrate that ABCC1 mediates the basolateral and ABCC2 the apical excretion of BPDE glutathione conjugates.", "entity1": "ABCC2", "entity2": "BPDE glutathione", "span1": [146, 151], "span2": [176, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11478": {"label": 0, "data": {"text": "We propose that the secondary role of yeast mitochondrial LeuRS in RNA splicing has impacted the functional evolution of this critical C-terminal domain.", "entity1": "yeast mitochondrial LeuRS", "entity2": "C", "span1": [38, 63], "span2": [135, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"784": {"label": 3, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "lipoxygenase", "entity2": "nordihydroguaiaretic acid", "span1": [241, 253], "span2": [205, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13678": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "human TLR7", "entity2": "imidazoquinoline", "span1": [118, 128], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3631": {"label": 5, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "CB2", "entity2": "AM630", "span1": [352, 355], "span2": [367, 372]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3616": {"label": 3, "data": {"text": "Taken together, our study demonstrated that SB365 inhibits the AKT/mTOR pathway, leading to the suppression of tumor growth and angiogenesis together with induction of apoptosis.", "entity1": "mTOR", "entity2": "SB365", "span1": [67, 71], "span2": [44, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1369": {"label": 0, "data": {"text": "We hypothesize that L0 interacts with the K(IR) N terminus in ligand-inhibited K(ATP) channels and put forward a model, based on the architecture of BtuCD, MsbA, and the KcsA channel, in which TMD0-L0 links the MDR-like core of SUR with the K(IR) pore.", "entity1": "K(IR)", "entity2": "N", "span1": [42, 47], "span2": [48, 49]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3081": {"label": 3, "data": {"text": "Only PLZ inhibited MAO and ALA-T and elevated ALA levels.", "entity1": "ALA-T", "entity2": "PLZ", "span1": [27, 32], "span2": [5, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8037": {"label": 3, "data": {"text": "Human stearoyl-CoA desaturase 1 (SCD-1) gene expression is negatively regulated by thyroid hormone without direct binding of thyroid hormone receptor to the gene promoter.", "entity1": "SCD-1", "entity2": "thyroid hormone", "span1": [33, 38], "span2": [83, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7148": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "vardenafil", "span1": [27, 46], "span2": [78, 88]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9664": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "rhIL-5", "entity2": "formyl-met-leu-phe", "span1": [165, 171], "span2": [192, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9786": {"label": 5, "data": {"text": "The delta-receptor antagonist, SB 244525 (10 mg/kg, i.p.", "entity1": "delta-receptor", "entity2": "SB 244525", "span1": [4, 18], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11622": {"label": 8, "data": {"text": "We isolated partial cDNAs that codified for enzymes implicated in the anthocyanin biosynthesis such as l-phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS), and an antioxidant enzyme such as ascorbate peroxidase (APX).", "entity1": "ascorbate peroxidase", "entity2": "anthocyanin", "span1": [202, 222], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"122": {"label": 3, "data": {"text": "Again, inhibition of the actin-activated myosin Mg2+-ATPase and myosin filament assembly by felodipine and the p-chloro analogue could be reversed by raising the calmodulin concentration.", "entity1": "myosin", "entity2": "felodipine", "span1": [41, 47], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3243": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "oxandrolone", "span1": [13, 16], "span2": [100, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5004": {"label": 1, "data": {"text": "Chalcogenopyrylium Dyes as Differential Modulators of Organic Anion Transport by MRP1, MRP2 and MRP4.", "entity1": "MRP4", "entity2": "Chalcogenopyrylium", "span1": [96, 100], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15286": {"label": 1, "data": {"text": "Repeated Low Dose Administration of the Monoacylglycerol Lipase Inhibitor JZL184 Retains CB1 Receptor Mediated Antinociceptive and Gastroprotective Effects.", "entity1": "CB1", "entity2": "JZL184", "span1": [89, 92], "span2": [74, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16025": {"label": 1, "data": {"text": "These results show that haloperidol promotes mTORC1- and S6K1-dependent phosphorylation of rpS6 at Ser240/244, in a subpopulation of striatal MSNs expressing D2Rs.", "entity1": "D2Rs", "entity2": "haloperidol", "span1": [158, 162], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10802": {"label": 3, "data": {"text": "We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays.", "entity1": "cyclooxygenases", "entity2": "flunixin", "span1": [111, 126], "span2": [92, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1718": {"label": 9, "data": {"text": "But, intracerebroventricular injection of each ginsenoside did not affect plasma IL-6 level induced by immobilization stress.", "entity1": "IL-6", "entity2": "ginsenoside", "span1": [81, 85], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8221": {"label": 1, "data": {"text": "With the exception of three residues, the specific amino acids that form the putative binding pocket for ICA in ERG are conserved in EAG.", "entity1": "ERG", "entity2": "ICA", "span1": [112, 115], "span2": [105, 108]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2464": {"label": 0, "data": {"text": "The updated bovine type II GnRH receptor gene sequence revealed inactivation by frame shifts, premature stop codons, and nucleotide changes specifying nonconservative replacement of amino acid residues, similar to inactivation of sheep type II GnRH receptor.", "entity1": "bovine type II GnRH receptor", "entity2": "nucleotide", "span1": [12, 40], "span2": [121, 131]}, "weak_labels": [0, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8573": {"label": 3, "data": {"text": "We report the discovery of a novel series of ATP-competitive Janus kinase 3 (JAK3) inhibitors based on the 5H-pyrrolo[2,3-b]pyrazine scaffold.", "entity1": "Janus kinase 3", "entity2": "5H-pyrrolo[2,3-b]pyrazine", "span1": [61, 75], "span2": [107, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7863": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "KARs", "entity2": "lavendustin A", "span1": [32, 36], "span2": [316, 329]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1343": {"label": 7, "data": {"text": "Among the [Fe-S] cluster biosynthetic proteins are included a pyridoxal phosphate-dependent enzyme (NifS) that is involved in the activation of sulphur from l-cysteine, and a molecular scaffold protein (NifU) upon which [Fe-S] cluster precursors are formed.", "entity1": "NifS", "entity2": "pyridoxal phosphate", "span1": [100, 104], "span2": [62, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"330": {"label": 1, "data": {"text": "The folding rate for wild-type RNase A is faster in the presence of the inhibitor 2'CMP than in its absence, indicating that the transition-state structure in the rate-determining step is stabilized by 2'CMP.", "entity1": "RNase A", "entity2": "2'CMP", "span1": [31, 38], "span2": [202, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6055": {"label": 3, "data": {"text": "Actinomycin D caused alpha-AR mRNA level to decrease with a half-life of 3.2 +/- 0.4 h and blocked the effect of H-7 to decrease basal alpha-AR mRNA level.", "entity1": "alpha-AR", "entity2": "Actinomycin D", "span1": [21, 29], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8327": {"label": 2, "data": {"text": "Treatment of these cells with Paeoniflorin significantly induced HO-1 expression.", "entity1": "HO-1", "entity2": "Paeoniflorin", "span1": [65, 69], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10909": {"label": 8, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "Pyridoxal kinase", "entity2": "pyridoxine", "span1": [0, 16], "span2": [86, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10629": {"label": 3, "data": {"text": "While fluoropyrimidine antimetabolites have other sites of action, antifolates ZD1694 (raltitrexed, Tomudex) and AG337 (Thymitag) are more specific and potent TS inhibitors.", "entity1": "TS", "entity2": "AG337", "span1": [159, 161], "span2": [113, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"434": {"label": 1, "data": {"text": "Ka values in nM for rauwolscine (19), WB-4101 (265), SKF-104078 (197), spiroxatrine (128), and prazosin (1531) for blocking relaxation in rat arteries were consistent with their affinities for binding at the alpha-2D adrenoceptor subtype.", "entity1": "alpha-2D adrenoceptor", "entity2": "SKF-104078", "span1": [208, 229], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14785": {"label": 1, "data": {"text": "In addition, TSA induced Nrf2 nuclear translocation and up-regulated the expression of Nrf2-ARE downstream antioxidant genes, whereas Nrf2 knockdown by RNA interference blocked the inhibition of TSA on myofibroblast differentiation.", "entity1": "Nrf2", "entity2": "TSA", "span1": [25, 29], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12376": {"label": 1, "data": {"text": "Almorexant effects on CYP3A4 activity studied by its simultaneous and time-separated administration with simvastatin and atorvastatin.", "entity1": "CYP3A4", "entity2": "Almorexant", "span1": [22, 28], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11663": {"label": 8, "data": {"text": "Thymidine kinase-1 (TK-1) and thymidylate synthase (TS) are key enzymes for salvage and de novo pyrimidine synthesis, respectively.", "entity1": "TK-1)", "entity2": "pyrimidine", "span1": [20, 25], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10635": {"label": 3, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "Bsep", "entity2": "Troglitazone", "span1": [76, 80], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1466": {"label": 0, "data": {"text": "By introducing the mutant-derived genomic library into a non-L-proline-utilizing strain, the mutant was found to carry an allele of the wild-type PRO1 gene encoding gamma-glutamyl kinase, which resulted in a single amino acid replacement; Asp (GAC) at position 154 was replaced by Asn (AAC).", "entity1": "gamma-glutamyl kinase", "entity2": "Asn", "span1": [165, 186], "span2": [281, 284]}, "weak_labels": [0, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7140": {"label": 1, "data": {"text": "This indicated that the N-terminal 46 amino acids in GAF-B are required for high vardenafil potency.", "entity1": "GAF-B", "entity2": "vardenafil", "span1": [53, 58], "span2": [81, 91]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13806": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "Abl", "entity2": "STI571", "span1": [118, 121], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6287": {"label": 1, "data": {"text": "In conclusion, (-)-pindolol modulates, both alone and together with 5-HT reuptake inhibitors, dopaminergic, adrenergic, and serotonergic transmission in the FCX via a complex pattern of actions at beta 1/2-ARs, 5-HT1A, and 5-HT1B receptors.", "entity1": "5-HT1A", "entity2": "(-)-pindolol", "span1": [211, 217], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9292": {"label": 2, "data": {"text": "Furthermore, the phosphorylation of myosin light chain produced by norepinephrine was greater than that produced by clonidine.", "entity1": "myosin light chain", "entity2": "norepinephrine", "span1": [36, 54], "span2": [67, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6038": {"label": 1, "data": {"text": "We conclude that despite small differences concerning the enantiomeric selectivity and affinity of rauwolscine and yohimbine, the close pharmacological identity of 5-HT receptors in rat stomach fundus and the recently cloned 5-HT2B receptor is maintained.", "entity1": "5-HT2B", "entity2": "yohimbine", "span1": [225, 231], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7834": {"label": 2, "data": {"text": "Nevertheless, low L-BMAA concentrations (\u2265 0.1mM, 48 h) increased protein ubiquitination, 20S proteasomal and caspase 12 activity, expression of the endoplasmic reticulum (ER) stress marker CHOP, and enhanced phosphorylation of elf2\u03b1 in SH-SY5Y cells.", "entity1": "elf2\u03b1", "entity2": "L-BMAA", "span1": [228, 233], "span2": [18, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11375": {"label": 1, "data": {"text": "Favorable enzyme profiles (high TP and low DPD) generate high intratumor levels of 5-FU that are effective against many tumors, especially those with low TS.", "entity1": "TS", "entity2": "5-FU", "span1": [154, 156], "span2": [83, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7929": {"label": 2, "data": {"text": "In addition, glucosamine attenuated p21 protein stability via the proteasomal proteolytic pathway, as well as inducing p21 nuclear accumulation.", "entity1": "p21", "entity2": "glucosamine", "span1": [119, 122], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7324": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT2", "entity2": "amino acids", "span1": [331, 336], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1500": {"label": 3, "data": {"text": "Sulindac sulfide inhibits epidermal growth factor-induced phosphorylation of extracellular-regulated kinase 1/2 and Bad in human colon cancer cells.", "entity1": "epidermal growth factor", "entity2": "Sulindac sulfide", "span1": [26, 49], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9023": {"label": 2, "data": {"text": "In addition to effects on cell proliferation, DHT increased the percentage of alkaline phosphatase (ALP) positive cells in all three bone cell systems tested, and this effect was inhibited by antiandrogens.", "entity1": "alkaline phosphatase", "entity2": "DHT", "span1": [78, 98], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13846": {"label": 5, "data": {"text": "Ambrisentan is an endothelin receptor antagonist (ERA) that was recently approved for treatment of pulmonary arterial hypertension (PAH).", "entity1": "endothelin receptor", "entity2": "Ambrisentan", "span1": [18, 37], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2089": {"label": 3, "data": {"text": "When amiloride was dropped on the eye surface on the first day of irradiation and subsequently daily until the end of the experiment, u-PA activity in both cornea and tear fluid was strongly inhibited.", "entity1": "u-PA", "entity2": "amiloride", "span1": [134, 138], "span2": [5, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7700": {"label": 2, "data": {"text": "atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans.", "entity1": "AChE", "entity2": "trimedoxime", "span1": [10, 14], "span2": [90, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11620": {"label": 8, "data": {"text": "We isolated partial cDNAs that codified for enzymes implicated in the anthocyanin biosynthesis such as l-phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS), and an antioxidant enzyme such as ascorbate peroxidase (APX).", "entity1": "chalcone synthase", "entity2": "anthocyanin", "span1": [143, 160], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5874": {"label": 1, "data": {"text": "Interestingly, amoxapine binds with a good affinity (IC50 = 0.30 microM) to 5-HT3 receptors labelled by [3H]zacopride in cortical membranes.", "entity1": "5-HT3", "entity2": "[3H]zacopride", "span1": [76, 81], "span2": [104, 117]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4620": {"label": 2, "data": {"text": "Consumption of alcohol for 8weeks induced severe liver damage with increases in prognostic indicators such as aspartate transaminase, alanine transaminase in serum whereas co-administration of CNF suppressed their increases.", "entity1": "aspartate transaminase", "entity2": "alcohol", "span1": [110, 132], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13722": {"label": 1, "data": {"text": "Phosphorylation of replication protein A (RPA2 subunit) and formation of damage-induced foci were strikingly evident following IC(50) doses of RTX.", "entity1": "RPA2", "entity2": "RTX", "span1": [42, 46], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9863": {"label": 8, "data": {"text": "Among the various enzymes, dicoumarol inhibitable cytosolic NAD(P)H:quinone oxidoreductase1 (NQO1) was shown to catalyse bioreductive activation of MMC leading to cross-linking of the DNA and cytotoxicity.", "entity1": "NAD(P)H:quinone oxidoreductase1", "entity2": "MMC", "span1": [60, 91], "span2": [148, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7152": {"label": 8, "data": {"text": "Phosphodiesterase-5 (PDE5) contains a catalytic domain (C domain) that hydrolyzes cGMP and a regulatory domain (R domain) that contains two mammalian cGMP-binding phosphodiesterase, Anabaena adenylyl cyclases, Escherichia coli FhlAs (GAFs) (A and B) and a phosphorylation site for cyclic nucleotide-dependent protein kinases (cNPKs).", "entity1": "Phosphodiesterase-5", "entity2": "cGMP", "span1": [0, 19], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15054": {"label": 8, "data": {"text": "The recent identification of zinc permeability of the lysosomal ion channel TRPML1 (transient receptor potential mucolipin 1), and the evidence of abnormal zinc levels in cells deficient in TRPML1, suggested a role for TRPML1\u00a0in zinc transport.", "entity1": "TRPML1", "entity2": "zinc", "span1": [219, 225], "span2": [229, 233]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4269": {"label": 2, "data": {"text": "Activation of AMP-activated Protein Kinase and Phosphorylation of Glycogen Synthase Kinase3 \u03b2 Mediate Ursolic Acid Induced Apoptosis in HepG2 Liver Cancer Cells.", "entity1": "Glycogen Synthase Kinase3 \u03b2", "entity2": "Ursolic Acid", "span1": [66, 93], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2899": {"label": 1, "data": {"text": "Dexmedetomidine was effective in blocking these sympathomimetic actions of cocaine even in all 7 subjects who were homozygous for the Del322-325 polymorphism in the alpha2C AR, a loss-of-function mutation that is highly enriched in blacks.", "entity1": "alpha2C AR", "entity2": "Dexmedetomidine", "span1": [165, 175], "span2": [0, 15]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7724": {"label": 3, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LH", "entity2": "leuprorelin", "span1": [260, 262], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14953": {"label": 1, "data": {"text": "Styrene oxide and 4-vinylphenol possessed similar affinity for CYP2E1.", "entity1": "CYP2E1", "entity2": "Styrene oxide", "span1": [63, 69], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"445": {"label": 1, "data": {"text": "Epinastine (WAL 801CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor.", "entity1": "5-HT1-like receptor", "entity2": "Epinastine", "span1": [114, 133], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11105": {"label": 1, "data": {"text": "Opioid receptors are the membrane proteins that mediate the pain-relieving effect of opioid drugs, such as morphine and fentanyl as well as endogenous opioid peptides enkephalins and endorphins.", "entity1": "Opioid receptors", "entity2": "morphine", "span1": [0, 16], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1152": {"label": 8, "data": {"text": "These studies suggest that HER2-overexpressing tumors are particularly susceptible to the inhibition of HER family tyrosinetyrosine kinase signaling and suggest novel strategies to treat these particularly aggressive tumors.", "entity1": "tyrosine kinase", "entity2": "tyrosine", "span1": [123, 138], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6938": {"label": 8, "data": {"text": "A double mutant of the two fumarate reductase isozyme genes (OSM1 and FRDS) showed a succinate productivity of 50% as compared to the parent when cells were incubated in glucose-buffered solution.", "entity1": "FRDS", "entity2": "succinate", "span1": [70, 74], "span2": [85, 94]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1427": {"label": 2, "data": {"text": "Culture of HepG2 cells with griseofulvin has now been shown to induce both the formation of intracellular aggregates containing K18 as well as an increase in the abundance of K18 mRNA.", "entity1": "K18", "entity2": "griseofulvin", "span1": [175, 178], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3880": {"label": 3, "data": {"text": "Western blots showed a decrease in nuclear p65 protein expression after exposure to different concentrations of cinobufagin, while the phosphorylation of GSK-3\u03b2 was simultaneously increased.", "entity1": "p65", "entity2": "cinobufagin", "span1": [43, 46], "span2": [112, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4944": {"label": 3, "data": {"text": "A novel benzo[d]imidazole derivate prevents the development of dextran sulfate sodium-induced murine experimental colitis via inhibition of NLRP3 inflammasome.", "entity1": "NLRP3", "entity2": "benzo[d]imidazole", "span1": [140, 145], "span2": [8, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6238": {"label": 1, "data": {"text": "Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.", "entity1": "5-HT1D", "entity2": "[3H]eletriptan", "span1": [127, 133], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12123": {"label": 8, "data": {"text": "A role of cytosolic NQO1 in protection of cells from oxidative stress, cytotoxicity, and mutagenicity of quinones was established.", "entity1": "NQO1", "entity2": "quinones", "span1": [20, 24], "span2": [105, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15571": {"label": 3, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "Lamp 2A", "entity2": "MPTP", "span1": [252, 259], "span2": [209, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6378": {"label": 3, "data": {"text": "Thirty-week administration of UFT with or without leucovorin markedly suppressed both colorectal carcinogenesis and tumor growth, resulted in the increase of thymidylate synthase inhibition and the decrease of thymidine kinase activity in the tumor cells.", "entity1": "thymidine kinase", "entity2": "UFT", "span1": [210, 226], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14443": {"label": 2, "data": {"text": "Induction of AhR by TCDD and prochloraz resulted in a time- and dose-dependent increase of ABCG2 gene expression and transporter protein levels.", "entity1": "AhR", "entity2": "prochloraz", "span1": [13, 16], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4895": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "aromatase", "entity2": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate", "span1": [148, 157], "span2": [0, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11228": {"label": 1, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "K(ATP) channel", "entity2": "mitiglinide", "span1": [149, 163], "span2": [59, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12441": {"label": 6, "data": {"text": "Discovery of ML326: The first sub-micromolar, selective M5 PAM.", "entity1": "M5", "entity2": "ML326", "span1": [56, 58], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15869": {"label": 1, "data": {"text": "Immunoblot studies showed that K(+)-depolarization increased CaMKII\u03b1 phosphorylation in a KN-62 sensitive manner and promoted CaMKII\u03b1 binding to D3 receptors.", "entity1": "CaMKII\u03b1", "entity2": "KN-62", "span1": [61, 68], "span2": [90, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4405": {"label": 1, "data": {"text": "However, one mGlu5 PAM, CPPHA (N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide), interacts with a separate allosteric site on mGlu5.", "entity1": "mGlu5", "entity2": "CPPHA", "span1": [167, 172], "span2": [24, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"1484": {"label": 9, "data": {"text": "Similarly, pretreatment with sulindac sulfide blocks the ability of EGF to induce ERK1/2 and Bad phosphorylation, but also down-regulates total Bad but not ERK1/2 protein levels.", "entity1": "ERK1/2", "entity2": "sulindac sulfide", "span1": [156, 162], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14006": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "receptor tyrosine kinases", "entity2": "XL184", "span1": [149, 174], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9820": {"label": 5, "data": {"text": "Methiothepin (intravenous, 1 mg/kg), whose serotonergic actions include 5-HT1 and 5-HT2 antagonism, typically raised serotonin levels (four of five cells) and always blocked inhibition by clomipramine (n = 3).", "entity1": "5-HT2", "entity2": "Methiothepin", "span1": [82, 87], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3733": {"label": 3, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "mTOR", "entity2": "BPs", "span1": [244, 248], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10838": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "KIT", "entity2": "STI571", "span1": [105, 108], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9706": {"label": 3, "data": {"text": "The reversible MAO-A inhibitor, befloxatone (0.3-3 mg/kg), and the irreversible MAO-A inhibitor, clorgyline (10-30 mg/kg), also reduced ethanol self-administration.", "entity1": "MAO-A", "entity2": "befloxatone", "span1": [15, 20], "span2": [32, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16009": {"label": 3, "data": {"text": "RESULTS: Pretreatment of ucOC (30ng/ml) prevented LA-induced apoptosis in insulin-stimulated endothelial cells; effects were abolished by pretreatment with the phosphatidylinositol 3-kinase (PI3-kinase) inhibitor, wortmannin.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "wortmannin", "span1": [160, 189], "span2": [214, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2567": {"label": 2, "data": {"text": "Brain tissue analyses revealed that neonatal quinpirole treatment produced a significant decrease in hippocampal NGF, BDNF and ChAT that was eliminated by olanzapine treatment.", "entity1": "ChAT", "entity2": "olanzapine", "span1": [127, 131], "span2": [155, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5120": {"label": 3, "data": {"text": "In addition, 5HHMF blocked LPS-induced phosphorylation of I\u03baB, resulting in suppression of the nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) subunits, namely p65 and p50, which are important molecules involved in the regulation of iNOS expression.", "entity1": "nuclear factor-\u03baB", "entity2": "5HHMF", "span1": [120, 137], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6959": {"label": 5, "data": {"text": "However, as with the human receptor, maraviroc was shown to be a high affinity, potent functional antagonist of macaque CCR5 thereby indicating that the macaque should be a suitable species in which to evaluate the pharmacology, safety and potential mechanism-related toxicology of novel CCR5 antagonists.", "entity1": "macaque CCR5", "entity2": "maraviroc", "span1": [112, 124], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"368": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "IFN-gamma", "entity2": "DEX", "span1": [80, 89], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9535": {"label": 8, "data": {"text": "System y+ cationic amino acid transport is mediated by proteins encoded by a family of genes, Cat1, Cat2, and Cat3.", "entity1": "Cat1", "entity2": "amino acid", "span1": [94, 98], "span2": [19, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2393": {"label": 0, "data": {"text": "Interestingly, deletion of the entire yeast mitochondrial LeuRS C-terminal domain enhanced its aminoacylation and amino acid editing activities.", "entity1": "yeast mitochondrial LeuRS", "entity2": "C", "span1": [38, 63], "span2": [64, 65]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8190": {"label": 3, "data": {"text": "Collectively, our data suggest that TAM can repress the miR-200 family and induce EMT via the up-regulation of c-Myc in endometrial cancer cells.", "entity1": "miR-200", "entity2": "TAM", "span1": [56, 63], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15273": {"label": 1, "data": {"text": "The CRF(1) receptor antagonist SSR125543 prevents stress-induced cognitive deficit associated with hippocampal dysfunction: Comparison with paroxetine and D-cycloserine.", "entity1": "CRF(1) receptor", "entity2": "D-cycloserine", "span1": [4, 19], "span2": [155, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2340": {"label": 1, "data": {"text": "NO rebinding in HNS from Staphylococcus aureus (SA-HNS) is faster than that measured for either Bacillus anthracis (BA-HNS) or for eNOS(HD) in both oxidized and reduced forms in the presence of arginine.", "entity1": "eNOS(HD)", "entity2": "NO", "span1": [131, 139], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11633": {"label": 1, "data": {"text": "In addition, the molecular configuration of vardenafil differs from that of sildenafil when bound to PDE5.", "entity1": "PDE5", "entity2": "vardenafil", "span1": [101, 105], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8856": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "c-Src", "entity2": "I3S", "span1": [19, 24], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"305": {"label": 4, "data": {"text": "2-(2-Aminoethyl)-quinoline (D-1997): a novel agonist at 5-hydroxytryptamine1-like receptors in the canine basilar artery.", "entity1": "5-hydroxytryptamine1-like receptors", "entity2": "2-(2-Aminoethyl)-quinoline", "span1": [56, 91], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2831": {"label": 3, "data": {"text": "Pharmacological treatment has been studied and it could be demonstrated, that some mutant currents may be insufficiently suppressed by drugs targeted to block the specific current such as, e.g., sotalol or ibutilide in patients with a mutation in the IKr-coding gene KCNH2 (HERG).", "entity1": "HERG", "entity2": "ibutilide", "span1": [274, 278], "span2": [206, 215]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6928": {"label": 8, "data": {"text": "When cultured in YPD medium containing 15% glucose under aerobic conditions, the KGD1 (alpha-ketoglutarate dehydrogenase) gene disrupted mutant produced a lower level of succinate than the wild-type strain, while the SDH1 (succinate dehydrogenase) gene-disrupted mutant produced an increased level of succinate.", "entity1": "KGD1", "entity2": "succinate", "span1": [81, 85], "span2": [170, 179]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2989": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Q817A", "entity2": "sildenafil", "span1": [216, 221], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13143": {"label": 1, "data": {"text": "The changes in CysLT1 receptor expression 24 h after NMDA injection and the effects of a CysLT1 receptor antagonist, pranlukast (0.01 and 0.1 mg/kg), an NMDA receptor antagonist, ketamine (30 mg/kg), and an antioxidant, edaravone (9 mg/kg) were observed.", "entity1": "CysLT1 receptor", "entity2": "NMDA", "span1": [15, 30], "span2": [53, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7094": {"label": 8, "data": {"text": "The glutamate-aspartate transporter GLAST mediates glutamate uptake at inner hair cell afferent synapses in the mammalian cochlea.", "entity1": "glutamate-aspartate transporter", "entity2": "glutamate", "span1": [4, 35], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11395": {"label": 3, "data": {"text": "Using whole-cell voltage clamp, we examined mibefradil block of four Na+ channel isoforms expressed in human embryonic kidney cells: Nav1.5 (cardiac), Nav1.4 (skeletal muscle), Nav1.2 (brain), and Nav1.7 (peripheral nerve).", "entity1": "Nav1.4", "entity2": "mibefradil", "span1": [151, 157], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14786": {"label": 1, "data": {"text": "The present study aimed at investigating the role of reactive oxygen species (ROS) scavenging by TSA on transforming growth factor-\u03b2 (TGF-\u03b2)-induced myofibroblast differentiation of corneal fibroblasts in vitro.", "entity1": "transforming growth factor-\u03b2", "entity2": "TSA", "span1": [104, 132], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"331": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "proline-42-to-alanine", "entity2": "2'-cytidine monophosphate", "span1": [114, 135], "span2": [206, 231]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4657": {"label": 1, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "SIRT1", "entity2": "resveratrol", "span1": [14, 19], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9849": {"label": 9, "data": {"text": "Salicylates do not promote dissociation of (125)I-ET-1 ETB receptor complexes.", "entity1": "ETB receptor", "entity2": "Salicylates", "span1": [55, 67], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"22": {"label": 3, "data": {"text": "The inhibitory effects of iloprost on tissue factor expression were also potentiated by isobutylmethylxanthine and mimicked by forskolin and dibutyryl cyclic AMP but not dibutyryl cyclic GMP.", "entity1": "tissue factor", "entity2": "isobutylmethylxanthine", "span1": [38, 51], "span2": [88, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13084": {"label": 1, "data": {"text": "This dual mode of action of sulfonylureas and glinides may open new perspectives for the molecular pharmacology of antidiabetic drugs, because it provides evidence that drugs can be designed that target both the sulfonylurea receptor and PPARgamma.", "entity1": "PPARgamma", "entity2": "glinides", "span1": [238, 247], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14570": {"label": 1, "data": {"text": "In conclusion, in this cellular model, DOX effectively protects against PQ toxicity by inducing P-gp and through the interaction with the choline transporter, suggesting that compounds presenting this double feature of promoting the efflux and limiting the uptake of PQ could be used as effective antidotes to treat intoxications.", "entity1": "choline transporter", "entity2": "DOX", "span1": [138, 157], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3905": {"label": 3, "data": {"text": "This stimulation was attenuated by the Pak inhibitor 2,2'-dihydroxy-1,1'-dinaphthyldisulfide (IPA3) or dominant-negative Pak1.", "entity1": "Pak", "entity2": "IPA3", "span1": [39, 42], "span2": [94, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9372": {"label": 1, "data": {"text": "However, recovery from modulation by cyclothiazide was twofold slower for GluR-AiBi than for homomeric GluR-Ai, indicating that the GluR-A and GluR-B subunits are not functionally equivalent in controlling sensitivity to cyclothiazide.", "entity1": "GluR-AiBi", "entity2": "cyclothiazide", "span1": [74, 83], "span2": [37, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6092": {"label": 2, "data": {"text": "The distribution pattern of Fos induced by amantadine was more similar to those seen with dopaminomimetics than with N-methyl-D-aspartate (NMDA) receptor antagonists.", "entity1": "Fos", "entity2": "amantadine", "span1": [28, 31], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8725": {"label": 9, "data": {"text": "This preference is partial because UGT2B10 did not conjugate the tertiary cyclic amine in trifluoperazine.", "entity1": "UGT2B10", "entity2": "trifluoperazine", "span1": [35, 42], "span2": [90, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12350": {"label": 3, "data": {"text": "NAC also suppressed the p-JNK and p-p38, but failed to reverse the effects of ISO.", "entity1": "JNK", "entity2": "NAC", "span1": [26, 29], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1030": {"label": 1, "data": {"text": "High p53 protein levels, but not genetic or functional p53 status, were associated with increased topotecan-induced DNA/topoisomerase I complex formation.", "entity1": "topoisomerase I", "entity2": "topotecan", "span1": [120, 135], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9854": {"label": 1, "data": {"text": "Salicylates inhibit (125)I-ET-1 binding to recombinant rat ETA receptors.", "entity1": "ET-1", "entity2": "(125)I", "span1": [27, 31], "span2": [20, 26]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3624": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "AM4054", "span1": [14, 17], "span2": [272, 278]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6767": {"label": 2, "data": {"text": "Hydralazine dose-dependently inhibited PHD activity and induced nonhydroxylated HIF-1alpha, evidence for HIF stabilization specifically by inhibition of PHD enzyme activity.", "entity1": "HIF-1alpha", "entity2": "Hydralazine", "span1": [80, 90], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5852": {"label": 4, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT4", "entity2": "zacopride", "span1": [28, 33], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6018": {"label": 3, "data": {"text": "(2) Exposure histories vary in secondary 11q23 leukemia, as the only topoisomerase II inhibitor was dactinomycin in one case, and, in another case, no topoisomerase II inhibitor was administered.", "entity1": "topoisomerase II", "entity2": "dactinomycin", "span1": [69, 85], "span2": [100, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14286": {"label": 9, "data": {"text": "Disturbances in these signaling pathways are likely to be a consequence of HDAC inhibition because VPD did not affect their expressions.", "entity1": "HDAC", "entity2": "VPD", "span1": [75, 79], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"747": {"label": 3, "data": {"text": "Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain.", "entity1": "LFA-1", "entity2": "lovastatin", "span1": [21, 26], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2344": {"label": 1, "data": {"text": "Lutein and eicosapentaenoic acid interact to modify iNOS mRNA levels through the PPARgamma/RXR pathway in chickens and HD11 cell lines.", "entity1": "PPARgamma", "entity2": "eicosapentaenoic acid", "span1": [81, 90], "span2": [11, 32]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14359": {"label": 5, "data": {"text": "Our results showed that bone remodeling was significantly decreased in CCL3(-/-) and CCR1(-/-) mice and in animals treated with Met-RANTES (an antagonist of CCR5 and CCR1).", "entity1": "CCR5", "entity2": "Met", "span1": [157, 161], "span2": [128, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4200": {"label": 3, "data": {"text": "Pterostilbene exerts antitumor activity against human osteosarcoma cells by inhibiting the JAK2/STAT3 signaling pathway.", "entity1": "STAT3", "entity2": "Pterostilbene", "span1": [96, 101], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14039": {"label": 4, "data": {"text": "Unexpectedly, both the mGluR(5)specific agonist, CHPG, and the group II mGluR (mGlu(2/3)) agonist, LY379268 (LY), induced a TTX-insensitive outward current/hyperpolarization.", "entity1": "group II mGluR", "entity2": "LY379268", "span1": [63, 77], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12553": {"label": 1, "data": {"text": "Intracellular protein-bound [57Co]Cbl fractionated with methionine synthase (MS) and methylmalonyl-CoA mutase (MU) activity.", "entity1": "methylmalonyl-CoA mutase", "entity2": "[57Co]Cbl", "span1": [85, 109], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3091": {"label": 4, "data": {"text": "Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders.", "entity1": "MT2", "entity2": "ramelteon", "span1": [43, 46], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9698": {"label": 4, "data": {"text": "The 5-HT1A agonist activity reported here clearly distinguishes ziprasidone from currently available antipsychotic agents and suggests that this property may play a significant role in its pharmacologic actions.", "entity1": "5-HT1A", "entity2": "ziprasidone", "span1": [4, 10], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8191": {"label": 9, "data": {"text": "In cultured cardiomyocytes, cardiomyocyte hypertrophy induced by the \u03b1(1)-agonist phenylephrine was inhibited by the overexpression of SIRT1 as well as resveratrol, both of which down-regulated p300 protein levels but not p300 mRNA levels.", "entity1": "p300", "entity2": "resveratrol", "span1": [222, 226], "span2": [152, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15891": {"label": 8, "data": {"text": "Targeted disruption of the gene encoding the N-glycosyltransferase, prlH, abolished pyralomicin production, and recombinant expression of PrlA confirms the activity of this enzyme as a sugar phosphate cyclase involved in the formation of the C7-cyclitol moiety.", "entity1": "PrlA", "entity2": "cyclitol", "span1": [138, 142], "span2": [245, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10881": {"label": 3, "data": {"text": "Irinotecan (CPT-11, 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin) has exhibited clinical activities against a broad spectrum of carcinomas by inhibiting DNA topoisomerase I (Topo I).", "entity1": "DNA topoisomerase I", "entity2": "CPT-11", "span1": [175, 194], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3797": {"label": 3, "data": {"text": "[-]-Huperzine A ([-]-Hup A), is a naturally occurring potent reversible AChE inhibitor that penetrates the blood-brain barrier.", "entity1": "AChE", "entity2": "[-]-Huperzine A", "span1": [72, 76], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7473": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "GluRs", "entity2": "L-glutamate", "span1": [50, 55], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12644": {"label": 1, "data": {"text": "Therefore, we conclude that the tissue and sub-cellular localization of calcium channel subunits as well as their specific associations are essential parameters to understand the in vivo effects of Mibefradil.", "entity1": "calcium channel", "entity2": "Mibefradil", "span1": [72, 87], "span2": [198, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11165": {"label": 8, "data": {"text": "To begin to examine whether these changes are mediated by alterations in gene expression for tryptophan hydroxylase (TPH), the rate-limiting enzyme in 5-HT biosynthesis, we quantitated its mRNA levels by competitive reverse transcription-polymerase chain reaction (RT-PCR).", "entity1": "tryptophan hydroxylase", "entity2": "5-HT", "span1": [93, 115], "span2": [151, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6890": {"label": 2, "data": {"text": "ABCG5 and ABCG8 themselves are regulated by cholesterol via liver X receptors (LXRs), which are also activated by oxysterols and some derivatives of plant sterols.", "entity1": "LXRs", "entity2": "sterols", "span1": [79, 83], "span2": [155, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11202": {"label": 1, "data": {"text": "Using Lac repressor-operator complexes as roadblocks, we show that ATP-bound TOP2 acts as a circular clamp capable of entering DNA ends and sliding on unobstructed duplex DNA.", "entity1": "TOP2", "entity2": "ATP", "span1": [77, 81], "span2": [67, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1595": {"label": 3, "data": {"text": "Nevertheless, 3 mM DMA, a higher concentration that inhibits NHE1, NHE2, and NHE3, significantly increased DBS.", "entity1": "NHE1", "entity2": "DMA", "span1": [61, 65], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14895": {"label": 2, "data": {"text": "FMO3 expression is induced by dietary bile acids by a mechanism that involves the farnesoid X receptor (FXR), a bile acid-activated nuclear receptor.", "entity1": "FMO3", "entity2": "bile acids", "span1": [0, 4], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15941": {"label": 1, "data": {"text": "We also recorded a significant correlation between M value increase and the decrease of vaspin, visfatin, and omentin-1 obtained with vildagliptin+metformin.", "entity1": "visfatin", "entity2": "vildagliptin", "span1": [96, 104], "span2": [134, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8867": {"label": 2, "data": {"text": "Activation of STAT3, which is phosphorylated by the IL-6 signaling pathways and thus is necessary for Th17 differentiation, was strongly stimulated by I3S and TCDD.", "entity1": "IL-6", "entity2": "I3S", "span1": [52, 56], "span2": [151, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11671": {"label": 1, "data": {"text": "Equilibrium sedimentation and cross-linking studies demonstrate the cooperative formation of a similarly sized S100A4/TFP oligomer in solution.", "entity1": "S100A4", "entity2": "TFP", "span1": [111, 117], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1200": {"label": 3, "data": {"text": "PURPOSE: Testosterone-to-estradiol ratio levels in infertile men improve during treatment with the aromatase inhibitor, testolactone, and resulting changes in semen parameters.", "entity1": "aromatase", "entity2": "testolactone", "span1": [99, 108], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15475": {"label": 9, "data": {"text": "Glutathione-S-transferase, a phase II enzyme, was inhibited by both arsenic and nicotine but no such inhibition was noted in arsenic-treated animals pre-exposed to nicotine.", "entity1": "Glutathione-S-transferase", "entity2": "arsenic", "span1": [0, 25], "span2": [125, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3056": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "SDF-1", "entity2": "AMD3100", "span1": [142, 147], "span2": [12, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10985": {"label": 3, "data": {"text": "Moreover, the specific PKC-inhibitor 2-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl) maleimide (GF 109203X) markedly increased the potency and E(max) of isoprenaline for all conditions used, including control conditions, and the synergistic effects of PMA and fenoterol were completely prevented.", "entity1": "PKC", "entity2": "2-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl) maleimide", "span1": [23, 26], "span2": [37, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14773": {"label": 3, "data": {"text": "Electrical stimulation, ATP, and insulin each increased fluorescent 2-NBD-Glucose (2-NBDG) uptake in primary myotubes, but only electrical stimulation and ATP-dependent 2-NBDG uptake were inhibited by adenosine-phosphate phosphatase and by purinergic receptor blockade (suramin).", "entity1": "adenosine-phosphate phosphatase", "entity2": "suramin", "span1": [201, 232], "span2": [270, 277]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"513": {"label": 4, "data": {"text": "Zolmitriptan (Zomig; formerly 311C90) is a novel 5-hydroxytryptamine (5HT)1B/1D receptor agonist with proven efficacy in the acute treatment of migraine with or without preceding aura.", "entity1": "5-hydroxytryptamine (5HT)1B/1D", "entity2": "311C90", "span1": [49, 79], "span2": [30, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8950": {"label": 1, "data": {"text": "Analysis of coenzyme binding by human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase and steroid 5----4-ene-isomerase using 5'-[p-(fluorosulfonyl)benzoyl]adenosine, an affinity labeling cofactor analog.", "entity1": "steroid 5----4-ene-isomerase", "entity2": "5'-[p-(fluorosulfonyl)benzoyl]adenosine", "span1": [95, 123], "span2": [130, 169]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"3567": {"label": 1, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u. ), exercise training also increased it in both groups (control, 13.6\u00a0\u00b1\u00a00.1; MSG, 22.2\u00a0\u00b1\u00a01.1\u00a0a.u.).", "entity1": "IRS-1", "entity2": "MSG", "span1": [42, 47], "span2": [209, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13240": {"label": 3, "data": {"text": "Glutamate stimulates glutamate receptor interacting protein 1 degradation by ubiquitin-proteasome system to regulate surface expression of GluR2.", "entity1": "glutamate receptor interacting protein 1", "entity2": "Glutamate", "span1": [21, 61], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10228": {"label": 3, "data": {"text": "Furthermore, thalidomide abolished the LPS-induced increase in CD14 expression and [Ca2+]i elevation in KCs.", "entity1": "CD14", "entity2": "thalidomide", "span1": [63, 67], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8516": {"label": 3, "data": {"text": "Synthesis of a DOTA (Gd(3+))-conjugate of proton-pump inhibitor pantoprazole for gastric wall imaging studies.", "entity1": "proton-pump", "entity2": "DOTA", "span1": [42, 53], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5175": {"label": 2, "data": {"text": "In PFC, DEX caused activation of AKT, augmentation of pro-survival Bcl-2 protein and enhanced Bcl-2/Bax protein ratio, as well Bcl-2 translocation to mitochondria.", "entity1": "Bcl-2", "entity2": "DEX", "span1": [94, 99], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3619": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "\u0394(9)-tetrahydrocannabinol", "span1": [14, 17], "span2": [38, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11237": {"label": 1, "data": {"text": "Taken together, these results reveal several differences between effects of MDMA and previously reported METH on DAT and VMAT-2; differences that may underlie the dissimilar neurotoxic profile of these agents.", "entity1": "VMAT-2", "entity2": "METH", "span1": [121, 127], "span2": [105, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8594": {"label": 2, "data": {"text": "Further, both the flavonoids were also found to increase the expression of some of the prominent markers for differentiation of osteoblast like osteopontin, osterix, RunX2, osteoprotegerin and osteocalcin.", "entity1": "osteopontin", "entity2": "flavonoids", "span1": [144, 155], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14982": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "p53", "entity2": "ATO", "span1": [58, 61], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7087": {"label": 3, "data": {"text": "These currents were produced by glutamate-aspartate transporters (GLAST) (excitatory amino acid transporter 1) because they were weakly inhibited by dihydrokainate, an antagonist of glutamate transporter-1 (excitatory amino acid transporter 2) and were absent from IPCs in GLAST-/- cochleas.", "entity1": "glutamate-aspartate transporters", "entity2": "dihydrokainate", "span1": [32, 64], "span2": [149, 163]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"14612": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ile24Val", "entity2": "dFdC", "span1": [71, 79], "span2": [230, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"16045": {"label": 1, "data": {"text": "The editing of ndhD-2 is also completely lost in albino mutants and norflurazon-treated seedlings.", "entity1": "ndhD-2", "entity2": "norflurazon", "span1": [15, 21], "span2": [68, 79]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5103": {"label": 2, "data": {"text": "In addition, cobalt protoporphyrin (CoPP), a specific HO-1 inducer, predominantly suppressed LPS-induced NO production.", "entity1": "HO-1", "entity2": "cobalt protoporphyrin", "span1": [54, 58], "span2": [13, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9864": {"label": 8, "data": {"text": "Among the various enzymes, dicoumarol inhibitable cytosolic NAD(P)H:quinone oxidoreductase1 (NQO1) was shown to catalyse bioreductive activation of MMC leading to cross-linking of the DNA and cytotoxicity.", "entity1": "NQO1", "entity2": "MMC", "span1": [93, 97], "span2": [148, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6578": {"label": 8, "data": {"text": "The bacterial enzyme maltodextrin phosphorylase (MalP) catalyses the phosphorolysis of an alpha-1,4-glycosidic bond in maltodextrins, removing the non-reducing glucosyl residues of linear oligosaccharides as glucose-1-phosphate (Glc1P).", "entity1": "MalP", "entity2": "glucose-1-phosphate", "span1": [49, 53], "span2": [208, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10133": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "zomepirac", "span1": [34, 37], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11856": {"label": 8, "data": {"text": "The calcium homeostasis proteins sarcoendoplasmic reticulum ATPase 2a (SERCA2a), sodium calcium exchanger-1, phospholamban (PLB), phospho-PLB, and calsequestrin 2 are important for contraction and relaxation.", "entity1": "sarcoendoplasmic reticulum ATPase 2a", "entity2": "calcium", "span1": [33, 69], "span2": [4, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5496": {"label": 3, "data": {"text": "4) High concentrations of I- inhibited the catalatic activity of thyroid peroxidase and lactoperoxidase in a manner similar to that described previously for peroxidase-catalyzed iodination.", "entity1": "thyroid peroxidase", "entity2": "I-", "span1": [65, 83], "span2": [26, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1849": {"label": 3, "data": {"text": "Some of these derivatives showed good inhibitory potency against two human CA isozymes involved in important physiological processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide.", "entity1": "human CA", "entity2": "methazolamide", "span1": [69, 77], "span2": [229, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16001": {"label": 2, "data": {"text": "Moreover, we also demonstrate that puerarin functions at least partially through activation of MEK/ERK and PI3K/Akt signaling.", "entity1": "MEK", "entity2": "puerarin", "span1": [95, 98], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10029": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "chymotrypsin", "entity2": "Arg", "span1": [126, 138], "span2": [54, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"259": {"label": 1, "data": {"text": "In conclusion, these data demonstrate that: (1) the Leu144-Gly150 loop and the FRS are both involved in the conformational transition linked to the binding of p-aminobenzamidine to the thrombin active site; (2) the extent of thrombin's capacity to undergo conformational transitions in alpha-, zeta- and gamma T forms is positively correlated to the free energy of activation for hydrolysis of macromolecular substrates interacting with both the catalytic domain and the FRS.", "entity1": "thrombin", "entity2": "p-aminobenzamidine", "span1": [185, 193], "span2": [159, 177]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13371": {"label": 2, "data": {"text": "Estrogen-regulated genes including cytokeratin 1-19 and Cyp2a4 were over-expressed, although Cyp3a25 was suppressed.", "entity1": "Cyp2a4", "entity2": "Estrogen", "span1": [56, 62], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"879": {"label": 5, "data": {"text": "This effect has been attributed to the antagonist effects of pindolol at the 5-HT(1A) receptor.", "entity1": "5-HT(1A)", "entity2": "pindolol", "span1": [77, 85], "span2": [61, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1013": {"label": 2, "data": {"text": "Moreover, IGFBP-rP2 noticeably increased in response to TGF-beta1 and all-trans retinoic acid (atRA) in HPEC and PC-3 cells, and it decreased in response to IGF-I in HPEC.", "entity1": "IGFBP-rP2", "entity2": "atRA", "span1": [10, 19], "span2": [95, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10067": {"label": 3, "data": {"text": "Omapatrilat, the prototypical vasopeptidase inhibitor, inhibits not only ACE but also neutral endopeptidase.", "entity1": "ACE", "entity2": "Omapatrilat", "span1": [73, 76], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8169": {"label": 1, "data": {"text": "In contrast to wild-type pol \u03b2, the ternary complex of the R283K mutant with an incoming dATP-analogue and templating 8-oxoG resembles a G-A mismatched structure with 8-oxoG adopting an anti-conformation.", "entity1": "pol \u03b2", "entity2": "dATP", "span1": [25, 30], "span2": [89, 93]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2953": {"label": 0, "data": {"text": "Cocrystal structures of PDE5 catalytic (C) domain with inhibitors reveal a hydrogen bond and hydrophobic interactions with Tyr-612, hydrogen bonds with Gln-817, a hydrophobic clamp formed by Phe-820 and Val-782, and contacts with His-613, Leu-765, and Phe-786 [Sung et al.", "entity1": "PDE5 catalytic (C) domain", "entity2": "Val", "span1": [24, 49], "span2": [203, 206]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6713": {"label": 9, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "Flt3", "entity2": "phenylaminopyrimidine", "span1": [52, 56], "span2": [77, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5730": {"label": 3, "data": {"text": "Rg1 attenuated the A\u03b225-35-associated mitochondrial apoptotic events, accompanied by inhibiting HIF-1\u03b1 expression followed by intracellular reactive nitrogen species generation, and protein nitrotyrosination.", "entity1": "HIF-1\u03b1", "entity2": "Rg1", "span1": [96, 102], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10079": {"label": 3, "data": {"text": "Aspirin and salicylate bind to immunoglobulin heavy chain binding protein (BiP) and inhibit its ATPase activity in human fibroblasts.", "entity1": "ATPase", "entity2": "salicylate", "span1": [96, 102], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2266": {"label": 1, "data": {"text": "The present results suggest the involvement of astrocytes in the regulation of the glutamatergic activation associated with withdrawal from free-choice ethanol consumption and point to differential adaptations of GS and GFAP to prolonged alcohol drinking in the PLC of P rats.", "entity1": "GFAP", "entity2": "ethanol", "span1": [220, 224], "span2": [152, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5467": {"label": 4, "data": {"text": "In the locus coeruleus, brexpiprazole reversed the inhibitory effect of the preferential 5-HT2A receptor agonist DOI (2,5-dimethoxy-4-iodoamphetamine) on norepinephrine neuronal firing (ED50 = 110 mug/kg), demonstrating 5-HT2A antagonistic action.", "entity1": "5-HT2A", "entity2": "2,5-dimethoxy-4-iodoamphetamine", "span1": [89, 95], "span2": [118, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8210": {"label": 2, "data": {"text": "Pb and BaP treatments significantly increased active caspase-3 levels in a time-dependent manner.", "entity1": "caspase-3", "entity2": "BaP", "span1": [53, 62], "span2": [7, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5853": {"label": 5, "data": {"text": "A number of selective 5-HT3 antagonists have been developed including ondansetron, granisetron, tropisetron renzapride and zacopride.", "entity1": "5-HT3", "entity2": "zacopride", "span1": [22, 27], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8736": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "diphenhydramine", "span1": [225, 231], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8523": {"label": 8, "data": {"text": "CYP3A5 carrier status had no influence on midazolam oral clearance or its inhibition by ketoconazole.", "entity1": "CYP3A5", "entity2": "midazolam", "span1": [0, 6], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10953": {"label": 8, "data": {"text": "These results provide biochemical evidence of a H(+)-coupled and saturable transport system, presumed to be a low-affinity monocarboxylate transporter MCT4 or other unknown H(+)-coupled monocarboxylate transport system, for nicotinate in rat cerebrocortical astrocytes.", "entity1": "H(+)-coupled monocarboxylate transport system", "entity2": "nicotinate", "span1": [173, 218], "span2": [224, 234]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10166": {"label": 1, "data": {"text": "Considerable evidence indicates that serotonergic mechanisms, particularly the serotonin transporter (5HTT), may mediate central effects of cocaine and may also be involved in impulsive and aggressive behavior.", "entity1": "5HTT", "entity2": "cocaine", "span1": [102, 106], "span2": [140, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"899": {"label": 3, "data": {"text": "Our data demonstrate differences in the mechanism of stimulation of phenylalanine hydroxylase and nitric oxide synthase by H(4)biopterin.", "entity1": "phenylalanine hydroxylase", "entity2": "H(4)biopterin", "span1": [68, 93], "span2": [123, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7868": {"label": 2, "data": {"text": "Fingolimod (FTY720), a novel drug approved for the treatment of relapsing-remitting multiple sclerosis, activates different sphingosine-1-phosphate receptor (S1PR) subtypes.", "entity1": "S1PR", "entity2": "FTY720", "span1": [158, 162], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8416": {"label": 1, "data": {"text": "Bisacylimidoselenocarbamates Cause G2/M Arrest Associated with the Modulation of CDK1 and Chk2 in Human Breast Cancer MCF-7 Cells.", "entity1": "Chk2", "entity2": "Bisacylimidoselenocarbamates", "span1": [90, 94], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6702": {"label": 1, "data": {"text": "Inhibitory effects of the monoamine oxidase inhibitor tranylcypromine on the cytochrome P450 enzymes CYP2C19, CYP2C9, and CYP2D6.", "entity1": "CYP2C19", "entity2": "tranylcypromine", "span1": [101, 108], "span2": [54, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"172": {"label": 1, "data": {"text": "The most potent compound, D,L-4-(3,4-dichlorobenzoylamino)-5-(dipentylamino)-5-oxo-pen tanoic acid (lorglumide, CR 1409), has a great affinity for the pancreatic CCK receptors and is a competitive, specific and potent CCK antagonist on the smooth muscles of the gall bladder and ileum of the guinea pig and on the CCK-induced amylase secretion of isolated pancreatic acini.", "entity1": "CCK receptors", "entity2": "CR 1409", "span1": [162, 175], "span2": [112, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2328": {"label": 3, "data": {"text": "Reboxetine, a selective norepinephrine reuptake inhibitor, exhibits high affinity and selectivity for the human norepinephrine transporter.", "entity1": "human norepinephrine transporter", "entity2": "Reboxetine", "span1": [106, 138], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5076": {"label": 2, "data": {"text": "Here, we have now found that activation of p38 MAPK by anisomycin potentiated induction of CYP2B6 mRNA by CAR ligand in HepG2 cells to levels observed in ligand-treated human primary hepatocytes.", "entity1": "CYP2B6", "entity2": "anisomycin", "span1": [91, 97], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3268": {"label": 1, "data": {"text": "Two TFP molecules bind within the hydrophobic target binding pocket of Ca(2+)-S100A4 with no significant conformational changes observed in the protein upon complex formation.", "entity1": "S100A4", "entity2": "TFP", "span1": [78, 84], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4539": {"label": 3, "data": {"text": "The in vivo inhibitory effect of harmaline on CYP2D6-catalyzed bufotenine formation was confirmed by in vitro study using purified CYP2D6.", "entity1": "CYP2D6", "entity2": "harmaline", "span1": [46, 52], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15522": {"label": 1, "data": {"text": "A highly potent inhibition of the peroxidase catalytic reaction by NO/SNO was seen in assays employing the coupled Prx-Trx system.", "entity1": "Trx", "entity2": "SNO", "span1": [119, 122], "span2": [70, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13774": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "c-KIT", "entity2": "INNO-406", "span1": [309, 314], "span2": [278, 286]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4048": {"label": 3, "data": {"text": "Neoechinulin A suppresses amyloid-\u03b2 oligomer-induced microglia activation and thereby protects PC-12 cells from inflammation-mediated toxicity.", "entity1": "amyloid-\u03b2", "entity2": "Neoechinulin A", "span1": [26, 35], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15160": {"label": 2, "data": {"text": "GnRH pulse frequency-dependent stimulation of FSH\u03b2 transcription is mediated via activation of PKA and CREB.", "entity1": "PKA", "entity2": "GnRH", "span1": [95, 98], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6397": {"label": 5, "data": {"text": "The glucocorticoid receptor antagonist RU-486 (mifepristone) significantly counteracted the effect of dexamethasone on glucocorticoid receptor activation, indicating that the dexamethasone effect is specific and is mediated through the glucocorticoid receptor.", "entity1": "glucocorticoid receptor", "entity2": "mifepristone", "span1": [4, 27], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1885": {"label": 9, "data": {"text": "I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance.", "entity1": "PKC-delta", "entity2": "I3A", "span1": [76, 85], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3531": {"label": 2, "data": {"text": "Phosphorylation of AMPK at Thr172 increased by 1.4-fold within 5 min, and remained elevated throughout a 30-min time course, in response to 2-deoxyglucose.", "entity1": "AMPK", "entity2": "2-deoxyglucose", "span1": [19, 23], "span2": [140, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9973": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-1", "entity2": "sulindac", "span1": [214, 219], "span2": [54, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3386": {"label": 6, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "GABA(A)R", "entity2": "neurosteroids", "span1": [24, 32], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12509": {"label": 1, "data": {"text": "Among all the organophosphates tested, the combination of a methyl group and a negatively charged oxygen attached to the P atom, CH3P(O)(O-)-AChE, conferred the greatest protection to the active site of aged or nonaged organophosphoryl conjugates of acetylcholinesterase.", "entity1": "acetylcholinesterase", "entity2": "organophosphoryl", "span1": [250, 270], "span2": [219, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14160": {"label": 4, "data": {"text": "In rat striatum and nucleus accumbens, mianserin stimulated [35S]GTPgammaS binding in a nor-BNI-sensitive manner with maximal effects lower than those of the full kappa-opioid agonists (-)-U50,488 and dynorphin A.", "entity1": "kappa-opioid", "entity2": "(-)-U50,488", "span1": [163, 175], "span2": [185, 196]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15137": {"label": 3, "data": {"text": "A large number of aromatic/heterocyclic sulfonamides and some 5-mercapto-1,3,4-thiadiazoles were investigated as TcCA inhibitors.", "entity1": "TcCA", "entity2": "5-mercapto-1,3,4-thiadiazoles", "span1": [113, 117], "span2": [62, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14591": {"label": 3, "data": {"text": "In addition, 17-AAG treatment reduced cell viability, CDK2, CDK4, cyclin E, cyclin D1, and phosphorylated Rb levels in AhR-expressing lung AD cells.", "entity1": "CDK2", "entity2": "17-AAG", "span1": [54, 58], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14495": {"label": 1, "data": {"text": "Estrogen effects are mediated not only through nuclear ERs but also through cytoplasmic/membrane ERs and G-protein-coupled ERs.", "entity1": "ERs", "entity2": "Estrogen", "span1": [55, 58], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5797": {"label": 0, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "EC 3.5.1.14", "entity2": "amino acid", "span1": [109, 120], "span2": [29, 39]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1127": {"label": 3, "data": {"text": "Pimozide blocked erg3 channel currents with an IC(50) of 103 nM and significant inhibition was noted at concentrations of 10 nM and higher.", "entity1": "erg3", "entity2": "Pimozide", "span1": [17, 21], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11869": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "peonidin", "span1": [118, 143], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10709": {"label": 1, "data": {"text": "The dextromethorphan analog dimemorfan attenuates kainate-induced seizures via sigma1 receptor activation: comparison with the effects of dextromethorphan.", "entity1": "sigma1 receptor", "entity2": "dextromethorphan", "span1": [79, 94], "span2": [138, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"496": {"label": 0, "data": {"text": "A factor X peptide duplicating the inter-EGF sequence Leu83-Phe84-Thr85-Arg86-Lys87-Leu88- (Gly) inhibited factor V/Va-independent prothrombin activation by HUVEC and blocked binding of 125I-factor Xa to these cells in a dose-dependent manner (IC50 approximately 20-40 microM).", "entity1": "factor X", "entity2": "Gly", "span1": [2, 10], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5503": {"label": 1, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "dezocine", "span1": [108, 126], "span2": [158, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1073": {"label": 1, "data": {"text": "However, fasciculin-2, a potent peptide inhibitor of acetylcholinesterase (IC50 24 nM), did prevent catabolism of acetylcholine in rat brain membranes with an atypical inhibition isotherm of [3H]-oxotremorine-M binding, thus permitting an estimation of the \"global affinity\" of acetylcholine (Ki 85 nM) for [3H]-oxotremorine-M-labelled muscarinic receptors in rat brain.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [336, 356], "span2": [307, 326]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13514": {"label": 1, "data": {"text": "Since 10(-3)M H(2)O(2) oxidises methionine and tryptophan residues in proteins, we examined calcium binding to calmodulin in the presence and absence of H(2)O(2) utilising (45)calcium.", "entity1": "calmodulin", "entity2": "H(2)O(2)", "span1": [111, 121], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15079": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "ESBL", "entity2": "ceftazidime", "span1": [192, 196], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6176": {"label": 3, "data": {"text": "Ibuprofen (300 microM) reduced CFTR Cl- current by 60+/-16% and this was explained by a short-lived block (approximately 1.2 ms) which causes an apparent reduction in single channel amplitude from 1.07+/-0.04 pA to 0.59+/-0.04 pA (n = 3).", "entity1": "CFTR", "entity2": "Ibuprofen", "span1": [31, 35], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14794": {"label": 2, "data": {"text": "In conclusion, this study provides the first evidence implicating that TSA inhibits TGF-\u03b2-induced ROS accumulation and myofibroblast differentiation via enhanced Nrf2-ARE signaling.", "entity1": "ARE", "entity2": "TSA", "span1": [167, 170], "span2": [71, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4617": {"label": 2, "data": {"text": "Chronic consumption of alcohol also stimulated abrupt increases in pro-inflammatory cytokines such as nuclear factor (NF)-\u03baB, tumor necrosis factor (TNF)-\u03b1 and interleukin (IL)-1\u03b2 in liver otherwise co-administration of CNF effectively suppressed production of these cytokines dose-dependently.", "entity1": "nuclear factor (NF)-\u03baB", "entity2": "alcohol", "span1": [102, 124], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13062": {"label": 3, "data": {"text": "Similar to AMR and AMROH, adriamycin and etoposide (VP-16) are DNA topoisomerase II inhibitors.", "entity1": "DNA topoisomerase II", "entity2": "etoposide", "span1": [63, 83], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12521": {"label": 3, "data": {"text": "These findings suggest that ceruletide specifically suppresses the barrel rotation evoked by SMS 201-995 in a long-lasting manner possibly acting through CCK-A receptor.", "entity1": "CCK-A receptor", "entity2": "ceruletide", "span1": [154, 168], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1080": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "pyridostigmine", "span1": [51, 71], "span2": [119, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9645": {"label": 4, "data": {"text": "Binding of hydroxyflutamide to m-AR in LNCaP cells resulted in a concentration-dependent stimulation of PSA expression, suggesting that hydroxyflutamide acted as an agonist of the m-AR.", "entity1": "AR", "entity2": "hydroxyflutamide", "span1": [182, 184], "span2": [136, 152]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5216": {"label": 2, "data": {"text": "In addition, vinblastine induces the DNA-binding activities of the transcription factor NF-\u03baB, HSF1, AP-1, and ATF-2, together with the expression of HSP70 and Bax proteins.", "entity1": "HSF1", "entity2": "vinblastine", "span1": [95, 99], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7390": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "Proline dehydrogenase", "entity2": "proline", "span1": [0, 21], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5411": {"label": 2, "data": {"text": "Type I deiodinase, liver fatty-acid binding protein and cytochrome P450 (CYP) 3A37 mRNA levels were significantly induced by TCPP, while TDCPP induced CYP3A37 and CYP2H1.", "entity1": "CYP2H1", "entity2": "TDCPP", "span1": [163, 169], "span2": [137, 142]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13554": {"label": 8, "data": {"text": "It is thought to play a critical role in the visual cycle by functioning as an acceptor of 11-cis-retinol from the isomerohydrolase reaction.", "entity1": "isomerohydrolase", "entity2": "11-cis-retinol", "span1": [115, 131], "span2": [91, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10408": {"label": 1, "data": {"text": "Unlike OFQ II(1-17), high concentrations of its C-terminal extension, OFQ II(1-28), stimulated [35S]-GTPgammaS binding in a mu (mu) opioid receptor-like distribution and the effect was blocked by naloxone.", "entity1": "mu (mu) opioid receptor", "entity2": "naloxone", "span1": [124, 147], "span2": [196, 204]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12205": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D5D", "entity2": "LNA", "span1": [290, 293], "span2": [250, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10074": {"label": 1, "data": {"text": "Salicylates inhibited ATPase activity stimulated by this specific heptapeptide but did not block ATP binding or induce BiP expression.", "entity1": "ATPase", "entity2": "ATP", "span1": [22, 28], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15811": {"label": 3, "data": {"text": "Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors.", "entity1": "kinase", "entity2": "imidazo[1,2-c]pyrimidine", "span1": [109, 115], "span2": [78, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13468": {"label": 8, "data": {"text": "The mitochondrial ACC2 is primarily expressed in heart and skeletal muscle, where it is involved in the regulation of fatty acid oxidation.", "entity1": "ACC2", "entity2": "fatty acid", "span1": [18, 22], "span2": [118, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4886": {"label": 3, "data": {"text": "Separate 5-aza-2'-deoxycytidine pretreatment or in combination with trichostatin A reduced (m)CpG and specific small interference RNAs targeting Mecp2 and Creb1 separately or together depleting Mecp2 and/or Creb1 binding of glut3-(m)CpGs reduced glut3 expression in HT22 cells.", "entity1": "Creb1", "entity2": "trichostatin A", "span1": [155, 160], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2909": {"label": 3, "data": {"text": "The fact that acetaminophen acts functionally as a selective COX-2 inhibitor led us to investigate the hypothesis of whether it works via preferential COX-2 blockade.", "entity1": "COX-2", "entity2": "acetaminophen", "span1": [61, 66], "span2": [14, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13580": {"label": 5, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "NMDA receptor", "entity2": "(+)-MK 801", "span1": [188, 201], "span2": [110, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2329": {"label": 9, "data": {"text": "Theophylline exposure resulted in a sustained increase in mRNA expression for CysS and PDE3A, but PDE4D gene expression was unchanged.", "entity1": "PDE4D", "entity2": "Theophylline", "span1": [98, 103], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2768": {"label": 3, "data": {"text": "Lumiracoxib is the first example of a marketed COX-2 inhibitor of the arylacetic acid class, and it is reported to be the most selective COXIB in vivo.", "entity1": "COX-2", "entity2": "Lumiracoxib", "span1": [47, 52], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13332": {"label": 9, "data": {"text": "Fluoxetine affected mainly the hSERT transport rate by reducing the availability of the transporter in the membrane with no significant alteration of either the total hSERT protein content or the hSERT mRNA level.", "entity1": "hSERT", "entity2": "Fluoxetine", "span1": [196, 201], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6613": {"label": 5, "data": {"text": "Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol.", "entity1": "Histamine H1-receptor", "entity2": "promethazine", "span1": [0, 21], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11385": {"label": 1, "data": {"text": "In this sample of neuroleptic-refractory schizophrenic patients, olanzapine and clozapine showed a different pattern of occupancy of D2-like receptor despite a common lack of extrapyramidal side-effects.", "entity1": "D2-like receptor", "entity2": "olanzapine", "span1": [133, 149], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1805": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "Erbitux", "span1": [0, 32], "span2": [224, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10158": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "fulvestrant", "span1": [110, 127], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7068": {"label": 2, "data": {"text": "Retinoid is a collective term for compounds which bind to and activate retinoic acid receptors (RARalpha, beta, gamma and RXRalpha, beta, gamma), members of nuclear hormone receptor superfamily.", "entity1": "nuclear hormone receptor", "entity2": "Retinoid", "span1": [157, 181], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7783": {"label": 2, "data": {"text": "We also investigated the epigenetic status of NIS promoter after PJ34 treatment in TPC1 cell line: in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3), surprisingly we observed also an increase of H3K27me3, a classical repressive mark.", "entity1": "H3K9K14ac", "entity2": "PJ34", "span1": [168, 177], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3007": {"label": 3, "data": {"text": "These results may have implications in the development of novel DPP-IV inhibitors based on the use of atorvastatin as a lead compound for the treatment of type 2 diabetes.", "entity1": "DPP-IV", "entity2": "atorvastatin", "span1": [64, 70], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10365": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-7", "entity2": "GW660511X", "span1": [64, 71], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13639": {"label": 0, "data": {"text": "Crystallographic data reveal that a conserved Gly residue (located at the juncture between the linker and C-terminal domains) is at one end of a short alpha-helix, which extends to the active site Tyr covalently linked to the DNA.", "entity1": "alpha-helix", "entity2": "Tyr", "span1": [151, 162], "span2": [197, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10994": {"label": 3, "data": {"text": "Tyrosine kinase inhibitors are quinazoline-derived, low molecular weight synthetic molecules that can block the intracellular tyrosine kinase domain of several receptors, including EGFR, Erb2, and vascular endothelial growth factor receptor, and thereby inhibit ligand-induced receptor phosphorylation and abrogate the biologic effect of EGFR signaling.", "entity1": "vascular endothelial growth factor receptor", "entity2": "quinazoline", "span1": [197, 240], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15294": {"label": 3, "data": {"text": "Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.", "entity1": "TF", "entity2": "bicyclic pyrazinone and pyrimidinone amides", "span1": [78, 80], "span2": [24, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"515": {"label": 4, "data": {"text": "Zolmitriptan (Zomig; formerly 311C90) is a novel 5-hydroxytryptamine (5HT)1B/1D receptor agonist with proven efficacy in the acute treatment of migraine with or without preceding aura.", "entity1": "5-hydroxytryptamine (5HT)1B/1D", "entity2": "Zolmitriptan", "span1": [49, 79], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15088": {"label": 3, "data": {"text": "Pharmacodynamic data suggest that ceftazidime-avibactam is rapidly bactericidal versus \u03b2-lactamase-producing Gram-negative bacilli that are not inhibited by ceftazidime alone.Clinical trials to date have reported that ceftazidime-avibactam is as effective as standard carbapenem therapy in complicated intra-abdominal infection and complicated urinary tract infection, including infection caused by cephalosporin-resistant Gram-negative isolates.", "entity1": "\u03b2-lactamase", "entity2": "ceftazidime", "span1": [87, 98], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"142": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited the actin-activated Mg2+-ATPase activity of smooth muscle myosin (IC50 = 25.1 microM).", "entity1": "myosin", "entity2": "Felodipine", "span1": [105, 111], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9169": {"label": 7, "data": {"text": "Chromatographic analysis of the metabolism of 14C-labeled arachidonic acid in this system revealed that PB-dependent inactivation of PHS is markedly increased in the presence of 100 microM H2O2.", "entity1": "PHS", "entity2": "PB", "span1": [133, 136], "span2": [104, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6173": {"label": 1, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "CFTR", "entity2": "cAMP", "span1": [182, 186], "span2": [89, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13346": {"label": 8, "data": {"text": "Lymphocytes possess the essential components of a cholinergic system, including acetylcholine (ACh); choline acetyltransferase (ChAT), its synthesizing enzyme; and both muscarinic and nicotinic ACh receptors (mAChRs and nAChRs, respectively).", "entity1": "choline acetyltransferase", "entity2": "acetylcholine", "span1": [101, 126], "span2": [80, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12223": {"label": 1, "data": {"text": "Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine.", "entity1": "Trace amine-associated receptor 1", "entity2": "para-hydroxyamphetamine", "span1": [0, 33], "span2": [128, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8069": {"label": 9, "data": {"text": "Contrary to the hypothesis, orlistat at 1 nM inhibited CES2 activity by 75% but no inhibition on CES1, placing CES2 one of the most sensitive targets of orlistat.", "entity1": "CES1", "entity2": "orlistat", "span1": [97, 101], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3135": {"label": 3, "data": {"text": "These results suggest that fluoxetine inhibited the activity of VMAT2 by a mechanism different from that of reserpine and did not directly interact with the active site of VMAT2.", "entity1": "VMAT2", "entity2": "fluoxetine", "span1": [172, 177], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11065": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "prednisone", "span1": [89, 95], "span2": [392, 402]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"722": {"label": 1, "data": {"text": "The dimeric C-terminal deletion mutant (Delta473-528) of hTH1 also showed negative cooperativity of H4biopterin binding (h = 0.4).", "entity1": "hTH1", "entity2": "H4biopterin", "span1": [57, 61], "span2": [100, 111]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14173": {"label": 2, "data": {"text": "The purpose of this review is to summarize current knowledge about oxysterol-dependent activation by LXR of genes involved in reverse cholesterol transport, and what these defects of cell cholesterol homeostasis can teach us about the critical pathways of oxysterol generation for expression of LXR-dependent genes.", "entity1": "LXR", "entity2": "oxysterol", "span1": [101, 104], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8040": {"label": 1, "data": {"text": "Exposure of H9c2 cells to high glucose reduced AMPK activity, inhibited Jun NH2-terminal kinase 1 (JNK1)-B-cell lymphoma 2 (Bcl-2) signaling, and promoted Beclin1 binding to Bcl-2.", "entity1": "Beclin1", "entity2": "glucose", "span1": [155, 162], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1890": {"label": 1, "data": {"text": "I3A was unable to cause the same extent of association of the C1b domain of PKC-delta with lipids, compared with PMA or the physiological regulator diacylglycerol, and was able to partially block the association induced by these agents, measured by surface plasmon resonance.", "entity1": "PKC-delta", "entity2": "PMA", "span1": [76, 85], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1373": {"label": 1, "data": {"text": "The L0 linker has been reported to be required for glibenclamide binding, and DeltaNK(IR)6.2/SUR1 channels exhibit reduced labeling of K(IR) with (125)I-azidoglibenclamide, implying that the K(IR) N terminus and L0 of SUR1 are in proximity.", "entity1": "SUR1", "entity2": "(125)I-azidoglibenclamide", "span1": [93, 97], "span2": [146, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14496": {"label": 1, "data": {"text": "Estrogen effects are mediated not only through nuclear ERs but also through cytoplasmic/membrane ERs and G-protein-coupled ERs.", "entity1": "ERs", "entity2": "Estrogen", "span1": [97, 100], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3633": {"label": 9, "data": {"text": "NaAsO(2) increased the mRNA levels of the light and medium subunits of neurofilament and decreased the mRNA levels of tau and tubulin in a dose-dependent manner; no significant effect was found in the mRNA levels of the heavy subunit of neurofilament, microtubule-associated protein 2, or actin.", "entity1": "heavy subunit of neurofilament", "entity2": "NaAsO(2)", "span1": [220, 250], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3599": {"label": 1, "data": {"text": "Interestingly, recent crystallographic evidence identified that ifenprodil, unlike zinc, binds at the interface of the GluN1/GluN2B amino terminal domain dimer by an induced-fit mechanism.", "entity1": "GluN2B", "entity2": "ifenprodil,", "span1": [125, 131], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"405": {"label": 3, "data": {"text": "Previous studies by this research team proved that vasodilating prostaglandins (PGs) E1, E2 and I2 inhibit carbonic anhydrase (CA) in vitro and in vivo, which suggested involvement of CA in gastric acid secretion inhibition and the increase of gastric mucosa blood flow produced by this group of PGs.", "entity1": "carbonic anhydrase", "entity2": "prostaglandins", "span1": [107, 125], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14633": {"label": 8, "data": {"text": "In conclusion, the Lys27Gln substitution does not significantly modulate CDA activity toward dFdC, and therefore would not contribute to interindividual variability in response to gemcitabine.", "entity1": "Lys27Gln", "entity2": "dFdC", "span1": [19, 27], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1588": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "butyrylcholinesterase", "entity2": "4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline", "span1": [36, 57], "span2": [313, 374]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13921": {"label": 3, "data": {"text": "Phenformin has a direct inhibitory effect on the ATP-sensitive potassium channel.", "entity1": "ATP-sensitive potassium channel", "entity2": "Phenformin", "span1": [49, 80], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14981": {"label": 2, "data": {"text": "Additionally, these effects of ATO on \u03b3-H2AX, Chk1, Chk2, p53, and p21(waf1/cip1) were reduced by an ATM inhibitor.", "entity1": "Chk2", "entity2": "ATO", "span1": [52, 56], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3939": {"label": 3, "data": {"text": "All compounds showed low activity toward inhibition of AChE caused by dichlorvos.", "entity1": "AChE", "entity2": "dichlorvos", "span1": [55, 59], "span2": [70, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8670": {"label": 2, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "c-Abl", "entity2": "cisplatin", "span1": [183, 188], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10438": {"label": 1, "data": {"text": "The holo-SDH contained PLP-OMS aldimine in the active site, indicating that OMS can form the Schiff base linkage with PLP, but the subsequent dehydration did not occur.", "entity1": "holo-SDH", "entity2": "aldimine", "span1": [4, 12], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14378": {"label": 3, "data": {"text": "NFD suppressed EGF-mediated protein levels of c-Jun and c-Fos, and reduced MMP-9 expression and activity, concomitantly with a marked inhibition on cell migration and invasion without obvious cellular cytotoxicity.", "entity1": "c-Fos", "entity2": "NFD", "span1": [56, 61], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"392": {"label": 1, "data": {"text": "The e2 domain thus plays some role in CP 55,940 binding but none in SR 141716A recognition, binding of the latter clearly implicating residues in the adjoining transmembrane helices.", "entity1": "e2 domain", "entity2": "SR 141716A", "span1": [4, 13], "span2": [68, 78]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1162": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "mitiglinide", "span1": [68, 72], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11706": {"label": 3, "data": {"text": "When further examined for its anticancer mechanism, SB365 effectively suppressed the AKT/mTOR pathway both in vitro and in vivo.", "entity1": "mTOR", "entity2": "SB365", "span1": [89, 93], "span2": [52, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3737": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates (N-BPs) induce apoptosis in tumor cells by inhibiting the prenylation of small G-proteins.", "entity1": "G-proteins", "entity2": "bisphosphonates", "span1": [115, 125], "span2": [20, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"611": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "interleukin-2", "entity2": "arachidonyl trifluoromethyl ketone", "span1": [178, 191], "span2": [130, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9725": {"label": 0, "data": {"text": "To identify key amino acids involved in factor IX activation, recombinant factor XIa proteins containing alanine substitutions for wild-type sequence were expressed in 293 fibroblasts and tested in a plasma clotting assay.", "entity1": "factor IX", "entity2": "amino acids", "span1": [40, 49], "span2": [16, 27]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5002": {"label": 1, "data": {"text": "Chalcogenopyrylium Dyes as Differential Modulators of Organic Anion Transport by MRP1, MRP2 and MRP4.", "entity1": "MRP1", "entity2": "Chalcogenopyrylium", "span1": [81, 85], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14813": {"label": 4, "data": {"text": "Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist \u0394(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054.", "entity1": "CB(1)", "entity2": "rimonabant", "span1": [151, 156], "span2": [221, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12273": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1a)", "entity2": "AVP", "span1": [133, 138], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7591": {"label": 3, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: Amiodarone analogues with better hERG channel inhibition and cytotoxicity profiles than the parent compound have been identified, demonstrating that cytotoxicity and hERG channel interaction are mechanistically distinct and separable properties of the compounds.", "entity1": "hERG", "entity2": "Amiodarone", "span1": [63, 67], "span2": [30, 40]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8587": {"label": 3, "data": {"text": "In addition, fisetin supplementation significantly reduced hepatic mRNA abundance of FAS, ATPCL and G6Pase compared to the control group.", "entity1": "ATPCL", "entity2": "fisetin", "span1": [90, 95], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13889": {"label": 3, "data": {"text": "Of these, the thrombin inhibitor dabigatran and factor Xa inhibitor rivaroxaban have recently been licensed for thromboprophylaxis after orthopaedic surgery mainly in Europe.", "entity1": "thrombin", "entity2": "dabigatran", "span1": [14, 22], "span2": [33, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12437": {"label": 6, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "M5", "entity2": "VU0467903", "span1": [173, 175], "span2": [188, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14266": {"label": 8, "data": {"text": "Metabolism of triethylenetetramine and 1,12-diamino-3,6,9-triazadodecane by the spermidine/spermine-N(1)-acetyltransferase and thialysine acetyltransferase.", "entity1": "spermidine/spermine-N(1)-acetyltransferase", "entity2": "triethylenetetramine", "span1": [80, 122], "span2": [14, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10955": {"label": 3, "data": {"text": "The marked antihypertensive efficacy of olmesartan medoxomil may result from a unique pharmacological interaction of the drug with the AT1 receptor, resulting in a potent, long-lasting, dose-dependent blockade of A-II.", "entity1": "A-II", "entity2": "olmesartan medoxomil", "span1": [213, 217], "span2": [40, 60]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1995": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "EL3", "entity2": "Pro", "span1": [91, 94], "span2": [47, 50]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10156": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "ICI 182,780", "span1": [110, 127], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8333": {"label": 5, "data": {"text": "Palonosetron, a second-generation 5-HT3 receptor antagonist with a different half-life, a different binding capacity and a different mechanism of action than the first-generation 5-HT3 receptor antagonists appears to be the most effective agent in its class.", "entity1": "5-HT3", "entity2": "Palonosetron", "span1": [34, 39], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9452": {"label": 1, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP4", "entity2": "1-OH-PGE1", "span1": [167, 170], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4526": {"label": 8, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "hCES2", "entity2": "acyl glucuronides", "span1": [143, 148], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13080": {"label": 1, "data": {"text": "Our work shows that sulfonylureas and glinides additionally bind to PPARgamma and exhibit PPARgamma agonistic activity.", "entity1": "PPARgamma", "entity2": "glinides", "span1": [68, 77], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3366": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-type voltage-gated calcium channels", "entity2": "neurosteroids", "span1": [114, 151], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8957": {"label": 7, "data": {"text": "FSA is a cofactor site-directed reagent that binds with similar affinity as a competitive inhibitor of NAD+ reduction by dehydrogenase (Ki = 162 microM) or as a stimulator of isomerase (Km = 153 microM).", "entity1": "dehydrogenase", "entity2": "NAD+", "span1": [121, 134], "span2": [103, 107]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"4149": {"label": 3, "data": {"text": "Local PGE2 administration prevented the increase of airway IL-13 and osteopontin and kept lung plasmacytoid dendritic cell counts close to baseline.", "entity1": "IL-13", "entity2": "PGE2", "span1": [59, 64], "span2": [6, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14508": {"label": 3, "data": {"text": "The MCAO-induced decrease in insulin receptor levels in the liver and skeletal muscle on day 1 was recovered to control levels by orexin-A, and this effect of orexin-A was reversed by the administration of SB334867 as well as by hypothalamic BDNF knockdown.", "entity1": "orexin-A", "entity2": "SB334867", "span1": [159, 167], "span2": [206, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4507": {"label": 3, "data": {"text": "Conclusion: Drug-drug interaction studies may be warranted for drugs that metabolize to acyl glucuronides due to the potential inhibition of hCESs.", "entity1": "hCESs", "entity2": "acyl glucuronides", "span1": [141, 146], "span2": [88, 105]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12302": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Fasn", "entity2": "Quercetin", "span1": [179, 183], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14091": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "DDB1", "entity2": "pomalidomide", "span1": [177, 181], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9326": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "dihydrokainate", "span1": [72, 77], "span2": [196, 210]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1296": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "EC 4.1.1.15", "entity2": "glutamate", "span1": [55, 66], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"11812": {"label": 2, "data": {"text": "Moreover, activities of caspase-3 and caspase-9 enzymes were also significantly higher in both kinds of cells exposed to SiO(2) NPs.", "entity1": "caspase-9", "entity2": "SiO(2)", "span1": [38, 47], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1496": {"label": 3, "data": {"text": "Similarly, pretreatment with sulindac sulfide blocks the ability of EGF to induce ERK1/2 and Bad phosphorylation, but also down-regulates total Bad but not ERK1/2 protein levels.", "entity1": "Bad", "entity2": "sulindac sulfide", "span1": [93, 96], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10270": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "OCT", "entity2": "MPP+", "span1": [123, 126], "span2": [55, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"8353": {"label": 3, "data": {"text": "This is distinct from Rock inhibitors based on non-amino acid derived quinazolinones, where high selectivity against PKA could be obtained.", "entity1": "Rock", "entity2": "quinazolinones", "span1": [22, 26], "span2": [70, 84]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2688": {"label": 3, "data": {"text": "Gene expression profiling (GEP) of GIST-S, GIST-R cells and two IM resistant GIST patients demonstrated that KIT is downregulated implying a major role in IM resistance.", "entity1": "KIT", "entity2": "IM", "span1": [109, 112], "span2": [155, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5153": {"label": 2, "data": {"text": "Taken together, our study for the first time suggests that 2-hydroxy-3-methylanthraquinone is able to enhance apoptosis of U937 cells, at least in part, through activation of p-p38MAPK and downregulation of p-ERK1/2.", "entity1": "p-p38MAPK", "entity2": "2-hydroxy-3-methylanthraquinone", "span1": [175, 184], "span2": [59, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"617": {"label": 3, "data": {"text": "Likewise, IL-2 steady-state mRNA expression was inhibited by both PLA2 inhibitors in a concentration-dependent fashion with > 90% inhibition at 1 microM BPB and 20 microM AACOCF3.", "entity1": "IL-2", "entity2": "BPB", "span1": [10, 14], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13317": {"label": 5, "data": {"text": "Exposure to mifepristone (a glucocorticoid receptor antagonist), but not spironolactone (a mineralocorticoid receptor antagonist), precluded both the corticosteroid-induced elevation in amiloride-sensitive I(sc) and the induced changes in beta- and gamma-ENaC mRNA.", "entity1": "glucocorticoid receptor", "entity2": "mifepristone", "span1": [28, 51], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5030": {"label": 5, "data": {"text": "Synthesis and in Vitro Characterisation of Ifenprodil-Based Fluorescein Conjugates as GluN1/GluN2B N-Methyl-D-aspartate Receptor Antagonists.", "entity1": "GluN2B", "entity2": "Ifenprodil", "span1": [92, 98], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7394": {"label": 8, "data": {"text": "Finally, we demonstrate that T. thermophilus PRODH reacts with O(2) producing superoxide.", "entity1": "T. thermophilus PRODH", "entity2": "O(2)", "span1": [29, 50], "span2": [63, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"661": {"label": 3, "data": {"text": "The effects of meloxicam were compared with those of diclofenac, a nonselective COX inhibitor.", "entity1": "COX", "entity2": "meloxicam", "span1": [80, 83], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7638": {"label": 3, "data": {"text": "We found compounds that inhibited Panx1 currents with a rank order of potency: carbenoxolone > disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate (DIDS) approximately disodium 4-acetamido-4'-isothiocyanato-stilben-2,2'-disulfonate approximately 5-nitro-2-(3-phenylpropylamino)benzoic acid > indanyloxyacetic acid 94 >> probenecid >> flufenamic acid = niflumic acid.", "entity1": "Panx1", "entity2": "disodium 4,4'-diisothiocyanatostilbene-2,2'-disulfonate", "span1": [34, 39], "span2": [95, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3060": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "SDF-1", "entity2": "bicyclam", "span1": [142, 147], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13117": {"label": 9, "data": {"text": "We failed to observe any significant activation of FAS promoter following exposure to the anti-metabolite 5-fluorouracil, the alkylating drug cisplatin, or the microtubule interfering-agents paclitaxel and vincristine.", "entity1": "FAS promoter", "entity2": "vincristine", "span1": [51, 63], "span2": [206, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1518": {"label": 9, "data": {"text": "), an analogue of okadaic acid lacking activity against protein phosphatases, did not affect the antinociceptive effect of morphine.", "entity1": "protein phosphatases", "entity2": "okadaic acid", "span1": [56, 76], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2743": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "kinase", "entity2": "BMS-354825", "span1": [109, 115], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3503": {"label": 2, "data": {"text": "The lysosomal inhibitor chloroquine significantly increased RCAN1 accumulation in +/+ cells, consistent with the hypothesis that higher lysosomal pH impairs RCAN1 degradation, leading to a higher RCAN1/NFATc1 ratio and consequently NFATc1 inhibition.", "entity1": "RCAN1", "entity2": "chloroquine", "span1": [60, 65], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"599": {"label": 3, "data": {"text": "Cyclopentenone prostaglandins suppress activation of microglia: down-regulation of inducible nitric-oxide synthase by 15-deoxy-Delta12,14-prostaglandin J2.", "entity1": "inducible nitric-oxide synthase", "entity2": "15-deoxy-Delta12,14-prostaglandin J2", "span1": [83, 114], "span2": [118, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5211": {"label": 1, "data": {"text": "In the present study, the exposure of melanoma cells to vinblastine was found to trigger apoptosis as evidenced by the loss of mitochondrial membrane potential, the release of both cytochrome c and apoptosis inducing factor, activation of caspase-9 and 3, and cleavage of Poly (ADP-ribose)-Polymerase.", "entity1": "apoptosis inducing factor", "entity2": "vinblastine", "span1": [198, 223], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"691": {"label": 1, "data": {"text": "Combined concentration-ratio analysis demonstrated that tamsulosin, which does not discriminate between alpha 1A- and alpha 1L-adrenoceptors, and RS-17053 competed for binding at the same site in the SMA.", "entity1": "alpha 1A", "entity2": "RS-17053", "span1": [104, 112], "span2": [146, 154]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5290": {"label": 3, "data": {"text": "Vandetanib (Caprelsa(\u00ae), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60\u00a0% of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors.", "entity1": "growth-factor receptor tyrosine kinase", "entity2": "Vandetanib", "span1": [134, 172], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2671": {"label": 3, "data": {"text": "However, a lower concentration of dipyridamole (3 microM) that blocks PDE9, PDE10, and PDE11, but not PDE8, did not inhibit ecto-phosphodiesterase activity.", "entity1": "PDE9", "entity2": "dipyridamole", "span1": [70, 74], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8293": {"label": 2, "data": {"text": "LY294002, a specific PI3K/AKT inhibitor, selectively activated the p38 MAPK kinase pathway and enhanced c-Jun phosphorylation, but did not activate JNK.", "entity1": "MAPK", "entity2": "LY294002", "span1": [71, 75], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14914": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "steroids", "span1": [266, 269], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8912": {"label": 5, "data": {"text": "Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene.", "entity1": "histamine H1-receptor", "entity2": "chlorpheniramine", "span1": [13, 34], "span2": [86, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9470": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "IP", "entity2": "iloprost", "span1": [210, 212], "span2": [179, 187]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15886": {"label": 3, "data": {"text": "The Bcl2/Bax ratio increased and Mfn2 expression decreased in MIN6 cells after glucose stimulation.", "entity1": "Mfn2", "entity2": "glucose", "span1": [33, 37], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16057": {"label": 3, "data": {"text": "Simvastatin and lovastatin metabolized through CYP3A have the highest potency for drug-drug interaction with potent CYP3A inhibitors such as ritonavir- or cobicistat-boosted HIV-PI or the hepatitis C virus (HCV) PI, telaprevir or boceprevir, and therefore their coadministration is contraindicated.", "entity1": "CYP3A", "entity2": "telaprevir", "span1": [116, 121], "span2": [216, 226]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1199": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "aminopeptidase B", "entity2": "4-methoxy-2-naphthylamide", "span1": [369, 385], "span2": [325, 350]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2177": {"label": 1, "data": {"text": "MELANOTAN (NDP-MSH) binds the MC1 receptor to significantly increase the eumelanin content of human skin cells.", "entity1": "MC1 receptor", "entity2": "NDP-MSH", "span1": [30, 42], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14816": {"label": 4, "data": {"text": "Cannabinoid receptor 1 (CB(1)) inverse agonists (e.g., rimonabant) have been reported to produce adverse effects including nausea, emesis, and anhedonia that limit their clinical applications.", "entity1": "Cannabinoid receptor 1", "entity2": "rimonabant", "span1": [0, 22], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10681": {"label": 3, "data": {"text": "In Experiment 1, Antag I, Antag II and TT-235 inhibited the integrated uterine response to oxytocin at 5 minutes by 76%, 77% and 80%, respectively, compared to controls (p<0.05).", "entity1": "oxytocin", "entity2": "TT-235", "span1": [91, 99], "span2": [39, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12841": {"label": 8, "data": {"text": "When expressed heterologously in a mammalian cell line, rabbit PAT1 mediates pH-dependent, Na(+)-independent uptake of proline, glycine, l-alanine and alpha-(methylamino)isobutyric acid.", "entity1": "rabbit PAT1", "entity2": "alpha-(methylamino)isobutyric acid", "span1": [56, 67], "span2": [151, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6277": {"label": 3, "data": {"text": "The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro.", "entity1": "angiotensin II type 1 receptor", "entity2": "EXP", "span1": [49, 79], "span2": [169, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4826": {"label": 1, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "GSK3", "entity2": "7KC", "span1": [202, 206], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13451": {"label": 2, "data": {"text": "Finally, PLA2 inhibitor methyl arachidonyl fluorophosphonate blocked the PUFA effects on COX-2 induction, promoter activity and arachidonic acid mobilization suggesting involvement of AA metabolites in PPAR activation.", "entity1": "PPAR", "entity2": "AA", "span1": [202, 206], "span2": [184, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8560": {"label": 3, "data": {"text": "LB-4b is the first synthetic APN inhibitor to be evaluated for both of its anti-invasion and anti-angiogenesis effects.", "entity1": "APN", "entity2": "LB-4b", "span1": [29, 32], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8518": {"label": 3, "data": {"text": "Synthesis of a DOTA (Gd(3+))-conjugate of proton-pump inhibitor pantoprazole for gastric wall imaging studies.", "entity1": "proton-pump", "entity2": "pantoprazole", "span1": [42, 53], "span2": [64, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3328": {"label": 3, "data": {"text": "In conclusion, the results suggest that the enhancement in the reduction of topo II activity by the combined MXF/VP-16 treatments was probably due to the increase in the level of the DNA-enzyme cleavable complexes formed by both drugs.", "entity1": "topo II", "entity2": "VP-16", "span1": [76, 83], "span2": [113, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"421": {"label": 1, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "Rec 15/2739", "span1": [258, 286], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9919": {"label": 1, "data": {"text": "Blood samples were taken from both alcohol-dependent and control subjects to determine 5-HTTLPR genotypes using PCR of lymphocyte DNA, and to perform platelet [3H]paroxetine binding (binding capacity: B(max); and dissociation constant: K(D)).", "entity1": "5-HTTLPR", "entity2": "[3H]paroxetine", "span1": [87, 95], "span2": [159, 173]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5683": {"label": 3, "data": {"text": "HZ mice are also more sensitive to the peripheral application of the selective AChE inhibitor donepezil or the mixed inhibitor physostigmine; extracellular ACh levels rise significantly after administration of both drugs; also glucose levels are moderately increased indicating potentially non-cholinergic effects of donepezil.", "entity1": "AChE", "entity2": "physostigmine", "span1": [79, 83], "span2": [127, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3038": {"label": 5, "data": {"text": "EP(1) and EP(3) receptor antagonists ONO-8713 and ONO-AE3-240, but not the EP(4) antagonists ONO-AE3-208 and AH 23848, inhibited tumor cell proliferation, indicating the significance of EP(1) and EP(3) but not EP(4) for MB growth.", "entity1": "EP(3) receptor", "entity2": "ONO-8713", "span1": [10, 24], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10915": {"label": 2, "data": {"text": "Both inhibitors, moreover, blunted the mucin secretory responses to beta-adrenergic agonist-generated second messenger, cAMP as well as adenylate cyclase activator, forskolin.", "entity1": "adenylate cyclase", "entity2": "forskolin", "span1": [136, 153], "span2": [165, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7652": {"label": 2, "data": {"text": "These findings indicate that captopril attenuates the development of monocrotaline-induced right ventricular hypertrophy in association with inhibition of MMP-2 and MMP-9 in rats.", "entity1": "MMP-2", "entity2": "monocrotaline", "span1": [155, 160], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6716": {"label": 9, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "Flt3", "entity2": "Imatinib", "span1": [52, 56], "span2": [116, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7066": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARalpha", "entity2": "retinoid", "span1": [38, 46], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2577": {"label": 2, "data": {"text": "Histamine content, HDC activity and HDC mRNA expression in nasal mucosa were also significantly increased after TDI provocation.", "entity1": "HDC", "entity2": "TDI", "span1": [36, 39], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12149": {"label": 0, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "Lys", "span1": [150, 156], "span2": [50, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4410": {"label": 6, "data": {"text": "However, one mGlu5 PAM, CPPHA (N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide), interacts with a separate allosteric site on mGlu5.", "entity1": "mGlu5", "entity2": "N-(4-chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl)-2-hydroxybenzamide", "span1": [13, 18], "span2": [31, 119]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"6164": {"label": 3, "data": {"text": "A case of therapy-related acute myeloblastic leukemia with t(16;21)(q24;q22) after chemotherapy with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and the alkylating agent, cyclophosphamide.", "entity1": "DNA-topoisomerase II", "entity2": "etoposide", "span1": [101, 121], "span2": [134, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10650": {"label": 3, "data": {"text": "We report here the pharmacological properties of a third selective COX-2 inhibitor, valdecoxib, which is the most potent and in vitro selective of the marketed COX-2 inhibitors that we have studied.", "entity1": "COX-2", "entity2": "valdecoxib", "span1": [67, 72], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10941": {"label": 3, "data": {"text": "Therefore, decreases of PLK and PNPO in the hippocampal CA1 region of aged brains may be involved in aging processes related with gamma-aminobutyric acid (GABA) function.", "entity1": "PNPO", "entity2": "GABA", "span1": [32, 36], "span2": [155, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3312": {"label": 1, "data": {"text": "The main findings from this study were as follows: 1) cTnC mutants demonstrated distinct functional phenotypes reminiscent of bona fide HCM, RCM, and DCM mutations; 2) a region in cTnC associated with increased Ca(2+) sensitivity in skinned fibers was identified; and 3) the F27W reporter mutation affected Ca(2+) sensitivity, maximal force, and ATPase activation of some mutants.", "entity1": "cTnC", "entity2": "Ca(2+)", "span1": [54, 58], "span2": [307, 313]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8083": {"label": 0, "data": {"text": "E235 also activated DNA damage response signaling, resulting in increased levels of Ser15-phosphorylated p53, \u03b3-H2AX, and phosphorylated checkpoint kinase 2 (Chk2), although E235 does not appear to cause physical DNA damage.", "entity1": "phosphorylated p53", "entity2": "Ser", "span1": [90, 108], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10745": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "fluoropyrimidine", "span1": [260, 280], "span2": [57, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2923": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "NCX", "entity2": "bepridil", "span1": [129, 132], "span2": [64, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4849": {"label": 3, "data": {"text": "Interestingly, disruption of the RhoA-ROCK pathway prevented the inhibitory effect of cucurbitacin I on Rac1 activation by heregulin.", "entity1": "Rac1", "entity2": "cucurbitacin I", "span1": [104, 108], "span2": [86, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13814": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "OSI-774", "span1": [233, 246], "span2": [169, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4956": {"label": 3, "data": {"text": "Fisetin treatment of preadipocytes reduced the phosphorylation of S6K1 and mTORC1 in a time- and concentration-dependent manner.", "entity1": "mTORC1", "entity2": "Fisetin", "span1": [75, 81], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14954": {"label": 1, "data": {"text": "Cooperative effects for CYP2E1 differ between styrene and its metabolites.", "entity1": "CYP2E1", "entity2": "styrene", "span1": [24, 30], "span2": [46, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12285": {"label": 1, "data": {"text": "(E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methy l benzenamine ((18)F-AV-45) is such as an agent currently in phase III clinical studies for PET of Abeta plaques in the brain.", "entity1": "Abeta", "entity2": "(E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methy l benzenamine", "span1": [181, 186], "span2": [0, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2858": {"label": 9, "data": {"text": "As expected, the hGSTA4 cells showed resistance to 4-HNE stimulated lipid peroxidation at all 4-HNE doses.", "entity1": "hGSTA4", "entity2": "4-HNE", "span1": [17, 23], "span2": [94, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8816": {"label": 3, "data": {"text": "Further, AICAR pretreatment blocked PAR-1-induced increase in permeability of mouse-lung microvessels.", "entity1": "PAR-1", "entity2": "AICAR", "span1": [36, 41], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3552": {"label": 2, "data": {"text": "The results demonstrated that intracerebral infusions of LTD4 (1 ng/mouse) produced memory impairment as determined by Morris water maze test and Y-maze test in mice, and caused the accumulation of A\u03b21-40 and A\u03b21-42 in the hippocampus and cortex through increased activity of \u03b2- and \u03b3-secretases accompanied with increased expression of amyloid precursor protein (APP).", "entity1": "APP", "entity2": "LTD4", "span1": [364, 367], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14703": {"label": 3, "data": {"text": "Further study showed that icariin dose-dependently inhibited the proliferation and activation of T lymphocytes, and suppressed pro-inflammatory cytokine levels of activated T cells.", "entity1": "cytokine", "entity2": "icariin", "span1": [144, 152], "span2": [26, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5037": {"label": 3, "data": {"text": "Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitrooxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.", "entity1": "cyclooxygenase-2", "entity2": "nitric oxide", "span1": [106, 122], "span2": [134, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12519": {"label": 1, "data": {"text": "The uncharged estramustine bound to both tubulin and MAPs, but no effects were seen on microtubule assembly, the composition of coassembled MAPs or the microtubule morphology.", "entity1": "MAPs", "entity2": "estramustine", "span1": [53, 57], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10662": {"label": 2, "data": {"text": "Of note, we demonstrated for the first time that telmisartan augmented GLUT4 protein expression and 2-deoxy glucose uptake both in basal and insulin-stimulated state of adipocytes, which may contribute, at least partly, to its insulin-sensitizing ability.", "entity1": "GLUT4", "entity2": "telmisartan", "span1": [71, 76], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12747": {"label": 9, "data": {"text": "(-)-[(3)H]-CGP12177 dissociated from the beta(1)-adrenoceptors with a fast component (k(off)=0.45 min(-1)), consistent with the L-site, and a slow component (k(off)=0.017-0.033 min(-1)), consistent with the H-site.", "entity1": "beta(1)-adrenoceptors", "entity2": "(-)-[(3)H]-CGP12177", "span1": [41, 62], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4682": {"label": 1, "data": {"text": "For this purpose, C57BL6 mice were injected intraperitoneally with V(5+) (5\u00a0mg/kg) in the absence and presence of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) (15\u00a0\u03bcg/kg) for 6 and 24\u00a0h. Furthermore, isolated hepatocytes from C57BL6 mice were treated with V(5+) (5, 10, and 20\u00a0\u03bcM) in the absence and presence of TCDD (1 nM) for 3, 6, 12, and 24\u00a0h. In vivo, V(5+) alone did not significantly alter Cyp1a1, Cyp1a2, or Cyp1b1 mRNA, protein, or catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "V(5+)", "span1": [402, 408], "span2": [354, 359]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15258": {"label": 1, "data": {"text": "Oxidation with hydrogen peroxide was similarly assessed, and adhesion of lysozyme and fibrinogen from phosphate buffered saline was then assayed by QCM and imaged by AFM.", "entity1": "lysozyme", "entity2": "hydrogen peroxide", "span1": [73, 81], "span2": [15, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5054": {"label": 3, "data": {"text": "A decrease in ADA activity was observed when the slices were exposed to organoselenium at the concentrations of 1, 10 and 30 \u00b5M.", "entity1": "ADA", "entity2": "organoselenium", "span1": [14, 17], "span2": [72, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1497": {"label": 3, "data": {"text": "The ability of sulindac to block ERK1/2 signaling by the EGF receptor may account for at least part of its potent growth-inhibitory effects against cancer cells.", "entity1": "EGF receptor", "entity2": "sulindac", "span1": [57, 69], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13584": {"label": 1, "data": {"text": "Initial evaluation of the pharmacological properties of DVS (J Pharmacol Exp Ther 318:657-665, 2006) revealed significantly reduced potency for the hNET expressed in membranes compared with whole cells when competing for [(3)H]nisoxetine (NIS) binding.", "entity1": "hNET", "entity2": "[(3)H]nisoxetine", "span1": [148, 152], "span2": [221, 237]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4289": {"label": 1, "data": {"text": "Flavonoids such as green tea catechins and quercetin glycosides have been shown to modulate the function of some OATPs.", "entity1": "OATPs", "entity2": "quercetin glycosides", "span1": [113, 118], "span2": [43, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7623": {"label": 3, "data": {"text": "BACKGROUND: Lapatinib, the first dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases, was approved by the US Food and Drug Administration (FDA) in 2007.", "entity1": "human epidermal growth factor receptor 2", "entity2": "Lapatinib", "span1": [95, 135], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6226": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-ht1f", "entity2": "rizatriptan", "span1": [135, 141], "span2": [60, 71]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5075": {"label": 2, "data": {"text": "Here, we have now found that activation of p38 MAPK by anisomycin potentiated induction of CYP2B6 mRNA by CAR ligand in HepG2 cells to levels observed in ligand-treated human primary hepatocytes.", "entity1": "MAPK", "entity2": "anisomycin", "span1": [47, 51], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11830": {"label": 3, "data": {"text": "To explore the molecular basis for CPT hypersensitivity in Top2\u03b2-deficient cells, we found that upon CPT exposure, the RNA polymerase II large subunit (RNAP LS) became progressively depleted, followed by recovery to nearly the original level in wild-type MEFs, whereas RNAP LS remained depleted without recovery in Top2\u03b2-deficient cells.", "entity1": "RNAP LS", "entity2": "CPT", "span1": [269, 276], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15123": {"label": 2, "data": {"text": "Notably, the antioxidant Trolox\u2122 reversed the Mn (20\u00a0mg/kg)-dependent augmentation in p38(MAPK) phosphorylation and reduced the Mn (20\u00a0mg/kg)-induced caspase activity and F(2)-isoprostane production.", "entity1": "caspase", "entity2": "Mn", "span1": [150, 157], "span2": [128, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"4837": {"label": 9, "data": {"text": "However, Rac1 activation was not affected by Jak2 or Stat3 RNA interference, suggesting that the effect of cucurbitacin I occurs through a Jak2-independent mechanism.", "entity1": "Jak2", "entity2": "cucurbitacin I", "span1": [139, 143], "span2": [107, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7905": {"label": 3, "data": {"text": "Systemic injection to mice of siRNA lipoplexes, rather than of cationic liposome, triggered a production of several cytokines in mice and replacement of plasmid by polyglutamate reduced the elevation of all assayed cytokines.", "entity1": "cytokines", "entity2": "polyglutamate", "span1": [215, 224], "span2": [164, 177]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7820": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor", "entity2": "LY293558", "span1": [190, 258], "span2": [360, 368]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3850": {"label": 7, "data": {"text": "Using the viral mimic polyinosinic:polycytidylic acid and the IFN\u03b1/\u03b2 antagonist B18R we furthermore demonstrate the capability of endogenous IFN to promote IL-22-induced STAT1 activation and expression of CXCL10.", "entity1": "IFN\u03b1/\u03b2", "entity2": "polyinosinic:polycytidylic acid", "span1": [62, 68], "span2": [22, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2309": {"label": 2, "data": {"text": "Sulindac metabolites simultaneously (a) increase cellular cyclic GMP and subsequently activate cyclic GMP-dependent protein kinase (PKG); (b) activate c-jun NH2-terminal kinase (JNK); (c) inhibit extracellular signal-regulated kinase 1/2 (ERK1/2); and (d) decrease beta-catenin protein expression at times and doses consistent with apoptosis.", "entity1": "cyclic GMP-dependent protein kinase", "entity2": "Sulindac", "span1": [95, 130], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10443": {"label": 7, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "(L-serine dehydratase", "entity2": "pyridoxal 5'-phosphate", "span1": [4, 25], "span2": [54, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4978": {"label": 2, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "caspase 3", "entity2": "vitamin E", "span1": [181, 190], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1117": {"label": 3, "data": {"text": "Acetazolamide, a specific inhibitor of CA, reduces the activity of CA I and CA II from red cells.", "entity1": "CA", "entity2": "Acetazolamide", "span1": [39, 41], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1326": {"label": 3, "data": {"text": "To eliminate the interaction of bupropion with DAT or NET, nomifensine or desipramine, respectively, was included in the superfusion buffer.", "entity1": "NET", "entity2": "bupropion", "span1": [54, 57], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10598": {"label": 1, "data": {"text": "Apart from the consequences of iron deprivation, gallium exerts cytotoxic effects by direct interaction with the iron-dependent enzyme ribonucleotide reductase, resulting in reduced dNTP pools and inhibition of DNA synthesis.", "entity1": "ribonucleotide reductase", "entity2": "iron", "span1": [135, 159], "span2": [113, 117]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14924": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "estrogen receptor-\u03b1", "entity2": "3\u03b2-hydroxyl", "span1": [236, 255], "span2": [144, 155]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3501": {"label": 2, "data": {"text": "For AII and ET1, MAP was also increased for the fenofibrate group but not in a dose-dependent fashion.", "entity1": "AII", "entity2": "fenofibrate", "span1": [4, 7], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"546": {"label": 1, "data": {"text": "The selective 5-HT reuptake inhibitors paroxetine, indalpine and fluvoxamine displayed a high affinity for the 5-HT transporter, whereas the norepinephrine reuptake inhibitor desipramine had a high affinity for the norepinephrine transporter.", "entity1": "5-HT transporter", "entity2": "indalpine", "span1": [111, 127], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9468": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "DP", "entity2": "BW868C", "span1": [164, 166], "span2": [153, 159]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7310": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT1", "entity2": "alanine", "span1": [224, 229], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2381": {"label": 3, "data": {"text": "Further characterization of sorafenib revealed that this molecule was a multikinase inhibitor that targeted the vascular endothelial growth factor receptor family (VEGFR-2 and VEGFR-3) and platelet-derived growth factor receptor family (PDGFR-beta and Kit), which play key roles in tumor progression and angiogenesis.", "entity1": "PDGFR-beta", "entity2": "sorafenib", "span1": [237, 247], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9734": {"label": 1, "data": {"text": "Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors.", "entity1": "hD(2) receptors", "entity2": "Yohimbine", "span1": [153, 168], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9365": {"label": 3, "data": {"text": "The present results suggest that the action of DMI in this animal model is unlikely to be directly related to a reduction in beta-adrenoceptors but may be related to a reduction in frontal cortical 5-HT2A receptors.", "entity1": "5-HT2A", "entity2": "DMI", "span1": [198, 204], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4186": {"label": 0, "data": {"text": "Furthermore, PTE treatment directly inhibited the phosphorylation of JAK2 at Tyr 1007 and the downstream activation of STAT3.", "entity1": "JAK2", "entity2": "Tyr", "span1": [69, 73], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4642": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [0, 6], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5891": {"label": 3, "data": {"text": "Mouse ornithine decarboxylase (ODC) was expressed in Escherichia coli and the purified recombinant enzyme used for determination of the binding site for pyridoxal 5'-phosphate and of the residues modified in the inactivation of the enzyme by the enzyme-activated irreversible inhibitor, alpha-difluoromethylornithine (DFMO).", "entity1": "Mouse ornithine decarboxylase", "entity2": "alpha-difluoromethylornithine", "span1": [0, 29], "span2": [287, 316]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11193": {"label": 8, "data": {"text": "The enzyme dimethylarginine dimethylaminohydrolase (DDAH) specifically hydrolyzes these asymmetrically methylated arginine residues to citrulline and methylamines.", "entity1": "dimethylarginine dimethylaminohydrolase", "entity2": "arginine", "span1": [11, 50], "span2": [114, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6990": {"label": 3, "data": {"text": "Valproic acid selectively inhibits conversion of arachidonic acid to arachidonoyl-CoA by brain microsomal long-chain fatty acyl-CoA synthetases: relevance to bipolar disorder.", "entity1": "brain microsomal long-chain fatty acyl-CoA synthetases", "entity2": "Valproic acid", "span1": [89, 143], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7102": {"label": 8, "data": {"text": "Proline oxidase (POX), a mitochondrial inner-membrane protein, catalyzes the rate-limiting oxidation of proline to pyrroline- 5-carboxylate (P5C).", "entity1": "Proline oxidase", "entity2": "proline", "span1": [0, 15], "span2": [104, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12412": {"label": 8, "data": {"text": "This methodology was subsequently used to assess the relative contribution of OATP1B1 uptake in human hepatocytes for olmesartan (42%-62%), valsartan (28%-81%), rosuvastatin (64%-72%), pitavastatin (84%-98%) and lopinavir (64%-89%).", "entity1": "OATP1B1", "entity2": "pitavastatin", "span1": [78, 85], "span2": [185, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15578": {"label": 1, "data": {"text": "The radioactivity was rapidly and widely distributed throughout the body, and remained detectable in all tissues investigated at later time points (24 and 48 hours for [(3)H]-MRP4 and [(3)H]-SSB siRNA, respectively).", "entity1": "MRP4", "entity2": "(3)H", "span1": [175, 179], "span2": [169, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13090": {"label": 1, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "PPARgamma", "entity2": "thiazolidinediones", "span1": [219, 228], "span2": [260, 278]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1834": {"label": 3, "data": {"text": "Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide.", "entity1": "SR-BI", "entity2": "glyburide", "span1": [20, 25], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7884": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "BSEP", "entity2": "RTV", "span1": [84, 88], "span2": [66, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5306": {"label": 3, "data": {"text": "In addition, prunetin inhibits NF-\u03baB-dependent inflammatory responses by modulating I\u03baB kinase (IKK)-inhibitor \u03baB\u03b1 (I\u03baB\u03b1)-NF-\u03baB signaling.", "entity1": "NF-\u03baB", "entity2": "prunetin", "span1": [31, 36], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9017": {"label": 4, "data": {"text": "The limitation of SRF by diazepam was not prevented by inverse or partial agonists at the BDZ receptor, including Ro 15-1788 and the beta CCs.", "entity1": "BDZ receptor", "entity2": "Ro 15-1788", "span1": [90, 102], "span2": [114, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2720": {"label": 3, "data": {"text": "Indomethacin treatment led to an increase in lipid peroxidation, glutathione peroxidase and glucose-6-phosphate dehydrogenase activities and to a decrease in catalase activity and glutathione levels in gastric mucosa.", "entity1": "catalase", "entity2": "Indomethacin", "span1": [158, 166], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3216": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "gallic acid", "span1": [282, 284], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12715": {"label": 3, "data": {"text": "However, when coapplied with 10 micro m GABA, ivermectin potentiated the GABA-evoked current of the GAB-1/HG1A receptor, but attenuated the GABA response of the GAB-1/HG1E receptor.", "entity1": "HG1E", "entity2": "ivermectin", "span1": [167, 171], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10886": {"label": 1, "data": {"text": "To understand this interaction, we determined the crystal structure of PDXK in complex with (R)-roscovitine, N6-methyl-(R)-roscovitine, and O6-(R)-roscovitine, the two latter derivatives being designed to bind to PDXK but not to CDKs.", "entity1": "PDXK", "entity2": "(R)-roscovitine", "span1": [71, 75], "span2": [92, 107]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9955": {"label": 9, "data": {"text": "For instance, meloxicam inhibits the growth of cultured colon cancer cells (HCA-7 and Moser-S) that express COX-2 but has no effect on HCT-116 tumor cells that do not express COX-2.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [175, 180], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14872": {"label": 1, "data": {"text": "One of these compounds is eicosanoyl-5-hydroxytryptamide (EHT), which ameliorates the phenotype of \u03b1-synuclein transgenic mice associated with decreased protein aggregation and phosphorylation, improved neuronal integrity and reduced neuroinflammation.", "entity1": "\u03b1-synuclein", "entity2": "eicosanoyl-5-hydroxytryptamide", "span1": [99, 110], "span2": [26, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10691": {"label": 3, "data": {"text": "Lumiracoxib inhibited purified COX-1 and COX-2 with K(i) values of 3 and 0.06 microM, respectively.", "entity1": "COX-2", "entity2": "Lumiracoxib", "span1": [41, 46], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9595": {"label": 3, "data": {"text": "The aromatic amino acid hydroxylases represent a superfamily of structurally and functionally closely related enzymes, one of those functions being reversible inhibition by catechol derivatives.", "entity1": "aromatic amino acid hydroxylases", "entity2": "catechol", "span1": [4, 36], "span2": [173, 181]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10501": {"label": 1, "data": {"text": "Responses to isoproterenol could be restored to normal by beta2AR blockade, suggesting a beta2AR-mediated inhibition of beta1AR signalling.", "entity1": "beta2AR", "entity2": "isoproterenol", "span1": [89, 96], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1969": {"label": 9, "data": {"text": "In contrast, NTG or ISDN does not affect HIF-1 activity.", "entity1": "HIF-1", "entity2": "NTG", "span1": [41, 46], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4502": {"label": 9, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES2", "entity2": "Diclofenac-\u03b2-d-glucuronide", "span1": [300, 305], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14671": {"label": 3, "data": {"text": "Furthermore, thrombin diminished cAMP production in ECs, which were prevented by treatment with genistein.", "entity1": "thrombin", "entity2": "genistein", "span1": [13, 21], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1818": {"label": 8, "data": {"text": "The IC50-values obtained for the inhibition of lipopolysaccharide (LPS)-induced release of prostaglandin E2 (PGE2) reflecting cyclooxygenase (COX)-2-mediated PGE2 release were 47 microg/ml and 0.6 microg/ml, for the Salix extract 1520L and rofecoxib-like research compound L745337, respectively.", "entity1": "cyclooxygenase (COX)-2", "entity2": "PGE2", "span1": [126, 148], "span2": [158, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12998": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "Erg2p", "entity2": "amorolfine", "span1": [166, 171], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11114": {"label": 1, "data": {"text": "Finally, a third nonadrenergic internal membrane site, labeled by [3H]IDX, was consistent with a subtype-I2 imidazol(in)e receptor site (rank order: cirazoline > IDX >> amiloride > moxonidine > clonidine).", "entity1": "subtype-I2 imidazol(in)e receptor", "entity2": "moxonidine", "span1": [97, 130], "span2": [181, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10073": {"label": 1, "data": {"text": "Aspirin and salicylate bind to immunoglobulin heavy chain binding protein (BiP) and inhibit its ATPase activity in human fibroblasts.", "entity1": "immunoglobulin heavy chain binding protein", "entity2": "salicylate", "span1": [31, 73], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13193": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "DAT", "entity2": "mZIENT", "span1": [278, 281], "span2": [67, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2867": {"label": 8, "data": {"text": "Specifically, hGSTA4 cells had significantly higher GSH concentrations when exposed to 5-15 microM 4-HNE, but not at 20 microM 4-HNE, suggesting extensive GSH utilization at high concentrations of 4-HNE.", "entity1": "hGSTA4", "entity2": "4-HNE", "span1": [14, 20], "span2": [127, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12880": {"label": 3, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "phosphatidylserine-O-methyl ester", "span1": [14, 20], "span2": [61, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"15257": {"label": 1, "data": {"text": "Selective oxidation of \u03c9-tertiary amine self-assembled thiol monolayers to tertiary amine N-oxides is shown to transform the adhesion of model proteins lysozyme and fibrinogen upon them.", "entity1": "fibrinogen", "entity2": "thiol", "span1": [165, 175], "span2": [55, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10143": {"label": 8, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "cyclooxygenase", "entity2": "prostaglandins", "span1": [77, 91], "span2": [140, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8536": {"label": 3, "data": {"text": "A catheterized rat model was used to define the intestinal and hepatic components of oral bioavailability for an 11\u03b2-HSD1 inhibitor, AMG 221.", "entity1": "11\u03b2-HSD1", "entity2": "AMG 221", "span1": [113, 121], "span2": [133, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7562": {"label": 1, "data": {"text": "It is more potent and selective than citalopram in inhibiting serotonin re-uptake in the CNS, and less potent than various other selective serotonin re-uptake inhibitors in relation to other transporter proteins and receptors: in particular, it is six times less potent than citalopram in binding to the histamine H1 and muscarinic receptors.", "entity1": "muscarinic receptors", "entity2": "citalopram", "span1": [321, 341], "span2": [275, 285]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11015": {"label": 2, "data": {"text": "Given the treatment with three doses of Captopril (15 approximately 45 mg/kg) markedly attenuated inhibition of vasodilator responses to ACh, and eliminated the increased level of malondialdehyde, the decreased level of NO, activity of PON1 and SOD in serum by single intragastric gavaged L-methionine.", "entity1": "PON1", "entity2": "Captopril", "span1": [236, 240], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2969": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "F786A", "entity2": "vardenafil", "span1": [88, 93], "span2": [29, 39]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"579": {"label": 2, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cdk2", "entity2": "Tomudex", "span1": [138, 142], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9928": {"label": 1, "data": {"text": "Arachidonic acid and nonsteroidal anti-inflammatory drugs induce conformational changes in the human prostaglandin endoperoxide H2 synthase-2 (cyclooxygenase-2).", "entity1": "cyclooxygenase-2", "entity2": "Arachidonic acid", "span1": [143, 159], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16055": {"label": 3, "data": {"text": "Simvastatin and lovastatin metabolized through CYP3A have the highest potency for drug-drug interaction with potent CYP3A inhibitors such as ritonavir- or cobicistat-boosted HIV-PI or the hepatitis C virus (HCV) PI, telaprevir or boceprevir, and therefore their coadministration is contraindicated.", "entity1": "CYP3A", "entity2": "ritonavir", "span1": [116, 121], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7897": {"label": 9, "data": {"text": "TCDD had no effect on AR activity in PC-3 cells, whereas the shortest AR variant was induced by TCDD in PNT1A cells.", "entity1": "AR", "entity2": "TCDD", "span1": [22, 24], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9614": {"label": 1, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "NBF1", "entity2": "8-azido-ATP", "span1": [200, 204], "span2": [177, 188]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8364": {"label": 1, "data": {"text": "About 99% of a dose of diflunisal is unavailable for reaction with the target enzyme, because diflunisal strongly binds to human serum albumin (HSA).", "entity1": "human serum albumin", "entity2": "diflunisal", "span1": [123, 142], "span2": [94, 104]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4018": {"label": 3, "data": {"text": "This study explored whether curcumin improves colonic inflammation in a rat colitis model through inhibition of the TLR4/NF-\u03baB signaling pathway and IL-27 expression.", "entity1": "NF-\u03baB", "entity2": "curcumin", "span1": [121, 126], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"333": {"label": 3, "data": {"text": "The refolding kinetics of guanidine-denatured disulfide-intact bovine pancreatic ribonuclease A (RNase A) and its proline-42-to-alanine mutant (Pro42Ala) have been studied by monitoring tyrosine burial and 2'-cytidine monophosphate (2'CMP) inhibitor binding.", "entity1": "bovine pancreatic ribonuclease A", "entity2": "2'-cytidine monophosphate", "span1": [63, 95], "span2": [206, 231]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12389": {"label": 0, "data": {"text": "The myosin-18A\u03b1 isoform, additionally, has an N-terminal PDZ domain.", "entity1": "PDZ domain", "entity2": "N", "span1": [57, 67], "span2": [46, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10436": {"label": 1, "data": {"text": "The holo-SDH crystallized with O-methylserine (OMS) was also determined at 2.6 A resolution by molecular replacement.", "entity1": "holo-SDH", "entity2": "O-methylserine", "span1": [4, 12], "span2": [31, 45]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4481": {"label": 3, "data": {"text": "In this study, we assessed the effects of clopidogrel and clarithromycin, known CYP2B6 and CYP3A inhibitors, respectively, on the enantioselective disposition of racemic sibutramine in conjunction with CYP2B6 polymorphisms in humans.", "entity1": "CYP2B6", "entity2": "clarithromycin", "span1": [80, 86], "span2": [58, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1551": {"label": 8, "data": {"text": "Even though the activities of MAT and GNMT were elevated, the concentration of liver S-adenosylmethionine was decreased (24%, p<0.001) and S-adenosylhomocysteine increased (113%, p<0.001) in the dwarf mice.", "entity1": "GNMT", "entity2": "S-adenosylhomocysteine", "span1": [38, 42], "span2": [139, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1272": {"label": 1, "data": {"text": "the NOS-catalyzed oxidation of NADPH in the absence of substrate or pterin that does not result in NO production.", "entity1": "NOS", "entity2": "NADPH", "span1": [4, 7], "span2": [31, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, 8, -1, 9]},
	"6008": {"label": 3, "data": {"text": "BACKGROUND: The active metabolite of the anti-inflammatory drug nabumetone has been characterized as a selective inhibitor of the inducible prostaglandin H synthase (PGHS).", "entity1": "PGHS", "entity2": "nabumetone", "span1": [166, 170], "span2": [64, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10096": {"label": 8, "data": {"text": "Celecoxib selectively suppressed PGE2 but not TxB2 at time points consistent with COX-2 activity, while producing analgesia.", "entity1": "COX-2", "entity2": "PGE2", "span1": [82, 87], "span2": [33, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"1902": {"label": 3, "data": {"text": "PKC isoforms did show different sensitivity and selectivity for down-regulation by I3A and phorbol 12-myristate 13-acetate (PMA) in WEHI-231, HOP-92, and Colo-205 cells.", "entity1": "PKC", "entity2": "PMA", "span1": [0, 3], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8989": {"label": 3, "data": {"text": "Removing medium Ca2+, blocking Ca2+ channels with 50 mumol/l verapamil, or inhibiting calmodulin activation with 20 mumol/l trifluoperazine, 10 mumol/l chlorpromazine or 10 mumol/l pimozide almost completely blocked hyposmolarity-induced secretion.", "entity1": "calmodulin", "entity2": "chlorpromazine", "span1": [86, 96], "span2": [152, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14534": {"label": 3, "data": {"text": "Data at transcriptional level also demonstrated that catalpol potently attenuated gene expressions involved in inflammation, such as iNOS, COX-2 and TLR4.", "entity1": "iNOS", "entity2": "catalpol", "span1": [133, 137], "span2": [53, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1084": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "galanthamine", "span1": [51, 71], "span2": [146, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4843": {"label": 2, "data": {"text": "Subsequent analysis revealed that cucurbitacin I strongly activates RhoA and the Rho effector Rho kinase (ROCK) in breast cancer cells and induces the formation of stress fibers.", "entity1": "Rho", "entity2": "cucurbitacin I", "span1": [81, 84], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14526": {"label": 3, "data": {"text": "In contrast, EGCG markedly downregulated major bile acid transporters (Asbt and Ost\u03b1) and regulatory molecules (Shp and Fgf15) in the ileum.", "entity1": "Asbt", "entity2": "EGCG", "span1": [71, 75], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5866": {"label": 3, "data": {"text": "Our conclusion is that chronic DPDPE treatment preferentially reduces delta-opioid receptor binding activity.", "entity1": "delta-opioid receptor", "entity2": "DPDPE", "span1": [70, 91], "span2": [31, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"585": {"label": 3, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cyclin E", "entity2": "Tomudex", "span1": [35, 43], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8585": {"label": 3, "data": {"text": "The high fat diet significantly increased hepatic mRNA expressions of PPAR\u03b3, SREBP1C and SCD-1 genes in comparison to the control diet, which was subsequently reversed by supplementation with fisetin.", "entity1": "SCD-1", "entity2": "fisetin", "span1": [89, 94], "span2": [192, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6312": {"label": 8, "data": {"text": "Activation of endothelial nitric oxide synthase (eNOS) results in the production of nitric oxide (NO) that mediates the vasorelaxing properties of endothelial cells.", "entity1": "eNOS", "entity2": "nitric oxide", "span1": [49, 53], "span2": [84, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9030": {"label": 2, "data": {"text": "Propranolol treatment (4 X 40 mg/day) increased the density of beta 2-adrenoceptors by 25% after 2 days; concomitantly PRA and heart rate were reduced.", "entity1": "beta 2-adrenoceptors", "entity2": "Propranolol", "span1": [63, 83], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2438": {"label": 0, "data": {"text": "The Turkish patient and her affected relatives all had a heterozygous A to G transition at codon 557 (AAG-->GAG) of exon 10 of MEN1 that results in a replacement of lysine by glutamic acid.", "entity1": "MEN1", "entity2": "glutamic acid", "span1": [127, 131], "span2": [175, 188]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8061": {"label": 3, "data": {"text": "Finally, expression of constitutive activate MKK6 or HA-p38 MAPK vectors in lung cancer cells was able to abrogate ERCC1 downregulation by metformin and paclitaxel as well as cell viability and DNA repair capacity.", "entity1": "ERCC1", "entity2": "paclitaxel", "span1": [115, 120], "span2": [153, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11565": {"label": 8, "data": {"text": "This surprising correlation between the lack of OTC expression and sensitivity of ASS-positive HCC cells shows that OTC-deficient HCCs are sensitive to rhArg-mediated arginine depletion.", "entity1": "rhArg", "entity2": "arginine", "span1": [152, 157], "span2": [167, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9809": {"label": 1, "data": {"text": "METHODS AND RESULTS: The effect of intravenous ajmaline (1 mg/kg), procainamide (10 mg/kg), or flecainide (2 mg/kg) on the ECG was studied in 34 patients with the syndrome and transient normalization of the ECG (group A), 11 members of 3 families in whom a SCN5A mutation was associated with the syndrome and 8 members in whom it was not (group B), and 53 control subjects (group C).", "entity1": "SCN5A", "entity2": "ajmaline", "span1": [257, 262], "span2": [47, 55]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4989": {"label": 1, "data": {"text": "Cobalt chloride, a typical HIF activator, induced the gene expression of CAR-target genes, including cyp2b9 and cyp2b10, an accumulation of nuclear CAR and an increase in the PB-responsive enhancer module-mediated transactivation in the mouse liver.", "entity1": "CAR", "entity2": "Cobalt chloride", "span1": [148, 151], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6783": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-1", "entity2": "carprofen", "span1": [268, 273], "span2": [148, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7634": {"label": 9, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "purine receptors", "entity2": "ATP", "span1": [125, 141], "span2": [26, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5627": {"label": 8, "data": {"text": "BACKGROUND: Norepinephrine transporter (NET) is involved in the regulation of norepinephrine (NE) turnover and metabolism.", "entity1": "NET", "entity2": "norepinephrine", "span1": [40, 43], "span2": [78, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10586": {"label": 5, "data": {"text": "BACKGROUND: To assess the sensitivity of biochemical, physiological, and pharmacological markers of peripheral norepinephrine (NE) transporter (NET) function, we chronically antagonized NET by a range of doses of duloxetine [(+)-N-methyl-3-(1-naphthalenyloxy)-2 thiophenepropanamine], which blocks the NE reuptake process.", "entity1": "NET", "entity2": "duloxetine", "span1": [186, 189], "span2": [213, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3396": {"label": 3, "data": {"text": "Although the inhibition of cyclooxygenases by aspirin, which leads to its anti-inflammatory/analgesic properties, has been well studied, the mechanisms involved in its chemopreventive effects as well as some of its adverse effects are as yet ill-defined.", "entity1": "cyclooxygenases", "entity2": "aspirin", "span1": [27, 42], "span2": [46, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14109": {"label": 1, "data": {"text": "The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide.", "entity1": "CRBN", "entity2": "thalidomide", "span1": [55, 59], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5032": {"label": 5, "data": {"text": "Synthesis and in Vitro Characterisation of Ifenprodil-Based Fluorescein Conjugates as GluN1/GluN2B N-Methyl-D-aspartate Receptor Antagonists.", "entity1": "GluN1", "entity2": "Fluorescein", "span1": [86, 91], "span2": [60, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10028": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Arg", "span1": [199, 208], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15301": {"label": 1, "data": {"text": "To map supercoiling, we used biotinylated trimethylpsoralen as a DNA structure probe to show that the human genome is organized into supercoiling domains.", "entity1": "supercoiling domains", "entity2": "biotinylated trimethylpsoralen", "span1": [133, 153], "span2": [29, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12139": {"label": 1, "data": {"text": "Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries.", "entity1": "alpha(2A)-adrenoceptor", "entity2": "brimonidine", "span1": [7, 29], "span2": [59, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9819": {"label": 5, "data": {"text": "Methiothepin (intravenous, 1 mg/kg), whose serotonergic actions include 5-HT1 and 5-HT2 antagonism, typically raised serotonin levels (four of five cells) and always blocked inhibition by clomipramine (n = 3).", "entity1": "5-HT1", "entity2": "Methiothepin", "span1": [72, 77], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13790": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "ABL", "entity2": "Dasatinib", "span1": [101, 104], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6080": {"label": 2, "data": {"text": "The antiarrhythmic effects of exogenous adenosine and Valsalva on this form of VT may be due to receptor-mediated inhibition of adenylate cyclase or to noncardiac receptor-mediated effects, i.e., exogenous adenosine may modulate VT through alterations in autonomic tone by activation of arterial chemoreceptors, and Valsalva has been shown to decrease venous return, resulting in a reduction in cardiac dimensions and myocardial stretch.", "entity1": "chemoreceptors", "entity2": "adenosine", "span1": [296, 310], "span2": [206, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1386": {"label": 3, "data": {"text": "Inhibition of human iNOS promoter-driven luciferase activity by gemfibrozil in cytokine-stimulated U373MG astroglial cells suggests that this compound inhibits the transcription of iNOS.", "entity1": "iNOS", "entity2": "gemfibrozil", "span1": [181, 185], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10380": {"label": 3, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "ACE", "entity2": "omapatrilat", "span1": [99, 102], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6744": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "CT53518", "span1": [273, 279], "span2": [234, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3719": {"label": 3, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "phosphorylated extracellular signal-regulated kinase", "entity2": "BPs", "span1": [43, 95], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8709": {"label": 3, "data": {"text": "Finally, SA-induced AT1R expression was found to be prevented both by NAC and specific JNK inhibitor, SP6001325, strongly indicating that AT1R upregulation is a result of the ROS-mediated activation of the JNK signaling pathway.", "entity1": "AT1R", "entity2": "SP6001325", "span1": [20, 24], "span2": [102, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"677": {"label": 8, "data": {"text": "Of the PDE inhibitors tested, dipyridamole was most effective, with IC50 values of 1.2 and 0.45 microM for inhibition of cAMP and cGMP hydrolysis, respectively.", "entity1": "PDE", "entity2": "cGMP", "span1": [7, 10], "span2": [130, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13361": {"label": 3, "data": {"text": "The expression of ER-alpha and PR isoform A in virgin mice was surprisingly much higher in BALB/c than in C57BL/6 mammary glands, and both receptors were downregulated in progestin-treated BALB/c mice (P < 0.05).", "entity1": "ER-alpha", "entity2": "progestin", "span1": [18, 26], "span2": [171, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9250": {"label": 1, "data": {"text": "Our results indicate that ergot compounds, especially ergovaline, bind to D2 dopamine receptors and elicit second messenger responses similar to that of dopamine.", "entity1": "D2 dopamine receptors", "entity2": "dopamine", "span1": [74, 95], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9586": {"label": 3, "data": {"text": "All three compounds displayed antagonistic properties against oxytocin in vitro, with carbetocin being the strongest inhibitor (pA2 = 8.21) and carbetocin metabolite II (pA2 = 8.01) being stronger than carbetocin metabolite I (pA2 = 7.81).", "entity1": "oxytocin", "entity2": "carbetocin", "span1": [62, 70], "span2": [144, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"538": {"label": 8, "data": {"text": "Because gastric AADC and COMT degrade levodopa, the drug is given with inhibitors of AADC (carbidopa or benserazide), and inhibitors of COMT will also enter clinical use.", "entity1": "COMT", "entity2": "levodopa", "span1": [25, 29], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"907": {"label": 1, "data": {"text": "The ability of betaxolol to interact with neurotoxin site 2 of the Na(+) channel and inhibit Na(+) influx may have a role in its neuroprotective action in paradigms of excitotoxicity/ischaemia and in its therapeutic effect in glaucoma.", "entity1": "Na(+) channel", "entity2": "betaxolol", "span1": [67, 80], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3373": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.2", "entity2": "DHP", "span1": [71, 79], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12202": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "alpha-linolenic acid", "span1": [282, 285], "span2": [228, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15248": {"label": 8, "data": {"text": "Furthermore, silymarin, silybin A, and silybin B (100 \u00b5M) significantly inhibited OATP-mediated estradiol-17\u03b2-glucuronide and rosuvastatin uptake into human hepatocytes.", "entity1": "OATP", "entity2": "estradiol-17\u03b2-glucuronide", "span1": [82, 86], "span2": [96, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8060": {"label": 3, "data": {"text": "Finally, expression of constitutive activate MKK6 or HA-p38 MAPK vectors in lung cancer cells was able to abrogate ERCC1 downregulation by metformin and paclitaxel as well as cell viability and DNA repair capacity.", "entity1": "ERCC1", "entity2": "metformin", "span1": [115, 120], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4267": {"label": 2, "data": {"text": "Interestingly, ursolic acid increased the phosphorylation of AMPK and coenzyme A carboxylase and also enhanced phosphorylation of GSK3\u03b2 at inactive form serine 9, whereas ursolic acid attenuated the phosphorylation of AKT and mTOR in HepG2 cells.", "entity1": "GSK3\u03b2", "entity2": "ursolic acid", "span1": [130, 135], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1290": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "EC 4.1.1.15", "entity2": "gamma-aminobutyric acid", "span1": [55, 66], "span2": [109, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"8984": {"label": 1, "data": {"text": "The smooth muscle relaxant, W-7, which is believed relatively specific in inhibiting the Ca2(+)-calmodulin interaction, depressed hyposmolarity-induced PRL secretion in a dose-dependent manner (r = -0.991, p less than 0.01).", "entity1": "calmodulin", "entity2": "W-7", "span1": [96, 106], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14616": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Lys27Gln", "entity2": "2',2'-difluorodeoxyuridine", "span1": [39, 47], "span2": [255, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7151": {"label": 2, "data": {"text": "Binding of cGMP to GAF-A increases cNPK phosphorylation of PDE5 and improves catalytic site affinity for cGMP or inhibitors.", "entity1": "PDE5", "entity2": "cGMP", "span1": [59, 63], "span2": [11, 15]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8829": {"label": 3, "data": {"text": "Matrix Metalloproteinase Inhibitors Based on the 3-Mercaptopyrrolidine Core.", "entity1": "Matrix Metalloproteinase", "entity2": "3-Mercaptopyrrolidine", "span1": [0, 24], "span2": [49, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7973": {"label": 1, "data": {"text": "Quantitative polymerase chain reaction, western blotting, immunohistochemical analysis and immunofluorescence were used to determine the changes in the expression of organic anion transporter (Oat)1 and Oat3 in rat kidney in response to 1,25(OH)(2)D(3) treatment.", "entity1": "(Oat)1", "entity2": "1,25(OH)(2)D(3)", "span1": [192, 198], "span2": [237, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14153": {"label": 3, "data": {"text": "When combined, mianserin antagonized the effects of the full kappa-opioid receptor agonists in [(35)S]GTPgammaS assays and reduced the stimulation of p38 MAPK and ERK1/2 phosphorylation by dynorphin A.", "entity1": "p38", "entity2": "mianserin", "span1": [150, 153], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1358": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "dopamine transporter", "entity2": "hydroxyl", "span1": [295, 315], "span2": [226, 234]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8498": {"label": 1, "data": {"text": "The present study aimed to determine the protective effects and the underlying mechanisms of curcumin on ovalbumin (OVA)-induced allergic inflammation in a mouse model of allergic asthma.", "entity1": "ovalbumin", "entity2": "curcumin", "span1": [105, 114], "span2": [93, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12924": {"label": 8, "data": {"text": "Pretreatment with H(2)S or NaHS significantly inhibited LPS-induced iNOS expression and NO production.", "entity1": "iNOS", "entity2": "NO", "span1": [68, 72], "span2": [88, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14431": {"label": 3, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C.", "entity1": "AMPK", "entity2": "compound C", "span1": [143, 147], "span2": [158, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12925": {"label": 8, "data": {"text": "While either blockage of HO activity by the HO inhibitor, tin protoporphyrin IX, or down-regulation of HO-1 expression by HO-1 small interfering RNA (siRNA) reversed the inhibitory effects of H(2)S on iNOS expression and NO production, HO-1 overexpression produced the same inhibitory effects of H(2)S. In addition, LPS-induced nuclear factor (NF)-kappaB activation was diminished in RAW264.7 macrophages preincubated with H(2)S. Interestingly, the inhibitory effect of H(2)S on NF-kappaB activation was reversed by the transient transfection with HO-1 siRNA, but was mimicked by either HO-1 gene transfection or treatment with carbon monoxide (CO), an end product of HO-1.", "entity1": "iNOS", "entity2": "NO", "span1": [201, 205], "span2": [221, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8548": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "histone deacetylase", "entity2": "pyrrole", "span1": [159, 178], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15894": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "NRPS", "entity2": "benzopyranopyrrole", "span1": [48, 52], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12967": {"label": 0, "data": {"text": "The phosphorylation by gammaPKC resulted in activation of DGKgamma because a DGKgamma mutant in which Ser-776 and Ser-779 were substituted with glutamic acid to mimic phosphorylation exhibited significantly higher activity compared with wild type DGKgamma and an unphosphorylatable DGKgamma mutant.", "entity1": "DGKgamma", "entity2": "Ser", "span1": [77, 85], "span2": [102, 105]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5329": {"label": 3, "data": {"text": "Pasireotide (Signifor(\u00ae)) is a new subcutaneous somatostatin analogue that acts via somatostatin receptors to inhibit the secretion of corticotropin from the pituitary adenoma in patients with Cushing's disease.", "entity1": "corticotropin", "entity2": "Signifor", "span1": [135, 148], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11929": {"label": 1, "data": {"text": "To evaluate whether fisetin regulates mTORC1 signaling, we investigated the phosphorylation and kinase activity of the 70-kDa ribosomal protein S6 kinase 1 (S6K1) and mTORC1 in 3T3-L1 preadipocytes.", "entity1": "mTORC1", "entity2": "fisetin", "span1": [38, 44], "span2": [20, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3436": {"label": 2, "data": {"text": "Epi increased both WNT6/Wnt6 and Cav1 expression in human GC cells and within the tumor area of a murine model of GC (CEA424-SV40 TAg).", "entity1": "Wnt6", "entity2": "Epi", "span1": [24, 28], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"24": {"label": 3, "data": {"text": "The inhibitory effects of iloprost on tissue factor expression were also potentiated by isobutylmethylxanthine and mimicked by forskolin and dibutyryl cyclic AMP but not dibutyryl cyclic GMP.", "entity1": "tissue factor", "entity2": "ibutyryl cyclic AMP", "span1": [38, 51], "span2": [142, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3550": {"label": 2, "data": {"text": "The results demonstrated that intracerebral infusions of LTD4 (1 ng/mouse) produced memory impairment as determined by Morris water maze test and Y-maze test in mice, and caused the accumulation of A\u03b21-40 and A\u03b21-42 in the hippocampus and cortex through increased activity of \u03b2- and \u03b3-secretases accompanied with increased expression of amyloid precursor protein (APP).", "entity1": "A\u03b21-42", "entity2": "LTD4", "span1": [209, 215], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15653": {"label": 2, "data": {"text": "Excess of cholesterol converted into 24OHC may up-regulate ApoE synthesis which is a scavenger for A\u03b2 and Tau.", "entity1": "ApoE", "entity2": "24OHC", "span1": [59, 63], "span2": [37, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2226": {"label": 9, "data": {"text": "Dasatinib (BMS-354825) is a novel orally bioavailable SRC/ABL inhibitor that has activity against multiple imatinib-resistant BCR-ABL isoforms in vitro that is presently showing considerable promise in early-phase clinical trials of chronic myeloid leukemia (CML).", "entity1": "ABL", "entity2": "imatinib", "span1": [130, 133], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7802": {"label": 9, "data": {"text": "However, 4'G-RSV, but not 3G-RSV, induced SIRT1-dependent histone H3 deacetylation and SOD2 expression in mouse C2C12 skeletal myoblasts; as with RSV, SIRT1 knockdown blunted these effects.", "entity1": "SOD2", "entity2": "3G-RSV", "span1": [87, 91], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13129": {"label": 2, "data": {"text": "RESULT(S): The expression of endometrial ERalpha, PRAB, PRB, and SRC-1 was increased significantly after 1 week of mifepristone, but the increase was no longer seen after 10 weeks.", "entity1": "PRAB", "entity2": "mifepristone", "span1": [50, 54], "span2": [115, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2504": {"label": 3, "data": {"text": "Chronic insulin (24 h) activates NHE3 through the classic phosphatidylinositol 3-kinase-serum- and glucocorticoid-dependent kinase 1 (PI3K-SGK1) pathway as insulin stimulates SGK1 phosphorylation and the insulin effect can be blocked by the PI3K inhibitor wortmannin or a dominant-negative SGK1.", "entity1": "PI3K", "entity2": "wortmannin", "span1": [241, 245], "span2": [256, 266]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5614": {"label": 3, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "cisapride", "span1": [131, 135], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6573": {"label": 1, "data": {"text": "In the active MalP enzyme, the residue Arg569 stabilizes the negative-charged Glc1P, whereas in the inactive form of GP this key residue is held away from the catalytic site by loop 280s and an allosteric transition of the mammalian enzyme is required for activation.", "entity1": "MalP", "entity2": "Glc1P", "span1": [14, 18], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"7736": {"label": 5, "data": {"text": "Abarelix was the first GnRH antagonist to be developed and was approved by the USA Food and Drug Administration in 2004 for the initiation of hormonal castration in advanced or metastasizing hormone-dependent prostate carcinoma, when rapid androgen suppression is necessary.", "entity1": "GnRH", "entity2": "Abarelix", "span1": [23, 27], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7275": {"label": 3, "data": {"text": "The best inhibitors were brinzolamide and sulpiride (KI values of 0.8-0.9 nM), the latter compound being also a CA VI-selective inhibitor.", "entity1": "CA VI", "entity2": "sulpiride", "span1": [112, 117], "span2": [42, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3622": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "AM2389", "span1": [14, 17], "span2": [201, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8070": {"label": 1, "data": {"text": "Carboxylesterase-2 is a highly sensitive target of the antiobesity agent orlistat with profound implications in the activation of anticancer prodrugs.", "entity1": "Carboxylesterase-2", "entity2": "orlistat", "span1": [0, 18], "span2": [73, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8644": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b2", "entity2": "ethanol", "span1": [14, 18], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15617": {"label": 3, "data": {"text": "Galangin decreased expression of pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-\u03b1, interleukin (IL)-6, IL-1\u03b2, and IL-8.", "entity1": "interleukin", "entity2": "Galangin", "span1": [100, 111], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14900": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO3", "entity2": "TMAO", "span1": [71, 75], "span2": [156, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14996": {"label": 1, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "peroxisome proliferator-activated receptor (PPAR)\u03b3", "entity2": "fatty acids", "span1": [157, 207], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12133": {"label": 1, "data": {"text": "Nicorandil 20 micromol/L reversed only 50% of the effect of ATX-II and failed to completely suppress TdP in the LQT3 model (5/6 to 3/6).", "entity1": "ATX-II", "entity2": "Nicorandil", "span1": [60, 66], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1819": {"label": 1, "data": {"text": "Quinone oxidoreductase 2 (QR2) purified from human red blood cells was recently shown to be a potential target of the quinoline antimalarial compounds [Graves et al., (2002) Mol.", "entity1": "Quinone oxidoreductase 2", "entity2": "quinoline", "span1": [0, 24], "span2": [118, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10731": {"label": 5, "data": {"text": "The binding domain of barusiban differs from the binding domain of the agonists and the nonselective oxytocin receptor antagonist d(CH2)5[Tyr-(Me)2,Thr4,Orn8,Tyr9]vasotocin that has been used in previous studies.", "entity1": "oxytocin receptor", "entity2": "d(CH2)5[Tyr-(Me)2,Thr4,Orn8,Tyr9]vasotocin", "span1": [101, 118], "span2": [130, 172]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9933": {"label": 2, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "Rel", "entity2": "12-O-tetradecanoylphorbol-13-acetate", "span1": [19, 22], "span2": [72, 108]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5944": {"label": 9, "data": {"text": "Pimozide and thioridazine had no effect on the estradiol binding properties of the MCF-7 ER, nor did pimozide interfere with the induction of progesterone receptors by estradiol.", "entity1": "ER", "entity2": "thioridazine", "span1": [89, 91], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10097": {"label": 8, "data": {"text": "These studies demonstrate the ability to assess the time course and selective effects of COX-2 inhibitors in vivo and suggest that suppression of COX-2 mediated PGE2 is temporally related to NSAID analgesia.", "entity1": "COX-2", "entity2": "PGE2", "span1": [146, 151], "span2": [161, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7134": {"label": 1, "data": {"text": "All PDE5 constructs had similar affinities for 3-isobutyl-1-methylxanthine, sildenafil, tadalafil, and UK-122764, but mutants containing a complete GAF-B had 7- to 18-fold higher affinity for vardenafil-based compounds compared with those lacking a complete GAF-B.", "entity1": "GAF-B", "entity2": "sildenafil", "span1": [148, 153], "span2": [76, 86]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3283": {"label": 3, "data": {"text": "Together these studies support a unique mode of inhibition in which phenothiazines disrupt the S100A4/myosin-IIA interaction by sequestering S100A4 via small molecule-induced oligomerization.", "entity1": "myosin-IIA", "entity2": "phenothiazines", "span1": [102, 112], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"501": {"label": 1, "data": {"text": "Felodipine and nicardipine have similar affinities for 60-kDa CaMPDE isozymes but bring about different levels of enzyme inhibition, suggesting the possibility of designing specific drugs that can protect the enzyme from inhibition by dihydropyridine Ca2+-channel blockers.", "entity1": "CaMPDE", "entity2": "Felodipine", "span1": [62, 68], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4131": {"label": 8, "data": {"text": "Absorption and secretion of fluoride increase at acid pH levels, possibly because of its non-ionized state at these pHs and/or because of participation of a F(-)/H(+) cotransporter or a F(-)/OH(-) antiporter.", "entity1": "F(-)/OH(-) antiporter", "entity2": "fluoride", "span1": [186, 207], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6739": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "PDGFbeta-receptor", "entity2": "phenylaminopyrimidine", "span1": [187, 204], "span2": [77, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4718": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Rspo2", "entity2": "TCDD", "span1": [304, 309], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11599": {"label": 8, "data": {"text": "In this study, we investigated the presence of H(2)S and the expression of H(2)S synthesizing enzymes, CSE and CBS, in isolated mouse pancreatic acini.", "entity1": "CBS", "entity2": "H(2)S", "span1": [111, 114], "span2": [75, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6906": {"label": 0, "data": {"text": "Unlike transferrin receptor, the protease domain of PSMA contains a binuclear zinc site, catalytic residues, and a proposed substrate-binding arginine patch.", "entity1": "protease domain", "entity2": "arginine", "span1": [33, 48], "span2": [142, 150]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11252": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "SERT", "entity2": "mazindol", "span1": [127, 131], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2285": {"label": 3, "data": {"text": "Also consistent with the involvement of Gq coupled EP1 receptors, the PGE1 stimulation is inhibited by the PKCI vector (encoding the PKC inhibitory domain), the PKC inhibitor Go 6976, thapsigargin, as well as the calmodulin antagonists W7 and W13.", "entity1": "PKC", "entity2": "thapsigargin", "span1": [161, 164], "span2": [184, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4485": {"label": 3, "data": {"text": "Endothelium-dependent relaxations, nitric oxide (NO) and endothelium derived hyperpolarizing factor (EDHF)-type, were studied in rabbit iliac artery and aortic rings using the G protein-coupled receptor agonist acetylcholine (ACh) and by cyclopiazonic acid (CPA), which promotes store-operated Ca(2+) entry by inhibiting the endothelial SERCA pump.", "entity1": "SERCA", "entity2": "CPA", "span1": [337, 342], "span2": [258, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5950": {"label": 3, "data": {"text": "Inhibition of MCF-7 cell growth by the selective calmodulin antagonists W-13 and W-12 is consistent with a role for calmodulin antagonism in the broad growth-inhibitory properties of pimozide.", "entity1": "calmodulin", "entity2": "pimozide", "span1": [116, 126], "span2": [183, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13327": {"label": 3, "data": {"text": "Sulfasalazine (also as a representative of the salicylates) inhibited the diabetes-induced upregulation of several inflammatory gene products, which are regulated by NF-kappaB, including vascular cell adhesion molecule, intracellular adhesion molecule-1, inducible nitric oxide synthase, and cyclooxygenase-2 in whole-retinal lysate.", "entity1": "inducible nitric oxide synthase", "entity2": "Sulfasalazine", "span1": [255, 286], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10104": {"label": 3, "data": {"text": "In addition, we also showed that the elevation in alanine levels and the inhibition of alanine transaminase in the brain are retained after 14 days of PLZ treatment, and that PLZ produces a marked increase in extracellular levels of alanine.", "entity1": "alanine transaminase", "entity2": "PLZ", "span1": [87, 107], "span2": [151, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12601": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "EGF domain", "entity2": "N", "span1": [203, 213], "span2": [316, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13409": {"label": 5, "data": {"text": "In the current project, we found that the selective H(1) antagonist pyrilamine also reversed the dizocilpine-induced impairment in PPI of tactile startle with an auditory prepulse.", "entity1": "H(1)", "entity2": "pyrilamine", "span1": [52, 56], "span2": [68, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1337": {"label": 4, "data": {"text": "Consistent with the weak transactivation activity of esterified-BM mediated by rat GR, there were few side effects, evaluated by thymus involution and body weight loss, in an antigen-induced asthmatic model in rats.", "entity1": "rat GR", "entity2": "BM", "span1": [79, 85], "span2": [64, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2210": {"label": 2, "data": {"text": "Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures.", "entity1": "CREB", "entity2": "morphine", "span1": [66, 70], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14167": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "HO-1", "entity2": "chalcones", "span1": [60, 64], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6916": {"label": 8, "data": {"text": "Elucidation of the PSMA structure combined with docking studies and a proposed catalytic mechanism provides insight into the recognition of inhibitors and the natural substrate N-acetyl-l-aspartyl-l-glutamate.", "entity1": "PSMA", "entity2": "N-acetyl-l-aspartyl-l-glutamate", "span1": [19, 23], "span2": [177, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15912": {"label": 1, "data": {"text": "These results suggest that E2 enhances cocaine-stimulated locomotion in mice predominantly through ER\u03b1.", "entity1": "ER\u03b1", "entity2": "cocaine", "span1": [99, 102], "span2": [39, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11540": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "TDI", "span1": [86, 89], "span2": [217, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12990": {"label": 1, "data": {"text": "The main molecular target of azole antifungals is the cytochrome P-450 protein Erg11p/Cyp51p.", "entity1": "Erg11p", "entity2": "azole", "span1": [79, 85], "span2": [29, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1476": {"label": 1, "data": {"text": "Eprosartan acts at vascular AT(1) receptors (postsynaptically) and at presynaptic AT(1) receptors, where it inhibits sympathetically stimulated noradrenaline release.", "entity1": "AT(1) receptors", "entity2": "Eprosartan", "span1": [82, 97], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12041": {"label": 8, "data": {"text": "We suggest that the latter can react with H2O2 in a catalase-like reaction, with evolution of O2.", "entity1": "catalase", "entity2": "O2", "span1": [52, 60], "span2": [94, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"344": {"label": 3, "data": {"text": "Sodium salicylate and aspirin also inhibited NF-kappa B-dependent transcription from the Ig kappa enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells.", "entity1": "NF-kappa B", "entity2": "aspirin", "span1": [45, 55], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11935": {"label": 1, "data": {"text": "To further our understanding of how fisetin negatively regulates mTORC1 signaling, we analyzed the phosphorylation of S6K1, mTOR and Akt in fisetin-treated TSC2-knockdown cells.", "entity1": "mTOR", "entity2": "fisetin", "span1": [124, 128], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6136": {"label": 0, "data": {"text": "To identify the molecular determinants for dofetilide block, we first engineered chimeras between HERG and BEAG and then used site-directed mutagenesis to localize single amino acid residues responsible for block.", "entity1": "BEAG", "entity2": "amino acid", "span1": [107, 111], "span2": [171, 181]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4505": {"label": 3, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES1", "entity2": "(R)-naproxen-\u03b2-d-glucuronide", "span1": [169, 174], "span2": [84, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12025": {"label": 1, "data": {"text": "The specificity of progestagens for the progesterone receptors in the cytosol fraction of MCF-7 cells was similar to that for progesterone receptors in human and rabbit myometrial cytosol but different from that for the progesterone receptor in rat myometrial cytosol.", "entity1": "progesterone receptors", "entity2": "progestagens", "span1": [126, 148], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14013": {"label": 3, "data": {"text": "Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.", "entity1": "MET", "entity2": "Cabozantinib", "span1": [30, 33], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9627": {"label": 1, "data": {"text": "Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide.", "entity1": "sulfonylurea receptor", "entity2": "glibenclamide", "span1": [44, 65], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5754": {"label": 3, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C. To further validate the result, we examined sub-cellular distribution of c-Rel in lungs of CS-exposed guinea pigs treated or untreated with vitamin C. Result showed that vitamin C treatment resulted in markedly reduced c-Rel nuclear translocation.", "entity1": "c-Rel", "entity2": "vitamin C", "span1": [398, 403], "span2": [349, 358]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12214": {"label": 1, "data": {"text": "This mechanism involves the calcium-dependent tyrosine kinase Pyk2, the non-receptor tyrosine kinase c-Src and the focal adhesion protein/steroid receptor co-factor, Hic-5.", "entity1": "tyrosine kinase", "entity2": "calcium", "span1": [46, 61], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9618": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "SUR1", "entity2": "nucleotide", "span1": [101, 105], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5074": {"label": 2, "data": {"text": "Here, we have now found that activation of p38 MAPK by anisomycin potentiated induction of CYP2B6 mRNA by CAR ligand in HepG2 cells to levels observed in ligand-treated human primary hepatocytes.", "entity1": "p38", "entity2": "anisomycin", "span1": [43, 46], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8927": {"label": 5, "data": {"text": "In anesthetized spontaneously hypertensive rats, the antihypertensive activity of carvedilol was nearly abolished by combined pretreatment of the rats with high doses of the alpha 1 adrenoceptor antagonist, prazosin (1 mg/kg, iv), and the nonselective beta adrenoceptor antagonist, propranolol (3 mg/kg, iv), suggesting that the majority of the antihypertensive response produced by carvedilol may be accounted for by blockade of beta and alpha 1 adrenoceptors.", "entity1": "beta adrenoceptor", "entity2": "propranolol", "span1": [252, 269], "span2": [282, 293]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1955": {"label": 1, "data": {"text": "It has previously been suggested that ergotamine produces external carotid vasoconstriction in vagosympathectomised dogs via 5-HT1B/1D receptors and alpha2-adrenoceptors.", "entity1": "alpha2-adrenoceptors", "entity2": "ergotamine", "span1": [149, 169], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11972": {"label": 2, "data": {"text": "Meanwhile, autophagy was detected as early as 12\u00a0h after an exposure to low-dose dioscin, as indicated by an up-regulated expression of LC3-II and beclin-1 proteins.", "entity1": "LC3-II", "entity2": "dioscin", "span1": [136, 142], "span2": [81, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10894": {"label": 1, "data": {"text": "This work provides detailed structural information on the interactions between PDXK and roscovitine and analogs.", "entity1": "PDXK", "entity2": "roscovitine", "span1": [79, 83], "span2": [88, 99]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4577": {"label": 1, "data": {"text": "Taken together, these findings indicate that antofine induces Cx43 gap junction disassembly by the PKC\u03b2 signaling pathway.", "entity1": "Cx43", "entity2": "antofine", "span1": [62, 66], "span2": [45, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6511": {"label": 3, "data": {"text": "There was a dose-dependent decrease in plasma renin activity, Ang I, and Ang II following single doses of Aliskiren starting with 40 mg. Inhibition was still marked and significant after repeated dosing with maximal decreases in Ang II levels by 89% and 75% on Days 1 and 8, respectively, when the highest dose of Aliskiren was compared with placebo.", "entity1": "Ang II", "entity2": "Aliskiren", "span1": [73, 79], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5207": {"label": 2, "data": {"text": "Correlation between activation of PPAR\u03b3 and resistin downregulation in a mouse adipocyte cell line by a series of thiazolidinediones.", "entity1": "PPAR\u03b3", "entity2": "thiazolidinediones", "span1": [34, 39], "span2": [114, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5708": {"label": 2, "data": {"text": "Lastly, As(III) increased soluble epoxide hydrolase activity in the lung, while it decreased its levels in the kidney and had no effect on the liver.", "entity1": "soluble epoxide hydrolase", "entity2": "As(III)", "span1": [26, 51], "span2": [8, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5592": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "clozapine", "span1": [111, 117], "span2": [128, 137]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14552": {"label": 8, "data": {"text": "Fluorescence of the reporter dye is turned on by rapid removal of the quinone quencher, an event that immediately occurs only after highly selective, two-electron reduction of the sterically and conformationally restricted quinone substrate by the cancer-associated human NAD(P)H:quinone oxidoreductase isozyme 1 (hNQO1).", "entity1": "human NAD(P)H:quinone oxidoreductase isozyme 1", "entity2": "quinone", "span1": [266, 312], "span2": [223, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9239": {"label": 3, "data": {"text": "The 15-lipoxygenase was similarly inhibited by triclosan with an IC-50 of 61 microM.", "entity1": "15-lipoxygenase", "entity2": "triclosan", "span1": [4, 19], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12642": {"label": 4, "data": {"text": "), attenuated the antitussive effects of codeine or SB 227122, indicating that the antitussive activity of both compounds is opioid receptor-mediated.", "entity1": "opioid receptor", "entity2": "codeine", "span1": [125, 140], "span2": [41, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12261": {"label": 8, "data": {"text": "LTC4 synthase (LTC4S), the pivotal enzyme for the biosynthesis of LTC4 (ref.", "entity1": "LTC4 synthase", "entity2": "LTC4", "span1": [0, 13], "span2": [66, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13910": {"label": 1, "data": {"text": "Additionally, phenformin inhibited the current elicited through the Kir6.2DeltaC26 (functional without SUR) channel with an IC50 of 1.78 mM.", "entity1": "SUR", "entity2": "phenformin", "span1": [103, 106], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4963": {"label": 2, "data": {"text": "Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo.", "entity1": "PXR", "entity2": "Amprenavir", "span1": [49, 52], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"860": {"label": 9, "data": {"text": "Addition of putrescine to DFMO-treated cell extracts did not increase caspase 3 activity.", "entity1": "caspase 3", "entity2": "putrescine", "span1": [70, 79], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1226": {"label": 3, "data": {"text": "It is not yet clear whether tamoxifen can reduce breast cancer incidence in women with BRCA1 and BRCA2 mutations, although preliminary evidence favors benefit for at least those with a BRCA2 mutation.", "entity1": "BRCA2", "entity2": "tamoxifen", "span1": [97, 102], "span2": [28, 37]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1988": {"label": 3, "data": {"text": "When selectively applied to channels after inducing slow inactivation with a 60-s pulse to -10 mV, mibefradil (1 microM) produced 45% fractional block in Nav1.5 and greater block (88%) in an isoform (Nav1.4) that slow-inactivates more completely.", "entity1": "Nav1.4", "entity2": "mibefradil", "span1": [200, 206], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13908": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR1", "entity2": "metformin", "span1": [231, 235], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8252": {"label": 0, "data": {"text": "N-terminal sequencing indicated that pro-BMP-2 was cleaved by FSAP at the canonical PC cleavage site, giving rise to mature BMP-2 (Arg(282)\u2193Gln(283)), as well as in the N-terminal heparin binding region of mature BMP-2, generating a truncated mature BMP-2 peptide (Arg(289)\u2193Lys(290)).", "entity1": "BMP-2", "entity2": "N", "span1": [213, 218], "span2": [169, 170]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13940": {"label": 1, "data": {"text": "The ER-targeting PROTACs are composed of an estradiol on one end and a hypoxia-inducing factor 1alpha (HIF-1alpha)-derived synthetic pentapeptide on the other.", "entity1": "ER", "entity2": "estradiol", "span1": [4, 6], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14588": {"label": 1, "data": {"text": "Aryl hydrocarbon receptor is a target of 17-Allylamino-17-demethoxygeldanamycin and enhances its anticancer activity in lung adenocarcinoma cells.", "entity1": "Aryl hydrocarbon receptor", "entity2": "17-Allylamino-17-demethoxygeldanamycin", "span1": [0, 25], "span2": [41, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"666": {"label": 3, "data": {"text": "METHODS: COX-1 inhibition was determined by measuring thromboxane B2 (TXB2)-generation from clotting whole blood ex vivo after single oral doses of 7.5 and 15 mg meloxicam and 75 mg diclofenac and at steady state (15 mg meloxicam daily and 150 mg diclofenac daily).", "entity1": "COX-1", "entity2": "diclofenac", "span1": [9, 14], "span2": [247, 257]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3509": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "AKRs", "entity2": "polycyclic aromatic hydrocarbons", "span1": [22, 26], "span2": [77, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11318": {"label": 3, "data": {"text": "Ten IU/mL urokinase was also incubated with pooled plasma of stroke patients, that was previously oxidized with the singlet oxygen (1O2) donor chloramine T (CT), to destroy plasmatic PAI-1 and alpha2-antiplasmin.", "entity1": "plasmatic PAI-1", "entity2": "singlet oxygen", "span1": [173, 188], "span2": [116, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11916": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "diglycerides", "span1": [174, 179], "span2": [68, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12276": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(1c)", "entity2": "AVP", "span1": [221, 226], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10290": {"label": 1, "data": {"text": "These differences from the horse might be the result of: (a) the presence in equine biological fluids of higher concentrations than in calves of the active PBZ metabolite, OPBZ; (b) a greater degree of binding of PBZ to plasma protein in calves; (c) species differences in the sensitivity to PBZ of the cyclo-oxygenase (COX) isoenzymes, COX-1 and COX-2 or; (d) a combination of these factors.", "entity1": "COX", "entity2": "PBZ", "span1": [320, 323], "span2": [292, 295]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12290": {"label": 1, "data": {"text": "Cabozantinib may provide clinical benefit by simultaneously targeting multiple pathways of importance in MTC, including MET, VEGFR2, and RET.", "entity1": "VEGFR2", "entity2": "Cabozantinib", "span1": [125, 131], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1692": {"label": 5, "data": {"text": "Memantine is an uncompetitive (channel blocking) NMDA receptor antagonist.", "entity1": "NMDA receptor", "entity2": "Memantine", "span1": [49, 62], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10975": {"label": 1, "data": {"text": "Preincubation (30 min) of bovine tracheal smooth muscle with various concentrations (0.1, 1 and 10 microM) of fenoterol decreased isoprenaline-induced maximal relaxation (E(max)) of methacholine-contracted preparations in a concentration dependent fashion, indicating desensitization of the beta(2)-adrenoceptor.", "entity1": "beta(2)-adrenoceptor", "entity2": "methacholine", "span1": [291, 311], "span2": [182, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"175": {"label": 5, "data": {"text": "Derivatives of 5-(dipentylamino)-5-oxo-pentanoic acid are a new class of non-peptide cholecystokinin (CCK) antagonists.", "entity1": "CCK", "entity2": "5-(dipentylamino)-5-oxo-pentanoic acid", "span1": [102, 105], "span2": [15, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8257": {"label": 4, "data": {"text": "Commercially-available 5-HT2C agonists (CP 809101, Ro 60-0175, WAY 161503, mCPP, and 1-methylpsilocin), novel\u00a04-phenyl-2-N,N-dimethyl-aminotetralin (PAT)-type 5-HT2C agonists (with 5-HT2A/2B antagonist activity), and antagonists selective for 5-HT2A (M100907), 5-HT2C (SB-242084), and 5-HT2B/2C (SB-206553) receptors attenuated the DOI-elicited-HTR.", "entity1": "5-HT2C", "entity2": "CP 809101", "span1": [23, 29], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13076": {"label": 8, "data": {"text": "Methylthioadenosine phosphorylase (MTAP) salvages purines by releasing adenine from methylthioadenosine and is often deleted in mesothelioma.", "entity1": "MTAP", "entity2": "adenine", "span1": [35, 39], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4434": {"label": 3, "data": {"text": "A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes.", "entity1": "DPP-4", "entity2": "xanthine", "span1": [173, 178], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"258": {"label": 1, "data": {"text": "An experimental strategy based on solution viscosity perturbation allowed us to study the energetics of amide-substrates, p-aminobenzamidine (p-ABZ) and proflavin binding to the catalytic site of two proteolyzed forms of alpha-thrombin, i.e.", "entity1": "alpha-thrombin", "entity2": "proflavin", "span1": [221, 235], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3663": {"label": 3, "data": {"text": "The mRNA levels of microphthalmia-associated transcription factor (MITF) and its downstream genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 were reduced by artemisinic acid treatment.", "entity1": "MITF", "entity2": "artemisinic acid", "span1": [67, 71], "span2": [172, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10471": {"label": 5, "data": {"text": "Pretreatment with a combination of (+/-)-2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2 -yl]phenoxy]propyl]amino]ethoxy]-benzamide methanesulfonate (CGP20712A, a selective beta(1)-adrenoceptor antagonist) and (+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-buta nol hydrochloride (ICI-118,5511, a selective beta(2)-adrenoceptor antagonist) (0.1 microM for each) produced a 14-fold rightward shift of the concentration-response curve for (-)-isoprenaline; however, the relaxation in response to (+/-)-CGP12177A was unaffected by the blockade of beta(1)- and beta(2)-adrenoceptors.", "entity1": "beta(1)-adrenoceptor", "entity2": "CGP20712A", "span1": [201, 221], "span2": [178, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10708": {"label": 1, "data": {"text": "The anticonvulsant action of dextromethorphan or dimemorfan was significantly counteracted by a selective sigma1 receptor antagonist BD 1047, suggesting that the anticonvulsant action of dextromethorphan or dimemorfan is, at least in part, related to sigma1 receptor-activated modulation of AP-1 transcription factors.", "entity1": "AP-1", "entity2": "dextromethorphan", "span1": [291, 295], "span2": [187, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6087": {"label": 2, "data": {"text": "However, amantadine induction of Fos in the striatum was unaffected by the dopamine D2 receptor antagonist, sulpiride.", "entity1": "Fos", "entity2": "amantadine", "span1": [33, 36], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1407": {"label": 8, "data": {"text": "Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxidenitric-oxide synthase in human astrocytes.", "entity1": "nitric-oxide synthase", "entity2": "nitric-oxide", "span1": [74, 95], "span2": [62, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11996": {"label": 1, "data": {"text": "It is also concluded that pyrethroid group of insecticide may cause hematological, biochemical, cytokine disturbances and possible mutagenic damage to the tissues.", "entity1": "cytokine", "entity2": "pyrethroid", "span1": [96, 104], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6411": {"label": 3, "data": {"text": "Isoproterenol (50 to 100 nmol/L) was used to mimic an increase in beta-adrenergic tone, d-sotalol (100 micromol/L) to block I(Kr) (LQT2 model), and ATX-II (20 nmol/L) to augment late I(Na) (LQT3 model).", "entity1": "ATX-II", "entity2": "Isoproterenol", "span1": [148, 154], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12391": {"label": 0, "data": {"text": "We apply DFTB in a QM/MM framework to perform vibrational analysis of buried aspartic acids in bacteriorhodopsin and channelrhodopsin-2.", "entity1": "channelrhodopsin-2", "entity2": "aspartic acids", "span1": [117, 135], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6170": {"label": 3, "data": {"text": "Unlike the nonselective MAO inhibitors, selegiline does not significantly potentiate tyramine-induced hypertension (the 'cheese effect') at the dosages (5 to 10 mg daily) used for the treatment of Parkinson's disease.", "entity1": "MAO", "entity2": "selegiline", "span1": [24, 27], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10696": {"label": 8, "data": {"text": "Ex vivo, lumiracoxib inhibited COX-1-derived thromboxane B(2) (TxB(2)) generation with an ID(50) of 33 mg kg(-1), whereas COX-2-derived production of prostaglandin E(2) (PGE(2)) in the lipopolysaccharide-stimulated rat air pouch was inhibited with an ID(50) value of 0.24 mg kg(-1).", "entity1": "COX-1", "entity2": "thromboxane B(2)", "span1": [31, 36], "span2": [45, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1911": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "capecitabine", "span1": [121, 123], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5901": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "low-density lipoproteins", "entity2": "fibric acids", "span1": [146, 170], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5945": {"label": 9, "data": {"text": "Pimozide and thioridazine had no effect on the estradiol binding properties of the MCF-7 ER, nor did pimozide interfere with the induction of progesterone receptors by estradiol.", "entity1": "progesterone receptors", "entity2": "pimozide", "span1": [142, 164], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14393": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "EGFR", "entity2": "NFD", "span1": [59, 63], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5376": {"label": 3, "data": {"text": "Rapamycin inhibits proteinase and selected peptidase activities of the catalytic core proteasome at low micromolar concentrations.", "entity1": "proteasome", "entity2": "Rapamycin", "span1": [86, 96], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4743": {"label": 3, "data": {"text": "Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects.", "entity1": "MLCK", "entity2": "genistin", "span1": [217, 221], "span2": [283, 291]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7096": {"label": 8, "data": {"text": "Proline oxidase (POX), a mitochondrial inner-membrane protein, catalyzes the rate-limiting oxidation of proline to pyrroline- 5-carboxylate (P5C).", "entity1": "Proline oxidase", "entity2": "pyrroline- 5-carboxylate", "span1": [0, 15], "span2": [115, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5652": {"label": 3, "data": {"text": "Arsenic trioxide (As(2)O(3)), which is used to treat acute promyelocytic leukemia, can cause LQTS type 2 (LQT2) by reducing the hERG current through the diversion of hERG trafficking to the cytoplasmic membrane.", "entity1": "hERG", "entity2": "As(2)O(3)", "span1": [128, 132], "span2": [18, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5185": {"label": 1, "data": {"text": "Dioscin-induced autophagy via ERK1/2 and JNK1/2 pathways may provide a protective mechanism for cell survival against dioscin-induced apoptosis to act as a cytoprotective reaction.", "entity1": "JNK1/2", "entity2": "Dioscin", "span1": [41, 47], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15103": {"label": 3, "data": {"text": "Upamostat (Mesupron\u00ae) is a new small molecule serine protease inhibitor.", "entity1": "serine protease", "entity2": "Upamostat", "span1": [46, 61], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15104": {"label": 3, "data": {"text": "Upamostat (Mesupron\u00ae) is a new small molecule serine protease inhibitor.", "entity1": "serine protease", "entity2": "Mesupron", "span1": [46, 61], "span2": [11, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15784": {"label": 8, "data": {"text": "A N,N-dimethylaminopropyl derivative showed promising inhibition of Trypanosoma cruzi OSC in combination with low cytotoxicity, and showed significant reduction of cholesterol biosynthesis in a human cell line.", "entity1": "Trypanosoma cruzi OSC", "entity2": "cholesterol", "span1": [68, 89], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9256": {"label": 2, "data": {"text": "These findings suggest that some of the deleterious effects of consumption of endophyte-infected tall fescue, which contains several ergot alkaloids including ergovaline, may be due to D2 dopamine receptor activation.", "entity1": "D2 dopamine receptor", "entity2": "ergot alkaloids", "span1": [185, 205], "span2": [133, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"455": {"label": 5, "data": {"text": "Pretreatment with tropisetron (1 microM), a 5-HT3 antagonist, ketanserin (10 microM), a 5-HT2 antagonist, thioperamide (10 microM), a histamine H3 antagonist, or phentolamine (10 microM), an alpha-adrenergic antagonist, however, had no effect.", "entity1": "5-HT3", "entity2": "tropisetron", "span1": [44, 49], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2090": {"label": 3, "data": {"text": "In conclusion, early application of amiloride inhibited u-PA activity in UVB-irradiated corneas as well as in tear fluid and diminished the development of corneal pathology.", "entity1": "u-PA", "entity2": "amiloride", "span1": [56, 60], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15753": {"label": 3, "data": {"text": "Our data showed that chronic ethanol over-activated CYP2E1 but suppressed HO-1 with concurrent hepatic oxidative damage, which was partially normalized by quercetin (100mg/kg.bw.).", "entity1": "HO-1", "entity2": "ethanol", "span1": [74, 78], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9584": {"label": 1, "data": {"text": "Oxytocin receptor binding and uterotonic activity of carbetocin and its metabolites following enzymatic degradation.", "entity1": "Oxytocin receptor", "entity2": "carbetocin", "span1": [0, 17], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2321": {"label": 9, "data": {"text": "Citalopram, which is devoid of affinity for the NET, exerted a significant reduction of immobility time in the NET-/- mice.", "entity1": "NET", "entity2": "Citalopram", "span1": [48, 51], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5703": {"label": 2, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [95, 100], "span2": [219, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1886": {"label": 1, "data": {"text": "I3A bound to PKC-alpha in the presence of phosphatidylserine with high affinity; however, under these assay conditions, little PKC isoform selectivity was observed.", "entity1": "PKC-alpha", "entity2": "I3A", "span1": [13, 22], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10739": {"label": 3, "data": {"text": "However, the flowcytometric analysis revealed that AZC and PCA decreased intracellular contents of CD3-zeta chain in these cells in dose dependent manner.", "entity1": "CD3-zeta chain", "entity2": "PCA", "span1": [99, 113], "span2": [59, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8994": {"label": 1, "data": {"text": "Enprofylline, a weak adenosine antagonist but potent inhibitor of cyclic AMP phosphodiesterase, did not alter ethanol's motor incoordination, further supporting involvement of brain adenosine receptor mechanism(s) in ethanol-adenosine interactions.", "entity1": "adenosine", "entity2": "ethanol", "span1": [225, 234], "span2": [217, 224]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14311": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "NQO1", "entity2": "DMF", "span1": [99, 103], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1951": {"label": 1, "data": {"text": "These results demonstrate that this receptor corresponds to the previously called \"P2t\" platelet receptor and show that the active metabolite of clopidogrel binds in a covalent manner to this receptor, thus explaining how it blocks the aggregating effect of ADP on platelets.", "entity1": "platelet receptor", "entity2": "ADP", "span1": [88, 105], "span2": [258, 261]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4941": {"label": 3, "data": {"text": "Moreover, protein and mRNA levels of DSS-induced proinflammatory cytokines in colon, including TNF-\u03b1, IL-1\u03b2, IL-18, IL-17A and IFN-\u03b3, were markedly suppressed by Fc11a-2.", "entity1": "IL-18", "entity2": "Fc11a-2", "span1": [109, 114], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3448": {"label": 1, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "DAT", "entity2": "(+/-)-Modafinil", "span1": [195, 198], "span2": [9, 24]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7160": {"label": 2, "data": {"text": "Since the suppression of AT1R expression was prevented by pretreatment with GW9662, a PPARgamma antagonist, PPARgamma should have participated in the process.", "entity1": "AT1R", "entity2": "GW9662", "span1": [25, 29], "span2": [76, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"447": {"label": 2, "data": {"text": "These results suggest that epinastine, although identified as a 5-HT antagonist, acts as a 5-HT1 agonist and that it inhibits the noncholinergic contraction in guinea-pig airways through stimulation of a prejunctional 5-HT1-like receptor, located to sensory nerves.", "entity1": "5-HT1-like receptor", "entity2": "epinastine", "span1": [218, 237], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14292": {"label": 3, "data": {"text": "The signaling of both Sox9 and Runx2, key regulators of chondrogenesis, was downregulated by VPA.", "entity1": "Runx2", "entity2": "VPA", "span1": [31, 36], "span2": [93, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"415": {"label": 1, "data": {"text": "The quinazoline antagonists, prazosin, doxazosin and alfuzosin displayed high affinity but were non selective for the three cloned human alpha 1 adrenoceptors.", "entity1": "human alpha 1 adrenoceptors", "entity2": "doxazosin", "span1": [131, 158], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4304": {"label": 1, "data": {"text": "Unable to reverse ERK1/2 phosphorylation, TXM-CB3 (NAc-Cys-Pro-Cys amide) appeared to function in part, through inhibiting ASK1-Trx dissociation.", "entity1": "ASK1", "entity2": "NAc-Cys-Pro-Cys amide", "span1": [123, 127], "span2": [51, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5915": {"label": 3, "data": {"text": "Acetylation of phenelzine at the N2 position presumably interferes with the inhibition of the transaminase enzymes for gamma-aminobutyric acid and alanine.", "entity1": "transaminase", "entity2": "phenelzine", "span1": [94, 106], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12986": {"label": 1, "data": {"text": "The C677T polymorphism of the methylene-tetrahydrofolate reductase (MTHFR) gene is associated with a reduction of catalytic activity and is suggested to modify cancer risk differently depending on folate status.", "entity1": "C677T", "entity2": "folate", "span1": [4, 9], "span2": [197, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"584": {"label": 3, "data": {"text": "Tomudex (ZD1694) is a specific antifolate-based thymidylate synthase inhibitor active in a variety of solid tumor malignancies.", "entity1": "thymidylate synthase", "entity2": "Tomudex", "span1": [48, 68], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13596": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "mazindol", "span1": [379, 383], "span2": [410, 418]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1663": {"label": 1, "data": {"text": "Inhibition of binding of the alpha2-receptor antagonist [3H]RX821002 to recombinant alpha2-receptors by etomidate was tested in human embryonic kidney (HEK293) cells in vitro.", "entity1": "alpha2-receptor", "entity2": "etomidate", "span1": [29, 44], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14689": {"label": 3, "data": {"text": "In the clinical study, small increases in the AUC(0-inf) of simvastatin [mean ratio (90% CI) of 1.34 (1.22, 1.48)] and rosuvastatin [mean ratio (90% CI) of 1.39 (1.30, 1.49)] were observed when co-administered with GSK1292263, which is consistent with an inhibitory effect on intestinal BCRP and CYP3A4.", "entity1": "CYP3A4", "entity2": "GSK1292263", "span1": [296, 302], "span2": [215, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13460": {"label": 3, "data": {"text": "Finally, PLA2 inhibitor methyl arachidonyl fluorophosphonate blocked the PUFA effects on COX-2 induction, promoter activity and arachidonic acid mobilization suggesting involvement of AA metabolites in PPAR activation.", "entity1": "COX-2", "entity2": "arachidonyl fluorophosphonate", "span1": [89, 94], "span2": [31, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12303": {"label": 2, "data": {"text": "These findings suggest that oral consumption of nicotine enhances the efficacy of nicotinic acetylcholine receptors.", "entity1": "nicotinic acetylcholine receptors", "entity2": "nicotine", "span1": [82, 115], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6540": {"label": 3, "data": {"text": "Chronic treatment with the NET inhibitor, desipramine (DMI), reduced NET levels in both control and Dbh -/- mice, demonstrating that NE is not required for the regulation of NET by antidepressant drugs.", "entity1": "NET", "entity2": "desipramine", "span1": [69, 72], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12238": {"label": 2, "data": {"text": "Using immunohistochemistry, the authors analyzed changes in CREB phosphorylation in the NAc after 5 days of cocaine, a short or long drug-free period, and a subsequent challenge injection.", "entity1": "CREB", "entity2": "cocaine", "span1": [60, 64], "span2": [108, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15009": {"label": 1, "data": {"text": "In agreement with these data, the exogenous treatment of SAH or inhibition of SAHH by specific siRNA or another type of inhibitor, 3-deazaadenosine (DAZA), similarly resulted in antitumorigenic responses, suppressive activity on Src, the alteration of actin cytoskeleton, and a change of the colocalization pattern between actin and Src.", "entity1": "Src", "entity2": "SAH", "span1": [333, 336], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4997": {"label": 2, "data": {"text": "Phenobarbital (PB), a typical CAR activator, increased the gene expression of HIF-target genes in the livers of mice, including erythropoietin, heme oxygenase-1 and vascular endothelial growth factor-a.", "entity1": "vascular endothelial growth factor-a", "entity2": "Phenobarbital", "span1": [165, 201], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11279": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "EC 2.1.2.1", "entity2": "glycine", "span1": [172, 182], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9732": {"label": 1, "data": {"text": "Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors.", "entity1": "h5-HT(1B)", "entity2": "Yohimbine", "span1": [127, 136], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1128": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "cardiac K(+) channel", "entity2": "sertindole", "span1": [143, 163], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"682": {"label": 8, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "GTP cyclohydrolase I", "entity2": "BH4", "span1": [56, 76], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"7993": {"label": 2, "data": {"text": "Furthermore, U0126 (an ERK1/2 inhibitor) significantly enhanced the ISO-induced the Bax/Bcl-2 ratio, the release of cytochrome c to the cytosol fraction, and the levels of cleaved caspase-3.", "entity1": "Bax", "entity2": "ISO", "span1": [84, 87], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4121": {"label": 1, "data": {"text": "Further, the inhibitors of insulin pathway prevented glucose uptake mediated by Tinospora cordifolia and palmatine which shows that the activity is majorly mediated through insulin pathway.", "entity1": "insulin", "entity2": "palmatine", "span1": [173, 180], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11319": {"label": 3, "data": {"text": "Ten IU/mL urokinase was also incubated with pooled plasma of stroke patients, that was previously oxidized with the singlet oxygen (1O2) donor chloramine T (CT), to destroy plasmatic PAI-1 and alpha2-antiplasmin.", "entity1": "plasmatic PAI-1", "entity2": "1O2", "span1": [173, 188], "span2": [132, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9665": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "human recombinant interleukin-5", "entity2": "FMLP", "span1": [132, 163], "span2": [212, 216]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13680": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "porcine TLR7", "entity2": "imiquimod", "span1": [83, 95], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5947": {"label": 1, "data": {"text": "We conclude that pimozide and thioridazine may be useful in the control of estradiol- and polypeptide hormone-induced growth of ER-positive and ER-negative human breast tumors.", "entity1": "polypeptide hormone", "entity2": "pimozide", "span1": [90, 109], "span2": [17, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9477": {"label": 4, "data": {"text": "M&B-28767, a putative EP3 agonist, and misoprostol, a putative EP2/EP3 agonist, also bound to this receptor with Ki values of 120 nM.", "entity1": "EP3", "entity2": "misoprostol", "span1": [67, 70], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14018": {"label": 1, "data": {"text": "Thiocolchicoside suppresses osteoclastogenesis induced by RANKL and cancer cells through inhibition of inflammatory pathways: a new use for an old drug.", "entity1": "RANKL", "entity2": "Thiocolchicoside", "span1": [58, 63], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15608": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "c-Jun", "entity2": "galangin", "span1": [88, 93], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8367": {"label": 1, "data": {"text": "The crystal structure of HSA complexed with fatty acid and acetyldiflunisal revealed that acetyldiflunisal binds to the IIA subdomain and that upon binding, it acetylates lysine 199.", "entity1": "HSA", "entity2": "fatty acid", "span1": [25, 28], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10068": {"label": 3, "data": {"text": "Omapatrilat, the prototypical vasopeptidase inhibitor, inhibits not only ACE but also neutral endopeptidase.", "entity1": "neutral endopeptidase", "entity2": "Omapatrilat", "span1": [86, 107], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10174": {"label": 3, "data": {"text": "Inhibition of human liver OATPs can explain the previously observed effects of rifamycin SV and rifampicin on hepatic organic anion elimination.", "entity1": "human liver OATPs", "entity2": "rifamycin SV", "span1": [14, 31], "span2": [79, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3571": {"label": 2, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u.", "entity1": "pIRS-1", "entity2": "MSG", "span1": [74, 80], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2746": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "ABL", "entity2": "BMS-354825", "span1": [146, 149], "span2": [67, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5145": {"label": 8, "data": {"text": "It has been claimed that hCTR1, the human high affinity copper transporter, is the major entry pathway for cDDP and related drugs via a mechanism that mimics copper.", "entity1": "hCTR1", "entity2": "cDDP", "span1": [25, 30], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3363": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-VGCCs", "entity2": "barbiturates", "span1": [153, 160], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1781": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1aAR", "entity2": "Tamsulosin", "span1": [40, 49], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2023": {"label": 5, "data": {"text": "CONCLUSION: Our results indicate that pranlukast inhibits IL-5 synthesis via a mechanism distinct from CysLTR1 antagonism.", "entity1": "CysLTR1", "entity2": "pranlukast", "span1": [103, 110], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12009": {"label": 2, "data": {"text": "The results showed that administration of AlCl3 resulted in a significant elevation in the levels of AchE activity, CRP, NF-\u03baB, and MCP-1 accompanied with a significant depletion in the Ach level.", "entity1": "AchE", "entity2": "AlCl3", "span1": [101, 105], "span2": [42, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11360": {"label": 1, "data": {"text": "The estimated plasma ziprasidone concentration associated with 50% maximal 5-HT(2) receptor occupancy was almost four times lower than that for D(2) receptor occupancy.", "entity1": "5-HT(2)", "entity2": "ziprasidone", "span1": [75, 82], "span2": [21, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10059": {"label": 3, "data": {"text": "Sulfasalazine, a potent suppressor of lymphoma growth by inhibition of the x(c)- cystine transporter: a new action for an old drug.", "entity1": "x(c)- cystine transporter", "entity2": "Sulfasalazine", "span1": [75, 100], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4228": {"label": 3, "data": {"text": "With the elevated doses of PhIP, malondialdehyde (MDA) contents, protein carbonyl (PCO) contents and DNA-protein crosslinks (DPC) coefficients were significantly raised in a dose-dependent manner; (3) PhIP at the doses of 10mg/kg and/or 15mg/kg significantly inhibited p16 mRNA and protein expression, whereas enhanced c-fos and c-jun expression relative to control.", "entity1": "p16", "entity2": "PhIP", "span1": [269, 272], "span2": [201, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4303": {"label": 8, "data": {"text": "Transport by OATP1B1 and OATP1B3 enhances the cytotoxicity of epigallocatechin 3-O-gallate and several quercetin derivatives.", "entity1": "OATP1B3", "entity2": "epigallocatechin 3-O-gallate", "span1": [25, 32], "span2": [62, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13116": {"label": 9, "data": {"text": "We failed to observe any significant activation of FAS promoter following exposure to the anti-metabolite 5-fluorouracil, the alkylating drug cisplatin, or the microtubule interfering-agents paclitaxel and vincristine.", "entity1": "FAS promoter", "entity2": "paclitaxel", "span1": [51, 63], "span2": [191, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13648": {"label": 0, "data": {"text": "The binding of U46619 to the PGIS protein was demonstrated by 1D NMR titration, and the significant perturbation of the chemical shifts of protons at C-11, H2C, and H20 of U46619 were observed upon U46619 binding to the engineered PGIS in a concentration-dependent manner.", "entity1": "PGIS", "entity2": "H2C", "span1": [29, 33], "span2": [156, 159]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9684": {"label": 3, "data": {"text": "6 In conclusion, HERG channel inhibition by cisapride exhibits features consistent with open and inactivated state binding and is sensitive to external potassium concentration.", "entity1": "HERG", "entity2": "cisapride", "span1": [17, 21], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5057": {"label": 1, "data": {"text": "These data provided a novel insight to the mechanisms of Rg1protective effects on A\u03b225-35-induced endothelial cells apoptosis, suggesting that GR-ERK signaling pathway might play an important role in it.", "entity1": "ERK", "entity2": "Rg1", "span1": [146, 149], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7864": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "mGlu1", "entity2": "lavendustin A", "span1": [40, 45], "span2": [316, 329]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15217": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "cyclooxygenase-2", "entity2": "clerosterol", "span1": [270, 286], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3461": {"label": 1, "data": {"text": "Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C.", "entity1": "DAT", "entity2": "cocaine", "span1": [23, 26], "span2": [124, 131]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4042": {"label": 3, "data": {"text": "In addition, we found that neoechinulin A significantly suppressed the production of neurotoxic inflammatory mediator tumour necrosis factor-\u03b1 (TNF-\u03b1), interleukin-1\u03b2 (IL-1\u03b2), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) in activated BV-2 cells.", "entity1": "interleukin-6", "entity2": "neoechinulin A", "span1": [176, 189], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6632": {"label": 5, "data": {"text": "Involvement of alpha(1)-adrenoceptors was established as mydriatic responses were inhibited by systemic administration of nonselective alpha-adrenoceptor antagonists, phentolamine (0.3-3 mg/kg) and phenoxybenzamine (0.03-0.3 mg/kg), as well as by the selective alpha(1)-adrenoceptor antagonist, prazosin (0.3 mg/kg).", "entity1": "alpha-adrenoceptor", "entity2": "phentolamine", "span1": [135, 153], "span2": [167, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5442": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "CA", "entity2": "tyrphostine", "span1": [149, 151], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10441": {"label": 7, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "SDH", "entity2": "pyridoxal 5'-phosphate", "span1": [0, 3], "span2": [54, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1626": {"label": 3, "data": {"text": "Structure-based design of aliskiren, a novel orally effective renin inhibitor.", "entity1": "renin", "entity2": "aliskiren", "span1": [62, 67], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13363": {"label": 1, "data": {"text": "Several genes involved with steroid metabolism also showed remarkable expression changes, including increased expression of 17beta-hydroxysteroid dehydrogenase-7 (HSD17beta7; involved in estradiol production) and decreased expression of HSD17beta5 (involved in testosterone production).", "entity1": "17beta-hydroxysteroid dehydrogenase-7", "entity2": "steroid", "span1": [124, 161], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12297": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Abcg5", "entity2": "Quercetin", "span1": [142, 147], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15822": {"label": 5, "data": {"text": "A series of structurally novel aryl ureas was derived from optimization of the HTS lead as selective histamine H3 receptor (H3R) antagonists.", "entity1": "H3R", "entity2": "aryl ureas", "span1": [124, 127], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1375": {"label": 1, "data": {"text": "Ntp opened K(IR)6.1/SUR1 channels normally silent in the absence of stimulatory Mg(-) nucleotide(s) and attenuated the coupling of high-affinity sulfonylurea binding with K(ATP) pore closure.", "entity1": "K(ATP)", "entity2": "sulfonylurea", "span1": [171, 177], "span2": [145, 157]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6504": {"label": 3, "data": {"text": "Pemetrexed disodium (ALIMTA) is a novel antimetabolite that inhibits at least three folate-dependent enzymes, thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase.", "entity1": "dihydrofolate reductase", "entity2": "ALIMTA", "span1": [132, 155], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15734": {"label": 4, "data": {"text": "Among 12 parabens with linear alkyl chains ranging in length from C1 to C12, heptylparaben (C7) and pentylparaben (C5) showed the most potent ER\u03b1 and ER\u03b2 agonistic activity in the order of 10(-7)M and 10(-8)M, respectively, and the activities decreased in a stepwise manner as the alkyl chain was shortened to C1 or lengthened to C12.", "entity1": "ER\u03b2", "entity2": "parabens", "span1": [150, 153], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3661": {"label": 3, "data": {"text": "Using paraoxon as a reference acetylcholinesterase (AChE) inhibitor, the objective of this study was to develop an adverse outcome pathway (AOP) that provided quantitative linkages across levels of biological organization during zebrafish embryogenesis.", "entity1": "AChE", "entity2": "paraoxon", "span1": [52, 56], "span2": [6, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13292": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "VEGFR", "entity2": "BAY43-9006", "span1": [300, 305], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11716": {"label": 0, "data": {"text": "Histone deacetylase 3 (Hdac3) is a nuclear enzyme that removes acetyl groups from lysine residues in histones and other proteins to epigenetically regulate gene expression.", "entity1": "histones", "entity2": "lysine", "span1": [101, 109], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2002": {"label": 0, "data": {"text": "[Trp(7)]GnRH-I and [Trp(8)]GnRH-I but not [His(5)]GnRH-I exhibit a higher potency in activating wild-type gmGnRHR-2 than native GnRH-I, indicating that amino acids at positions 7 and 8 of GnRHs are more important than position 5 for differential recognition by type I and type II GnRHRs.", "entity1": "GnRHs", "entity2": "amino acids", "span1": [188, 193], "span2": [152, 163]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14861": {"label": 2, "data": {"text": "Using surface biotinylation, we observed that treatment of N-38 neurons with estradiol or with a membrane impermeant estradiol elevated plasma membrane ER\u03b1 protein levels, indicating that membrane signaling increased receptor insertion into the cell membrane.", "entity1": "ER\u03b1", "entity2": "estradiol", "span1": [152, 155], "span2": [77, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"991": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "eNOS", "entity2": "BH(4)", "span1": [114, 118], "span2": [59, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"6314": {"label": 8, "data": {"text": "Activation of endothelial nitric oxide synthase (eNOS) results in the production of nitric oxide (NO) that mediates the vasorelaxing properties of endothelial cells.", "entity1": "eNOS", "entity2": "NO", "span1": [49, 53], "span2": [98, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3239": {"label": 1, "data": {"text": "Serotonin transporter (SERT) has been associated with drugs of abuse like d-methamphetamine (METH).", "entity1": "Serotonin transporter", "entity2": "METH", "span1": [0, 21], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15805": {"label": 2, "data": {"text": "When dual angiogenic growth factors (GFs), such as platelet-derived GF (PDGF) and vascular endothelial GF (VEGF), are encapsulated separately in the core and shell domains, respectively, the VEGF release rate is much greater than that of PDGF, and the difference of the cumulative release percentage between the two GFs is about 30% on day 7 with LMW core PLGA and more than 45% with HMW core PLGA.", "entity1": "VEGF", "entity2": "PLGA", "span1": [191, 195], "span2": [393, 397]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15624": {"label": 1, "data": {"text": "HP1\u03b1 responded only to BHA.", "entity1": "HP1\u03b1", "entity2": "BHA", "span1": [0, 4], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13799": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "Bcr", "entity2": "Imatinib mesylate", "span1": [114, 117], "span2": [60, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13183": {"label": 1, "data": {"text": "Chase studies with citalopram and methylphenidate demonstrated that this uptake is the result of preferential binding to the SERT.", "entity1": "SERT", "entity2": "citalopram", "span1": [125, 129], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4207": {"label": 3, "data": {"text": "These data suggest that inhibition of JAK2/STAT3 signaling is a novel mechanism of action for PTE during therapeutic intervention in osteosarcoma cancers.", "entity1": "STAT3", "entity2": "PTE", "span1": [43, 48], "span2": [94, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13563": {"label": 8, "data": {"text": "Our optimized L-citrulline production assay to measure DDAH activity correlated closely with the direct measure of the rate of asymmetric dimethylarginine consumption.", "entity1": "DDAH", "entity2": "dimethylarginine", "span1": [55, 59], "span2": [138, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6185": {"label": 2, "data": {"text": "Additional neuroendocrine experiments in a parallel group of rats revealed a dose-related increase in plasma prolactin and ACTH levels after i.v. mCPP, pointing to a general state of arousal in these mCPP-treated animals.", "entity1": "ACTH", "entity2": "mCPP", "span1": [123, 127], "span2": [146, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9346": {"label": 3, "data": {"text": "One group of experimental animals was treated with 5-lipoxygenase (5-LO) inhibitor, diethylcarbamazine (DEC, Sigma, St. Louis, Missouri) (50 mg/kg, i.v.", "entity1": "5-lipoxygenase", "entity2": "diethylcarbamazine", "span1": [51, 65], "span2": [84, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9124": {"label": 1, "data": {"text": "To determine the factors that influence the interaction between phenoxybenzamine and calmodulin, the binding of phenoxybenzamine to calmodulin was determined by equilibrium dialysis under a variety of experimental conditions.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [132, 142], "span2": [112, 128]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13094": {"label": 2, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "insulin", "entity2": "glinides", "span1": [118, 125], "span2": [150, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8815": {"label": 3, "data": {"text": "Activation of AMPK using AICAR resulted in STIM1 phosphorylation on serine residues and prevented PAR-1-induced Ca2+ entry.", "entity1": "PAR-1", "entity2": "AICAR", "span1": [98, 103], "span2": [25, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1952": {"label": 1, "data": {"text": "The antiaggregating effect of clopidogrel is attributed to an irreversible inhibition of ADP binding to a purinergic receptor present at the platelet surface.", "entity1": "purinergic receptor", "entity2": "clopidogrel", "span1": [106, 125], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12392": {"label": 1, "data": {"text": "The normal 46,XY genital virilization depends on androgen receptor gene expression, which is tissue specific, and requires normal androgen receptor mRNA levels in androgen sensitive tissues.", "entity1": "androgen receptor", "entity2": "androgen", "span1": [130, 147], "span2": [163, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11500": {"label": 8, "data": {"text": "Density functional theory calculations using the hybrid functional B3LYP have been performed to study the methyl transfer step in glycine N-methyltransferase (GNMT).", "entity1": "GNMT", "entity2": "methyl", "span1": [159, 163], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13334": {"label": 9, "data": {"text": "These results suggest that the effect of fluoxetine on the expression of hSERT is post-translational and has shown itself to be independent of PKC and PKA activity.", "entity1": "PKA", "entity2": "fluoxetine", "span1": [151, 154], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1778": {"label": 2, "data": {"text": "(3)H-CGP 12177A saturation binding, in the presence of propranolol, increased approximately 5-fold following overexpression of beta(1)-adrenoceptors.", "entity1": "beta(1)-adrenoceptors", "entity2": "(3)H-CGP 12177A", "span1": [127, 148], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10450": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "SDH", "entity2": "pyruvate", "span1": [0, 3], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13942": {"label": 4, "data": {"text": "Recent studies indicate that tamoxifen initially acts as an antagonist, but later functions as an ER agonist, promoting tumor growth.", "entity1": "ER", "entity2": "tamoxifen", "span1": [98, 100], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"931": {"label": 3, "data": {"text": "In conclusion, F3(d)Thd, an antimetabolite that inhibits TS activity, may be effective against 5-FU and/or FdUrd-resistance in colorectal cancer cells caused by amplification of TS and/or deletion of orotate phosphoribosyltransferase.", "entity1": "TS", "entity2": "F3(d)Thd", "span1": [57, 59], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6593": {"label": 3, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "D(2)", "entity2": "clozapine", "span1": [245, 249], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2085": {"label": 3, "data": {"text": "Am80 inhibited VEGF-induced phosphorylation of VEGF receptor.", "entity1": "VEGF receptor", "entity2": "Am80", "span1": [47, 60], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"537": {"label": 8, "data": {"text": "Because gastric AADC and COMT degrade levodopa, the drug is given with inhibitors of AADC (carbidopa or benserazide), and inhibitors of COMT will also enter clinical use.", "entity1": "AADC", "entity2": "levodopa", "span1": [16, 20], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10682": {"label": 5, "data": {"text": "In conclusion, TT-235 may inhibit the uterine response to oxytocin by decreasing oxytocin receptor numbers and oxytocin binding affinity, which might explain the prolonged oxytocin antagonist activity of TT-235.", "entity1": "oxytocin", "entity2": "TT-235", "span1": [172, 180], "span2": [204, 210]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15557": {"label": 1, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "GDNF", "entity2": "puerarin", "span1": [125, 129], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12727": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "AChE", "entity2": "ACh", "span1": [22, 26], "span2": [165, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11811": {"label": 2, "data": {"text": "Moreover, activities of caspase-3 and caspase-9 enzymes were also significantly higher in both kinds of cells exposed to SiO(2) NPs.", "entity1": "caspase-3", "entity2": "SiO(2)", "span1": [24, 33], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14877": {"label": 3, "data": {"text": "Additionally, in SH-SY5Y cells, MPP(+)-induced demethylation of phosphoprotein phosphatase 2A (PP2A), the master regulator of the cellular phosphoregulatory network, and cytotoxicity were ameliorated by EHT.", "entity1": "phosphoprotein phosphatase 2A", "entity2": "MPP(+)", "span1": [64, 93], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15225": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "inducible nitric oxide synthase", "entity2": "CLS", "span1": [296, 327], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9807": {"label": 8, "data": {"text": "Mitochondrially-bound dihydroorotate dehydrogenase (EC 1.3.99.11) catalyzes the fourth sequential step in the de novo synthesis of uridine monophosphate.", "entity1": "EC 1.3.99.11", "entity2": "uridine monophosphate", "span1": [52, 64], "span2": [131, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9267": {"label": 8, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "cyclic AMP", "span1": [50, 53], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3771": {"label": 3, "data": {"text": "Furthermore, RA significantly inhibited the CCl(4)-induced apoptosis, which was evident from decreased cleavage of caspase-3.", "entity1": "caspase-3", "entity2": "CCl(4)", "span1": [115, 124], "span2": [44, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3236": {"label": 1, "data": {"text": "Serotonin transporter (SERT) has been associated with drugs of abuse like d-methamphetamine (METH).", "entity1": "SERT", "entity2": "d-methamphetamine", "span1": [23, 27], "span2": [74, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14056": {"label": 3, "data": {"text": "Rectal mucosal samples from patients given aspirin had reduced phosphorylation of S6K1 and S6.", "entity1": "S6", "entity2": "aspirin", "span1": [91, 93], "span2": [43, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13101": {"label": 4, "data": {"text": "Glinides, sulfonylureas, and other acidified sulfonamides may be promising leads in the development of new PPARgamma agonists.", "entity1": "PPARgamma", "entity2": "sulfonylureas", "span1": [107, 116], "span2": [10, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12922": {"label": 8, "data": {"text": "Here, we show that at noncytotoxic concentrations, H(2)S was able to inhibit NO production and inducible NO synthase (iNOS) expression via heme oxygenase (HO-1) expression in RAW264.7 macrophages stimulated with lipopolysaccharide (LPS).", "entity1": "inducible NO synthase", "entity2": "NO", "span1": [95, 116], "span2": [77, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6815": {"label": 2, "data": {"text": "These results suggest that pitavastatin efficiently increases apoA-I in the culture medium of HepG2 cells by promoting apoA-I production through inhibition of HMG-CoA reductase and suppression of Rho activity and by protecting apoA-I from catabolism through ABCA1 induction and lipidation of apoA-I.", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [119, 125], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5765": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "UCHL- 1", "entity2": "MPTP", "span1": [286, 293], "span2": [140, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5985": {"label": 1, "data": {"text": "Fibrinogen appears to exert its stimulatory properties mainly through effects on the enzyme, two-chain rec-t-PA, with a Ka of approximately 3.7 microM in activation systems containing physiological levels of Cl-.", "entity1": "t-PA", "entity2": "Cl-", "span1": [107, 111], "span2": [208, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6206": {"label": 1, "data": {"text": "Furthermore, since they have equipotent anticonvulsant effects and similar binding affinities to sigma-1 receptors, the very low affinity of DF at PCP sites may suggest that acting on the PCP sites may not be the requisite for mediating the anticonvulsant activity of these DM analogs.", "entity1": "sigma-1 receptors", "entity2": "DF", "span1": [97, 114], "span2": [141, 143]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13492": {"label": 1, "data": {"text": "The LS/SS genotype of the promoter for SLC6A4 was associated with enhanced weight loss with sibutramine.", "entity1": "SLC6A4", "entity2": "sibutramine", "span1": [39, 45], "span2": [92, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7937": {"label": 9, "data": {"text": "Structure-activity relationship analysis of highly potent subtype-selective ligands (MT(2) EC(50) 10-90 pM) revealed that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT(2) potency and at the same time decreased MT(1) potency.", "entity1": "MT(1)", "entity2": "benzyloxyl", "span1": [274, 279], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10973": {"label": 3, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "RAR-gamma", "entity2": "retinoid", "span1": [40, 49], "span2": [154, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3404": {"label": 3, "data": {"text": "To further characterize the inhibitory mechanisms of PSE at the transcriptional level, we examined the transcriptional activities of nuclear factor kappa B (NF-kappaB), nuclear factor of activated T cells (NFAT), and activator protein-1 (AP-1) transcription factors and found that PSE inhibited NF-kappaB-dependent transcriptional activity without affecting either the phosphorylation, the degradation of the cytoplasmic NF-kappaB inhibitory protein, IkappaBalpha or the DNA-binding activity.", "entity1": "NF-kappaB", "entity2": "PSE", "span1": [295, 304], "span2": [281, 284]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4002": {"label": 3, "data": {"text": "Further, compared with vemurafenib, another BRAF(V600E) inhibitor, dabrafenib showed greater brain penetration with a similar dose.", "entity1": "BRAF", "entity2": "vemurafenib", "span1": [44, 48], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5839": {"label": 3, "data": {"text": "In contrast, inhibition of rat liver squalene epoxidase only occurs at higher drug concentrations (Ki = 77 microM), and is competitive with squalene.", "entity1": "rat liver squalene epoxidase", "entity2": "squalene", "span1": [27, 55], "span2": [140, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5474": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "MPA", "span1": [106, 127], "span2": [247, 250]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6537": {"label": 3, "data": {"text": "Lovastatin, a specific inhibitor of HMG-CoA reductase, induces a pronounced apoptotic response in a specific subset of tumor types, including HNSCC and CC.", "entity1": "HMG-CoA reductase", "entity2": "Lovastatin", "span1": [36, 53], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15008": {"label": 1, "data": {"text": "In agreement with these data, the exogenous treatment of SAH or inhibition of SAHH by specific siRNA or another type of inhibitor, 3-deazaadenosine (DAZA), similarly resulted in antitumorigenic responses, suppressive activity on Src, the alteration of actin cytoskeleton, and a change of the colocalization pattern between actin and Src.", "entity1": "actin", "entity2": "SAH", "span1": [323, 328], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14707": {"label": 3, "data": {"text": "Moreover, icariin treatment inhibited the phosphorylations of STAT1 and STAT3 in CD4(+) T cells, which were the crucial transcription factors for Th1 and Th17 respectively.", "entity1": "STAT3", "entity2": "icariin", "span1": [72, 77], "span2": [10, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2483": {"label": 3, "data": {"text": "CP-690550, a JAK3 inhibitor is currently in phase II clinical trials.FK778, is a synthetic malononitrilamide that targets the critical enzyme of the de novo pyrimidine synthesis, dihydroorotic acid dehydrogenase, and receptor-associated tyrosine kinases has completed phase II trials.", "entity1": "JAK3", "entity2": "CP-690550", "span1": [13, 17], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8858": {"label": 2, "data": {"text": "Indoxyl 3-sulfate stimulates Th17 differentiation enhancing phosphorylation of c-Src and STAT3 to worsen experimental autoimmune encephalomyelitis.", "entity1": "c-Src", "entity2": "Indoxyl 3-sulfate", "span1": [79, 84], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11152": {"label": 8, "data": {"text": "From these data, it is inferred that both the SERT and NET contribute to the active clearance of exogenously applied 5-HT in the dentate gyrus.", "entity1": "SERT", "entity2": "5-HT", "span1": [46, 50], "span2": [117, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"758": {"label": 1, "data": {"text": "Mutations of another voltage-gated chloride channel, CLC-Kb, are associated with a form of Bartter's syndrome, whereas other forms of Bartter's syndrome are caused by mutations in the bumetanidebumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC2) and the potassium channel, ROMK.", "entity1": "bumetanide-sensitive sodium-potassium-chloride cotransporter", "entity2": "bumetanide", "span1": [194, 254], "span2": [184, 194]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"8973": {"label": 5, "data": {"text": "Using the alpha 1-adrenoceptor subtype-selective antagonists chlorethylclonidine (CEC), WB4101, and 5-methyl-urapidil, we have examined the possible heterogeneity in the alpha 1-adrenoceptor populations in rabbit aorta.", "entity1": "alpha 1-adrenoceptor", "entity2": "CEC", "span1": [10, 30], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"89": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "phenylalanine 4-monooxygenase", "entity2": "adrenaline", "span1": [81, 110], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9904": {"label": 1, "data": {"text": "It is proposed that the UCP-3 gene is regulated in skeletal muscle during lactation in response to changes in circulating free fatty acids by mechanisms involving activation of PPARs.", "entity1": "UCP-3", "entity2": "fatty acids", "span1": [24, 29], "span2": [127, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3592": {"label": 3, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "p70-S6 kinase", "entity2": "Wogonoside", "span1": [86, 99], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11596": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "CBS", "entity2": "H(2)S", "span1": [140, 143], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11227": {"label": 1, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "SUR1", "entity2": "mitiglinide", "span1": [104, 108], "span2": [59, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2156": {"label": 3, "data": {"text": "Thalidomide reduced COX-2 expression accompanied by a decrease of bcl-2 protein, TNFalpha, VEGF, GSH and an increased cytochrome c, but had no effect on that of COX-1, in MCF-7 and HL-60.", "entity1": "COX-2", "entity2": "Thalidomide", "span1": [20, 25], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6683": {"label": 2, "data": {"text": "The Ca(2+) response of hVR1-transfected HEK293 cells to the endogenous VR1 agonist N-arachidonoyl-dopamine was potentiated by low pH.", "entity1": "hVR1", "entity2": "N-arachidonoyl-dopamine", "span1": [23, 27], "span2": [83, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4257": {"label": 2, "data": {"text": "Repression of farnesyltransferase (FNTA) by siRNA and the enzyme inhibitor manumycin A caused elevation of ApoA-I secretion from hepatocytes and from transgenic mice expressing hApoA-I and cholesterol ester transfer protein transgenes.", "entity1": "hApoA-I", "entity2": "manumycin A", "span1": [177, 184], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10952": {"label": 8, "data": {"text": "These results provide biochemical evidence of a H(+)-coupled and saturable transport system, presumed to be a low-affinity monocarboxylate transporter MCT4 or other unknown H(+)-coupled monocarboxylate transport system, for nicotinate in rat cerebrocortical astrocytes.", "entity1": "MCT4", "entity2": "nicotinate", "span1": [151, 155], "span2": [224, 234]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2480": {"label": 1, "data": {"text": "Fingolimod (FTY720), a synthetic sphingosine phosphate receptor modulator that reduces the recirculation of lymphocytes to blood and peripheral tissues including inflammatory lesions and graft sites is undergoing phase III trials.", "entity1": "sphingosine phosphate receptor", "entity2": "FTY720", "span1": [33, 63], "span2": [12, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11816": {"label": 1, "data": {"text": "In the present study, the extent to which six substituted quercetin derivatives (1-6) affected the function of OATP1B1 and OATP1B3 was investigated.", "entity1": "OATP1B3", "entity2": "quercetin", "span1": [123, 130], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9139": {"label": 1, "data": {"text": "Certain analogs of caffeine in which the methyl group at the 1- or 7-position is replaced with a propargyl or propyl group display selectivity for A2 receptors.", "entity1": "A2 receptors", "entity2": "caffeine", "span1": [147, 159], "span2": [19, 27]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2419": {"label": 8, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "arginases", "entity2": "NO", "span1": [21, 30], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13435": {"label": 2, "data": {"text": "Elevated extracellular D-glucose increases transforming growth factor beta1 (TGF-beta1) release from human umbilical vein endothelium (HUVEC).", "entity1": "transforming growth factor beta1", "entity2": "D-glucose", "span1": [43, 75], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9901": {"label": 1, "data": {"text": "Conversely, when mice are fed a high-fat diet after parturition, the downregulation of UCP-3 mRNA and UCP-3 protein levels due to lactation is partially reversed, as is the reduction in serum free fatty acid levels.", "entity1": "UCP-3", "entity2": "fatty acid", "span1": [87, 92], "span2": [197, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"11541": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "dexamethasone", "span1": [86, 89], "span2": [255, 268]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8370": {"label": 3, "data": {"text": "The cyclooxygenase-2 inhibitor, diflunisal, is used in the clinic for its anti-inflammatory activity.", "entity1": "cyclooxygenase-2", "entity2": "diflunisal", "span1": [4, 20], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5897": {"label": 1, "data": {"text": "Probucol acts by a newly described mechanism, i.e. accelerating reverse transport of cholesteryl esters from high-density lipoproteins to lower-density lipoproteins.", "entity1": "high-density lipoproteins", "entity2": "Probucol", "span1": [109, 134], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7922": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "carboplatin", "span1": [27, 32], "span2": [143, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3411": {"label": 3, "data": {"text": "NFAT cooperates with c-Jun, a compound of the AP-1 complex, to activate target genes, and we also found that PSE inhibited both JNK activation and AP-1 transcriptional activity.", "entity1": "JNK", "entity2": "PSE", "span1": [128, 131], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12705": {"label": 1, "data": {"text": "However, when coapplied with 10 micro m GABA, ivermectin potentiated the GABA-evoked current of the GAB-1/HG1A receptor, but attenuated the GABA response of the GAB-1/HG1E receptor.", "entity1": "GAB-1", "entity2": "GABA", "span1": [100, 105], "span2": [73, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7408": {"label": 8, "data": {"text": "Asparagine secretion by MSCs was directly related to their ASNS expression levels, suggesting a mechanism - increased concentrations of asparagine in the leukemic cell microenvironment - for the protective effects we observed.", "entity1": "ASNS", "entity2": "Asparagine", "span1": [59, 63], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1089": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "parathion", "span1": [242, 262], "span2": [175, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2300": {"label": 5, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "AH 6809", "span1": [258, 261], "span2": [249, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15915": {"label": 8, "data": {"text": "The Intermediate-conductance Calcium-activated Potassium Channel KCa3.1 Regulates Vascular Smooth Muscle Cell Proliferation via Controlling Calcium-dependent Signaling.", "entity1": "Intermediate-conductance Calcium-activated Potassium Channel KCa3.1", "entity2": "Calcium", "span1": [4, 71], "span2": [140, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4994": {"label": 2, "data": {"text": "Cobalt chloride, a typical HIF activator, induced the gene expression of CAR-target genes, including cyp2b9 and cyp2b10, an accumulation of nuclear CAR and an increase in the PB-responsive enhancer module-mediated transactivation in the mouse liver.", "entity1": "HIF", "entity2": "Cobalt chloride", "span1": [27, 30], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9327": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "NMDA", "span1": [72, 77], "span2": [213, 217]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13281": {"label": 9, "data": {"text": "The imatinib-resistant KIT(D816V) mutant, associated with systemic mastocytosis, was found to be resistant to sorafenib.", "entity1": "D816V", "entity2": "sorafenib", "span1": [27, 32], "span2": [110, 119]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11468": {"label": 1, "data": {"text": "Apolipoprotein E was chemically bound via linkers to loperamide-loaded HSA-NP.", "entity1": "Apolipoprotein E", "entity2": "loperamide", "span1": [0, 16], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7225": {"label": 1, "data": {"text": "GnRH-induced Pyk2 activation opposed the association of Hic-5 with androgen receptor as overexpression of a dominant negative Pyk2 enhanced the GnRH-induced nuclear translocation of a green fluorescent protein-tagged human androgen receptor.", "entity1": "human androgen receptor", "entity2": "GnRH", "span1": [217, 240], "span2": [144, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3950": {"label": 8, "data": {"text": "These observations suggest that uptake of phenformin into liver mitochondria is at least partly mediated by OCTN1 and functionally relevant to its inhibition potential of complex I respiration.", "entity1": "OCTN1", "entity2": "phenformin", "span1": [108, 113], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13797": {"label": 3, "data": {"text": "The most successful example of kinase blockers is Imatinib (Imatinib mesylate, Gleevec, STI571), the inhibitor of Bcr/Abl oncoprotein, which has become a first-line therapy for chronic myelogenous leukemia.", "entity1": "Abl", "entity2": "Imatinib", "span1": [118, 121], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3519": {"label": 3, "data": {"text": "We have previously reported that TZDs reduce estrogen synthesis by inhibiting aromatase activity in human granulosa cells (HGC).", "entity1": "aromatase", "entity2": "TZDs", "span1": [78, 87], "span2": [33, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5453": {"label": 3, "data": {"text": "In addition, pretreatment with Z-Val-Ala-Asp-fluoromethylketone (Z-VAD-fmk), a broad spectrum of caspase inhibitor, could not rescue apoptotic cells from ClpP toxicity.", "entity1": "caspase", "entity2": "Z-Val-Ala-Asp-fluoromethylketone", "span1": [97, 104], "span2": [31, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15650": {"label": 1, "data": {"text": "Excess of cholesterol converted into 24OHC may up-regulate ApoE synthesis which is a scavenger for A\u03b2 and Tau.", "entity1": "A\u03b2", "entity2": "cholesterol", "span1": [99, 101], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"827": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "17-phenyl-trinor-PGE2", "span1": [258, 275], "span2": [309, 330]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1377": {"label": 3, "data": {"text": "Micromolar Ntp dose-dependently increased the mean open channel probability in ligand-free solution (P(O(max))) and attenuated the ATP inhibition of K(IR)6.2/SUR1, but had no effect on homomeric K(IR)6.2 channels.", "entity1": "SUR1", "entity2": "ATP", "span1": [158, 162], "span2": [131, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10246": {"label": 8, "data": {"text": "Substrate specificity using lysates of oxidase-transfected HEK-293 cells revealed that the newly identified oxidase strongly favoured spermine over N (1)-acetylspermine and that it failed to act on N (1)-acetylspermidine, spermidine or the preferred PAO substrate, N (1), N (12)-diacetylspermine.", "entity1": "oxidase", "entity2": "spermine", "span1": [108, 115], "span2": [134, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5682": {"label": 3, "data": {"text": "HZ mice are also more sensitive to the peripheral application of the selective AChE inhibitor donepezil or the mixed inhibitor physostigmine; extracellular ACh levels rise significantly after administration of both drugs; also glucose levels are moderately increased indicating potentially non-cholinergic effects of donepezil.", "entity1": "AChE", "entity2": "donepezil", "span1": [79, 83], "span2": [317, 326]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15172": {"label": 2, "data": {"text": "GnRH pulse frequency-dependent stimulation of FSH\u03b2 transcription is mediated via activation of PKA and CREB.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [46, 50], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10968": {"label": 1, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "RAR-beta", "entity2": "retinoic acid", "span1": [27, 35], "span2": [77, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"116": {"label": 1, "data": {"text": "Finally, the effects of felodipine and the three analogues on two processes which are dependent on myosin phosphorylation were examined, namely the actin-activated Mg2+-ATPase activity of myosin and the assembly of myosin filaments.", "entity1": "myosin", "entity2": "felodipine", "span1": [188, 194], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8877": {"label": 1, "data": {"text": "TCDD treatment of the cells largely prevented the activation of eukaryotic translation initiation factor 4E-binding protein 1, a regulator of translation initiation and substrate of the mammalian target of rapamycin (mTOR).", "entity1": "mammalian target of rapamycin", "entity2": "TCDD", "span1": [186, 215], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3421": {"label": 9, "data": {"text": "In this study, our biochemical analyses revealed that the introduction of the T790M mutation confers gefitinib resistance on the G719S mutant.", "entity1": "G719S", "entity2": "gefitinib", "span1": [129, 134], "span2": [101, 110]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15394": {"label": 0, "data": {"text": "Furthermore, we demonstrated that p14ARF binds to both the N-terminal domain and the ligand-binding domain of AR, and the human double minute 2 (HDM2)-binding motif of p14ARF is required for the interaction of p14ARF and AR proteins.", "entity1": "AR", "entity2": "N", "span1": [110, 112], "span2": [59, 60]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14581": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "PRT062607", "span1": [103, 106], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5895": {"label": 3, "data": {"text": "Mechanism of the irreversible inactivation of mouse ornithine decarboxylase by alpha-difluoromethylornithine.", "entity1": "mouse ornithine decarboxylase", "entity2": "alpha-difluoromethylornithine", "span1": [46, 75], "span2": [79, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9631": {"label": 1, "data": {"text": "Analogous to the antiandrogens, bicalutamide and hydroxyflutamide, binding of estramustine phosphate metabolites to the androgen receptor was observed.", "entity1": "androgen receptor", "entity2": "bicalutamide", "span1": [120, 137], "span2": [32, 44]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4398": {"label": 0, "data": {"text": "The M6P (mannose 6-phosphate)/IGF2R (insulin-like growth factor II receptor) interacts with a variety of factors that impinge on tumour invasion and metastasis.", "entity1": "IGF2R", "entity2": "M6P", "span1": [30, 35], "span2": [4, 7]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4572": {"label": 2, "data": {"text": "The values of mean corpuscular hemoglobin concentration and mean corpuscular hemoglobin increased in the STX group.", "entity1": "hemoglobin", "entity2": "STX", "span1": [31, 41], "span2": [105, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7222": {"label": 1, "data": {"text": "Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5.", "entity1": "Hic-5", "entity2": "Gonadotropin-releasing hormone", "span1": [172, 177], "span2": [0, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1985": {"label": 3, "data": {"text": "Mibefradil blocked currents of all Na+ channel isoforms with similar affinity and a dependence on holding potential, and drug off-rate was slowed at depolarized potentials (k(off) was 0.024/s at -130 mV and 0.007/s at -100 mV for Nav1.5).", "entity1": "Nav1.5", "entity2": "Mibefradil", "span1": [230, 236], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6098": {"label": 3, "data": {"text": "bolus); finally, 8 rabbits received aurintrycarboxilic acid (ATA), an inhibitor of platelet glycoprotein Ib/von Willebrand factor interaction (10 mg/kg i.v.", "entity1": "glycoprotein Ib", "entity2": "aurintrycarboxilic acid", "span1": [92, 107], "span2": [36, 59]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4806": {"label": 3, "data": {"text": "The modification of the inhibitor scaffold of 1 and 2 from a dihydroquinolinone core to a tetrahydropyrazolopyridinone core led to discovery of a new series of potent KAT II inhibitors with excellent physicochemical properties.", "entity1": "KAT II", "entity2": "dihydroquinolinone", "span1": [167, 173], "span2": [61, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9186": {"label": 1, "data": {"text": "Penicillin-binding proteins and role of amdinocillin in causing bacterial cell death.", "entity1": "Penicillin-binding proteins", "entity2": "amdinocillin", "span1": [0, 27], "span2": [40, 52]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3383": {"label": 6, "data": {"text": "Benzodiazepines (BDZs) depress neuronal excitability via positive allosteric modulation of inhibitory GABA(A) receptors (GABA(A)R).", "entity1": "GABA(A)R", "entity2": "Benzodiazepines", "span1": [121, 129], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"6252": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "human serotonin transporter", "entity2": "chlorpromazine", "span1": [58, 85], "span2": [122, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5388": {"label": 3, "data": {"text": "Methylphenidate, an inhibitor of dopamine and norepinephrine transporters (DAT and NET, respectively), is a standard treatment for ADHD.", "entity1": "dopamine and norepinephrine transporters", "entity2": "Methylphenidate", "span1": [33, 73], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"466": {"label": 4, "data": {"text": "(+/-)-Tamsulosin effectively antagonized the positive inotropic effect of phenylephrine even after inactivation of alpha 1B-adrenoceptors by treatment with chlorethylclonidine, which is an indication that the (+/-)-tamsulosin-sensitive subtype belongs to a class resistant to chlorethylclonidine.", "entity1": "alpha 1B-adrenoceptors", "entity2": "phenylephrine", "span1": [115, 137], "span2": [74, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"339": {"label": 3, "data": {"text": "The folding rate for wild-type RNase A is faster in the presence of the inhibitor 2'CMP than in its absence, indicating that the transition-state structure in the rate-determining step is stabilized by 2'CMP.", "entity1": "RNase A", "entity2": "2'CMP", "span1": [31, 38], "span2": [82, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9134": {"label": 1, "data": {"text": "The following was demonstrated in the rat and confirmed in man: interaction of Anandron with the prostatic androgen receptor, antiandrogen activity against testosterone (in particular against the early transient rise induced by LHRH analogs) and adrenal androgens.", "entity1": "prostatic androgen receptor", "entity2": "Anandron", "span1": [97, 124], "span2": [79, 87]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14058": {"label": 3, "data": {"text": "RESULTS: Aspirin reduced mTOR signaling in CRC cells by inhibiting the mTOR effectors S6K1 and 4E-BP1.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [71, 75], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1029": {"label": 1, "data": {"text": "We thus confirm a possible role for p53 protein in modulating topoisomerase I activity but conclude that the major molecular determinants of topotecan sensitivity in glioma cells await identification.", "entity1": "p53", "entity2": "topotecan", "span1": [36, 39], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7774": {"label": 5, "data": {"text": "Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-\u03b1 pharmacology.", "entity1": "IAP", "entity2": "GDC-0152", "span1": [35, 38], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12484": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO3", "entity2": "methimazole", "span1": [81, 85], "span2": [103, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15425": {"label": 1, "data": {"text": "Cell-pre-incubation with bradykinin induced changes in ABCG expression levels after 7-ketostigmasterol-incubation; however, the energetic metabolism inhibition reduced NPC1L1 expression only in 7-ketocholesterol-incubated cells.", "entity1": "ABCG", "entity2": "7-ketostigmasterol", "span1": [55, 59], "span2": [84, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3992": {"label": 3, "data": {"text": "In this study, we found that BGG showed low cytotoxicity in Raw264.7 murine macrophages and effectively inhibited AR activity as measured by a decrease in sorbitol accumulation.", "entity1": "AR", "entity2": "BGG", "span1": [114, 116], "span2": [29, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10262": {"label": 8, "data": {"text": "Amongst the three OCTs expressed in the SCG, OCT3 best fits the profile of substrates and antagonists that cause trans-stimulation and trans-inhibition, respectively, of [3H]-MPP+ release.", "entity1": "OCTs", "entity2": "[3H]-MPP+", "span1": [18, 22], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13582": {"label": 5, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "NMDA receptor", "entity2": "D-AP5", "span1": [188, 201], "span2": [166, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15862": {"label": 0, "data": {"text": "Molecular docking studies were performed with Human Serum Albumin (HSA: PDB 1E78), showing binding pattern with amino acid residues Arg218, Arg222 and Lys444, identifies the ligand-HSA interaction for the transportation affinity of the ligand at the specific site of the target.", "entity1": "HSA", "entity2": "Arg", "span1": [67, 70], "span2": [140, 143]}, "weak_labels": [0, -1, -1, 1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14299": {"label": 3, "data": {"text": "\u03b1-TOCO plus a pancaspase inhibitor completely abolished AMD/TNF-induced cytotoxicity.", "entity1": "pancaspase", "entity2": "\u03b1-TOCO", "span1": [14, 24], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"105": {"label": 5, "data": {"text": "The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosages of the nonsedating histamine H1-receptor antagonists terfenadine, astemizole, loratadine, and acrivastine are reviewed.", "entity1": "histamine H1-receptor", "entity2": "loratadine", "span1": [114, 135], "span2": [173, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10769": {"label": 2, "data": {"text": "Treatment of head and neck squamous carcinoma cells with clinically relevant concentrations of imatinib-induced changes in cell morphology and growth similar to changes associated with epidermal growth factor receptor (EGFR) activation.", "entity1": "epidermal growth factor receptor", "entity2": "imatinib", "span1": [185, 217], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7360": {"label": 1, "data": {"text": "Since glial cells were shown to express significant levels of ERalpha, we investigated a possible indirect mechanism of estrogen-mediated neuroprotection through glial cell interaction.", "entity1": "ERalpha", "entity2": "estrogen", "span1": [62, 69], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2108": {"label": 1, "data": {"text": "On the basis of FIP1L1-PDGFRa fusion gene hypereosinophilic syndrome would be classified as a clonal disease and in the FIP1L1-PDGFRa positive cases the tyrosine kinase inhibitor imatinib mesylate (Glivec) would be effective.", "entity1": "FIP1L1", "entity2": "imatinib mesylate", "span1": [120, 126], "span2": [179, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6547": {"label": 9, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "F1004A", "entity2": "cilostazol", "span1": [26, 32], "span2": [196, 206]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13431": {"label": 2, "data": {"text": "High D-glucose increases L-arginine transport and eNOS expression following TbetaRII activation by TGF-beta1 involving p42/44(mapk) and Smad2 in HUVEC.", "entity1": "Smad2", "entity2": "D-glucose", "span1": [136, 141], "span2": [5, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9160": {"label": 3, "data": {"text": "Most reducing cofactors for the peroxidase protect PHS and prostacyclin synthase from inactivation by hydroperoxides.", "entity1": "PHS", "entity2": "hydroperoxides", "span1": [51, 54], "span2": [102, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"3123": {"label": 8, "data": {"text": "alpha-Tocopherol transfer protein (alpha-TTP), the product of the gene responsible for familial isolated vitamin E deficiency, plays an important role in maintaining the plasma alpha-tocopherol level by mediating the secretion of alpha-tocopherol by the liver.", "entity1": "alpha-TTP", "entity2": "alpha-tocopherol", "span1": [35, 44], "span2": [230, 246]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11818": {"label": 8, "data": {"text": "Cytotoxicity assays demonstrated that epigallocatechin 3-O-gallate (EGCG) and most of compounds 1-6 killed preferentially OATP-expressing CHO cells.", "entity1": "OATP", "entity2": "EGCG", "span1": [122, 126], "span2": [68, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4744": {"label": 3, "data": {"text": "Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects.", "entity1": "ATPase", "entity2": "Genistin", "span1": [148, 154], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11106": {"label": 1, "data": {"text": "Opioid receptors are the membrane proteins that mediate the pain-relieving effect of opioid drugs, such as morphine and fentanyl as well as endogenous opioid peptides enkephalins and endorphins.", "entity1": "Opioid receptors", "entity2": "fentanyl", "span1": [0, 16], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1651": {"label": 5, "data": {"text": "The 5-HT(2B/2C)-receptor antagonist SB 206553 facilitated hyperglycemia induced by clomipramine, although the 5-HT(2A)-receptor antagonist ketanserin was without effect.", "entity1": "5-HT(2B/2C)-receptor", "entity2": "SB 206553", "span1": [4, 24], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14935": {"label": 8, "data": {"text": "Phosphodiesterase type 5 (PDE5) mediates the degradation of cGMP in a variety of tissues including brain.", "entity1": "PDE5", "entity2": "cGMP", "span1": [26, 30], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1271": {"label": 9, "data": {"text": "the NOS-catalyzed oxidation of NADPH in the absence of substrate or pterin that does not result in NO production.", "entity1": "NOS", "entity2": "NO", "span1": [4, 7], "span2": [99, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, 8, -1, 9]},
	"10671": {"label": 9, "data": {"text": "Antag I and Antag II did not alter oxytocin receptor number or binding affinity significantly at each time point studied compared with controls.", "entity1": "oxytocin receptor", "entity2": "Antag II", "span1": [35, 52], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12792": {"label": 1, "data": {"text": "Genetic variants at the beta(2)-adrenergic receptor (beta(2)AR) may modify asthma severity and albuterol responsiveness.", "entity1": "beta(2)AR", "entity2": "albuterol", "span1": [53, 62], "span2": [95, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12026": {"label": 1, "data": {"text": "The specificity of progestagens for the progesterone receptors in the cytosol fraction of MCF-7 cells was similar to that for progesterone receptors in human and rabbit myometrial cytosol but different from that for the progesterone receptor in rat myometrial cytosol.", "entity1": "progesterone receptor", "entity2": "progestagens", "span1": [220, 241], "span2": [19, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3": {"label": 4, "data": {"text": "Labetalol (> or = 3 x 10(-8) M) and dilevalol (> or = 10(-8) M) caused surmountable antagonism of the isoprenaline responses of the atria and the pA2 values were 8.60 and 8.98 at the beta 1-adrenoceptors of the rat left atria and 7.90 and 8.31, respectively, on the guinea-pig left atria which has functional beta 1- and beta 2-adrenoceptors.", "entity1": "beta 1-adrenoceptors", "entity2": "isoprenaline", "span1": [183, 203], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3971": {"label": 1, "data": {"text": "To control for possible interactions between the expression of the estrogen receptor genes and other learning-related steroid receptors, androgen receptors (AR), corticosterone-binding glucocorticoid receptors (GR) and mineralocorticoid receptors (MR) were also measured.", "entity1": "GR", "entity2": "corticosterone", "span1": [211, 213], "span2": [162, 176]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12989": {"label": 1, "data": {"text": "The main molecular target of azole antifungals is the cytochrome P-450 protein Erg11p/Cyp51p.", "entity1": "cytochrome P-450", "entity2": "azole", "span1": [54, 70], "span2": [29, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10538": {"label": 1, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "blr1", "entity2": "RA", "span1": [420, 424], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13196": {"label": 8, "data": {"text": "MicroPET imaging in nonhuman primates with [11C]1 and [11C]2 demonstrated that both tracers behave similarly in vivo with high uptake being observed in the SERT-rich brain regions and peak uptake being achieved in about 55 min postinjection.", "entity1": "SERT", "entity2": "11C", "span1": [156, 160], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10061": {"label": 8, "data": {"text": "The x(c)- cystine transporter represents a novel target for sulfasalazine-like drugs with high potential for application in therapy of lymphoblastic and other malignancies dependent on extracellular cyst(e)ine.", "entity1": "x(c)- cystine transporter", "entity2": "cyst(e)ine", "span1": [4, 29], "span2": [199, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1941": {"label": 3, "data": {"text": "The aim of this study was to evaluate the influence of hepatic impairment on the pharmacokinetics (PK) of the novel cyclooxygenase-2 (COX-2) selective inhibitor lumiracoxib (Prexige), so that dose recommendations for clinical use can be provided.", "entity1": "cyclooxygenase-2", "entity2": "Prexige", "span1": [116, 132], "span2": [174, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13682": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "human TLR7", "entity2": "imiquimod", "span1": [118, 128], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5602": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "clozapine", "span1": [59, 65], "span2": [128, 137]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5176": {"label": 2, "data": {"text": "In PFC, DEX caused activation of AKT, augmentation of pro-survival Bcl-2 protein and enhanced Bcl-2/Bax protein ratio, as well Bcl-2 translocation to mitochondria.", "entity1": "Bax", "entity2": "DEX", "span1": [100, 103], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8180": {"label": 3, "data": {"text": "Furthermore, MDZ caused mechanism-based inactivation of cytochrome P450 3A-dependent TRZ 1'-hydroxylation in mouse, rat and human intestinal microsomes with similar potencies.", "entity1": "cytochrome P450 3A", "entity2": "MDZ", "span1": [56, 74], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7911": {"label": 2, "data": {"text": "We found that helenalin markedly induced endoplasmic reticulum (ER) stress-related genes, such as regulated in development and DNA damage responses (REDD) 1, activating transcription factor-4 (ATF4) and/or the CCAAT enhancer-binding protein-homologous protein (CHOP).", "entity1": "CCAAT enhancer-binding protein-homologous protein", "entity2": "helenalin", "span1": [210, 259], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14283": {"label": 0, "data": {"text": "The mutant Fc domain (AglycoT-Fc1004) contained a total of 5 amino acid substitutions that conferred an activating to inhibitory ratio of 25 (A/I ratio; FcyRIIa-R131:Fc\u03b3RIIb).", "entity1": "Fc\u03b3RIIb", "entity2": "amino acid", "span1": [166, 173], "span2": [61, 71]}, "weak_labels": [0, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11182": {"label": 3, "data": {"text": "To investigate the possibility that felbamate's favorable toxicity profile could be related to NMDA receptor subtype selectivity, we examined the specificity of felbamate block of recombinant NMDA receptors composed of the NR1a subunit and various NR2 subunits.", "entity1": "NR2", "entity2": "felbamate", "span1": [248, 251], "span2": [161, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3205": {"label": 3, "data": {"text": "Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids.", "entity1": "mammalian isoforms I-XIV", "entity2": "phenolic acids", "span1": [14, 38], "span2": [88, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15745": {"label": 1, "data": {"text": "Quercetin suppressed CYP2E1-dependent ethanol hepatotoxicity via depleting heme pool and releasing CO.", "entity1": "CYP2E1", "entity2": "ethanol", "span1": [21, 27], "span2": [38, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"897": {"label": 3, "data": {"text": "N(5)-Substituted H(4)biopterin derivatives were not oxidized to products serving as substrates for dihydropteridine reductase and,depending on the substituent, were competitive inhibitors of phenylalanine hydroxylase: N(5)-methyl- and N(5)-hydroxymethyl H(4)biopterin inhibited phenylalanine hydroxylase, whereas N(5)-formyl- and N(5)-acetyl H(4)biopterin had no effect.", "entity1": "phenylalanine hydroxylase", "entity2": "N(5)-methyl", "span1": [278, 303], "span2": [218, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"11776": {"label": 1, "data": {"text": "Western blot analyses showed significant effects of Pb exposure on DNMT1, DNMT3a, and MeCP2 expression, with effects often seen at the lowest level of exposure and modified by sex and developmental window of Pb exposure.", "entity1": "MeCP2", "entity2": "Pb", "span1": [86, 91], "span2": [52, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2061": {"label": 8, "data": {"text": "Mutation of arginine 228 to lysine enhances the glucosyltransferase activity of bovine beta-1,4-galactosyltransferase I.\tBeta-1,4-galactosyltransferase I (beta4Gal-T1) normally transfers Gal from UDP-Gal to GlcNAc in the presence of Mn(2+) ion (Gal-T activity) and also transfers Glc from UDP-Glc to GlcNAc (Glc-T activity), albeit at only 0.3% efficiency.", "entity1": "Glc-T", "entity2": "UDP-Glc", "span1": [308, 313], "span2": [289, 296]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5617": {"label": 8, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "Cs+", "span1": [131, 135], "span2": [145, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13862": {"label": 8, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "17beta-hydroxysteroid-dehydrogenase type 1", "entity2": "estradiol", "span1": [266, 308], "span2": [213, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3154": {"label": 4, "data": {"text": "Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity.", "entity1": "TrkB", "entity2": "Amitriptyline", "span1": [28, 32], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15940": {"label": 1, "data": {"text": "We also recorded a significant correlation between M value increase and the decrease of vaspin, visfatin, and omentin-1 obtained with vildagliptin+metformin.", "entity1": "vaspin", "entity2": "vildagliptin", "span1": [88, 94], "span2": [134, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12593": {"label": 1, "data": {"text": "The kinetics of onset of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor desensitization by glutamate, and the extent of attenuation of AMPA receptor desensitization by cyclothiazide, showed pronounced cell-to-cell variation in cultures of rat hippocampal neurons.", "entity1": "(AMPA) receptor", "entity2": "glutamate", "span1": [82, 97], "span2": [117, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1253": {"label": 3, "data": {"text": "The effects of theophylline (unspecific PDE inhibitor), vinpocetine (PDE1 inhibitor), EHNA (PDE2 inhibitor) and the PDE5 inhibitors zaprinast and E 4021 were weak.", "entity1": "PDE5", "entity2": "E 4021", "span1": [116, 120], "span2": [146, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6551": {"label": 1, "data": {"text": "Identification of interaction sites of cyclic nucleotide phosphodiesterase type 3A with milrinone and cilostazol using molecular modeling and site-directed mutagenesis.", "entity1": "phosphodiesterase type 3A", "entity2": "cilostazol", "span1": [57, 82], "span2": [102, 112]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6465": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "dihydrofolate reductase", "entity2": "LY231514", "span1": [112, 135], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3410": {"label": 3, "data": {"text": "In addition, PSE inhibited the transcriptional activity of NFAT without interfering with the calcium-induced NFAT dephosphorylation event, which represents the major signaling pathway for its activation.", "entity1": "NFAT", "entity2": "PSE", "span1": [59, 63], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7398": {"label": 3, "data": {"text": "Consequently, PDE4 inhibitors including cilomilast and AWD 12-281 have been tested in several models of allergic and irritant skin inflammation.", "entity1": "PDE4", "entity2": "AWD 12-281", "span1": [14, 18], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"427": {"label": 5, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "SL 89,0591", "span1": [258, 286], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6413": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes.", "entity1": "PPARalpha", "entity2": "bezafibrate", "span1": [50, 59], "span2": [73, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2548": {"label": 3, "data": {"text": "Given that M-CSF signalling through c-FMS plays an important role in osteoclast biology, we speculated that blocking such a pathway with imatinib may modulate osteoclast activity.", "entity1": "M-CSF", "entity2": "imatinib", "span1": [11, 16], "span2": [137, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1367": {"label": 8, "data": {"text": "Several active analogues were also evaluated for their ability to block uptake of DA, 5-HT, and NE and inhibit binding of [(125)I] RTI-55 at HEK-hDAT, HEK-hSERT, and HEK-hNET cells.", "entity1": "hDAT", "entity2": "DA", "span1": [145, 149], "span2": [82, 84]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7236": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "METH", "span1": [192, 229], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6605": {"label": 1, "data": {"text": "These radiotracers are close analogues of reboxetine, a potent and selective ligand for the norepinephrine transporter (NET).", "entity1": "norepinephrine transporter", "entity2": "reboxetine", "span1": [92, 118], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1841": {"label": 3, "data": {"text": "Here, we show that one BLT, [1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea] (BLT-4), blocked ABCA1-mediated cholesterol efflux to lipid-poor apoA-I at a potency similar to that for its inhibition of SR-BI (IC(50) approximately 55-60 microM).", "entity1": "SR-BI", "entity2": "BLT", "span1": [197, 202], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4576": {"label": 1, "data": {"text": "Antofine-induced connexin43 gap junction disassembly in rat astrocytes involves protein kinase C\u03b2.", "entity1": "protein kinase C\u03b2", "entity2": "Antofine", "span1": [80, 97], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12279": {"label": 3, "data": {"text": "This study identified four clinically approved antihypertensive drugs (efonidipine, felodipine, isradipine, and nitrendipine) as potent T-channel blockers (IC(50) < 3 microM).", "entity1": "T-channel", "entity2": "felodipine", "span1": [136, 145], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2206": {"label": 3, "data": {"text": "Doxycycline was shown to decrease cerebral MMP-9 activities and angiogenesis induced by vascular endothelial growth factor (VEGF).", "entity1": "vascular endothelial growth factor", "entity2": "Doxycycline", "span1": [88, 122], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10437": {"label": 1, "data": {"text": "The holo-SDH crystallized with O-methylserine (OMS) was also determined at 2.6 A resolution by molecular replacement.", "entity1": "holo-SDH", "entity2": "OMS", "span1": [4, 12], "span2": [47, 50]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8381": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "acid phosphatase", "entity2": "Cd", "span1": [148, 164], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12595": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "PHBP", "entity2": "N", "span1": [27, 31], "span2": [140, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"356": {"label": 1, "data": {"text": "A cocaine-sensitive Drosophila serotonin transporter: cloning, expression, and electrophysiological characterization.", "entity1": "Drosophila serotonin transporter", "entity2": "cocaine", "span1": [20, 52], "span2": [2, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2689": {"label": 3, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "c-Kit", "entity2": "MP470", "span1": [136, 141], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15498": {"label": 1, "data": {"text": "Benzoquinone Reveals a Cysteine-Dependent Desensitization Mechanism of TRPA1.", "entity1": "TRPA1", "entity2": "Benzoquinone", "span1": [71, 76], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5850": {"label": 4, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT4", "entity2": "cisapride", "span1": [232, 237], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1744": {"label": 8, "data": {"text": "CPT I (carnitine palmitoyltransferase I) catalyses the conversion of palmitoyl-CoA into palmitoylcarnitine in the presence of L-carnitine, facilitating the entry of fatty acids into mitochondria.", "entity1": "carnitine palmitoyltransferase I", "entity2": "palmitoyl-CoA", "span1": [7, 39], "span2": [69, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"10851": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Glivec", "span1": [110, 113], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4250": {"label": 2, "data": {"text": "Furthermore, butein treatment caused nuclear accumulation of nuclear factor-E2-related factor 2 (Nrf2) and increased the promoter activity of antioxidant response elements (AREs).", "entity1": "antioxidant response elements", "entity2": "butein", "span1": [142, 171], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6490": {"label": 4, "data": {"text": "RESULTS: The alpha(2)-adrenoceptor agonists induced vasoconstriction in the porcine ciliary artery with the following potency order (EC(50)) expressed in nanomolar: brimonidine 2.11, oxymetazoline 5.26, and apraclonidine 13.0.", "entity1": "alpha(2)-adrenoceptor", "entity2": "oxymetazoline", "span1": [13, 34], "span2": [183, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6399": {"label": 1, "data": {"text": "CONCLUSIONS: Quetiapine shows a transiently high D2 occupancy, which decreases to very low levels by the end of the dosing interval.", "entity1": "D2", "entity2": "Quetiapine", "span1": [49, 51], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3638": {"label": 3, "data": {"text": "NaAsO(2) increased the mRNA levels of the light and medium subunits of neurofilament and decreased the mRNA levels of tau and tubulin in a dose-dependent manner; no significant effect was found in the mRNA levels of the heavy subunit of neurofilament, microtubule-associated protein 2, or actin.", "entity1": "tau", "entity2": "NaAsO(2)", "span1": [118, 121], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13726": {"label": 2, "data": {"text": "RTX treatment also induced foci of RAD51, gamma-H2AX, phospho-Chk1, and phospho-NBS1, although the extent of co-localization with RPA2 foci varied.", "entity1": "phospho-NBS1", "entity2": "RTX", "span1": [72, 84], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11723": {"label": 1, "data": {"text": "To investigate the effects of \u03b2-ionone on apoptosis initiation and its possible mechanisms of action, we qualified cell apoptosis, proteins related to apoptosis and a phosphatidylinositol 3-kinase (PI3K)-AKT pathway in human gastric adenocarcinoma cancer SGC-7901 cells.", "entity1": "AKT", "entity2": "\u03b2-ionone", "span1": [204, 207], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11094": {"label": 1, "data": {"text": "Characterization of an alpha 1D-adrenoceptor mediating the contractile response of rat aorta to noradrenaline.", "entity1": "alpha 1D-adrenoceptor", "entity2": "noradrenaline", "span1": [23, 44], "span2": [96, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12333": {"label": 2, "data": {"text": "GHRP-6 is a growth hormone secretagogue that also enhances tissue viability in different organs.", "entity1": "growth hormone", "entity2": "GHRP-6", "span1": [12, 26], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2957": {"label": 0, "data": {"text": "Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors.", "entity1": "phosphodiesterase-5", "entity2": "amino acids", "span1": [24, 43], "span2": [9, 20]}, "weak_labels": [0, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11790": {"label": 2, "data": {"text": "Meanwhile, the serum level of KC (a functional homolog of IL-8 and the main proinflammatory alpha chemokine in mice) in apoE(-/-) mice was up to 357pg/ml in SFO-HD treated group.", "entity1": "IL-8", "entity2": "SFO", "span1": [58, 62], "span2": [157, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9130": {"label": 1, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "alpha-adrenergic", "entity2": "clonidine", "span1": [81, 97], "span2": [137, 146]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11724": {"label": 2, "data": {"text": "The concentration response to levcromakalim (LEVC), a K(ATP) channel opener, was significantly shifted to the left in the inflamed smooth-muscle cells.", "entity1": "K(ATP) channel", "entity2": "levcromakalim", "span1": [54, 68], "span2": [30, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1828": {"label": 1, "data": {"text": "As is the case with BLTs, glyburide increased the apparent affinity of HDL binding to SR-BI.", "entity1": "HDL", "entity2": "glyburide", "span1": [71, 74], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11272": {"label": 8, "data": {"text": "The ratio between the GDC/SHMT and C1-THF synthase/SHMT pathways of Ser synthesis from [alpha-(13)C]Gly and [(13)C]formate, respectively, in Arabidopsis shoots was 21 : 1; in roots, 9 : 1.", "entity1": "GDC", "entity2": "[alpha-(13)C]Gly", "span1": [22, 25], "span2": [87, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11900": {"label": 8, "data": {"text": "Cytochrome P450 epoxygenase 2J2 (CYP2J2) metabolizes arachidonic acids to form epoxyeicosatrienoic acids (EETs), which possess various beneficial effects on the cardiovascular system.", "entity1": "CYP2J2", "entity2": "arachidonic acids", "span1": [33, 39], "span2": [53, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6013": {"label": 8, "data": {"text": "Moreover, the production of TXB2 during whole blood clotting was assessed as an index of the cyclooxygenase activity of platelet PGHS-1 ex vivo.", "entity1": "PGHS-1", "entity2": "TXB2", "span1": [129, 135], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12470": {"label": 3, "data": {"text": "Arsenic deregulates the autophagic pathway through blockage of autophagic flux, resulting in accumulation of autophagosomes and sequestration of p62, Keap1, and LC3.", "entity1": "Keap1", "entity2": "Arsenic", "span1": [150, 155], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15895": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "polyketide synthases", "entity2": "benzopyranopyrrole", "span1": [58, 78], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7018": {"label": 1, "data": {"text": "Inhibition of [3H]5-HT or [3H]NE uptake by DVS for the hSERT or hNET produced IC50 values of 47.3 +/- 19.4 and 531.3 +/- 113.0 nM, respectively.", "entity1": "hSERT", "entity2": "DVS", "span1": [55, 60], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5395": {"label": 4, "data": {"text": "The experiments were performed on 80 male Wistar rats, 58 of which survived, subdivided into 3 groups: C-control rats, I-EAP group, and II-EAP group treated with the adenosine A3 receptor agonist IB-MECA (1-deoxy-1-6[[(3-iodophenyl) methyl]amino]-9H-purin-9-yl)-N-methyl-B-D-ribofuronamide at a dose of 0.75\u00a0mg/kg b.w.", "entity1": "adenosine A3 receptor", "entity2": "(1-deoxy-1-6[[(3-iodophenyl) methyl]amino]-9H-purin-9-yl)-N-methyl-B-D-ribofuronamide", "span1": [166, 187], "span2": [204, 289]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5429": {"label": 8, "data": {"text": "Cholesterol esterase (CE) induced surface erosion of poly(ethylene carbonate) (PEC) and drug release from PEC under mild physiological environment was investigated.", "entity1": "Cholesterol esterase", "entity2": "poly(ethylene carbonate)", "span1": [0, 20], "span2": [53, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3431": {"label": 1, "data": {"text": "Epi increased the activity of the human WNT6 promoter through Cav1-dependent binding of \u03b2-catenin to the proximal WNT6 promoter.", "entity1": "Cav1", "entity2": "Epi", "span1": [62, 66], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14172": {"label": 1, "data": {"text": "The purpose of this review is to summarize current knowledge about oxysterol-dependent activation by LXR of genes involved in reverse cholesterol transport, and what these defects of cell cholesterol homeostasis can teach us about the critical pathways of oxysterol generation for expression of LXR-dependent genes.", "entity1": "LXR", "entity2": "oxysterol", "span1": [295, 298], "span2": [256, 265]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4428": {"label": 1, "data": {"text": "The keto and phenolic -OH are major factors that are prominently involved in interaction with COX-2 active site.", "entity1": "COX-2", "entity2": "OH", "span1": [94, 99], "span2": [23, 25]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5746": {"label": 3, "data": {"text": "Vitamin C forestalls cigarette smoke induced NF-\u03baB activation in alveolar epithelial cells.", "entity1": "NF-\u03baB", "entity2": "Vitamin C", "span1": [45, 50], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9485": {"label": 3, "data": {"text": "Under voltage-clamp conditions, cisapride block of HERG is dose dependent with a half-maximal inhibitory concentration of 6.5 nM at 22 degrees C (n = 25 cells).", "entity1": "HERG", "entity2": "cisapride", "span1": [51, 55], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8148": {"label": 2, "data": {"text": "Increased urinary excretion of albumin, hemopexin, transferrin and VDBP correlates with chronic sensitization to gentamicin nephrotoxicity in rats.", "entity1": "VDBP", "entity2": "gentamicin", "span1": [67, 71], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"708": {"label": 8, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "acetylcholinesterase", "entity2": "acetylcholine", "span1": [108, 128], "span2": [193, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5776": {"label": 9, "data": {"text": "This binding was not significantly inhibited by the lysine analogue epsilon-amino caproic acid (EACA), indicating that plasminogen binding was not just through lysine binding sites as suggested for other plasminogen binding sites.", "entity1": "plasminogen", "entity2": "EACA", "span1": [119, 130], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5033": {"label": 5, "data": {"text": "Synthesis and in Vitro Characterisation of Ifenprodil-Based Fluorescein Conjugates as GluN1/GluN2B N-Methyl-D-aspartate Receptor Antagonists.", "entity1": "GluN2B", "entity2": "Fluorescein", "span1": [92, 98], "span2": [60, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1515": {"label": 3, "data": {"text": "Sildenafil is inhibitory of PDE5 at a rate tenfold higher than for the next PDE (PDE6), which produces visual changes through the retinal rods.", "entity1": "PDE6", "entity2": "Sildenafil", "span1": [81, 85], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"366": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "IL-4", "entity2": "DEX", "span1": [65, 69], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5512": {"label": 1, "data": {"text": "Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists.", "entity1": "mu and delta opioid", "entity2": "dezocine", "span1": [103, 122], "span2": [71, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8955": {"label": 7, "data": {"text": "Analysis of coenzyme binding by human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase and steroid 5----4-ene-isomerase using 5'-[p-(fluorosulfonyl)benzoyl]adenosine, an affinity labeling cofactor analog.", "entity1": "human placental 3 beta-hydroxy-5-ene-steroid dehydrogenase", "entity2": "5'-[p-(fluorosulfonyl)benzoyl]adenosine", "span1": [32, 90], "span2": [130, 169]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"3615": {"label": 3, "data": {"text": "Taken together, our study demonstrated that SB365 inhibits the AKT/mTOR pathway, leading to the suppression of tumor growth and angiogenesis together with induction of apoptosis.", "entity1": "AKT", "entity2": "SB365", "span1": [63, 66], "span2": [44, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11793": {"label": 2, "data": {"text": "Fisetin treatment showed a significant decline in the levels of blood glucose, glycosylated hemoglobin (HbA1c), NF-kB p65 unit (in pancreas) and IL-1\u03b2 (plasma), serum nitric oxide (NO) with an elevation in plasma insulin.", "entity1": "insulin", "entity2": "Fisetin", "span1": [213, 220], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5302": {"label": 1, "data": {"text": "In addition, prunetin inhibits NF-\u03baB-dependent inflammatory responses by modulating I\u03baB kinase (IKK)-inhibitor \u03baB\u03b1 (I\u03baB\u03b1)-NF-\u03baB signaling.", "entity1": "NF-\u03baB", "entity2": "prunetin", "span1": [122, 127], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1933": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "CrAT", "entity2": "myristoyl-CoA", "span1": [18, 22], "span2": [93, 106]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6228": {"label": 1, "data": {"text": "Kinetic studies comparing the binding of [3H]eletriptan and [3H]sumatriptan to the human recombinant 5-HT1B and 5-HT1D receptors expressed in HeLa cells revealed that both radioligands bound with high specificity (>90%) and reached equilibrium within 10-15 min.", "entity1": "5-HT1D", "entity2": "[3H]eletriptan", "span1": [112, 118], "span2": [41, 55]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11167": {"label": 1, "data": {"text": "Both the phosphotriesterase and physostigmine treatments protected the brain AChE activities measured 24 h after sarin exposure.", "entity1": "AChE", "entity2": "physostigmine", "span1": [77, 81], "span2": [32, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4097": {"label": 3, "data": {"text": "The upregulation of calpain, tBid and caspase-3 activity were further inhibited by treatment with EGTA in the presence of ALD.", "entity1": "tBid", "entity2": "EGTA", "span1": [29, 33], "span2": [98, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3843": {"label": 3, "data": {"text": "TCDD decreased the expression of the glucose transporter, SLC2A1, and most of the glycolytic transcripts, followed by decreases in glycolytic intermediates, including pyruvate.", "entity1": "glucose transporter", "entity2": "TCDD", "span1": [37, 56], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"322": {"label": 1, "data": {"text": "The folding rate monitored by 2'CMP binding to the major slow-folding species of Pro42Ala RNase A is faster than the folding rate monitored by tyrosine burial; however, the folding rate monitored by inhibitor binding to the minor slow-folding species is decreased significantly over the folding rate monitored by tyrosine burial, indicating that the major and minor slow-folding species of Pro42Ala fold to the native state with different transition-state conformations in the rate-determining step.", "entity1": "Pro42Ala", "entity2": "2'CMP", "span1": [81, 89], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13522": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "CDO", "entity2": "l-cysteine", "span1": [22, 25], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"316": {"label": 1, "data": {"text": "Recent studies highlight the capacity of sucralfate to bind basic fibroblast growth factor (bFGF) and deliver it in high concentration to the ulcer.", "entity1": "basic fibroblast growth factor", "entity2": "sucralfate", "span1": [60, 90], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2754": {"label": 1, "data": {"text": "The chemical identity and position of the substituents on the lower aniline ring were important in determining the potency and extent of COX inhibition as well as COX-2 selectivity.", "entity1": "COX-2", "entity2": "aniline", "span1": [163, 168], "span2": [68, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14446": {"label": 4, "data": {"text": "As these regulatory motifs mediate regulation of target genes by AhR agonists including TCDD and prochloraz, we have systematically investigated the effect of both contaminants on functional ABCG2 transport activity in primary bovine mammary epithelial cells.", "entity1": "AhR", "entity2": "prochloraz", "span1": [65, 68], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9129": {"label": 1, "data": {"text": "The binding of phenoxybenzamine to calmodulin was fairly selective in that other alpha-adrenergic agents such as prazosin, yohimbine and clonidine failed to bind to calmodulin when examined under the same experimental conditions.", "entity1": "alpha-adrenergic", "entity2": "yohimbine", "span1": [81, 97], "span2": [123, 132]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2725": {"label": 3, "data": {"text": "Sulindac sulfide inhibited PPARdelta protein expression and PPARdelta transcriptional activity.", "entity1": "PPARdelta", "entity2": "Sulindac sulfide", "span1": [60, 69], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7841": {"label": 2, "data": {"text": "We observed that ribavirin enhanced ELL3 recruitment to F7, whereas knockdown of ELL3 diminished ribavirin-induced FVII mRNA up-regulation.", "entity1": "F7", "entity2": "ribavirin", "span1": [56, 58], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2317": {"label": 3, "data": {"text": "Glyphosate affects aromatic amino acid biosynthesis by inhibiting 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS).", "entity1": "5-enolpyruvylshikimate-3-phosphate synthase", "entity2": "Glyphosate", "span1": [66, 109], "span2": [0, 10]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14414": {"label": 5, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile", "span1": [183, 187], "span2": [61, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4701": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "TCDD", "span1": [241, 247], "span2": [214, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5747": {"label": 3, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [88, 93], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14248": {"label": 1, "data": {"text": "Androstanol and androstenol, estrone, 17\u03b2-estradiol, TCPOBOP, and CITCO showed compound-specific but similar affinities for both CARs.", "entity1": "CARs", "entity2": "17\u03b2-estradiol", "span1": [129, 133], "span2": [38, 51]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7131": {"label": 1, "data": {"text": "All PDE5 constructs had similar affinities for 3-isobutyl-1-methylxanthine, sildenafil, tadalafil, and UK-122764, but mutants containing a complete GAF-B had 7- to 18-fold higher affinity for vardenafil-based compounds compared with those lacking a complete GAF-B.", "entity1": "PDE5", "entity2": "3-isobutyl-1-methylxanthine", "span1": [4, 8], "span2": [47, 74]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3809": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Sar", "span1": [66, 71], "span2": [44, 47]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12653": {"label": 1, "data": {"text": "This study shows that aspirin and sodium salicylate, its major blood metabolite, reverse contractile actions of endothelin-1 (ET-1) in isolated rat aorta and human mammary arteries.", "entity1": "endothelin-1", "entity2": "sodium salicylate", "span1": [112, 124], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13760": {"label": 1, "data": {"text": "Bosutinib did not inhibit KIT or platelet-derived growth factor receptor, but prominently targeted the apoptosis-linked STE20 kinases.", "entity1": "STE20 kinases", "entity2": "Bosutinib", "span1": [120, 133], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14740": {"label": 9, "data": {"text": "Here we found that arsenic trioxide, a frontline agent for acute promyelocytic leukemia, inhibits \u0394Np63 but not TAp63 expression in time- and dose-dependent manners.", "entity1": "TAp63", "entity2": "arsenic trioxide", "span1": [112, 117], "span2": [19, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7914": {"label": 8, "data": {"text": "DRG neurons display substantial capacity for accumulating copper via a transport process mediated by rCtr1, but appear able to resist copper toxicity and use alternative mechanisms to take up oxaliplatin.", "entity1": "rCtr1", "entity2": "copper", "span1": [101, 106], "span2": [58, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1019": {"label": 1, "data": {"text": "In COS cells transfected with alpha(1b) adrenoceptor cDNA and in DDT(1) MF-2 cells which express native alpha(1B) adrenoceptors, [(3)H]-prazosin was displaced by unlabelled prazosin in a normal equilibrium process, with no prazosin paradox in concentrations up to 10(-6) M. In DDT(1) MF-2 cells, [(3)H]-prazosin was displaced likewise by a series of alpha(1) adrenergic agonists, none of which increased the binding of [(3)H]-prazosin.", "entity1": "alpha(1B) adrenoceptors", "entity2": "prazosin", "span1": [104, 127], "span2": [173, 181]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5443": {"label": 3, "data": {"text": "Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae \u03b2-carbonic anhydrase.", "entity1": "Saccharomyces cerevisiae \u03b2-carbonic anhydrase", "entity2": "Benzenesulfonamides", "span1": [76, 121], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15989": {"label": 1, "data": {"text": "Using small interfering double-stranded RNA technology, we further demonstrate that the effects of puerarin on proliferation, differentiation and survival are mediated by both ER\u03b1 and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "puerarin", "span1": [176, 179], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"715": {"label": 3, "data": {"text": "This action can be related to the ability of torasemide to block the increase of [Ca(2+)](i) induced by Ang II in VSMCs.", "entity1": "Ang II", "entity2": "torasemide", "span1": [104, 110], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4588": {"label": 1, "data": {"text": "The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs.", "entity1": "GPCRs", "entity2": "fatty acid", "span1": [78, 83], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"12901": {"label": 3, "data": {"text": "Pretreatment with H(2)S or NaHS significantly inhibited LPS-induced iNOS expression and NO production.", "entity1": "iNOS", "entity2": "NaHS", "span1": [68, 72], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12084": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "3 beta-HSD", "entity2": "dehydroepiandrosterone", "span1": [74, 84], "span2": [197, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11265": {"label": 3, "data": {"text": "On the other hand, high doses of okadaic acid (10 ng/mouse, i.c.v.) ), which also block PP1, and calyculin-A (0.1 fg/mouse-1 ng/mouse, i.c.v.", "entity1": "PP1", "entity2": "okadaic acid", "span1": [88, 91], "span2": [33, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8339": {"label": 3, "data": {"text": "Aqueous ethanol (80%) extract of lentil hulls exhibited high antioxidant and anti-inflammatory activities preferentially inhibiting 15-LOX (IC(50), 55 \u03bcg/ml), with moderate COX-1 (IC(50), 66 \u03bcg/ml) and COX-2 (IC(50), 119 \u03bcg/ml) inhibitory effects on the COX pathway, whereas faba bean hull extracts exerted relatively mild LOX inhibitory activity.", "entity1": "COX-1", "entity2": "ethanol", "span1": [173, 178], "span2": [8, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4696": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "TCDD", "span1": [103, 109], "span2": [72, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12493": {"label": 1, "data": {"text": "The 2B4-paroxetine structure is nearly superimposable on a previously solved closed structure in a ligand free state.", "entity1": "2B4", "entity2": "paroxetine", "span1": [4, 7], "span2": [8, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9221": {"label": 3, "data": {"text": "Since both TFP and W-7 are potent inhibitors of calmodulin, we investigated the possibility that inhibition of calmodulin was responsible for the loss of receptors.", "entity1": "calmodulin", "entity2": "W-7", "span1": [48, 58], "span2": [19, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8461": {"label": 3, "data": {"text": "Hinokitiol inhibited the phosphorylation of phospholipase C (PLC)\u03b32, protein kinase C (PKC), mitogen-activated protein kinases (MAPKs), and Akt in collagen-activated human platelets, and significantly reduced intracellular calcium mobilization and hydroxyl radical (OH) formation.", "entity1": "Akt", "entity2": "Hinokitiol", "span1": [140, 143], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3740": {"label": 1, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "AhR", "entity2": "2,3,7,8-tetrachlorodibenzo-p-dioxin", "span1": [61, 64], "span2": [73, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4309": {"label": 2, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "JNK", "entity2": "AuF", "span1": [64, 67], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7409": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "NR1", "entity2": "NMDA", "span1": [15, 18], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13072": {"label": 1, "data": {"text": "These data indicate that suppression of constitutive MTAP has no effect on pemetrexed activity when the primary target is TS.", "entity1": "TS", "entity2": "pemetrexed", "span1": [122, 124], "span2": [75, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13685": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "gardiquimod", "span1": [100, 104], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11039": {"label": 4, "data": {"text": "A selective retinoid X receptor agonist bexarotene (LGD1069, targretin) inhibits angiogenesis and metastasis in solid tumours.", "entity1": "retinoid X receptor", "entity2": "bexarotene", "span1": [12, 31], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14523": {"label": 3, "data": {"text": "The mechanism of PAK1 inhibition and induction of membranous translocation of adhesion proteins by 5-ASA might be independent of its known anti-inflammatory action.", "entity1": "PAK1", "entity2": "5-ASA", "span1": [17, 21], "span2": [99, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11398": {"label": 3, "data": {"text": "State-dependent mibefradil block of Na+ channels.", "entity1": "Na+ channels", "entity2": "mibefradil", "span1": [36, 48], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9446": {"label": 9, "data": {"text": "16,16-dimethyl-PGE2 and two putative EP1 antagonists, AH6809 and SC-19220, did not show any significant binding to this receptor.", "entity1": "EP1", "entity2": "16,16-dimethyl-PGE2", "span1": [37, 40], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13510": {"label": 1, "data": {"text": "Since 10(-3)M H(2)O(2) oxidises methionine and tryptophan residues in proteins, we examined calcium binding to calmodulin in the presence and absence of H(2)O(2) utilising (45)calcium.", "entity1": "calmodulin", "entity2": "calcium", "span1": [111, 121], "span2": [92, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12286": {"label": 1, "data": {"text": "(E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methy l benzenamine ((18)F-AV-45) is such as an agent currently in phase III clinical studies for PET of Abeta plaques in the brain.", "entity1": "Abeta", "entity2": "(18)F-AV-45", "span1": [181, 186], "span2": [97, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"794": {"label": 1, "data": {"text": "Lithium modulates desensitization of the glutamate receptor subtype gluR3 in Xenopus oocytes.", "entity1": "gluR3", "entity2": "glutamate", "span1": [68, 73], "span2": [41, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5229": {"label": 1, "data": {"text": "OBJECTIVETo describe and make available an interactive, 24-variable homeostasis model assessment (iHOMA2) that extends the HOMA2 model, enabling the modeling of physiology and treatment effects, to present equations of the HOMA2 and iHOMA2 models, and to exemplify iHOMA2 in two widely differing scenarios: changes in insulin sensitivity with thiazolidinediones and changes in renal threshold with sodium glucose transporter (SGLT2) inhibition.RESEARCH DESIGN AND METHODSiHOMA2 enables a user of the available software to examine and modify the mathematical functions describing the organs and tissues involved in the glucose and hormonal compartments.", "entity1": "insulin", "entity2": "thiazolidinediones", "span1": [318, 325], "span2": [343, 361]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7039": {"label": 8, "data": {"text": "The tissue RA level is maintained through a cascade of metabolic reactions where retinal dehydrogenases (RALDHs) catalyze the terminal reaction of RA biosynthesis from retinal, a rate-limiting step.", "entity1": "RALDHs", "entity2": "retinal", "span1": [105, 111], "span2": [168, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10400": {"label": 1, "data": {"text": "Taken together, these findings support the view that (1) OFQ is the only ppOFQ peptide that binds to and activates the ORL1 receptor and (2) OFQ II(1-28) does not bind or stimulate [35S]-GTPgammaS binding in cells expressing the mu opioid receptor.", "entity1": "OFQ", "entity2": "[35S]-GTPgammaS", "span1": [57, 60], "span2": [181, 196]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"383": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "CD3", "entity2": "Dexamethasone", "span1": [39, 42], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5533": {"label": 2, "data": {"text": "In direct adenylyl cyclase activation, in effects on adenylyl cyclase after pretreatment of intact cells, and in guinea pig tracheal relaxation assays, IAS and the parent drug salmeterol behave essentially the same.", "entity1": "adenylyl cyclase", "entity2": "salmeterol", "span1": [53, 69], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3282": {"label": 3, "data": {"text": "Together these studies support a unique mode of inhibition in which phenothiazines disrupt the S100A4/myosin-IIA interaction by sequestering S100A4 via small molecule-induced oligomerization.", "entity1": "S100A4", "entity2": "phenothiazines", "span1": [95, 101], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11640": {"label": 8, "data": {"text": "Tumor-growth-promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets.", "entity1": "cyclooxygenase-2", "entity2": "prostaglandin E2", "span1": [23, 39], "span2": [40, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1960": {"label": 3, "data": {"text": "To explore for the existence of an auxiliary hydrophobic binding register remote from the active site of PSMA a series of phenylalkylphosphonamidate derivatives of glutamic acid were synthesized and evaluated for their inhibitory potencies against PSMA.", "entity1": "PSMA", "entity2": "phenylalkylphosphonamidate", "span1": [248, 252], "span2": [122, 148]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9033": {"label": 5, "data": {"text": "To study the mechanism underlying this phenomenon, the effects of the nonselective beta-adrenoceptor antagonists propranolol [no intrinsic sympathomimetic activity (ISA)], alprenolol (weak ISA) and mepindolol (strong ISA) on lymphocyte beta 2-adrenoceptor density--assessed by (+/-)-[125I]-iodocyanopindolol (ICYP) binding--and plasma renin activity (PRA) were investigated in male healthy volunteers aged 23-35 years.", "entity1": "beta-adrenoceptor", "entity2": "alprenolol", "span1": [83, 100], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2062": {"label": 8, "data": {"text": "Mutation of arginine 228 to lysine enhances the glucosyltransferase activity of bovine beta-1,4-galactosyltransferase I.\tBeta-1,4-galactosyltransferase I (beta4Gal-T1) normally transfers Gal from UDP-Gal to GlcNAc in the presence of Mn(2+) ion (Gal-T activity) and also transfers Glc from UDP-Glc to GlcNAc (Glc-T activity), albeit at only 0.3% efficiency.", "entity1": "Gal-T", "entity2": "UDP-Gal", "span1": [245, 250], "span2": [196, 203]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6715": {"label": 9, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "Flt3", "entity2": "Gleevec", "span1": [52, 56], "span2": [107, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8850": {"label": 1, "data": {"text": "I3S increased expression of ROR\u03b3t, the master transcription factor for Th17 differentiation, and stimulated Th17 differentiation, in a comparative manner as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), a prototypical AhR ligand.", "entity1": "AhR", "entity2": "2,3,7,8-tetrachlorodibenzo-p-dioxin", "span1": [216, 219], "span2": [157, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"494": {"label": 5, "data": {"text": "Conversely, opioid antagonists such as naloxone and naltrexone (which bind to non-selectively opioid receptors) have been shown to decrease alcohol consumption under various experimental conditions.", "entity1": "opioid receptors", "entity2": "naloxone", "span1": [94, 110], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13267": {"label": 1, "data": {"text": "We studied in a clinical trial whether isolated isoflavone treatment in postmenopausal women could affect reverse cholesterol transport as evaluated by adenosine triphosphate-binding cassette A1- (ABCA1), dependent cholesterol efflux from macrophages.", "entity1": "adenosine triphosphate-binding cassette A1", "entity2": "isoflavone", "span1": [152, 194], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5028": {"label": 1, "data": {"text": "We had previously reported a fluorescein conjugate that was shown (by confocal microscopy imaging of DS-red-labelled cortical neurons) to bind specifically to GluN2B.", "entity1": "GluN2B", "entity2": "fluorescein", "span1": [159, 165], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13636": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "linker domain", "entity2": "C", "span1": [113, 126], "span2": [171, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9329": {"label": 1, "data": {"text": "Cell lines stably expressing EAA3a protein formed homomeric ligand-gated ion channels responsive, in order of decreasing affinity to domoate, kainate, L-glutamate and (RS)-alpha-amino-3-hydroxy-5- methylisoxazole-propionate (AMPA).", "entity1": "EAA3a", "entity2": "L-glutamate", "span1": [29, 34], "span2": [151, 162]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5963": {"label": 3, "data": {"text": "These data suggested that ambenonium had a dual effect on tissue responses to acetylcholine-producing potentiation by blockade of acetylcholinesterase and concomitant antagonism by blockade of muscarinic receptors.", "entity1": "acetylcholinesterase", "entity2": "ambenonium", "span1": [130, 150], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10771": {"label": 2, "data": {"text": "Western blot analysis of cells incubated with imatinib demonstrated activation of EGFR and downstream signaling that was reduced by inhibition of mitogen-activated protein/extracellular signal-regulated kinase kinase 1 (MEK1) and EGFR, but not Her2/ErbB2.", "entity1": "EGFR", "entity2": "imatinib", "span1": [82, 86], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6336": {"label": 1, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "losartan", "span1": [18, 21], "span2": [213, 221]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"957": {"label": 5, "data": {"text": "In the rabbit pulmonary artery, rilmenidine and oxymetazoline are potent full agonists, whereas in the human atrial appendages they are antagonists at the alpha(2)-autoreceptors, sharing this property with rauwolscine, phentolamine, and idazoxan.", "entity1": "alpha(2)-autoreceptors", "entity2": "rilmenidine", "span1": [155, 177], "span2": [32, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13145": {"label": 2, "data": {"text": "RESULTS: In the NMDA-injured brain, the CysLT1 receptor mRNA, and protein expression were upregulated, and the receptor was mainly localized in the neurons and not in the astrocytes.", "entity1": "CysLT1 receptor", "entity2": "NMDA", "span1": [40, 55], "span2": [16, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9958": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-1", "entity2": "indomethacin", "span1": [214, 219], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9991": {"label": 9, "data": {"text": "Fibroblast cultures from the patient exhibited severe reduction of the rotenone-sensitive NADH-->UQ oxidoreductase activity of complex I, which was insensitive to cAMP stimulation.", "entity1": "NADH-->UQ oxidoreductase", "entity2": "cAMP", "span1": [90, 114], "span2": [163, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12793": {"label": 3, "data": {"text": "In a human whole blood assay, IC(50) values for lumiracoxib were 0.13 microM for COX-2 and 67 microM for COX-1 (COX-1/COX-2 selectivity ratio 515).", "entity1": "COX-2", "entity2": "lumiracoxib", "span1": [81, 86], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16066": {"label": 1, "data": {"text": "Given its efficacy and tolerability, once-daily, oral ibrutinib is an emerging treatment option for patients with relapsed/refractory MCL or CLL and CLL patients with del 17p or TP53 mutation.", "entity1": "TP53", "entity2": "ibrutinib", "span1": [178, 182], "span2": [54, 63]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3297": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mTOR", "entity2": "Everolimus", "span1": [75, 79], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8621": {"label": 1, "data": {"text": "In a different group of BMT patients treated with cyclosporine, the magnitude of interaction with IL-6 was under predicted ~3-fold.", "entity1": "IL-6", "entity2": "cyclosporine", "span1": [98, 102], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"765": {"label": 0, "data": {"text": "The inhibitor binds at the base of the active site gorge of TcAChE, interacting with both the choline-binding site (Trp-84) and the acyl-binding pocket (Phe-288, Phe-290).", "entity1": "TcAChE", "entity2": "Phe", "span1": [60, 66], "span2": [153, 156]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9105": {"label": 8, "data": {"text": "These results are consistent with the interpretation that both piriprost and diethylcarbamazine inhibit leukotriene formation but that they act on sequential steps in the biosynthetic pathway in such a manner as to synergistically interfere with the availability or utilization of LTA4 in the leukotriene C synthetase reaction.", "entity1": "leukotriene C synthetase", "entity2": "LTA4", "span1": [293, 317], "span2": [281, 285]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14215": {"label": 6, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "eseroline", "span1": [83, 88], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15013": {"label": 1, "data": {"text": "Taken together, these results suggest that SAH/SAHH-mediated transmethylation could be linked to the tumorigenic processes through cross-regulation between the actin cytoskeleton and Src kinase activity.", "entity1": "Src", "entity2": "SAH", "span1": [183, 186], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6798": {"label": 3, "data": {"text": "After 12 months of treatment, carvedilol significantly improved all end points (plasma concentration of B-type natriuretic peptide [BNP] from 175 (35 to 209) to 106 (52 to 160) pg/ml, mean (95% confidence interval) p <0.01; New York Heart Association functional class from 2.37 (2.13 to 2.61) to 1.56 (1.21 to 1.91), p <0.01; exercise capacity estimated with the Specific Activity Scale from 4.75 (4.50 to 5.00) to 5.68 (5.22 to 6.14) METs, p <0.02), whereas conventional therapy did not (plasma BNP concentration from 150 (114 to 186) to 174 (100 to 248) pg/ml; New York Heart Association functional class from 2.29 (2.08 to 2.50) to 2.11 (1.73 to 2.49); exercise capacity from 4.57 (4.34 to 4.80) to 4.72 (4.41 to 5.03) METs).", "entity1": "B-type natriuretic peptide", "entity2": "carvedilol", "span1": [104, 130], "span2": [30, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10679": {"label": 3, "data": {"text": "In Experiment 1, Antag I, Antag II and TT-235 inhibited the integrated uterine response to oxytocin at 5 minutes by 76%, 77% and 80%, respectively, compared to controls (p<0.05).", "entity1": "oxytocin", "entity2": "Antag I", "span1": [91, 99], "span2": [17, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12664": {"label": 1, "data": {"text": "Various drugs used in the treatment of IBD, such as glucocorticoids, 5-aminosalicylic acid, and sulfasalazine, interfere with NF-kappaB/Rel signaling.", "entity1": "Rel", "entity2": "5-aminosalicylic acid", "span1": [136, 139], "span2": [69, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9191": {"label": 2, "data": {"text": "This agent acts synergistically with many penicillins, such as ampicillin, carbenicillin, and the like, and with cephalosporins, cefazolin, cefamandole, or cefoxitin to inhibit gram-negative bacilli, probably on the basis of binding to different proteins needed for the production of the peptidoglycan of the bacterial cell wall.", "entity1": "peptidoglycan", "entity2": "cefazolin", "span1": [288, 301], "span2": [129, 138]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14783": {"label": 3, "data": {"text": "A series of anthra[1,2-d]imidazole-6,11-dione derivatives were synthesized and evaluated for telomerase inhibition, hTERT expression and suppression of cancer cell growth in vitro.", "entity1": "telomerase", "entity2": "anthra[1,2-d]imidazole-6,11-dione", "span1": [93, 103], "span2": [12, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5062": {"label": 3, "data": {"text": "Rg1 attenuated the A\u03b225-35-associated mitochondrial apoptotic events, accompanied by inhibiting HIF-1\u03b1 expression followed by intracellular reactive nitrogen species generation, and protein nitrotyrosination.", "entity1": "HIF-1\u03b1", "entity2": "Rg1", "span1": [96, 102], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15357": {"label": 8, "data": {"text": "CONCLUSION: Our findings demonstrate that (R)-omeprazole HI correlated better with CYP2C19 genotype groups than racemic-omeprazole HI, and these results may be useful for classification among patients in CYP2C19 genotype groups prior to omeprazole treatment.", "entity1": "CYP2C19", "entity2": "(R)-omeprazole", "span1": [83, 90], "span2": [42, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3473": {"label": 3, "data": {"text": "The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test was inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and was not serotonin-dependent, as it persisted in serotonin-deficient mice and upon blockade of either 5-HT(1A) receptors by WAY100635, or 5-HT(2A/2C) receptors by ritanserin.", "entity1": "5-HT(1A)", "entity2": "WAY100635", "span1": [252, 260], "span2": [274, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4437": {"label": 3, "data": {"text": "The activity of the human nasal mucosa microsomes was inhibited by 8-methoxypsoralen, a known CYP2A inhibitor.", "entity1": "CYP2A", "entity2": "8-methoxypsoralen", "span1": [94, 99], "span2": [67, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7666": {"label": 1, "data": {"text": "Indeed, indapamide bound to CA II has no interactions with active site water molecules.", "entity1": "CA II", "entity2": "indapamide", "span1": [28, 33], "span2": [8, 18]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1102": {"label": 3, "data": {"text": "Carvedilol reduced the risk of death or heart failure in patients with above-median levels of N-BNP or adrenomedullin, or both, to rates not significantly different from those observed in patients with levels below the median value.", "entity1": "N-BNP", "entity2": "Carvedilol", "span1": [94, 99], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3208": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "ferulic acid", "span1": [282, 284], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7798": {"label": 5, "data": {"text": "Serotonin-induced or neurotensin-induced reversal was blocked by \u03b2-ARK1 inhibitor, dynasore, or cPKC antagonist 5,6,7,13-tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4c]carbazole-12-propanenitrile (G\u00f66976).", "entity1": "cPKC", "entity2": "5,6,7,13-tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4c]carbazole-12-propanenitrile", "span1": [96, 100], "span2": [112, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14244": {"label": 8, "data": {"text": "Disruption of microtubule prevented insulin-induced actin remodeling and distal insulin signal transduction, with reduction in surface glucose transporter isoform 4 (GLUT4) and glucose uptake.", "entity1": "glucose transporter isoform 4", "entity2": "glucose", "span1": [135, 164], "span2": [177, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12885": {"label": 8, "data": {"text": "This aminophospholipid \"flippase\" selectively transports PS to the cytosolic leaflet of the bilayer and is sensitive to vanadate, Ca(2+), and modification by sulfhydryl reagents.", "entity1": "flippase", "entity2": "PS", "span1": [24, 32], "span2": [57, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10322": {"label": 2, "data": {"text": "Results indicate that imiquimod and resiquimod induce IFN-alpha and IFN-omega from purified pDC, and pDC are the principle IFN-producing cells in the blood.", "entity1": "IFN-omega", "entity2": "imiquimod", "span1": [68, 77], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12589": {"label": 1, "data": {"text": "The complex patterns of sensitivity to cyclothiazide seen in hippocampal neurons could be reconstituted by assembly of recombinant AMPA receptor subunits generated from cDNAs encoding the flip (i) and flop (o) splice variants of the GluR-A and GluR-B subunits.", "entity1": "AMPA receptor", "entity2": "cyclothiazide", "span1": [131, 144], "span2": [39, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15829": {"label": 8, "data": {"text": "However, enzymes contributing to oxidative metabolism of anandamide, namely cyclooxygenase-1 and Cyp2D6, were increased in the brain of aged mice, possibly enhancing the oxidative breakdown of anandamide.", "entity1": "Cyp2D6", "entity2": "anandamide", "span1": [97, 103], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1464": {"label": 0, "data": {"text": "By introducing the mutant-derived genomic library into a non-L-proline-utilizing strain, the mutant was found to carry an allele of the wild-type PRO1 gene encoding gamma-glutamyl kinase, which resulted in a single amino acid replacement; Asp (GAC) at position 154 was replaced by Asn (AAC).", "entity1": "gamma-glutamyl kinase", "entity2": "amino acid", "span1": [165, 186], "span2": [215, 225]}, "weak_labels": [0, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3814": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Ile", "span1": [148, 153], "span2": [58, 61]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11144": {"label": 3, "data": {"text": "We have examined the effect of dihydropyridine Ca2+-channel blockers felodipine and nicardipine on CaMPDE.", "entity1": "Ca2+-channel", "entity2": "nicardipine", "span1": [47, 59], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2024": {"label": 1, "data": {"text": "Data from heterologous expression of wild-type and mutant HERG genes indicate the mutation causes a 20-fold increase in IC50 of d-sotalol but only a 5.8-fold increase in IC50 of quinidine.", "entity1": "HERG", "entity2": "quinidine", "span1": [58, 62], "span2": [178, 187]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6194": {"label": 3, "data": {"text": "The cardiovascular effects of three different acetylcholinesterase inhibitors: physostigmine, tacrine and rivastigmine injected by intravenous (i.v.)", "entity1": "acetylcholinesterase", "entity2": "tacrine", "span1": [46, 66], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2389": {"label": 8, "data": {"text": "In the present study, we have evaluated possible participation of monocarboxylate transporters (MCTs) responsible for the bidirectional membrane transport of pyruvate in the cytoprotective property in osteoblasts.", "entity1": "monocarboxylate transporters", "entity2": "pyruvate", "span1": [66, 94], "span2": [158, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5509": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "nalbuphine", "span1": [108, 126], "span2": [362, 372]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6606": {"label": 1, "data": {"text": "These radiotracers are close analogues of reboxetine, a potent and selective ligand for the norepinephrine transporter (NET).", "entity1": "NET", "entity2": "reboxetine", "span1": [120, 123], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5773": {"label": 9, "data": {"text": "NSDA neurons displayed significant axon terminal degeneration (as indexed by decreases in DA, tyrosine hydroxylase (TH) and DA transporter concentrations in the striatum) as well as loss of TH-immunoreactive (IR) neurons in the substantia nigra (SN) following MPTP, whereas TIDA neurons revealed no overt axon terminal pathology or loss of TH-IR cell bodies.", "entity1": "TH", "entity2": "MPTP", "span1": [340, 342], "span2": [260, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12253": {"label": 8, "data": {"text": "Because of their low asparagine synthetase (ASNS) expression and asparagine biosynthesis, acute lymphoblastic leukemia (ALL) cells are exquisitely sensitive to asparagine depletion.", "entity1": "ASNS", "entity2": "asparagine", "span1": [44, 48], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7237": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "METH", "span1": [231, 237], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5010": {"label": 3, "data": {"text": "Of 9 CGPs with IC50's \u22642 \u03bcM, two belonged to Class I, two to Class III and five to Class V. When tested in the intact cells, only 4 of 16 CGPs (at 10 \u03bcM) inhibited MRP1-mediated calcein efflux by >50% (III-1, V-3, -4, -6) while a fifth (I-5) inhibited efflux by just 23%.", "entity1": "MRP1", "entity2": "CGPs", "span1": [164, 168], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11536": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "toluene diisocyanate", "span1": [103, 106], "span2": [195, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6776": {"label": 1, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX", "entity2": "piroxicam", "span1": [119, 122], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13527": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "2H1C class of non-heme iron enzymes", "entity2": "O2", "span1": [133, 168], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10178": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "OATP-C", "entity2": "rifamycin SV", "span1": [162, 168], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6204": {"label": 3, "data": {"text": "Cocaine block of hH1 channels was greater than block of mu1 channels at voltages between -120 mV and -90 mV, suggesting that greater steady-state inactivation of hH1 channels in this voltage range makes them more susceptible to cocaine block.", "entity1": "hH1 channels", "entity2": "Cocaine", "span1": [162, 174], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5239": {"label": 8, "data": {"text": "The slower CL was due to the reduction of hepatic biliary excretion (67.0% decrease) and hepatic CYP3A subfamily-mediated metabolism (21.9% decrease) of doxorubicin.", "entity1": "CYP3A", "entity2": "doxorubicin", "span1": [97, 102], "span2": [153, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11414": {"label": 0, "data": {"text": "The orientation of the O4 hydroxyl of glucose causes a steric hindrance to the side chain carboxylate group of Glu317, accounting for the enzyme's low Glc-T activity.", "entity1": "Glc-T", "entity2": "carboxylate", "span1": [151, 156], "span2": [90, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"30": {"label": 0, "data": {"text": "A major part of this processing requires endoproteolytic cleavage at specific pairs of basic amino acid residues, an event necessary for the maturation of a variety of important biologically active proteins, such as insulin and nerve growth factor.", "entity1": "insulin", "entity2": "amino acid", "span1": [216, 223], "span2": [93, 103]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15253": {"label": 1, "data": {"text": "Tertiary amine-functionalized sensors adsorbed multilayers of aggregated lysozyme, whereas tertiary amine N-oxides and triethylene glycol-terminated monolayers are consistent with small protein aggregates.", "entity1": "lysozyme", "entity2": "triethylene glycol", "span1": [73, 81], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5906": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "LDL", "entity2": "nicotinic acid", "span1": [172, 175], "span2": [32, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13445": {"label": 1, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "COX-2 promoter", "entity2": "EPA", "span1": [113, 127], "span2": [140, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1757": {"label": 3, "data": {"text": "GW572016, a reversible small molecule inhibitor of EGFR and ErbB2 tyrosine kinases, inhibits baseline p95ErbB2 phosphorylation in BT474 cells and tumor xenografts.", "entity1": "p95ErbB2", "entity2": "GW572016", "span1": [102, 110], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"566": {"label": 1, "data": {"text": "Previously, we reported that a primary heparin or heparan sulfate binding site resides in a distinct sequence in immunoglobulin (Ig)-like module II of the three modules of FGFR.", "entity1": "FGFR", "entity2": "sulfate", "span1": [172, 176], "span2": [58, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14232": {"label": 1, "data": {"text": "The residence time of a stoichiometric bioscavenger, human butyrylcholinesterase (huBuChE), in the plasma more closely matches that of VX than do the residence times of conventional therapy drugs (oxime, anti-muscarinic, anticonvulsant).", "entity1": "huBuChE", "entity2": "oxime", "span1": [82, 89], "span2": [197, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12538": {"label": 1, "data": {"text": "Isolation and characterization of labeled peptides from phenoxybenzamine-modified calmodulins indicated that peptides encompassing residues 38-75, 107-126, and 127-148 contained phenoxybenzamine label.", "entity1": "calmodulins", "entity2": "phenoxybenzamine", "span1": [82, 93], "span2": [56, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10287": {"label": 3, "data": {"text": "An inhibitor of type B monoamine oxidase (MAO-B), (-)deprenyl (selegiline), was reported to have neuroprotective activity, but clinical trials failed to confirm it.", "entity1": "type B monoamine oxidase", "entity2": "selegiline", "span1": [16, 40], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5973": {"label": 3, "data": {"text": "Phenol oxidase inhibitors such as phenylthiourea, potassium cyanide, and sodium azide inhibited the reaction drastically, suggesting the participation of the active site copper of the enzyme in the catalysis.", "entity1": "Phenol oxidase", "entity2": "phenylthiourea", "span1": [0, 14], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13868": {"label": 1, "data": {"text": "Cyan fluorescent protein was fused to the C terminus of the M(2) muscarinic receptor, and a specific binding sequence for the small fluorescent compound fluorescein arsenical hairpin binder, FlAsH, was inserted into the third intracellular loop; the latter site was labeled in intact cells by incubation with FlAsH.", "entity1": "M(2) muscarinic receptor", "entity2": "fluorescein", "span1": [60, 84], "span2": [153, 164]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3785": {"label": 2, "data": {"text": "Phillyrin attenuates high glucose-induced lipid accumulation in human HepG2 hepatocytes through the activation of LKB1/AMP-activated protein kinase-dependent signalling.", "entity1": "LKB1", "entity2": "Phillyrin", "span1": [114, 118], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10498": {"label": 1, "data": {"text": "Responses to isoproterenol could be restored to normal by beta2AR blockade, suggesting a beta2AR-mediated inhibition of beta1AR signalling.", "entity1": "beta1AR", "entity2": "isoproterenol", "span1": [120, 127], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11524": {"label": 1, "data": {"text": "CONCLUSIONS: We suggest that the additional effects of prednisolone on the MR explain the different responses to these glucocorticoids in the same depressed patients.", "entity1": "MR", "entity2": "prednisolone", "span1": [75, 77], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4613": {"label": 3, "data": {"text": "In this study, a novel series of 2-hydroxydiarylamide derivatives were synthesized and evaluated for inhibiting TMPRSS4 serine protease activity and suppressing cancer cell invasion.", "entity1": "TMPRSS4", "entity2": "2-hydroxydiarylamide", "span1": [112, 119], "span2": [33, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15424": {"label": 1, "data": {"text": "Cell-pre-incubation with bradykinin induced changes in ABCG expression levels after 7-ketostigmasterol-incubation; however, the energetic metabolism inhibition reduced NPC1L1 expression only in 7-ketocholesterol-incubated cells.", "entity1": "bradykinin", "entity2": "7-ketostigmasterol", "span1": [25, 35], "span2": [84, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12245": {"label": 0, "data": {"text": "The 2.0-A resolution structure of Thermus thermophilus PRODH reveals a distorted (betaalpha)(8) barrel catalytic core domain and a hydrophobic alpha-helical domain located above the carboxyl-terminal ends of the strands of the barrel.", "entity1": "Thermus thermophilus PRODH", "entity2": "carboxyl", "span1": [34, 60], "span2": [182, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8480": {"label": 1, "data": {"text": "Wild-type mice were more sensitive to DEX-dependent decreases in insulin sensitivity than GR(dim/dim) mice.", "entity1": "insulin", "entity2": "DEX", "span1": [65, 72], "span2": [38, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4216": {"label": 1, "data": {"text": "Although dopaminergic neurons within the nigrostriatal pathway appear intact, Mn-induced irregularities in DA transmission have been observed including decreased amphetamine-induced DA release and loss of the dopamine transporter (DAT).", "entity1": "dopamine transporter", "entity2": "Mn", "span1": [209, 229], "span2": [78, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10787": {"label": 2, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "IFN-gamma", "entity2": "simvastatin", "span1": [133, 142], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5430": {"label": 8, "data": {"text": "Cholesterol esterase (CE) induced surface erosion of poly(ethylene carbonate) (PEC) and drug release from PEC under mild physiological environment was investigated.", "entity1": "CE", "entity2": "poly(ethylene carbonate)", "span1": [22, 24], "span2": [53, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11642": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "GABA-T", "entity2": "PLZ", "span1": [269, 275], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"904": {"label": 7, "data": {"text": "Tetrahydrobiopterin [(6R)-5,6,7,8-tetrahydro-L-biopterin, H(4)biopterin] is one of several cofactors of nitric oxide synthases (EC 1.14.13.39).", "entity1": "nitric oxide synthases", "entity2": "(6R)-5,6,7,8-tetrahydro-L-biopterin", "span1": [104, 126], "span2": [21, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"15471": {"label": 3, "data": {"text": "A series of substituted 3-(benzylthio)-5-(1H-indol-3-yl)-4H-1,2,4-triazol-4-amines has been synthesised and tested in vitro as potential pro-apoptotic Bcl-2-inhibitory anticancer agents.", "entity1": "Bcl-2", "entity2": "3-(benzylthio)-5-(1H-indol-3-yl)-4H-1,2,4-triazol-4-amines", "span1": [151, 156], "span2": [24, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15218": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "COX-2", "entity2": "clerosterol", "span1": [288, 293], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1690": {"label": 3, "data": {"text": "Blockade of NMDA receptors by memantine could theoretically confer disease-modifying activity in AD by inhibiting the \"weak\" NMDA receptor-dependent excitotoxicity that has been hypothesized to play a role in the progressive neuronal loss that underlies the evolving dementia.", "entity1": "NMDA receptors", "entity2": "memantine", "span1": [12, 26], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9860": {"label": 3, "data": {"text": "Among the various enzymes, dicoumarol inhibitable cytosolic NAD(P)H:quinone oxidoreductase1 (NQO1) was shown to catalyse bioreductive activation of MMC leading to cross-linking of the DNA and cytotoxicity.", "entity1": "NAD(P)H:quinone oxidoreductase1", "entity2": "dicoumarol", "span1": [60, 91], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1435": {"label": 1, "data": {"text": "To determine whether 3,4-methylenedioxymethamphetamine (MDMA)-induced reductions in SERT density could be related to such a mechanism, p-chlorophenylalanine or MDMA was administered to rats, and brain serotonin and SERT density were measured.", "entity1": "SERT", "entity2": "MDMA", "span1": [215, 219], "span2": [160, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9280": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "(+)-butaclamol", "span1": [166, 186], "span2": [52, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13254": {"label": 2, "data": {"text": "RESULTS: Leukotriene D(4) upregulated MUC2/5AC gene expression and mucin secretion in a dose dependent pattern.", "entity1": "mucin", "entity2": "Leukotriene D(4)", "span1": [67, 72], "span2": [9, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13181": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "DAT", "entity2": "2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane", "span1": [278, 281], "span2": [82, 148]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12070": {"label": 0, "data": {"text": "This lysine is contained in the sequence PFYAVKC, which is found in all known ODCs from eukaryotes.", "entity1": "ODCs", "entity2": "PFYAVKC", "span1": [78, 82], "span2": [41, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1390": {"label": 3, "data": {"text": "Similar to gemfibrozil, clofibrate, another fibrate drug, also inhibited the expression of iNOS.", "entity1": "iNOS", "entity2": "clofibrate", "span1": [91, 95], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11234": {"label": 1, "data": {"text": "Taken together, these results reveal several differences between effects of MDMA and previously reported METH on DAT and VMAT-2; differences that may underlie the dissimilar neurotoxic profile of these agents.", "entity1": "DAT", "entity2": "MDMA", "span1": [113, 116], "span2": [76, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7873": {"label": 8, "data": {"text": "Renal clearance of unbound anagliptin and unbound M1 far exceeded glomerular filtration rate, indicating active renal elimination: that might reflect the fact that anagliptin may be a substrate of OAT1, OAT3, MDR1 and MRP2, and M1 a substrate of OAT3, BCRP, MRP2 and MRP4.", "entity1": "OAT1", "entity2": "anagliptin", "span1": [197, 201], "span2": [164, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8344": {"label": 8, "data": {"text": "Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine.", "entity1": "Histidine decarboxylase", "entity2": "amine", "span1": [0, 23], "span2": [80, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14442": {"label": 2, "data": {"text": "Induction of AhR by TCDD and prochloraz resulted in a time- and dose-dependent increase of ABCG2 gene expression and transporter protein levels.", "entity1": "AhR", "entity2": "TCDD", "span1": [13, 16], "span2": [20, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7756": {"label": 2, "data": {"text": "However, chronic treatment of cLH rats with MPEP did not reverse learned helplessness, indicating that the enhanced mGlu5 receptor function is not the only player in the behavioral phenotype of this genetic model of depression.", "entity1": "mGlu5 receptor", "entity2": "MPEP", "span1": [116, 130], "span2": [44, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15266": {"label": 2, "data": {"text": "Three variables of cardiac vagal effects (the root mean square of successive differences [rMSSD] in the interbeat interval of the heart rate [IBI], heart-rate variability [HRV] caused by peak-valley respiratory sinus arrhythmia [pvRSA], and high-frequency power [HF]) and heart rate (HR) were obtained at seven time points during the clamps, characterised by increasing levels of insulin (achieved by administering insulin plus glucose, glucose only, glucose and GLP-1, and glucose and GLP-1 combined with arginine).", "entity1": "insulin", "entity2": "glucose", "span1": [380, 387], "span2": [474, 481]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12913": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CSE", "entity2": "H(2)S", "span1": [119, 122], "span2": [18, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1428": {"label": 3, "data": {"text": "They included the COX-1 inhibitor indomethacin; the COX-2 inhibitor NS-398; the mixed COX-1/COX-2 inhibitor ibuprofen; the nitric oxide (NO) derivatives of indomethacin, ibuprofen and flurbiprofen; the 5-LOX inhibitor REV 5901; and the 5-LOX activating protein (FLAP) inhibitor MK-886.", "entity1": "5-LOX", "entity2": "REV 5901", "span1": [202, 207], "span2": [218, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8446": {"label": 1, "data": {"text": "The docking data indicated that l-glutamine bind to the GLP-1 receptor.", "entity1": "GLP-1 receptor", "entity2": "l-glutamine", "span1": [56, 70], "span2": [32, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6656": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "cyclooxygenase-2", "entity2": "salsalate", "span1": [62, 78], "span2": [164, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16020": {"label": 0, "data": {"text": "These results show that haloperidol promotes mTORC1- and S6K1-dependent phosphorylation of rpS6 at Ser240/244, in a subpopulation of striatal MSNs expressing D2Rs.", "entity1": "rpS6", "entity2": "Ser", "span1": [91, 95], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6747": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "c-Kit", "entity2": "STI571", "span1": [208, 213], "span2": [99, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4570": {"label": 3, "data": {"text": "Nitric oxide products of VP-16 displayed significantly diminished topoisomerase II-dependent cleavage of DNA and cytotoxicity to human HL-60 leukemia cells.", "entity1": "topoisomerase II", "entity2": "VP-16", "span1": [66, 82], "span2": [25, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4741": {"label": 3, "data": {"text": "Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects.", "entity1": "MLCK", "entity2": "Genistin", "span1": [46, 50], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7027": {"label": 8, "data": {"text": "Inhibition of [3H]5-HT or [3H]NE uptake by DVS for the hSERT or hNET produced IC50 values of 47.3 +/- 19.4 and 531.3 +/- 113.0 nM, respectively.", "entity1": "hNET", "entity2": "[3H]NE", "span1": [64, 68], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4278": {"label": 3, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "caspase 3", "entity2": "compound C", "span1": [100, 109], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"291": {"label": 0, "data": {"text": "The carbonic anhydrase V produced by a vector containing the full coding sequence, which includes a possible NH2-terminal mitochondrial targeting signal, was proteolytically processed by E. coli and contained several amino-terminal ends.", "entity1": "The carbonic anhydrase V", "entity2": "NH2", "span1": [0, 24], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8820": {"label": 8, "data": {"text": "The precise fashion in which these proteins interact and move cholesterol from the OMM to P450scc, and the means by which cholesterol is loaded into the OMM, remain unclear.", "entity1": "P450scc", "entity2": "cholesterol", "span1": [90, 97], "span2": [62, 73]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3849": {"label": 1, "data": {"text": "Using the viral mimic polyinosinic:polycytidylic acid and the IFN\u03b1/\u03b2 antagonist B18R we furthermore demonstrate the capability of endogenous IFN to promote IL-22-induced STAT1 activation and expression of CXCL10.", "entity1": "CXCL10", "entity2": "polyinosinic:polycytidylic acid", "span1": [205, 211], "span2": [22, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8385": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "HSD", "entity2": "Cd", "span1": [258, 261], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16054": {"label": 3, "data": {"text": "The HCV-PIs boceprevir and telaprevir are both, to different extents, inhibitors of CYP3A.", "entity1": "CYP3A", "entity2": "telaprevir", "span1": [84, 89], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15651": {"label": 1, "data": {"text": "Excess of cholesterol converted into 24OHC may up-regulate ApoE synthesis which is a scavenger for A\u03b2 and Tau.", "entity1": "Tau", "entity2": "cholesterol", "span1": [106, 109], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7836": {"label": 2, "data": {"text": "L-BMAA induced ER stress and enhanced caspase 12 cleavage in human neuroblastoma SH-SY5Y cells at low nonexcitotoxic concentrations.", "entity1": "caspase 12", "entity2": "L-BMAA", "span1": [38, 48], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13945": {"label": 1, "data": {"text": "denopamine for beta(1); clenbuterol, AZ 40140d, salbutamol for beta(2)) were found to have subtype-selective intrinsic efficacy.", "entity1": "beta(1)", "entity2": "denopamine", "span1": [15, 22], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13258": {"label": 2, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "mucin", "entity2": "leukotriene D(4)", "span1": [114, 119], "span2": [60, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3063": {"label": 5, "data": {"text": "Plerixafor, a CXCR4 antagonist for the mobilization of hematopoietic stem cells.", "entity1": "CXCR4", "entity2": "Plerixafor", "span1": [14, 19], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13502": {"label": 3, "data": {"text": "In this study the neuromuscular blocking drug vecuronium and the controls gallamine and pancuronium slowed the rate of atropine induced [(3)H]N-methylscopolamine dissociation from Chinese hamster ovary cells expressing recombinant human muscarinic M2 receptors K(off) values min(-1); vecuronium (125 nM), atropine 0.45+/-0.07+blocker 0.04+/-0.02; gallamine (21 nM), atropine 0.42+/-0.05+blocker 0.15+/-0.04; pancuronium(21 nM), atropine 0.36+/-0.03+blocker 0.03+/-0.01).", "entity1": "human muscarinic M2 receptors", "entity2": "vecuronium", "span1": [231, 260], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11079": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "calmodulin-dependent enzymes", "entity2": "t-butyl", "span1": [56, 84], "span2": [257, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10259": {"label": 3, "data": {"text": "The ensuing radioactive outflow from these cultures was enhanced by desipramine and reserpine, but reduced (in the presence of desipramine) by the OCT3 inhibitors cyanine 863, oestradiol and corticosterone.", "entity1": "OCT3", "entity2": "corticosterone", "span1": [147, 151], "span2": [191, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5623": {"label": 8, "data": {"text": "Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M.", "entity1": "HERG", "entity2": "K+", "span1": [99, 103], "span2": [41, 43]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3368": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.3", "entity2": "pentobarbital", "span1": [0, 8], "span2": [41, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4433": {"label": 3, "data": {"text": "A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes.", "entity1": "dipeptidyl peptidase 4", "entity2": "xanthine", "span1": [149, 171], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4174": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "cinnamic aldehyde", "span1": [118, 122], "span2": [204, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7277": {"label": 8, "data": {"text": "Some of the compounds investigated in this study might be used as additives in toothpastes for reducing the acidification produced by the relevant CO2 hydrase activity of enamel CA VI, which leads to the formation of protons and bicarbonate and may have a role in cariogenesis.", "entity1": "CA VI", "entity2": "bicarbonate", "span1": [178, 183], "span2": [229, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13475": {"label": 1, "data": {"text": "In contrast, GLP-1 exerts glucoregulatory actions via slowing of gastric emptying and glucose-dependent inhibition of glucagon secretion.", "entity1": "glucagon", "entity2": "glucose", "span1": [118, 126], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7437": {"label": 4, "data": {"text": "(-)-Stepholidine (SPD), an active ingredient of the Chinese herb Stephania, is the first compound found to have dual function as a dopamine receptor D1 agonist and D2 antagonist.", "entity1": "dopamine receptor D1", "entity2": "(-)-Stepholidine", "span1": [131, 151], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10197": {"label": 3, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP-B", "entity2": "rifampicin", "span1": [56, 62], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13344": {"label": 8, "data": {"text": "Lymphocytes possess the essential components of a cholinergic system, including acetylcholine (ACh); choline acetyltransferase (ChAT), its synthesizing enzyme; and both muscarinic and nicotinic ACh receptors (mAChRs and nAChRs, respectively).", "entity1": "choline acetyltransferase", "entity2": "ACh", "span1": [101, 126], "span2": [95, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12015": {"label": 1, "data": {"text": "We investigated the diurnal expression of clock genes and clock-controlled genes (CCGs) in 3-hour intervals for a 24-h period in the livers of male streptozotocin (STZ)-treated rats, male spontaneous type 1 diabetic LEW.1AR1-iddm (Iddm) rats, and Iddm rats treated for 10 days with insulin.", "entity1": "clock-controlled genes", "entity2": "STZ", "span1": [58, 80], "span2": [164, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7067": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARbeta", "entity2": "retinoid", "span1": [52, 59], "span2": [115, 123]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13316": {"label": 1, "data": {"text": "ENaC expression and activity could account for the low Na(+) concentration that is typical of milk.", "entity1": "ENaC", "entity2": "Na(+)", "span1": [0, 4], "span2": [55, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7467": {"label": 8, "data": {"text": "We have expressed VIAAT and the plasmalemmal transporters for glycine and GABA in a neuroendocrine cell line and measured the quantal release of glycine and GABA using a novel double-sniffer patch-clamp technique.", "entity1": "plasmalemmal transporters", "entity2": "glycine", "span1": [32, 57], "span2": [62, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15604": {"label": 1, "data": {"text": "All three agents induced mdr1a.fLUC expression (bioluminescence), but only PCN and docetaxel appeared to act primarily via PXR.", "entity1": "PXR", "entity2": "PCN", "span1": [123, 126], "span2": [75, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8933": {"label": 9, "data": {"text": "A positively charged derivative, estramustine sarcosinate, did not inhibit microtubule assembly or alter the composition of the coassembled MAPs.", "entity1": "MAPs", "entity2": "estramustine sarcosinate", "span1": [140, 144], "span2": [33, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"57": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "renin", "entity2": "A-64662", "span1": [41, 46], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5523": {"label": 4, "data": {"text": "Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.", "entity1": "beta2-adrenergic receptor", "entity2": "Salmeterol", "span1": [28, 53], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10253": {"label": 2, "data": {"text": "Although a significant platelet hyperreactivity was observed in the patients, the HPA-1 genotype did not influence basal or ADP-induced CD62P expression.", "entity1": "CD62P", "entity2": "ADP", "span1": [136, 141], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11306": {"label": 3, "data": {"text": "The decrement of p-CREB protein in the nucleus accumbens remained at 24 h (-35 %) and 72 h (-28 %) of ethanol withdrawal, which recovered toward control level after 7 d of ethanol withdrawal.", "entity1": "p-CREB", "entity2": "ethanol", "span1": [17, 23], "span2": [102, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4775": {"label": 3, "data": {"text": "These results suggested that DMBT could inhibit invasion and angiogenesis by downregulation of VEGFand MMP-9, resulting from the inhibition of Akt pathway.", "entity1": "Akt", "entity2": "DMBT", "span1": [143, 146], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14849": {"label": 2, "data": {"text": "Moreover, Acrolein resulted in activation of astrocytes, up-regulation of BACE-1 in cortex and down-regulation of ADAM-10 in hippocampus and cortex.", "entity1": "BACE-1", "entity2": "Acrolein", "span1": [74, 80], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6431": {"label": 3, "data": {"text": "The group treated with pyridostigmine alone showed decreased plasma butyrylcholinesterase (BChE) activity (87% of control), whereas pyridostigmine plus exercise significantly decreased the BChE activity (79% of control), indicating an interactive effect of the combination.", "entity1": "BChE", "entity2": "pyridostigmine", "span1": [91, 95], "span2": [23, 37]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"843": {"label": 3, "data": {"text": "The anticonvulsant felbamate blocks N-methyl-D-asparate (NMDA) receptors but fails to exhibit the neurobehavioral toxicity characteristic of other NMDA receptor antagonists.", "entity1": "N-methyl-D-asparate (NMDA) receptors", "entity2": "felbamate", "span1": [36, 72], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4644": {"label": 2, "data": {"text": "AhR-dependent reporter gene expression in transfected HepG2 cells was increased by pelargonidin in a concentration-dependent manner at 24h.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [0, 3], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7282": {"label": 3, "data": {"text": "Here, we report that the antifibrotic drug 5-methyl-1-phenyl-2-(1H)-pyridone (pirfenidone, PFD) elicits growth-inhibitory effects and reduces TGF-beta2 protein levels in human glioma cell lines.", "entity1": "TGF-beta2", "entity2": "PFD", "span1": [142, 151], "span2": [91, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1839": {"label": 3, "data": {"text": "The activities of ABCA1 and other ATP binding cassette superfamily members are inhibited by the drug glyburide, and SR-BI-mediated lipid transport is blocked by small molecule inhibitors called BLTs.", "entity1": "ATP binding cassette superfamily", "entity2": "glyburide", "span1": [34, 66], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13968": {"label": 3, "data": {"text": "With exposure to rofecoxib, a selective COX-2 inhibitor, breast cancer risk reduction was appreciable (46%), suggesting a possible role for selective COX-2 inhibitors in breast cancer prophylaxis.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [150, 155], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1396": {"label": 3, "data": {"text": "Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes.", "entity1": "nitric-oxide synthase", "entity2": "Gemfibrozil", "span1": [62, 83], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16036": {"label": 3, "data": {"text": "In line with this observation, incubation of striatal slices with okadaic acid and calyculin A, two inhibitors of PP-1, increased Ser240/244 phosphorylation.", "entity1": "PP-1", "entity2": "calyculin A", "span1": [114, 118], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11810": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "p16", "entity2": "PhIP", "span1": [141, 144], "span2": [63, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14971": {"label": 3, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANKL", "entity2": "serine", "span1": [182, 187], "span2": [84, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14550": {"label": 3, "data": {"text": "Six days after (PhTe)(2) injection we found persistent astrogliosis, increased propidium iodide (PI) positive cells in NeuN positive population evidenced by flow cytometry and reduced immunofluorescence for NeuN, suggesting that the in vivo exposure to (PhTe)(2) progressed to neuronal death.", "entity1": "NeuN", "entity2": "(PhTe)(2)", "span1": [207, 211], "span2": [253, 262]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1350": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "dopamine transporter", "entity2": "aryl", "span1": [295, 315], "span2": [139, 143]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10938": {"label": 3, "data": {"text": "Therefore, decreases of PLK and PNPO in the hippocampal CA1 region of aged brains may be involved in aging processes related with gamma-aminobutyric acid (GABA) function.", "entity1": "PLK", "entity2": "gamma-aminobutyric acid", "span1": [24, 27], "span2": [130, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9517": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "RAR beta", "entity2": "retinoid", "span1": [121, 129], "span2": [4, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10389": {"label": 3, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "AChE", "entity2": "rivastigmine", "span1": [143, 147], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7617": {"label": 3, "data": {"text": "Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases.", "entity1": "human epidermal growth factor receptor", "entity2": "Lapatinib", "span1": [31, 69], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2138": {"label": 1, "data": {"text": "Although incubating HASMCs for 48h with thiazolidinediones had no effect on ENT1 mRNA and protein levels, troglitazone acutely inhibited [3H]adenosine uptake and [3H]NBMPR binding of HASMCs with IC50 values of 2.35+/-0.35 and 3.99+/-0.57microM, respectively.", "entity1": "ENT1", "entity2": "[3H]NBMPR", "span1": [76, 80], "span2": [162, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13808": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "Gefitinib", "span1": [233, 246], "span2": [138, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11246": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "SERT", "entity2": "4',7,8-trichloro", "span1": [127, 131], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10685": {"label": 3, "data": {"text": "This manuscript presents the preclinical profile of lumiracoxib, a novel cyclooxygenase-2 (COX-2) selective inhibitor.", "entity1": "cyclooxygenase-2", "entity2": "lumiracoxib", "span1": [73, 89], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5712": {"label": 8, "data": {"text": "AKR1C3 is upregulated in CRPC where it catalyzes the formation of potent androgens.", "entity1": "AKR1C3", "entity2": "androgens", "span1": [0, 6], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3245": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "testosterone", "span1": [13, 16], "span2": [141, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1099": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "physostigmine", "span1": [242, 262], "span2": [96, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15000": {"label": 2, "data": {"text": "In monocytes, both EPA and DHA increased interleukin (IL)-10 without affecting tumor necrosis factor (TNF)-\u03b1 and IL-6.", "entity1": "interleukin (IL)-10", "entity2": "DHA", "span1": [41, 60], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10937": {"label": 5, "data": {"text": "Losartan (COZAAR) is the prototype of a new class of potent and selective angiotensin II (AII) type 1 (AT(1)) receptor antagonists with the largest published preclinical and clinical data base.", "entity1": "angiotensin II (AII) type 1 (AT(1)) receptor", "entity2": "COZAAR", "span1": [74, 118], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3765": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "NF-\u03baB", "entity2": "CCl(4)", "span1": [106, 111], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13670": {"label": 3, "data": {"text": "INTERVENTIONS: In the 8-week run-in period, all participants received the ACE inhibitor cilazapril (5 mg), the ARB telmisartan (80 mg), and the diuretic hydrochlorothiazide (12.5 mg) as double RAAS blockade to achieve the target blood pressure of less than 130/80 mm Hg.", "entity1": "ACE", "entity2": "cilazapril", "span1": [74, 77], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6996": {"label": 3, "data": {"text": "Furthermore, PS liposome-induced PGE2 production was significantly suppressed by indomethacin, a preferential COX-1 inhibitor, but not by NS-398, a selective COX-2 inhibitor.", "entity1": "COX-1", "entity2": "indomethacin", "span1": [110, 115], "span2": [81, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"11214": {"label": 1, "data": {"text": "In a panel of human breast cancer and other epithelial tumor cell lines, HER2-overexpressing tumors were particularly sensitive to ZD1839.", "entity1": "HER2", "entity2": "ZD1839", "span1": [73, 77], "span2": [131, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6711": {"label": 3, "data": {"text": "Inhibitory effects of the monoamine oxidase inhibitor tranylcypromine on the cytochrome P450 enzymes CYP2C19, CYP2C9, and CYP2D6.", "entity1": "monoamine oxidase", "entity2": "tranylcypromine", "span1": [26, 43], "span2": [54, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14204": {"label": 1, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "AChE", "entity2": "codeine", "span1": [135, 139], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10692": {"label": 3, "data": {"text": "However, consistent with its low COX-1 inhibitory activity, lumiracoxib at a dose of 100 mg kg(-1) orally caused no ulcers and was significantly less ulcerogenic than diclofenac (P<0.05).", "entity1": "COX-1", "entity2": "diclofenac", "span1": [33, 38], "span2": [167, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12892": {"label": 1, "data": {"text": "While either blockage of HO activity by the HO inhibitor, tin protoporphyrin IX, or down-regulation of HO-1 expression by HO-1 small interfering RNA (siRNA) reversed the inhibitory effects of H(2)S on iNOS expression and NO production, HO-1 overexpression produced the same inhibitory effects of H(2)S. In addition, LPS-induced nuclear factor (NF)-kappaB activation was diminished in RAW264.7 macrophages preincubated with H(2)S. Interestingly, the inhibitory effect of H(2)S on NF-kappaB activation was reversed by the transient transfection with HO-1 siRNA, but was mimicked by either HO-1 gene transfection or treatment with carbon monoxide (CO), an end product of HO-1.", "entity1": "HO-1", "entity2": "H(2)S", "span1": [587, 591], "span2": [470, 475]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13702": {"label": 1, "data": {"text": "Estimated affinities for the fast-inactivated channel state were 81 nM, 312 nM and 227 nM for 4-iodopropofol, 4-bromopropofol and 4-chloropropofol in Na(V)1.4, and 450 nM for 4-chloropropofol in Na(V)1.2.", "entity1": "Na(V)1.4", "entity2": "4-bromopropofol", "span1": [150, 158], "span2": [110, 125]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9602": {"label": 9, "data": {"text": "Here, we report that MgATP and MgADP, but not the Mg salt of gamma-thio-ATP, stabilize the binding of prebound 8-azido-[alpha-32P]ATP to SUR1.", "entity1": "SUR1", "entity2": "Mg", "span1": [137, 141], "span2": [50, 52]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"414": {"label": 1, "data": {"text": "The quinazoline antagonists, prazosin, doxazosin and alfuzosin displayed high affinity but were non selective for the three cloned human alpha 1 adrenoceptors.", "entity1": "human alpha 1 adrenoceptors", "entity2": "prazosin", "span1": [131, 158], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8976": {"label": 5, "data": {"text": "The Schild plots for the competitive antagonists WB4101 and 5-methyl-urapidil against alpha 1a-adrenoceptor-selective agonist methoxamine-induced contraction were linear and had slopes not significantly different from unity, with a pA2 of 9.07 +/- 0.07 (n = 5) for WB4101 and 9.09 +/- 0.05 (n = 3) for 5-methyl-urapidil.", "entity1": "alpha 1a-adrenoceptor", "entity2": "5-methyl-urapidil", "span1": [86, 107], "span2": [60, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2533": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "heterocyclic amine", "span1": [311, 317], "span2": [139, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2190": {"label": 0, "data": {"text": "Comparisons of the structures of the cyanobacterial toxin:phosphatase complexes explain the biochemical mechanism by which microcystins but not nodularins permanently modify their protein phosphatase targets by covalent addition to an active site cysteine residue.", "entity1": "protein phosphatase", "entity2": "cysteine", "span1": [180, 199], "span2": [247, 255]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15468": {"label": 0, "data": {"text": "Here, we report that a specific 29-amino acid peptide derived from the intracellular domain fragment of p75(NTR) interacts with and potentiates binding of NGF to TrkA-expressing cells, leading to increased neurite outgrowth in sympathetic neurons as a result of enhanced Erk1/2 and Akt signaling.", "entity1": "p75(NTR)", "entity2": "amino acid", "span1": [104, 112], "span2": [35, 45]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10594": {"label": 1, "data": {"text": "Even though its inability to shift between the trivalent and a divalent oxidation state precludes that gallium behaves as an iron analogue in every respect, it strongly interferes with cellular acquisition of iron from blood by competitive interaction with transferrin and transferrin receptor-mediated endocytosis.", "entity1": "transferrin receptor", "entity2": "gallium", "span1": [273, 293], "span2": [103, 110]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5999": {"label": 2, "data": {"text": "Whole-cell voltage-clamp of hNET-293 cells reveals NE-induced, Na(+)-dependent currents blocked by antidepressants and cocaine that are absent in parental cells.", "entity1": "hNET", "entity2": "NE", "span1": [28, 32], "span2": [51, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6337": {"label": 1, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "eprosartan", "span1": [18, 21], "span2": [226, 236]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10698": {"label": 8, "data": {"text": "Ex vivo, lumiracoxib inhibited COX-1-derived thromboxane B(2) (TxB(2)) generation with an ID(50) of 33 mg kg(-1), whereas COX-2-derived production of prostaglandin E(2) (PGE(2)) in the lipopolysaccharide-stimulated rat air pouch was inhibited with an ID(50) value of 0.24 mg kg(-1).", "entity1": "COX-2", "entity2": "prostaglandin E(2)", "span1": [122, 127], "span2": [150, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4910": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "superoxide dismutase", "entity2": "glucose", "span1": [161, 181], "span2": [276, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7419": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA.", "entity1": "D6D", "entity2": "ALA", "span1": [31, 34], "span2": [241, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5831": {"label": 3, "data": {"text": "The benzothiophene hydroxyurea, zileuton, is the first selective 5-LO inhibitor evaluated for the treatment of patients with IBD.", "entity1": "5-LO", "entity2": "zileuton", "span1": [65, 69], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3506": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "Aldo-keto reductases", "entity2": "oxygen", "span1": [0, 20], "span2": [167, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"458": {"label": 5, "data": {"text": "Chlorpheniramine (10 microM), another histamine H1 receptor antagonist without significant 5-HT receptor binding affinity, did not produce any inhibition of the eNANC contraction.", "entity1": "histamine H1 receptor", "entity2": "Chlorpheniramine", "span1": [38, 59], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12962": {"label": 3, "data": {"text": "Reduction of cerebral infarct size by the AT1-receptor blocker candesartan, the HMG-CoA reductase inhibitor rosuvastatin and their combination.", "entity1": "AT1", "entity2": "candesartan", "span1": [42, 45], "span2": [63, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"971": {"label": 3, "data": {"text": "Expression of the dominant negative mutants rab5A-N133I or rab7-N125I blunted U50,488H-induced down-regulation.", "entity1": "N133I", "entity2": "U50,488H", "span1": [50, 55], "span2": [78, 86]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2339": {"label": 1, "data": {"text": "NO rebinding in HNS from Staphylococcus aureus (SA-HNS) is faster than that measured for either Bacillus anthracis (BA-HNS) or for eNOS(HD) in both oxidized and reduced forms in the presence of arginine.", "entity1": "BA-HNS", "entity2": "NO", "span1": [116, 122], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1653": {"label": 5, "data": {"text": "The 5-HT(1/2/5/7)-receptor antagonist methysergide and the 5-HT(2A/2B/2C)-receptor antagonist LY 53857 enhanced clomipramine-induced hyperglycemia, while the 5-HT(1A/1B)-receptor antagonist (-)-propranolol and the 5-HT(3/4)-receptor antagonist tropisetron did not affect it.", "entity1": "5-HT(2A/2B/2C)-receptor", "entity2": "LY 53857", "span1": [59, 82], "span2": [94, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4670": {"label": 3, "data": {"text": "SIRT1 co-precipitated with PPAR\u03b1 and nicotinamide increased the acetylation of the PPAR\u03b1 coactivator PGC-1\u03b1, which was suppressed by resveratrol.", "entity1": "PGC-1\u03b1", "entity2": "resveratrol", "span1": [101, 107], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6805": {"label": 9, "data": {"text": "Because thalidomide does not completely inhibit COX-2 expression or PG biosynthesis, a therapeutic strategy combining celecoxib with thalidomide might be more effective than using either agent alone.", "entity1": "COX-2", "entity2": "thalidomide", "span1": [48, 53], "span2": [8, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"929": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "5-Fluorouracil", "span1": [238, 240], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"638": {"label": 9, "data": {"text": "The effect of sumatriptan, but not of LY 344864, was prevented by pretreatment with the antagonist SDZ 21-009, which displays high affinity for rat 5-HT1B receptors.", "entity1": "rat 5-HT1B", "entity2": "LY 344864", "span1": [144, 154], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6818": {"label": 2, "data": {"text": "Each statin induced apoA-I expression (mRNA and protein) dose-dependently: the rank order of the apoA-I induction pitavastatin (3 microM)>simvastatin (10 microM)>atorvastatin (30 microM).", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [97, 103], "span2": [114, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5597": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "clozapine", "span1": [171, 177], "span2": [128, 137]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15389": {"label": 3, "data": {"text": "7-Methoxy-6-[4-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-5-yl]-1,3-benzothiazole 11 (TASP0382088) was synthesized and evaluated as transforming growth factor-\u03b2 (TGF-\u03b2) type I receptor (also known as activin receptor-like kinase 5 or ALK5) inhibitor.", "entity1": "ALK5", "entity2": "TASP0382088", "span1": [231, 235], "span2": [83, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10666": {"label": 0, "data": {"text": "We found a strong interaction of baseline FEV(1) with the Arg16Glycine (Gly) polymorphism in predicting bronchodilator response.", "entity1": "Arg16Glycine", "entity2": "Gly", "span1": [58, 70], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9336": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "kainate", "span1": [72, 77], "span2": [102, 109]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7549": {"label": 8, "data": {"text": "ORN levels (measured by an HPLC procedure) were dose- and time-dependently increased in PLZ-treated animals, with levels reaching approximately 650% of control at 6 and 12 h. Pretreatment with TCP completely abolished the PLZ-induced increase in brain ORN, suggesting, as with GABA, that a metabolite of PLZ formed by the action of MAO is responsible for the elevation of brain ORN observed.", "entity1": "MAO", "entity2": "PLZ", "span1": [332, 335], "span2": [304, 307]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9570": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "IFN-gamma", "entity2": "fenoterol", "span1": [31, 40], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15625": {"label": 9, "data": {"text": "Furthermore, nobiletin could inhibit HGF-induced the membrane localization of phosphorylated c-Met, ERK2, and Akt, but not phosphorylated JNK1/2 and p38.", "entity1": "p38", "entity2": "nobiletin", "span1": [149, 152], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9303": {"label": 3, "data": {"text": "The present study utilized blood from normal volunteers and 125I-fibrinogen in a dilute whole blood clot assay to determine the relative concentrations of lysine analogues required for inhibition of clot lysis induced by exogenous t-PA. AMCA (0.06 mM) and EACA (0.6 mM) were effective in prolonging clot lysis if (1) whole blood clots were formed and then exposed to a lysine analogue and exogenous t-PA or if (2) whole blood clots were formed in the presence of exogenous t-PA and a lysine analogue.", "entity1": "t-PA", "entity2": "EACA", "span1": [399, 403], "span2": [256, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3699": {"label": 3, "data": {"text": "Insulin secretion stimulated by both 200 \u03bcM tolbutamide and 20 \u03bcM gliclazide, concentrations that had equivalent effects on membrane potential, was inhibited by thapsigargin (1 \u03bcM) or the L-type Ca(2+) channel blocker nicardipine (2 \u03bcM) and was potentiated by 8-pCPT-2'-O-Me-cAMP-AM at concentrations \u22652 \u03bcM in INS-1 cells.", "entity1": "L-type Ca(2+) channel", "entity2": "nicardipine", "span1": [188, 209], "span2": [218, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2547": {"label": 9, "data": {"text": "Imatinib was also found to inhibit M-CSF-induced osteoclast survival as well as M-CSF-induced osteoclast bone resorbing activity, but was without effect on interleukin 1alpha (IL-1alpha) and receptor activator of nuclear factor kappa B ligand (RANKL)-induced inhibition of osteoclasts apoptosis, further supporting the hypothesis that imatinib may affect mature osteoclasts through the inhibition of c-FMS.", "entity1": "RANKL", "entity2": "Imatinib", "span1": [244, 249], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12047": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPV2", "entity2": "apomorphine", "span1": [27, 33], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4639": {"label": 2, "data": {"text": "Overall, although most anthocyanidins had no effects on AhR-CYP1A1 signaling, pelargonidin can bind to and activate the AhR and AhR-dependent gene expression, and pelargonidin and delphinidin inhibit the CYP1A1 catalytic activity.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [120, 123], "span2": [78, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14003": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "MET", "entity2": "XL184", "span1": [86, 89], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4599": {"label": 3, "data": {"text": "A significant decrease in HLA-DR expression was observed in the AP and fractionated procyanidin-treated cells in the presence of ovalbumin (OVA), but no effect on CD86 expression was observed.", "entity1": "HLA-DR", "entity2": "procyanidin", "span1": [26, 32], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2282": {"label": 2, "data": {"text": "In addition to this evidence (for the involvement of EP2 receptors), evidence for the involvement of EP1 receptors in the PGE1 mediated stimulation of Na,K-ATPase beta subunit gene transcription includes the stimulatory effect of 17-phenyl trinor PGE2, as well as the inhibitory effects of SC-51089.", "entity1": "Na,K-ATPase beta", "entity2": "PGE1", "span1": [151, 167], "span2": [122, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13287": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "VEGFR", "entity2": "Sorafenib", "span1": [300, 305], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4367": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "cytochrome P450 3A", "entity2": "dexamethasone 21-phosphate", "span1": [151, 169], "span2": [192, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10920": {"label": 3, "data": {"text": "Using [(3)H]glucosamine-labeled gastric mucosal cells, we show that stimulatory effect of beta-adrenergic agonist, isoproterenol, on mucin secretion was inhibited by EGFR kinase inhibitor, PD153035, as well as wortmannin, a specific inhibitor of PI3K.", "entity1": "mucin", "entity2": "wortmannin", "span1": [133, 138], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5362": {"label": 3, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C. To further validate the result, we examined sub-cellular distribution of c-Rel in lungs of CS-exposed guinea pigs treated or untreated with vitamin C. Result showed that vitamin C treatment resulted in markedly reduced c-Rel nuclear translocation.", "entity1": "c-Rel", "entity2": "vitamin C", "span1": [398, 403], "span2": [349, 358]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7952": {"label": 2, "data": {"text": "A reporter construct driven by 4 kb of the chicken ras-dva 5'-flanking region, containing six putative pituitary-specific transcription factor-1 (Pit-1) binding sites and two potential glucocorticoid receptor (GR) binding sites, was highly activated in embryonic pituitary cells and up-regulated by corticosterone.", "entity1": "glucocorticoid receptor (GR) binding sites", "entity2": "corticosterone", "span1": [185, 227], "span2": [299, 313]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6820": {"label": 2, "data": {"text": "Each statin induced apoA-I expression (mRNA and protein) dose-dependently: the rank order of the apoA-I induction pitavastatin (3 microM)>simvastatin (10 microM)>atorvastatin (30 microM).", "entity1": "apoA-I", "entity2": "atorvastatin", "span1": [97, 103], "span2": [162, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3324": {"label": 2, "data": {"text": "Apoptosis studies (DAPI staining and caspase 3 activity) showed a marked increase in the presence of MXF and VP-16 compared to VP-16 alone.", "entity1": "caspase 3", "entity2": "MXF", "span1": [37, 46], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5419": {"label": 1, "data": {"text": "CONCLUSIONS: The SSRI citalopram modulates central noradrenergic neurotransmission by activation, through endogenous serotonin, of 5-HT3 receptors expressed in the somatodendritic (LC) and terminal (PFC) areas, which subsequently promote an enhancement of local NA.", "entity1": "5-HT3", "entity2": "citalopram", "span1": [131, 136], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7002": {"label": 8, "data": {"text": "These observations strongly suggest that the up-regulation of terminal PGESs that are preferentially coupled with COX-1, especially mPGES-2, plays the pivotal role in PS liposome-induced PGE2 production by microglia.", "entity1": "mPGES-2", "entity2": "PGE2", "span1": [132, 139], "span2": [187, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7271": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "sulpiride", "span1": [218, 224], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5922": {"label": 1, "data": {"text": "Analysis of this relationship shows that estramustine phosphate and tubulin compete for common MAP2 sites, that MAP2 can bind 5-6 moles.mole-1 estramustine phosphate, and that the Kd of these sites is congruent to 20 microM estramustine phosphate.", "entity1": "MAP2", "entity2": "estramustine phosphate", "span1": [112, 116], "span2": [224, 246]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12939": {"label": 8, "data": {"text": "Sources of L-arg include dietary proteins and endogenous synthesis by argininosuccinate synthetase and argininosuccinate lyase.", "entity1": "argininosuccinate synthetase", "entity2": "L-arg", "span1": [70, 98], "span2": [11, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11403": {"label": 1, "data": {"text": "Here, we show that meclofenamic acid (meclofenamate) and diclofenac, two related molecules previously used as anti-inflammatory drugs, act as novel KCNQ2/Q3 channel openers.", "entity1": "KCNQ2/Q3", "entity2": "meclofenamic acid", "span1": [148, 156], "span2": [19, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3166": {"label": 1, "data": {"text": "A few compounds, 17alpha-methyltestosterone (17alpha-MT), vinclozolin and linuron, were studied using a real world scenario, i.e., assuming that their interaction with the AR was not known: A prescreening for agonism and true, competitive antagonism was used to select conditions such as the appropriate mode of action, and the working range excluding cytotoxicity for the final screening.", "entity1": "AR", "entity2": "17alpha-MT", "span1": [172, 174], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9869": {"label": 1, "data": {"text": "In this study, we investigated the effect of troglitazone, a ligand of the nuclear receptor peroxisome proliferator activated receptor-gamma, on PAI-1 expression and secretion in human adipocytes.", "entity1": "peroxisome proliferator activated receptor-gamma", "entity2": "troglitazone", "span1": [92, 140], "span2": [45, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10449": {"label": 8, "data": {"text": "Formation of pyruvate by SDH is a two-step reaction in which the hydroxyl group of serine is cleaved to produce aminoacrylate, and then the aminoacrylate is deaminated by nonenzymatic hydrolysis to produce pyruvate.", "entity1": "SDH", "entity2": "pyruvate", "span1": [25, 28], "span2": [206, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4719": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Rspo3", "entity2": "TCDD", "span1": [314, 319], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1136": {"label": 6, "data": {"text": "A great deal of information has now accumulated pertaining to the mechanisms by which nuclear receptors, such as the androgen receptor, modulate the activity of responsive genes.", "entity1": "nuclear receptors", "entity2": "androgen", "span1": [86, 103], "span2": [117, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2223": {"label": 9, "data": {"text": "This mutation is inherently resistant to imatinib and, to date, there remains no effective curative therapy for systemic mastocytosis associated with KITD816V.", "entity1": "KIT", "entity2": "imatinib", "span1": [150, 153], "span2": [41, 49]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9790": {"label": 3, "data": {"text": "New modes of therapy have recently been introduced, and data on the cyclooxygenase-2 (COX-2)-specific inhibitors celecoxib and rofecoxib suggest that these agents will meet the need for safe and effective therapeutic alternatives to conventional NSAIDs.", "entity1": "cyclooxygenase-2", "entity2": "celecoxib", "span1": [68, 84], "span2": [113, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9974": {"label": 8, "data": {"text": "COX-2 produces prostaglandins that inhibit apoptosis and stimulate angiogenesis and invasiveness.", "entity1": "COX-2", "entity2": "prostaglandins", "span1": [0, 5], "span2": [15, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12679": {"label": 1, "data": {"text": "Rofecoxib has greater selectivity for COX-2 than celecoxib, meloxicam, diclofenac and indomethacin.", "entity1": "COX-2", "entity2": "diclofenac", "span1": [38, 43], "span2": [71, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7122": {"label": 0, "data": {"text": "Truncated proteins with a complete GAF-B were dimers, but those lacking the N-terminal 46 amino acids of GAF-B were monomers, indicating that these residues are vital for GAF-B-mediated PDE5 dimerization.", "entity1": "GAF-B", "entity2": "N", "span1": [105, 110], "span2": [76, 77]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9175": {"label": 1, "data": {"text": "Each adduct had a reduced ability to activate cyclic nucleotide phosphodiesterase and myosin light chain kinase, and the chlorpromazine binding capacities of the phenoxybenzamine-calmodulin adducts were diminished to the extent of phenoxybenzamine incorporation into each adduct.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [179, 189], "span2": [162, 178]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6269": {"label": 3, "data": {"text": "At clinically relevant concentrations, candesartan is an insurmountable and long-lasting antagonist of the vascular contractile responses to Ang II.", "entity1": "Ang II", "entity2": "candesartan", "span1": [141, 147], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5158": {"label": 3, "data": {"text": "ThioTEPA (CYP2B6 inhibitor, 25 \u03bcM) and the monoclonal antibody against CYP2B6 but not troleandomycin (CYP3A4 inhibitor, 25 \u03bcM) or the monoclonal antibody against CYP3A4 inhibited ketamine N-demethylation at clinically relevant concentrations.", "entity1": "CYP3A4", "entity2": "troleandomycin", "span1": [102, 108], "span2": [86, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5109": {"label": 2, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "HO-1", "entity2": "5HHMF", "span1": [174, 178], "span2": [43, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14104": {"label": 1, "data": {"text": "Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.", "entity1": "Cereblon", "entity2": "pomalidomide", "span1": [0, 8], "span2": [110, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4663": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "NADPH oxidase", "entity2": "resveratrol", "span1": [85, 98], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7754": {"label": 0, "data": {"text": "The structures of active and inactive alanine-mutated cyclic peptides, and of phospholamban (1-36), were determined by NMR.", "entity1": "cyclic peptides", "entity2": "alanine", "span1": [54, 69], "span2": [38, 45]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12067": {"label": 1, "data": {"text": "The second part of this study consisted of looking for possible changes in central 5-HT receptors 24 h after either a single or a repeated (for 14 days) treatment with amoxapine (10 mg/kg i.p. each day) or amitriptyline (10 mg/kg i.p.).", "entity1": "5-HT receptors", "entity2": "amitriptyline", "span1": [83, 97], "span2": [206, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9937": {"label": 3, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "NF-kappaB", "entity2": "sulfasalazine", "span1": [9, 18], "span2": [269, 282]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10688": {"label": 3, "data": {"text": "Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2.", "entity1": "cyclooxygenase-2", "entity2": "lumiracoxib", "span1": [72, 88], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8524": {"label": 9, "data": {"text": "CYP3A4 and CYP3A5 metabolized BDP via hydroxylation ([M4] and [M6]) and dehydrogenation ([M5]) at similar rates; CYP3A7 did not metabolize BDP.", "entity1": "CYP3A7", "entity2": "BDP", "span1": [113, 119], "span2": [139, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8363": {"label": 1, "data": {"text": "Reduced binding affinity means that diflunisal is more easily released from acetylated albumin into the circulation.", "entity1": "acetylated albumin", "entity2": "diflunisal", "span1": [76, 94], "span2": [36, 46]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10597": {"label": 1, "data": {"text": "Apart from the consequences of iron deprivation, gallium exerts cytotoxic effects by direct interaction with the iron-dependent enzyme ribonucleotide reductase, resulting in reduced dNTP pools and inhibition of DNA synthesis.", "entity1": "ribonucleotide reductase", "entity2": "gallium", "span1": [135, 159], "span2": [49, 56]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8207": {"label": 1, "data": {"text": "Stenesen and colleagues (2012) activate AMPK both directly and indirectly by altering AMP biosynthesis to slow aging in Drosophila, highlighting AMPK as a conserved life span modulator that links energy sensing to longevity.", "entity1": "AMPK", "entity2": "AMP", "span1": [40, 44], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3050": {"label": 8, "data": {"text": "PGE(2) is synthesized from arachidonic acid by cyclooxygenases (COX) and prostaglandin E synthases (PGES) and mediates its biological activity through binding to the four prostanoid receptors EP(1) through EP(4).", "entity1": "PGES", "entity2": "arachidonic acid", "span1": [100, 104], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12806": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "c-kit", "entity2": "Gleevec", "span1": [120, 125], "span2": [88, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4458": {"label": 2, "data": {"text": "However, after 12h CdCl2 treatment, cell viability diminished in 50%, accompanied by a drastic decrease of metallothionein-II production, and an increase in p53 activation and the pro-apoptotic protein Bax.", "entity1": "p53", "entity2": "CdCl2", "span1": [157, 160], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13369": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "ghrelin", "entity2": "estrogen", "span1": [131, 138], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8450": {"label": 2, "data": {"text": "The objective of the present investigation was to evaluate l-glutamine increases glucagon like peptide-1 (GLP-1) (7-36) amide secretion in streptozotocin-nicotinamide (STZ-NTM) induced diabetic Sprague Dawley rats.", "entity1": "GLP-1", "entity2": "l-glutamine", "span1": [106, 111], "span2": [59, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7197": {"label": 2, "data": {"text": "ADP initiates platelet aggregation by 'simultaneous activation of two G protein-coupled receptors, P2Y1 and P2Y12.", "entity1": "P2Y1", "entity2": "ADP", "span1": [99, 103], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11774": {"label": 1, "data": {"text": "Western blot analyses showed significant effects of Pb exposure on DNMT1, DNMT3a, and MeCP2 expression, with effects often seen at the lowest level of exposure and modified by sex and developmental window of Pb exposure.", "entity1": "DNMT1", "entity2": "Pb", "span1": [67, 72], "span2": [52, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15605": {"label": 1, "data": {"text": "All three agents induced mdr1a.fLUC expression (bioluminescence), but only PCN and docetaxel appeared to act primarily via PXR.", "entity1": "PXR", "entity2": "docetaxel", "span1": [123, 126], "span2": [83, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12807": {"label": 3, "data": {"text": "However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50.", "entity1": "COX-2", "entity2": "carprofen", "span1": [164, 169], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3003": {"label": 1, "data": {"text": "Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors.", "entity1": "phosphodiesterase-5", "entity2": "cyclic guanosine monophosphate", "span1": [24, 43], "span2": [107, 137]}, "weak_labels": [0, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12415": {"label": 8, "data": {"text": "This methodology was subsequently used to assess the relative contribution of OATP1B1 uptake in human hepatocytes for olmesartan (42%-62%), valsartan (28%-81%), rosuvastatin (64%-72%), pitavastatin (84%-98%) and lopinavir (64%-89%).", "entity1": "OATP1B1", "entity2": "valsartan", "span1": [78, 85], "span2": [140, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3433": {"label": 2, "data": {"text": "Epi increased the activity of the human WNT6 promoter through Cav1-dependent binding of \u03b2-catenin to the proximal WNT6 promoter.", "entity1": "human WNT6 promoter", "entity2": "Epi", "span1": [34, 53], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15987": {"label": 8, "data": {"text": "Protein levels of the glucose transporter (GLUT4) involved in glucose transport via these two pathways were also increased.", "entity1": "glucose transporter", "entity2": "glucose", "span1": [22, 41], "span2": [62, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7432": {"label": 1, "data": {"text": "Potential binding conformations of D1 and D2 receptors were obtained, and the D1-SPD and D2-SPD complexes were generated, which are in good agreement with most of experimental data.", "entity1": "D1", "entity2": "SPD", "span1": [78, 80], "span2": [81, 84]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2315": {"label": 3, "data": {"text": "Sulindac metabolites simultaneously (a) increase cellular cyclic GMP and subsequently activate cyclic GMP-dependent protein kinase (PKG); (b) activate c-jun NH2-terminal kinase (JNK); (c) inhibit extracellular signal-regulated kinase 1/2 (ERK1/2); and (d) decrease beta-catenin protein expression at times and doses consistent with apoptosis.", "entity1": "c-jun NH2-terminal kinase", "entity2": "Sulindac", "span1": [151, 176], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15929": {"label": 1, "data": {"text": "Posttranslational modification of the neural cell adhesion molecule (NCAM) by polysialic acid (polySia) is well studied in the nervous system and described as a dynamic modulator of plastic processes like precursor cell migration, axon fasciculation, and synaptic plasticity.", "entity1": "neural cell adhesion molecule", "entity2": "polySia", "span1": [38, 67], "span2": [95, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14106": {"label": 1, "data": {"text": "Our biophysical, biochemical and gene silencing studies show that CRBN is a proximate, therapeutically important molecular target of lenalidomide and pomalidomide.", "entity1": "CRBN", "entity2": "lenalidomide", "span1": [66, 70], "span2": [133, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9074": {"label": 1, "data": {"text": "13cisRA and ROAc, but not 4HPR, caused a dose-dependent reduction in plasma osteocalcin, an effect that correlated with retinoid-induced bone effects.", "entity1": "osteocalcin", "entity2": "retinoid", "span1": [76, 87], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1417": {"label": 4, "data": {"text": "RESULTS: In drug discrimination studies, lisuride fully mimicked the 5-HT(1A) agonist LY 293284, only partially substituted for LSD and DOI, and failed to substitute for (+)-amphetamine.", "entity1": "5-HT(1A)", "entity2": "LY 293284", "span1": [69, 77], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6626": {"label": 1, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "ornithine", "span1": [3, 9], "span2": [33, 42]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13540": {"label": 2, "data": {"text": "The transcriptional activity of torafugu PPARalpha1 was enhanced 4.5- and 11.5-fold by Wy-14643 and 5,8,11,14-eicosatetraynoic acid (ETYA) each at 10 microM, respectively, whereas that of PPARalpha2, 4.5- and 7.3-fold at the same concentration of the respective ligands, respectively.", "entity1": "PPARalpha1", "entity2": "Wy-14643", "span1": [41, 51], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12006": {"label": 2, "data": {"text": "The results showed that administration of AlCl3 resulted in a significant elevation in the levels of AchE activity, CRP, NF-\u03baB, and MCP-1 accompanied with a significant depletion in the Ach level.", "entity1": "CRP", "entity2": "AlCl3", "span1": [116, 119], "span2": [42, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14724": {"label": 4, "data": {"text": "We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenine moiety.", "entity1": "TLR7", "entity2": "adenine", "span1": [57, 61], "span2": [187, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5816": {"label": 9, "data": {"text": "In four cultured human corticotropic adenomas, loperamide was not able to reduce basal and CRH-induced ACTH secretion.", "entity1": "ACTH", "entity2": "loperamide", "span1": [103, 107], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8970": {"label": 5, "data": {"text": "Using the alpha 1-adrenoceptor subtype-selective antagonists chlorethylclonidine (CEC), WB4101, and 5-methyl-urapidil, we have examined the possible heterogeneity in the alpha 1-adrenoceptor populations in rabbit aorta.", "entity1": "alpha 1-adrenoceptor", "entity2": "5-methyl-urapidil", "span1": [10, 30], "span2": [100, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9856": {"label": 3, "data": {"text": "Inhibition of the actions of ET-1 by salicylates is apparently competitive.", "entity1": "ET-1", "entity2": "salicylates", "span1": [29, 33], "span2": [37, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4793": {"label": 8, "data": {"text": "Taken together, these data demonstrate that baicalin inhibits the metabolism of DXM in a concentration-dependent manner in rats, possibly through inhibiting hepatic CYP2D and CYP3A activities.", "entity1": "CYP3A", "entity2": "DXM", "span1": [175, 180], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10090": {"label": 8, "data": {"text": "Three replicate studies in the oral surgery model of acute pain used submucosal microdialysis sample collection for the measurement of prostaglandin E2 (PGE2; a product of both COX-1 and COX-2) and thromboxane B2 (as a biomarker for COX-1 activity) with parallel assessments of pain.", "entity1": "COX-1", "entity2": "prostaglandin E2", "span1": [177, 182], "span2": [135, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9444": {"label": 9, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP4", "entity2": "AH-6809", "span1": [118, 121], "span2": [64, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5530": {"label": 2, "data": {"text": "In direct adenylyl cyclase activation, in effects on adenylyl cyclase after pretreatment of intact cells, and in guinea pig tracheal relaxation assays, IAS and the parent drug salmeterol behave essentially the same.", "entity1": "adenylyl cyclase", "entity2": "IAS", "span1": [10, 26], "span2": [152, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7955": {"label": 4, "data": {"text": "To investigate the role of mGluR8 in modulating the synaptic responses of retinal ganglion cells, we used a recently identified positive allosteric modulator of mGluR8, AZ12216052 (AZ) and the mGluR8-specific orthosteric agonist (S)-3,4-dicarboxyphenylglycine (DCPG).", "entity1": "mGluR8", "entity2": "(S)-3,4-dicarboxyphenylglycine", "span1": [193, 199], "span2": [229, 259]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"3770": {"label": 2, "data": {"text": "CCl(4) intoxication caused hepatic necrosis and increased serum ALT activity.", "entity1": "ALT", "entity2": "CCl(4)", "span1": [64, 67], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13": {"label": 1, "data": {"text": "Prostacyclin analogues inhibit tissue factor expression in the human monocytic cell line THP-1 via a cyclic AMP-dependent mechanism.", "entity1": "tissue factor", "entity2": "cyclic AMP", "span1": [31, 44], "span2": [101, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"954": {"label": 2, "data": {"text": "On the basis of data obtained in rabbits, the imidazoline receptor ligand rilmenidine has been suggested to decrease blood pressure in humans by activating central alpha(2A)-adrenoceptors.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "rilmenidine", "span1": [164, 187], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15649": {"label": 1, "data": {"text": "Seventy-four CD8+ clones expressing different V\u03b2 receptors were shown to proliferate and kill target cells via different mechanisms when exposed to abacavir.", "entity1": "V\u03b2 receptors", "entity2": "abacavir", "span1": [46, 58], "span2": [148, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12158": {"label": 9, "data": {"text": "The density of AR in testis and ovary tissues showed no significant difference between NP group and control group at every time-point (P > 0.05).", "entity1": "AR", "entity2": "NP", "span1": [15, 17], "span2": [87, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8429": {"label": 3, "data": {"text": "N-acetylcysteine (NAC, 33 mM) and the c-jun N-terminal kinase (JNK) inhibitor (SP600125, 33 \u03bcM) further decreased the viability in the presence of DEP (200 \u03bcg/ml) and 3.3% FCS.", "entity1": "JNK", "entity2": "SP600125", "span1": [63, 66], "span2": [79, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11582": {"label": 2, "data": {"text": "As add-on therapy in patients with suboptimal glycaemic control despite oral antihyperglycaemic treatment, sitagliptin improved HbA(1c) to a significantly greater extent than placebo when added to metformin or pioglitazone and was noninferior to glipizide when added to metformin.", "entity1": "HbA(1c)", "entity2": "sitagliptin", "span1": [128, 135], "span2": [107, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5510": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "[-]-metazocine", "span1": [108, 126], "span2": [374, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15993": {"label": 1, "data": {"text": "Treatment with the ER antagonist ICI 182,780 abolishes the above actions of puerarin on osteoblast-derived cells.", "entity1": "ER", "entity2": "puerarin", "span1": [19, 21], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3024": {"label": 3, "data": {"text": "In ex vivo experiments with tumor cells from refractory chronic lymphoblastic leukemia, dose-dependent CDK2 inhibition associated with apoptotic changes was seen at concentrations greater than 100 nM of flavopiridol.", "entity1": "CDK2", "entity2": "flavopiridol", "span1": [103, 107], "span2": [203, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15645": {"label": 1, "data": {"text": "These data suggest that T-cells can be activated by abacavir through a direct interaction with surface and intracellular major histocompatibility complex (MHC) molecules.", "entity1": "MHC", "entity2": "abacavir", "span1": [155, 158], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7860": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "KARs", "entity2": "okadaic acid", "span1": [32, 36], "span2": [254, 266]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4521": {"label": 8, "data": {"text": "Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also interact with carboxylesterases.", "entity1": "carboxylesterases", "entity2": "carboxylic acids", "span1": [70, 87], "span2": [133, 149]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10605": {"label": 1, "data": {"text": "Here, we show that the synaptic vesicle protein SV2A is the brain binding site of levetiracetam (LEV), a new antiepileptic drug with a unique activity profile in animal models of seizure and epilepsy.", "entity1": "synaptic vesicle protein SV2A", "entity2": "LEV", "span1": [23, 52], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11417": {"label": 1, "data": {"text": "The crystal structure of R228K-Gal-T1 complexed with LA, UDP-Gal, and Mn(2+) determined at 1.9 A resolution shows that the Asp318 side chain exhibits a minor alternate conformation, compared to that in the wild type.", "entity1": "R228K", "entity2": "UDP-Gal", "span1": [25, 30], "span2": [57, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3446": {"label": 5, "data": {"text": "LY541850 was claimed from human mGlu receptors expressed in non-neuronal cells to be a selective orthosteric mGlu2 agonist and mGlu3 antagonist.", "entity1": "mGlu3", "entity2": "LY541850", "span1": [127, 132], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7013": {"label": 3, "data": {"text": "Sorafenib has the added advantage of inhibiting multiple different Raf isoforms, which enables it to target TGF-alpha/EGFR signaling and may also enhance its inhibition of VEGFR and PDGFR-beta.", "entity1": "TGF-alpha", "entity2": "Sorafenib", "span1": [108, 117], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4520": {"label": 8, "data": {"text": "Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also interact with carboxylesterases.", "entity1": "Uridine 5'-diphosphate- glucuronosyltransferases", "entity2": "carboxylic acids", "span1": [0, 48], "span2": [133, 149]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2726": {"label": 3, "data": {"text": "Sulindac sulfide inhibited 14-3-3epsilon proteins in HT-29 and DLD-1 cells in a time- and concentration-dependent manner.", "entity1": "14-3-3epsilon proteins", "entity2": "Sulindac sulfide", "span1": [27, 49], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1135": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "erg1", "entity2": "pimozide", "span1": [213, 217], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"658": {"label": 3, "data": {"text": "Inhibition of gelatinase A (MMP-2) by batimastat and captopril reduces tumor growth and lung metastases in mice bearing Lewis lung carcinoma.", "entity1": "MMP-2", "entity2": "captopril", "span1": [28, 33], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16018": {"label": 5, "data": {"text": "The involvement of the various DA receptor subtypes in the motor effects of N/OFQ and NOP receptor antagonists was evaluated pharmacologically, using D1/D5 (SCH23390), D2/D3 (raclopride, amisulpride) and D3 (S33084) receptor antagonists, and by using D2 receptor knockout mice.", "entity1": "D3", "entity2": "amisulpride", "span1": [171, 173], "span2": [187, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12177": {"label": 2, "data": {"text": "However, plasma high-density lipoprotein-cholesterol (HDL-C) and HDL-C/total-C ratio levels and plasma paraoxonase activity were only significantly higher in vitamin E group after 8 weeks.", "entity1": "high-density lipoprotein", "entity2": "vitamin E", "span1": [16, 40], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8964": {"label": 1, "data": {"text": "Radioligand binding studies with the nonselective alpha 1-adrenoceptor antagonist radioligand 125I-BE2254 showed that 73-87% of the binding sites in rabbit aorta are CEC sensitive and they are predominantly low affinity sites both for WB4101 (pKd = 8.1) and for 5-methylurapidil (pKd = 7.1).", "entity1": "alpha 1-adrenoceptor", "entity2": "5-methylurapidil", "span1": [50, 70], "span2": [262, 278]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1761": {"label": 3, "data": {"text": "Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016.", "entity1": "ErbB2", "entity2": "GW572016", "span1": [142, 147], "span2": [165, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6316": {"label": 8, "data": {"text": "We found that 5-HT stimulated the conversion of [3H]L-arginine ([3H]L-Arg) to [3H]L-Cit, indicating eNOS activation.", "entity1": "eNOS", "entity2": "[3H]L-Arg", "span1": [100, 104], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14001": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "FLT3", "entity2": "Cabozantinib", "span1": [258, 262], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12219": {"label": 1, "data": {"text": "In response to METH, AMPH, or POHA exposure, the accumulation of cAMP by HEK-293 cells stably expressing different species of TAAR1 was concentration- and isomer-dependent.", "entity1": "TAAR1", "entity2": "METH", "span1": [126, 131], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1798": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "Iressa", "span1": [0, 32], "span2": [113, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12277": {"label": 1, "data": {"text": "It is approved by the FDA for use in combination with capecitabine for the treatment of HER2-positive MBC that has progressed with standard treatment.", "entity1": "HER2", "entity2": "capecitabine", "span1": [88, 92], "span2": [54, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15775": {"label": 3, "data": {"text": "We observed that the administration of ICI at 08:00h on proestrus day produced a 15% inhibition of luminal epithelial cell proliferation, reduced uterine wet weight by 21% and caused reduction of Akt phosphorylation at Ser 473 as compared to vehicle-treated animals, whereas ICI treatment at 00:00h on estrus day had no effect on these parameters.", "entity1": "Akt", "entity2": "ICI", "span1": [196, 199], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9616": {"label": 1, "data": {"text": "Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide.", "entity1": "sulfonylurea receptor", "entity2": "MgADP", "span1": [44, 65], "span2": [31, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"118": {"label": 3, "data": {"text": "Felodipine and the p-chloro analogue inhibited the actin-activated Mg2+-ATPase activity of smooth muscle myosin (IC50 = 25.1 microM).", "entity1": "Mg2+-ATPase", "entity2": "p-chloro", "span1": [67, 78], "span2": [19, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12819": {"label": 1, "data": {"text": "Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives.", "entity1": "pyridoxal kinase", "entity2": "roscovitine", "span1": [21, 37], "span2": [54, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1997": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "EL3", "entity2": "Ser-Glu-Pro", "span1": [91, 94], "span2": [76, 87]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5487": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "progestagens", "span1": [68, 85], "span2": [434, 446]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1591": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "AChE", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine", "span1": [26, 30], "span2": [381, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13766": {"label": 3, "data": {"text": "Here, we characterized the target profile of the dual SRC/ABL inhibitor bosutinib employing a two-tiered approach using chemical proteomics to identify natural binders in whole cell lysates of primary CML and K562 cells in parallel to in vitro kinase assays against a large recombinant kinase panel.", "entity1": "ABL", "entity2": "bosutinib", "span1": [58, 61], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12871": {"label": 2, "data": {"text": "Weakly translocated lipids (PE, phosphatidylhydroxypropionate, and phosphatidylhomoserine) are also weak Atp8a1 activators.", "entity1": "Atp8a1", "entity2": "PE", "span1": [105, 111], "span2": [28, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1632": {"label": 1, "data": {"text": "Changes of phosphorylation of cAMP response element binding protein in rat nucleus accumbens after chronic ethanol intake: naloxone reversal.", "entity1": "cAMP response element binding protein", "entity2": "naloxone", "span1": [30, 67], "span2": [123, 131]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6276": {"label": 3, "data": {"text": "The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro.", "entity1": "angiotensin II type 1 receptor", "entity2": "EXP 3174", "span1": [49, 79], "span2": [159, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1074": {"label": 1, "data": {"text": "In the present study, the capacity of acetylcholinesterase inhibitors to interact with muscarinic receptors was assessed by their ability to displace both [3H]-oxotremorine-M and [3H]-quinuclinidyl benzilate binding in rat brain membranes.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [87, 107], "span2": [155, 174]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4327": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "CDK4", "entity2": "Pinosylvin", "span1": [211, 215], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1354": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "dopamine transporter", "entity2": "methoxy", "span1": [295, 315], "span2": [186, 193]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2094": {"label": 3, "data": {"text": "Effects of inhibition of urokinase-type plasminogen activator (u-PA) by amiloride in the cornea and tear fluid of eyes irradiated with UVB.", "entity1": "u-PA", "entity2": "amiloride", "span1": [63, 67], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2780": {"label": 8, "data": {"text": "In the presence of the system L inhibitor BCH, Na(+)-dependent l-alanine uptake in WKY and SHR PTE cells was inhibited by alanine, serine, and cysteine, which is consistent with amino acid transport through ASCT2.", "entity1": "ASCT2", "entity2": "amino acid", "span1": [207, 212], "span2": [178, 188]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10812": {"label": 3, "data": {"text": "As expected, comparison of IC50 indicated that meloxicam and carprofen are more selective inhibitors of COX-2 than phenylbutazone and flunixin; meloxicam was the most advantageous for horses of four NSAIDs examined.", "entity1": "COX-2", "entity2": "carprofen", "span1": [104, 109], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"52": {"label": 3, "data": {"text": "The effects of two reversible, predominantly monoamine oxidase-A (MAO-A) inhibitors, moclobemide (150 mg three times daily) and toloxatone (400-200-400 mg day-1) on monoamine metabolites and psychometric performance were compared in a double-blind placebo controlled crossover study in 12 healthy subjects.", "entity1": "monoamine oxidase-A", "entity2": "toloxatone", "span1": [45, 64], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9977": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "alpha-methyl-dopahydrazine", "span1": [80, 84], "span2": [107, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11305": {"label": 9, "data": {"text": "Naloxone (alone) treatment of rats had no effect on the levels of CREB and p-CREB protein in the nucleus accumbens.", "entity1": "CREB", "entity2": "Naloxone", "span1": [66, 70], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12865": {"label": 9, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "phosphatidylinositol", "span1": [13, 19], "span2": [123, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14453": {"label": 2, "data": {"text": "We observed similar effects of Ag NPs on inflammatory mediator expression in vitro and in vivo with increase of interleukin-8 (IL-8)/macrophage inflammatory protein 2, IL-1RI, and tumor necrosis factor-\u03b1 expression in both models and increased IL-8 protein release in vitro.", "entity1": "IL-1RI", "entity2": "Ag", "span1": [168, 174], "span2": [31, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15898": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "O-methyltransferase", "entity2": "benzopyranopyrrole", "span1": [217, 236], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"754": {"label": 5, "data": {"text": "This work showed that appropriate structural modification of diphenidol can lead to M2-selective muscarinic antagonists of possible interest in the field of Alzheimer's disease.", "entity1": "M2", "entity2": "diphenidol", "span1": [84, 86], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8576": {"label": 3, "data": {"text": "Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.", "entity1": "kinase", "entity2": "5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers", "span1": [89, 95], "span2": [31, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"198": {"label": 1, "data": {"text": "The aim of the study was to determine whether the dihydroxylated antiestrogen LY117018, with a high affinity for the estrogen receptor and low intrinsic estrogenic activity, could inhibit the uterotropic actions of steroidal [estradiol-17 beta (E2)] and nonsteroidal [ICI 3188 and trianisylchloroethylene (TACE)] estrogens in immature rats and also the uterotropic actions of tamoxifen and monohydroxytamoxifen in the ovariectomized mouse and immature rat.", "entity1": "estrogen receptor", "entity2": "LY117018", "span1": [117, 134], "span2": [78, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4516": {"label": 8, "data": {"text": "Uridine 5'-diphosphate- glucuronosyltransferases are colocalized with carboxylesterases and have the potential to further metabolize carboxylic acids to acyl glucuronides, but it is currently unknown if acyl glucuronides, being esters, also interact with carboxylesterases.", "entity1": "Uridine 5'-diphosphate- glucuronosyltransferases", "entity2": "acyl glucuronides", "span1": [0, 48], "span2": [203, 220]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7279": {"label": 8, "data": {"text": "Transmembrane isoforms of adenylate cyclases (AC) integrate a wide variety of extracellular signals from neurotransmitters to morphogens and can also regulate cAMP production in response to calcium entry.", "entity1": "AC", "entity2": "cAMP", "span1": [46, 48], "span2": [159, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10710": {"label": 1, "data": {"text": "The anticonvulsant action of dextromethorphan or dimemorfan was significantly counteracted by a selective sigma1 receptor antagonist BD 1047, suggesting that the anticonvulsant action of dextromethorphan or dimemorfan is, at least in part, related to sigma1 receptor-activated modulation of AP-1 transcription factors.", "entity1": "sigma1 receptor", "entity2": "dimemorfan", "span1": [251, 266], "span2": [207, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14923": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "27-hydroxycholesterol", "span1": [266, 269], "span2": [78, 99]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15221": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "clerosterol", "span1": [340, 363], "span2": [123, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11215": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "glucose", "span1": [4, 11], "span2": [25, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8376": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "GLUT4", "entity2": "BPA", "span1": [119, 124], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9622": {"label": 1, "data": {"text": "This direct biochemical evidence of cooperative interaction in nucleotide binding of the two NBFs of SUR1 suggests that glibenclamide both blocks this cooperative binding of ATP and MgADP and, in cooperation with the MgADP bound at NBF2, causes ATP to be released from NBF1.", "entity1": "NBF2", "entity2": "MgADP", "span1": [232, 236], "span2": [182, 187]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5656": {"label": 2, "data": {"text": "We reported that superfusion of hERG-expressing HEK293 (hERG-HEK) cells with matrine (1, 10 \u03bcM) increased the hERG current by promoting hERG channel activation.", "entity1": "hERG", "entity2": "matrine", "span1": [110, 114], "span2": [77, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2470": {"label": 2, "data": {"text": "Liver BHMT activity was 1.3-fold higher in rats fed the Met deficient diet containing choline, which was reflected in corresponding increases in mRNA content and immunodetectable protein.", "entity1": "BHMT", "entity2": "choline", "span1": [6, 10], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10348": {"label": 9, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "BrBK2-8", "entity2": "GW660511X", "span1": [107, 114], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"7431": {"label": 8, "data": {"text": "The parallel pattern of accumulation of 24:6n-3 and DHA in response to increasing concentrations of ALA suggests that the competition between 24:5n-3 and ALA for D6D may contribute to the limited accumulation of DHA in cell membranes.", "entity1": "D6D", "entity2": "ALA", "span1": [162, 165], "span2": [154, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1122": {"label": 3, "data": {"text": "Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action.", "entity1": "carbonic anhydrase", "entity2": "acetazolamide", "span1": [23, 41], "span2": [114, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"694": {"label": 1, "data": {"text": "Prazosin antagonized all agonists with a low potency (pA2: 8.29-8.80) indicating the involvement of alpha 1L-rather than alpha 1A-adrenoceptors.", "entity1": "alpha 1A-adrenoceptors", "entity2": "Prazosin", "span1": [121, 143], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7290": {"label": 3, "data": {"text": "In addition, PFD reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-beta target gene and furin substrate involved in carcinogenesis.", "entity1": "matrix metalloproteinase (MMP)-11", "entity2": "PFD", "span1": [51, 84], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4936": {"label": 3, "data": {"text": "The mechanism of action of Fc11a-2 was related to the inhibition of the cleavage of pro-caspase-1, pro-IL-1\u03b2 and pro-IL-18 which in turn suppressed the activation of NLRP3 inflammasome.", "entity1": "pro-IL-1\u03b2", "entity2": "Fc11a-2", "span1": [99, 108], "span2": [27, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14260": {"label": 8, "data": {"text": "By contrast, 1,12-diamino-3,6,9-triazadodecane(SpmTrien), a charge-deficient spermine analog, was an extremely poor substrate of human recombinant SSAT2 and was metabolized by SSAT1 in HEPG2 cells and in wild-type primary hepatocytes.", "entity1": "human recombinant SSAT2", "entity2": "1,12-diamino-3,6,9-triazadodecane", "span1": [129, 152], "span2": [13, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"859": {"label": 0, "data": {"text": "The functional protein contains 1160 amino acids with a large central mucin domain, three consensus sites for glycosaminoglycan attachment, two epidermal growth factor-like repeats, a putative hyaluronan-binding motif, and a potential transmembrane domain near the C-terminal.", "entity1": "hyaluronan-binding motif", "entity2": "amino acids", "span1": [193, 217], "span2": [37, 48]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11216": {"label": 1, "data": {"text": "The insulin responses to glucose, mitiglinide, tolbutamide, and glibenclamide in MIN6 cells after chronic mitiglinide, nateglinide, or repaglinide treatment were comparable to those after chronic tolbutamide and glibenclamide treatment.", "entity1": "insulin", "entity2": "mitiglinide", "span1": [4, 11], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5864": {"label": 1, "data": {"text": "To our surprise, when mu-receptor binding was determined by using [3H]Tyr-D-Ala-Gly-MePhe-Gly-ol (DAMGO), a 10-15% decrease in binding was also observed in the midbrain and cortex after 4 days of DPDPE treatment.", "entity1": "mu-receptor", "entity2": "DAMGO", "span1": [22, 33], "span2": [98, 103]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10499": {"label": 1, "data": {"text": "Adenovirally-mediated overexpression of NCX, at levels, which did not alter basal contraction of myocytes, markedly depressed the isoproterenol concentration-response curve.", "entity1": "NCX", "entity2": "isoproterenol", "span1": [40, 43], "span2": [130, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4817": {"label": 1, "data": {"text": "We provide STD NMR data which confirms a physical interaction between LolA and the thiourea degradation product of MAC13243, with a Kd of ~150 \u03bcM.", "entity1": "LolA", "entity2": "thiourea", "span1": [70, 74], "span2": [83, 91]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15513": {"label": 1, "data": {"text": "Our findings that NO/SNO target both Prx and Trx reductase may have implications for understanding the impact of nitrosylation on cellular redox homeostasis.", "entity1": "Prx", "entity2": "SNO", "span1": [37, 40], "span2": [21, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13606": {"label": 0, "data": {"text": "The key difference in structure of Lp(a) and plasminogen is replacement of Arg with Ser at position 560.", "entity1": "plasminogen", "entity2": "Arg", "span1": [45, 56], "span2": [75, 78]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"887": {"label": 1, "data": {"text": "As compared with N(5)-methyl H(4)biopterin, N(5)-formyl H(4)biopterin bound with twice the capacity but stimulated nitric oxide synthase to a lesser extent.", "entity1": "nitric oxide synthase", "entity2": "N(5)-methyl H(4)biopterin", "span1": [115, 136], "span2": [17, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13785": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "PTK787", "span1": [14, 16], "span2": [197, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5811": {"label": 4, "data": {"text": "The antinociceptive activity of the alpha 2-adrenoceptor agonist clonidine was also increased in mice treated with alpha N-acetyl beta-endorphin-(1-31).", "entity1": "alpha 2-adrenoceptor", "entity2": "clonidine", "span1": [36, 56], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3464": {"label": 1, "data": {"text": "Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C.", "entity1": "I159C", "entity2": "[2-(trimethylammonium)ethyl]-methanethiosulfonate", "span1": [240, 245], "span2": [164, 213]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2126": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "Monocarboxylate transporters", "entity2": "lactate", "span1": [0, 28], "span2": [126, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10018": {"label": 5, "data": {"text": "In conclusion, AS-8112 is a potent dopamine D2, D3 and 5-HT3 receptors antagonist, and a novel anti-emetic agent with a broad-spectrum of anti-emetic activity.", "entity1": "5-HT3 receptors", "entity2": "AS-8112", "span1": [55, 70], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2765": {"label": 3, "data": {"text": "Using standard assays, lumiracoxib was found to be a poor inhibitor of purified ovine COX-1 and a relatively weak inhibitor of purified human COX-2.", "entity1": "human COX-2", "entity2": "lumiracoxib", "span1": [136, 147], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3213": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "phenolic acids", "span1": [286, 296], "span2": [12, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7961": {"label": 0, "data": {"text": "Control of hypercholesterolemia and atherosclerosis using the cholesterol recognition/interaction amino acid sequence of the translocator protein TSPO.", "entity1": "translocator protein TSPO", "entity2": "amino acid", "span1": [125, 150], "span2": [98, 108]}, "weak_labels": [0, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1789": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "erbB", "entity2": "CI-1033", "span1": [96, 100], "span2": [67, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5314": {"label": 3, "data": {"text": "A series of phosphorylated flavonoids were synthesized and investigated in\u00a0vitro as inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE).", "entity1": "cholesterol esterase", "entity2": "phosphorylated flavonoids", "span1": [109, 129], "span2": [12, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11779": {"label": 3, "data": {"text": "There was no significant difference in TLR4, NF-\u03baB, and IL-27 mRNA and proteins between curcumin-treated and sulfasalazine-treated groups.", "entity1": "NF-\u03baB", "entity2": "curcumin", "span1": [45, 50], "span2": [88, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3830": {"label": 3, "data": {"text": "In combination with clofarabine, the ability of resveratrol to reduce the contents of Sp1 and its target gene products was also evident in a time- and dose-dependent experiment.", "entity1": "Sp1", "entity2": "resveratrol", "span1": [86, 89], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14826": {"label": 3, "data": {"text": "rivaroxaban and apixaban, are potent, oral direct inhibitors of prothrombinase-bound, clot-associated or free FXa.", "entity1": "prothrombinase", "entity2": "rivaroxaban", "span1": [64, 78], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6905": {"label": 0, "data": {"text": "Unlike transferrin receptor, the protease domain of PSMA contains a binuclear zinc site, catalytic residues, and a proposed substrate-binding arginine patch.", "entity1": "transferrin receptor", "entity2": "arginine", "span1": [7, 27], "span2": [142, 150]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11092": {"label": 1, "data": {"text": "Overall, these findings suggest that monohydroxytamoxifen and LY117018 probably act through the same mechanism of action via the estrogen receptor.", "entity1": "estrogen receptor", "entity2": "LY117018", "span1": [129, 146], "span2": [62, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9120": {"label": 1, "data": {"text": "However, in contrast to the reversible binding of most phenothiazines to calmodulin, phenoxybenzamine bound to calmodulin irreversibly.", "entity1": "calmodulin", "entity2": "phenothiazines", "span1": [73, 83], "span2": [55, 69]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5851": {"label": 4, "data": {"text": "Some 5-HT3 antagonists have 5-HT4 agonist activity (for example, renzapride, zacopride) and others do not (for example, ondansetron, granisetron), while tropisetron in high concentrations is a 5-HT4 antagonist.", "entity1": "5-HT4", "entity2": "renzapride", "span1": [28, 33], "span2": [65, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15814": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFRbeta", "entity2": "Tyr", "span1": [89, 98], "span2": [149, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3932": {"label": 2, "data": {"text": "The reactivation of brain AChE inhibited with tabun demonstrated better activity of new compound BT-07-4M, TMB-4 and obidoxime from symmetric oximes, and BT-05 and BT-03 possessing asymmetric structure.", "entity1": "AChE", "entity2": "BT-07-4M", "span1": [26, 30], "span2": [97, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4574": {"label": 1, "data": {"text": "Inhibition of lysosomes or proteasomes by co-treatment with antofine and their respective specific inhibitors, NH4Cl or MG132, partially inhibited the antofine-induced decrease in Cx43 protein levels, but did not inhibit the antofine-induced inhibition of GJIC.", "entity1": "Cx43", "entity2": "MG132", "span1": [180, 184], "span2": [120, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8302": {"label": 3, "data": {"text": "An autophagic signaling was evidenced by an increase of Beclin-1, ATG 5-12, and LC3-II expression whereas the p53(mut) presence decreased with CoCl2 time exposure.", "entity1": "p53", "entity2": "CoCl2", "span1": [110, 113], "span2": [143, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12195": {"label": 1, "data": {"text": "A follow-up study of the expression of D6D and D5D genes in Chinese who live in European countries with high SFA and MUFA diets would be of interest.", "entity1": "D5D", "entity2": "SFA", "span1": [47, 50], "span2": [109, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6247": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "human 5-HT1B", "entity2": "zolmitriptan", "span1": [101, 113], "span2": [30, 42]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3681": {"label": 2, "data": {"text": "Our data demonstrate that the actions of both tolbutamide and gliclazide are strongly potentiated by 8-pCPT-2'-O-Me-cAMP-AM, that gliclazide can stimulate phospholipase C activity via a partially pertussis toxin-sensitive mechanism, and that 8-pCPT-2'-O-Me-cAMP-AM potentiation of tolbutamide action may involve activation of a 2-APB-sensitive Ca(2+) influx.", "entity1": "phospholipase C", "entity2": "gliclazide", "span1": [155, 170], "span2": [130, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9580": {"label": 1, "data": {"text": "Both carbetocin, carbetocin metabolite I and carbetocin metabolite II displayed binding affinities to the myometrial oxytocin receptor of a similar magnitude as oxytocin.", "entity1": "oxytocin receptor", "entity2": "carbetocin", "span1": [117, 134], "span2": [5, 15]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1657": {"label": 5, "data": {"text": "Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists.", "entity1": "histamine H1-receptor", "entity2": "cetirizine", "span1": [97, 118], "span2": [62, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10576": {"label": 2, "data": {"text": "Imiquimod (IMQ), an activator of Toll-like receptor-7 (TLR-7), induces by several routes a profound anti-viral and anti-tumor effect in vivo.", "entity1": "TLR-7", "entity2": "IMQ", "span1": [55, 60], "span2": [11, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3656": {"label": 8, "data": {"text": "However, CYP2B4 is not an inhibitor of CYP2E1-mediated p-nitrophenol hydroxylation.", "entity1": "CYP2E1", "entity2": "p-nitrophenol", "span1": [39, 45], "span2": [55, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15770": {"label": 2, "data": {"text": "Furthermore, we detected that ICI treatment induced glycogen synthase kinase (Gsk3-\u03b2) Ser 9 phosphorylation, which correlates with cyclin D1 nuclear localization.", "entity1": "Gsk3-\u03b2", "entity2": "ICI", "span1": [78, 84], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2406": {"label": 1, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "NOS", "entity2": "Nor-NOHA", "span1": [198, 201], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6812": {"label": 2, "data": {"text": "Further study revealed that pitavastatin increased ABCA1 mRNA in HMG-CoA reductase-dependent manner and that Rho and Rho kinase inhibitor (C3T and Y27632) increased apoA-I production in the HepG2 cells.", "entity1": "ABCA1", "entity2": "pitavastatin", "span1": [51, 56], "span2": [28, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3682": {"label": 2, "data": {"text": "Both tolbutamide and gliclazide stimulated phospholipase C activity; however, only gliclazide did so independently of its activity at K(ATP) channels, and this activity was partially inhibited by pertussis toxin.", "entity1": "phospholipase C", "entity2": "tolbutamide", "span1": [43, 58], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4488": {"label": 4, "data": {"text": "Endothelium-dependent relaxations, nitric oxide (NO) and endothelium derived hyperpolarizing factor (EDHF)-type, were studied in rabbit iliac artery and aortic rings using the G protein-coupled receptor agonist acetylcholine (ACh) and by cyclopiazonic acid (CPA), which promotes store-operated Ca(2+) entry by inhibiting the endothelial SERCA pump.", "entity1": "G protein-coupled receptor", "entity2": "ACh", "span1": [176, 202], "span2": [226, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"46": {"label": 3, "data": {"text": "Before the next drug intake, MAO-A inhibition, as judged by the decrease of plasma DHPG concentration, was significantly different from placebo with moclobemide but not with toloxatone.", "entity1": "MAO-A", "entity2": "toloxatone", "span1": [29, 34], "span2": [174, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7276": {"label": 8, "data": {"text": "Some of the compounds investigated in this study might be used as additives in toothpastes for reducing the acidification produced by the relevant CO2 hydrase activity of enamel CA VI, which leads to the formation of protons and bicarbonate and may have a role in cariogenesis.", "entity1": "CA VI", "entity2": "CO2", "span1": [178, 183], "span2": [147, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9473": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "TP", "entity2": "I-BOP", "span1": [248, 250], "span2": [225, 230]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11439": {"label": 1, "data": {"text": "We also studied the effects of thalidomide on COX-1, COX-2 or bcl-2 expression, TNFalpha, VEGF, GSH and cytochrome c in these cells.", "entity1": "COX-2", "entity2": "thalidomide", "span1": [53, 58], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15925": {"label": 1, "data": {"text": "As shown in a cell culture model, polySia-NCAM-140 was kept in the late trans-Golgi apparatus of lung epithelial cells and stimulation by IL-1\u03b2 or lipopolysaccharide induced metalloprotease-mediated ectodomain shedding, resulting in the secretion of soluble polySia-NCAM.", "entity1": "NCAM-140", "entity2": "polySia", "span1": [42, 50], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14744": {"label": 1, "data": {"text": "In addition, we found that arsenic trioxide decreases the stability of \u0394Np63 protein via a proteasome-dependent pathway but has little effect on the level of \u0394Np63 transcript.", "entity1": "proteasome", "entity2": "arsenic trioxide", "span1": [91, 101], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10427": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "retinoid receptors", "entity2": "acetylenic retinoid", "span1": [113, 131], "span2": [17, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7110": {"label": 1, "data": {"text": "Tamoxifen blocks the action of estrogen by binding to the ER, and possesses both ER-agonist and antagonist properties.", "entity1": "ER", "entity2": "estrogen", "span1": [58, 60], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15151": {"label": 2, "data": {"text": "The mRNA level for nestin (Nes, biomarker for stem Leydig cells) was significantly increased in the control testis on day 4 post-EDS, but not in the DEHP treated testes, suggesting that these nestin positive stem cells were differentiated into progenitor Leydig cells in the DEHP-treated testes.", "entity1": "Nes", "entity2": "EDS", "span1": [27, 30], "span2": [129, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7258": {"label": 2, "data": {"text": "Finally, we showed that chlorate activated endocrine cell development by inducing neurogenin 3 (Neurog3) expression in early endocrine progenitor cells.", "entity1": "neurogenin 3", "entity2": "chlorate", "span1": [82, 94], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13313": {"label": 3, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "B-RAF", "entity2": "Nexavar", "span1": [52, 57], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12781": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "S-1", "span1": [0, 20], "span2": [147, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14423": {"label": 2, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C.", "entity1": "proghrelin", "entity2": "compound C", "span1": [54, 64], "span2": [158, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6757": {"label": 2, "data": {"text": "Hydralazine induced rapid and transient expression of HIF-1alpha and downstream targets of HIF (endothelin-1, adrenomedullin, haem oxygenase 1, and vascular endothelial growth factor [VEGF]) in endothelial and smooth muscle cells and induced endothelial cell-specific proliferation.", "entity1": "endothelin-1", "entity2": "Hydralazine", "span1": [96, 108], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8572": {"label": 1, "data": {"text": "Phlebotomy and dietary iron restriction reduces serum transaminase in NAFLD/NASH patients.", "entity1": "serum transaminase", "entity2": "iron", "span1": [48, 66], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15999": {"label": 2, "data": {"text": "Puerarin stimulates proliferation and differentiation and protects against cell death in human osteoblastic MG-63 cells via ER-dependent MEK/ERK and PI3K/Akt activation.", "entity1": "PI3K", "entity2": "Puerarin", "span1": [149, 153], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1096": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "neostigmine", "span1": [51, 71], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3866": {"label": 3, "data": {"text": "HSYA treatment also decreased NF-\u03baB p65 nuclear translocation and inhibited the phosphorylation of p38 mitogen-activated protein kinase (p38 MAPK).", "entity1": "mitogen-activated protein kinase", "entity2": "HSYA", "span1": [103, 135], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14830": {"label": 3, "data": {"text": "rivaroxaban and apixaban, are potent, oral direct inhibitors of prothrombinase-bound, clot-associated or free FXa.", "entity1": "FXa", "entity2": "apixaban", "span1": [110, 113], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1954": {"label": 1, "data": {"text": "It has previously been suggested that ergotamine produces external carotid vasoconstriction in vagosympathectomised dogs via 5-HT1B/1D receptors and alpha2-adrenoceptors.", "entity1": "5-HT1B/1D", "entity2": "ergotamine", "span1": [125, 134], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8669": {"label": 2, "data": {"text": "While imatinib was unable to block cisplatin-induced DNA damage and damage response, such as the upregulation of p53, imatinib inhibited the cisplatin-induced nuclear accumulation of c-Abl/TAp73 and the subsequent downregulation of TAp63 and upregulation of Bax, thereby abrogating oocyte cell death.", "entity1": "TAp63", "entity2": "imatinib", "span1": [232, 237], "span2": [118, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7032": {"label": 2, "data": {"text": "Further, cholesterol metabolites, predominantly the oxysterols, the natural ligands for liver X receptor (LXR), induced these genes via upregulation of sterol regulatory element binding protein-1c (SREBP-1c) that bound to the regulatory regions of these genes.", "entity1": "sterol regulatory element binding protein-1c", "entity2": "cholesterol", "span1": [152, 196], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12343": {"label": 8, "data": {"text": "In this work, the metabolism of four frequently prescribed inhaled GCs, triamcinolone acetonide, flunisolide, budesonide, and fluticasone propionate, by the CYP3A family of enzymes was studied to identify differences in their rates of clearance and to identify their metabolites.", "entity1": "CYP3A", "entity2": "flunisolide", "span1": [157, 162], "span2": [97, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2935": {"label": 8, "data": {"text": "Adenylosuccinate synthetase (AdSS) catalyzes the Mg2+ dependent condensation of a molecule of IMP with aspartate to form adenylosuccinate, in a reaction driven by the hydrolysis of GTP to GDP.", "entity1": "Adenylosuccinate synthetase", "entity2": "adenylosuccinate", "span1": [0, 27], "span2": [121, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2238": {"label": 3, "data": {"text": "Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.", "entity1": "D816V", "entity2": "Dasatinib", "span1": [35, 40], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11844": {"label": 8, "data": {"text": "Methods: The stability of six acyl glucuronides in the presence of hCES1, hCES2, and buffer alone (100 mM potassium phosphate, pH 7.4, 37\u00b0C) were investigated.", "entity1": "hCES2", "entity2": "acyl glucuronides", "span1": [74, 79], "span2": [30, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13892": {"label": 1, "data": {"text": "We determined whether an angiotensin-converting enzyme (ACE) inhibitor, captopril, inhibits MMP-2 activity in peritoneal effluents from patients on CAPD, and simulated molecular models of the MMP-2-captopril complex.", "entity1": "MMP-2", "entity2": "captopril", "span1": [192, 197], "span2": [198, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12940": {"label": 8, "data": {"text": "Sources of L-arg include dietary proteins and endogenous synthesis by argininosuccinate synthetase and argininosuccinate lyase.", "entity1": "argininosuccinate lyase", "entity2": "L-arg", "span1": [103, 126], "span2": [11, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5951": {"label": 5, "data": {"text": "Inhibition of MCF-7 cell growth by the selective calmodulin antagonists W-13 and W-12 is consistent with a role for calmodulin antagonism in the broad growth-inhibitory properties of pimozide.", "entity1": "calmodulin", "entity2": "W-13", "span1": [49, 59], "span2": [72, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"644": {"label": 3, "data": {"text": "Sumatriptan and LY 344864 decreased the number of capsaicin-induced c-fos-like immunoreactive cells within trigeminal nucleus caudalis (ID50 = 0.04 and 0.6 mg kg(-1)).", "entity1": "c-fos", "entity2": "Sumatriptan", "span1": [68, 73], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15410": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "TNF\u03b1", "entity2": "stigmasterol", "span1": [84, 88], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"15362": {"label": 1, "data": {"text": "Taken together, these findings identify a signature hepatic gene-network associated with repeated oxycodone administration in rats and demonstrate that oxycodone alters the expression of many transporters and DMEs (without direct activation of PXR, CAR, and AhR), which could lead to undesirable DDIs after coadministration of substrates of these transporters/DMEs with oxycodone.", "entity1": "PXR", "entity2": "oxycodone", "span1": [244, 247], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"13777": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Lapatinib ditosylate", "span1": [14, 16], "span2": [104, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7855": {"label": 3, "data": {"text": "The potentiation of heteromeric KARs by mGlu1 activation was attenuated by GDP\u03b2S, blocked by an inhibitor of phospholipase C or the calcium chelator 1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA), prolonged by the phosphatase inhibitor okadaic acid, but unaffected by the tyrosine kinase inhibitor lavendustin A.", "entity1": "KARs", "entity2": "1,2-bis(o-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid", "span1": [32, 36], "span2": [149, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14355": {"label": 3, "data": {"text": "mRNA levels of receptor activator of nuclear factor kappa-B (RANK), its ligand RANKL, tumor necrosis factor alpha (TNF-\u03b1) and RANKL/osteoprotegerin (OPG) ratio were diminished in the periodontium of CCL3(-/-) mice and in the group treated with Met-RANTES.", "entity1": "OPG", "entity2": "Met", "span1": [149, 152], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9758": {"label": 5, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "halpha(2A)-AR", "entity2": "yohimbine", "span1": [78, 91], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3594": {"label": 3, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "mammalian target of rapamycin", "entity2": "Wogonoside", "span1": [45, 74], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7393": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "P5CDH", "entity2": "proline", "span1": [82, 87], "span2": [124, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4814": {"label": 1, "data": {"text": "In vivo HIF-mediated reductive carboxylation is regulated by citrate levels and sensitizes VHL-deficient cells to glutamine deprivation.", "entity1": "HIF", "entity2": "citrate", "span1": [8, 11], "span2": [61, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13118": {"label": 2, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "FAS promoter", "entity2": "doxorubicin", "span1": [156, 168], "span2": [82, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"253": {"label": 3, "data": {"text": "The competitive inhibitor of hCOX-1, mefenamic acid, also displayed competitive inhibition of hCOX-2.", "entity1": "hCOX-2", "entity2": "mefenamic acid", "span1": [94, 100], "span2": [37, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8434": {"label": 1, "data": {"text": "HENA failed to activate the channels made of cbv1 + \u03b22, \u03b23, \u03b24, or \u03b21T169A, indicating that this drug selectively targets \u03b21-containing BK channels via the BK \u03b21 steroid-sensing site.", "entity1": "BK \u03b21", "entity2": "HENA", "span1": [156, 161], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4736": {"label": 3, "data": {"text": "Additionally, the expression of hepatic fibrosis-related factors such as \u03b1-smooth muscle actin and transforming growth factor-\u03b21 (TGF-\u03b21), were reduced in rats treated with sinapic acid.", "entity1": "\u03b1-smooth muscle actin", "entity2": "sinapic acid", "span1": [73, 94], "span2": [173, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4051": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "p38", "entity2": "neoechinulin A", "span1": [144, 147], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9113": {"label": 9, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c.", "entity1": "cytochrome c", "entity2": "phenoxybenzamine", "span1": [122, 134], "span2": [13, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5067": {"label": 3, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "p-ERK", "entity2": "U0126", "span1": [92, 97], "span2": [108, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11933": {"label": 1, "data": {"text": "To evaluate whether fisetin regulates mTORC1 signaling, we investigated the phosphorylation and kinase activity of the 70-kDa ribosomal protein S6 kinase 1 (S6K1) and mTORC1 in 3T3-L1 preadipocytes.", "entity1": "mTORC1", "entity2": "fisetin", "span1": [167, 173], "span2": [20, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13399": {"label": 2, "data": {"text": "In hearts treated with metformin, [AMP] was increased at 50 min and AMPK activity, phosphorylated AMPK, and phosphorylated acetyl-CoA carboxylase were elevated at 61 min.", "entity1": "phosphorylated acetyl-CoA carboxylase", "entity2": "metformin", "span1": [108, 145], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1323": {"label": 3, "data": {"text": "Bupropion, an efficacious antidepressant and smoking cessation agent, inhibits dopamine and norepinephrine transporters (DAT and NET, respectively).", "entity1": "DAT", "entity2": "Bupropion", "span1": [121, 124], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"77": {"label": 3, "data": {"text": "Aspirin (ASA) and other non-steroidal anti-inflammatory drugs, which are cyclooxygenase (COX) inhibitors, precipitate asthmatic attacks in ASA-intolerant patients, while sodium salicylate, hardly active on COX by itself, is well tolerated by these patients.", "entity1": "cyclooxygenase", "entity2": "ASA", "span1": [73, 87], "span2": [9, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9281": {"label": 1, "data": {"text": "Incubation of rat aortic membranes with the irreversible alpha 1B-adrenoceptor antagonist, chloroethylclonidine (CEC: 10 microM) did not change the KD of [3H]-prazosin binding in comparison to untreated membranes, but reduced by 88% the total number of binding sites (Bmax).", "entity1": "alpha 1B-adrenoceptor", "entity2": "[3H]-prazosin", "span1": [57, 78], "span2": [154, 167]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12148": {"label": 0, "data": {"text": "The four lysine residues located in the SMG loop, Lys-260, Lys-263, Lys-265, and Lys-268, also play an important role in mediating the sensitivity of OTCase to ornithine and to arginase and appear to be involved in transducing and enhancing the signal given by ornithine for the closure of the catalytic domain.", "entity1": "OTCase", "entity2": "lysine", "span1": [150, 156], "span2": [9, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4869": {"label": 3, "data": {"text": "Only FFAs that increased ceramides caused impairment of AKt and PTP1B phosphorylation at Ser 50.", "entity1": "PTP1B", "entity2": "ceramides", "span1": [64, 69], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11556": {"label": 1, "data": {"text": "Several single nucleotide polymorphisms (SNPs) in VKORC1 are associated with warfarin dose across the normal dose range.", "entity1": "VKORC1", "entity2": "warfarin", "span1": [50, 56], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2435": {"label": 3, "data": {"text": "Epididymal tissue from wild-type mice responded in vitro to noradrenaline and isoprenaline with increased glycerol release, reduced IL-6 release, and increased cAMP accumulation.", "entity1": "IL-6", "entity2": "noradrenaline", "span1": [132, 136], "span2": [60, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4648": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A1", "entity2": "TCDD", "span1": [0, 6], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2486": {"label": 3, "data": {"text": "Licofelone reduced intima/media ratio in injured arteries, the macrophages infiltration in the neointimal area, monocyte chemoattractant protein-1 (MCP-1) gene expression, and the activation of nuclear factor-kappaB in rabbit atheroma.", "entity1": "monocyte chemoattractant protein-1", "entity2": "Licofelone", "span1": [112, 146], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9100": {"label": 3, "data": {"text": "Inhibition of the leukotriene synthetase of rat basophil leukemia cells by diethylcarbamazine, and synergism between diethylcarbamazine and piriprost, a 5-lipoxygenase inhibitor.", "entity1": "5-lipoxygenase", "entity2": "piriprost", "span1": [153, 167], "span2": [140, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4329": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "retinoblastoma protein", "entity2": "Pinosylvin", "span1": [228, 250], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5821": {"label": 3, "data": {"text": "After the combined pituitary stimulation test (100 micrograms human CRH, 100 micrograms GnRH, 100 micrograms GH-releasing hormone, and 200 micrograms TRH), the ACTH peak (maximum increase at 30 min) was significantly blunted by loperamide from 9 +/- 1 to 4 +/- 1 pmol/L (P less than 0.001) and the area under the curve of ACTH from 0-120 min was reduced from 35 +/- 5 to 23 +/- 4 pmol/L.2 h (P less than 0.05).", "entity1": "GH-releasing hormone", "entity2": "loperamide", "span1": [109, 129], "span2": [228, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11882": {"label": 1, "data": {"text": "It remains to be fully elucidated whether use of metformin, an insulin sensitizer, and/or sulfonylureas, insulin secretagogues, affect cancer incidence in subjects with T2DM.", "entity1": "insulin", "entity2": "sulfonylureas", "span1": [105, 112], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14919": {"label": 1, "data": {"text": "However, other steroids, including \u0394(5)-androstenediol, 5\u03b1-androstanediol and 27-hydroxycholesterol, which have a saturated A ring containing a 3\u03b2-hydroxyl and a C19 methyl group, also mediate physiological responses through binding to estrogen receptor-\u03b1 (ER\u03b1) and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "5\u03b1-androstanediol", "span1": [257, 260], "span2": [56, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6327": {"label": 3, "data": {"text": "The turnover of SERT was determined from the rate of recovery of binding after administration of RTI-76, an irreversible inhibitor of ligand binding.", "entity1": "SERT", "entity2": "RTI-76", "span1": [16, 20], "span2": [97, 103]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6878": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "CBS", "entity2": "H2S", "span1": [65, 68], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3068": {"label": 3, "data": {"text": "The effects of PLZ on both amino acids and their transaminases were blocked by pre-treatment with the MAO inhibitor tranylcypromine.", "entity1": "MAO", "entity2": "tranylcypromine", "span1": [102, 105], "span2": [116, 131]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"649": {"label": 1, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "metalloproteinase", "entity2": "BB-94", "span1": [164, 181], "span2": [94, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2581": {"label": 3, "data": {"text": "Pretreatment with dexamethasone significantly suppressed nasal allergy-like behaviors, up-regulation of histamine content, HDC activity and HDC mRNA induced by TDI in TDI-sensitized rats.", "entity1": "HDC", "entity2": "dexamethasone", "span1": [123, 126], "span2": [18, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1767": {"label": 1, "data": {"text": "This study demonstrates enhanced cardiostimulation by CGP 12177A (in the presence of propranolol) in rat ventricular myocytes overexpressing beta(1)-adrenoceptors, mediated by a Gs/cAMP signalling pathway.", "entity1": "Gs", "entity2": "CGP 12177A", "span1": [178, 180], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5655": {"label": 2, "data": {"text": "We reported that superfusion of hERG-expressing HEK293 (hERG-HEK) cells with matrine (1, 10 \u03bcM) increased the hERG current by promoting hERG channel activation.", "entity1": "hERG", "entity2": "matrine", "span1": [56, 60], "span2": [77, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7974": {"label": 1, "data": {"text": "Quantitative polymerase chain reaction, western blotting, immunohistochemical analysis and immunofluorescence were used to determine the changes in the expression of organic anion transporter (Oat)1 and Oat3 in rat kidney in response to 1,25(OH)(2)D(3) treatment.", "entity1": "Oat3", "entity2": "1,25(OH)(2)D(3)", "span1": [203, 207], "span2": [237, 252]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13244": {"label": 3, "data": {"text": "Down-regulation of GRIP1 by glutamate was blocked by carbobenzoxyl-leucinyl-leucinyl-leucinal (MG132), a proteasome inhibitor and by expression of K48R-ubiquitin, a dominant negative form of ubiquitin.", "entity1": "proteasome", "entity2": "MG132", "span1": [105, 115], "span2": [95, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7969": {"label": 2, "data": {"text": "We concluded that in overweight and obese women with PCOS Orlistat administration, combined with diet and physical exercise, for 24 weeks, resulted in significant weight loss, improvement of hyperandrogenism and insulin sensitivity, and increased serum AMH levels.", "entity1": "AMH", "entity2": "Orlistat", "span1": [253, 256], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12966": {"label": 0, "data": {"text": "Mass spectrometric analysis and mutation studies revealed that gammaPKC phosphorylated Ser-776 and Ser-779 in the AD of DGKgamma.", "entity1": "DGKgamma", "entity2": "Ser", "span1": [120, 128], "span2": [99, 102]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2191": {"label": 1, "data": {"text": "We have elucidated the crystal structures of the cyanotoxins, motuporin (nodularin-V) and dihydromicrocystin-LA bound to human protein phosphatase-1c (gamma isoform).", "entity1": "human protein phosphatase-1c (gamma isoform)", "entity2": "nodularin-V", "span1": [121, 165], "span2": [73, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11964": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I", "entity2": "PI(4,5)P2", "span1": [16, 66], "span2": [252, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3977": {"label": 8, "data": {"text": "To identify important covariates associated with interindividual variation in CYP2B6 activity in vivo, we evaluated these effects in healthy volunteers using bupropion (Wellbutrin SR GlaxoSmithKline, Research Triangle Park, NC) as a CYP2B6 probe substrate.", "entity1": "CYP2B6", "entity2": "Wellbutrin SR", "span1": [233, 239], "span2": [169, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9841": {"label": 1, "data": {"text": "gamma-Butyrobetaine hydroxylase catalyse the last step in carnitine biosynthesis, the formation of L-carnitine from gamma-butyrobetaine, a reaction dependent on Fe2+, alpha-ketoglutarate, ascorbate and oxygen.", "entity1": "gamma-Butyrobetaine hydroxylase", "entity2": "Fe2+", "span1": [0, 31], "span2": [161, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1336": {"label": 4, "data": {"text": "Moreover, in rat hepatoma H4-II-E cells, the esterified-BM failed to induce tyrosine aminotransferase, which is regulated by GR-mediated transactivation activity.", "entity1": "GR", "entity2": "BM", "span1": [125, 127], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16031": {"label": 3, "data": {"text": "This effect was prevented by rapamycin, an inhibitor of the mammalian target of rapamycin complex 1 (mTORC1), or by PF470867, a selective inhibitor of the p70 ribosomal S6 kinase 1 (S6K1).", "entity1": "mTORC1", "entity2": "rapamycin", "span1": [101, 107], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15544": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "TNF-\u03b1", "entity2": "DMN", "span1": [252, 257], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12873": {"label": 2, "data": {"text": "Weakly translocated lipids (PE, phosphatidylhydroxypropionate, and phosphatidylhomoserine) are also weak Atp8a1 activators.", "entity1": "Atp8a1", "entity2": "phosphatidylhomoserine", "span1": [105, 111], "span2": [67, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6281": {"label": 3, "data": {"text": "In contrast, the administration of 7.5 and 15 mg of meloxicam caused dose-dependent reductions in monocyte COX-2 activity by 51% and 70%, respectively, and in platelet COX-1 activity by 25% and 35%, respectively.", "entity1": "COX-1", "entity2": "meloxicam", "span1": [168, 173], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2200": {"label": 3, "data": {"text": "Minocycline showed more potent inhibition on MMP-9 mRNA expression, starting at 1 (P<0.005) and further at more than 30 (P<0.001) mg/kg/day.", "entity1": "MMP-9", "entity2": "Minocycline", "span1": [45, 50], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11462": {"label": 0, "data": {"text": "The IL-2/gamma(c) interface itself exhibits the smallest buried surface and the fewest hydrogen bonds in the complex, which is consistent with its promiscuous use in other cytokine receptor complexes.", "entity1": "IL-2", "entity2": "hydrogen", "span1": [4, 8], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7710": {"label": 3, "data": {"text": "They act by reactivation of AChE inhibited by OP.", "entity1": "AChE", "entity2": "OP", "span1": [28, 32], "span2": [46, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2643": {"label": 8, "data": {"text": "The latter reaction, catalyzed by aspartoacylase (ASPA), produces acetyl groups plus aspartate and has been proposed to occur in both soluble and membranous subfractions of white matter.", "entity1": "aspartoacylase", "entity2": "acetyl", "span1": [34, 48], "span2": [66, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"8220": {"label": 1, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "potassium channels", "entity2": "ICA-105574", "span1": [113, 131], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9987": {"label": 3, "data": {"text": "Since this compound retains good AChE inhibitory activity and its hexahydrochromeno[4,3-b]pyrrole moiety is reminiscent of the hexahydropyrrolo[2,3-b]indole of physostigmine (3), we have designed and synthesized carbamates 4-6, and their biological evaluation has been assessed in vitro against human AChE and BChE.", "entity1": "AChE", "entity2": "hexahydropyrrolo[2,3-b]indole of physostigmine", "span1": [33, 37], "span2": [127, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9270": {"label": 1, "data": {"text": "Saturation experiments showed that [3H]prazosin labelled a single population of binding sites in the spleen (alpha 1B) and hippocampus (alpha 1A and alpha 1B) (dissociation constants (KD): 0.26 nM and 0.14 nM respectively).", "entity1": "alpha 1B", "entity2": "[3H]prazosin", "span1": [109, 117], "span2": [35, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"495": {"label": 0, "data": {"text": "Factor Xa or catalytically inactive 5-dimethylaminonaphthalene-1sulfonyl (dansyl) Glu-Gly-Arg-(DEGR)-chloromethylketone-factor Xa bound indistinguishably to HUVEC and EPR-1 transfectants, and inhibited equally well the binding of 125I-factor Xa to these cells.", "entity1": "factor Xa", "entity2": "5-dimethylaminonaphthalene-1sulfonyl (dansyl) Glu-Gly-Arg-(DEGR)-chloromethylketone", "span1": [120, 129], "span2": [36, 119]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15872": {"label": 1, "data": {"text": "Presynaptic CaMKII\u03b1 modulates dopamine D3 receptor activation in striatonigral terminals of the rat brain in a Ca(2+) dependent manner.", "entity1": "dopamine D3 receptor", "entity2": "Ca(2+)", "span1": [30, 50], "span2": [111, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2115": {"label": 1, "data": {"text": "Diethylcarbamazine activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway.", "entity1": "inducible nitric-oxide synthase", "entity2": "Diethylcarbamazine", "span1": [80, 111], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14979": {"label": 2, "data": {"text": "Osteoblasts survive the arsenic trioxide treatment by activation of ATM-mediated pathway.", "entity1": "ATM", "entity2": "arsenic trioxide", "span1": [68, 71], "span2": [24, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14031": {"label": 8, "data": {"text": "Although genetic polymorphisms in the endothelial nitric oxide synthase (eNOS) gene may impair endogenous NO formation, there is little information about how eNOS polymorphisms and haplotypes affect the responses to sildenafil.", "entity1": "eNOS", "entity2": "NO", "span1": [73, 77], "span2": [106, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1947": {"label": 9, "data": {"text": "Several purinergic receptors have been described on platelets; P2X (1), a calcium channel, and P2Y1 a Gq-coupled seven-transmembrane domain receptor, have been found not to be antagonized by clopidogrel.", "entity1": "Gq-coupled seven-transmembrane domain receptor", "entity2": "clopidogrel", "span1": [102, 148], "span2": [191, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6960": {"label": 5, "data": {"text": "However, as with the human receptor, maraviroc was shown to be a high affinity, potent functional antagonist of macaque CCR5 thereby indicating that the macaque should be a suitable species in which to evaluate the pharmacology, safety and potential mechanism-related toxicology of novel CCR5 antagonists.", "entity1": "CCR5", "entity2": "maraviroc", "span1": [288, 292], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9547": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "IL-3", "entity2": "cyclic adenosine monophosphate", "span1": [70, 74], "span2": [172, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6535": {"label": 3, "data": {"text": "Fulvestrant, the first agent in this new class, not only induces the degradation of the estrogen receptor but also is an estrogen antagonist; further, its lack of agonist activity provides a better safety profile.", "entity1": "estrogen receptor", "entity2": "Fulvestrant", "span1": [88, 105], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2642": {"label": 8, "data": {"text": "Unlike mouse RetSat (mRetSat), zRetSat A had an altered bond specificity saturating either the 13-14 or 7-8 double bonds of all-trans-retinol to produce either all-trans-13,14-dihydroretinol or all-trans-7,8-dihydroretinol, respectively.", "entity1": "zRetSat A", "entity2": "all-trans-retinol", "span1": [31, 40], "span2": [124, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13516": {"label": 1, "data": {"text": "Taken together H(2)O(2)-mediated oxidation affects calcium binding in calmodulin leading to perturbed calcium homeostasis and perturbed l-phenylalanine-uptake in the epidermis of acute vitiligo.", "entity1": "calmodulin", "entity2": "H(2)O(2)", "span1": [70, 80], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2127": {"label": 8, "data": {"text": "Monocarboxylate transporters (MCTs) are proton-linked membrane carriers involved in the transport of monocarboxylates such as lactate, pyruvate, as well as ketone bodies.", "entity1": "MCTs", "entity2": "lactate", "span1": [30, 34], "span2": [126, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8726": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT2B10", "entity2": "amitriptyline", "span1": [61, 68], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3041": {"label": 5, "data": {"text": "EP(1) and EP(3) receptor antagonists ONO-8713 and ONO-AE3-240, but not the EP(4) antagonists ONO-AE3-208 and AH 23848, inhibited tumor cell proliferation, indicating the significance of EP(1) and EP(3) but not EP(4) for MB growth.", "entity1": "EP(4)", "entity2": "ONO-AE3-208", "span1": [75, 80], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10218": {"label": 2, "data": {"text": "Metformin increases AMP-activated protein kinase activity in skeletal muscle of subjects with type 2 diabetes.", "entity1": "AMP-activated protein kinase", "entity2": "Metformin", "span1": [20, 48], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8410": {"label": 3, "data": {"text": "Secondary point mutations in the Fms-like tyrosine kinase 3 (FLT3) tyrosine kinase domain (KD) are common causes of acquired clinical resistance to the FLT3 inhibitors AC220 (quizartinib) and sorafenib.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [152, 156], "span2": [192, 201]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8491": {"label": 9, "data": {"text": "Curcuminoids Modulate Pro-Oxidant-Antioxidant Balance but not the Immune Response to Heat Shock Protein 27 and Oxidized LDL in Obese Individuals.", "entity1": "Oxidized LDL", "entity2": "Curcuminoids", "span1": [111, 123], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5364": {"label": 3, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [88, 93], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9366": {"label": 1, "data": {"text": "We show that the binding of thalidomide photoaffinity label to authentic human AGP is competed with both thalidomide and the nonradioactive photoaffinity label at concentrations comparable to those required for inhibition of production of tumor necrosis factor alpha from human monocytes, suggesting that AGP may be involved in the immunomodulatory activity of thalidomide.", "entity1": "human AGP", "entity2": "thalidomide", "span1": [73, 82], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15449": {"label": 8, "data": {"text": "Currently, the most important insecticides are neonicotinoids, which are metabolized in vitro by AOX on reduction of the nitroimino group and by CYPs via oxidation reactions.", "entity1": "AOX", "entity2": "nitroimino", "span1": [97, 100], "span2": [121, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12126": {"label": 8, "data": {"text": "Thymidylate synthase and thymidine kinase are key enzymes involved in the de novo and salvage pathways for pyrimidine nucleotide synthesis, respectively.", "entity1": "Thymidylate synthase", "entity2": "pyrimidine nucleotide", "span1": [0, 20], "span2": [107, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"763": {"label": 0, "data": {"text": "The inhibitor binds at the base of the active site gorge of TcAChE, interacting with both the choline-binding site (Trp-84) and the acyl-binding pocket (Phe-288, Phe-290).", "entity1": "TcAChE", "entity2": "Trp", "span1": [60, 66], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5418": {"label": 1, "data": {"text": "Local LC citalopram effect was abolished by LC presence of the 5-HT3 receptor antagonist MDL72222 (1\u00a0\u03bcM) but not the 5-HT1/2 receptor antagonist methiothepin (1\u00a0\u03bcM).", "entity1": "5-HT3", "entity2": "citalopram", "span1": [63, 68], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15421": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "HMGCoA", "entity2": "cholesterol", "span1": [219, 225], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"7466": {"label": 8, "data": {"text": "We have expressed VIAAT and the plasmalemmal transporters for glycine and GABA in a neuroendocrine cell line and measured the quantal release of glycine and GABA using a novel double-sniffer patch-clamp technique.", "entity1": "VIAAT", "entity2": "glycine", "span1": [18, 23], "span2": [62, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12004": {"label": 3, "data": {"text": "CP[c]Ph has, comparably to B[a]P, a potential to repress expression of tumor suppressor p53, in the head kidney of rainbow trout.", "entity1": "tumor suppressor p53", "entity2": "B[a]P", "span1": [71, 91], "span2": [27, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8392": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "glutathione peroxidase", "entity2": "Cd", "span1": [160, 182], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1914": {"label": 3, "data": {"text": "SL-11158 inhibited SSAT activity with a mixed type of inhibition in which the analogue had a 70-fold higher affinity for the enzyme than the natural substrate, spermine.", "entity1": "SSAT", "entity2": "SL-11158", "span1": [19, 23], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11430": {"label": 1, "data": {"text": "In the presence of alphaAR blockade, concentration-response curves for isoproterenol, norepinephrine, and epinephrine suggested that a beta1AR was involved in this response, and the rank order of potency was isoproterenol > norepinephrine = epinephrine.", "entity1": "beta1AR", "entity2": "epinephrine", "span1": [135, 142], "span2": [106, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4413": {"label": 6, "data": {"text": "Using cell-based assays and brain slice preparations, we characterized the interaction of a potent and efficacious mGlu5 PAM from the CPPHA series termed NCFP (N-(4-chloro-2-((4-fluoro-1,3-dioxoisoindolin-2-yl)methyl)phenyl)picolinamide).", "entity1": "mGlu5", "entity2": "N-(4-chloro-2-((4-fluoro-1,3-dioxoisoindolin-2-yl)methyl)phenyl)picolinamide", "span1": [115, 120], "span2": [160, 236]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14411": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "Rap1", "entity2": "nucleotide", "span1": [268, 272], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15351": {"label": 4, "data": {"text": "Full agonists to the peroxisome proliferator-activated receptor (PPAR)\u03b3, such as Rosiglitazone, have been associated with a series of undesired side effects, such as weight gain, fluid retention, cardiac hypertrophy, and hepatotoxicity.", "entity1": "peroxisome proliferator-activated receptor (PPAR)\u03b3", "entity2": "Rosiglitazone", "span1": [21, 71], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11484": {"label": 1, "data": {"text": "CONCLUSIONS: Ketorolac is relatively COX-1 selective while bromfenac is potently selective for COX-2 over COX-1.", "entity1": "COX-1", "entity2": "bromfenac", "span1": [106, 111], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13834": {"label": 3, "data": {"text": "Subsequent studies demonstrated that wild-type and hyperinsulinemia/hyperammonemia forms of GDH are inhibited by the green tea polyphenols, epigallocatechin gallate and epicatechin gallate.", "entity1": "GDH", "entity2": "epigallocatechin gallate", "span1": [92, 95], "span2": [140, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7245": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "TYR", "span1": [231, 237], "span2": [76, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11032": {"label": 3, "data": {"text": "Sorafenib, which belongs chemically to a class that can be described as bis-aryl ureas, was selected for further pharmacologic characterization based on potent inhibition of Raf-1 and its favorable kinase selectivity profile.", "entity1": "kinase", "entity2": "bis-aryl ureas", "span1": [198, 204], "span2": [72, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7316": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "solute carrier 1", "entity2": "amino acids", "span1": [172, 188], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12068": {"label": 0, "data": {"text": "This lysine is contained in the sequence PFYAVKC, which is found in all known ODCs from eukaryotes.", "entity1": "PFYAVKC", "entity2": "lysine", "span1": [41, 48], "span2": [5, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9263": {"label": 3, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "dopamine", "span1": [50, 53], "span2": [169, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6793": {"label": 3, "data": {"text": "CONCLUSIONS AND CLINICAL RELEVANCE: Canine COX-2 was selectively inhibited by etodolac, nimesulide, and NS398; tolfenamic acid and carprofen also appeared to be preferential COX-2 inhibitors in dogs.", "entity1": "COX-2", "entity2": "tolfenamic acid", "span1": [174, 179], "span2": [111, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9836": {"label": 3, "data": {"text": "Geldanamycin also disrupts the T-cell receptor-mediated activation of nuclear factor of activated T-cells (NF-AT).", "entity1": "T-cell receptor", "entity2": "Geldanamycin", "span1": [31, 46], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13719": {"label": 1, "data": {"text": "When RAD51, which is a central component of HR, was depleted by siRNA cells were sensitized to raltitrexed (RTX), which specifically inhibits TS.", "entity1": "RAD51", "entity2": "RTX", "span1": [5, 10], "span2": [108, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11618": {"label": 8, "data": {"text": "We isolated partial cDNAs that codified for enzymes implicated in the anthocyanin biosynthesis such as l-phenylalanine ammonia-lyase (PAL) and chalcone synthase (CHS), and an antioxidant enzyme such as ascorbate peroxidase (APX).", "entity1": "l-phenylalanine ammonia-lyase", "entity2": "anthocyanin", "span1": [103, 132], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15289": {"label": 3, "data": {"text": "The monoacylglycerol lipase (MAGL) inhibitor JZL184 produces antinociceptive and anti-inflammatory effects.", "entity1": "MAGL", "entity2": "JZL184", "span1": [29, 33], "span2": [45, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6710": {"label": 3, "data": {"text": "The results demonstrated that tranylcypromine is a competitive inhibitor of CYP2C19 (Ki = 32 microM) and CYP2D6 (Ki = 367 microM) and a noncompetitive inhibitor of CYP2C9 (Ki = 56 microM).", "entity1": "CYP2C9", "entity2": "tranylcypromine", "span1": [164, 170], "span2": [30, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1863": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "kushenol H", "span1": [221, 251], "span2": [89, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6528": {"label": 3, "data": {"text": "The earliest known AChE inhibitors, namely, physostigmine and tacrine, performed poorly in clinical trials (e.g., poor oral activity, brain penetration, and hepatotoxic liability).", "entity1": "AChE", "entity2": "tacrine", "span1": [19, 23], "span2": [62, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15083": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "extended-spectrum \u00df-lactamase", "entity2": "avibactam", "span1": [161, 190], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"426": {"label": 5, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "(-)-tamsulosin", "span1": [258, 286], "span2": [16, 30]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6402": {"label": 0, "data": {"text": "Finally, cysteine 53 in the M1P1 external loop is required for functional expression of TWIK-2 but is not critical for subunit self-assembly.", "entity1": "M1P1 external loop", "entity2": "cysteine", "span1": [28, 46], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12199": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D5D", "entity2": "linoleic acid", "span1": [290, 293], "span2": [205, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4071": {"label": 3, "data": {"text": "In study 1, cyclic ewes received vehicle, cortisol, PF 915275 (PF; a selective inhibitor of HSD11B1), cortisol and PF, meloxicam (a selective inhibitor of PTGS2), cortisol and meloxicam, recombinant ovine IFNT, or IFNT and PF into the uterus from day 10 to day14 after estrus.", "entity1": "PTGS2", "entity2": "meloxicam", "span1": [155, 160], "span2": [119, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2574": {"label": 3, "data": {"text": "These results show that olanzapine eliminates D2 receptor priming and cognitive impairment and also alleviates decreases in neurotrophins and acetylcholinergic markers produced by D2 priming in the hippocampus.", "entity1": "D2 receptor", "entity2": "olanzapine", "span1": [46, 57], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12599": {"label": 0, "data": {"text": "The predicted structure of PHBP showed three epidermal growth factor (EGF) domains, a kringle domain and a serine protease domain, from its N-terminus, although HGFA has a fibronectin type II domain, an EGF domain, a fibronectin type I domain, an EGF domain, a kringle domain, and a serine protease domain, from its N-terminus.", "entity1": "HGFA", "entity2": "N", "span1": [161, 165], "span2": [316, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2418": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "mitochondrial arginase II", "entity2": "nitric oxide", "span1": [234, 259], "span2": [21, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13093": {"label": 2, "data": {"text": "Most drugs currently employed in the treatment of type 2 diabetes either target the sulfonylurea receptor stimulating insulin release (sulfonylureas, glinides), or target the peroxisome proliferator-activated receptor (PPARgamma) improving insulin resistance (thiazolidinediones).", "entity1": "insulin", "entity2": "sulfonylureas", "span1": [118, 125], "span2": [135, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"393": {"label": 1, "data": {"text": "The antagonist SR 141716A has a high specificity for the central CB1 cannabinoid receptor and negligeable affinity for the peripheral CB2 receptor, making it an excellent tool for probing receptor structure-activity relationships.", "entity1": "CB1", "entity2": "SR 141716A", "span1": [65, 68], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5833": {"label": 8, "data": {"text": "The unique role of the enzyme 5-lipoxygenase (5-LO) in the production of leukotrienes (LTs) makes it a likely target for biochemical manipulation.", "entity1": "5-LO", "entity2": "leukotrienes", "span1": [46, 50], "span2": [73, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12292": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Fnta", "entity2": "Quercetin", "span1": [107, 111], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6242": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-ht1f", "entity2": "Eletriptan", "span1": [135, 141], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13326": {"label": 3, "data": {"text": "Sulfasalazine (also as a representative of the salicylates) inhibited the diabetes-induced upregulation of several inflammatory gene products, which are regulated by NF-kappaB, including vascular cell adhesion molecule, intracellular adhesion molecule-1, inducible nitric oxide synthase, and cyclooxygenase-2 in whole-retinal lysate.", "entity1": "intracellular adhesion molecule-1", "entity2": "Sulfasalazine", "span1": [220, 253], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"16010": {"label": 3, "data": {"text": "RESULTS: Pretreatment of ucOC (30ng/ml) prevented LA-induced apoptosis in insulin-stimulated endothelial cells; effects were abolished by pretreatment with the phosphatidylinositol 3-kinase (PI3-kinase) inhibitor, wortmannin.", "entity1": "PI3-kinase", "entity2": "wortmannin", "span1": [191, 201], "span2": [214, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3262": {"label": 1, "data": {"text": "Numerous studies have suggested that increased TS levels are associated closely with resistance to fluoropyrimidine-based chemotherapy.", "entity1": "TS", "entity2": "fluoropyrimidine", "span1": [47, 49], "span2": [99, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9603": {"label": 9, "data": {"text": "Here, we report that MgATP and MgADP, but not the Mg salt of gamma-thio-ATP, stabilize the binding of prebound 8-azido-[alpha-32P]ATP to SUR1.", "entity1": "SUR1", "entity2": "gamma-thio-ATP", "span1": [137, 141], "span2": [61, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3576": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u.", "entity1": "pIR", "entity2": "MSG", "span1": [53, 56], "span2": [81, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7255": {"label": 4, "data": {"text": "Interestingly, both isomers of METH were full agonists at mTAAR1 and h-rChTAAR1, whereas both were partial agonists at rTAAR1.", "entity1": "h-rChTAAR1", "entity2": "METH", "span1": [69, 79], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5122": {"label": 3, "data": {"text": "In addition, 5HHMF blocked LPS-induced phosphorylation of I\u03baB, resulting in suppression of the nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) subunits, namely p65 and p50, which are important molecules involved in the regulation of iNOS expression.", "entity1": "p65", "entity2": "5HHMF", "span1": [163, 166], "span2": [13, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5013": {"label": 8, "data": {"text": "Five classes of chalcogenopyrylium dyes (CGPs) were examined for their ability to modulate transport of [(3)H]estradiol glucuronide (E217\u03b2G) (a prototypical MRP substrate) into MRP-enriched inside-out membrane vesicles.", "entity1": "MRP", "entity2": "E217\u03b2G", "span1": [157, 160], "span2": [133, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, 8, 8, -1, -1, -1, -1]},
	"15547": {"label": 2, "data": {"text": "DMN-induced cyclooxygenase-2 (COX-2) expression and nuclear factor-kappa B (NF-\u03baB) activation was reduced by CK treatment.", "entity1": "cyclooxygenase-2", "entity2": "DMN", "span1": [12, 28], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8738": {"label": 1, "data": {"text": "In conclusion, this study expands the understanding of the substrate specificity of UGT2B10, highlighting its preference for tertiary amines with higher affinities and clearance values than those of UGT1A4 and UGT1A3.", "entity1": "UGT1A4", "entity2": "tertiary amines", "span1": [199, 205], "span2": [125, 140]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4916": {"label": 3, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "superoxide dismutase", "entity2": "kinsenoside", "span1": [161, 181], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"346": {"label": 1, "data": {"text": "In animals, the R-enantiomer of timolol causes a significant reduction in intraocular pressure but had only 1/80 the activity of the S-enantiomer at extraocular receptors.", "entity1": "extraocular receptors", "entity2": "R-enantiomer of timolol", "span1": [149, 170], "span2": [16, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"528": {"label": 2, "data": {"text": "Exogenous C2-ceramide activates c-fos serum response element via Rac-dependent signalling pathway.", "entity1": "c-fos serum response element", "entity2": "C2-ceramide", "span1": [32, 60], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12386": {"label": 1, "data": {"text": "Evidence also outlines a role for oxytocin in the prosocial effects of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy) in both rodents and humans.", "entity1": "oxytocin", "entity2": "MDMA", "span1": [34, 42], "span2": [106, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10613": {"label": 1, "data": {"text": "Their affinity for GABA was moderate (EC50 = 30 microM), and the Hill coefficient was 1.3, corresponding to two GABA binding sites.", "entity1": "GABA binding sites", "entity2": "GABA", "span1": [112, 130], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13336": {"label": 1, "data": {"text": "Fluoxetine affected mainly the hSERT transport rate by reducing the availability of the transporter in the membrane with no significant alteration of either the total hSERT protein content or the hSERT mRNA level.", "entity1": "hSERT", "entity2": "Fluoxetine", "span1": [31, 36], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1463": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "MAO", "entity2": "N-propargyl-1R(+)-aminoindan", "span1": [95, 98], "span2": [12, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9494": {"label": 3, "data": {"text": "Monoamine uptake inhibitors structurally analogous to cocaine (cocaethylene, CFT, betaCIT, CPT, (+)-cocaine, norcocaine, and benztropine) also produced this rapid pressor response, whereas structurally unrelated uptake inhibitors with diverse monoamine transporter selectivities (BTCP, indatraline, GBR 12935, mazindol, nomifensine, and zimeldine) either did not produce a rapid pressor response or produced only a small pressor response.", "entity1": "monoamine transporter", "entity2": "zimeldine", "span1": [243, 264], "span2": [337, 346]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, 9]},
	"6655": {"label": 1, "data": {"text": "In the future, codon 49 and 389 genotypes or beta(1)-adrenergic receptor haplotypes might be used to predict the diastolic blood pressure response to metoprolol in patients with hypertension.", "entity1": "beta(1)-adrenergic receptor", "entity2": "metoprolol", "span1": [45, 72], "span2": [150, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10358": {"label": 1, "data": {"text": "In rat plasma the BrBK half-life values in the absence or in the presence of GW660511X (530 nM) or omapatrilat (50 nM) were 9.31 +/- 1.7, 22.06 +/- 3.1 and 25.3 +/- 1.7 min, respectively and BrBK was degraded into BrBK1-8, BrBK1-7, BrBK1-5 and Br-Phe5 plus BrBK2-9, BrBK4-8 and BrBK2-8 metabolites not found in human plasma.", "entity1": "BrBK", "entity2": "omapatrilat", "span1": [18, 22], "span2": [99, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"732": {"label": 2, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "Human and rat renin", "entity2": "losartan", "span1": [0, 19], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"479": {"label": 0, "data": {"text": "Despite a low amino acid identity between TWIK-1 and TREK-1 (approximately 28%), both channel proteins share the same overall structural arrangement consisting of two pore-forming domains and four transmembrane segments (TMS).", "entity1": "TWIK-1", "entity2": "amino acid", "span1": [42, 48], "span2": [14, 24]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9925": {"label": 1, "data": {"text": "The finding that arachidonate can also induce a conformational change in PGHS-2 was unexpected, and the magnitude of changes suggests this structural flexibility may be integral to the cyclooxygenase catalytic mechanism.", "entity1": "PGHS-2", "entity2": "arachidonate", "span1": [73, 79], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"248": {"label": 3, "data": {"text": "Indomethacin inhibited both hCOX-1 and hCOX-2, whereas NS-398 and Dup-697 selectively inhibited hCOX-2.", "entity1": "hCOX-2", "entity2": "Dup-697", "span1": [96, 102], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13830": {"label": 1, "data": {"text": "Hexachlorophene forms a ring around the internal cavity in GDH through aromatic stacking interactions between the drug and GDH as well as between the drug molecules themselves.", "entity1": "GDH", "entity2": "Hexachlorophene", "span1": [123, 126], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7776": {"label": 0, "data": {"text": "Tub tyrosine phosphorylation (Tub-p-tyr) is modulated by nutritional status.", "entity1": "Tub", "entity2": "tyrosine", "span1": [0, 3], "span2": [4, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4462": {"label": 3, "data": {"text": "Catalpol also suppressed AGE-induced phosphorylation of mitogen activated protein (MAP) kinases, degradation of I\u03baB\u03b1 and the nuclear localization of NF-\u03baB.", "entity1": "NF-\u03baB", "entity2": "Catalpol", "span1": [149, 154], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4330": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "pRb", "entity2": "Pinosylvin", "span1": [252, 255], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2137": {"label": 1, "data": {"text": "Thiazolidinediones are a new class of anti-diabetic agents which increase insulin sensitivity by binding to the peroxisome proliferator-activated receptor gamma (PPAR(gamma)) and stimulating the expression of insulin-responsive genes involved in glucose and lipid metabolism.", "entity1": "PPAR(gamma)", "entity2": "Thiazolidinediones", "span1": [162, 173], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13857": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "dydrogesterone", "span1": [252, 261], "span2": [60, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8918": {"label": 2, "data": {"text": "Carvedilol (0.3 mg/kg, iv) produced a significant inhibition of the beta 1 adrenoceptor mediated positive chronotropic response to isoproterenol.", "entity1": "beta 1 adrenoceptor", "entity2": "isoproterenol", "span1": [68, 87], "span2": [131, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"7554": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "eNOS", "entity2": "NO", "span1": [158, 162], "span2": [14, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"1976": {"label": 3, "data": {"text": "SNP inhibits the accumulation of HIF-1alpha, the regulatory subunit of HIF-1, and the transcriptional activation of HIF-1alpha via a mechanism that is not dependent on either NO or soluble guanylate cyclase.", "entity1": "HIF-1", "entity2": "SNP", "span1": [71, 76], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"553": {"label": 8, "data": {"text": "The purified phosphodiester alpha-GlcNAcase has a specific activity of 498 micromol of [3H]GlcNAc-alpha-phosphomannose-alpha-methyl cleaved per h per mg of protein using 0.5 mM [3H]GlcNAc-alpha-phosphomannose-alpha-methyl as substrate.", "entity1": "phosphodiester alpha-GlcNAcase", "entity2": "[3H]GlcNAc-alpha-phosphomannose-alpha-methyl", "span1": [13, 43], "span2": [87, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1168": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "nateglinide", "span1": [161, 165], "span2": [201, 212]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13845": {"label": 8, "data": {"text": "BACKGROUND: Peripheral inflammatory pain is associated with an upregulation of spinal cord COX-2 (cyclooxygenase-2), with a subsequent increase in central prostaglandin E2 (PGE2) levels associated with the development of hyperalgesia.", "entity1": "cyclooxygenase-2", "entity2": "PGE2", "span1": [98, 114], "span2": [173, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5253": {"label": 0, "data": {"text": "Fasting plasma glucose (FPG), fasting plasma insulin, CC-peptide (insulin secretory rate [ISR]), fasting plasma glucagon, and bioactive glucagon-like peptide (GLP-1) and gastrointestinal insulinotropic peptide (GIP) was measured.RESULTSFPG decreased from P, 160 \u00b1 4 to M, 150 \u00b1 4; S, 154 \u00b1 4; and M+S, 125 \u00b1 3 mg/dL.", "entity1": "C-peptide", "entity2": "C", "span1": [55, 64], "span2": [54, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12522": {"label": 1, "data": {"text": "Results from R-PIA and N6-(S-phenylisopropyl)adenosine experiments showed nearly a 40-fold greater potency of R-vs. S-diastereoisomer, suggesting predominance of adenosine A1 subtype.", "entity1": "adenosine A1", "entity2": "N6-(S-phenylisopropyl)adenosine", "span1": [162, 174], "span2": [23, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13758": {"label": 9, "data": {"text": "Although in vivo bosutinib is inactive against ABL T315I, we found this clinically important mutant to be enzymatically inhibited in the mid-nanomolar range.", "entity1": "ABL", "entity2": "bosutinib", "span1": [47, 50], "span2": [17, 26]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4448": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "MAO", "entity2": "2-benzofuran-1(3H)-one", "span1": [195, 198], "span2": [247, 269]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1644": {"label": 1, "data": {"text": "Compounds 4b-h were either inactive (4e,f) or weaker than 4a as affinity ligands for GluR1-4 and GluR5 with relative potencies comparable with those of the corresponding AMPA analogues as AMPA receptor agonists.", "entity1": "GluR5", "entity2": "AMPA", "span1": [97, 102], "span2": [170, 174]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7490": {"label": 3, "data": {"text": "Phenserine is also unique because of differing actions of its enantiomers: (-)-phenserine is the active enantiomer for inhibition of AChE, whereas (+)-phenserine ('posiphen') has weak activity as an AChE inhibitor and can be dosed much higher.", "entity1": "AChE", "entity2": "(+)-phenserine", "span1": [199, 203], "span2": [147, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7405": {"label": 1, "data": {"text": "These data support the novel finding that clofibrate treatment does not directly regulate BAT activity but does alter the subcellular localization of BAT.", "entity1": "BAT", "entity2": "clofibrate", "span1": [150, 153], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10453": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "SDH", "entity2": "ammonia", "span1": [0, 3], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11579": {"label": 8, "data": {"text": "These results suggest that PDE4B mediates the antipsychotic effects of rolipram in CAR and that the PDE4B-regulated cyclic adenosine monophosphate signaling pathway may play a role in the pathophysiology and pharmacotherapy of psychosis.", "entity1": "PDE4B", "entity2": "cyclic adenosine monophosphate", "span1": [100, 105], "span2": [116, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4436": {"label": 3, "data": {"text": "A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes.", "entity1": "DPP-4", "entity2": "xanthine", "span1": [173, 178], "span2": [84, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10101": {"label": 3, "data": {"text": "Acute and chronic PLZ administration increase brain GABA levels, an effect due, at least in part, to an inhibition of the activity of the GABA metabolizing enzyme, GABA transaminase (GABA-T).", "entity1": "GABA-T", "entity2": "PLZ", "span1": [183, 189], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9562": {"label": 2, "data": {"text": "The observed inhibition on IFN-gamma, GM-CSF, and IL-3 mRNA was blocked by the selective beta2AR antagonist ICI 118,551 (10(-6) M) and by timolol (10(-6) M), a nonselective antagonist.", "entity1": "IFN-gamma", "entity2": "timolol", "span1": [27, 36], "span2": [138, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3303": {"label": 3, "data": {"text": "A phase III randomized placebo-controlled trial has examined the impact of everolimus in patients with clear cell renal cancers and progressive disease on or within 6 months of the VEGFR tyrosine kinase inhibitors sunitinib and/or sorafenib.", "entity1": "VEGFR", "entity2": "sunitinib", "span1": [181, 186], "span2": [214, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"180": {"label": 1, "data": {"text": "In vitro studies, however, revealed that EO inhibits fibrin clot formation because of the Ca2+-chelating ability of its constituent ethanolamine, although oleate or benzyl alcohol exhibited procoagulant activity in FPA formation in vitro.", "entity1": "FPA", "entity2": "oleate", "span1": [215, 218], "span2": [155, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13829": {"label": 1, "data": {"text": "Hexachlorophene forms a ring around the internal cavity in GDH through aromatic stacking interactions between the drug and GDH as well as between the drug molecules themselves.", "entity1": "GDH", "entity2": "Hexachlorophene", "span1": [59, 62], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1929": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "M564G", "entity2": "acyl-CoAs", "span1": [4, 9], "span2": [66, 75]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15200": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "COX-2", "entity2": "buthanol", "span1": [288, 293], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9278": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "YM-09151-2", "span1": [166, 186], "span2": [120, 130]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1989": {"label": 3, "data": {"text": "Our results suggest that mibefradil blocks Na+ channels in a state-dependent manner that does not depend on fast inactivation but probably involves interaction with one or more slow-inactivated state(s).", "entity1": "Na+ channels", "entity2": "mibefradil", "span1": [43, 55], "span2": [25, 35]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8036": {"label": 3, "data": {"text": "Human stearoyl-CoA desaturase 1 (SCD-1) gene expression is negatively regulated by thyroid hormone without direct binding of thyroid hormone receptor to the gene promoter.", "entity1": "Human stearoyl-CoA desaturase 1", "entity2": "thyroid hormone", "span1": [0, 31], "span2": [83, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"471": {"label": 5, "data": {"text": "(+/-)-Tamsulosin, over the range of concentrations at which it antagonized the positive inotropic effect mediated by alpha 1-adrenoceptors, did not affect the accumulation of [3H]inositol phosphates that was induced by 10 microM phenylephrine.", "entity1": "alpha 1-adrenoceptors", "entity2": "(+/-)-Tamsulosin", "span1": [117, 138], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3374": {"label": 3, "data": {"text": "All GABA(A)R modulators induced a negative shift in the steady-state inactivation curve of Ca(v)1.3 channels, but only BDZs and pentobarbital induced a negative shift in Ca(v)1.2 channel inactivation.", "entity1": "Ca(v)1.2", "entity2": "BDZs", "span1": [170, 178], "span2": [119, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7481": {"label": 1, "data": {"text": "Phenserine deserves attention for an additional quality of action: in addition to inhibiting AChE, it modulates the amount of beta-amyloid precursor protein (APP) in neuronal cell culture by reducing APP translation.", "entity1": "beta-amyloid precursor protein", "entity2": "Phenserine", "span1": [126, 156], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4591": {"label": 3, "data": {"text": "Our previous work, built on the early pioneering multikinase inhibitor LY294002, resulted in the only PI3K vascular-targeted PI3K inhibitor prodrug, SF1126, which has now completed Phase I clinical trials.", "entity1": "PI3K", "entity2": "SF1126", "span1": [102, 106], "span2": [149, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1711": {"label": 9, "data": {"text": "Two mutations that were generated by PCR mutagenesis of the ERG1 gene and that conferred terbinafine resistance mapped in the same regions of the Erg1 protein, with one resulting in an L251F exchange and the other resulting in an F433S exchange.", "entity1": "Erg1", "entity2": "terbinafine", "span1": [146, 150], "span2": [89, 100]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11098": {"label": 1, "data": {"text": "The effects of these metabolites on the expression of uteroglobin (UG) and progesterone receptor (PR) genes, both regulated by progesterone (P4), were evaluated in the uterus of prepubertal female rabbits that were simultaneously treated with P4 (1.0 mg) for 5 consecutive days.", "entity1": "PR", "entity2": "progesterone (P4)", "span1": [98, 100], "span2": [127, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13827": {"label": 8, "data": {"text": "CYP2D6 inhibitors, such as paroxetine, are associated with changes in atomoxetine pharmacokinetics similar to those observed among poor CYP2D6 metabolizers.", "entity1": "CYP2D6", "entity2": "atomoxetine", "span1": [136, 142], "span2": [70, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10430": {"label": 9, "data": {"text": "These characteristics of the bound PLP suggest that SDH catalysis is not facilitated by forming the resonance-stabilized structure of the PLP-Ser aldimine as seen in aminotransferases.", "entity1": "SDH", "entity2": "PLP-Ser aldimine", "span1": [52, 55], "span2": [138, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"8961": {"label": 1, "data": {"text": "Radioligand binding studies with the nonselective alpha 1-adrenoceptor antagonist radioligand 125I-BE2254 showed that 73-87% of the binding sites in rabbit aorta are CEC sensitive and they are predominantly low affinity sites both for WB4101 (pKd = 8.1) and for 5-methylurapidil (pKd = 7.1).", "entity1": "alpha 1-adrenoceptor", "entity2": "125I-BE2254", "span1": [50, 70], "span2": [94, 105]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13170": {"label": 1, "data": {"text": "Progestin activation of Src/MAPK occurred outside the nucleus with the B isoform of PR that was distributed between the cytoplasm and nucleus, but not with PR-A that was predominantly nuclear.", "entity1": "B isoform of PR", "entity2": "Progestin", "span1": [71, 86], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10646": {"label": 1, "data": {"text": "The overall saturation binding affinity for COX-2 of valdecoxib is 2.6 nM (compared with 1.6 nM for celecoxib, 51 nM for rofecoxib, and 260 nM for etoricoxib), with a slow off-rate (t(1/2) approximately 98 min).", "entity1": "COX-2", "entity2": "etoricoxib", "span1": [44, 49], "span2": [147, 157]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6273": {"label": 3, "data": {"text": "The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro.", "entity1": "angiotensin II type 1 receptor", "entity2": "irbesartan", "span1": [49, 79], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10821": {"label": 9, "data": {"text": "Treatment with valsartan, doxazosin, or N-acetylcysteine did not significantly affect HIF-1alpha and VEGF proteins expression in the banding groups.", "entity1": "VEGF", "entity2": "N-acetylcysteine", "span1": [101, 105], "span2": [40, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10326": {"label": 2, "data": {"text": "Resiquimod-stimulated pDC also produce a number of other cytokines including TNF-alpha and IP-10.", "entity1": "IP-10", "entity2": "Resiquimod", "span1": [91, 96], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9007": {"label": 9, "data": {"text": "Limitation of SRF was produced by the anticonvulsant BDZs (diazepam, clonazepam, nitrazepam and lorazepam) at low to mid nanomolar concentrations, by a convulsant BDZ which does not bind to high affinity BDZ receptors (Ro 5-4864) at high nanomolar concentrations and by a BDZ receptor weak partial agonist (Ro 15-1788) at micromolar concentrations.", "entity1": "BDZ receptors", "entity2": "Ro 5-4864", "span1": [204, 217], "span2": [219, 228]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"6140": {"label": 1, "data": {"text": "Moreover, the reverse mutation BEAG T432S increased the affinity of BEAG K+ channels for dofetilide, whereas C-type inactivation could not be recovered.", "entity1": "T432S", "entity2": "dofetilide", "span1": [36, 41], "span2": [89, 99]}, "weak_labels": [-1, -1, 0, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11852": {"label": 2, "data": {"text": "It has been reported that oligomeric procyanidins of lotus seedpod (LSOPC) is effective in the alleviation of Alzheimer's disease and diabetes through its antioxidant and insulin-potentiating activities.", "entity1": "insulin", "entity2": "procyanidins", "span1": [171, 178], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8866": {"label": 2, "data": {"text": "Activation of STAT3, which is phosphorylated by the IL-6 signaling pathways and thus is necessary for Th17 differentiation, was strongly stimulated by I3S and TCDD.", "entity1": "STAT3", "entity2": "I3S", "span1": [14, 19], "span2": [151, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5527": {"label": 1, "data": {"text": "To determine the position of the phenyl ring of the aralkyloxyalkyl side chain of salmeterol in the beta 2AR binding site, we designed and synthesized the agonist photoaffinity label [(125)I]iodoazidosalmeterol ([125I]IAS).", "entity1": "beta 2AR", "entity2": "phenyl", "span1": [100, 108], "span2": [33, 39]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15823": {"label": 5, "data": {"text": "Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (Part I).", "entity1": "histamine H3 receptor", "entity2": "aryl ureas", "span1": [64, 85], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10579": {"label": 2, "data": {"text": "Imiquimod, a Toll-like receptor-7 agonist, induces perforin in cytotoxic T lymphocytes in vitro.", "entity1": "perforin", "entity2": "Imiquimod", "span1": [51, 59], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2189": {"label": 9, "data": {"text": "Comparisons of the structures of the cyanobacterial toxin:phosphatase complexes explain the biochemical mechanism by which microcystins but not nodularins permanently modify their protein phosphatase targets by covalent addition to an active site cysteine residue.", "entity1": "protein phosphatase", "entity2": "nodularins", "span1": [180, 199], "span2": [144, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3240": {"label": 1, "data": {"text": "Serotonin transporter (SERT) has been associated with drugs of abuse like d-methamphetamine (METH).", "entity1": "SERT", "entity2": "METH", "span1": [23, 27], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8775": {"label": 0, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-Akt", "entity2": "Ser", "span1": [74, 85], "span2": [86, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6582": {"label": 3, "data": {"text": "OBJECTIVE: Fondaparinux sodium is the first in a new class of synthetic factor Xa inhibitors that binds reversibly with high affinity to antithrombin III.", "entity1": "factor Xa", "entity2": "Fondaparinux sodium", "span1": [72, 81], "span2": [11, 30]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1897": {"label": 2, "data": {"text": "I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction.", "entity1": "cytokine", "entity2": "I3A", "span1": [60, 68], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13422": {"label": 8, "data": {"text": "Furthermore, the enzymatic activity of alanine aminotransferase (ALT), which converts the critical gluconeogenic amino acid alanine into pyruvate, is decreased (approximately 50%) in KLF15-/- hepatocytes.", "entity1": "ALT", "entity2": "alanine", "span1": [65, 68], "span2": [124, 131]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"14774": {"label": 3, "data": {"text": "Electrical stimulation, ATP, and insulin each increased fluorescent 2-NBD-Glucose (2-NBDG) uptake in primary myotubes, but only electrical stimulation and ATP-dependent 2-NBDG uptake were inhibited by adenosine-phosphate phosphatase and by purinergic receptor blockade (suramin).", "entity1": "purinergic receptor", "entity2": "suramin", "span1": [240, 259], "span2": [270, 277]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2444": {"label": 9, "data": {"text": "Colonic cyclooxygenase-2 and interkeukin-1beta mRNA and spinal c-FOS mRNA expression were significantly down-regulated by ATB-429, but not by mesalamine.", "entity1": "cyclooxygenase-2", "entity2": "mesalamine", "span1": [8, 24], "span2": [142, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5485": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "MPA", "span1": [68, 85], "span2": [208, 211]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6758": {"label": 2, "data": {"text": "Hydralazine induced rapid and transient expression of HIF-1alpha and downstream targets of HIF (endothelin-1, adrenomedullin, haem oxygenase 1, and vascular endothelial growth factor [VEGF]) in endothelial and smooth muscle cells and induced endothelial cell-specific proliferation.", "entity1": "adrenomedullin", "entity2": "Hydralazine", "span1": [110, 124], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4480": {"label": 3, "data": {"text": "In this study, we assessed the effects of clopidogrel and clarithromycin, known CYP2B6 and CYP3A inhibitors, respectively, on the enantioselective disposition of racemic sibutramine in conjunction with CYP2B6 polymorphisms in humans.", "entity1": "CYP3A", "entity2": "clopidogrel", "span1": [91, 96], "span2": [42, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11419": {"label": 1, "data": {"text": "The crystal structure of R228K-Gal-T1 complexed with LA, UDP-Gal, and Mn(2+) determined at 1.9 A resolution shows that the Asp318 side chain exhibits a minor alternate conformation, compared to that in the wild type.", "entity1": "Gal-T1", "entity2": "Mn(2+)", "span1": [31, 37], "span2": [70, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10863": {"label": 2, "data": {"text": "Moreover, 4-methylhistamine potently activated the hH(4)R (pEC(50) = 7.4 +/- 0.1; alpha = 1), and this response was competitively antagonized by the selective H(4)R antagonist JNJ 7777120 [1-[(5-chloro-1H-indol-2-yl)-carbonyl]-4-methylpiperazine] (pA(2) = 7.8).", "entity1": "hH(4)R", "entity2": "4-methylhistamine", "span1": [51, 57], "span2": [10, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9040": {"label": 1, "data": {"text": "Evidence has been obtained in man for interaction with alpha-adrenoceptors in the brain; and in the peripheral circulation bevantolol does not, as do other beta blockers, increase peripheral vascular resistance, but reduces it.", "entity1": "alpha-adrenoceptors", "entity2": "bevantolol", "span1": [55, 74], "span2": [123, 133]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1796": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "Her2", "entity2": "GW572016", "span1": [242, 246], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11260": {"label": 8, "data": {"text": "The COX pathway generates inflammatory prostaglandins, while the 5-LOX pathway generates inflammatory leukotrienes.", "entity1": "5-LOX", "entity2": "leukotrienes", "span1": [65, 70], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4538": {"label": 3, "data": {"text": "Pharmacokinetic Interactions between Monoamine Oxidase A Inhibitor Harmaline and 5-Methoxy-N,N-Dimethyltryptamine, and the Impact of CYP2D6 Status.", "entity1": "Monoamine Oxidase A", "entity2": "Harmaline", "span1": [37, 56], "span2": [67, 76]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7594": {"label": 1, "data": {"text": "Apo-alpha-lactalbumin, obtained by treatment with EDTA, displays one binding site for fatty acids, the association constants for oleic and palmitic acids being 1.9.10(6) and 4.2.10(5) M(-1), respectively.", "entity1": "Apo-alpha-lactalbumin", "entity2": "fatty acids", "span1": [0, 21], "span2": [86, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6911": {"label": 8, "data": {"text": "PSMA acts as a glutamate carboxypeptidase (GCPII) on small molecule substrates, including folate, the anticancer drug methotrexate, and the neuropeptide N-acetyl-l-aspartyl-l-glutamate.", "entity1": "PSMA", "entity2": "methotrexate", "span1": [0, 4], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9994": {"label": 1, "data": {"text": "We report here that a human degradation-resistant GLP-2 analogue, h[Gly2]-GLP-2 significantly improves survival, reduces bacteremia, attenuates epithelial injury, and inhibits crypt apoptosis in the murine gastrointestinal tract after administration of topoisomerase I inhibitor irinotecan hydrochloride or the antimetabolite 5-fluorouracil.", "entity1": "GLP-2", "entity2": "Gly2", "span1": [50, 55], "span2": [68, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3258": {"label": 1, "data": {"text": "The rates of hAR transport for the exogenous steroids methyltrienelone (MET), nandrolone (NAN), and oxandrolone (OXA) are lower than that of testosterone and similar to those of the endogenous steroids ANE and DHT.", "entity1": "hAR", "entity2": "nandrolone", "span1": [13, 16], "span2": [78, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8308": {"label": 3, "data": {"text": "Cellular responses to DNA damage induced by etoposide or doxorubicin include down-regulation of endogenous supervillin coincident with increases in p53.", "entity1": "supervillin", "entity2": "etoposide", "span1": [107, 118], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13902": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "K(ATP)", "entity2": "metformin", "span1": [62, 68], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14348": {"label": 3, "data": {"text": "mRNA levels of receptor activator of nuclear factor kappa-B (RANK), its ligand RANKL, tumor necrosis factor alpha (TNF-\u03b1) and RANKL/osteoprotegerin (OPG) ratio were diminished in the periodontium of CCL3(-/-) mice and in the group treated with Met-RANTES.", "entity1": "receptor activator of nuclear factor kappa-B", "entity2": "Met", "span1": [15, 59], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9693": {"label": 1, "data": {"text": "Pretreatment with the 5-HT1A antagonist WAY-100,635 (10 micrograms/kg i.v.) prevented the ziprasidone-induced inhibition; the same dose of WAY-100,635 had little effect on the inhibition produced by clozapine and olanzapine.", "entity1": "5-HT1A", "entity2": "olanzapine", "span1": [22, 28], "span2": [213, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11771": {"label": 1, "data": {"text": "Furthermore, orbitrap MS data support the adduction of Cys-113 in the Pin1 active site upon HNE treatment of MDA-MB-231 cells.", "entity1": "Pin1", "entity2": "HNE", "span1": [70, 74], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14741": {"label": 1, "data": {"text": "In addition, we found that arsenic trioxide decreases the stability of \u0394Np63 protein via a proteasome-dependent pathway but has little effect on the level of \u0394Np63 transcript.", "entity1": "\u0394Np63", "entity2": "arsenic trioxide", "span1": [158, 163], "span2": [27, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10711": {"label": 1, "data": {"text": "The anticonvulsant action of dextromethorphan or dimemorfan was significantly counteracted by a selective sigma1 receptor antagonist BD 1047, suggesting that the anticonvulsant action of dextromethorphan or dimemorfan is, at least in part, related to sigma1 receptor-activated modulation of AP-1 transcription factors.", "entity1": "AP-1", "entity2": "dimemorfan", "span1": [291, 295], "span2": [207, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4626": {"label": 4, "data": {"text": "The results suggested that both the EtOAc extract and berberine were able to activate PPAR\u03b1/\u03b2/\u03b3, and Rhizoma Coptis contains potential natural agonists of PPARs besides berberine.", "entity1": "PPAR\u03b1/\u03b2/\u03b3", "entity2": "EtOAc", "span1": [86, 95], "span2": [36, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8322": {"label": 2, "data": {"text": "Furthermore, inhibition of HO-1 with zinc protoporphyrin IX (ZNPP) significantly reversed the protective effect of Paeoniflorin against radiation-induced damage in EA.hy926 cells.", "entity1": "HO-1", "entity2": "Paeoniflorin", "span1": [27, 31], "span2": [115, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14343": {"label": 2, "data": {"text": "The expression of the osteoblast markers runt-related transcription factor 2 (RUNX2) and periostin was decreased, while osteocalcin (OCN) was augmented in CCL3(-/-) and Met-RANTES-treated mice.", "entity1": "osteocalcin", "entity2": "Met", "span1": [120, 131], "span2": [169, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4240": {"label": 8, "data": {"text": "These findings, derived from a variety of analytical and functional approaches, provide evidence for a novel nongenomic signaling mechanism for androgen action in the microvasculature: TES-stimulated vasodilation mediated primarily by peroxynitrite formed from xanthine oxidase-generated superoxide and NO.", "entity1": "xanthine oxidase", "entity2": "superoxide", "span1": [261, 277], "span2": [288, 298]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2326": {"label": 3, "data": {"text": "A pronounced NET knockout-induced shortening of the immobility time in the TST (by ca 50%) compared to WT mice was not reduced any further by NET-inhibiting ADs such as reboxetine, desipramine, and imipramine.", "entity1": "NET", "entity2": "imipramine", "span1": [142, 145], "span2": [198, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7410": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "NR2A", "entity2": "NMDA", "span1": [19, 23], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8164": {"label": 3, "data": {"text": "Furthermore, DPEP inhibited the LPS-induced phosphorylation of inhibitor \u03baB (I\u03baB)-\u03b1 and NF-\u03baB p50.", "entity1": "NF-\u03baB", "entity2": "DPEP", "span1": [88, 93], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2803": {"label": 3, "data": {"text": "Inhibition of endogenous production of H(2)S by PAG significantly suppressed SP concentration, PPT-A expression and NK1-R expression in the acini.", "entity1": "PPT-A", "entity2": "H(2)S", "span1": [95, 100], "span2": [39, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5357": {"label": 1, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "c-Rel", "entity2": "vitamin C", "span1": [169, 174], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15933": {"label": 2, "data": {"text": "Processing of polysialylated NCAM was reproduced in a mouse model by bleomycin administration leading to an activation of the inflammasome and secretion of interleukin (IL)-1\u03b2.", "entity1": "interleukin (IL)-1\u03b2", "entity2": "bleomycin", "span1": [156, 175], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8803": {"label": 0, "data": {"text": "Amino acid sequences of cynomolgus FMO1-5, respectively, shared high sequence identities (94-98%) and were closely clustered in a phylogenetic tree, with human FMO1-5.", "entity1": "FMO1-5", "entity2": "Amino acid", "span1": [35, 41], "span2": [0, 10]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14070": {"label": 2, "data": {"text": "Exogenous stimulation of PKA activity, achieved by forskolin treatment, protected K-ras-transformed cells from apoptosis induced by glucose deprivation, enhanced complex I activity, intracellular adenosine triphosphate (ATP) levels, mitochondrial fusion and decreased intracellular reactive oxygen species (ROS) levels.", "entity1": "PKA", "entity2": "forskolin", "span1": [25, 28], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6742": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "piperazonyl quinazoline", "span1": [273, 279], "span2": [210, 233]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2998": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "F820A", "entity2": "IBMX", "span1": [265, 270], "span2": [103, 107]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4136": {"label": 2, "data": {"text": "Upon activation by phenobarbital, nuclear receptor CAR binds the 97-bp response element (-2441/-2345) within the Kcnk1 promoter.", "entity1": "nuclear receptor", "entity2": "phenobarbital", "span1": [34, 50], "span2": [19, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4665": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "NOX4", "entity2": "resveratrol", "span1": [159, 163], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2281": {"label": 1, "data": {"text": "Also consistent with the involvement of Gq coupled EP1 receptors, the PGE1 stimulation is inhibited by the PKCI vector (encoding the PKC inhibitory domain), the PKC inhibitor Go 6976, thapsigargin, as well as the calmodulin antagonists W7 and W13.", "entity1": "EP1 receptors", "entity2": "PGE1", "span1": [51, 64], "span2": [70, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12867": {"label": 1, "data": {"text": "This aminophospholipid \"flippase\" selectively transports PS to the cytosolic leaflet of the bilayer and is sensitive to vanadate, Ca(2+), and modification by sulfhydryl reagents.", "entity1": "flippase", "entity2": "Ca(2+)", "span1": [24, 32], "span2": [130, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3073": {"label": 3, "data": {"text": "PURPOSE: To compare phenelzine (PLZ), an antidepressant drug with anxiolytic properties which inhibits monoamine oxidase (MAO) but also elevates rat brain levels of the amino acids ?-aminobutyric acid (GABA) and alanine (ALA), with vigabatrin (VIG), an anticonvulsant which elevates brain GABA by inhibition of GABA transaminase (GABA-T), with regard to their actions on brain levels of GABA and ALA and on activities of MAO, GABA-T and ALA transaminase (ALA-T).", "entity1": "GABA-T", "entity2": "vigabatrin", "span1": [330, 336], "span2": [232, 242]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4911": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "SOD", "entity2": "glucose", "span1": [183, 186], "span2": [276, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7604": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(2)", "entity2": "Tolvaptan", "span1": [44, 48], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11275": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "GDC", "entity2": "glycine", "span1": [111, 114], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9894": {"label": 5, "data": {"text": "UNLABELLED: Apparent muscarinic acetylcholine (mAch) receptor occupancy in mouse cerebral cortex, hippocampus, and striatum by scopolamine, an antagonist, and biperiden, a relatively selective M1 antagonist, was estimated with competitive binding studies using two different radioligands: 3H-N-methyl piperidyl benzilate (3H-NMPB) and 3H-quinuclidinyl benzilate (3H-QNB).", "entity1": "muscarinic acetylcholine (mAch) receptor", "entity2": "scopolamine", "span1": [21, 61], "span2": [127, 138]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3070": {"label": 3, "data": {"text": "PURPOSE: To compare phenelzine (PLZ), an antidepressant drug with anxiolytic properties which inhibits monoamine oxidase (MAO) but also elevates rat brain levels of the amino acids ?-aminobutyric acid (GABA) and alanine (ALA), with vigabatrin (VIG), an anticonvulsant which elevates brain GABA by inhibition of GABA transaminase (GABA-T), with regard to their actions on brain levels of GABA and ALA and on activities of MAO, GABA-T and ALA transaminase (ALA-T).", "entity1": "monoamine oxidase", "entity2": "phenelzine", "span1": [103, 120], "span2": [20, 30]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11022": {"label": 3, "data": {"text": "Comparison of captopril and enalapril to study the role of the sulfhydryl-group in improvement of endothelial dysfunction with ACE inhibitors in high dieted methionine mice.", "entity1": "ACE", "entity2": "captopril", "span1": [127, 130], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5047": {"label": 1, "data": {"text": "Recent advances in saxitoxin research are discussed, including the molecular biology of toxin synthesis, new protein targets, association with metal-binding motifs and methods of detection.", "entity1": "metal-binding motifs", "entity2": "saxitoxin", "span1": [143, 163], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10611": {"label": 1, "data": {"text": "LEV and related compounds bind to SV2A expressed in fibroblasts, indicating that SV2A is sufficient for LEV binding.", "entity1": "SV2A", "entity2": "LEV", "span1": [81, 85], "span2": [104, 107]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9009": {"label": 9, "data": {"text": "These findings suggest that limitation of SRF was produced by binding of BDZs, but not beta CCs, to voltage-dependent sodium channels and not to high affinity central BDZ receptors, and that BDZs limit SRF by slowing recovery of sodium channels from inactivation.", "entity1": "BDZ receptors", "entity2": "beta CCs", "span1": [167, 180], "span2": [87, 95]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"11322": {"label": 8, "data": {"text": "For determination of [PA+Pli]-activity, arginine was added after this incubation.", "entity1": "Pli", "entity2": "arginine", "span1": [25, 28], "span2": [40, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13121": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "topoisomerase IIalpha", "entity2": "doxorubicin", "span1": [41, 62], "span2": [82, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13360": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "progesterone receptor", "entity2": "Medroxyprogesterone acetate", "span1": [92, 113], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14834": {"label": 1, "data": {"text": "As the Mg(2+) ion concentration was increased, there was a consistent decrease of the enzyme catalytic turnover from 0.31 s(-1) (0 \u03bcM Mg(2+)) to 0.050 s(-1) (6000 \u03bcM Mg(2+)) and a distinct shift in steady-state conformational population from one that favors the ALDH1-NADH complex with the shorter fluorescence lifetime (33% excess) in the absence of magnesium ion to one that favors the ALDH1-NADH complex with the longer fluorescence lifetime (13% excess) at 6000 \u03bcM Mg(2+).", "entity1": "ALDH1", "entity2": "NADH", "span1": [388, 393], "span2": [394, 398]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9311": {"label": 5, "data": {"text": "The enhancement of the depolarizing afterpotential by histamine was mimicked by the histamine H1-receptor agonist 2-thiazolylethylamine and was reduced or blocked by the H1-receptor antagonist promethazine, but was not blocked or reduced in the presence of the histamine H2-receptor antagonist, cimetidine.", "entity1": "histamine H2-receptor", "entity2": "cimetidine", "span1": [261, 282], "span2": [295, 305]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"400": {"label": 2, "data": {"text": "Histamine and Ca added to NSAIDs amplified the activating effect of the latter on CA II.", "entity1": "CA II", "entity2": "Ca", "span1": [82, 87], "span2": [14, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12120": {"label": 9, "data": {"text": "Losartan, EXP, and irbesartan caused a rightward parallel shift without any major effects on the maximal response to Ang II.", "entity1": "Ang II", "entity2": "EXP", "span1": [117, 123], "span2": [10, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1007": {"label": 5, "data": {"text": "Effects of a serotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans.", "entity1": "serotonin 5-HT(4) receptor", "entity2": "SB-207266", "span1": [13, 39], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14876": {"label": 2, "data": {"text": "Additionally, in SH-SY5Y cells, MPP(+)-induced demethylation of phosphoprotein phosphatase 2A (PP2A), the master regulator of the cellular phosphoregulatory network, and cytotoxicity were ameliorated by EHT.", "entity1": "PP2A", "entity2": "EHT", "span1": [95, 99], "span2": [203, 206]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5658": {"label": 2, "data": {"text": "Long-term treatment with 1 \u03bcM matrine or oxymatrine increased expression of the hERG protein and rescued the hERG surface expression disrupted by As(2)O(3).", "entity1": "hERG", "entity2": "matrine", "span1": [80, 84], "span2": [30, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9114": {"label": 1, "data": {"text": "The site at which phenoxybenzamine bound to calmodulin appears to be similar to that at which certain antipsychotic agents bind, since several of them, including penfluridol, pimozide and spiroperidol, prevented the binding of phenoxybenzamine to calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [44, 54], "span2": [18, 34]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14502": {"label": 3, "data": {"text": "Western blot analysis indicated that TSN inhibits the CDC42/MEKK1/JNK pathway.", "entity1": "MEKK1", "entity2": "TSN", "span1": [60, 65], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13487": {"label": 1, "data": {"text": "Amyloid activates platelets through 2 pathways: one is through CD36, p38(MAPK), thromboxane A2-mediated induction of aggregation; the other is through glycoprotein Ib alpha-mediated aggregation and agglutination.", "entity1": "Amyloid", "entity2": "thromboxane A2", "span1": [0, 7], "span2": [80, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12318": {"label": 2, "data": {"text": "Ribavirin unregulated ELL (eleven-nineteen lysine-rich leukaemia) 3 mRNA expression before F7 up-regulation.", "entity1": "ELL", "entity2": "Ribavirin", "span1": [22, 25], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2529": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "4-aminobiphenyl", "span1": [311, 317], "span2": [81, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13919": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "Kir6.2", "entity2": "Phenformin", "span1": [224, 230], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13611": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "platelet-derived growth factor receptor beta", "entity2": "Sorafenib", "span1": [164, 208], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12036": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "peroxidases", "entity2": "EOI", "span1": [18, 29], "span2": [155, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12524": {"label": 9, "data": {"text": "13cisRA-dosed animals showed no change in prothrombin times.", "entity1": "prothrombin", "entity2": "13cisRA", "span1": [42, 53], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4156": {"label": 3, "data": {"text": "6-Ethyl-N-[1-(hydroxyacetyl)piperidin-4-yl]-1-methyl-4-oxo-5-(2-oxo-2-phenylethyl)-3-(2,2,2-trifluoroethoxy)-4,5-dihydro-1H-pyrrolo[3,2-c]pyridine-2-carboxamide (TAK-441) is a potent, selective hedgehog signaling pathway inhibitor that binds to Smo and is being developed for the treatment of cancer.", "entity1": "hedgehog", "entity2": "TAK-441", "span1": [194, 202], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1683": {"label": 8, "data": {"text": "Cat-1, the transporter for the essential amino acids, arginine and lysine, is one of the up-regulated genes.", "entity1": "Cat-1", "entity2": "arginine", "span1": [0, 5], "span2": [54, 62]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13491": {"label": 8, "data": {"text": "We show that murine Rdh12 and human RDH13 do not reveal activity towards the checked steroids, but that human type 12 RDH reduces dihydrotestosterone to androstanediol, and is thus also involved in steroid metabolism.", "entity1": "human type 12 RDH", "entity2": "androstanediol", "span1": [104, 121], "span2": [153, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1479": {"label": 7, "data": {"text": "Racemization of serine is catalyzed by serine racemase, a pyridoxal 5'-phosphate-dependent enzyme expressed mainly in brain and liver.", "entity1": "serine racemase", "entity2": "pyridoxal 5'-phosphate", "span1": [39, 54], "span2": [58, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9441": {"label": 8, "data": {"text": "The hydrolysis of fluorescein diphosphate by PTP epsilon and PTPmeg1 was sensitive to alendronate, with IC50 values of less than 1 microM; PTPsigma, however, under the same conditions, was inhibited by only 50% with 141 microM alendronate.", "entity1": "PTPmeg1", "entity2": "diphosphate", "span1": [61, 68], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"901": {"label": 7, "data": {"text": "Tetrahydrobiopterin [(6R)-5,6,7,8-tetrahydro-L-biopterin, H(4)biopterin] is one of several cofactors of nitric oxide synthases (EC 1.14.13.39).", "entity1": "nitric oxide synthases", "entity2": "Tetrahydrobiopterin", "span1": [104, 126], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"9629": {"label": 8, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "NBF2", "entity2": "MgATP", "span1": [151, 155], "span2": [142, 147]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4616": {"label": 1, "data": {"text": "This effect requires cold-induced, TRPA-1-mediated calcium influx and a calcium-sensitive PKC that signals to the transcription factor DAF-16/FOXO.", "entity1": "PKC", "entity2": "calcium", "span1": [90, 93], "span2": [72, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13017": {"label": 8, "data": {"text": "Phospholipase C beta (PLC-beta)-coupled G protein-coupled receptor (GPCR) activities traditionally are assessed by measuring Ca2+ triggered by D-myo-inositol 1,4,5-trisphosphate (IP3), a PLC-beta hydrolysis product, or by measuring the production of inositol phosphate using cumbersome radioactive assays.", "entity1": "PLC-beta", "entity2": "D-myo-inositol 1,4,5-trisphosphate", "span1": [187, 195], "span2": [143, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10110": {"label": 8, "data": {"text": "Acute and chronic PLZ administration increase brain GABA levels, an effect due, at least in part, to an inhibition of the activity of the GABA metabolizing enzyme, GABA transaminase (GABA-T).", "entity1": "GABA-T", "entity2": "GABA", "span1": [183, 189], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10998": {"label": 8, "data": {"text": "The functional characteristics of rabbit PAT1 in either mammalian cells or renal BBMV suggest that PAT1 is the low-affinity transporter of proline, glycine and hydroxyproline believed to be defective in patients with iminoglycinuria.", "entity1": "PAT1", "entity2": "glycine", "span1": [99, 103], "span2": [148, 155]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5465": {"label": 4, "data": {"text": "In the DRN, brexpiprazole completely inhibited the firing of 5-HT neurons via 5-HT1A agonism and was more potent than aripiprazole (ED50 = 230 and 700 mug/kg, respectively).", "entity1": "5-HT1A", "entity2": "aripiprazole", "span1": [78, 84], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12018": {"label": 1, "data": {"text": "CRE and EB treatment also recovered TH immunopositive fibers and cells, respectively, from MPTP toxicity.", "entity1": "TH", "entity2": "MPTP", "span1": [36, 38], "span2": [91, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9180": {"label": 8, "data": {"text": "Staining around the edges of the brown fat cells was observed with the SSAO substrates, tyramine and benzylamine.", "entity1": "SSAO", "entity2": "benzylamine", "span1": [71, 75], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7285": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "TGF-beta2", "entity2": "PFD", "span1": [28, 37], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10260": {"label": 8, "data": {"text": "However, desipramine at a low concentration essentially blocked the radioactive outflow induced by all of these substances with the exception of MPP+, indicating the NAT and not an OCT as their primary site of action.", "entity1": "NAT", "entity2": "MPP+", "span1": [166, 169], "span2": [145, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3926": {"label": 5, "data": {"text": "Identification of a novel benzimidazole derivative as a highly potent NPY Y5 receptor antagonist with an anti-obesity profile.", "entity1": "NPY Y5 receptor", "entity2": "benzimidazole", "span1": [70, 85], "span2": [26, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5916": {"label": 3, "data": {"text": "Acetylation of phenelzine at the N2 position presumably interferes with the inhibition of the transaminase enzymes for gamma-aminobutyric acid and alanine.", "entity1": "transaminase", "entity2": "N2", "span1": [94, 106], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2836": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "pyridoxal 5-phosphate", "span1": [83, 99], "span2": [124, 145]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8761": {"label": 8, "data": {"text": "In conclusion, this study expands the understanding of the substrate specificity of UGT2B10, highlighting its preference for tertiary amines with higher affinities and clearance values than those of UGT1A4 and UGT1A3.", "entity1": "UGT2B10", "entity2": "tertiary amines", "span1": [84, 91], "span2": [125, 140]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15093": {"label": 3, "data": {"text": "Avibactam (formerly NXL104, AVE1330A) is a synthetic non-\u03b2-lactam, \u03b2-lactamase inhibitor that inhibits the activities of Ambler class A and C \u03b2-lactamases and some Ambler class D enzymes.", "entity1": "\u03b2-lactamase", "entity2": "Avibactam", "span1": [67, 78], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13835": {"label": 3, "data": {"text": "Subsequent studies demonstrated that wild-type and hyperinsulinemia/hyperammonemia forms of GDH are inhibited by the green tea polyphenols, epigallocatechin gallate and epicatechin gallate.", "entity1": "GDH", "entity2": "epicatechin gallate", "span1": [92, 95], "span2": [169, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4290": {"label": 8, "data": {"text": "Uptake of the radiolabeled model substrates estradiol 17\u03b2-glucuronide, estrone 3-sulfate, and dehydroepiandrosterone sulfate (DHEAS) was determined in the absence and presence of compounds 1-6 using Chinese hamster ovary (CHO) cells stably expressing either OATP1B1 or OATP1B3.", "entity1": "OATP1B1", "entity2": "estradiol 17\u03b2-glucuronide", "span1": [258, 265], "span2": [44, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11963": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "PIP5K1B", "entity2": "PI(4,5)P2", "span1": [0, 7], "span2": [252, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3910": {"label": 3, "data": {"text": "Importantly, pre-treatment with buthionine sulfoximine (BSO), an inhibitor of \u03b3-GCS, prevented \u03b1-MeDA induced increase in GSH levels, but did not augment this metabolite cytotoxicity.", "entity1": "\u03b3-GCS", "entity2": "buthionine sulfoximine", "span1": [78, 83], "span2": [32, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13241": {"label": 3, "data": {"text": "Down-regulation of GRIP1 by glutamate was blocked by carbobenzoxyl-leucinyl-leucinyl-leucinal (MG132), a proteasome inhibitor and by expression of K48R-ubiquitin, a dominant negative form of ubiquitin.", "entity1": "GRIP1", "entity2": "glutamate", "span1": [19, 24], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1676": {"label": 4, "data": {"text": "BACKGROUND: The intravenous anesthetic etomidate exhibits structural similarities to specific alpha2-adrenoceptor agonists of the type such as dexmedetomidine.", "entity1": "alpha2-adrenoceptor", "entity2": "dexmedetomidine", "span1": [94, 113], "span2": [143, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10759": {"label": 1, "data": {"text": "Induction of heparin-binding EGF-like growth factor and activation of EGF receptor in imatinib mesylate-treated squamous carcinoma cells.", "entity1": "heparin-binding EGF-like growth factor", "entity2": "imatinib mesylate", "span1": [13, 51], "span2": [86, 103]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4584": {"label": 0, "data": {"text": "The approach is demonstrated by selective labeling of proteins in bacterial cells immobilized in the center of a laminar-flow microfluidic channel, where they are exposed to overlapping, opposed gradients of inducers of the N- and C-terminal MetRS fragments.", "entity1": "MetRS", "entity2": "C", "span1": [242, 247], "span2": [231, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12769": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "5-FU", "span1": [0, 20], "span2": [80, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6690": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "Ca(2+)-permeable channel", "entity2": "menthol", "span1": [18, 42], "span2": [88, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2164": {"label": 1, "data": {"text": "There was close correspondence between peak increases in DA and DAT occupancy.", "entity1": "DAT", "entity2": "DA", "span1": [64, 67], "span2": [57, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7061": {"label": 1, "data": {"text": "Retinoid is a collective term for compounds which bind to and activate retinoic acid receptors (RARalpha, beta, gamma and RXRalpha, beta, gamma), members of nuclear hormone receptor superfamily.", "entity1": "retinoic acid receptors", "entity2": "Retinoid", "span1": [71, 94], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1380": {"label": 9, "data": {"text": "Interestingly, gemfibrozil strongly inhibited the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of GAS in cytokine-stimulated astroglial cells.", "entity1": "cytokine", "entity2": "gemfibrozil", "span1": [118, 126], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15423": {"label": 1, "data": {"text": "In non-pre-treated cells, only efflux transporters were down-regulated by 7-ketosterols, showing a greater influence upon ABCG5 expression.", "entity1": "ABCG5", "entity2": "7-ketosterols", "span1": [122, 127], "span2": [74, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14613": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala119Gly", "entity2": "dFdC", "span1": [81, 90], "span2": [230, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7550": {"label": 8, "data": {"text": "PLZ is also a substrate for MAO, and studies suggest that a metabolite formed by the action of this enzyme on PLZ may be responsible for the increase in GABA observed.", "entity1": "MAO", "entity2": "PLZ", "span1": [28, 31], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10546": {"label": 1, "data": {"text": "A transcription factor-transcription factor binding array analysis of nuclear lysate from RA-treated cells indicated several prominent RARalpha binding partners; among these, Oct1, NFATc3, and CREB2 were identified by competition EMSA and supershift and chromatin immunoprecipitation assays as components of the complex.", "entity1": "RARalpha", "entity2": "RA", "span1": [135, 143], "span2": [90, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11018": {"label": 3, "data": {"text": "These results suggested that Captopril can protect the vascular endothelium against the damages induced by L-methionine in rats, and the beneficial effects of Captopril may be related to attenuating the decrease in PON1 activity and NO levels.", "entity1": "PON1", "entity2": "L-methionine", "span1": [215, 219], "span2": [107, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6509": {"label": 3, "data": {"text": "In conclusion, the renin inhibitor Aliskiren dose-dependently decreases Ang II levels in humans following oral administration.", "entity1": "Ang II", "entity2": "Aliskiren", "span1": [72, 78], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6143": {"label": 1, "data": {"text": "Thus, the serine in position HERG 620 may participate directly in dofetilide binding; however, an intact C-type inactivation process seems to be crucial for high-affinity drug binding.", "entity1": "HERG", "entity2": "dofetilide", "span1": [29, 33], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5870": {"label": 9, "data": {"text": "By contrast, neither amoxapine nor amitriptyline can be considered as possible ligands of 5-HT1A and 5-HT1B receptors because their affinities for these sites are in the micromolar range (or even worse).", "entity1": "5-HT1B", "entity2": "amitriptyline", "span1": [101, 107], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7194": {"label": 8, "data": {"text": "KIEs were measured on the arsenolysis of 5'-methylthioadenosine (MTA) catalyzed by MTAP and were corrected for the forward commitment to catalysis.", "entity1": "MTAP", "entity2": "MTA", "span1": [83, 87], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3449": {"label": 1, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "human dopamine transporter", "entity2": "[(3)H]WIN 35428", "span1": [167, 193], "span2": [140, 155]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14867": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "protein kinase C", "entity2": "BIS", "span1": [74, 90], "span2": [136, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12417": {"label": 1, "data": {"text": "Plasma glucose, active GLP-1 (7-36) amide concentration and insulin levels were measured after glucose loading.", "entity1": "GLP-1", "entity2": "glucose", "span1": [23, 28], "span2": [95, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11126": {"label": 1, "data": {"text": "Prazosin was found to be unselective; 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101), 5-methyl-urapidil, indoramin and (+)-niguldipine were confirmed as selective for the alpha 1A-adrenoceptor, whereas spiperone was weakly alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptor", "entity2": "2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane", "span1": [192, 213], "span2": [38, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1183": {"label": 2, "data": {"text": "In the present study, we investigated the effect of fenoterol-induced constitutive beta(2)-adrenoceptor activity on muscarinic receptor agonist- and histamine-induced bovine tracheal smooth muscle contractions.", "entity1": "beta(2)-adrenoceptor", "entity2": "fenoterol", "span1": [83, 103], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5361": {"label": 3, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.", "entity1": "I-\u03baB\u03b5", "entity2": "vitamin C", "span1": [93, 98], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14199": {"label": 1, "data": {"text": "Furthermore, these findings imply that CHOP may be a possible candidate as the chemosensitizing factor for induction of cytotoxicity in ATC cells exposed to SU5416.", "entity1": "CHOP", "entity2": "SU5416", "span1": [39, 43], "span2": [157, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14902": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "flavin mono-oxygenase", "entity2": "trimethylamine", "span1": [24, 45], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5550": {"label": 2, "data": {"text": "This study investigates the involvement of alpha(2)-adrenergic receptors (AR) in mouse brain induced by a low dose of methamphetamine (METH, 2 mg/kg).", "entity1": "AR", "entity2": "METH", "span1": [74, 76], "span2": [135, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1078": {"label": 1, "data": {"text": "The capacity of acetylcholinesterase inhibitors, with the exception of tacrine and ambenonium, to displace bound [3H]-oxotremorine-M in preference to [3H]quinuclinidyl benzilate predicts that the former compounds could act as potential agonists at muscarinic receptors.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [248, 268], "span2": [113, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14490": {"label": 8, "data": {"text": "Human liver microsomes of the wild-type CYP2D6 metabolized 5-methoxytryptamine to serotonin more effectively than did the defective CYP2D6*4*4 ones.", "entity1": "CYP2D6", "entity2": "5-methoxytryptamine", "span1": [40, 46], "span2": [59, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1583": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "AChE", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine", "span1": [26, 30], "span2": [231, 306]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5090": {"label": 1, "data": {"text": "Aldosterone-induced ENaC and basal Na(+)/K(+)-ATPase trafficking via protein kinase D1-phosphatidylinositol 4-kinaseIII\u03b2 trans Golgi signalling in M1 cortical collecting duct cells.", "entity1": "phosphatidylinositol 4-kinaseIII\u03b2", "entity2": "Aldosterone", "span1": [87, 120], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12529": {"label": 8, "data": {"text": "The test procedure was verified with respect to intestinal lactose hydrolysis by demonstrating a linear relationship between lactose/lactulose excretion and log jejunal mucosal lactase activity by in vitro assay (R2 = 0.95) in a further group of subjects.", "entity1": "lactase", "entity2": "lactulose", "span1": [177, 184], "span2": [133, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7842": {"label": 2, "data": {"text": "Ribavirin-induced intracellular GTP depletion activates transcription elongation in coagulation factor VII gene expression.", "entity1": "coagulation factor VII", "entity2": "Ribavirin", "span1": [84, 106], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11927": {"label": 3, "data": {"text": "HbA1c level in DM12W group was higher than in DM4W group, HbA1c level in EtOH+DM8W group was lower than in DM8W group.", "entity1": "HbA1c", "entity2": "EtOH", "span1": [58, 63], "span2": [73, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8630": {"label": 2, "data": {"text": "Collectively, these findings provide evidence that arsenic causes prolonged activation of Nrf2 through autophagy dysfunction, possibly providing a similar scenario to constitutive activation of Nrf2 found in certain human cancers.", "entity1": "Nrf2", "entity2": "arsenic", "span1": [90, 94], "span2": [51, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"981": {"label": 2, "data": {"text": "The BH(4) treatment was associated with a 2-fold increase in eNOS activity as well as a 70% reduction in endothelial O(2)(-) production compared with those in fructose-fed rats.", "entity1": "eNOS", "entity2": "BH(4)", "span1": [61, 65], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11242": {"label": 1, "data": {"text": "Finally, we illustrate how BH4 might transform the NOS dimer into an efficient S-nitrosoglutathione synthase,and briefly touch on some more speculative aspects of the role of BH4 in NO synthesis.", "entity1": "S-nitrosoglutathione synthase", "entity2": "BH4", "span1": [79, 108], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10729": {"label": 4, "data": {"text": "Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin.", "entity1": "oxytocin receptor", "entity2": "oxytocin", "span1": [59, 76], "span2": [128, 136]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4438": {"label": 2, "data": {"text": "PP242-induced reversal of deptor suppression by TGF\u03b2 was associated with a significant inhibition of TGF\u03b2-stimulated protein synthesis and hypertrophy.", "entity1": "deptor", "entity2": "PP242", "span1": [26, 32], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11454": {"label": 1, "data": {"text": "A previous crystal structure of a microcystin bound to the catalytic subunit of protein phosphatase-1 (PP-1c) showed distinct changes in the active site region when compared with protein phosphatase-1 structures bound to other toxins.", "entity1": "protein phosphatase-1", "entity2": "microcystin", "span1": [80, 101], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7127": {"label": 0, "data": {"text": "Truncated proteins with a complete GAF-B were dimers, but those lacking the N-terminal 46 amino acids of GAF-B were monomers, indicating that these residues are vital for GAF-B-mediated PDE5 dimerization.", "entity1": "GAF-B", "entity2": "amino acids", "span1": [105, 110], "span2": [90, 101]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13629": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "Top1p", "entity2": "C", "span1": [0, 5], "span2": [53, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9951": {"label": 9, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-1", "entity2": "celecoxib", "span1": [180, 185], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8355": {"label": 3, "data": {"text": "SAR and lead optimization studies for Rock inhibitors based on amino acid-derived quinazolines are described.", "entity1": "Rock", "entity2": "amino acid", "span1": [38, 42], "span2": [63, 73]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3541": {"label": 1, "data": {"text": "These results suggest that LTD4 increases A\u03b2 peptide burden via activation of CysLT(1)R, which further affects APP levels and activity of \u03b2- and \u03b3-secretases via the NF-\u03baB pathway.", "entity1": "NF-\u03baB", "entity2": "LTD4", "span1": [166, 171], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4982": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bcl2", "entity2": "DZN", "span1": [155, 159], "span2": [245, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7780": {"label": 2, "data": {"text": "Accordingly, in transfection experiments performed in TPC1 cells, treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence.", "entity1": "NIS promoter", "entity2": "PJ34", "span1": [96, 108], "span2": [81, 85]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4441": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "MAO", "entity2": "isatin", "span1": [147, 150], "span2": [50, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6848": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "methionine synthase", "entity2": "Hcy", "span1": [144, 163], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1780": {"label": 9, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1bAR", "entity2": "Tamsulosin", "span1": [85, 94], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1317": {"label": 2, "data": {"text": "In addition to this pronounced loss of function, M1766L also showed a 10-fold increase in the persistent late sodium current.", "entity1": "M1766L", "entity2": "sodium", "span1": [49, 55], "span2": [110, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3671": {"label": 3, "data": {"text": "Additionally, the mRNA levels of melanogenesis-related genes (c-KIT, stem cell factor (SCF), and macrophage migration inhibitory factor (MIF)) were down-regulated by artemisinic acid.", "entity1": "MIF", "entity2": "artemisinic acid", "span1": [137, 140], "span2": [166, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9283": {"label": 5, "data": {"text": "Incubation of rat aortic membranes with the irreversible alpha 1B-adrenoceptor antagonist, chloroethylclonidine (CEC: 10 microM) did not change the KD of [3H]-prazosin binding in comparison to untreated membranes, but reduced by 88% the total number of binding sites (Bmax).", "entity1": "alpha 1B-adrenoceptor", "entity2": "chloroethylclonidine", "span1": [57, 78], "span2": [91, 111]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5": {"label": 5, "data": {"text": "Labetalol (> or = 3 x 10(-8) M) and dilevalol (> or = 10(-8) M) caused surmountable antagonism of the isoprenaline responses of the atria and the pA2 values were 8.60 and 8.98 at the beta 1-adrenoceptors of the rat left atria and 7.90 and 8.31, respectively, on the guinea-pig left atria which has functional beta 1- and beta 2-adrenoceptors.", "entity1": "beta 1-adrenoceptors", "entity2": "dilevalol", "span1": [183, 203], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7232": {"label": 2, "data": {"text": "In contrast to testosterone, GnRH-induced nuclear translocation did not transcriptionally activate the androgen receptor.", "entity1": "androgen receptor", "entity2": "testosterone", "span1": [103, 120], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1790": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "tyrosine kinase", "entity2": "CI-1033", "span1": [101, 116], "span2": [67, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7452": {"label": 2, "data": {"text": "Ovariectomy downregulates glutaredoxin and renders female mice vulnerable to L-BOAA toxicity as evidenced by activation of AP1, loss of GSH and complex I activity indicating the important role of glutaredoxin in neuroprotection.", "entity1": "AP1", "entity2": "L-BOAA", "span1": [123, 126], "span2": [77, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2970": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "Y612F", "entity2": "sildenafil", "span1": [64, 69], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10764": {"label": 2, "data": {"text": "Inhibitors and neutralizing antibodies against heparin-binding epidermal growth factor-like growth factor (HB-EGF), and to a lesser extent transforming growth factor-alpha, reduced imatinib-mediated mitogen activated protein kinase (MAPK) activation.", "entity1": "mitogen activated protein kinase", "entity2": "imatinib", "span1": [199, 231], "span2": [181, 189]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10905": {"label": 8, "data": {"text": "Pyridoxal kinase (PDXK) catalyzes the phosphorylation of pyridoxal, pyridoxamine, and pyridoxine in the presence of ATP and Zn2+.", "entity1": "Pyridoxal kinase", "entity2": "pyridoxal", "span1": [0, 16], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5358": {"label": 1, "data": {"text": "It is possible that vitamin C, an antioxidant, may prevent cigarette smoke (CS)-induced NF-\u03baB activation that involves degradation of I-\u03baB\u03b5 and nuclear translocation of c-Rel/p50 in alveolar epithelial cells.", "entity1": "p50", "entity2": "vitamin C", "span1": [175, 178], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15418": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "TNF\u03b1", "entity2": "cholesterol", "span1": [84, 88], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"9497": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "dyclonine", "span1": [28, 42], "span2": [83, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3937": {"label": 2, "data": {"text": "The reactivation of brain AChE inhibited with tabun demonstrated better activity of new compound BT-07-4M, TMB-4 and obidoxime from symmetric oximes, and BT-05 and BT-03 possessing asymmetric structure.", "entity1": "AChE", "entity2": "BT-03", "span1": [26, 30], "span2": [164, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4104": {"label": 1, "data": {"text": "In this study, we investigated SFO-induced atherosclerotic plaque vulnerability (possibility of rupture) in apolipoprotein E-knockout (apoE(-/-)) mice.", "entity1": "apolipoprotein E", "entity2": "SFO", "span1": [108, 124], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7907": {"label": 9, "data": {"text": "However, down-regulation of ATF4 and/or CHOP expression by siRNA had no effect on helenalin-induced apoptosis in Caki and HCT116 cells.", "entity1": "CHOP", "entity2": "helenalin", "span1": [40, 44], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7906": {"label": 9, "data": {"text": "However, down-regulation of ATF4 and/or CHOP expression by siRNA had no effect on helenalin-induced apoptosis in Caki and HCT116 cells.", "entity1": "ATF4", "entity2": "helenalin", "span1": [28, 32], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10057": {"label": 3, "data": {"text": "It showed high rat lymphoma growth-inhibitory and lytic activity in vitro (IC50 = 0.16 mM), based specifically on inhibition of x(c)--mediated cystine uptake, in contrast to its colonic metabolites, sulfapyridine and 5-aminosalicylic acid.", "entity1": "x(c)", "entity2": "sulfapyridine", "span1": [128, 132], "span2": [199, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14683": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "3A4", "entity2": "GSK1292263", "span1": [116, 119], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8044": {"label": 3, "data": {"text": "Exposure of H9c2 cells to high glucose reduced AMPK activity, inhibited Jun NH2-terminal kinase 1 (JNK1)-B-cell lymphoma 2 (Bcl-2) signaling, and promoted Beclin1 binding to Bcl-2.", "entity1": "Jun NH2-terminal kinase 1", "entity2": "glucose", "span1": [72, 97], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14655": {"label": 3, "data": {"text": "Here we present boronic and borinic acid derivatives as a new class of potent and nontoxic APT inhibitors.", "entity1": "APT", "entity2": "boronic", "span1": [91, 94], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2664": {"label": 3, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "PDE4", "entity2": "4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one", "span1": [178, 182], "span2": [196, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8204": {"label": 3, "data": {"text": "We previously reported that caffeoyl-amino acidyl-hydroxamic acid (CA-Xaa-NHOH) acted as both a good antioxidant and tyrosinase inhibitor, in particular when caffeic acid was conjugated with proline or amino acids having aromatic ring like phenylalanine.", "entity1": "tyrosinase", "entity2": "caffeoyl-amino acidyl-hydroxamic acid", "span1": [117, 127], "span2": [28, 65]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15592": {"label": 8, "data": {"text": "IPI-926 is both a substrate and inhibitor (IC50\u2009=\u20091.9\u2009\u00b5M) of P-glycoprotein.", "entity1": "P-glycoprotein", "entity2": "IPI-926", "span1": [61, 75], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3067": {"label": 3, "data": {"text": "Pretreatment of rats with the MAO inhibitor tranylcypromine prevented the increase in brain GABA and ALA levels with PLZ, but did not block the effect of VIG on GABA.", "entity1": "MAO", "entity2": "tranylcypromine", "span1": [30, 33], "span2": [44, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13414": {"label": 9, "data": {"text": "The mRNA expression of PtdSer synthase 1 (PSS1) and PtdSer synthase 2 (PSS2) was not reduced by ethanol.", "entity1": "PtdSer synthase 2", "entity2": "ethanol", "span1": [52, 69], "span2": [96, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15892": {"label": 8, "data": {"text": "Targeted disruption of the gene encoding the N-glycosyltransferase, prlH, abolished pyralomicin production, and recombinant expression of PrlA confirms the activity of this enzyme as a sugar phosphate cyclase involved in the formation of the C7-cyclitol moiety.", "entity1": "sugar phosphate cyclase", "entity2": "cyclitol", "span1": [185, 208], "span2": [245, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"892": {"label": 1, "data": {"text": "Here we compared the action of N(5)-substituted derivatives on recombinant rat neuronal nitric oxide synthase with their effects on dihydropteridine reductase (EC 1.6.99.7) and phenylalanine hydroxylase (EC 1.14.16.1),the well-studied classical H(4)biopterin-dependent reactions.", "entity1": "phenylalanine hydroxylase", "entity2": "N(5)", "span1": [177, 202], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7902": {"label": 1, "data": {"text": "The AhR target gene CYP1A1 mRNA expression was induced by TCDD, but was not affected by the AR CAG length.", "entity1": "AhR", "entity2": "TCDD", "span1": [4, 7], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14564": {"label": 1, "data": {"text": "For example, involvement of \u03b2-catenin in LH\u03b2 induction by GnRH has been discovered.", "entity1": "\u03b2-catenin", "entity2": "GnRH", "span1": [28, 37], "span2": [58, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"964": {"label": 9, "data": {"text": "U50, 488H caused a significant down-regulation of the hkor, although etorphine did not.", "entity1": "hkor", "entity2": "etorphine", "span1": [54, 58], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11471": {"label": 1, "data": {"text": "This study examined the effect of theophylline on the gene expression of secretory proteins and phosphodiesterases in the submaxillary gland.", "entity1": "phosphodiesterases", "entity2": "theophylline", "span1": [96, 114], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11782": {"label": 3, "data": {"text": "There was no significant difference in TLR4, NF-\u03baB, and IL-27 mRNA and proteins between curcumin-treated and sulfasalazine-treated groups.", "entity1": "NF-\u03baB", "entity2": "sulfasalazine", "span1": [45, 50], "span2": [109, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9668": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "rhIL-5", "entity2": "cytochalasin B", "span1": [165, 171], "span2": [220, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7288": {"label": 3, "data": {"text": "PFD leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin.", "entity1": "pro-protein convertase", "entity2": "PFD", "span1": [152, 174], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"12255": {"label": 1, "data": {"text": "Variants in the IMPDH2 gene may account for the large inter-individual variability in baseline enzyme activity, immunosuppressive efficacy and side effects in transplant recipients receiving mycophenolic acid.", "entity1": "IMPDH2", "entity2": "mycophenolic acid", "span1": [16, 22], "span2": [191, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8687": {"label": 3, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "TAp73", "entity2": "imatinib", "span1": [146, 151], "span2": [27, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1120": {"label": 3, "data": {"text": "Indomethacin completely antagonizes CA activity, i.e. abolishes the inhibitory effect of acetazolamide on CA.", "entity1": "CA", "entity2": "acetazolamide", "span1": [36, 38], "span2": [89, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"157": {"label": 5, "data": {"text": "ORF 17583, a histamine H2-receptor antagonist, inhibited gastric acid secretion in pylorus-ligated rats (ED50 = 4.9 mg/kg intraduodenal; 3.4 mg/kg p.o.", "entity1": "histamine H2-receptor", "entity2": "ORF 17583", "span1": [13, 34], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4195": {"label": 3, "data": {"text": "Furthermore, PTE treatment directly inhibited the phosphorylation of JAK2 at Tyr 1007 and the downstream activation of STAT3.", "entity1": "STAT3", "entity2": "PTE", "span1": [119, 124], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1042": {"label": 1, "data": {"text": "In addition, ADP was shown to strongly antagonize TOP2-mediated DNA cleavage induced by ATP-sensitive but not ATP-insensitive TOP2 poisons.", "entity1": "TOP2", "entity2": "ADP", "span1": [50, 54], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16023": {"label": 1, "data": {"text": "These results show that haloperidol promotes mTORC1- and S6K1-dependent phosphorylation of rpS6 at Ser240/244, in a subpopulation of striatal MSNs expressing D2Rs.", "entity1": "mTORC1", "entity2": "haloperidol", "span1": [45, 51], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14457": {"label": 9, "data": {"text": "Moreover, mutation of ECII can alter this coupled equilibrium from GTP-insensitive agonist binding to more conventional GTP-sensitive binding.", "entity1": "ECII", "entity2": "GTP", "span1": [22, 26], "span2": [67, 70]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3774": {"label": 1, "data": {"text": "Opioid receptor binding affinity and activity were assessed using [(3)H]-diprenorphine binding, guanosine-5'-O-(3-[35S]-thio) triphosphate ([(35)S]-GTP\u03b3S) binding and isolated guinea-pig ileum.", "entity1": "Opioid receptor", "entity2": "guanosine-5'-O-(3-[35S]-thio) triphosphate", "span1": [0, 15], "span2": [96, 138]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15122": {"label": 2, "data": {"text": "Notably, the antioxidant Trolox\u2122 reversed the Mn (20\u00a0mg/kg)-dependent augmentation in p38(MAPK) phosphorylation and reduced the Mn (20\u00a0mg/kg)-induced caspase activity and F(2)-isoprostane production.", "entity1": "MAPK", "entity2": "Mn", "span1": [90, 94], "span2": [46, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"5071": {"label": 9, "data": {"text": "In addition to CYP2B6, anisomycin co-treatment potentiated an increase in CYP2A7 and CYP2C9 mRNAs but not CYP3A4 or UDP-glucuronosyltransferase 1A1 mRNAs.", "entity1": "CYP3A4", "entity2": "anisomycin", "span1": [106, 112], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"663": {"label": 3, "data": {"text": "METHODS: COX-1 inhibition was determined by measuring thromboxane B2 (TXB2)-generation from clotting whole blood ex vivo after single oral doses of 7.5 and 15 mg meloxicam and 75 mg diclofenac and at steady state (15 mg meloxicam daily and 150 mg diclofenac daily).", "entity1": "COX-1", "entity2": "meloxicam", "span1": [9, 14], "span2": [162, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7708": {"label": 3, "data": {"text": "The mechanism of OP poisoning involves inhibition of acetylcholinesterase (AChE) leading to inactivation of the enzyme which has an important role in neurotransmission.", "entity1": "acetylcholinesterase", "entity2": "OP", "span1": [53, 73], "span2": [17, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7609": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(2)", "entity2": "Vaprisol", "span1": [187, 191], "span2": [222, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14952": {"label": 1, "data": {"text": "We hypothesized that styrene metabolites have lower affinity than styrene toward CYP2E1 and limited ability to induce cooperative effects during metabolism.", "entity1": "CYP2E1", "entity2": "styrene", "span1": [81, 87], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"594": {"label": 9, "data": {"text": "The action of 15d-PGJ2 does not appear to involve its nuclear receptor peroxisome proliferator-activated receptor gamma (PPARgamma) because troglitazone, a specific ligand of PPARgamma, was unable to inhibit iNOS induction, and neither troglitazone nor 15d-PGJ2 could stimulate the activity of a PPAR-dependent promoter in the absence of cotransfected PPARgamma.", "entity1": "PPAR", "entity2": "troglitazone", "span1": [296, 300], "span2": [236, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15413": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "HMGCoA", "entity2": "stigmasterol", "span1": [219, 225], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"9475": {"label": 4, "data": {"text": "M&B-28767, a putative EP3 agonist, and misoprostol, a putative EP2/EP3 agonist, also bound to this receptor with Ki values of 120 nM.", "entity1": "EP3", "entity2": "M&B-28767", "span1": [22, 25], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4031": {"label": 3, "data": {"text": "Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.", "entity1": "leukotriene A(4) hydrolase", "entity2": "benzofuran", "span1": [65, 91], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8026": {"label": 1, "data": {"text": "Apomorphine is a bimodal modulator of TRPA1 channels.", "entity1": "TRPA1", "entity2": "Apomorphine", "span1": [38, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12479": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO2", "entity2": "benzydamine", "span1": [17, 21], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10496": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "CGP 12177", "span1": [392, 423], "span2": [344, 353]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1800": {"label": 3, "data": {"text": "Epidermal growth factor receptor inhibitors currently under investigation include the small molecules gefitinib (Iressa, ZD1839) and erlotinib (Tarceva, OSI-774), as well as monoclonal antibodies such as cetuximab (IMC-225, Erbitux).", "entity1": "Epidermal growth factor receptor", "entity2": "erlotinib", "span1": [0, 32], "span2": [133, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11206": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel.", "entity1": "human brain K(+) channel", "entity2": "sertindole", "span1": [62, 86], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5889": {"label": 1, "data": {"text": "Mouse ornithine decarboxylase (ODC) was expressed in Escherichia coli and the purified recombinant enzyme used for determination of the binding site for pyridoxal 5'-phosphate and of the residues modified in the inactivation of the enzyme by the enzyme-activated irreversible inhibitor, alpha-difluoromethylornithine (DFMO).", "entity1": "Mouse ornithine decarboxylase", "entity2": "pyridoxal 5'-phosphate", "span1": [0, 29], "span2": [153, 175]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5142": {"label": 1, "data": {"text": "An intermediate GTX2,3-aldehyde was first synthesized by activating the NH2 group of the 2nd and 8th amino acid residues with three different aldehydes and two artificial complete antigens GTX2,3-aldehyde-bovine serum albumin (BSA) and GTX2,3-aldehyde- keyhole limpet hemocyanin (KLH) were then prepared by cross-linking the intermediate with BSA or KLH.", "entity1": "keyhole limpet hemocyanin", "entity2": "GTX2,3-aldehyde", "span1": [253, 278], "span2": [236, 251]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3602": {"label": 1, "data": {"text": "We found distinct differences in the action of ifenprodil at GluN1/GluN2B in comparison with previous studies on the effect of zinc on GluN1/GluN2A gating, which may arise due to their unique binding sites.", "entity1": "GluN1", "entity2": "zinc", "span1": [135, 140], "span2": [127, 131]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11989": {"label": 2, "data": {"text": "Such model of Nox4 activity regulation could provide new insight into the understanding of the molecular mechanism of the electron transfer through the enzyme, i.e., its potential redox regulation, and could also define new therapeutic targets in diseases in which quinones and Nox4 are implicated.", "entity1": "Nox4", "entity2": "quinones", "span1": [14, 18], "span2": [265, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12648": {"label": 1, "data": {"text": "Salicylic acid promotes dissociation of (125)I-ET-1 ETA receptor complexes both in the absence and the presence of unlabeled ET-1.", "entity1": "ETA receptor", "entity2": "(125)I", "span1": [52, 64], "span2": [40, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15237": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B1", "entity2": "silybin B", "span1": [0, 7], "span2": [214, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"13723": {"label": 2, "data": {"text": "RTX treatment also induced foci of RAD51, gamma-H2AX, phospho-Chk1, and phospho-NBS1, although the extent of co-localization with RPA2 foci varied.", "entity1": "RAD51", "entity2": "RTX", "span1": [35, 40], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9750": {"label": 4, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "(5-HT)(1A)", "entity2": "yohimbine", "span1": [120, 130], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7057": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RXRs", "entity2": "Am80", "span1": [88, 92], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7212": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "c-jun", "entity2": "Cd", "span1": [172, 177], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10636": {"label": 3, "data": {"text": "Troglitazone, bosentan and glibenclamide inhibit the bile salt export pump (Bsep) which transports taurocholate into bile.", "entity1": "bile salt export pump", "entity2": "bosentan", "span1": [53, 74], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7622": {"label": 3, "data": {"text": "BACKGROUND: Lapatinib, the first dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases, was approved by the US Food and Drug Administration (FDA) in 2007.", "entity1": "EGFR", "entity2": "Lapatinib", "span1": [85, 89], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"567": {"label": 5, "data": {"text": "In another experiment, cyanopindolol, an antagonist of the serotonin terminal autoreceptor, also prolonged the clearance of 5-HT from the CA3 region.", "entity1": "serotonin terminal autoreceptor", "entity2": "cyanopindolol", "span1": [59, 90], "span2": [23, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7647": {"label": 3, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "Panx1", "entity2": "ATP", "span1": [78, 83], "span2": [26, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5654": {"label": 2, "data": {"text": "We reported that superfusion of hERG-expressing HEK293 (hERG-HEK) cells with matrine (1, 10 \u03bcM) increased the hERG current by promoting hERG channel activation.", "entity1": "hERG", "entity2": "matrine", "span1": [32, 36], "span2": [77, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6300": {"label": 2, "data": {"text": "These findings lend evidence of a 5-HT1B receptor/eNOS pathway, accounting in part for the activation of eNOS by 5-HT.", "entity1": "eNOS", "entity2": "5-HT", "span1": [105, 109], "span2": [113, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13432": {"label": 2, "data": {"text": "TGF-beta1 release was higher ( approximately 1.6-fold) in 25 mM (high) compared with 5 mM (normal) D-glucose.", "entity1": "TGF-beta1", "entity2": "D-glucose", "span1": [0, 9], "span2": [99, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6579": {"label": 8, "data": {"text": "The bacterial enzyme maltodextrin phosphorylase (MalP) catalyses the phosphorolysis of an alpha-1,4-glycosidic bond in maltodextrins, removing the non-reducing glucosyl residues of linear oligosaccharides as glucose-1-phosphate (Glc1P).", "entity1": "maltodextrin phosphorylase", "entity2": "Glc1P", "span1": [21, 47], "span2": [229, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2954": {"label": 0, "data": {"text": "Cocrystal structures of PDE5 catalytic (C) domain with inhibitors reveal a hydrogen bond and hydrophobic interactions with Tyr-612, hydrogen bonds with Gln-817, a hydrophobic clamp formed by Phe-820 and Val-782, and contacts with His-613, Leu-765, and Phe-786 [Sung et al.", "entity1": "PDE5 catalytic (C) domain", "entity2": "His", "span1": [24, 49], "span2": [230, 233]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15456": {"label": 4, "data": {"text": "Of the compounds active in the present assay system, the most potent compound 7, platyphyllonol-5-O-\u03b2-d-xylopyranoside, significantly suppressed the induction of peroxisome proliferator activated receptor \u03b3 (PPAR\u03b3 and CCAAT/enhancer binding protein \u03b1 (C/EBP\u03b1) protein expression, and inhibited adipocyte differentiation induced by troglitazone, a PPAR\u03b3 agonist.", "entity1": "PPAR\u03b3", "entity2": "troglitazone", "span1": [347, 352], "span2": [331, 343]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10506": {"label": 9, "data": {"text": "Exploration of potential mechanisms of resistance in SUM185 cells revealed failure of GW572016 to inhibit downstream ERK and Akt activation, despite inhibition of HER2 phosphorylation.", "entity1": "Akt", "entity2": "GW572016", "span1": [125, 128], "span2": [86, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1523": {"label": 3, "data": {"text": "administration of very low doses of okadaic acid (0.001-1 pg/mouse) and cantharidin (0.001-1 ng/mouse), which inhibit PP2A, produced a dose-dependent antagonism of the antinociception induced by morphine (s.c.).", "entity1": "PP2A", "entity2": "okadaic acid", "span1": [118, 122], "span2": [36, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12968": {"label": 0, "data": {"text": "The phosphorylation by gammaPKC resulted in activation of DGKgamma because a DGKgamma mutant in which Ser-776 and Ser-779 were substituted with glutamic acid to mimic phosphorylation exhibited significantly higher activity compared with wild type DGKgamma and an unphosphorylatable DGKgamma mutant.", "entity1": "DGKgamma", "entity2": "Ser", "span1": [77, 85], "span2": [114, 117]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4284": {"label": 3, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "GSK3\u03b2", "entity2": "SB216763", "span1": [41, 46], "span2": [57, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5586": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "5-fluorouracil", "span1": [121, 123], "span2": [71, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"6061": {"label": 3, "data": {"text": "NE, phorbol esters, and bradykinin each decreased alpha-AR mRNA levels by 70-80%.", "entity1": "alpha-AR", "entity2": "NE", "span1": [50, 58], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9521": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "RAR gamma", "entity2": "adapalene", "span1": [134, 143], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4268": {"label": 2, "data": {"text": "Activation of AMP-activated Protein Kinase and Phosphorylation of Glycogen Synthase Kinase3 \u03b2 Mediate Ursolic Acid Induced Apoptosis in HepG2 Liver Cancer Cells.", "entity1": "AMP-activated Protein Kinase", "entity2": "Ursolic Acid", "span1": [14, 42], "span2": [102, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1859": {"label": 3, "data": {"text": "Four prenylflavonoids, kurarinone ( 1), a chalcone of 1, kuraridin ( 2), kurarinol ( 3), kushenol H ( 4) and kushenol K ( 5) isolated from the roots of Sophora flavescens were investigated for their inhibitory effects on diacylglycerol acyltransferase (DGAT).", "entity1": "diacylglycerol acyltransferase", "entity2": "kurarinol", "span1": [221, 251], "span2": [73, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16013": {"label": 5, "data": {"text": "The involvement of the various DA receptor subtypes in the motor effects of N/OFQ and NOP receptor antagonists was evaluated pharmacologically, using D1/D5 (SCH23390), D2/D3 (raclopride, amisulpride) and D3 (S33084) receptor antagonists, and by using D2 receptor knockout mice.", "entity1": "D1", "entity2": "SCH23390", "span1": [150, 152], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1044": {"label": 3, "data": {"text": "Second, C427A mutant human TOP2alpha, which exhibits reduced ATPase activity, was shown to exhibit cross-resistance to all ATP-sensitive but not ATP-insensitive TOP2 poisons.", "entity1": "ATPase", "entity2": "ATP", "span1": [61, 67], "span2": [145, 148]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10424": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "retinoid receptors", "entity2": "Tazarotene", "span1": [113, 131], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6737": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "CEP-701", "span1": [273, 279], "span2": [193, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2919": {"label": 3, "data": {"text": "Existing ion channel blockers, such as amiodarone, dronedarone, bepridil, aprindine, and cibenzoline, have been found to have an NCX inhibitory action.", "entity1": "NCX", "entity2": "amiodarone", "span1": [129, 132], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13982": {"label": 5, "data": {"text": "Effects of the histamine H1 antagonist chlorcyclizine on rat fetal palate development.", "entity1": "histamine H1", "entity2": "chlorcyclizine", "span1": [15, 27], "span2": [39, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4177": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "NRF2", "entity2": "hydrogen peroxide", "span1": [151, 155], "span2": [227, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2096": {"label": 0, "data": {"text": "This 40 kDa PEG-conjugated IFNalpha(2a) ((40)PEG-IFNalpha(2a)) is obtained by the covalent binding of one 40 kDa branched PEG-polymer to a lysine side-chain of IFNalpha(2a).", "entity1": "IFNalpha(2a)", "entity2": "PEG", "span1": [27, 39], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13903": {"label": 9, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "Kir6.1", "entity2": "metformin", "span1": [166, 172], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6296": {"label": 3, "data": {"text": "UNLABELLED: Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor.", "entity1": "catechol-O-methyltransferase", "entity2": "Entacapone", "span1": [59, 87], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5542": {"label": 9, "data": {"text": "A slight decrease in P-selectin surface expression on platelets was found which was not modified by the presence of neutrophils and therefore by the neutrophil-derived NO.", "entity1": "P-selectin", "entity2": "NO", "span1": [21, 31], "span2": [168, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13133": {"label": 2, "data": {"text": "CONCLUSION(S): Short-term exposure of mifepristone in new starters of DMPA increases the expression of endometrial ERalpha, PRAB, PRB, and SRC-1 and promotes cell proliferation.", "entity1": "PRAB", "entity2": "mifepristone", "span1": [124, 128], "span2": [38, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13564": {"label": 8, "data": {"text": "We found that the removal of urea with urease is necessary since urea also produces a positive reaction.", "entity1": "urease", "entity2": "urea", "span1": [39, 45], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10572": {"label": 9, "data": {"text": "Perforin release from peripheral blood CTLs after PMA/ionomycin-stimulation was not influenced significantly by IMQ.", "entity1": "Perforin", "entity2": "IMQ", "span1": [0, 8], "span2": [112, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3105": {"label": 2, "data": {"text": "Prolonged use of tolvaptan leads to increased endogenous levels of AVP and perhaps over-stimulation of V(1A) receptors.", "entity1": "V(1A) receptors", "entity2": "tolvaptan", "span1": [103, 118], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3491": {"label": 2, "data": {"text": "In the CCl4 hepatotoxicity model, pre-treatment with PSM or silymarin resulted in significantly increased activities of ethylmorphine-N-demethylase and aniline 4-hydroxylase activity and cytochrome P450, compared to the CCl4 only group.", "entity1": "ethylmorphine-N-demethylase", "entity2": "CCl4", "span1": [120, 147], "span2": [220, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11647": {"label": 1, "data": {"text": "Tolvaptan is a breakthrough in the therapy of hyponatremia as it directly combats elevated AVP levels associated with the syndrome of inappropriate secretion of antidiuretic hormone, congestive heart failure, and cirrhosis of the liver.", "entity1": "AVP", "entity2": "Tolvaptan", "span1": [91, 94], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2492": {"label": 3, "data": {"text": "Licofelone, a balanced inhibitor of cyclooxygenase and 5-lipoxygenase, reduces inflammation in a rabbit model of atherosclerosis.", "entity1": "cyclooxygenase", "entity2": "Licofelone", "span1": [36, 50], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8102": {"label": 2, "data": {"text": "We found that wogonin can suppress the H2O2-stimulated actin remodeling and albumin uptake of HUVECs, as well as transendothelial cell migration of the human breast carcinoma cell MDA-MB-231.", "entity1": "actin", "entity2": "H2O2", "span1": [55, 60], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15384": {"label": 5, "data": {"text": "These results provide an example that attachment of a bulky side chain to the C-7\u03b1 position of E2 can produce ER antagonists with ER affinity comparable to that of ICI-182,780.", "entity1": "ER", "entity2": "ICI-182,780", "span1": [130, 132], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12408": {"label": 1, "data": {"text": "Cerebrovascular Dilation via Selective Targeting of the Cholane Steroid-Recognition Site in the BK Channel \u03b21-Subunit by a Novel Nonsteroidal Agent.", "entity1": "BK Channel \u03b21-Subunit", "entity2": "Cholane", "span1": [96, 117], "span2": [56, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14524": {"label": 2, "data": {"text": "This study shows ability of EGCG to raise plasma bile acid concentrations, mainly through Cyp7a1 upregulation, and to decrease bile production through reduction in Mrp2-mediated bile acid-independent bile flow.", "entity1": "Cyp7a1", "entity2": "EGCG", "span1": [90, 96], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2299": {"label": 5, "data": {"text": "Also consistent with the involvement of Gq coupled EP1 receptors, the PGE1 stimulation is inhibited by the PKCI vector (encoding the PKC inhibitory domain), the PKC inhibitor Go 6976, thapsigargin, as well as the calmodulin antagonists W7 and W13.", "entity1": "calmodulin", "entity2": "W13", "span1": [213, 223], "span2": [243, 246]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12687": {"label": 1, "data": {"text": "To elucidate the target genes regulated by these compounds, we treated Zucker diabetic fatty rats (ZDF) for 15 days with a PPAR-alpha-specific compound, fenofibrate, a PPAR-gamma-specific ligand, rosiglitazone, and a PPAR-alpha/-gamma coagonist, GW2331, and measured the levels of several messenger RNAs (mRNAs) in liver by real-time polymerase chain reaction.", "entity1": "PPAR-alpha", "entity2": "fenofibrate", "span1": [123, 133], "span2": [153, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9982": {"label": 1, "data": {"text": "In a search for less flexible analogues of caproctamine (1), a diamine diamide endowed with an interesting AChE affinity profile, we discovered compound 2, in which the terminal 2-methoxybenzyl groups of 1 have been incorporated into a tricyclic system.", "entity1": "AChE", "entity2": "diamide", "span1": [107, 111], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1188": {"label": 4, "data": {"text": "Bovine tracheal smooth muscle strips were incubated with 10 microM fenoterol or vehicle for various periods of time (5, 30 min, 18 h) at 37 degrees C. After extensive washout (3 h, 37 degrees C), isometric contractions were measured to the full muscarinic receptor agonist methacholine, the partial muscarinic receptor agonist 4-(m-chlorophenyl-carbamoyloxy)-2-butynyltrimethylammonium (McN-A-343) and histamine.", "entity1": "muscarinic receptor", "entity2": "methacholine", "span1": [245, 264], "span2": [273, 285]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6964": {"label": 1, "data": {"text": "As CRABPI was elevated far more than any other genes, we observed that the retinoids, all-trans retinoic acid and 9-cis retinoic acid, that bind CRABPI, promoted nitroblue tetrazolium-associated functional cell differentiation in p75NTR PC-3 cells, but not in neo control PC-3 cells.", "entity1": "CRABPI", "entity2": "retinoids", "span1": [145, 151], "span2": [75, 84]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10181": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "OATP8", "entity2": "rifamycin SV", "span1": [229, 234], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10680": {"label": 3, "data": {"text": "In Experiment 1, Antag I, Antag II and TT-235 inhibited the integrated uterine response to oxytocin at 5 minutes by 76%, 77% and 80%, respectively, compared to controls (p<0.05).", "entity1": "oxytocin", "entity2": "Antag II", "span1": [91, 99], "span2": [26, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4703": {"label": 2, "data": {"text": "V(5+) also increased serum hemoglobin (Hb) levels in animals treated for 24\u00a0h. Upon treatment of isolated hepatocytes with Hb alone or in the presence of TCDD, there was an increase in the AhR-dependent luciferase activity.", "entity1": "AhR", "entity2": "TCDD", "span1": [189, 192], "span2": [154, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8589": {"label": 2, "data": {"text": "Western blot assay demonstrated that DICO decreased Bcl-2 level and induced Bax translocation to cause cytochrome c release.", "entity1": "Bax", "entity2": "DICO", "span1": [76, 79], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9610": {"label": 1, "data": {"text": "Here, we report that MgATP and MgADP, but not the Mg salt of gamma-thio-ATP, stabilize the binding of prebound 8-azido-[alpha-32P]ATP to SUR1.", "entity1": "SUR1", "entity2": "8-azido-[alpha-32P]ATP", "span1": [137, 141], "span2": [111, 133]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14099": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "lenalidomide", "span1": [142, 146], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10516": {"label": 3, "data": {"text": "Exploration of potential mechanisms of resistance in SUM185 cells revealed failure of GW572016 to inhibit downstream ERK and Akt activation, despite inhibition of HER2 phosphorylation.", "entity1": "HER2", "entity2": "GW572016", "span1": [163, 167], "span2": [86, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3394": {"label": 1, "data": {"text": "The effects of amphetamine (AMPH) and cocaine (COC), for example, depend on the ability to increase dopamine in the synapse, by effects on either the plasma membrane transporter DAT or the vesicular transporter for monoamine storage, VMAT2.", "entity1": "DAT", "entity2": "COC", "span1": [178, 181], "span2": [47, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1381": {"label": 2, "data": {"text": "Since gemfibrozil is known to activate peroxisome proliferator-activated receptor-alpha (PPAR-alpha), we investigated the role of PPAR-alpha in gemfibrozil-mediated inhibition of iNOS.", "entity1": "peroxisome proliferator-activated receptor-alpha", "entity2": "gemfibrozil", "span1": [39, 87], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10734": {"label": 5, "data": {"text": "Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin.", "entity1": "oxytocin receptor", "entity2": "barusiban", "span1": [59, 76], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12734": {"label": 3, "data": {"text": "Agents which have recently been shown to block cyclin D1 translation by regulating calcium levels are the unsaturated essential fatty acid, eicosapentaenoic acid (EPA), the antidiabetic thiazolidinediones, and the antifungal agent, clotrimazole.", "entity1": "cyclin D1", "entity2": "EPA", "span1": [47, 56], "span2": [163, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10005": {"label": 1, "data": {"text": "Domperidone and haloperidol, which have affinity for dopamine D3 receptor, also inhibited R(+)-7-OH-DPAT-induced hypothermia.", "entity1": "dopamine D3 receptor", "entity2": "Domperidone", "span1": [53, 73], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15062": {"label": 1, "data": {"text": "Similarly, intraperitoneal administration of \u03b1-santalol (100mg/kg BW) and sandalwood oil (1g/kg BW) for two weeks modulated parameters such as serum aminotransferases, alkaline phosphatase, bilirubin, superoxide dismutase, catalase, free sulfhydryl, protein carbonyl, nitric oxide, liver lipid peroxide contents, and antioxidant capacity in d-galactose mediated oxidative stress induced mice.", "entity1": "alkaline phosphatase", "entity2": "\u03b1-santalol", "span1": [168, 188], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5271": {"label": 2, "data": {"text": "In fact, we demonstrated a significant stimulation of Nox4 activity by 4 quinone derivatives (AA-861, tBuBHQ, tBuBQ, and duroquinone) observed in 3 different cellular models, HEK293E, T-REx\u2122, and chondrocyte cell lines.", "entity1": "Nox4", "entity2": "tBuBHQ", "span1": [54, 58], "span2": [102, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6672": {"label": 8, "data": {"text": "Ribonucleotide reductase (RR) is responsible for the de novo conversion of the ribonucleoside diphosphates to deoxyribonucleoside diphosphates, which are essential for DNA synthesis and repair.", "entity1": "Ribonucleotide reductase", "entity2": "ribonucleoside diphosphates", "span1": [0, 24], "span2": [79, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4875": {"label": 3, "data": {"text": "Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.", "entity1": "BRAF", "entity2": "N-(thiophen-2-yl) benzamide", "span1": [75, 79], "span2": [32, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15731": {"label": 4, "data": {"text": "Fourteen of 17 parabens exhibited hER\u03b1 and/or hER\u03b2 agonistic activity at concentrations of \u2a7d1\u00d710(-5)M, whereas none of the 17 parabens showed AR agonistic or antagonistic activity.", "entity1": "hER\u03b1", "entity2": "parabens", "span1": [34, 38], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11521": {"label": 1, "data": {"text": "Dexamethasone probes glucocorticoid receptor (GR) function, while prednisolone probes both GR and mineralocorticoid receptor (MR) function.", "entity1": "GR", "entity2": "prednisolone", "span1": [91, 93], "span2": [66, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7418": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "Delta 6 desaturase", "entity2": "DHA", "span1": [11, 29], "span2": [232, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"2111": {"label": 1, "data": {"text": "Western blot analysis was used to determine any effect of DEC on the production of COX and inducible nitric-oxide synthase (iNOS) proteins.", "entity1": "COX", "entity2": "DEC", "span1": [83, 86], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9420": {"label": 8, "data": {"text": "We have identified adenosine deaminase, an enzyme involved in purine metabolism whose deficiency is associated with severe combined immunodeficiency, as a Grb3-3 binding protein that is not able to bind to Grb2.", "entity1": "adenosine deaminase", "entity2": "purine", "span1": [19, 38], "span2": [62, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8058": {"label": 3, "data": {"text": "Metformin-mediated downregulation of p38 mitogen-activated protein kinase-dependent excision repair cross-complementing 1 decreases DNA repair capacity and sensitizes human lung cancer cells to paclitaxel.", "entity1": "mitogen-activated protein kinase", "entity2": "Metformin", "span1": [41, 73], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"207": {"label": 3, "data": {"text": "Alprenolol and BAAM at 10(-7), 3 x 10(-7), and 10(-6) M inhibited the cardiac stimulation response slightly, which is indicative of membrane-stabilizing activity independent of beta-adrenoceptor blockade.", "entity1": "beta-adrenoceptor", "entity2": "Alprenolol", "span1": [177, 194], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14366": {"label": 3, "data": {"text": "The quinolizidine alkaloids (natural products) such as oxymatrine, sophoridine, sophocarpine and matrine carry the common molecular structure of O=C=N-C-C-C-N that possessed positive ionotropic effect and hERG blocking activity.", "entity1": "hERG", "entity2": "sophocarpine", "span1": [205, 209], "span2": [80, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"226": {"label": 3, "data": {"text": "The estrogenic agent 3 beta,5 alpha-NET and estradiol at a dose of 1.0 mg also inhibited the UG gene expression induced by P4.", "entity1": "UG", "entity2": "estradiol", "span1": [93, 95], "span2": [44, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3913": {"label": 1, "data": {"text": "To clarify the cause of age differences on selenite cataract formation in rats, mRNA expression of GPx1, MsrA and MsrB1, as well as GPx activity in Wistar rat lens at different ages were assayed, level of lipid peroxidation, extent of lens damage induced by sodium selenite and barricade function of blood-retinal barrier (BRB) were investigated.", "entity1": "GPx1", "entity2": "sodium selenite", "span1": [99, 103], "span2": [258, 273]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1441": {"label": 3, "data": {"text": "However, only MDMA reduced SERT density.", "entity1": "SERT", "entity2": "MDMA", "span1": [27, 31], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1176": {"label": 3, "data": {"text": "Patch-clamp analysis using inside-out recording configuration showed that mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 microM).", "entity1": "SUR1", "entity2": "mitiglinide", "span1": [106, 110], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"942": {"label": 3, "data": {"text": "Stereochemical studies established that PAM inactivation by 4-oxo-5-acetamido-6-(2-thienyl)-hex-2-enoic acid is stereospecific with respect to the moiety at the P(2) position, which is consistent with previous results with substrates and reversible inhibitors.", "entity1": "PAM", "entity2": "4-oxo-5-acetamido-6-(2-thienyl)-hex-2-enoic acid", "span1": [40, 43], "span2": [60, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6781": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-1", "entity2": "NS398", "span1": [268, 273], "span2": [141, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"249": {"label": 3, "data": {"text": "Both NS-398 and Dup-697 exhibited time-dependent inactivation of hCOX-2, as did indomethacin on both enzymes.", "entity1": "hCOX-2", "entity2": "NS-398", "span1": [65, 71], "span2": [5, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1635": {"label": 3, "data": {"text": "CONCLUSION: A long-term intake of ethanol solution down-regulates the phosphorylation of CREB in the nucleus accumbens, and those changes can be reversed by naloxone, which may be one kind of the molecular mechanisms associated with ethanol dependence.", "entity1": "CREB", "entity2": "ethanol", "span1": [89, 93], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6498": {"label": 5, "data": {"text": "The following alpha(2)-adrenoceptor antagonists were applied: BRL44408 (alpha(2A)-selective), ARC239 (alpha(2B)- and alpha(2C)-selective), and prazosin (alpha(2B)- and alpha(2C)-selective).", "entity1": "alpha(2B)", "entity2": "prazosin", "span1": [153, 162], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2563": {"label": 9, "data": {"text": "Neonatal quinpirole treatment produced a significant decrease in BDNF and ChAT in the frontal cortex that was unaffected by olanzapine treatment.", "entity1": "ChAT", "entity2": "olanzapine", "span1": [74, 78], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8779": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "Akt1", "entity2": "CAPE", "span1": [56, 60], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12904": {"label": 3, "data": {"text": "Collectively, our results suggest that H(2)S can inhibit NO production and NF-kappaB activation in LPS-stimulated macrophages through a mechanism that involves the action of HO-1/CO.", "entity1": "NF-kappaB", "entity2": "H(2)S", "span1": [75, 84], "span2": [39, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5615": {"label": 3, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "cisapride", "span1": [71, 75], "span2": [112, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3116": {"label": 8, "data": {"text": "First, addition of apolipoprotein A-I (apoA-I), a direct acceptor of the ATP-binding cassette transporter A1 (ABCA1)-secreted lipids, increased alpha-tocopherol secretion in a dose-dependent manner.", "entity1": "apolipoprotein A-I", "entity2": "alpha-tocopherol", "span1": [19, 37], "span2": [144, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2012": {"label": 1, "data": {"text": "Pranlukast-induced inhibition of IL-5 mRNA expression was noted in various cells, irrespective of their CysLTR1 mRNA expression status.", "entity1": "CysLTR1", "entity2": "Pranlukast", "span1": [104, 111], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7281": {"label": 3, "data": {"text": "Here, we report that the antifibrotic drug 5-methyl-1-phenyl-2-(1H)-pyridone (pirfenidone, PFD) elicits growth-inhibitory effects and reduces TGF-beta2 protein levels in human glioma cell lines.", "entity1": "TGF-beta2", "entity2": "pirfenidone", "span1": [142, 151], "span2": [78, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11264": {"label": 3, "data": {"text": "Cetrorelix also abolished the developmental rise of the gonadotropin beta subunit mRNAs during the two periods of the study.", "entity1": "gonadotropin beta", "entity2": "Cetrorelix", "span1": [56, 73], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4198": {"label": 3, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "Mcl-1", "entity2": "PTE", "span1": [111, 116], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"531": {"label": 8, "data": {"text": "Consistent with these results, the translocation of cPLA2 protein as well as the release of arachidonic acid, a principal product of phospholipase A2, was rapidly induced by the addition of C2-ceramide in a Rac-dependent manner.", "entity1": "phospholipase A2", "entity2": "arachidonic acid", "span1": [133, 149], "span2": [92, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12886": {"label": 1, "data": {"text": "This fundamental significance of NMDA receptor-related excitotoxicity is discussed in the context of the developing clinical success of Memantine, but moreover set into relation to various proteomic and genetic markers of said diseases.", "entity1": "NMDA receptor", "entity2": "Memantine", "span1": [33, 46], "span2": [136, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11187": {"label": 3, "data": {"text": "We conclude that felbamate exhibits modest selectivity for NMDA receptors composed of NR1a/NR2B subunits.", "entity1": "NR2B", "entity2": "felbamate", "span1": [91, 95], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6973": {"label": 1, "data": {"text": "Recently, a G-protein-coupled receptor, termed GPR109A (HM74A in humans, PUMA-G in mice), was described and shown to mediate the nicotinic acid-induced antilipolytic effects in adipocytes.", "entity1": "GPR109A", "entity2": "nicotinic acid", "span1": [47, 54], "span2": [129, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11807": {"label": 1, "data": {"text": "Effects of 2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine (PhIP) on histopathology, oxidative stress, and expression of c-fos, c-jun and p16 in rat stomachs.", "entity1": "p16", "entity2": "2-amino-1-methyl-6-phenylimidazo [4, 5-b] pyridine", "span1": [141, 144], "span2": [11, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3878": {"label": 3, "data": {"text": "Furthermore, we validated the inhibition of GSK-3\u03b2/NF-\u03baB signaling following cinobufagin treatment.", "entity1": "GSK-3\u03b2", "entity2": "cinobufagin", "span1": [44, 50], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10397": {"label": 9, "data": {"text": "Taken together, these findings support the view that (1) OFQ is the only ppOFQ peptide that binds to and activates the ORL1 receptor and (2) OFQ II(1-28) does not bind or stimulate [35S]-GTPgammaS binding in cells expressing the mu opioid receptor.", "entity1": "OFQ II(1-28)", "entity2": "[35S]-GTPgammaS", "span1": [141, 153], "span2": [181, 196]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5343": {"label": 2, "data": {"text": "These findings suggest that S1P activates the PI3K/Akt signaling pathway leading to the promotion of nuclear translocation of \u03b2-catenin in osteoblast-like cells, resulting in the upregulation of osteoptotegerin and osteoblast differentiation markers including alkaline phosphatase, probably relating to the inhibition of osteoclast formation and the mineralization, respectively.", "entity1": "PI3K", "entity2": "S1P", "span1": [46, 50], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2187": {"label": 7, "data": {"text": "Co-C bond activation in methylmalonyl-CoA mutase by stabilization of the post-homolysis product Co2+ cobalamin.", "entity1": "methylmalonyl-CoA mutase", "entity2": "Co2+", "span1": [24, 48], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6049": {"label": 9, "data": {"text": "Only strains of P. aeruginosa producing large amounts of beta-lactamase may be resistant to both ceftazidime and cefepime.", "entity1": "beta-lactamase", "entity2": "ceftazidime", "span1": [57, 71], "span2": [97, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11131": {"label": 1, "data": {"text": "Risperidone was equipotent to prazosin at alpha 1A-adrenoceptors in rat vas deferens and kidney.", "entity1": "alpha 1A-adrenoceptors", "entity2": "Risperidone", "span1": [42, 64], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15570": {"label": 3, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "Lamp 2A", "entity2": "puerarin", "span1": [252, 259], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6600": {"label": 4, "data": {"text": "Although only clozapine and ziprasidone are directly acting 5-HT(1A) agonists, WAY100635, a selective 5-HT(1A) antagonist, partially attenuates these atypical APD-induced increases in cortical DA release that may be due to combined 5-HT(2A) and D(2) blockade.", "entity1": "5-HT(1A)", "entity2": "ziprasidone", "span1": [60, 68], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11225": {"label": 1, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "SUR1", "entity2": "sulfonylureas", "span1": [104, 108], "span2": [44, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14720": {"label": 0, "data": {"text": "AF10 has mostly been studied in the context of the leukemic MLL-AF10 fusion protein, which lacks the N-terminal PHD fingers of AF10.", "entity1": "AF10", "entity2": "N", "span1": [127, 131], "span2": [101, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12858": {"label": 1, "data": {"text": "BACKGROUND AND AIMS: Thymidylate synthase (TS) is an important enzyme for DNA synthesis and the target for 5-fluorouracil (5-FU).", "entity1": "TS", "entity2": "5-FU", "span1": [43, 45], "span2": [123, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10721": {"label": 0, "data": {"text": "For both agonists, important binding domains were the extracellular N-terminus (=E1) and the extracellular loops E2 and E3 from the oxytocin receptor.", "entity1": "oxytocin receptor", "entity2": "N", "span1": [132, 149], "span2": [68, 69]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13055": {"label": 3, "data": {"text": "Late INa induced by the VGSC long QT mutant R1623Q was reduced by resveratrol and quercetin.", "entity1": "VGSC", "entity2": "quercetin", "span1": [24, 28], "span2": [82, 91]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9500": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "quinidine", "span1": [28, 42], "span2": [120, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5083": {"label": 3, "data": {"text": "FCEO significantly inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) by suppressing the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, respectively.", "entity1": "inducible nitric oxide synthase", "entity2": "NO", "span1": [116, 147], "span2": [43, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10595": {"label": 1, "data": {"text": "Even though its inability to shift between the trivalent and a divalent oxidation state precludes that gallium behaves as an iron analogue in every respect, it strongly interferes with cellular acquisition of iron from blood by competitive interaction with transferrin and transferrin receptor-mediated endocytosis.", "entity1": "transferrin", "entity2": "iron", "span1": [257, 268], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12844": {"label": 1, "data": {"text": "However, there were some significant differences among Captopril (30 mg/kg or 45 mg/kg), enalapril (20 mg/kg), and N-acetylcysteine particular in the activity of PON1 and ACE.", "entity1": "PON1", "entity2": "enalapril", "span1": [162, 166], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7420": {"label": 8, "data": {"text": "The accumulation of the post-D6D products of 22:5n-3, 24:6n-3 and DHA, in cell phospholipids was saturated at concentrations of >18 microM ALA. Supplementation of HepG2 cells with preformed DHA revealed that, although the accumulation of DHA in cell phospholipids approached saturation, the level of DHA in cell phospholipids was significantly greater compared with the accumulation of DHA from ALA, indicating that the accumulation of DHA from ALA was not limited by incorporation.", "entity1": "D6D", "entity2": "DHA", "span1": [29, 32], "span2": [66, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8785": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "FOXO1", "entity2": "CAPE", "span1": [122, 127], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5335": {"label": 3, "data": {"text": "No effects were observed when fenclozic acid was assessed for P450-dependent and P450-independent cytotoxicity to THLE cell lines, time-dependent inhibition of five major human cytochrome P450 enzymes, inhibition of the biliary efflux transporters BSEP and MRP2 or mitochondrial toxicity to THLE or HepG2 cells.", "entity1": "efflux transporters", "entity2": "fenclozic acid", "span1": [228, 247], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13765": {"label": 3, "data": {"text": "Here, we characterized the target profile of the dual SRC/ABL inhibitor bosutinib employing a two-tiered approach using chemical proteomics to identify natural binders in whole cell lysates of primary CML and K562 cells in parallel to in vitro kinase assays against a large recombinant kinase panel.", "entity1": "SRC", "entity2": "bosutinib", "span1": [54, 57], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6118": {"label": 3, "data": {"text": "Amezinium and debrisoquine are substrates of uptake1 and potent inhibitors of monoamine oxidase in perfused lungs of rats.", "entity1": "monoamine oxidase", "entity2": "Amezinium", "span1": [78, 95], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8813": {"label": 2, "data": {"text": "Activation of AMPK using AICAR resulted in STIM1 phosphorylation on serine residues and prevented PAR-1-induced Ca2+ entry.", "entity1": "AMPK", "entity2": "AICAR", "span1": [14, 18], "span2": [25, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7178": {"label": 3, "data": {"text": "In order to produce potent new leads for anticancer drugs, a new series of quinazoline analogs was designed to resemble methotrexate (MTX, 1) structure features and fitted with functional groups believed to enhance inhibition of mammalian DHFR activity.", "entity1": "mammalian DHFR", "entity2": "quinazoline", "span1": [229, 243], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9387": {"label": 1, "data": {"text": "The interactions of GYKI 52466 and cyclothiazide on AMPA receptor-mediated e.p.s.cs in area CA1 of hippocampal slices provide evidence that the decay time constant of these synaptic events are not governed by desensitization.", "entity1": "AMPA receptor", "entity2": "cyclothiazide", "span1": [52, 65], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13984": {"label": 0, "data": {"text": "PRINCIPAL FINDINGS: With the knowledge that all general anesthetics positively modulate GABA(A)-R-mediated inhibitory transmission, site-directed mutagenesis comparing sequences of GABA(A)-R subunits of varying sensitivity led to identification of amino acid residues in the transmembrane domain that are critical for the drug actions in vitro.", "entity1": "GABA(A)-R", "entity2": "amino acid", "span1": [88, 97], "span2": [248, 258]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13966": {"label": 2, "data": {"text": "Our findings suggest that R316C causes reduced association with and impaired release of NCoR, resulting in RTH predominantly at the pituitary level, and that slightly elevated serum TSH level with high dose of levothyroxine might be optimum for normal growth.", "entity1": "TSH", "entity2": "levothyroxine", "span1": [182, 185], "span2": [210, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10789": {"label": 2, "data": {"text": "Simvastatin, an HMG-CoA reductase inhibitor with mild inhibition of LFA-1, induced the production of interleukin (IL)-18, tumor necrosis factor (TNF)-alpha and interferon (IFN)-gamma in human peripheral blood mononuclear cells (PBMC).", "entity1": "interleukin (IL)-18", "entity2": "Simvastatin", "span1": [101, 120], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1032": {"label": 2, "data": {"text": "High p53 protein levels, but not genetic or functional p53 status, were associated with increased topotecan-induced DNA/topoisomerase I complex formation.", "entity1": "p53", "entity2": "topotecan", "span1": [5, 8], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10653": {"label": 3, "data": {"text": "Valdecoxib potently inhibits recombinant COX-2, with an IC(50) of 0.005 microM; this compares with IC values of 0.05 microM for celecoxib, 0.5 microM for rofecoxib, and 5 microM for etoricoxib.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [41, 46], "span2": [128, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14635": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "DCK", "entity2": "dFdC", "span1": [117, 120], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12580": {"label": 0, "data": {"text": "PC3 is a type I proinsulin-processing enzyme that initiates the sequential processing of proinsulin to insulin by cleaving the proinsulin molecule on the COOH-terminal side of the dibasic peptide, Arg31-Arg32, joining the B-chain and C-peptide.", "entity1": "proinsulin", "entity2": "COOH", "span1": [127, 137], "span2": [154, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14277": {"label": 1, "data": {"text": "Cytochrome b5 has shown to be an essential component in P450 3A4 catalyzed 5-hydroxyelzasonan formation and provides insights on the disconnect between human liver microsomes data and that of rCYP.", "entity1": "Cytochrome b5", "entity2": "5-hydroxyelzasonan", "span1": [0, 13], "span2": [75, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11156": {"label": 1, "data": {"text": "LY 344864 appears to attenuate c-fos-like immunoreactivity via 5-HT1F receptors, while sumatriptan acts via 5-HT1B receptors.", "entity1": "5-HT1B", "entity2": "sumatriptan", "span1": [108, 114], "span2": [87, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3296": {"label": 3, "data": {"text": "A phase III randomized placebo-controlled trial has examined the impact of everolimus in patients with clear cell renal cancers and progressive disease on or within 6 months of the VEGFR tyrosine kinase inhibitors sunitinib and/or sorafenib.", "entity1": "tyrosine kinase", "entity2": "sorafenib", "span1": [187, 202], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9659": {"label": 1, "data": {"text": "FMLP/CB-stimulated translocation of cPLA2 to the nuclear envelope assessed by specific immunohistochemical staining also was blocked by FP.", "entity1": "cPLA2", "entity2": "FMLP", "span1": [36, 41], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6524": {"label": 5, "data": {"text": "Aliskiren has the potential to become the first orally active renin inhibitor that provides a true alternative to ACE-inhibitors and Ang II receptor antagonists in therapy for hypertension and other cardiovascular and renal diseases.", "entity1": "Ang II receptor", "entity2": "Aliskiren", "span1": [133, 148], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15879": {"label": 2, "data": {"text": "Additionally, treatment with glucose/iron showed a higher HO activity.", "entity1": "HO", "entity2": "iron", "span1": [58, 60], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4426": {"label": 1, "data": {"text": "The keto and phenolic -OH are major factors that are prominently involved in interaction with COX-2 active site.", "entity1": "COX-2", "entity2": "keto", "span1": [94, 99], "span2": [4, 8]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9238": {"label": 3, "data": {"text": "Triclosan also inhibited 5-lipoxygenase with an IC-50 of 43 microM.", "entity1": "5-lipoxygenase", "entity2": "Triclosan", "span1": [25, 39], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14750": {"label": 3, "data": {"text": "Together, these data suggest that arsenic degrades \u0394Np63 protein at least in part via Pirh2-dependent proteolysis and that inhibition of \u0394Np63 expression facilitates tumor cells to arsenic-induced death.", "entity1": "\u0394Np63", "entity2": "arsenic", "span1": [137, 142], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12035": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "EO", "entity2": "EOI", "span1": [48, 50], "span2": [155, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3341": {"label": 1, "data": {"text": "The affinities of dfbp and dfbp-o for the regulatory domain of cTnC were measured in the absence and presence of cTnI by NMR spectroscopy, and dfbp-o was found to bind more strongly than dfbp.", "entity1": "cTnC", "entity2": "dfbp-o", "span1": [63, 67], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1667": {"label": 1, "data": {"text": "In membranes from HEK293 cells transfected with alpha2-receptors, etomidate inhibited binding of the alpha2-antagonist, [3H]RX821002, with higher potency from alpha2B- and alpha2C-receptors than from alpha2A-receptors (Ki alpha2A 208 microm, alpha2B 26 microm, alpha2C 56 microm).", "entity1": "alpha2-receptors", "entity2": "etomidate", "span1": [48, 64], "span2": [66, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8126": {"label": 3, "data": {"text": "We used nutlin-3, a well-known disruptor of p53-Mdm2 interaction, to validate the specificity of the assay.", "entity1": "Mdm2", "entity2": "nutlin-3", "span1": [48, 52], "span2": [8, 16]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15155": {"label": 1, "data": {"text": "A dominant negative PKA (DNPKA) reduced GnRH-stimulated pCREB and markedly decreased GnRH stimulation of FSH\u03b2 mRNA and FSH\u03b2LUC activity, but had little effect on LH\u03b2LUC activity, indicating relative specificity of this pathway.", "entity1": "LH\u03b2", "entity2": "GnRH", "span1": [162, 165], "span2": [85, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11734": {"label": 0, "data": {"text": "The 3D-structure of HmTx consists of three conserved alpha-helices: h1 (Lys24-His34), h2 (Cys59-Asp71), and h3 (Ala80-Phe89).", "entity1": "HmTx", "entity2": "Phe", "span1": [20, 24], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15853": {"label": 8, "data": {"text": "To confirm the role of each transporter, we analyzed HEK293 cells stably expressing human ABCA1 or ABCG1; we clearly observed 24-OHC efflux in the presence of HDL, whereas efflux in the presence of apolipoprotein A-I was marginal.", "entity1": "ABCG1", "entity2": "24-OHC", "span1": [99, 104], "span2": [126, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1930": {"label": 8, "data": {"text": "The M564G mutated CrAT showed higher activity toward longer chain acyl-CoAs: activity toward myristoyl-CoA was 1250-fold higher than that of the wild-type CrAT, and lower activity toward its natural substrate, acetyl-CoA.", "entity1": "CrAT", "entity2": "acyl-CoAs", "span1": [18, 22], "span2": [66, 75]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14351": {"label": 3, "data": {"text": "mRNA levels of receptor activator of nuclear factor kappa-B (RANK), its ligand RANKL, tumor necrosis factor alpha (TNF-\u03b1) and RANKL/osteoprotegerin (OPG) ratio were diminished in the periodontium of CCL3(-/-) mice and in the group treated with Met-RANTES.", "entity1": "tumor necrosis factor alpha", "entity2": "Met", "span1": [86, 113], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5993": {"label": 2, "data": {"text": "The activation of human [Glu1]plasminogen [( Glu1]Pg) by human recombinant (rec) two-chain tissue plasminogen activator (t-PA) is inhibited by Cl-, at physiological concentrations, and stimulated by epsilon-aminocaproic acid (EACA), as well as fibrin(ogen).", "entity1": "tissue plasminogen activator", "entity2": "EACA", "span1": [91, 119], "span2": [226, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3334": {"label": 3, "data": {"text": "Etoposide (VP-16) is a topoisomerase-II (topo II) inhibitor chemotherapeutic agent.", "entity1": "topo II", "entity2": "VP-16", "span1": [41, 48], "span2": [11, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1525": {"label": 3, "data": {"text": "), which also block PP1, and calyculin-A (0.1 fg/mouse-1 ng/mouse, i.c.v. ), which inhibits equally both PP1 and PP2A, did not modify the morphine-induced antinociception.", "entity1": "PP1", "entity2": "calyculin-A", "span1": [105, 108], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10039": {"label": 2, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "acyl-coenzyme A (CoA) oxidase", "entity2": "GW2331", "span1": [45, 74], "span2": [16, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6215": {"label": 1, "data": {"text": "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan.", "entity1": "sigma-1 receptor", "entity2": "dimemorfan", "span1": [25, 41], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5524": {"label": 4, "data": {"text": "Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.", "entity1": "beta 2AR", "entity2": "Salmeterol", "span1": [55, 63], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10854": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "PDGFRA", "entity2": "Glivec", "span1": [124, 130], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6536": {"label": 3, "data": {"text": "A recent study showed that anastrozole, an aromatase inhibitor, is as effective or even superior to tamoxifen when used as a first-line therapy.", "entity1": "aromatase", "entity2": "anastrozole", "span1": [43, 52], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6961": {"label": 5, "data": {"text": "The aim of this study was to determine if macaque represents a suitable species for the pre-clinical evaluation of novel CCR5 antagonists, such as maraviroc (UK-427,857).", "entity1": "CCR5", "entity2": "maraviroc", "span1": [121, 125], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6543": {"label": 4, "data": {"text": "Probes were perfused with artificial cerebrospinal fluid containing nicotine, the specific alpha(4)beta(2*) nAChR agonist metanicotine, or nicotine plus nAChR antagonists and norepinephrine measured in the microdialysates.", "entity1": "alpha(4)beta(2*) nAChR", "entity2": "nicotine", "span1": [91, 113], "span2": [139, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15216": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "TNF- \u03b1", "entity2": "methanol", "span1": [365, 371], "span2": [59, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5196": {"label": 3, "data": {"text": "High glucose (HG) induces apoptosis of podocytes, inhibits AMPK activation, inactivates tuberin and activates mTOR.", "entity1": "tuberin", "entity2": "glucose", "span1": [88, 95], "span2": [5, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12131": {"label": 3, "data": {"text": "Initial in vitro studies utilizing HEP-G2 liver cells revealed that addition of eicosapentaenoic acid (EPA) blocked Delta-5-desaturase activity, the terminal enzymatic step in AA synthesis.", "entity1": "Delta-5-desaturase", "entity2": "eicosapentaenoic acid", "span1": [116, 134], "span2": [80, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14682": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "2D6", "entity2": "GSK1292263", "span1": [111, 114], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13928": {"label": 2, "data": {"text": "In pig parathyroid cells, paricalcitol and the active form of doxercalciferol induced VDR translocation from the cytoplasm into the nucleus, suppressed PTH mRNA expression and inhibited cell proliferation in a similar manner, although paricalcitol induced the expression of CaSR mRNA more effectively.", "entity1": "CaSR", "entity2": "paricalcitol", "span1": [274, 278], "span2": [235, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14128": {"label": 1, "data": {"text": "Celastrol highlights the therapeutic potential of agents targeting TAK1 as a key node in this pro-oncogenic TGF-\u03b2-NF-\u03baB signal pathway.", "entity1": "TGF-\u03b2", "entity2": "Celastrol", "span1": [108, 113], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9217": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "EGF", "entity2": "TFP", "span1": [261, 264], "span2": [159, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8284": {"label": 3, "data": {"text": "Moreover, the D2R inhibitor raclopride blocked the increase of both GDNF and Zif268 expression following potassium-evoked dopamine release in SH-SY5Y cells.", "entity1": "Zif268", "entity2": "raclopride", "span1": [77, 83], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9314": {"label": 3, "data": {"text": "The goal of the present study was to compare the effects of three potent reference renin inhibitors (remikiren, CGP 38560A, and enalkiren) in sodium-depleted normotensive squirrel monkeys.", "entity1": "renin", "entity2": "remikiren", "span1": [83, 88], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5383": {"label": 3, "data": {"text": "MNU-induced lesions presented markers indicative of an aggressive phenotype: lack of basal cells, rupture of the smooth muscle cell layer, loss of E-cadherin, and high MGMT staining.", "entity1": "E-cadherin", "entity2": "MNU", "span1": [147, 157], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4230": {"label": 2, "data": {"text": "The current U.S. military and civilian oxime countermeasure, 2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride (2-PAM), is under consideration for replacement with a more effective acetylcholinesterase reactivator, 1,1'-methylenebis{4-hydroxyiminomethyl}pyridinium dimethanesulfonate (MMB-4).", "entity1": "acetylcholinesterase", "entity2": "1,1'-methylenebis{4-hydroxyiminomethyl}pyridinium dimethanesulfonate", "span1": [187, 207], "span2": [221, 289]}, "weak_labels": [-1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5743": {"label": 1, "data": {"text": "Molecular docking studies suggested that SB has a good affinity towards vinblastine-binding site on \u03b2-tubulin subunit.", "entity1": "\u03b2-tubulin", "entity2": "vinblastine", "span1": [100, 109], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5333": {"label": 9, "data": {"text": "No effects were observed when fenclozic acid was assessed for P450-dependent and P450-independent cytotoxicity to THLE cell lines, time-dependent inhibition of five major human cytochrome P450 enzymes, inhibition of the biliary efflux transporters BSEP and MRP2 or mitochondrial toxicity to THLE or HepG2 cells.", "entity1": "P450", "entity2": "fenclozic acid", "span1": [81, 85], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3170": {"label": 1, "data": {"text": "Tinzaparin binds to VLA-4 with affinity in the low micromolar range (4.61 x 10(-6) M), which clearly indicates specific molecular recognition.", "entity1": "VLA-4", "entity2": "Tinzaparin", "span1": [20, 25], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14405": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile", "span1": [320, 324], "span2": [61, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3026": {"label": 1, "data": {"text": "The microtubule binding affinities of a series of synthetic taxanes have been measured with the aims of dissecting individual group contributions and obtaining a rationale for the design of novel compounds with the ability to overcome drug resistance.", "entity1": "microtubule", "entity2": "taxanes", "span1": [4, 15], "span2": [60, 67]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10109": {"label": 8, "data": {"text": "Acute and chronic PLZ administration increase brain GABA levels, an effect due, at least in part, to an inhibition of the activity of the GABA metabolizing enzyme, GABA transaminase (GABA-T).", "entity1": "GABA transaminase", "entity2": "GABA", "span1": [164, 181], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1180": {"label": 3, "data": {"text": "Nateglinide inhibits Kir6.2/SUR1 and Kir6.2/SUR2B channels at 100 nM, and inhibits Kir6.2/SUR2A channels at high concentrations (1 microM).", "entity1": "SUR2B", "entity2": "Nateglinide", "span1": [44, 49], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6612": {"label": 5, "data": {"text": "The effects of histamine H1-receptor antagonists, promethazine and homochlorcyclizine, both of which are inhibitors of CYP2D6, on the steady-state plasma concentrations (Css) of haloperidol and reduced haloperidol were studied in 23 schizophrenic inpatients receiving haloperidol, 12 to 36 mg/d, for 2 to 29 weeks.", "entity1": "histamine H1-receptor", "entity2": "homochlorcyclizine", "span1": [15, 36], "span2": [67, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"725": {"label": 2, "data": {"text": "Ribonucleotide reductase activity was found to be strongly increased in the gemcitabine-selected line and purine nucleoside phosphorylase was increased in the 2-chlorodeoxyadenosine-selected line.", "entity1": "purine nucleoside phosphorylase", "entity2": "2-chlorodeoxyadenosine", "span1": [106, 137], "span2": [159, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2898": {"label": 5, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1D)-adrenoceptor", "entity2": "8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride", "span1": [235, 257], "span2": [128, 222]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15982": {"label": 1, "data": {"text": "Immunoregulatory effects of Glycyrrhizic acid exerts anti-asthmatic effects via modulation of Th1/Th2 cytokines and enhancement of CD4(+)CD25(+)Foxp3(+) regulatory T cells in ovalbumin-sensitized mice.", "entity1": "ovalbumin", "entity2": "Glycyrrhizic acid", "span1": [175, 184], "span2": [28, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"512": {"label": 3, "data": {"text": "These actions are consistent with a pre-junctional inhibition of neuropeptide release from perivascular afferents of the trigeminal nerve, as confirmed by independent studies showing that zolmitriptan blocks elevations of calcitonin-gene-related peptide in jugular venous blood during electrical stimulation of the trigeminal ganglion.", "entity1": "calcitonin-gene-related peptide", "entity2": "zolmitriptan", "span1": [222, 253], "span2": [188, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7063": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARbeta", "entity2": "tamibarotene", "span1": [52, 59], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"781": {"label": 9, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "COX", "entity2": "sulindac sulfone", "span1": [188, 191], "span2": [120, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12661": {"label": 1, "data": {"text": "However, inter-helical distances calculated and determined by EPR for PGHS-2 complexed with arachidonic acid, flurbiprofen, and SC-58125 were in close agreement with those obtained from the cognate crystal structures.", "entity1": "PGHS-2", "entity2": "flurbiprofen", "span1": [70, 76], "span2": [110, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5014": {"label": 8, "data": {"text": "Sixteen of 34 CGPs inhibited MRP1-mediated E217\u03b2G uptake by >50% (IC50's 0.7-7.6 \u03bcM).", "entity1": "MRP1", "entity2": "E217\u03b2G", "span1": [29, 33], "span2": [43, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3305": {"label": 1, "data": {"text": "Predicting cardiomyopathic phenotypes by altering Ca2+ affinity of cardiac troponin C.", "entity1": "cardiac troponin C", "entity2": "Ca2+", "span1": [67, 85], "span2": [50, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13619": {"label": 1, "data": {"text": "One is that the binding of retinoids to nuclear retinoic acid receptors (RARs) does not match their therapeutic efficacy: acitretin activates the three receptor subtypes, RAR-alpha, -beta and -gamma, without measurable receptor binding, whereas tazarotene preferentially binds to and activates RAR-beta and -gamma in preference to RAR-alpha.", "entity1": "RARs", "entity2": "retinoids", "span1": [73, 77], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13074": {"label": 3, "data": {"text": "Based on selective nucleoside protection, TS was found to be the primary pemetrexed target in both cell lines with GARFT inhibition requiring 20- to 30-fold higher pemetrexed concentrations.", "entity1": "GARFT", "entity2": "pemetrexed", "span1": [115, 120], "span2": [164, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11302": {"label": 3, "data": {"text": "Topiramate also partially depressed predominantly AMPA-receptor-mediated EPSCs, but with lower efficacy.", "entity1": "AMPA-receptor", "entity2": "Topiramate", "span1": [50, 63], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7301": {"label": 8, "data": {"text": "UNLABELLED: Bile acid-coenzyme A:amino acid N-acyltransferase (BAAT) is the sole enzyme responsible for conjugation of primary and secondary bile acids to taurine and glycine.", "entity1": "BAAT", "entity2": "bile acids", "span1": [63, 67], "span2": [141, 151]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13010": {"label": 2, "data": {"text": "It has been known for decades that lithium chloride (LiCl) leads to D-myo-inositol 1-phosphate accumulation on GPCR activation by inhibiting inositol monophosphatase, the final enzyme of the IP3 metabolic cascade.", "entity1": "GPCR", "entity2": "lithium chloride", "span1": [111, 115], "span2": [35, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10421": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "retinoid receptors", "entity2": "tazarotenic acid", "span1": [113, 131], "span2": [61, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"469": {"label": 5, "data": {"text": "(+/-)-Tamsulosin effectively antagonized the positive inotropic effect of phenylephrine even after inactivation of alpha 1B-adrenoceptors by treatment with chlorethylclonidine, which is an indication that the (+/-)-tamsulosin-sensitive subtype belongs to a class resistant to chlorethylclonidine.", "entity1": "alpha 1B-adrenoceptors", "entity2": "(+/-)-Tamsulosin", "span1": [115, 137], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"406": {"label": 3, "data": {"text": "Previous studies by this research team proved that vasodilating prostaglandins (PGs) E1, E2 and I2 inhibit carbonic anhydrase (CA) in vitro and in vivo, which suggested involvement of CA in gastric acid secretion inhibition and the increase of gastric mucosa blood flow produced by this group of PGs.", "entity1": "CA", "entity2": "prostaglandins", "span1": [127, 129], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8929": {"label": 5, "data": {"text": "The mechanism(s) responsible for arterial vasodilation observed following acute administration of racemic carvedilol, a novel vasodilator/beta adrenoceptor antagonist, has been investigated in rats.", "entity1": "beta adrenoceptor", "entity2": "racemic carvedilol", "span1": [138, 155], "span2": [98, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13969": {"label": 3, "data": {"text": "METHODS: We conducted a case-control study to measure the association between selective cox-2 inhibitors, particularly celecoxib, rofecoxib, valdecoxib and non-specific NSAID subgroups, and breast cancer risk.", "entity1": "cox-2", "entity2": "celecoxib", "span1": [88, 93], "span2": [119, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8746": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "tamoxifen", "span1": [18, 25], "span2": [157, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6155": {"label": 1, "data": {"text": "For example, it is clear that the closed conformation of the regulatory N-terminal domain in Ca2+-bound cardiac troponin C (cTnC) presents a much different binding surface for Ca2+-sensitizing compounds than previously thought.", "entity1": "cardiac troponin C", "entity2": "Ca2+", "span1": [104, 122], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5930": {"label": 3, "data": {"text": "It is proposed that two molecules of estramustine phosphate interact with each of the three tubulin-binding sites of MAP2 and inhibit the MAP2:tubulin interaction by neutralising two highly conserved basic residues.", "entity1": "tubulin", "entity2": "estramustine phosphate", "span1": [143, 150], "span2": [37, 59]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15986": {"label": 3, "data": {"text": "Enhanced beta cell function and anti-inflammatory effect after chronic treatment with the dipeptidyl peptidase-4 inhibitor vildagliptin in an advanced-aged diet-induced obesity mouse model.", "entity1": "dipeptidyl peptidase-4", "entity2": "vildagliptin", "span1": [90, 112], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14171": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "IL-5", "entity2": "chalcones", "span1": [104, 108], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4283": {"label": 3, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "AMPK", "entity2": "compound C", "span1": [12, 16], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3128": {"label": 1, "data": {"text": "The neuronal vesicular monoamine transporter (VMAT2) is the target molecule of action of some psychostimulants, such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA).", "entity1": "VMAT2", "entity2": "methamphetamine", "span1": [46, 51], "span2": [120, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13575": {"label": 3, "data": {"text": "The next large phase III adjuvant trial for this subset of breast cancer is an international collaboration designed to evaluate the added or alternative benefit of an oral tyrosine kinase inhibitor targeting HER2/neu as well as the epidermal growth factor receptor (EGFR), lapatinib.", "entity1": "epidermal growth factor receptor", "entity2": "lapatinib", "span1": [232, 264], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5459": {"label": 3, "data": {"text": "Considerable attention has focused on the antitumor effect of histone deacetylase inhibitor (Trichostatin A, TSA) as well as the coding gene expression-induced apoptosis of cancer cells.", "entity1": "histone deacetylase", "entity2": "Trichostatin A", "span1": [62, 81], "span2": [93, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"465": {"label": 4, "data": {"text": "These results indicate that the positive inotropic effect, mediated via (+/-)-tamsulosin- and oxymetazoline-sensitive subtype of alpha 1-adrenoceptors, is exerted by a subcellular mechanism that is independent of the accumulation of inositol phosphates.", "entity1": "alpha 1-adrenoceptors", "entity2": "oxymetazoline", "span1": [129, 150], "span2": [94, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"188": {"label": 1, "data": {"text": "Readdition of a small quantity of dialyzed serum to cytosol preparations yielded a profile of steroid binding similar to that of the kidney mineralocorticoid receptor (aldosterone greater than desoxycorticosterone greater than corticosterone).", "entity1": "mineralocorticoid receptor", "entity2": "steroid", "span1": [140, 166], "span2": [94, 101]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9727": {"label": 0, "data": {"text": "Substitutions for Ile(183)-Val(191) and Ser(195)-Ile(197) at the N terminus and for Ser(258)-Ser(264) at the C terminus of the A3 domain markedly decreased factor XI coagulant activity.", "entity1": "A3 domain", "entity2": "N", "span1": [127, 136], "span2": [65, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12369": {"label": 0, "data": {"text": "Methylation of histone H3 on lysine 4 by the lysine methyltransferase SET1 protein is needed for normal clock gene expression.", "entity1": "histone H3", "entity2": "lysine", "span1": [15, 25], "span2": [29, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14865": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "PKC", "entity2": "bisindolylmaleimide", "span1": [92, 95], "span2": [115, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10678": {"label": 3, "data": {"text": "Oxytocin antagonist (OTA), TT-235, was developed by our group and shown to inhibit either spontaneous or oxytocin-induced uterine contractions in primates.", "entity1": "oxytocin", "entity2": "TT-235", "span1": [105, 113], "span2": [27, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3490": {"label": 2, "data": {"text": "In the CCl4 hepatotoxicity model, pre-treatment with PSM or silymarin resulted in significantly increased activities of ethylmorphine-N-demethylase and aniline 4-hydroxylase activity and cytochrome P450, compared to the CCl4 only group.", "entity1": "cytochrome P450", "entity2": "silymarin", "span1": [187, 202], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3798": {"label": 3, "data": {"text": "[-]-Huperzine A ([-]-Hup A), is a naturally occurring potent reversible AChE inhibitor that penetrates the blood-brain barrier.", "entity1": "AChE", "entity2": "[-]-Hup A", "span1": [72, 76], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12654": {"label": 1, "data": {"text": "This study shows that aspirin and sodium salicylate, its major blood metabolite, reverse contractile actions of endothelin-1 (ET-1) in isolated rat aorta and human mammary arteries.", "entity1": "ET-1", "entity2": "sodium salicylate", "span1": [126, 130], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11615": {"label": 8, "data": {"text": "The alpha class human GSTA4-4 enzyme (hGSTA4-4) has a particularly high catalytic efficiency toward 4-HNE conjugation.", "entity1": "human GSTA4-4", "entity2": "4-HNE", "span1": [16, 29], "span2": [100, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10362": {"label": 2, "data": {"text": "GW660511X and omapatrilat increased the production of both BrBK1-8 and Br-Phe5 but not that of BrBK4-8 and BrBK2-8.", "entity1": "Br-Phe5", "entity2": "omapatrilat", "span1": [71, 78], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"9554": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "betaAR", "entity2": "cAMP", "span1": [17, 23], "span2": [204, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9319": {"label": 3, "data": {"text": "One possible explanation is that, in our model, remikiren in contrast to CGP 38560A and enalkiren is able to inhibit renin in a functionally important extraplasmatic compartment.", "entity1": "renin", "entity2": "enalkiren", "span1": [117, 122], "span2": [88, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13876": {"label": 2, "data": {"text": "Ibuprofen activates PPARgamma in neuron-like PC12 and B104 cells.", "entity1": "PPARgamma", "entity2": "Ibuprofen", "span1": [20, 29], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6346": {"label": 5, "data": {"text": "Losartan was the first, but by no means remained the only, AT1 receptor antagonist.", "entity1": "AT1", "entity2": "Losartan", "span1": [59, 62], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15010": {"label": 1, "data": {"text": "Involvement of Src and the actin cytoskeleton in the antitumorigenic action of adenosine dialdehyde.", "entity1": "Src", "entity2": "adenosine dialdehyde", "span1": [15, 18], "span2": [79, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10475": {"label": 1, "data": {"text": "BACKGROUND: The norepinephrine transporter (NET) is a high-affinity transporter for catecholamines.", "entity1": "NET", "entity2": "catecholamines", "span1": [44, 47], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1517": {"label": 9, "data": {"text": "However, L-nor-okadaone (0.001 pg/mouse-1 ng/mouse, i.c.v. ), an analogue of okadaic acid lacking activity against protein phosphatases, did not affect the antinociceptive effect of morphine.", "entity1": "protein phosphatases", "entity2": "L-nor-okadaone", "span1": [115, 135], "span2": [9, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13365": {"label": 2, "data": {"text": "Various genes controlled by estrogen, including X-inactive-specific transcript, anterior gradient-2, trefoil factor-1, CRP-ductin, ghrelin, and small proline-rich protein-2A, were dramatically over-expressed.", "entity1": "X-inactive-specific transcript", "entity2": "estrogen", "span1": [48, 78], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3998": {"label": 0, "data": {"text": "Dabrafenib is a BRAF (gene encoding serine/threonine-protein kinase B-Raf) inhibitor that has been developed to selectively target the valine 600 to glutamic acid substitution (BRAF(V600E)), which is commonly found in metastatic melanoma.", "entity1": "BRAF", "entity2": "valine", "span1": [177, 181], "span2": [135, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12495": {"label": 8, "data": {"text": "Recent literature shows that Brassica vegetables (Cruciferae) possess therapeutic effects particularly ascribed due to their content in glucosinolates, which upon myrosinase hydrolysis release the corresponding isothiocyanates.", "entity1": "myrosinase", "entity2": "isothiocyanates", "span1": [163, 173], "span2": [211, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8246": {"label": 5, "data": {"text": "PURPOSE: To characterise further the previously observed cytochrome P450 3A4 (CYP3A4) interaction of the dual orexin receptor antagonist almorexant.", "entity1": "orexin receptor", "entity2": "almorexant", "span1": [110, 125], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11831": {"label": 1, "data": {"text": "However, NCFP provides greater mGlu5 subtype selectivity than does CPPHA, making it more suitable for studies of effects on mGlu5 in CNS preparations.", "entity1": "mGlu5", "entity2": "NCFP", "span1": [31, 36], "span2": [9, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7351": {"label": 1, "data": {"text": "Reticulated platelets and uninhibited COX-1 and COX-2 decrease the antiplatelet effects of aspirin.", "entity1": "COX-2", "entity2": "aspirin", "span1": [48, 53], "span2": [91, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6240": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "human 5-HT1B", "entity2": "Eletriptan", "span1": [101, 113], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3385": {"label": 6, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "GABA(A)R", "entity2": "ethanol", "span1": [24, 32], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4951": {"label": 1, "data": {"text": "In this study, we have demonstrated that fisetin prevents diet-induced obesity through regulation of the signaling of mammalian target of rapamycin complex 1 (mTORC1), a central mediator of cellular growth, cellular proliferation and lipid biosynthesis.", "entity1": "mammalian target of rapamycin complex 1", "entity2": "fisetin", "span1": [118, 157], "span2": [41, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15508": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "peroxidase", "entity2": "cysteines", "span1": [188, 198], "span2": [90, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1433": {"label": 3, "data": {"text": "They included the COX-1 inhibitor indomethacin; the COX-2 inhibitor NS-398; the mixed COX-1/COX-2 inhibitor ibuprofen; the nitric oxide (NO) derivatives of indomethacin, ibuprofen and flurbiprofen; the 5-LOX inhibitor REV 5901; and the 5-LOX activating protein (FLAP) inhibitor MK-886.", "entity1": "COX-2", "entity2": "ibuprofen", "span1": [92, 97], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7311": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT2", "entity2": "alanine", "span1": [235, 240], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13768": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "VEGF receptor", "entity2": "SU 11248", "span1": [233, 246], "span2": [202, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9583": {"label": 1, "data": {"text": "Both carbetocin, carbetocin metabolite I and carbetocin metabolite II displayed binding affinities to the myometrial oxytocin receptor of a similar magnitude as oxytocin.", "entity1": "oxytocin receptor", "entity2": "oxytocin", "span1": [117, 134], "span2": [161, 169]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13340": {"label": 2, "data": {"text": "In addition, activation of protein kinase C and increases in intracellular cAMP also enhance cholinergic activity in T cells, and lymphocyte function associated antigen-1 (LFA-1; CD11a/CD18) is an important mediator of leukocyte migration and T cell activation.", "entity1": "LFA-1", "entity2": "cAMP", "span1": [172, 177], "span2": [75, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15101": {"label": 3, "data": {"text": "Ceftazidime-avibactam: a novel cephalosporin/\u03b2-lactamase inhibitor combination.", "entity1": "\u03b2-lactamase", "entity2": "avibactam", "span1": [45, 56], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8853": {"label": 1, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "AhR", "entity2": "TCDD", "span1": [61, 64], "span2": [104, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15850": {"label": 8, "data": {"text": "Because 24(S)-hydroxycholesterol (24-OHC), produced by 24-hydroxylase, induces apoptosis of neuronal cells, it is vital to eliminate it rapidly from cells.", "entity1": "24-hydroxylase", "entity2": "24(S)-hydroxycholesterol", "span1": [55, 69], "span2": [8, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12963": {"label": 3, "data": {"text": "Our purpose was to test the impact of single and/or combined treatment with the AT(1)-receptor blocker candesartan and the HMG-CoA reductase inhibitor rosuvastatin on infarct size and neuroscore in transient cerebral ischemia in rats.", "entity1": "HMG-CoA reductase", "entity2": "rosuvastatin", "span1": [123, 140], "span2": [151, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3896": {"label": 2, "data": {"text": "In contrast to parenteral delivery of rBChE, which currently requires posttranslational modification for good plasma stability, an unmodified aer-rBChE pretreatment given 1-40h prior to >1 LD50 of aer-paraoxon (Px) was able to prevent inhibition of circulating cholinesterase in a dose-dependent manner.", "entity1": "cholinesterase", "entity2": "paraoxon", "span1": [261, 275], "span2": [201, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10926": {"label": 3, "data": {"text": "Using [(3)H]glucosamine-labeled gastric mucosal cells, we show that stimulatory effect of beta-adrenergic agonist, isoproterenol, on mucin secretion was inhibited by EGFR kinase inhibitor, PD153035, as well as wortmannin, a specific inhibitor of PI3K.", "entity1": "EGFR", "entity2": "PD153035", "span1": [166, 170], "span2": [189, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2978": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "H613A", "entity2": "tadalafil", "span1": [120, 125], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9042": {"label": 5, "data": {"text": "UNLABELLED: Bevantolol is a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension.", "entity1": "beta-1 adrenoceptor", "entity2": "Bevantolol", "span1": [28, 47], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14241": {"label": 2, "data": {"text": "Verrucarin A sensitizes TRAIL-induced apoptosis via the upregulation of DR5 in an eIF2\u03b1/CHOP-dependent manner.", "entity1": "eIF2\u03b1", "entity2": "Verrucarin A", "span1": [82, 87], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10176": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "human organic anion transporting polypeptide C", "entity2": "rifamycin SV", "span1": [104, 150], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3107": {"label": 3, "data": {"text": "Tolvaptan is a selective arginine vasopressin (AVP) V(2) receptor blocker used to induce free water diuresis in the treatment of euvolemic or hypervolemic hyponatremia.", "entity1": "arginine vasopressin (AVP) V(2) receptor", "entity2": "Tolvaptan", "span1": [25, 65], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3495": {"label": 3, "data": {"text": "A significant decrease of aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase (LDH) activities and glutathione (GSH) levels and an increase of malondialdehyde (MDA) quantity was observed after CCl4 and PC administration alone.", "entity1": "alanine aminotransferase", "entity2": "CCl4", "span1": [54, 78], "span2": [217, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12825": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "PNPO", "entity2": "pyridoxal 5'-phosphate", "span1": [156, 160], "span2": [45, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13581": {"label": 5, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "NMDA receptor", "entity2": "D-(-)-2-amino-5-phosphonopentanoic acid", "span1": [188, 201], "span2": [125, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5182": {"label": 1, "data": {"text": "Dioscin-induced autophagy mitigates cell apoptosis through modulation of PI3K/Akt and ERK and JNK signaling pathways in human lung cancer cell lines.", "entity1": "ERK", "entity2": "Dioscin", "span1": [86, 89], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9306": {"label": 3, "data": {"text": "However, their inhibitory effect was markedly reduced if clots were formed in the presence of t-PA and then exposed to either of the lysine analogues.", "entity1": "t-PA", "entity2": "lysine", "span1": [94, 98], "span2": [133, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14602": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Lys27Gln", "entity2": "Ara-C", "span1": [39, 47], "span2": [222, 227]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15181": {"label": 2, "data": {"text": "Sophocarpine alleviates hepatocyte steatosis through activating AMPK signaling pathway.", "entity1": "AMPK", "entity2": "Sophocarpine", "span1": [64, 68], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7218": {"label": 2, "data": {"text": "Cd rapidly increased c-jun, c-fos and PDGFA expression.", "entity1": "PDGFA", "entity2": "Cd", "span1": [38, 43], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12407": {"label": 3, "data": {"text": "In conclusion, BPA has adverse effects on phosphorylation of Akt, GLUT4 translocation and (14)C-glucose oxidation.", "entity1": "Akt", "entity2": "BPA", "span1": [61, 64], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4839": {"label": 9, "data": {"text": "Cucurbitacin I also failed to affect the activation of P-Rex1 by heregulin.", "entity1": "heregulin", "entity2": "Cucurbitacin I", "span1": [65, 74], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14873": {"label": 1, "data": {"text": "One of these compounds is eicosanoyl-5-hydroxytryptamide (EHT), which ameliorates the phenotype of \u03b1-synuclein transgenic mice associated with decreased protein aggregation and phosphorylation, improved neuronal integrity and reduced neuroinflammation.", "entity1": "\u03b1-synuclein", "entity2": "EHT", "span1": [99, 110], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3810": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Sar", "span1": [148, 153], "span2": [44, 47]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4706": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "TCDD", "span1": [123, 129], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"81": {"label": 1, "data": {"text": "The high-affinity binding of L-noradrenaline to phenylalanine hydroxylase, as studied by equilibrium microdialysis (anaerobically) and ultrafiltration (aerobically), shows positive cooperativity (h = 1.9); at pH 7.2 and 20 degrees C the rat enzyme binds about 0.5 mol L-noradrenaline/mol subunit with a half-maximal binding (S50) at 0.25 microM L-noradrenaline.", "entity1": "phenylalanine hydroxylase", "entity2": "L-noradrenaline", "span1": [48, 73], "span2": [29, 44]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2694": {"label": 4, "data": {"text": "Combining in vivo and in vitro findings, we identified nine AhR agonists, six of which are marketed therapeutics and have been approved by the U.S. Food and Drug Administration, including leflunomide, flutamide, and nimodipine.", "entity1": "AhR", "entity2": "nimodipine", "span1": [60, 63], "span2": [216, 226]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10020": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Arg", "span1": [199, 208], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4331": {"label": 3, "data": {"text": "Suppression of Src/ERK and GSK-3/\u03b2-catenin signaling by pinosylvin inhibits the growth of human colorectal cancer cells.", "entity1": "Src", "entity2": "pinosylvin", "span1": [15, 18], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11047": {"label": 8, "data": {"text": "Some of the new compounds proved in a slightly modified colorimetric Ellmann's assay to be potent inhibitors of acetylcholinesterase and of butyrylcholinesterase which is another catalytic enzyme hydrolysing acetylcholine.", "entity1": "butyrylcholinesterase", "entity2": "acetylcholine", "span1": [140, 161], "span2": [208, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9301": {"label": 3, "data": {"text": "The present study utilized blood from normal volunteers and 125I-fibrinogen in a dilute whole blood clot assay to determine the relative concentrations of lysine analogues required for inhibition of clot lysis induced by exogenous t-PA. AMCA (0.06 mM) and EACA (0.6 mM) were effective in prolonging clot lysis if (1) whole blood clots were formed and then exposed to a lysine analogue and exogenous t-PA or if (2) whole blood clots were formed in the presence of exogenous t-PA and a lysine analogue.", "entity1": "t-PA", "entity2": "AMCA", "span1": [399, 403], "span2": [237, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11093": {"label": 1, "data": {"text": "5-Methyl-urapidil was selective for cloned alpha 1A adrenoceptors.", "entity1": "alpha 1A adrenoceptors", "entity2": "5-Methyl-urapidil", "span1": [43, 65], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6062": {"label": 3, "data": {"text": "NE, phorbol esters, and bradykinin each decreased alpha-AR mRNA levels by 70-80%.", "entity1": "alpha-AR", "entity2": "phorbol esters", "span1": [50, 58], "span2": [4, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"888": {"label": 1, "data": {"text": "As compared with N(5)-methyl H(4)biopterin, N(5)-formyl H(4)biopterin bound with twice the capacity but stimulated nitric oxide synthase to a lesser extent.", "entity1": "nitric oxide synthase", "entity2": "N(5)-formyl H(4)biopterin", "span1": [115, 136], "span2": [44, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15835": {"label": 1, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "RXR", "entity2": "retinoic acid", "span1": [143, 146], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8101": {"label": 2, "data": {"text": "The mechanism revealed that wogonin inhibited H2O2-induced phosphorylation of caveolin-1 (cav-1) associating with the suppression of stabilization of VE-cadherin and \u03b2-catenin.", "entity1": "cav-1", "entity2": "H2O2", "span1": [90, 95], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"802": {"label": 2, "data": {"text": "Neuron, 21 (1998) 907-918) further confirms that lithium enhances GluR3 responses by reducing desensitization, since lithium's effects are reversed in this mutant.", "entity1": "GluR3", "entity2": "lithium", "span1": [66, 71], "span2": [49, 56]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2737": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "BCR", "entity2": "Dasatinib", "span1": [95, 98], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1098": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "physostigmine", "span1": [51, 71], "span2": [96, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11602": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "CBS", "entity2": "Hydrogen sulphide", "span1": [140, 143], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10162": {"label": 5, "data": {"text": "Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride) is a novel antiallergic/histamine H1-receptor antagonistic drug that was synthesized and evaluated in our laboratories.", "entity1": "histamine H1-receptor", "entity2": "olopatadine", "span1": [165, 186], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6945": {"label": 1, "data": {"text": "Vitamin E supplementation was found to alter the plasma HDL-C-related factors; meanwhile, probucol supplementation was very effective in enhancing cholesterol metabolism, except for a negative effect that reduced plasma HDL-C concentration.", "entity1": "HDL", "entity2": "Vitamin E", "span1": [56, 59], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15426": {"label": 1, "data": {"text": "Relative expression of cholesterol transport-related proteins and inflammation markers through the induction of 7-ketosterol-mediated stress in Caco-2 cells.", "entity1": "holesterol transport-related proteins", "entity2": "7-ketosterol", "span1": [24, 61], "span2": [112, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2224": {"label": 9, "data": {"text": "This mutation is inherently resistant to imatinib and, to date, there remains no effective curative therapy for systemic mastocytosis associated with KITD816V.", "entity1": "D816V", "entity2": "imatinib", "span1": [153, 158], "span2": [41, 49]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13612": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "PDGFR-beta", "entity2": "Sorafenib", "span1": [210, 220], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13500": {"label": 1, "data": {"text": "In this study the neuromuscular blocking drug vecuronium and the controls gallamine and pancuronium slowed the rate of atropine induced [(3)H]N-methylscopolamine dissociation from Chinese hamster ovary cells expressing recombinant human muscarinic M2 receptors K(off) values min(-1); vecuronium (125 nM), atropine 0.45+/-0.07+blocker 0.04+/-0.02; gallamine (21 nM), atropine 0.42+/-0.05+blocker 0.15+/-0.04; pancuronium(21 nM), atropine 0.36+/-0.03+blocker 0.03+/-0.01).", "entity1": "human muscarinic M2 receptors", "entity2": "atropine", "span1": [231, 260], "span2": [119, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15562": {"label": 1, "data": {"text": "Taken together, our data demonstrate that puerarin attenuates MPTP-induced dopaminergic neuronal degeneration via modulating GDNF expression, PI3K/Akt pathway and GSH activation, which subsequently ameliorate MPTP-induced ROS formation and decrease of Lamp 2A expression.", "entity1": "Akt", "entity2": "MPTP", "span1": [147, 150], "span2": [62, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7387": {"label": 8, "data": {"text": "Proline dehydrogenase (PRODH) and Delta(1)-pyrroline-5-carboxylate dehydrogenase (P5CDH) catalyze the two-step oxidation of proline to glutamate.", "entity1": "P5CDH", "entity2": "glutamate", "span1": [82, 87], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3644": {"label": 1, "data": {"text": "DBDCT induced the release of cytochrome c from the mitochondria to the cytosol and the generation of reactive oxygen species.", "entity1": "cytochrome c", "entity2": "DBDCT", "span1": [29, 41], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10446": {"label": 7, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "(L-serine dehydratase", "entity2": "PLP", "span1": [4, 25], "span2": [78, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5200": {"label": 3, "data": {"text": "High glucose (HG) induces apoptosis of podocytes, inhibits AMPK activation, inactivates tuberin and activates mTOR.", "entity1": "AMPK", "entity2": "glucose", "span1": [59, 63], "span2": [5, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13312": {"label": 3, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "B-RAF", "entity2": "BAY43-9006", "span1": [52, 57], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12662": {"label": 1, "data": {"text": "However, inter-helical distances calculated and determined by EPR for PGHS-2 complexed with arachidonic acid, flurbiprofen, and SC-58125 were in close agreement with those obtained from the cognate crystal structures.", "entity1": "PGHS-2", "entity2": "SC-58125", "span1": [70, 76], "span2": [128, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11141": {"label": 1, "data": {"text": "However, because clozapine competes with endogenous dopamine, the in vivo concentration of clozapine (to occupy dopamine D4 receptors) can be derived to be about 13 nM, agreeing with the value of 12 to 20 nM in the plasma water or spinal fluid observed in treated patients.", "entity1": "dopamine D4 receptors", "entity2": "clozapine", "span1": [112, 133], "span2": [91, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1443": {"label": 1, "data": {"text": "Atomoxetine inhibited binding of radioligands to clonal cell lines transfected with human NE, serotonin (5-HT) and dopamine (DA) transporters with dissociation constants (K(i)) values of 5, 77 and 1451 nM, respectively, demonstrating selectivity for NE transporters.", "entity1": "NE transporters", "entity2": "Atomoxetine", "span1": [250, 265], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7668": {"label": 3, "data": {"text": "Some of these structurally related compounds have a very different behavior against the widespread isozyme CA II, with chlorthalidone, trichloromethiazide, and furosemide being efficient inhibitors against CA II (K(I)s of 65-138 nM), whereas indapamide is a much weaker one (K(I) of 2520 nM).", "entity1": "CA II", "entity2": "trichloromethiazide", "span1": [206, 211], "span2": [135, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15106": {"label": 0, "data": {"text": "Moreover, we show that USP22 is acetylated on multiple lysine residues and that alteration of a single lysine (K129) within the ZnF-UBP domain is sufficient to alter interaction of the DUBm with the core SAGA complex.", "entity1": "ZnF-UBP domain", "entity2": "lysine", "span1": [128, 142], "span2": [103, 109]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2233": {"label": 3, "data": {"text": "In this study, we demonstrate significant inhibitory activity of dasatinib against both wild-type KIT and the KITD816V mutation in the nanomolar range in in vitro and cell-based kinase assays.", "entity1": "KIT", "entity2": "dasatinib", "span1": [110, 113], "span2": [65, 74]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2227": {"label": 1, "data": {"text": "Computer modeling suggests that the KITD816V mutation destabilizes the inactive conformation of the KIT activation loop to which imatinib binds, but it is not predicted to impair binding of KIT by dasatinib.", "entity1": "KIT", "entity2": "imatinib", "span1": [36, 39], "span2": [129, 137]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7719": {"label": 2, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "gonadotrophin-releasing hormone (GnRH) receptor", "entity2": "goserelin", "span1": [140, 187], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13936": {"label": 1, "data": {"text": "Thalidomide initiates its teratogenic effects by binding to CRBN and inhibiting the associated ubiquitin ligase activity.", "entity1": "CRBN", "entity2": "Thalidomide", "span1": [60, 64], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11365": {"label": 1, "data": {"text": "The relatively high D(2) receptor occupancy, even at trough plasma levels, suggests that ziprasidone is more similar to risperidone and olanzapine in receptor occupancy profile than to clozapine and quetiapine.", "entity1": "D(2) receptor", "entity2": "risperidone", "span1": [20, 33], "span2": [120, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9963": {"label": 3, "data": {"text": "Selective COX-2 inhibitors, such as meloxicam, celecoxib (SC-58635), and rofecoxib (MK-0966), are NSAIDs that have been modified chemically to preferentially inhibit COX-2 but not COX-1.", "entity1": "COX-2", "entity2": "SC-58635", "span1": [166, 171], "span2": [58, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8787": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-FOXO1", "entity2": "CAPE", "span1": [137, 150], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7552": {"label": 3, "data": {"text": "As further support, alpha-methyl-DL-aspartate, an inhibitor of argininosuccinate synthase (AS), a component of the citrulline-NO cycle, inhibited NO production in a dose-dependent manner.", "entity1": "AS", "entity2": "alpha-methyl-DL-aspartate", "span1": [91, 93], "span2": [20, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8724": {"label": 9, "data": {"text": "This preference is partial because UGT2B10 did not conjugate the tertiary cyclic amine in trifluoperazine.", "entity1": "UGT2B10", "entity2": "tertiary cyclic amine", "span1": [35, 42], "span2": [65, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3019": {"label": 2, "data": {"text": "Statins increase p21 through inhibition of histone deacetylase activity and release of promoter-associated HDAC1/2.", "entity1": "HDAC1/2", "entity2": "Statins", "span1": [107, 114], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8128": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "pCREB", "entity2": "Sal", "span1": [77, 82], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8155": {"label": 3, "data": {"text": "Additionally, DPEP suppressed the production of inflammatory cytokines, including tumor necrosis factor-\u03b1 (TNF-\u03b1), interleukin (IL)-1\u03b2, and IL-6.", "entity1": "tumor necrosis factor-\u03b1", "entity2": "DPEP", "span1": [82, 105], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3322": {"label": 1, "data": {"text": "MXF or VP-16 slightly affected cellular topo II activity in nuclear extracts derived from drug-treated cells while the combination enhanced inhibitory activity and the reduction in band depletion of topo II.", "entity1": "topo II", "entity2": "MXF", "span1": [40, 47], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6473": {"label": 3, "data": {"text": "Nordihydroguaiaretic acid (NDGA) has been shown to inhibit both 5-lipoxygenase and ornithine decarboxylase and is active against several cancer cell lines and at least one mouse tumor model.", "entity1": "ornithine decarboxylase", "entity2": "Nordihydroguaiaretic acid", "span1": [83, 106], "span2": [0, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5741": {"label": 5, "data": {"text": "SB225002 (SB) is an IL-8 receptor B (IL-8RB) antagonist that has previously been shown to inhibit IL-8-based cancer cell invasion, and to possess in vivo anti-inflammatory and anti-nociceptive effects.", "entity1": "IL-8 receptor B", "entity2": "SB225002", "span1": [20, 35], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6807": {"label": 1, "data": {"text": "Thalidomide decreased the stability of TNF-mRNA and COX-2 mRNA.", "entity1": "COX-2", "entity2": "Thalidomide", "span1": [52, 57], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10651": {"label": 3, "data": {"text": "We report here the pharmacological properties of a third selective COX-2 inhibitor, valdecoxib, which is the most potent and in vitro selective of the marketed COX-2 inhibitors that we have studied.", "entity1": "COX-2", "entity2": "valdecoxib", "span1": [160, 165], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4375": {"label": 2, "data": {"text": "CYP3A induction in the liver increased depending on the dose of DEX-P, whereas that in intestine showed a mild increase, but the induction level was almost constant regardless of the dose of DEX-P. 4.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [0, 5], "span2": [64, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4302": {"label": 8, "data": {"text": "Transport by OATP1B1 and OATP1B3 enhances the cytotoxicity of epigallocatechin 3-O-gallate and several quercetin derivatives.", "entity1": "OATP1B1", "entity2": "epigallocatechin 3-O-gallate", "span1": [13, 20], "span2": [62, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11389": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "NTG", "span1": [143, 148], "span2": [74, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4551": {"label": 1, "data": {"text": "The present study was designed to test the hypothesis that alcohol alters global DNA methylation, and modulates expression of the DNA methyltransferases (DNMTs) and various methyl CpG-binding proteins.", "entity1": "DNA methyltransferases", "entity2": "alcohol", "span1": [130, 152], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15689": {"label": 1, "data": {"text": "Finally, the involvement of PKC and PKA was also studied, and we showed that both play a role in the antinociceptive mechanism of CAT.", "entity1": "PKC", "entity2": "CAT", "span1": [28, 31], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7600": {"label": 4, "data": {"text": "In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use.", "entity1": "V(1a)", "entity2": "terlipressin", "span1": [174, 179], "span2": [160, 172]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11749": {"label": 3, "data": {"text": "Based on these suggestions, the rational redesign of furanopyrimidine 24 (clog\u2009P=7.41; Aurora\u2005A IC(50) =43\u2005nM; HCT-116 IC(50) =400\u2005nM) led to the identification of quinazoline 67 (clog\u2009P=5.28; Aurora\u2005A IC(50) =25\u2005nM; HCT-116 IC(50) =23\u2005nM).", "entity1": "Aurora\u2005A", "entity2": "furanopyrimidine", "span1": [87, 95], "span2": [53, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"987": {"label": 3, "data": {"text": "Moreover, BH(4) treatment of the fructose-fed rats markedly reduced the lipid peroxide content of both aortic and cardiac tissues and inhibited the activation of 2 redox-sensitive transcription factors, nuclear factor-kappaB and activating protein-1, which were increased in fructose-fed rats.", "entity1": "activating protein-1", "entity2": "BH(4)", "span1": [229, 249], "span2": [10, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2880": {"label": 2, "data": {"text": "At PND35, the medial prefrontal cortex (mPFC) of rats given MPH showed 55% greater immunoreactivity (-ir) for the catecholamine marker tyrosine hydroxylase (TH), 60% more Nissl-stained cells, and 40% less norepinephrine transporter (NET)-ir density.", "entity1": "tyrosine hydroxylase", "entity2": "MPH", "span1": [135, 155], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6912": {"label": 8, "data": {"text": "PSMA acts as a glutamate carboxypeptidase (GCPII) on small molecule substrates, including folate, the anticancer drug methotrexate, and the neuropeptide N-acetyl-l-aspartyl-l-glutamate.", "entity1": "glutamate carboxypeptidase", "entity2": "methotrexate", "span1": [15, 41], "span2": [118, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14844": {"label": 8, "data": {"text": "Aldehyde dehydrogenase 1 (ALDH1A1) catalyzes the oxidation of toxic aldehydes to carboxylic acids.", "entity1": "Aldehyde dehydrogenase 1", "entity2": "carboxylic acids", "span1": [0, 24], "span2": [81, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5403": {"label": 2, "data": {"text": "The data show that CP[c]Ph is less potent at inducing CYP1A gene expression in rainbow trout than benzo[a]pyrene (B[a]P), a well-known Ah-receptor agonist.", "entity1": "CYP1A", "entity2": "benzo[a]pyrene", "span1": [54, 59], "span2": [98, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15629": {"label": 3, "data": {"text": "Next, nobiletin significantly decreased the levels of phospho-ERK2 and phospho-Akt in ERK2 or Akt siRNA-transfected cells concomitantly with a marked reduction on cell invasion and migration.", "entity1": "Akt", "entity2": "nobiletin", "span1": [94, 97], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11539": {"label": 1, "data": {"text": "The objectives of the present study were to examine the changes of histamine content, HDC activity and HDC mRNA expression in the nasal mucosa of allergy model rats sensitized by the exposure to toluene diisocyanate (TDI) and to investigate the effect of dexamethasone on the above mentioned allergic parameters.", "entity1": "HDC", "entity2": "toluene diisocyanate", "span1": [86, 89], "span2": [195, 215]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10536": {"label": 1, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "cyclic AMP response element binding factor", "entity2": "RA", "span1": [309, 351], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2205": {"label": 3, "data": {"text": "Doxycycline was shown to decrease cerebral MMP-9 activities and angiogenesis induced by vascular endothelial growth factor (VEGF).", "entity1": "MMP-9", "entity2": "Doxycycline", "span1": [43, 48], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4543": {"label": 8, "data": {"text": "The in vivo inhibitory effect of harmaline on CYP2D6-catalyzed bufotenine formation was confirmed by in vitro study using purified CYP2D6.", "entity1": "CYP2D6", "entity2": "bufotenine", "span1": [131, 137], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14860": {"label": 2, "data": {"text": "These results indicate that membrane ER\u03b1 levels in N-38 neurons are dynamically autoregulated by estradiol.", "entity1": "ER\u03b1", "entity2": "estradiol", "span1": [37, 40], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9463": {"label": 1, "data": {"text": "7. 8-Epi-PGF2 alpha showed only weak binding to the IP, TP, FP, EP2 and EP3 receptor at 10 microM concentration.", "entity1": "TP", "entity2": "7. 8-Epi-PGF2", "span1": [56, 58], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5766": {"label": 2, "data": {"text": "A similar pattern of susceptibility is observed following acute exposure to the neurotoxicant 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), and the resistance of TIDA neurons to MPTP is associated with increased expression of parkin and ubiquitin carboxy-terminal hydrolase L-1 (UCHL- 1).", "entity1": "UCHL- 1", "entity2": "MPTP", "span1": [286, 293], "span2": [185, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8159": {"label": 3, "data": {"text": "DPEP inhibited LPS-induced phosphorylation of ERK, JNK, and p38.", "entity1": "ERK", "entity2": "DPEP", "span1": [46, 49], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5138": {"label": 3, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "HO-1", "entity2": "5HHMF", "span1": [192, 196], "span2": [126, 131]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3483": {"label": 2, "data": {"text": "Anti-diabetic Activity of Swertiamarin is due to an Active Metabolite, Gentianine, that Upregulates PPAR-\u03b3 Gene Expression in 3T3-L1 cells.", "entity1": "PPAR-\u03b3", "entity2": "Gentianine", "span1": [100, 106], "span2": [71, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10704": {"label": 8, "data": {"text": "The Cl(-) secretory response is mediated via a non-CFTR pathway, and the driving force for Cl(-) secretion is enhanced by the effect of P2Y(2) activation to also inhibit epithelial Na(+) transport.", "entity1": "CFTR", "entity2": "Cl(-)", "span1": [51, 55], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10477": {"label": 4, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "formoterol", "span1": [392, 423], "span2": [189, 199]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9184": {"label": 1, "data": {"text": "Amdinocillin is a beta-amidino penicillanic acid derivative that binds specifically to penicillin-binding protein 2.", "entity1": "penicillin-binding protein 2", "entity2": "Amdinocillin", "span1": [87, 115], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7556": {"label": 8, "data": {"text": "Nitric oxide (NO) is an important vasorelaxant produced along with L-citrulline from L-arginine in a reaction catalyzed by endothelial nitric oxide synthase (eNOS).", "entity1": "eNOS", "entity2": "Nitric oxide", "span1": [158, 162], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1]},
	"13517": {"label": 8, "data": {"text": "Patients with acute vitiligo have low epidermal catalase expression/activities and accumulate 10(-3) M H(2)O(2).", "entity1": "catalase", "entity2": "H(2)O(2)", "span1": [48, 56], "span2": [103, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7673": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "carbonic anhydrase", "entity2": "Thiazide", "span1": [93, 111], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6403": {"label": 0, "data": {"text": "Finally, cysteine 53 in the M1P1 external loop is required for functional expression of TWIK-2 but is not critical for subunit self-assembly.", "entity1": "TWIK-2", "entity2": "cysteine", "span1": [88, 94], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4887": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "ezetimibe", "span1": [83, 86], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7683": {"label": 9, "data": {"text": "Sergliflozin etabonate increased urinary glucose excretion in a dose-dependent manner, and inhibited the increase in plasma glucose after sucrose loading independently of insulin secretion in normal rats.", "entity1": "insulin", "entity2": "Sergliflozin etabonate", "span1": [171, 178], "span2": [0, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6929": {"label": 8, "data": {"text": "When cultured in YPD medium containing 15% glucose under aerobic conditions, the KGD1 (alpha-ketoglutarate dehydrogenase) gene disrupted mutant produced a lower level of succinate than the wild-type strain, while the SDH1 (succinate dehydrogenase) gene-disrupted mutant produced an increased level of succinate.", "entity1": "alpha-ketoglutarate dehydrogenase", "entity2": "succinate", "span1": [87, 120], "span2": [170, 179]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4366": {"label": 2, "data": {"text": "Time-dependent changes in hepatic and intestinal induction of cytochrome P450 3A after administration of dexamethasone to rats.", "entity1": "cytochrome P450 3A", "entity2": "dexamethasone", "span1": [62, 80], "span2": [105, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15880": {"label": 2, "data": {"text": "The Bcl2/Bax ratio increased and Mfn2 expression decreased in MIN6 cells after glucose stimulation.", "entity1": "Bcl2", "entity2": "glucose", "span1": [4, 8], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10874": {"label": 2, "data": {"text": "CPT-11 and SN-38 may also stimulate the production of pro-inflammatory cytokines and prostaglandins (PGs), thus inducing the secretion of Na(+) and Cl(-).", "entity1": "cytokines", "entity2": "CPT-11", "span1": [71, 80], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6241": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "5-HT1D", "entity2": "Eletriptan", "span1": [115, 121], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4684": {"label": 1, "data": {"text": "Modulation of cytochrome P450 1 (Cyp1) by vanadium in hepatic tissue and isolated hepatocyte of C57BL/6 mice.", "entity1": "cytochrome P450 1", "entity2": "vanadium", "span1": [14, 31], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1745": {"label": 3, "data": {"text": "TAS-102 currently undergoing clinical trials, has been demonstrated to have at least two mechanisms, inhibition of TS and incorporation into DNA.", "entity1": "TS", "entity2": "TAS-102", "span1": [115, 117], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12616": {"label": 1, "data": {"text": "The nuclear gene transcription factors RAR beta and RAR gamma mediate the retinoid activity of adapalene.", "entity1": "RAR gamma", "entity2": "adapalene", "span1": [52, 61], "span2": [95, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8345": {"label": 8, "data": {"text": "Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine.", "entity1": "HDC", "entity2": "amine", "span1": [25, 28], "span2": [80, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15027": {"label": 3, "data": {"text": "Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner.", "entity1": "SAHH", "entity2": "AdOx", "span1": [127, 131], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10805": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-1", "entity2": "flunixin", "span1": [0, 5], "span2": [61, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9395": {"label": 2, "data": {"text": "We thus speculated that activation of PGHS-1 might be a mechanism by which minoxidil (2,4-diamino-6-piperidinopyrimidine-3-oxyde) stimulates hair growth in vivo.", "entity1": "PGHS-1", "entity2": "2,4-diamino-6-piperidinopyrimidine-3-oxyde", "span1": [38, 44], "span2": [86, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11380": {"label": 1, "data": {"text": "P2Y12, a new platelet ADP receptor, target of clopidogrel.", "entity1": "ADP receptor", "entity2": "clopidogrel", "span1": [22, 34], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10013": {"label": 5, "data": {"text": "Other 5-HT3 receptor antagonists also produced such a shift in the following antagonistic-potency order: granisetron> ondansetron=AS-8112>>metoclopramide.", "entity1": "5-HT3 receptor", "entity2": "granisetron", "span1": [6, 20], "span2": [105, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2069": {"label": 3, "data": {"text": "In this study, using a model of gentamicin C (GMC)-induced reduction in SGLT1 activity, we examined whether ligands for megalin protect LLC-PK1 cells from the GMC-induced reduction in SGLT1 activity.", "entity1": "SGLT1", "entity2": "GMC", "span1": [184, 189], "span2": [159, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8435": {"label": 1, "data": {"text": "The endogenous steroid lithocholic acid (LCA) dilates cerebral arteries via BK channel activation, which requires recognition by a BK \u03b21 site that includes Thr169.", "entity1": "BK \u03b21", "entity2": "steroid", "span1": [131, 136], "span2": [15, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12056": {"label": 1, "data": {"text": "Our results demonstrated that acute As(III) treatment (12.5\u2009mg/kg) altered CYP epoxygenases, CYP \u03c9-hydroxylases and EPHX2 mRNA levels that were isozyme and tissue specific.", "entity1": "\u03c9-hydroxylases", "entity2": "As(III)", "span1": [97, 111], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1340": {"label": 4, "data": {"text": "Dexamethasone (DEX), betamethasone (BM), and their esterified-derivatives had full transrepression agonistic activity in a reporter assay using CV-1 cells transfected with either human or rat GR.", "entity1": "human or rat GR", "entity2": "betamethasone", "span1": [179, 194], "span2": [21, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4732": {"label": 2, "data": {"text": "These results indicate transcription of FDX1 is regulated by the NR5A family and cAMP signaling, and participates in steroid hormone production in ovarian granulosa cells.", "entity1": "FDX1", "entity2": "cAMP", "span1": [40, 44], "span2": [81, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14358": {"label": 3, "data": {"text": "Met-RANTES treatment also reduced the levels of cathepsin K and metalloproteinase 13 (MMP13).", "entity1": "MMP13", "entity2": "Met", "span1": [86, 91], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8552": {"label": 3, "data": {"text": "Herein we report novel pyrrole- and benzene-based hydroxamates (8, 10) and 2'-aminoanilides (9, 11) bearing the tert-butylcarbamate group at the CAP moiety as histone deacetylase (HDAC) inhibitors.", "entity1": "histone deacetylase", "entity2": "hydroxamates", "span1": [159, 178], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8016": {"label": 3, "data": {"text": "In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A(2) (hnps-PLA(2)) and human leukotriene A(4) hydrolase (LTA(4)H-h) was found.", "entity1": "LTA(4)H-h", "entity2": "JMC08-4", "span1": [237, 246], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6855": {"label": 9, "data": {"text": "Bosentan also decreased serum glucose level without any effect on insulin secretion in mild diabetic rats and potentiated the hypoglycemic action of insulin.", "entity1": "insulin", "entity2": "Bosentan", "span1": [66, 73], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4489": {"label": 8, "data": {"text": "Our results suggest that arsenite can potentiate EDHF-type relaxations via a mechanism that is dependent on hydrogen peroxide, thus demonstrating that dismutation of the superoxide anion generated by NADPH oxidase can potentially offset loss of NO bioavailability under conditions of reduced eNOS activity.", "entity1": "NADPH oxidase", "entity2": "superoxide", "span1": [200, 213], "span2": [170, 180]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11465": {"label": 1, "data": {"text": "Involvement of EP1 and EP2 receptors in the regulation of the Na,K-ATPase by prostaglandins in MDCK cells.", "entity1": "EP2 receptors", "entity2": "prostaglandins", "span1": [23, 36], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6030": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "renzapride", "span1": [63, 69], "span2": [220, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3005": {"label": 8, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Q817A", "entity2": "tadalafil", "span1": [216, 221], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7620": {"label": 3, "data": {"text": "BACKGROUND: Lapatinib, the first dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases, was approved by the US Food and Drug Administration (FDA) in 2007.", "entity1": "tyrosine kinases", "entity2": "Lapatinib", "span1": [143, 159], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13620": {"label": 1, "data": {"text": "One is that the binding of retinoids to nuclear retinoic acid receptors (RARs) does not match their therapeutic efficacy: acitretin activates the three receptor subtypes, RAR-alpha, -beta and -gamma, without measurable receptor binding, whereas tazarotene preferentially binds to and activates RAR-beta and -gamma in preference to RAR-alpha.", "entity1": "RAR-alpha", "entity2": "tazarotene", "span1": [331, 340], "span2": [245, 255]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12453": {"label": 8, "data": {"text": "Cytochrome P450 2E1 (CYP 450 2E1), activity was determined as hydroxylation of aniline in liver microsomes.", "entity1": "Cytochrome P450 2E1", "entity2": "aniline", "span1": [0, 19], "span2": [79, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"111": {"label": 9, "data": {"text": "Similarly, felodipine and the p-chloro analogue blocked myosin filament assembly induced by low concentrations of calmodulin, whereas the oxidized and t-butyl analogues did not.", "entity1": "myosin", "entity2": "t-butyl", "span1": [56, 62], "span2": [151, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11986": {"label": 8, "data": {"text": "6-DHSG was metabolised by GSH to form a GSH conjugate (GS-6-DHSG) in RAW 264.7 cells, via a potential mechanism involving the catalytic activity of glutathione-S-transferase (GST).", "entity1": "glutathione-S-transferase", "entity2": "6-DHSG", "span1": [148, 173], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9798": {"label": 3, "data": {"text": "With respect to the substrate dihydroorotate, atovaquone was an uncompetitive inhibitor of human dihydroorotate dehydrogenase (Kiu = 11.6 microM) and a non-competitive inhibitor of the rat enzyme (Kiu = 905/ Kic = 1,012 nM).", "entity1": "human dihydroorotate dehydrogenase", "entity2": "dihydroorotate", "span1": [91, 125], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"9526": {"label": 3, "data": {"text": "We thus conclude that the more potent nisoldipine inhibition of smooth muscle versus cardiac L-type Ca2+ channels is not attributable to differences in channel inactivation or activation.", "entity1": "cardiac L-type Ca2+ channels", "entity2": "nisoldipine", "span1": [85, 113], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15637": {"label": 3, "data": {"text": "Among them, nobiletin markedly inhibited HGF-induced the abilities of the adhesion, invasion, and migration by cell-matrix adhesion assay and transwell-chamber invasion/migration assay under non-cytotoxic concentrations.", "entity1": "HGF", "entity2": "nobiletin", "span1": [41, 44], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12568": {"label": 9, "data": {"text": "Glutathione-independent prostaglandin D synthase [prostaglandin-H2 D-isomerase; (5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase, EC 5.3.99.2] is an enzyme responsible for biosynthesis of prostaglandin D2 in the central nervous system.", "entity1": "(5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase", "entity2": "Glutathione", "span1": [80, 163], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2619": {"label": 3, "data": {"text": "The activity of polymerases containing mutations known to confer resistance to foscarnet (V715M, T700A and N495K) was inhibited by concentrations of foscarnet eight to 14 times higher than those required to inhibit wild-type polymerases.", "entity1": "V715M", "entity2": "foscarnet", "span1": [90, 95], "span2": [149, 158]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6772": {"label": 3, "data": {"text": "Novel mechanism of action for hydralazine: induction of hypoxia-inducible factor-1alpha, vascular endothelial growth factor, and angiogenesis by inhibition of prolyl hydroxylases.", "entity1": "prolyl hydroxylases", "entity2": "hydralazine", "span1": [159, 178], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13154": {"label": 1, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "Bcl-2", "entity2": "paclitaxel", "span1": [279, 284], "span2": [378, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"851": {"label": 3, "data": {"text": "Troglitazone inhibited LTB(4) production by the supernatant fraction of RBL-2H3 cell lysate with similar potency to zileuton, suggesting that troglitazone inhibits LT production by direct inhibition of 5-LOX activity.", "entity1": "5-LOX", "entity2": "zileuton", "span1": [202, 207], "span2": [116, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14182": {"label": 0, "data": {"text": "CBDP irreversibly inhibits butyrylcholinesterase (BChE) in human plasma by forming adducts on the active site serine (Ser-198).", "entity1": "BChE", "entity2": "Ser", "span1": [50, 54], "span2": [118, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11392": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "sodium nitroprusside", "span1": [143, 148], "span2": [113, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4034": {"label": 8, "data": {"text": "Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4).", "entity1": "LTA(4)H", "entity2": "LTB(4)", "span1": [28, 35], "span2": [124, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2246": {"label": 3, "data": {"text": "BACKGROUND: Since the introduction of the first cholinesterase inhibitor (ChEI) in 1997, most clinicians and probably most patients would consider the cholinergic drugs, donepezil, galantamine and rivastigmine, to be the first line pharmacotherapy for mild to moderate Alzheimer's disease.The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase.", "entity1": "cholinesterase", "entity2": "galantamine", "span1": [48, 62], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"673": {"label": 0, "data": {"text": "The deduced amino acid sequence contains 779 amino acids, including a putative cGMP binding sequence in the amino-terminal portion of the molecule and a catalytic domain that is 16-47% identical in amino acid sequence to those of other PDE families.", "entity1": "PDE", "entity2": "amino", "span1": [236, 239], "span2": [108, 113]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14856": {"label": 3, "data": {"text": "Interestingly, Acrolein increased proteins' levels of amyloid precursor protein (APP), \u03b2-secretase (BACE-1) and the amyloid \u03b2-peptide transporter receptor for advanced glycation end products, and decreased A-disintegrin and metalloprotease (ADAM) 10 levels.", "entity1": "A-disintegrin and metalloprotease (ADAM) 10", "entity2": "Acrolein", "span1": [206, 249], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"5881": {"label": 1, "data": {"text": "Labetalol and the enantiomers lacked affinity at alpha 2-adrenoceptors while at alpha 1-adrenoceptors the order of potency was prazosin much greater than RR-SR greater than labetalol.", "entity1": "alpha 1-adrenoceptors", "entity2": "labetalol", "span1": [80, 101], "span2": [173, 182]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5102": {"label": 2, "data": {"text": "Thus, we found that 5HHMF enhances heme oxygenase-1 (HO-1) expression via nuclear factor-erythroid 2-related factor 2 (Nrf2) activation.", "entity1": "Nrf2", "entity2": "5HHMF", "span1": [119, 123], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3579": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [184, 187], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4920": {"label": 3, "data": {"text": "The vascular protective effects of kinsenoside were speculated to be attributed to oxidative stress inhibition and the reduction of nuclear factor kappa B (NF-\u03baB) mRNA expression levels in high glucose conditions.", "entity1": "nuclear factor kappa B", "entity2": "kinsenoside", "span1": [132, 154], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11554": {"label": 1, "data": {"text": "CONCLUSIONS: We were able to demonstrate a moderate 5-HT(2A) and D(1) occupancy under clinically relevant doses of flupentixol, albeit lower than expected from in vitro data and clearly below saturation.", "entity1": "5-HT(2A)", "entity2": "flupentixol", "span1": [52, 60], "span2": [115, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"227": {"label": 3, "data": {"text": "The inhibition of UG synthesis and PR down-regulation by 5 alpha-NET and 3 beta,5 alpha-NET indicates that these NET metabolites possess antiprogestational properties.", "entity1": "UG", "entity2": "5 alpha-NET", "span1": [18, 20], "span2": [57, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"587": {"label": 3, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "thymidylate synthase", "entity2": "Tomudex", "span1": [205, 225], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12721": {"label": 1, "data": {"text": "In human plasma the BrBK half-life values in the absence or in the presence of GW660511X (3.8 microM) or omapatrilat (32 nM) were 38.7 +/- 2.4, 51.2 +/- 4.7 and 114.7 +/- 9.3 min, respectively and BrBK was degraded into BrBK1-8, BrBK1-7, BrBK1-5 and Br-Phe.", "entity1": "BrBK", "entity2": "GW660511X", "span1": [20, 24], "span2": [79, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2180": {"label": 2, "data": {"text": "Tissue-type plasminogen activator (tPA), a serine protease well known for generating plasmin, has been demonstrated to induce matrix metalloproteinase-9 (MMP-9) gene expression and protein secretion in renal interstitial fibroblasts.", "entity1": "matrix metalloproteinase-9", "entity2": "serine", "span1": [126, 152], "span2": [43, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10790": {"label": 2, "data": {"text": "Simvastatin, an HMG-CoA reductase inhibitor with mild inhibition of LFA-1, induced the production of interleukin (IL)-18, tumor necrosis factor (TNF)-alpha and interferon (IFN)-gamma in human peripheral blood mononuclear cells (PBMC).", "entity1": "tumor necrosis factor (TNF)-alpha", "entity2": "Simvastatin", "span1": [122, 155], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6501": {"label": 3, "data": {"text": "Pemetrexed disodium (ALIMTA) is a novel antimetabolite that inhibits at least three folate-dependent enzymes, thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase.", "entity1": "dihydrofolate reductase", "entity2": "Pemetrexed disodium", "span1": [132, 155], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11016": {"label": 2, "data": {"text": "Given the treatment with three doses of Captopril (15 approximately 45 mg/kg) markedly attenuated inhibition of vasodilator responses to ACh, and eliminated the increased level of malondialdehyde, the decreased level of NO, activity of PON1 and SOD in serum by single intragastric gavaged L-methionine.", "entity1": "SOD", "entity2": "Captopril", "span1": [245, 248], "span2": [40, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16070": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "BTK", "entity2": "Ibrutinib", "span1": [123, 126], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"193": {"label": 9, "data": {"text": "The nonsteroidal antiandrogen RU 23908 ( Anandron ) weakly interacts with the prostatic cytosolic androgen receptor and shows a fast dissociation rate.", "entity1": "androgen receptor", "entity2": "Anandron", "span1": [98, 115], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4707": {"label": 3, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a1", "entity2": "V(5+)", "span1": [241, 247], "span2": [194, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8453": {"label": 9, "data": {"text": "In the present study, hinokitiol (1 and 2\u03bcM) inhibited the collagen-induced aggregation of human platelets, but did not inhibit the activation of platelets by other agonists, including thrombin, arachidonic acid, and ADP.", "entity1": "thrombin", "entity2": "hinokitiol", "span1": [185, 193], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5506": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "buprenorphine", "span1": [108, 126], "span2": [320, 333]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12578": {"label": 0, "data": {"text": "This cDNA clone, designated EAA3a, shares a 90% nucleotide identity with the previously reported rat GluR5-2b cDNA splice variant and differed from human GluR5-1d in the amino and carboxy terminal regions.", "entity1": "human GluR5-1d", "entity2": "carboxy", "span1": [148, 162], "span2": [180, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10867": {"label": 4, "data": {"text": "Most of the tested H(2)R agonists and imidazole-based H(3)R ligands show micromolar-to-nanomolar range hH(4)R affinity, and these ligands exert different intrinsic hH(4)R activities, ranging from full agonists to inverse agonists.", "entity1": "hH(4)R", "entity2": "imidazole", "span1": [164, 170], "span2": [38, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14941": {"label": 2, "data": {"text": "Peginesatide, a polyethylene glycol (PEG)ylated peptide-based erythropoiesis-stimulating agent, stimulates the erythropoietin receptor dimer that governs erythropoiesis.", "entity1": "erythropoietin receptor", "entity2": "Peginesatide", "span1": [111, 134], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9182": {"label": 1, "data": {"text": "Binding of penicillins to penicillin-binding protein 1Bs produces lysis, binding to penicillin-binding protein 2 produces round cells, and binding to penicillin-binding protein 3 produces long filaments.", "entity1": "penicillin-binding protein 3", "entity2": "penicillins", "span1": [150, 178], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14739": {"label": 8, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "3\u03b2-HSD", "entity2": "raisanberine", "span1": [83, 89], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3766": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "tumor necrosis factor-alpha", "entity2": "CCl(4)", "span1": [152, 179], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11009": {"label": 1, "data": {"text": "Cyproheptadine is a piperidine antihistamine that increases appetite through its antiserotonergic effect on 5-HT2 receptors in the brain.", "entity1": "5-HT2", "entity2": "Cyproheptadine", "span1": [108, 113], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9404": {"label": 1, "data": {"text": "Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).", "entity1": "nuclear transcription factors", "entity2": "adapalene", "span1": [133, 162], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6849": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "MS", "entity2": "Hcy", "span1": [165, 167], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8891": {"label": 1, "data": {"text": "These results indicate that the anabolic effects of clenbuterol are dependent on interaction with the beta 2-adrenoceptor.", "entity1": "beta 2-adrenoceptor", "entity2": "clenbuterol", "span1": [102, 121], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4015": {"label": 3, "data": {"text": "Curcumin improves TNBS-induced colitis in rats by inhibiting IL-27 expression via the TLR4/NF-\u03baB signaling pathway.", "entity1": "IL-27", "entity2": "Curcumin", "span1": [61, 66], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3764": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "nuclear factor-kappaB", "entity2": "CCl(4)", "span1": [83, 104], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1316": {"label": 1, "data": {"text": "A novel SCN5A arrhythmia mutation, M1766L, with expression defect rescued by mexiletine.", "entity1": "SCN5A", "entity2": "mexiletine", "span1": [8, 13], "span2": [77, 87]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13467": {"label": 8, "data": {"text": "The cytosolic ACC1 is expressed primarily in liver and adipose tissue, and uses malonyl-coenzyme A as a key building block in fatty acid biosynthesis.", "entity1": "ACC1", "entity2": "fatty acid", "span1": [14, 18], "span2": [126, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10621": {"label": 1, "data": {"text": "Cerebral histamine H1 receptor (H(1)R) binding was measured in 10 patients with major depression and in 10 normal age-matched subjects using PET and [(11)C]-doxepin.", "entity1": "histamine H1 receptor", "entity2": "[(11)C]-doxepin", "span1": [9, 30], "span2": [149, 164]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7327": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT1", "entity2": "MNI", "span1": [224, 229], "span2": [123, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5490": {"label": 7, "data": {"text": "Mechanisms that have been proposed for peroxidase-catalyzed iodination require the utilization of 1 mol of H2O2 for organic binding of 1 mol of iodide.", "entity1": "peroxidase", "entity2": "H2O2", "span1": [39, 49], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5082": {"label": 3, "data": {"text": "FCEO significantly inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) by suppressing the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, respectively.", "entity1": "iNOS", "entity2": "nitric oxide", "span1": [149, 153], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12059": {"label": 1, "data": {"text": "These results confirm and strengthen the idea of alpha N-acetyl beta-endorphin-(1-31) acting as a non-competitive regulator of mu opioid- and alpha 2-adrenoceptor-mediated supraspinal antinociception.", "entity1": "mu opioid", "entity2": "N-acetyl", "span1": [127, 136], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10269": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "transmembrane transporters", "entity2": "[3H]-MPP+", "span1": [135, 161], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"9899": {"label": 1, "data": {"text": "4-chloro-6-[(2,3-xylidine)-pirimidinylthio] acetic acid (WY-14,643), a specific ligand of the PPAR-alpha subtype, causes the most dramatic increase in UCP-3 mRNA, whereas troglitazone, a specific activator of PPAR-gamma, also significantly increases UCP-3 mRNA abundance in skeletal muscle of lactating mice.", "entity1": "PPAR-alpha", "entity2": "WY-14,643", "span1": [94, 104], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6585": {"label": 8, "data": {"text": "It is caused by a deficiency of propionyl-CoA carboxylase (PCC, EC 6.4.1.3), a biotin-dependent enzyme that catalyzes the carboxylation of propionyl-CoA to D-methylmalonyl-CoA.", "entity1": "EC 6.4.1.3", "entity2": "propionyl-CoA", "span1": [64, 74], "span2": [139, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"582": {"label": 3, "data": {"text": "Studies were carried out in vitro to evaluate downstream molecular alterations induced as a consequence of the potent and sustained inhibition of thymidylate synthase by Tomudex.", "entity1": "thymidylate synthase", "entity2": "Tomudex", "span1": [146, 166], "span2": [170, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7689": {"label": 8, "data": {"text": "The low-affinity sodium glucose cotransporter (SGLT2) is responsible for most of the glucose reabsorption in the kidney and has been highlighted as a novel therapeutic target for the treatment of diabetes.", "entity1": "sodium glucose cotransporter", "entity2": "glucose", "span1": [17, 45], "span2": [85, 92]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10211": {"label": 8, "data": {"text": "Direct transport of rifampicin could be shown for OATP-C (apparent K(m) value 13 micromol/L) and OATP8 (2.3 micromol/L).", "entity1": "OATP8", "entity2": "rifampicin", "span1": [97, 102], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10207": {"label": 8, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP8", "entity2": "BSP", "span1": [48, 53], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8444": {"label": 5, "data": {"text": "CONCLUSIONS: The sum of these preclinical data, the first of their kind applied to H3 antagonists, indicates that ABT-288 is unlikely to possess a high potential for abuse in the human population and suggests that H3 antagonists, as a class, are similar in this regard.", "entity1": "H3", "entity2": "ABT-288", "span1": [214, 216], "span2": [114, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4124": {"label": 0, "data": {"text": "Here, we identify a Zn\u00b2\u207a-driven N-terminal to C-terminal tertiary interaction in PrP(C).", "entity1": "PrP(C)", "entity2": "N", "span1": [81, 87], "span2": [32, 33]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6233": {"label": 1, "data": {"text": "However, [3H]eletriptan had over 6-fold higher affinity than [3H]sumatriptan at the 5-HT1D receptor (K(D)): 0.92 and 6.58 nM, respectively) and over 3-fold higher affinity than [3H]sumatriptan at the 5-HT1B receptor (K(D): 3.14 and 11.07 nM, respectively).", "entity1": "5-HT1D", "entity2": "[3H]sumatriptan", "span1": [84, 90], "span2": [61, 76]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3382": {"label": 6, "data": {"text": "Benzodiazepines (BDZs) depress neuronal excitability via positive allosteric modulation of inhibitory GABA(A) receptors (GABA(A)R).", "entity1": "GABA(A) receptors", "entity2": "Benzodiazepines", "span1": [102, 119], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"586": {"label": 3, "data": {"text": "The studies with dThyd rescue from cyclin E-cdk2 protein overexpression and growth inhibition by Tomudex indicate that increased cyclin E-cdk2 protein expression is associated with effective inhibition of thymidylate synthase and resultant dNTP pool imbalance.", "entity1": "cdk2", "entity2": "Tomudex", "span1": [44, 48], "span2": [97, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1563": {"label": 8, "data": {"text": "One of the enzymes responsible for the production of KA, kynurenine aminotransferase I (KATI), also catalyses the reversible transamination of glutamine to oxoglutaramic acid (GTK, EC 2.6.1.15).", "entity1": "KATI", "entity2": "glutamine", "span1": [88, 92], "span2": [143, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, 9]},
	"672": {"label": 0, "data": {"text": "The deduced amino acid sequence contains 779 amino acids, including a putative cGMP binding sequence in the amino-terminal portion of the molecule and a catalytic domain that is 16-47% identical in amino acid sequence to those of other PDE families.", "entity1": "PDE", "entity2": "amino acids", "span1": [236, 239], "span2": [45, 56]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4455": {"label": 0, "data": {"text": "Also, ROS from NADPH oxidase favors ERK1/2 activation that phosphorylates Stat3 in serine, resulting in a compensatory or adaptive survival response such as production of metallothionein-II in short Cd exposure times.", "entity1": "Stat3", "entity2": "serine", "span1": [74, 79], "span2": [83, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4649": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A2", "entity2": "TCDD", "span1": [11, 17], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"163": {"label": 3, "data": {"text": "Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex.", "entity1": "AChE", "entity2": "organophosphate", "span1": [22, 26], "span2": [45, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1194": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "aminopeptidase N", "entity2": "L-alanine", "span1": [170, 186], "span2": [156, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12475": {"label": 9, "data": {"text": "UGT2B10 was inactive in the glucuronidation of desipramine, nortriptyline, carbamazepine and afloqualone.", "entity1": "UGT2B10", "entity2": "afloqualone", "span1": [0, 7], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14549": {"label": 2, "data": {"text": "Also, reactive astrogliosis takes part of the early responses to the insult with (PhTe)(2), evidenced by upregulated GFAP in Western blot, PCR and immunofluorescence analysis.", "entity1": "GFAP", "entity2": "(PhTe)(2)", "span1": [117, 121], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11005": {"label": 1, "data": {"text": "In this study, antidepressants with selectivity for the noradrenaline transporter (reboxetine and desipramine), or the serotonin transporter (fluoxetine and clomipramine) were examined in terms of their ability to promote an anti-inflammatory cytokine phenotype in human blood.", "entity1": "serotonin transporter", "entity2": "clomipramine", "span1": [119, 140], "span2": [157, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"633": {"label": 3, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "Phospholipase A2", "entity2": "arachidonyl trifluoromethyl ketone", "span1": [0, 16], "span2": [56, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10879": {"label": 3, "data": {"text": "Irinotecan (CPT-11, 7-ethyl-10-[4-(1-piperidino)-1-piperidino] carbonyloxycamptothecin) has exhibited clinical activities against a broad spectrum of carcinomas by inhibiting DNA topoisomerase I (Topo I).", "entity1": "DNA topoisomerase I", "entity2": "Irinotecan", "span1": [175, 194], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14755": {"label": 1, "data": {"text": "Moreover, jaceosidin treatment resulted in phosphorylation of ERK, and pretreatment with the ERK inhibitor, PD98059, attenuated cell growth inhibition by jaceosidin.", "entity1": "ERK", "entity2": "jaceosidin", "span1": [62, 65], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15865": {"label": 1, "data": {"text": "These experiments show that in striatonigral projections, CaMKII\u03b1 inhibits the action of D3 receptors in a Ca(2+) dependent manner blocking their modulatory effects on GABA release.", "entity1": "CaMKII\u03b1", "entity2": "Ca(2+)", "span1": [58, 65], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11675": {"label": 1, "data": {"text": "The potential role of DAT as a target for AMPH and COC has been reviewed extensively.", "entity1": "DAT", "entity2": "COC", "span1": [22, 25], "span2": [51, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"653": {"label": 3, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "matrix metalloproteinase", "entity2": "batimastat", "span1": [46, 70], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5887": {"label": 1, "data": {"text": "The pyridoxal 5'-phosphate binding lysine in mouse ODC was identified as lysine 69 of the mouse sequence by reduction of the purified holoenzyme form with NaB[3H]4 followed by digestion of the carboxymethylated protein with endoproteinase Lys-C, radioactive peptide mapping using reversed-phase high pressure liquid chromatography and gas-phase peptide sequencing.", "entity1": "mouse ODC", "entity2": "pyridoxal 5'-phosphate", "span1": [45, 54], "span2": [4, 26]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6720": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "AG1296", "span1": [268, 272], "span2": [74, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7979": {"label": 1, "data": {"text": "These results indicate that neonatal diazinon exposure impaired the hippocampus-dependent novel object recognition ability, accompanied by a modulation in the expressions of the NMDA receptor and neurotrophin in young adult and adult mice.", "entity1": "NMDA receptor", "entity2": "diazinon", "span1": [178, 191], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5606": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "amisulpride", "span1": [59, 65], "span2": [200, 211]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14967": {"label": 3, "data": {"text": "The peptide YR-11 (YLEIEFSLKHR), obtained by direct substitution of cysteine with a serine residue in the template sequence, significantly (p<0.05) inhibited RANK-RANKL binding, and RANKL induced TRAP activity and formation of multinucleated osteoclasts without any cytotoxicity.", "entity1": "RANKL", "entity2": "YR-11", "span1": [182, 187], "span2": [12, 17]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15032": {"label": 3, "data": {"text": "Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1).", "entity1": "matrix metalloproteinase-1", "entity2": "methyl rosmarinate", "span1": [87, 113], "span2": [28, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8346": {"label": 8, "data": {"text": "Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine.", "entity1": "Histidine decarboxylase", "entity2": "histamine", "span1": [0, 23], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13931": {"label": 3, "data": {"text": "Both drugs at the tested doses (0.042-0.33 mug/kg) suppressed PTH mRNA expression and serum PTH effectively in the 5/6 NX rats, but paricalcitol was less potent in raising serum Ca than doxercalciferol.", "entity1": "PTH", "entity2": "doxercalciferol", "span1": [92, 95], "span2": [186, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8782": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "phospho-Akt", "entity2": "CAPE", "span1": [74, 85], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6771": {"label": 3, "data": {"text": "Hydralazine dose-dependently inhibited PHD activity and induced nonhydroxylated HIF-1alpha, evidence for HIF stabilization specifically by inhibition of PHD enzyme activity.", "entity1": "PHD", "entity2": "Hydralazine", "span1": [153, 156], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2551": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "BCR", "entity2": "imatinib mesylate", "span1": [119, 122], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12809": {"label": 3, "data": {"text": "However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50.", "entity1": "COX-2", "entity2": "flunixin", "span1": [76, 81], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"603": {"label": 3, "data": {"text": "Cyclopentenone prostaglandins were potent inhibitors of iNOS induction and were more effective than their precursors, prostaglandins E2 and D2.", "entity1": "iNOS", "entity2": "prostaglandins E2 and D2", "span1": [56, 60], "span2": [118, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12823": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "PLK", "entity2": "pyridoxal 5'-phosphate", "span1": [114, 117], "span2": [45, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5345": {"label": 2, "data": {"text": "Sphingosine-1-phosphate promotes the nuclear translocation of \u03b2-catenin and thereby induces osteoprotegerin gene expression in osteoblast-like cell lines.", "entity1": "osteoprotegerin", "entity2": "Sphingosine-1-phosphate", "span1": [92, 107], "span2": [0, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4261": {"label": 1, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "PARP", "entity2": "compound C", "span1": [91, 95], "span2": [27, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4694": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "V(5+)", "span1": [111, 117], "span2": [36, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1622": {"label": 3, "data": {"text": "The cytosine analog 5-aza-2'-deoxycytidine (decitabine) hypomethylates DNA by inhibiting DNA methyltransferase.", "entity1": "DNA methyltransferase", "entity2": "decitabine", "span1": [89, 110], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14949": {"label": 2, "data": {"text": "LPA1-induced cytoskeleton reorganization therefore makes a previously unrecognized but critically important contribution to the profibrotic activities of LPA by driving MRTF-dependent CTGF expression, which, in turn, drives fibroblast proliferation.-Sakai, N., Chun, J., Duffield, J. S., Wada, T., Luster, A. D., Tager, A. M. LPA1-induced cytoskeleton reorganization drives fibrosis through CTGF-dependent fibroblast proliferation.", "entity1": "CTGF", "entity2": "LPA", "span1": [184, 188], "span2": [154, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9164": {"label": 3, "data": {"text": "Inactivation of prostaglandin H synthase and prostacyclin synthase by phenylbutazone.", "entity1": "prostacyclin synthase", "entity2": "phenylbutazone", "span1": [45, 66], "span2": [70, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3558": {"label": 3, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "NF-\u03baB", "entity2": "pranlukast", "span1": [50, 55], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7024": {"label": 5, "data": {"text": "To mimic chronic selective serotonin reuptake inhibitor treatment and to block the inhibitory 5-HT(1A) autoreceptors, a 5-HT(1A) antagonist, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclo hexanecarboxamide maleate salt (WAY-100635) (0.3 mg/kg s.c.), was administered with DVS (30 mg/kg orally).", "entity1": "5-HT(1A)", "entity2": "N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclo hexanecarboxamide maleate salt", "span1": [120, 128], "span2": [141, 237]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8290": {"label": 3, "data": {"text": "Synthesis and biological evaluation of 1,3,4-thiadiazole analogues as novel AChE and BuChE inhibitors.", "entity1": "BuChE", "entity2": "1,3,4-thiadiazole", "span1": [85, 90], "span2": [39, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4980": {"label": 2, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bax", "entity2": "DZN", "span1": [151, 154], "span2": [245, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3470": {"label": 2, "data": {"text": "In addition, Silibinin caused an increase in p53 and p21 protein level as well as mRNA levels.", "entity1": "p53", "entity2": "Silibinin", "span1": [45, 48], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11887": {"label": 8, "data": {"text": "Ferredoxin 1 (FDX1; adrenodoxin) is an iron-sulfur protein that is involved in various metabolic processes, including steroid hormone synthesis in mammalian tissues.", "entity1": "Ferredoxin 1", "entity2": "steroid", "span1": [0, 12], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3687": {"label": 2, "data": {"text": "Insulin secretion stimulated by both 200 \u03bcM tolbutamide and 20 \u03bcM gliclazide, concentrations that had equivalent effects on membrane potential, was inhibited by thapsigargin (1 \u03bcM) or the L-type Ca(2+) channel blocker nicardipine (2 \u03bcM) and was potentiated by 8-pCPT-2'-O-Me-cAMP-AM at concentrations \u22652 \u03bcM in INS-1 cells.", "entity1": "Insulin", "entity2": "tolbutamide", "span1": [0, 7], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7453": {"label": 2, "data": {"text": "Ovariectomy downregulates glutaredoxin and renders female mice vulnerable to L-BOAA toxicity as evidenced by activation of AP1, loss of GSH and complex I activity indicating the important role of glutaredoxin in neuroprotection.", "entity1": "complex I", "entity2": "L-BOAA", "span1": [144, 153], "span2": [77, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11978": {"label": 0, "data": {"text": "We examined the specificity and initial sites of recruitment of Arf-dependent adaptors (AP-1 and GGAs) in response to the Golgi or endosomal localization of specific cargo proteins (furin, mannose-6-phosphate receptor (M6PR) and M6PR lacking a C-terminal domain M6PR\u0394C).", "entity1": "M6PR\u0394C", "entity2": "C", "span1": [262, 268], "span2": [244, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9153": {"label": 3, "data": {"text": "Inhibition of testicular LDH-X from laboratory animals and man by gossypol and its isomers.", "entity1": "LDH-X", "entity2": "gossypol", "span1": [25, 30], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1016": {"label": 1, "data": {"text": "In COS cells transfected with alpha(1b) adrenoceptor cDNA and in DDT(1) MF-2 cells which express native alpha(1B) adrenoceptors, [(3)H]-prazosin was displaced by unlabelled prazosin in a normal equilibrium process, with no prazosin paradox in concentrations up to 10(-6) M. In DDT(1) MF-2 cells, [(3)H]-prazosin was displaced likewise by a series of alpha(1) adrenergic agonists, none of which increased the binding of [(3)H]-prazosin.", "entity1": "alpha(1b) adrenoceptor", "entity2": "[(3)H]-prazosin", "span1": [30, 52], "span2": [129, 144]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12729": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "BuChE", "entity2": "ACh", "span1": [91, 96], "span2": [165, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"916": {"label": 5, "data": {"text": "Betaxolol, a beta(1)-adrenoceptor antagonist used for the treatment of glaucoma, is known to be neuroprotective in paradigms of ischaemia/excitotoxicity.", "entity1": "beta(1)-adrenoceptor", "entity2": "Betaxolol", "span1": [13, 33], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6141": {"label": 1, "data": {"text": "Moreover, the reverse mutation BEAG T432S increased the affinity of BEAG K+ channels for dofetilide, whereas C-type inactivation could not be recovered.", "entity1": "BEAG", "entity2": "dofetilide", "span1": [68, 72], "span2": [89, 99]}, "weak_labels": [-1, -1, 0, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4929": {"label": 1, "data": {"text": "Correlations between matrices made it possible to conclude that EROD activity in PBL should be considered as a sensitive, convenient and non-destructive approach for (i) evaluating EROD activity in liver, which was found to represent 98% of the observed EROD activities in the three tested matrices and (ii) evaluating oral exposure of homogeneous groups of farm animals (race, diet) to CYP inducing PAH and PHH.", "entity1": "CYP", "entity2": "PHH", "span1": [387, 390], "span2": [408, 411]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8022": {"label": 8, "data": {"text": "Dual function inhibitors targeting phospholipase A(2) (PLA(2)) and leukotriene A(4) hydrolase (LTA(4)H) may balance the arachidonic acid (AA) metabolic network and be used as new anti-inflammatory drugs.", "entity1": "leukotriene A(4) hydrolase", "entity2": "arachidonic acid", "span1": [67, 93], "span2": [120, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"560": {"label": 5, "data": {"text": "Both the 5 alpha-reductase inhibitor finasteride and alpha 1-adrenoceptor antagonists (e.g. alfuzosin, doxazosin, prazosin, tamsulosin and terazosin) have been recommended as appropriate treatment options for patients with lower urinary tract symptoms (LUTS) associated with benign prostatic obstruction (BPO), and their efficacy has been proven in several placebo-controlled trials.", "entity1": "alpha 1-adrenoceptor", "entity2": "terazosin", "span1": [53, 73], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7101": {"label": 8, "data": {"text": "We conclude that in the presence of proline, high POX activity is sufficient to induce mitochondria-mediated apoptosis.", "entity1": "POX", "entity2": "proline", "span1": [50, 53], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1589": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "acetylcholinesterase", "entity2": "4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline", "span1": [4, 24], "span2": [313, 374]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4274": {"label": 2, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "PARP", "entity2": "ursolic acid", "span1": [91, 95], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"489": {"label": 1, "data": {"text": "Conversely, opioid antagonists such as naloxone and naltrexone (which bind to non-selectively opioid receptors) have been shown to decrease alcohol consumption under various experimental conditions.", "entity1": "opioid receptors", "entity2": "naltrexone", "span1": [94, 110], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15852": {"label": 8, "data": {"text": "To confirm the role of each transporter, we analyzed HEK293 cells stably expressing human ABCA1 or ABCG1; we clearly observed 24-OHC efflux in the presence of HDL, whereas efflux in the presence of apolipoprotein A-I was marginal.", "entity1": "human ABCA1", "entity2": "24-OHC", "span1": [84, 95], "span2": [126, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7680": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "CA", "entity2": "ethoxzolamide", "span1": [113, 115], "span2": [238, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10927": {"label": 3, "data": {"text": "Using [(3)H]glucosamine-labeled gastric mucosal cells, we show that stimulatory effect of beta-adrenergic agonist, isoproterenol, on mucin secretion was inhibited by EGFR kinase inhibitor, PD153035, as well as wortmannin, a specific inhibitor of PI3K.", "entity1": "kinase", "entity2": "PD153035", "span1": [171, 177], "span2": [189, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"154": {"label": 5, "data": {"text": "Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs.", "entity1": "histamine H2-receptor", "entity2": "nizatidine", "span1": [35, 56], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14089": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "pomalidomide", "span1": [142, 146], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12933": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine gamma-lyase", "entity2": "L-Cys", "span1": [92, 117], "span2": [182, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15722": {"label": 1, "data": {"text": "Comparative study on transcriptional activity of 17 parabens mediated by estrogen receptor \u03b1 and \u03b2 and androgen receptor.", "entity1": "androgen receptor", "entity2": "parabens", "span1": [103, 120], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6016": {"label": 1, "data": {"text": "Emedastine (0.1%) failed to significantly attenuate either serotonin or platelet-activating-factor induced vascular permeability changes indicating high selectivity for the histamine H1 receptor.", "entity1": "histamine H1 receptor", "entity2": "Emedastine", "span1": [173, 194], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1578": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "[1,8]naphthyridines", "span1": [59, 64], "span2": [135, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11512": {"label": 8, "data": {"text": "Choline dehydrogenase (CHDH) and betaine-homocysteine methyltransferase (BHMT) are 2 enzymes involved in choline oxidation.", "entity1": "BHMT", "entity2": "choline", "span1": [73, 77], "span2": [105, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5285": {"label": 2, "data": {"text": "TCDD also caused a fast (within 30min as judged by the increase in its mRNA level) activation of cytosolic phospholipase A2 (cPLA2).", "entity1": "cytosolic phospholipase A2", "entity2": "TCDD", "span1": [97, 123], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13590": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "WY-46824", "span1": [6, 10], "span2": [245, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14800": {"label": 3, "data": {"text": "Human immortalized corneal fibroblasts were treated with TGF-\u03b2 in the presence of TSA, the NAD(P)H oxidase inhibitor diphenyleneiodonium (DPI), the antioxidant N-acetyl-cysteine (NAC), the NF-E2-related factor 2-antioxidant response element (Nrf2-ARE) activator sulforaphane, or small interfering RNA.", "entity1": "NAD(P)H oxidase", "entity2": "diphenyleneiodonium", "span1": [91, 106], "span2": [117, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5436": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "ScCA", "entity2": "cyanoacrylamide", "span1": [196, 200], "span2": [46, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13251": {"label": 1, "data": {"text": "Cytokines, lipopolysaccharides and other inflammatory mediators such as prostaglandin and leukotriene are related to the secretion and production of mucin.", "entity1": "mucin", "entity2": "leukotriene", "span1": [149, 154], "span2": [90, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6735": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "kinase", "entity2": "PKC412", "span1": [273, 279], "span2": [182, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2260": {"label": 4, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "nuclear pregnane X receptor", "entity2": "rifampicin", "span1": [70, 97], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"604": {"label": 3, "data": {"text": "In activated microglia, 15d-PGJ2 suppressed iNOS promoter activity, iNOS mRNA, and protein levels.", "entity1": "iNOS promoter", "entity2": "15d-PGJ2", "span1": [44, 57], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1083": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "edrophonium", "span1": [242, 262], "span2": [134, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11778": {"label": 3, "data": {"text": "There was no significant difference in TLR4, NF-\u03baB, and IL-27 mRNA and proteins between curcumin-treated and sulfasalazine-treated groups.", "entity1": "TLR4", "entity2": "curcumin", "span1": [39, 43], "span2": [88, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12689": {"label": 9, "data": {"text": "Olopatadine exerted no significant effects on action potential duration in isolated guinea pig ventricular myocytes, myocardium and human ether-a-go-go-related gene channel.", "entity1": "human ether-a-go-go-related gene channel", "entity2": "Olopatadine", "span1": [132, 172], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14430": {"label": 3, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C. Furthermore, the AMPK activator 5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) significantly inhibited ghrelin secretion.", "entity1": "ghrelin", "entity2": "AICAR", "span1": [286, 293], "span2": [255, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8579": {"label": 3, "data": {"text": "ATO inhibited the phosphorylation and activation of AKT and STAT3 through Notch signaling blockade.", "entity1": "AKT", "entity2": "ATO", "span1": [52, 55], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"628": {"label": 3, "data": {"text": "Inhibition > 90% of IL-2 secretion was observed at 1 microM BPB and 10 microM AACOCF3 compared to the respective vehicle control.", "entity1": "IL-2", "entity2": "AACOCF3", "span1": [20, 24], "span2": [78, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1261": {"label": 4, "data": {"text": "Injections of m-CPBG, a selective 5-HT3 receptor agonist, induced a significant increase in blood glucose in non-stressed rats in both fasted and in fed states.", "entity1": "5-HT3", "entity2": "m-CPBG", "span1": [34, 39], "span2": [14, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"205": {"label": 1, "data": {"text": "The affinities of a number of alpha 1-adrenoceptor antagonists were determined by displacement of [3H]-prazosin binding from cloned human alpha 1A-adrenoceptors (previously designated cloned alpha 1c subtype), alpha 1B alpha 1D and rat alpha 1D-adrenoceptors, stably expressed in rat-1 fibroblasts.", "entity1": "alpha 1-adrenoceptor", "entity2": "[3H]-prazosin", "span1": [30, 50], "span2": [98, 111]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1064": {"label": 3, "data": {"text": "Consistent with these locations, N-ethylmaleimide, an inhibitor of ACS4, inhibited ACS activity 47% in MAM and 28% in endoplasmic reticulum.", "entity1": "ACS4", "entity2": "N-ethylmaleimide", "span1": [67, 71], "span2": [33, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7943": {"label": 2, "data": {"text": "We show that the expression of PIM-1 is induced in response to estradiol in MCF-7 cells and that the induction is mediated by ER\u03b1-regulated enhancers located distally upstream from the gene.", "entity1": "PIM-1", "entity2": "estradiol", "span1": [31, 36], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3915": {"label": 3, "data": {"text": "(-)-6-(7-Methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one (KCA-1490) exhibits moderate dual PDE3/4-inhibitory activity and promises as a combined bronchodilatory/anti-inflammatory agent.", "entity1": "PDE3/4", "entity2": "(-)-6-(7-Methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one", "span1": [139, 145], "span2": [0, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5709": {"label": 3, "data": {"text": "Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17\u03b2-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.", "entity1": "AKR1C3", "entity2": "indomethacin", "span1": [81, 87], "span2": [36, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15778": {"label": 1, "data": {"text": "A series of aminopropylindenes, designed as mimics of a cationic high energy intermediate in the oxidosqualene cyclase(1) (OSC)-mediated cyclization of 2,3-oxidosqualen to lanosterol was prepared from Grundmann's ketone.", "entity1": "oxidosqualene cyclase(1)", "entity2": "aminopropylindenes", "span1": [97, 121], "span2": [12, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8859": {"label": 2, "data": {"text": "Indoxyl 3-sulfate stimulates Th17 differentiation enhancing phosphorylation of c-Src and STAT3 to worsen experimental autoimmune encephalomyelitis.", "entity1": "STAT3", "entity2": "Indoxyl 3-sulfate", "span1": [89, 94], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6043": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "SCH 23390", "span1": [63, 69], "span2": [157, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5695": {"label": 1, "data": {"text": "Apomorphine is a bimodal modulator of TRPA1 channels.", "entity1": "TRPA1", "entity2": "Apomorphine", "span1": [38, 43], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7249": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "PEA", "span1": [231, 237], "span2": [108, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3829": {"label": 3, "data": {"text": "In combination with clofarabine, the ability of resveratrol to reduce the contents of Sp1 and its target gene products was also evident in a time- and dose-dependent experiment.", "entity1": "Sp1", "entity2": "clofarabine", "span1": [86, 89], "span2": [20, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7259": {"label": 2, "data": {"text": "Finally, we showed that chlorate activated endocrine cell development by inducing neurogenin 3 (Neurog3) expression in early endocrine progenitor cells.", "entity1": "Neurog3", "entity2": "chlorate", "span1": [96, 103], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8517": {"label": 3, "data": {"text": "Synthesis of a DOTA (Gd(3+))-conjugate of proton-pump inhibitor pantoprazole for gastric wall imaging studies.", "entity1": "proton-pump", "entity2": "Gd(3+)", "span1": [42, 53], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1217": {"label": 1, "data": {"text": "In addition to affecting DAT function, MDMA rapidly decreased vesicular DA transport as assessed in striatal vesicles prepared from treated rats.", "entity1": "DAT", "entity2": "MDMA", "span1": [25, 28], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15802": {"label": 2, "data": {"text": "These results indicate that tBHQ suppresses body weight gain in mice, possibly at least related to the up-regulation of ACOX1 gene expression.", "entity1": "ACOX1", "entity2": "tBHQ", "span1": [120, 125], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5613": {"label": 3, "data": {"text": "We found that although inactivation facilitated cisapride block of the HERG K+ current, it was not coupled with cisapride block of HERG when the Cs+ current was recorded.", "entity1": "HERG", "entity2": "cisapride", "span1": [131, 135], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2427": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "NOS", "entity2": "L-arginine", "span1": [200, 203], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8117": {"label": 3, "data": {"text": "Both CE and E(2) alone increased DNA synthesis and reduced apoptosis with activation of MAPK, Akt, and p70S6K and up-regulation of antiapoptotic factors survivin, Bcl-2, and X-linked inhibitor of apoptosis protein, These effects could be completely blocked by BZA.", "entity1": "survivin", "entity2": "BZA", "span1": [153, 161], "span2": [260, 263]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14452": {"label": 2, "data": {"text": "We observed similar effects of Ag NPs on inflammatory mediator expression in vitro and in vivo with increase of interleukin-8 (IL-8)/macrophage inflammatory protein 2, IL-1RI, and tumor necrosis factor-\u03b1 expression in both models and increased IL-8 protein release in vitro.", "entity1": "macrophage inflammatory protein 2", "entity2": "Ag", "span1": [133, 166], "span2": [31, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9001": {"label": 4, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "5'-(N-cyclopropyl)-carboxamidoadenosine", "span1": [0, 9], "span2": [94, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8276": {"label": 8, "data": {"text": "This investigation tested the hypothesis that CYP2B6 is a prominent CYP isoform responsible for clinical methadone N-demethylation and clearance, using the in vivo mechanism-based CYP2B6 inhibitor ticlopidine, given orally for 4 days.", "entity1": "CYP2B6", "entity2": "methadone", "span1": [46, 52], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6078": {"label": 4, "data": {"text": "The specific binding is displaced by the selective 5-HT1D agonist sumatriptan but not by the mixed 5-HT1A/1D agonist 5-carboxyamidotryptamine.", "entity1": "5-HT1D", "entity2": "sumatriptan", "span1": [51, 57], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11991": {"label": 2, "data": {"text": "In this study, using reverse transcriptase PCR (RT-PCR) and ELISA, we showed that TCDD up-regulated the expression and secretion of tumor necrosis factor-alpha (TNF-\u03b1) in a time-dependent manner in cultured HAPI microglial cells.", "entity1": "TNF-\u03b1", "entity2": "TCDD", "span1": [161, 166], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4411": {"label": 6, "data": {"text": "Using cell-based assays and brain slice preparations, we characterized the interaction of a potent and efficacious mGlu5 PAM from the CPPHA series termed NCFP (N-(4-chloro-2-((4-fluoro-1,3-dioxoisoindolin-2-yl)methyl)phenyl)picolinamide).", "entity1": "mGlu5", "entity2": "CPPHA", "span1": [115, 120], "span2": [134, 139]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8314": {"label": 1, "data": {"text": "Despite the importance of UDP-glucuronosyltransferase (UGT) 1A1*28 in irinotecan pharmacogenetics, our capability to predict drug-induced severe toxicity remains limited.", "entity1": "UDP-glucuronosyltransferase (UGT) 1A1", "entity2": "irinotecan", "span1": [26, 63], "span2": [70, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3793": {"label": 3, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "FAS", "entity2": "Phillyrin", "span1": [71, 74], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14930": {"label": 1, "data": {"text": "Moreover, selective estrogen response modulators (SERMs) with diverse structures also regulate transcription of ER\u03b1 and ER\u03b2.", "entity1": "ER\u03b1", "entity2": "estrogen", "span1": [112, 115], "span2": [20, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4918": {"label": 3, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "catalase", "entity2": "kinsenoside", "span1": [193, 201], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14275": {"label": 8, "data": {"text": "We recently showed that TETA is metabolized in vitro by polyamine catabolic enzyme spermidine/spermine-N(1)-acetyltransferase (SSAT1) and by thialysine acetyltransferase (SSAT2) to its monoacetylated derivative (MAT).", "entity1": "spermidine/spermine-N(1)-acetyltransferase", "entity2": "polyamine", "span1": [83, 125], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"757": {"label": 5, "data": {"text": "Synthesis and antagonistic activity at muscarinic receptor subtypes of some 2-carbonyl derivatives of diphenidol.", "entity1": "muscarinic receptor", "entity2": "2-carbonyl", "span1": [39, 58], "span2": [76, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1557": {"label": 5, "data": {"text": "Kynurenic acid (KA) is an endogenous glutamate receptor antagonist at the level of the different ionotropic glutamate receptors.", "entity1": "ionotropic glutamate receptors", "entity2": "Kynurenic acid", "span1": [97, 127], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10377": {"label": 3, "data": {"text": "In this work a novel approach combining HPLC-UV on-line with oaTOF-MS and ICPMS was applied to investigate in human and rat plasma the metabolism of labelled BK (79/81 Br-Phe5) BrBK in the presence of two new dual ACE/NEP inhibitors (GW660511X and omapatrilat) currently under clinical trial.", "entity1": "NEP", "entity2": "GW660511X", "span1": [218, 221], "span2": [234, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4139": {"label": 2, "data": {"text": "Here, we have determined the molecular mechanism of this male-specific activation of the Kcnk1 gene and characterized KCNK1 as a phenobarbital-inducible antihyperplasia factor.", "entity1": "Kcnk1", "entity2": "phenobarbital", "span1": [89, 94], "span2": [129, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8519": {"label": 3, "data": {"text": "Second, EPSCs were recorded from rat hippocampal slices before and after their superfusion with the reversible AChE inhibitor donepezil (100nM).", "entity1": "AChE", "entity2": "donepezil", "span1": [111, 115], "span2": [126, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15194": {"label": 8, "data": {"text": "To evaluate to what extent the regional differences in expression of P-gp and P450 enzymes affect the absorption of a dual substrate, we investigated the transport of darunavir across different small intestinal segments (duodenum, proximal jejunum and ileum).", "entity1": "P-gp", "entity2": "darunavir", "span1": [69, 73], "span2": [167, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"1505": {"label": 4, "data": {"text": "RESULTS: DRF 2655 showed concentration-dependent transactivation of PPARalpha and PPARgamma.", "entity1": "PPARalpha", "entity2": "DRF 2655", "span1": [68, 77], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3929": {"label": 3, "data": {"text": "Western blot analysis revealed that OMT decreased the expression of Bax and repaired the balance of pro- and anti-apoptotic proteins.", "entity1": "Bax", "entity2": "OMT", "span1": [68, 71], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4523": {"label": 8, "data": {"text": "Carboxylesterases hydrolyze esters, amides, and thioesters to produce carboxylic acids and resulting alcohols, amines, and thiols, respectively.", "entity1": "Carboxylesterases", "entity2": "amides", "span1": [0, 17], "span2": [36, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4961": {"label": 2, "data": {"text": "Amprenavir-mediated PXR activation stimulated the expression of several key intestinal genes involved in lipid homeostasis.", "entity1": "PXR", "entity2": "Amprenavir", "span1": [20, 23], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14367": {"label": 1, "data": {"text": "Multifunctional targets of dietary polyphenols in disease: a case for the chemokine network and energy metabolism.", "entity1": "chemokine", "entity2": "polyphenols", "span1": [74, 83], "span2": [35, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1146": {"label": 3, "data": {"text": "The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.", "entity1": "tyrosine kinase", "entity2": "ZD1839", "span1": [4, 19], "span2": [30, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9399": {"label": 0, "data": {"text": "In Drosophila, glutamyl-prolyl-tRNA synthetase is a multifunctional synthetase encoded by a unique gene and composed of three domains: the amino- and carboxy-terminal domains catalyze the aminoacylation of glutamic acid and proline tRNA species, respectively, and the central domain is made of 75 amino acids repeated six times amongst which 46 are highly conserved and constitute the repeated motifs [Cerini, C., Kerjan, P., Astier, M., Gratecos, D., Mirande, M. & Semeriva, M. (1991) EMBO J.", "entity1": "glutamyl-prolyl-tRNA synthetase", "entity2": "glutamic acid", "span1": [15, 46], "span2": [206, 219]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10049": {"label": 0, "data": {"text": "We have previously isolated from human hemofiltrate an N-terminally truncated form of the hemofiltrate CC chemokine 1 (HCC-1), and characterized HCC-1[9-74] as a strong agonist of CCR1, CCR5, and to a lower extent CCR3.", "entity1": "HCC-1", "entity2": "N", "span1": [119, 124], "span2": [55, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11122": {"label": 1, "data": {"text": "Rec 15/2739, WB 4101, SL 89,0591, (+)- and (-)- tamsulosin showed selectivity for alpha 1A and alpha 1D adrenoceptors relative to the alpha 1B subtype.", "entity1": "alpha 1B subtype", "entity2": "SL 89,0591", "span1": [134, 150], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6724": {"label": 3, "data": {"text": "Compounds of several other structural families, including the quinoxaline AG1296, the bis(1H-2-indolyl)-1-methanone D-65476, the indolinones SU5416 and SU11248, the indolocarbazoles PKC412 and CEP-701, and the piperazonyl quinazoline CT53518, are potent inhibitors of Flt3 kinase.", "entity1": "Flt3", "entity2": "D-65476", "span1": [268, 272], "span2": [116, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11829": {"label": 3, "data": {"text": "To explore the molecular basis for CPT hypersensitivity in Top2\u03b2-deficient cells, we found that upon CPT exposure, the RNA polymerase II large subunit (RNAP LS) became progressively depleted, followed by recovery to nearly the original level in wild-type MEFs, whereas RNAP LS remained depleted without recovery in Top2\u03b2-deficient cells.", "entity1": "RNAP LS", "entity2": "CPT", "span1": [152, 159], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6892": {"label": 8, "data": {"text": "NPC1L1 could recently be identified as a major sterol transporter for the intestinal uptake of cholesterol as well as plant sterols.", "entity1": "sterol transporter", "entity2": "cholesterol", "span1": [47, 65], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1002": {"label": 0, "data": {"text": "Peptide sequences selected using MICA4 were rich in basic or hydroxyl-containing amino acids, and the surface of the GAD65 PLP-binding domain surrounding Lys358, which is known to be critical for MICA4 binding, was likewise rich in these amino acids.", "entity1": "GAD65 PLP-binding domain", "entity2": "amino acids", "span1": [117, 141], "span2": [81, 92]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"29": {"label": 3, "data": {"text": "Effectiveness of endopeptidase inhibition (candoxatril) in congestive heart failure.", "entity1": "endopeptidase", "entity2": "candoxatril", "span1": [17, 30], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2800": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "NK-1R", "entity2": "caerulein", "span1": [138, 143], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4037": {"label": 8, "data": {"text": "Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4).", "entity1": "Leukotriene A(4) hydrolase", "entity2": "LTA(4)", "span1": [0, 26], "span2": [114, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4749": {"label": 3, "data": {"text": "(S)-3-(Aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole (GSK2251052) is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase, and that has been in development for the treatment of serious Gram-negative infections.", "entity1": "bacterial leucyl tRNA synthetase", "entity2": "(S)-3-(Aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole", "span1": [147, 179], "span2": [0, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6376": {"label": 5, "data": {"text": "The nonselective opioid receptor partial agonist buprenorphine and the nonselective opioid receptor antagonist (-)-quadazocine exhibited pure antagonism at rat brain receptors, but displayed partial agonism at human ORL1 receptors.", "entity1": "opioid receptor", "entity2": "(-)-quadazocine", "span1": [84, 99], "span2": [111, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5958": {"label": 9, "data": {"text": "Loperamide modifies but does not block the corticotropin-releasing hormone-induced ACTH response in patients with Addison's disease.", "entity1": "ACTH", "entity2": "Loperamide", "span1": [83, 87], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3930": {"label": 3, "data": {"text": "Furthermore, OMT significantly reversed the up-regulation of NR2B and inhibited the calcium overload in the cultured neurons after challenging the NMDA.", "entity1": "NR2B", "entity2": "OMT", "span1": [61, 65], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8728": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "amitriptyline", "span1": [225, 231], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4213": {"label": 1, "data": {"text": "Mn was also shown to decrease DA uptake and amphetamine-induced DA efflux in DAT containing cells.", "entity1": "DAT", "entity2": "Mn", "span1": [77, 80], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4587": {"label": 1, "data": {"text": "The present review will consider the advantages and challenges associated with allosteric GPCR ligands, and examine how the particular properties of these ligands may be exploited to uncover the therapeutic potential for free fatty acid sensitive GPCRs.", "entity1": "GPCRs", "entity2": "fatty acid", "span1": [247, 252], "span2": [226, 236]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"6803": {"label": 9, "data": {"text": "Although celecoxib inhibits PG biosynthesis, most do not affect the peroxidase activity of COX, which can generate proximate carcinogens.", "entity1": "peroxidase", "entity2": "celecoxib", "span1": [68, 78], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"966": {"label": 9, "data": {"text": "Neither U50,488H nor etorphine caused down-regulation of the rat kappa-opioid receptor.", "entity1": "rat kappa-opioid receptor", "entity2": "etorphine", "span1": [61, 86], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11118": {"label": 1, "data": {"text": "Indoramin and SNAP 1069 showed selectivity for alpha 1A and alpha 1B adrenoceptors relative to the alpha 1D subtype.", "entity1": "alpha 1D subtype", "entity2": "Indoramin", "span1": [99, 115], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10217": {"label": 2, "data": {"text": "Metformin treatment for 10 weeks significantly increased AMPK alpha2 activity in the skeletal muscle, and this was associated with increased phosphorylation of AMPK on Thr172 and decreased acetyl-CoA carboxylase-2 activity.", "entity1": "AMPK", "entity2": "Metformin", "span1": [160, 164], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6546": {"label": 9, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "D950A", "entity2": "cilostazol", "span1": [15, 20], "span2": [196, 206]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"429": {"label": 5, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "SNAP 1069", "span1": [258, 286], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14869": {"label": 5, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "ER", "entity2": "ICI 182,780", "span1": [36, 38], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5734": {"label": 5, "data": {"text": "These protective effects were abolished by glucocorticoid receptor (GR) antagonist RU486 or p-ERK inhibitor U0126 rather than estrogen receptor \u03b1 antagonist ICI 82,780.", "entity1": "estrogen receptor \u03b1", "entity2": "ICI 82,780", "span1": [126, 145], "span2": [157, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10473": {"label": 5, "data": {"text": "Pretreatment with a combination of (+/-)-2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2 -yl]phenoxy]propyl]amino]ethoxy]-benzamide methanesulfonate (CGP20712A, a selective beta(1)-adrenoceptor antagonist) and (+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-buta nol hydrochloride (ICI-118,5511, a selective beta(2)-adrenoceptor antagonist) (0.1 microM for each) produced a 14-fold rightward shift of the concentration-response curve for (-)-isoprenaline; however, the relaxation in response to (+/-)-CGP12177A was unaffected by the blockade of beta(1)- and beta(2)-adrenoceptors.", "entity1": "beta(2)-adrenoceptor", "entity2": "ICI-118,5511", "span1": [365, 385], "span2": [339, 351]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11233": {"label": 4, "data": {"text": "These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug.", "entity1": "K(ATP) channel", "entity2": "mitiglinide", "span1": [149, 163], "span2": [182, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11073": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "caldesmon kinase", "entity2": "p-chloro", "span1": [110, 126], "span2": [234, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10273": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "transmembrane transporters", "entity2": "guanidine", "span1": [135, 161], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"3304": {"label": 3, "data": {"text": "A phase III randomized placebo-controlled trial has examined the impact of everolimus in patients with clear cell renal cancers and progressive disease on or within 6 months of the VEGFR tyrosine kinase inhibitors sunitinib and/or sorafenib.", "entity1": "tyrosine kinase", "entity2": "sunitinib", "span1": [187, 202], "span2": [214, 223]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12762": {"label": 1, "data": {"text": "This study compared the sedative profiles of the second-generation antihistamines, fexofenadine and cetirizine, using 3 different criteria: subjective sleepiness evaluated by the Stanford Sleepiness Scale, objective psychomotor tests (simple and choice reaction time tests and visual discrimination tests at 4 different exposure durations), and measurement of histamine H1-receptor occupancy (H1RO) in the brain.", "entity1": "histamine H1-receptor", "entity2": "antihistamines", "span1": [360, 381], "span2": [67, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14731": {"label": 1, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "StAR", "entity2": "Apocynin", "span1": [74, 78], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13934": {"label": 3, "data": {"text": "In pig parathyroid cells, paricalcitol and the active form of doxercalciferol induced VDR translocation from the cytoplasm into the nucleus, suppressed PTH mRNA expression and inhibited cell proliferation in a similar manner, although paricalcitol induced the expression of CaSR mRNA more effectively.", "entity1": "PTH", "entity2": "paricalcitol", "span1": [152, 155], "span2": [26, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4698": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "TCDD", "span1": [123, 129], "span2": [72, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4193": {"label": 2, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "p21", "entity2": "PTE", "span1": [303, 306], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10715": {"label": 2, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "c-fos", "entity2": "KA", "span1": [69, 74], "span2": [45, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10607": {"label": 1, "data": {"text": "These experimental results suggest that SV2A is the binding site of LEV in the brain and that LEV acts by modulating the function of SV2A, supporting previous indications that LEV possesses a mechanism of action distinct from that of other antiepileptic drugs.", "entity1": "SV2A", "entity2": "LEV", "span1": [40, 44], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13139": {"label": 2, "data": {"text": "Levels of mRNA encoding insulin 1, ICA512, and PC1/3 were increased in the pancreatic islets of GalN-treated rats.", "entity1": "insulin 1", "entity2": "GalN", "span1": [24, 33], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4449": {"label": 5, "data": {"text": "A novel class of quinoxalines has been discovered as antagonists of the IgG:FcRn protein-protein interaction through optimization of a hit derived from a virtual ligand-based screen.", "entity1": "IgG", "entity2": "quinoxalines", "span1": [72, 75], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6879": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "Cystathionine-gamma-lyase", "entity2": "H2S", "span1": [0, 25], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4740": {"label": 3, "data": {"text": "Genistin decreased myosin light chain kinase (MLCK) protein contents and MLCK mRNA expression in IJS, and inhibited both phosphorylation and Mg(2+)-ATPase activity of purified myosin, implicating that the decrease of MLCK contents and inhibition of MLCK activity are involved in the genistin-induced inhibitory effects.", "entity1": "myosin light chain kinase", "entity2": "Genistin", "span1": [19, 44], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14574": {"label": 8, "data": {"text": "The herbicide paraquat (PQ) is a P-gp substrate responsible for thousands of fatal intoxications worldwide that still lacks an effective antidote.", "entity1": "P-gp", "entity2": "paraquat", "span1": [33, 37], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8017": {"label": 3, "data": {"text": "In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A(2) (hnps-PLA(2)) and human leukotriene A(4) hydrolase (LTA(4)H-h) was found.", "entity1": "human nonpancreatic secretory phospholipase A(2)", "entity2": "JMC08-4", "span1": [136, 184], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3108": {"label": 8, "data": {"text": "In addition, tolvaptan is metabolized by the CYP3A4 system; thus physicians should be aware of the potential for increased interactions with other medications.", "entity1": "CYP3A4", "entity2": "tolvaptan", "span1": [45, 51], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10138": {"label": 3, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "COX", "entity2": "steroidal", "span1": [93, 96], "span2": [4, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2196": {"label": 1, "data": {"text": "We have elucidated the crystal structures of the cyanotoxins, motuporin (nodularin-V) and dihydromicrocystin-LA bound to human protein phosphatase-1c (gamma isoform).", "entity1": "human protein phosphatase-1c (gamma isoform)", "entity2": "motuporin", "span1": [121, 165], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3928": {"label": 3, "data": {"text": "OMT showed partial protection in the cortical neurons via down-regulation of NR2B containing NMDA receptors and up-regulation of Bcl-2 family.", "entity1": "NMDA receptors", "entity2": "OMT", "span1": [93, 107], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9450": {"label": 1, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP2", "entity2": "AH-13205", "span1": [90, 93], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15628": {"label": 3, "data": {"text": "Next, nobiletin significantly decreased the levels of phospho-ERK2 and phospho-Akt in ERK2 or Akt siRNA-transfected cells concomitantly with a marked reduction on cell invasion and migration.", "entity1": "ERK2", "entity2": "nobiletin", "span1": [86, 90], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"430": {"label": 5, "data": {"text": "(+)-Tamsulosin, (-)-tamsulosin, SL 89,0591, Rec 15/2739, SNAP 1069 and RS 17053 appeared to act as competitive antagonists of noradrenaline-mediated contractions of rat aorta yielding pA2 affinity estimates which were similar to binding affinities at cloned human alpha 1D adrenoceptors.", "entity1": "human alpha 1D adrenoceptors", "entity2": "RS 17053", "span1": [258, 286], "span2": [71, 79]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10647": {"label": 1, "data": {"text": "Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib).", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [99, 104], "span2": [145, 154]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9720": {"label": 3, "data": {"text": "This study confirms the feasibility of using continuous measurement of AChE activity in CSF over prolonged periods, that rivastigmine markedly inhibits CSF AChE after a single oral dose of 3 mg, and that the inhibition of central AChE is substantially greater than that of peripheral AChE or BuChE.", "entity1": "AChE", "entity2": "rivastigmine", "span1": [156, 160], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12685": {"label": 1, "data": {"text": "Different forms of therapy, potassium and magnesium substitution, spironolactone and indomethacin failed to fully correct hypokalemia and hypomagnesemia, but markedly improved growth velocity and normalized IGF-I levels in the three patients with short stature.", "entity1": "IGF-I", "entity2": "indomethacin", "span1": [207, 212], "span2": [85, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10119": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "cyclooxygenase-2", "entity2": "NS-389", "span1": [162, 178], "span2": [237, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6191": {"label": 5, "data": {"text": "These data indicate that mixed 5-HT1/5-HT2 receptor antagonists such as pizotifen and methysergide, and mixed 5-HT and catecholamine antagonists such as mianserin and mirtazapine are more potent antagonists of mCPP-induced behavioural inhibition in rats than the more selective 5-HT2A/5-HT2C antagonist ritanserin.", "entity1": "5-HT2", "entity2": "methysergide", "span1": [37, 42], "span2": [86, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6135": {"label": 0, "data": {"text": "To identify the molecular determinants for dofetilide block, we first engineered chimeras between HERG and BEAG and then used site-directed mutagenesis to localize single amino acid residues responsible for block.", "entity1": "HERG", "entity2": "amino acid", "span1": [98, 102], "span2": [171, 181]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11497": {"label": 3, "data": {"text": "RESULTS: Ketorolac was six times more active against COX-1 (IC(50) = 0.02 microM) than COX-2 (IC(50) = 0.12 microM) while bromfenac was approximately 32 times more active against COX-2 (IC(50) = 0.0066 microM) than COX-1 (IC(50) = 0.210 microM).", "entity1": "COX-1", "entity2": "bromfenac", "span1": [53, 58], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15138": {"label": 3, "data": {"text": "Cloning, Characterization, and Sulfonamide and Thiol Inhibition Studies of an \u03b1-Carbonic Anhydrase from Trypanosoma cruzi, the Causative Agent of Chagas Disease.", "entity1": "\u03b1-Carbonic Anhydrase", "entity2": "Sulfonamide", "span1": [78, 98], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13979": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Insig1", "entity2": "chlorcyclizine", "span1": [122, 128], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7696": {"label": 3, "data": {"text": "A PKC or MAP kinase inhibitor blocked the inhibitory effect of fenoldopam on insulin receptor expression, indicating that PKC and MAP kinase were involved in the signaling pathway.", "entity1": "insulin receptor", "entity2": "fenoldopam", "span1": [77, 93], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2384": {"label": 3, "data": {"text": "A novel class of biaryl urea that inhibits C-RAF kinase was discovered using a combination of medicinal and combinatorial chemistry approaches.", "entity1": "kinase", "entity2": "biaryl urea", "span1": [49, 55], "span2": [17, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"385": {"label": 9, "data": {"text": "The replacement of the conserved cysteine residues in e2 of CB2 by serine also eliminated CP 55,940 binding, but replacement of those in CB1 resulted in the sequestration of the mutated receptors in the cell cytoplasm.", "entity1": "CB2", "entity2": "CP 55,940", "span1": [60, 63], "span2": [90, 99]}, "weak_labels": [-1, 0, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7850": {"label": 1, "data": {"text": "Neuropeptide Y Y1 receptor knockdown can modify glutathione peroxidase and c-AMP response element-binding protein in phenylpropanolamine-treated rats.", "entity1": "glutathione peroxidase", "entity2": "phenylpropanolamine", "span1": [48, 70], "span2": [117, 136]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3344": {"label": 1, "data": {"text": "Dfbp-o also increased the affinity of cTnI for cTnC.", "entity1": "cTnI", "entity2": "Dfbp-o", "span1": [38, 42], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12795": {"label": 3, "data": {"text": "In a human whole blood assay, IC(50) values for lumiracoxib were 0.13 microM for COX-2 and 67 microM for COX-1 (COX-1/COX-2 selectivity ratio 515).", "entity1": "COX-1", "entity2": "lumiracoxib", "span1": [112, 117], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3281": {"label": 3, "data": {"text": "Assays examining the ability of TFP to block S100A4-mediated disassembly of myosin-IIA filaments demonstrate that significant inhibition of S100A4 function occurs only at TFP concentrations that promote S100A4 oligomerization.", "entity1": "S100A4", "entity2": "TFP", "span1": [140, 146], "span2": [171, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13329": {"label": 3, "data": {"text": "Sulfasalazine (also as a representative of the salicylates) inhibited the diabetes-induced upregulation of several inflammatory gene products, which are regulated by NF-kappaB, including vascular cell adhesion molecule, intracellular adhesion molecule-1, inducible nitric oxide synthase, and cyclooxygenase-2 in whole-retinal lysate.", "entity1": "NF-kappaB", "entity2": "salicylates", "span1": [166, 175], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15371": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "RARs", "entity2": "atRA", "span1": [221, 225], "span2": [107, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4955": {"label": 3, "data": {"text": "Fisetin treatment of preadipocytes reduced the phosphorylation of S6K1 and mTORC1 in a time- and concentration-dependent manner.", "entity1": "S6K1", "entity2": "Fisetin", "span1": [66, 70], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14874": {"label": 2, "data": {"text": "Reductions in striatal dopamine and tyrosine hydroxylase content were also less pronounced with EHT treatment.", "entity1": "tyrosine hydroxylase", "entity2": "EHT", "span1": [36, 56], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6867": {"label": 9, "data": {"text": "In contrast, caspase-8 activation and Bid truncation triggered by Jo2 were not diminished by minocycline pretreatment in mouse livers.", "entity1": "Bid", "entity2": "minocycline", "span1": [38, 41], "span2": [93, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8588": {"label": 3, "data": {"text": "In addition, fisetin supplementation significantly reduced hepatic mRNA abundance of FAS, ATPCL and G6Pase compared to the control group.", "entity1": "G6Pase", "entity2": "fisetin", "span1": [100, 106], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10183": {"label": 3, "data": {"text": "In complementary RNA (cRNA)-injected Xenopus laevis oocytes, rifamycin SV (10 micromol/L) cis-inhibited human organic anion transporting polypeptide C (SLC21A6) (OATP-C), human organic anion transporting polypeptide 8 (SLC21A8) (OATP8), human organic anion transporting polypeptide B (SLC21A9) (OATP-B), and human organic anion transporting polypeptide A (SLC21A3) (OATP-A) mediated BSP uptake by 69%, 79%, 89%, and 57%, respectively, as compared with uptake into control oocytes.", "entity1": "SLC21A9", "entity2": "rifamycin SV", "span1": [285, 292], "span2": [61, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7210": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "kinases", "entity2": "Cd", "span1": [127, 134], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12977": {"label": 6, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "protein kinase C", "entity2": "DAG", "span1": [56, 72], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"2261": {"label": 8, "data": {"text": "The concomitantly administered effects of rifampicin on other drugs can result in their altered metabolism or transportation that are metabolised by cytochromes P450 or transported by p-glycoprotein in the gastrointestinal tract and liver.", "entity1": "p-glycoprotein", "entity2": "rifampicin", "span1": [184, 198], "span2": [42, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1063": {"label": 2, "data": {"text": "Re-feeding normal chow or a high sucrose diet for 24 h after a 48-h fast increased both ACS1 and ACS4 protein expression 1.5-2.0-fold, consistent with inhibition studies.", "entity1": "ACS4", "entity2": "sucrose", "span1": [97, 101], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14554": {"label": 3, "data": {"text": "Synthesis, biological evaluation, and molecular modeling of glycyrrhizin derivatives as potent high-mobility group box-1 inhibitors with anti-heart-failure activity in vivo.", "entity1": "high-mobility group box-1", "entity2": "glycyrrhizin", "span1": [95, 120], "span2": [60, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10609": {"label": 1, "data": {"text": "Brain membranes and purified synaptic vesicles from mice lacking SV2A do not bind a tritiated LEV derivative, indicating that SV2A is necessary for LEV binding.", "entity1": "SV2A", "entity2": "LEV", "span1": [126, 130], "span2": [148, 151]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8050": {"label": 2, "data": {"text": "In this current study, paclitaxel was found to increase phosphorylation of mitogen-activated protein kinase (MAPK) kinase 3/6 (MKK3/6)-p38 MAPK as well as protein and mRNA levels of ERCC1 in H1650 and H1703 cells.", "entity1": "p38", "entity2": "paclitaxel", "span1": [135, 138], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"803": {"label": 2, "data": {"text": "Analysis of splice variants and site-directed mutants of the AMPA receptor GluR3 expressed in Xenopus oocytes has shown that lithium produces a large potentiation of the GluR3 flop splice variant and suggested that lithium might inhibit rapid desensitization, which is characteristic of this receptor (Karkanias, N. and Papke, R., Subtype-specific effects of lithium on glutamate receptor function.", "entity1": "GluR3 flop", "entity2": "lithium", "span1": [170, 180], "span2": [125, 132]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5174": {"label": 2, "data": {"text": "In PFC, DEX caused activation of AKT, augmentation of pro-survival Bcl-2 protein and enhanced Bcl-2/Bax protein ratio, as well Bcl-2 translocation to mitochondria.", "entity1": "Bcl-2", "entity2": "DEX", "span1": [67, 72], "span2": [8, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2154": {"label": 9, "data": {"text": "Thalidomide reduced COX-2 expression accompanied by a decrease of bcl-2 protein, TNFalpha, VEGF, GSH and an increased cytochrome c, but had no effect on that of COX-1, in MCF-7 and HL-60.", "entity1": "COX-1", "entity2": "Thalidomide", "span1": [161, 166], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8238": {"label": 5, "data": {"text": "However the \u03b17 receptor antagonist methyllycaconitine was unable to reverse these anxiety-like effects seen with PNU-282987.", "entity1": "\u03b17 receptor", "entity2": "methyllycaconitine", "span1": [12, 23], "span2": [35, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13379": {"label": 8, "data": {"text": "The expression of key genes important in methionine metabolism, such as methionine adenosyltransferase-1a, betaine-homocysteine methyltransferase and thioether S-methyltransferase, were suppressed.", "entity1": "thioether S-methyltransferase", "entity2": "methionine", "span1": [150, 179], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"375": {"label": 3, "data": {"text": "In conclusion, the production of IL-4 and IL-5 by T-cell clones (derived either from BAL or blood) was more sensitive to inhibition by DEX than that of IFN-gamma, which may account for the therapeutic effects of glucocorticosteroids in patients with asthma.", "entity1": "IL-4", "entity2": "DEX", "span1": [33, 37], "span2": [135, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5491": {"label": 8, "data": {"text": "Mechanisms that have been proposed for peroxidase-catalyzed iodination require the utilization of 1 mol of H2O2 for organic binding of 1 mol of iodide.", "entity1": "peroxidase", "entity2": "iodide", "span1": [39, 49], "span2": [144, 150]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2287": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "17-phenyl trinor PGE2", "span1": [19, 22], "span2": [96, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12241": {"label": 8, "data": {"text": "The carboxylation of glutamic acid residues to gamma-carboxyglutamic acid (Gla) by the vitamin K-dependent gamma-glutamyl carboxylase (gamma-carboxylase) is an essential posttranslational modification required for the biological activity of a number of proteins, including proteins involved in blood coagulation and its regulation.", "entity1": "vitamin K-dependent gamma-glutamyl carboxylase", "entity2": "Gla", "span1": [87, 133], "span2": [75, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7076": {"label": 1, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "thermoTRPs", "entity2": "cinnamaldehyde", "span1": [152, 162], "span2": [37, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15612": {"label": 1, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "nuclear factor-\u03baB", "entity2": "galangin", "span1": [156, 173], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1543": {"label": 8, "data": {"text": "Purified PAOh1/SMO oxidizes both spermine (K(m)=1.6 microM) and N(1)-acetylspermine (K(m)=51 microM), but does not oxidize spermidine.", "entity1": "PAOh1", "entity2": "spermine", "span1": [9, 14], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6472": {"label": 8, "data": {"text": "Diacylglycerol kinase (DGK) catalyzes the conversion of diacylglycerol to phosphatidic acid, making it an attractive candidate for a signal transduction component.", "entity1": "DGK", "entity2": "diacylglycerol", "span1": [23, 26], "span2": [56, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"6795": {"label": 3, "data": {"text": "Acarbose served as inhibitor of an interfering acid alpha-glucosidase present in neutrophils, which allowed the lysosomal enzyme implicated in Pompe disease to be selectively analyzed.", "entity1": "acid alpha-glucosidase", "entity2": "Acarbose", "span1": [47, 69], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1882": {"label": 1, "data": {"text": "OBJECTIVE: Ziprasidone is an atypical antipsychotic drug that shows a higher affinity for serotonin 5-HT(2) receptors compared with dopamine D(2) receptors in vitro.", "entity1": "5-HT(2) receptors", "entity2": "Ziprasidone", "span1": [100, 117], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9264": {"label": 3, "data": {"text": "Ergovaline inhibition of radioligand binding to the D2 dopamine receptor and ergot alkaloid inhibition of vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production in GH4ZR7 cells, stably transfected with a rat D2 dopamine receptor, were evaluated.", "entity1": "vasoactive intestinal peptide", "entity2": "ergot alkaloid", "span1": [106, 135], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15121": {"label": 2, "data": {"text": "Notably, the antioxidant Trolox\u2122 reversed the Mn (20\u00a0mg/kg)-dependent augmentation in p38(MAPK) phosphorylation and reduced the Mn (20\u00a0mg/kg)-induced caspase activity and F(2)-isoprostane production.", "entity1": "p38", "entity2": "Mn", "span1": [86, 89], "span2": [46, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"5751": {"label": 3, "data": {"text": "We observed a significant reduction in CSE induced luciferase expression, NF-\u03baB DNA binding, I-\u03baB\u03b5 degradation and c-Rel nuclear translocation in cells pretreated with vitamin C.", "entity1": "NF-\u03baB", "entity2": "vitamin C", "span1": [74, 79], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13343": {"label": 3, "data": {"text": "We found that simvastatin abolishes anti-CD11a mAb-induced increases in lymphocytic cholinergic activity in a manner independent of its cholesterol-lowering activity.", "entity1": "CD11a", "entity2": "simvastatin", "span1": [41, 46], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14663": {"label": 1, "data": {"text": "Phytoestrogen genistein protects against endothelial barrier dysfunction in vascular endothelial cells through PKA-mediated suppression of RhoA signaling.", "entity1": "RhoA", "entity2": "genistein", "span1": [139, 143], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"397": {"label": 1, "data": {"text": "The pharmacologic properties of fluticasone propionate-including high lipophilicity, high selectivity and affinity for the glucocorticoid receptor, low systemic absorption, and rapid metabolism and clearance-combine to give fluticasone propionate a high therapeutic index.", "entity1": "glucocorticoid receptor", "entity2": "fluticasone propionate", "span1": [123, 146], "span2": [32, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5178": {"label": 8, "data": {"text": "Accordingly, loss of pip5k1\u03b2 function in FRDA cells was accompanied by decreased PI(4,5)P2 levels and was shown instrumental for destabilization of the actin network and delayed cell spreading.", "entity1": "pip5k1\u03b2", "entity2": "PI(4,5)P2", "span1": [21, 28], "span2": [81, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5554": {"label": 3, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "GR", "entity2": "BCNU", "span1": [63, 65], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1915": {"label": 8, "data": {"text": "bis(Ethyl) oligoamine analogues of polyamines, such as SL-11144 and SL-11158, as well as arylamine analogues [BW-1, a bis(phenylbenzyl) 3-7-3 analogue] blocked uptake and interconversion of spermine at micromolar levels and, in the case of BW-1, acted as substrate for PAO.", "entity1": "PAO", "entity2": "BW-1", "span1": [269, 272], "span2": [240, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 8, -1]},
	"7215": {"label": 2, "data": {"text": "Cd also increased ERK1/2, Akt and PDGFRalpha phosphorylation while ICI blocked it.", "entity1": "PDGFRalpha", "entity2": "Cd", "span1": [34, 44], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"88": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "EC 1.14.16.1", "entity2": "adrenaline", "span1": [139, 151], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7363": {"label": 1, "data": {"text": "CREB-dependent gene transcription, which may underlie long-lasting drug-induced changes in behavior and the subjective effects of cocaine, varies depending on the stage of drug exposure or withdrawal and the cell population involved.", "entity1": "CREB", "entity2": "cocaine", "span1": [0, 4], "span2": [130, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13301": {"label": 3, "data": {"text": "We investigated the efficacy of sorafenib at inhibiting mutants of the receptor tyrosine kinases PDGFRbeta, KIT, and FLT3, which are implicated in the pathogenesis of myeloid malignancies.", "entity1": "FLT3", "entity2": "sorafenib", "span1": [117, 121], "span2": [32, 41]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10912": {"label": 9, "data": {"text": "The inhibition of ERK, moreover, did not cause attenuation in mucin secretion in response to cAMP and forskolin.", "entity1": "mucin", "entity2": "cAMP", "span1": [62, 67], "span2": [93, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4914": {"label": 3, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "lactic dehydrogenase", "entity2": "kinsenoside", "span1": [133, 153], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12672": {"label": 8, "data": {"text": "The physiological role of NKCC1-mediated Cl- uptake remains to be determined.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [26, 31], "span2": [41, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2517": {"label": 3, "data": {"text": "Our results demonstrated that auranofin suppressed TLR4-mediated activation of transcription factors, NF-kappaB and IRF3, and expression of COX-2, a pro-inflammatory enzyme.", "entity1": "NF-kappaB", "entity2": "auranofin", "span1": [102, 111], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12579": {"label": 0, "data": {"text": "PC3 is a type I proinsulin-processing enzyme that initiates the sequential processing of proinsulin to insulin by cleaving the proinsulin molecule on the COOH-terminal side of the dibasic peptide, Arg31-Arg32, joining the B-chain and C-peptide.", "entity1": "proinsulin", "entity2": "COOH", "span1": [89, 99], "span2": [154, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4691": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1a2", "entity2": "V(5+)", "span1": [111, 117], "span2": [20, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3226": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "ellagic acid", "span1": [248, 261], "span2": [175, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12640": {"label": 1, "data": {"text": "The sulfonylurea glibenclamide caused release of prebound 8-azido-[alpha-32P]ATP from SUR1 in the presence of MgADP or MgATP in a concentration-dependent manner.", "entity1": "SUR1", "entity2": "MgADP", "span1": [86, 90], "span2": [110, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8124": {"label": 2, "data": {"text": "The reduction of BiFC signal mediated by nutlin-3 was correlated with an increase in Puma transactivation, PARP cleavage, and cell death.", "entity1": "PARP", "entity2": "nutlin-3", "span1": [107, 111], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14100": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "DNA damage binding protein-1", "entity2": "lenalidomide", "span1": [147, 175], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5171": {"label": 1, "data": {"text": "Results of RT-PCR analysis showed decrease of p53 mRNA level and no significant difference in Bcl-2 and Bax mRNA expressions in DEX-treated rats.", "entity1": "Bax", "entity2": "DEX", "span1": [104, 107], "span2": [128, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15215": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "tumor necrosis factor-\u03b1", "entity2": "methanol", "span1": [340, 363], "span2": [59, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4879": {"label": 1, "data": {"text": "Recruitment of Creb1-Mecp2 by glut3-(m)CpG contributes towards transactivation, formulating an escape from (m)CpG-induced gene suppression, and thereby promoting developmental neuronal glut3 gene transcription and expression.", "entity1": "glut3", "entity2": "(m)CpG", "span1": [30, 35], "span2": [36, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12997": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "delta 14 reductase", "entity2": "amorolfine", "span1": [142, 160], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14901": {"label": 8, "data": {"text": "FMO3 overexpression in mice significantly increases plasma TMAO levels while silencing FMO3 decreases TMAO levels.", "entity1": "FMO3", "entity2": "TMAO", "span1": [87, 91], "span2": [102, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13981": {"label": 5, "data": {"text": "BACKGROUND: The effects of histamine H1 antagonist chlorcyclizine on rat palate development were characterized following in utero exposure.", "entity1": "histamine H1", "entity2": "chlorcyclizine", "span1": [27, 39], "span2": [51, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13401": {"label": 2, "data": {"text": "Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration.", "entity1": "AMP-activated protein kinase", "entity2": "phenformin", "span1": [34, 62], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5508": {"label": 4, "data": {"text": "In pigeons trained to discriminate 1.7 mg/kg dezocine from saline, a series of opioids with activity at the mu opioid receptor substituted completely for the dezocine stimulus with a rank order of potency similar to that obtained in other assays sensitive to the effects of mu agonists (i.e., fentanyl >[-]-cyclazocine >buprenorphine = butorphanol >l-methadone >nalbuphine >[-]-metazocine >morphine).", "entity1": "mu opioid receptor", "entity2": "l-methadone", "span1": [108, 126], "span2": [349, 360]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9495": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "acetylprocainamide", "span1": [28, 42], "span2": [52, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3535": {"label": 2, "data": {"text": "2-Deoxyglucose increased phosphorylation of tuberous sclerosis complex 2 (TSC2) on AMPK consensus sites but did not change the amount of TSC1 bound to TSC2.", "entity1": "TSC2", "entity2": "2-Deoxyglucose", "span1": [74, 78], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4939": {"label": 3, "data": {"text": "Moreover, protein and mRNA levels of DSS-induced proinflammatory cytokines in colon, including TNF-\u03b1, IL-1\u03b2, IL-18, IL-17A and IFN-\u03b3, were markedly suppressed by Fc11a-2.", "entity1": "TNF-\u03b1", "entity2": "Fc11a-2", "span1": [95, 100], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7879": {"label": 3, "data": {"text": "Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors.", "entity1": "protease", "entity2": "LPV", "span1": [15, 23], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12996": {"label": 1, "data": {"text": "The phenylmorpholines, of which amorolfine is the sole representative in human therapy, affect two targets in the ergosterol pathway: Erg24p (delta 14 reductase) and Erg2p (delta 8-delta 7 isomerase).", "entity1": "Erg24p", "entity2": "amorolfine", "span1": [134, 140], "span2": [32, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14539": {"label": 3, "data": {"text": "Catalpol inhibits LPS plus IFN-\u03b3-induced inflammatory response in astrocytes primary cultures.", "entity1": "IFN-\u03b3", "entity2": "Catalpol", "span1": [27, 32], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5546": {"label": 2, "data": {"text": "Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice.", "entity1": "Galpha(o)", "entity2": "Methamphetamine", "span1": [76, 85], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4759": {"label": 3, "data": {"text": "The expression of regucalcin is stimulated through the action of insulin in liver cells in vitro and in vivo and it is decreased in the liver of rats with type I diabetes induced by streptozotocin administration in vivo.", "entity1": "regucalcin", "entity2": "streptozotocin", "span1": [18, 28], "span2": [182, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6166": {"label": 3, "data": {"text": "A low tyramine diet is recommended if selegiline is used together with nonselective MAO inhibitors or the selective, reversible MAO-A inhibitor, moclobemide.", "entity1": "MAO", "entity2": "selegiline", "span1": [84, 87], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2293": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "SC-51089", "span1": [258, 261], "span2": [221, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8456": {"label": 3, "data": {"text": "Hinokitiol inhibited the phosphorylation of phospholipase C (PLC)\u03b32, protein kinase C (PKC), mitogen-activated protein kinases (MAPKs), and Akt in collagen-activated human platelets, and significantly reduced intracellular calcium mobilization and hydroxyl radical (OH) formation.", "entity1": "phospholipase C (PLC)\u03b32", "entity2": "Hinokitiol", "span1": [44, 67], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6253": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "human serotonin transporter", "entity2": "ziprasidone", "span1": [58, 85], "span2": [142, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4208": {"label": 1, "data": {"text": "In HepG2 cells, GCs induced a decreased expression of FXR and SHP, and inhibited the regulatory effect of GW4064 on FXR-target genes.", "entity1": "FXR", "entity2": "GW4064", "span1": [116, 119], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9704": {"label": 3, "data": {"text": "The nonselective and irreversible MAO inhibitors, phenelzine (3-10 mg/kg), tranylcypromine (1-3 mg/kg), and nialamide (30 mg/kg), decreased rates of responding maintained by ethanol reinforcement.", "entity1": "MAO", "entity2": "nialamide", "span1": [34, 37], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4549": {"label": 8, "data": {"text": "Given these findings, a unified PK model including the inhibition of MAO-A- and CYP2D6-catalyzed 5-MeO-DMT metabolism by harmaline was developed to describe blood harmaline, 5-MeO-DMT, and bufotenine PK profiles in both wild-type and Tg-CYP2D6 mouse models.", "entity1": "CYP2D6", "entity2": "5-MeO-DMT", "span1": [80, 86], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6381": {"label": 3, "data": {"text": "Thymidylate synthase is inhibited by 5-fluorodeoxyuridine monophosphate, forming an inactive ternary complex with intracellular folate.", "entity1": "Thymidylate synthase", "entity2": "5-fluorodeoxyuridine monophosphate", "span1": [0, 20], "span2": [37, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8993": {"label": 1, "data": {"text": "Adenosine agonists and antagonists dose dependently accentuated and attenuated, respectively, ethanol-induced motor incoordination, thereby suggesting a central mechanism of adenosine modulation of this effect of ethanol and confirmed our previous reports in which adenosine agonists and antagonists were given i.p.", "entity1": "adenosine", "entity2": "ethanol", "span1": [174, 183], "span2": [213, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15168": {"label": 2, "data": {"text": "GnRH stimulation of CREB phosphorylation (pCREB) in the gonadotrope-derived L\u03b2T2 cell line was attenuated by a protein kinase A (PKA) inhibitor, H89.", "entity1": "CREB", "entity2": "GnRH", "span1": [20, 24], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1559": {"label": 5, "data": {"text": "Kynurenic acid (KA) is an endogenous glutamate receptor antagonist at the level of the different ionotropic glutamate receptors.", "entity1": "ionotropic glutamate receptors", "entity2": "KA", "span1": [97, 127], "span2": [16, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14245": {"label": 8, "data": {"text": "Disruption of microtubule prevented insulin-induced actin remodeling and distal insulin signal transduction, with reduction in surface glucose transporter isoform 4 (GLUT4) and glucose uptake.", "entity1": "GLUT4", "entity2": "glucose", "span1": [166, 171], "span2": [177, 184]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12243": {"label": 8, "data": {"text": "The carboxylation of glutamic acid residues to gamma-carboxyglutamic acid (Gla) by the vitamin K-dependent gamma-glutamyl carboxylase (gamma-carboxylase) is an essential posttranslational modification required for the biological activity of a number of proteins, including proteins involved in blood coagulation and its regulation.", "entity1": "vitamin K-dependent gamma-glutamyl carboxylase", "entity2": "glutamic acid", "span1": [87, 133], "span2": [21, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6857": {"label": 1, "data": {"text": "Bosentan also decreased serum glucose level without any effect on insulin secretion in mild diabetic rats and potentiated the hypoglycemic action of insulin.", "entity1": "insulin", "entity2": "Bosentan", "span1": [149, 156], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7970": {"label": 2, "data": {"text": "Diet, physical exercise and Orlistat administration increase serum Anti-M\u00fcllerian Hormone (AMH) levels in women with polycystic ovary syndrome (PCOS).", "entity1": "Anti-M\u00fcllerian Hormone", "entity2": "Orlistat", "span1": [67, 89], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6669": {"label": 8, "data": {"text": "Ribonucleotide reductase (RR) is responsible for the de novo conversion of the ribonucleoside diphosphates to deoxyribonucleoside diphosphates, which are essential for DNA synthesis and repair.", "entity1": "RR", "entity2": "deoxyribonucleoside diphosphates", "span1": [26, 28], "span2": [110, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4219": {"label": 2, "data": {"text": "The data indicated that PhIP could cause stomach injury, oxidative stress in rat stomachs as well as the activation of c-fos and c-jun and inactivation of p16, which may play a role in the pathogenesis of PhIP-associated stomach cancer.", "entity1": "c-jun", "entity2": "PhIP", "span1": [129, 134], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1475": {"label": 1, "data": {"text": "Eprosartan acts at vascular AT(1) receptors (postsynaptically) and at presynaptic AT(1) receptors, where it inhibits sympathetically stimulated noradrenaline release.", "entity1": "AT(1) receptors", "entity2": "Eprosartan", "span1": [28, 43], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3162": {"label": 0, "data": {"text": "Cellular mechanisms of insulin resistance: role of stress-regulated serine kinases and insulin receptor substrates (IRS) serine phosphorylation.", "entity1": "insulin receptor substrates", "entity2": "serine", "span1": [87, 114], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14417": {"label": 1, "data": {"text": "Our results show that Metformin directly inhibits stomach ghrelin production and secretion through AMPK.", "entity1": "AMPK", "entity2": "Metformin", "span1": [99, 103], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15399": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-1\u03b2", "entity2": "7-ketosterols", "span1": [64, 69], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"182": {"label": 2, "data": {"text": "The activation may be accelerated by an acute inflammatory process provoked by oleate, which is supported by such clinical manifestations as mild fever, retrosternal pain leukocytosis and an increase in plasma fibrinogen level which was observed in all during the period.", "entity1": "fibrinogen", "entity2": "oleate", "span1": [210, 220], "span2": [79, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14680": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "2C9", "entity2": "GSK1292263", "span1": [100, 103], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8192": {"label": 0, "data": {"text": "We found that SIRT1 induced p300 down-regulation via the ubiquitin-proteasome pathway by deacetylation of lysine residues for ubiquitination.", "entity1": "ubiquitin", "entity2": "lysine", "span1": [57, 66], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8768": {"label": 5, "data": {"text": "Of note, SB265610 which is a close structural analogue of SB225002 with a potent IL-8RB antagonistic activity did not exhibit a similar antimitotic activity.", "entity1": "IL-8RB", "entity2": "SB265610", "span1": [81, 87], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5287": {"label": 2, "data": {"text": "However, Ca(2+) blockers also obviously attenuated NF-\u03baB activation and transnuclear transport induced by TCDD.", "entity1": "NF-\u03baB", "entity2": "TCDD", "span1": [51, 56], "span2": [106, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6264": {"label": 1, "data": {"text": "A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study.", "entity1": "TPA", "entity2": "argatroban", "span1": [105, 108], "span2": [35, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10742": {"label": 3, "data": {"text": "The compounds 5'-azacytidine (AZC) and procainamide (PCA) belong to inhibitors of DNMT1, whose low activity correlates with increase in transcription of various genes.", "entity1": "DNMT1", "entity2": "procainamide", "span1": [82, 87], "span2": [39, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15245": {"label": 8, "data": {"text": "In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17\u03b2-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated.", "entity1": "OATP1B1", "entity2": "estradiol-17\u03b2-glucuronide", "span1": [30, 37], "span2": [60, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6519": {"label": 3, "data": {"text": "We tested the new orally active nonpeptidic renin inhibitor SPP100 (Aliskiren, an octanamide with a 50% inhibitory concentration [IC50] in the low nanomolar range) in 18 healthy volunteers on a constant 100 mmol/d sodium diet using a double-blind, 3-way crossover protocol.", "entity1": "renin", "entity2": "Aliskiren", "span1": [44, 49], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9496": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "dibucaine", "span1": [28, 42], "span2": [72, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15204": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "TNF- \u03b1", "entity2": "buthanol", "span1": [365, 371], "span2": [16, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3263": {"label": 3, "data": {"text": "TAS-102 is a novel drug containing trifluorothymidine, which is phosphorylated by TK-1 to its active monophosphated form, that in turn can inhibit TS.", "entity1": "TS", "entity2": "TAS-102", "span1": [147, 149], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"884": {"label": 3, "data": {"text": "Flutamide, an effective competitive inhibitor of the androgen receptor used orally for palliative treatment of prostatic carcinoma and regulation of prostatic hyperplasia was evaluated for its genotoxic effects in the intact rat and in primary cultures of human hepatocytes.", "entity1": "androgen receptor", "entity2": "Flutamide", "span1": [53, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8213": {"label": 3, "data": {"text": "TAA also increased the numbers of ED2(+), cyclooxygenase-2(+), and heme oxygenase-1(+) liver cells, as well as the number of CD3(+) lymphocytes.", "entity1": "cyclooxygenase-2", "entity2": "TAA", "span1": [42, 58], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6821": {"label": 2, "data": {"text": "Based on HMG-CoA reductase inhibition, pitavastatin-induced apoA-I more efficiently than simvastatin and atorvastatin.", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [60, 66], "span2": [39, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13408": {"label": 5, "data": {"text": "It is currently not known how much this H(1) antagonism of clozapine contributes to the therapeutic or adverse side effects of clozapine.", "entity1": "H(1)", "entity2": "clozapine", "span1": [40, 44], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7694": {"label": 3, "data": {"text": "The inhibitory effect of fenoldopam on insulin-mediated VSMC proliferation was receptor specific, because its effect could be blocked by SCH23390, a D1-like receptor antagonist.", "entity1": "insulin", "entity2": "fenoldopam", "span1": [39, 46], "span2": [25, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14878": {"label": 3, "data": {"text": "Additionally, in SH-SY5Y cells, MPP(+)-induced demethylation of phosphoprotein phosphatase 2A (PP2A), the master regulator of the cellular phosphoregulatory network, and cytotoxicity were ameliorated by EHT.", "entity1": "PP2A", "entity2": "MPP(+)", "span1": [95, 99], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14492": {"label": 8, "data": {"text": "The obtained results indicate that rat brain CYP2D isoforms catalyze the formation of serotonin from 5-methoxytryptamine, and that the deficit or genetic defect of CYP2D may affect serotonin metabolism in the brain.", "entity1": "rat brain CYP2D", "entity2": "5-methoxytryptamine", "span1": [35, 50], "span2": [101, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2237": {"label": 3, "data": {"text": "Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis.", "entity1": "KIT", "entity2": "Dasatinib", "span1": [32, 35], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3702": {"label": 2, "data": {"text": "In addition, the number and area of glutathione S-transferase placental form (GST-P) positive foci and proliferating cell nuclear antigen (PCNA) positive cell ratios in the hepatocytes were significantly increased in the male and female rats that were administered 100mg/kg MEG compared with the control animals.", "entity1": "GST-P", "entity2": "MEG", "span1": [78, 83], "span2": [274, 277]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15261": {"label": 3, "data": {"text": "Further investigation demonstrated that 8k reduced H2O2-induced activation of mitochondrial apoptosis by inhibiting the expression of Bax and elevating the expression of Bcl-2.", "entity1": "Bcl-2", "entity2": "H2O2", "span1": [170, 175], "span2": [51, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3120": {"label": 8, "data": {"text": "ATP-binding cassette transporter A1 is involved in hepatic alpha-tocopherol secretion.", "entity1": "ATP-binding cassette transporter A1", "entity2": "alpha-tocopherol", "span1": [0, 35], "span2": [59, 75]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6701": {"label": 5, "data": {"text": "Known VR1 antagonists (BCTC, thio-BCTC and capsazepine) were also able to block the response of TRPM8 to menthol (IC(50): 0.8+/-1.0, 3.5+/-1.1 and 18+/-1.1 microM, respectively).", "entity1": "VR1", "entity2": "capsazepine", "span1": [6, 9], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14879": {"label": 3, "data": {"text": "The neuroinflammatory response to MPTP was markedly attenuated, and indices of oxidative stress and JNK activation were significantly prevented with EHT.", "entity1": "JNK", "entity2": "EHT", "span1": [100, 103], "span2": [149, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1423": {"label": 9, "data": {"text": "In addition, escitalopram has negligible effects on cytochrome P450 drug-metabolising enzymes in vitro, suggesting a low potential for drug-drug interactions.", "entity1": "cytochrome P450", "entity2": "escitalopram", "span1": [52, 67], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2846": {"label": 0, "data": {"text": "The cAspAT TZD-responsive site was restricted to a single AGGACA hexanucleotide located at -381 to -376 bp whose mutation impaired the specific RORalpha binding.", "entity1": "cAspAT", "entity2": "AGGACA", "span1": [4, 10], "span2": [58, 64]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12092": {"label": 8, "data": {"text": "The results suggest that most of the HVA in plasma is derived from deamination of DA by MAO-A in peripheral neurons; that DOPAC in plasma is derived from cells outside the central nervous system; that DHPG in plasma is derived virtually exclusively from the metabolism of norepinephrine in sympathetic nerve endings and that residual levels of HVA after treatment with debrisoquin provide an improved but limited indication of central dopaminergic activity.", "entity1": "MAO-A", "entity2": "DA", "span1": [88, 93], "span2": [82, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13793": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "SU101", "span1": [14, 16], "span2": [267, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3874": {"label": 2, "data": {"text": "Western blots showed a decrease in nuclear p65 protein expression after exposure to different concentrations of cinobufagin, while the phosphorylation of GSK-3\u03b2 was simultaneously increased.", "entity1": "GSK-3\u03b2", "entity2": "cinobufagin", "span1": [154, 160], "span2": [112, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16073": {"label": 3, "data": {"text": "Ibrutinib (Imbruvica(R)) is a first-in-class, potent, orally administered, covalent inhibitor of Bruton's tyrosine kinase (BTK) that inhibits B-cell antigen receptor signalling downstream of BTK.", "entity1": "BTK", "entity2": "Imbruvica(R)", "span1": [123, 126], "span2": [11, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12883": {"label": 3, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "phosphoserine", "span1": [14, 20], "span2": [146, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"13615": {"label": 3, "data": {"text": "Sorafenib and sunitinib are synthetic, orally active agents shown to directly inhibit vascular endothelial growth factor receptors -2 and -3 (VEGFR-2, VEGFR-3) and platelet-derived growth factor receptor beta (PDGFR-beta), while temsirolimus is an mTOR inhibitor.", "entity1": "platelet-derived growth factor receptor beta", "entity2": "sunitinib", "span1": [164, 208], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11577": {"label": 1, "data": {"text": "A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors.", "entity1": "tyrosine kinase", "entity2": "imatinib", "span1": [8, 23], "span2": [49, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1105": {"label": 3, "data": {"text": "Carvedilol reduced mortality and heart failure in patients with higher pre-treatment plasma N-BNP and adrenomedullin.", "entity1": "adrenomedullin", "entity2": "Carvedilol", "span1": [102, 116], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11513": {"label": 1, "data": {"text": "FK778, is a synthetic malononitrilamide that targets the critical enzyme of the de novo pyrimidine synthesis, dihydroorotic acid dehydrogenase, and receptor-associated tyrosine kinases has completed phase II trials.", "entity1": "dihydroorotic acid dehydrogenase", "entity2": "FK778", "span1": [110, 142], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5631": {"label": 1, "data": {"text": "AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C.", "entity1": "AMP-activated protein kinase", "entity2": "compound C", "span1": [0, 28], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15936": {"label": 1, "data": {"text": "Vildagliptin+metformin were more effective than placebo+metformin in reducing body weight and BMI, glycemic control, HOMA-IR, glucagon and insulin resistance measurements.", "entity1": "glucagon", "entity2": "metformin", "span1": [126, 134], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14214": {"label": 6, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "codeine", "span1": [193, 198], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14057": {"label": 3, "data": {"text": "CONCLUSIONS: Aspirin is an inhibitor of mTOR and an activator of AMPK, targeting regulators of intracellular energy homeostasis and metabolism.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [40, 44], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15793": {"label": 8, "data": {"text": "Consistent with two glucose uptake pathways, induced uptake of 2-NBDG, a fluorescent glucose derivative, was decreased by inhibition of HCs or glucose transporter (GLUT4), and blocked by dual blockade.", "entity1": "glucose transporter", "entity2": "glucose", "span1": [143, 162], "span2": [20, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10950": {"label": 8, "data": {"text": "Because l-lactate reduced to 67% of the nicotinate uptake even at 10mM, it is unlikely that nicotinate uptake in rat astrocytes is mediated by MCT1 and/or MCT2.", "entity1": "MCT2", "entity2": "nicotinate", "span1": [155, 159], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12976": {"label": 6, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "PKC", "entity2": "Diacylglycerol", "span1": [74, 77], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"1648": {"label": 3, "data": {"text": "These results suggest that clomipramine induces hyperglycemia in mice by blocking the 5-HT(2B )and/or 5-HT(2C) receptors, which results in facilitation of adrenaline release.", "entity1": "5-HT(2C)", "entity2": "clomipramine", "span1": [102, 110], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1510": {"label": 3, "data": {"text": "With the use of sildenafil, it has been clearly, clinically demonstrated that the selective inhibition of PDE5 is an appropriate, effective, safe method for the treatment of ED of all aetiologies and severities.", "entity1": "PDE5", "entity2": "sildenafil", "span1": [106, 110], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13732": {"label": 2, "data": {"text": "Nicotinic acid (NA), a widely used drug to lower elevated plasma lipid levels, induced NNMT enzyme activity in white adipose tissue of mice.", "entity1": "NNMT", "entity2": "Nicotinic acid", "span1": [87, 91], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15381": {"label": 8, "data": {"text": "The human cytosolic sulfotransferase hSULT2A1 catalyzes the sulfation of a broad range of xenobiotics, as well as endogenous hydroxysteroids and bile acids.", "entity1": "human cytosolic sulfotransferase hSULT2A1", "entity2": "bile acids", "span1": [4, 45], "span2": [145, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"92": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "phenylalanine 4-monooxygenase", "entity2": "noradrenaline", "span1": [81, 110], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13658": {"label": 1, "data": {"text": "The binding of U46619 to the PGIS protein was demonstrated by 1D NMR titration, and the significant perturbation of the chemical shifts of protons at C-11, H2C, and H20 of U46619 were observed upon U46619 binding to the engineered PGIS in a concentration-dependent manner.", "entity1": "PGIS", "entity2": "U46619", "span1": [231, 235], "span2": [198, 204]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3924": {"label": 3, "data": {"text": "Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group facilitates both enhancement of PDE4-inhibitory activity and restoration of potent PDE3 inhibition.", "entity1": "PDE3", "entity2": "N", "span1": [166, 170], "span2": [69, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7500": {"label": 1, "data": {"text": "Additional pharmacological effects evoked by AICAR and phenformin on I(ouabain), with potential secondary effects on apical Na+ conductance, ENaC activity and monolayer resistance, have important consequences for their use as pharmacological activators of AMPK in cell systems where Na+K+ATPase is an important component.", "entity1": "ENaC", "entity2": "AICAR", "span1": [141, 145], "span2": [45, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5441": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "\u03b2-carbonic anhydrase", "entity2": "tyrphostine", "span1": [127, 147], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10657": {"label": 8, "data": {"text": "The discovery of a second isoform of cyclooxygenase (COX) led to the search for compounds that could selectively inhibit COX-2 in humans while sparing prostaglandin formation from COX-1.", "entity1": "COX-1", "entity2": "prostaglandin", "span1": [180, 185], "span2": [151, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7268": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "dorzolamide", "span1": [218, 224], "span2": [104, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3587": {"label": 1, "data": {"text": "Wogonoside also suppressed the activation of mammalian target of rapamycin (mTOR) and p70-S6 kinase (p70S6K) by regulating the expression of the extracellular signal-regulated kinase (ERK1/2) and p38 involved mitogen-activated protein kinase (MAPK) signaling pathway.", "entity1": "MAPK", "entity2": "Wogonoside", "span1": [243, 247], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12262": {"label": 8, "data": {"text": "LTC4 synthase (LTC4S), the pivotal enzyme for the biosynthesis of LTC4 (ref.", "entity1": "LTC4S", "entity2": "LTC4", "span1": [15, 20], "span2": [66, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2109": {"label": 1, "data": {"text": "On the basis of FIP1L1-PDGFRa fusion gene hypereosinophilic syndrome would be classified as a clonal disease and in the FIP1L1-PDGFRa positive cases the tyrosine kinase inhibitor imatinib mesylate (Glivec) would be effective.", "entity1": "PDGFRa", "entity2": "imatinib mesylate", "span1": [127, 133], "span2": [179, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3648": {"label": 1, "data": {"text": "PC12 cell apoptosis induced by DBDCT was confirmed by annexin V/propidium iodide staining, and characterized by cleavage of caspase-9 and caspase-3 proteins.", "entity1": "caspase-3", "entity2": "DBDCT", "span1": [138, 147], "span2": [31, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"524": {"label": 1, "data": {"text": "Together, our findings suggest the critical role of 'Rac and subsequent activation of phospholipase A2' in ceramide-signalling to nucleus.", "entity1": "Rac", "entity2": "ceramide", "span1": [53, 56], "span2": [107, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14243": {"label": 0, "data": {"text": "Though microtubule mediated actin remodeling through PKC\u03b6, reorganization of microtubule depended on tyrosine phosphorylation of insulin receptor, the mechanism is different from insulin-induced actin remodeling, which relied on the activity of PI3-kinase and PKC\u03b6.", "entity1": "insulin receptor", "entity2": "tyrosine", "span1": [129, 145], "span2": [101, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1250": {"label": 3, "data": {"text": "The effects of theophylline (unspecific PDE inhibitor), vinpocetine (PDE1 inhibitor), EHNA (PDE2 inhibitor) and the PDE5 inhibitors zaprinast and E 4021 were weak.", "entity1": "PDE", "entity2": "theophylline", "span1": [40, 43], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2712": {"label": 2, "data": {"text": "There was also an increase in c-kit, Trio, Rho-A, Rac-3, EGFR, Notch-4, Dvl-2, Ezrin, beta catenin and mutant p53 protein expression in the parathion-treated cells.", "entity1": "Dvl-2", "entity2": "parathion", "span1": [72, 77], "span2": [140, 149]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12767": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "5-fluorouracil", "span1": [0, 20], "span2": [64, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10017": {"label": 5, "data": {"text": "The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist.", "entity1": "5-HT3 receptors", "entity2": "AS-8112", "span1": [80, 95], "span2": [43, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3196": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "metalloenzyme", "entity2": "p-coumaric acid", "span1": [248, 261], "span2": [87, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15621": {"label": 3, "data": {"text": "The inhibitory effect of galangin on theses pro-inflammatory cytokines was related with c-Jun N-terminal kinases, and p38 mitogen-activated protein kinase, nuclear factor-\u03baB, and caspase-1.", "entity1": "cytokines", "entity2": "galangin", "span1": [61, 70], "span2": [25, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8175": {"label": 1, "data": {"text": "These results demonstrate that the incoming nucleotide is unable to induce a syn-8-oxoG conformation without minor groove DNA polymerase interactions that influence templating (anti-/syn-equilibrium) of 8-oxoG while modulating fidelity.", "entity1": "minor groove", "entity2": "syn-8-oxoG", "span1": [109, 121], "span2": [77, 87]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15574": {"label": 1, "data": {"text": "Our results revealed an important role of base excision repair (BER) as the ntg1, ntg2, apn1 and apn2 mutants showed pronounced sensitivity to essential oil and nerolidol.", "entity1": "ntg1", "entity2": "nerolidol", "span1": [76, 80], "span2": [161, 170]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6823": {"label": 3, "data": {"text": "Further study revealed that pitavastatin increased ABCA1 mRNA in HMG-CoA reductase-dependent manner and that Rho and Rho kinase inhibitor (C3T and Y27632) increased apoA-I production in the HepG2 cells.", "entity1": "Rho", "entity2": "Y27632", "span1": [109, 112], "span2": [147, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11486": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "COX", "entity2": "bromfenac", "span1": [42, 45], "span2": [196, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5847": {"label": 3, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT3", "entity2": "cisapride", "span1": [96, 101], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14910": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO3", "entity2": "choline", "span1": [71, 75], "span2": [144, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"548": {"label": 1, "data": {"text": "The selective 5-HT reuptake inhibitors paroxetine, indalpine and fluvoxamine displayed a high affinity for the 5-HT transporter, whereas the norepinephrine reuptake inhibitor desipramine had a high affinity for the norepinephrine transporter.", "entity1": "norepinephrine transporter", "entity2": "desipramine", "span1": [215, 241], "span2": [175, 186]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13977": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Fgfr2", "entity2": "chlorcyclizine", "span1": [105, 110], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2565": {"label": 2, "data": {"text": "Brain tissue analyses revealed that neonatal quinpirole treatment produced a significant decrease in hippocampal NGF, BDNF and ChAT that was eliminated by olanzapine treatment.", "entity1": "NGF", "entity2": "olanzapine", "span1": [113, 116], "span2": [155, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1139": {"label": 1, "data": {"text": "Significant differences were observed in a different region (loop B93-B101), that we identified as binding site of amiloride to the tissue plasminogen activator (tPA).", "entity1": "tPA", "entity2": "amiloride", "span1": [162, 165], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4249": {"label": 2, "data": {"text": "Butein also increased heme oxygenase-1 (HO-1) protein expression and HO activity.", "entity1": "HO-1", "entity2": "Butein", "span1": [40, 44], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13229": {"label": 1, "data": {"text": "Our results suggest that glutamate induces GRIP1 degradation by proteasome through an NMDA receptor-Ca2+ pathway and that GRIP1 degradation may play an important role in regulating GluR2 surface expression.", "entity1": "proteasome", "entity2": "glutamate", "span1": [64, 74], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7052": {"label": 3, "data": {"text": "We evaluated imatinib, a tyrosine kinase inhibitor currently used to treat chronic myelogenous leukemia and gastrointestinal stromal tumors, as a potential drug for systemic treatment of MTC, in 2 MTC-derived cell lines expressing multiple endocrine neoplasia-associated mutant RET receptors.", "entity1": "tyrosine kinase", "entity2": "imatinib", "span1": [25, 40], "span2": [13, 21]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7034": {"label": 2, "data": {"text": "Further, cholesterol metabolites, predominantly the oxysterols, the natural ligands for liver X receptor (LXR), induced these genes via upregulation of sterol regulatory element binding protein-1c (SREBP-1c) that bound to the regulatory regions of these genes.", "entity1": "sterol regulatory element binding protein-1c", "entity2": "oxysterols", "span1": [152, 196], "span2": [52, 62]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14401": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "insulin", "entity2": "nucleotide", "span1": [334, 341], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14392": {"label": 3, "data": {"text": "NFD abrogated EGF-induced phosphorylation of EGF receptor (EGFR) and phosphatidylinositol 3-kinase (PI3K)/Akt.", "entity1": "EGF receptor", "entity2": "NFD", "span1": [45, 57], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9598": {"label": 3, "data": {"text": "Here we present the crystal structure of the dimeric catalytic domain (residues 117-424) of human phenylalanine hydroxylase (hPheOH), cocrystallized with various potent and well-known catechol inhibitors and refined at a resolution of 2.0 A.", "entity1": "hPheOH", "entity2": "catechol", "span1": [125, 131], "span2": [184, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12240": {"label": 8, "data": {"text": "The carboxylation of glutamic acid residues to gamma-carboxyglutamic acid (Gla) by the vitamin K-dependent gamma-glutamyl carboxylase (gamma-carboxylase) is an essential posttranslational modification required for the biological activity of a number of proteins, including proteins involved in blood coagulation and its regulation.", "entity1": "gamma-carboxylase", "entity2": "gamma-carboxyglutamic acid", "span1": [135, 152], "span2": [47, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"891": {"label": 1, "data": {"text": "Here we compared the action of N(5)-substituted derivatives on recombinant rat neuronal nitric oxide synthase with their effects on dihydropteridine reductase (EC 1.6.99.7) and phenylalanine hydroxylase (EC 1.14.16.1),the well-studied classical H(4)biopterin-dependent reactions.", "entity1": "EC 1.6.99.7", "entity2": "N(5)", "span1": [160, 171], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8835": {"label": 3, "data": {"text": "RESULTS: By Western blot analysis of spinal cord tissues, we have demonstrated that treatment with bioactive RS -GRA significantly decreased nuclear factor (NF)-kB translocation, pro-inflammatory cytokine production such as interleukin-1\u03b2 (IL-1\u03b2), and apoptosis (Bax and caspase 3 expression).", "entity1": "nuclear factor (NF)-kB", "entity2": "RS -GRA", "span1": [141, 163], "span2": [109, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4772": {"label": 3, "data": {"text": "These results suggested that DMBT could inhibit invasion and angiogenesis by downregulation of VEGFand MMP-9, resulting from the inhibition of Akt pathway.", "entity1": "MMP-9", "entity2": "DMBT", "span1": [103, 108], "span2": [29, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4672": {"label": 8, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "SIRT1", "entity2": "superoxide", "span1": [14, 19], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6602": {"label": 3, "data": {"text": "OBJECTIVE: Because of these physiological effects and the widespread use of the selective COX-2 inhibitor, celecoxib, we wanted to determine if inhibition of COX-2 would affect incisional skin wound healing.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [90, 95], "span2": [107, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5297": {"label": 0, "data": {"text": "These results support the hypothesis that apoplastic amino acids acting through heteromeric GLR3.2/GLR3.4 channels affect lateral root development via Ca(2+) signaling in the phloem.", "entity1": "GLR3.4", "entity2": "amino acids", "span1": [99, 105], "span2": [53, 64]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1273": {"label": 1, "data": {"text": "We describe the function of BH4 in aromatic amino acid hydroxylation, and discuss the allosteric and structural effects that BH4 exerts on NOS.", "entity1": "NOS", "entity2": "BH4", "span1": [139, 142], "span2": [125, 128]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"13398": {"label": 2, "data": {"text": "In hearts treated with metformin, [AMP] was increased at 50 min and AMPK activity, phosphorylated AMPK, and phosphorylated acetyl-CoA carboxylase were elevated at 61 min.", "entity1": "AMPK", "entity2": "metformin", "span1": [98, 102], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7532": {"label": 8, "data": {"text": "10), is an 18-kDa integral nuclear membrane protein that belongs to a superfamily of membrane-associated proteins in eicosanoid and glutathione metabolism that includes 5-lipoxygenase-activating protein, microsomal glutathione S-transferases (MGSTs), and microsomal prostaglandin E synthase 1 (ref.", "entity1": "microsomal glutathione S-transferases", "entity2": "eicosanoid", "span1": [204, 241], "span2": [117, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"361": {"label": 9, "data": {"text": "GCS therapy results in reduced mRNA expression of interleukin-4 (IL-4) and IL-5 in cells from bronchoalveolar lavage (BAL) but not of IFN-gamma.", "entity1": "IFN-gamma", "entity2": "GCS", "span1": [134, 143], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11412": {"label": 3, "data": {"text": "Treatment with carvedilol is associated with a reversal of abnormal regulation of HIF-1alpha and VEGF in the failing ventricular myocardium.", "entity1": "VEGF", "entity2": "carvedilol", "span1": [97, 101], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5408": {"label": 2, "data": {"text": "Type I deiodinase, liver fatty-acid binding protein and cytochrome P450 (CYP) 3A37 mRNA levels were significantly induced by TCPP, while TDCPP induced CYP3A37 and CYP2H1.", "entity1": "liver fatty-acid binding protein", "entity2": "TCPP", "span1": [19, 51], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9806": {"label": 8, "data": {"text": "Mitochondrially-bound dihydroorotate dehydrogenase (EC 1.3.99.11) catalyzes the fourth sequential step in the de novo synthesis of uridine monophosphate.", "entity1": "dihydroorotate dehydrogenase", "entity2": "uridine monophosphate", "span1": [22, 50], "span2": [131, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7240": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "POHA", "span1": [192, 229], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12352": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPV1", "entity2": "apomorphine", "span1": [19, 25], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10984": {"label": 3, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "beta(2)-adrenoceptor", "entity2": "phorbol 12-myristate 13-acetate", "span1": [225, 245], "span2": [68, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2879": {"label": 3, "data": {"text": "Miglustat, a small iminosugar molecule approved for the treatment of Gaucher disease, reversibly inhibits glucosylceramide synthase, which catalyses the first committed step in glycosphingolipid synthesis.", "entity1": "glucosylceramide synthase", "entity2": "Miglustat", "span1": [106, 131], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6620": {"label": 0, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "Cys", "span1": [3, 9], "span2": [88, 91]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4060": {"label": 9, "data": {"text": "Jaspamide also inhibited other channels including Cav1.2, Cav3.2, and HCN2; however, the Kv11.1 (hERG) channel was minimally affected.", "entity1": "hERG", "entity2": "Jaspamide", "span1": [97, 101], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"460": {"label": 1, "data": {"text": "The influence of (+/-)-tamsulosin, a selective alpha 1A-adrenoceptor antagonist, on the positive inotropic effect and the accumulation of inositol phosphates that are induced via alpha 1-adrenoceptors was studied in comparison with that of another alpha 1A-adrenoceptor ligand oxymetazoline in the rabbit ventricular myocardium.", "entity1": "alpha 1A-adrenoceptor", "entity2": "oxymetazoline", "span1": [248, 269], "span2": [277, 290]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7517": {"label": 2, "data": {"text": "KEY RESULTS: Phenformin, AICAR and metformin increased AMPK (alpha1) activity and decreased I(amiloride).", "entity1": "AMPK (alpha1)", "entity2": "metformin", "span1": [55, 68], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15956": {"label": 1, "data": {"text": "In addition, inhibitors for EGFR or ERK1/2 remarkably suppressed OHT-induced truncation of cyclin E, suggesting involvement of EGFR signaling.", "entity1": "cyclin E", "entity2": "OHT", "span1": [91, 99], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10570": {"label": 4, "data": {"text": "To verify the hypothesis that the non-conventional partial agonist (-)-CGP12177 binds at two beta(1)-adrenoceptor sites, human beta(1)-adrenoceptors, expressed in CHO cells, were labelled with (-)-[(3)H]-CGP12177.", "entity1": "human beta(1)-adrenoceptors", "entity2": "(-)-CGP12177", "span1": [121, 148], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8160": {"label": 3, "data": {"text": "DPEP inhibited LPS-induced phosphorylation of ERK, JNK, and p38.", "entity1": "JNK", "entity2": "DPEP", "span1": [51, 54], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3781": {"label": 1, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "SREBP-1c", "entity2": "Phillyrin", "span1": [147, 155], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10047": {"label": 3, "data": {"text": "Fenofibrate and GW2331 induced expression of acyl-coenzyme A (CoA) oxidase and enoyl-CoA hydratase and reduced apolipoprotein C-III and phosphoenolpyruvate carboxykinase mRNAs.", "entity1": "phosphoenolpyruvate carboxykinase", "entity2": "GW2331", "span1": [136, 169], "span2": [16, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7201": {"label": 9, "data": {"text": "Cd decreased ERalpha expression, but not ERbeta.", "entity1": "ERbeta", "entity2": "Cd", "span1": [41, 47], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8464": {"label": 3, "data": {"text": "In conclusion, hinokitiol may inhibit platelet activation by inhibiting the PLC\u03b32-PKC cascade and hydroxyl radical formation, followed by suppressing the activation of MAPKs and Akt.", "entity1": "PLC\u03b32", "entity2": "hinokitiol", "span1": [76, 81], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"748": {"label": 1, "data": {"text": "The inhibitory effect of endothelin-1 on the contraction induced by 5-HT is abolished by deendothelialization, by the endothelin ET(B) receptor antagonist RES 701-1, by indomethacin, or by glibenclamide.", "entity1": "endothelin-1", "entity2": "RES 701-1", "span1": [25, 37], "span2": [155, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3578": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u.", "entity1": "pIR", "entity2": "MSG", "span1": [53, 56], "span2": [97, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11334": {"label": 1, "data": {"text": "Antitumor activity of TAS-102 appears to be associated with TK, tumor growth and TS.", "entity1": "TS", "entity2": "TAS-102", "span1": [81, 83], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9882": {"label": 5, "data": {"text": "We examined the effect of JTH-601 (3- inverted question markN-[2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethyl]-N-methylaminom ethyl inverted question mark-4-methoxy-2,5,6-trimethylphenol hemifumarate), a new alpha(1L)-adrenoceptor antagonist, on prostatic function in isolated canine prostate and in anesthetized dogs.", "entity1": "alpha(1L)-adrenoceptor", "entity2": "4-methoxy-2,5,6-trimethylphenol hemifumarate", "span1": [208, 230], "span2": [155, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"282": {"label": 4, "data": {"text": "The aim of the present study was to evaluate the cardiac effects of the beta 3-adrenoceptor agonist BRL35135, and determine whether beta 3-receptors are involved in mediating chronotropic or inotropic responses in man.", "entity1": "beta 3-adrenoceptor", "entity2": "BRL35135", "span1": [72, 91], "span2": [100, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15401": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-10", "entity2": "7-ketosterols", "span1": [77, 82], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"4041": {"label": 3, "data": {"text": "In addition, we found that neoechinulin A significantly suppressed the production of neurotoxic inflammatory mediator tumour necrosis factor-\u03b1 (TNF-\u03b1), interleukin-1\u03b2 (IL-1\u03b2), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) in activated BV-2 cells.", "entity1": "IL-1\u03b2", "entity2": "neoechinulin A", "span1": [168, 173], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12951": {"label": 3, "data": {"text": "BG also showed a protective effect in the presence of a DNA polymerase beta inhibitor (cytosine arabinoside-3-phosphate, Ara-C), demonstrating that BG does not act through an anti-mutagenic mechanism of action involving DNA polymerase beta.", "entity1": "DNA polymerase beta", "entity2": "cytosine arabinoside-3-phosphate", "span1": [56, 75], "span2": [87, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9276": {"label": 1, "data": {"text": "Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors.", "entity1": "alpha 1B-adrenoceptors", "entity2": "risperidone", "span1": [105, 127], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11434": {"label": 1, "data": {"text": "Here we have investigated the contribution of the nitric oxide and cyclooxygenase (COX) pathways to the activity of DEC against B. malayi microfilariae in mice.", "entity1": "cyclooxygenase", "entity2": "DEC", "span1": [67, 81], "span2": [116, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2659": {"label": 3, "data": {"text": "A broad-spectrum phosphodiesterase (PDE) inhibitor (1,3-isobutyl-1-methylxanthine, 300 microM, n=6) and an ecto-phosphodiesterase inhibitor (1,3-dipropyl-8-p-sulfophenylxanthine, 1 mM, n=6) significantly attenuated cAMP-induced AMP secretion by 60 and 74%, respectively.", "entity1": "phosphodiesterase", "entity2": "1,3-isobutyl-1-methylxanthine", "span1": [17, 34], "span2": [52, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9266": {"label": 5, "data": {"text": "Inhibition of cyclic AMP production by ergovaline was blocked by the dopamine receptor antagonist, (-)-sulpiride (IC50, 300 +/- 150 nM).", "entity1": "dopamine receptor", "entity2": "(-)-sulpiride", "span1": [69, 86], "span2": [99, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10105": {"label": 8, "data": {"text": "In the study reported here, the effects of acute PLZ treatment on the levels of various amino acids, some of which are also metabolized by pyridoxal phosphate-dependent transaminases were compared in rat whole brain.", "entity1": "pyridoxal phosphate-dependent transaminases", "entity2": "amino acids", "span1": [139, 182], "span2": [88, 99]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15967": {"label": 1, "data": {"text": "We recently showed that the first domain of human CCS (hCCSD1) is responsible for copper transfer to its protein partner, human SOD1 (hSOD1).", "entity1": "hCCSD1", "entity2": "copper", "span1": [55, 61], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8652": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRA", "entity2": "ethanol", "span1": [20, 23], "span2": [73, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3468": {"label": 8, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "DAT", "entity2": "DA", "span1": [195, 198], "span2": [125, 127]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4660": {"label": 3, "data": {"text": "Inhibition of SIRT1 significantly increased vascular superoxide production, enhanced NADPH oxidase activity, and mRNA expression of its subunits p22(phox) and NOX4, which were prevented by resveratrol.", "entity1": "NADPH oxidase", "entity2": "resveratrol", "span1": [85, 98], "span2": [189, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15631": {"label": 3, "data": {"text": "Nobiletin attenuates metastasis via both ERK and PI3K/Akt pathways in HGF-treated liver cancer HepG2 cells.", "entity1": "PI3K", "entity2": "Nobiletin", "span1": [49, 53], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14164": {"label": 5, "data": {"text": "When combined, mianserin antagonized the effects of the full kappa-opioid receptor agonists in [(35)S]GTPgammaS assays and reduced the stimulation of p38 MAPK and ERK1/2 phosphorylation by dynorphin A.", "entity1": "kappa-opioid receptor", "entity2": "mianserin", "span1": [61, 82], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9816": {"label": 3, "data": {"text": "Mibefradil (Ro 40-5967) belongs to a new chemical class of these molecules which differs from other Ca2+ antagonists by its ability to potently block T-type Ca2+ channels.", "entity1": "T-type Ca2+ channels", "entity2": "Ro 40-5967", "span1": [150, 170], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3775": {"label": 1, "data": {"text": "Opioid receptor binding affinity and activity were assessed using [(3)H]-diprenorphine binding, guanosine-5'-O-(3-[35S]-thio) triphosphate ([(35)S]-GTP\u03b3S) binding and isolated guinea-pig ileum.", "entity1": "Opioid receptor", "entity2": "[(35)S]-GTP\u03b3S", "span1": [0, 15], "span2": [140, 153]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4783": {"label": 3, "data": {"text": "The activity of CYP3A in excised liver samples from rats following multiple baicalin treatment was significantly decreased compared to that of the control group (P<0.05), whereas multiple doses of baicalin had no obvious effect on the activity of CYP2D.", "entity1": "CYP3A", "entity2": "baicalin", "span1": [16, 21], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"114": {"label": 1, "data": {"text": "Finally, the effects of felodipine and the three analogues on two processes which are dependent on myosin phosphorylation were examined, namely the actin-activated Mg2+-ATPase activity of myosin and the assembly of myosin filaments.", "entity1": "myosin", "entity2": "felodipine", "span1": [99, 105], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8217": {"label": 0, "data": {"text": "With the exception of three residues, the specific amino acids that form the putative binding pocket for ICA in ERG are conserved in EAG.", "entity1": "EAG", "entity2": "amino acids", "span1": [133, 136], "span2": [51, 62]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5355": {"label": 2, "data": {"text": "Results: The administration of prallethrin 1.6% w/w created significant increased changes in the levels of total WBC, lymphocytes, RBC, hemoglobin, packed cell volume, platelets, mean corpuscular volume, and mean corpuscular hemoglobin in rats after 24, 48, and 72\u2009h of continuous inhalation; however, there was a significant reduction in neutrophils at transient reduction in the monocytes after 24 and 48\u2009h to return to normal after 72\u2009h. Significant increases in the levels of CK, \u03b3-GT, SOD, NO, MDA, AFP, IL-2, and TNF\u03b1 were recorded.", "entity1": "hemoglobin", "entity2": "prallethrin", "span1": [225, 235], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12099": {"label": 1, "data": {"text": "Although there is a high probability that the action of aldosterone to cause cardiac fibrosis in this experimental model is an effect via non-epithelial MR, the locus of aldosterone action remains to be established, as do the molecular mechanisms linking MR occupancy by aldosterone and collagen deposition.", "entity1": "MR", "entity2": "aldosterone", "span1": [153, 155], "span2": [56, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9156": {"label": 3, "data": {"text": "Gossypol and its isomers were non-competitive inhibitors of human and hamster LDH-X with respect to the coenzyme NADH, competitive inhibitors of human LDH-X and noncompetitive-competitive inhibitors of hamster LDH-X with respect to the substrate alpha-ketobutyrate.", "entity1": "human and hamster LDH-X", "entity2": "Gossypol", "span1": [60, 83], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"855": {"label": 0, "data": {"text": "The functional protein contains 1160 amino acids with a large central mucin domain, three consensus sites for glycosaminoglycan attachment, two epidermal growth factor-like repeats, a putative hyaluronan-binding motif, and a potential transmembrane domain near the C-terminal.", "entity1": "hyaluronan-binding motif", "entity2": "C", "span1": [193, 217], "span2": [265, 266]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8116": {"label": 3, "data": {"text": "In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of fused oxadiazepines such as 7i which had an improved hERG inhibition profile and was a highly efficacious GSM in vitro and in vivo in rats.", "entity1": "hERG", "entity2": "oxadiazepines", "span1": [255, 259], "span2": [208, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12506": {"label": 1, "data": {"text": "Among all the organophosphates tested, the combination of a methyl group and a negatively charged oxygen attached to the P atom, CH3P(O)(O-)-AChE, conferred the greatest protection to the active site of aged or nonaged organophosphoryl conjugates of acetylcholinesterase.", "entity1": "AChE", "entity2": "oxygen", "span1": [141, 145], "span2": [98, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12065": {"label": 9, "data": {"text": "), whereas amitriptyline is essentially inactive on 5-HT3 receptors.", "entity1": "5-HT3", "entity2": "amitriptyline", "span1": [52, 57], "span2": [11, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4467": {"label": 3, "data": {"text": "Catalpol reduced the expression of pro-inflammatory mediates, such as monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-\u03b1 (TNF-\u03b1), inducible NO synthase (iNOS), and receptor for AGE (RAGE).", "entity1": "TNF-\u03b1", "entity2": "Catalpol", "span1": [135, 140], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3821": {"label": 0, "data": {"text": "The nucleotide sequence of HmTx contains 649 bp, and the mature protein is predicted to have 131 amino acid residues-104 of which make up the large subunit, and 27 of which make up the small subunit.", "entity1": "HmTx", "entity2": "amino acid", "span1": [27, 31], "span2": [97, 107]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5179": {"label": 3, "data": {"text": "Regarding urease inhibition, n-butanol was the most potent fraction (IC50: 97 \u00b5g/mL).", "entity1": "urease", "entity2": "n-butanol", "span1": [10, 16], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11627": {"label": 8, "data": {"text": "Indoleamine 2,3-dioxygenase (IDO), a tryptophan catabolizing enzyme, has been implicated in the pathogenesis of various neurological disorders.", "entity1": "Indoleamine 2,3-dioxygenase", "entity2": "tryptophan", "span1": [0, 27], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2881": {"label": 2, "data": {"text": "At PND35, the medial prefrontal cortex (mPFC) of rats given MPH showed 55% greater immunoreactivity (-ir) for the catecholamine marker tyrosine hydroxylase (TH), 60% more Nissl-stained cells, and 40% less norepinephrine transporter (NET)-ir density.", "entity1": "TH", "entity2": "MPH", "span1": [157, 159], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"825": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "PGE1", "span1": [258, 275], "span2": [298, 302]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3189": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "p-hydroxybenzoic acid", "span1": [262, 280], "span2": [64, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10612": {"label": 1, "data": {"text": "Furthermore, there is a high degree of correlation between binding affinities of a series of LEV derivatives to SV2A in fibroblasts and to the LEV-binding site in brain.", "entity1": "SV2A", "entity2": "LEV", "span1": [112, 116], "span2": [93, 96]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8071": {"label": 3, "data": {"text": "Contrary to the hypothesis, orlistat at 1 nM inhibited CES2 activity by 75% but no inhibition on CES1, placing CES2 one of the most sensitive targets of orlistat.", "entity1": "CES2", "entity2": "orlistat", "span1": [55, 59], "span2": [153, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15832": {"label": 9, "data": {"text": "When the expression of ABCA1 and ABCG1 was induced, 24-OHC efflux was stimulated in the presence of high density lipoprotein (HDL), whereas apolipoprotein A-I was not an efficient acceptor.", "entity1": "apolipoprotein A-I", "entity2": "24-OHC", "span1": [140, 158], "span2": [52, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9658": {"label": 1, "data": {"text": "By contrast, membrane expression of annexin-1, which was not minimal at 30 min, was substantial at 48 h for eosinophils treated with > 10(-)10 M FP, and inhibition of LTC4 synthesis was reversed by exogenous arachidonic acid (AA).", "entity1": "annexin-1", "entity2": "FP", "span1": [36, 45], "span2": [145, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11617": {"label": 8, "data": {"text": "HepG2 cells transfected with an hGSTA4 vector construct exhibited high steady-state hGSTA4 mRNA, high GST-44-HNE catalytic activities, but lower basal glutathione (GSH) concentrations relative to insert-free vector (control) cells.", "entity1": "GST-4", "entity2": "4-HNE", "span1": [102, 107], "span2": [107, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14762": {"label": 3, "data": {"text": "Jaceosidin, isolated from dietary mugwort (Artemisia princeps), induces G2/M cell cycle arrest by inactivating cdc25C-cdc2 via ATM-Chk1/2 activation.", "entity1": "cdc2", "entity2": "Jaceosidin", "span1": [118, 122], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10081": {"label": 8, "data": {"text": "The specific activity of only ornithine aminotransferase (OAT), the rate-limiting enzyme in the conversion of ornithine to proline, increased in 2 weeks of hypertrophy.", "entity1": "OAT", "entity2": "proline", "span1": [58, 61], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"11321": {"label": 8, "data": {"text": "For determination of [PA+Pli]-activity, arginine was added after this incubation.", "entity1": "PA", "entity2": "arginine", "span1": [22, 24], "span2": [40, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12740": {"label": 8, "data": {"text": "In vivo, A431NET tumors demonstrated a 33-fold higher [(123)I]MIBG uptake than parental tumors.", "entity1": "NET", "entity2": "[(123)I]MIBG", "span1": [13, 16], "span2": [54, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"523": {"label": 1, "data": {"text": "Consistent with these results, the translocation of cPLA2 protein as well as the release of arachidonic acid, a principal product of phospholipase A2, was rapidly induced by the addition of C2-ceramide in a Rac-dependent manner.", "entity1": "Rac", "entity2": "C2-ceramide", "span1": [207, 210], "span2": [190, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1717": {"label": 1, "data": {"text": "Molecular analysis of these mutants revealed single base pair exchanges in the ERG1 gene coding for squalene epoxidase, the target of terbinafine.", "entity1": "squalene epoxidase", "entity2": "terbinafine", "span1": [100, 118], "span2": [134, 145]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2153": {"label": 3, "data": {"text": "2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors.", "entity1": "CXCL8", "entity2": "2-Arylpropionic", "span1": [81, 86], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12879": {"label": 2, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "PS", "span1": [13, 19], "span2": [256, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14190": {"label": 9, "data": {"text": "After SU5416 treatment, cell viability, PARP-1, and caspase-3 protein levels were not changed.", "entity1": "PARP-1", "entity2": "SU5416", "span1": [40, 46], "span2": [6, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2797": {"label": 2, "data": {"text": "Furthermore, substance P (SP) concentration in the acini and expression of SP gene (preprotachykinin-A, PPT-A) and neurokinin-1 receptor (NK-1R), the primary receptor for SP, are increased in secretagogue caerulein-treated acinar cells.", "entity1": "preprotachykinin-A", "entity2": "caerulein", "span1": [84, 102], "span2": [205, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2240": {"label": 3, "data": {"text": "Dasatinib (BMS-354825) is a novel orally bioavailable SRC/ABL inhibitor that has activity against multiple imatinib-resistant BCR-ABL isoforms in vitro that is presently showing considerable promise in early-phase clinical trials of chronic myeloid leukemia (CML).", "entity1": "SRC", "entity2": "Dasatinib", "span1": [54, 57], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7325": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT4", "entity2": "amino acids", "span1": [342, 347], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3856": {"label": 0, "data": {"text": "The cDNAs of the full-length version of Ves a 1s revealed that the Ves a 1 gene consists of a 1005-bp ORF, which encodes 334 amino acid residues, and 67- and 227-bp 5' and 3' UTRs, respectively.", "entity1": "Ves a 1", "entity2": "amino acid", "span1": [67, 74], "span2": [125, 135]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4338": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "extracellular signal-regulated kinase", "entity2": "Pinosylvin", "span1": [112, 149], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15163": {"label": 2, "data": {"text": "Correlating with FSH\u03b2 activation, both PKA activity and levels of pCREB were increased to a greater extent by low compared with high GnRH pulse frequencies, and the induction of pCREB was also attenuated by overexpression of DNPKA at both low and high pulse frequencies.", "entity1": "pCREB", "entity2": "GnRH", "span1": [178, 183], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8991": {"label": 1, "data": {"text": "There was no escape of i.c.v.-administered [3H]R-PIA from brain to the peripheral circulation ruling out a peripheral and supporting a central mechanism of ethanol-adenosine interaction.", "entity1": "adenosine", "entity2": "ethanol", "span1": [164, 173], "span2": [156, 163]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4425": {"label": 6, "data": {"text": "Evidence for a new binding mode to GSK-3: allosteric regulation by the marine compound palinurin.", "entity1": "GSK-3", "entity2": "palinurin", "span1": [35, 40], "span2": [87, 96]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"8401": {"label": 9, "data": {"text": "Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD.", "entity1": "FLT3", "entity2": "AC220", "span1": [91, 95], "span2": [50, 55]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15479": {"label": 3, "data": {"text": "The toxic effects of MAO significantly attenuated with nicotine pre-exposure.", "entity1": "MAO", "entity2": "nicotine", "span1": [21, 24], "span2": [55, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13923": {"label": 3, "data": {"text": "Additionally, phenformin inhibited the current elicited through the Kir6.2DeltaC26 (functional without SUR) channel with an IC50 of 1.78 mM.", "entity1": "Kir6.2DeltaC26", "entity2": "phenformin", "span1": [68, 82], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15156": {"label": 2, "data": {"text": "A dominant negative PKA (DNPKA) reduced GnRH-stimulated pCREB and markedly decreased GnRH stimulation of FSH\u03b2 mRNA and FSH\u03b2LUC activity, but had little effect on LH\u03b2LUC activity, indicating relative specificity of this pathway.", "entity1": "pCREB", "entity2": "GnRH", "span1": [56, 61], "span2": [40, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14685": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "OATP1B3", "entity2": "GSK1292263", "span1": [127, 134], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11576": {"label": 8, "data": {"text": "OBJECTIVE: The aim was to test whether the common deletion [T/-] in the promoter of FADS2 affects the PUFA biosynthetic pathway and consequently modifies the effect of alpha-linolenic acid (ALA) on myocardial infarction (MI).", "entity1": "FADS2", "entity2": "ALA", "span1": [84, 89], "span2": [190, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9827": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "kinases", "entity2": "geldanamycin", "span1": [81, 88], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3652": {"label": 3, "data": {"text": "DBDCT up-regulated the expression of Bax, down-regulated the expression of Bcl-2, and significantly increased the ratio of Bax/Bcl-2.", "entity1": "Bcl-2", "entity2": "DBDCT", "span1": [75, 80], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3466": {"label": 8, "data": {"text": "METHODS: (+/-)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria.", "entity1": "DAT", "entity2": "[(3)H] dopamine", "span1": [195, 198], "span2": [108, 123]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6817": {"label": 2, "data": {"text": "These results suggest that pitavastatin efficiently increases apoA-I in the culture medium of HepG2 cells by promoting apoA-I production through inhibition of HMG-CoA reductase and suppression of Rho activity and by protecting apoA-I from catabolism through ABCA1 induction and lipidation of apoA-I.", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [292, 298], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9060": {"label": 1, "data": {"text": "7-Hydroxy levomepromazine, 3-hydroxy levomepromazine and 7-hydroxy fluphenazine had only 10% of the potency of the parent drug in histamine H1 receptor binding, while the 7-hydroxy-metabolites of chlorpromazine and perphenazine had about 75% of the potency of the parent drug in this binding system.", "entity1": "histamine H1 receptor", "entity2": "7-hydroxy", "span1": [130, 151], "span2": [171, 180]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4215": {"label": 1, "data": {"text": "Mn-induced internalization of DAT may provide an explanation for disruption in DA transmission previously reported in the striatum.", "entity1": "DAT", "entity2": "Mn", "span1": [30, 33], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14516": {"label": 1, "data": {"text": "PAK1 emerged as a consensus target of 5-ASA, orchestrating these pathways.", "entity1": "PAK1", "entity2": "5-ASA", "span1": [0, 4], "span2": [38, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9183": {"label": 1, "data": {"text": "Binding of penicillins to penicillin-binding protein 1Bs produces lysis, binding to penicillin-binding protein 2 produces round cells, and binding to penicillin-binding protein 3 produces long filaments.", "entity1": "penicillin-binding protein 1Bs", "entity2": "penicillins", "span1": [26, 56], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15817": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFbeta receptor", "entity2": "Tyr", "span1": [70, 87], "span2": [165, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9504": {"label": 9, "data": {"text": "Saturation and competition studies in the presence or absence of the histamine H1 receptor antagonist, levocabastine, revealed that [3H]SR 142948A bound with similar affinities to both the levocabastine-insensitive neurotensin NT1 receptors (20% of the total binding population) and the recently cloned levocabastine-sensitive neurotensin NT2 receptors (80% of the receptors) (Kd = 6.8 and 4.8 nM, respectively).", "entity1": "neurotensin NT1 receptors", "entity2": "levocabastine", "span1": [215, 240], "span2": [189, 202]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7602": {"label": 5, "data": {"text": "In addition to OT and to a lesser extent AVP (pitressin), a number of OT and AVP analogues; such as carbetocin (OT agonist) dDAVP (desmopressin, V(2) agonist), terlipressin (V(1a) agonist), felypressin (V(1a) agonist) and atosiban (Tractocile OT antagonist) are also in clinical use.", "entity1": "OT", "entity2": "atosiban", "span1": [243, 245], "span2": [222, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12805": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "PDGFRA", "entity2": "Gleevec", "span1": [109, 115], "span2": [88, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12258": {"label": 1, "data": {"text": "Consequently, other cation species may compete with Na+ to regulate the time KARs remain in the open state.", "entity1": "KARs", "entity2": "Na+", "span1": [77, 81], "span2": [52, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15632": {"label": 3, "data": {"text": "Nobiletin attenuates metastasis via both ERK and PI3K/Akt pathways in HGF-treated liver cancer HepG2 cells.", "entity1": "Akt", "entity2": "Nobiletin", "span1": [54, 57], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6985": {"label": 9, "data": {"text": "Furthermore, brain microsomal Acsl did not produce valproyl-CoA.", "entity1": "brain microsomal Acsl", "entity2": "valproyl-CoA", "span1": [13, 34], "span2": [51, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12167": {"label": 8, "data": {"text": "Of these two enzymes, cystathionine-gamma-lyase (CSE) is believed to be the key enzyme that forms H2S in the cardiovascular system.", "entity1": "CSE", "entity2": "H2S", "span1": [49, 52], "span2": [98, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5151": {"label": 9, "data": {"text": "Our results showed that 2-hydroxy-3-methylanthraquinone decreased phosphorylation-ERK1/2 (p-ERK1/2), and increased p-p38MAPK, but did not affect expressions of p-JNK1/2 in U937 cells.", "entity1": "p-JNK1/2", "entity2": "2-hydroxy-3-methylanthraquinone", "span1": [160, 168], "span2": [24, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1108": {"label": 2, "data": {"text": "Indomethacin completely antagonizes CA activity, i.e.", "entity1": "CA", "entity2": "Indomethacin", "span1": [36, 38], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13833": {"label": 2, "data": {"text": "The recently discovered hyperinsulinism/hyperammonemia disorder showed that the loss of allosteric inhibition of GDH by GTP causes excessive secretion of insulin.", "entity1": "insulin", "entity2": "GTP", "span1": [154, 161], "span2": [120, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"12049": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "mTRPV4", "entity2": "apomorphine", "span1": [47, 53], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13155": {"label": 2, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "Fas-associated death domain-containing protein", "entity2": "paclitaxel", "span1": [56, 102], "span2": [378, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8592": {"label": 2, "data": {"text": "Quercetin and rutin also increased alkaline phosphatase activity by about 150 and 240% and demonstrated mineralization up to 110 and 200% respectively as compared to control (which was considered as 100%).", "entity1": "alkaline phosphatase", "entity2": "Quercetin", "span1": [35, 55], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15697": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "TRP channels", "entity2": "CAT", "span1": [46, 58], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9393": {"label": 2, "data": {"text": "Activation of cytoprotective prostaglandin synthase-1 by minoxidil as a possible explanation for its hair growth-stimulating effect.", "entity1": "prostaglandin synthase-1", "entity2": "minoxidil", "span1": [29, 53], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15442": {"label": 3, "data": {"text": "When mice were treated ip with the major neonicotinoid imidacloprid (IMI), metabolism by CYP oxidation reactions was not appreciably affected, whereas the AOX-generated nitrosoguanidine metabolite was decreased by 30% with tungsten and 56% with hydralazine and 86% in the AOX-deficient mice.", "entity1": "AOX", "entity2": "hydralazine", "span1": [155, 158], "span2": [245, 256]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3551": {"label": 2, "data": {"text": "The results demonstrated that intracerebral infusions of LTD4 (1 ng/mouse) produced memory impairment as determined by Morris water maze test and Y-maze test in mice, and caused the accumulation of A\u03b21-40 and A\u03b21-42 in the hippocampus and cortex through increased activity of \u03b2- and \u03b3-secretases accompanied with increased expression of amyloid precursor protein (APP).", "entity1": "amyloid precursor protein", "entity2": "LTD4", "span1": [337, 362], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14723": {"label": 4, "data": {"text": "We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenine moiety.", "entity1": "TLR7", "entity2": "N", "span1": [57, 61], "span2": [166, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10134": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "indomethacin", "span1": [34, 37], "span2": [152, 164]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7093": {"label": 8, "data": {"text": "The glutamate-aspartate transporter GLAST mediates glutamate uptake at inner hair cell afferent synapses in the mammalian cochlea.", "entity1": "GLAST", "entity2": "glutamate", "span1": [36, 41], "span2": [51, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8007": {"label": 3, "data": {"text": "In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-\u03b1-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.", "entity1": "PAI-1", "entity2": "IMG", "span1": [172, 177], "span2": [127, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11383": {"label": 1, "data": {"text": "5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs.", "entity1": "5-HT1B", "entity2": "ergotamine", "span1": [0, 6], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5492": {"label": 8, "data": {"text": "This was shown to be attributable to catalase-like activity of these enzymes, resulting in unproductive cleavage of H2O2.", "entity1": "catalase", "entity2": "H2O2", "span1": [37, 45], "span2": [116, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14817": {"label": 4, "data": {"text": "Cannabinoid receptor 1 (CB(1)) inverse agonists (e.g., rimonabant) have been reported to produce adverse effects including nausea, emesis, and anhedonia that limit their clinical applications.", "entity1": "CB(1)", "entity2": "rimonabant", "span1": [24, 29], "span2": [55, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10108": {"label": 8, "data": {"text": "The elevation in brain alanine levels could be explained, at least in part, by a time- and dose-dependent inhibitory effect of PLZ on alanine transaminase (ALA-T), although as with GABA the increases are higher than expected from the degree of enzyme inhibition produced.", "entity1": "ALA-T", "entity2": "alanine", "span1": [156, 161], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9242": {"label": 3, "data": {"text": "In cell culture experiments, it was found that triclosan inhibited IL-1 beta induced prostaglandin E2 production by human gingival fibroblasts in a concentration dependent manner, and at relatively low concentrations.", "entity1": "IL-1 beta", "entity2": "triclosan", "span1": [67, 76], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10767": {"label": 2, "data": {"text": "Although, imatinib primarily inhibits tyrosine kinases, it also stimulates the activity of EGFR tyrosine kinase in head and neck squamous tumors.", "entity1": "EGFR", "entity2": "imatinib", "span1": [91, 95], "span2": [10, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1569": {"label": 3, "data": {"text": "These compounds are competitive and, in a few cases, non-competitive inhibitors for AChE, the most potent being compound (14), though three-fold less active than tacrine.", "entity1": "AChE", "entity2": "tacrine", "span1": [84, 88], "span2": [162, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10216": {"label": 2, "data": {"text": "Metformin treatment for 10 weeks significantly increased AMPK alpha2 activity in the skeletal muscle, and this was associated with increased phosphorylation of AMPK on Thr172 and decreased acetyl-CoA carboxylase-2 activity.", "entity1": "AMPK alpha2", "entity2": "Metformin", "span1": [57, 68], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10751": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "2'-deoxyuridine", "span1": [260, 280], "span2": [160, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10750": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "N4-pentoxycarbonyl-5'-5-fluorocytidine", "span1": [282, 284], "span2": [97, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12947": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "conivaptan", "span1": [39, 59], "span2": [140, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6432": {"label": 3, "data": {"text": "The group treated with pyridostigmine alone showed decreased plasma butyrylcholinesterase (BChE) activity (87% of control), whereas pyridostigmine plus exercise significantly decreased the BChE activity (79% of control), indicating an interactive effect of the combination.", "entity1": "BChE", "entity2": "pyridostigmine", "span1": [189, 193], "span2": [132, 146]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1862": {"label": 3, "data": {"text": "These data suggest that the lavandulyl side chain and the position of the hydroxy group are important for high DGAT inhibitory activity.", "entity1": "DGAT", "entity2": "hydroxy", "span1": [111, 115], "span2": [74, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9135": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "n-propyl", "span1": [124, 136], "span2": [54, 62]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13641": {"label": 0, "data": {"text": "In the presence of drug, the linker is rigid and this alpha-helix extends to include Gly and the preceding Leu.", "entity1": "alpha-helix", "entity2": "Leu", "span1": [54, 65], "span2": [107, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11784": {"label": 1, "data": {"text": "The effects of jaspamide on human cardiomyocyte function and cardiac ion channel activity.", "entity1": "cardiac ion channel", "entity2": "jaspamide", "span1": [61, 80], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8862": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "c-Src", "entity2": "TCDD", "span1": [406, 411], "span2": [327, 331]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3630": {"label": 5, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "vanilloid receptor type I", "entity2": "capsazepine", "span1": [248, 273], "span2": [285, 296]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3984": {"label": 0, "data": {"text": "Bioinformatic analyses of several vertebrate genomes were undertaken using known ALDH2 and ALDH1B1 amino acid sequences.", "entity1": "ALDH1B1", "entity2": "amino acid", "span1": [91, 98], "span2": [99, 109]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14729": {"label": 3, "data": {"text": "Inhibitors based on a benzo-fused spirocyclic oxazepine scaffold were discovered for stearoyl-coenzyme A (CoA) desaturase 1 (SCD1) and subsequently optimized to potent compounds with favorable pharmacokinetic profiles and in vivo efficacy in reducing the desaturation index in a mouse model.", "entity1": "stearoyl-coenzyme A (CoA) desaturase 1", "entity2": "benzo-fused spirocyclic oxazepine", "span1": [85, 123], "span2": [22, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4713": {"label": 3, "data": {"text": "Thus, the TCDD-induced reduction in canonical Wnt signaling is associated with a decrease in activators (Rspo2 and Rspo3) rather than an increase in inhibitors (Dkk1 and Dkk2) of the pathway.", "entity1": "Dkk1", "entity2": "TCDD", "span1": [161, 165], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8753": {"label": 8, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT2B10", "entity2": "imipramine", "span1": [61, 68], "span2": [88, 98]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5404": {"label": 2, "data": {"text": "The data show that CP[c]Ph is less potent at inducing CYP1A gene expression in rainbow trout than benzo[a]pyrene (B[a]P), a well-known Ah-receptor agonist.", "entity1": "CYP1A", "entity2": "B[a]P", "span1": [54, 59], "span2": [114, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12536": {"label": 1, "data": {"text": "Adenosine analogs in particular the N6-substituted compounds are more potent at A1 receptors than at A2 receptors.", "entity1": "A2 receptors", "entity2": "N6", "span1": [101, 113], "span2": [36, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"294": {"label": 3, "data": {"text": "In catalytic properties, mouse CA V is closest to CA I; however, in inhibition by acetazolamide, ethoxzolamide, and cyanate, CA V is very similar to CA II.", "entity1": "CA II", "entity2": "acetazolamide", "span1": [149, 154], "span2": [82, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8015": {"label": 3, "data": {"text": "In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A(2) (hnps-PLA(2)) and human leukotriene A(4) hydrolase (LTA(4)H-h) was found.", "entity1": "human leukotriene A(4) hydrolase", "entity2": "JMC08-4", "span1": [203, 235], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6846": {"label": 1, "data": {"text": "We studied several single nucleotide polymorphisms (SNP) in Hcy-regulating genes [methylenetetrahydrofolate reductase (MTHFR) C677T and A1298C; methionine synthase (MS) A2756G; methionine synthase reductase (MTRR) A66G] in relation to total plasma Hcy levels, transplant coronary artery disease and thromboembolic episodes in 84 heart transplant patients, and we compared the incidence of these polymorphisms with those in a healthy adult controls.", "entity1": "C677T", "entity2": "Hcy", "span1": [126, 131], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14051": {"label": 3, "data": {"text": "RESULTS: Aspirin reduced mTOR signaling in CRC cells by inhibiting the mTOR effectors S6K1 and 4E-BP1.", "entity1": "mTOR", "entity2": "Aspirin", "span1": [25, 29], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12411": {"label": 1, "data": {"text": "HENA failed to dilate the arteries from the KCNMB1 knockout mouse, underscoring BK \u03b21's role in HENA action.", "entity1": "BK \u03b21", "entity2": "HENA", "span1": [80, 85], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8638": {"label": 1, "data": {"text": "Ethanol and melatonin exert opposite effects on E2 and P4, and they differentially regulate the expression of sex steroid receptors in female reproductive tissues.", "entity1": "sex steroid receptors", "entity2": "Ethanol", "span1": [110, 131], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11062": {"label": 1, "data": {"text": "These two antibodies recognize closely spaced epitopes on the 55 kD chain of the IL-2 R. IL-2 R expression was examined on peripheral blood small lymphocytes in three groups of patients who received: (A) cyclosporine CsA and prednisone for baseline immunosuppression (n = 9); (B) anti-Tac with CsA and prednisone as baseline immunosuppression (n = 12); and (C) anti-Tac with azathioprine and prednisone as baseline immunosuppression (n = 5).", "entity1": "IL-2 R", "entity2": "CsA", "span1": [89, 95], "span2": [294, 297]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4401": {"label": 1, "data": {"text": "The mannose 6-phosphate-binding sites of M6P/IGF2R determine its capacity to suppress matrix invasion by squamous cell carcinoma cells.", "entity1": "IGF2R", "entity2": "mannose 6-phosphate", "span1": [45, 50], "span2": [4, 23]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5274": {"label": 2, "data": {"text": "Nox4 oxidase activity is thought to be constitutive and regulated at the transcriptional level; however, we challenge this point of view and suggest that specific quinone derivatives could modulate this activity.", "entity1": "Nox4", "entity2": "quinone", "span1": [0, 4], "span2": [163, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4377": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "dexamethasone 21-phosphate", "span1": [280, 285], "span2": [192, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11697": {"label": 3, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "TNF-\u03b1", "entity2": "cisplatin", "span1": [153, 158], "span2": [212, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7655": {"label": 2, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-9", "entity2": "monocrotaline", "span1": [10, 15], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"990": {"label": 7, "data": {"text": "We have reported that a deficiency of tetrahydrobiopterin (BH(4)), an active cofactor of endothelial NO synthase (eNOS), contributes to the endothelial dysfunction through reduced eNOS activity and increased superoxide anion (O(2)(-)) generation in the insulin-resistant state.", "entity1": "endothelial NO synthase", "entity2": "tetrahydrobiopterin", "span1": [89, 112], "span2": [38, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"11388": {"label": 1, "data": {"text": "We investigated the effect of the clinically used nitrates nitroglycerin (NTG), isosorbide dinitrate (ISDN), and sodium nitroprusside (SNP) on HIF-1-mediated transcriptional responses to hypoxia.", "entity1": "HIF-1", "entity2": "nitroglycerin", "span1": [143, 148], "span2": [59, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10717": {"label": 3, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "c-fos", "entity2": "Dimemorfan", "span1": [69, 74], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10293": {"label": 5, "data": {"text": "A streamlined and high-yielding synthesis of aprepitant (1), a potent substance P (SP) receptor antagonist, is described.", "entity1": "substance P (SP) receptor", "entity2": "aprepitant", "span1": [70, 95], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6250": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "human serotonin transporter", "entity2": "triflupromazine", "span1": [58, 85], "span2": [91, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6322": {"label": 3, "data": {"text": "We report that the radiation-induced activation of the kinase Cds1 [4] (also known as Chk2 [5]) is inhibited by caffeine in vivo and that ATM kinase activity is directly inhibited by caffeine in vitro.", "entity1": "Chk2", "entity2": "caffeine", "span1": [86, 90], "span2": [112, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6708": {"label": 3, "data": {"text": "The results demonstrated that tranylcypromine is a competitive inhibitor of CYP2C19 (Ki = 32 microM) and CYP2D6 (Ki = 367 microM) and a noncompetitive inhibitor of CYP2C9 (Ki = 56 microM).", "entity1": "CYP2C19", "entity2": "tranylcypromine", "span1": [76, 83], "span2": [30, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12037": {"label": 8, "data": {"text": "Compound I of the peroxidases is represented as EO, and oxidation of I- by EO is postulated to form enzyme-bound hypoiodite, represented in our scheme as [EOI]-.", "entity1": "peroxidases", "entity2": "I-", "span1": [18, 29], "span2": [69, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11958": {"label": 8, "data": {"text": "We have developed a convenient quantitative multi-well plate assay to measure the glucuronidation rate of 7-hydroxy-4-trifluoromethylcoumarin (HFC) for several UGTs.", "entity1": "UGTs", "entity2": "HFC", "span1": [160, 164], "span2": [143, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10374": {"label": 3, "data": {"text": "This study shows that the potency of GW660511X in comparison with omapatrilat is more than 100-fold lower in human, but less than 10-fold lower in rat plasma, suggesting that rat may not be a suitable in vivo model for the evaluation of ACE/NEP inhibition in relation to effects in humans.", "entity1": "NEP", "entity2": "GW660511X", "span1": [241, 244], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10763": {"label": 2, "data": {"text": "Induction of heparin-binding EGF-like growth factor and activation of EGF receptor in imatinib mesylate-treated squamous carcinoma cells.", "entity1": "EGF receptor", "entity2": "imatinib mesylate", "span1": [70, 82], "span2": [86, 103]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6549": {"label": 0, "data": {"text": "To identify amino acid residues involved in PDE3-selective inhibitor binding, we selected eight presumed interacting residues in the substrate-binding pocket of PDE3A using a model created on basis of homology to the PDE4B crystal structure.", "entity1": "PDE3", "entity2": "amino acid", "span1": [44, 48], "span2": [12, 22]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1493": {"label": 3, "data": {"text": "EGF-stimulated phosphorylation of ERK and Bad is blocked by pretreatment with U0126, a selective MAP kinase kinase (MKK)1/2 inhibitor.", "entity1": "ERK", "entity2": "U0126", "span1": [34, 37], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15845": {"label": 2, "data": {"text": "The expression of ABCA1 and ABCG1 was induced by 24-OHC, as well as TO901317 and retinoic acid, which are ligands of the nuclear receptors LXR/RXR.", "entity1": "ABCG1", "entity2": "retinoic acid", "span1": [28, 33], "span2": [81, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14883": {"label": 2, "data": {"text": "Substantial evidence shows that H(2)S is involved in aging by inhibiting free-radical reactions, activating SIRT1, and probably interacting with the age-related gene Klotho.", "entity1": "SIRT1", "entity2": "H(2)S", "span1": [108, 113], "span2": [32, 37]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11961": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I", "entity2": "phosphatidylinositol-4,5-bisphosphate", "span1": [16, 66], "span2": [213, 250]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4340": {"label": 3, "data": {"text": "Pinosylvin was also found to attenuate the activation of proteins involved in focal adhesion kinase (FAK)/c-Src/extracellular signal-regulated kinase (ERK) signaling, and phosphoinositide 3-kinase (PI3K)/Akt/ glycogen synthase kinase 3\u03b2 (GSK-3\u03b2) signaling pathway.", "entity1": "phosphoinositide 3-kinase", "entity2": "Pinosylvin", "span1": [171, 196], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9143": {"label": 1, "data": {"text": "The profile of a series of adenosine analogs or of xanthine antagonists can be used to define the nature of adenosine receptors.", "entity1": "adenosine receptors", "entity2": "xanthine", "span1": [108, 127], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2": {"label": 1, "data": {"text": "Labetalol and dilevalol (both at > or = 10(-7) M) attenuated the spontaneous contractile activity of the rat portal vein and the attenuation to labetalol at 10(-6) M was abolished by ICI 118,551 which illustrates that the labetalol-induced attenuation is beta 2-adrenoceptor mediated.", "entity1": "beta 2-adrenoceptor", "entity2": "labetalol", "span1": [255, 274], "span2": [222, 231]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3029": {"label": 1, "data": {"text": "Optimization of taxane binding to microtubules: binding affinity dissection and incremental construction of a high-affinity analog of paclitaxel.", "entity1": "microtubules", "entity2": "paclitaxel", "span1": [34, 46], "span2": [134, 144]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12503": {"label": 8, "data": {"text": "These findings indicate that human pulmonary ethanol-metabolizing activities differ significantly with respect to genetic polymorphism at both the ADH2 and the ALDH2 loci.", "entity1": "ALDH2", "entity2": "ethanol", "span1": [160, 165], "span2": [45, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4202": {"label": 3, "data": {"text": "PTE, used in combination with a known JAK2/STAT3 inhibitor, AG490, further decreased the viability of osteosarcoma cells.", "entity1": "JAK2", "entity2": "AG490", "span1": [38, 42], "span2": [60, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14560": {"label": 0, "data": {"text": "In this study, we present the synthesis and pharmacological properties of new analogues of arginine vasopressin modified in the N-terminal part of the molecule with proline derivatives: indoline-2-carboxylic acid (Ica) and (2S,4R)-4-(naphthalene-2-ylmethyl)pyrrolidine-2-carboxylic acid.", "entity1": "arginine vasopressin", "entity2": "N", "span1": [91, 111], "span2": [128, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10163": {"label": 5, "data": {"text": "Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride) is a novel antiallergic/histamine H1-receptor antagonistic drug that was synthesized and evaluated in our laboratories.", "entity1": "histamine H1-receptor", "entity2": "11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride", "span1": [165, 186], "span2": [40, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14735": {"label": 3, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "p66Shc", "entity2": "raisanberine", "span1": [169, 175], "span2": [13, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15983": {"label": 1, "data": {"text": "Immunoregulatory effects of Glycyrrhizic acid exerts anti-asthmatic effects via modulation of Th1/Th2 cytokines and enhancement of CD4(+)CD25(+)Foxp3(+) regulatory T cells in ovalbumin-sensitized mice.", "entity1": "cytokines", "entity2": "Glycyrrhizic acid", "span1": [102, 111], "span2": [28, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2460": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "ABCC2", "entity2": "paclitaxel", "span1": [62, 67], "span2": [161, 171]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14435": {"label": 1, "data": {"text": "TCDD or prochloraz doubled ABCG2-mediated Hoechst H33342 secretion.", "entity1": "ABCG2", "entity2": "prochloraz", "span1": [27, 32], "span2": [8, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6360": {"label": 8, "data": {"text": "The mNQO activity showed significantly higher affinity for NADH than NADPH as electron donors and catalyzed reduction of 2,6-dichlorophenolindophenol and menadione.", "entity1": "mNQO", "entity2": "2,6-dichlorophenolindophenol", "span1": [4, 8], "span2": [121, 149]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13717": {"label": 5, "data": {"text": "Irbesartan (Aprovel, Avapro, Irbetan, Karvea), an angiotensin II receptor type 1 antagonist, is approved in many countries worldwide for the treatment of hypertension.", "entity1": "angiotensin II receptor type 1", "entity2": "Karvea", "span1": [50, 80], "span2": [38, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11042": {"label": 4, "data": {"text": "The present study determined the influence of a retinoid X receptor agonist bexarotene on angiogenesis and metastasis in solid tumours.", "entity1": "retinoid X receptor", "entity2": "bexarotene", "span1": [48, 67], "span2": [76, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10625": {"label": 5, "data": {"text": "A novel membrane sensor for histamine H1-receptor antagonist \"fexofenadine\".", "entity1": "histamine H1-receptor", "entity2": "fexofenadine", "span1": [28, 49], "span2": [62, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13261": {"label": 3, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "MUC2/5AC", "entity2": "ONO-1078", "span1": [85, 93], "span2": [20, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9067": {"label": 1, "data": {"text": "The present study reports the in vitro binding affinities of the same compounds for muscarinic cholinergic receptors and for histamine H1 receptors in rat brain, using 3H-quinuclidinyl benzilate and 3H-mepyramine as radioligands.", "entity1": "muscarinic cholinergic receptors", "entity2": "3H-quinuclidinyl benzilate", "span1": [84, 116], "span2": [168, 194]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7476": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "Kainate-selective ionotropic glutamate receptors", "entity2": "Cl-", "span1": [0, 48], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9878": {"label": 5, "data": {"text": "In these tissues, JTH-601, prazosin (a non-selective alpha(1)-adrenoceptor antagonist), and tamsulosin (an alpha(1A)-adrenoceptor antagonist) competitively antagonized contraction in a concentration-dependent manner.", "entity1": "alpha(1A)-adrenoceptor", "entity2": "tamsulosin", "span1": [107, 129], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1907": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "TP", "entity2": "5-FU", "span1": [121, 123], "span2": [87, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4416": {"label": 2, "data": {"text": "Notably, 17-HDHA treatment reduced adipose tissue expression of inflammatory cytokines, increased adiponectin expression and improved glucose tolerance parallel to insulin sensitivity in obese mice.", "entity1": "insulin", "entity2": "17-HDHA", "span1": [164, 171], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"522": {"label": 1, "data": {"text": "Consistent with these results, the translocation of cPLA2 protein as well as the release of arachidonic acid, a principal product of phospholipase A2, was rapidly induced by the addition of C2-ceramide in a Rac-dependent manner.", "entity1": "cPLA2", "entity2": "C2-ceramide", "span1": [52, 57], "span2": [190, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11722": {"label": 1, "data": {"text": "To investigate the effects of \u03b2-ionone on apoptosis initiation and its possible mechanisms of action, we qualified cell apoptosis, proteins related to apoptosis and a phosphatidylinositol 3-kinase (PI3K)-AKT pathway in human gastric adenocarcinoma cancer SGC-7901 cells.", "entity1": "PI3K", "entity2": "\u03b2-ionone", "span1": [198, 202], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8941": {"label": 1, "data": {"text": "Two new negatively charged estramustine derivatives, estramustine sulphate and estramustine glucuronide, were found to be similar MAP-dependent microtubule inhibitors.", "entity1": "MAP", "entity2": "estramustine", "span1": [130, 133], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9296": {"label": 8, "data": {"text": "Consistent with these data, only GLUT2-expressing RIN or AtT-20ins cells transported STZ efficiently.", "entity1": "GLUT2", "entity2": "STZ", "span1": [33, 38], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9381": {"label": 3, "data": {"text": "In conclusion, our data suggest that chronic cocaine use is associated with modestly reduced levels of striatal DA and the DA transporter in some subjects and that these changes might contribute to the neurological and psychiatric effects of the drug.", "entity1": "DA transporter", "entity2": "cocaine", "span1": [123, 137], "span2": [45, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4403": {"label": 0, "data": {"text": "Previous work has extensively characterized a common allosteric site on mGlu5, termed the MPEP (2-Methyl-6-(phenylethynyl)pyridine) binding site.", "entity1": "mGlu5", "entity2": "MPEP", "span1": [72, 77], "span2": [90, 94]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"2727": {"label": 3, "data": {"text": "Indomethacin and SC-236, a selective cyclooxygenase-2 (COX-2) inhibitor, exerted a similar effect as sulindac.", "entity1": "cyclooxygenase-2", "entity2": "Indomethacin", "span1": [37, 53], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15367": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "RARs", "entity2": "all-trans retinoic acid", "span1": [221, 225], "span2": [82, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6175": {"label": 3, "data": {"text": "Ibuprofen inhibits cystic fibrosis transmembrane conductance regulator-mediated Cl- secretion.", "entity1": "cystic fibrosis transmembrane conductance regulator", "entity2": "Ibuprofen", "span1": [19, 70], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2144": {"label": 2, "data": {"text": "Thiazolidinediones are a new class of anti-diabetic agents which increase insulin sensitivity by binding to the peroxisome proliferator-activated receptor gamma (PPAR(gamma)) and stimulating the expression of insulin-responsive genes involved in glucose and lipid metabolism.", "entity1": "insulin", "entity2": "Thiazolidinediones", "span1": [74, 81], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3674": {"label": 3, "data": {"text": "Artemisinic acid inhibits melanogenesis through downregulation of C/EBP \u03b1-dependent expression of HMG-CoA reductase gene.", "entity1": "HMG-CoA reductase", "entity2": "Artemisinic acid", "span1": [98, 115], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4753": {"label": 3, "data": {"text": "Moreover, overexpressed CYP2J2 and EETs inhibited Ang II-induced macrophage migration in a VSMC-macrophage coculture system.", "entity1": "Ang II", "entity2": "EETs", "span1": [50, 56], "span2": [35, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11715": {"label": 0, "data": {"text": "Histone deacetylase 3 (Hdac3) is a nuclear enzyme that removes acetyl groups from lysine residues in histones and other proteins to epigenetically regulate gene expression.", "entity1": "histones", "entity2": "acetyl", "span1": [101, 109], "span2": [63, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13941": {"label": 3, "data": {"text": "With the pentapeptide linked through the C7alpha position of estradiol, the resulting PROTAC shows the most effective ER degradation and highest affinity for the estrogen receptor.", "entity1": "ER", "entity2": "estradiol", "span1": [118, 120], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8278": {"label": 8, "data": {"text": "This investigation tested the hypothesis that CYP2B6 is a prominent CYP isoform responsible for clinical methadone N-demethylation and clearance, using the in vivo mechanism-based CYP2B6 inhibitor ticlopidine, given orally for 4 days.", "entity1": "CYP2B6", "entity2": "N", "span1": [46, 52], "span2": [115, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4052": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "apoptosis signal-regulating kinase 1", "entity2": "neoechinulin A", "span1": [149, 185], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2995": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "F820A", "entity2": "3-isobutyl-1-methylxanthine", "span1": [265, 270], "span2": [74, 101]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3749": {"label": 3, "data": {"text": "Disruption of contact inhibition, which was induced by toxic AhR ligands 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or polycyclic aromatic hydrocarbons in epithelial WB-F344 cells, reduced Cx43 protein levels, possibly via enhanced proteasomal degradation, significantly decreased the amount of gap junction plaques and downregulated GJIC, in an AhR-dependent manner.", "entity1": "Cx43", "entity2": "polycyclic aromatic hydrocarbons", "span1": [189, 193], "span2": [119, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5820": {"label": 3, "data": {"text": "After the combined pituitary stimulation test (100 micrograms human CRH, 100 micrograms GnRH, 100 micrograms GH-releasing hormone, and 200 micrograms TRH), the ACTH peak (maximum increase at 30 min) was significantly blunted by loperamide from 9 +/- 1 to 4 +/- 1 pmol/L (P less than 0.001) and the area under the curve of ACTH from 0-120 min was reduced from 35 +/- 5 to 23 +/- 4 pmol/L.2 h (P less than 0.05).", "entity1": "GnRH", "entity2": "loperamide", "span1": [88, 92], "span2": [228, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5305": {"label": 3, "data": {"text": "Consistent with these results, prunetin significantly reduced serum levels of inflammatory cytokines and mortality in mice challenged with lipopolysaccharide.", "entity1": "cytokines", "entity2": "prunetin", "span1": [91, 100], "span2": [31, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13428": {"label": 2, "data": {"text": "TGF-beta1 and high D-glucose increased p42/44(mapk) and Smad2 phosphorylation, an effect blocked by PD-98059 (MEK1/2 inhibitor).", "entity1": "Smad2", "entity2": "D-glucose", "span1": [56, 61], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8127": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "pAkt", "entity2": "Sal", "span1": [36, 40], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"177": {"label": 5, "data": {"text": "The most potent compound, D,L-4-(3,4-dichlorobenzoylamino)-5-(dipentylamino)-5-oxo-pen tanoic acid (lorglumide, CR 1409), has a great affinity for the pancreatic CCK receptors and is a competitive, specific and potent CCK antagonist on the smooth muscles of the gall bladder and ileum of the guinea pig and on the CCK-induced amylase secretion of isolated pancreatic acini.", "entity1": "CCK", "entity2": "lorglumide", "span1": [218, 221], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7168": {"label": 4, "data": {"text": "OBJECTIVE: Telmisartan, an angiotensin II type 1 receptor (AT1R) antagonist, was found to have a unique property: it is a partial agonist of peroxisome proliferator-activated receptor gamma (PPARgamma).", "entity1": "PPARgamma", "entity2": "Telmisartan", "span1": [191, 200], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6274": {"label": 3, "data": {"text": "The functional inhibitory characteristics of the angiotensin II type 1 receptor blockers (ARB) candesartan; irbesartan; and losartan and its active metabolite EXP 3174 (EXP) were studied in rabbit aortic strips and rat portal vein preparations in vitro.", "entity1": "angiotensin II type 1 receptor", "entity2": "candesartan", "span1": [49, 79], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6243": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "human 5-HT1B", "entity2": "sumatriptan", "span1": [101, 113], "span2": [17, 28]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14213": {"label": 6, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "codeine", "span1": [83, 88], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1278": {"label": 3, "data": {"text": "CONCLUSIONS: In the maximum registered dosage, nabumetone inhibits thromboxane production much more than meloxicam, signifying less COX-2 selectivity of the former.", "entity1": "COX-2", "entity2": "nabumetone", "span1": [132, 137], "span2": [47, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10508": {"label": 9, "data": {"text": "Resistance to GW572016 was not due to a lack of receptor inhibition, but rather with a lack of inhibition of ERK and Akt, suggesting that measurement of inhibition of crucial signaling pathways may better predict response than inhibition of receptor phosphorylation.", "entity1": "Akt", "entity2": "GW572016", "span1": [117, 120], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14899": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO1", "entity2": "TMAO", "span1": [62, 66], "span2": [156, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9922": {"label": 1, "data": {"text": "By using the technique of site-directed spin labeling combined with EPR spectroscopy, we have observed that binding of arachidonic acid and nonsteroidal anti-inflammatory drugs induces conformational changes in the human prostaglandin endoperoxide H(2) synthase enzyme (PGHS-2).", "entity1": "human prostaglandin endoperoxide H(2) synthase enzyme", "entity2": "arachidonic acid", "span1": [215, 268], "span2": [119, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14732": {"label": 1, "data": {"text": "Apocynin and raisanberine alleviate intermittent hypoxia induced abnormal StAR and 3\u03b2-HSD and low testosterone by suppressing endoplasmic reticulum stress and activated p66Shc in rat testes.", "entity1": "3\u03b2-HSD", "entity2": "Apocynin", "span1": [83, 89], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5728": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "fibrates", "span1": [83, 86], "span2": [147, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15843": {"label": 1, "data": {"text": "These results suggest that ABCA1 actively eliminates 24-OHC in the presence of HDL as a lipid acceptor and protects neuronal cells.", "entity1": "HDL", "entity2": "24-OHC", "span1": [79, 82], "span2": [53, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4005": {"label": 8, "data": {"text": "In vitro accumulation studies conducted in Madin-Darby canine kidney II cells indicate that dabrafenib is an avid substrate for both P-gp and BCRP.", "entity1": "BCRP", "entity2": "dabrafenib", "span1": [142, 146], "span2": [92, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15189": {"label": 3, "data": {"text": "The involvement of P-gp in the absorption of darunavir was clearly shown by coperfusion of darunavir with the P-gp inhibitor zosuquidar.", "entity1": "P-gp", "entity2": "zosuquidar", "span1": [110, 114], "span2": [125, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4113": {"label": 3, "data": {"text": "Synthesis, molecular modeling and evaluation of novel N'-2-(4-benzylpiperidin-/piperazin-1-yl)acylhydrazone derivatives as dual inhibitors for cholinesterases and A\u03b2 aggregation.", "entity1": "cholinesterases", "entity2": "N'-2-(4-benzylpiperidin-/piperazin-1-yl)acylhydrazone", "span1": [143, 158], "span2": [54, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15075": {"label": 9, "data": {"text": "Pharmacodynamic data suggest that ceftazidime-avibactam is rapidly bactericidal versus \u03b2-lactamase-producing Gram-negative bacilli that are not inhibited by ceftazidime alone.Clinical trials to date have reported that ceftazidime-avibactam is as effective as standard carbapenem therapy in complicated intra-abdominal infection and complicated urinary tract infection, including infection caused by cephalosporin-resistant Gram-negative isolates.", "entity1": "\u03b2-lactamase", "entity2": "ceftazidime", "span1": [87, 98], "span2": [157, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"9150": {"label": 9, "data": {"text": "Co-incubation with human serum albumin or poly-L-lysine but not lysine protected human and hamster LDH-X from gossypol.", "entity1": "human and hamster LDH-X", "entity2": "gossypol", "span1": [81, 104], "span2": [110, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1967": {"label": 5, "data": {"text": "Brain but not spinal NR2B receptor is responsible for the anti-allodynic effect of an NR2B subunit-selective antagonist CP-101,606 in a rat chronic constriction injury model.", "entity1": "NR2B", "entity2": "CP-101,606", "span1": [86, 90], "span2": [120, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6363": {"label": 1, "data": {"text": "The affinity and functional profile of opioids possessing activity at the nociceptin receptor was determined using [3H]nociceptin and nociceptin-stimulated [35S]GTPgammaS binding.", "entity1": "nociceptin receptor", "entity2": "[35S]GTPgammaS", "span1": [74, 93], "span2": [156, 170]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5193": {"label": 1, "data": {"text": "Though FUR alone obviously induced endoplasmic reticulum stress, this signaling pathway may not contribute to the synergetic anti-proliferative effect as the protein expression of CHOP and BIP was similar in FUR alone and combined treatment group.", "entity1": "CHOP", "entity2": "FUR", "span1": [180, 184], "span2": [208, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8430": {"label": 3, "data": {"text": "N-acetylcysteine (NAC, 33 mM) and the c-jun N-terminal kinase (JNK) inhibitor (SP600125, 33 \u03bcM) further decreased the viability in the presence of DEP (200 \u03bcg/ml) and 3.3% FCS.", "entity1": "c-jun N-terminal kinase", "entity2": "SP600125", "span1": [38, 61], "span2": [79, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12362": {"label": 1, "data": {"text": "During base excision repair of this mispair, DNA polymerase (pol) \u03b2 is confronted with gap filling opposite 8-oxoG.", "entity1": "DNA polymerase (pol) \u03b2", "entity2": "8-oxoG", "span1": [45, 67], "span2": [108, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2404": {"label": 1, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "arginases", "entity2": "N(omega)-hydroxy-nor-L-arginine", "span1": [203, 212], "span2": [136, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3259": {"label": 2, "data": {"text": "Here, translocation studies using the human androgen receptor (hAR) and the human glucocorticoid receptor (hGR) were performed to aid in identifying the mechanism by which anabolic-androgenic steroids (AAS) were activating hAR and potentially interacting with hGR and how glucocorticoid ligands were interacting with the hGR and hAR.", "entity1": "hAR", "entity2": "steroids", "span1": [223, 226], "span2": [192, 200]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15995": {"label": 1, "data": {"text": "Here we show that puerarin increases proliferation and differentiation and opposes cisplatin-induced apoptosis in human osteoblastic MG-63 cells containing two estrogen receptor (ER) isoforms.", "entity1": "estrogen receptor", "entity2": "puerarin", "span1": [160, 177], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6481": {"label": 3, "data": {"text": "Reactivation potentials of BuChE (the difference between oxime-reactivated and -unreactivated enzyme activity) declined significantly with time after organophosphate ingestion.", "entity1": "BuChE", "entity2": "organophosphate", "span1": [27, 32], "span2": [150, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4055": {"label": 3, "data": {"text": "In this study, focus was given to evaluate the ability of neoechinulin A, an indole alkaloid isolated from marine-derived Microsporum sp., to attenuate microglial activation by oligomeric amyloid-\u03b2 1-42 (A\u03b242).", "entity1": "A\u03b242", "entity2": "neoechinulin A", "span1": [204, 208], "span2": [58, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14420": {"label": 2, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C. Furthermore, the AMPK activator 5-amino-1-\u03b2-D-ribofuranosyl-imidazole-4-carboxamide (AICAR) significantly inhibited ghrelin secretion.", "entity1": "AMPK", "entity2": "AICAR", "span1": [187, 191], "span2": [255, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1000": {"label": 8, "data": {"text": "The frdA gene coding for subunit A of FRD, and two control genes, copA and copP associated with the export of copper out of H. pylori, were inactivated by insertion of the chloramphenicol acetyltransferase cassette into these individual genes.", "entity1": "copP", "entity2": "copper", "span1": [75, 79], "span2": [110, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10600": {"label": 1, "data": {"text": "Both the abundance of transferrin receptors and upregulation of ribonucleotide reductase render tumors susceptible to gallium-induced cytotoxicity.", "entity1": "ribonucleotide reductase", "entity2": "gallium", "span1": [64, 88], "span2": [118, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7234": {"label": 3, "data": {"text": "GnRH-induced Pyk2 activation opposed the association of Hic-5 with androgen receptor as overexpression of a dominant negative Pyk2 enhanced the GnRH-induced nuclear translocation of a green fluorescent protein-tagged human androgen receptor.", "entity1": "androgen receptor", "entity2": "GnRH", "span1": [67, 84], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14620": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Ala119Gly", "entity2": "2',2'-difluorodeoxyuridine", "span1": [81, 90], "span2": [255, 281]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11837": {"label": 1, "data": {"text": "There was a significant overlap (42 genes) between the 3 and 30 ppb differentially expressed gene lists, with two of these genes (CYP17A1 and SAMHD1) present in all three atrazine treatments.", "entity1": "CYP17A1", "entity2": "atrazine", "span1": [130, 137], "span2": [171, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13753": {"label": 1, "data": {"text": "The L-type calcium channel (LTCC) isoforms Ca(v)1.2 and Ca(v)1.3 display similar 1,4-dihydropyridine (DHP) binding properties and are both expressed in mammalian brain.", "entity1": "Ca(v)1.2", "entity2": "1,4-dihydropyridine", "span1": [43, 51], "span2": [81, 100]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2555": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "c-FMS", "entity2": "imatinib mesylate", "span1": [271, 276], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4602": {"label": 8, "data": {"text": "In relation to zinc bioavailability, \u03b1-CPPs, \u03b2-CPPs, \u03b1(s1)-CN(64-74)4P and \u03b2-CN(1-25)4P increased zinc uptake.", "entity1": "\u03b1(s1)-CN", "entity2": "zinc", "span1": [53, 61], "span2": [98, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11346": {"label": 3, "data": {"text": "Block of human NaV1.5 sodium channels by novel alpha-hydroxyphenylamide analogues of phenytoin.", "entity1": "human NaV1.5", "entity2": "alpha-hydroxyphenylamide", "span1": [9, 21], "span2": [47, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3763": {"label": 6, "data": {"text": "Hydrogen sulfide as an allosteric modulator of ATP-sensitive potassium channels in colonic inflammation.", "entity1": "ATP-sensitive potassium channels", "entity2": "Hydrogen sulfide", "span1": [47, 79], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"2679": {"label": 9, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "c-Kit", "entity2": "IM", "span1": [50, 55], "span2": [93, 95]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5830": {"label": 3, "data": {"text": "The benzothiophene hydroxyurea, zileuton, is the first selective 5-LO inhibitor evaluated for the treatment of patients with IBD.", "entity1": "5-LO", "entity2": "benzothiophene hydroxyurea", "span1": [65, 69], "span2": [4, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14541": {"label": 3, "data": {"text": "Biochemical analyses showed that NO and ROS production and iNOS activity were significantly reduced by catalpol.", "entity1": "iNOS", "entity2": "catalpol", "span1": [59, 63], "span2": [103, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6513": {"label": 3, "data": {"text": "Angiotensin II suppression in humans by the orally active renin inhibitor Aliskiren (SPP100): comparison with enalapril.", "entity1": "Angiotensin II", "entity2": "SPP100", "span1": [0, 14], "span2": [85, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2383": {"label": 3, "data": {"text": "A novel class of biaryl urea that inhibits C-RAF kinase was discovered using a combination of medicinal and combinatorial chemistry approaches.", "entity1": "C-RAF", "entity2": "biaryl urea", "span1": [43, 48], "span2": [17, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1155": {"label": 4, "data": {"text": "In an earlier report, DRD2 E8 A/A genotype was associated with reduced responsiveness to the dopamine D2 agonist apomorphine; however, it is not clear whether both findings share the same biological basis.", "entity1": "dopamine D2", "entity2": "apomorphine", "span1": [93, 104], "span2": [113, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12487": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO3", "entity2": "trimethylamine", "span1": [81, 85], "span2": [119, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13160": {"label": 2, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "FADD", "entity2": "paclitaxel", "span1": [319, 323], "span2": [378, 388]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11867": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "AhR", "entity2": "malvidin", "span1": [145, 148], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14644": {"label": 8, "data": {"text": "Gemcitabine (dFdC, 2',2'-difluorodeoxycytidine) is metabolized by cytidine deaminase (CDA) and deoxycytidine kinase (DCK), but the contribution of genetic variation in these enzymes to the variability in systemic exposure and response observed in cancer patients is unclear.", "entity1": "deoxycytidine kinase", "entity2": "2',2'-difluorodeoxycytidine", "span1": [95, 115], "span2": [19, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13220": {"label": 9, "data": {"text": "EGTA and 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetra acetic acid tetrakis (BAPTA), two Ca2+ chelators, but not nifedipine, an L-type Ca2+ channel blocker, prevented GRIP1 degradation.", "entity1": "GRIP1", "entity2": "nifedipine", "span1": [167, 172], "span2": [113, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12193": {"label": 8, "data": {"text": "VGLUT1 is localized in transcytotic vesicles and accumulates L-glutamate.", "entity1": "VGLUT1", "entity2": "L-glutamate", "span1": [0, 6], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11020": {"label": 3, "data": {"text": "We compared the effects of Captopril (an ACE inhibitor with -SH group), enalapril (an ACE-inhibitor without -SH group), N-acetylcysteine (only -SH group not ACE inhibitor) on endothelial dysfunction injured by methionine-induced hyperhomocysteinemia (HHcy) in rats.", "entity1": "ACE", "entity2": "SH", "span1": [41, 44], "span2": [61, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6630": {"label": 1, "data": {"text": "5TFI was incorporated into a model target protein, murine dihydrofolate reductase (mDHFR), in an isoleucine auxotrophic Escherichia coli host strain suspended in 5TFI-supplemented minimal medium depleted of isoleucine.", "entity1": "murine dihydrofolate reductase", "entity2": "5TFI", "span1": [51, 81], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4712": {"label": 3, "data": {"text": "Thus, the TCDD-induced reduction in canonical Wnt signaling is associated with a decrease in activators (Rspo2 and Rspo3) rather than an increase in inhibitors (Dkk1 and Dkk2) of the pathway.", "entity1": "Rspo3", "entity2": "TCDD", "span1": [115, 120], "span2": [10, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3580": {"label": 3, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u. ); on the other hand, exercise training increased pIR by 76\u00a0% in MSG mice without affecting control mice (MSG, 11.8\u00a0\u00b1\u00a00.3; control, 12.8\u00a0\u00b1\u00a00.2\u00a0a.u.).", "entity1": "pIR", "entity2": "MSG", "span1": [53, 56], "span2": [199, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12237": {"label": 1, "data": {"text": "These data indicate that neuroprotection provided by estrogen against MPP(+) toxicity is mediated by ERalpha and involves an interplay among at least two cell types.", "entity1": "ERalpha", "entity2": "estrogen", "span1": [101, 108], "span2": [53, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9121": {"label": 1, "data": {"text": "However, in contrast to the reversible binding of most phenothiazines to calmodulin, phenoxybenzamine bound to calmodulin irreversibly.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [111, 121], "span2": [85, 101]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15185": {"label": 2, "data": {"text": "While sophocarpine treatment resulted in: significant improvement of steatosis (>50% decrease), decrease of leptin expression (<0.57-fold) and increase of adiponectin expression (>1.48-fold).", "entity1": "adiponectin", "entity2": "sophocarpine", "span1": [155, 166], "span2": [6, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15162": {"label": 2, "data": {"text": "Correlating with FSH\u03b2 activation, both PKA activity and levels of pCREB were increased to a greater extent by low compared with high GnRH pulse frequencies, and the induction of pCREB was also attenuated by overexpression of DNPKA at both low and high pulse frequencies.", "entity1": "PKA", "entity2": "GnRH", "span1": [39, 42], "span2": [133, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15824": {"label": 5, "data": {"text": "Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (Part I).", "entity1": "histamine H3 receptor", "entity2": "aryl amides", "span1": [64, 85], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2655": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "5-nitro-2,N,N-trimethylbenzenesulfonamide", "span1": [397, 414], "span2": [317, 358]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12227": {"label": 2, "data": {"text": "EC50 values for S-(+)-METH were 0.89, 0.92, and 4.44 microM for rTAAR1, mTAAR1, and h-rChTAAR1, respectively.", "entity1": "h-rChTAAR1", "entity2": "S-(+)-METH", "span1": [84, 94], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4380": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "midazolam", "span1": [171, 176], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10387": {"label": 1, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "BuChE", "entity2": "MF-8622", "span1": [75, 80], "span2": [103, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3172": {"label": 4, "data": {"text": "Terbutaline (Bricanyl) and its prodrug Bambuterol (Bambec) are highly potent beta(2)-adrenoceptor agonists often used in asthma patients.", "entity1": "beta(2)-adrenoceptor", "entity2": "Bambec", "span1": [77, 97], "span2": [51, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12450": {"label": 1, "data": {"text": "Meanwhile, the alterations of cyclin A and B1, p-CDK1 and p-cdc25c levels were also observed in response to DICO treatment.", "entity1": "p-cdc25c", "entity2": "DICO", "span1": [58, 66], "span2": [108, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2425": {"label": 8, "data": {"text": "Mitochondrial arginase II modulates nitric-oxide synthesis through nonfreely exchangeable L-arginine pools in human endothelial cells.", "entity1": "Mitochondrial arginase II", "entity2": "L-arginine", "span1": [0, 25], "span2": [90, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13189": {"label": 1, "data": {"text": "2beta-carbomethoxy-3beta-(3'-((Z)-2-iodoethenyl)phenyl)nortropane (mZIENT, 1) and 2beta-carbomethoxy-3beta-(3'-((Z)-2-bromoethenyl)phenyl)nortropane (mZBrENT, 2) were synthesized and evaluated for binding to the human serotonin, dopamine, and norepinephrine transporters (SERT, DAT, and NET, respectively) using transfected cells.", "entity1": "SERT", "entity2": "mZBrENT", "span1": [272, 276], "span2": [150, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4369": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "dexamethasone 21-phosphate", "span1": [280, 285], "span2": [192, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6745": {"label": 3, "data": {"text": "Although highly homologous to other class III RTKs, Flt3 is resistant to the phenylaminopyrimidine STI571 (Gleevec, Imatinib), a potent inhibitor of other RTKs in the family, such as the PDGFbeta-receptor or c-Kit.", "entity1": "RTKs", "entity2": "STI571", "span1": [155, 159], "span2": [99, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6814": {"label": 2, "data": {"text": "These results suggest that pitavastatin efficiently increases apoA-I in the culture medium of HepG2 cells by promoting apoA-I production through inhibition of HMG-CoA reductase and suppression of Rho activity and by protecting apoA-I from catabolism through ABCA1 induction and lipidation of apoA-I.", "entity1": "apoA-I", "entity2": "pitavastatin", "span1": [62, 68], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15407": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-1\u03b2", "entity2": "stigmasterol", "span1": [64, 69], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"13030": {"label": 2, "data": {"text": "inactivation of cortisol to cortisone) to prevent activation of the mineralocorticoid receptor (MR) by cortisol.", "entity1": "MR", "entity2": "cortisol", "span1": [96, 98], "span2": [103, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1116": {"label": 2, "data": {"text": "RESULTS: Indomethacin, in vitro and in vivo. induces an increase in erythorcyte CA I and CA II activity.", "entity1": "CA II", "entity2": "Indomethacin", "span1": [89, 94], "span2": [9, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6004": {"label": 0, "data": {"text": "The N-terminal portion of TSG-6 shows sequence homology to members of the cartilage link protein family of hyaluronan binding proteins.", "entity1": "TSG-6", "entity2": "N", "span1": [26, 31], "span2": [4, 5]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5769": {"label": 3, "data": {"text": "NSDA neurons displayed significant axon terminal degeneration (as indexed by decreases in DA, tyrosine hydroxylase (TH) and DA transporter concentrations in the striatum) as well as loss of TH-immunoreactive (IR) neurons in the substantia nigra (SN) following MPTP, whereas TIDA neurons revealed no overt axon terminal pathology or loss of TH-IR cell bodies.", "entity1": "DA transporter", "entity2": "MPTP", "span1": [124, 138], "span2": [260, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12918": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "CSE", "entity2": "Hydrogen sulfide", "span1": [119, 122], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1048": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "etoposide", "span1": [162, 166], "span2": [194, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13518": {"label": 9, "data": {"text": "Moreover, the CDO active site is essentially unreactive toward NO in the absence of substrate, suggesting an obligate ordered binding of l-cysteine prior to NO.", "entity1": "CDO", "entity2": "NO", "span1": [14, 17], "span2": [63, 65]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8575": {"label": 3, "data": {"text": "Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors.", "entity1": "JAK3", "entity2": "5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers", "span1": [84, 88], "span2": [31, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15576": {"label": 1, "data": {"text": "Our results revealed an important role of base excision repair (BER) as the ntg1, ntg2, apn1 and apn2 mutants showed pronounced sensitivity to essential oil and nerolidol.", "entity1": "apn1", "entity2": "nerolidol", "span1": [88, 92], "span2": [161, 170]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2232": {"label": 3, "data": {"text": "In this study, we demonstrate significant inhibitory activity of dasatinib against both wild-type KIT and the KITD816V mutation in the nanomolar range in in vitro and cell-based kinase assays.", "entity1": "KIT", "entity2": "dasatinib", "span1": [98, 101], "span2": [65, 74]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"737": {"label": 7, "data": {"text": "Angiotensin-converting enzyme inhibition and AT1 receptor blockade modify the pressure-natriuresis relationship by additive mechanisms in rats with human renin and angiotensinogen genes.", "entity1": "angiotensinogen", "entity2": "Angiotensin", "span1": [164, 179], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7540": {"label": 3, "data": {"text": "Phenelzine (PLZ), a nonselective irreversible inhibitor of monoamine oxidase (MAO), also inhibits GABA-transaminase (GABA-T), markedly increasing brain GABA levels.", "entity1": "MAO", "entity2": "Phenelzine", "span1": [78, 81], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7596": {"label": 1, "data": {"text": "The interaction of holo- and apo-forms of human alpha-lactalbumin with fatty acids was studied by a partition equilibrium method.", "entity1": "human alpha-lactalbumin", "entity2": "fatty acids", "span1": [42, 65], "span2": [71, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1202": {"label": 9, "data": {"text": "Also in contrast to effects of multiple METH injections, 1) MDMA caused little or no decrease in binding of the DAT ligand WIN35428, and 2) neither prevention of hyperthermia nor prior depletion of DA prevented the MDMA-induced reduction in plasmalemmal DA transport.", "entity1": "DAT", "entity2": "MDMA", "span1": [112, 115], "span2": [60, 64]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1204": {"label": 1, "data": {"text": "Also in contrast to effects of multiple METH injections, 1) MDMA caused little or no decrease in binding of the DAT ligand WIN35428, and 2) neither prevention of hyperthermia nor prior depletion of DA prevented the MDMA-induced reduction in plasmalemmal DA transport.", "entity1": "DAT", "entity2": "WIN35428", "span1": [112, 115], "span2": [123, 131]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11445": {"label": 1, "data": {"text": "Effect of thalidomide on COX-1 and COX-2 in vivo was consistent with that of in vitro.", "entity1": "COX-2", "entity2": "thalidomide", "span1": [35, 40], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10486": {"label": 5, "data": {"text": "The aim of this study was, therefore, to provide comparative binding characteristics of agonists (epinephrine, norepinephrine, isoproterenol, fenoterol, salbutamol, salmeterol, terbutalin, formoterol, broxaterol) and antagonists (propranolol, alprenolol, atenolol, metoprolol, bisoprolol, carvedilol, pindolol, BRL 37344, CGP 20712, SR 59230A, CGP 12177, ICI 118551) at all three subtypes of human beta-adrenergic receptors in an identical cellular background.", "entity1": "human beta-adrenergic receptors", "entity2": "propranolol", "span1": [392, 423], "span2": [230, 241]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"657": {"label": 3, "data": {"text": "Inhibition of gelatinase A (MMP-2) by batimastat and captopril reduces tumor growth and lung metastases in mice bearing Lewis lung carcinoma.", "entity1": "gelatinase A", "entity2": "captopril", "span1": [14, 26], "span2": [53, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2894": {"label": 4, "data": {"text": "Noradrenaline and phenylephrine (alpha(1)-adrenoceptor agonist) each produced a concentration-dependent tonic contraction, their pD(2) values being 6.87+/-0.08 and 6.10+/-0.05, respectively.", "entity1": "alpha(1)-adrenoceptor", "entity2": "Noradrenaline", "span1": [33, 54], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8404": {"label": 0, "data": {"text": "Substitution of the FLT3 \"gatekeeper\" phenylalanine with leucine (F691L) conferred mild resistance to ponatinib, but substitutions at the FLT3 activation loop (AL) residue D835 conferred a high degree of resistance.", "entity1": "FLT3", "entity2": "leucine", "span1": [20, 24], "span2": [57, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8120": {"label": 3, "data": {"text": "Both CE and E(2) alone increased DNA synthesis and reduced apoptosis with activation of MAPK, Akt, and p70S6K and up-regulation of antiapoptotic factors survivin, Bcl-2, and X-linked inhibitor of apoptosis protein, These effects could be completely blocked by BZA.", "entity1": "MAPK", "entity2": "BZA", "span1": [88, 92], "span2": [260, 263]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15359": {"label": 9, "data": {"text": "Neither oxycodone nor its metabolites activated PXR, CAR, or AhR.", "entity1": "PXR", "entity2": "oxycodone", "span1": [48, 51], "span2": [8, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10355": {"label": 1, "data": {"text": "Investigation of bradykinin metabolism in human and rat plasma in the presence of the dual ACE/NEP inhibitors GW660511X and omapatrilat.", "entity1": "bradykinin", "entity2": "GW660511X", "span1": [17, 27], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7239": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "AMPH", "span1": [231, 237], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14370": {"label": 3, "data": {"text": "Several effects of polyphenols are useful in this scenario, including a reduction in the activities of cytokines and modulation of cellular metabolism through histone deacetylase inhibitors, AMPK activators, calorie-restriction mimetics or epigenetic regulators.", "entity1": "histone deacetylase", "entity2": "polyphenols", "span1": [159, 178], "span2": [19, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"101": {"label": 4, "data": {"text": "The anti-amnesic effect of minaprine on the cycloheximide-induced memory impairment was also antagonized by a serotonin (5-HT) releaser, p-chloroamphetamine, and by a 5-HT precursor, 5-hydroxytryptophan, whereas a 5-HT1A-selective agonist, 8-hydroxy-2-(di-n-propylamino)tetralin, was inactive.", "entity1": "5-HT1A", "entity2": "8-hydroxy-2-(di-n-propylamino)tetralin", "span1": [214, 220], "span2": [240, 278]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15603": {"label": 1, "data": {"text": "TCPOBOP, a CAR ligand, modestly induced mdr1a.fLUC in pxr(+/+) and pxr(-/-) strains, consistent with CAR's minor role in mdr1a regulation.", "entity1": "mdr1a", "entity2": "TCPOBOP", "span1": [121, 126], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"211": {"label": 5, "data": {"text": "We conclude that alprenolol and BAAM are competitive slowly reversible beta 1-adrenoceptor antagonists on rat left atria.", "entity1": "beta 1-adrenoceptor", "entity2": "BAAM", "span1": [71, 90], "span2": [32, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8900": {"label": 5, "data": {"text": "In the hot-plate test in mice, the antinociceptive action of the alpha 2-adrenoceptor agonist, UK 14,304, was abolished by the alpha 2-adrenoceptor antagonist, idazoxan, the potent alpha 2A-adrenoceptor antagonist, RX 821002 and the preferential alpha 2A-adrenoceptor antagonist, BRL 44408.", "entity1": "alpha 2A-adrenoceptor", "entity2": "RX 821002", "span1": [181, 202], "span2": [215, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2478": {"label": 5, "data": {"text": "beta(1)-Adrenoceptor antagonism (10 mg kg(-1) bisoprolol) prevented 92% (P < 0.05) of apoptosis induced by all three agonists, but clenbuterol-induced apoptosis could also be prevented by 96% (P < 0.05) by beta(2)-AR antagonism (10 mg kg(-1) ICI 118 551).", "entity1": "beta(1)-Adrenoceptor", "entity2": "bisoprolol", "span1": [0, 20], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14665": {"label": 1, "data": {"text": "Phytoestrogen genistein protects against endothelial barrier dysfunction in vascular endothelial cells through PKA-mediated suppression of RhoA signaling.", "entity1": "PKA", "entity2": "genistein", "span1": [111, 114], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3789": {"label": 2, "data": {"text": "Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation.", "entity1": "FAS", "entity2": "glucose", "span1": [71, 74], "span2": [34, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1847": {"label": 8, "data": {"text": "SR-BI is a receptor that binds HDL with high affinity and mediates both the selective lipid uptake of cholesteryl esters from lipid-rich HDL to cells and the efflux of unesterified cholesterol from cells to HDL.", "entity1": "SR-BI", "entity2": "cholesteryl esters", "span1": [0, 5], "span2": [102, 120]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10175": {"label": 3, "data": {"text": "Inhibition of human liver OATPs can explain the previously observed effects of rifamycin SV and rifampicin on hepatic organic anion elimination.", "entity1": "human liver OATPs", "entity2": "rifampicin", "span1": [14, 31], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4373": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "midazolam", "span1": [280, 285], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15153": {"label": 1, "data": {"text": "Expression of pituitary FSH and LH, under the control of pulsatile GnRH, is essential for fertility.", "entity1": "LH", "entity2": "GnRH", "span1": [32, 34], "span2": [67, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8904": {"label": 8, "data": {"text": "The identity of the lung beta-ADHs was further demonstrated by their characteristic pH-activity profiles for ethanol oxidation, Km values for NAD and ethanol, and inhibition by 4-methylpyrazole or 1,10-phenanthroline.", "entity1": "beta-ADHs", "entity2": "ethanol", "span1": [25, 34], "span2": [109, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9195": {"label": 1, "data": {"text": "We have found that certain naphthalenesulfonamides [e.g., N-6(-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7)] and phenothiazines [e.g., trifluoperazine (TFP)] induce a loss of cell-surface receptors for alpha 2-macroglobulin, and epidermal growth factor (EGF) in fibroblasts.", "entity1": "alpha 2-macroglobulin", "entity2": "naphthalenesulfonamides", "span1": [209, 230], "span2": [27, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12645": {"label": 1, "data": {"text": "Salicylic acid promotes dissociation of (125)I-ET-1 ETA receptor complexes both in the absence and the presence of unlabeled ET-1.", "entity1": "ET-1", "entity2": "Salicylic acid", "span1": [47, 51], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10705": {"label": 1, "data": {"text": "Dextromethorphan and dimemorfan are high-affinity ligands at sigma1 receptors.", "entity1": "sigma1 receptors", "entity2": "Dextromethorphan", "span1": [61, 77], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10206": {"label": 8, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP-C", "entity2": "BSP", "span1": [36, 42], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3607": {"label": 6, "data": {"text": "Ifenprodil is an allosteric inhibitor of GluN1/GluN2B N-methyl-D-aspartate receptors.", "entity1": "GluN2B", "entity2": "Ifenprodil", "span1": [47, 53], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"828": {"label": 3, "data": {"text": "SC-51089 (10(-5) M), a selective EP1-receptor antagonist, showed no effect on the PGE1- or PGE2-induced inhibition of the HVA ICa, thereby indicating that PGE1- and PGE2-induced inhibition of the HVA Ca2+ channels is possibly mediated by the EP3 receptor.", "entity1": "HVA Ca2+ channels", "entity2": "PGE1", "span1": [196, 213], "span2": [155, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4656": {"label": 1, "data": {"text": "Endothelial dysfunction induced by SIRT1 inhibition was prevented by treatment of the vessels with the NADPH oxidase inhibitor apocynin or superoxide dismutase.", "entity1": "SIRT1", "entity2": "apocynin", "span1": [35, 40], "span2": [127, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3124": {"label": 8, "data": {"text": "alpha-Tocopherol transfer protein (alpha-TTP), the product of the gene responsible for familial isolated vitamin E deficiency, plays an important role in maintaining the plasma alpha-tocopherol level by mediating the secretion of alpha-tocopherol by the liver.", "entity1": "alpha-Tocopherol transfer protein", "entity2": "alpha-tocopherol", "span1": [0, 33], "span2": [230, 246]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2405": {"label": 1, "data": {"text": "To determine whether arginases modulate the endothelial NO synthesis, we investigated the effects of the competitive arginase inhibitor N(omega)-hydroxy-nor-L-arginine (Nor-NOHA) on the activity of NOS, arginases, and L-arginine transporter and on NO release at surface of human umbilical vein endothelial cells (HUVECs).", "entity1": "L-arginine transporter", "entity2": "N(omega)-hydroxy-nor-L-arginine", "span1": [218, 240], "span2": [136, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14312": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "HO-1", "entity2": "DMF", "span1": [105, 109], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5423": {"label": 1, "data": {"text": "Additionally, MPTP significantly down-regulated Bcl-2 expression in the mitochondria of dopaminergic cells in the SN, followed by an increase in Bax expression, cytochrome C translocation to the cytosol, andcleaved-caspase-3 expression, whereas these were inhibited by CRE or EB treatment.", "entity1": "cytochrome C", "entity2": "MPTP", "span1": [161, 173], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2274": {"label": 8, "data": {"text": "CONCLUSIONS: Total vitamin B6 is abnormally high in autism, consistent with previous reports of an impaired pyridoxal kinase for the conversion of pyridoxine and pyridoxal to PLP.", "entity1": "pyridoxal kinase", "entity2": "pyridoxal", "span1": [108, 124], "span2": [162, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7227": {"label": 1, "data": {"text": "GnRH-induced c-Src activation resulted in the phosphorylation of expressed Hic-5 and promoted its association with the human androgen receptor.", "entity1": "human androgen receptor", "entity2": "GnRH", "span1": [119, 142], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12829": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "PNPO", "entity2": "PLP", "span1": [156, 160], "span2": [69, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3883": {"label": 3, "data": {"text": "However, combined treatment with cinobufagin and SB216367 resulted in a significant reduction in p65 and an increase in cleaved-PARP in U2OS cells.", "entity1": "p65", "entity2": "SB216367", "span1": [97, 100], "span2": [49, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7472": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "Kainate-selective ionotropic glutamate receptors", "entity2": "L-glutamate", "span1": [0, 48], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11281": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "GDC", "entity2": "Gly", "span1": [111, 114], "span2": [198, 201]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8722": {"label": 3, "data": {"text": "From the 10 isolated compounds, methyl-3,5-di-O-caffeoylquinate showed the most potent inhibition, with IC50 values of 0.30 and 0.67\u00a0\u03bcM for rAR and rhAR, respectively.", "entity1": "rAR", "entity2": "methyl-3,5-di-O-caffeoylquinate", "span1": [140, 143], "span2": [32, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4376": {"label": 2, "data": {"text": "CYP3A induction in the liver increased depending on the dose of DEX-P, whereas that in intestine showed a mild increase, but the induction level was almost constant regardless of the dose of DEX-P.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [0, 5], "span2": [191, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2038": {"label": 8, "data": {"text": "L-serine dehydratase (SDH), a member of the beta-family of pyridoxal phosphate-dependent (PLP) enzymes, catalyzes the deamination of L-serine and L-threonine to yield pyruvate or 2-oxobutyrate.", "entity1": "SDH", "entity2": "2-oxobutyrate", "span1": [22, 25], "span2": [179, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"15058": {"label": 8, "data": {"text": "Furthermore, they suggest that TRPML1 works in concert with ZnT4 to regulate zinc translocation between the cytoplasm and lysosomes.", "entity1": "TRPML1", "entity2": "zinc", "span1": [31, 37], "span2": [77, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5846": {"label": 3, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT3", "entity2": "metoclopramide", "span1": [96, 101], "span2": [58, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5717": {"label": 1, "data": {"text": "The AKR1C3\u00b7NADP(+)\u00b72'-des-methyl-indomethacin crystal structure was determined, and it revealed a unique inhibitor binding mode.", "entity1": "AKR1C3", "entity2": "NADP(+)", "span1": [4, 10], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6109": {"label": 5, "data": {"text": "In extending these initial findings, we have shown that cardiac fibrosis (i) is not reversed by correction of mineralocorticoid-induced hypokalemia; (ii) appears not to involve the plasma or tissue renin-angiotensin systems, as fibrosis is largely unaffected by concurrent administration of Losartan or Perindopril; (iii) is independent of cardiac hypertrophy, in that it is equally seen in right and left ventricles, and in rats rendered hypertensive without cardiac hypertrophy by the administration of 9 alpha-fluorocortisol; (iv) is independent of elevated blood pressure, in that it is found in normotensive animals infused peripherally with aldosterone and intracerebroventricularly with the mineralocorticoid receptor (MR) antagonist RU28318; (v) is via classical MR, in that it is blocked by concurrent administration of the MR antagonist potassium canrenoate; and (vi) may or may not be a direct cardiac effect, inasmuch as data for in vivo effects on collagen formation by cardiac fibroblasts are conflicting.", "entity1": "MR", "entity2": "potassium canrenoate", "span1": [771, 773], "span2": [847, 867]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15990": {"label": 1, "data": {"text": "Using small interfering double-stranded RNA technology, we further demonstrate that the effects of puerarin on proliferation, differentiation and survival are mediated by both ER\u03b1 and ER\u03b2.", "entity1": "ER\u03b2", "entity2": "puerarin", "span1": [184, 187], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9161": {"label": 3, "data": {"text": "Most reducing cofactors for the peroxidase protect PHS and prostacyclin synthase from inactivation by hydroperoxides.", "entity1": "prostacyclin synthase", "entity2": "hydroperoxides", "span1": [59, 80], "span2": [102, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"2448": {"label": 3, "data": {"text": "In healthy rats, ATB-429 dose dependently (25, 50, or 100 mg/kg) attenuated CRD-induced hypersensitivity and significantly inhibited CRD-induced overexpression of spinal c-FOS mRNA, whereas mesalamine had no effect.", "entity1": "c-FOS", "entity2": "ATB-429", "span1": [170, 175], "span2": [17, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13396": {"label": 2, "data": {"text": "In hearts treated with phenformin for 18 min and then perfused for 20 min with Krebs-Henseleit buffer, [AMP] began to increase at 26 min and AMPK activity was elevated at 36 min.", "entity1": "AMPK", "entity2": "phenformin", "span1": [141, 145], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1209": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "DA transporter", "entity2": "methylenedioxymethamphetamine", "span1": [149, 163], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11825": {"label": 1, "data": {"text": "In preclinical studies, the mammalian target of rapamycin (mTOR) in the medial prefrontal cortex and the eukaryotic elongation factor (eEF2) in the hippocampus have been proposed as critical mediators of ketamine's rapid antidepressant actions.", "entity1": "mTOR", "entity2": "ketamine", "span1": [59, 63], "span2": [204, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4313": {"label": 3, "data": {"text": "The Trx mimetics peptides (TXM) protected insulinoma INS 832/13 cells from oxidative stress induced by selectively inhibiting TrxR with auranofin (AuF).", "entity1": "TrxR", "entity2": "AuF", "span1": [126, 130], "span2": [147, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"95": {"label": 3, "data": {"text": "Catecholamines (adrenaline, noradrenaline and dopamine) are potent inhibitors of phenylalanine 4-monooxygenase (phenylalanine hydroxylase, EC 1.14.16.1).", "entity1": "phenylalanine 4-monooxygenase", "entity2": "dopamine", "span1": [81, 110], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1345": {"label": 1, "data": {"text": "Several active analogues were also evaluated for their ability to block uptake of DA, 5-HT, and NE and inhibit binding of [(125)I] RTI-55 at HEK-hDAT, HEK-hSERT, and HEK-hNET cells.", "entity1": "hDAT", "entity2": "[(125)I] RTI-55", "span1": [145, 149], "span2": [122, 137]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10056": {"label": 3, "data": {"text": "Sulfasalazine was fortuitously found to be a novel, potent inhibitor of the x(c)- transporter.", "entity1": "x(c)- transporter", "entity2": "Sulfasalazine", "span1": [76, 93], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6644": {"label": 1, "data": {"text": "On the other hand, ligands for the renal Na(+)-transporter (amiloride and triamterene) and for imidazoline recognition sites (guanabenz, guanfacine and agmatine) displaced the binding of [(3)H]prazosin to phentolamine-insensitive sites at micromolar concentrations.", "entity1": "Na(+)-transporter", "entity2": "amiloride", "span1": [41, 58], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12052": {"label": 1, "data": {"text": "Acute arsenic treatment alters cytochrome P450 expression and arachidonic acid metabolism in lung, liver and kidney of C57Bl/6 mice.", "entity1": "cytochrome P450", "entity2": "arsenic", "span1": [31, 46], "span2": [6, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3084": {"label": 3, "data": {"text": "CONCLUSIONS: At the doses studied, PLZ was as effective as VIG at elevating brain GABA levels, but, unlike VIG, also inhibited MAO and ALA-T (and increased brain ALA levels).", "entity1": "MAO", "entity2": "VIG", "span1": [127, 130], "span2": [107, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5108": {"label": 2, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "Nrf2", "entity2": "5HHMF", "span1": [159, 163], "span2": [43, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3329": {"label": 3, "data": {"text": "Etoposide (VP-16) is a topoisomerase-II (topo II) inhibitor chemotherapeutic agent.", "entity1": "topoisomerase-II", "entity2": "Etoposide", "span1": [23, 39], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8901": {"label": 5, "data": {"text": "In the hot-plate test in mice, the antinociceptive action of the alpha 2-adrenoceptor agonist, UK 14,304, was abolished by the alpha 2-adrenoceptor antagonist, idazoxan, the potent alpha 2A-adrenoceptor antagonist, RX 821002 and the preferential alpha 2A-adrenoceptor antagonist, BRL 44408.", "entity1": "alpha 2A-adrenoceptor", "entity2": "BRL 44408", "span1": [246, 267], "span2": [280, 289]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11981": {"label": 8, "data": {"text": "Doxorubicin is mainly excreted into the bile via P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (Mrp2) in hepatobiliary route and metabolized via cytochrome P450 (CYP) 3A subfamily.", "entity1": "multidrug resistance-associated protein 2", "entity2": "Doxorubicin", "span1": [75, 116], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6318": {"label": 3, "data": {"text": "We report that the radiation-induced activation of the kinase Cds1 [4] (also known as Chk2 [5]) is inhibited by caffeine in vivo and that ATM kinase activity is directly inhibited by caffeine in vitro.", "entity1": "kinase", "entity2": "caffeine", "span1": [142, 148], "span2": [183, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14977": {"label": 1, "data": {"text": "In this small library of novel bioactive macrocyclic lathyrane diterpene derivatives, designed to evaluate structure-activity relationships essential in overcoming multidrug resistance (MDR), some correlations between MDR reversal and molecular weight, accessible solvent areas, and octanol/water partition coefficient were identified that can contribute to the development of new selective P-gp reversal agents.", "entity1": "P-gp", "entity2": "lathyrane diterpene", "span1": [391, 395], "span2": [53, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14207": {"label": 1, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "galantamine", "span1": [83, 88], "span2": [61, 72]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"563": {"label": 0, "data": {"text": "Ig module I and the C-terminus of Ig module III are dispensable for high-affinity binding of FGF-1, FGF-2, and FGF-7.", "entity1": "Ig module III", "entity2": "C", "span1": [34, 47], "span2": [20, 21]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10407": {"label": 1, "data": {"text": "Unlike OFQ II(1-17), high concentrations of its C-terminal extension, OFQ II(1-28), stimulated [35S]-GTPgammaS binding in a mu (mu) opioid receptor-like distribution and the effect was blocked by naloxone.", "entity1": "mu (mu) opioid receptor", "entity2": "[35S]-GTPgammaS", "span1": [124, 147], "span2": [95, 110]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8032": {"label": 3, "data": {"text": "Whereas the addition of apomorphine in the low micromolar range produced an irreversible activation of the channel, application of higher concentrations caused a reversible voltage-dependent inhibition of heterologously expressed TRPA1 channels, resulting from a reduction of single-channel open times.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [230, 235], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9518": {"label": 1, "data": {"text": "The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RAR beta and RAR gamma.", "entity1": "RAR gamma", "entity2": "retinoid", "span1": [134, 143], "span2": [4, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15084": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "ESBL", "entity2": "avibactam", "span1": [192, 196], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8887": {"label": 3, "data": {"text": "The induction of IGFBP-4 protein was dependent on a functional aryl hydrocarbon receptor and was preceded by a rapid increase in the level of IGFBP-4 mRNA indicating that IGFBP-4 is a previously unknown transcriptional target of TCDD in 5L cells.", "entity1": "IGFBP-4", "entity2": "TCDD", "span1": [142, 149], "span2": [229, 233]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9190": {"label": 2, "data": {"text": "This agent acts synergistically with many penicillins, such as ampicillin, carbenicillin, and the like, and with cephalosporins, cefazolin, cefamandole, or cefoxitin to inhibit gram-negative bacilli, probably on the basis of binding to different proteins needed for the production of the peptidoglycan of the bacterial cell wall.", "entity1": "peptidoglycan", "entity2": "cephalosporins", "span1": [288, 301], "span2": [113, 127]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5724": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "bile acid", "span1": [33, 36], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13300": {"label": 3, "data": {"text": "We investigated the efficacy of sorafenib at inhibiting mutants of the receptor tyrosine kinases PDGFRbeta, KIT, and FLT3, which are implicated in the pathogenesis of myeloid malignancies.", "entity1": "KIT", "entity2": "sorafenib", "span1": [108, 111], "span2": [32, 41]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3646": {"label": 1, "data": {"text": "In rats exposed to DBDCT, apoptosis was also observed in brain, as shown by the detection of cleaved caspase-9 and caspase-3 proteins and increased TUNEL positive staining.", "entity1": "caspase-3", "entity2": "DBDCT", "span1": [115, 124], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11096": {"label": 1, "data": {"text": "The effects of these metabolites on the expression of uteroglobin (UG) and progesterone receptor (PR) genes, both regulated by progesterone (P4), were evaluated in the uterus of prepubertal female rabbits that were simultaneously treated with P4 (1.0 mg) for 5 consecutive days.", "entity1": "UG", "entity2": "progesterone (P4)", "span1": [67, 69], "span2": [127, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5450": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "AR", "entity2": "juglone", "span1": [206, 208], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3812": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Gln", "span1": [148, 153], "span2": [51, 54]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4402": {"label": 1, "data": {"text": "The present study also shows that some of the biological activities of M6P/IGF2R in SCC-VII cells strongly depend on a functional M6P-binding site within domain 3, thus providing further evidence for the non-redundant cellular functions of the individual carbohydrate-binding domains of the receptor.", "entity1": "IGF2R", "entity2": "M6P", "span1": [75, 80], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12403": {"label": 2, "data": {"text": "On the basis of these findings, we conclude that HEP and HCB have additive and synergistic effects on the development of GST-P-positive foci and that higher risks are associated with a combination of residual organochlorine pesticides in foods than with individual residual organochlorine pesticides.", "entity1": "GST-P", "entity2": "HCB", "span1": [121, 126], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1256": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "fluticasone", "span1": [277, 280], "span2": [77, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8494": {"label": 3, "data": {"text": "AlCl3 markedly reduced AA performance and activities of cytochrome c oxidase (COX) and acetylcholinesterase (AChE) in all regions.", "entity1": "COX", "entity2": "AlCl3", "span1": [78, 81], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12179": {"label": 2, "data": {"text": "However, plasma high-density lipoprotein-cholesterol (HDL-C) and HDL-C/total-C ratio levels and plasma paraoxonase activity were only significantly higher in vitamin E group after 8 weeks.", "entity1": "HDL", "entity2": "vitamin E", "span1": [65, 68], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12539": {"label": 1, "data": {"text": "Isolation and characterization of labeled peptides from phenoxybenzamine-modified calmodulins indicated that peptides encompassing residues 38-75, 107-126, and 127-148 contained phenoxybenzamine label.", "entity1": "calmodulins", "entity2": "phenoxybenzamine", "span1": [82, 93], "span2": [178, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7158": {"label": 2, "data": {"text": "Telmisartan downregulates angiotensin II type 1 receptor through activation of peroxisome proliferator-activated receptor gamma.", "entity1": "peroxisome proliferator-activated receptor gamma", "entity2": "Telmisartan", "span1": [79, 127], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15336": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "benzo[c]phenanthrene", "span1": [287, 296], "span2": [13, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13199": {"label": 1, "data": {"text": "In vivo, cromolyn inhibited tumor growth in mice bearing tumor with endogenous S100P (BxPC-3: control, mean = 1.6 x 10(9) photons/s, versus cromolyn, mean = 4.4 x 10(8) photons/s, difference = 1.2 x 10(9) photons/s; 95% CI = 6.2 x 10(8) to 1.6 x 10(9) photons/s; P<.001, n = 5; MPanc-96: control, mean = 1.1 x 10(10) photons/s, versus cromolyn, mean = 4.8 x 10(9) photons/s, difference = 6.2 x 10(9) photons/s; 95% CI = 1.9 x 10(9) to 1.0 x 10(10) photons/s; P = .009, n = 5) and increased the effectiveness of gemcitabine (BxPC-3: gemcitabine, mean = 9.2 x 10(8) photons/s, versus combination, mean = 1.8 x 10(8) photons/s, difference = 7.4 x 10(8) photons/s; 95% CI = 4.5 x 10(8) to 1.0 x 10(9) photons/s; P<.001; MPanc-96: gemcitabine, mean = 4.1 x 10(9) photons/s, versus combination, mean = 2.0 x 10(9) photons/s, difference = 2.1 x 10(9) photons/s; 95% CI = 4.4 x 10(8) to 3.8 x 10(9) photons/s; P<.001).", "entity1": "S100P", "entity2": "gemcitabine", "span1": [79, 84], "span2": [532, 543]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4325": {"label": 3, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "cyclin dependent kinase 2", "entity2": "Pinosylvin", "span1": [177, 202], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3462": {"label": 1, "data": {"text": "Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C.", "entity1": "DAT", "entity2": "[2-(trimethylammonium)ethyl]-methanethiosulfonate", "span1": [232, 235], "span2": [164, 213]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10249": {"label": 8, "data": {"text": "The PAO inhibitor, MDL-72,527, only partially blocked oxidation of spermine while a previously reported PAO substrate, N (1)-( n -octanesulphonyl)spermine, potently inhibited the reaction.", "entity1": "PAO", "entity2": "N (1)-( n -octanesulphonyl)spermine", "span1": [104, 107], "span2": [119, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10024": {"label": 0, "data": {"text": "Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium.", "entity1": "factor Xa", "entity2": "Lys", "span1": [199, 208], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1439": {"label": 3, "data": {"text": "To determine whether 3,4-methylenedioxymethamphetamine (MDMA)-induced reductions in SERT density could be related to such a mechanism, p-chlorophenylalanine or MDMA was administered to rats, and brain serotonin and SERT density were measured.", "entity1": "SERT", "entity2": "3,4-methylenedioxymethamphetamine", "span1": [84, 88], "span2": [21, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15720": {"label": 8, "data": {"text": "d-Amino acid oxidase (DAAO) catalyzes the oxidation of d-amino acids including d-serine, a coagonist of the N-methyl-d-aspartate receptor.", "entity1": "DAAO", "entity2": "d-amino acids", "span1": [22, 26], "span2": [55, 68]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1710": {"label": 9, "data": {"text": "Two mutations that were generated by PCR mutagenesis of the ERG1 gene and that conferred terbinafine resistance mapped in the same regions of the Erg1 protein, with one resulting in an L251F exchange and the other resulting in an F433S exchange.", "entity1": "ERG1", "entity2": "terbinafine", "span1": [60, 64], "span2": [89, 100]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14055": {"label": 3, "data": {"text": "Rectal mucosal samples from patients given aspirin had reduced phosphorylation of S6K1 and S6.", "entity1": "S6K1", "entity2": "aspirin", "span1": [82, 86], "span2": [43, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1462": {"label": 3, "data": {"text": "Rasagiline [N-propargyl-1R(+)-aminoindan; TVP1012] is a potent irreversible monoamine oxidase (MAO) inhibitor with selectivity for type B of the enzyme, which is being developed for treatment of Parkinson's disease.", "entity1": "monoamine oxidase", "entity2": "N-propargyl-1R(+)-aminoindan", "span1": [76, 93], "span2": [12, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9222": {"label": 3, "data": {"text": "Three lines of evidence suggest that calmodulin inhibition is not responsible for the inhibition of binding and endocytosis: 1) Promethazine, a phenothiazine that is a poor inhibitor of calmodulin, is nearly as effective as TFP at inhibiting endocytosis; calmidazolium, a potent inhibitor of several calmodulin functions, did not cause a loss of binding; 2) the microinjection of calmodulin into cells did not reverse the effects of W-7; using pressure microinjection, we introduced up to a 100-fold excess of calmodulin over native levels into individual gerbil fibroma cells; using rhodamine-labeled alpha 2-macroglobulin, we saw that the W-7 induced inhibition of receptor-mediated endocytosis was the same in injected and uninjected cells; 3) we injected calcineurin, a calmodulin-binding protein, into cells (1-3 pg/cell) and observed no effect on the receptor-mediated endocytosis of rhodamine-labeled alpha 2-macroglobulin.", "entity1": "calmodulin", "entity2": "Promethazine", "span1": [300, 310], "span2": [128, 140]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9969": {"label": 3, "data": {"text": "For instance, meloxicam inhibits the growth of cultured colon cancer cells (HCA-7 and Moser-S) that express COX-2 but has no effect on HCT-116 tumor cells that do not express COX-2.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [108, 113], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10796": {"label": 3, "data": {"text": "Moreover, simvastatin concentration-dependently inhibited the expression of ICAM-1 and induced the expression of CD40 on monocytes.", "entity1": "ICAM-1", "entity2": "simvastatin", "span1": [76, 82], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6619": {"label": 0, "data": {"text": "In OTCase, mutations of putative ornithine binding residues, Asp-182, Asn-184, Asn-185, Cys-289, and Glu-256 greatly reduced the affinity for ornithine and impaired the interaction with arginase.", "entity1": "OTCase", "entity2": "Asn", "span1": [3, 9], "span2": [79, 82]}, "weak_labels": [-1, -1, 0, 1, 1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11629": {"label": 3, "data": {"text": "Acetaminophen plasma concentrations remained above the in vitro IC(50) for COX-2 for at least 5 h postadministration.", "entity1": "COX-2", "entity2": "Acetaminophen", "span1": [75, 80], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10125": {"label": 1, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "zomepirac", "span1": [34, 37], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7761": {"label": 3, "data": {"text": "Rescue of this impaired extinction consolidation/retrieval was achieved with d-cycloserine (N-methly-d-aspartate partial agonist) or MS-275 (histone deacetylase (HDAC) inhibitor), applied after extinction training.", "entity1": "HDAC", "entity2": "MS-275", "span1": [162, 166], "span2": [133, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5872": {"label": 9, "data": {"text": "By contrast, neither amoxapine nor amitriptyline can be considered as possible ligands of 5-HT1A and 5-HT1B receptors because their affinities for these sites are in the micromolar range (or even worse).", "entity1": "5-HT1B", "entity2": "amoxapine", "span1": [101, 107], "span2": [21, 30]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"164": {"label": 3, "data": {"text": "Acetylcholinesterase (AChE) inhibited by the organophosphate soman (1,2,2-trimethyl-propylmethylphosphonofluoridate) rapidly becomes resistant to reactivation by oximes due to dealkylation of the soman-enzyme complex.", "entity1": "Acetylcholinesterase", "entity2": "soman", "span1": [0, 20], "span2": [61, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11661": {"label": 1, "data": {"text": "In contrast, thyroid papillary carcinomas, lung adenocarcinomas, hepatocellular carcinomas, pancreatic ductal carcinomas, and renal cell carcinomas, which exhibit low TK-1 expression, may be resistant to TAS-102.", "entity1": "TK-1", "entity2": "TAS-102", "span1": [167, 171], "span2": [204, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9912": {"label": 2, "data": {"text": "Treatment of lactating mice with a single injection of bezafibrate, an activator of the peroxisome proliferator-activated receptor (PPAR), raises UCP-3 mRNA in skeletal muscle to levels similar to those in virgin mice.", "entity1": "UCP-3", "entity2": "bezafibrate", "span1": [146, 151], "span2": [55, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6514": {"label": 3, "data": {"text": "There was a dose-dependent decrease in plasma renin activity, Ang I, and Ang II following single doses of Aliskiren starting with 40 mg. Inhibition was still marked and significant after repeated dosing with maximal decreases in Ang II levels by 89% and 75% on Days 1 and 8, respectively, when the highest dose of Aliskiren was compared with placebo.", "entity1": "Ang II", "entity2": "Aliskiren", "span1": [229, 235], "span2": [314, 323]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"598": {"label": 1, "data": {"text": "15d-PGJ2 did not block nuclear translocation or DNA-binding activity of the transcription factor NFkappaB, but it did inhibit the activity of an NFkappaB reporter construct, suggesting that the mechanism of suppression of microglial iNOS by 15d-PGJ2 may involve interference with NFkappaB transcriptional activity in the nucleus.", "entity1": "NFkappaB", "entity2": "15d-PGJ2", "span1": [280, 288], "span2": [241, 249]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6069": {"label": 3, "data": {"text": "The protein kinase C inhibitor (+)-1-(5-isoquinolinesulfonyl)-2-methylpiperazine dihydrochloride (H-7) abolished the effects of phorbol esters and NE and decreased basal mRNA levels by 52 +/- 3%.", "entity1": "protein kinase C", "entity2": "H-7", "span1": [4, 20], "span2": [98, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15129": {"label": 3, "data": {"text": "Nocapyrone H (1) reduced the pro-inflammatory factor such as nitric oxide (NO), prostaglandin E2 (PGE2) and interleukin-1\u03b2 (IL-1\u03b2).", "entity1": "IL-1\u03b2", "entity2": "Nocapyrone H", "span1": [124, 129], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14422": {"label": 2, "data": {"text": "Metformin significantly reduced ghrelin secretion and proghrelin mRNA production and both these effects were blocked by co-incubation with the AMPK inhibitor compound C.", "entity1": "ghrelin", "entity2": "compound C", "span1": [32, 39], "span2": [158, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1786": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1dAR", "entity2": "terazosin", "span1": [54, 63], "span2": [154, 163]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14436": {"label": 1, "data": {"text": "Fungicide prochloraz and environmental pollutant dioxin induce the ABCG2 transporter in bovine mammary epithelial cells by the arylhydrocarbon receptor signaling pathway.", "entity1": "arylhydrocarbon receptor", "entity2": "prochloraz", "span1": [127, 151], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1129": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "HERG", "entity2": "sertindole", "span1": [173, 177], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11641": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "MAO", "entity2": "PLZ", "span1": [264, 267], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10779": {"label": 3, "data": {"text": "Imatinib mesylate is a tyrosine kinase inhibitor of the ABL, platelet-derived growth factor receptor (PDGFR), and c-kit kinases.", "entity1": "ABL", "entity2": "Imatinib mesylate", "span1": [56, 59], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6163": {"label": 3, "data": {"text": "A 59-year-old female suffering from malignant lymphoma developed therapy-related acute myeloblastic leukemia (t-AML) after chemotherapy consisting of treatment with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and an alkylating agent, cyclophosphamide.", "entity1": "DNA-topoisomerase II", "entity2": "mitoxantrone", "span1": [165, 185], "span2": [212, 224]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4995": {"label": 2, "data": {"text": "Phenobarbital (PB), a typical CAR activator, increased the gene expression of HIF-target genes in the livers of mice, including erythropoietin, heme oxygenase-1 and vascular endothelial growth factor-a.", "entity1": "erythropoietin", "entity2": "Phenobarbital", "span1": [128, 142], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14565": {"label": 2, "data": {"text": "\u03b2-catenin regulates GnRH-induced FSH\u03b2 gene expression.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [33, 37], "span2": [20, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8215": {"label": 3, "data": {"text": "TAA also increased the numbers of ED2(+), cyclooxygenase-2(+), and heme oxygenase-1(+) liver cells, as well as the number of CD3(+) lymphocytes.", "entity1": "CD3", "entity2": "TAA", "span1": [125, 128], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12063": {"label": 3, "data": {"text": "In seven normal subjects, basal ACTH plasma levels were significantly suppressed 3 h after loperamide administration (16 mg, orally) from 5 +/- 1 to 2 +/- 0 pmol/L (P less than 0.0001).", "entity1": "ACTH", "entity2": "loperamide", "span1": [32, 36], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7026": {"label": 8, "data": {"text": "Inhibition of [3H]5-HT or [3H]NE uptake by DVS for the hSERT or hNET produced IC50 values of 47.3 +/- 19.4 and 531.3 +/- 113.0 nM, respectively.", "entity1": "hSERT", "entity2": "[3H]5-HT", "span1": [55, 60], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2763": {"label": 3, "data": {"text": "Taken together with a recent crystal structure of a lumiracoxib-COX-2 complex, the kinetic analyses presented herein of the inhibition of mutant COX-2s by lumiracoxib allows the definition of the molecular basis of COX-2 inhibition.", "entity1": "COX-2s", "entity2": "lumiracoxib", "span1": [145, 151], "span2": [155, 166]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11418": {"label": 1, "data": {"text": "The crystal structure of R228K-Gal-T1 complexed with LA, UDP-Gal, and Mn(2+) determined at 1.9 A resolution shows that the Asp318 side chain exhibits a minor alternate conformation, compared to that in the wild type.", "entity1": "Gal-T1", "entity2": "UDP-Gal", "span1": [31, 37], "span2": [57, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11530": {"label": 3, "data": {"text": "Our results first demonstrate that auranofin suppresses the multiple steps in TLR4 signaling, especially the homodimerization of TLR4.", "entity1": "TLR4", "entity2": "auranofin", "span1": [129, 133], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2278": {"label": 3, "data": {"text": "The work of Chen and colleagues shows that dasatinib is a particularly potent inhibitor of PDGFR and that the compound also targets Src kinase.", "entity1": "PDGFR", "entity2": "dasatinib", "span1": [91, 96], "span2": [43, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14185": {"label": 1, "data": {"text": "Cresyl saligenin phosphate makes multiple adducts on free histidine, but does not form an adduct on histidine 438 of human butyrylcholinesterase.", "entity1": "human butyrylcholinesterase", "entity2": "Cresyl saligenin phosphate", "span1": [117, 144], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14184": {"label": 1, "data": {"text": "Mass spectral analysis of CBDP-inhibited BChE digested with Glu-C showed an o-hydroxybenzyl adduct (+106amu) on lysine 499, a residue far from the active site, but not on His-438.", "entity1": "BChE", "entity2": "Glu", "span1": [41, 45], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"50": {"label": 3, "data": {"text": "Comparison of the monoamine oxidase inhibiting properties of two reversible and selective monoamine oxidase-A inhibitors moclobemide and toloxatone, and assessment of their effect on psychometric performance in healthy subjects.", "entity1": "monoamine oxidase", "entity2": "toloxatone", "span1": [18, 35], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13206": {"label": 8, "data": {"text": "In addition, we found that selenophosphate synthetase 2 could synthesize monoselenophosphate in vitro but selenophosphate synthetase 1 could not.", "entity1": "selenophosphate synthetase 2", "entity2": "monoselenophosphate", "span1": [27, 55], "span2": [73, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8447": {"label": 2, "data": {"text": "l-glutamine decreased plasma glucose, increased plasma and pancreatic insulin, increased plasma and colonic active GLP-1 (7-36) amide secretion as well as decreased oxidative stress in streptozotocin-nicotinamide induced diabetic rats.", "entity1": "insulin", "entity2": "l-glutamine", "span1": [70, 77], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4188": {"label": 1, "data": {"text": "PTE, used in combination with a known JAK2/STAT3 inhibitor, AG490, further decreased the viability of osteosarcoma cells.", "entity1": "STAT3", "entity2": "PTE", "span1": [43, 48], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4453": {"label": 3, "data": {"text": "3'-R/S-Hydroxyvoacamine, a potent acetylcholinesterase inhibitor from Tabernaemontana divaricata.", "entity1": "acetylcholinesterase", "entity2": "3'-R/S-Hydroxyvoacamine", "span1": [34, 54], "span2": [0, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13114": {"label": 9, "data": {"text": "We failed to observe any significant activation of FAS promoter following exposure to the anti-metabolite 5-fluorouracil, the alkylating drug cisplatin, or the microtubule interfering-agents paclitaxel and vincristine.", "entity1": "FAS promoter", "entity2": "5-fluorouracil", "span1": [51, 63], "span2": [106, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2994": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Q817A", "entity2": "3-isobutyl-1-methylxanthine", "span1": [216, 221], "span2": [74, 101]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5699": {"label": 1, "data": {"text": "In addition, we provide evidence that apomorphine also acts on endogenous TRPA1 in cultured dorsal root ganglion neurons from rats and in the enterochromaffin model cell line QGP-1, from which serotonin is released upon activation of TRPA1.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [234, 239], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5427": {"label": 8, "data": {"text": "Cholesterol esterase (CE) induced surface erosion of poly(ethylene carbonate) (PEC) and drug release from PEC under mild physiological environment was investigated.", "entity1": "Cholesterol esterase", "entity2": "PEC", "span1": [0, 20], "span2": [79, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3402": {"label": 3, "data": {"text": "We found that PSE inhibits interleukin-2 (IL-2) and tumor necrosis factor (TNF) alpha-gene transcription in stimulated Jurkat cells, a human T-cell leukemia cell line.", "entity1": "interleukin-2", "entity2": "PSE", "span1": [27, 40], "span2": [14, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15946": {"label": 1, "data": {"text": "Vildagliptin, in addition to metformin, proved to be effective in improving \u03b2-cell function and in reducing insulin resistance measurements.", "entity1": "insulin", "entity2": "Vildagliptin", "span1": [108, 115], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3837": {"label": 3, "data": {"text": "Taken together, the data provide evidence that the synergistic antiproliferative effect of resveratrol and clofarabine is linked to the inhibition of Akt and Sp1 activities, and suggest that this combination may have therapeutic value in treatment of malignant mesothelioma.", "entity1": "Sp1", "entity2": "clofarabine", "span1": [158, 161], "span2": [107, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14334": {"label": 3, "data": {"text": "Dimethylfumarate attenuates renal fibrosis via NF-E2-related factor 2-mediated inhibition of transforming growth factor-beta/Smad signaling.", "entity1": "transforming growth factor-beta", "entity2": "Dimethylfumarate", "span1": [93, 124], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11785": {"label": 8, "data": {"text": "The primary aim of these studies was to test the hypothesis that HSD11B1-derived cortisol has a biological role in endometrial function and conceptus development during early pregnancy in sheep.", "entity1": "HSD11B1", "entity2": "cortisol", "span1": [65, 72], "span2": [81, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"437": {"label": 1, "data": {"text": "Ka values for rauwolscine and WB-4101, drugs distinguishing the alpha-2D from the alpha-2A adrenoceptor subtype, were significantly higher in blocking relaxation of rat arteries compared with pig arteries, suggesting the alpha-2D adrenoceptor subtype mediates NO-induced relaxation in rat arteries.", "entity1": "alpha-2A adrenoceptor", "entity2": "rauwolscine", "span1": [82, 103], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5670": {"label": 2, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "DNMT1", "entity2": "geranylgeranyl-pyrophosphate", "span1": [126, 131], "span2": [180, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2291": {"label": 4, "data": {"text": "The involvement of EP1 and EP2 receptors is indicated by studies with the EP1 selective agonist 17-phenyl trinor PGE2, and the EP2 selective agonist butaprost (which stimulate), as well as by studies with the antagonists SC-51089 (EP1 specific) and AH 6809 (EP1 and EP2 specific).", "entity1": "EP1", "entity2": "SC-51089", "span1": [19, 22], "span2": [221, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7250": {"label": 2, "data": {"text": "The discovery that METH and AMPH activate the rTAAR1 motivated us to study the effect of these drugs on the mouse TAAR1 (mTAAR1) and a human-rat chimera (hrChTAAR1).", "entity1": "rTAAR1", "entity2": "METH", "span1": [46, 52], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6611": {"label": 5, "data": {"text": "The effects of histamine H1-receptor antagonists, promethazine and homochlorcyclizine, both of which are inhibitors of CYP2D6, on the steady-state plasma concentrations (Css) of haloperidol and reduced haloperidol were studied in 23 schizophrenic inpatients receiving haloperidol, 12 to 36 mg/d, for 2 to 29 weeks.", "entity1": "histamine H1-receptor", "entity2": "promethazine", "span1": [15, 36], "span2": [50, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12943": {"label": 8, "data": {"text": "We hypothesized that preservation of plasma L-arg in CRF may be, partly, due to downregulation/inhibition of arginase.", "entity1": "arginase", "entity2": "L-arg", "span1": [109, 117], "span2": [44, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10336": {"label": 2, "data": {"text": "Pre-treatment with arsenite increased protein kinase B (Akt) and extracellular signal regulated kinase 1/2 (ERK1/2) phosphorylation after H2O2.", "entity1": "Akt", "entity2": "H2O2", "span1": [56, 59], "span2": [138, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13832": {"label": 1, "data": {"text": "Mammalian glutamate dehydrogenase (GDH) is a homohexameric enzyme that catalyzes the reversible oxidative deamination of l-glutamate to 2-oxoglutarate using NAD(P)(+) as coenzyme.", "entity1": "GDH", "entity2": "NAD(P)(+)", "span1": [35, 38], "span2": [157, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6317": {"label": 3, "data": {"text": "We report that the radiation-induced activation of the kinase Cds1 [4] (also known as Chk2 [5]) is inhibited by caffeine in vivo and that ATM kinase activity is directly inhibited by caffeine in vitro.", "entity1": "ATM", "entity2": "caffeine", "span1": [138, 141], "span2": [183, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10076": {"label": 1, "data": {"text": "The Kd values of SA binding to crude extract and to recombinant BiP were 45.2 and 54.6 microM, respectively.", "entity1": "BiP", "entity2": "SA", "span1": [64, 67], "span2": [17, 19]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3762": {"label": 2, "data": {"text": "Sulfhydration of sulfonylurea receptor 2B (SUR2B) was induced by NaHS and colonic inflammation.", "entity1": "SUR2B", "entity2": "NaHS", "span1": [43, 48], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8917": {"label": 1, "data": {"text": "Carvedilol produced significant inhibition of the alpha 1 adrenoceptor mediated pressor response to cirazoline in the pithed rat, but had no effect on the alpha 2 adrenoceptor mediated pressor response to B-HT 933, suggesting that carvedilol is also an alpha 1 adrenoceptor antagonist at antihypertensive doses.", "entity1": "alpha 2 adrenoceptor", "entity2": "B-HT 933", "span1": [155, 175], "span2": [205, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10785": {"label": 2, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "IL-12", "entity2": "simvastatin", "span1": [112, 117], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9425": {"label": 1, "data": {"text": "The hydrolysis of fluorescein diphosphate by PTP epsilon and PTPmeg1 was sensitive to alendronate, with IC50 values of less than 1 microM; PTPsigma, however, under the same conditions, was inhibited by only 50% with 141 microM alendronate.", "entity1": "PTPmeg1", "entity2": "alendronate", "span1": [61, 68], "span2": [86, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5048": {"label": 0, "data": {"text": "Intravenous treatment, during coronary artery occlusion, with the melanocortin analogs [Nle(4), D-Phe(7)]\u03b1-melanocyte-stimulating hormone (NDP-\u03b1-MSH) and adrenocorticotropic hormone 1-24 [ACTH-(1-24)], induced a left ventricle up-regulation of pJAK2, pERK1/2 and pTyr-STAT3 (JAK-dependent), and a reduction in pJNK and TNF-\u03b1 levels; these effects of NDP-\u03b1-MSH and ACTH-(1-24) were associated with over-expression of the pro-survival proteins HO-1 and Bcl-XL, and marked decrease of the myocardial infarct size.", "entity1": "\u03b1-melanocyte-stimulating hormone", "entity2": "Nle", "span1": [105, 137], "span2": [88, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7204": {"label": 1, "data": {"text": "Estradiol (E2) stimulates BC cells proliferation by binding the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "E2", "span1": [64, 81], "span2": [11, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2749": {"label": 3, "data": {"text": "PURPOSE: Dasatinib (BMS-354825), a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL, has recently been approved for the treatment of chronic myelogenous leukaemia (CML) in imatinib-acquired resistance and intolerance.", "entity1": "BCR", "entity2": "BMS-354825", "span1": [95, 98], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10957": {"label": 3, "data": {"text": "Effects of granulocyte colony-stimulating factor (G-CSF) and neutrophil elastase inhibitor (ONO-5046) on acid-induced lung injury in rats.", "entity1": "granulocyte colony-stimulating factor", "entity2": "ONO-5046", "span1": [11, 48], "span2": [92, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14622": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "CDA", "entity2": "dFdU", "span1": [34, 37], "span2": [283, 287]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12210": {"label": 1, "data": {"text": "P2Y12 has been shown to be the target of the thienopyridine drugs, ticlopidine and clopidogrel.", "entity1": "P2Y12", "entity2": "ticlopidine", "span1": [0, 5], "span2": [67, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8614": {"label": 2, "data": {"text": "Conversely, cell pre-treatment with Vermentino white wine extract with smaller phenolic fraction showed only a partial NOX1 down-regulation and was ineffective in interleukin synthesis induced by dietary oxysterols.", "entity1": "interleukin", "entity2": "oxysterols", "span1": [163, 174], "span2": [204, 214]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"9653": {"label": 3, "data": {"text": "RESULTS: Administration of SC-236 to cirrhotic animals did not produce significant renal effects, whereas administration of the nonselective COX-1/COX-2 inhibitor, ketorolac, resulted in a marked reduction in urine volume, urinary excretion of prostaglandins, and glomerular filtration rate and in a significant impairment in renal water metabolism.", "entity1": "COX-1", "entity2": "ketorolac", "span1": [141, 146], "span2": [164, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"12119": {"label": 9, "data": {"text": "Losartan, EXP, and irbesartan caused a rightward parallel shift without any major effects on the maximal response to Ang II.", "entity1": "Ang II", "entity2": "Losartan", "span1": [117, 123], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6181": {"label": 3, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "CFTR", "entity2": "salicylic acid", "span1": [182, 186], "span2": [66, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2770": {"label": 3, "data": {"text": "Inhibition studies demonstrated that the methyl group on the phenylacetic acid ring is required for COX-2 selectivity.", "entity1": "COX-2", "entity2": "phenylacetic acid", "span1": [100, 105], "span2": [61, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4308": {"label": 2, "data": {"text": "The TXM peptides were effective in inhibiting AuF-induced MAPK, JNK and p38(MAPK) phosphorylation, in correlation with preventing caspase-3 cleavage and thereby PARP-1 dissociation.", "entity1": "MAPK", "entity2": "AuF", "span1": [58, 62], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7176": {"label": 3, "data": {"text": "In order to produce potent new leads for anticancer drugs, a new series of quinazoline analogs was designed to resemble methotrexate (MTX, 1) structure features and fitted with functional groups believed to enhance inhibition of mammalian DHFR activity.", "entity1": "mammalian DHFR", "entity2": "methotrexate", "span1": [229, 243], "span2": [120, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2235": {"label": 3, "data": {"text": "Additionally, dasatinib leads to growth inhibition of a KITD816V-harboring human masto-cytosis cell line.", "entity1": "KIT", "entity2": "dasatinib", "span1": [56, 59], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10141": {"label": 3, "data": {"text": "Accordingly, docking of different COX inhibitors, including selective and non-selective ligands: rofecoxib, ketoprofen, suprofen, carprofen, zomepirac, indomethacin, diclofenac and meclofenamic acid were undertaken using the AMBER program.", "entity1": "COX", "entity2": "suprofen", "span1": [34, 37], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12609": {"label": 1, "data": {"text": "Cyclothiazide (330 microM) shifted the concentration-response curve for the effects of GYKI 52466 on AMPA receptor-mediated e.p.s.c.", "entity1": "AMPA receptor", "entity2": "Cyclothiazide", "span1": [101, 114], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10193": {"label": 3, "data": {"text": "In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2.", "entity1": "Oatp1", "entity2": "rifamycin SV", "span1": [156, 161], "span2": [9, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15494": {"label": 0, "data": {"text": "We used whole-cell recordings of human embryonic kidney cells heterologously expressing either wild-type TRPA1 or TRPA1 with three serine-substituted cysteines crucial for electrophile activation (C621S, C641S, C665S).", "entity1": "C641S", "entity2": "cysteines", "span1": [204, 209], "span2": [150, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2648": {"label": 8, "data": {"text": "LDH is responsible for pyruvate conversion to lactate through glycolysis.", "entity1": "LDH", "entity2": "pyruvate", "span1": [0, 3], "span2": [23, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"6583": {"label": 8, "data": {"text": "It is caused by a deficiency of propionyl-CoA carboxylase (PCC, EC 6.4.1.3), a biotin-dependent enzyme that catalyzes the carboxylation of propionyl-CoA to D-methylmalonyl-CoA.", "entity1": "propionyl-CoA carboxylase", "entity2": "propionyl-CoA", "span1": [32, 57], "span2": [139, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7628": {"label": 2, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "ERK", "entity2": "7-OH-DPAT", "span1": [102, 105], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13911": {"label": 1, "data": {"text": "These findings suggest that phenformin interacts directly with the pore-forming Kir6.0 subunit however the sulphonylurea receptor is able to significantly modulate the affinity.", "entity1": "sulphonylurea receptor", "entity2": "phenformin", "span1": [107, 129], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4088": {"label": 2, "data": {"text": "ALD increased calpain expression and caspase-3 activity and promoted Bid cleavage.", "entity1": "calpain", "entity2": "ALD", "span1": [14, 21], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3991": {"label": 3, "data": {"text": "Beta-glucogallin (BGG), a recently described AR inhibitor, was purified from extracts of the Indian gooseberry (Emblica officinalis).", "entity1": "AR", "entity2": "BGG", "span1": [45, 47], "span2": [18, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15470": {"label": 0, "data": {"text": "An endogenous intracellular domain fragment of p75(NTR) (p75(ICD)) containing these 29 amino acids is produced by regulated proteolysis of the full-length receptor.", "entity1": "p75(ICD)", "entity2": "amino acids", "span1": [57, 65], "span2": [87, 98]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6293": {"label": 5, "data": {"text": "In distinction, the preferential beta 1-AR antagonist, betaxolol, and the preferential beta 2-AR antagonist, ICI118,551, did not increase basal levels of DA, NAD, or 5-HT.", "entity1": "beta 2-AR", "entity2": "ICI118,551", "span1": [87, 96], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9478": {"label": 5, "data": {"text": "16,16-dimethyl-PGE2 and two putative EP1 antagonists, AH6809 and SC-19220, did not show any significant binding to this receptor.", "entity1": "EP1", "entity2": "AH6809", "span1": [37, 40], "span2": [54, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15679": {"label": 0, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "Histone 3", "entity2": "Ser", "span1": [177, 186], "span2": [190, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12353": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPV2", "entity2": "apomorphine", "span1": [27, 33], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12984": {"label": 8, "data": {"text": "Diacylglycerol (DAG) acts as an allosteric activator of protein kinase C (PKC) and is converted to phosphatidic acid by DAG kinase (DGK).", "entity1": "DGK", "entity2": "DAG", "span1": [132, 135], "span2": [16, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1]},
	"6058": {"label": 3, "data": {"text": "Both NE and phorbol esters increased the rate of alpha-AR mRNA degradation.", "entity1": "alpha-AR", "entity2": "phorbol esters", "span1": [49, 57], "span2": [12, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1371": {"label": 0, "data": {"text": "SUR-dependent modulation of KATP channels by an N-terminal KIR6.2 peptide.", "entity1": "KIR6.2", "entity2": "N", "span1": [59, 65], "span2": [48, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3872": {"label": 1, "data": {"text": "These studies are the first to reveal the involvement of the GSK-3\u03b2/NF-\u03baB pathway in cinobufagin-induced apoptosis.", "entity1": "GSK-3\u03b2", "entity2": "cinobufagin", "span1": [61, 67], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1602": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE", "entity2": "5-(N,N-dimethyl)-amiloride", "span1": [91, 94], "span2": [0, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"355": {"label": 9, "data": {"text": "dSERT1 shows little transport of other monoamines and is Na+ and Cl- dependent.", "entity1": "dSERT1", "entity2": "monoamines", "span1": [0, 6], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4668": {"label": 3, "data": {"text": "To determine whether dysregulation of SIRT1 promotes NADPH oxidase-dependent production of reactive oxygen species (ROS) and impairs endothelial function we assessed the effects of three structurally different inhibitors of SIRT1 (nicotinamide, sirtinol, EX527) in aorta segments isolated from young Wistar rats.", "entity1": "SIRT1", "entity2": "EX527", "span1": [224, 229], "span2": [255, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1335": {"label": 4, "data": {"text": "The esterified-BM, however, had only partial transactivation agonistic activity in cells transfected with rat GR, whereas BM and esterified-DEX had full transactivation agonistic activity.", "entity1": "rat GR", "entity2": "DEX", "span1": [106, 112], "span2": [140, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15644": {"label": 1, "data": {"text": "These data suggest that T-cells can be activated by abacavir through a direct interaction with surface and intracellular major histocompatibility complex (MHC) molecules.", "entity1": "major histocompatibility complex", "entity2": "abacavir", "span1": [121, 153], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5162": {"label": 8, "data": {"text": "The CYP2B6*6 allele is associated with reduced enzyme expression and activity that may lead to interindividual variability in ketamine metabolism.", "entity1": "CYP2B6*6", "entity2": "ketamine", "span1": [4, 12], "span2": [126, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11408": {"label": 3, "data": {"text": "Treatment with carvedilol reversed both protein and mRNA of HIF-1alpha, VEGF, BNP, and NGF-beta to the baseline values.", "entity1": "HIF-1alpha", "entity2": "carvedilol", "span1": [60, 70], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9427": {"label": 1, "data": {"text": "PTP inhibition by hisphosphonates or vanadate was diminished by the metal chelating agent EDTA, or by the reducing agent dithiothreitol, suggesting that a metal ion and the oxidation of a cysteine residue are required for full inhibition.", "entity1": "PTP", "entity2": "EDTA", "span1": [0, 3], "span2": [90, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11268": {"label": 8, "data": {"text": "The ratio between the GDC/SHMT and C1-THF synthase/SHMT pathways of Ser synthesis from [alpha-(13)C]Gly and [(13)C]formate, respectively, in Arabidopsis shoots was 21 : 1; in roots, 9 : 1.", "entity1": "SHMT", "entity2": "Ser", "span1": [26, 30], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10462": {"label": 3, "data": {"text": "Thus, Ras utilizes autocrine signaling through EGFR to increase radioresistance, and the EGFR KI GW572016 acts as a radiosensitizer.", "entity1": "Ras", "entity2": "GW572016", "span1": [6, 9], "span2": [97, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3522": {"label": 8, "data": {"text": "The ultimate carcinogenic Phase I BP metabolite anti-BP-7,8-dihydrodiol-9,10-epoxide (BPDE) can be detoxified by glutathione conjugate formation catalyzed by glutathione S-transferases.", "entity1": "glutathione S-transferases", "entity2": "glutathione", "span1": [158, 184], "span2": [113, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"9970": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-2", "entity2": "aspirin", "span1": [159, 164], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10624": {"label": 5, "data": {"text": "Histamine H1-receptor (H1R) antagonists, or antihistamines, often induce sedative side effects when used for the treatment of allergic disorders.", "entity1": "H1R", "entity2": "antihistamines", "span1": [23, 26], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"467": {"label": 5, "data": {"text": "The influence of (+/-)-tamsulosin, a selective alpha 1A-adrenoceptor antagonist, on the positive inotropic effect and the accumulation of inositol phosphates that are induced via alpha 1-adrenoceptors was studied in comparison with that of another alpha 1A-adrenoceptor ligand oxymetazoline in the rabbit ventricular myocardium.", "entity1": "alpha 1A-adrenoceptor", "entity2": "(+/-)-tamsulosin", "span1": [47, 68], "span2": [17, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5756": {"label": 3, "data": {"text": "MNU-induced lesions presented markers indicative of an aggressive phenotype: lack of basal cells, rupture of the smooth muscle cell layer, loss of E-cadherin, and high MGMT staining.", "entity1": "E-cadherin", "entity2": "MNU", "span1": [147, 157], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9723": {"label": 3, "data": {"text": "This study confirms the feasibility of using continuous measurement of AChE activity in CSF over prolonged periods, that rivastigmine markedly inhibits CSF AChE after a single oral dose of 3 mg, and that the inhibition of central AChE is substantially greater than that of peripheral AChE or BuChE.", "entity1": "BuChE", "entity2": "rivastigmine", "span1": [292, 297], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5921": {"label": 1, "data": {"text": "Analysis of this relationship shows that estramustine phosphate and tubulin compete for common MAP2 sites, that MAP2 can bind 5-6 moles.mole-1 estramustine phosphate, and that the Kd of these sites is congruent to 20 microM estramustine phosphate.", "entity1": "MAP2", "entity2": "estramustine phosphate", "span1": [112, 116], "span2": [143, 165]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11686": {"label": 1, "data": {"text": "Thiazolidinediones (TZDs) affect osteoblast viability and biomarkers independently of the TZD effects on aromatase.", "entity1": "aromatase", "entity2": "TZD", "span1": [105, 114], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2910": {"label": 3, "data": {"text": "Ex vivo COX inhibition and pharmacokinetics of acetaminophen were assessed in 5 volunteers receiving single 1000 mg doses orally.", "entity1": "COX", "entity2": "acetaminophen", "span1": [8, 11], "span2": [47, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1532": {"label": 8, "data": {"text": "The beta subunit has been cloned and shown to lower the K(m) of methionine adenosyltransferase II alpha2 (the MAT2A product) for methionine and to render the enzyme more susceptible to S-adenosylmethionine inhibition.", "entity1": "MAT2A", "entity2": "methionine", "span1": [110, 115], "span2": [129, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7812": {"label": 8, "data": {"text": "The bihelical apolipoprotein mimetic peptide 5A effluxes cholesterol from cells and reduces inflammation and atherosclerosis in animal models.", "entity1": "apolipoprotein mimetic peptide 5A", "entity2": "cholesterol", "span1": [14, 47], "span2": [57, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10808": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-2", "entity2": "carprofen", "span1": [10, 15], "span2": [71, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1490": {"label": 3, "data": {"text": "The ability of sulindac to block ERK1/2 signaling by the EGF receptor may account for at least part of its potent growth-inhibitory effects against cancer cells.", "entity1": "ERK1/2", "entity2": "sulindac", "span1": [33, 39], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7411": {"label": 1, "data": {"text": "Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40).", "entity1": "Abeta(1-40)", "entity2": "NMDA", "span1": [122, 133], "span2": [39, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12791": {"label": 1, "data": {"text": "Genetic variants at the beta(2)-adrenergic receptor (beta(2)AR) may modify asthma severity and albuterol responsiveness.", "entity1": "beta(2)-adrenergic receptor", "entity2": "albuterol", "span1": [24, 51], "span2": [95, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3369": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.2", "entity2": "pentobarbital", "span1": [71, 79], "span2": [41, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13791": {"label": 3, "data": {"text": "Others kinase inhibitors used recently in cancer therapy include Dasatinib (BMS-354825) specific for ABL non-receptor cytoplasmic kinase, Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva) and Sunitinib (SU 11248, Sutent) specific for VEGF receptor kinase, AMN107 (Nilotinib) and INNO-406 (NS-187) specific for c-KIT kinase.", "entity1": "non-receptor cytoplasmic kinase", "entity2": "Dasatinib", "span1": [105, 136], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"195": {"label": 3, "data": {"text": "Although inhibition of LH release can be achieved by estrogen and progestins, an optimal inhibitory effect on the prostate is obtained by the combined administration of the antiandrogen with an LHRH agonist that causes a specific blockage of testicular androgen biosynthesis as well as an inhibition of the LH responsiveness to LHRH.", "entity1": "LH", "entity2": "progestins", "span1": [23, 25], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9939": {"label": 3, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "NF-kappaB-inducing kinase", "entity2": "sulfasalazine", "span1": [131, 156], "span2": [269, 282]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11738": {"label": 1, "data": {"text": "These results show that the robust effects of TCDD on the mRNA expression of Snrpn, Peg3 and Igf2r genes in the sperm and of Igf2r in the muscle and liver are unrelated to changes in methylation in their respective genes.", "entity1": "Igf2r", "entity2": "TCDD", "span1": [125, 130], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14030": {"label": 1, "data": {"text": "Endothelial nitric oxide synthase genotypes and haplotypes modify the responses to sildenafil in patients with erectile dysfunction.", "entity1": "Endothelial nitric oxide synthase", "entity2": "sildenafil", "span1": [0, 33], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6999": {"label": 8, "data": {"text": "Involvement of COX-1 and up-regulated prostaglandin E synthases in phosphatidylserine liposome-induced prostaglandin E2 production by microglia.", "entity1": "prostaglandin E synthases", "entity2": "prostaglandin E2", "span1": [38, 63], "span2": [103, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10532": {"label": 1, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "RAR-RXR binding element", "entity2": "RA", "span1": [31, 54], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5806": {"label": 8, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "metalloprotein", "entity2": "N-acylated L-amino acids", "span1": [133, 147], "span2": [216, 240]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7844": {"label": 2, "data": {"text": "These data suggest that ribavirin-induced intracellular GTP depletion recruits a super elongation complex containing P-TEFb, AFF4 and ELL3, to F7, and modulates FVII mRNA transcription elongation.", "entity1": "P-TEFb", "entity2": "ribavirin", "span1": [117, 123], "span2": [24, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15540": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "MMP-13", "entity2": "DMN", "span1": [164, 170], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9340": {"label": 1, "data": {"text": "The relative potency of compounds in displacing [3H]-kainate binding to EAA3a receptor was: domoate > kainate > L-glutamate = quisqualate > 6,7-dinitroquinoxaline-2,3-dione (DNQX) = CNQX > AMPA > dihydrokainate > NMDA.", "entity1": "EAA3a", "entity2": "DNQX", "span1": [72, 77], "span2": [174, 178]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13248": {"label": 5, "data": {"text": "The GRIP1 reduction was inhibited by MK-801, an N-methyl-d-aspartate (NMDA) receptor antagonist, but not by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an AMPA receptor antagonist.", "entity1": "AMPA receptor", "entity2": "6-cyano-7-nitroquinoxaline-2,3-dione", "span1": [156, 169], "span2": [108, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10164": {"label": 5, "data": {"text": "Olopatadine is a selective histamine H1-receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and thromboxane from human polymorphonuclear leukocytes and eosinophils.", "entity1": "histamine H1-receptor", "entity2": "Olopatadine", "span1": [27, 48], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1535": {"label": 3, "data": {"text": "However, topiramate at low concentrations causes slow inhibition of GluR5 kainate receptor-mediated synaptic currents in the basolateral amygdala, indicating that it may protect against seizures, at least in part, through suppression of GluR5 kainate receptor responses.", "entity1": "GluR5", "entity2": "topiramate", "span1": [237, 242], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14124": {"label": 1, "data": {"text": "Crizotinib has demonstrated efficacy against ALK-rearranged NSCLC, and has potential for broader application in select subsets of lung cancer.", "entity1": "ALK", "entity2": "Crizotinib", "span1": [45, 48], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9771": {"label": 5, "data": {"text": "Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors.", "entity1": "5-HT(1D)", "entity2": "yohimbine", "span1": [142, 150], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15182": {"label": 2, "data": {"text": "Moreover, compared with the model group, sophocarpine could significantly increase P-AMPK\u03b1 (>5.82-fold), AMPK\u03b1 (>1.29-fold) and ACC (>3.27-fold) protein expressions, and reduce P-ACC (<0.30-fold) and HNF-4\u03b1 (<0.20-fold) protein expression.", "entity1": "ACC", "entity2": "sophocarpine", "span1": [128, 131], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15366": {"label": 2, "data": {"text": "The pleiotropic effects of vitamin A are exerted mainly by one active metabolite, all-trans retinoic acid (atRA), which regulates the expression of a battery of target genes through several families of nuclear receptors (RARs, RXRs and PPAR\u03b2/\u03b4), polymorphic retinoic acid (RA) response elements and multiple coregulators.", "entity1": "nuclear receptors", "entity2": "all-trans retinoic acid", "span1": [202, 219], "span2": [82, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3750": {"label": 3, "data": {"text": "Although both intracellular and membrane Cx43 pools were markedly reduced in cells released from contact inhibition by TCDD, siRNA-mediated Cx43 knock-down was not sufficient to stimulate proliferation in contact-inhibited cells.", "entity1": "Cx43", "entity2": "TCDD", "span1": [41, 45], "span2": [119, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9678": {"label": 3, "data": {"text": "We conclude that decreased NET synthesis may contribute to the chronic, but not acute, effect of desipramine to downregulate the NET.", "entity1": "NET", "entity2": "desipramine", "span1": [129, 132], "span2": [97, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15618": {"label": 3, "data": {"text": "Galangin decreased expression of pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-\u03b1, interleukin (IL)-6, IL-1\u03b2, and IL-8.", "entity1": "(IL)-6", "entity2": "Galangin", "span1": [112, 118], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1795": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "epidermal growth factor receptor", "entity2": "GW572016", "span1": [205, 237], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1215": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "vesicular monoamine transporter-2", "entity2": "MDMA", "span1": [174, 207], "span2": [123, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9171": {"label": 1, "data": {"text": "Drug-protein interactions: isolation and characterization of covalent adducts of phenoxybenzamine and calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [102, 112], "span2": [81, 97]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8100": {"label": 2, "data": {"text": "The mechanism revealed that wogonin inhibited H2O2-induced phosphorylation of caveolin-1 (cav-1) associating with the suppression of stabilization of VE-cadherin and \u03b2-catenin.", "entity1": "caveolin-1", "entity2": "H2O2", "span1": [78, 88], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15063": {"label": 1, "data": {"text": "Similarly, intraperitoneal administration of \u03b1-santalol (100mg/kg BW) and sandalwood oil (1g/kg BW) for two weeks modulated parameters such as serum aminotransferases, alkaline phosphatase, bilirubin, superoxide dismutase, catalase, free sulfhydryl, protein carbonyl, nitric oxide, liver lipid peroxide contents, and antioxidant capacity in d-galactose mediated oxidative stress induced mice.", "entity1": "superoxide dismutase", "entity2": "\u03b1-santalol", "span1": [201, 221], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"381": {"label": 3, "data": {"text": "Dexamethasone (DEX) inhibited the anti-CD3-induced production of IL-4, IL-5 and IFN-gamma in all 20 clones tested.", "entity1": "CD3", "entity2": "DEX", "span1": [39, 42], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5931": {"label": 3, "data": {"text": "4-MA, a well known 5 alpha-reductase inhibitor, is also a potent inhibitor of 3 beta-HSD with a Ki value of 56 nM.", "entity1": "5 alpha-reductase", "entity2": "4-MA", "span1": [19, 36], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12300": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Cd36", "entity2": "Quercetin", "span1": [162, 166], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15772": {"label": 2, "data": {"text": "The overall results indicate that ICI may exert agonistic and antagonistic effects on uterine cell proliferation through differential activation of the Akt pathway depending on the administration period during the estrous cycle, and indicates that the mechanism of cell proliferation during the physiological conditions of the estrous cycle, is under a different and more complex regulation than in the ovariectomized +E2 animal model.", "entity1": "Akt", "entity2": "ICI", "span1": [152, 155], "span2": [34, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"762": {"label": 3, "data": {"text": "This hypothesis was tested by investigating whether, in subjects with essential hypertension, the natriuretic response to specific renin-angiotensin-aldosterone system (RAAS) blockade by renin-inhibitor remikiren could be predicted from pretreatment renal vascular tone.", "entity1": "renin", "entity2": "remikiren", "span1": [187, 192], "span2": [203, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13386": {"label": 1, "data": {"text": "Our structural studies provide a view of a synthetic inhibitory compound in a sirtuin active site revealing that suramin binds into the NAD(+), the product, and the substrate-binding site.", "entity1": "sirtuin", "entity2": "suramin", "span1": [78, 85], "span2": [113, 120]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, -1]},
	"4180": {"label": 2, "data": {"text": "Firstly, in the normal human renal epithelial HK-2 cells, the measurement of the expression of 30 previously reported NRF2 target genes in response to NRF2 inducers (sulforaphane, tert-butylhydroquinone, cinnamic aldehyde, and hydrogen peroxide) showed that the aldo-keto reductase (AKR) 1C1 is highly inducible by all treatments.", "entity1": "aldo-keto reductase (AKR) 1C1", "entity2": "tert-butylhydroquinone", "span1": [262, 291], "span2": [180, 202]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13050": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "RALDH2", "entity2": "retinal", "span1": [213, 219], "span2": [111, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3065": {"label": 5, "data": {"text": "In many countries, a mu-opioid receptor antagonist naltrexone has been used in the treatment of alcohol dependence.", "entity1": "mu-opioid receptor", "entity2": "naltrexone", "span1": [21, 39], "span2": [51, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13359": {"label": 2, "data": {"text": "INTRODUCTION: Medroxyprogesterone acetate (MPA) induces estrogen receptor (ER)-positive and progesterone receptor (PR)-positive ductal invasive mammary carcinomas in BALB/c mice.", "entity1": "ER", "entity2": "Medroxyprogesterone acetate", "span1": [75, 77], "span2": [14, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2895": {"label": 5, "data": {"text": "Prazosin (nonselective alpha(1)-adrenoceptor antagonist), silodosin (selective alpha(1A)-adrenoceptor antagonist) and BMY-7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride) (selective alpha(1D)-adrenoceptor antagonist) competitively antagonized the phenylephrine-induced contraction (pA(2) values, 8.60+/-0.07, 9.44+/-0.06 and 5.75+/-0.07, respectively).", "entity1": "alpha(1)-adrenoceptor", "entity2": "Prazosin", "span1": [23, 44], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1750": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "AKT", "entity2": "GW572016", "span1": [137, 140], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4077": {"label": 2, "data": {"text": "Pretreatment of human breast carcinoma MCF-7 cells for 24 h with the groundnut extract and soybean isoflavone increased gene expression of heme oxygenase-1 (HO-1), a major antioxidative stress enzyme.", "entity1": "HO-1", "entity2": "isoflavone", "span1": [157, 161], "span2": [99, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3958": {"label": 1, "data": {"text": "Moreover, VK2-2,3 epoxide, an intracellular metabolite of VK2, was shown to covalently bind to the cysteine-166 residue of Bak.", "entity1": "Bak", "entity2": "VK2", "span1": [123, 126], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11201": {"label": 1, "data": {"text": "These results suggest that ATP-bound TOP2 may be the specific target of ATP-sensitive TOP2 poisons.", "entity1": "TOP2", "entity2": "ATP", "span1": [37, 41], "span2": [72, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4836": {"label": 4, "data": {"text": "This inhibition was blocked when mice were pretreated with the selective H3R agonist R-(alpha)-methyl-histamine (10\u00a0mg/kg).", "entity1": "H3R", "entity2": "R-(alpha)-methyl-histamine", "span1": [73, 76], "span2": [85, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2170": {"label": 0, "data": {"text": "Binding sites for hERG blockers have been mapped within the inner cavity of the channel and include aromatic residues in the S6 helix (Tyr-652, Phe-656) and residues in the pore helix (Thr-623, Ser-624, Val-625).", "entity1": "hERG", "entity2": "Phe", "span1": [18, 22], "span2": [144, 147]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12147": {"label": 1, "data": {"text": "(S,S)-[(11)C]-MeNER has the potential to be the first successful PET ligand to image NET.", "entity1": "NET", "entity2": "(S,S)-[(11)C]-MeNER", "span1": [85, 88], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7967": {"label": 2, "data": {"text": "GIP potentiates glucose-stimulated insulin secretion and induces energy accumulation into adipose tissue, resulting in obesity.", "entity1": "insulin", "entity2": "glucose", "span1": [35, 42], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6924": {"label": 1, "data": {"text": "Our results provided direct evidence indicating that HM74A, but not HM74, was sufficient to mediate anti-lipolytic effect of niacin in adipose tissue.", "entity1": "HM74A", "entity2": "niacin", "span1": [53, 58], "span2": [125, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3114": {"label": 8, "data": {"text": "Ambrisentan is an endothelin type A (ET(A))-selective receptor antagonist that is metabolized primarily by glucuronidation but also undergoes oxidative metabolism by CYP3A4.", "entity1": "CYP3A4", "entity2": "Ambrisentan", "span1": [166, 172], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"703": {"label": 5, "data": {"text": "The potency of the selective alpha 1D-adrenoceptor antagonist BMY 7378 against noradrenaline (pA2 = 6.16 +/- 0.13) and of the selective alpha 1A-adrenoceptor antagonist RS-17053 against noradrenaline (pKB = 8.35 +/- 0.10) and against the selective alpha 1A-adrenoceptor agonist A-61603 (pKB = 8.40 +/- 0.09) were too low to account for alpha 1D- and alpha 1A-adrenoceptor involvement.", "entity1": "alpha 1D-adrenoceptor", "entity2": "BMY 7378", "span1": [29, 50], "span2": [62, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2469": {"label": 9, "data": {"text": "Liver choline dehydrogenase and kidney betaine-homocysteine methyltransferase expression are not affected by methionine or choline intake in growing rats.", "entity1": "choline dehydrogenase", "entity2": "choline", "span1": [6, 27], "span2": [123, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"16005": {"label": 2, "data": {"text": "Moreover, we also demonstrate that puerarin functions at least partially through activation of MEK/ERK and PI3K/Akt signaling.", "entity1": "Akt", "entity2": "puerarin", "span1": [112, 115], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4678": {"label": 2, "data": {"text": "In conclusion, IL-8 production and neutrophil infiltration are increased in high-glucose environment due to elevated ROS level and contributed to impaired wound healing in diabetic skin.", "entity1": "IL-8", "entity2": "glucose", "span1": [15, 19], "span2": [81, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"251": {"label": 3, "data": {"text": "Both NS-398 and Dup-697 exhibited time-dependent inactivation of hCOX-2, as did indomethacin on both enzymes.", "entity1": "hCOX-2", "entity2": "indomethacin", "span1": [65, 71], "span2": [80, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8593": {"label": 2, "data": {"text": "Quercetin and rutin also increased alkaline phosphatase activity by about 150 and 240% and demonstrated mineralization up to 110 and 200% respectively as compared to control (which was considered as 100%).", "entity1": "alkaline phosphatase", "entity2": "rutin", "span1": [35, 55], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"622": {"label": 3, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "IL-2", "entity2": "p-bromophenacyl bromide", "span1": [117, 121], "span2": [28, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11358": {"label": 1, "data": {"text": "METHOD: The authors conducted a PET study to evaluate D(2) occupancy (using [(11)C]raclopride) and 5-HT(2) occupancy (using [(18)F]setoperone) in brain regions of interest in 16 patients with schizophrenia or schizoaffective disorder randomly assigned to receive 40, 80, 120, or 160 mg/day of ziprasidone, which reflected the recommended dose range.", "entity1": "D(2)", "entity2": "[(11)C]raclopride", "span1": [54, 58], "span2": [76, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2390": {"label": 8, "data": {"text": "In the present study, we have evaluated possible participation of monocarboxylate transporters (MCTs) responsible for the bidirectional membrane transport of pyruvate in the cytoprotective property in osteoblasts.", "entity1": "MCTs", "entity2": "pyruvate", "span1": [96, 100], "span2": [158, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11965": {"label": 8, "data": {"text": "PIP5K1B encodes phosphatidylinositol 4-phosphate 5-kinase \u03b2 type I (pip5k1\u03b2), an enzyme functionally linked to actin cytoskeleton dynamics that phosphorylates phosphatidylinositol 4-phosphate [PI(4)P] to generate phosphatidylinositol-4,5-bisphosphate [PI(4,5)P2].", "entity1": "pip5k1\u03b2", "entity2": "PI(4,5)P2", "span1": [68, 75], "span2": [252, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6260": {"label": 1, "data": {"text": "Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM).", "entity1": "human serotonin transporter", "entity2": "neuroleptics", "span1": [58, 85], "span2": [6, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"396": {"label": 5, "data": {"text": "Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A.", "entity1": "CB1", "entity2": "SR 141716A", "span1": [100, 103], "span2": [115, 125]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6308": {"label": 8, "data": {"text": "Here, we tested the hypothesis that 5-HT receptors mediate eNOS activation by measuring agonist-stimulated [3H]L-citrulline ([3H]L-Cit) formation in BAEC cultures.", "entity1": "eNOS", "entity2": "[3H]L-citrulline", "span1": [59, 63], "span2": [107, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14626": {"label": 8, "data": {"text": "All four DCK proteins yielded comparable metabolic activity for Ara-C and dFdC monophosphorylation, except for DCK24Val, which demonstrated an approximately 2-fold increase (P < 0.05) in the intrinsic clearance of dFdC monophosphorylation due to a 40% decrease in K(m) (P < 0.05).", "entity1": "DCK", "entity2": "Ara-C", "span1": [9, 12], "span2": [64, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1867": {"label": 3, "data": {"text": "In vitro inhibition of diacylglycerol acyltransferase by prenylflavonoids from Sophora flavescens.", "entity1": "diacylglycerol acyltransferase", "entity2": "prenylflavonoids", "span1": [23, 53], "span2": [57, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11076": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "cAMP phosphodiesterase", "entity2": "p-chloro", "span1": [86, 108], "span2": [234, 242]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4164": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "p65", "entity2": "rocaglate", "span1": [180, 183], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8714": {"label": 2, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "CAT", "entity2": "Na2SeO3", "span1": [25, 28], "span2": [99, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11420": {"label": 1, "data": {"text": "The orientation of the O4 hydroxyl of glucose causes a steric hindrance to the side chain carboxylate group of Glu317, accounting for the enzyme's low Glc-T activity.", "entity1": "Glc-T", "entity2": "O4 hydroxyl of glucose", "span1": [151, 156], "span2": [23, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2570": {"label": 3, "data": {"text": "Brain tissue analyses revealed that neonatal quinpirole treatment produced a significant decrease in hippocampal NGF, BDNF and ChAT that was eliminated by olanzapine treatment.", "entity1": "BDNF", "entity2": "quinpirole", "span1": [118, 122], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1415": {"label": 4, "data": {"text": "Lisuride dose dependently decreased body temperature in rats with a potency similar to that of the selective 5-HT(1A) agonist LY 293284.", "entity1": "5-HT(1A)", "entity2": "LY 293284", "span1": [109, 117], "span2": [126, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10848": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "PDGFRA", "entity2": "Gleevec", "span1": [124, 130], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1861": {"label": 3, "data": {"text": "These data suggest that the lavandulyl side chain and the position of the hydroxy group are important for high DGAT inhibitory activity.", "entity1": "DGAT", "entity2": "lavandulyl", "span1": [111, 115], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13096": {"label": 4, "data": {"text": "Among the measured compounds, gliquidone and glipizide (two sulfonylureas), as well as nateglinide (a glinide), exhibit PPARgamma agonistic activity at concentrations comparable with those reached under pharmacological treatment.", "entity1": "PPARgamma", "entity2": "glipizide", "span1": [120, 129], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14880": {"label": 3, "data": {"text": "In cultured primary microglia and astrocytes, EHT had a direct anti-inflammatory effect demonstrated by repression of lipopolysaccharide-induced NF\u03baB activation, iNOS induction, and nitric oxide production.", "entity1": "NF\u03baB", "entity2": "EHT", "span1": [145, 149], "span2": [46, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7154": {"label": 8, "data": {"text": "K(m) values of the mutants for cGMP were similar to that of full-length PDE5.", "entity1": "PDE5", "entity2": "cGMP", "span1": [72, 76], "span2": [31, 35]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12051": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPM3", "entity2": "apomorphine", "span1": [78, 84], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12516": {"label": 1, "data": {"text": "These results demonstrate the presence of a dehydrogenase activity separate from the nicotinamide-adenine dinucleotide phosphate (NADP)-dependent 11 beta hydroxysteroid dehydrogenase recently purified and cloned from rat liver.", "entity1": "11 beta hydroxysteroid dehydrogenase", "entity2": "NADP", "span1": [146, 182], "span2": [130, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3039": {"label": 5, "data": {"text": "EP(1) and EP(3) receptor antagonists ONO-8713 and ONO-AE3-240, but not the EP(4) antagonists ONO-AE3-208 and AH 23848, inhibited tumor cell proliferation, indicating the significance of EP(1) and EP(3) but not EP(4) for MB growth.", "entity1": "EP(1)", "entity2": "ONO-AE3-240", "span1": [0, 5], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12040": {"label": 8, "data": {"text": "We suggest that the latter can react with H2O2 in a catalase-like reaction, with evolution of O2.", "entity1": "catalase", "entity2": "H2O2", "span1": [52, 60], "span2": [42, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15500": {"label": 1, "data": {"text": "Interestingly, following pBQN desensitization, wild-type TRPA1 had dramatically reduced response to the nonelectrophile agonist carvacrol, whereas the triple cysteine mutant TRPA1 retained its full response.", "entity1": "TRPA1", "entity2": "pBQN", "span1": [57, 62], "span2": [25, 29]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11777": {"label": 1, "data": {"text": "We begin by capturing RISC using a complementary 2'-O-methyl oligonucleotide tethered to beads.", "entity1": "RISC", "entity2": "2'-O-methyl", "span1": [22, 26], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8470": {"label": 1, "data": {"text": "Of the new compounds, Dmt(1)-(R)-\u03b2Pro(2)-Trp(3)-(2-furyl)Map(4) (analogue 12) displayed the highest affinity toward MOR, in the picomolar range (Ki(\u03bc) = 3.72 pM).", "entity1": "MOR", "entity2": "(2-furyl)Map", "span1": [116, 119], "span2": [48, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9025": {"label": 2, "data": {"text": "We conclude that androgens can stimulate human and murine osteoblastic cell proliferation in vitro, and induce expression of the osteoblast-line differentiation marker ALP, presumably by an androgen receptor mediated mechanism.", "entity1": "osteoblast-line differentiation marker", "entity2": "androgens", "span1": [129, 167], "span2": [17, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5332": {"label": 9, "data": {"text": "No effects were observed when fenclozic acid was assessed for P450-dependent and P450-independent cytotoxicity to THLE cell lines, time-dependent inhibition of five major human cytochrome P450 enzymes, inhibition of the biliary efflux transporters BSEP and MRP2 or mitochondrial toxicity to THLE or HepG2 cells.", "entity1": "P450", "entity2": "fenclozic acid", "span1": [62, 66], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11309": {"label": 1, "data": {"text": "This study also investigated the effect of zuclopenthixol on cortical and hippocampal monoaminergic neurotransmitters' levels together with acetylcholinesterase enzyme (AChE) activity, both of which are known to be important in control of cognitive function.", "entity1": "acetylcholinesterase", "entity2": "zuclopenthixol", "span1": [140, 160], "span2": [43, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9419": {"label": 5, "data": {"text": "This study was designed to determine the gastroprotective properties of cinitapride (CNT), a novel prokinetic benzamide derivative agonist of 5-HT4 and 5-HT1 receptors and 5-HT2 antagonist, on mucosal injury produced by 50% (v/v) ethanol.", "entity1": "5-HT2", "entity2": "CNT", "span1": [172, 177], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"55": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "renin", "entity2": "Enalkiren", "span1": [41, 46], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13820": {"label": 1, "data": {"text": "Currently, the use of orally administered MAO inhibitor antidepressants (eg, phenelzine, tranylcypromine) is limited by the risk of tyramine-provoked events (eg, acute hypertension and headache, also known as the \"cheese reaction\") when combined with dietary tyramine.", "entity1": "MAO", "entity2": "tyramine", "span1": [42, 45], "span2": [132, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7529": {"label": 9, "data": {"text": "While vitamin C is essential for PHD activity in vitro, N-acetyl-L-cysteine had no effect, and gallic acid or n-propyl gallate efficiently inhibited the activity of all three PHDs, demonstrating different functions of these antioxidants.", "entity1": "PHD", "entity2": "N-acetyl-L-cysteine", "span1": [33, 36], "span2": [56, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7373": {"label": 1, "data": {"text": "Histamine regulates many functions by binding to four histamine G-coupled receptor proteins (H1R, H2R, H3R and H4R).", "entity1": "H3R", "entity2": "Histamine", "span1": [103, 106], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15928": {"label": 1, "data": {"text": "Processing of polysialylated NCAM was reproduced in a mouse model by bleomycin administration leading to an activation of the inflammasome and secretion of interleukin (IL)-1\u03b2.", "entity1": "polysialylated NCAM", "entity2": "bleomycin", "span1": [14, 33], "span2": [69, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13786": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "ZK 222584", "span1": [14, 16], "span2": [204, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3767": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "TNF-\u03b1", "entity2": "CCl(4)", "span1": [181, 186], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14303": {"label": 8, "data": {"text": "Human serum butyrylcholinesterase (HuBChE) is currently the most suitable bioscavenger for the prophylaxis of highly toxic organophosphate (OP) nerve agents.", "entity1": "Human serum butyrylcholinesterase", "entity2": "organophosphate", "span1": [0, 33], "span2": [123, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4378": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [280, 285], "span2": [220, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4023": {"label": 3, "data": {"text": "The anti-inflammatory actions of curcumin on colitis may involve inhibition of the TLR4/NF-\u03baB signaling pathway and of IL-27 expression.", "entity1": "NF-\u03baB", "entity2": "curcumin", "span1": [88, 93], "span2": [33, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3769": {"label": 2, "data": {"text": "CCl(4) administration triggered inflammatory response in mice livers by activating nuclear factor-kappaB (NF-\u03baB), which coincided with the induction of tumor necrosis factor-alpha (TNF-\u03b1) and cyclooxygenase-2 (COX-2).", "entity1": "COX-2", "entity2": "CCl(4)", "span1": [210, 215], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10942": {"label": 1, "data": {"text": "This process was reduced by a protonophore, carbonylcyanide p-trifluoromethoxyphenylhydrazone, and a typical monocarboxylate transporter (MCT) inhibitor, alpha-cyano-4-hydroxycinnamic acid, suggesting that nicotinate uptake by rat astrocytes is mediated by H(+)-coupled monocarboxylate transport system.", "entity1": "monocarboxylate transport system", "entity2": "H(+)", "span1": [270, 302], "span2": [257, 261]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9131": {"label": 1, "data": {"text": "In addition, phenoxybenzamine showed little or no calcium-dependent binding to the S-100 protein, bovine serum albumin or cytochrome c. The irreversible complex between phenoxybenzamine and calmodulin may be useful for inhibiting certain calmodulin-dependent reactions and for studying the various biological functions of calmodulin.", "entity1": "S-100 protein", "entity2": "calcium", "span1": [83, 96], "span2": [50, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12954": {"label": 0, "data": {"text": "METHODS: We identified seven SNP(single nucleotide polymorphism) (-141Cins>del, TaqIB, TaqID, Ser311Cys, rs6275, rs6277 and TaqIA) in the DRD2 gene in 146 schizophrenic inpatients (59 with EPS and 87 without EPS according to the Simpson-Angus Scale) treated with chlorpromazine after 8 weeks.", "entity1": "DRD2", "entity2": "nucleotide", "span1": [138, 142], "span2": [40, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12783": {"label": 8, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "2-deoxythymidine-5-monophosphate", "span1": [0, 20], "span2": [216, 248]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13794": {"label": 3, "data": {"text": "The following TK blockers for treatment of various human tumors are in clinical development: Lapatinib (Lapatinib ditosylate, Tykerb, GW-572016), Canertinib (CI-1033), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).", "entity1": "TK", "entity2": "Arava", "span1": [14, 16], "span2": [274, 279]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7755": {"label": 0, "data": {"text": "By synthesizing and testing a series of alanine point-mutated cyclic peptides, we identified which amino acid was important for the inhibition of the phospholamban function.", "entity1": "cyclic peptides", "entity2": "alanine", "span1": [62, 77], "span2": [40, 47]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14696": {"label": 4, "data": {"text": "This work investigated the drug interaction potential of GSK1292263, a novel GPR119 agonist, with the HMG-coA reductase inhibitors simvastatin and rosuvastatin.", "entity1": "GPR119", "entity2": "GSK1292263", "span1": [77, 83], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11116": {"label": 2, "data": {"text": "DEX enhanced the ratio IFN-gamma/IL-4 (mean +/- SEM: control, 28.7 +/- 17.6; with 10-7 M DEX, 55.0 +/- 27.5, P<0.005).", "entity1": "IFN-gamma", "entity2": "DEX", "span1": [23, 32], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2759": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "Val-349 to Ile", "entity2": "2-chloro-6-methyl", "span1": [17, 31], "span2": [125, 142]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1722": {"label": 2, "data": {"text": "Thus, it can be suggested that the inhibitory action of ginseng saponins against the immobilization stress-induced increase of plasma IL-6 level would be in periphery; at least in part, mediated by blocking norepinephrine- and/or epinephrine-induced increase of IL-6 level in macrophage rather than in the brain.", "entity1": "IL-6", "entity2": "norepinephrine", "span1": [262, 266], "span2": [207, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13211": {"label": 9, "data": {"text": "Triflusal (30 mg/kg) or aspirin treatment (30 mg/kg) did not reduce the levels of GFAP or Hsp27 immunostaining.", "entity1": "GFAP", "entity2": "aspirin", "span1": [82, 86], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4632": {"label": 1, "data": {"text": "Ligand binding analysis demonstrated that pelargonidin was a weak ligand of AhR.", "entity1": "AhR", "entity2": "pelargonidin", "span1": [76, 79], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4429": {"label": 8, "data": {"text": "Type 2 11\u03b2-hydroxysteroid dehydrogenase encoded by the HSD11B2 gene converts cortisol to inactive cortisone, and alteration in this enzymatic activity might affect glucose homeostasis by affecting circulating levels or tissue availability of glucocorticoids.", "entity1": "Type 2 11\u03b2-hydroxysteroid dehydrogenase", "entity2": "cortisol", "span1": [0, 39], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"8080": {"label": 8, "data": {"text": "On stimulation by G(s), the activities of ACs can be further selectively modulated by other pathways to ensure precise control of intracellular cAMP responses to specific stimuli.", "entity1": "ACs", "entity2": "cAMP", "span1": [42, 45], "span2": [144, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1875": {"label": 1, "data": {"text": "Monodemethylated mifepristone bound to rabbit thymic GR with higher affinity than monodemethylated CDB-2914 or CDB-4124.", "entity1": "rabbit thymic GR", "entity2": "mifepristone", "span1": [39, 55], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11912": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "triglycerides", "span1": [174, 179], "span2": [46, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2804": {"label": 3, "data": {"text": "Inhibition of endogenous production of H(2)S by PAG significantly suppressed SP concentration, PPT-A expression and NK1-R expression in the acini.", "entity1": "NK1-R", "entity2": "H(2)S", "span1": [116, 121], "span2": [39, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6079": {"label": 1, "data": {"text": "), a cholinesterase inhibitor that potentiates the effects of acetylcholine at the muscarinic cholinergic receptor, terminated VT in four of four patients, an effect that was reversed by atropine.", "entity1": "muscarinic cholinergic receptor", "entity2": "acetylcholine", "span1": [83, 114], "span2": [62, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9138": {"label": 1, "data": {"text": "Replacement of the methyl groups of theophylline with n-propyl or larger alkyl groups yields xanthines with selectivity for A1 receptors, particularly when combined with an 8-phenyl moiety.", "entity1": "A1 receptors", "entity2": "8-phenyl", "span1": [124, 136], "span2": [173, 181]}, "weak_labels": [-1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15800": {"label": 8, "data": {"text": "Opening of Panx1 HCs during repetitive activation allows efflux of ATP, influx of glucose and possibly Ca(2+) too, which are required for potentiation of contraction.", "entity1": "Panx1", "entity2": "Ca(2+)", "span1": [11, 16], "span2": [103, 109]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4770": {"label": 3, "data": {"text": "Inhibition of angiogenesis and invasion by DMBT is mediated by downregulation of VEGF and MMP-9 through Akt pathway in MDA-MB-231 breast cancer cells.", "entity1": "MMP-9", "entity2": "DMBT", "span1": [90, 95], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10353": {"label": 9, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "NEP", "entity2": "GW660511X", "span1": [142, 145], "span2": [126, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2219": {"label": 4, "data": {"text": "Systemic administration of beta2-adrenoceptor agonists, formoterol and salmeterol, elicit skeletal muscle hypertrophy in rats at micromolar doses.", "entity1": "beta2-adrenoceptor", "entity2": "formoterol", "span1": [27, 45], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8223": {"label": 1, "data": {"text": "Mutations introduced into EAG to replicate the ICA binding site in ERG did not alter the functional response to ICA.", "entity1": "EAG", "entity2": "ICA", "span1": [26, 29], "span2": [47, 50]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10263": {"label": 8, "data": {"text": "Amongst the three OCTs expressed in the SCG, OCT3 best fits the profile of substrates and antagonists that cause trans-stimulation and trans-inhibition, respectively, of [3H]-MPP+ release.", "entity1": "OCT3", "entity2": "[3H]-MPP+", "span1": [45, 49], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12029": {"label": 1, "data": {"text": "On the basis of these observations and other findings, we have proposed a scheme which offers a possible explanation for iodide-dependent catalatic activity of thyroid peroxidase and lactoperoxidase.", "entity1": "thyroid peroxidase", "entity2": "iodide", "span1": [160, 178], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"600": {"label": 3, "data": {"text": "In activated microglia, 15d-PGJ2 suppressed iNOS promoter activity, iNOS mRNA, and protein levels.", "entity1": "iNOS", "entity2": "15d-PGJ2", "span1": [68, 72], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2741": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "BCR", "entity2": "dasatinib", "span1": [142, 145], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10544": {"label": 1, "data": {"text": "Within this sequence DNase I footprinting revealed that RA induced binding of a nuclear protein complex to an element containing two GT boxes.", "entity1": "nuclear protein complex", "entity2": "RA", "span1": [80, 103], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14005": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "VEGFR2", "entity2": "XL184", "span1": [111, 117], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11670": {"label": 1, "data": {"text": "The Ca(2+)-S100A4/prochlorperazine (PCP) complex exhibits a similar pentameric assembly.", "entity1": "S100A4", "entity2": "PCP", "span1": [11, 17], "span2": [36, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15419": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "NPC1L1", "entity2": "cholesterol", "span1": [202, 208], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"4070": {"label": 3, "data": {"text": "In study 1, cyclic ewes received vehicle, cortisol, PF 915275 (PF; a selective inhibitor of HSD11B1), cortisol and PF, meloxicam (a selective inhibitor of PTGS2), cortisol and meloxicam, recombinant ovine IFNT, or IFNT and PF into the uterus from day 10 to day14 after estrus.", "entity1": "HSD11B1", "entity2": "PF 915275", "span1": [92, 99], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3087": {"label": 4, "data": {"text": "Ramelteon (Rozerem; Takeda Pharmaceutical Company Limited, Osaka, Japan) is an orally active, highly selective melatonin MT(1)/MT(2) receptor agonist.", "entity1": "MT(2)", "entity2": "Ramelteon", "span1": [127, 132], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15854": {"label": 8, "data": {"text": "24(S)-hydroxycholesterol is actively eliminated from neuronal cells by ABCA1.", "entity1": "ABCA1", "entity2": "24(S)-hydroxycholesterol", "span1": [71, 76], "span2": [0, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1134": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "human ether-a-go-go-related gene", "entity2": "pimozide", "span1": [179, 211], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2889": {"label": 4, "data": {"text": "Noradrenaline and phenylephrine (alpha(1)-adrenoceptor agonist) each produced a concentration-dependent tonic contraction, their pD(2) values being 6.87+/-0.08 and 6.10+/-0.05, respectively.", "entity1": "alpha(1)-adrenoceptor", "entity2": "phenylephrine", "span1": [33, 54], "span2": [18, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9949": {"label": 3, "data": {"text": "The decrease in substrate phosphorylation by IKK-alpha and -beta is associated with a decrease in autophosphorylation of IKKs and can be antagonized by excess adenosine triphosphate.", "entity1": "IKKs", "entity2": "adenosine triphosphate", "span1": [121, 125], "span2": [159, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 5, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5469": {"label": 5, "data": {"text": "In the lateral geniculate nucleus, brexpiprazole displayed alpha1B-adrenoceptor antagonistic action.", "entity1": "alpha1B-adrenoceptor", "entity2": "brexpiprazole", "span1": [59, 79], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10806": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-2", "entity2": "flunixin", "span1": [10, 15], "span2": [61, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7889": {"label": 1, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "FAS", "entity2": "geranylgeranyl-pyrophosphate", "span1": [32, 35], "span2": [180, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11157": {"label": 8, "data": {"text": "Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A).", "entity1": "PDE10A", "entity2": "cAMP", "span1": [100, 106], "span2": [85, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6108": {"label": 5, "data": {"text": "In extending these initial findings, we have shown that cardiac fibrosis (i) is not reversed by correction of mineralocorticoid-induced hypokalemia; (ii) appears not to involve the plasma or tissue renin-angiotensin systems, as fibrosis is largely unaffected by concurrent administration of Losartan or Perindopril; (iii) is independent of cardiac hypertrophy, in that it is equally seen in right and left ventricles, and in rats rendered hypertensive without cardiac hypertrophy by the administration of 9 alpha-fluorocortisol; (iv) is independent of elevated blood pressure, in that it is found in normotensive animals infused peripherally with aldosterone and intracerebroventricularly with the mineralocorticoid receptor (MR) antagonist RU28318; (v) is via classical MR, in that it is blocked by concurrent administration of the MR antagonist potassium canrenoate; and (vi) may or may not be a direct cardiac effect, inasmuch as data for in vivo effects on collagen formation by cardiac fibroblasts are conflicting.", "entity1": "MR", "entity2": "RU28318", "span1": [726, 728], "span2": [741, 748]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13384": {"label": 1, "data": {"text": "To provide insights into how sirtuin function is altered by inhibitors, we determined two crystal structures of SIRT5, one in complex with ADP-ribose, the other bound to suramin.", "entity1": "SIRT5", "entity2": "ADP", "span1": [112, 117], "span2": [139, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11763": {"label": 1, "data": {"text": "The Effects of Carbohydrate, Unsaturated Fat, and Protein Intake on Measures of Insulin Sensitivity: Results from the OmniHeart Trial.", "entity1": "Insulin", "entity2": "Carbohydrate", "span1": [80, 87], "span2": [15, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8860": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "c-Src", "entity2": "I3S", "span1": [406, 411], "span2": [319, 322]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15487": {"label": 0, "data": {"text": "Electrophilic chemicals activate both insect and vertebrate TRPA1 via covalent modification of cysteine residues in the amino-terminal region.", "entity1": "TRPA1", "entity2": "amino", "span1": [60, 65], "span2": [120, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2751": {"label": 9, "data": {"text": "Mutation of Ser-530 to Ala or Val-349 to Ala or Leu abolished the potent inhibition observed with wild-type human COX-2 and key lumiracoxib analogs.", "entity1": "Ser-530 to Ala", "entity2": "lumiracoxib", "span1": [12, 26], "span2": [128, 139]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15071": {"label": 2, "data": {"text": "Importantly, expression of the acute-phase reactant serum amyloid A (SAA) significantly increased after ritodrine injection, with values indicating the largest fold-change.", "entity1": "SAA", "entity2": "ritodrine", "span1": [69, 72], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10727": {"label": 4, "data": {"text": "We have analyzed binding domains of the oxytocin receptor for barusiban, a highly selective oxytocin receptor antagonist, in comparison to the combined vasopressin V1A/oxytocin receptor antagonist atosiban and the agonists oxytocin and carbetocin.", "entity1": "vasopressin V1A/oxytocin receptor", "entity2": "oxytocin", "span1": [152, 185], "span2": [223, 231]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"239": {"label": 1, "data": {"text": "In all cases at both the 5-HT2A and 5-HT2C receptors, the affinities of the isomers of MDMA and MDA were at least 2-3 orders of magnitude less than 5-HT.", "entity1": "5-HT2A", "entity2": "5-HT", "span1": [25, 31], "span2": [148, 152]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6168": {"label": 3, "data": {"text": "Selegiline (deprenyl), a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B) is widely used in the treatment of Parkinson's disease.", "entity1": "monoamine oxidase type B", "entity2": "Selegiline", "span1": [62, 86], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6356": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "eprosartan", "span1": [25, 28], "span2": [126, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1784": {"label": 1, "data": {"text": "Tamsulosin, which has high affinity for alpha1aAR and alpha1dAR subtypes but not for alpha1bAR, shows efficacy similar to the nonsubtype selective agents terazosin and doxazosin.", "entity1": "alpha1dAR", "entity2": "doxazosin", "span1": [54, 63], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15263": {"label": 2, "data": {"text": "Three variables of cardiac vagal effects (the root mean square of successive differences [rMSSD] in the interbeat interval of the heart rate [IBI], heart-rate variability [HRV] caused by peak-valley respiratory sinus arrhythmia [pvRSA], and high-frequency power [HF]) and heart rate (HR) were obtained at seven time points during the clamps, characterised by increasing levels of insulin (achieved by administering insulin plus glucose, glucose only, glucose and GLP-1, and glucose and GLP-1 combined with arginine).", "entity1": "insulin", "entity2": "glucose", "span1": [380, 387], "span2": [428, 435]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14995": {"label": 9, "data": {"text": "In monocytes, both EPA and DHA increased interleukin (IL)-10 without affecting tumor necrosis factor (TNF)-\u03b1 and IL-6.", "entity1": "IL-6", "entity2": "DHA", "span1": [113, 117], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15256": {"label": 1, "data": {"text": "Selective oxidation of \u03c9-tertiary amine self-assembled thiol monolayers to tertiary amine N-oxides is shown to transform the adhesion of model proteins lysozyme and fibrinogen upon them.", "entity1": "lysozyme", "entity2": "thiol", "span1": [152, 160], "span2": [55, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3831": {"label": 3, "data": {"text": "In combination with clofarabine, the ability of resveratrol to reduce the contents of Sp1 and its target gene products was also evident in a time- and dose-dependent experiment.", "entity1": "Sp1", "entity2": "clofarabine", "span1": [86, 89], "span2": [20, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12775": {"label": 1, "data": {"text": "Thymidylate synthase (TS) continues to be a critical target for 5-fluorouracil (5-FU) and its prodrugs, UFT/LV (Orzel), capecitabine (Xeloda), and S-1, primarily because this enzyme is essential for the synthesis of 2-deoxythymidine-5-monophosphate, a precursor for DNA synthesis.", "entity1": "Thymidylate synthase", "entity2": "Orzel", "span1": [0, 20], "span2": [112, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8834": {"label": 3, "data": {"text": "RESULTS: By Western blot analysis of spinal cord tissues, we have demonstrated that treatment with bioactive RS -GRA significantly decreased nuclear factor (NF)-kB translocation, pro-inflammatory cytokine production such as interleukin-1\u03b2 (IL-1\u03b2), and apoptosis (Bax and caspase 3 expression).", "entity1": "caspase 3", "entity2": "RS -GRA", "span1": [271, 280], "span2": [109, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1320": {"label": 3, "data": {"text": "Thus, bupropion acts as an antagonist at alpha3beta2* and alpha3beta4* nAChRs in rat striatum and hippocampus, respectively, across the same concentration range that inhibits DAT and NET function.", "entity1": "DAT", "entity2": "bupropion", "span1": [175, 178], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10535": {"label": 1, "data": {"text": "The ability of this cis-acting RAR-RXR binding element to activate transcription in response to RA also depended on downstream sequences where an octamer transcription factor 1 (Oct1) site and a nuclear factor of activated T cells (NFATc) site between this element and the transcriptional start, as well as a cyclic AMP response element binding factor (CREB) site between the transcriptional start and first exon of the blr1 gene, were necessary.", "entity1": "NFATc", "entity2": "RA", "span1": [232, 237], "span2": [96, 98]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7676": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "carbonic anhydrase", "entity2": "acetazolamide", "span1": [93, 111], "span2": [204, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12532": {"label": 8, "data": {"text": "Differential lactose/lactulose/L-rhamnose absorption provides a non-invasive and sensitive index of small intestinal integrity of value for the interpretation of prolonged or otherwise complicated enteritis and the distinction of primary secondary intestinal lactase deficiency.", "entity1": "lactase", "entity2": "L-rhamnose", "span1": [259, 266], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8288": {"label": 3, "data": {"text": "In this paper a series of new 1,3,4-thiadiazole derivatives has been designed, synthesized and evaluated as the acetyl- and butyrylcholinesterase inhibitors.", "entity1": "acetyl- and butyrylcholinesterase", "entity2": "1,3,4-thiadiazole", "span1": [112, 145], "span2": [30, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9785": {"label": 5, "data": {"text": "The nonselective opioid receptor antagonist, naloxone (3 mg/kg, i.m.", "entity1": "opioid receptor", "entity2": "naloxone", "span1": [17, 32], "span2": [45, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7272": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "indisulam", "span1": [218, 224], "span2": [158, 167]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13858": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "17beta-hydroxysteroid-dehydrogenase type 1", "entity2": "dydrogesterone", "span1": [266, 308], "span2": [60, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6": {"label": 5, "data": {"text": "The isoprenaline attenuation responses of the portal vein were inhibited by labetalol and dilevalol (both at > or = 10(-7) M) and the pA2 value for the labetalol at beta 2-adrenoceptors was 7.59.", "entity1": "beta 2-adrenoceptors", "entity2": "labetalol", "span1": [165, 185], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4145": {"label": 3, "data": {"text": "ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.", "entity1": "BCL-2", "entity2": "ABT-199", "span1": [32, 37], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1298": {"label": 3, "data": {"text": "OBJECTIVE: Celecoxib and rofecoxib are two relatively new nonsteroidal anti-inflammatory drugs (NSAIDs) that selectively inhibit the cyclo-oxygenase-2 (COX-2) isoenzyme at therapeutic concentrations.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [152, 157], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12486": {"label": 8, "data": {"text": "Cynomolgus FMO1, FMO2, FMO3, and FMO5 metabolized benzydamine, and FMO1/FMO3 and FMO3 also metabolized methimazole and trimethylamine, respectively.", "entity1": "FMO3", "entity2": "trimethylamine", "span1": [72, 76], "span2": [119, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5794": {"label": 0, "data": {"text": "Comparison of the amino acid sequence of porcine ACY-1 with those of other Zn2+-binding metalloenzymes showed no significant homologies in either the overall sequence or the consensus sequences for the metal binding sites.", "entity1": "Zn2+-binding metalloenzymes", "entity2": "amino acid", "span1": [75, 102], "span2": [18, 28]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4371": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "DEX-P", "span1": [171, 176], "span2": [220, 225]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14140": {"label": 1, "data": {"text": "In [(35)S]GTPgammaS assays, mianserin selectively activated kappa-opioid receptors.", "entity1": "kappa-opioid receptors", "entity2": "[(35)S]GTPgammaS", "span1": [60, 82], "span2": [3, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8294": {"label": 2, "data": {"text": "LY294002, a specific PI3K/AKT inhibitor, selectively activated the p38 MAPK kinase pathway and enhanced c-Jun phosphorylation, but did not activate JNK.", "entity1": "kinase", "entity2": "LY294002", "span1": [76, 82], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1950": {"label": 1, "data": {"text": "These results demonstrate that this receptor corresponds to the previously called \"P2t\" platelet receptor and show that the active metabolite of clopidogrel binds in a covalent manner to this receptor, thus explaining how it blocks the aggregating effect of ADP on platelets.", "entity1": "P2t", "entity2": "ADP", "span1": [83, 86], "span2": [258, 261]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9931": {"label": 9, "data": {"text": "Activation of extracellular signal-related kinase (ERK) 1 and 2, c-Jun-N-terminal kinase (JNK) 1, and p38 was unaffected by sulfasalazine.", "entity1": "p38", "entity2": "sulfasalazine", "span1": [102, 105], "span2": [124, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6428": {"label": 2, "data": {"text": "Creatine phosphokinase activity in plasma increased slightly (compared to control, pyridostigmine or exercise group) in mice treated with pyridostigmine plus exercise, which may be indicative of perturbation in the integrity of the skeletal muscle due to combination.", "entity1": "Creatine phosphokinase", "entity2": "pyridostigmine", "span1": [0, 22], "span2": [83, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8979": {"label": 3, "data": {"text": "The suppressive effect of ceruletide on barrel rotation could be partially countered by MK-329, a selective peripheral CCK (CCK-A) receptor antagonist.", "entity1": "CCK", "entity2": "ceruletide", "span1": [119, 122], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"149": {"label": 3, "data": {"text": "Loperamide is a peripheral opiate agonist able to inhibit ACTH secretion.", "entity1": "ACTH", "entity2": "Loperamide", "span1": [58, 62], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14742": {"label": 1, "data": {"text": "Arsenic suppresses cell survival via Pirh2-mediated proteasomal degradation of \u0394Np63 protein.", "entity1": "\u0394Np63", "entity2": "Arsenic", "span1": [79, 84], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12902": {"label": 3, "data": {"text": "While either blockage of HO activity by the HO inhibitor, tin protoporphyrin IX, or down-regulation of HO-1 expression by HO-1 small interfering RNA (siRNA) reversed the inhibitory effects of H(2)S on iNOS expression and NO production, HO-1 overexpression produced the same inhibitory effects of H(2)S. In addition, LPS-induced nuclear factor (NF)-kappaB activation was diminished in RAW264.7 macrophages preincubated with H(2)S. Interestingly, the inhibitory effect of H(2)S on NF-kappaB activation was reversed by the transient transfection with HO-1 siRNA, but was mimicked by either HO-1 gene transfection or treatment with carbon monoxide (CO), an end product of HO-1.", "entity1": "iNOS", "entity2": "H(2)S", "span1": [201, 205], "span2": [192, 197]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11646": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "ALA-T", "entity2": "VIG", "span1": [280, 285], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12560": {"label": 1, "data": {"text": "Risperidone was 120-fold more selective for the alpha 1B-adrenoceptor with respect to the alpha 1A-adrenoceptor (Ki values: 2.3 +/- 1.2 nM and 283.6 +/- 174.1 nM respectively).", "entity1": "alpha 1A-adrenoceptor", "entity2": "Risperidone", "span1": [90, 111], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7716": {"label": 1, "data": {"text": "Two pure GnRH antagonists have been developed, abarelix and degarelix, that are devoid of any agonist effect on the GnRH receptor and consequently do not result in testosterone flare.", "entity1": "GnRH receptor", "entity2": "abarelix", "span1": [116, 129], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14249": {"label": 1, "data": {"text": "Androstanol and androstenol, estrone, 17\u03b2-estradiol, TCPOBOP, and CITCO showed compound-specific but similar affinities for both CARs.", "entity1": "CARs", "entity2": "TCPOBOP", "span1": [129, 133], "span2": [53, 60]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2598": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "D(1)", "entity2": "risperidone", "span1": [57, 61], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2204": {"label": 3, "data": {"text": "This study provided the evidence that the tetracyclines inhibit stimulated cerebral MMP-9 at multiple levels and are effective at very low doses, offering great potential for therapeutic use.", "entity1": "MMP-9", "entity2": "tetracyclines", "span1": [84, 89], "span2": [42, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8492": {"label": 9, "data": {"text": "Curcuminoids Modulate Pro-Oxidant-Antioxidant Balance but not the Immune Response to Heat Shock Protein 27 and Oxidized LDL in Obese Individuals.", "entity1": "Heat Shock Protein 27", "entity2": "Curcuminoids", "span1": [85, 106], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9034": {"label": 5, "data": {"text": "To study the mechanism underlying this phenomenon, the effects of the nonselective beta-adrenoceptor antagonists propranolol [no intrinsic sympathomimetic activity (ISA)], alprenolol (weak ISA) and mepindolol (strong ISA) on lymphocyte beta 2-adrenoceptor density--assessed by (+/-)-[125I]-iodocyanopindolol (ICYP) binding--and plasma renin activity (PRA) were investigated in male healthy volunteers aged 23-35 years.", "entity1": "beta-adrenoceptor", "entity2": "mepindolol", "span1": [83, 100], "span2": [198, 208]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10664": {"label": 8, "data": {"text": "An angiotensin II AT1 receptor antagonist, telmisartan augments glucose uptake and GLUT4 protein expression in 3T3-L1 adipocytes.", "entity1": "GLUT4", "entity2": "glucose", "span1": [83, 88], "span2": [64, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12078": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "3 beta-HSD", "entity2": "3-keto-4-ene-steroids", "span1": [74, 84], "span2": [292, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9220": {"label": 3, "data": {"text": "Since both TFP and W-7 are potent inhibitors of calmodulin, we investigated the possibility that inhibition of calmodulin was responsible for the loss of receptors.", "entity1": "calmodulin", "entity2": "TFP", "span1": [48, 58], "span2": [11, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"304": {"label": 3, "data": {"text": "The effects of D-1997 in the basilar artery were not modified by incubation with either the 5-HT2 receptor antagonist ketanserin (0.01-1 microM), the 5-HT3 and 5-HT4 receptor antagonist ICS205930 (tropisetron; 0.1-10 microM), the 5-HT1A receptor antagonist spiroxatrine (0.01-1 microM), the beta-adrenoceptor blocker with high affinity for 5-HT1A and 5-HT1B binding sites (+/-)-pindolol (0.01-1 microM), or the alpha 1-adrenoceptor antagonist prazosin (0.01-1 microM).", "entity1": "beta-adrenoceptor", "entity2": "(+/-)-pindolol", "span1": [291, 308], "span2": [372, 386]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6942": {"label": 1, "data": {"text": "As examples, ketorolac, flurbiprofen, ketoprofen and indomethacin have increased COX-1 selectivity when compared with naproxen and ibuprofen.", "entity1": "COX-1", "entity2": "indomethacin", "span1": [81, 86], "span2": [53, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9374": {"label": 1, "data": {"text": "Recovery from modulation by cyclothiazide was slower for GluR-AiBi and GluR-AoBi than for GluR-AiBo and GluR-AoBo.", "entity1": "GluR-AiBi", "entity2": "cyclothiazide", "span1": [57, 66], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13546": {"label": 2, "data": {"text": "Furthermore, the activities of the two torafugu PPARalphas were enhanced 4.3- and 7.6-fold by arachidonic acid, 4.4- and 5.2-fold by docosahexaenoic acid, and 6.7- and 8.0-fold by eicosapentaenoic acid each at 50 microM, respectively.", "entity1": "torafugu PPARalphas", "entity2": "arachidonic acid", "span1": [39, 58], "span2": [94, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3443": {"label": 4, "data": {"text": "LY541850 was claimed from human mGlu receptors expressed in non-neuronal cells to be a selective orthosteric mGlu2 agonist and mGlu3 antagonist.", "entity1": "mGlu2", "entity2": "LY541850", "span1": [109, 114], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6778": {"label": 1, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX", "entity2": "diclofenac", "span1": [119, 122], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15918": {"label": 4, "data": {"text": "The current study examined the bioactivation potential of ghrelin receptor inverse agonists, 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(imidazo[2,1-b]thiazol-6-yl)ethanone (1) and 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone (2), containing a fused imidazo[2,1-b]thiazole motif in the core structure.", "entity1": "ghrelin receptor", "entity2": "1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(imidazo[2,1-b]thiazol-6-yl)ethanone", "span1": [58, 74], "span2": [93, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9642": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "androgen receptor", "entity2": "estramustine", "span1": [162, 179], "span2": [85, 97]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10010": {"label": 4, "data": {"text": "In mice, AS-8112 (1.0 - 3.0 mg kg(-1) s.c.) potently inhibited hypothermia induced by the dopamine D3 receptor agonist; R(+)-7-OH-DPAT (R(+)-7-hydroxy-2-(N,N-di-n-propylamino)tetraline) (0.3 mg kg(-1) s.c.).", "entity1": "dopamine D3 receptor", "entity2": "R(+)-7-OH-DPAT", "span1": [90, 110], "span2": [120, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11803": {"label": 1, "data": {"text": "In this study, we assessed the antitumor activity of PTE against human osteosarcoma cells and explored the role of JAK2/STAT3 and apoptosis-related signaling pathways on the activity of PTE.", "entity1": "STAT3", "entity2": "PTE", "span1": [120, 125], "span2": [186, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2554": {"label": 3, "data": {"text": "Recent studies have reported that imatinib mesylate, a kinase inhibitor that targets the intracellular tyrosine kinase BCR-ABL and the platelet derived growth factor (PDGF) receptor, is an effective inhibitor of the macrophage colony stimulating factor (M-CSF) receptor, c-FMS.", "entity1": "macrophage colony stimulating factor (M-CSF) receptor", "entity2": "imatinib mesylate", "span1": [216, 269], "span2": [34, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14250": {"label": 1, "data": {"text": "Androstanol and androstenol, estrone, 17\u03b2-estradiol, TCPOBOP, and CITCO showed compound-specific but similar affinities for both CARs.", "entity1": "CARs", "entity2": "CITCO", "span1": [129, 133], "span2": [66, 71]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15416": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "IL-8", "entity2": "cholesterol", "span1": [71, 75], "span2": [273, 284]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"11002": {"label": 1, "data": {"text": "In this study, antidepressants with selectivity for the noradrenaline transporter (reboxetine and desipramine), or the serotonin transporter (fluoxetine and clomipramine) were examined in terms of their ability to promote an anti-inflammatory cytokine phenotype in human blood.", "entity1": "noradrenaline transporter", "entity2": "reboxetine", "span1": [56, 81], "span2": [83, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"9093": {"label": 3, "data": {"text": "Kinetic analysis revealed that the inhibition of the leukotriene C synthetase reaction by diethylcarbamazine was competitive with respect to LTA4.", "entity1": "leukotriene C synthetase", "entity2": "diethylcarbamazine", "span1": [53, 77], "span2": [90, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3664": {"label": 3, "data": {"text": "The mRNA levels of microphthalmia-associated transcription factor (MITF) and its downstream genes tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 were reduced by artemisinic acid treatment.", "entity1": "tyrosinase", "entity2": "artemisinic acid", "span1": [98, 108], "span2": [172, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1274": {"label": 7, "data": {"text": "Ever since the discovery that (6R)-5,6,7,8-tetrahydro-L-biopterin (BH4) is a cofactor of NOS, its function has been the object of intense research and occasional controversy.", "entity1": "NOS", "entity2": "(6R)-5,6,7,8-tetrahydro-L-biopterin", "span1": [89, 92], "span2": [30, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"8079": {"label": 3, "data": {"text": "This study was designed to test the hypothesis that orlistat inhibits CESs with higher potency toward CES1 than CES2, a carboxylesterase with little lipase activity.", "entity1": "lipase", "entity2": "orlistat", "span1": [149, 155], "span2": [52, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4948": {"label": 3, "data": {"text": "In addition, the disease activity index, histopathologic scores and myeloperoxidase activity were also significantly reduced by Fc11a-2 treatment.", "entity1": "myeloperoxidase", "entity2": "Fc11a-2", "span1": [68, 83], "span2": [128, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7945": {"label": 2, "data": {"text": "Distinct roles of methamphetamine in modulating spatial memory consolidation, retrieval, reconsolidation and the accompanying changes of ERK and CREB activation in hippocampus and prefrontal cortex.", "entity1": "CREB", "entity2": "methamphetamine", "span1": [145, 149], "span2": [18, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5454": {"label": 3, "data": {"text": "In addition, pretreatment with Z-Val-Ala-Asp-fluoromethylketone (Z-VAD-fmk), a broad spectrum of caspase inhibitor, could not rescue apoptotic cells from ClpP toxicity.", "entity1": "caspase", "entity2": "Z-VAD-fmk", "span1": [97, 104], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8744": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "olanzapine", "span1": [18, 25], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"12856": {"label": 1, "data": {"text": "BACKGROUND AND AIMS: Thymidylate synthase (TS) is an important enzyme for DNA synthesis and the target for 5-fluorouracil (5-FU).", "entity1": "TS", "entity2": "5-fluorouracil", "span1": [43, 45], "span2": [107, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7263": {"label": 3, "data": {"text": "Some clinically used compounds, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, sulpiride, and indisulam, or the orphan drug benzolamide, showed effective hCA VI inhibitory activity, with inhibition constants of 0.8-79 nM.", "entity1": "hCA VI", "entity2": "acetazolamide", "span1": [218, 224], "span2": [40, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1736": {"label": 5, "data": {"text": "The alpha(1)-adrenoceptor antagonist, tamsulosin, is selective for alpha(1A)- and alpha(1D)- over alpha(1B)-adrenoceptors.", "entity1": "alpha(1)-adrenoceptor", "entity2": "tamsulosin", "span1": [4, 25], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15119": {"label": 2, "data": {"text": "Mn exposure (20\u00a0mg/kg) increased p38(MAPK) and Akt phosphorylation, but decreased DARPP-32-Thr-34 phosphorylation.", "entity1": "Akt", "entity2": "Mn", "span1": [47, 50], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"934": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "FdUrd", "span1": [216, 236], "span2": [49, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9469": {"label": 1, "data": {"text": "The DP, IP and TP receptors showed high ligand binding specificity and only bound their own putative ligands with high affinity such as PGD2, BW245C and BW868C for DP, cicaprost, iloprost and isocabacyclin for IP, and S-145, I-BOP and GR 32191 for TP.", "entity1": "IP", "entity2": "cicaprost", "span1": [210, 212], "span2": [168, 177]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8777": {"label": 3, "data": {"text": "Caffeic Acid Phenethyl Ester Suppresses Proliferation and Survival of TW2.6 Human Oral Cancer Cells via Inhibition of Akt Signaling.", "entity1": "Akt", "entity2": "Caffeic Acid Phenethyl Ester", "span1": [118, 121], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2203": {"label": 3, "data": {"text": "In vitro, minocycline, but not doxycycline, inhibits MMP-9, at least in part, via the extracellular signaling-related kinase 1/2 (ERK1/2)-mediated pathway.", "entity1": "MMP-9", "entity2": "doxycycline", "span1": [53, 58], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13441": {"label": 1, "data": {"text": "The inhibitory effects of GW9662 and T0070907 (PPARgamma antagonists), on COX-2 expression and on stimulation of COX-2 promoter activity by EPA and GLA suggest that PPARgamma is implicated in COX-2 induction.", "entity1": "COX-2", "entity2": "GW9662", "span1": [74, 79], "span2": [26, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3164": {"label": 3, "data": {"text": "Furthermore, the Panx1 channel blockers carbenoxolone and Probenecid were less effective in inhibiting Panx1 currents when Kvbeta3 was co-expressed.", "entity1": "Panx1", "entity2": "Probenecid", "span1": [17, 22], "span2": [58, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1845": {"label": 8, "data": {"text": "Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide.", "entity1": "SR-BI", "entity2": "cholesterol", "span1": [20, 25], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5346": {"label": 2, "data": {"text": "S1P increased the amount of osteoprotegerin at both mRNA and protein levels, and increased the activity of alkaline phosphatase, leading to the mineralization.", "entity1": "osteoprotegerin", "entity2": "S1P", "span1": [28, 43], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3053": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "CXCR4", "entity2": "Plerixafor", "span1": [173, 178], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9804": {"label": 3, "data": {"text": "With respect to the quinone co-substrate of the dihydroorotate dehydrogenase, atovaquone (Kic = 2.7 microM) and dichloroally-lawsone (Kic = 9.8 nM) were shown to be competitive inhibitors of human dihydroorotate dehydrogenase.", "entity1": "human dihydroorotate dehydrogenase", "entity2": "atovaquone", "span1": [191, 225], "span2": [78, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12798": {"label": 8, "data": {"text": "As thiamine metabolism deficiencies have been seen in placental infarcts previously, these indicate that PP20/hTPK may have a role in placental diseases.", "entity1": "hTPK", "entity2": "thiamine", "span1": [110, 114], "span2": [3, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3215": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "carbonic anhydrase", "entity2": "gallic acid", "span1": [262, 280], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6762": {"label": 2, "data": {"text": "In vivo, hydralazine induced HIF-1alpha and VEGF protein in tissue extracts and elevated plasma VEGF levels.", "entity1": "VEGF", "entity2": "hydralazine", "span1": [96, 100], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14274": {"label": 8, "data": {"text": "We recently showed that TETA is metabolized in vitro by polyamine catabolic enzyme spermidine/spermine-N(1)-acetyltransferase (SSAT1) and by thialysine acetyltransferase (SSAT2) to its monoacetylated derivative (MAT).", "entity1": "SSAT2", "entity2": "TETA", "span1": [171, 176], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1266": {"label": 3, "data": {"text": "Increased IL-5 activity in the serum was inhibited by both pranlukast and MCI-826 by over 90%.", "entity1": "IL-5", "entity2": "pranlukast", "span1": [10, 14], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2308": {"label": 2, "data": {"text": "Cotreatment with U0126 and YC-1 synergistically increases apoptosis in colorectal cancer cells and recapitulates the effects of sulindac treatment on ERK1/2, JNK, and beta-catenin.", "entity1": "JNK", "entity2": "sulindac", "span1": [158, 161], "span2": [128, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6113": {"label": 3, "data": {"text": "Amezinium is much less potent as a MAO inhibitor in cells with the uptake2 transporter, such as the myocardial cells of the heart.", "entity1": "MAO", "entity2": "Amezinium", "span1": [35, 38], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11049": {"label": 3, "data": {"text": "For some, pharmacologic inhibitors are available, including sorafenib for BRAF, farnesyltransferase inhibitors for NRAS, PD-0325901 for mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, rapamycin analogues for mammalian target of rapamycin, and agents that inhibit either vascular endothelial growth factor or its receptors.", "entity1": "BRAF", "entity2": "sorafenib", "span1": [74, 78], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6169": {"label": 3, "data": {"text": "Selegiline (deprenyl), a selective, irreversible inhibitor of monoamine oxidase type B (MAO-B) is widely used in the treatment of Parkinson's disease.", "entity1": "MAO-B", "entity2": "Selegiline", "span1": [88, 93], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15601": {"label": 1, "data": {"text": "All three agents induced mdr1a.fLUC expression (bioluminescence), but only PCN and docetaxel appeared to act primarily via PXR.", "entity1": "mdr1a", "entity2": "PCN", "span1": [25, 30], "span2": [75, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11514": {"label": 1, "data": {"text": "FK778, is a synthetic malononitrilamide that targets the critical enzyme of the de novo pyrimidine synthesis, dihydroorotic acid dehydrogenase, and receptor-associated tyrosine kinases has completed phase II trials.", "entity1": "receptor-associated tyrosine kinases", "entity2": "FK778", "span1": [148, 184], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2098": {"label": 1, "data": {"text": "In higher cortical structures such as the hippocampus, norepinephrine, via beta adrenergic receptor (AR) activation, has been shown to reinforce the cognitive processes of attention and memory.", "entity1": "beta adrenergic receptor", "entity2": "norepinephrine", "span1": [75, 99], "span2": [55, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"554": {"label": 8, "data": {"text": "The purified phosphodiester alpha-GlcNAcase has a specific activity of 498 micromol of [3H]GlcNAc-alpha-phosphomannose-alpha-methyl cleaved per h per mg of protein using 0.5 mM [3H]GlcNAc-alpha-phosphomannose-alpha-methyl as substrate.", "entity1": "phosphodiester alpha-GlcNAcase", "entity2": "[3H]GlcNAc-alpha-phosphomannose-alpha-methyl", "span1": [13, 43], "span2": [177, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"15354": {"label": 8, "data": {"text": "The (R)-omeprazole hydroxylation index reflects CYP2C19 activity in healthy Japanese volunteers.", "entity1": "CYP2C19", "entity2": "(R)-omeprazole", "span1": [48, 55], "span2": [4, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4435": {"label": 3, "data": {"text": "A series of xanthine derivatives in which a methylene was inserted at position 8 of xanthine scaffold was synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes.", "entity1": "dipeptidyl peptidase 4", "entity2": "xanthine", "span1": [149, 171], "span2": [84, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8923": {"label": 3, "data": {"text": "This same dose of carvedilol also inhibited, but to a lesser degree, the beta 2 adrenoceptor mediated vasodepressor response to salbutamol in pithed rats whose blood pressure was elevated by a constant intravenous infusion of angiotensin II.", "entity1": "beta 2 adrenoceptor", "entity2": "carvedilol", "span1": [73, 92], "span2": [18, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4244": {"label": 1, "data": {"text": "In addition, butein-dependent HO-1 expression was required for the inhibition of H2O2-induced cell death and ROS generation.", "entity1": "HO-1", "entity2": "butein", "span1": [30, 34], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2544": {"label": 9, "data": {"text": "Imatinib was also found to inhibit M-CSF-induced osteoclast survival as well as M-CSF-induced osteoclast bone resorbing activity, but was without effect on interleukin 1alpha (IL-1alpha) and receptor activator of nuclear factor kappa B ligand (RANKL)-induced inhibition of osteoclasts apoptosis, further supporting the hypothesis that imatinib may affect mature osteoclasts through the inhibition of c-FMS.", "entity1": "interleukin 1alpha", "entity2": "Imatinib", "span1": [156, 174], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1474": {"label": 8, "data": {"text": "Interestingly, the allele of PRO1 was shown to enhance the activities of gamma-glutamyl kinase and gamma-glutamyl phosphate reductase, both of which catalyze the first two steps of L-proline synthesis from L-glutamate and which together may form a complex in vivo.", "entity1": "gamma-glutamyl phosphate reductase", "entity2": "L-glutamate", "span1": [99, 133], "span2": [206, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"948": {"label": 3, "data": {"text": "Experimental cystathioninuria was induced in rats by administration of the cystathionine gamma-lyase inhibitor, D,L-propargylglycine.", "entity1": "cystathionine gamma-lyase", "entity2": "D,L-propargylglycine", "span1": [75, 100], "span2": [112, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14227": {"label": 5, "data": {"text": "Adult ovariectomised rats were divided into six groups and injected either with vehicle or a single dose of oestradiol, a selective ER\u03b1 agonist-PPT [4,4',4\u2033-(4-propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol], a selective ER\u03b2 agonist-DPN [2,3-bis(4-hydroxyphenyl)-propionitrile], a selective ER\u03b1 antagonist-MPP [1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride] or a selective ER\u03b2 antagonist-PHTPP (4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol).", "entity1": "ER\u03b1", "entity2": "1,3-bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol", "span1": [288, 291], "span2": [308, 374]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6991": {"label": 3, "data": {"text": "CONCLUSIONS: This study shows that valproic acid acts as a non-competitive inhibitor of brain microsomal Acsl, and that inhibition is substrate-selective.", "entity1": "brain microsomal Acsl", "entity2": "valproic acid", "span1": [88, 109], "span2": [35, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"3906": {"label": 9, "data": {"text": "Cells exposed to \u03b1-MeDA showed an increase in intracellular glutathione (GSH) levels, which, at the 48 h time-point, was not dependent in the activity increase of \u03b3-glutamylcysteine synthetase (\u03b3-GCS), revealing a possible transient effect.", "entity1": "\u03b3-glutamylcysteine synthetase", "entity2": "\u03b1-MeDA", "span1": [163, 192], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12897": {"label": 3, "data": {"text": "CO treatment also inhibited LPS-induced NO production and iNOS expression via its inactivation of NF-kappaB.", "entity1": "iNOS", "entity2": "CO", "span1": [58, 62], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"240": {"label": 1, "data": {"text": "In all cases at both the 5-HT2A and 5-HT2C receptors, the affinities of the isomers of MDMA and MDA were at least 2-3 orders of magnitude less than 5-HT.", "entity1": "5-HT2C", "entity2": "5-HT", "span1": [36, 42], "span2": [148, 152]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10972": {"label": 3, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "RAR-beta", "entity2": "retinoid", "span1": [27, 35], "span2": [154, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14814": {"label": 4, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1)", "entity2": "SR141716A", "span1": [28, 33], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3695": {"label": 3, "data": {"text": "8-pCPT-2'-O-Me-cAMP-AM potentiation of insulin secretion stimulated by tolbutamide was markedly inhibited by 2-APB (25 \u03bcM) and enhanced by the PKC inhibitor bisindolylmaleimide I (1 \u03bcM).", "entity1": "PKC", "entity2": "bisindolylmaleimide I", "span1": [143, 146], "span2": [157, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"228": {"label": 3, "data": {"text": "The inhibition of UG synthesis and PR down-regulation by 5 alpha-NET and 3 beta,5 alpha-NET indicates that these NET metabolites possess antiprogestational properties.", "entity1": "UG", "entity2": "3 beta,5 alpha-NET", "span1": [18, 20], "span2": [73, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6491": {"label": 4, "data": {"text": "RESULTS: The alpha(2)-adrenoceptor agonists induced vasoconstriction in the porcine ciliary artery with the following potency order (EC(50)) expressed in nanomolar: brimonidine 2.11, oxymetazoline 5.26, and apraclonidine 13.0.", "entity1": "alpha(2)-adrenoceptor", "entity2": "apraclonidine", "span1": [13, 34], "span2": [207, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7917": {"label": 8, "data": {"text": "Heterologous expression of rCtr1 in HEK293 cells (HEK/rCtr1 cells) increased the uptake and cytotoxicity of copper, oxaliplatin, cisplatin and carboplatin, in comparison to isogenic vector-transfected control cells.", "entity1": "rCtr1", "entity2": "copper", "span1": [54, 59], "span2": [108, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10458": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "(L-serine dehydratase", "entity2": "L-serine", "span1": [4, 25], "span2": [108, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13032": {"label": 3, "data": {"text": "Ingestion of competitive inhibitors of 11beta-HSD2 such as liquorice and carbenoxolone result in a similar but milder clinical phenotype.", "entity1": "11beta-HSD2", "entity2": "carbenoxolone", "span1": [39, 50], "span2": [73, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15790": {"label": 1, "data": {"text": "Immunocytochemical analyses and function were consistent with pannexin1 localization to T-tubules intercalated with dihydropyridine and ryanodine receptors in slow (soleus) and fast (extensor digitorum longus, EDL) muscles.", "entity1": "pannexin1", "entity2": "dihydropyridine", "span1": [62, 71], "span2": [116, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3822": {"label": 3, "data": {"text": "In muscle and liver, TCDD (10 ng/kg/day) induced increases in methylation and decreases in mRNA expression of Igf2r.", "entity1": "Igf2r", "entity2": "TCDD", "span1": [110, 115], "span2": [21, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12804": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "c-kit", "entity2": "Gleevec", "span1": [120, 125], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10752": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "2'-deoxyuridine", "span1": [282, 284], "span2": [160, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7318": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "alanine serine cysteine transporter 1", "entity2": "amino acids", "span1": [196, 233], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3438": {"label": 2, "data": {"text": "These results showed that WNT6 and Cav1 are upregulated by chemotherapeutics and enhance the resistance of GC cells to anthracycline drugs.", "entity1": "WNT6", "entity2": "anthracycline", "span1": [26, 30], "span2": [119, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8219": {"label": 1, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "ERG", "entity2": "ICA-105574", "span1": [109, 112], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8878": {"label": 1, "data": {"text": "TCDD treatment of the cells largely prevented the activation of eukaryotic translation initiation factor 4E-binding protein 1, a regulator of translation initiation and substrate of the mammalian target of rapamycin (mTOR).", "entity1": "mTOR", "entity2": "TCDD", "span1": [217, 221], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7142": {"label": 1, "data": {"text": "A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization.", "entity1": "phosphodiesterase-5", "entity2": "sildenafil", "span1": [27, 46], "span2": [102, 112]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3920": {"label": 3, "data": {"text": "N-alkylation of the pyridazinone ring markedly enhances potency against PDE4 but suppresses PDE3 inhibition.", "entity1": "PDE3", "entity2": "pyridazinone", "span1": [92, 96], "span2": [20, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7654": {"label": 2, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-2", "entity2": "monocrotaline", "span1": [0, 5], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4715": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Lgr5", "entity2": "TCDD", "span1": [482, 486], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3400": {"label": 2, "data": {"text": "In addition, PSE inhibited the transcriptional activity of NFAT without interfering with the calcium-induced NFAT dephosphorylation event, which represents the major signaling pathway for its activation.", "entity1": "NFAT", "entity2": "calcium", "span1": [109, 113], "span2": [93, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11041": {"label": 4, "data": {"text": "A selective retinoid X receptor agonist bexarotene (LGD1069, targretin) inhibits angiogenesis and metastasis in solid tumours.", "entity1": "retinoid X receptor", "entity2": "targretin", "span1": [12, 31], "span2": [61, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3863": {"label": 3, "data": {"text": "HSYA suppressed the expression of TLR-4, Myd88, ICAM-1, TNF\u03b1, IL-1\u03b2 and IL-6 at the mRNA and protein level, and inhibited the adhesion of leukocytes to A549 cells.", "entity1": "IL-6", "entity2": "HSYA", "span1": [72, 76], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13480": {"label": 4, "data": {"text": "This report reviews published and unpublished data that suggest that aripiprazole acts as a selective partial agonist at the dopamine D(2) receptor and does not affect 5-HT receptors at therapeutic doses.", "entity1": "dopamine D(2) receptor", "entity2": "aripiprazole", "span1": [125, 147], "span2": [69, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11677": {"label": 2, "data": {"text": "In a recent study using protein-specific anti-acetyl lysine antibodies and immunological methods, we demonstrated the ability of aspirin to acetylate the tumor suppressor protein p53.", "entity1": "tumor suppressor protein p53", "entity2": "aspirin", "span1": [154, 182], "span2": [129, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11162": {"label": 8, "data": {"text": "Recombinant PDE10A transfected and expressed in COS-7 cells hydrolyzed cAMP and cGMP with Km values of 0.26 and 7.2 microM, respectively, and Vmax with cGMP was almost twice that with cAMP.", "entity1": "PDE10A", "entity2": "cGMP", "span1": [12, 18], "span2": [80, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4765": {"label": 3, "data": {"text": "Furthermore, BRN-250 inhibited the VEGF-induced phosphorylation and intracellular tyrosine kinase activity of VEGF receptor 2 (VEGFR2) and the activation of its downstream AKT pathway.", "entity1": "tyrosine kinase", "entity2": "BRN-250", "span1": [82, 97], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12242": {"label": 8, "data": {"text": "The carboxylation of glutamic acid residues to gamma-carboxyglutamic acid (Gla) by the vitamin K-dependent gamma-glutamyl carboxylase (gamma-carboxylase) is an essential posttranslational modification required for the biological activity of a number of proteins, including proteins involved in blood coagulation and its regulation.", "entity1": "gamma-carboxylase", "entity2": "Gla", "span1": [135, 152], "span2": [75, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10782": {"label": 1, "data": {"text": "In the presence of IL-18, simvastatin suppressed the expression of ICAM-1 and CD40 as well as the production of IL-12, TNF-alpha and IFN-gamma in PBMC, contributing to the anti-inflammatory effect of simvastatin.", "entity1": "IL-18", "entity2": "simvastatin", "span1": [19, 24], "span2": [26, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13397": {"label": 2, "data": {"text": "In hearts treated with metformin, [AMP] was increased at 50 min and AMPK activity, phosphorylated AMPK, and phosphorylated acetyl-CoA carboxylase were elevated at 61 min.", "entity1": "AMPK", "entity2": "metformin", "span1": [68, 72], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9355": {"label": 2, "data": {"text": "Expressions of insulin and PC3, but not PC2, are coordinately regulated by glucose, consistent with the important role of PC3 in regulating proinsulin processing.", "entity1": "insulin", "entity2": "glucose", "span1": [15, 22], "span2": [75, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4072": {"label": 8, "data": {"text": "During early pregnancy in sheep, the elongating conceptus secretes interferon-\u03c4 (IFNT) and the conceptus as well as endometrial epithelia produce prostaglandins (PG) via PG synthase 2 (PTGS2) and cortisol via hydroxysteroid (11-\u03b2) dehydrogenase 1 (HSD11B1).", "entity1": "PG synthase 2", "entity2": "prostaglandins", "span1": [170, 183], "span2": [146, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7610": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(1a)", "entity2": "Vaprisol", "span1": [192, 197], "span2": [222, 230]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15647": {"label": 1, "data": {"text": "With the former, abacavir seemingly participates in the MHC T-cell receptor binding interaction.", "entity1": "T-cell receptor", "entity2": "abacavir", "span1": [60, 75], "span2": [17, 25]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10009": {"label": 4, "data": {"text": "In guinea-pig isolated colon, AS-8112 produced a rightward shift of the concentration-response curves of 2-methyl-5HT, a 5-HT3 receptor agonist (pA2 value of 7.04).", "entity1": "5-HT3 receptor", "entity2": "2-methyl-5HT", "span1": [121, 135], "span2": [105, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10122": {"label": 5, "data": {"text": "A TXA2 receptor antagonist (S-1452) attenuated the contraction in a concentration-dependent manner.", "entity1": "TXA2 receptor", "entity2": "S-1452", "span1": [2, 15], "span2": [28, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13946": {"label": 1, "data": {"text": "denopamine for beta(1); clenbuterol, AZ 40140d, salbutamol for beta(2)) were found to have subtype-selective intrinsic efficacy.", "entity1": "beta(2)", "entity2": "clenbuterol", "span1": [63, 70], "span2": [24, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7871": {"label": 3, "data": {"text": "The disposition of anagliptin, an orally active, highly selective dipeptidyl peptidase-4 inhibitor, was investigated after a single oral dose of 100 mg/1.92 MBq [(14)C]anagliptin to six healthy men.", "entity1": "dipeptidyl peptidase-4", "entity2": "anagliptin", "span1": [66, 88], "span2": [19, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10518": {"label": 3, "data": {"text": "CONCLUSION: GW572016 potently inhibits receptor phosphorylation in either EGFR- or HER2-overexpressing cell lines and has both antiproliferative and radiosensitizing effects.", "entity1": "HER2", "entity2": "GW572016", "span1": [83, 87], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7192": {"label": 3, "data": {"text": "Decitabine inhibits DNA methyltransferase and has shown therapeutic effects in patients with hematologic malignancies.", "entity1": "DNA methyltransferase", "entity2": "Decitabine", "span1": [20, 41], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4892": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "sulfatase", "entity2": "F", "span1": [162, 171], "span2": [99, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2256": {"label": 1, "data": {"text": "In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities.", "entity1": "p-glycoprotein", "entity2": "rifampicin", "span1": [166, 180], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6754": {"label": 3, "data": {"text": "STI571 binding to Flt3 is prevented by the phenylalanine 691 side-chain in the ATP binding center and mutating this site to threonine renders the corresponding Flt3 mutant sensitive to STI571.", "entity1": "Flt3", "entity2": "STI571", "span1": [160, 164], "span2": [185, 191]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5723": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "ezetimibe", "span1": [33, 36], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"256": {"label": 1, "data": {"text": "An experimental strategy based on solution viscosity perturbation allowed us to study the energetics of amide-substrates, p-aminobenzamidine (p-ABZ) and proflavin binding to the catalytic site of two proteolyzed forms of alpha-thrombin, i.e.", "entity1": "alpha-thrombin", "entity2": "p-aminobenzamidine", "span1": [221, 235], "span2": [122, 140]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"399": {"label": 2, "data": {"text": "Indomethacin abolished the inhibitory effect of acetazolamide on CA I and CA II.", "entity1": "CA II", "entity2": "Indomethacin", "span1": [74, 79], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10106": {"label": 8, "data": {"text": "In addition, we also showed that the elevation in alanine levels and the inhibition of alanine transaminase in the brain are retained after 14 days of PLZ treatment, and that PLZ produces a marked increase in extracellular levels of alanine.", "entity1": "alanine transaminase", "entity2": "alanine", "span1": [87, 107], "span2": [50, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11297": {"label": 2, "data": {"text": "The protein exhibited modest H(2)O(2)-dependent peroxidase activities with guaiacol, potassium iodide, and 2,2(')-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS).", "entity1": "peroxidase", "entity2": "H(2)O(2)", "span1": [48, 58], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7608": {"label": 5, "data": {"text": "While a number of orally active non-peptide V(2) antagonists (Vaptans); notably, Tolvaptan, Lixivaptan and Satavaptan, are currently in Phase III clinical trials; to date, only the mixed V(2)/V(1a), antagonist Conivaptan (Vaprisol), has been approved by the US FDA for clinical use (by i.v.", "entity1": "V(1a)", "entity2": "Conivaptan", "span1": [192, 197], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12576": {"label": 0, "data": {"text": "This cDNA clone, designated EAA3a, shares a 90% nucleotide identity with the previously reported rat GluR5-2b cDNA splice variant and differed from human GluR5-1d in the amino and carboxy terminal regions.", "entity1": "rat GluR5-2b", "entity2": "nucleotide", "span1": [97, 109], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8203": {"label": 3, "data": {"text": "Synthesis and dual biological effects of hydroxycinnamoyl phenylalanyl/prolyl hydroxamic acid derivatives as tyrosinase inhibitor and antioxidant.", "entity1": "tyrosinase", "entity2": "prolyl hydroxamic acid", "span1": [109, 119], "span2": [71, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15439": {"label": 3, "data": {"text": "Liver AOX activity was reduced by 45% with tungsten and 61% with hydralazine and 81% in AOX-deficient mice relative to controls.", "entity1": "AOX", "entity2": "tungsten", "span1": [6, 9], "span2": [43, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2810": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "iNOS", "entity2": "1400W dihydrochloride", "span1": [208, 212], "span2": [96, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1638": {"label": 3, "data": {"text": "RESULTS: Ethanol given to rats in drinking water decreased the level of p-CREB protein in the nucleus accumbens (-75 %) at the time of exposure to ethanol.", "entity1": "p-CREB", "entity2": "Ethanol", "span1": [72, 78], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10369": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-7", "entity2": "omapatrilat", "span1": [64, 71], "span2": [109, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10431": {"label": 0, "data": {"text": "Formation of pyruvate by SDH is a two-step reaction in which the hydroxyl group of serine is cleaved to produce aminoacrylate, and then the aminoacrylate is deaminated by nonenzymatic hydrolysis to produce pyruvate.", "entity1": "SDH", "entity2": "hydroxyl", "span1": [25, 28], "span2": [65, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13520": {"label": 1, "data": {"text": "The unusual {FeNO}7 (S = 1/2) electronic configuration adopted by the substrate-bound iron-nitrosyl CDO (termed {ES-NO}7) is a result of the bidentate thiol/amine coordination of l-cysteine in the NO-bound CDO active site.", "entity1": "CDO", "entity2": "NO", "span1": [206, 209], "span2": [197, 199]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"14987": {"label": 2, "data": {"text": "Furthermore, a mixture of isoflavonoid parent compounds, and a mixture of isoflavonoid metabolites were found to have PPAR\u03b3 activating abilities.", "entity1": "PPAR\u03b3", "entity2": "isoflavonoid", "span1": [118, 123], "span2": [26, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10149": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "estrogen receptor", "entity2": "ICI 164,384", "span1": [110, 127], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10530": {"label": 3, "data": {"text": "The inhibitory effects of metformin on insulin secretion may therefore need to be considered with respect to the use of this drug for the treatment of type 2 diabetes.", "entity1": "insulin", "entity2": "metformin", "span1": [39, 46], "span2": [26, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2525": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "cyt b5", "entity2": "hydroxylamines", "span1": [311, 317], "span2": [44, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5739": {"label": 1, "data": {"text": "These data provided a novel insight to the mechanisms of Rg1protective effects on A\u03b225-35-induced endothelial cells apoptosis, suggesting that GR-ERK signaling pathway might play an important role in it.", "entity1": "ERK", "entity2": "Rg1", "span1": [146, 149], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9911": {"label": 2, "data": {"text": "Impaired expression of the uncoupling protein-3 gene in skeletal muscle during lactation: fibrates and troglitazone reverse lactation-induced downregulation of the uncoupling protein-3 gene.", "entity1": "uncoupling protein-3", "entity2": "troglitazone", "span1": [164, 184], "span2": [103, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11736": {"label": 1, "data": {"text": "These results show that the robust effects of TCDD on the mRNA expression of Snrpn, Peg3 and Igf2r genes in the sperm and of Igf2r in the muscle and liver are unrelated to changes in methylation in their respective genes.", "entity1": "Peg3", "entity2": "TCDD", "span1": [84, 88], "span2": [46, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14033": {"label": 2, "data": {"text": "Here, we report biochemical evidence that mercury alone induces NF-\u03baB activation, resulting in the induced expression of COX-2 and iNOS.", "entity1": "NF-\u03baB", "entity2": "mercury", "span1": [64, 69], "span2": [42, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6515": {"label": 3, "data": {"text": "In conclusion, the renin inhibitor Aliskiren dose-dependently decreases Ang II levels in humans following oral administration.", "entity1": "renin", "entity2": "Aliskiren", "span1": [19, 24], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14098": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "CRBN", "entity2": "lenalidomide", "span1": [121, 125], "span2": [42, 54]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9465": {"label": 1, "data": {"text": "7. 8-Epi-PGF2 alpha showed only weak binding to the IP, TP, FP, EP2 and EP3 receptor at 10 microM concentration.", "entity1": "EP2", "entity2": "7. 8-Epi-PGF2", "span1": [64, 67], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10117": {"label": 3, "data": {"text": "Cyclooxygenase-1 (COX-1) inhibitors (flurbiprofen, ketoprofen and ketrolack) attenuated the nicotine-induced contraction in a concentration-dependent manner, and cyclooxygenase-2 (COX-2) inhibitors at high concentrations (nimesulide and NS-389) slightly attenuated the contraction.", "entity1": "cyclooxygenase-2", "entity2": "nimesulide", "span1": [162, 178], "span2": [222, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5085": {"label": 3, "data": {"text": "FCEO significantly inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) by suppressing the protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, respectively.", "entity1": "cyclooxygenase (COX)-2", "entity2": "prostaglandin E2", "span1": [159, 181], "span2": [51, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4579": {"label": 2, "data": {"text": "Co-treatment of astrocytes with antofine and the intracellular Ca(2+) chelator BAPTA-AM prevented downregulation of Cx43 and inhibition of GJIC.", "entity1": "Cx43", "entity2": "BAPTA-AM", "span1": [116, 120], "span2": [79, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8371": {"label": 9, "data": {"text": "Although there was no change in the levels of insulin receptor (IR), Akt (protein kinase B) and glucose transporter-4 (GLUT4) messenger RNA, BPA significantly decreased the IR, Akt and GLUT4 protein levels (both plasma membrane and cytosolic fraction) of the gastrocnemius muscle.", "entity1": "insulin receptor", "entity2": "BPA", "span1": [46, 62], "span2": [141, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1522": {"label": 1, "data": {"text": "These results suggest that the activation of type 2A serine/threonine protein phosphatases may play a role in the antinociceptive effect of morphine, and that PP1 might counterbalace this activity.", "entity1": "type 2A serine/threonine protein phosphatases", "entity2": "morphine", "span1": [45, 90], "span2": [140, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15343": {"label": 3, "data": {"text": "Coumarin 7-hydroxylation, catalyzed by P450 2A13, was strongly inhibited by 2'-methoxy-5,7-dihydroxyflavone, 2-ethynylnaphthalene, 2'-methoxyflavone, 2-naphththalene propargyl ether, acenaphthene, acenaphthylene, naphthalene, 1-acetylpyrene, flavanone, chrysin, 3-ethynylphenanthrene, flavone, and 7-hydroxyflavone; these chemicals induced Type I spectral changes with low Ks values.", "entity1": "P450 2A13", "entity2": "chrysin", "span1": [39, 48], "span2": [253, 260]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10593": {"label": 1, "data": {"text": "Even though its inability to shift between the trivalent and a divalent oxidation state precludes that gallium behaves as an iron analogue in every respect, it strongly interferes with cellular acquisition of iron from blood by competitive interaction with transferrin and transferrin receptor-mediated endocytosis.", "entity1": "transferrin", "entity2": "gallium", "span1": [257, 268], "span2": [103, 110]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8882": {"label": 2, "data": {"text": "This inhibition was mediated by a TCDD-induced secreted factor which was identified as insulin-like growth factor binding protein 4 (IGFBP-4).", "entity1": "insulin-like growth factor binding protein 4", "entity2": "TCDD", "span1": [87, 131], "span2": [34, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6139": {"label": 1, "data": {"text": "Moreover, the reverse mutation BEAG T432S increased the affinity of BEAG K+ channels for dofetilide, whereas C-type inactivation could not be recovered.", "entity1": "BEAG", "entity2": "dofetilide", "span1": [31, 35], "span2": [89, 99]}, "weak_labels": [-1, -1, 0, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9670": {"label": 1, "data": {"text": "Eosinophils were isolated from peripheral blood, treated with either buffer or 10(-)10 M to 10(-)6 M FP in the presence of 10 pg/ml human recombinant interleukin-5 (rhIL-5) and activated with formyl-met-leu-phe (FMLP) + cytochalasin B (CB).", "entity1": "rhIL-5", "entity2": "CB", "span1": [165, 171], "span2": [236, 238]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11896": {"label": 8, "data": {"text": "Cytochrome P450 epoxygenase 2J2 (CYP2J2) metabolizes arachidonic acids to form epoxyeicosatrienoic acids (EETs), which possess various beneficial effects on the cardiovascular system.", "entity1": "CYP2J2", "entity2": "EETs", "span1": [33, 39], "span2": [106, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9286": {"label": 1, "data": {"text": "Taken together with our previous finding that the desipramine-induced enhancement of aggressive behavior can be blocked by yohimbine, an alpha 2-adrenoceptor antagonist, the present results indicate that not only alpha 2- but also beta 2-adrenoceptor stimulation plays important roles in modulation of aggressive behavior in long-term isolated mice.", "entity1": "beta 2-adrenoceptor", "entity2": "desipramine", "span1": [231, 250], "span2": [50, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, 5, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5541": {"label": 2, "data": {"text": "RESULTS: After treatment with triflusal, there was an increase in NO production by neutrophils and an increase in endothelial nitric oxide synthase (eNOS) protein expression in neutrophils.", "entity1": "eNOS", "entity2": "triflusal", "span1": [149, 153], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"12294": {"label": 1, "data": {"text": "Quercetin supplementation altered expression profiles of several lipid metabolism-related genes, including Fnta, Pon1, Pparg, Aldh1b1, Apoa4, Abcg5, Gpam, Acaca, Cd36, Fdft1, and Fasn, relative to those in HFD control mice.", "entity1": "Pparg", "entity2": "Quercetin", "span1": [119, 124], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9273": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "clozapine", "span1": [166, 186], "span2": [68, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6610": {"label": 3, "data": {"text": "Thus, the current study suggests that coadministration of clinical doses of promethazine and homochlorcyclizine increases the Css of haloperidol and reduced haloperidol via the inhibitory effects on the CYP2D6-catalyzed metabolism of haloperidol and reduced haloperidol.", "entity1": "CYP2D6", "entity2": "homochlorcyclizine", "span1": [203, 209], "span2": [93, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"7731": {"label": 4, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LHRH", "entity2": "leuprorelin", "span1": [39, 43], "span2": [85, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6694": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "TRPM8", "entity2": "icilin", "span1": [0, 5], "span2": [112, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2112": {"label": 1, "data": {"text": "Western blot analysis was used to determine any effect of DEC on the production of COX and inducible nitric-oxide synthase (iNOS) proteins.", "entity1": "nitric-oxide synthase", "entity2": "DEC", "span1": [101, 122], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4275": {"label": 2, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "caspase 3", "entity2": "ursolic acid", "span1": [100, 109], "span2": [121, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"5118": {"label": 3, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "HO-1", "entity2": "NO", "span1": [174, 178], "span2": [60, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1579": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "AChE", "entity2": "4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines", "span1": [26, 30], "span2": [163, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5968": {"label": 5, "data": {"text": "Ambenonium is known to be an inhibitor of acetylcholinesterase, and recent data have shown this drug to antagonize muscarinic receptors as well.", "entity1": "muscarinic receptors", "entity2": "Ambenonium", "span1": [115, 135], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6492": {"label": 5, "data": {"text": "Schild analyses for the antagonists against brimonidine yielded regression lines with slopes of unity and functional antagonist potencies (pK(B)) for BRL44408 (7.8), ARC 239 (5.8) and for prazosin (6.0) suggesting the presence of functional alpha(2A)-adrenoceptors.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "BRL44408", "span1": [241, 264], "span2": [150, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8569": {"label": 4, "data": {"text": "Other dams received 1.8ng/kg/day of a mixture of aryl hydrocarbon receptor (AhR) agonists (non-ortho PCBs, PC-dibenzodioxins and PC-dibenzofurans) without or with 0.5M (0.5MAhR).", "entity1": "aryl hydrocarbon receptor", "entity2": "PC-dibenzofurans", "span1": [49, 74], "span2": [129, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14120": {"label": 3, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "pomalidomide", "span1": [135, 139], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1379": {"label": 9, "data": {"text": "However, DeltahPPAR-alpha was unable to abrogate gemfibrozil-mediated inhibition of iNOS suggesting that gemfibrozil inhibits iNOS independent of PPAR-alpha.", "entity1": "PPAR-alpha", "entity2": "gemfibrozil", "span1": [146, 156], "span2": [105, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12547": {"label": 8, "data": {"text": "From these results, it is proposed that tyrosine hydroxylase activity determines p-HPAA concentrations by regulating p-tyrosine availability.", "entity1": "tyrosine hydroxylase", "entity2": "p-tyrosine", "span1": [40, 60], "span2": [117, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5137": {"label": 3, "data": {"text": "In contrast, zinc protoporphyrin (ZnPP), a specific HO-1 inhibitor, showed a partial suppressive effect of 5HHMF on LPS-induced NO production.", "entity1": "HO-1", "entity2": "ZnPP", "span1": [52, 56], "span2": [34, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11207": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide block erg3, a human brain K(+) channel.", "entity1": "erg3", "entity2": "pimozide", "span1": [54, 58], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10239": {"label": 8, "data": {"text": "During polyamine catabolism, spermine and spermidine are first acetylated by spermidine/spermine N(1)-acetyltransferase (SSAT) and subsequently oxidized by polyamine oxidase (PAO) to produce spermidine and putrescine, respectively.", "entity1": "SSAT", "entity2": "spermine", "span1": [121, 125], "span2": [29, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4575": {"label": 1, "data": {"text": "Antofine-induced connexin43 gap junction disassembly in rat astrocytes involves protein kinase C\u03b2.", "entity1": "connexin43", "entity2": "Antofine", "span1": [17, 27], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1220": {"label": 8, "data": {"text": "Also in contrast to effects of multiple METH injections, 1) MDMA caused little or no decrease in binding of the DAT ligand WIN35428, and 2) neither prevention of hyperthermia nor prior depletion of DA prevented the MDMA-induced reduction in plasmalemmal DA transport.", "entity1": "DAT", "entity2": "DA", "span1": [112, 115], "span2": [254, 256]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14538": {"label": 3, "data": {"text": "In addition, our exploration further revealed that the suppressive action of catalpol on inflammation was mediated via inhibiting nuclear factor-\u03baB (NF-\u03baB) activation.", "entity1": "nuclear factor-\u03baB", "entity2": "catalpol", "span1": [130, 147], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15014": {"label": 1, "data": {"text": "Taken together, these results suggest that SAH/SAHH-mediated transmethylation could be linked to the tumorigenic processes through cross-regulation between the actin cytoskeleton and Src kinase activity.", "entity1": "kinase", "entity2": "SAH", "span1": [187, 193], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3862": {"label": 3, "data": {"text": "HSYA suppressed the expression of TLR-4, Myd88, ICAM-1, TNF\u03b1, IL-1\u03b2 and IL-6 at the mRNA and protein level, and inhibited the adhesion of leukocytes to A549 cells.", "entity1": "IL-1\u03b2", "entity2": "HSYA", "span1": [62, 67], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13974": {"label": 1, "data": {"text": "The altered genes associated with chlorcyclizine-induced cleft palate included Wnt5a, Bmp2, Bmp4, Fgf10, Fgfr2, Msx1, and Insig1 but the magnitude of the change was relatively small (1.5- to 2-fold).", "entity1": "Bmp2", "entity2": "chlorcyclizine", "span1": [86, 90], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6646": {"label": 5, "data": {"text": "However, other alpha(1)-adrenoceptor antagonists (tamsulosin, WB4101 and corynanthine) did not inhibit the binding at a range of concentrations that generally exhibit alpha(1)-adrenoceptor antagonism, and noradrenaline, rauwolscine and propranolol were without effect on the [(3)H]prazosin binding.", "entity1": "alpha(1)-adrenoceptor", "entity2": "tamsulosin", "span1": [15, 36], "span2": [50, 60]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6926": {"label": 9, "data": {"text": "On the other hand, the FUM1 (fumarase) gene disrupted mutant produced significantly higher levels of fumarate but did not form malate at all.", "entity1": "FUM1", "entity2": "malate", "span1": [23, 27], "span2": [127, 133]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"14212": {"label": 6, "data": {"text": "Galantamine is a reversible, competitive acetylcholinesterase (AChE) inhibitor and allosteric potentiating ligand of nicotinic acetylcholine receptors (nAChR-APL) that shares many common structural elements with morphinan-based opioids.", "entity1": "nAChR", "entity2": "Galantamine", "span1": [152, 157], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1]},
	"12030": {"label": 1, "data": {"text": "On the basis of these observations and other findings, we have proposed a scheme which offers a possible explanation for iodide-dependent catalatic activity of thyroid peroxidase and lactoperoxidase.", "entity1": "lactoperoxidase", "entity2": "iodide", "span1": [183, 198], "span2": [121, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7055": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RXRs", "entity2": "tamibarotene", "span1": [88, 92], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14500": {"label": 3, "data": {"text": "Toosendanin induces apoptosis through suppression of JNK signaling pathway in HL-60 cells.", "entity1": "JNK", "entity2": "Toosendanin", "span1": [53, 56], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9403": {"label": 1, "data": {"text": "Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).", "entity1": "RARs", "entity2": "tretinoin", "span1": [189, 193], "span2": [115, 124]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"798": {"label": 1, "data": {"text": "Lithium modulates desensitization of the glutamate receptor subtype gluR3 in Xenopus oocytes.", "entity1": "gluR3", "entity2": "Lithium", "span1": [68, 73], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8388": {"label": 3, "data": {"text": "Acute intoxication with Cd was also followed by significantly decreased activity of the antioxidant defence system (superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR), glutathione (GSH), and glutathione-S-transferase (GST)).", "entity1": "superoxide dismutase", "entity2": "Cd", "span1": [116, 136], "span2": [24, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15187": {"label": 3, "data": {"text": "Moreover, compared with the model group, sophocarpine could significantly increase P-AMPK\u03b1 (>5.82-fold), AMPK\u03b1 (>1.29-fold) and ACC (>3.27-fold) protein expressions, and reduce P-ACC (<0.30-fold) and HNF-4\u03b1 (<0.20-fold) protein expression.", "entity1": "HNF-4\u03b1", "entity2": "sophocarpine", "span1": [200, 206], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10004": {"label": 0, "data": {"text": "This mutation is the first described in exon 9 and impairs the last 27 amino acids of the hormone-binding domain.", "entity1": "hormone-binding domain", "entity2": "amino acids", "span1": [90, 112], "span2": [71, 82]}, "weak_labels": [0, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13400": {"label": 2, "data": {"text": "Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration.", "entity1": "AMP-activated protein kinase", "entity2": "Metformin", "span1": [34, 62], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9927": {"label": 1, "data": {"text": "Line shape broadening resulting from spin-spin coupling of nitroxide pairs introduced into the membrane-binding helices of PGHS-2 was used to calculate the inter-helical distances and changes in these distances that occur in response to binding various ligands.", "entity1": "PGHS-2", "entity2": "nitroxide", "span1": [123, 129], "span2": [59, 68]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1106": {"label": 1, "data": {"text": "In view of the role of CA in acid-base balance as well as the fact that an increase or decrease in its activity is accompanied by an increase or decrease in intra- and extracellular pH, our results suggest that: firstly, CA activation induced by indomethacin might cause changes in COX activity; secondly, PGs are synthetized as a consequence of the changes in COX activity, a hypothesis that requires further study.", "entity1": "COX", "entity2": "indomethacin", "span1": [361, 364], "span2": [246, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"615": {"label": 2, "data": {"text": "Phospholipase A2 inhibitors p-bromophenacyl bromide and arachidonyl trifluoromethyl ketone suppressed interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "Phospholipase A2", "entity2": "p-bromophenacyl bromide", "span1": [0, 16], "span2": [28, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1758": {"label": 3, "data": {"text": "Inhibition of p95ErbB2, p185ErbB2, and EGFR phosphorylation by GW572016 resulted in the inhibition of downstream phospho-Erk1/2, phospho-AKT, and cyclin D steady-state protein levels.", "entity1": "p95ErbB2", "entity2": "GW572016", "span1": [14, 22], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13293": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "receptor tyrosine kinases", "entity2": "Nexavar", "span1": [168, 193], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"407": {"label": 3, "data": {"text": "Previous studies by this research team proved that vasodilating prostaglandins (PGs) E1, E2 and I2 inhibit carbonic anhydrase (CA) in vitro and in vivo, which suggested involvement of CA in gastric acid secretion inhibition and the increase of gastric mucosa blood flow produced by this group of PGs.", "entity1": "carbonic anhydrase", "entity2": "PGs", "span1": [107, 125], "span2": [80, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11954": {"label": 8, "data": {"text": "UGT1A6 exhibited a significantly higher Vmax and Km values toward both HFC and UDP-glucuronic acid than the other UGTs.", "entity1": "UGT1A6", "entity2": "UDP", "span1": [0, 6], "span2": [79, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12903": {"label": 3, "data": {"text": "CO treatment also inhibited LPS-induced NO production and iNOS expression via its inactivation of NF-kappaB.", "entity1": "NF-kappaB", "entity2": "CO", "span1": [98, 107], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5040": {"label": 3, "data": {"text": "New classes of pyrrole-derived nitrooxyalkyl inverse esters, carbonates, and ethers (7-10) as COX-2 selective inhibitors and NO donors were synthesized and are herein reported.", "entity1": "COX-2", "entity2": "nitrooxyalkyl", "span1": [94, 99], "span2": [31, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2355": {"label": 3, "data": {"text": "Thus, sorafenib may inhibit tumor growth by a dual mechanism, acting either directly on the tumor (through inhibition of Raf and Kit signaling) and/or on tumor angiogenesis (through inhibition of VEGFR and PDGFR signaling).", "entity1": "Raf", "entity2": "sorafenib", "span1": [121, 124], "span2": [6, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6271": {"label": 3, "data": {"text": "In both vascular preparations, candesartan caused a marked decrease in the maximal contractile response of the angiotensin II (Ang II) concentration-response curve.", "entity1": "Ang II", "entity2": "candesartan", "span1": [127, 133], "span2": [31, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1904": {"label": 3, "data": {"text": "5-FU interferes with DNA synthesis by blocking thymidylate synthase (TS) but is inactivated by dihydropyrimidine dehydrogenase (DPD).", "entity1": "TS", "entity2": "5-FU", "span1": [69, 71], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12785": {"label": 1, "data": {"text": "Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity.", "entity1": "cyclooxygenase-2", "entity2": "Valdecoxib", "span1": [26, 42], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6364": {"label": 1, "data": {"text": "Lofentanil exhibited full agonism for enhancement of [35S]GTPgammaS binding to human recombinant ORL1 receptors (EC(50) 50 nM).", "entity1": "ORL1", "entity2": "[35S]GTPgammaS", "span1": [97, 101], "span2": [53, 67]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"761": {"label": 3, "data": {"text": "This hypothesis was tested by investigating whether, in subjects with essential hypertension, the natriuretic response to specific renin-angiotensin-aldosterone system (RAAS) blockade by renin-inhibitor remikiren could be predicted from pretreatment renal vascular tone.", "entity1": "angiotensin", "entity2": "remikiren", "span1": [137, 148], "span2": [203, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11705": {"label": 3, "data": {"text": "When further examined for its anticancer mechanism, SB365 effectively suppressed the AKT/mTOR pathway both in vitro and in vivo.", "entity1": "AKT", "entity2": "SB365", "span1": [85, 88], "span2": [52, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15278": {"label": 1, "data": {"text": "Aryl sulfonamide antagonists bind to CCR4 at an intracellular allosteric site denoted site II.", "entity1": "CCR4", "entity2": "Aryl sulfonamide", "span1": [37, 41], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, 6, -1, -1, -1, -1, -1, -1, 9]},
	"8084": {"label": 1, "data": {"text": "E235-mediated induction of senescence was not dependent on p21 or p53; however, p21 conferred protection against the growth inhibitory effects of E235.", "entity1": "p21", "entity2": "E235", "span1": [80, 83], "span2": [146, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4099": {"label": 3, "data": {"text": "Furthermore, treatment with spironoclactone not only attenuated the pro-apoptotic effect of ALD but reversed the ALD-induced increase of calpain and AIF levels.", "entity1": "calpain", "entity2": "spironoclactone", "span1": [137, 144], "span2": [28, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14402": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile", "span1": [254, 258], "span2": [61, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2032": {"label": 7, "data": {"text": "The activation appears to be due to an increase of GAD affinity for its cofactor, pyridoxal phosphate (PLP).", "entity1": "GAD", "entity2": "pyridoxal phosphate", "span1": [51, 54], "span2": [82, 101]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"7785": {"label": 3, "data": {"text": "Since PARP-1 is supposed to be part of a multimeric repressor of sodium iodide symporter (NIS) expression, in this study the effect of the PARP inhibitor PJ34 on several properties of thyroid cancer cell lines was investigated.", "entity1": "PARP", "entity2": "PJ34", "span1": [139, 143], "span2": [154, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3313": {"label": 1, "data": {"text": "The main findings from this study were as follows: 1) cTnC mutants demonstrated distinct functional phenotypes reminiscent of bona fide HCM, RCM, and DCM mutations; 2) a region in cTnC associated with increased Ca(2+) sensitivity in skinned fibers was identified; and 3) the F27W reporter mutation affected Ca(2+) sensitivity, maximal force, and ATPase activation of some mutants.", "entity1": "cTnC", "entity2": "Ca(2+)", "span1": [180, 184], "span2": [307, 313]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10463": {"label": 3, "data": {"text": "Blocking EGFR signaling with the EGFR/HER-2 kinase inhibitor (KI) GW572016 decreased the postradiation survival of irradiated Ras-transformed cells and normal cells but had no effect on the survival of unirradiated cells.", "entity1": "EGFR", "entity2": "GW572016", "span1": [33, 37], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"951": {"label": 1, "data": {"text": "On the basis of data obtained in rabbits, the imidazoline receptor ligand rilmenidine has been suggested to decrease blood pressure in humans by activating central alpha(2A)-adrenoceptors.", "entity1": "imidazoline receptor", "entity2": "rilmenidine", "span1": [46, 66], "span2": [74, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13417": {"label": 8, "data": {"text": "Furthermore, the enzymatic activity of alanine aminotransferase (ALT), which converts the critical gluconeogenic amino acid alanine into pyruvate, is decreased (approximately 50%) in KLF15-/- hepatocytes.", "entity1": "alanine aminotransferase", "entity2": "pyruvate", "span1": [39, 63], "span2": [137, 145]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 9]},
	"6917": {"label": 0, "data": {"text": "The two active sites of dimeric 5-aminolevulinate synthase (ALAS), a pyridoxal 5'-phosphate (PLP)-dependent enzyme, are located on the subunit interface with contribution of essential amino acids from each subunit.", "entity1": "5-aminolevulinate synthase", "entity2": "amino acids", "span1": [32, 58], "span2": [184, 195]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15821": {"label": 5, "data": {"text": "A series of structurally novel aryl ureas was derived from optimization of the HTS lead as selective histamine H3 receptor (H3R) antagonists.", "entity1": "histamine H3 receptor", "entity2": "aryl ureas", "span1": [101, 122], "span2": [31, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5972": {"label": 0, "data": {"text": "Phenol oxidase inhibitors such as phenylthiourea, potassium cyanide, and sodium azide inhibited the reaction drastically, suggesting the participation of the active site copper of the enzyme in the catalysis.", "entity1": "Phenol oxidase", "entity2": "copper", "span1": [0, 14], "span2": [170, 176]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11501": {"label": 8, "data": {"text": "The starting point for the calculations is the recent X-ray crystal structure of GNMT complexed with SAM and acetate.", "entity1": "GNMT", "entity2": "SAM", "span1": [81, 85], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12550": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "TC", "entity2": "CN-Cbl", "span1": [228, 230], "span2": [176, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6448": {"label": 2, "data": {"text": "Clenbuterol caused significant increases in both NGF mRNA and protein in 3T3 cells; with maxima at 10 nM and at 8-12 h exposure.", "entity1": "NGF", "entity2": "Clenbuterol", "span1": [49, 52], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12145": {"label": 2, "data": {"text": "BACKGROUND: The novel antiepileptic drug retigabine is the first selective M-current potassium channel opener for KCNQ2/3 and KCNQ3/5 channels.", "entity1": "KCNQ3/5", "entity2": "retigabine", "span1": [126, 133], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6137": {"label": 0, "data": {"text": "Thus, the serine in position HERG 620 may participate directly in dofetilide binding; however, an intact C-type inactivation process seems to be crucial for high-affinity drug binding.", "entity1": "HERG", "entity2": "serine", "span1": [29, 33], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15997": {"label": 2, "data": {"text": "Puerarin stimulates proliferation and differentiation and protects against cell death in human osteoblastic MG-63 cells via ER-dependent MEK/ERK and PI3K/Akt activation.", "entity1": "MEK", "entity2": "Puerarin", "span1": [137, 140], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10064": {"label": 3, "data": {"text": "Like conventional ACE inhibitors, omapatrilat causes extracellular volume reduction and vasodilatation; moreover, it increases levels of atrial and brain natriuretic peptides and bradykinin.", "entity1": "ACE", "entity2": "omapatrilat", "span1": [18, 21], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15282": {"label": 1, "data": {"text": "Mice given daily injections of high dose JZL184 (\u226516 mg/kg) for six days displayed decreased CB(1) receptor density and function in brain, as assessed in [(3)H]SR141716A binding and CP55,940-stimulated [(35)S]GTP\u03b3S binding assays, respectively.", "entity1": "CB(1)", "entity2": "[(3)H]SR141716A", "span1": [93, 98], "span2": [154, 169]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14725": {"label": 4, "data": {"text": "The introduction of the amino group resulted in not only improved water solubility but also enhanced TLR7 agonistic activity.", "entity1": "TLR7", "entity2": "amino", "span1": [101, 105], "span2": [24, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12934": {"label": 8, "data": {"text": "Moreover, NO production in LPS-stimulated macrophages that are expressing CSE mRNA was significantly reduced by the addition of L-Cys, a substrate for H(2)S, but enhanced by the selective CSE inhibitor beta-cyano-L-alanine but not by the CBS inhibitor aminooxyacetic acid.", "entity1": "CSE", "entity2": "L-Cys", "span1": [74, 77], "span2": [128, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, 8, -1, 9]},
	"14156": {"label": 4, "data": {"text": "CONCLUSIONS AND IMPLICATIONS: In different cell systems, mianserin directly activates kappa-opioid receptors, displaying partial agonist activity at brain receptors.", "entity1": "kappa-opioid receptors", "entity2": "mianserin", "span1": [86, 108], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2523": {"label": 8, "data": {"text": "On the basis of our findings with structurally similar arylhydroxylamine metabolites of therapeutic drugs, we hypothesized that the reductive detoxification of arylhydroxylamine carcinogens was catalyzed by NADH cytochrome b5 reductase (b5R) and cytochrome b5 (cyt b5).", "entity1": "cyt b5", "entity2": "arylhydroxylamine", "span1": [261, 267], "span2": [160, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"4461": {"label": 9, "data": {"text": "Promoter and electromobility shift assays showed that transcriptional activation of NF-\u03baB was significantly reduced by catalpol treatment, while AP-1 was not.", "entity1": "AP-1", "entity2": "catalpol", "span1": [145, 149], "span2": [119, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9737": {"label": 1, "data": {"text": "In [(35)S]GTPgammaS binding protocols, yohimbine exerts antagonist actions at halpha(2A)-AR, h5-HT(1B), h5-HT(1D), and hD(2) sites, yet partial agonist actions at h5-HT(1A) sites.", "entity1": "h5-HT(1B)", "entity2": "(35)S", "span1": [93, 102], "span2": [4, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13886": {"label": 3, "data": {"text": "These findings support that PPARgamma plays an essential role in mediating the RhoA-inhibiting effect of ibuprofen.", "entity1": "RhoA", "entity2": "ibuprofen", "span1": [79, 83], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2603": {"label": 0, "data": {"text": "In addition to the N-terminal and Src homology 2 domains that mediate these interactions, SOCS proteins contain a C-terminal SOCS box.", "entity1": "SOCS box", "entity2": "C", "span1": [125, 133], "span2": [114, 115]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11459": {"label": 8, "data": {"text": "Spermidine/spermine N1-acetyltransferase (SSAT) is a key enzyme in the control of polyamine levels in human cells, as acetylation of spermidine and spermine triggers export or degradation.", "entity1": "Spermidine/spermine N1-acetyltransferase", "entity2": "polyamine", "span1": [0, 40], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7766": {"label": 1, "data": {"text": "Our study determined whether there was a significant dose-dependent correlation between increasing Hg exposure from dental amalgams and GST-\u03b1 and GST-\u03c0 as biomarkers of kidney integrity.", "entity1": "GST-\u03c0", "entity2": "Hg", "span1": [146, 151], "span2": [99, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"241": {"label": 1, "data": {"text": "At the 5-HT2C receptor, both R(-) and S(+)MDA were equipotent at stimulating PI hydrolysis, with the S(+) isomer of MDMA being more efficacious at the 5-HT2C receptor compared with the R(-) isomer.", "entity1": "5-HT2C", "entity2": "R(-) and S(+)MDA", "span1": [7, 13], "span2": [29, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14116": {"label": 3, "data": {"text": "Long-term selection for lenalidomide resistance in H929 myeloma cell lines was accompanied by a reduction in CRBN, while in DF15R myeloma cells resistant to both pomalidomide and lenalidomide, CRBN protein was undetectable.", "entity1": "CRBN", "entity2": "lenalidomide", "span1": [109, 113], "span2": [24, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7939": {"label": 1, "data": {"text": "Structure-activity relationship analysis of highly potent subtype-selective ligands (MT(2) EC(50) 10-90 pM) revealed that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT(2) potency and at the same time decreased MT(1) potency.", "entity1": "MT(2)", "entity2": "benzyloxyl", "span1": [229, 234], "span2": [124, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1223": {"label": 9, "data": {"text": "Tamoxifen does not reduce the incidence of ER-negative cancers, nor does it appear to be effective in preventing the appearance of one third of ER-positive cancers.", "entity1": "ER", "entity2": "Tamoxifen", "span1": [43, 45], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4408": {"label": 2, "data": {"text": "NCFP binds to the CPPHA site on mGlu5 and potentiates mGlu5-mediated responses in both recombinant and native systems.", "entity1": "mGlu5", "entity2": "NCFP", "span1": [54, 59], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15411": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "NPC1L1", "entity2": "stigmasterol", "span1": [202, 208], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"1231": {"label": 3, "data": {"text": "Inhibition of MCP-1 and MIP-2 transcription and translation by mimosine in muscle tissue infected with the parasite Trichinella spiralis.", "entity1": "MIP-2", "entity2": "mimosine", "span1": [24, 29], "span2": [63, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16028": {"label": 2, "data": {"text": "Haloperidol promotes mTORC1-dependent phosphorylation of ribosomal protein S6 via dopamine- and cAMP-regulated phosphoprotein of 32 kDa and inhibition of protein phosphatase-1.", "entity1": "ribosomal protein S6", "entity2": "Haloperidol", "span1": [57, 77], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1149": {"label": 3, "data": {"text": "The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.", "entity1": "tyrosine kinase", "entity2": "Iressa", "span1": [4, 19], "span2": [39, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13315": {"label": 1, "data": {"text": "We conclude that Na(+) movement across mammary epithelia is modulated by corticosteroids via a glucocorticoid receptor-mediated mechanism that regulates the expression of the beta- and gamma-subunits of ENaC.", "entity1": "glucocorticoid receptor", "entity2": "Na(+)", "span1": [95, 118], "span2": [17, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10740": {"label": 3, "data": {"text": "The compounds 5'-azacytidine (AZC) and procainamide (PCA) belong to inhibitors of DNMT1, whose low activity correlates with increase in transcription of various genes.", "entity1": "DNMT1", "entity2": "5'-azacytidine", "span1": [82, 87], "span2": [14, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1755": {"label": 3, "data": {"text": "GW572016, a reversible small molecule inhibitor of EGFR and ErbB2 tyrosine kinases, inhibits baseline p95ErbB2 phosphorylation in BT474 cells and tumor xenografts.", "entity1": "ErbB2", "entity2": "GW572016", "span1": [60, 65], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2428": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "arginase I", "entity2": "L-arginine", "span1": [219, 229], "span2": [128, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"5261": {"label": 3, "data": {"text": "Synthesis and antitumor activity of 1,3,4-oxadiazole possessing 1,4-benzodioxan moiety as a novel class of potent methionine aminopeptidase type II inhibitors.", "entity1": "methionine aminopeptidase type II", "entity2": "1,3,4-oxadiazole", "span1": [114, 147], "span2": [36, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5727": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "bile acid", "span1": [83, 86], "span2": [121, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1028": {"label": 9, "data": {"text": "High p53 protein levels, but not genetic or functional p53 status, were associated with increased topotecan-induced DNA/topoisomerase I complex formation.", "entity1": "p53", "entity2": "topotecan", "span1": [55, 58], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13296": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "vascular endothelial growth factor receptor", "entity2": "Nexavar", "span1": [255, 298], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7930": {"label": 2, "data": {"text": "Altogether, our results suggest that a high dose of glucosamine may inhibit cell proliferation through apoptosis and disturb cell cycle progression with a halt at G(0)/G(1) phase, and that this occurs, at least in part, by a reduction in Rb phosphorylation together with modulation of p21, p53 and HO-1 expression, and nuclear p21 accumulation.", "entity1": "p21", "entity2": "glucosamine", "span1": [327, 330], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1241": {"label": 3, "data": {"text": "Amrinone and milrinone, selective PDE3 inhibitors, suppressed TNF secretion to a lesser extent.", "entity1": "TNF", "entity2": "milrinone", "span1": [62, 65], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10282": {"label": 2, "data": {"text": "Rasagiline prevented the PT in mitochondria directly and also indirectly through induction of antiapoptotic Bcl-2 and a neurotrophic factor, glial cell line-derived neurotrophic factor (GDNF).", "entity1": "neurotrophic factor", "entity2": "Rasagiline", "span1": [120, 139], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12671": {"label": 8, "data": {"text": "In conclusion, OMCD tubules from deoxycorticosterone pivalate-treated rats secrete Cl- into the luminal fluid through NKCC1-mediated Cl- uptake across the basolateral membrane in series with Cl- efflux across the apical membrane.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [118, 123], "span2": [191, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"289": {"label": 0, "data": {"text": "Investigation of a site-specific mutant of CA V containing the replacement Tyr64-->His showed that the unique kinetic properties of CA V are not due to the presence of tyrosine at position 64.", "entity1": "CA V", "entity2": "His", "span1": [43, 47], "span2": [83, 86]}, "weak_labels": [-1, 0, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1338": {"label": 4, "data": {"text": "Dexamethasone (DEX), betamethasone (BM), and their esterified-derivatives had full transrepression agonistic activity in a reporter assay using CV-1 cells transfected with either human or rat GR.", "entity1": "human or rat GR", "entity2": "Dexamethasone", "span1": [179, 194], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1351": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "DAT", "entity2": "aryl", "span1": [317, 320], "span2": [139, 143]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14544": {"label": 3, "data": {"text": "Protein tyrosine phosphatase 1B inhibitory effect by dammarane-type triterpenes from hydrolyzate of total Gynostemma pentaphyllum saponins.", "entity1": "Protein tyrosine phosphatase 1B", "entity2": "triterpenes", "span1": [0, 31], "span2": [68, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10822": {"label": 3, "data": {"text": "Carvedilol prevents cardiac hypertrophy and overexpression of hypoxia-inducible factor-1alpha and vascular endothelial growth factor in pressure-overloaded rat heart.", "entity1": "hypoxia-inducible factor-1alpha", "entity2": "Carvedilol", "span1": [62, 93], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6388": {"label": 1, "data": {"text": "The selective alpha(2)-adrenoceptor ligand rauwolscine antagonized acidification rate changes with an affinity independent of the agonist used; the affinity (mean pK(B)) against noradrenaline was 8.43.", "entity1": "alpha(2)-adrenoceptor", "entity2": "rauwolscine", "span1": [14, 35], "span2": [43, 54]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1630": {"label": 1, "data": {"text": "AIM: To study the changes in the expression and phosphorylation of cAMP response element binding protein (CREB) in the rat nucleus accumbens after chronic ethanol intake and its withdrawal.", "entity1": "cAMP response element binding protein", "entity2": "ethanol", "span1": [67, 104], "span2": [155, 162]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15979": {"label": 5, "data": {"text": "We have recently reported that a mono-hydroxylated metabolite of the synthetic aminoalkylindole cannabinoid JHW-073 (3) exhibits neutral antagonist activity at CB1Rs and thus may serve as a promising lead for the development of novel alcohol abuse therapies.", "entity1": "CB1Rs", "entity2": "JHW-073", "span1": [160, 165], "span2": [108, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14699": {"label": 9, "data": {"text": "Proteins Aus1 and Dan1 were not found to be involved in steroid import.", "entity1": "Dan1", "entity2": "steroid", "span1": [18, 22], "span2": [56, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6259": {"label": 1, "data": {"text": "At the human dopamine transporter, only pimozide (K(D) = 69+/-3) ziprasidone (K(D) = 76+/-5) had notable potency.", "entity1": "human dopamine transporter", "entity2": "ziprasidone", "span1": [7, 33], "span2": [65, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"14632": {"label": 8, "data": {"text": "All four DCK proteins yielded comparable metabolic activity for Ara-C and dFdC monophosphorylation, except for DCK24Val, which demonstrated an approximately 2-fold increase (P < 0.05) in the intrinsic clearance of dFdC monophosphorylation due to a 40% decrease in K(m) (P < 0.05).", "entity1": "DCK", "entity2": "dFdC", "span1": [111, 114], "span2": [214, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10559": {"label": 3, "data": {"text": "[3H]DMI trapped in membranes was displaceable by the structurally unrelated NET inhibitor, nisoxetine, in a concentration-dependent manner, implying interaction of retained [3H]DMI with the NET.", "entity1": "NET", "entity2": "nisoxetine", "span1": [76, 79], "span2": [91, 101]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3927": {"label": 2, "data": {"text": "OMT showed partial protection in the cortical neurons via down-regulation of NR2B containing NMDA receptors and up-regulation of Bcl-2 family.", "entity1": "Bcl-2", "entity2": "OMT", "span1": [129, 134], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13915": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "Kir6.1", "entity2": "Phenformin", "span1": [166, 172], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14757": {"label": 1, "data": {"text": "These data suggest that jaceosidin, isolated from Japanese mugwort, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells.", "entity1": "ATM", "entity2": "jaceosidin", "span1": [86, 89], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14307": {"label": 1, "data": {"text": "Claudin-3 and claudin-4 regulate sensitivity to cisplatin by controlling expression of the copper and cisplatin influx transporter CTR1.", "entity1": "claudin-4", "entity2": "cisplatin", "span1": [14, 23], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2386": {"label": 3, "data": {"text": "Sorafenib inhibited the kinase activity of both C-RAF and B-RAF (wild type and V600E mutant).", "entity1": "C-RAF", "entity2": "Sorafenib", "span1": [48, 53], "span2": [0, 9]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15": {"label": 3, "data": {"text": "These results suggest that prostacyclin may play a role in downregulating tissue factor expression in monocytes, at least in part via elevation of intracellular levels of cyclic AMP.", "entity1": "tissue factor", "entity2": "prostacyclin", "span1": [74, 87], "span2": [27, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8653": {"label": 6, "data": {"text": "Conversely, ovarian PRA and PRB were positively regulated by ethanol and ethanol-melatonin combination, whereas PRA was down-regulated in the uterus and oviduct after ethanol consumption.", "entity1": "PRB", "entity2": "ethanol", "span1": [28, 31], "span2": [73, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3960": {"label": 2, "data": {"text": "Although Bak and Bcl-2-associated X protein (Bax), another member of the Bcl-2 family, are generally thought to be functionally redundant, only Bak is necessary and sufficient for VK2-induced cytochrome c (cyt c) release and cell death.", "entity1": "cytochrome c", "entity2": "VK2", "span1": [192, 204], "span2": [180, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13085": {"label": 1, "data": {"text": "Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach.", "entity1": "peroxisome proliferator-activated receptor gamma", "entity2": "Sulfonylureas", "span1": [35, 83], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11446": {"label": 1, "data": {"text": "DAT occupancy was determined by displacement of 8-(2-[(18)F]fluroethyl)2beta-carbomethoxy-3beta-(4-chlorophenyl)nortropane (FECNT).", "entity1": "DAT", "entity2": "8-(2-[(18)F]fluroethyl)2beta-carbomethoxy-3beta-(4-chlorophenyl)nortropane", "span1": [0, 3], "span2": [48, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1652": {"label": 5, "data": {"text": "The 5-HT(2B/2C)-receptor antagonist SB 206553 facilitated hyperglycemia induced by clomipramine, although the 5-HT(2A)-receptor antagonist ketanserin was without effect.", "entity1": "5-HT(2A)", "entity2": "ketanserin", "span1": [110, 118], "span2": [139, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3692": {"label": 3, "data": {"text": "Insulin secretion stimulated by both 200 \u03bcM tolbutamide and 20 \u03bcM gliclazide, concentrations that had equivalent effects on membrane potential, was inhibited by thapsigargin (1 \u03bcM) or the L-type Ca(2+) channel blocker nicardipine (2 \u03bcM) and was potentiated by 8-pCPT-2'-O-Me-cAMP-AM at concentrations \u22652 \u03bcM in INS-1 cells.", "entity1": "Insulin", "entity2": "thapsigargin", "span1": [0, 7], "span2": [161, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10774": {"label": 2, "data": {"text": "Together, these results suggested that imatinib affects EGFR activation and signaling pathways through rapid release and increased expression of endogenous EGFR-activating ligands.", "entity1": "EGFR", "entity2": "imatinib", "span1": [156, 160], "span2": [39, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6680": {"label": 4, "data": {"text": "or were chronically pretreated with the selective beta(2)-adrenoceptor agonist salbutamol (40 microg/kg/h) for 1 week to induce beta(2)-adrenoceptor desensitization.", "entity1": "beta(2)-adrenoceptor", "entity2": "salbutamol", "span1": [50, 70], "span2": [79, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4561": {"label": 3, "data": {"text": "In addition, ethanol induced degradation of DNA methyltransferases (DNMT-1, DNMT-3a, and DNMT-3b), as well as the methyl CpG-binding proteins (MeCP-2, MBD-2 and MBD-3), in MEF cells by the proteasomal pathway.", "entity1": "MeCP-2", "entity2": "ethanol", "span1": [143, 149], "span2": [13, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13040": {"label": 2, "data": {"text": "The retinoic acid-induced elevated expression of CD1d is coupled to enhanced iNKT cell activation.", "entity1": "CD1d", "entity2": "retinoic acid", "span1": [49, 53], "span2": [4, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1719": {"label": 2, "data": {"text": "Thus, it can be suggested that the inhibitory action of ginseng saponins against the immobilization stress-induced increase of plasma IL-6 level would be in periphery; at least in part, mediated by blocking norepinephrine- and/or epinephrine-induced increase of IL-6 level in macrophage rather than in the brain.", "entity1": "IL-6", "entity2": "epinephrine", "span1": [262, 266], "span2": [230, 241]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2147": {"label": 3, "data": {"text": "From these results, it is suggested that troglitazone may enhance the vasodilatory effect of adenosine by inhibiting ENT1.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [117, 121], "span2": [41, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9803": {"label": 3, "data": {"text": "Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid.", "entity1": "human and rat dihydroorotate dehydrogenase", "entity2": "lawsone", "span1": [26, 68], "span2": [84, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11804": {"label": 1, "data": {"text": "Results of studies to evaluate the effect of Mn and DA on cell viability in control and DAT-transfected HEK cells reveal that Mn is equally toxic to both cell lines whereas DA was only toxic to cells containing DAT.", "entity1": "DAT", "entity2": "Mn", "span1": [211, 214], "span2": [126, 128]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4024": {"label": 0, "data": {"text": "RESULTS: In an animal study with (129)I-labeled EPO in Han-Wistar rats, an increase of (129)I-EPO is observed after dose administration.", "entity1": "EPO", "entity2": "(129)I", "span1": [48, 51], "span2": [33, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15087": {"label": 1, "data": {"text": "Potential future roles for ceftazidime-avibactam include the treatment of suspected or documented infections caused by resistant Gram-negative-bacilli producing extended-spectrum \u00df-lactamase (ESBL), Klebsiella pneumoniae carbapenemases (KPCs) and/or AmpC \u00df-lactamases.", "entity1": "AmpC \u00df-lactamases", "entity2": "avibactam", "span1": [250, 267], "span2": [39, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6339": {"label": 5, "data": {"text": "The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174).", "entity1": "AT1", "entity2": "saprisartan", "span1": [25, 28], "span2": [185, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15968": {"label": 1, "data": {"text": "We recently showed that the first domain of human CCS (hCCSD1) is responsible for copper transfer to its protein partner, human SOD1 (hSOD1).", "entity1": "human SOD1", "entity2": "copper", "span1": [122, 132], "span2": [82, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2197": {"label": 2, "data": {"text": "Expression of L-type pyruvate kinase (L-PK) is upregulated in the liver by dietary carbohydrate.", "entity1": "L-PK", "entity2": "carbohydrate", "span1": [38, 42], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11632": {"label": 0, "data": {"text": "This short AdSS has two large deletions that map to the middle and C-terminus of the protein.", "entity1": "AdSS", "entity2": "C", "span1": [11, 15], "span2": [67, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12044": {"label": 1, "data": {"text": "Carrier-free radioiodinated [125I]IAS was used to photolabel epitope-tagged human beta 2AR in membranes prepared from stably transfected HEK 293 cells.", "entity1": "human beta 2AR", "entity2": "[125I]IAS", "span1": [76, 90], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12094": {"label": 1, "data": {"text": "SB 200646, which demonstrates some selectivity for 5-HT receptors in rat stomach fundus, should provide a useful ligand for confirmation of this view and allow discrimination of 5-HT2B function both in vitro and in vivo.", "entity1": "5-HT receptors", "entity2": "SB 200646", "span1": [51, 65], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7209": {"label": 2, "data": {"text": "In conclusion, our results indicate that Cd increases BC cell proliferation in vitro by stimulating Akt, ERK1/2 and PDGFRalpha kinases activity likely by activating c-fos, c-jun and PDGFA by an ERalpha-dependent mechanism.", "entity1": "PDGFRalpha", "entity2": "Cd", "span1": [116, 126], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12900": {"label": 3, "data": {"text": "Pretreatment with H(2)S or NaHS significantly inhibited LPS-induced iNOS expression and NO production.", "entity1": "iNOS", "entity2": "H(2)S", "span1": [68, 72], "span2": [18, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14646": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Lys27Gln", "entity2": "cytarabine", "span1": [39, 47], "span2": [210, 220]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7474": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "Kainate-selective ionotropic glutamate receptors", "entity2": "Na+", "span1": [0, 48], "span2": [74, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10213": {"label": 1, "data": {"text": "The increase in AMPK alpha2 activity was likely due to a change in muscle energy status because ATP and phosphocreatine concentrations were lower after metformin treatment.", "entity1": "AMPK alpha2", "entity2": "phosphocreatine", "span1": [16, 27], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"457": {"label": 5, "data": {"text": "Pretreatment with tropisetron (1 microM), a 5-HT3 antagonist, ketanserin (10 microM), a 5-HT2 antagonist, thioperamide (10 microM), a histamine H3 antagonist, or phentolamine (10 microM), an alpha-adrenergic antagonist, however, had no effect.", "entity1": "histamine H3", "entity2": "thioperamide", "span1": [134, 146], "span2": [106, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11994": {"label": 3, "data": {"text": "Anti-inflammatory effect of prunetin via the suppression of NF-\u03baB pathway.", "entity1": "NF-\u03baB", "entity2": "prunetin", "span1": [60, 65], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2271": {"label": 8, "data": {"text": "Astrocytes may play a role in these manifestations because astrocytes are essential in the regulation of released glutamate and its conversion to glutamine through the enzyme glutamine synthetase (GS).", "entity1": "GS", "entity2": "glutamate", "span1": [197, 199], "span2": [114, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4320": {"label": 2, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "CIP1", "entity2": "Pinosylvin", "span1": [291, 295], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1529": {"label": 3, "data": {"text": "The beta subunit has been cloned and shown to lower the K(m) of methionine adenosyltransferase II alpha2 (the MAT2A product) for methionine and to render the enzyme more susceptible to S-adenosylmethionine inhibition.", "entity1": "methionine adenosyltransferase II alpha2", "entity2": "S-adenosylmethionine", "span1": [64, 104], "span2": [185, 205]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"727": {"label": 9, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "rat ACE", "entity2": "losartan", "span1": [171, 178], "span2": [95, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10386": {"label": 1, "data": {"text": "Experimental evidence from the use of agents with enhanced selectivity for BuChE (cymserine analogues, MF-8622) and the dual inhibitor of both AChE and BuChE, rivastigmine, indicates potential therapeutic benefits of inhibiting both AChE and BuChE in AD and related dementias.", "entity1": "BuChE", "entity2": "cymserine", "span1": [75, 80], "span2": [82, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12731": {"label": 1, "data": {"text": "A low toxicity maintenance regime, using eicosapentaenoic acid and readily available drugs, for mantle cell lymphoma and other malignancies with excess cyclin D1 levels.", "entity1": "cyclin D1", "entity2": "eicosapentaenoic acid", "span1": [152, 161], "span2": [41, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3405": {"label": 3, "data": {"text": "Pseudoephedrine inhibits T-cell activation by targeting NF-kappaB, NFAT and AP-1 signaling pathways.", "entity1": "NF-kappaB", "entity2": "Pseudoephedrine", "span1": [56, 65], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15586": {"label": 1, "data": {"text": "A series of N-substituted lobelane analogues was synthesized and evaluated for their [(3)H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [(3)H]dopamine uptake.", "entity1": "vesicular monoamine transporter", "entity2": "[(3)H]dihydrotetrabenazine", "span1": [136, 167], "span2": [85, 111]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7669": {"label": 3, "data": {"text": "Some of these structurally related compounds have a very different behavior against the widespread isozyme CA II, with chlorthalidone, trichloromethiazide, and furosemide being efficient inhibitors against CA II (K(I)s of 65-138 nM), whereas indapamide is a much weaker one (K(I) of 2520 nM).", "entity1": "CA II", "entity2": "furosemide", "span1": [206, 211], "span2": [160, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7401": {"label": 1, "data": {"text": "Ca2+ activation targets the PKCalpha C2 domain to the plasma membrane and the cPLA2alpha C2 domain to the internal membranes, with no detectable spatial overlap.", "entity1": "cPLA2alpha C2 domain", "entity2": "Ca2+", "span1": [78, 98], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12175": {"label": 1, "data": {"text": "Vitamin E supplementation alters HDL-cholesterol concentration and paraoxonase activity in rabbits fed high-cholesterol diet: comparison with probucol.", "entity1": "paraoxonase", "entity2": "Vitamin E", "span1": [67, 78], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"504": {"label": 3, "data": {"text": "The results suggest that the 63-kDa (PDE 1B1) and 60-kDa (PDE 1A2) CaMPDE isozymes are inhibited by felodipine and nicardipine by partial competitive inhibition and that these two Ca2+ antagonists appear to counteract each other.", "entity1": "PDE 1A2", "entity2": "felodipine", "span1": [58, 65], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2681": {"label": 9, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "AXL", "entity2": "IM", "span1": [68, 71], "span2": [93, 95]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6123": {"label": 8, "data": {"text": "Amezinium is much less potent as a MAO inhibitor in cells with the uptake2 transporter, such as the myocardial cells of the heart.", "entity1": "uptake2 transporter", "entity2": "Amezinium", "span1": [67, 86], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13473": {"label": 8, "data": {"text": "In contrast, the RA catabolising enzymes Cyp26A1 and Cyp26B1 which are known to be RA-responsive were not expressed at all in the developing eye.", "entity1": "Cyp26A1", "entity2": "RA", "span1": [41, 48], "span2": [17, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10507": {"label": 9, "data": {"text": "Resistance to GW572016 was not due to a lack of receptor inhibition, but rather with a lack of inhibition of ERK and Akt, suggesting that measurement of inhibition of crucial signaling pathways may better predict response than inhibition of receptor phosphorylation.", "entity1": "ERK", "entity2": "GW572016", "span1": [109, 112], "span2": [14, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6508": {"label": 2, "data": {"text": "At the same time, mean plasma active renin was increased 16- and 34-fold at the highest dose of Aliskiren.", "entity1": "renin", "entity2": "Aliskiren", "span1": [37, 42], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3621": {"label": 4, "data": {"text": "Direct-acting CB1 agonists, including \u0394(9)-tetrahydrocannabinol, WIN 55,212 [R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate], AM2389 [9\u03b2-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol], and AM4054 [9\u03b2-(hydroxymethyl)-3-(1-adamantyl)-hexahydrocannabinol], produced dose-dependent increases in diuresis and decreases in colonic temperature, with slightly lower ED(50) values for diuresis than for hypothermia.", "entity1": "CB1", "entity2": "R-(1)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate", "span1": [14, 17], "span2": [77, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4162": {"label": 3, "data": {"text": "In addition, the new compound perviridicin B (2), three known rocaglate derivatives (9, 11, 12), and a known sesquiterpene, 2-oxaisodauc-5-en-12-al (17), showed significant NF-\u03baB (p65) inhibitory activity in an ELISA assay.", "entity1": "p65", "entity2": "perviridicin B", "span1": [180, 183], "span2": [30, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5534": {"label": 5, "data": {"text": "Labeling with [(125)I]IAS was blocked by 10 microM (-)-alprenolol and inhibited by addition of GTP gamma S, and [125I]IAS migrated at the same position on an SDS-PAGE gel as the beta 2AR labeled by the antagonist photoaffinity label [125I]iodoazidobenzylpindolol ([125I]IABP).", "entity1": "beta 2AR", "entity2": "[125I]iodoazidobenzylpindolol", "span1": [178, 186], "span2": [233, 262]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8010": {"label": 3, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "FXa", "entity2": "IMG", "span1": [131, 134], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7074": {"label": 1, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "thermoTRPs", "entity2": "menthol", "span1": [152, 162], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5984": {"label": 1, "data": {"text": "Analysis of the results of this paper reveals that normal plasma components, Cl- and fibrinogen, exert major regulatory roles on the ability of [Glu1]Pg to be activated by two-chain rec-t-PA, in in vitro systems.", "entity1": "t-PA", "entity2": "Cl-", "span1": [186, 190], "span2": [77, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5938": {"label": 3, "data": {"text": "Inhibitory effect of synthetic progestins, 4-MA and cyanoketone on human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase activity.", "entity1": "human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase", "entity2": "4-MA", "span1": [67, 139], "span2": [43, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11133": {"label": 9, "data": {"text": "TREK-1 currents are insensitive to pharmacological agents that block TWIK-1 activity such as quinine and quinidine.", "entity1": "TREK-1", "entity2": "quinidine", "span1": [0, 6], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15179": {"label": 1, "data": {"text": "Sophocarpine, an effective compound derived from foxtail-like sophora herb and seed, has been reported that it can alleviate non-alcoholic steatohepatitis (NASH) in rats and affect adipocytokine synthesis.", "entity1": "adipocytokine", "entity2": "Sophocarpine", "span1": [181, 194], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4128": {"label": 1, "data": {"text": "The cellular prion protein PrP(C) consists of two domains--a flexible N-terminal domain, which participates in copper and zinc regulation, and a largely helical C-terminal domain that converts to \u03b2 sheet in the course of prion disease.", "entity1": "prion protein PrP(C)", "entity2": "zinc", "span1": [13, 33], "span2": [122, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7523": {"label": 3, "data": {"text": "With this background, the present study was designed to explore the possible effect of nimesulide (a preferential COX-2 inhibitor) against pentylenetetrazol (PTZ)-induced kindling epilepsy in mice.", "entity1": "COX-2", "entity2": "nimesulide", "span1": [114, 119], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12129": {"label": 1, "data": {"text": "The selective alpha(1)-adrenoceptor ligands prazosin and doxazosin (each 3 microM) had no effect on noradrenaline responses.", "entity1": "alpha(1)-adrenoceptor", "entity2": "doxazosin", "span1": [14, 35], "span2": [57, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4211": {"label": 2, "data": {"text": "In Alexander cells, only when they were transfected with FXR+RXR, GW4064 caused up-regulation of SHP and OST\u03b2, and a down-regulation of CYP27A1.", "entity1": "OST\u03b2", "entity2": "GW4064", "span1": [105, 109], "span2": [66, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4607": {"label": 3, "data": {"text": "Although thioredoxin reductase (TRR) inhibitors (aurothioglucose and Sb(III)) inhibited cytosolic DMAs(V) reduction, recombinant rat TRR plus NADPH, alone or when added to the cytosol, failed to support DMAs(V) reduction.", "entity1": "TRR", "entity2": "aurothioglucose", "span1": [32, 35], "span2": [49, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12706": {"label": 1, "data": {"text": "However, when coapplied with 10 micro m GABA, ivermectin potentiated the GABA-evoked current of the GAB-1/HG1A receptor, but attenuated the GABA response of the GAB-1/HG1E receptor.", "entity1": "HG1A", "entity2": "GABA", "span1": [106, 110], "span2": [73, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3825": {"label": 3, "data": {"text": "While none of the phenethylamides (n = 2) were active, most of the anilides (n = 0) turned out to moderately or strongly inhibit 17\u03b2-HSD2.", "entity1": "17\u03b2-HSD2", "entity2": "anilides", "span1": [129, 137], "span2": [67, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11498": {"label": 3, "data": {"text": "RESULTS: Ketorolac was six times more active against COX-1 (IC(50) = 0.02 microM) than COX-2 (IC(50) = 0.12 microM) while bromfenac was approximately 32 times more active against COX-2 (IC(50) = 0.0066 microM) than COX-1 (IC(50) = 0.210 microM).", "entity1": "COX-2", "entity2": "bromfenac", "span1": [87, 92], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2198": {"label": 2, "data": {"text": "Expression of L-type pyruvate kinase (L-PK) is upregulated in the liver by dietary carbohydrate.", "entity1": "L-type pyruvate kinase", "entity2": "carbohydrate", "span1": [14, 36], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6280": {"label": 3, "data": {"text": "In contrast, the administration of 7.5 and 15 mg of meloxicam caused dose-dependent reductions in monocyte COX-2 activity by 51% and 70%, respectively, and in platelet COX-1 activity by 25% and 35%, respectively.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [107, 112], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5584": {"label": 8, "data": {"text": "PURPOSE: The fluoropyrimidine carbamate (capecitabine) is converted to 5-fluorouracil (5-FU) by thymidine phosphorylase (TP) inside target tissues.", "entity1": "thymidine phosphorylase", "entity2": "5-fluorouracil", "span1": [96, 119], "span2": [71, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"11055": {"label": 9, "data": {"text": "Activation of Atp8a1 is also reduced by these modifications; phosphatidylserine-O-methyl ester, lysophosphatidylserine, glycerophosphoserine, and phosphoserine, which are not transported by the plasma membrane flippase, do not activate Atp8a1.", "entity1": "Atp8a1", "entity2": "phosphatidylserine-O-methyl ester", "span1": [236, 242], "span2": [61, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"15503": {"label": 4, "data": {"text": "Although naturally occurring electrophilic plant compounds, such as mustard oil and cinnamaldehyde, are TRPA1 agonists, it is unknown whether arthropod-produced electrophiles activate mammalian TRPA1.", "entity1": "TRPA1", "entity2": "cinnamaldehyde", "span1": [104, 109], "span2": [84, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13632": {"label": 0, "data": {"text": "We report that mutation of this conserved Gly in yeast Top1p alters enzyme sensitivity to CPT.", "entity1": "yeast Top1p", "entity2": "Gly", "span1": [49, 60], "span2": [42, 45]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6662": {"label": 3, "data": {"text": "Patients stable on warfarin therapy and concurrently taking a cyclooxygenase-2 (COX-2) inhibitor comparator (traditional nonsteroidal antiinflammatory medications, salsalate, or acetaminophen) randomly received celecoxib 200 mg/day or rofecoxib 25 mg/day for three weeks.", "entity1": "cyclooxygenase-2", "entity2": "rofecoxib", "span1": [62, 78], "span2": [235, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13459": {"label": 3, "data": {"text": "Finally, PLA2 inhibitor methyl arachidonyl fluorophosphonate blocked the PUFA effects on COX-2 induction, promoter activity and arachidonic acid mobilization suggesting involvement of AA metabolites in PPAR activation.", "entity1": "PLA2", "entity2": "arachidonyl fluorophosphonate", "span1": [9, 13], "span2": [31, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3511": {"label": 8, "data": {"text": "Aldo-keto reductases (AKRs) metabolize a wide range of substrates, including polycyclic aromatic hydrocarbons (PAHs), generating metabolites (o-quinones) and reactive oxygen species (ROS), which are capable of initiating and promoting carcinogenesis.", "entity1": "AKRs", "entity2": "PAHs", "span1": [22, 26], "span2": [111, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"12558": {"label": 1, "data": {"text": "With the exception of risperidone, all the antipsychotic drugs tested failed to show selectivity for either of the alpha 1-adrenoceptor subtypes.", "entity1": "alpha 1-adrenoceptor", "entity2": "risperidone", "span1": [115, 135], "span2": [22, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5129": {"label": 3, "data": {"text": "In this study, we found that 5-hydroxy-3,6,7,8,3'4'-hexamethoxyflavone (5HHMF) from Hizikia fusiforme considerably inhibits lipopolysaccharide (LPS)-stimulated NO production by suppressing the expression of inducible NO synthase (iNOS) in BV2 microglia.", "entity1": "inducible NO synthase", "entity2": "5HHMF", "span1": [207, 228], "span2": [72, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7021": {"label": 3, "data": {"text": "Competitive radioligand binding assays were performed using cells expressing either the human serotonin (5-HT) transporter (hSERT) or norepinephrine (NE) transporter (hNET) with K(i) values for DVS of 40.2 +/- 1.6 and 558.4 +/- 121.6 nM, respectively.", "entity1": "hSERT", "entity2": "DVS", "span1": [124, 129], "span2": [194, 197]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12686": {"label": 1, "data": {"text": "To elucidate the target genes regulated by these compounds, we treated Zucker diabetic fatty rats (ZDF) for 15 days with a PPAR-alpha-specific compound, fenofibrate, a PPAR-gamma-specific ligand, rosiglitazone, and a PPAR-alpha/-gamma coagonist, GW2331, and measured the levels of several messenger RNAs (mRNAs) in liver by real-time polymerase chain reaction.", "entity1": "PPAR-gamma", "entity2": "rosiglitazone", "span1": [168, 178], "span2": [196, 209]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10334": {"label": 2, "data": {"text": "H2O2 caused cell loss and increased cell death with features of apoptosis, i.e. TdT-mediated dUTP nick-end labelling (TUNEL) reaction and caspase-3 activation.", "entity1": "caspase-3", "entity2": "H2O2", "span1": [138, 147], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1503": {"label": 3, "data": {"text": "db/db mice treated with DRF 2655 showed 5- and 3.6-fold inhibition in phosphoenolpyruvate carboxykinase and glucose 6-phosphatase activity and 651% and 77% increases in the beta-oxidation enzymes carnitine palmitoyltransferase and carnitine acetyltransferase, respectively.", "entity1": "phosphoenolpyruvate carboxykinase", "entity2": "DRF 2655", "span1": [70, 103], "span2": [24, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12229": {"label": 2, "data": {"text": "Furthermore, because S-(+)-isomers of METH and AMPH are reported to be more potent and efficacious in vivo than R-(-), we determined the enantiomeric selectivity of all three species of TAAR1.", "entity1": "TAAR1", "entity2": "AMPH", "span1": [186, 191], "span2": [47, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9501": {"label": 3, "data": {"text": "At nonconvulsant doses, the sodium channel blockers acetylprocainamide, dibucaine, dyclonine, prilocaine, proparacaine, quinidine, and tetracaine produced a small pressor response or no increase in BP.", "entity1": "sodium channel", "entity2": "tetracaine", "span1": [28, 42], "span2": [135, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11189": {"label": 2, "data": {"text": "Orlistat treatment also results in modest improvements in total cholesterol, low-density lipoprotein, blood pressure, and fasting glucose and insulin concentrations.", "entity1": "insulin", "entity2": "Orlistat", "span1": [142, 149], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11244": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "hDAT", "entity2": "4',7,8-trichloro", "span1": [96, 100], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"552": {"label": 8, "data": {"text": "N-Acetylglucosamine-1-phosphodiester alpha-N-Acetylglucosaminidase (EC 3.1.4.45; phosphodiester alpha-GlcNAcase) catalyzes the second step in the synthesis of the mannose 6-phosphate determinant required for efficient intracellular targeting of newly synthesized lysosomal hydrolases to the lysosome.", "entity1": "phosphodiester alpha-GlcNAcase", "entity2": "mannose 6-phosphate", "span1": [81, 111], "span2": [163, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"11078": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "myosin light chain kinase", "entity2": "t-butyl", "span1": [131, 156], "span2": [257, 264]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10157": {"label": 1, "data": {"text": "ICI 182,780 (fulvestrant) (Faslodex) and ICI 164,384 are competitive inhibitors of estrogen by binding to the estrogen receptor (ER).", "entity1": "ER", "entity2": "ICI 182,780", "span1": [129, 131], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1445": {"label": 1, "data": {"text": "The expression of the neuronal activity marker Fos was increased 3.7-fold in PFC by atomoxetine administration, but was not increased in the striatum or nucleus accumbens, consistent with the regional distribution of increased DA(EX).", "entity1": "Fos", "entity2": "atomoxetine", "span1": [47, 50], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1398": {"label": 3, "data": {"text": "Interestingly, gemfibrozil strongly inhibited the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of GAS in cytokine-stimulated astroglial cells.", "entity1": "NF-kappaB", "entity2": "gemfibrozil", "span1": [64, 73], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"155": {"label": 5, "data": {"text": "Nizatidine (LY139037), a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion.", "entity1": "histamine H2-receptor", "entity2": "Nizatidine", "span1": [35, 56], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3423": {"label": 0, "data": {"text": "The Met790 side chain of the G719S/T790M double mutant, in the apo form and gefitinib- and AMPPNP-bound forms, adopts different conformations that explain the accommodation of these ligands.", "entity1": "T790M", "entity2": "Met", "span1": [35, 40], "span2": [4, 7]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6495": {"label": 5, "data": {"text": "The following alpha(2)-adrenoceptor antagonists were applied: BRL44408 (alpha(2A)-selective), ARC239 (alpha(2B)- and alpha(2C)-selective), and prazosin (alpha(2B)- and alpha(2C)-selective).", "entity1": "alpha(2A)", "entity2": "BRL44408", "span1": [72, 81], "span2": [62, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14413": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "EPAC", "entity2": "nucleotide", "span1": [320, 324], "span2": [172, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8068": {"label": 3, "data": {"text": "Overall, our results suggest that inhibition of the p38 MAPK signaling by metformin coupled with paclitaxel therapy in human NSCLC cells may be a clinically useful combination, which however will require further validation.", "entity1": "MAPK", "entity2": "metformin", "span1": [56, 60], "span2": [74, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3618": {"label": 4, "data": {"text": "In further studies, the diuretic effects of the CB1 agonist AM4054 were similar in male and female rats, displayed a relatively rapid onset to action, and were dose-dependently antagonized by 30 minutes pretreatment with rimonabant, but not by the vanilloid receptor type I antagonist capsazepine, nor were the effects of WIN 55,212 antagonized by the CB2 antagonist AM630 [(6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl) methanone)].", "entity1": "CB2", "entity2": "WIN 55,212", "span1": [352, 355], "span2": [322, 332]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12709": {"label": 1, "data": {"text": "We demonstrated that the coexpressed HG1 and GAB-1 receptors are GABA-responsive, and provide evidence for the possible involvement of GABA receptors in the mechanism of ivermectin resistance.", "entity1": "HG1", "entity2": "GABA", "span1": [37, 40], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1606": {"label": 3, "data": {"text": "5-(N,N-dimethyl)-amiloride (50 microM; DMA), a concentration that selectively inhibits the NHE isoforms NHE1 and NHE2, but not NHE3, did not affect DBS.", "entity1": "NHE", "entity2": "DMA", "span1": [91, 94], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9431": {"label": 3, "data": {"text": "With either substrate, alendronate was a slow binding inhibitor of PTPmeg1.", "entity1": "PTPmeg1", "entity2": "alendronate", "span1": [67, 74], "span2": [23, 34]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2612": {"label": 8, "data": {"text": "Possession of CYP2C9*2 or CYP2C9*3 variant alleles, which result in decreased enzyme activity, is associated with a significant decrease in the mean warfarin dose.", "entity1": "CYP2C9", "entity2": "warfarin", "span1": [26, 32], "span2": [149, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7514": {"label": 2, "data": {"text": "BACKGROUND AND PURPOSE: AMP-activated protein kinase (AMPK) is activated by metformin, phenformin, and the AMP mimetic, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR).", "entity1": "AMPK", "entity2": "phenformin", "span1": [54, 58], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14133": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "tumor necrosis factor-alpha", "entity2": "Celastrol", "span1": [195, 222], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"655": {"label": 3, "data": {"text": "Inhibition of gelatinase A (MMP-2) by batimastat and captopril reduces tumor growth and lung metastases in mice bearing Lewis lung carcinoma.", "entity1": "gelatinase A", "entity2": "batimastat", "span1": [14, 26], "span2": [38, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3659": {"label": 3, "data": {"text": "We then showed that static exposure of embryos to paraoxon (31.2-500 nM) from 5 to 96 hpf resulted in significant stage- and concentration-dependent AChE inhibition, albeit these effects were fully reversible within 48 h following transfer to clean water.", "entity1": "AChE", "entity2": "paraoxon", "span1": [149, 153], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"975": {"label": 3, "data": {"text": "Thus, U50,488H-induced internalization and down-regulation of the hkor share initial common mechanisms.", "entity1": "hkor", "entity2": "U50,488H", "span1": [66, 70], "span2": [6, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4454": {"label": 0, "data": {"text": "ROS produced by this oxidase activates Src, enable that in turn, transactivates EGFR that activates Stat3 in tyrosine, allowing its dimerization.", "entity1": "Stat3", "entity2": "tyrosine", "span1": [100, 105], "span2": [109, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1447": {"label": 3, "data": {"text": "The selective norepinephrine (NE) transporter inhibitor atomoxetine (formerly called tomoxetine or LY139603) has been shown to alleviate symptoms in Attention Deficit/Hyperactivity Disorder (ADHD).", "entity1": "norepinephrine (NE) transporter", "entity2": "tomoxetine", "span1": [14, 45], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8577": {"label": 3, "data": {"text": "ATO inhibited the phosphorylation and activation of AKT and STAT3 through Notch signaling blockade.", "entity1": "Notch", "entity2": "ATO", "span1": [74, 79], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8231": {"label": 2, "data": {"text": "ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.", "entity1": "ERG", "entity2": "ICA-105574", "span1": [109, 112], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4231": {"label": 2, "data": {"text": "The current U.S. military and civilian oxime countermeasure, 2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride (2-PAM), is under consideration for replacement with a more effective acetylcholinesterase reactivator, 1,1'-methylenebis{4-hydroxyiminomethyl}pyridinium dimethanesulfonate (MMB-4).", "entity1": "acetylcholinesterase", "entity2": "MMB-4", "span1": [187, 207], "span2": [291, 296]}, "weak_labels": [-1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3004": {"label": 1, "data": {"text": "Affinity of V782A for cGMP, vardenafil, sildenafil, tadalafil, or IBMX was reduced 5.5-, 23-, 10-, 3-, and 12-fold, respectively.", "entity1": "V782A", "entity2": "cGMP", "span1": [12, 17], "span2": [22, 26]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8674": {"label": 2, "data": {"text": "Surprisingly, the conditional deletion of Trp63, but not \u0394Np63, in oocytes inhibited apoptosis, as well as the accumulation of c-Abl and TAp73 caused by cisplatin.", "entity1": "TAp73", "entity2": "cisplatin", "span1": [137, 142], "span2": [153, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5952": {"label": 5, "data": {"text": "Inhibition of MCF-7 cell growth by the selective calmodulin antagonists W-13 and W-12 is consistent with a role for calmodulin antagonism in the broad growth-inhibitory properties of pimozide.", "entity1": "calmodulin", "entity2": "W-12", "span1": [49, 59], "span2": [81, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6918": {"label": 0, "data": {"text": "The two active sites of dimeric 5-aminolevulinate synthase (ALAS), a pyridoxal 5'-phosphate (PLP)-dependent enzyme, are located on the subunit interface with contribution of essential amino acids from each subunit.", "entity1": "ALAS", "entity2": "amino acids", "span1": [60, 64], "span2": [184, 195]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12112": {"label": 3, "data": {"text": "HERG/IKr channels are a prime target for the pharmacological management of arrhythmias and are selectively blocked by class III antiarrhythmic methanesulfonanilide drugs, such as dofetilide, E4031, and MK-499, at submicromolar concentrations.", "entity1": "IKr", "entity2": "dofetilide", "span1": [5, 8], "span2": [179, 189]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13375": {"label": 8, "data": {"text": "Several genes involved with steroid metabolism also showed remarkable expression changes, including increased expression of 17beta-hydroxysteroid dehydrogenase-7 (HSD17beta7; involved in estradiol production) and decreased expression of HSD17beta5 (involved in testosterone production).", "entity1": "HSD17beta7", "entity2": "estradiol", "span1": [163, 173], "span2": [187, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14546": {"label": 0, "data": {"text": "Neurodegeneration was related with decreased [(3)H]glutamate uptake and decreased Akt immunoreactivity, however phospho-GSK-3-\u03b2 (Ser9) was not altered in (PhTe)(2) injected rat.", "entity1": "phospho-GSK-3-\u03b2", "entity2": "Ser", "span1": [112, 127], "span2": [129, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1332": {"label": 9, "data": {"text": "Moreover, in rat hepatoma H4-II-E cells, the esterified-BM failed to induce tyrosine aminotransferase, which is regulated by GR-mediated transactivation activity.", "entity1": "tyrosine aminotransferase", "entity2": "BM", "span1": [76, 101], "span2": [56, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9523": {"label": 1, "data": {"text": "Intrinsic, gating-independent DHP receptor binding affinity differences must be invoked to explain the isoform-specific sensitivity of the DHP block.", "entity1": "DHP receptor", "entity2": "DHP", "span1": [30, 42], "span2": [139, 142]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2003": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "amino acids", "span1": [121, 125], "span2": [42, 53]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4495": {"label": 9, "data": {"text": "Diclofenac-\u03b2-d-glucuronide, clopidogrel-\u03b2-d-glucuronide, ibuprofen-\u03b2-d-glucuronide, (R)-naproxen-\u03b2-d-glucuronide, and (S)-naproxen-\u03b2-d-glucuronide selectively inhibited hCES1, with Ki values of 4.32 \u00b1 0.47, 24.8 \u00b1 4.2, 355 \u00b1 38, 468 \u00b1 21, 707 \u00b1 64 \u00b5M, respectively, but did not significantly inhibit hCES2.", "entity1": "hCES2", "entity2": "(R)-naproxen-\u03b2-d-glucuronide", "span1": [300, 305], "span2": [84, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8384": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "3\u03b2-hydroxysteroid dehydrogenase", "entity2": "Cd", "span1": [225, 256], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5568": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase 1 (DDAH1) is an enzyme that metabolizes methylated arginine to citrulline and methylamine, thus working to produce nitric oxide (NO).", "entity1": "DDAH1", "entity2": "citrulline", "span1": [43, 48], "span2": [103, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8342": {"label": 3, "data": {"text": "Aqueous ethanol (80%) extract of lentil hulls exhibited high antioxidant and anti-inflammatory activities preferentially inhibiting 15-LOX (IC(50), 55 \u03bcg/ml), with moderate COX-1 (IC(50), 66 \u03bcg/ml) and COX-2 (IC(50), 119 \u03bcg/ml) inhibitory effects on the COX pathway, whereas faba bean hull extracts exerted relatively mild LOX inhibitory activity.", "entity1": "LOX", "entity2": "ethanol", "span1": [323, 326], "span2": [8, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1992": {"label": 2, "data": {"text": "Extracellular application of meclofenamate (EC(50) = 25 microM) and diclofenac (EC(50) = 2.6 microM) resulted in the activation of KCNQ2/Q3 K(+) currents, heterologously expressed in Chinese hamster ovary cells.", "entity1": "KCNQ2/Q3", "entity2": "meclofenamate", "span1": [131, 139], "span2": [29, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"250": {"label": 3, "data": {"text": "Both NS-398 and Dup-697 exhibited time-dependent inactivation of hCOX-2, as did indomethacin on both enzymes.", "entity1": "hCOX-2", "entity2": "Dup-697", "span1": [65, 71], "span2": [16, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2766": {"label": 3, "data": {"text": "Kinetic studies with lumiracoxib demonstrated that it was a time-dependent and slowly reversible inhibitor of human COX-2 that exhibited at least two binding steps during inhibition.", "entity1": "human COX-2", "entity2": "lumiracoxib", "span1": [110, 121], "span2": [21, 32]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7650": {"label": 2, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-2", "entity2": "monocrotaline", "span1": [0, 5], "span2": [90, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14571": {"label": 2, "data": {"text": "In conclusion, in this cellular model, DOX effectively protects against PQ toxicity by inducing P-gp and through the interaction with the choline transporter, suggesting that compounds presenting this double feature of promoting the efflux and limiting the uptake of PQ could be used as effective antidotes to treat intoxications.", "entity1": "P-gp", "entity2": "DOX", "span1": [96, 100], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9566": {"label": 2, "data": {"text": "Secretion of GM-CSF protein in the presence of increasing concentrations of isoproterenol followed a similar pattern as observed for GM-CSF mRNA.", "entity1": "GM-CSF", "entity2": "isoproterenol", "span1": [133, 139], "span2": [76, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2162": {"label": 1, "data": {"text": "Similar to cocaine, other local anesthetics bind to the dopamine transporter (DAT) and inhibit DA uptake in rodent and monkey brain.", "entity1": "dopamine transporter", "entity2": "cocaine", "span1": [56, 76], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14203": {"label": 1, "data": {"text": "The structurally diverse opioids codeine and eseroline, like galantamine, are also nAChR-APL that have greatly diminished affinity for AChE, representing potential lead compounds for selective nAChR-APL development.", "entity1": "nAChR", "entity2": "codeine", "span1": [83, 88], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4098": {"label": 3, "data": {"text": "Additionally, AIF levels in the cytosol decreased due to EGTA but not due to calpeptin.", "entity1": "AIF", "entity2": "EGTA", "span1": [14, 17], "span2": [57, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1896": {"label": 2, "data": {"text": "I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction.", "entity1": "interleukin 6", "entity2": "I3A", "span1": [69, 82], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8074": {"label": 3, "data": {"text": "Inhibition of this carboxylesterase probably presents a major source for altered therapeutic activity of these medicines if co-administered with orlistat.", "entity1": "carboxylesterase", "entity2": "orlistat", "span1": [19, 35], "span2": [145, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14854": {"label": 2, "data": {"text": "Interestingly, Acrolein increased proteins' levels of amyloid precursor protein (APP), \u03b2-secretase (BACE-1) and the amyloid \u03b2-peptide transporter receptor for advanced glycation end products, and decreased A-disintegrin and metalloprotease (ADAM) 10 levels.", "entity1": "receptor for advanced glycation end products", "entity2": "Acrolein", "span1": [146, 190], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"1614": {"label": 3, "data": {"text": "Inhibition of GluR5 kainate receptors could represent a key mechanism underlying the anticonvulsant activity of topiramate.", "entity1": "kainate receptors", "entity2": "topiramate", "span1": [20, 37], "span2": [112, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1957": {"label": 5, "data": {"text": "bolus injection of, either physiological saline (0.3 ml/kg; control), or the antagonists SB224289 (300 microg/kg; 5-HT1B), BRL15572 (300 microg/kg; 5-HT1D), rauwolscine (300 microg/kg; alpha2), SB224289 + BRL15572 (300 microg/kg each), SB224289 + rauwolscine (300 microg/kg each), BRL15572 + rauwolscine (300 microg/kg each), rauwolscine (300 microg/kg) + prazosin (100 microg/kg; alpha1), SB224289 (300 microg/kg) + prazosin (100 microg/kg), SB224289 (300 microg/kg) + rauwolscine (300 microg/kg) + prazosin (100 microg/kg), SB224289 (300 microg/kg) + prazosin (100 microg/kg) + BRL44408 (1,000 microg/kg; alpha2A), SB224289 (300 microg/kg) + prazosin (100 microg/kg)+ imiloxan (1,000 microg/kg; alpha2B), or SB224289 (300 microg/kg) + prazosin (100 microg/kg) + MK912 (300 microg/kg; alpha2C).", "entity1": "5-HT1D", "entity2": "BRL15572", "span1": [148, 154], "span2": [123, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3125": {"label": 2, "data": {"text": "AMPK activators metformin and AICAR partly prevented the cell cycle block, oxidative stress and apoptosis induced by compound C. The small interfering RNA (siRNA) targeting of human AMPK mimicked compound C-induced G(2)/M cell cycle arrest, but failed to induce oxidative stress and apoptosis in U251 glioma cells.", "entity1": "AMPK", "entity2": "metformin", "span1": [0, 4], "span2": [16, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1966": {"label": 5, "data": {"text": "Brain but not spinal NR2B receptor is responsible for the anti-allodynic effect of an NR2B subunit-selective antagonist CP-101,606 in a rat chronic constriction injury model.", "entity1": "NR2B", "entity2": "CP-101,606", "span1": [21, 25], "span2": [120, 130]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8747": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "ketoconazole", "span1": [18, 25], "span2": [168, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10173": {"label": 1, "data": {"text": "In conclusion, these results show that rifamycin SV and rifampicin interact with OATP-mediated substrate transport to different extents.", "entity1": "OATP", "entity2": "rifampicin", "span1": [81, 85], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"11721": {"label": 1, "data": {"text": "To investigate the effects of \u03b2-ionone on apoptosis initiation and its possible mechanisms of action, we qualified cell apoptosis, proteins related to apoptosis and a phosphatidylinositol 3-kinase (PI3K)-AKT pathway in human gastric adenocarcinoma cancer SGC-7901 cells.", "entity1": "phosphatidylinositol 3-kinase", "entity2": "\u03b2-ionone", "span1": [167, 196], "span2": [30, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11696": {"label": 3, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "tumor necrosis factor alpha", "entity2": "cisplatin", "span1": [124, 151], "span2": [212, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15012": {"label": 1, "data": {"text": "Taken together, these results suggest that SAH/SAHH-mediated transmethylation could be linked to the tumorigenic processes through cross-regulation between the actin cytoskeleton and Src kinase activity.", "entity1": "actin", "entity2": "SAH", "span1": [160, 165], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11251": {"label": 1, "data": {"text": "The 4',7,8-trichloro analogue (38) of mazindol was the most potent and selective ligand for HEK-hDAT cells (DAT K(i) = 1.1 nM; SERT/DAT = 1283 and NET/DAT = 38).", "entity1": "DAT", "entity2": "mazindol", "span1": [108, 111], "span2": [38, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4420": {"label": 9, "data": {"text": "Experimental studies performed for characterizing the inhibitory mechanism indicate that GSK-3\u03b2 inhibition by palinurin cannot be competed out by ATP nor peptide substrate.", "entity1": "GSK-3\u03b2", "entity2": "ATP", "span1": [89, 95], "span2": [146, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"5018": {"label": 0, "data": {"text": "These variants are expected to encode either a full length (OATP2B1-FL) or shortened protein lacking 22 N-terminus amino acids (OATP2B-Short).", "entity1": "OATP2B1-FL", "entity2": "N", "span1": [60, 70], "span2": [104, 105]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8526": {"label": 8, "data": {"text": "CYP3A4 and CYP3A5 metabolized BDP via hydroxylation ([M4] and [M6]) and dehydrogenation ([M5]) at similar rates; CYP3A7 did not metabolize BDP.", "entity1": "CYP3A5", "entity2": "BDP", "span1": [11, 17], "span2": [30, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2123": {"label": 2, "data": {"text": "The positive correlation between vitamin A and immunoglobulin A concentrations might be the result of the vitamin A inductive effect during immunoglobulins A synthesis.", "entity1": "immunoglobulins A", "entity2": "vitamin A", "span1": [140, 157], "span2": [106, 115]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12208": {"label": 8, "data": {"text": "During embryogenesis, lratb is expressed in mostly non-overlapping domains opposite to retinal dehydrogenase 2 (raldh2), the key enzyme for retinoic acid synthesis.", "entity1": "raldh2", "entity2": "retinoic acid", "span1": [112, 118], "span2": [140, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11713": {"label": 1, "data": {"text": "We examined the ability of the EPAC-selective cAMP analog 8-pCPT-2'-O-Me-cAMP-AM to potentiate the action of these drugs and the mechanism that might account for it.", "entity1": "EPAC", "entity2": "8-pCPT-2'-O-Me-cAMP-AM", "span1": [31, 35], "span2": [58, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12336": {"label": 8, "data": {"text": "Contributions of rat Ctr1 to the uptake and toxicity of copper and platinum anticancer drugs in dorsal root ganglion neurons.", "entity1": "rat Ctr1", "entity2": "platinum", "span1": [17, 25], "span2": [67, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6925": {"label": 2, "data": {"text": "We present our studies to demonstrate that HM74A, but not HM74, binds niacin at high affinities and effectively mediates Gi signaling events in human embryonic kidney HEK293 cells as well as in 3T3L1 adipocytes expressing HM74A.", "entity1": "Gi", "entity2": "niacin", "span1": [121, 123], "span2": [70, 76]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11940": {"label": 3, "data": {"text": "We also observed that fisetin efficiently suppressed the phosphorylation of Akt, S6K1 and mTORC1 in adipose tissue.", "entity1": "S6K1", "entity2": "fisetin", "span1": [81, 85], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9887": {"label": 1, "data": {"text": "UNLABELLED: Apparent muscarinic acetylcholine (mAch) receptor occupancy in mouse cerebral cortex, hippocampus, and striatum by scopolamine, an antagonist, and biperiden, a relatively selective M1 antagonist, was estimated with competitive binding studies using two different radioligands: 3H-N-methyl piperidyl benzilate (3H-NMPB) and 3H-quinuclidinyl benzilate (3H-QNB).", "entity1": "muscarinic acetylcholine (mAch) receptor", "entity2": "3H-QNB", "span1": [21, 61], "span2": [363, 369]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11635": {"label": 1, "data": {"text": "In this report, we demonstrate the utility of reversed-phase protein chromatography and FT-ICR mass spectrometry in analyzing CCNU (lomustine, 1-(2-chloroethyl)-3-cyclohexyl-1-nitroso-urea, MW: 233.7Da) modification of stathmin.", "entity1": "stathmin", "entity2": "lomustine", "span1": [219, 227], "span2": [132, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9368": {"label": 1, "data": {"text": "We show that the binding of thalidomide photoaffinity label to authentic human AGP is competed with both thalidomide and the nonradioactive photoaffinity label at concentrations comparable to those required for inhibition of production of tumor necrosis factor alpha from human monocytes, suggesting that AGP may be involved in the immunomodulatory activity of thalidomide.", "entity1": "AGP", "entity2": "thalidomide", "span1": [305, 308], "span2": [361, 372]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7153": {"label": 8, "data": {"text": "Phosphodiesterase-5 (PDE5) contains a catalytic domain (C domain) that hydrolyzes cGMP and a regulatory domain (R domain) that contains two mammalian cGMP-binding phosphodiesterase, Anabaena adenylyl cyclases, Escherichia coli FhlAs (GAFs) (A and B) and a phosphorylation site for cyclic nucleotide-dependent protein kinases (cNPKs).", "entity1": "PDE5", "entity2": "cGMP", "span1": [21, 25], "span2": [82, 86]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7200": {"label": 3, "data": {"text": "Our results imply that P2Y12 has the potential to be inhibited by ADP/ATP analogs, and it suggests that P2Y12 acts as a target of new drugs that inhibit platelet aggregation.", "entity1": "P2Y12", "entity2": "ATP", "span1": [23, 28], "span2": [70, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5301": {"label": 1, "data": {"text": "In addition, prunetin inhibits NF-\u03baB-dependent inflammatory responses by modulating I\u03baB kinase (IKK)-inhibitor \u03baB\u03b1 (I\u03baB\u03b1)-NF-\u03baB signaling.", "entity1": "I\u03baB\u03b1", "entity2": "prunetin", "span1": [116, 120], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10199": {"label": 3, "data": {"text": "In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2.", "entity1": "organic anion transporting polypeptides", "entity2": "rifampicin", "span1": [116, 155], "span2": [26, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9265": {"label": 3, "data": {"text": "Ergovaline inhibition of radioligand binding to the D2 dopamine receptor and ergot alkaloid inhibition of vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production in GH4ZR7 cells, stably transfected with a rat D2 dopamine receptor, were evaluated.", "entity1": "VIP", "entity2": "ergot alkaloid", "span1": [137, 140], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7674": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "CA", "entity2": "acetazolamide", "span1": [113, 115], "span2": [204, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"829": {"label": 3, "data": {"text": "SC-51089 (10(-5) M), a selective EP1-receptor antagonist, showed no effect on the PGE1- or PGE2-induced inhibition of the HVA ICa, thereby indicating that PGE1- and PGE2-induced inhibition of the HVA Ca2+ channels is possibly mediated by the EP3 receptor.", "entity1": "HVA Ca2+ channels", "entity2": "PGE2", "span1": [196, 213], "span2": [165, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9095": {"label": 3, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "leukotriene synthetase", "entity2": "diethylcarbamazine", "span1": [251, 273], "span2": [15, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3082": {"label": 3, "data": {"text": "Neurochemical effects of the monoamine oxidase inhibitor phenelzine on brain GABA and alanine: A comparison with vigabatrin.", "entity1": "monoamine oxidase", "entity2": "phenelzine", "span1": [29, 46], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9615": {"label": 1, "data": {"text": "Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide.", "entity1": "sulfonylurea receptor", "entity2": "ATP", "span1": [44, 65], "span2": [23, 26]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11296": {"label": 8, "data": {"text": "BACKGROUND & AIMS: Of the 2 genes (MAT1A, MAT2A) encoding methionine adenosyltransferase, the enzyme that synthesizes S-adenosylmethionine, MAT1A, is expressed in liver, whereas MAT2A is expressed in extrahepatic tissues.", "entity1": "methionine adenosyltransferase", "entity2": "S-adenosylmethionine", "span1": [58, 88], "span2": [118, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1666": {"label": 1, "data": {"text": "RESULTS: In vivo, loss and recovery of the righting reflex required similar times after intraperitoneal injection of etomidate in wild-type and in alpha2A-receptor-deficient mice, indicating that the hypnotic effect of etomidate in mice does not require the alpha2A-receptor subtype.", "entity1": "alpha2A-receptor", "entity2": "etomidate", "span1": [147, 163], "span2": [117, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6424": {"label": 8, "data": {"text": "Uncoupling proteins (UCPs) are inner mitochondrial membrane transporters which act as pores for H(+) ions, dissipating the electrochemical gradient that develops during mitochondrial respiration at the expense of ATP synthesis.", "entity1": "UCPs", "entity2": "H(+)", "span1": [21, 25], "span2": [96, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15378": {"label": 8, "data": {"text": "Studies on the kinetics of the hSULT2A1-catalyzed sulfation of dehydroepiandrosterone (DHEA) showed the effects of disulfide bond formation on the substrate inhibition characteristics of the enzyme.", "entity1": "hSULT2A1", "entity2": "dehydroepiandrosterone", "span1": [31, 39], "span2": [63, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1, -1]},
	"13856": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "17beta-hydroxysteroid-dehydrogenase type 1", "entity2": "progestogens", "span1": [266, 308], "span2": [37, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15467": {"label": 8, "data": {"text": "The present study demonstrated that human multidrug resistance-associated protein 3 vesicles accepted conjugated 3\u03b2-hydroxy-\u0394(5)-bile acids along with common bile acids such as glycocholic acid and taurolithocholic acid 3-sulfate.", "entity1": "human multidrug resistance-associated protein 3", "entity2": "taurolithocholic acid 3-sulfate", "span1": [36, 83], "span2": [198, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15363": {"label": 1, "data": {"text": "Taken together, these findings identify a signature hepatic gene-network associated with repeated oxycodone administration in rats and demonstrate that oxycodone alters the expression of many transporters and DMEs (without direct activation of PXR, CAR, and AhR), which could lead to undesirable DDIs after coadministration of substrates of these transporters/DMEs with oxycodone.", "entity1": "CAR", "entity2": "oxycodone", "span1": [249, 252], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"4748": {"label": 3, "data": {"text": "(S)-3-(Aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole (GSK2251052) is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase, and that has been in development for the treatment of serious Gram-negative infections.", "entity1": "bacterial leucyl tRNA synthetase", "entity2": "GSK2251052", "span1": [147, 179], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14271": {"label": 8, "data": {"text": "We recently showed that TETA is metabolized in vitro by polyamine catabolic enzyme spermidine/spermine-N(1)-acetyltransferase (SSAT1) and by thialysine acetyltransferase (SSAT2) to its monoacetylated derivative (MAT).", "entity1": "spermidine/spermine-N(1)-acetyltransferase", "entity2": "TETA", "span1": [83, 125], "span2": [24, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15757": {"label": 3, "data": {"text": "Quercetin suppressed CYP2E1-dependent ethanol hepatotoxicity via depleting heme pool and releasing CO.", "entity1": "CYP2E1", "entity2": "Quercetin", "span1": [21, 27], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12588": {"label": 1, "data": {"text": "The kinetics of onset of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor desensitization by glutamate, and the extent of attenuation of AMPA receptor desensitization by cyclothiazide, showed pronounced cell-to-cell variation in cultures of rat hippocampal neurons.", "entity1": "AMPA receptor", "entity2": "cyclothiazide", "span1": [161, 174], "span2": [194, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1879": {"label": 1, "data": {"text": "In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone.", "entity1": "glucocorticoid receptor", "entity2": "mifepristone", "span1": [74, 97], "span2": [187, 199]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13430": {"label": 2, "data": {"text": "High D-glucose increases L-arginine transport and eNOS expression following TbetaRII activation by TGF-beta1 involving p42/44(mapk) and Smad2 in HUVEC.", "entity1": "TbetaRII", "entity2": "D-glucose", "span1": [76, 84], "span2": [5, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6951": {"label": 3, "data": {"text": "Hepatic ACAT activity was significantly lower in both vitamin E and probucol groups than in HC-control group, while HMG-CoA reductase activity was the highest only in the probucol group.", "entity1": "ACAT", "entity2": "probucol", "span1": [8, 12], "span2": [68, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1009": {"label": 5, "data": {"text": "METHODS: Part A compared the effects of placebo to four doses of a 5-HT(4) receptor antagonist (SB-207266) on the cisapride mediated increase in plasma aldosterone (a 5-HT(4) mediated response) and orocaecal transit in 18 subjects.", "entity1": "5-HT(4)", "entity2": "SB-207266", "span1": [167, 174], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3089": {"label": 4, "data": {"text": "Unlike the sedative hypnotics that target GABA(A) receptor complexes, ramelteon is a chronohypnotic that acts on the melatonin MT(1) and MT(2) receptors, which are primarily located in the suprachiasmatic nucleus, the body's \"master clock.\"", "entity1": "MT(2)", "entity2": "ramelteon", "span1": [137, 142], "span2": [70, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12304": {"label": 1, "data": {"text": "Overall, the present study, using a different and more sensitive statistical model than the parent study, revealed a statistically significant dose-dependent correlation between cumulative exposure to Hg from dental amalgams and urinary levels of GST-\u03b1, after covariate adjustment; where as, a nonsignificant relationship was observed with urinary levels of GST-\u03c0.", "entity1": "GST-\u03b1", "entity2": "Hg", "span1": [247, 252], "span2": [201, 203]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11066": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "caldesmon kinase", "entity2": "Ca2+", "span1": [110, 126], "span2": [181, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9845": {"label": 8, "data": {"text": "gamma-Butyrobetaine hydroxylase catalyse the last step in carnitine biosynthesis, the formation of L-carnitine from gamma-butyrobetaine, a reaction dependent on Fe2+, alpha-ketoglutarate, ascorbate and oxygen.", "entity1": "gamma-Butyrobetaine hydroxylase", "entity2": "carnitine", "span1": [0, 31], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"782": {"label": 3, "data": {"text": "In this report, we evaluated the growth-inhibitory effects of sulindac sulfide, a COX-1 and COX-2 inhibitor; exisulind (sulindac sulfone), a novel proapoptotic agent that does not inhibit COX enzymes; and nordihydroguaiaretic acid (NDGA), a lipoxygenase inhibitor on human lung cancer cell lines.", "entity1": "COX-1", "entity2": "sulindac sulfide", "span1": [82, 87], "span2": [62, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10631": {"label": 8, "data": {"text": "The availability of the 5-FU prodrugs offers the possibility of greater therapeutic selectivity based on the demonstration that thymidine phosphorylase, the activating enzyme for 5-FU, is expressed at a higher level in tumor tissue compared with normal tissue counterparts.", "entity1": "thymidine phosphorylase", "entity2": "5-FU", "span1": [128, 151], "span2": [179, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6958": {"label": 1, "data": {"text": "Maraviroc inhibited binding of [125I]-MIP-1beta to CCR5 from macaque and human with similar potency (IC50 = 17.50 +/- 1.24 nM and 7.18 +/- 0.93 nM, respectively) and antagonised MIP-1beta induced intracellular calcium release mediated through CCR5 from macaque and human with similar potency (IC50 = 17.50 +/- 3.30 nM and 12.07 +/- 1.89, respectively).", "entity1": "CCR5", "entity2": "125I", "span1": [51, 55], "span2": [32, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8879": {"label": 1, "data": {"text": "By \"working upwards\" from mTOR, we observed that TCDD inhibited endogenous and IGF-I-induced AKT and ERK activation by interfering with tyrosine phosphorylation of insulin receptor substrate 1.", "entity1": "insulin receptor substrate 1", "entity2": "TCDD", "span1": [164, 192], "span2": [49, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2245": {"label": 3, "data": {"text": "BACKGROUND: Since the introduction of the first cholinesterase inhibitor (ChEI) in 1997, most clinicians and probably most patients would consider the cholinergic drugs, donepezil, galantamine and rivastigmine, to be the first line pharmacotherapy for mild to moderate Alzheimer's disease.The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase.", "entity1": "acetylcholinesterase", "entity2": "donepezil", "span1": [492, 512], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1848": {"label": 8, "data": {"text": "SR-BI is a receptor that binds HDL with high affinity and mediates both the selective lipid uptake of cholesteryl esters from lipid-rich HDL to cells and the efflux of unesterified cholesterol from cells to HDL.", "entity1": "SR-BI", "entity2": "cholesterol", "span1": [0, 5], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"156": {"label": 5, "data": {"text": "Nizatidine (LY139037), a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion.", "entity1": "histamine H2-receptor", "entity2": "LY139037", "span1": [35, 56], "span2": [12, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15663": {"label": 3, "data": {"text": "3-HPT inhibits HDAC 6 and HDAC 8 with an IC50 of 681 and 3675 nM, respectively.", "entity1": "HDAC 6", "entity2": "3-HPT", "span1": [15, 21], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1195": {"label": 8, "data": {"text": "Different substrates were used as the relative specific substrates for the determination of aminopeptidase enzymatic activity: 4-methoxy-2-naphthylamide of L-alanine for aminopeptidase N, 4-methoxy-2-naphthylamide of L-leucine for leucine aminopeptidase, 4-methoxy-2-naphthylamide of L-glutamic acid for aminopeptidase A and 4-methoxy-2-naphthylamide of L-arginine for aminopeptidase B.", "entity1": "leucine aminopeptidase", "entity2": "4-methoxy-2-naphthylamide", "span1": [231, 253], "span2": [188, 213]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2030": {"label": 1, "data": {"text": "The activation appears to be due to an increase of GAD affinity for its cofactor, pyridoxal phosphate (PLP).", "entity1": "GAD", "entity2": "PLP", "span1": [51, 54], "span2": [103, 106]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"9705": {"label": 3, "data": {"text": "The irreversible MAO-B inhibitors, pargyline (30 mg/kg) and l-deprenyl (3-10 mg/kg) also decreased responding maintained by ethanol reinforcement; these results are consistent with previous findings that both drugs decreased ethanol intake in mice.", "entity1": "MAO-B", "entity2": "pargyline", "span1": [17, 22], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6100": {"label": 3, "data": {"text": "bolus); finally, 8 rabbits received aurintrycarboxilic acid (ATA), an inhibitor of platelet glycoprotein Ib/von Willebrand factor interaction (10 mg/kg i.v.", "entity1": "glycoprotein Ib", "entity2": "ATA", "span1": [92, 107], "span2": [61, 64]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1221": {"label": 8, "data": {"text": "Also in contrast to effects of multiple METH injections, 1) MDMA caused little or no decrease in binding of the DAT ligand WIN35428, and 2) neither prevention of hyperthermia nor prior depletion of DA prevented the MDMA-induced reduction in plasmalemmal DA transport.", "entity1": "DAT", "entity2": "DA", "span1": [112, 115], "span2": [198, 200]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5475": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "norethisterone", "span1": [106, 127], "span2": [271, 285]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15686": {"label": 2, "data": {"text": "Treatment with EVn-50 or VB1 resulted in arresting the MDA-MB-435 and SMMC-7721 cells at G2/M phase, which was further supported by observations of increased phosphorylation of Histone 3 at Ser10, phosphorylation of Cdk1 at Tyr15, expression of cyclin B1, and decreased expression of Cdc25c.", "entity1": "cyclin B1", "entity2": "VB1", "span1": [245, 254], "span2": [25, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9530": {"label": 8, "data": {"text": "Methylenetetrahydrofolate reductase deficiency impairs methyltetrahydrofolate synthesis, defects in cytosolic reduction of hydroxocobalamin (CblC/D) impair the synthesis of both methyl- and adenosyl cobalamin and deficiencies of methionine synthase (CblE/G) are associated with defective methyl cobalamin synthesis.", "entity1": "Methylenetetrahydrofolate reductase", "entity2": "methyltetrahydrofolate", "span1": [0, 35], "span2": [55, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5904": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "VLDL", "entity2": "nicotinic acid", "span1": [133, 137], "span2": [32, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12173": {"label": 1, "data": {"text": "Niacin mediates lipolysis in adipose tissue through its G-protein coupled receptor HM74A.", "entity1": "G-protein coupled receptor HM74A", "entity2": "Niacin", "span1": [56, 88], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13148": {"label": 3, "data": {"text": "Pranlukast, ketamine and edaravone decreased NMDA-induced injury; pranlukast (0.1 mg/kg) and ketamine inhibited the upregulated expression of the CysLT1 receptor.", "entity1": "CysLT1 receptor", "entity2": "pranlukast", "span1": [146, 161], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8172": {"label": 1, "data": {"text": "In contrast to wild-type pol \u03b2, the ternary complex of the R283K mutant with an incoming dATP-analogue and templating 8-oxoG resembles a G-A mismatched structure with 8-oxoG adopting an anti-conformation.", "entity1": "R283K", "entity2": "8-oxoG", "span1": [59, 64], "span2": [167, 173]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12657": {"label": 1, "data": {"text": "The cytosolic fractions from liver and colon tissues of NQO1-/- mice showed similar amounts of DNA cross-linking upon exposure to MMC, as observed in NQO1+/+ mice.", "entity1": "NQO1", "entity2": "MMC", "span1": [150, 154], "span2": [130, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6670": {"label": 8, "data": {"text": "Ribonucleotide reductase (RR) is responsible for the de novo conversion of the ribonucleoside diphosphates to deoxyribonucleoside diphosphates, which are essential for DNA synthesis and repair.", "entity1": "Ribonucleotide reductase", "entity2": "deoxyribonucleoside diphosphates", "span1": [0, 24], "span2": [110, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3539": {"label": 1, "data": {"text": "These results suggest that LTD4 increases A\u03b2 peptide burden via activation of CysLT(1)R, which further affects APP levels and activity of \u03b2- and \u03b3-secretases via the NF-\u03baB pathway.", "entity1": "APP", "entity2": "LTD4", "span1": [111, 114], "span2": [27, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12726": {"label": 8, "data": {"text": "Acetylcholinesterase (AChE) predominates in the healthy brain, with butyrylcholinesterase (BuChE) considered to play a minor role in regulating brain acetylcholine (ACh) levels.", "entity1": "Acetylcholinesterase", "entity2": "acetylcholine", "span1": [0, 20], "span2": [150, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6571": {"label": 3, "data": {"text": "Mutants Y751A, D950A, and F1004A had reduced sensitivity to milrinone (K(i) changed from 0.66 microM for the recombinant PDE3A to 7.5 to 156 microM for the mutants), and diminished sensitivity to cilostazol (K(i) of the mutants were 18- to 371-fold higher than that of the recombinant PDE3A).", "entity1": "PDE3A", "entity2": "cilostazol", "span1": [285, 290], "span2": [196, 206]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4757": {"label": 1, "data": {"text": "Regucalcin (RGN/SMP30) was originally discovered in 1978 as a unique calcium-binding protein that does not contain the EF-hand motif of calcium-binding domain.", "entity1": "RGN", "entity2": "calcium", "span1": [12, 15], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12005": {"label": 1, "data": {"text": "In this paper the effect of shRNA LRRK2 knock-down on Mn toxicity was examined in control and DAT transfected HEK293 cells.", "entity1": "DAT", "entity2": "Mn", "span1": [94, 97], "span2": [54, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4093": {"label": 2, "data": {"text": "Furthermore, treatment with spironoclactone not only attenuated the pro-apoptotic effect of ALD but reversed the ALD-induced increase of calpain and AIF levels.", "entity1": "calpain", "entity2": "ALD", "span1": [137, 144], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11048": {"label": 8, "data": {"text": "Novel highly affine histamine H3 receptor ligands with additional inhibitory effects on the main histamine metabolizing enzyme in the brain, N-methyltransferase, chemically show structural elements of the acetylcholinesterase inhibitor tacrine.", "entity1": "N-methyltransferase", "entity2": "histamine", "span1": [141, 160], "span2": [97, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12057": {"label": 1, "data": {"text": "Our results demonstrated that acute As(III) treatment (12.5\u2009mg/kg) altered CYP epoxygenases, CYP \u03c9-hydroxylases and EPHX2 mRNA levels that were isozyme and tissue specific.", "entity1": "EPHX2", "entity2": "As(III)", "span1": [116, 121], "span2": [36, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3527": {"label": 0, "data": {"text": "While DNA damage does not affect phosphorylation at the PDK-1 site Thr350/Thr308 of AKT-1, it increased phosphorylation at Ser517/Ser473.", "entity1": "AKT-1", "entity2": "Ser", "span1": [84, 89], "span2": [123, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11449": {"label": 1, "data": {"text": "DAT occupancy was between 66 and 82% and <10-41% for doses of dimethocaine and procaine that maintained maximum response rates, respectively.", "entity1": "DAT", "entity2": "procaine", "span1": [0, 3], "span2": [79, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14263": {"label": 8, "data": {"text": "By contrast, 1,12-diamino-3,6,9-triazadodecane(SpmTrien), a charge-deficient spermine analog, was an extremely poor substrate of human recombinant SSAT2 and was metabolized by SSAT1 in HEPG2 cells and in wild-type primary hepatocytes.", "entity1": "SSAT1", "entity2": "spermine", "span1": [176, 181], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"56": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "human renin", "entity2": "Enalkiren", "span1": [93, 104], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"13859": {"label": 3, "data": {"text": "As discussed in this review, various progestogens including dydrogesterone and its 20alpha-dihydro-derivative, medrogestone, promegestone, nomegestrol acetate and norelgestromin can reduce intratissular levels of estradiol in breast cancer by blocking sulfatase and 17beta-hydroxysteroid-dehydrogenase type 1 activities.", "entity1": "sulfatase", "entity2": "medrogestone", "span1": [252, 261], "span2": [111, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15327": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "pyrene", "span1": [287, 296], "span2": [88, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6946": {"label": 2, "data": {"text": "Hepatic ACAT activity was significantly lower in both vitamin E and probucol groups than in HC-control group, while HMG-CoA reductase activity was the highest only in the probucol group.", "entity1": "HMG-CoA reductase", "entity2": "probucol", "span1": [116, 133], "span2": [171, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5825": {"label": 3, "data": {"text": "Loperamide, an opiate agonist of high specificity for mu-receptors, was recently reported to suppress ACTH and cortisol levels in normal subjects, but not in patients with proven ACTH-dependent Cushing's disease.", "entity1": "ACTH", "entity2": "Loperamide", "span1": [102, 106], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11510": {"label": 8, "data": {"text": "Choline dehydrogenase (CHDH) and betaine-homocysteine methyltransferase (BHMT) are 2 enzymes involved in choline oxidation.", "entity1": "CHDH", "entity2": "choline", "span1": [23, 27], "span2": [105, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16": {"label": 3, "data": {"text": "The present studies were undertaken to determine whether stable analogues of prostacyclin, a potent endothelium-derived platelet inhibitor and vasodilator, could inhibit tissue factor expression by human monocytic cells.", "entity1": "tissue factor", "entity2": "prostacyclin", "span1": [170, 183], "span2": [77, 89]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10376": {"label": 3, "data": {"text": "In this work a novel approach combining HPLC-UV on-line with oaTOF-MS and ICPMS was applied to investigate in human and rat plasma the metabolism of labelled BK (79/81 Br-Phe5) BrBK in the presence of two new dual ACE/NEP inhibitors (GW660511X and omapatrilat) currently under clinical trial.", "entity1": "ACE", "entity2": "GW660511X", "span1": [214, 217], "span2": [234, 243]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6887": {"label": 1, "data": {"text": "ABCG5 and ABCG8 themselves are regulated by cholesterol via liver X receptors (LXRs), which are also activated by oxysterols and some derivatives of plant sterols.", "entity1": "LXRs", "entity2": "cholesterol", "span1": [79, 83], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5077": {"label": 2, "data": {"text": "siRNA knockdown of p38 MAPK abrogated the ability of anisomycin to synergistically induce CYP2B6 mRNA.", "entity1": "CYP2B6", "entity2": "anisomycin", "span1": [90, 96], "span2": [53, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4650": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A1", "entity2": "TCDD", "span1": [159, 165], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14382": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "EGFR", "entity2": "AG1478", "span1": [203, 207], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4669": {"label": 3, "data": {"text": "Endothelial dysfunction induced by SIRT1 inhibition was prevented by treatment of the vessels with the NADPH oxidase inhibitor apocynin or superoxide dismutase.", "entity1": "NADPH oxidase", "entity2": "apocynin", "span1": [103, 116], "span2": [127, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11750": {"label": 3, "data": {"text": "Based on these suggestions, the rational redesign of furanopyrimidine 24 (clog\u2009P=7.41; Aurora\u2005A IC(50) =43\u2005nM; HCT-116 IC(50) =400\u2005nM) led to the identification of quinazoline 67 (clog\u2009P=5.28; Aurora\u2005A IC(50) =25\u2005nM; HCT-116 IC(50) =23\u2005nM).", "entity1": "Aurora\u2005A", "entity2": "quinazoline", "span1": [193, 201], "span2": [164, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11700": {"label": 0, "data": {"text": "The active site of the metalloproteinase domain has a consensus HEXXHXXGXXHD sequence and a Met-turn.", "entity1": "metalloproteinase domain", "entity2": "Met", "span1": [23, 47], "span2": [92, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14811": {"label": 4, "data": {"text": "Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist \u0394(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054.", "entity1": "CB(1)", "entity2": "AM4054", "span1": [151, 156], "span2": [311, 317]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7372": {"label": 1, "data": {"text": "Furthermore, with respect to GSTM1 and GSTT1 there were statistically significant differences in TTCA-levels between genotypes among exposed workers but not among controls.", "entity1": "GSTT1", "entity2": "TTCA", "span1": [39, 44], "span2": [97, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1773": {"label": 1, "data": {"text": "Overexpression of beta 1-adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for 'putative' beta 4-adrenoceptor pharmacology.", "entity1": "beta 4-adrenoceptor", "entity2": "CGP 12177A", "span1": [140, 159], "span2": [82, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2703": {"label": 2, "data": {"text": "Sitagliptin, an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, improves glycaemic control by inhibiting DPP-4 inactivation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.", "entity1": "glucose-dependent insulinotropic polypeptide", "entity2": "Sitagliptin", "span1": [176, 220], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15319": {"label": 1, "data": {"text": "Racemic IKM-159 was crystallized with the ligand-binding domain of GluA2, and the structure revealed a complex containing (2R)-IKM-159 at the glutamate binding site.", "entity1": "GluA2", "entity2": "Racemic IKM-159", "span1": [67, 72], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1263": {"label": 1, "data": {"text": "OBJECTIVE: We examined the effect of CysLT antagonists (pranlukast and MCI-826) on antigen inhalation-induced eosinophilia in peripheral blood and lung, and on IL-5 activity in serum during late increase of airway resistance (late asthmatic response, LAR) in sensitized guinea-pigs.", "entity1": "IL-5", "entity2": "pranlukast", "span1": [160, 164], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13260": {"label": 3, "data": {"text": "Pranlukast hydrate (ONO-1078, 100 microM) downregulated the leukotriene D(4)-induced MUC2/5AC gene expression and mucin secretion.", "entity1": "mucin", "entity2": "Pranlukast hydrate", "span1": [114, 119], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2501": {"label": 8, "data": {"text": "Licofelone almost abolished 5-LOX activity by inhibiting leukotriene B4 generation in rabbit neutrophils and prevented platelet thromboxane B2 production from whole blood.", "entity1": "5-LOX", "entity2": "thromboxane B2", "span1": [28, 33], "span2": [128, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13841": {"label": 9, "data": {"text": "Systemic bupivacaine did not modify either the hyperalgesia and local inflammation or COX expression.", "entity1": "COX", "entity2": "bupivacaine", "span1": [86, 89], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2063": {"label": 8, "data": {"text": "Mutation of arginine 228 to lysine enhances the glucosyltransferase activity of bovine beta-1,4-galactosyltransferase I.\tBeta-1,4-galactosyltransferase I (beta4Gal-T1) normally transfers Gal from UDP-Gal to GlcNAc in the presence of Mn(2+) ion (Gal-T activity) and also transfers Glc from UDP-Glc to GlcNAc (Glc-T activity), albeit at only 0.3% efficiency.", "entity1": "beta4Gal-T1", "entity2": "UDP-Gal", "span1": [155, 166], "span2": [196, 203]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13523": {"label": 1, "data": {"text": "In these experiments, CDO exhibits an ordered binding of l-cysteine prior to NO (and presumably O2) similar to that observed for the 2H1C class of non-heme iron enzymes.", "entity1": "2H1C class of non-heme iron enzymes", "entity2": "l-cysteine", "span1": [133, 168], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13124": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "TOP2A", "entity2": "etopoxide", "span1": [64, 69], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1451": {"label": 3, "data": {"text": "Rasagiline does not modify CNS monoamine tissue levels or monoamine-induced behavioural syndromes at doses which selectively inhibit MAO-B but not MAO-A.", "entity1": "MAO-A", "entity2": "Rasagiline", "span1": [147, 152], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10672": {"label": 1, "data": {"text": "In Experiment 2, TT-235 induced a significant decrease (p<0.05) in oxytocin receptor number and binding affinity at both 0.5 and 4 hours compared with controls.", "entity1": "oxytocin receptor", "entity2": "TT-235", "span1": [67, 84], "span2": [17, 23]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15842": {"label": 1, "data": {"text": "To confirm the role of each transporter, we analyzed HEK293 cells stably expressing human ABCA1 or ABCG1; we clearly observed 24-OHC efflux in the presence of HDL, whereas efflux in the presence of apolipoprotein A-I was marginal.", "entity1": "apolipoprotein A-I", "entity2": "24-OHC", "span1": [198, 216], "span2": [126, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"3554": {"label": 2, "data": {"text": "LTD4 also induced expression of cysteinyl leukotriene receptor 1 (CysLT(1)R) and NF-\u03baB p65 in the hippocampus and cortex.", "entity1": "CysLT(1)R", "entity2": "LTD4", "span1": [66, 75], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8966": {"label": 5, "data": {"text": "The Schild plots for the competitive antagonists WB4101 and 5-methyl-urapidil against alpha 1a-adrenoceptor-selective agonist methoxamine-induced contraction were linear and had slopes not significantly different from unity, with a pA2 of 9.07 +/- 0.07 (n = 5) for WB4101 and 9.09 +/- 0.05 (n = 3) for 5-methyl-urapidil.", "entity1": "alpha 1a-adrenoceptor", "entity2": "WB4101", "span1": [86, 107], "span2": [265, 271]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4263": {"label": 1, "data": {"text": "Furthermore, proteosomal inhibitor MG132 suppressed AMPK activation, GSK3\u03b2 phosphorylation, cleaved PARP and deceased AEG-1 induced by ursolic acid in HepG2 cells.", "entity1": "PARP", "entity2": "MG132", "span1": [100, 104], "span2": [35, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1964": {"label": 5, "data": {"text": "In order to examine the site of action of an NR2B subtype-selective NMDA antagonist CP-101,606, we investigated its analgesic effect in a rat model of neuropathic pain at various routes of administration.", "entity1": "NR2B", "entity2": "CP-101,606", "span1": [45, 49], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14510": {"label": 5, "data": {"text": "Small interfering RNA directed BDNF, orexin-A, and SB334867 [N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl urea; a specific orexin-1 receptor antagonist] were administered directly into the hypothalamus.", "entity1": "orexin-1 receptor", "entity2": "SB334867", "span1": [131, 148], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15120": {"label": 2, "data": {"text": "Mn (10 and 20\u00a0mg/kg) increased caspase activity and F(2)-isoprostane production (a biological marker of lipid peroxidation).", "entity1": "caspase", "entity2": "Mn", "span1": [31, 38], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"15404": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "ABCG5/8", "entity2": "7-ketosterols", "span1": [210, 217], "span2": [245, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"12542": {"label": 1, "data": {"text": "Amine oxidase activities in brown adipose tissue of the rat: identification of semicarbazide-sensitive (clorgyline-resistant) activity at the fat cell membrane.", "entity1": "Amine oxidase", "entity2": "clorgyline", "span1": [0, 13], "span2": [104, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2734": {"label": 3, "data": {"text": "A KCC inhibitor-[(dihydroindenyl)oxy] alkanoic acid (DIOA)-blocked RVD more in HCEC than RCEC.", "entity1": "KCC", "entity2": "DIOA", "span1": [2, 5], "span2": [53, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11682": {"label": 1, "data": {"text": "Despite the importance of AKRs in PAHs metabolism, there are no studies that evaluate, in general human populations, the effect of PAHs on AKRs expression in peripheral blood lymphocytes (PBLs).", "entity1": "AKRs", "entity2": "PAHs", "span1": [139, 143], "span2": [131, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14333": {"label": 3, "data": {"text": "Dimethylfumarate attenuates renal fibrosis via NF-E2-related factor 2-mediated inhibition of transforming growth factor-beta/Smad signaling.", "entity1": "Smad", "entity2": "Dimethylfumarate", "span1": [125, 129], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1049": {"label": 3, "data": {"text": "First, in the presence of 1 mm ATP or the nonhydrolyzable analog adenosine 5'-(beta,gamma-imino)triphosphate, TOP2-mediated DNA cleavage induced by ATP-sensitive TOP2 poisons (e.g. doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g.", "entity1": "TOP2", "entity2": "mitoxantrone", "span1": [110, 114], "span2": [205, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12870": {"label": 2, "data": {"text": "Similar to the plasma membrane PS transporter, Atp8a1 is activated only by the naturally occurring sn-1,2-glycerol isomer of PS and not the sn-2,3-glycerol stereoisomer.", "entity1": "Atp8a1", "entity2": "sn-1,2-glycerol", "span1": [47, 53], "span2": [99, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"14377": {"label": 3, "data": {"text": "NFD suppressed EGF-mediated protein levels of c-Jun and c-Fos, and reduced MMP-9 expression and activity, concomitantly with a marked inhibition on cell migration and invasion without obvious cellular cytotoxicity.", "entity1": "c-Jun", "entity2": "NFD", "span1": [46, 51], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9800": {"label": 3, "data": {"text": "Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid.", "entity1": "human and rat dihydroorotate dehydrogenase", "entity2": "brequinar sodium", "span1": [26, 68], "span2": [105, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2211": {"label": 2, "data": {"text": "Galanin attenuates cyclic AMP regulatory element-binding protein (CREB) phosphorylation induced by chronic morphine and naloxone challenge in Cath.a cells and primary striatal cultures.", "entity1": "cyclic AMP regulatory element-binding protein", "entity2": "naloxone", "span1": [19, 64], "span2": [120, 128]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4440": {"label": 3, "data": {"text": "Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties of a series of phthalide [2-benzofuran-1(3H)-one] analogues.", "entity1": "monoamine oxidase", "entity2": "isatin", "span1": [128, 145], "span2": [50, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1830": {"label": 3, "data": {"text": "Here, we show that one BLT, [1-(2-methoxy-phenyl)-3-naphthalen-2-yl-urea] (BLT-4), blocked ABCA1-mediated cholesterol efflux to lipid-poor apoA-I at a potency similar to that for its inhibition of SR-BI (IC(50) approximately 55-60 microM).", "entity1": "ABCA1", "entity2": "BLT-4", "span1": [91, 96], "span2": [75, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14433": {"label": 1, "data": {"text": "Through identification of mammary ABCG2 as a novel target gene of pesticide prochloraz and dioxin, our results may therefore help to improve the protection of breast-feeding infants and the consumer of dairy products.", "entity1": "ABCG2", "entity2": "dioxin", "span1": [34, 39], "span2": [91, 97]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10648": {"label": 1, "data": {"text": "Unique binding interactions of valdecoxib with COX-2 translate into a fast rate of inactivation of COX-2 (110,000 M/s compared with 7000 M/s for rofecoxib and 80 M/s for etoricoxib).", "entity1": "COX-2", "entity2": "etoricoxib", "span1": [99, 104], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, 1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9680": {"label": 3, "data": {"text": "The antidepressant desipramine has been shown to decrease synaptic membrane concentrations of the norepinephrine re-uptake transporter (NET) in vivo and in vitro, on both an acute and a chronic basis.", "entity1": "norepinephrine re-uptake transporter", "entity2": "desipramine", "span1": [98, 134], "span2": [19, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9884": {"label": 8, "data": {"text": "The salivary fluid secretory mechanism is thought to require Na(+)/K(+)/2Cl(-) cotransporter-mediated Cl(-) uptake.", "entity1": "Na(+)/K(+)/2Cl(-) cotransporter", "entity2": "Cl(-)", "span1": [61, 92], "span2": [102, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10810": {"label": 3, "data": {"text": "COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis.", "entity1": "COX-2", "entity2": "meloxicam", "span1": [10, 15], "span2": [85, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10716": {"label": 2, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "c-jun", "entity2": "KA", "span1": [75, 80], "span2": [45, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9443": {"label": 9, "data": {"text": "The two receptors were discriminated by butaprost, AH-13205 and AH-6809 that bound to the EP2 receptor but not to the EP4 receptor, and by 1-OH-PGE1 that bound to the EP4 but not to the EP2 receptor.", "entity1": "EP4", "entity2": "AH-13205", "span1": [118, 121], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1748": {"label": 1, "data": {"text": "Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016.", "entity1": "ErbB3", "entity2": "GW572016", "span1": [97, 102], "span2": [165, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5707": {"label": 2, "data": {"text": "As(III) also increased total epoxygenases activity in the lung while it decreased its levels in the kidney and had no effect on the liver.", "entity1": "epoxygenases", "entity2": "As(III)", "span1": [29, 41], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2683": {"label": 1, "data": {"text": "Molecular modeling of the kinase domain of mutant c-Kit (V654A) and AXL showed no binding to IM but efficient binding to MP470, a novel c-Kit/AXL kinase inhibitor.", "entity1": "kinase domain", "entity2": "MP470", "span1": [26, 39], "span2": [121, 126]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3272": {"label": 1, "data": {"text": "Together these studies support a unique mode of inhibition in which phenothiazines disrupt the S100A4/myosin-IIA interaction by sequestering S100A4 via small molecule-induced oligomerization.", "entity1": "S100A4", "entity2": "phenothiazines", "span1": [141, 147], "span2": [68, 82]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6530": {"label": 0, "data": {"text": "Experimentation using isoforms of alefacept engineered to have amino acid substitutions in the IgG1 C(H)2 domain that impact Fc gamma R binding indicate that alefacept mediates cognate interactions between cells expressing human CD2 and CD16 to activate cells, e.g., increase extracellular signal-regulated kinase phosphorylation, up-regulate cell surface expression of the activation marker CD25, and induce release of granzyme B.", "entity1": "alefacept", "entity2": "amino acid", "span1": [34, 43], "span2": [63, 73]}, "weak_labels": [0, -1, -1, 1, 1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4127": {"label": 1, "data": {"text": "The cellular prion protein PrP(C) consists of two domains--a flexible N-terminal domain, which participates in copper and zinc regulation, and a largely helical C-terminal domain that converts to \u03b2 sheet in the course of prion disease.", "entity1": "prion protein PrP(C)", "entity2": "copper", "span1": [13, 33], "span2": [111, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"7675": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "EC 4.2.1.1", "entity2": "acetazolamide", "span1": [117, 127], "span2": [204, 217]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7256": {"label": 4, "data": {"text": "PEA was a potent and full agonist at each species of TAAR1, whereas TYR was a full agonist for the rodent TAAR1s but was a partial agonist at h-rChTAAR1.", "entity1": "h-rChTAAR1", "entity2": "TYR", "span1": [142, 152], "span2": [68, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6870": {"label": 3, "data": {"text": "Our results suggest that easing of Fas-triggered fulminant hepatitis by minocycline may involve a mitochondrial apoptotic pathway, probably through preventing cytochrome c release and thereby blocking downstream caspase activation.", "entity1": "caspase", "entity2": "minocycline", "span1": [212, 219], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3639": {"label": 3, "data": {"text": "NaAsO(2) increased the mRNA levels of the light and medium subunits of neurofilament and decreased the mRNA levels of tau and tubulin in a dose-dependent manner; no significant effect was found in the mRNA levels of the heavy subunit of neurofilament, microtubule-associated protein 2, or actin.", "entity1": "tubulin", "entity2": "NaAsO(2)", "span1": [126, 133], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4652": {"label": 3, "data": {"text": "Enzyme kinetic analyses using human liver microsomes revealed inhibition of CYP1A1 activity by delphinidin (IC50 78 \u03bcM) and pelargonidin (IC50 33 \u03bcM).", "entity1": "CYP1A1", "entity2": "delphinidin", "span1": [76, 82], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14137": {"label": 3, "data": {"text": "Celastrol, a TAK1 inhibitor and anti-inflammatory compound used in traditional Chinese medicine, also decreased TGF-\u03b21-induced phosphorylation of TAK1 and RELA, and suppressed basal, TGF-\u03b21- and tumor necrosis factor-alpha (TNF-\u03b1)-induced NF-\u03baB reporter gene activity.", "entity1": "NF-\u03baB", "entity2": "Celastrol", "span1": [239, 244], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"453": {"label": 5, "data": {"text": "Pretreatment of the tissues with combined 5-HT1/5-HT2 antagonists, methysergide (1 microM) or methiothepin (0.1 microM), significantly attenuated the inhibitory effect of epinastine on the noncholinergic contraction.", "entity1": "5-HT1", "entity2": "methiothepin", "span1": [42, 47], "span2": [94, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9305": {"label": 3, "data": {"text": "Inhibitory effects of lysine analogues on t-PA induced whole blood clot lysis.", "entity1": "t-PA", "entity2": "lysine", "span1": [42, 46], "span2": [22, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14609": {"label": 8, "data": {"text": "Wild-type enzymes and variants of CDA (Lys27Gln and Ala70Thr) and DCK (Ile24Val, Ala119Gly, and Pro122Ser) were expressed in and purified from Escherichia coli, and enzyme kinetic parameters were estimated for cytarabine (Ara-C), dFdC, and its metabolite 2',2'-difluorodeoxyuridine (dFdU) as substrates.", "entity1": "Lys27Gln", "entity2": "dFdC", "span1": [39, 47], "span2": [230, 234]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11644": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "MAO", "entity2": "VIG", "span1": [264, 267], "span2": [55, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2604": {"label": 3, "data": {"text": "In the interaction of GAL and CAR, AChE inhibition was stronger but without any statistical significance.", "entity1": "AChE", "entity2": "GAL", "span1": [35, 39], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2860": {"label": 8, "data": {"text": "4-Hydroxynonenal (4-HNE) is a mutagenic alpha,beta-unsaturated aldehyde produced during oxidative injury that is conjugated by several glutathione S-transferase (GST) isoforms.", "entity1": "GST", "entity2": "4-HNE", "span1": [162, 165], "span2": [18, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5573": {"label": 3, "data": {"text": "Carbonic anhydrase inhibitors: aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity.", "entity1": "Carbonic anhydrase", "entity2": "adamantyl", "span1": [0, 18], "span2": [84, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1618": {"label": 2, "data": {"text": "Weekly subcutaneous decitabine produces cumulative increases in HbF and total hemoglobin through a noncytotoxic mechanism of action.", "entity1": "hemoglobin", "entity2": "decitabine", "span1": [78, 88], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6864": {"label": 2, "data": {"text": "Pre-irradiation administration of RP-1 enhanced levels of GSH induced increase in complex I (upto 16 h), complex I/III (4 h) complex II/III activity (upto 24 h; p < 0.01) and inhibited the radiation-induced decrease in MMP significantly (24 h; p < 0.01).", "entity1": "complex II/III", "entity2": "GSH", "span1": [125, 139], "span2": [58, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9943": {"label": 3, "data": {"text": "RESULTS: NF-kappaB/Rel activity induced by tumor necrosis factor alpha, 12-O-tetradecanoylphorbol-13-acetate, or overexpression of NF-kappaB-inducing kinase, IKK-alpha, IKK-beta, or constitutively active IKK-alpha and IKK-beta mutants was inhibited dose dependently by sulfasalazine.", "entity1": "IKK-beta", "entity2": "sulfasalazine", "span1": [218, 226], "span2": [269, 282]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1137": {"label": 9, "data": {"text": "Amiloride is a specific inhibitor of uPA but does not inhibit tPA.", "entity1": "tPA", "entity2": "Amiloride", "span1": [62, 65], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15234": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B1", "entity2": "silybin A", "span1": [0, 7], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"12378": {"label": 1, "data": {"text": "Methods: Cocktail approach was used to evaluate the influence of IR and IPC on the activities of CYP1A2, CYP2C9, CYP2E1, CYP2D6 and CYP3A4, which were reflected by the changes of pharmacokinetic parameters of five specific probe drugs: caffeine, chlorzoxazone, tolbutamide, metoprolol and midazolam, respectively.", "entity1": "CYP2C9", "entity2": "chlorzoxazone", "span1": [105, 111], "span2": [246, 259]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8910": {"label": 3, "data": {"text": "Combined application of dexamethasone and amrinone caused additive inhibition of TNF biosynthesis in vitro.", "entity1": "TNF", "entity2": "amrinone", "span1": [81, 84], "span2": [42, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14304": {"label": 1, "data": {"text": "Claudin-3 and claudin-4 regulate sensitivity to cisplatin by controlling expression of the copper and cisplatin influx transporter CTR1.", "entity1": "CTR1", "entity2": "cisplatin", "span1": [131, 135], "span2": [48, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9321": {"label": 3, "data": {"text": "Inhibition of cytokine-primed eosinophil chemotaxis by nedocromil sodium.", "entity1": "cytokine", "entity2": "nedocromil sodium", "span1": [14, 22], "span2": [55, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4646": {"label": 2, "data": {"text": "CYP1A1 and CYP1A2 mRNAs were also increased by pelargonidin in three primary human hepatocytes cultures (approximately 5% of TCDD potency) and the increase in CYP1A1 protein in HepG2 and LS174T cells was comparable to the increase in catalytic activity of CYP1A1 enzyme.", "entity1": "CYP1A1", "entity2": "pelargonidin", "span1": [159, 165], "span2": [47, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15006": {"label": 8, "data": {"text": "In the in vitro model we observed high permeability of imperatorin and isoimperatorin with the P-gp-mediated efflux ratios of 0.53 and 0.06, as well as medium permeability of cnidilin with 0.82.", "entity1": "P-gp", "entity2": "cnidilin", "span1": [95, 99], "span2": [175, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9796": {"label": 3, "data": {"text": "Another inhibitor, brequinar was previously reported to be a slow-binding inhibitor of the human dihydroorotate dehydrogenase [W. Knecht, M. Loffler, Species-related inhibition of human and rat dihyroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives, Biochem.", "entity1": "human and rat dihyroorotate dehydrogenase", "entity2": "isoxazol", "span1": [180, 221], "span2": [243, 251]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13843": {"label": 8, "data": {"text": "BACKGROUND: Peripheral inflammatory pain is associated with an upregulation of spinal cord COX-2 (cyclooxygenase-2), with a subsequent increase in central prostaglandin E2 (PGE2) levels associated with the development of hyperalgesia.", "entity1": "cyclooxygenase-2", "entity2": "prostaglandin E2", "span1": [98, 114], "span2": [155, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13276": {"label": 8, "data": {"text": "Thus, isoflavone supplementation did not affect ABCA1-dependent cholesterol efflux to serum.", "entity1": "ABCA1", "entity2": "cholesterol", "span1": [48, 53], "span2": [64, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4524": {"label": 8, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "human carboxylesterases 1", "entity2": "acyl glucuronides", "span1": [102, 127], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4381": {"label": 8, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "midazolam", "span1": [280, 285], "span2": [231, 240]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11751": {"label": 3, "data": {"text": "Three different 3D-QSAR models were built and validated by using a set of 66 pyrazole (Model\u2005I) and furanopyrimidine (Model\u2005II) compounds with IC(50) values toward Aurora kinase\u2005A ranging from 33\u2005nM to 10.5\u2005\u03bcM.", "entity1": "Aurora kinase\u2005A", "entity2": "pyrazole", "span1": [164, 179], "span2": [77, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12851": {"label": 2, "data": {"text": "In addition, sorafenib demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular-endothelial growth factor (VEGFR)-2, VEGFR-3, platelet-derived growth factor (PDGFR)-beta Flt-3, and c-KIT.", "entity1": "c-KIT", "entity2": "sorafenib", "span1": [273, 278], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6462": {"label": 3, "data": {"text": "Pemetrexed disodium (Alimta, LY231514) is a novel, multitargeted antifolate that inhibits thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyl transferase.", "entity1": "dihydrofolate reductase", "entity2": "Alimta", "span1": [112, 135], "span2": [21, 27]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4721": {"label": 3, "data": {"text": "In support of the hypothesis that TCDD decreases canonical Wnt signaling, we identify inhibitory effects of TCDD on multiple components of the canonical Wnt signaling pathway in the UGS that temporally coincide with the inhibitory effect of TCDD on prostatic bud formation: (1) expression of R-spondins (Rspo2 and Rspo3) that promote canonical Wnt signaling is reduced; (2) expression of Lef1, Tcf1, and Wif1, established canonical Wnt target genes, is decreased; (3) expression of Lgr5, a RSPO receptor that activates canonical Wnt signaling, is reduced; and (4) expression of Dickkopfs (Dkks), inhibitors of canonical Wnt signaling, is not increased by TCDD.", "entity1": "Tcf1", "entity2": "TCDD", "span1": [394, 398], "span2": [241, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13550": {"label": 5, "data": {"text": "Combination chemotherapy with a substance P receptor antagonist (aprepitant) and melarsoprol in a mouse model of human African trypanosomiasis.", "entity1": "substance P receptor", "entity2": "melarsoprol", "span1": [32, 52], "span2": [81, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7465": {"label": 8, "data": {"text": "The mechanisms that specify the vesicular phenotype of inhibitory interneurons in vertebrates are poorly understood because the two main inhibitory transmitters, glycine and GABA, share the same vesicular inhibitory amino acid transporter (VIAAT) and are both present in neurons during postnatal development.", "entity1": "VIAAT", "entity2": "GABA", "span1": [240, 245], "span2": [174, 178]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"5848": {"label": 4, "data": {"text": "While the substituted benzamide prokinetics (for example, metoclopramide, cisapride) also block 5-HT3 receptors in high concentrations, their prokinetic action is believed to be on the basis of their agonist effects on the putative 5-HT4 receptor.", "entity1": "5-HT4", "entity2": "benzamide", "span1": [232, 237], "span2": [22, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11643": {"label": 1, "data": {"text": "METHODS: Male rats were administered PLZ (10 mg/kg) or VIG (1,000 mg/kg) i.p., and the rats were euthanized 4 hours later and the brains removed for analysis of levels of GABA and ALA (by electron capture gas chromatography after derivatization) and activities of MAO, GABA-T and ALA-T (radiochemical assays).", "entity1": "ALA-T", "entity2": "PLZ", "span1": [280, 285], "span2": [37, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4332": {"label": 3, "data": {"text": "Suppression of Src/ERK and GSK-3/\u03b2-catenin signaling by pinosylvin inhibits the growth of human colorectal cancer cells.", "entity1": "ERK", "entity2": "pinosylvin", "span1": [19, 22], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7898": {"label": 1, "data": {"text": "In conclusion, the CAG length dependent effect of TCDD on AR activity in PNT1A, but not in PC-3 cells, indicates as a cell-specific effect of TCDD on AR activity.", "entity1": "AR", "entity2": "TCDD", "span1": [58, 60], "span2": [50, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4279": {"label": 3, "data": {"text": "Conversely, AMPK inhibitor compound C or GSK3\u03b2 inhibitor SB216763 blocked the cleavages of PARP and caspase 3 induced by ursolic acid in HepG2 cells.", "entity1": "caspase 3", "entity2": "SB216763", "span1": [100, 109], "span2": [57, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"10277": {"label": 8, "data": {"text": "The outflow of [3H]-MPP+ was significantly enhanced by MPP+, guanidine, choline and amantadine as potential substrates for OCT-related transmembrane transporters.", "entity1": "transmembrane transporters", "entity2": "amantadine", "span1": [135, 161], "span2": [84, 94]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"5933": {"label": 3, "data": {"text": "Cyproterone acetate, a progestin used in the treatment of hirsutism, acne and prostate cancer as well as norgestrel and norethindrone that are widely used as oral contraceptives also inhibit 3 beta-HSD activity at Ki values of 1.5, 1.7 and 2.5 microM, respectively.", "entity1": "3 beta-HSD", "entity2": "Cyproterone acetate", "span1": [191, 201], "span2": [0, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5298": {"label": 1, "data": {"text": "In addition, prunetin inhibits NF-\u03baB-dependent inflammatory responses by modulating I\u03baB kinase (IKK)-inhibitor \u03baB\u03b1 (I\u03baB\u03b1)-NF-\u03baB signaling.", "entity1": "I\u03baB kinase", "entity2": "prunetin", "span1": [84, 94], "span2": [13, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12165": {"label": 3, "data": {"text": "Moreover, minocycline efficiently suppressed the release of cytochrome c from mitochondria of the liver tissues from Jo2-challenged mice.", "entity1": "cytochrome c", "entity2": "minocycline", "span1": [60, 72], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8214": {"label": 3, "data": {"text": "TAA also increased the numbers of ED2(+), cyclooxygenase-2(+), and heme oxygenase-1(+) liver cells, as well as the number of CD3(+) lymphocytes.", "entity1": "heme oxygenase-1", "entity2": "TAA", "span1": [67, 83], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1186": {"label": 4, "data": {"text": "Bovine tracheal smooth muscle strips were incubated with 10 microM fenoterol or vehicle for various periods of time (5, 30 min, 18 h) at 37 degrees C. After extensive washout (3 h, 37 degrees C), isometric contractions were measured to the full muscarinic receptor agonist methacholine, the partial muscarinic receptor agonist 4-(m-chlorophenyl-carbamoyloxy)-2-butynyltrimethylammonium (McN-A-343) and histamine.", "entity1": "muscarinic receptor", "entity2": "4-(m-chlorophenyl-carbamoyloxy)-2-butynyltrimethylammonium", "span1": [299, 318], "span2": [327, 385]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1300": {"label": 3, "data": {"text": "This study was conducted in order to understand the association between acute renal failure and the two COX-2 inhibitors celecoxib and rofecoxib.", "entity1": "COX-2", "entity2": "rofecoxib", "span1": [104, 109], "span2": [135, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3225": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "quercetin", "span1": [286, 296], "span2": [160, 169]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10146": {"label": 8, "data": {"text": "Non-steroidal anti-inflammatory drugs (NSAIDs) are competitive inhibitors of cyclooxygenase (COX), the enzyme that mediates biosynthesis of prostaglandins and thromboxanes from arachidonic acid.", "entity1": "COX", "entity2": "thromboxanes", "span1": [93, 96], "span2": [159, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9978": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "alpha-monofluoromethyldopa", "span1": [80, 84], "span2": [136, 162]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12459": {"label": 2, "data": {"text": "This report concerns the marked up-regulation in differentiated CaCo-2 colonic epithelial cells of two key inflammatory interleukins, IL-6 and IL-8, caused by a mixture of oxysterols representative of a high cholesterol diet.", "entity1": "IL-6", "entity2": "cholesterol", "span1": [134, 138], "span2": [208, 219]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15233": {"label": 3, "data": {"text": "In overexpressing cell lines, OATP1B1- and OATP1B3-mediated estradiol-17\u03b2-glucuronide uptake and OATP2B1-mediated estrone-3-sulfate uptake were inhibited by most of the silymarin flavonolignans investigated.", "entity1": "OATP2B1", "entity2": "flavonolignans", "span1": [97, 104], "span2": [179, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2037": {"label": 8, "data": {"text": "L-serine dehydratase (SDH), a member of the beta-family of pyridoxal phosphate-dependent (PLP) enzymes, catalyzes the deamination of L-serine and L-threonine to yield pyruvate or 2-oxobutyrate.", "entity1": "L-serine dehydratase", "entity2": "2-oxobutyrate", "span1": [0, 20], "span2": [179, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2963": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "H613A", "entity2": "cGMP", "span1": [71, 76], "span2": [23, 27]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5946": {"label": 1, "data": {"text": "Pimozide and thioridazine had no effect on the estradiol binding properties of the MCF-7 ER, nor did pimozide interfere with the induction of progesterone receptors by estradiol.", "entity1": "ER", "entity2": "estradiol", "span1": [89, 91], "span2": [47, 56]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3811": {"label": 0, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "AngII", "entity2": "Gln", "span1": [66, 71], "span2": [51, 54]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7784": {"label": 2, "data": {"text": "We also investigated the epigenetic status of NIS promoter after PJ34 treatment in TPC1 cell line: in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3), surprisingly we observed also an increase of H3K27me3, a classical repressive mark.", "entity1": "H3K4me3", "entity2": "PJ34", "span1": [179, 186], "span2": [65, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15883": {"label": 2, "data": {"text": "Our study revealed that high glucose/Fe concentrations in MIN6 cells induced an increase of the Bcl2/Bax ratio, an indicator of increased cell apoptosis.", "entity1": "Bax", "entity2": "glucose", "span1": [101, 104], "span2": [29, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6891": {"label": 8, "data": {"text": "NPC1L1 could recently be identified as a major sterol transporter for the intestinal uptake of cholesterol as well as plant sterols.", "entity1": "NPC1L1", "entity2": "cholesterol", "span1": [0, 6], "span2": [95, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9087": {"label": 1, "data": {"text": "These multiple affinity states of receptor in the hybrid cells are agonist-specific, and the percentage of total opiate receptor in high affinity state is relatively constant in various concentrations of Na+.", "entity1": "opiate receptor", "entity2": "Na+", "span1": [113, 128], "span2": [204, 207]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5163": {"label": 8, "data": {"text": "We examined the N-demethylation of individual ketamine enantiomers using human liver microsomes (HLMs) genotyped for the CYP2B6*6 allele, insect cell expressed recombinant CYP2B6 and CYP3A4 enzymes and COS-1 cell expressed recombinant CYP2B6.1 and CYP2B6.6 protein variant.", "entity1": "CYP2B6*6", "entity2": "ketamine", "span1": [121, 129], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14200": {"label": 1, "data": {"text": "Moreover, we investigated the roles of CHOP in cell survival under condition of SU5416 treatment in FRO ATC cells.", "entity1": "CHOP", "entity2": "SU5416", "span1": [39, 43], "span2": [80, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5456": {"label": 2, "data": {"text": "Among these differentially expressed lncRNAs, the greatest change was noted for uc002mbe.2, which had more than 300 folds induction upon TSA treatment.", "entity1": "uc002mbe.2", "entity2": "TSA", "span1": [80, 90], "span2": [137, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11405": {"label": 1, "data": {"text": "Here, we show that meclofenamic acid (meclofenamate) and diclofenac, two related molecules previously used as anti-inflammatory drugs, act as novel KCNQ2/Q3 channel openers.", "entity1": "KCNQ2/Q3", "entity2": "diclofenac", "span1": [148, 156], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5425": {"label": 2, "data": {"text": "Additionally, MPTP significantly down-regulated Bcl-2 expression in the mitochondria of dopaminergic cells in the SN, followed by an increase in Bax expression, cytochrome C translocation to the cytosol, andcleaved-caspase-3 expression, whereas these were inhibited by CRE or EB treatment.", "entity1": "caspase-3", "entity2": "MPTP", "span1": [215, 224], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11840": {"label": 1, "data": {"text": "These results suggest that the enantioselective disposition of sibutramine and its active metabolites are influenced by the altered genetic and environmental factors of CYP2B6 and CYP3A activity in vivo.", "entity1": "CYP3A", "entity2": "sibutramine", "span1": [180, 185], "span2": [63, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10435": {"label": 1, "data": {"text": "These characteristics of the bound PLP suggest that SDH catalysis is not facilitated by forming the resonance-stabilized structure of the PLP-Ser aldimine as seen in aminotransferases.", "entity1": "SDH", "entity2": "PLP", "span1": [52, 55], "span2": [35, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"3203": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "caffeic acid", "span1": [286, 296], "span2": [104, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3343": {"label": 1, "data": {"text": "The affinities of dfbp and dfbp-o for the regulatory domain of cTnC were measured in the absence and presence of cTnI by NMR spectroscopy, and dfbp-o was found to bind more strongly than dfbp.", "entity1": "cTnC", "entity2": "dfbp", "span1": [63, 67], "span2": [187, 191]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6932": {"label": 8, "data": {"text": "On the other hand, the FUM1 (fumarase) gene disrupted mutant produced significantly higher levels of fumarate but did not form malate at all.", "entity1": "FUM1", "entity2": "fumarate", "span1": [23, 27], "span2": [101, 109]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"14138": {"label": 3, "data": {"text": "Celastrol highlights the therapeutic potential of agents targeting TAK1 as a key node in this pro-oncogenic TGF-\u03b2-NF-\u03baB signal pathway.", "entity1": "TAK1", "entity2": "Celastrol", "span1": [67, 71], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"345": {"label": 3, "data": {"text": "Sodium salicylate and aspirin also inhibited NF-kappa B-dependent transcription from the Ig kappa enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells.", "entity1": "Ig kappa", "entity2": "aspirin", "span1": [89, 97], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4314": {"label": 5, "data": {"text": "Since the original discovery of azoles analogs as PXR antagonists, we have preliminarily defined an important PXR antagonist pharmacophore and developed less-toxic PXR antagonists.", "entity1": "PXR", "entity2": "azoles", "span1": [50, 53], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15670": {"label": 3, "data": {"text": "3-Hydroxypyridin-2-thione as Novel Zinc Binding Group for Selective Histone Deacetylase Inhibition.", "entity1": "Histone Deacetylase", "entity2": "3-Hydroxypyridin-2-thione", "span1": [68, 87], "span2": [0, 25]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9104": {"label": 8, "data": {"text": "In contrast to diethylcarbamazine, piriprost (U-60,257; 6,9-deepoxy-6,9-(phenylimino)-delta 6,8-prostaglandin I1), which inhibits the formation of sulfidopeptide leuktrienes in RBL cells at the 5-lipoxygenase step (EC50 5 microM), did not inhibit the leukotriene synthetase of these cells.", "entity1": "5-lipoxygenase", "entity2": "sulfidopeptide leuktrienes", "span1": [194, 208], "span2": [147, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6406": {"label": 3, "data": {"text": "In a physiological K(+) gradient, TWIK-2 is half inhibited by 0.1 mm Ba(2+), quinine, and quinidine.", "entity1": "TWIK-2", "entity2": "quinidine", "span1": [34, 40], "span2": [90, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13291": {"label": 1, "data": {"text": "Sorafenib (BAY43-9006, Nexavar) is a small molecule B-RAF inhibitor that is used for the treatment of renal cell carcinoma, and has been shown to have activity against receptor tyrosine kinases from the platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR) families.", "entity1": "vascular endothelial growth factor receptor", "entity2": "BAY43-9006", "span1": [255, 298], "span2": [11, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15580": {"label": 9, "data": {"text": "We also rescued RO3306-resistant clones using exogenous Cdk1 without inhibitory phosphorylation sites, indicating that the mitotic surge of Cdk1 activity is dispensable for cell proliferation.", "entity1": "Cdk1", "entity2": "RO3306", "span1": [56, 60], "span2": [16, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13501": {"label": 1, "data": {"text": "In this study the neuromuscular blocking drug vecuronium and the controls gallamine and pancuronium slowed the rate of atropine induced [(3)H]N-methylscopolamine dissociation from Chinese hamster ovary cells expressing recombinant human muscarinic M2 receptors K(off) values min(-1); vecuronium (125 nM), atropine 0.45+/-0.07+blocker 0.04+/-0.02; gallamine (21 nM), atropine 0.42+/-0.05+blocker 0.15+/-0.04; pancuronium(21 nM), atropine 0.36+/-0.03+blocker 0.03+/-0.01).", "entity1": "human muscarinic M2 receptors", "entity2": "[(3)H]N-methylscopolamine", "span1": [231, 260], "span2": [136, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6698": {"label": 4, "data": {"text": "The Ca(2+) response of hVR1-transfected HEK293 cells to the endogenous VR1 agonist N-arachidonoyl-dopamine was potentiated by low pH.", "entity1": "VR1", "entity2": "N-arachidonoyl-dopamine", "span1": [71, 74], "span2": [83, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9998": {"label": 8, "data": {"text": "OBJECTIVES: The hypothesis of the present study was that differences among dopamine transporter (DAT) ligands in potency and effectiveness as a positive reinforcers were related to potency and effectiveness as DA uptake inhibitors.", "entity1": "DAT", "entity2": "DA", "span1": [97, 100], "span2": [210, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"102": {"label": 5, "data": {"text": "The memory-improving effect of minaprine on cycloheximide-induced amnesia was potentiated by a selective 5-HT2 antagonist, ritanserin.", "entity1": "5-HT2", "entity2": "ritanserin", "span1": [105, 110], "span2": [123, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7116": {"label": 0, "data": {"text": "This indicated that the N-terminal 46 amino acids in GAF-B are required for high vardenafil potency.", "entity1": "GAF-B", "entity2": "N", "span1": [53, 58], "span2": [24, 25]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14280": {"label": 8, "data": {"text": "The rCYP data was normalized relative to the levels of each CYP form in native human liver microsomes to better assess the contribution of each rCYP in the metabolism of elzasonan.", "entity1": "rCYP", "entity2": "elzasonan", "span1": [144, 148], "span2": [170, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"527": {"label": 2, "data": {"text": "By reporter gene analysis following transient transfections with various plasmids expressing a dominant negative mutant form of Cdc42, Rac1 or RhoA, C2-ceramide-induced SRE activation was shown to be selectively repressed by pEXV-RacN17 encoding a dominant negative mutant of Rac1, suggesting that Rac activity is essential for the signalling cascade of ceramide to the nucleus.", "entity1": "SRE", "entity2": "C2-ceramide", "span1": [169, 172], "span2": [149, 160]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16035": {"label": 3, "data": {"text": "Haloperidol promotes mTORC1-dependent phosphorylation of ribosomal protein S6 via dopamine- and cAMP-regulated phosphoprotein of 32 kDa and inhibition of protein phosphatase-1.", "entity1": "protein phosphatase-1", "entity2": "Haloperidol", "span1": [154, 175], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12590": {"label": 1, "data": {"text": "The complex patterns of sensitivity to cyclothiazide seen in hippocampal neurons could be reconstituted by assembly of recombinant AMPA receptor subunits generated from cDNAs encoding the flip (i) and flop (o) splice variants of the GluR-A and GluR-B subunits.", "entity1": "GluR-A", "entity2": "cyclothiazide", "span1": [233, 239], "span2": [39, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2787": {"label": 2, "data": {"text": "To determine whether H(2)S itself provoked inflammation in acinar cells, the cells were treated with H(2)S donor drug, sodium hydrosulphide (NaHS), (10, 50 and 100 muM), that resulted in a significant increase in SP concentration and expression of PPT-A and NK1-R in acinar cells.", "entity1": "SP", "entity2": "sodium hydrosulphide", "span1": [213, 215], "span2": [119, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14008": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "KIT", "entity2": "XL184", "span1": [244, 247], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12697": {"label": 8, "data": {"text": "Most halogenated cysteine S-conjugates are metabolized by cysteine S-conjugate beta-lyases to pyruvate, ammonia, and an alpha-chloroenethiolate (with DCVC) or an alpha-difluoroalkylthiolate (with TFEC) that may eliminate halide to give a thioacyl halide, which reacts with epsilon-amino groups of lysine residues in proteins.", "entity1": "beta-lyases", "entity2": "ammonia", "span1": [79, 90], "span2": [104, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"63": {"label": 3, "data": {"text": "Enalkiren (A-64662), a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen.", "entity1": "human renin", "entity2": "dipeptide", "span1": [93, 104], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"618": {"label": 3, "data": {"text": "Likewise, IL-2 steady-state mRNA expression was inhibited by both PLA2 inhibitors in a concentration-dependent fashion with > 90% inhibition at 1 microM BPB and 20 microM AACOCF3.", "entity1": "IL-2", "entity2": "AACOCF3", "span1": [10, 14], "span2": [171, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13153": {"label": 0, "data": {"text": "We have previously demonstrated that phosphorylation of Fas-associated death domain-containing protein (FADD) at 194 serine through c-jun NH2-terminal kinase (JNK) activation sensitizes breast cancer cells to chemotherapy through accelerating cell cycle arrest at G2/M, and that Bcl-2 phosphorylation downstream of JNK/FADD plays an important role in cell growth suppression by paclitaxel.", "entity1": "FADD", "entity2": "serine", "span1": [104, 108], "span2": [117, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1533": {"label": 3, "data": {"text": "However, topiramate at low concentrations causes slow inhibition of GluR5 kainate receptor-mediated synaptic currents in the basolateral amygdala, indicating that it may protect against seizures, at least in part, through suppression of GluR5 kainate receptor responses.", "entity1": "GluR5", "entity2": "topiramate", "span1": [68, 73], "span2": [9, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1255": {"label": 3, "data": {"text": "In human blood, the tested glucocorticoids beclomethasone, dexamethasone and fluticasone inhibited the LPS induced TNF release potently in a concentration dependent manner, whereas in dispersed human nasal polyp cells, the effect of the glucocorticoids on allergically induced TNF release, with the exception of dexamethasone, was much less pronounced.", "entity1": "TNF", "entity2": "dexamethasone", "span1": [277, 280], "span2": [59, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5233": {"label": 1, "data": {"text": "Treatment of C57 BL/6 mice with bleomycin increased fibroblast viability and collagen production and significantly downregulated Nrf2.", "entity1": "collagen", "entity2": "bleomycin", "span1": [77, 85], "span2": [32, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"836": {"label": 3, "data": {"text": "One of the mechanism of mifepristone action on decreasing leiomyomata volume may be related to suppression on expression of PR gene.", "entity1": "PR gene", "entity2": "mifepristone", "span1": [124, 131], "span2": [24, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12429": {"label": 8, "data": {"text": "These studies show that CYP3A4 and CYP3A5 metabolize BDP to inactive metabolites and suggest that differences in the expression or function of these enzymes in the lung and/or liver could influence BDP disposition in humans.", "entity1": "CYP3A5", "entity2": "BDP", "span1": [35, 41], "span2": [53, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5265": {"label": 1, "data": {"text": "Quinone compounds regulate the level of ROS production by the NADPH oxidase Nox4.", "entity1": "NADPH oxidase", "entity2": "Quinone", "span1": [62, 75], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13318": {"label": 5, "data": {"text": "Exposure to mifepristone (a glucocorticoid receptor antagonist), but not spironolactone (a mineralocorticoid receptor antagonist), precluded both the corticosteroid-induced elevation in amiloride-sensitive I(sc) and the induced changes in beta- and gamma-ENaC mRNA.", "entity1": "mineralocorticoid receptor", "entity2": "spironolactone", "span1": [91, 117], "span2": [73, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13918": {"label": 3, "data": {"text": "Phenformin but not metformin inhibits a number of variants of K(ATP) including the cloned equivalents of currents present in vascular and non-vascular smooth muscle (Kir6.1/SUR2B and Kir6.2/SUR2B) and pancreatic beta-cells (Kir6.2/SUR1).", "entity1": "SUR2B", "entity2": "Phenformin", "span1": [190, 195], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"545": {"label": 1, "data": {"text": "The selective 5-HT reuptake inhibitors paroxetine, indalpine and fluvoxamine displayed a high affinity for the 5-HT transporter, whereas the norepinephrine reuptake inhibitor desipramine had a high affinity for the norepinephrine transporter.", "entity1": "5-HT transporter", "entity2": "paroxetine", "span1": [111, 127], "span2": [39, 49]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5464": {"label": 4, "data": {"text": "In the DRN, brexpiprazole completely inhibited the firing of 5-HT neurons via 5-HT1A agonism and was more potent than aripiprazole (ED50 = 230 and 700 mug/kg, respectively).", "entity1": "5-HT1A", "entity2": "brexpiprazole", "span1": [78, 84], "span2": [12, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6609": {"label": 3, "data": {"text": "Thus, the current study suggests that coadministration of clinical doses of promethazine and homochlorcyclizine increases the Css of haloperidol and reduced haloperidol via the inhibitory effects on the CYP2D6-catalyzed metabolism of haloperidol and reduced haloperidol.", "entity1": "CYP2D6", "entity2": "promethazine", "span1": [203, 209], "span2": [76, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13600": {"label": 5, "data": {"text": "Using hNET in transfected human embryonic kidney-293 cells, this difference in potency for DVS at sites labeled by [(3)H]NIS was found to distinguish DVS, the DVS analog rac-(1-[1-(3-chloro-phenyl)-2-(4-methylpiperazin-1-yl)-ethyl]cyclohexanol (WY-46824), methylphenidate, and the cocaine analog 3beta-(4-iodophenyl)tropane-2beta-carboxylic acid methyl ester (RTI-55) from other hNET antagonists, such as NIS, mazindol, tricyclic antidepressants, and cocaine.", "entity1": "hNET", "entity2": "cocaine", "span1": [379, 383], "span2": [451, 458]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6799": {"label": 3, "data": {"text": "After 12 months of treatment, carvedilol significantly improved all end points (plasma concentration of B-type natriuretic peptide [BNP] from 175 (35 to 209) to 106 (52 to 160) pg/ml, mean (95% confidence interval) p <0.01; New York Heart Association functional class from 2.37 (2.13 to 2.61) to 1.56 (1.21 to 1.91), p <0.01; exercise capacity estimated with the Specific Activity Scale from 4.75 (4.50 to 5.00) to 5.68 (5.22 to 6.14) METs, p <0.02), whereas conventional therapy did not (plasma BNP concentration from 150 (114 to 186) to 174 (100 to 248) pg/ml; New York Heart Association functional class from 2.29 (2.08 to 2.50) to 2.11 (1.73 to 2.49); exercise capacity from 4.57 (4.34 to 4.80) to 4.72 (4.41 to 5.03) METs).", "entity1": "BNP", "entity2": "carvedilol", "span1": [132, 135], "span2": [30, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13971": {"label": 3, "data": {"text": "METHODS: We conducted a case-control study to measure the association between selective cox-2 inhibitors, particularly celecoxib, rofecoxib, valdecoxib and non-specific NSAID subgroups, and breast cancer risk.", "entity1": "cox-2", "entity2": "valdecoxib", "span1": [88, 93], "span2": [141, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8177": {"label": 8, "data": {"text": "This leads to decreased expression of glutamate aspartate transporter, which in turn reduces glutamate transport.", "entity1": "glutamate aspartate transporter", "entity2": "glutamate", "span1": [38, 69], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"13626": {"label": 3, "data": {"text": "Based on the results from those studies, we concluded that rasagiline PO QD, at the therapeutic dosage range of 0.5 to 1 rag/d, is effective and well tolerated and completely, selectively, and specifically inhibited MAO-B.", "entity1": "MAO-B", "entity2": "rasagiline", "span1": [216, 221], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4450": {"label": 5, "data": {"text": "A novel class of quinoxalines has been discovered as antagonists of the IgG:FcRn protein-protein interaction through optimization of a hit derived from a virtual ligand-based screen.", "entity1": "FcRn", "entity2": "quinoxalines", "span1": [76, 80], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5517": {"label": 3, "data": {"text": "The acute toxicity of organophosphorus (OP) compounds in mammals is due to their irreversible inhibition of acetylcholinesterase (AChE) in the nervous system, which leads to increased synaptic acetylcholine levels.", "entity1": "acetylcholinesterase", "entity2": "OP", "span1": [108, 128], "span2": [40, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2172": {"label": 1, "data": {"text": "Drug binding interactions in the inner cavity of HERG channels: molecular insights from structure-activity relationships of clofilium and ibutilide analogs.", "entity1": "HERG", "entity2": "clofilium", "span1": [49, 53], "span2": [124, 133]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1131": {"label": 3, "data": {"text": "The antipsychotic drugs sertindole and pimozide are known to prolong the QT interval on the electrocardiogram via a high affinity block of the cardiac K(+) channel known as HERG (human ether-a-go-go-related gene; erg1).", "entity1": "erg1", "entity2": "sertindole", "span1": [213, 217], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1893": {"label": 1, "data": {"text": "Characterization of the interaction of ingenol 3-angelate with protein kinase C.", "entity1": "protein kinase C", "entity2": "ingenol 3-angelate", "span1": [63, 79], "span2": [39, 57]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3758": {"label": 3, "data": {"text": "The results demonstrated that \u03b2-ionone-induced apoptosis in a dose-dependent manner in SGC-7901 cells treated with \u03b2-ionone (25, 50, 100 and 200\u00a0\u03bcmol/L) for 24\u00a0h. \u03b2-ionone was also shown to induce the expression of cleaved-caspase-3 and inhibit bcl-2 expression in SGC-7901 cells in a dose-dependent manner.", "entity1": "bcl-2", "entity2": "\u03b2-ionone", "span1": [245, 250], "span2": [163, 171]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3645": {"label": 1, "data": {"text": "In rats exposed to DBDCT, apoptosis was also observed in brain, as shown by the detection of cleaved caspase-9 and caspase-3 proteins and increased TUNEL positive staining.", "entity1": "caspase-9", "entity2": "DBDCT", "span1": [101, 110], "span2": [19, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10465": {"label": 3, "data": {"text": "Ras-CM and TGF-alpha also increase PI3-K activity downstream of the EGFR and increase postradiation survival, both of which are abrogated by GW572016.", "entity1": "PI3-K", "entity2": "GW572016", "span1": [35, 40], "span2": [141, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10196": {"label": 3, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP8", "entity2": "rifampicin", "span1": [48, 53], "span2": [15, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14002": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "kinase", "entity2": "XL184", "span1": [41, 47], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6903": {"label": 2, "data": {"text": "In vitro studies demonstrated that the retinoid X receptor (RXR) retinoid, bexarotene, at biologically relevant concentrations of 10(-6) M to 10(-8) M, upregulated both the p55 and p75 subunits of the IL-2R and enhanced 5- to 10-fold the susceptibility of T-cell leukemia cells to denileukin diftitox.", "entity1": "p75", "entity2": "bexarotene", "span1": [181, 184], "span2": [75, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8383": {"label": 3, "data": {"text": "The obtained results showed that Cd increased lipid peroxidation and abnormal sperm count and decreased plasma testosterone, lactate dehydrogenase, acid phosphatase, alkaline phosphatase and testicular steroidogenic enzymes: 3\u03b2-hydroxysteroid dehydrogenase (HSD), 17\u03b2-HSD activities as well as epididymal sperm counts and motility, while RUT and Se treatment reversed this change to control values.", "entity1": "testicular steroidogenic enzymes", "entity2": "Cd", "span1": [191, 223], "span2": [33, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"354": {"label": 2, "data": {"text": "These nonadrenoceptor binding sites may explain certain novel platelet aggregatory properties previously ascribed to clonidine and endogenous clonidine-displacing substance(s), and may serve as markers of imidazoline receptors in humans.", "entity1": "imidazoline receptors", "entity2": "clonidine", "span1": [205, 226], "span2": [117, 126]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3054": {"label": 3, "data": {"text": "Plerixafor (AMD3100, Genzyme Corporation) is a bicyclam molecule that antagonizes the binding of the chemokine stromal cell-derived factor-1 (SDF-1) to its cognate receptor CXCR4.", "entity1": "chemokine", "entity2": "Plerixafor", "span1": [101, 110], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1832": {"label": 3, "data": {"text": "Reciprocally, glyburide blocked SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC(50) approximately 275-300 microM).", "entity1": "ABCA1", "entity2": "glyburide", "span1": [132, 137], "span2": [14, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14090": {"label": 1, "data": {"text": "Our studies demonstrate that thalidomide, lenalidomide and another immunomodulatory drug, pomalidomide, bound endogenous CRBN and recombinant CRBN-DNA damage binding protein-1 (DDB1) complexes.", "entity1": "DNA damage binding protein-1", "entity2": "pomalidomide", "span1": [147, 175], "span2": [90, 102]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13646": {"label": 1, "data": {"text": "We report that mutation of this conserved Gly in yeast Top1p alters enzyme sensitivity to CPT.", "entity1": "yeast Top1p", "entity2": "CPT", "span1": [49, 60], "span2": [90, 93]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9696": {"label": 1, "data": {"text": "Comparison of the novel antipsychotic ziprasidone with clozapine and olanzapine: inhibition of dorsal raphe cell firing and the role of 5-HT1A receptor activation.", "entity1": "5-HT1A receptor", "entity2": "olanzapine", "span1": [136, 151], "span2": [69, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6828": {"label": 3, "data": {"text": "MATERIALS AND METHODS: Seeking to improve efficacy against otherwise intractable end-stage pancreatic islet tumors, two receptor tyrosine kinase inhibitors, imatinib and SU11248, were used to disrupt PDGFR-mediated pericyte support of tumor endothelial cells in concert with maximum-tolerated dose (MTD) or metronomic chemotherapy and/or VEGFR inhibition.", "entity1": "PDGFR", "entity2": "imatinib", "span1": [200, 205], "span2": [157, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12339": {"label": 1, "data": {"text": "In sum, identification of PIM-1 as an ER\u03b1 target gene adds a novel potential mechanism by which estrogens can contribute to breast cancer cell proliferation and carcinogenesis.", "entity1": "ER\u03b1", "entity2": "estrogens", "span1": [38, 41], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2247": {"label": 3, "data": {"text": "BACKGROUND: Since the introduction of the first cholinesterase inhibitor (ChEI) in 1997, most clinicians and probably most patients would consider the cholinergic drugs, donepezil, galantamine and rivastigmine, to be the first line pharmacotherapy for mild to moderate Alzheimer's disease.The drugs have slightly different pharmacological properties, but they all work by inhibiting the breakdown of acetylcholine, an important neurotransmitter associated with memory, by blocking the enzyme acetylcholinesterase.", "entity1": "acetylcholinesterase", "entity2": "galantamine", "span1": [492, 512], "span2": [181, 192]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5939": {"label": 3, "data": {"text": "Inhibitory effect of synthetic progestins, 4-MA and cyanoketone on human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase activity.", "entity1": "human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene-isomerase", "entity2": "cyanoketone", "span1": [67, 139], "span2": [52, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3204": {"label": 3, "data": {"text": "Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids.", "entity1": "mammalian isoforms I-XIV", "entity2": "polyphenols", "span1": [14, 38], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6707": {"label": 3, "data": {"text": "The inhibitory effects of tranylcypromine, a nonselective irreversible inhibitor of monoamine oxidase (MAO), on three cytochrome P450 (CYP) enzymes, namely CYP2C9, CYP2C19, and CYP2D6, have been evaluated in vitro.", "entity1": "MAO", "entity2": "tranylcypromine", "span1": [103, 106], "span2": [26, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2171": {"label": 0, "data": {"text": "Binding sites for hERG blockers have been mapped within the inner cavity of the channel and include aromatic residues in the S6 helix (Tyr-652, Phe-656) and residues in the pore helix (Thr-623, Ser-624, Val-625).", "entity1": "hERG", "entity2": "Thr", "span1": [18, 22], "span2": [185, 188]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7672": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "EC 4.2.1.1", "entity2": "Thiazide", "span1": [117, 127], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9552": {"label": 1, "data": {"text": "In addition, the betaAR-mediated inhibition of IFN-gamma, GM-CSF, and IL-3 mRNA accumulation and GM-CSF protein secretion were related to the accumulation of intracellular cyclic adenosine monophosphate (cAMP) levels.", "entity1": "GM-CSF", "entity2": "cAMP", "span1": [97, 103], "span2": [204, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16060": {"label": 8, "data": {"text": "Drug-drug interactions are dependent on statins' pharmacokinetic profile: simvastatin, lovastatin and atorvastatin are metabolized through cytochrome P450 (CYP) 3A, while the metabolism of the other statins is independent of this CYP.", "entity1": "cytochrome P450 (CYP) 3A", "entity2": "lovastatin", "span1": [139, 163], "span2": [87, 97]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13999": {"label": 3, "data": {"text": "Cabozantinib (XL184) is a small-molecule kinase inhibitor with potent activity toward MET and VEGF receptor 2 (VEGFR2), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3.", "entity1": "KIT", "entity2": "Cabozantinib", "span1": [244, 247], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5107": {"label": 2, "data": {"text": "Further, 5HHMF increased specific DNA-binding activity of Nrf2, and transient knockdown with Nrf2 siRNA subsequently reversed 5HHMF-induced NO inhibition, which was followed by suppression of HO-1 activity.", "entity1": "Nrf2", "entity2": "5HHMF", "span1": [58, 62], "span2": [9, 14]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6415": {"label": 2, "data": {"text": "Peroxisome proliferator-activated receptor alpha (PPARalpha) activators, bezafibrate and Wy-14,643, increase uncoupling protein-3 mRNA levels without modifying the mitochondrial membrane potential in primary culture of rat preadipocytes.", "entity1": "PPARalpha", "entity2": "Wy-14,643", "span1": [50, 59], "span2": [89, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9258": {"label": 3, "data": {"text": "Ergot alkaloids were also effective in inhibiting VIP-stimulated cyclic AMP production, with EC50 values for ergovaline, ergonovine, alpha-ergocryptine, ergotamine, and dopamine of 8 +/- 2, 47 +/- 2, 28 +/- 2, 2 +/- 1, and 8 +/- 1 nM, respectively.", "entity1": "VIP", "entity2": "Ergot alkaloids", "span1": [50, 53], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5924": {"label": 1, "data": {"text": "Stoichiometry of estramustine phosphate binding to MAP2 measured by the disassembly of chick brain MAP2:tubulin microtubules.", "entity1": "MAP2", "entity2": "estramustine phosphate", "span1": [51, 55], "span2": [17, 39]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7320": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "ASCT2", "entity2": "amino acids", "span1": [247, 252], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7231": {"label": 2, "data": {"text": "GnRH-induced c-Src activation resulted in the phosphorylation of expressed Hic-5 and promoted its association with the human androgen receptor.", "entity1": "c-Src", "entity2": "GnRH", "span1": [13, 18], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11653": {"label": 1, "data": {"text": "The effects of CDCA and GW4064 on expression of Cdx2 and MUC2 were abolished by guggulsterone.", "entity1": "Cdx2", "entity2": "GW4064", "span1": [48, 52], "span2": [24, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4988": {"label": 3, "data": {"text": "Crocin (25 and 50mg/kg) or vitamin E improved histopathological damages, decreased MDA and CK-MB, increased GSH content and attenuated the increase of Bax/Bcl2 ratio, activation of caspase 3 and release of cytochrome c to the cytosol induced by DZN.", "entity1": "Bcl2", "entity2": "vitamin E", "span1": [155, 159], "span2": [27, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10468": {"label": 4, "data": {"text": "(-)-Isoprenaline and a nonconventional beta(3)-adrenoceptor agonist, (+/-)-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimida zol-2-one] hydrochloride ((+/-)-CGP12177A), induced concentration-dependent relaxation of (-)-phenylephrine (0.3 microM) preconstricted spiral preparations.", "entity1": "beta(3)-adrenoceptor", "entity2": "(+/-)-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-1,3-dihydro-2H-benzimida zol-2-one] hydrochloride", "span1": [39, 59], "span2": [69, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6875": {"label": 3, "data": {"text": "Also, prophylactic, as well as therapeutic, treatment with the CSE inhibitor, DL-propargylglycine (PAG), significantly reduced the severity of caerulein-induced pancreatitis and associated lung injury, as determined by 1) hyperamylasemia [plasma amylase (U/L) (control, 1204+/-59); prophylactic treatment: placebo, 10635+/-305; PAG, 7904+/-495; therapeutic treatment: placebo, 10427+/-470; PAG, 7811+/-428; P<0.05 PAG c.f.", "entity1": "CSE", "entity2": "PAG", "span1": [63, 66], "span2": [99, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3820": {"label": 0, "data": {"text": "The nucleotide sequence of HmTx contains 649 bp, and the mature protein is predicted to have 131 amino acid residues-104 of which make up the large subunit, and 27 of which make up the small subunit.", "entity1": "HmTx", "entity2": "nucleotide", "span1": [27, 31], "span2": [4, 14]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9151": {"label": 9, "data": {"text": "Co-incubation with human serum albumin or poly-L-lysine but not lysine protected human and hamster LDH-X from gossypol.", "entity1": "human and hamster LDH-X", "entity2": "lysine", "span1": [81, 104], "span2": [64, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9926": {"label": 1, "data": {"text": "The finding that arachidonate can also induce a conformational change in PGHS-2 was unexpected, and the magnitude of changes suggests this structural flexibility may be integral to the cyclooxygenase catalytic mechanism.", "entity1": "cyclooxygenase", "entity2": "arachidonate", "span1": [185, 199], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7454": {"label": 3, "data": {"text": "Female mice express higher levels of glutaredoxin in certain CNS regions and downregulation of glutaredoxin using antisense oligonucleotides sensitizes them to L-BOAA toxicity seen as mitochondrial complex I loss.", "entity1": "mitochondrial complex I", "entity2": "L-BOAA", "span1": [184, 207], "span2": [160, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5737": {"label": 3, "data": {"text": "Taken together, our results suggested that Rg1 protected against A\u03b225-35-induced apoptosis at least in part by two complementary GR-dependent ERK phosphorylation pathways: (1) down-regulating HIF-1\u03b1 initiated protein nitrotyrosination, and (2) inhibiting mitochondrial apoptotic cascades.", "entity1": "HIF-1\u03b1", "entity2": "Rg1", "span1": [192, 198], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11638": {"label": 8, "data": {"text": "Risperidone is metabolized to its active metabolite, 9-hydroxyrisperidone, mainly by the cytochrome P450 enzymes CYP2D6 and 3A4.", "entity1": "cytochrome P450", "entity2": "9-hydroxyrisperidone", "span1": [89, 104], "span2": [53, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10382": {"label": 3, "data": {"text": "Investigation of bradykinin metabolism in human and rat plasma in the presence of the dual ACE/NEP inhibitors GW660511X and omapatrilat.", "entity1": "ACE", "entity2": "GW660511X", "span1": [91, 94], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14589": {"label": 3, "data": {"text": "Although treatment with 17-AAG reduced AhR levels and AhR-regulated gene expression in lung AD cells, AhR expression increased anticancer activity of 17-AAG.", "entity1": "AhR", "entity2": "17-AAG", "span1": [39, 42], "span2": [24, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6236": {"label": 1, "data": {"text": "Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.", "entity1": "5-HT receptor", "entity2": "eletriptan", "span1": [24, 37], "span2": [57, 67]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12737": {"label": 3, "data": {"text": "The observation that Ras-transformed cells can be sensitized to killing by ionizing radiation with GW572016 demonstrates that EGFR KIs could potentially be used to radiosensitize tumors in which radioresistance is dependent on Ras-driven autocrine signaling through EGFR.", "entity1": "Ras", "entity2": "GW572016", "span1": [21, 24], "span2": [99, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"342": {"label": 3, "data": {"text": "Sodium salicylate and aspirin also inhibited NF-kappa B-dependent transcription from the Ig kappa enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells.", "entity1": "NF-kappa B", "entity2": "Sodium salicylate", "span1": [45, 55], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15746": {"label": 1, "data": {"text": "Thus, CYP2E1-mediated ethanol hepatotoxicity was alleviated by quercetin through HO-1 induction.", "entity1": "CYP2E1", "entity2": "ethanol", "span1": [6, 12], "span2": [22, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3832": {"label": 3, "data": {"text": "In combination with clofarabine, the ability of resveratrol to reduce the contents of Sp1 and its target gene products was also evident in a time- and dose-dependent experiment.", "entity1": "Sp1", "entity2": "resveratrol", "span1": [86, 89], "span2": [48, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6071": {"label": 0, "data": {"text": "Degenerate oligonucleotides corresponding to conserved amino acids from transmembrane domains III, V, and VI of known receptors [5-HT1A, 5-HT1C, and 5-HT2; 5-HT is serotonin (5-hydroxytryptamine)] were used as primers for the sequential reactions.", "entity1": "5-HT1C", "entity2": "amino acids", "span1": [137, 143], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13529": {"label": 1, "data": {"text": "Moreover, the CDO active site is essentially unreactive toward NO in the absence of substrate, suggesting an obligate ordered binding of l-cysteine prior to NO.", "entity1": "CDO", "entity2": "NO", "span1": [14, 17], "span2": [157, 159]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10945": {"label": 1, "data": {"text": "These results provide biochemical evidence of a H(+)-coupled and saturable transport system, presumed to be a low-affinity monocarboxylate transporter MCT4 or other unknown H(+)H(+)-coupled monocarboxylate transport system, for nicotinate in rat cerebrocortical astrocytes.", "entity1": "H(+)-coupled monocarboxylate transport system", "entity2": "H(+)", "span1": [177, 222], "span2": [173, 177]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2560": {"label": 1, "data": {"text": "In randomized controlled trials, bisphosphonates (pamidronate and zoledronic acid) and selective estrogen receptor modulators (raloxifene and toremifene) increased bone mineral density in GnRH agonist-treated men.", "entity1": "estrogen receptor", "entity2": "toremifene", "span1": [97, 114], "span2": [142, 152]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 4, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13433": {"label": 2, "data": {"text": "TGF-beta1 and high D-glucose increased hCAT-1 mRNA expression ( approximately 8-fold) and maximal transport velocity (V(max)), L-[(3)H]citrulline formation from L-[(3)H]arginine (index of NO synthesis) and endothelial NO synthase (eNOS) protein abundance, but did not alter eNOS phosphorylation.", "entity1": "hCAT-1", "entity2": "D-glucose", "span1": [39, 45], "span2": [19, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, 9]},
	"927": {"label": 3, "data": {"text": "5-Fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd) and 5-trifluorothymidine (F3(d)Thd) are antimetabolites which are metabolized to their corresponding active forms which inhibit DNA synthesis via inhibition of thymidylate synthase (TS).", "entity1": "TS", "entity2": "5-FU", "span1": [238, 240], "span2": [16, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"819": {"label": 3, "data": {"text": "Prostaglandin E1, E2, STA2 (a stable analogue of thromboxane A2), 17-phenyl-trinor-PGE2 (an EP1-selective agonist) and sulprostone (an EP3-selective agonist) inhibited the HVA Ca2+ current (HVA ICa) dose-dependently, and the rank order of potency to inhibit HVA Ca2+ channels was sulprostone>PGE2, PGE1>STA2>>17-phenyl-trinor-PGE2.", "entity1": "HVA Ca2+ channels", "entity2": "17-phenyl-trinor-PGE2", "span1": [258, 275], "span2": [66, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2303": {"label": 9, "data": {"text": "Inhibition of ERK1/2 with U0126 induces apoptosis but fails to activate JNK phosphorylation or down-regulate beta-catenin protein expression.", "entity1": "beta-catenin", "entity2": "U0126", "span1": [109, 121], "span2": [26, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4627": {"label": 4, "data": {"text": "The results suggested that both the EtOAc extract and berberine were able to activate PPAR\u03b1/\u03b2/\u03b3, and Rhizoma Coptis contains potential natural agonists of PPARs besides berberine.", "entity1": "PPAR\u03b1/\u03b2/\u03b3", "entity2": "berberine", "span1": [86, 95], "span2": [54, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3190": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "CA", "entity2": "p-hydroxybenzoic acid", "span1": [282, 284], "span2": [64, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5726": {"label": 3, "data": {"text": "In patients who do not reach the LDL-C target, combination therapy with additional LDL-C lowering drugs (e.g. ezetimibe, bile acid sequestrants or fibrates) should be considered.", "entity1": "LDL", "entity2": "ezetimibe", "span1": [83, 86], "span2": [110, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15669": {"label": 3, "data": {"text": "Subsequent optimization led to several novel 3HPT-based HDACi that are selective for HDAC 6 and HDAC 8.", "entity1": "HDAC 8", "entity2": "3HPT", "span1": [96, 102], "span2": [45, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4908": {"label": 1, "data": {"text": "In the in vitro assay, kinsenoside (20 and 50\u03bcg/mL) markedly inhibited changes in various biochemical substances (nitric oxide (NO), lactic dehydrogenase (LDH), superoxide dismutase (SOD), and catalase (CAT)) in human umbilical vein endothelial cells (HUVECs) damaged by high glucose (35mM) and restored vascular endothelial structure by balancing the matrix metalloproteinases-the tissue inhibitors of matrix metalloproteinases (MMP-TIMP) system.", "entity1": "lactic dehydrogenase", "entity2": "glucose", "span1": [133, 153], "span2": [276, 283]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13511": {"label": 1, "data": {"text": "The results showed that all four calcium atoms exchanged per molecule of calmodulin.", "entity1": "calmodulin", "entity2": "calcium", "span1": [73, 83], "span2": [33, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12799": {"label": 1, "data": {"text": "STI 571 (imatinib mesylate [Gleevec]) might be an effective therapy in this case, since Gleevec targets both PDGFRA and c-kit oncoproteins.", "entity1": "PDGFRA", "entity2": "STI 571", "span1": [109, 115], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3723": {"label": 3, "data": {"text": "Furthermore, N-BPs decreased the levels of phosphorylated extracellular signal-regulated kinase (ERK) and mTOR via suppression of Ras prenylation and enhanced Bim expression.", "entity1": "Ras", "entity2": "BPs", "span1": [130, 133], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6192": {"label": 3, "data": {"text": "Tacrine was chosen as a model to study the mechanisms underlying the cardiovascular effects of i.v. cholinesterase inhibitors.", "entity1": "cholinesterase", "entity2": "Tacrine", "span1": [100, 114], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7080": {"label": 2, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "TRPV3", "entity2": "menthol", "span1": [101, 106], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12914": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine beta-synthase", "entity2": "H(2)S", "span1": [131, 158], "span2": [18, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7818": {"label": 5, "data": {"text": "To determine if control of seizures and survival are still possible without pretreatment or immediate pharmacologic intervention, we studied the anticonvulsant efficacy of the GluK1 (GluR5)/\u03b1-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid (LY293558) in rats that did not receive any treatment until 20 minutes after exposure to the nerve agent soman.", "entity1": "GluK1", "entity2": "LY293558", "span1": [176, 181], "span2": [360, 368]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3458": {"label": 1, "data": {"text": "R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less.", "entity1": "Y156F", "entity2": "S-modafinil", "span1": [53, 58], "span2": [103, 114]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10700": {"label": 4, "data": {"text": "Denufosol is metabolically more stable and better tolerated, and may enhance mucociliary clearance for a longer period of time than previously investigated P2Y(2) agonists.", "entity1": "P2Y(2)", "entity2": "Denufosol", "span1": [156, 162], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7660": {"label": 3, "data": {"text": "These findings indicate that captopril attenuates the development of monocrotaline-induced right ventricular hypertrophy in association with inhibition of MMP-2 and MMP-9 in rats.", "entity1": "MMP-2", "entity2": "captopril", "span1": [155, 160], "span2": [29, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8143": {"label": 3, "data": {"text": "Isoproterenol induced myocardial infarcted rats showed a significant increase in the levels of cardiac diagnostic markers, heart mitochondrial lipid peroxidation, calcium, and a significant decrease in the activities/levels of heart mitochondrial glutathione peroxidase, glutathione reductase, reduced glutathione, isocitrate, succinate, malate, \u03b1-ketoglutarate and NADH-dehydrogenases, cytochrome-C-oxidase and adenosine triphosphate.", "entity1": "NADH-dehydrogenases", "entity2": "Isoproterenol", "span1": [366, 385], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3557": {"label": 3, "data": {"text": "Moreover, LTD4-induced increases in CysLT(1)R and NF-\u03baB p65 in the brain were also attenuated by pranlukast.", "entity1": "CysLT(1)R", "entity2": "pranlukast", "span1": [36, 45], "span2": [97, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12081": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase", "entity2": "17 alpha-hydroxy pregnenolone", "span1": [0, 72], "span2": [149, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6787": {"label": 3, "data": {"text": "RESULTS: Aspirin, diclofenac, indomethacin, ketoprofen, meclofenamic acid, and piroxicam had little selectivity toward COX isozymes, whereas NS398, carprofen, tolfenamic acid, nimesulide, and etodolac had more than 5 times greater preference for inhibiting COX-2 than COX-1.", "entity1": "COX-1", "entity2": "nimesulide", "span1": [268, 273], "span2": [176, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2823": {"label": 3, "data": {"text": "Dexamethasone (DXM) decreased the expression of CXCL-8, VEGF, and iNOS induced by reIL-4, while 1400W dihydrochloride (1400W), a selective inhibitor of iNOS, decreased the expression of E-selectin, VEGF, and iNOS.", "entity1": "iNOS", "entity2": "DXM", "span1": [66, 70], "span2": [15, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7765": {"label": 1, "data": {"text": "Our study determined whether there was a significant dose-dependent correlation between increasing Hg exposure from dental amalgams and GST-\u03b1 and GST-\u03c0 as biomarkers of kidney integrity.", "entity1": "GST-\u03b1", "entity2": "Hg", "span1": [136, 141], "span2": [99, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"40": {"label": 3, "data": {"text": "These G-proteins are likely to be involved in the adrenaline-induced inhibition of dihydropyridine-sensitive Ca2+ currents and in other signal transduction pathways contributing to the adrenaline-induced inhibition of insulin secretion.", "entity1": "insulin", "entity2": "adrenaline", "span1": [218, 225], "span2": [185, 195]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8795": {"label": 9, "data": {"text": "Using siRNA we found that ATF4, but not Nrf2, is important for fisetin's ability to increase GSH levels under basal conditions whereas both ATF4 and Nrf2 appear to cooperate to increase GSH levels under oxidative stress conditions.", "entity1": "Nrf2", "entity2": "fisetin", "span1": [40, 44], "span2": [63, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10092": {"label": 8, "data": {"text": "Three replicate studies in the oral surgery model of acute pain used submucosal microdialysis sample collection for the measurement of prostaglandin E2 (PGE2; a product of both COX-1 and COX-2) and thromboxane B2 (as a biomarker for COX-1 activity) with parallel assessments of pain.", "entity1": "COX-1", "entity2": "PGE2", "span1": [177, 182], "span2": [153, 157]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6992": {"label": 8, "data": {"text": "Valproic acid selectively inhibits conversion of arachidonic acid to arachidonoyl-CoA by brain microsomal long-chain fatty acyl-CoA synthetases: relevance to bipolar disorder.", "entity1": "brain microsomal long-chain fatty acyl-CoA synthetases", "entity2": "arachidonoyl-CoA", "span1": [89, 143], "span2": [69, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3833": {"label": 3, "data": {"text": "The inhibition of phosphoinositide 3-kinase using Ly294002 augmented a decrease in the p21 level induced by their combination, but it showed no significant effects on expression of Sp1 and cyclin D1.", "entity1": "p21", "entity2": "Ly294002", "span1": [87, 90], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9695": {"label": 1, "data": {"text": "Comparison of the novel antipsychotic ziprasidone with clozapine and olanzapine: inhibition of dorsal raphe cell firing and the role of 5-HT1A receptor activation.", "entity1": "5-HT1A receptor", "entity2": "clozapine", "span1": [136, 151], "span2": [55, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7337": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT1", "entity2": "glutamine", "span1": [323, 328], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"9957": {"label": 3, "data": {"text": "In contrast, aspirin-like nonselective NSAIDs such as sulindac and indomethacin inhibit not only the enzymatic action of the highly inducible, proinflammatory COX-2 but the constitutively expressed, cytoprotective COX-1 as well.", "entity1": "COX-2", "entity2": "indomethacin", "span1": [159, 164], "span2": [67, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15036": {"label": 8, "data": {"text": "All the compounds were evaluated for their anti-tumor activity against MCF-7, A549 and B16-F10 tumor cell lines as well as cyclooxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) inhibitory activity of murine macrophage RAW 264.7 cell line.", "entity1": "COX-2", "entity2": "PGE2", "span1": [141, 146], "span2": [174, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9396": {"label": 2, "data": {"text": "We demonstrate here that minoxidil is a potent activator of purified PGHS-1 (AC50 = 80 microM), as assayed by oxygen consumption and PGE2 production.", "entity1": "PGHS-1", "entity2": "minoxidil", "span1": [69, 75], "span2": [25, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"384": {"label": 9, "data": {"text": "The CB1 and CB2 second extracellular loops, e2, were exchanged, modifications that had no effect on SR 141716A binding in the CB1 variant but that eliminated CP 55,940 binding in both mutants.", "entity1": "CB1", "entity2": "CP 55,940", "span1": [126, 129], "span2": [158, 167]}, "weak_labels": [-1, -1, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3690": {"label": 2, "data": {"text": "8-pCPT-2'-O-Me-cAMP-AM potentiation of insulin secretion stimulated by tolbutamide was markedly inhibited by 2-APB (25 \u03bcM) and enhanced by the PKC inhibitor bisindolylmaleimide I (1 \u03bcM).", "entity1": "insulin", "entity2": "8-pCPT-2'-O-Me-cAMP-AM", "span1": [39, 46], "span2": [0, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11487": {"label": 1, "data": {"text": "RESULTS: Ketorolac was six times more active against COX-1 (IC(50) = 0.02 microM) than COX-2 (IC(50) = 0.12 microM) while bromfenac was approximately 32 times more active against COX-2 (IC(50) = 0.0066 microM) than COX-1 (IC(50) = 0.210 microM).", "entity1": "COX-1", "entity2": "Ketorolac", "span1": [53, 58], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8271": {"label": 8, "data": {"text": "Methadone N-demethylation in vitro is catalyzed by hepatic cytochrome P4502B6 (CYP2B6) and CYP3A4, but clinical disposition is often attributed to CYP3A4.", "entity1": "CYP3A4", "entity2": "N", "span1": [147, 153], "span2": [10, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"6024": {"label": 3, "data": {"text": "6-Methoxy-2-naphthylacetic acid, the active metabolite of Relafen, inhibits murine PGHS-2 preferentially.", "entity1": "PGHS-2", "entity2": "Relafen", "span1": [83, 89], "span2": [58, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2324": {"label": 3, "data": {"text": "A pronounced NET knockout-induced shortening of the immobility time in the TST (by ca 50%) compared to WT mice was not reduced any further by NET-inhibiting ADs such as reboxetine, desipramine, and imipramine.", "entity1": "NET", "entity2": "reboxetine", "span1": [142, 145], "span2": [169, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1212": {"label": 1, "data": {"text": "To determine whether these responses were common to other amphetamines of abuse, effects of methylenedioxymethamphetamine (MDMA) on the plasmalemmal DA transporter (DAT) and vesicular monoamine transporter-2 (VMAT-2) were assessed.", "entity1": "VMAT-2", "entity2": "methylenedioxymethamphetamine", "span1": [209, 215], "span2": [92, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"2837": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "PLP", "span1": [83, 99], "span2": [147, 150]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8039": {"label": 1, "data": {"text": "Finally, chronic administration of metformin in diabetic mice restored cardiac autophagy by activating JNK1-Bcl-2 pathways and dissociating Beclin1 and Bcl-2.", "entity1": "Beclin1", "entity2": "metformin", "span1": [140, 147], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15996": {"label": 1, "data": {"text": "Here we show that puerarin increases proliferation and differentiation and opposes cisplatin-induced apoptosis in human osteoblastic MG-63 cells containing two estrogen receptor (ER) isoforms.", "entity1": "ER", "entity2": "puerarin", "span1": [179, 181], "span2": [18, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14691": {"label": 3, "data": {"text": "This work investigated the drug interaction potential of GSK1292263, a novel GPR119 agonist, with the HMG-coA reductase inhibitors simvastatin and rosuvastatin.", "entity1": "HMG-coA reductase", "entity2": "simvastatin", "span1": [102, 119], "span2": [131, 142]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14989": {"label": 9, "data": {"text": "Both fatty acids, but DHA to a lesser extent compared with EPA, selectively and dose-dependently reduced the percentage of cytokine-expressing Th cells in a peroxisome proliferator-activated receptor (PPAR)\u03b3-dependent fashion, whereas the expression of the cell surface marker CD69 was unaltered on activated T cells.", "entity1": "CD69", "entity2": "fatty acids", "span1": [277, 281], "span2": [5, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9320": {"label": 3, "data": {"text": "RESULTS: Nedocromil sodium inhibited the chemotactic response toward FMLP and NAF/IL-8 of GM-CSF primed eosinophils approximately 60% (inhibitory concentration of 50% [IC50] approximately 1 to 10 nmol/L), whereas these responses of IL-3 primed eosinophils was completely inhibited (IC50 approximately 1 nmol/L).", "entity1": "GM-CSF", "entity2": "Nedocromil sodium", "span1": [90, 96], "span2": [9, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4133": {"label": 2, "data": {"text": "KCNK1, a member of the family of two-pore K(+) ion channels, is specifically induced in the livers of male mice after phenobarbital treatment.", "entity1": "KCNK1", "entity2": "phenobarbital", "span1": [0, 5], "span2": [118, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14807": {"label": 1, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1) receptor", "entity2": "rimonabant", "span1": [155, 169], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2433": {"label": 1, "data": {"text": "SSTR2 and SSTR5 are usually expressed in GH-secreting pituitary tumors, and both octreotide and lanreotide bind preferentially to SSTR2 and, to a lesser extent, to SSTR5.", "entity1": "SSTR5", "entity2": "lanreotide", "span1": [164, 169], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10204": {"label": 8, "data": {"text": "Rifampicin (10 micromol/L) inhibited OATP8-mediated BSP uptake by 50%, whereas inhibition of OATP-C-, OATP-B-, and OATP-A-mediated BSP transport was below 15%.", "entity1": "OATP-B", "entity2": "BSP", "span1": [102, 108], "span2": [131, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5622": {"label": 3, "data": {"text": "Furthermore, cisapride block of the HERG K+ current was not linked with inactivation in the mutant HERG channels F656V and F656M.", "entity1": "HERG", "entity2": "cisapride", "span1": [99, 103], "span2": [13, 22]}, "weak_labels": [-1, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2371": {"label": 3, "data": {"text": "Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature.", "entity1": "tyrosine kinases", "entity2": "Nexavar", "span1": [110, 126], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3145": {"label": 1, "data": {"text": "Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity.", "entity1": "TrkA", "entity2": "Amitriptyline", "span1": [64, 68], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15957": {"label": 1, "data": {"text": "In addition, inhibitors for EGFR or ERK1/2 remarkably suppressed OHT-induced truncation of cyclin E, suggesting involvement of EGFR signaling.", "entity1": "EGFR", "entity2": "OHT", "span1": [127, 131], "span2": [65, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14470": {"label": 1, "data": {"text": "Loss of agonist binding was observed on intact human embryonic kidney 293 cells expressing the W203A receptor, conditions where high GTP levels are present; however, high affinity binding [(3)H]PGE(2) was observed in broken cell preparations washed free of GTP.", "entity1": "W203A", "entity2": "GTP", "span1": [95, 100], "span2": [133, 136]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15165": {"label": 2, "data": {"text": "Taken together, these data indicate that a PKA-mediated signaling pathway mediates GnRH activation of CREB at low-pulse frequencies, playing a significant role in the decoding of the hypothalamic GnRH signal to result in frequency-dependent FSH\u03b2 activation.", "entity1": "FSH\u03b2", "entity2": "GnRH", "span1": [241, 245], "span2": [196, 200]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2319": {"label": 3, "data": {"text": "Glufosinate inhibits glutamine synthetase and blocks biosynthesis of glutamine.", "entity1": "glutamine synthetase", "entity2": "Glufosinate", "span1": [21, 41], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3898": {"label": 2, "data": {"text": "Ozone plus PM(2.5) exposure, however, induced CRP, IL-6, CK, LDH and MDA increase, SOD and HRV decrease significantly in a dose-response way.", "entity1": "IL-6", "entity2": "Ozone", "span1": [51, 55], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2549": {"label": 3, "data": {"text": "Imatinib was also found to inhibit M-CSF-induced osteoclast survival as well as M-CSF-induced osteoclast bone resorbing activity, but was without effect on interleukin 1alpha (IL-1alpha) and receptor activator of nuclear factor kappa B ligand (RANKL)-induced inhibition of osteoclasts apoptosis, further supporting the hypothesis that imatinib may affect mature osteoclasts through the inhibition of c-FMS.", "entity1": "c-FMS", "entity2": "imatinib", "span1": [400, 405], "span2": [335, 343]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"735": {"label": 2, "data": {"text": "Human and rat renin and angiotensinogen genes were downregulated in dTGR and were increased by losartan and cilazapril treatments, whereas no changes in the expression of rat ACE and AT1A receptor genes were observed.", "entity1": "angiotensinogen", "entity2": "cilazapril", "span1": [24, 39], "span2": [108, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5664": {"label": 2, "data": {"text": "Therefore, matrine and oxymatrine may have the potential to cure LQT2 as a potassium channel activator by promoting hERG channel activation and increasing hERG channel expression.", "entity1": "hERG", "entity2": "oxymatrine", "span1": [116, 120], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8073": {"label": 3, "data": {"text": "Orlistat has been the most used anti-obesity drug and the mechanism of its action is to reduce lipid absorption by inhibiting gastrointestinal lipases.", "entity1": "lipases", "entity2": "Orlistat", "span1": [143, 150], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12022": {"label": 1, "data": {"text": "Using electrophysiologic techniques, the present study assessed the in vivo action of brexpiprazole on serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1B, and 5-HT2A; dopamine (DA) D2 autoreceptors, and alpha1- and alpha2-adrenergic receptors.", "entity1": "5-HT2A", "entity2": "brexpiprazole", "span1": [158, 164], "span2": [86, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8625": {"label": 1, "data": {"text": "Thus, arsenic activates Nrf2 through a non-canonical mechanism (p62-dependent), leading to a chronic, sustained activation of Nrf2.", "entity1": "p62", "entity2": "arsenic", "span1": [64, 67], "span2": [6, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15732": {"label": 4, "data": {"text": "Fourteen of 17 parabens exhibited hER\u03b1 and/or hER\u03b2 agonistic activity at concentrations of \u2a7d1\u00d710(-5)M, whereas none of the 17 parabens showed AR agonistic or antagonistic activity.", "entity1": "hER\u03b2", "entity2": "parabens", "span1": [46, 50], "span2": [15, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9835": {"label": 3, "data": {"text": "Moreover, geldanamycin decreases the amount and phosphorylation of Lck and Raf-1 kinases and prevents activation of the extracellular signal regulated kinase (ERK)-2 kinase.", "entity1": "kinase", "entity2": "geldanamycin", "span1": [166, 172], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12367": {"label": 2, "data": {"text": "Tamoxifen represses miR-200 microRNAs and promotes epithelial-to-mesenchymal transition by up-regulating c-Myc in endometrial carcinoma cell lines.", "entity1": "c-Myc", "entity2": "Tamoxifen", "span1": [105, 110], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5390": {"label": 3, "data": {"text": "Methylphenidate, an inhibitor of dopamine and norepinephrine transporters (DAT and NET, respectively), is a standard treatment for ADHD.", "entity1": "NET", "entity2": "Methylphenidate", "span1": [83, 86], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7876": {"label": 8, "data": {"text": "Renal clearance of unbound anagliptin and unbound M1 far exceeded glomerular filtration rate, indicating active renal elimination: that might reflect the fact that anagliptin may be a substrate of OAT1, OAT3, MDR1 and MRP2, and M1 a substrate of OAT3, BCRP, MRP2 and MRP4.", "entity1": "MRP2", "entity2": "anagliptin", "span1": [218, 222], "span2": [164, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10980": {"label": 2, "data": {"text": "Preincubation with 1 microM of the protein kinase C (PKC) activator phorbol 12-myristate 13-acetate (PMA) caused a small but significant decrease in isoprenaline-induced E(max), indicating activated PKC-mediated heterologous beta(2)-adrenoceptor desensitization.", "entity1": "PKC", "entity2": "phorbol 12-myristate 13-acetate", "span1": [53, 56], "span2": [68, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13935": {"label": 3, "data": {"text": "In pig parathyroid cells, paricalcitol and the active form of doxercalciferol induced VDR translocation from the cytoplasm into the nucleus, suppressed PTH mRNA expression and inhibited cell proliferation in a similar manner, although paricalcitol induced the expression of CaSR mRNA more effectively.", "entity1": "PTH", "entity2": "doxercalciferol", "span1": [152, 155], "span2": [62, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3349": {"label": 1, "data": {"text": "The high resolution NMR solution structure of the cTnC-cTnI-dfbp-o ternary complex showed that dfbp-o bound at the hydrophobic interface formed by cTnC and cTnI making critical interactions with residues such as Arg147 of cTnI.", "entity1": "cTnI", "entity2": "dfbp-o", "span1": [156, 160], "span2": [95, 101]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12077": {"label": 8, "data": {"text": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase (3 beta-HSD) purified from human placenta transforms C-21 (pregnenolone and 17 alpha-hydroxy pregnenolone) as well as C-19 (dehydroepiandrosterone and androst-5-ene-3 beta, 17 beta-diol) steroids into the corresponding 3-keto-4-ene-steroids and is thus involved in the biosynthesis of all classes of hormonal steroids.", "entity1": "Human placental 3 beta-hydroxysteroid dehydrogenase/5----4-ene isomerase", "entity2": "3-keto-4-ene-steroids", "span1": [0, 72], "span2": [292, 313]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13573": {"label": 3, "data": {"text": "The next large phase III adjuvant trial for this subset of breast cancer is an international collaboration designed to evaluate the added or alternative benefit of an oral tyrosine kinase inhibitor targeting HER2/neu as well as the epidermal growth factor receptor (EGFR), lapatinib.", "entity1": "HER2", "entity2": "lapatinib", "span1": [208, 212], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12741": {"label": 1, "data": {"text": "Responses to isoproterenol were largely mediated through the beta1AR in control myocytes.", "entity1": "beta1AR", "entity2": "isoproterenol", "span1": [61, 68], "span2": [13, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3900": {"label": 2, "data": {"text": "Ozone plus PM(2.5) exposure, however, induced CRP, IL-6, CK, LDH and MDA increase, SOD and HRV decrease significantly in a dose-response way.", "entity1": "LDH", "entity2": "Ozone", "span1": [61, 64], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2933": {"label": 3, "data": {"text": "Phosphate, a product of the reaction, was found to be a potent inhibitor of MjAdSS showing biphasic inhibition of enzyme activity.", "entity1": "MjAdSS", "entity2": "Phosphate", "span1": [76, 82], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5342": {"label": 1, "data": {"text": "S1P activated phosphatidylinositol 3-kinase (PI3K)/Akt signaling, leading to the inhibition of glycogen synthase kinase-3\u03b2 and the nuclear translocation of \u03b2-catenin, followed by the increase of the transcriptional activity by \u03b2-catenin/T-cell factor complex formation in both SaOS-2 cells and MC3T3-E1 cells.", "entity1": "T-cell factor", "entity2": "S1P", "span1": [237, 250], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4138": {"label": 2, "data": {"text": "These results indicate that phenobarbital treatment induces KCNK1 to elicit a male-specific and growth-suppressing signal.", "entity1": "KCNK1", "entity2": "phenobarbital", "span1": [60, 65], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15205": {"label": 3, "data": {"text": "In HaCaT cells, buthanol and ethylacetate fractions of 80% methanol C. fragile extract (CFB or CFE) and a single compound, clerosterol (CLS) isolated from CFE attenuated UVB (60mJ/cm(2))-induced cytotoxicity and reduced expression of pro-inflammatory proteins including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and tumor necrosis factor-\u03b1 (TNF- \u03b1).", "entity1": "cyclooxygenase-2", "entity2": "ethylacetate", "span1": [270, 286], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4140": {"label": 3, "data": {"text": "The therapeutic potential of directly inhibiting prosurvival proteins was unveiled with the development of navitoclax, a selective inhibitor of both BCL-2 and BCL-2-like 1 (BCL-X(L)), which has shown clinical efficacy in some BCL-2-dependent hematological cancers.", "entity1": "BCL-2", "entity2": "navitoclax", "span1": [149, 154], "span2": [107, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11095": {"label": 1, "data": {"text": "The effects of these metabolites on the expression of uteroglobin (UG) and progesterone receptor (PR) genes, both regulated by progesterone (P4), were evaluated in the uterus of prepubertal female rabbits that were simultaneously treated with P4 (1.0 mg) for 5 consecutive days.", "entity1": "uteroglobin", "entity2": "progesterone (P4)", "span1": [54, 65], "span2": [127, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9776": {"label": 4, "data": {"text": "The nonselective opioid receptor antagonist, naloxone (3 mg/kg, i.m. ), attenuated the antitussive effects of codeine or SB 227122, indicating that the antitussive activity of both compounds is opioid receptor-mediated.", "entity1": "opioid receptor", "entity2": "codeine", "span1": [17, 32], "span2": [110, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13634": {"label": 0, "data": {"text": "Top1p clamps around duplex DNA, wherein the core and C-terminal domains are connected by extended alpha-helices (linker domain), which position the active site Tyr of the C-terminal domain within the catalytic pocket.", "entity1": "alpha-helices", "entity2": "Tyr", "span1": [98, 111], "span2": [160, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8279": {"label": 8, "data": {"text": "This investigation tested the hypothesis that CYP2B6 is a prominent CYP isoform responsible for clinical methadone N-demethylation and clearance, using the in vivo mechanism-based CYP2B6 inhibitor ticlopidine, given orally for 4 days.", "entity1": "CYP", "entity2": "N", "span1": [68, 71], "span2": [115, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14863": {"label": 3, "data": {"text": "Insertion of ER\u03b1 was blocked by the ER antagonist ICI 182,780 or with the protein kinase C (PKC) pathway inhibitor bisindolylmaleimide (BIS).", "entity1": "ER\u03b1", "entity2": "bisindolylmaleimide", "span1": [13, 16], "span2": [115, 134]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9947": {"label": 3, "data": {"text": "Sulfasalazine inhibited tumor necrosis factor alpha-induced activation of endogenous IKK in Jurkat T cells and SW620 colon cells, as well as the catalytic activity of purified IKK-alpha and IKK-beta in vitro.", "entity1": "IKK-beta", "entity2": "Sulfasalazine", "span1": [190, 198], "span2": [0, 13]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6877": {"label": 8, "data": {"text": "Cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS) utilize L-cysteine as substrate to form H2S.", "entity1": "cystathionine-beta-synthase", "entity2": "H2S", "span1": [36, 63], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"7425": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA. We examined this using an in vitro model of fatty acid metabolism to measure the accumulation of the long-chain metabolites of ALA in HepG2 cell phospholipids.", "entity1": "D6D", "entity2": "DHA", "span1": [31, 34], "span2": [232, 235]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"15267": {"label": 2, "data": {"text": "Three variables of cardiac vagal effects (the root mean square of successive differences [rMSSD] in the interbeat interval of the heart rate [IBI], heart-rate variability [HRV] caused by peak-valley respiratory sinus arrhythmia [pvRSA], and high-frequency power [HF]) and heart rate (HR) were obtained at seven time points during the clamps, characterised by increasing levels of insulin (achieved by administering insulin plus glucose, glucose only, glucose and GLP-1, and glucose and GLP-1 combined with arginine).", "entity1": "insulin", "entity2": "arginine", "span1": [380, 387], "span2": [506, 514]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11179": {"label": 1, "data": {"text": "[Effect of mifepristone on the expression of progesterone receptor messenger RNA and protein in uterine leiomyomata].", "entity1": "progesterone receptor", "entity2": "mifepristone", "span1": [45, 66], "span2": [11, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6298": {"label": 2, "data": {"text": "We found that 5-HT stimulated the conversion of [3H]L-arginine ([3H]L-Arg) to [3H]L-Cit, indicating eNOS activation.", "entity1": "eNOS", "entity2": "5-HT", "span1": [100, 104], "span2": [14, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4872": {"label": 2, "data": {"text": "A head-to-head comparison between insulin detemir and NPH insulin in women with type 1 diabetes showed that while foetal outcomes did not differ, fasting plasma glucose improved with insulin detemir without an increased incidence of hypoglycaemia.", "entity1": "insulin", "entity2": "glucose", "span1": [183, 190], "span2": [161, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2739": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "kinase", "entity2": "dasatinib", "span1": [109, 115], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12889": {"label": 1, "data": {"text": "Here, we show that at noncytotoxic concentrations, H(2)S was able to inhibit NO production and inducible NO synthase (iNOS) expression via heme oxygenase (HO-1) expression in RAW264.7 macrophages stimulated with lipopolysaccharide (LPS).", "entity1": "heme oxygenase", "entity2": "H(2)S", "span1": [139, 153], "span2": [51, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7659": {"label": 3, "data": {"text": "MMP-2 and MMP-9 expressions and activities in right ventricles increased significantly in monocrotaline-injected rats and captopril inhibited them.", "entity1": "MMP-9", "entity2": "captopril", "span1": [10, 15], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5220": {"label": 2, "data": {"text": "Also, vinblastine enhances the phosphorylation of Ras homologous protein A, the accumulation of reactive oxygen species, the release of intracellular Ca(2+), as well as the activation of apoptosis signal-regulating kinase 1, c-jun-N-terminal kinase, p38, inhibitor of kappaB\u03b1 (I\u03baB\u03b1) kinase, and inositol requiring enzyme 1\u03b1.", "entity1": "apoptosis signal-regulating kinase 1", "entity2": "vinblastine", "span1": [187, 223], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12206": {"label": 8, "data": {"text": "Our data suggest that l-arginine is taken up by Sertoli cells and peritubular cells, principally via system y(+)L (SLC3A2/SLC7A6) and system y(+) (SLC7A1 and SLC7A2), with system B(0+) making a minor contribution.", "entity1": "SLC3A2", "entity2": "l-arginine", "span1": [115, 121], "span2": [22, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11341": {"label": 8, "data": {"text": "Phosphatidylserine (PtdSer) is made in mammalian cells by two PtdSer synthases, PSS1 and PSS2.", "entity1": "PtdSer synthases", "entity2": "Phosphatidylserine", "span1": [62, 78], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8341": {"label": 3, "data": {"text": "Aqueous ethanol (80%) extract of lentil hulls exhibited high antioxidant and anti-inflammatory activities preferentially inhibiting 15-LOX (IC(50), 55 \u03bcg/ml), with moderate COX-1 (IC(50), 66 \u03bcg/ml) and COX-2 (IC(50), 119 \u03bcg/ml) inhibitory effects on the COX pathway, whereas faba bean hull extracts exerted relatively mild LOX inhibitory activity.", "entity1": "COX", "entity2": "ethanol", "span1": [254, 257], "span2": [8, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11270": {"label": 8, "data": {"text": "On the other hand, the accumulation of Ser through the C1-THF synthase/SHMT pathway in glyD plants was 2.5-fold greater than that in WT plants.", "entity1": "SHMT", "entity2": "Ser", "span1": [71, 75], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13645": {"label": 1, "data": {"text": "Mutation of Gly721 alters DNA topoisomerase I active site architecture and sensitivity to camptothecin.", "entity1": "DNA topoisomerase I", "entity2": "camptothecin", "span1": [26, 45], "span2": [90, 102]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5902": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "LDL", "entity2": "fibric acids", "span1": [172, 175], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14594": {"label": 3, "data": {"text": "In addition, 17-AAG treatment reduced cell viability, CDK2, CDK4, cyclin E, cyclin D1, and phosphorylated Rb levels in AhR-expressing lung AD cells.", "entity1": "cyclin D1", "entity2": "17-AAG", "span1": [76, 85], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"286": {"label": 0, "data": {"text": "The two NH2-terminal truncated vectors deleted, respectively, 1) the 29-amino acid putative targeting sequence and 2) 51 amino acids, yielding a protein equivalent to a carbonic anhydrase (CA) V isolated from mouse liver mitochondria; and both vectors produced homogeneous protein fractions.", "entity1": "carbonic anhydrase (CA) V", "entity2": "NH2", "span1": [169, 194], "span2": [8, 11]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9817": {"label": 3, "data": {"text": "Postoperative concentrations of plasminogen were decreased significantly in the tranexamic acid group (P < 0.001).", "entity1": "plasminogen", "entity2": "tranexamic acid", "span1": [32, 43], "span2": [80, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8149": {"label": 3, "data": {"text": "Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors.", "entity1": "telomerase", "entity2": "2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one", "span1": [137, 147], "span2": [30, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6065": {"label": 3, "data": {"text": "The mechanism by which norepinephrine (NE) down-regulates alpha 1B-adrenergic receptor (alpha-AR) mRNA was studied in rabbit aortic smooth muscle cells.", "entity1": "alpha 1B-adrenergic receptor", "entity2": "NE", "span1": [58, 86], "span2": [39, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3816": {"label": 1, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "D281A", "entity2": "Sar", "span1": [109, 114], "span2": [44, 47]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"28": {"label": 3, "data": {"text": "Candoxatril is a novel, orally active inhibitor of neutral endopeptidase EC 3.4.24.11, the enzyme that degrades atrial natriuretic peptide (ANP).", "entity1": "EC 3.4.24.11", "entity2": "Candoxatril", "span1": [73, 85], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10267": {"label": 8, "data": {"text": "Reuptake of extracellular noradrenaline (NA) into superior cervical ganglion (SCG) neurones is mediated by means of the noradrenaline transporter (NAT, uptake 1).", "entity1": "NAT", "entity2": "NA", "span1": [147, 150], "span2": [41, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"14421": {"label": 2, "data": {"text": "Finally, Metformin treatment caused a significant increase in the level of phosphorylated (active) AMPK.", "entity1": "phosphorylated (active) AMPK", "entity2": "Metformin", "span1": [75, 103], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15049": {"label": 1, "data": {"text": "The contrasting activity of iodido versus chlorido ruthenium and osmium arene azo- and imino-pyridine anticancer complexes: control of cell selectivity, cross-resistance, p53 dependence, and apoptosis pathway.", "entity1": "p53", "entity2": "osmium arene azo- and imino-pyridine", "span1": [171, 174], "span2": [65, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13890": {"label": 3, "data": {"text": "Of these, the thrombin inhibitor dabigatran and factor Xa inhibitor rivaroxaban have recently been licensed for thromboprophylaxis after orthopaedic surgery mainly in Europe.", "entity1": "factor Xa", "entity2": "rivaroxaban", "span1": [48, 57], "span2": [68, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1747": {"label": 4, "data": {"text": "Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol].", "entity1": "beta(2)-adrenoceptor", "entity2": "eformoterol", "span1": [92, 112], "span2": [133, 144]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8665": {"label": 2, "data": {"text": "Our findings indicate that imatinib protects oocytes from cisplatin-induced cell death by inhibiting c-Abl kinase, which would otherwise activate TAp73-BAX-mediated apoptosis.", "entity1": "BAX", "entity2": "cisplatin", "span1": [152, 155], "span2": [58, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7383": {"label": 5, "data": {"text": "(2) Does in vivo administration of (R)-(alpha)-(-)-methylhistamine dihydrobromide (RAMH) (H3R agonist), thioperamide maleate (H3R antagonist) or histamine, in the absence/presence of thioperamide maleate, to bile duct ligated (BDL) rats regulate cholangiocyte proliferation?", "entity1": "H3R", "entity2": "thioperamide maleate", "span1": [126, 129], "span2": [104, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9274": {"label": 1, "data": {"text": "The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the alpha 1-adrenoceptor.", "entity1": "alpha 1-adrenoceptor", "entity2": "haloperidol", "span1": [166, 186], "span2": [79, 90]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14177": {"label": 0, "data": {"text": "Mass spectral analysis of CBDP-inhibited BChE digested with Glu-C showed an o-hydroxybenzyl adduct (+106amu) on lysine 499, a residue far from the active site, but not on His-438.", "entity1": "BChE", "entity2": "His", "span1": [41, 45], "span2": [171, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10346": {"label": 3, "data": {"text": "Arsenite triggered strong induction of HSPs, which was prevented by 1 micro g/mL cycloheximide (CXH).", "entity1": "HSPs", "entity2": "CXH", "span1": [39, 43], "span2": [96, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5667": {"label": 2, "data": {"text": "Therefore, matrine and oxymatrine may have the potential to cure LQT2 as a potassium channel activator by promoting hERG channel activation and increasing hERG channel expression.", "entity1": "hERG", "entity2": "oxymatrine", "span1": [155, 159], "span2": [23, 33]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6447": {"label": 2, "data": {"text": "The present studies were undertaken to compare two compounds, a vitamin D(3) analogue (CB1093) with minimal calcaemic effects, and clenbuterol, a long-acting beta(2)-adrenoceptor agonist, both of which induce NGF synthesis in vivo.", "entity1": "NGF", "entity2": "clenbuterol", "span1": [209, 212], "span2": [131, 142]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8843": {"label": 2, "data": {"text": "There was also an increase in \u03b3-GCS and HO-1 levels in calycopterin pretreated cells.", "entity1": "\u03b3-GCS", "entity2": "calycopterin", "span1": [30, 35], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"443": {"label": 1, "data": {"text": "Epinastine (WAL 801CL) is an antihistaminic drug with binding affinity at certain other receptors, including alpha-adrenergic receptors and various serotonin (5-HT) receptor subtypes.", "entity1": "alpha-adrenergic receptors", "entity2": "WAL 801CL", "span1": [109, 135], "span2": [12, 21]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13454": {"label": 2, "data": {"text": "Given the anti-inflammatory properties of EPA, we suggest that induction of COX-2 in keratinocytes may be important in the anti-inflammatory and protective mechanism of action of PUFAs n-3 or n-6.", "entity1": "COX-2", "entity2": "PUFAs n-3", "span1": [76, 81], "span2": [179, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16021": {"label": 1, "data": {"text": "Haloperidol promotes mTORC1-dependent phosphorylation of ribosomal protein S6 via dopamine- and cAMP-regulated phosphoprotein of 32 kDa and inhibition of protein phosphatase-1.", "entity1": "mTORC1", "entity2": "Haloperidol", "span1": [21, 27], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8087": {"label": 2, "data": {"text": "E235 also activated DNA damage response signaling, resulting in increased levels of Ser15-phosphorylated p53, \u03b3-H2AX, and phosphorylated checkpoint kinase 2 (Chk2), although E235 does not appear to cause physical DNA damage.", "entity1": "phosphorylated p53", "entity2": "E235", "span1": [90, 108], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10423": {"label": 1, "data": {"text": "Tazarotene is an acetylenic retinoid which is metabolised to tazarotenic acid and which binds selectively to the retinoid receptors RARbeta and RARgamma.", "entity1": "RARgamma", "entity2": "tazarotenic acid", "span1": [144, 152], "span2": [61, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14281": {"label": 0, "data": {"text": "The mutant Fc domain (AglycoT-Fc1004) contained a total of 5 amino acid substitutions that conferred an activating to inhibitory ratio of 25 (A/I ratio; FcyRIIa-R131:Fc\u03b3RIIb).", "entity1": "AglycoT-Fc1004", "entity2": "amino acid", "span1": [22, 36], "span2": [61, 71]}, "weak_labels": [0, -1, 0, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12955": {"label": 1, "data": {"text": "CONCLUSION: Our results did not lend strong support to the view that the genetic variation of the DRD2 gene plays a major role in the individually variable adverse effect induced by chlorpromazine, at least in Chinese patients with schizophrenia.", "entity1": "DRD2", "entity2": "chlorpromazine", "span1": [98, 102], "span2": [182, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3890": {"label": 3, "data": {"text": "Pharmacophore identification of c-Myc inhibitor 10074-G5.", "entity1": "c-Myc", "entity2": "10074-G5", "span1": [32, 37], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5928": {"label": 3, "data": {"text": "The concentration of estramustine phosphate required to inhibit the assembly or to induce the disassembly of chick brain MAP2:tubulin microtubules is markedly dependent upon the microtubule protein concentration.", "entity1": "tubulin", "entity2": "estramustine phosphate", "span1": [126, 133], "span2": [21, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7477": {"label": 2, "data": {"text": "Kainate-selective ionotropic glutamate receptors (GluRs) require external Na+ and Cl- as well as the neurotransmitter L-glutamate for activation.", "entity1": "GluRs", "entity2": "Cl-", "span1": [50, 55], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1654": {"label": 5, "data": {"text": "The potent histamine H(1)-receptor antagonist cetirizine (Zyrtec) is a racemic mixture of levocetirizine (now available under the trademark Xyzal and dextrocetirizine.", "entity1": "histamine H(1)-receptor", "entity2": "cetirizine", "span1": [11, 34], "span2": [46, 56]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5589": {"label": 3, "data": {"text": "5-FU interferes with DNA synthesis by blocking thymidylate synthase (TS) but is inactivated by dihydropyrimidine dehydrogenase (DPD).", "entity1": "TS", "entity2": "5-FU", "span1": [69, 71], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5645": {"label": 3, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "K(+) channel", "entity2": "Arsenic trioxide", "span1": [30, 42], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15060": {"label": 1, "data": {"text": "Similarly, intraperitoneal administration of \u03b1-santalol (100mg/kg BW) and sandalwood oil (1g/kg BW) for two weeks modulated parameters such as serum aminotransferases, alkaline phosphatase, bilirubin, superoxide dismutase, catalase, free sulfhydryl, protein carbonyl, nitric oxide, liver lipid peroxide contents, and antioxidant capacity in d-galactose mediated oxidative stress induced mice.", "entity1": "catalase", "entity2": "\u03b1-santalol", "span1": [223, 231], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5795": {"label": 0, "data": {"text": "Comparison of the amino acid sequence of porcine ACY-1 with those of other Zn2+-binding metalloenzymes showed no significant homologies in either the overall sequence or the consensus sequences for the metal binding sites.", "entity1": "porcine ACY-1", "entity2": "amino acid", "span1": [41, 54], "span2": [18, 28]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11489": {"label": 1, "data": {"text": "RESULTS: Ketorolac was six times more active against COX-1 (IC(50) = 0.02 microM) than COX-2 (IC(50) = 0.12 microM) while bromfenac was approximately 32 times more active against COX-2 (IC(50) = 0.0066 microM) than COX-1 (IC(50) = 0.210 microM).", "entity1": "COX-2", "entity2": "bromfenac", "span1": [179, 184], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5017": {"label": 3, "data": {"text": "Methods: Stabilized anaplastic thyroid cancer cell lines (BHT-101 and CAL-62) and primary cultures from patients who underwent thyroidectomy for anaplastic thyroid cancer were treated with the histone deacetylase inhibitor LBH589.", "entity1": "histone deacetylase", "entity2": "LBH589", "span1": [193, 212], "span2": [223, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11878": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "anthocyanidins", "span1": [118, 143], "span2": [27, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9636": {"label": 3, "data": {"text": "Down-regulation of prostate-specific antigen (PSA) expression, an AR-target gene, by estramustine and bicalutamide was accompanied by the blockade of the mutated androgen receptor.", "entity1": "PSA", "entity2": "estramustine", "span1": [46, 49], "span2": [85, 97]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12471": {"label": 3, "data": {"text": "Arsenic deregulates the autophagic pathway through blockage of autophagic flux, resulting in accumulation of autophagosomes and sequestration of p62, Keap1, and LC3.", "entity1": "LC3", "entity2": "Arsenic", "span1": [161, 164], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15897": {"label": 8, "data": {"text": "This includes nonribosomal peptide synthetases (NRPS) and polyketide synthases (PKS) required for the formation of the benzopyranopyrrole core unit, as well as a suite of tailoring enzymes (e.g., four halogenases, an O-methyltransferase, and an N-glycosyltransferase) necessary for further modifications of the core structure.", "entity1": "halogenases", "entity2": "benzopyranopyrrole", "span1": [201, 212], "span2": [119, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6358": {"label": 9, "data": {"text": "The mNQO activity was insensitive to dicoumarol, a potent inhibitor of cytosolic NQO1.", "entity1": "mNQO", "entity2": "dicoumarol", "span1": [4, 8], "span2": [37, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13119": {"label": 2, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "FAS promoter", "entity2": "etopoxide", "span1": [156, 168], "span2": [98, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15361": {"label": 9, "data": {"text": "Neither oxycodone nor its metabolites activated PXR, CAR, or AhR.", "entity1": "AhR", "entity2": "oxycodone", "span1": [61, 64], "span2": [8, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4592": {"label": 3, "data": {"text": "Our previous work, built on the early pioneering multikinase inhibitor LY294002, resulted in the only PI3K vascular-targeted PI3K inhibitor prodrug, SF1126, which has now completed Phase I clinical trials.", "entity1": "PI3K", "entity2": "SF1126", "span1": [125, 129], "span2": [149, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2979": {"label": 1, "data": {"text": "Change in affinity for cGMP, vardenafil, sildenafil, or IBMX in Y612F, H613A, L765A, or F786A was less, but affinity of H613A or F786A for tadalafil was weakened 37- and 17-fold, respectively.", "entity1": "F786A", "entity2": "tadalafil", "span1": [129, 134], "span2": [139, 148]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13048": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "retinol dehydrogenase 10", "entity2": "retinal", "span1": [148, 172], "span2": [111, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8178": {"label": 3, "data": {"text": "Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.", "entity1": "aromatase", "entity2": "Tetrahydropyrroloquinolinone", "span1": [53, 62], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15730": {"label": 4, "data": {"text": "These results indicate that parabens are selective agonists for ER\u03b2 over ER\u03b1; their interactions with ER\u03b1/\u03b2 are dependent on the size and bulkiness of the alkyl groups; and they are metabolized by carboxylesterases, leading to attenuation of their estrogenic activity.", "entity1": "ER\u03b1", "entity2": "parabens", "span1": [73, 76], "span2": [28, 36]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8185": {"label": 2, "data": {"text": "Consistent with zinc finger E-box binding homeobox 2, which was confirmed as a direct target of miR-200b in endometrial cancer cell lines, some other key factors of EMT such as Snail and N-cadherin increased, whereas E-cadherin decreased in the TAM-treated cells, contributing to TAM-induced EMT in these endometrial cancer cells.", "entity1": "N-cadherin", "entity2": "TAM", "span1": [187, 197], "span2": [245, 248]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14832": {"label": 5, "data": {"text": "Although parenteral oral direct thrombin inhibitors (DTIs), such as argatroban and bivalirudin, have been on the market for years, DTIs such as dabigatran are novel synthetic thrombin antagonists.", "entity1": "thrombin", "entity2": "dabigatran", "span1": [175, 183], "span2": [144, 154]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13747": {"label": 1, "data": {"text": "Inhibition of (+)-[(3)H]isradipine binding to Ca(v)1.2DHP(-/-) (predominantly Ca(v)1.3) and wild-type (predominantly Ca(v)1.2) brain membranes by unlabeled DHPs revealed a 3- to 4-fold selectivity of nitrendipine and nifedipine for the Ca(v)1.2 binding pocket, a finding further confirmed with heterologously expressed channels.", "entity1": "Ca(v)1.2", "entity2": "nifedipine", "span1": [236, 244], "span2": [217, 227]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12830": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "pyridoxal kinase", "entity2": "PLP", "span1": [96, 112], "span2": [69, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3651": {"label": 2, "data": {"text": "DBDCT up-regulated the expression of Bax, down-regulated the expression of Bcl-2, and significantly increased the ratio of Bax/Bcl-2.", "entity1": "Bax", "entity2": "DBDCT", "span1": [37, 40], "span2": [0, 5]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4223": {"label": 2, "data": {"text": "The results showed that (1) 15mg/kg body weight PhIP induced obvious histopathological changes in gastric mucosa; (2) PhIP (10 and/or 15mg/kg) significantly decreased superoxide dismutase (SOD) and glutathioneperoxidase (GPx) activities, while increased catalase (CAT) activity compared with the control.", "entity1": "CAT", "entity2": "PhIP", "span1": [264, 267], "span2": [118, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2543": {"label": 8, "data": {"text": "Polyclonal antisera to either b5R or cyt b5 significantly inhibited N-hydroxy-4-aminobiphenyl (NHOH-4-ABP) reduction by 95 and 89%, respectively, and immunoreactive cyt b5 protein content in individual HLM was significantly correlated with individual reduction of both NHOH-4-ABP and N-hydroxy-PhIP (NHOH-PhIP).", "entity1": "cyt b5", "entity2": "NHOH-4-ABP", "span1": [37, 43], "span2": [95, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7186": {"label": 2, "data": {"text": "CONCLUSION: Intake of high SFAs and MUFAs appears to increase expression of PBMC D6D and D5D genes, whilst high EFAs intake appears to decrease expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "MUFAs", "span1": [81, 84], "span2": [36, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7627": {"label": 2, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "extracellular signal-regulated kinase", "entity2": "7-OH-DPAT", "span1": [63, 100], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5479": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "Org 2058", "span1": [106, 127], "span2": [485, 493]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9542": {"label": 5, "data": {"text": "The study demonstrates for the first time the marked gastrokinetic properties of the new CCK-A receptor antagonist lintitript in humans.", "entity1": "CCK-A receptor", "entity2": "lintitript", "span1": [89, 103], "span2": [115, 125]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4065": {"label": 3, "data": {"text": "Among the isolated compounds, trans-dihydromorin (8), oxyresveratrol (9), and steppogenin (12) were found to exhibit significant tyrosinase inhibition activities.", "entity1": "tyrosinase", "entity2": "oxyresveratrol", "span1": [129, 139], "span2": [54, 68]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11292": {"label": 8, "data": {"text": "We concluded that FDH has no direct role in the regulation of the above two pathways of Ser synthesis; the breakdown of formate to CO(2) by the FDH reaction is the primary and preferred fate of the organic acid in Arabidopsis.", "entity1": "FDH", "entity2": "formate", "span1": [144, 147], "span2": [120, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1903": {"label": 3, "data": {"text": "5-FU interferes with DNA synthesis by blocking thymidylate synthase (TS) but is inactivated by dihydropyrimidine dehydrogenase (DPD).", "entity1": "thymidylate synthase", "entity2": "5-FU", "span1": [47, 67], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12862": {"label": 9, "data": {"text": "The purified Atp8a1 is inactive in detergent micelles or in micelles containing phosphatidylcholine, phosphatidic acid, or phosphatidylinositol, is minimally activated by phosphatidylglycerol or phosphatidylethanolamine (PE), and is maximally activated by PS.", "entity1": "Atp8a1", "entity2": "phosphatidylcholine", "span1": [13, 19], "span2": [80, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13411": {"label": 5, "data": {"text": "In summary, the therapeutic effect of clozapine in reversing PPI impairment was mimicked by the H(1) antagonist pyrilamine, while pyrilamine had a mixed effect on cognition.", "entity1": "H(1)", "entity2": "pyrilamine", "span1": [96, 100], "span2": [130, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"915": {"label": 5, "data": {"text": "In this study, we examined whether betaxolol and other beta-adrenoceptor antagonists interact directly with neurotoxin binding to sites 1 and 2 of the voltage-sensitive sodium channel (Na(+) channel) in rat cerebrocortical synaptosomes.", "entity1": "beta-adrenoceptor", "entity2": "betaxolol", "span1": [55, 72], "span2": [35, 44]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9006": {"label": 9, "data": {"text": "Limitation of SRF was produced by the anticonvulsant BDZs (diazepam, clonazepam, nitrazepam and lorazepam) at low to mid nanomolar concentrations, by a convulsant BDZ which does not bind to high affinity BDZ receptors (Ro 5-4864) at high nanomolar concentrations and by a BDZ receptor weak partial agonist (Ro 15-1788) at micromolar concentrations.", "entity1": "BDZ receptors", "entity2": "BDZ", "span1": [204, 217], "span2": [163, 166]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"15235": {"label": 3, "data": {"text": "OATP1B1-, OATP1B3-, and OATP2B1-mediated substrate transport was inhibited efficiently by silymarin (IC50 values of 1.3, 2.2 and 0.3 \u00b5M, respectively), silybin A (IC50 values of 9.7, 2.7 and 4.5 \u00b5M, respectively), silybin B (IC50 values of 8.5, 5.0 and 0.8 \u00b5M, respectively), and silychristin (IC50 values of 9.0, 36.4, and 3.6 \u00b5M, respectively).", "entity1": "OATP1B3", "entity2": "silybin A", "span1": [10, 17], "span2": [152, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"15970": {"label": 1, "data": {"text": "The NMR solution structure of the copper(I)-loaded form of hCCSD1 reported here contributes further to characterization of the copper-transfer mechanism to hSOD1.", "entity1": "hCCSD1", "entity2": "copper(I)", "span1": [59, 65], "span2": [34, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1055": {"label": 3, "data": {"text": "doxorubicin, etoposide, mitoxantrone, and 4'-(9-acridinylamino)methanesulfon-m-anisidide) was 30-100-fold stimulated, whereas DNA cleavage induced by ATP-insensitive TOP2 poisons (e.g. amonafide, batracylin, and menadione) was only slightly (less than 3-fold) affected.", "entity1": "TOP2", "entity2": "menadione", "span1": [166, 170], "span2": [212, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4238": {"label": 2, "data": {"text": "Functional and biochemical studies indicated that TES signaling involved activity of the phosphoinositide 3 (PI3) kinase-protein kinase B (Akt) cascade initiated by activation of the androgen receptor and culminated in enhanced production of cGMP and microvascular vasodilation.", "entity1": "androgen receptor", "entity2": "TES", "span1": [183, 200], "span2": [50, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2802": {"label": 3, "data": {"text": "Inhibition of endogenous production of H(2)S by PAG significantly suppressed SP concentration, PPT-A expression and NK1-R expression in the acini.", "entity1": "SP", "entity2": "H(2)S", "span1": [77, 79], "span2": [39, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8706": {"label": 2, "data": {"text": "To delineate the pathogenesis, we examined changes in the mRNA levels of 2 angiotensin II Type I receptor (AT1R) subtypes, AT1AR and AT1BR, in a mouse aortic endothelial cell line, END-D. Quantitative real-time PCR analysis revealed significant increases in the mRNA levels of 2 AT1R subtypes, AT1AR and AT1BR following sodium arsenite (SA) treatment.", "entity1": "AT1R", "entity2": "sodium arsenite", "span1": [279, 283], "span2": [320, 335]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7402": {"label": 1, "data": {"text": "For the cPLA2alpha C2 domain, the target lipid phosphatidylcholine (PC) appears to be sufficient to drive membrane targeting to an internal membrane mimic at physiological Ca2+ levels, although the results do not rule out a second, unknown target molecule.", "entity1": "cPLA2alpha C2 domain", "entity2": "phosphatidylcholine", "span1": [8, 28], "span2": [47, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9735": {"label": 1, "data": {"text": "Yohimbine displays marked affinity at human (h)alpha(2A)-, halpha(2B)- and halpha(2C)-ARs, significant affinity for h5-HT(1A), h5-HT(1B), h5-HT(1D), and hD(2) receptors and weak affinity for hD(3) receptors.", "entity1": "hD(3) receptors", "entity2": "Yohimbine", "span1": [191, 206], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1031": {"label": 1, "data": {"text": "We thus confirm a possible role for p53 protein in modulating topoisomerase I activity but conclude that the major molecular determinants of topotecan sensitivity in glioma cells await identification.", "entity1": "topoisomerase I", "entity2": "topotecan", "span1": [62, 77], "span2": [141, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10603": {"label": 3, "data": {"text": "However, some experimental findings raise the question whether these effects resulting from the iron-mimicking properties of gallium are solely responsible for its antineoplastic activity or whether additional mechanisms are involved, such as antimitotic effects which result from its capability of inhibiting tubulin polymerization.", "entity1": "tubulin", "entity2": "gallium", "span1": [310, 317], "span2": [125, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2530": {"label": 8, "data": {"text": "We found that reduction of the carcinogenic hydroxylamines of the aromatic amine 4-aminobiphenyl (4-ABP; found in cigarette smoke) and the heterocyclic amine 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP; found in grilled meats) was indeed catalyzed by a purified system containing only human b5R and cyt b5.", "entity1": "human b5R", "entity2": "4-ABP", "span1": [297, 306], "span2": [98, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5744": {"label": 5, "data": {"text": "Of note, SB265610 which is a close structural analogue of SB225002 with a potent IL-8RB antagonistic activity did not exhibit a similar antimitotic activity.", "entity1": "IL-8RB", "entity2": "SB265610", "span1": [81, 87], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6193": {"label": 3, "data": {"text": "The cardiovascular effects of three different acetylcholinesterase inhibitors: physostigmine, tacrine and rivastigmine injected by intravenous (i.v.)", "entity1": "acetylcholinesterase", "entity2": "physostigmine", "span1": [46, 66], "span2": [79, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5063": {"label": 3, "data": {"text": "Taken together, our results suggested that Rg1 protected against A\u03b225-35-induced apoptosis at least in part by two complementary GR-dependent ERK phosphorylation pathways: (1) down-regulating HIF-1\u03b1 initiated protein nitrotyrosination, and (2) inhibiting mitochondrial apoptotic cascades.", "entity1": "A\u03b225-35", "entity2": "Rg1", "span1": [65, 72], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2004": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Leu", "span1": [121, 125], "span2": [55, 58]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2097": {"label": 0, "data": {"text": "This 40 kDa PEG-conjugated IFNalpha(2a) ((40)PEG-IFNalpha(2a)) is obtained by the covalent binding of one 40 kDa branched PEG-polymer to a lysine side-chain of IFNalpha(2a).", "entity1": "IFNalpha(2a)", "entity2": "lysine", "span1": [160, 172], "span2": [139, 145]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1792": {"label": 3, "data": {"text": "Agents that have only begun to undergo clinical evaluation include CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, and PKI166 and GW572016, both examples of dual kinase inhibitors (inhibiting epidermal growth factor receptor and Her2).", "entity1": "epidermal growth factor receptor", "entity2": "PKI166", "span1": [205, 237], "span2": [132, 138]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15105": {"label": 0, "data": {"text": "Moreover, we show that USP22 is acetylated on multiple lysine residues and that alteration of a single lysine (K129) within the ZnF-UBP domain is sufficient to alter interaction of the DUBm with the core SAGA complex.", "entity1": "USP22", "entity2": "lysine", "span1": [23, 28], "span2": [55, 61]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1404": {"label": 3, "data": {"text": "These results suggest that gemfibrozil inhibits the induction of iNOS probably by inhibiting the activation of NF-kappaB, AP-1, and C/EBPbeta and that gemfibrozil, a prescribed drug for humans, may further find its therapeutic use in neuroinflammatory diseases.", "entity1": "C/EBPbeta", "entity2": "gemfibrozil", "span1": [132, 141], "span2": [27, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2510": {"label": 3, "data": {"text": "IRF3 activation induced by MyD88-independent signaling components, TRIF and TBK1, was also downregulated by auranofin.", "entity1": "IRF3", "entity2": "auranofin", "span1": [0, 4], "span2": [108, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12146": {"label": 2, "data": {"text": "BACKGROUND: The novel antiepileptic drug retigabine is the first selective M-current potassium channel opener for KCNQ2/3 and KCNQ3/5 channels.", "entity1": "M-current potassium channel", "entity2": "retigabine", "span1": [75, 102], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15951": {"label": 1, "data": {"text": "4-Hydroxytamoxifen (OHT, tamoxifen's active form) failed to prevent E2-induced proteolysis of cyclin E and migration, but rather triggered cyclin E cleavage coincident with augmented migration.", "entity1": "cyclin E", "entity2": "4-Hydroxytamoxifen", "span1": [139, 147], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3565": {"label": 1, "data": {"text": "Although the treatment with MSG increased IRS-1 tyrosine phosphorylation (pIRS-1) by 96\u00a0% (MSG, 17.02\u00a0\u00b1\u00a00.6; control, 8.7\u00a0\u00b1\u00a00.2\u00a0a.u.", "entity1": "IRS-1", "entity2": "MSG", "span1": [42, 47], "span2": [28, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14579": {"label": 3, "data": {"text": "P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.", "entity1": "SYK", "entity2": "P505-15", "span1": [118, 121], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"505": {"label": 3, "data": {"text": "The results suggest that the 63-kDa (PDE 1B1) and 60-kDa (PDE 1A2) CaMPDE isozymes are inhibited by felodipine and nicardipine by partial competitive inhibition and that these two Ca2+ antagonists appear to counteract each other.", "entity1": "CaMPDE", "entity2": "felodipine", "span1": [67, 73], "span2": [100, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5646": {"label": 2, "data": {"text": "Arsenic trioxide-induced hERG K(+) channel deficiency can be rescued by matrine and oxymatrine through up-regulating transcription factor Sp1 expression.", "entity1": "hERG", "entity2": "matrine", "span1": [25, 29], "span2": [72, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8837": {"label": 1, "data": {"text": "In the presence of H2O2, calycopterin inhibited decrease in GSH level and SOD activity.", "entity1": "SOD", "entity2": "H2O2", "span1": [74, 77], "span2": [19, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14170": {"label": 1, "data": {"text": "Effect of chalcones on lipid peroxidation, heme oxygenase 1(HO-1), cyclooxygenase (COX), interleukin 5 (IL-5), nitric oxide (NO) and expression of cell adhesion molecules (CAM) is summarized stepwise.", "entity1": "interleukin 5", "entity2": "chalcones", "span1": [89, 102], "span2": [10, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6151": {"label": 1, "data": {"text": "Drug dependent changes in the NMR heteronuclear single-quantum coherence spectra of [methyl-13C]Met-labeled cTnC indicate that bepridil and trifluoperazine bind to similar sites but only in the presence of Ca2+.", "entity1": "cTnC", "entity2": "bepridil", "span1": [108, 112], "span2": [127, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15328": {"label": 1, "data": {"text": "In addition, benzo[c]phenanthrene, fluoranthene, 2,3-dihydroxy-2,3-dihydrofluoranthene, pyrene, 1-hydroxypyrene, 1-nitropyrene, 1-acetylpyrene, 2-acetylpyrene, 2,5,2',5'-tetrachlorobiphenyl, 7-hydroxyflavone, chrysin, and galangin were found to induce a Type I spectral change only with P450 2A13.", "entity1": "P450 2A13", "entity2": "1-hydroxypyrene", "span1": [287, 296], "span2": [96, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8631": {"label": 2, "data": {"text": "Collectively, these findings provide evidence that arsenic causes prolonged activation of Nrf2 through autophagy dysfunction, possibly providing a similar scenario to constitutive activation of Nrf2 found in certain human cancers.", "entity1": "Nrf2", "entity2": "arsenic", "span1": [194, 198], "span2": [51, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7493": {"label": 3, "data": {"text": "Phenserine, a derivative of physostigmine, was first described as an inhibitor of acetylcholinesterase (AChE) and was shown to improve cognition in various experimental paradigms in rodents and dogs.", "entity1": "acetylcholinesterase", "entity2": "physostigmine", "span1": [82, 102], "span2": [28, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13044": {"label": 8, "data": {"text": "Here we demonstrate that PPARgamma, turns on retinoic acid synthesis by inducing the expression of retinol and retinal metabolizing enzymes such as retinol dehydrogenase 10 and retinaldehyde dehydrogenase type 2 (RALDH2).", "entity1": "RALDH2", "entity2": "retinoic acid", "span1": [213, 219], "span2": [45, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6840": {"label": 1, "data": {"text": "Differences in cobalamin and folate levels with the MTRR A66G and MS A2756G polymorphisms were noted.", "entity1": "MTRR", "entity2": "cobalamin", "span1": [52, 56], "span2": [15, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3698": {"label": 3, "data": {"text": "Tolbutamide and gliclazide block the K(ATP) channel K(ir)6.2/Sur1, causing membrane depolarization and stimulating insulin secretion in pancreatic beta cells.", "entity1": "Sur1", "entity2": "Tolbutamide", "span1": [61, 65], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8876": {"label": 1, "data": {"text": "The observations suggest that in 5L cells the Igfbp-4 gene may have got under the control of a promoter containing dioxin responsive element(s) leading to the induction of IGFBP-4 by TCDD.", "entity1": "dioxin responsive element(s)", "entity2": "TCDD", "span1": [115, 143], "span2": [183, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1169": {"label": 1, "data": {"text": "Binding experiments on mitiglinide, nateglinide, and repaglinide to SUR1 expressed in COS-1 cells revealed that they inhibit the binding of [3H]glibenclamide to SUR1 (IC50 values: mitiglinide, 280 nM; nateglinide, 8 microM; repaglinide, 1.6 microM), suggesting that they all share a glibenclamide binding site.", "entity1": "SUR1", "entity2": "repaglinide", "span1": [161, 165], "span2": [224, 235]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14759": {"label": 2, "data": {"text": "Additional mechanistic studies revealed that jaceosidin treatment resulted in an increase in phosphorylation of Cdc25C and ATM-Chk1/2.", "entity1": "ATM", "entity2": "jaceosidin", "span1": [123, 126], "span2": [45, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16037": {"label": 0, "data": {"text": "These compounds resulted from our efforts to merge the pharmacophores of selective factor Xa inhibitor rivaroxaban with a mimic of the Arg-Gly-Asp (RGD) sequence of fibrinogen to obtain designed multiple ligands with potential antithrombotic activity.", "entity1": "fibrinogen", "entity2": "Arg-Gly-Asp", "span1": [165, 175], "span2": [135, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15108": {"label": 1, "data": {"text": "Interestingly, GPx1a was the most sensitive to selenium availability in non stressful conditions, whereas GPx1b1 and GPx1b2 were highly induced by exposure to selenium levels that had some toxic effects on the cells.", "entity1": "GPx1a", "entity2": "selenium", "span1": [15, 20], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8216": {"label": 0, "data": {"text": "With the exception of three residues, the specific amino acids that form the putative binding pocket for ICA in ERG are conserved in EAG.", "entity1": "ERG", "entity2": "amino acids", "span1": [112, 115], "span2": [51, 62]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6936": {"label": 8, "data": {"text": "A double mutant of the two fumarate reductase isozyme genes (OSM1 and FRDS) showed a succinate productivity of 50% as compared to the parent when cells were incubated in glucose-buffered solution.", "entity1": "fumarate reductase", "entity2": "succinate", "span1": [27, 45], "span2": [85, 94]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14907": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO3", "entity2": "TMA", "span1": [71, 75], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10372": {"label": 3, "data": {"text": "The production of Br-Phe5 was reduced with GW660511X while no significant change was observed with omapatrilat after 4 h of incubation.", "entity1": "Br-Phe5", "entity2": "GW660511X", "span1": [18, 25], "span2": [43, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"642": {"label": 2, "data": {"text": "c-fos expression was induced in urethane-anaesthetized rats by intracisternal capsaicin administration.", "entity1": "c-fos", "entity2": "capsaicin", "span1": [0, 5], "span2": [78, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2409": {"label": 2, "data": {"text": "When HUVECs were stimulated by thrombin without extracellular L-arginine, Nor-NOHA dose-dependently increased the NOS activity and the NO release with maximal effects at 20 microM.", "entity1": "NOS", "entity2": "Nor-NOHA", "span1": [114, 117], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9503": {"label": 5, "data": {"text": "cocaine (0.03-3 mg/kg) produced dose-dependent, rapid, and brief increases in blood pressure (BP) in conscious rats pretreated with the dopamine receptor antagonist, SCH 23390.", "entity1": "dopamine receptor", "entity2": "SCH 23390", "span1": [136, 153], "span2": [166, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"5205": {"label": 0, "data": {"text": "We analysed the role of the MBD in MeCP2-chromatin associations in vivo using an MeCP2 mutant Rett syndrome mouse model (Mecp2(tm)(1)(. )(1)(Jae)) in which exon 3 deletion results in an N-terminal truncation of the protein, including most of the MBD.", "entity1": "MeCP2", "entity2": "N", "span1": [81, 86], "span2": [186, 187]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8150": {"label": 3, "data": {"text": "DPEP induced dose-dependent reduction of the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and concomitant reduction in the production of NO and prostaglandin E(2) (PGE(2)).", "entity1": "inducible nitric oxide synthase", "entity2": "DPEP", "span1": [63, 94], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9312": {"label": 9, "data": {"text": "Furthermore, adapalene does not bind to members of the cellular retinoic acid binding protein family.", "entity1": "retinoic acid binding protein", "entity2": "adapalene", "span1": [64, 93], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2275": {"label": 3, "data": {"text": "In this article, the action of dasatinib (BMS-354825) is contrasted with that of imatinib, a kinase inhibitor that is currently being used to treat chronic myelogenous leukemia and other disorders.", "entity1": "kinase", "entity2": "dasatinib", "span1": [93, 99], "span2": [31, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5807": {"label": 8, "data": {"text": "A cDNA encoding the complete amino acid sequence of aminoacylase 1 (N-acylamino acid aminohydrolase, ACY-1) [EC 3.5.1.14], a dimeric metalloprotein having two Zn2+ in the molecule, which catalyzes the deacylation of N-acylated L-amino acids except L-aspartic acid, has been isolated from porcine kidney lambda gt10 cDNA library and sequenced.", "entity1": "aminoacylase 1", "entity2": "N-acylated L-amino acids", "span1": [52, 66], "span2": [216, 240]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"1669": {"label": 1, "data": {"text": "In alpha2B-receptor-expressing HEK293 cells, etomidate rapidly increased phosphorylation of the extracellular signal-related kinases ERK1/2.", "entity1": "alpha2B-receptor", "entity2": "etomidate", "span1": [3, 19], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5838": {"label": 3, "data": {"text": "Terbinafine (Lamisil) has primarily fungicidal action against many fungi as a result of its specific mechanism of squalene epoxidase inhibition.", "entity1": "squalene epoxidase", "entity2": "Terbinafine", "span1": [114, 132], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5157": {"label": 3, "data": {"text": "ThioTEPA (CYP2B6 inhibitor, 25 \u03bcM) and the monoclonal antibody against CYP2B6 but not troleandomycin (CYP3A4 inhibitor, 25 \u03bcM) or the monoclonal antibody against CYP3A4 inhibited ketamine N-demethylation at clinically relevant concentrations.", "entity1": "CYP2B6", "entity2": "ThioTEPA", "span1": [10, 16], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12492": {"label": 8, "data": {"text": "Cynomolgus FMO6 metabolized benzydamine only slightly, but minimal expression of FMO6 in all tissue precludes the importance of FMO6 in drug metabolism, unlike cynomolgus FMO1, FMO2, FMO3, and FMO5 which were all functional.", "entity1": "FMO5", "entity2": "benzydamine", "span1": [193, 197], "span2": [28, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8814": {"label": 2, "data": {"text": "Activation of AMPK using AICAR resulted in STIM1 phosphorylation on serine residues and prevented PAR-1-induced Ca2+ entry.", "entity1": "STIM1", "entity2": "AICAR", "span1": [43, 48], "span2": [25, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9421": {"label": 9, "data": {"text": "Alendronate inhibited PTPmeg1 with an IC50 value of 23 microM, PTPsigma with an IC50 value of 2 microM, and did not inhibit PTP epsilon at concentrations up to 1 mM.", "entity1": "PTP epsilon", "entity2": "Alendronate", "span1": [124, 135], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15870": {"label": 1, "data": {"text": "Immunoblot studies showed that K(+)-depolarization increased CaMKII\u03b1 phosphorylation in a KN-62 sensitive manner and promoted CaMKII\u03b1 binding to D3 receptors.", "entity1": "CaMKII\u03b1", "entity2": "K(+)", "span1": [61, 68], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13407": {"label": 5, "data": {"text": "Thus, H(1) antagonism seems to play a role in part of the beneficial actions of antipsychotics, such as clozapine.", "entity1": "H(1)", "entity2": "clozapine", "span1": [6, 10], "span2": [104, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1356": {"label": 1, "data": {"text": "A series of mazindol (2) and homomazindol (3) analogues with a variety of electron-donating and electron-withdrawing groups in the pendant aryl group and the benzo ring C, as well as H, methoxy, and alkyl groups replacing the hydroxyl group were synthesized, and their binding affinities at the dopamine transporter (DAT) on rat or guinea pig striatal membranes were determined.", "entity1": "dopamine transporter", "entity2": "alkyl", "span1": [295, 315], "span2": [199, 204]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8810": {"label": 1, "data": {"text": "The Ca2+ sensor STIM1 is crucial for activation of store-operated Ca2+ entry (SOCE) through TRPC and Orai channels.", "entity1": "STIM1", "entity2": "Ca2+", "span1": [16, 21], "span2": [4, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8643": {"label": 3, "data": {"text": "Oviduct ER-\u03b1, ER-\u03b2 and uterine ER-\u03b2 were down-regulated by either ethanol or melatonin.", "entity1": "ER-\u03b1", "entity2": "ethanol", "span1": [8, 12], "span2": [66, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"461": {"label": 1, "data": {"text": "Phenylephrine elicited a concentration-dependent positive inotropic effect via alpha 1-adrenoceptors in the presence of either (+/-)-bupranolol or S(-)-timolol.", "entity1": "alpha 1-adrenoceptors", "entity2": "(+/-)-bupranolol", "span1": [79, 100], "span2": [127, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2422": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "arginase I", "entity2": "NO", "span1": [219, 229], "span2": [35, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"542": {"label": 3, "data": {"text": "DHODH inhibition occurs at lower concentrations of A77 1726 than that of tyrosine kinases and is currently considered the major mode of action.", "entity1": "DHODH", "entity2": "A77 1726", "span1": [0, 5], "span2": [51, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9173": {"label": 1, "data": {"text": "Each adduct had a reduced ability to activate cyclic nucleotide phosphodiesterase and myosin light chain kinase, and the chlorpromazine binding capacities of the phenoxybenzamine-calmodulin adducts were diminished to the extent of phenoxybenzamine incorporation into each adduct.", "entity1": "calmodulin", "entity2": "chlorpromazine", "span1": [179, 189], "span2": [121, 135]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15700": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "ASICs", "entity2": "capsaicin", "span1": [63, 68], "span2": [113, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6833": {"label": 3, "data": {"text": "RESULTS: Imatinib, despite equivocal efficacy as monotherapy, reduced pericyte coverage of tumor vessels and enhanced efficacy in combination with metronomic chemotherapy or VEGFR inhibition.", "entity1": "VEGFR", "entity2": "Imatinib", "span1": [174, 179], "span2": [9, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9730": {"label": 0, "data": {"text": "Identification of amino acids in the factor XI apple 3 domain required for activation of factor IX.", "entity1": "factor IX", "entity2": "amino acids", "span1": [89, 98], "span2": [18, 29]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2471": {"label": 2, "data": {"text": "Independent of dietary choline, supplemental Met increased hepatic BHMT activity approximately 30%.", "entity1": "BHMT", "entity2": "choline", "span1": [67, 71], "span2": [23, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15128": {"label": 3, "data": {"text": "Nocapyrone H (1) reduced the pro-inflammatory factor such as nitric oxide (NO), prostaglandin E2 (PGE2) and interleukin-1\u03b2 (IL-1\u03b2).", "entity1": "interleukin-1\u03b2", "entity2": "Nocapyrone H", "span1": [108, 122], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5593": {"label": 1, "data": {"text": "The patients were divided into two groups according to the 5HT-2A affinity of the individual medications (high 5HT-2A affinity--clozapine, olanzapine, risperidone vs. low 5HT-2A affinity--quetiapine, amisulpride).", "entity1": "5HT-2A", "entity2": "olanzapine", "span1": [111, 117], "span2": [139, 149]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4258": {"label": 3, "data": {"text": "Repression of farnesyltransferase (FNTA) by siRNA and the enzyme inhibitor manumycin A caused elevation of ApoA-I secretion from hepatocytes and from transgenic mice expressing hApoA-I and cholesterol ester transfer protein transgenes.", "entity1": "farnesyltransferase", "entity2": "manumycin A", "span1": [14, 33], "span2": [75, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6325": {"label": 1, "data": {"text": "Citalopram protected against the RTI-76-induced inhibition of SERT binding.", "entity1": "SERT", "entity2": "Citalopram", "span1": [62, 66], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9254": {"label": 1, "data": {"text": "Ergovaline inhibition of the binding of the D2-specific radioligand, [3H]YM-09151-2, exhibited a KI (inhibition constant) of 6.9 +/- 2.6 nM, whereas dopamine was much less potent (370 +/- 160 nM).", "entity1": "D2", "entity2": "dopamine", "span1": [44, 46], "span2": [149, 157]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5029": {"label": 5, "data": {"text": "Synthesis and in Vitro Characterisation of Ifenprodil-Based Fluorescein Conjugates as GluN1/GluN2B N-Methyl-D-aspartate Receptor Antagonists.", "entity1": "GluN1", "entity2": "Ifenprodil", "span1": [86, 91], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12677": {"label": 1, "data": {"text": "Rofecoxib has greater selectivity for COX-2 than celecoxib, meloxicam, diclofenac and indomethacin.", "entity1": "COX-2", "entity2": "celecoxib", "span1": [38, 43], "span2": [49, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"500": {"label": 1, "data": {"text": "Although FGF-2 strongly binds to basement membrane heparan sulfate in skin and most other tissue sites examined, FGF-7 fails to bind to basement membrane heparan sulfate in most locations.", "entity1": "FGF-2", "entity2": "sulfate", "span1": [9, 14], "span2": [59, 66]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1071": {"label": 1, "data": {"text": "The capacity of these inhibitors to displace [3H]-oxotremorine-M binding preclude their utilisation for the prevention of acetylcholine catabolism in rat brain membranes, the latter being required to estimate the binding of acetylcholine to [3H]-oxotremorine-M-labelled muscarinic receptors.", "entity1": "muscarinic receptors", "entity2": "[3H]-oxotremorine-M", "span1": [270, 290], "span2": [241, 260]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"606": {"label": 3, "data": {"text": "15d-PGJ2 did not block nuclear translocation or DNA-binding activity of the transcription factor NFkappaB, but it did inhibit the activity of an NFkappaB reporter construct, suggesting that the mechanism of suppression of microglial iNOS by 15d-PGJ2 may involve interference with NFkappaB transcriptional activity in the nucleus.", "entity1": "iNOS", "entity2": "15d-PGJ2", "span1": [233, 237], "span2": [241, 249]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3817": {"label": 1, "data": {"text": "However, a lid conformation was induced by [Sar(1),Gln(2),Ile(8)] AngII, a specific analog that binds to the D281A mutant with better affinity than AngII.", "entity1": "D281A", "entity2": "Gln", "span1": [109, 114], "span2": [51, 54]}, "weak_labels": [-1, -1, 0, 1, -1, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6129": {"label": 5, "data": {"text": "We have investigated the effects of CP-99,994 [(+)-(2s,3s)-3-(2-methoxybenzylamino)-2-phenylpiperidine], a tachykinin NK1 receptor antagonist, HOE 140 (D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin), a bradykinin B2 receptor antagonist, and ketotifen (4-(1-methyl-4-piperidylidene)4 H-benzo[4,5]cycloheptal[1,2-b]thiophen-10(9H)-one hydrogen fumarate), a histamine H1 receptor antagonist with mast cell-stabilizing properties, on microvascular leakage induced by gaseous formaldehyde.", "entity1": "tachykinin NK1 receptor", "entity2": "CP-99,994", "span1": [107, 130], "span2": [36, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10002": {"label": 8, "data": {"text": "The purpose of this study was to determine whether rat outer medullary collecting duct (OMCD) secretes Cl- and whether transepithelial Cl- transport occurs, in part, through Cl- uptake across the basolateral membrane mediated by NKCC1 in series with Cl- efflux across the apical membrane.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [229, 234], "span2": [174, 177]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8474": {"label": 0, "data": {"text": "We report that two common variants of high-temperature requirement A1 (HTRA1) that increase the inherited risk of neovascular age-related macular degeneration (NvAMD) harbor synonymous SNPs within exon 1 of HTRA1 that convert common codons for Ala34 and Gly36 to less frequently used codons.", "entity1": "high-temperature requirement A1", "entity2": "Ala", "span1": [38, 69], "span2": [244, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"3149": {"label": 1, "data": {"text": "Truncation of amitriptyline binding motif on TrkA abrogates the receptor dimerization by amitriptyline.", "entity1": "TrkA", "entity2": "amitriptyline", "span1": [45, 49], "span2": [89, 102]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9037": {"label": 3, "data": {"text": "Interference with lipoxygenase enzymes, rather than a steroid-like inhibition of arachidonic acid release from intracellular phospholipids, seems to be the mode of action.", "entity1": "lipoxygenase", "entity2": "steroid", "span1": [18, 30], "span2": [54, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11937": {"label": 1, "data": {"text": "Fisetin regulates obesity by targeting mTORC1 signaling.", "entity1": "mTORC1", "entity2": "Fisetin", "span1": [39, 45], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12944": {"label": 5, "data": {"text": "However, several promising nonpeptide, vasopressin receptor antagonists have been described; these agents are VPA-985 (lixivaptan), YM-087 (conivaptan), OPC-41061 (tolvaptan), and SR-121463.", "entity1": "vasopressin receptor", "entity2": "VPA-985", "span1": [39, 59], "span2": [110, 117]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8776": {"label": 2, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "p27Kip", "entity2": "CAPE", "span1": [292, 298], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12927": {"label": 8, "data": {"text": "Hydrogen sulfide (H(2)S), a regulatory gaseous molecule that is endogenously synthesized by cystathionine gamma-lyase (CSE) and/or cystathionine beta-synthase (CBS) from L-cysteine (L-Cys) metabolism, is a putative vasodilator, and its role in nitric oxide (NO) production is unexplored.", "entity1": "cystathionine beta-synthase", "entity2": "L-cysteine", "span1": [131, 158], "span2": [170, 180]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1006": {"label": 4, "data": {"text": "METHODS: Part A compared the effects of placebo to four doses of a 5-HT(4) receptor antagonist (SB-207266) on the cisapride mediated increase in plasma aldosterone (a 5-HT(4) mediated response) and orocaecal transit in 18 subjects.", "entity1": "5-HT(4)", "entity2": "cisapride", "span1": [67, 74], "span2": [114, 123]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8897": {"label": 4, "data": {"text": "The preferential alpha 2A-adrenoceptor partial agonist, guanfacine, partially inhibited UK 14,304-induced antinociception.", "entity1": "alpha 2A-adrenoceptor", "entity2": "guanfacine", "span1": [17, 38], "span2": [56, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6970": {"label": 1, "data": {"text": "The mouse orthologue of GPR109A, PUMA-G, is highly expressed in macrophages and other immune cells, and transplantation of wild-type bone marrow into irradiated PUMA-G-deficient mice restored the nicotinic acid-induced flushing response.", "entity1": "PUMA-G", "entity2": "nicotinic acid", "span1": [161, 167], "span2": [196, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8403": {"label": 0, "data": {"text": "Substitution of the FLT3 \"gatekeeper\" phenylalanine with leucine (F691L) conferred mild resistance to ponatinib, but substitutions at the FLT3 activation loop (AL) residue D835 conferred a high degree of resistance.", "entity1": "FLT3", "entity2": "phenylalanine", "span1": [20, 24], "span2": [38, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3909": {"label": 3, "data": {"text": "Neither the superoxide radical scavenger, tiron, nor the inhibitor of the dopamine (DA) transporter, GBR 12909, prevented the metabolites' toxicity.", "entity1": "dopamine (DA) transporter", "entity2": "GBR 12909", "span1": [74, 99], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8023": {"label": 8, "data": {"text": "Dual function inhibitors targeting phospholipase A(2) (PLA(2)) and leukotriene A(4) hydrolase (LTA(4)H) may balance the arachidonic acid (AA) metabolic network and be used as new anti-inflammatory drugs.", "entity1": "LTA(4)H", "entity2": "arachidonic acid", "span1": [95, 102], "span2": [120, 136]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8778": {"label": 3, "data": {"text": "Treatment with CAPE decreased protein abundance of Akt, Akt1, Akt2, Akt3, phospho-Akt Ser473, phospho-Akt Thr 308, GSK3\u03b2, FOXO1, FOXO3a, phospho-FOXO1 Thr24, phospho-FoxO3a Thr32, NF-\u03baB, phospho-NF-\u03baB Ser536, Rb, phospho-Rb Ser807/811, Skp2, and cyclin D1, but increased cell cycle inhibitor p27Kip.", "entity1": "Akt", "entity2": "CAPE", "span1": [51, 54], "span2": [15, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14909": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO1", "entity2": "choline", "span1": [62, 66], "span2": [144, 151]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1304": {"label": 1, "data": {"text": "The results reinforce previous assumptions that dopamine may interact with eicosanoid metabolism by means of D(2) receptor activation, and implicate an involvement of cPLA(2) and COX-2 in this effect.", "entity1": "COX-2", "entity2": "dopamine", "span1": [179, 184], "span2": [48, 56]}, "weak_labels": [-1, -1, -1, -1, 1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13675": {"label": 0, "data": {"text": "Both porcine TLR7 and TLR8 proteins were expressed in cell lines and were N-glycosylated.", "entity1": "TLR8", "entity2": "N", "span1": [22, 26], "span2": [74, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10539": {"label": 1, "data": {"text": "A transcription factor-transcription factor binding array analysis of nuclear lysate from RA-treated cells indicated several prominent RARalpha binding partners; among these, Oct1, NFATc3, and CREB2 were identified by competition EMSA and supershift and chromatin immunoprecipitation assays as components of the complex.", "entity1": "Oct1", "entity2": "RA", "span1": [175, 179], "span2": [90, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2599": {"label": 1, "data": {"text": "In vitro data show comparable affinity to dopamine D(2), D(1) and 5-HT(2A) receptors and recently, FLX showed to be not inferior to risperidone in schizophrenic patients with predominant negative symptomatology, which was implicated with flupentixol's interaction with 5-HT(2A) and/or D(1) receptors.", "entity1": "5-HT(2A) receptors", "entity2": "risperidone", "span1": [66, 84], "span2": [132, 143]}, "weak_labels": [-1, -1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8566": {"label": 2, "data": {"text": "Under NaCl and sorbitol stresses, catalase (CAT) activity in wnk8 mutant was 1.92- and 3.7-times of that in Col-0, respectively.", "entity1": "CAT", "entity2": "sorbitol", "span1": [44, 47], "span2": [15, 23]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8921": {"label": 3, "data": {"text": "The vasopressor response to the calcium channel activator, BAY-K-8644, which is mediated through the opening of voltage dependent calcium channels and the subsequent translocation of extracellular calcium, was significantly inhibited by carvedilol (1 mg/kg, iv), suggesting that carvedilol is also a calcium channel antagonist, consistent with our previous in vitro studies.", "entity1": "voltage dependent calcium channels", "entity2": "carvedilol", "span1": [112, 146], "span2": [237, 247]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10843": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "PDGFRB,", "entity2": "STI571", "span1": [136, 143], "span2": [10, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1712": {"label": 0, "data": {"text": "The amino acid changes caused by the point mutations were clustered in two regions of the Erg1 protein.", "entity1": "Erg1", "entity2": "amino acid", "span1": [90, 94], "span2": [4, 14]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2176": {"label": 1, "data": {"text": "MELANOTAN (NDP-MSH) binds the MC1 receptor to significantly increase the eumelanin content of human skin cells.", "entity1": "MC1 receptor", "entity2": "MELANOTAN", "span1": [30, 42], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7753": {"label": 0, "data": {"text": "By synthesizing and testing a series of alanine point-mutated cyclic peptides, we identified which amino acid was important for the inhibition of the phospholamban function.", "entity1": "phospholamban", "entity2": "amino acid", "span1": [150, 163], "span2": [99, 109]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2345": {"label": 1, "data": {"text": "Lutein and eicosapentaenoic acid interact to modify iNOS mRNA levels through the PPARgamma/RXR pathway in chickens and HD11 cell lines.", "entity1": "RXR", "entity2": "eicosapentaenoic acid", "span1": [91, 94], "span2": [11, 32]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14111": {"label": 2, "data": {"text": "CRBN mediated antiproliferative activities of lenalidomide and pomalidomide in myeloma cells, as well as lenalidomide- and pomalidomide-induced cytokine production in T cells.", "entity1": "cytokine", "entity2": "pomalidomide", "span1": [144, 152], "span2": [123, 135]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8193": {"label": 0, "data": {"text": "We found that SIRT1 induced p300 down-regulation via the ubiquitin-proteasome pathway by deacetylation of lysine residues for ubiquitination.", "entity1": "proteasome", "entity2": "lysine", "span1": [67, 77], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"38": {"label": 1, "data": {"text": "In membranes of control but not of pertussis toxin-treated cells, adrenaline via alpha 2-adrenoceptors stimulated incorporation of the photo-reactive GTP analog [alpha-32P]GTP azidoanilide into pertussis toxin substrates comigrating with the alpha-subunits of Gi2, Go2, and the not further identified Go subtype.", "entity1": "alpha 2-adrenoceptors", "entity2": "adrenaline", "span1": [81, 102], "span2": [66, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, 9]},
	"7246": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rat trace amine-associated receptor 1", "entity2": "beta-phenylethylamine", "span1": [192, 229], "span2": [85, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8030": {"label": 2, "data": {"text": "Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.", "entity1": "TRPA1", "entity2": "apomorphine", "span1": [95, 100], "span2": [49, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7033": {"label": 2, "data": {"text": "Further, cholesterol metabolites, predominantly the oxysterols, the natural ligands for liver X receptor (LXR), induced these genes via upregulation of sterol regulatory element binding protein-1c (SREBP-1c) that bound to the regulatory regions of these genes.", "entity1": "SREBP-1c", "entity2": "cholesterol", "span1": [198, 206], "span2": [9, 20]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4234": {"label": 3, "data": {"text": "Particularly, the effects of doxycycline used as a non selective MMP inhibitor in experimental and clinical studies will be discussed.", "entity1": "MMP", "entity2": "doxycycline", "span1": [65, 68], "span2": [29, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15795": {"label": 8, "data": {"text": "Consistent with two glucose uptake pathways, induced uptake of 2-NBDG, a fluorescent glucose derivative, was decreased by inhibition of HCs or glucose transporter (GLUT4), and blocked by dual blockade.", "entity1": "glucose transporter", "entity2": "2-NBDG", "span1": [143, 162], "span2": [63, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15139": {"label": 3, "data": {"text": "Cloning, Characterization, and Sulfonamide and Thiol Inhibition Studies of an \u03b1-Carbonic Anhydrase from Trypanosoma cruzi, the Causative Agent of Chagas Disease.", "entity1": "\u03b1-Carbonic Anhydrase", "entity2": "Thiol", "span1": [78, 98], "span2": [47, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9703": {"label": 3, "data": {"text": "The nonselective and irreversible MAO inhibitors, phenelzine (3-10 mg/kg), tranylcypromine (1-3 mg/kg), and nialamide (30 mg/kg), decreased rates of responding maintained by ethanol reinforcement.", "entity1": "MAO", "entity2": "tranylcypromine", "span1": [34, 37], "span2": [75, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12323": {"label": 2, "data": {"text": "Ribavirin also enhanced recruitment of CDK9 (cyclin-dependent kinase 9) and AFF4 to F7.", "entity1": "AFF4", "entity2": "Ribavirin", "span1": [76, 80], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4832": {"label": 2, "data": {"text": "To this end, 158N murine oligodendrocytes were treated with 7KC or 7\u03b2OHC inducing an apoptotic mode of cell death characterized by condensation/fragmentation of the nuclei, dephosphorylation of Akt and GSK3, mitochondrial depolarization involving Mcl-1, and caspase-3 activation.", "entity1": "caspase-3", "entity2": "7KC", "span1": [258, 267], "span2": [60, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8740": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "amitriptyline", "span1": [18, 25], "span2": [79, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"930": {"label": 3, "data": {"text": "When DLD-1/FdUrd cells expressing increased TS mRNA were treated with FdUrd and F3(d)Thd for only 4 h, the resistance ratios of DLD-1/FdUrd cells to parental DLD-1 cells were markedly different for FdUrd and F3(d)Thd, suggesting that the cytotoxicity with short-time exposure to F3(d)Thd is due to a mechanism other than TS inhibition, although the cytotoxicity of F3(d)Thd in the short-time is low compared to that of long-time exposure.", "entity1": "TS", "entity2": "F3(d)Thd", "span1": [321, 323], "span2": [279, 287]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"42": {"label": 3, "data": {"text": "Adrenaline inhibits insulin secretion via pertussis toxin-sensitive mechanisms.", "entity1": "insulin", "entity2": "Adrenaline", "span1": [20, 27], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12623": {"label": 1, "data": {"text": "In addition, three IP ligands, iloprost, carbacyclin and isocarbacyclin, and one TP ligand, STA2, bound to this receptor with Ki values comparable to the Ki values of these compounds for the IP and TP receptors, respectively.", "entity1": "TP", "entity2": "STA2", "span1": [81, 83], "span2": [92, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10845": {"label": 3, "data": {"text": "Imatinib (STI571, Gleevec, Glivec; Novartis Pharmaceuticals, East Hanover, NJ), a selective inhibitor of KIT, ABL, BCR-ABL, PDGFRA, and PDGFRB, represents a new paradigm of targeted cancer therapy and has revolutionized the treatment of patients with chronic myelogenous leukemia and GISTs.", "entity1": "ABL", "entity2": "Gleevec", "span1": [110, 113], "span2": [18, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1658": {"label": 5, "data": {"text": "Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists.", "entity1": "histamine H1-receptor", "entity2": "levocetirizine", "span1": [97, 118], "span2": [77, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11490": {"label": 1, "data": {"text": "RESULTS: Ketorolac was six times more active against COX-1 (IC(50) = 0.02 microM) than COX-2 (IC(50) = 0.12 microM) while bromfenac was approximately 32 times more active against COX-2 (IC(50) = 0.0066 microM) than COX-1 (IC(50) = 0.210 microM).", "entity1": "COX-1", "entity2": "bromfenac", "span1": [215, 220], "span2": [122, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15414": {"label": 1, "data": {"text": "This study evaluates the production of inflammatory biomarkers (IL-1\u03b2, IL-8, IL-10, TNF\u03b1) and the influence of gene expression transporters and enzymes related to cholesterol absorption and metabolism (NPC1L1, ABCG5/8, HMGCoA, ACAT) produced by 7-ketosterols (stigmasterol/cholesterol) in Caco-2 cells.", "entity1": "ACAT", "entity2": "stigmasterol", "span1": [227, 231], "span2": [260, 272]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1, -1]},
	"5837": {"label": 3, "data": {"text": "Terbinafine: mode of action and properties of the squalene epoxidase inhibition.", "entity1": "squalene epoxidase", "entity2": "Terbinafine", "span1": [50, 68], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12893": {"label": 1, "data": {"text": "Collectively, our results suggest that H(2)S can inhibit NO production and NF-kappaB activation in LPS-stimulated macrophages through a mechanism that involves the action of HO-1/CO.", "entity1": "HO-1", "entity2": "H(2)S", "span1": [174, 178], "span2": [39, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"8085": {"label": 2, "data": {"text": "We identified one compound, E235 (N-(1-benzyl-piperidin-4-yl)-2-(4-fluoro-phenyl)-benzo[d]imidazo[2,1-b]thiazole-7-carboxamide), that activated the ISR and dose-dependently increased levels of ATF4 in transformed cells.", "entity1": "ATF4", "entity2": "E235", "span1": [193, 197], "span2": [28, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13924": {"label": 1, "data": {"text": "In pig parathyroid cells, paricalcitol and the active form of doxercalciferol induced VDR translocation from the cytoplasm into the nucleus, suppressed PTH mRNA expression and inhibited cell proliferation in a similar manner, although paricalcitol induced the expression of CaSR mRNA more effectively.", "entity1": "VDR", "entity2": "paricalcitol", "span1": [86, 89], "span2": [26, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8861": {"label": 2, "data": {"text": "Phosphorylation of c-Src, which was shown to be activated by AhR ligands, was also increased by I3S and TCDD, and blocking of c-Src activity by 4-amino-5-(4-chlorophenyl)-7-(t-butyl) pyrazolo[3,4-d]pyrimidine (PP2) inhibited phosphorylation of both c-Src and STAT3, raising a possibility that stimulatory activities of I3S and TCDD on Th17 differentiation could be exerted via increased phosphorylation of c-Src, which in turn stimulates STAT3 activation.", "entity1": "STAT3", "entity2": "I3S", "span1": [438, 443], "span2": [319, 322]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7340": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "neutral amino acid transporters", "entity2": "alanine", "span1": [133, 164], "span2": [90, 97]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6614": {"label": 5, "data": {"text": "Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol.", "entity1": "Histamine H1-receptor", "entity2": "homochlorcyclizine", "span1": [0, 21], "span2": [52, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6927": {"label": 9, "data": {"text": "On the other hand, the FUM1 (fumarase) gene disrupted mutant produced significantly higher levels of fumarate but did not form malate at all.", "entity1": "fumarase", "entity2": "malate", "span1": [29, 37], "span2": [127, 133]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"7171": {"label": 5, "data": {"text": "OBJECTIVE: Telmisartan, an angiotensin II type 1 receptor (AT1R) antagonist, was found to have a unique property: it is a partial agonist of peroxisome proliferator-activated receptor gamma (PPARgamma).", "entity1": "angiotensin II type 1 receptor", "entity2": "Telmisartan", "span1": [27, 57], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2476": {"label": 4, "data": {"text": "The beta(2)-adrenoceptor (beta(2)-AR) agonists clenbuterol and fenoterol have similar beneficial effects in animal models of heart failure.", "entity1": "beta(2)-AR", "entity2": "fenoterol", "span1": [26, 36], "span2": [63, 72]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"449": {"label": 4, "data": {"text": "Pretreatment of the tissues with combined 5-HT1/5-HT2 antagonists, methysergide (1 microM) or methiothepin (0.1 microM), significantly attenuated the inhibitory effect of epinastine on the noncholinergic contraction.", "entity1": "5-HT1", "entity2": "epinastine", "span1": [42, 47], "span2": [171, 181]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4689": {"label": 2, "data": {"text": "Upon co-exposure to V(5+) and TCDD, V(5+) significantly potentiated the TCDD-mediated induction of the Cyp1a1, Cyp1a2, and Cyp1b1 mRNA, protein, and catalytic activity levels at 24\u00a0h. In vitro, V(5+) decreased the TCDD-mediated induction of Cyp1a1 mRNA, protein, and catalytic activity levels.", "entity1": "Cyp1b1", "entity2": "TCDD", "span1": [123, 129], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10210": {"label": 8, "data": {"text": "Direct transport of rifampicin could be shown for OATP-C (apparent K(m) value 13 micromol/L) and OATP8 (2.3 micromol/L).", "entity1": "OATP-C", "entity2": "rifampicin", "span1": [50, 56], "span2": [20, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7426": {"label": 8, "data": {"text": "The use of Delta 6 desaturase (D6D) twice in the conversion of alpha-linolenic acid (ALA; 18:3n-3) to docosahexaenoic acid (DHA; 22:6n-3) suggests that this enzyme may play a key regulatory role in the synthesis and accumulation of DHA from ALA.", "entity1": "Delta 6 desaturase", "entity2": "ALA", "span1": [11, 29], "span2": [241, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"13001": {"label": 1, "data": {"text": "The short lifetime of IP3 makes this detection very challenging in measuring GPCR responses.", "entity1": "GPCR", "entity2": "IP3", "span1": [77, 81], "span2": [22, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3807": {"label": 4, "data": {"text": "As far as we are aware, the compound's 1,3,5-triazine scaffold represents a new core structure for CB2 agonists.", "entity1": "CB2", "entity2": "1,3,5-triazine", "span1": [99, 102], "span2": [39, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"941": {"label": 1, "data": {"text": "In contrast, 2, 4-dioxo-5-acetamido-6-phenylhexanoic acid, which is a competitive inhibitor with respect to ascorbate, exhibits a low degree of stereospecificity in binding to the ascorbate sites of both PAM and dopamine-beta-hydroxylase.", "entity1": "dopamine-beta-hydroxylase", "entity2": "2, 4-dioxo-5-acetamido-6-phenylhexanoic acid", "span1": [212, 237], "span2": [13, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10596": {"label": 1, "data": {"text": "Even though its inability to shift between the trivalent and a divalent oxidation state precludes that gallium behaves as an iron analogue in every respect, it strongly interferes with cellular acquisition of iron from blood by competitive interaction with transferrin and transferrin receptor-mediated endocytosis.", "entity1": "transferrin receptor", "entity2": "iron", "span1": [273, 293], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"16063": {"label": 8, "data": {"text": "Simvastatin and lovastatin metabolized through CYP3A have the highest potency for drug-drug interaction with potent CYP3A inhibitors such as ritonavir- or cobicistat-boosted HIV-PI or the hepatitis C virus (HCV) PI, telaprevir or boceprevir, and therefore their coadministration is contraindicated.", "entity1": "CYP3A", "entity2": "lovastatin", "span1": [47, 52], "span2": [16, 26]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11069": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "caldesmon kinase", "entity2": "felodipine", "span1": [110, 126], "span2": [202, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13640": {"label": 0, "data": {"text": "In the presence of drug, the linker is rigid and this alpha-helix extends to include Gly and the preceding Leu.", "entity1": "alpha-helix", "entity2": "Gly", "span1": [54, 65], "span2": [85, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6157": {"label": 1, "data": {"text": "We report here the use of Met methyl groups as site-specific structural markers to identify drug binding sites for trifluoperazine and bepridil on cTnC.", "entity1": "cTnC", "entity2": "trifluoperazine", "span1": [147, 151], "span2": [115, 130]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7632": {"label": 9, "data": {"text": "Triphosphate nucleotides (ATP, GTP, and UTP) rapidly and reversibly inhibited Panx1 currents via mechanism(s) independent of purine receptors.", "entity1": "purine receptors", "entity2": "UTP", "span1": [125, 141], "span2": [40, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3485": {"label": 2, "data": {"text": "On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-\u03b3, GLUT-4 and adiponectin.", "entity1": "PPAR-\u03b3", "entity2": "gentianine", "span1": [158, 164], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"608": {"label": 1, "data": {"text": "Therefore, the objective of the present study was to investigate the effects of PLA2 inhibitors p-bromophenacyl bromide (BPB) and arachidonyl trifluoromethyl ketone (AACOCF3) on interleukin-2 (IL-2) expression in murine primary splenocytes.", "entity1": "IL-2", "entity2": "p-bromophenacyl bromide", "span1": [193, 197], "span2": [96, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2851": {"label": 2, "data": {"text": "cAspAT activity, as well as the incorporation of [(14)C]aspartate into the neutral lipid fraction of 3T3-F442A adipocytes was stimulated by the thiazolidinedione (TZD) rosiglitazone.", "entity1": "cAspAT", "entity2": "TZD", "span1": [0, 6], "span2": [163, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12840": {"label": 8, "data": {"text": "When expressed heterologously in a mammalian cell line, rabbit PAT1 mediates pH-dependent, Na(+)-independent uptake of proline, glycine, l-alanine and alpha-(methylamino)isobutyric acid.", "entity1": "rabbit PAT1", "entity2": "l-alanine", "span1": [56, 67], "span2": [137, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6162": {"label": 3, "data": {"text": "A 59-year-old female suffering from malignant lymphoma developed therapy-related acute myeloblastic leukemia (t-AML) after chemotherapy consisting of treatment with DNA-topoisomerase II inhibitors, etoposide and mitoxantrone, and an alkylating agent, cyclophosphamide.", "entity1": "DNA-topoisomerase II", "entity2": "etoposide", "span1": [165, 185], "span2": [198, 207]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10747": {"label": 3, "data": {"text": "Clinical studies in cancer patients treated with the new fluoropyrimidine analogue capecitabine (N4-pentoxycarbonyl-5'-5-fluorocytidine) have shown that plasma 2'-deoxyuridine was significantly elevated after 1 week of treatment, consistent with inhibition of thymidylate synthase (TS).", "entity1": "thymidylate synthase", "entity2": "capecitabine", "span1": [260, 280], "span2": [83, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2053": {"label": 0, "data": {"text": "In this study, we show that mutation of Arg228, a residue in the vicinity of Glu317, to lysine (R228K-Gal-T1) results in a 15-fold higher Glc-T activity, which is further enhanced by LA to nearly 25% of the Gal-T activity of the wild type.", "entity1": "Gal-T", "entity2": "lysine", "span1": [207, 212], "span2": [88, 94]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4107": {"label": 2, "data": {"text": "Thus, SFO contributes to the instability of atherosclerotic plaque in apoE(-/-) mice through activating p75(NTR) and IL-8 and cell apoptosis in plaque.", "entity1": "IL-8", "entity2": "SFO", "span1": [117, 121], "span2": [6, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9596": {"label": 3, "data": {"text": "Crystallographic comparison with the structurally related rat tyrosine hydroxylase binary complex with the oxidized cofactor 7,8-dihydrobiopterin revealed overlapping binding sites for the catechols and the cofactor, compatible with a competitive type of inhibition of the catechols versus BH4.", "entity1": "rat tyrosine hydroxylase", "entity2": "catechols", "span1": [58, 82], "span2": [273, 282]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"15545": {"label": 2, "data": {"text": "Reverse transcription polymerase chain reaction (RT-PCR) and western blot analyses revealed that CK inhibited DMN-induced increases in matrix metalloproteinase-13 (MMP-13), tissue inhibitor of metalloproteinase-1 (TIMP-1), and tumor necrosis factor-\u03b1 (TNF-\u03b1) mRNA, and collagen type I and \u03b1-smooth muscle actin protein.", "entity1": "collagen type I", "entity2": "DMN", "span1": [269, 284], "span2": [110, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4248": {"label": 2, "data": {"text": "Butein also increased heme oxygenase-1 (HO-1) protein expression and HO activity.", "entity1": "heme oxygenase-1", "entity2": "Butein", "span1": [22, 38], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13893": {"label": 1, "data": {"text": "Molecular models of the MMP-2-captopril complex were simulated by 1000 iterations of random docking and energy minimization.", "entity1": "MMP-2", "entity2": "captopril", "span1": [24, 29], "span2": [30, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4352": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "survivin", "entity2": "pinosylvin", "span1": [261, 269], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8521": {"label": 3, "data": {"text": "We then evaluated the interactions with the CYP3A inhibitor ketoconazole (400\u2009mg q.d.)", "entity1": "CYP3A", "entity2": "ketoconazole", "span1": [44, 49], "span2": [60, 72]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6224": {"label": 1, "data": {"text": "Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.", "entity1": "human 5-HT1B", "entity2": "rizatriptan", "span1": [101, 113], "span2": [60, 71]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10930": {"label": 1, "data": {"text": "Losartan (parent compound), has moderate affinity for the AT(1) receptor (competitive inhibition).", "entity1": "AT(1) receptor", "entity2": "Losartan", "span1": [58, 72], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9426": {"label": 1, "data": {"text": "Similarly, with the src-pY527 substrate, alendronate inhibition was also PTP dependent.", "entity1": "PTP", "entity2": "alendronate", "span1": [73, 76], "span2": [41, 52]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10733": {"label": 5, "data": {"text": "We have analyzed binding domains of the oxytocin receptor for barusiban, a highly selective oxytocin receptor antagonist, in comparison to the combined vasopressin V1A/oxytocin receptor antagonist atosiban and the agonists oxytocin and carbetocin.", "entity1": "oxytocin receptor", "entity2": "barusiban", "span1": [92, 109], "span2": [62, 71]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12563": {"label": 1, "data": {"text": "5-Methylurapidil and phentolamine were confirmed as selective for the alpha 1A-adrenoceptors, whereas spiperone was alpha 1B-selective.", "entity1": "alpha 1A-adrenoceptors", "entity2": "5-Methylurapidil", "span1": [70, 92], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7070": {"label": 1, "data": {"text": "The cholesterol-lowering drug simvastatin inhibits LFA-1 signaling by binding to an allosteric site on CD11a (LFA-1 alpha chain), which leads to immunomodulation.", "entity1": "CD11a", "entity2": "simvastatin", "span1": [103, 108], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 6, 6, -1, -1, -1, -1, -1, -1, -1]},
	"4573": {"label": 1, "data": {"text": "Inhibition of lysosomes or proteasomes by co-treatment with antofine and their respective specific inhibitors, NH4Cl or MG132, partially inhibited the antofine-induced decrease in Cx43 protein levels, but did not inhibit the antofine-induced inhibition of GJIC.", "entity1": "Cx43", "entity2": "NH4Cl", "span1": [180, 184], "span2": [111, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3463": {"label": 1, "data": {"text": "Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C.", "entity1": "E2C", "entity2": "[2-(trimethylammonium)ethyl]-methanethiosulfonate", "span1": [236, 239], "span2": [164, 213]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3889": {"label": 1, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "Myc", "entity2": "N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine", "span1": [198, 201], "span2": [85, 149]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10780": {"label": 3, "data": {"text": "Imatinib mesylate is a tyrosine kinase inhibitor of the ABL, platelet-derived growth factor receptor (PDGFR), and c-kit kinases.", "entity1": "platelet-derived growth factor receptor", "entity2": "Imatinib mesylate", "span1": [61, 100], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15064": {"label": 9, "data": {"text": "The increase in SAA expression is specific to ritodrine-induced liver damage, because SAA expression was not induced by other hepatotoxic drugs such as acetaminophen, valproic acid, or metformin.", "entity1": "SAA", "entity2": "acetaminophen", "span1": [86, 89], "span2": [152, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4773": {"label": 3, "data": {"text": "Gelatin zymography showed that DMBT inhibited secretion and activity of MMP-9.", "entity1": "MMP-9", "entity2": "DMBT", "span1": [72, 77], "span2": [31, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15916": {"label": 4, "data": {"text": "The current study examined the bioactivation potential of ghrelin receptor inverse agonists, 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(imidazo[2,1-b]thiazol-6-yl)ethanone (1) and 1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone (2), containing a fused imidazo[2,1-b]thiazole motif in the core structure.", "entity1": "ghrelin receptor", "entity2": "1-(2-(2-chloro-4-(2H-1,2,3-triazol-2-yl)benzyl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone", "span1": [58, 74], "span2": [219, 344]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12410": {"label": 1, "data": {"text": "Finally, carotid artery-infusion of HENA (45 \u03bcM) dilated the pial cerebral arterioles via selective BK-channel targeting.", "entity1": "BK-channel", "entity2": "HENA", "span1": [100, 110], "span2": [36, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7679": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "carbonic anhydrase", "entity2": "methazolamide", "span1": [93, 111], "span2": [219, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11731": {"label": 0, "data": {"text": "The 3D-structure of HmTx consists of three conserved alpha-helices: h1 (Lys24-His34), h2 (Cys59-Asp71), and h3 (Ala80-Phe89).", "entity1": "HmTx", "entity2": "Cys", "span1": [20, 24], "span2": [90, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2673": {"label": 3, "data": {"text": "However, a lower concentration of dipyridamole (3 microM) that blocks PDE9, PDE10, and PDE11, but not PDE8, did not inhibit ecto-phosphodiesterase activity.", "entity1": "PDE11", "entity2": "dipyridamole", "span1": [87, 92], "span2": [34, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"808": {"label": 1, "data": {"text": "The modulation of high-voltage-activated (HVA) Ca2+ channels by the prostaglandin E series (PGE1 and PGE2) was studied in the paratracheal ganglion cells.", "entity1": "high-voltage-activated (HVA) Ca2+ channels", "entity2": "PGE2", "span1": [18, 60], "span2": [101, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1399": {"label": 3, "data": {"text": "Interestingly, gemfibrozil strongly inhibited the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of GAS in cytokine-stimulated astroglial cells.", "entity1": "AP-1", "entity2": "gemfibrozil", "span1": [75, 79], "span2": [15, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3864": {"label": 3, "data": {"text": "HSYA suppressed the expression of TLR-4, Myd88, ICAM-1, TNF\u03b1, IL-1\u03b2 and IL-6 at the mRNA and protein level, and inhibited the adhesion of leukocytes to A549 cells.", "entity1": "TLR-4", "entity2": "HSYA", "span1": [34, 39], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3919": {"label": 3, "data": {"text": "N-alkylation of the pyridazinone ring markedly enhances potency against PDE4 but suppresses PDE3 inhibition.", "entity1": "PDE4", "entity2": "pyridazinone", "span1": [72, 76], "span2": [20, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"498": {"label": 1, "data": {"text": "In summary, distinct and specific affinities of heparan sulfates for different FGFs were identified that may affect growth factor activation and local distribution.", "entity1": "FGFs", "entity2": "sulfates", "span1": [79, 83], "span2": [56, 64]}, "weak_labels": [-1, -1, -1, -1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13679": {"label": 1, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "imidazoquinoline", "span1": [138, 142], "span2": [4, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4501": {"label": 9, "data": {"text": "Lastly, both hCES1 and hCES2 were shown not to catalyze the hydrolysis of the acyl glucuronides studied.", "entity1": "hCES2", "entity2": "acyl glucuronides", "span1": [23, 28], "span2": [78, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, 9]},
	"3365": {"label": 3, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "L-VGCCs", "entity2": "ethanol", "span1": [153, 160], "span2": [69, 76]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11397": {"label": 3, "data": {"text": "Using whole-cell voltage clamp, we examined mibefradil block of four Na+ channel isoforms expressed in human embryonic kidney cells: Nav1.5 (cardiac), Nav1.4 (skeletal muscle), Nav1.2 (brain), and Nav1.7 (peripheral nerve).", "entity1": "Nav1.7", "entity2": "mibefradil", "span1": [197, 203], "span2": [44, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14221": {"label": 1, "data": {"text": "These results suggest that the regulation of nitrergic system by ERs may play a role in the control of oestrogen-dependent physiological mechanisms regulated by the SON and the PVN.", "entity1": "ERs", "entity2": "oestrogen", "span1": [65, 68], "span2": [103, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3185": {"label": 4, "data": {"text": "RGM-1 cells were treated with CDCA or GW4064, an FXR agonist, in the presence or absence of guggulsterone, an FXR antagonist.", "entity1": "FXR", "entity2": "CDCA", "span1": [49, 52], "span2": [30, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11480": {"label": 1, "data": {"text": "OBJECTIVE: To compare the cyclooxygenase (COX) activity and anti-inflammatory effects of the nonsteroidal anti-inflammatory drugs (NSAIDs) ketorolac tromethamine (ketorolac) and bromfenac sodium (bromfenac).", "entity1": "cyclooxygenase", "entity2": "bromfenac sodium", "span1": [26, 40], "span2": [178, 194]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4321": {"label": 2, "data": {"text": "Pinosylvin inhibited the proliferation of HCT 116 cells by arresting transition of cell cycle from G1 to S phase along with the downregulation of cyclin D1, cyclin E, cyclin A, cyclin dependent kinase 2 (CDK2), CDK4, c-Myc, and retinoblastoma protein (pRb), and the upregulation of p21(WAF1/CIP1) and p53.", "entity1": "p53", "entity2": "Pinosylvin", "span1": [301, 304], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9611": {"label": 1, "data": {"text": "These results suggest that SUR1 binds 8-azido-ATP strongly at NBF1 and that MgADP, either by direct binding to NBF2 or by hydrolysis of bound MgATP at NBF2, stabilizes prebound 8-azido-ATP binding at NBF1.", "entity1": "SUR1", "entity2": "8-azido-ATP", "span1": [27, 31], "span2": [38, 49]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5042": {"label": 3, "data": {"text": "New classes of pyrrole-derived nitrooxyalkyl inverse esters, carbonates, and ethers (7-10) as COX-2 selective inhibitors and NO donors were synthesized and are herein reported.", "entity1": "COX-2", "entity2": "carbonates", "span1": [94, 99], "span2": [61, 71]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4667": {"label": 3, "data": {"text": "To determine whether dysregulation of SIRT1 promotes NADPH oxidase-dependent production of reactive oxygen species (ROS) and impairs endothelial function we assessed the effects of three structurally different inhibitors of SIRT1 (nicotinamide, sirtinol, EX527) in aorta segments isolated from young Wistar rats.", "entity1": "SIRT1", "entity2": "sirtinol", "span1": [224, 229], "span2": [245, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2229": {"label": 1, "data": {"text": "Computer modeling suggests that the KITD816V mutation destabilizes the inactive conformation of the KIT activation loop to which imatinib binds, but it is not predicted to impair binding of KIT by dasatinib.", "entity1": "KIT", "entity2": "imatinib", "span1": [190, 193], "span2": [129, 137]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"8048": {"label": 3, "data": {"text": "Exposure of H9c2 cells to high glucose reduced AMPK activity, inhibited Jun NH2-terminal kinase 1 (JNK1)-B-cell lymphoma 2 (Bcl-2) signaling, and promoted Beclin1 binding to Bcl-2.", "entity1": "AMPK", "entity2": "glucose", "span1": [47, 51], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"978": {"label": 3, "data": {"text": "Pretreatment with lysosomal enzyme inhibitors [(2S, 3S)trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester or chloroquine] or proteasome inhibitors (proteasome inhibitor I, MG-132, or lactacystin) decreased the extent of U50,488H-induced down-regulation.", "entity1": "proteasome", "entity2": "MG-132", "span1": [158, 168], "span2": [182, 188]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7838": {"label": 2, "data": {"text": "We found that intracellular GTP depletion by ribavirin as well as other IMPDH (inosine-5'-monophosphate dehydrogenase) inhibitors, such as mycophenolic acid and 6-mercaptopurine, up-regulated F7 expression.", "entity1": "F7", "entity2": "mycophenolic acid", "span1": [192, 194], "span2": [139, 156]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5899": {"label": 3, "data": {"text": "Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms.", "entity1": "plasma very-low-density lipoproteins", "entity2": "fibric acids", "span1": [95, 131], "span2": [18, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11894": {"label": 8, "data": {"text": "Cycloxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) has been shown to be important in esophageal tumorigenesis.", "entity1": "COX-2", "entity2": "PGE2", "span1": [17, 22], "span2": [50, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7450": {"label": 1, "data": {"text": "Ovariectomy downregulates glutaredoxin and renders female mice vulnerable to L-BOAA toxicity as evidenced by activation of AP1, loss of GSH and complex I activity indicating the important role of glutaredoxin in neuroprotection.", "entity1": "glutaredoxin", "entity2": "L-BOAA", "span1": [26, 38], "span2": [77, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11600": {"label": 8, "data": {"text": "Hydrogen sulphide (H(2)S) is synthesized from L-cysteine via the action of cystathionine-gamma-lyase (CSE) and cystathionine-beta-synthase (CBS).", "entity1": "CSE", "entity2": "Hydrogen sulphide", "span1": [102, 105], "span2": [0, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14399": {"label": 3, "data": {"text": "Herein, we report the identification and characterization of 3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile (ESI-09), a novel noncyclic nucleotide EPAC antagonist that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic \u03b2 cells.", "entity1": "insulin", "entity2": "3-(5-tert-butyl-isoxazol-3-yl)-2-[(3-chloro-phenyl)-hydrazono]-3-oxo-propionitrile", "span1": [334, 341], "span2": [61, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13033": {"label": 8, "data": {"text": "11Beta-HSD1 activates cortisone to cortisol to facilitate glucocorticoid receptor (GR)-mediated action.", "entity1": "11Beta-HSD1", "entity2": "cortisol", "span1": [0, 11], "span2": [35, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2651": {"label": 9, "data": {"text": "Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.", "entity1": "phosphodiesterase", "entity2": "erythro-9-(2-hydroxy-3-nonyl)adenine", "span1": [397, 414], "span2": [82, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2457": {"label": 9, "data": {"text": "The adenosine triphosphate binding cassette (ABC)-transporter ABCC2 (MRP2/cMOAT) can mediate resistance against the commonly used anticancer drugs cisplatin and paclitaxel.", "entity1": "MRP2", "entity2": "cisplatin", "span1": [69, 73], "span2": [147, 156]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10294": {"label": 5, "data": {"text": "Practical asymmetric synthesis of aprepitant, a potent human NK-1 receptor antagonist, via a stereoselective Lewis acid-catalyzed trans acetalization reaction.", "entity1": "NK-1 receptor", "entity2": "aprepitant", "span1": [61, 74], "span2": [34, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"10278": {"label": 2, "data": {"text": "Long-term administration of propargylamines to rats increased the activities of antioxidative enzymes superoxide dismutase (SOD) and catalase in the brain regions containing dopamine neurons.", "entity1": "superoxide dismutase", "entity2": "propargylamines", "span1": [102, 122], "span2": [28, 43]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12748": {"label": 2, "data": {"text": "Thus, the biological activity of IMQ appears to exceed its previously known functions, inasmuch as it boosts up significantly the perforin-granule system.", "entity1": "perforin", "entity2": "IMQ", "span1": [130, 138], "span2": [33, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8415": {"label": 1, "data": {"text": "Bisacylimidoselenocarbamates Cause G2/M Arrest Associated with the Modulation of CDK1 and Chk2 in Human Breast Cancer MCF-7 Cells.", "entity1": "CDK1", "entity2": "Bisacylimidoselenocarbamates", "span1": [81, 85], "span2": [0, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14045": {"label": 1, "data": {"text": "mTOR was still inhibited by aspirin in CRC cells after siRNA knockdown of AMPKalpha, indicating AMPK-dependent and AMPK-independent mechanisms of aspirin-induced inhibition of mTOR.", "entity1": "AMPK", "entity2": "aspirin", "span1": [96, 100], "span2": [146, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13922": {"label": 3, "data": {"text": "The extent and rate of inhibition are similar to that seen with the known K(ATP) blocker PNU 37883A.", "entity1": "K(ATP)", "entity2": "PNU 37883A", "span1": [74, 80], "span2": [89, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3064": {"label": 5, "data": {"text": "[Pharmacological effects of a mu-opioid receptor antagonist naltrexone on alcohol dependence].", "entity1": "mu-opioid receptor", "entity2": "naltrexone", "span1": [30, 48], "span2": [60, 70]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7682": {"label": 3, "data": {"text": "Thiazide and high ceiling diuretics were recently shown to inhibit all mammalian isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with a very different profile as compared to classical inhibitors, such as acetazolamide, methazolamide, and ethoxzolamide.", "entity1": "carbonic anhydrase", "entity2": "ethoxzolamide", "span1": [93, 111], "span2": [238, 251]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13161": {"label": 1, "data": {"text": "5-HT3 receptor antagonism with alosetron reduced responses to 5-HT in controls but not during inflammation.", "entity1": "5-HT3 receptor", "entity2": "5-HT", "span1": [0, 14], "span2": [62, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"10472": {"label": 5, "data": {"text": "Pretreatment with a combination of (+/-)-2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2 -yl]phenoxy]propyl]amino]ethoxy]-benzamide methanesulfonate (CGP20712A, a selective beta(1)-adrenoceptor antagonist) and (+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-buta nol hydrochloride (ICI-118,5511, a selective beta(2)-adrenoceptor antagonist) (0.1 microM for each) produced a 14-fold rightward shift of the concentration-response curve for (-)-isoprenaline; however, the relaxation in response to (+/-)-CGP12177A was unaffected by the blockade of beta(1)- and beta(2)-adrenoceptors.", "entity1": "beta(2)-adrenoceptor", "entity2": "(+/-)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-buta nol hydrochloride", "span1": [365, 385], "span2": [238, 337]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4049": {"label": 3, "data": {"text": "The molecular mechanism studies suggested that neoechinulin A may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regulating kinase 1 (ASK-1) and nuclear translocation of nuclear factor-\u03baB (NF-\u03baB) p65 and p50 subunits.", "entity1": "mitogen-activated protein kinase", "entity2": "neoechinulin A", "span1": [95, 127], "span2": [47, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5471": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "levonorgestrel", "span1": [106, 127], "span2": [168, 182]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4233": {"label": 2, "data": {"text": "Quantitative real-time polymerase chain reaction analysis showed that following the exposure of cells to SiO(2) NPs, the messenger RNA level of apoptotic genes (caspase-3 and caspase-9) were upregulated in a dose-dependent manner.", "entity1": "caspase-9", "entity2": "SiO(2)", "span1": [175, 184], "span2": [105, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6494": {"label": 5, "data": {"text": "Schild analyses for the antagonists against brimonidine yielded regression lines with slopes of unity and functional antagonist potencies (pK(B)) for BRL44408 (7.8), ARC 239 (5.8) and for prazosin (6.0) suggesting the presence of functional alpha(2A)-adrenoceptors.", "entity1": "alpha(2A)-adrenoceptors", "entity2": "prazosin", "span1": [241, 264], "span2": [188, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9811": {"label": 1, "data": {"text": "METHODS AND RESULTS: The effect of intravenous ajmaline (1 mg/kg), procainamide (10 mg/kg), or flecainide (2 mg/kg) on the ECG was studied in 34 patients with the syndrome and transient normalization of the ECG (group A), 11 members of 3 families in whom a SCN5A mutation was associated with the syndrome and 8 members in whom it was not (group B), and 53 control subjects (group C).", "entity1": "SCN5A", "entity2": "flecainide", "span1": [257, 262], "span2": [95, 105]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"1178": {"label": 3, "data": {"text": "Nateglinide inhibits Kir6.2/SUR1 and Kir6.2/SUR2B channels at 100 nM, and inhibits Kir6.2/SUR2A channels at high concentrations (1 microM).", "entity1": "SUR1", "entity2": "Nateglinide", "span1": [28, 32], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13482": {"label": 1, "data": {"text": "Autoradiography studies with [(3)H](-)-CP 55,940 show that chronic treatment with SR 141716A for 15 days twice daily (1 mg/kg i.p.) significantly increases the density of CB1 receptors in the PVN.", "entity1": "CB1 receptors", "entity2": "[(3)H](-)-CP 55,940", "span1": [171, 184], "span2": [29, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14059": {"label": 3, "data": {"text": "RESULTS: Aspirin reduced mTOR signaling in CRC cells by inhibiting the mTOR effectors S6K1 and 4E-BP1.", "entity1": "S6K1", "entity2": "Aspirin", "span1": [86, 90], "span2": [9, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3094": {"label": 1, "data": {"text": "N-(Diphenylmethyl)-2-phenyl-4-quinazolinamine (SoRI-9804), N-(2,2-diphenylethyl)-2-phenyl-4-quinazolinamine (SoRI-20040), and N-(3,3-diphenylpropyl)-2-phenyl-4-quinazolinamine (SoRI-20041) partially inhibited [(125)I]3beta-(4'-iodophenyl)tropan-2beta-carboxylic acid methyl ester (RTI-55) binding, slowed the dissociation rate of [(125)I]RTI-55 from the DAT, and partially inhibited [(3)H]dopamine uptake.", "entity1": "DAT", "entity2": "SoRI-20040", "span1": [354, 357], "span2": [109, 119]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11949": {"label": 9, "data": {"text": "The activities of UGTs 1A3, 1A8, 1A9, 2B4 and 2B7 were low, whereas UGT1A1 and UGT2B17 exhibited no HFC glucuronidation activity.", "entity1": "UGT2B17", "entity2": "HFC", "span1": [79, 86], "span2": [100, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14562": {"label": 2, "data": {"text": "Liver X Receptor (LXR) \u03b1 and LXR \u03b2 are nuclear receptors activated by oxysterols, oxidized derivatives of cholesterol.", "entity1": "Liver X Receptor (LXR) \u03b1", "entity2": "oxysterols", "span1": [0, 24], "span2": [70, 80]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14678": {"label": 3, "data": {"text": "In vitro, GSK1292263 demonstrated little/weak inhibition (IC50 values >30 \u03bcM) towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), Pgp, OATP1B3, or OCT2.", "entity1": "CYPs", "entity2": "GSK1292263", "span1": [86, 90], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6797": {"label": 3, "data": {"text": "Univariate regression analyses showed that only the use of carvedilol was correlated with the decrease in plasma BNP concentration (p <0.03).", "entity1": "plasma BNP", "entity2": "carvedilol", "span1": [106, 116], "span2": [59, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2413": {"label": 3, "data": {"text": "In unstimulated cells, Nor-NOHA dose-dependently reduced the arginase activity with maximal inhibition at 20 microM.", "entity1": "arginase", "entity2": "Nor-NOHA", "span1": [61, 69], "span2": [23, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12048": {"label": 9, "data": {"text": "Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment.", "entity1": "rTRPV3", "entity2": "apomorphine", "span1": [35, 41], "span2": [162, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12140": {"label": 8, "data": {"text": "DHFS is present exclusively in the mitochondria, making this compartment the sole site of synthesis of dihydrofolate in the plant cell.", "entity1": "DHFS", "entity2": "dihydrofolate", "span1": [0, 4], "span2": [103, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4021": {"label": 3, "data": {"text": "Curcumin improves TNBS-induced colitis in rats by inhibiting IL-27 expression via the TLR4/NF-\u03baB signaling pathway.", "entity1": "NF-\u03baB", "entity2": "Curcumin", "span1": [91, 96], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7123": {"label": 0, "data": {"text": "To probe potential PDE5 R domain effects on catalytic site affinity for certain inhibitors, four N-terminal truncation mutants were generated: PDE5Delta1-321 contained GAF-B domain, C domain, and the sequence between GAF-A and -B; PDE5Delta1-419 contained GAF-B and C domain; PDE5Delta1-465 contained the C domain and the C-terminal portion of GAF-B; and PDE5Delta1-534 contained only C domain.", "entity1": "GAF-B", "entity2": "C", "span1": [344, 349], "span2": [322, 323]}, "weak_labels": [-1, -1, 0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"539": {"label": 3, "data": {"text": "Two mechanisms of action have been identified for A77 1726: inhibition of dihydroorotate dehydrogenase (DHODH) and inhibition of tyrosine kinases.", "entity1": "dihydroorotate dehydrogenase", "entity2": "A77 1726", "span1": [74, 102], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1492": {"label": 3, "data": {"text": "EGF-stimulated phosphorylation of ERK and Bad is blocked by pretreatment with U0126, a selective MAP kinase kinase (MKK)1/2 inhibitor.", "entity1": "EGF", "entity2": "U0126", "span1": [0, 3], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1081": {"label": 3, "data": {"text": "Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent.", "entity1": "acetylcholinesterase", "entity2": "pyridostigmine", "span1": [242, 262], "span2": [119, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8743": {"label": 8, "data": {"text": "Using recombinant UGT2B10, we found that it catalyzes the N-glucuronidation of amitriptyline, imipramine, ketotifen, pizotifen, olanzapine, diphenhydramine, tamoxifen, ketoconazole and midazolam.", "entity1": "UGT2B10", "entity2": "pizotifen", "span1": [18, 25], "span2": [117, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"2781": {"label": 8, "data": {"text": "In conclusion, immortalized SHR and WKY PTE cells take up l-alanine mainly through a high-affinity Na(+)-dependent amino acid transporter, with functional features of ASCT2 transport.", "entity1": "Na(+)-dependent amino acid transporter", "entity2": "l-alanine", "span1": [99, 137], "span2": [58, 67]}, "weak_labels": [0, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11364": {"label": 1, "data": {"text": "The relatively high D(2) receptor occupancy, even at trough plasma levels, suggests that ziprasidone is more similar to risperidone and olanzapine in receptor occupancy profile than to clozapine and quetiapine.", "entity1": "D(2) receptor", "entity2": "ziprasidone", "span1": [20, 33], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5641": {"label": 3, "data": {"text": "Compound C diminished AMPK phosphorylation and enzymatic activity, resulting in reduced phosphorylation of its target acetyl CoA carboxylase.", "entity1": "AMPK", "entity2": "Compound C", "span1": [22, 26], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3287": {"label": 1, "data": {"text": "Prednisolone fast feedback was only reduced by glucocorticoid receptor antagonist pretreatment and not by mineralocorticoid receptor antagonism, suggesting a glucocorticoid receptor-mediated pathway.", "entity1": "glucocorticoid receptor", "entity2": "Prednisolone", "span1": [158, 181], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7062": {"label": 1, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARalpha", "entity2": "tamibarotene", "span1": [38, 46], "span2": [12, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5116": {"label": 3, "data": {"text": "Taken together, our findings indicate that 5HHMF suppresses NO production through modulation of iNOS, consequently suppressing NF-\u03baB activity and induction of Nrf2-dependent HO-1 activity.", "entity1": "NF-\u03baB", "entity2": "NO", "span1": [127, 132], "span2": [60, 62]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, 8, -1, -1]},
	"491": {"label": 1, "data": {"text": "There is, however, much information on the direct (acute and chronic) effects of alcohol on the binding properties of opioid receptors, as well as modulation of opioid peptide synthesis and secretion (e.g.", "entity1": "opioid peptide", "entity2": "alcohol", "span1": [161, 175], "span2": [81, 88]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12341": {"label": 9, "data": {"text": "In contrast, flunisolide was only metabolized via CYP3A4, with no significant turnover by CYP3A5 or CYP3A7.", "entity1": "CYP3A7", "entity2": "flunisolide", "span1": [100, 106], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5407": {"label": 2, "data": {"text": "Type I deiodinase, liver fatty-acid binding protein and cytochrome P450 (CYP) 3A37 mRNA levels were significantly induced by TCPP, while TDCPP induced CYP3A37 and CYP2H1.", "entity1": "Type I deiodinase", "entity2": "TCPP", "span1": [0, 17], "span2": [125, 129]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7697": {"label": 4, "data": {"text": "Although the D1-like receptor, by itself, had no effect on VSMC proliferation, stimulation with fenoldopam, a D1-like receptor agonist, inhibited the stimulatory effect of insulin.", "entity1": "D1-like receptor", "entity2": "fenoldopam", "span1": [110, 126], "span2": [96, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11091": {"label": 1, "data": {"text": "Overall, these findings suggest that monohydroxytamoxifen and LY117018 probably act through the same mechanism of action via the estrogen receptor.", "entity1": "estrogen receptor", "entity2": "monohydroxytamoxifen", "span1": [129, 146], "span2": [37, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8894": {"label": 4, "data": {"text": "These effects were not mimicked by oral administration of the beta 2-adrenoceptor agonist salbutamol even at high dose (52 mg/kg diet), and the effects of clenbuterol were not inhibited by addition of DL-propranolol (200 mg/kg diet).", "entity1": "beta 2-adrenoceptor", "entity2": "clenbuterol", "span1": [62, 81], "span2": [155, 166]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4079": {"label": 3, "data": {"text": "Overall, higher alcohol production was reduced by ammonium supplementation, and this can be correlated with a general downregulation of genes encoding decarboxylases and dehydrogenases of the Ehrlich pathway.", "entity1": "decarboxylases", "entity2": "ammonium", "span1": [151, 165], "span2": [50, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14697": {"label": 4, "data": {"text": "Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design.", "entity1": "GPR119", "entity2": "GSK1292263", "span1": [49, 55], "span2": [35, 45]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14528": {"label": 3, "data": {"text": "In contrast, EGCG markedly downregulated major bile acid transporters (Asbt and Ost\u03b1) and regulatory molecules (Shp and Fgf15) in the ileum.", "entity1": "Shp", "entity2": "EGCG", "span1": [112, 115], "span2": [13, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8097": {"label": 2, "data": {"text": "Moreover, wogonin repressed anisomycin-induced phosphorylation of p38, cav-1 and vascular permeability.", "entity1": "cav-1", "entity2": "anisomycin", "span1": [71, 76], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13232": {"label": 1, "data": {"text": "Glutamate stimulates glutamate receptor interacting protein 1 degradation by ubiquitin-proteasome system to regulate surface expression of GluR2.", "entity1": "proteasome", "entity2": "Glutamate", "span1": [87, 97], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15043": {"label": 8, "data": {"text": "Its head-space aroma displayed new volatile phytomolecules and also had higher levels of green volatiles from the lipoxygenase (LOX)-pathway (one having as precursors the polyunsaturated fatty acids containing a cis-cis-1,4-pentadiene system).", "entity1": "lipoxygenase", "entity2": "polyunsaturated fatty acids", "span1": [114, 126], "span2": [171, 198]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"807": {"label": 2, "data": {"text": "Analysis of splice variants and site-directed mutants of the AMPA receptor GluR3 expressed in Xenopus oocytes has shown that lithium produces a large potentiation of the GluR3 flop splice variant and suggested that lithium might inhibit rapid desensitization, which is characteristic of this receptor (Karkanias, N. and Papke, R., Subtype-specific effects of lithium on glutamate receptor function.", "entity1": "GluR3 flop", "entity2": "lithium", "span1": [170, 180], "span2": [215, 222]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1288": {"label": 8, "data": {"text": "BACKGROUND AND AIMS: Glutamic acid decarboxylase (GAD, EC 4.1.1.15) catalyses the conversion of glutamate to gamma-aminobutyric acid (GABA).", "entity1": "Glutamic acid decarboxylase", "entity2": "gamma-aminobutyric acid", "span1": [21, 48], "span2": [109, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 8, -1]},
	"4483": {"label": 0, "data": {"text": "The activation of the complement cascade, a cornerstone of the innate immune response, produces a number of small (74-77 amino acid) fragments, originally termed anaphylatoxins, that are potent chemoattractants and secretagogues that act on a wide variety of cell types.", "entity1": "anaphylatoxins", "entity2": "amino acid", "span1": [162, 176], "span2": [121, 131]}, "weak_labels": [0, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"1302": {"label": 3, "data": {"text": "OBJECTIVE: Celecoxib and rofecoxib are two relatively new nonsteroidal anti-inflammatory drugs (NSAIDs) that selectively inhibit the cyclo-oxygenase-2 (COX-2) isoenzyme at therapeutic concentrations.", "entity1": "COX-2", "entity2": "Celecoxib", "span1": [152, 157], "span2": [11, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12043": {"label": 3, "data": {"text": "Both the phosphotriesterase and physostigmine treatments protected the brain AChE activities measured 24 h after sarin exposure.", "entity1": "AChE", "entity2": "sarin", "span1": [77, 81], "span2": [113, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9248": {"label": 1, "data": {"text": "Ergovaline inhibition of radioligand binding to the D2 dopamine receptor and ergot alkaloid inhibition of vasoactive intestinal peptide (VIP)-stimulated cyclic AMP production in GH4ZR7 cells, stably transfected with a rat D2 dopamine receptor, were evaluated.", "entity1": "D2 dopamine receptor", "entity2": "Ergovaline", "span1": [52, 72], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10545": {"label": 1, "data": {"text": "Both GT boxes were needed for binding the complex, and mutation of either GT box caused the loss of transcriptional activation by RA.", "entity1": "GT boxes", "entity2": "RA", "span1": [5, 13], "span2": [130, 132]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12461": {"label": 1, "data": {"text": "In the African-American cohort, after excluding Y186C carriers, homozygous carriers of C29R showed 27% higher DPD activity as compared with noncarriers (609\u2009\u00b1\u2009152 and 480\u2009\u00b1\u2009152 pmol 5-FU min(-1) mg(-1), respectively; P = 0.013).Clinical Pharmacology & Therapeutics (2013); advance online publication 1 May 2013. doi:10.1038/clpt.2013.69.", "entity1": "C29R", "entity2": "5-FU", "span1": [87, 91], "span2": [182, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12436": {"label": 1, "data": {"text": "While SAR within the HTS series was very shallow and unable to be optimized, grafting the phenethyl ether linkage onto the ML129/ML172 cores led to the first sub-micromolar M5 PAM, ML326 (VU0467903), (human and rat M5 EC50s of 409nM and 500nM, respectively) with excellent mAChR selectivity (M1-M4 EC50s >30\u03bcM) and a robust 20-fold leftward shift of the ACh CRC.", "entity1": "mAChR", "entity2": "ML326", "span1": [273, 278], "span2": [181, 186]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14238": {"label": 2, "data": {"text": "Furthermore, salubrinal, a specific eIF2\u03b1 phosphorylation-inducing agent, increased CHOP and DR5 expression in the presence of VA.", "entity1": "CHOP", "entity2": "salubrinal", "span1": [84, 88], "span2": [13, 23]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8405": {"label": 1, "data": {"text": "Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD.", "entity1": "kinase domain", "entity2": "ponatinib", "span1": [66, 79], "span2": [12, 21]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12275": {"label": 1, "data": {"text": "Oxytocin (OT) and vasopressin (AVP) mediate their biological actions by acting on four known receptors: The OT (uterine) and the AVP V(1a) (vasopressor), V(1b) (pituitary), V(2) (renal) receptors and a fifth putative AVP V(1c)?", "entity1": "V(2)", "entity2": "AVP", "span1": [173, 177], "span2": [31, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"810": {"label": 1, "data": {"text": "PGE1 and PGE2 also inhibited the remaining ICa in a saturating concentration of nifedipine, omega-conotoxin-GVIA and omega-conotoxin-MVIIC, suggesting that R-type Ca2+ channels are involved.", "entity1": "R-type Ca2+ channels", "entity2": "PGE1", "span1": [156, 176], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4511": {"label": 3, "data": {"text": "Reversible inhibition of human carboxylesterases by acyl glucuronides.", "entity1": "human carboxylesterases", "entity2": "acyl glucuronides", "span1": [25, 48], "span2": [52, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4251": {"label": 2, "data": {"text": "Furthermore, butein treatment caused nuclear accumulation of nuclear factor-E2-related factor 2 (Nrf2) and increased the promoter activity of antioxidant response elements (AREs).", "entity1": "AREs", "entity2": "butein", "span1": [173, 177], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"775": {"label": 3, "data": {"text": "Compared with WT, DeltaKPQ I(Na) was more sensitive to flecainide, and flecainide preferentially inhibited late I(Na) (mean current between 20 and 23.5 ms after depolarization) compared with peak I(Na).", "entity1": "DeltaKPQ", "entity2": "flecainide", "span1": [18, 26], "span2": [71, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2107": {"label": 5, "data": {"text": "In contrast, the selective beta2AR antagonists ICI-118,551 and butoxamine inhibited isoproterenol-mediated enhancement with apparent low affinities (K(b) of 222 +/- 61 and 9268 +/- 512 nM, respectively).", "entity1": "beta2AR", "entity2": "ICI-118,551", "span1": [27, 34], "span2": [47, 58]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15484": {"label": 3, "data": {"text": "We developed a computational model of the hypothalamic-pituitary-gonadal (HPG) axis in female fathead minnows to predict dose-response and time-course (DRTC) behaviors for endocrine effects of the aromatase inhibitor, fadrozole (FAD).", "entity1": "aromatase", "entity2": "FAD", "span1": [197, 206], "span2": [229, 232]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5160": {"label": 8, "data": {"text": "These results indicate a major role of CYP2B6 in ketamine N-demethylation in vitro and a significant impact of the CYP2B6*6 allele on enzyme-ketamine binding and catalytic activity.", "entity1": "CYP2B6", "entity2": "ketamine", "span1": [39, 45], "span2": [49, 57]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8537": {"label": 3, "data": {"text": "Intestinal and hepatic first-pass extraction of the 11\u03b2-HSD1 inhibitor AMG 221 in rats with chronic vascular catheters.", "entity1": "11\u03b2-HSD1", "entity2": "AMG 221", "span1": [52, 60], "span2": [71, 78]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13263": {"label": 5, "data": {"text": "METHODS: The effect of leukotriene D(4) and the leukotriene receptor antagonist, pranlukast hydrate (ONO-1078) on the regulation of MUC2/5AC gene expression and mucin secretion were observed in human airway NCI-H292 epithelial cells.", "entity1": "leukotriene receptor", "entity2": "pranlukast hydrate", "span1": [48, 68], "span2": [81, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3751": {"label": 3, "data": {"text": "The pretreatment with 20\u00a0mg\u2009L(-1) La(III) could alleviate the effects of UV-B radiation on the activities of nitrate reductase, glutamine synthetase, glutamate synthase, and glutamate dehydrogenase, promoting amino acid conversion and protein synthesis in soybean seedlings.", "entity1": "nitrate reductase", "entity2": "La(III)", "span1": [109, 126], "span2": [34, 41]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"4838": {"label": 9, "data": {"text": "Cucurbitacin I also failed to affect the activation of P-Rex1 by heregulin.", "entity1": "P-Rex1", "entity2": "Cucurbitacin I", "span1": [55, 61], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5639": {"label": 2, "data": {"text": "AMPK activators metformin and AICAR partly prevented the cell cycle block, oxidative stress and apoptosis induced by compound C. The small interfering RNA (siRNA) targeting of human AMPK mimicked compound C-induced G(2)/M cell cycle arrest, but failed to induce oxidative stress and apoptosis in U251 glioma cells.", "entity1": "AMPK", "entity2": "AICAR", "span1": [0, 4], "span2": [30, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"478": {"label": 5, "data": {"text": "The potency of the antipsychotic drug, risperidone, to antagonize alpha 1A-adrenoceptor-mediated contraction in rat vas deferens and vasoconstriction in rat perfused kidney, and alpha 1B-adrenoceptor-mediated contractions in spleen from guinea-pig and mouse was evaluated and compared to that of alpha 1-adrenoceptor subtype-discriminating antagonists.", "entity1": "alpha 1A-adrenoceptor", "entity2": "risperidone", "span1": [66, 87], "span2": [39, 50]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3274": {"label": 3, "data": {"text": "Using a unique biosensor-based assay, trifluoperazine (TFP) was identified as an inhibitor that disrupts the S100A4/myosin-IIA interaction.", "entity1": "S100A4", "entity2": "trifluoperazine", "span1": [109, 115], "span2": [38, 53]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13959": {"label": 3, "data": {"text": "Its S-isomer, TVP1022 is thousand times less potent as an MAO-B inhibitor.", "entity1": "MAO-B", "entity2": "TVP1022", "span1": [58, 63], "span2": [14, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10793": {"label": 2, "data": {"text": "Moreover, simvastatin concentration-dependently inhibited the expression of ICAM-1 and induced the expression of CD40 on monocytes.", "entity1": "CD40", "entity2": "simvastatin", "span1": [113, 117], "span2": [10, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2118": {"label": 3, "data": {"text": "Furthermore, experiments showed that treatment with DEC results in a reduction in the amount of COX-1 protein in peritoneal exudate cells.", "entity1": "COX-1", "entity2": "DEC", "span1": [96, 101], "span2": [52, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"387": {"label": 0, "data": {"text": "The replacement of the conserved cysteine residues in e2 of CB2 by serine also eliminated CP 55,940 binding, but replacement of those in CB1 resulted in the sequestration of the mutated receptors in the cell cytoplasm.", "entity1": "CB2", "entity2": "cysteine", "span1": [60, 63], "span2": [33, 41]}, "weak_labels": [-1, 0, 0, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3706": {"label": 2, "data": {"text": "The present results indicated that N-BPs induce apoptosis by decreasing the mitochondrial transmembrane potential, increasing the activation of caspase-9 and caspase-3, and enhancing Bim expression through inhibition of the Ras/MEK/ERK and Ras/mTOR pathways.", "entity1": "caspase-9", "entity2": "N", "span1": [144, 153], "span2": [35, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5478": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "3-keto-desogestrel", "span1": [106, 127], "span2": [462, 480]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14016": {"label": 3, "data": {"text": "Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.", "entity1": "VEGFR2", "entity2": "XL184", "span1": [38, 44], "span2": [14, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14795": {"label": 2, "data": {"text": "Trichostatin A inhibits transforming growth factor-\u03b2-induced reactive oxygen species accumulation and myofibroblast differentiation via enhanced NF-E2-related factor 2-antioxidant response element signaling.", "entity1": "NF-E2-related factor 2", "entity2": "Trichostatin A", "span1": [145, 167], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12328": {"label": 0, "data": {"text": "Using site-directed mutagenesis, we identified three serines (Ser833, Ser836, and Ser840) within the membrane proximal region of the GluK5 C-terminal domain that, in combination, are required for mGlu1-mediated potentiation of KARs.", "entity1": "GluK5", "entity2": "Ser", "span1": [133, 138], "span2": [82, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6199": {"label": 5, "data": {"text": "administration of the non-selective muscarinic receptor antagonist atropine (ID50 = 1.45 microg), the muscarinic M1 receptor antagonist pirenzepine (ID50 = 4.33 microg), the muscarinic M2 receptor antagonist methoctramine (ID50 = 1.39 microg) and the muscarinic M3 receptor antagonist para-fluoro-hexahydro-sila-difenidol (ID50 = 31.19 microg).", "entity1": "muscarinic M1 receptor", "entity2": "pirenzepine", "span1": [102, 124], "span2": [136, 147]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1068": {"label": 3, "data": {"text": "Triacsin C, a competitive inhibitor of both ACS1 and ACS4, inhibited ACS activity similarly in endoplasmic reticulum, MAM, and mitochondria, suggesting that a hitherto unidentified triacsin-sensitive ACS is present in mitochondria.", "entity1": "ACS1", "entity2": "Triacsin C", "span1": [44, 48], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5451": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "PSA", "entity2": "juglone", "span1": [213, 216], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12549": {"label": 1, "data": {"text": "Extracellular Cbl (protein bound and free) and intracellular Cbl (protein bound and free) were determined after culturing L-1210 cells in the presence of [57Co]cyanocobalamin (CN-Cbl) bound to transcobalamin II (transcobalamin, TC).", "entity1": "transcobalamin", "entity2": "CN-Cbl", "span1": [212, 226], "span2": [176, 182]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12209": {"label": 1, "data": {"text": "P2Y12 has been shown to be the target of the thienopyridine drugs, ticlopidine and clopidogrel.", "entity1": "P2Y12", "entity2": "thienopyridine", "span1": [0, 5], "span2": [45, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1628": {"label": 9, "data": {"text": "However, chronic ethanol, as well as ethanol withdrawal failed to produce any significant alteration in the level of CREB protein in the nucleus accumbens.", "entity1": "CREB", "entity2": "ethanol", "span1": [117, 121], "span2": [37, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3370": {"label": 3, "data": {"text": "Ca(v)1.3 channels were less sensitive to pentobarbital inhibition than Ca(v)1.2 channels, similar to dihydropyridine (DHP) L-VGCC antagonists.", "entity1": "Ca(v)1.3", "entity2": "dihydropyridine", "span1": [0, 8], "span2": [101, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2718": {"label": 2, "data": {"text": "Indomethacin treatment led to an increase in lipid peroxidation, glutathione peroxidase and glucose-6-phosphate dehydrogenase activities and to a decrease in catalase activity and glutathione levels in gastric mucosa.", "entity1": "glutathione peroxidase", "entity2": "Indomethacin", "span1": [65, 87], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2687": {"label": 3, "data": {"text": "Gene expression profiling (GEP) of GIST-S, GIST-R cells and two IM resistant GIST patients demonstrated that KIT is downregulated implying a major role in IM resistance.", "entity1": "KIT", "entity2": "IM", "span1": [109, 112], "span2": [64, 66]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9178": {"label": 8, "data": {"text": "Positive staining of mitochondria was achieved in the presence of the MAO substrate, tryptamine.", "entity1": "MAO", "entity2": "tryptamine", "span1": [70, 73], "span2": [85, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"10712": {"label": 2, "data": {"text": "Dimemorfan pre-treatment also attenuated the KA-induced increases in c-fos/c-jun expression, activator protein (AP)-1 DNA-binding activity, and loss of cells in the CA1 and CA3 fields of the hippocampus.", "entity1": "activator protein (AP)-1", "entity2": "KA", "span1": [93, 117], "span2": [45, 47]}, "weak_labels": [-1, -1, -1, 1, -1, -1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11135": {"label": 3, "data": {"text": "TREK-1 currents are insensitive to pharmacological agents that block TWIK-1 activity such as quinine and quinidine.", "entity1": "TWIK-1", "entity2": "quinidine", "span1": [69, 75], "span2": [105, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14314": {"label": 1, "data": {"text": "However, downregulation of the antioxidant response element (ARE)-driven Nrf2 target genes such as NQO1, HO-1 and glutathione S-transferase (GST) did not reverse the inhibitory effect of DMF on TGF-beta-induced upregulation of profibrotic genes or extracellular matrix proteins, suggesting an ARE-independent anti-fibrotic activity of DMF.", "entity1": "GST", "entity2": "DMF", "span1": [141, 144], "span2": [187, 190]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3852": {"label": 0, "data": {"text": "Glutaraldehyde crosslinked albumin nanoparticles with a size of approximately 100nm were loaded with the multikinase inhibitor 17864-L(x)-a platinum-bound sunitinib analogue-which couples the drug to methionine residues of albumin and is released in a reductive environment.", "entity1": "albumin", "entity2": "methionine", "span1": [223, 230], "span2": [200, 210]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9405": {"label": 1, "data": {"text": "Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).", "entity1": "retinoic acid receptors", "entity2": "adapalene", "span1": [164, 187], "span2": [101, 110]}, "weak_labels": [-1, -1, -1, 1, -1, 1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12310": {"label": 8, "data": {"text": "Recent studies, however, have demonstrated a promising potential treatment option with the help of the serum enzyme butyrylcholinesterase (BChE), which is capable of breaking down naturally occurring (-)-cocaine before the drug can influence the reward centers of the brain or affect other areas of the body.", "entity1": "BChE", "entity2": "(-)-cocaine", "span1": [139, 143], "span2": [200, 211]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11862": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "CYP1A1", "entity2": "cyanidin", "span1": [150, 156], "span2": [43, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4226": {"label": 3, "data": {"text": "The results showed that (1) 15mg/kg body weight PhIP induced obvious histopathological changes in gastric mucosa; (2) PhIP (10 and/or 15mg/kg) significantly decreased superoxide dismutase (SOD) and glutathioneperoxidase (GPx) activities, while increased catalase (CAT) activity compared with the control.", "entity1": "glutathioneperoxidase", "entity2": "PhIP", "span1": [198, 219], "span2": [118, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4738": {"label": 3, "data": {"text": "Additionally, the expression of hepatic fibrosis-related factors such as \u03b1-smooth muscle actin and transforming growth factor-\u03b21 (TGF-\u03b21), were reduced in rats treated with sinapic acid.", "entity1": "TGF-\u03b21", "entity2": "sinapic acid", "span1": [130, 136], "span2": [173, 185]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4106": {"label": 2, "data": {"text": "Thus, SFO contributes to the instability of atherosclerotic plaque in apoE(-/-) mice through activating p75(NTR) and IL-8 and cell apoptosis in plaque.", "entity1": "p75(NTR)", "entity2": "SFO", "span1": [104, 112], "span2": [6, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4354": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "MMP7", "entity2": "pinosylvin", "span1": [282, 286], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6668": {"label": 3, "data": {"text": "In PC3 cells, hydroxyurea inhibited hRRM2 and resulted in increased sensitivity to UV irradiation.", "entity1": "hRRM2", "entity2": "hydroxyurea", "span1": [36, 41], "span2": [14, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7338": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT2", "entity2": "glutamine", "span1": [331, 336], "span2": [76, 85]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"15816": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFRbeta", "entity2": "Tyr", "span1": [89, 98], "span2": [157, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3851": {"label": 0, "data": {"text": "Glutaraldehyde crosslinked albumin nanoparticles with a size of approximately 100nm were loaded with the multikinase inhibitor 17864-L(x)-a platinum-bound sunitinib analogue-which couples the drug to methionine residues of albumin and is released in a reductive environment.", "entity1": "albumin", "entity2": "Glutaraldehyde", "span1": [27, 34], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1225": {"label": 1, "data": {"text": "Raloxifene is a selective ER modulator with less uterine estrogen agonist activity than tamoxifen, and it is hoped that it will result in fewer uterine cancers but will be equally efficacious in reducing the risk of breast cancer.", "entity1": "ER", "entity2": "Raloxifene", "span1": [26, 28], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 4, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14812": {"label": 4, "data": {"text": "Results indicate that AM4054 serves as an effective CB(1) discriminative stimulus, with an onset and time course of action comparable with that of the CB(1) agonist \u0394(9)-tetrahydrocannabinol, and that the inverse agonist rimonabant and the neutral antagonist AM4113 produce dose-related rightward shifts in the AM4054 dose-effect curve, indicating that both drugs surmountably antagonize the discriminative stimulus effects of AM4054.", "entity1": "CB(1)", "entity2": "AM4054", "span1": [151, 156], "span2": [427, 433]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"854": {"label": 0, "data": {"text": "The functional protein contains 1160 amino acids with a large central mucin domain, three consensus sites for glycosaminoglycan attachment, two epidermal growth factor-like repeats, a putative hyaluronan-binding motif, and a potential transmembrane domain near the C-terminal.", "entity1": "mucin domain", "entity2": "C", "span1": [70, 82], "span2": [265, 266]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6180": {"label": 3, "data": {"text": "Based on these results, we conclude that the NSAIDs ibuprofen and salicylic acid inhibit cAMP-mediated Cl- secretion in human colonic and airway epithelia via a direct inhibition of CFTR Cl- channels as well as basolateral membrane K+ channels.", "entity1": "K+ channels", "entity2": "ibuprofen", "span1": [232, 243], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11699": {"label": 3, "data": {"text": "The obtained results showed that pioglitazone improved the renal function, structural changes, renal malondialdehyde (MDA), tumor necrosis factor alpha (TNF-\u03b1), nuclear factor kappa B (NF-\u03baB) genes expression in cisplatin injected rats.", "entity1": "NF-\u03baB", "entity2": "cisplatin", "span1": [185, 190], "span2": [212, 221]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15654": {"label": 3, "data": {"text": "Cholesterol also increases Amyloid \u03b2 (A\u03b2) deposition and tau pathology.", "entity1": "Amyloid \u03b2", "entity2": "Cholesterol", "span1": [27, 36], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1970": {"label": 9, "data": {"text": "In contrast, NTG or ISDN does not affect HIF-1 activity.", "entity1": "HIF-1", "entity2": "ISDN", "span1": [41, 46], "span2": [20, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15701": {"label": 1, "data": {"text": "In an investigation into the participation of TRP channels and ASICs in CAT's antinociceptive mechanism, we used capsaicin (2.2\u03bcg/paw), cinnamaldehyde (10mmol/paw), menthol (1.2mmol/paw) and acidified saline (2% acetic acid, pH 1.98).", "entity1": "TRP channels", "entity2": "cinnamaldehyde", "span1": [46, 58], "span2": [136, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14119": {"label": 3, "data": {"text": "Lenalidomide and pomalidomide inhibited autoubiquitination of CRBN in HEK293T cells expressing thalidomide-binding competent wild-type CRBN, but not thalidomide-binding defective CRBN(YW/AA).", "entity1": "CRBN", "entity2": "pomalidomide", "span1": [62, 66], "span2": [17, 29]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11835": {"label": 2, "data": {"text": "Dietary EPA/DHA treatment restored endogenous biosynthesis of n-3 derived lipid mediators in obesity while attenuating adipose tissue inflammation and improving insulin sensitivity.", "entity1": "insulin", "entity2": "DHA", "span1": [161, 168], "span2": [12, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11872": {"label": 1, "data": {"text": "We examined the effects of anthocyanidins (cyanidin, delphinidin, malvidin, peonidin, petunidin, pelargonidin) on the aryl hydrocarbon receptor (AhR)-CYP1A1 signaling pathway in human hepatocytes, hepatic HepG2 and intestinal LS174T cancer cells.", "entity1": "aryl hydrocarbon receptor", "entity2": "petunidin", "span1": [118, 143], "span2": [86, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13822": {"label": 3, "data": {"text": "Currently, the use of orally administered MAO inhibitor antidepressants (eg, phenelzine, tranylcypromine) is limited by the risk of tyramine-provoked events (eg, acute hypertension and headache, also known as the \"cheese reaction\") when combined with dietary tyramine.", "entity1": "MAO", "entity2": "tranylcypromine", "span1": [42, 45], "span2": [89, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13253": {"label": 2, "data": {"text": "RESULTS: Leukotriene D(4) upregulated MUC2/5AC gene expression and mucin secretion in a dose dependent pattern.", "entity1": "MUC2/5AC", "entity2": "Leukotriene D(4)", "span1": [38, 46], "span2": [9, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1733": {"label": 1, "data": {"text": "Agonist competition assays with [3H]DHA showed the following rank order of potency: isoproterenol>epinephrine> norepinephrine, consistent with beta2AR interaction.", "entity1": "beta2AR", "entity2": "norepinephrine", "span1": [143, 150], "span2": [111, 125]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3384": {"label": 6, "data": {"text": "BDZs and other positive GABA(A)R modulators, including barbiturates, ethanol, and neurosteroids, can also inhibit L-type voltage-gated calcium channels (L-VGCCs), which could contribute to reduced neuronal excitability.", "entity1": "GABA(A)R", "entity2": "barbiturates", "span1": [24, 32], "span2": [55, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10512": {"label": 1, "data": {"text": "GW572016 radiosensitized EGFR-overexpressing cell lines, but HER2-overexpressing cells were unable to form colonies after brief exposure to GW572016 even in the absence of radiation, and thus could not be evaluated for radiosensitization.", "entity1": "HER2", "entity2": "GW572016", "span1": [61, 65], "span2": [140, 148]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15510": {"label": 0, "data": {"text": "In particular, nitrosylation promoted disulfide formation involving the pair of catalytic cysteines (Cys-52 and Cys-173) and disrupted the oligomeric structure of Prx1, leading to loss of peroxidase activity.", "entity1": "peroxidase", "entity2": "Cys", "span1": [188, 198], "span2": [101, 104]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12443": {"label": 6, "data": {"text": "An HTS campaign identified several weak M5 PAMs (M5 EC50 >10\u03bcM) with a structurally related isatin core that possessed a southern phenethyl ether linkage.", "entity1": "M5", "entity2": "phenethyl ether", "span1": [49, 51], "span2": [130, 145]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4011": {"label": 3, "data": {"text": "Compared with the untreated colitis group, the curcumin-treated group showed significant decreases in the disease activity index, colonic mucosa damage index, histological score, myeloperoxidase activity, and expressions of NF-\u03baB mRNA, IL-27 mRNA, TLR4 protein, NF-\u03baB p65 protein, and IL-27 p28 protein (p < 0.05).", "entity1": "NF-\u03baB", "entity2": "curcumin", "span1": [262, 267], "span2": [47, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1996": {"label": 0, "data": {"text": "Furthermore, a combinatory mutation (Pro(7.31)-Pro(7.32)-Ser(7.33) motif to Ser-Glu-Pro in EL3 and Leu(7.38), Leu(7.43), Ala(7.46), and Pro(7.47) to those of rat GnRHR) in gmGnRH-2 exhibited an approximately 500-fold increased sensitivity to GnRH-I, indicating that these residues are critical for discriminating GnRH-II from GnRH-I.", "entity1": "EL3", "entity2": "Ser", "span1": [91, 94], "span2": [57, 60]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6014": {"label": 8, "data": {"text": "The daily administration of low-dose aspirin (40 mg), a selective inhibitor of platelet PGHS-1, caused a cumulative inhibition of urinary 11-dehydro-TXB2 and whole blood TXB2 production that recovered with a timecourse consistent with platelet turnover.", "entity1": "PGHS-1", "entity2": "11-dehydro-TXB2", "span1": [88, 94], "span2": [138, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9656": {"label": 8, "data": {"text": "RESULTS: Administration of SC-236 to cirrhotic animals did not produce significant renal effects, whereas administration of the nonselective COX-1/COX-2 inhibitor, ketorolac, resulted in a marked reduction in urine volume, urinary excretion of prostaglandins, and glomerular filtration rate and in a significant impairment in renal water metabolism.", "entity1": "COX-1", "entity2": "prostaglandins", "span1": [141, 146], "span2": [244, 258]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"6576": {"label": 7, "data": {"text": "The 2.0A crystal structure of the MalP/Glc1P binary complex shows that the Glc1P substrate adopts a conformation seen previously with both inactive and active forms of mammalian GP, with the phosphate group not in close contact with the 5'-phosphate group of the essential pyridoxal phosphate (PLP) cofactor.", "entity1": "MalP", "entity2": "PLP", "span1": [34, 38], "span2": [294, 297]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, 8, -1, -1, -1, -1, 9]},
	"7315": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "neutral amino acid transporters", "entity2": "amino acids", "span1": [133, 164], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10072": {"label": 1, "data": {"text": "Aspirin and salicylate bind to immunoglobulin heavy chain binding protein (BiP) and inhibit its ATPase activity in human fibroblasts.", "entity1": "immunoglobulin heavy chain binding protein", "entity2": "Aspirin", "span1": [31, 73], "span2": [0, 7]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8398": {"label": 3, "data": {"text": "The tyrosine hydroxylase inhibitor \u03b1-methyltyrosine (300\u00b5M, 24h) completely abolished MeHg-induced DA release.", "entity1": "tyrosine hydroxylase", "entity2": "\u03b1-methyltyrosine", "span1": [4, 24], "span2": [35, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11637": {"label": 1, "data": {"text": "Insight into the structural basis for this improvement was gained with molecular modeling and NMR data obtained for microtubule-bound docetaxel.", "entity1": "microtubule", "entity2": "docetaxel", "span1": [116, 127], "span2": [134, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"842": {"label": 3, "data": {"text": "The higher affinity of felbamate block of NMDA receptors containing the NR2B subunit could be accounted for by more rapid association and slower dissociation from these sites.", "entity1": "NR2B", "entity2": "felbamate", "span1": [72, 76], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"99": {"label": 1, "data": {"text": "These results suggest that the beneficial effect of minaprine on cycloheximide-induced amnesia may be related not only to cholinergic but also serotonergic neuronal systems (5-HT2 receptors).", "entity1": "5-HT2 receptors", "entity2": "minaprine", "span1": [174, 189], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"6640": {"label": 5, "data": {"text": "alpha(1A)-Adrenoceptor selective antagonists, 2-([2,6-dimethoxyphenoxyethyl]aminomethyl)-1,4-benzodioxane (WB-4101; 0.1-1 mg/kg) and 5-methylurapidil (0.1-1 mg/kg), the alpha(1B)-adrenoceptor selective antagonist, 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765314; 0.3-1 mg/kg), as well as the alpha(1D)-adrenoceptor selective antagonist, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY-7378; 1 mg/kg), were used to delineate the adrenoceptor subtypes involved.", "entity1": "alpha(1B)-adrenoceptor", "entity2": "L-765314", "span1": [169, 191], "span2": [332, 340]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9123": {"label": 1, "data": {"text": "Characteristics of the binding of phenoxybenzamine to calmodulin.", "entity1": "calmodulin", "entity2": "phenoxybenzamine", "span1": [54, 64], "span2": [34, 50]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11906": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "PTP1B", "entity2": "triglycerides", "span1": [174, 179], "span2": [46, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12204": {"label": 3, "data": {"text": "A significant positive correlation was found between dietary intake of total SFAs and total MUFAs and expression of PBMC D6D and D5D genes, but a significant negative correlation between dietary intake of linoleic acid (LA) and alpha-linolenic acid (LNA) and the expression of PBMC D6D and D5D genes.", "entity1": "D6D", "entity2": "LNA", "span1": [282, 285], "span2": [250, 253]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12691": {"label": 1, "data": {"text": "Corticosteroids act, at least in part, by recruitment of histone deacetylases (HDACs) to the site of active inflammatory gene transcription.", "entity1": "HDACs", "entity2": "Corticosteroids", "span1": [79, 84], "span2": [0, 15]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6034": {"label": 9, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "8-OH-DPAT", "span1": [63, 69], "span2": [276, 285]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5060": {"label": 2, "data": {"text": "Activating glucocorticoid receptor-ERK signaling pathway contributes to ginsenoside Rg1 protection against \u03b2-amyloid peptide-induced human endothelial cells apoptosis.", "entity1": "ERK", "entity2": "ginsenoside Rg1", "span1": [35, 38], "span2": [72, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1418": {"label": 5, "data": {"text": "Only pMPPI [4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridynyl-benzamide hydrochloride], a selective 5-HT(1A) antagonist, was effective in inhibiting all 5-HT syndrome behaviors produced by lisuride, whereas pMPPI was without effect on any behavior induced by LSD.", "entity1": "5-HT(1A)", "entity2": "4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridynyl-benzamide hydrochloride", "span1": [116, 124], "span2": [12, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"6045": {"label": 4, "data": {"text": "In addition several ligands known to act as agonists at either 5-HT2A or 5-HT2C receptors including 1-m-chlorophenylpiperazine (m-CPP), Ru 24969, MK 212 and SCH 23390 were also agonists in rat fundus whilst sumatriptan, renzapride and 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) were very weak or inactive.", "entity1": "5-HT2A", "entity2": "1-m-chlorophenylpiperazine", "span1": [63, 69], "span2": [100, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12142": {"label": 1, "data": {"text": "Because rhoA requires GGPP for its function, this links the microarray and biochemical data and identifies rhoA as a potential mediator of the anticancer properties of lovastatin.", "entity1": "rhoA", "entity2": "lovastatin", "span1": [107, 111], "span2": [168, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3700": {"label": 1, "data": {"text": "In vivo genotoxicity of methyleugenol in gpt delta transgenic rats following medium-term exposure.", "entity1": "gpt", "entity2": "methyleugenol", "span1": [41, 44], "span2": [24, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7451": {"label": 1, "data": {"text": "Ovariectomy downregulates glutaredoxin and renders female mice vulnerable to L-BOAA toxicity as evidenced by activation of AP1, loss of GSH and complex I activity indicating the important role of glutaredoxin in neuroprotection.", "entity1": "glutaredoxin", "entity2": "L-BOAA", "span1": [196, 208], "span2": [77, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3808": {"label": 4, "data": {"text": "Discovery of novel cannabinoid receptor ligands by a virtual screening approach: further development of 2,4,6-trisubstituted 1,3,5-triazines as CB2 agonists.", "entity1": "CB2", "entity2": "2,4,6-trisubstituted 1,3,5-triazines", "span1": [144, 147], "span2": [104, 140]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8601": {"label": 2, "data": {"text": "LPO was increased while as GSH, CAT and GPx decreased by the administration of CCl4 and TAA (p<0.001); co-administration of NAC restored these liver markers to normal levels (p<0.001).", "entity1": "GPx", "entity2": "NAC", "span1": [40, 43], "span2": [124, 127]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10373": {"label": 3, "data": {"text": "This study shows that the potency of GW660511X in comparison with omapatrilat is more than 100-fold lower in human, but less than 10-fold lower in rat plasma, suggesting that rat may not be a suitable in vivo model for the evaluation of ACE/NEP inhibition in relation to effects in humans.", "entity1": "ACE", "entity2": "GW660511X", "span1": [237, 240], "span2": [37, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9069": {"label": 1, "data": {"text": "The present study reports the in vitro binding affinities of the same compounds for muscarinic cholinergic receptors and for histamine H1 receptors in rat brain, using 3H-quinuclidinyl benzilate and 3H-mepyramine as radioligands.", "entity1": "muscarinic cholinergic receptors", "entity2": "3H-mepyramine", "span1": [84, 116], "span2": [199, 212]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11786": {"label": 8, "data": {"text": "These results suggest that HSD11B1-derived cortisol mediates, in part, actions of ovarian progesterone and the conceptus on endometrial function and support the hypothesis that IFNT, PG, and cortisol coordinately regulate endometrial functions important for conceptus elongation and implantation during early pregnancy in sheep.", "entity1": "HSD11B1", "entity2": "cortisol", "span1": [27, 34], "span2": [43, 51]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10370": {"label": 3, "data": {"text": "Unlike GW660511X, omapatrilat abolished the production of BrBK1-5 and BrBK1-7, suggesting a better ACE inhibition effect over GW660511X as no NEP activity was found.", "entity1": "BrBK1-5", "entity2": "omapatrilat", "span1": [58, 65], "span2": [18, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9784": {"label": 4, "data": {"text": "Parenteral administration of selective agonists of the delta-opioid receptor (SB 227122), mu-opioid receptor (codeine and hydrocodone), and kappa-opioid receptor (BRL 52974) produced dose-related inhibition of citric acid-induced cough with ED(50) values of 7.3, 5.2, 5.1, and 5.3 mg/kg, respectively.", "entity1": "mu-opioid receptor", "entity2": "hydrocodone", "span1": [90, 108], "span2": [122, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7851": {"label": 1, "data": {"text": "Neuropeptide Y Y1 receptor knockdown can modify glutathione peroxidase and c-AMP response element-binding protein in phenylpropanolamine-treated rats.", "entity1": "c-AMP response element-binding protein", "entity2": "phenylpropanolamine", "span1": [75, 113], "span2": [117, 136]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12720": {"label": 3, "data": {"text": "However, while Akt phosphorylation was prevented by CHX, Erk1/2 phosphorylation was further enhanced by CHX.", "entity1": "Akt", "entity2": "CHX", "span1": [15, 18], "span2": [104, 107]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"674": {"label": 0, "data": {"text": "The deduced amino acid sequence contains 779 amino acids, including a putative cGMP binding sequence in the amino-terminal portion of the molecule and a catalytic domain that is 16-47% identical in amino acid sequence to those of other PDE families.", "entity1": "PDE", "entity2": "amino acid", "span1": [236, 239], "span2": [198, 208]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4194": {"label": 2, "data": {"text": "PTE also down-regulated the expression of STAT3 target genes, including the anti-apoptotic proteins Bcl-xL and Mcl-1, leading to the up-regulation of mitochondrial apoptosis pathway-related proteins (Bax, Bak, cytosolic Cytochrome c, and cleaved Caspase3) and cyclin-dependent kinase inhibitors such as p21 and p27.", "entity1": "p27", "entity2": "PTE", "span1": [311, 314], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14818": {"label": 5, "data": {"text": "In the present studies, the CB(1) inverse agonist SR141716A (rimonabant) and the CB(1) neutral antagonist AM4113 were compared for their ability to modify CB(1) receptor-mediated discriminative stimulus effects in nonhuman primates trained to discriminate the novel CB(1) full agonist AM4054.", "entity1": "CB(1)", "entity2": "AM4113", "span1": [81, 86], "span2": [106, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10155": {"label": 1, "data": {"text": "EM-800 and EM-652 are the most potent pure antiestrogens and EM-652 has the highest affinity of all antiestrogens to ER.", "entity1": "ER", "entity2": "EM-652", "span1": [117, 119], "span2": [61, 67]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2833": {"label": 0, "data": {"text": "The deduced amino acid sequence showed significant identity to plant and mammalian serine racemases and contained conserved pyridoxal 5-phosphate (PLP)-binding lysine and PLP-interacting amino acid residues.", "entity1": "serine racemases", "entity2": "amino acid", "span1": [83, 99], "span2": [187, 197]}, "weak_labels": [0, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3739": {"label": 3, "data": {"text": "Nitrogen-containing bisphosphonates (N-BPs) induce apoptosis in tumor cells by inhibiting the prenylation of small G-proteins.", "entity1": "G-proteins", "entity2": "BPs", "span1": [115, 125], "span2": [39, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15673": {"label": 2, "data": {"text": "Maqui berry (Aristotelia chilensis) and the constituent delphinidin glycoside inhibit photoreceptor cell death induced by visible light.", "entity1": "photoreceptor", "entity2": "delphinidin glycoside", "span1": [86, 99], "span2": [56, 77]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6884": {"label": 1, "data": {"text": "ABCG5 and ABCG8 themselves are regulated by cholesterol via liver X receptors (LXRs), which are also activated by oxysterols and some derivatives of plant sterols.", "entity1": "ABCG5", "entity2": "cholesterol", "span1": [0, 5], "span2": [44, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13763": {"label": 3, "data": {"text": "Finally, bosutinib is the first kinase inhibitor shown to target CAMK2G, recently implicated in myeloid leukemia cell proliferation.", "entity1": "kinase", "entity2": "bosutinib", "span1": [32, 38], "span2": [9, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11136": {"label": 1, "data": {"text": "Most typical neuroleptics have radioligand-independent values of 0.3 to 5 nM at dopamine D2 receptors, making them more resistant to displacement by endogenous dopamine.", "entity1": "dopamine D2 receptors", "entity2": "dopamine", "span1": [80, 101], "span2": [160, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"462": {"label": 1, "data": {"text": "Phenylephrine elicited a concentration-dependent positive inotropic effect via alpha 1-adrenoceptors in the presence of either (+/-)-bupranolol or S(-)-timolol.", "entity1": "alpha 1-adrenoceptors", "entity2": "S(-)-timolol", "span1": [79, 100], "span2": [147, 159]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4525": {"label": 8, "data": {"text": "Objective: This study explores the ability of acyl glucuronides to act as substrates or inhibitors of human carboxylesterases 1 (hCES1) and 2 (hCES2).", "entity1": "hCES1", "entity2": "acyl glucuronides", "span1": [129, 134], "span2": [46, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"1953": {"label": 1, "data": {"text": "The antiaggregating effect of clopidogrel is attributed to an irreversible inhibition of ADP binding to a purinergic receptor present at the platelet surface.", "entity1": "purinergic receptor", "entity2": "ADP", "span1": [106, 125], "span2": [89, 92]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7214": {"label": 2, "data": {"text": "Cd also increased ERK1/2, Akt and PDGFRalpha phosphorylation while ICI blocked it.", "entity1": "Akt", "entity2": "Cd", "span1": [26, 29], "span2": [0, 2]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9488": {"label": 1, "data": {"text": "Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine.", "entity1": "sodium channel", "entity2": "cocaine", "span1": [26, 40], "span2": [85, 92]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11161": {"label": 8, "data": {"text": "Recombinant PDE10A transfected and expressed in COS-7 cells hydrolyzed cAMP and cGMP with Km values of 0.26 and 7.2 microM, respectively, and Vmax with cGMP was almost twice that with cAMP.", "entity1": "PDE10A", "entity2": "cAMP", "span1": [12, 18], "span2": [71, 75]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10564": {"label": 1, "data": {"text": "We conclude that (-)-[(3)H]-CGP12177 binds at two sites in the recombinant beta(1)-adrenoceptor.", "entity1": "beta(1)-adrenoceptor", "entity2": "(-)-[(3)H]-CGP12177", "span1": [75, 95], "span2": [17, 36]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8884": {"label": 2, "data": {"text": "The observations suggest that in 5L cells the Igfbp-4 gene may have got under the control of a promoter containing dioxin responsive element(s) leading to the induction of IGFBP-4 by TCDD.", "entity1": "IGFBP-4", "entity2": "TCDD", "span1": [172, 179], "span2": [183, 187]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11791": {"label": 2, "data": {"text": "Meanwhile, the serum level of KC (a functional homolog of IL-8 and the main proinflammatory alpha chemokine in mice) in apoE(-/-) mice was up to 357pg/ml in SFO-HD treated group.", "entity1": "alpha chemokine", "entity2": "SFO", "span1": [92, 107], "span2": [157, 160]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"225": {"label": 3, "data": {"text": "The estrogenic agent 3 beta,5 alpha-NET and estradiol at a dose of 1.0 mg also inhibited the UG gene expression induced by P4.", "entity1": "UG", "entity2": "3 beta,5 alpha-NET", "span1": [93, 95], "span2": [21, 39]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10464": {"label": 3, "data": {"text": "Blocking EGFR signaling with the EGFR/HER-2 kinase inhibitor (KI) GW572016 decreased the postradiation survival of irradiated Ras-transformed cells and normal cells but had no effect on the survival of unirradiated cells.", "entity1": "HER-2", "entity2": "GW572016", "span1": [38, 43], "span2": [66, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4116": {"label": 2, "data": {"text": "G6PC2: A Negative Regulator of Basal Glucose-Stimulated Insulin Secretion.", "entity1": "Insulin", "entity2": "Glucose", "span1": [56, 63], "span2": [37, 44]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12641": {"label": 1, "data": {"text": "The sulfonylurea glibenclamide caused release of prebound 8-azido-[alpha-32P]ATP from SUR1 in the presence of MgADP or MgATP in a concentration-dependent manner.", "entity1": "SUR1", "entity2": "MgATP", "span1": [86, 90], "span2": [119, 124]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9976": {"label": 3, "data": {"text": "To assess the feasibility of targeting these high AAAD levels for chemotherapy, AAAD inhibitors carbidopa (alpha-methyl-dopahydrazine), alpha-monofluoromethyldopa (MFMD), and 3-hydroxybenzylhydrazine (NSD-1015) were incubated (72 h) with NCI-H727 human lung carcinoid cells.", "entity1": "AAAD", "entity2": "carbidopa", "span1": [80, 84], "span2": [96, 105]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13837": {"label": 8, "data": {"text": "Mammalian glutamate dehydrogenase (GDH) is a homohexameric enzyme that catalyzes the reversible oxidative deamination of l-glutamate to 2-oxoglutarate using NAD(P)(+) as coenzyme.", "entity1": "Mammalian glutamate dehydrogenase", "entity2": "2-oxoglutarate", "span1": [0, 33], "span2": [136, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"13184": {"label": 1, "data": {"text": "Chase studies with citalopram and methylphenidate demonstrated that this uptake is the result of preferential binding to the SERT.", "entity1": "SERT", "entity2": "methylphenidate", "span1": [125, 129], "span2": [34, 49]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12251": {"label": 9, "data": {"text": "Treatment with rosiglitazone or cholestyramine had no effect on BAT activity in any subcellular compartment.", "entity1": "BAT", "entity2": "rosiglitazone", "span1": [64, 67], "span2": [15, 28]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7717": {"label": 1, "data": {"text": "Two pure GnRH antagonists have been developed, abarelix and degarelix, that are devoid of any agonist effect on the GnRH receptor and consequently do not result in testosterone flare.", "entity1": "GnRH receptor", "entity2": "degarelix", "span1": [116, 129], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5023": {"label": 8, "data": {"text": "Using a transient heterologous cell expression system, we find that the transport activities of the short OATP2B1 variant towards substrates estrone sulfate and rosuvastatin are similar to the well-characterized full length variant.", "entity1": "short OATP2B1", "entity2": "rosuvastatin", "span1": [100, 113], "span2": [161, 173]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, 8, -1, -1, -1, -1]},
	"5522": {"label": 1, "data": {"text": "Probing the salmeterol binding site on the beta 2-adrenergic receptor using a novel photoaffinity ligand, [(125)I]iodoazidosalmeterol.", "entity1": "beta 2-adrenergic receptor", "entity2": "salmeterol", "span1": [43, 69], "span2": [12, 22]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15026": {"label": 3, "data": {"text": "Treatment with adenosine dialdehyde (AdOx), an inhibitor of transmethylation-suppressive adenosylhomocysteine (SAH) hydrolase (SAHH), enhanced the level of SAH and effectively blocked the proliferation, migration, and invasion of cancer cells; the treatment also induced the differentiation of C6 glioma cells and suppressed the neovascular genesis of eggs in a dose-dependent manner.", "entity1": "adenosylhomocysteine (SAH) hydrolase", "entity2": "AdOx", "span1": [89, 125], "span2": [37, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7205": {"label": 1, "data": {"text": "Estradiol (E2) stimulates BC cells proliferation by binding the estrogen receptor (ER).", "entity1": "ER", "entity2": "E2", "span1": [83, 85], "span2": [11, 13]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14418": {"label": 1, "data": {"text": "Metformin directly inhibits ghrelin secretion through AMP-activated protein kinase in rat primary gastric cells.", "entity1": "AMP-activated protein kinase", "entity2": "Metformin", "span1": [54, 82], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3298": {"label": 3, "data": {"text": "Everolimus (RAD001, Afinitor((R)) Novartis) is the first oral inhibitor of mTOR (mammalian target of rapamycin) to reach the oncology clinic.", "entity1": "mammalian target of rapamycin", "entity2": "Everolimus", "span1": [81, 110], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8848": {"label": 3, "data": {"text": "Herein, we investigated the effect of a natural neuroprotective flavonoid, calycopterin, on H2O2-induced disruption of phase II detoxifying enzyme system and cAMP response element binding protein (CREB) phosphorylation.", "entity1": "cAMP response element binding protein", "entity2": "H2O2", "span1": [158, 195], "span2": [92, 96]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15975": {"label": 1, "data": {"text": "Design, Synthesis and Biological Evaluation of Aminoalkylindole Derivatives as Cannabinoid Receptor Ligands with Potential for Treatment of Alcohol Abuse.", "entity1": "Cannabinoid Receptor", "entity2": "Aminoalkylindole", "span1": [79, 99], "span2": [47, 63]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14664": {"label": 1, "data": {"text": "These findings demonstrated that genistein improves thrombin-induced endothelial barrier dysfunction in ECs through PKA-mediated suppression of RhoA signaling.", "entity1": "RhoA", "entity2": "genistein", "span1": [144, 148], "span2": [33, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6705": {"label": 1, "data": {"text": "Inhibitory effects of the monoamine oxidase inhibitor tranylcypromine on the cytochrome P450 enzymes CYP2C19, CYP2C9, and CYP2D6.", "entity1": "cytochrome P450", "entity2": "tranylcypromine", "span1": [77, 92], "span2": [54, 69]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"652": {"label": 3, "data": {"text": "Here we report that captopril treatment resulted in decreased transcription and protein levels of gelatinase A by 3LL cells.", "entity1": "gelatinase A", "entity2": "captopril", "span1": [98, 110], "span2": [20, 29]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6213": {"label": 1, "data": {"text": "This study therefore characterized the binding of DF to the sigma receptors and NMDA-linked PCP sites and examined the anticonvulsant as well as locomotor effects of DF in mice in comparison with those of DM and DR. We found that DF, DM, and DR were relative high-affinity ligands at sigma-1 receptors (Ki=151, 205, 144 nM, respectively) while all of them were with low affinity at sigma-2 receptors (Ki=4-11 microM).", "entity1": "sigma-2 receptors", "entity2": "DR", "span1": [382, 399], "span2": [242, 244]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5630": {"label": 8, "data": {"text": "Neuronal NE reuptake may be impaired in individuals with renal disease and/or hypertension due to dysfunction of the NE transporter.", "entity1": "NE transporter", "entity2": "NE", "span1": [117, 131], "span2": [9, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5215": {"label": 2, "data": {"text": "In addition, vinblastine induces the DNA-binding activities of the transcription factor NF-\u03baB, HSF1, AP-1, and ATF-2, together with the expression of HSP70 and Bax proteins.", "entity1": "NF-\u03baB", "entity2": "vinblastine", "span1": [88, 93], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7243": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "para-tyramine", "span1": [231, 237], "span2": [61, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2992": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "F820A", "entity2": "tadalafil", "span1": [265, 270], "span2": [60, 69]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3542": {"label": 2, "data": {"text": "Leukotriene D4 induces cognitive impairment through enhancement of CysLT\u2081 R-mediated amyloid-\u03b2 generation in mice.", "entity1": "CysLT\u2081 R", "entity2": "Leukotriene D4", "span1": [67, 75], "span2": [0, 14]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13207": {"label": 8, "data": {"text": "SecS required selenophosphate and O-phosphoseryl-tRNA([Ser]Sec) as substrates to generate selenocysteyl-tRNA([Ser]Sec).", "entity1": "SecS", "entity2": "O-phosphoseryl", "span1": [0, 4], "span2": [34, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"2473": {"label": 2, "data": {"text": "Liver BHMT activity was 1.3-fold higher in rats fed the Met deficient diet containing choline, which was reflected in corresponding increases in mRNA content and immunodetectable protein.", "entity1": "BHMT", "entity2": "choline", "span1": [6, 10], "span2": [86, 93]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10656": {"label": 3, "data": {"text": "Valdecoxib inhibits COX-1 in a competitive fashion only at very high concentrations (IC(50) = 150 microM).", "entity1": "COX-1", "entity2": "Valdecoxib", "span1": [20, 25], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8694": {"label": 8, "data": {"text": "Among the possible transporters involved in the uptake of Cd(2+) and Mn(2+), the expression of ZIP8 (Zrt-, Irt-related protein 8), encoded by Slc39a8, showed a marked suppression in both RBL-Cdr and RBL-Mnr cells.", "entity1": "Zrt-, Irt-related protein 8", "entity2": "Cd(2+)", "span1": [101, 128], "span2": [58, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7314": {"label": 8, "data": {"text": "Here, we describe a new photolabile alanine derivative based on protection of alanine with the 4-methoxy-7-nitroindolinyl (MNI) caging group, which we use for pre-steady-state kinetic analysis of alanine transport by ASCT2, SNAT1, and SNAT2.", "entity1": "SNAT2", "entity2": "4-methoxy-7-nitroindolinyl", "span1": [235, 240], "span2": [95, 121]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"665": {"label": 3, "data": {"text": "METHODS: COX-1 inhibition was determined by measuring thromboxane B2 (TXB2)-generation from clotting whole blood ex vivo after single oral doses of 7.5 and 15 mg meloxicam and 75 mg diclofenac and at steady state (15 mg meloxicam daily and 150 mg diclofenac daily).", "entity1": "COX-1", "entity2": "meloxicam", "span1": [9, 14], "span2": [220, 229]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"324": {"label": 1, "data": {"text": "The folding rate monitored by 2'CMP binding to the major slow-folding species of Pro42Ala RNase A is faster than the folding rate monitored by tyrosine burial; however, the folding rate monitored by inhibitor binding to the minor slow-folding species is decreased significantly over the folding rate monitored by tyrosine burial, indicating that the major and minor slow-folding species of Pro42Ala fold to the native state with different transition-state conformations in the rate-determining step.", "entity1": "Pro42Ala", "entity2": "tyrosine", "span1": [81, 89], "span2": [143, 151]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5056": {"label": 1, "data": {"text": "These data provided a novel insight to the mechanisms of Rg1protective effects on A\u03b225-35-induced endothelial cells apoptosis, suggesting that GR-ERK signaling pathway might play an important role in it.", "entity1": "GR", "entity2": "Rg1", "span1": [143, 145], "span2": [57, 60]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5472": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel, the major metabolite of desogestrel, for the progesterone receptor in intact MCF-7 cells was twice that of levonorgestrel and Org 2058, three times that of medroxy-progesterone acetate (MPA), 4.5 times that of norethisterone and 5 times that of progesterone and cyproterone acetate whereas at 4 degrees C in the cytosol fraction of MCF-7 cells exposed to molybdate (nontransformed receptor complexes) 3-keto-desogestrel and Org 2058 displayed similar affinity.", "entity1": "progesterone receptor", "entity2": "Org 2058", "span1": [106, 127], "span2": [187, 195]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15960": {"label": 1, "data": {"text": "4-Hydroxytamoxifen-stimulated processing of cyclin E is mediated via G protein-coupled receptor 30 (GPR30) and accompanied by enhanced migration in MCF-7 breast cancer cells.", "entity1": "G protein-coupled receptor 30", "entity2": "4-Hydroxytamoxifen", "span1": [69, 98], "span2": [0, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7626": {"label": 2, "data": {"text": "Quinpirole and 7-OH-DPAT also increased the phosphorylation of extracellular signal-regulated kinase (ERK) within minutes, an effect blocked by pretreatment with SB-277011-A.", "entity1": "ERK", "entity2": "Quinpirole", "span1": [102, 105], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11997": {"label": 1, "data": {"text": "We found that in vitro rapamycin also regulates the proteasome, an essential intracellular protease of the ubiquitin-proteasome pathway.", "entity1": "proteasome", "entity2": "rapamycin", "span1": [52, 62], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2028": {"label": 1, "data": {"text": "Hence, it is proposed that a conformational change is induced when ApoCaM interacts with GAD65 or tGAD67, resulting in an increase of GAD affinity for PLP and the activation of GAD.", "entity1": "GAD", "entity2": "PLP", "span1": [134, 137], "span2": [151, 154]}, "weak_labels": [-1, -1, -1, -1, 1, 1, 2, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9592": {"label": 1, "data": {"text": "Crystallographic comparison with the structurally related rat tyrosine hydroxylase binary complex with the oxidized cofactor 7,8-dihydrobiopterin revealed overlapping binding sites for the catechols and the cofactor, compatible with a competitive type of inhibition of the catechols versus BH4.", "entity1": "rat tyrosine hydroxylase", "entity2": "7,8-dihydrobiopterin", "span1": [58, 82], "span2": [125, 145]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"8734": {"label": 1, "data": {"text": "Kinetic analyses revealed that the affinity and clearance of UGT2B10 for amitriptyline, imipramine, and diphenhydramine are significantly higher than the corresponding values of UGT1A4 and UGT1A3, although the Vmax values of UGT1A4 toward these drugs are considerably higher.", "entity1": "UGT1A4", "entity2": "diphenhydramine", "span1": [178, 184], "span2": [104, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5934": {"label": 3, "data": {"text": "Cyproterone acetate, a progestin used in the treatment of hirsutism, acne and prostate cancer as well as norgestrel and norethindrone that are widely used as oral contraceptives also inhibit 3 beta-HSD activity at Ki values of 1.5, 1.7 and 2.5 microM, respectively.", "entity1": "3 beta-HSD", "entity2": "progestin", "span1": [191, 201], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12494": {"label": 1, "data": {"text": "An X-ray crystal structure of cytochrome P450 2B4 in complex with the drug paroxetine was solved at 2.14 \u00c5 resolution.", "entity1": "cytochrome P450 2B4", "entity2": "paroxetine", "span1": [30, 49], "span2": [75, 85]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"873": {"label": 8, "data": {"text": "Depletion of putrescine, spermidine, and spermine by DL-alpha-difluoromethylornithine (DFMO), a specific inhibitor of ornithine decarboxylase (ODC) that is the first rate-limiting enzyme for polyamine biosynthesis, decreased the apoptotic index.", "entity1": "ornithine decarboxylase", "entity2": "spermine", "span1": [118, 141], "span2": [41, 49]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9004": {"label": 5, "data": {"text": "adenosine agonists, N6-(R-phenylisopropyl)adenosine (R-PIA), N6-(S-phenylisopropyl)adenosine, 5'-(N-cyclopropyl)-carboxamidoadenosine, antagonists, theophylline and 8-p-(sulfophenyl)theophylline as well as enprofylline on ethanol-(i.p.", "entity1": "adenosine", "entity2": "enprofylline", "span1": [0, 9], "span2": [206, 218]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5221": {"label": 2, "data": {"text": "Also, vinblastine enhances the phosphorylation of Ras homologous protein A, the accumulation of reactive oxygen species, the release of intracellular Ca(2+), as well as the activation of apoptosis signal-regulating kinase 1, c-jun-N-terminal kinase, p38, inhibitor of kappaB\u03b1 (I\u03baB\u03b1) kinase, and inositol requiring enzyme 1\u03b1.", "entity1": "c-jun-N-terminal kinase", "entity2": "vinblastine", "span1": [225, 248], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11277": {"label": 8, "data": {"text": "One major route involves the tetrahydrofolate (THF)-dependent activities of the glycine decarboxylase complex (GDC, EC 2.1.1.10) and serine hydroxymethyltransferase (SHMT, EC 2.1.2.1) with glycine (Gly) as one-carbon (1-C) source.", "entity1": "serine hydroxymethyltransferase", "entity2": "glycine", "span1": [133, 164], "span2": [189, 196]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4781": {"label": 3, "data": {"text": "Concentration-dependent inhibitory effects of baicalin on the metabolism of dextromethorphan, a dual probe of CYP2D and CYP3A, in rats.", "entity1": "CYP2D", "entity2": "baicalin", "span1": [110, 115], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"230": {"label": 3, "data": {"text": "The inhibition of UG synthesis and PR down-regulation by 5 alpha-NET and 3 beta,5 alpha-NET indicates that these NET metabolites possess antiprogestational properties.", "entity1": "UG", "entity2": "NET", "span1": [18, 20], "span2": [113, 116]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2064": {"label": 9, "data": {"text": "As a result, we demonstrated that the apoE3 significantly protects these cells from GMC-induced reduction in AMG uptake, but neither lactoferrin nor albumin does.", "entity1": "lactoferrin", "entity2": "GMC", "span1": [133, 144], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15376": {"label": 0, "data": {"text": "Thus, the formation of disulfide bonds in hSULT2A1 is a potentially important reversible mechanism for alterations in the rates of sulfation of both endogenous and xenobiotic substrates.", "entity1": "hSULT2A1", "entity2": "disulfide", "span1": [42, 50], "span2": [23, 32]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6321": {"label": 3, "data": {"text": "We report that the radiation-induced activation of the kinase Cds1 [4] (also known as Chk2 [5]) is inhibited by caffeine in vivo and that ATM kinase activity is directly inhibited by caffeine in vitro.", "entity1": "Cds1", "entity2": "caffeine", "span1": [62, 66], "span2": [112, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12669": {"label": 8, "data": {"text": "In conclusion, OMCD tubules from deoxycorticosterone pivalate-treated rats secrete Cl- into the luminal fluid through NKCC1-mediated Cl- uptake across the basolateral membrane in series with Cl- efflux across the apical membrane.", "entity1": "NKCC1", "entity2": "Cl-", "span1": [118, 123], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11551": {"label": 1, "data": {"text": "Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol.", "entity1": "serotonin (2A) receptors", "entity2": "flupentixol", "span1": [38, 62], "span2": [102, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7323": {"label": 8, "data": {"text": "Na+-Dependent transmembrane transport of small neutral amino acids, such as glutamine and alanine, is mediated, among others, by the neutral amino acid transporters of the solute carrier 1 [SLC1, alanine serine cysteine transporter 1 (ASCT1), and ASCT2] and SLC38 families [sodium-coupled neutral amino acid transporter 1 (SNAT1), SNAT2, and SNAT4].", "entity1": "SNAT1", "entity2": "amino acids", "span1": [323, 328], "span2": [55, 66]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"1494": {"label": 3, "data": {"text": "EGF-stimulated phosphorylation of ERK and Bad is blocked by pretreatment with U0126, a selective MAP kinase kinase (MKK)1/2 inhibitor.", "entity1": "Bad", "entity2": "U0126", "span1": [42, 45], "span2": [78, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8924": {"label": 3, "data": {"text": "Carvedilol produced significant inhibition of the alpha 1 adrenoceptor mediated pressor response to cirazoline in the pithed rat, but had no effect on the alpha 2 adrenoceptor mediated pressor response to B-HT 933, suggesting that carvedilol is also an alpha 1 adrenoceptor antagonist at antihypertensive doses.", "entity1": "alpha 1 adrenoceptor", "entity2": "Carvedilol", "span1": [50, 70], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"13673": {"label": 9, "data": {"text": "Two imidazoquinoline molecules, imiquimod and gardiquimod, markedly activated both porcine TLR7 and TLR8 whereas only human TLR7, but not TLR8, was activated by the ligands.", "entity1": "TLR8", "entity2": "gardiquimod", "span1": [138, 142], "span2": [46, 57]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15674": {"label": 3, "data": {"text": "These findings indicate that MBE and its anthocyanidins suppress the light-induced photoreceptor cell death by inhibiting ROS production, suggesting that the inhibition of phosphorylated-p38 may be involved in the underlying mechanism.", "entity1": "phosphorylated-p38", "entity2": "anthocyanidins", "span1": [172, 190], "span2": [41, 55]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"590": {"label": 3, "data": {"text": "Orlistat is a new inhibitor of pancreatic lipase enzyme.", "entity1": "pancreatic lipase", "entity2": "Orlistat", "span1": [31, 48], "span2": [0, 8]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7081": {"label": 2, "data": {"text": "Similar to menthol, both camphor and cinnamaldehyde (initially reported to be specific activators of TRPV3 and TRPA1, respectively) also modulate other thermoTRPs.", "entity1": "TRPA1", "entity2": "menthol", "span1": [111, 116], "span2": [11, 18]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 6, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2008": {"label": 0, "data": {"text": "Point-mutation studies indicate that four amino acids, Leu/Phe(7.38), Leu/Phe(7.43), Ala/Pro(7.46), and Pro/Cys(7.47) in TMH7 are critical for ligand selectivity as well as receptor conformation.", "entity1": "TMH7", "entity2": "Ala", "span1": [121, 125], "span2": [85, 88]}, "weak_labels": [0, -1, 0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"317": {"label": 1, "data": {"text": "Recent studies highlight the capacity of sucralfate to bind basic fibroblast growth factor (bFGF) and deliver it in high concentration to the ulcer.", "entity1": "bFGF", "entity2": "sucralfate", "span1": [92, 96], "span2": [41, 51]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14072": {"label": 3, "data": {"text": "Exogenous stimulation of PKA activity, achieved by forskolin treatment, protected K-ras-transformed cells from apoptosis induced by glucose deprivation, enhanced complex I activity, intracellular adenosine triphosphate (ATP) levels, mitochondrial fusion and decreased intracellular reactive oxygen species (ROS) levels.", "entity1": "K-ras", "entity2": "glucose", "span1": [82, 87], "span2": [132, 139]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4564": {"label": 1, "data": {"text": "Adenosine, an enzymatic ATP degradation product, acts at prejunctional A1 adenosine receptors (A1Rs) to inhibit NE release.", "entity1": "A1 adenosine receptors", "entity2": "Adenosine", "span1": [71, 93], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10455": {"label": 8, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "(L-serine dehydratase", "entity2": "ammonia", "span1": [4, 25], "span2": [139, 146]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"5097": {"label": 2, "data": {"text": "Aldosterone-induced ENaC and basal Na(+)/K(+)-ATPase trafficking via protein kinase D1-phosphatidylinositol 4-kinaseIII\u03b2 trans Golgi signalling in M1 cortical collecting duct cells.", "entity1": "Na(+)/K(+)-ATPase", "entity2": "Aldosterone", "span1": [35, 52], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2447": {"label": 1, "data": {"text": "Taken together, these data suggest that ATB-429 inhibits hypersensitivity induced by CRD in both healthy and postcolitic, allodynic rats by a K(ATP) channel-mediated mechanism.", "entity1": "K(ATP) channel", "entity2": "ATB-429", "span1": [142, 156], "span2": [40, 47]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2146": {"label": 3, "data": {"text": "Using the nucleoside transporter deficient PK15NTD cells stably expressing ENT1 and ENT2, it was found that troglitazone inhibited ENT1 but had no effect on ENT2.", "entity1": "ENT1", "entity2": "troglitazone", "span1": [131, 135], "span2": [108, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"12863": {"label": 9, "data": {"text": "However, N-methyl-phosphatidylserine, which is transported by the plasma membrane flippase at a rate equivalent to PS, is incapable of activating Atp8a1 activity.", "entity1": "Atp8a1", "entity2": "N-methyl-phosphatidylserine", "span1": [146, 152], "span2": [9, 36]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"11200": {"label": 1, "data": {"text": "These results suggest that ATP-bound TOP2 may be the specific target of ATP-sensitive TOP2 poisons.", "entity1": "TOP2", "entity2": "ATP", "span1": [37, 41], "span2": [27, 30]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10302": {"label": 3, "data": {"text": "Sildenafil exhibits inhibitory potency against PDE5 and a 10-fold lower dose-related inhibitory potency against rod outer segment PDE6, the predominant PDE in the phototransduction cascade in rods.", "entity1": "PDE5", "entity2": "Sildenafil", "span1": [47, 51], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13308": {"label": 3, "data": {"text": "Sorafenib induced a cell cycle block and apoptosis in the acute myeloid leukemia cell lines MV4-11 and MOLM-13, both expressing FLT3 with an internal tandem duplication, whereas no effect was observed on four other acute myeloid leukemia cell lines.", "entity1": "FLT3", "entity2": "Sorafenib", "span1": [128, 132], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12042": {"label": 2, "data": {"text": "Both the phosphotriesterase and physostigmine treatments protected the brain AChE activities measured 24 h after sarin exposure.", "entity1": "AChE", "entity2": "physostigmine", "span1": [77, 81], "span2": [32, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5481": {"label": 1, "data": {"text": "At 37 degrees C the relative affinity of 3-keto-desogestrel for the androgen receptor in intact MCF-7 cells was half that of levonorgestrel, similar to that of norethisterone and medroxyprogesterone acetate (MPA) and at least three times higher than that of progestagens with anti-androgenic activity whereas at 4 degrees C in the cytosol fraction exposed to molybdate there was no clear difference between the relative affinities of progestagens with androgenic and anti-androgenic properties.", "entity1": "androgen receptor", "entity2": "3-keto-desogestrel", "span1": [68, 85], "span2": [41, 59]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9005": {"label": 5, "data": {"text": "Enprofylline, a weak adenosine antagonist but potent inhibitor of cyclic AMP phosphodiesterase, did not alter ethanol's motor incoordination, further supporting involvement of brain adenosine receptor mechanism(s) in ethanol-adenosine interactions.", "entity1": "adenosine", "entity2": "Enprofylline", "span1": [21, 30], "span2": [0, 12]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15191": {"label": 8, "data": {"text": "The involvement of P-gp in the absorption of darunavir was clearly shown by coperfusion of darunavir with the P-gp inhibitor zosuquidar.", "entity1": "P-gp", "entity2": "darunavir", "span1": [19, 23], "span2": [45, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6809": {"label": 1, "data": {"text": "Effect of pitavastatin on apolipoprotein A-I production in HepG2 cell.", "entity1": "apolipoprotein A-I", "entity2": "pitavastatin", "span1": [26, 44], "span2": [10, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4934": {"label": 1, "data": {"text": "In the present study, we aimed at examining the effect of 1-ethyl-5-methyl-2-phenyl-1H-benzo[d]imidazole, a synthetic small molecular compound also named Fc11a-2, for the treatment of dextran sulfate sodium (DSS)-induced experimental colitis in mice via targeting NLRP3 inflammasome.", "entity1": "NLRP3", "entity2": "Fc11a-2", "span1": [264, 269], "span2": [154, 161]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7976": {"label": 3, "data": {"text": "Moreover, 1,25(OH)(2)D(3) decreased expression of Oat1 and Oat3 in rat kidney.", "entity1": "Oat1", "entity2": "1,25(OH)(2)D(3)", "span1": [50, 54], "span2": [10, 25]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10445": {"label": 7, "data": {"text": "SDH (L-serine dehydratase, EC 4.3.1.17) catalyzes the pyridoxal 5'-phosphate (PLP)-dependent dehydration of L-serine to yield pyruvate and ammonia.", "entity1": "EC 4.3.1.17", "entity2": "PLP", "span1": [27, 38], "span2": [78, 81]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"3568": {"label": 1, "data": {"text": "The results showed that IR tyrosine phosphorylation (pIR) was reduced by 42\u00a0% in MSG-obese mice (MSG, 6.7\u00a0\u00b1\u00a00.2\u00a0arbitrary units (a.u.", "entity1": "IR", "entity2": "MSG", "span1": [24, 26], "span2": [81, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12587": {"label": 1, "data": {"text": "Coexpression of the flip and flop splice variants of GluR-A, in the absence of GluR-B, revealed that heteromeric AMPA receptors with intermediate sensitivity to cyclothiazide, similar to responses observed for the combinations GluR-AoBi or GluR-AiBo, could be generated independently of the presence of the GluR-B subunit.", "entity1": "GluR-B", "entity2": "cyclothiazide", "span1": [307, 313], "span2": [161, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7377": {"label": 1, "data": {"text": "Histamine regulates many functions by binding to four histamine G-coupled receptor proteins (H1R, H2R, H3R and H4R).", "entity1": "H2R", "entity2": "Histamine", "span1": [98, 101], "span2": [0, 9]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5959": {"label": 1, "data": {"text": "After loperamide administration ACTH levels fell to a nadir of 135 +/- 76 pg/ml, and then CRH was still able to induce an ACTH increase; the pattern of ACTH response to CRH was slightly delayed.", "entity1": "CRH", "entity2": "loperamide", "span1": [90, 93], "span2": [6, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7895": {"label": 2, "data": {"text": "Further we found stimulation of FAS-expression as a result of epigenetic DNA demethylation that was due to down-regulation of DNMT1, which was rescued by re-isoprenylation by both geranylgeranyl-pyrophosphate and farnesylpyrophosphate.", "entity1": "DNMT1", "entity2": "geranylgeranyl-pyrophosphate", "span1": [126, 131], "span2": [180, 208]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12571": {"label": 8, "data": {"text": "Glutathione-independent prostaglandin D synthase [prostaglandin-H2 D-isomerase; (5Z,13E)-(15S)-9 alpha,11 alpha-epidioxy-15-hydroxyprosta-5,13-dienoate D-isomerase, EC 5.3.99.2] is an enzyme responsible for biosynthesis of prostaglandin D2 in the central nervous system.", "entity1": "prostaglandin-H2 D-isomerase", "entity2": "prostaglandin D2", "span1": [50, 78], "span2": [223, 239]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13125": {"label": 3, "data": {"text": "SK-Br3 cells cultured in the presence of topoisomerase IIalpha (TOP2A) inhibitors doxorubicin and etopoxide (VP-16) demonstrated a 2- to 3-fold increase in FAS promoter activity when compared with control cells growing in drug-free culture conditions.", "entity1": "topoisomerase IIalpha", "entity2": "VP-16", "span1": [41, 62], "span2": [109, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2960": {"label": 1, "data": {"text": "Affinity of V782A for cGMP, vardenafil, sildenafil, tadalafil, or IBMX was reduced 5.5-, 23-, 10-, 3-, and 12-fold, respectively.", "entity1": "V782A", "entity2": "tadalafil", "span1": [12, 17], "span2": [52, 61]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4363": {"label": 5, "data": {"text": "However, recent clinical studies have shown that a single low-dose injection of ketamine, an N-methyl d-aspartate receptor (NMDAR) antagonist, has rapid antidepressant effects that are observed within hours and are long lasting.", "entity1": "NMDAR", "entity2": "ketamine", "span1": [124, 129], "span2": [80, 88]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3119": {"label": 8, "data": {"text": "First, addition of apolipoprotein A-I (apoA-I), a direct acceptor of the ATP-binding cassette transporter A1 (ABCA1)-secreted lipids, increased alpha-tocopherol secretion in a dose-dependent manner.", "entity1": "ABCA1", "entity2": "alpha-tocopherol", "span1": [110, 115], "span2": [144, 160]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5561": {"label": 3, "data": {"text": "Treatment of cells with BCNU to inhibit glutathione reductase (GR) enhanced the CpG-induced intracellular oxidation and decreased the GSH/GSSG, with increased activation of NF-kappaB and a doubling in the CpG-induced production of IL-6 and TNF-alpha.", "entity1": "IL-6", "entity2": "GSH", "span1": [231, 235], "span2": [134, 137]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, 2, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"678": {"label": 7, "data": {"text": "In contrast, there was little change in mRNA levels for GTP cyclohydrolase I (GTPCH), the rate limiting enzyme in synthesis of the tetrahydrobiopterin (BH4), the obligate cofactor for TPH.", "entity1": "TPH", "entity2": "tetrahydrobiopterin", "span1": [184, 187], "span2": [131, 150]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 7, -1, -1, -1, -1, -1, -1]},
	"11888": {"label": 8, "data": {"text": "Ferredoxin 1 (FDX1; adrenodoxin) is an iron-sulfur protein that is involved in various metabolic processes, including steroid hormone synthesis in mammalian tissues.", "entity1": "FDX1", "entity2": "steroid hormone", "span1": [14, 18], "span2": [118, 133]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12749": {"label": 2, "data": {"text": "Ang II level in plasma and mesenteric arteries in imidapril group was significantly lower than that in irbesartan group (P<0.05).", "entity1": "Ang II", "entity2": "irbesartan", "span1": [0, 6], "span2": [103, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"976": {"label": 3, "data": {"text": "Previously, we showed that the human kappa-opioid receptor (hkor) stably expressed in Chinese hamster ovary (CHO) cells underwent down-regulation after prolonged U50,488H treatment.", "entity1": "human kappa-opioid receptor", "entity2": "U50,488H", "span1": [31, 58], "span2": [162, 170]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10969": {"label": 1, "data": {"text": "mRNA levels for RAR-alpha, RAR-beta and RAR-gamma, the nuclear receptors for retinoic acid, decreased during activation of freshly isolated HSC even with retinoid supplementation.", "entity1": "RAR-gamma", "entity2": "retinoic acid", "span1": [40, 49], "span2": [77, 90]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14494": {"label": 1, "data": {"text": "In breast cancer (BC) epithelial cells, the mitogenic action of estradiol is transduced through binding to two receptors, ER\u03b1 and ER\u03b2, which act as transcription factors.", "entity1": "ER\u03b2", "entity2": "estradiol", "span1": [130, 133], "span2": [64, 73]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11451": {"label": 1, "data": {"text": "The present study examined the reinforcing and DAT effects of the local anesthetics dimethocaine, procaine and cocaine using in vivo techniques.", "entity1": "DAT", "entity2": "procaine", "span1": [47, 50], "span2": [98, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15640": {"label": 3, "data": {"text": "Furthermore, nobiletin could inhibit HGF-induced the membrane localization of phosphorylated c-Met, ERK2, and Akt, but not phosphorylated JNK1/2 and p38.", "entity1": "c-Met", "entity2": "nobiletin", "span1": [93, 98], "span2": [13, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"9839": {"label": 3, "data": {"text": "The Hsp90-specific inhibitor geldanamycin selectively disrupts kinase-mediated signaling events of T-lymphocyte activation.", "entity1": "Hsp90", "entity2": "geldanamycin", "span1": [4, 9], "span2": [29, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2396": {"label": 0, "data": {"text": "In striking contrast, deletion of the corresponding C-terminal domain of Escherichia coli LeuRS abolished aminoacylation of tRNALeu and also amino acid editing of mischarged tRNA molecules.", "entity1": "Escherichia coli LeuRS", "entity2": "amino acid", "span1": [73, 95], "span2": [141, 151]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2155": {"label": 2, "data": {"text": "Thalidomide reduced COX-2 expression accompanied by a decrease of bcl-2 protein, TNFalpha, VEGF, GSH and an increased cytochrome c, but had no effect on that of COX-1, in MCF-7 and HL-60.", "entity1": "cytochrome c", "entity2": "Thalidomide", "span1": [118, 130], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2379": {"label": 3, "data": {"text": "Further characterization of sorafenib revealed that this molecule was a multikinase inhibitor that targeted the vascular endothelial growth factor receptor family (VEGFR-2 and VEGFR-3) and platelet-derived growth factor receptor family (PDGFR-beta and Kit), which play key roles in tumor progression and angiogenesis.", "entity1": "VEGFR-3", "entity2": "sorafenib", "span1": [176, 183], "span2": [28, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11070": {"label": 1, "data": {"text": "We have examined the effects on the activities of three calmodulin-dependent enzymes (cAMP phosphodiesterase, caldesmon kinase and myosin light chain kinase) of the dihydropyridine Ca2+ channel blocker felodipine and three analogues (p-chloro, oxidized and t-butyl) exhibiting different pharmacological potencies.", "entity1": "myosin light chain kinase", "entity2": "felodipine", "span1": [131, 156], "span2": [202, 212]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6910": {"label": 8, "data": {"text": "PSMA acts as a glutamate carboxypeptidase (GCPII) on small molecule substrates, including folate, the anticancer drug methotrexate, and the neuropeptide N-acetyl-l-aspartyl-l-glutamate.", "entity1": "GCPII", "entity2": "folate", "span1": [43, 48], "span2": [90, 96]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"130": {"label": 3, "data": {"text": "The cAMP phosphodiesterase was inhibited completely by felodipine and the p-chloro analogue with IC50 values of 3.7 and 1.5 microM respectively.", "entity1": "cAMP phosphodiesterase", "entity2": "p-chloro", "span1": [4, 26], "span2": [74, 82]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10737": {"label": 9, "data": {"text": "Using the reverse-transcription and real-time quantitative PCR (RQ-PCR) analysis, we indicated that AZC and PCA did not profoundly affect on CD3-zeta chain transcription in Jurkat T leukemia cells clone E6-1.", "entity1": "CD3-zeta chain", "entity2": "PCA", "span1": [141, 155], "span2": [108, 111]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11477": {"label": 0, "data": {"text": "LeucylLeucyl-tRNA synthetase (LeuRS) performs dual essential roles in group I intron RNA splicing as well as protein synthesis within the yeast mitochondria.", "entity1": "Leucyl-tRNA synthetase", "entity2": "Leucyl", "span1": [6, 28], "span2": [0, 6]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10756": {"label": 1, "data": {"text": "An in vitro kinase assay showed that imatinib did not directly affect EGFR kinase activity, suggesting involvement of EGFR-activating molecules.", "entity1": "EGFR", "entity2": "imatinib", "span1": [118, 122], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15146": {"label": 9, "data": {"text": "The mRNA level for nestin (Nes, biomarker for stem Leydig cells) was significantly increased in the control testis on day 4 post-EDS, but not in the DEHP treated testes, suggesting that these nestin positive stem cells were differentiated into progenitor Leydig cells in the DEHP-treated testes.", "entity1": "Nes", "entity2": "DEHP", "span1": [27, 30], "span2": [149, 153]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"13339": {"label": 2, "data": {"text": "In addition, activation of protein kinase C and increases in intracellular cAMP also enhance cholinergic activity in T cells, and lymphocyte function associated antigen-1 (LFA-1; CD11a/CD18) is an important mediator of leukocyte migration and T cell activation.", "entity1": "lymphocyte function associated antigen-1", "entity2": "cAMP", "span1": [130, 170], "span2": [75, 79]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9423": {"label": 1, "data": {"text": "These observations show substrate- and enzyme-specific PTP inhibition by alendronate and support the possibility that a certain PTP(s) may be the molecular target for alendronate action.", "entity1": "PTP", "entity2": "alendronate", "span1": [128, 131], "span2": [167, 178]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"4115": {"label": 3, "data": {"text": "Furthermore, DOX-treated WT and p65(-/-) MEFs differed in their expression of various apoptosis-associated molecules, when the former demonstrated a decrease in the percentage of p65-positive and a more prominent decrease in the percentage of p53-positive cells, while a decreased percentage of I\u03baB\u03b1-positive and a more prominent decrease in the percentage of bcl-2-positive cells was detected among the latter.", "entity1": "p65", "entity2": "DOX", "span1": [179, 182], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9014": {"label": 4, "data": {"text": "Limitation of SRF was produced by the anticonvulsant BDZs (diazepam, clonazepam, nitrazepam and lorazepam) at low to mid nanomolar concentrations, by a convulsant BDZ which does not bind to high affinity BDZ receptors (Ro 5-4864) at high nanomolar concentrations and by a BDZ receptor weak partial agonist (Ro 15-1788) at micromolar concentrations.", "entity1": "BDZ receptor", "entity2": "Ro 15-1788", "span1": [272, 284], "span2": [307, 317]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"8001": {"label": 2, "data": {"text": "Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs.", "entity1": "thrombin", "entity2": "IMG", "span1": [182, 190], "span2": [140, 143]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"10337": {"label": 2, "data": {"text": "The results show that transient arsenite pre-treatment induces Hsp72, HO-1 and, to a lesser extent, Hsp27; it reduces H2O2-induced astrocyte death; and it causes selective activation of Akt following H2O2.", "entity1": "Akt", "entity2": "arsenite", "span1": [186, 189], "span2": [32, 40]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7195": {"label": 8, "data": {"text": "Blocking retinyl ester formation by a targeted knock down of Lratb results in significantly increased retinoic acid levels, which lead to severe embryonic patterning defects.", "entity1": "Lratb", "entity2": "retinyl ester", "span1": [61, 66], "span2": [9, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5439": {"label": 3, "data": {"text": "A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the \u03b2-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA.", "entity1": "EC 4.2.1.1", "entity2": "tyrphostine", "span1": [153, 163], "span2": [72, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10209": {"label": 8, "data": {"text": "100 micromol/L rifampicin inhibited OATP-C- and OATP8-, OATP-B- and OATP-A-mediated BSP uptake by 66%, 96%, 25%, and 49%, respectively.", "entity1": "OATP-A", "entity2": "BSP", "span1": [68, 74], "span2": [84, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9538": {"label": 8, "data": {"text": "However, the apparent affinity for lysine transport was 2.4 times lower in Cat1(-/-) cells when compared with wild type cells, a property characteristic of Cat3-mediated transport.", "entity1": "Cat3", "entity2": "lysine", "span1": [156, 160], "span2": [35, 41]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"10757": {"label": 1, "data": {"text": "An in vitro kinase assay showed that imatinib did not directly affect EGFR kinase activity, suggesting involvement of EGFR-activating molecules.", "entity1": "EGFR", "entity2": "imatinib", "span1": [70, 74], "span2": [37, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2993": {"label": 1, "data": {"text": "Catalytic-site affinities for cGMP, vardenafil, sildenafil, tadalafil, or 3-isobutyl-1-methylxanthine (IBMX) were respectively weakened 14-, 123-, 30-, 51-, and 43-fold for Y612A; 63-, 511-, 43-, 95- and 61-fold for Q817A; and 59-, 448-, 71-, 137-, and 93-fold for F820A.", "entity1": "Y612A", "entity2": "3-isobutyl-1-methylxanthine", "span1": [173, 178], "span2": [74, 101]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7725": {"label": 3, "data": {"text": "Luteinizing hormone-releasing hormone (LHRH) agonists, such as buserelin, goserelin, leuprorelin and triptorelin, stimulate the pituitary's gonadotrophin-releasing hormone (GnRH) receptor, ultimately leading to its de-sensitization and subsequent reduction of LH and testosterone levels.", "entity1": "LH", "entity2": "triptorelin", "span1": [260, 262], "span2": [101, 112]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11035": {"label": 1, "data": {"text": "In vivo angiogenesis assay utilising gelfoam sponges, bexarotene reduced angiogenesis in sponges containing vascular endothelial growth factor, epidermal growth factor and basic fibroblast growth factor to various extent.", "entity1": "fibroblast growth factor", "entity2": "bexarotene", "span1": [178, 202], "span2": [54, 64]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7247": {"label": 1, "data": {"text": "Recently, it was reported that METH, AMPH, POHA, and the TAs para-tyramine (TYR) and beta-phenylethylamine (PEA) stimulate cAMP production in human embryonic kidney (HEK)-293 cells expressing rat trace amine-associated receptor 1 (rTAAR1).", "entity1": "rTAAR1", "entity2": "beta-phenylethylamine", "span1": [231, 237], "span2": [85, 106]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"9571": {"label": 3, "data": {"text": "Concanavalin A (Con A)-induced IFN-gamma, GM-CSF, and IL-3 mRNAs are dose-dependently inhibited by the nonselective betaAR agonist isoproterenol and by the selective beta2AR agonist fenoterol.", "entity1": "GM-CSF", "entity2": "fenoterol", "span1": [42, 48], "span2": [182, 191]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"15819": {"label": 0, "data": {"text": "In the present report, we show that Fer associates with the activated PDGFbeta receptor (PDGFRbeta) through multiple autophosphorylation sites, i.e. Tyr579, Tyr581, Tyr740 and Tyr1021.", "entity1": "PDGFbeta receptor", "entity2": "Tyr", "span1": [70, 87], "span2": [176, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2014": {"label": 3, "data": {"text": "RESULTS: Pretreatment of lung tissues with pranlukast alone significantly decreased the amount of IL-5 protein in the culture medium by 40%.", "entity1": "IL-5", "entity2": "pranlukast", "span1": [98, 102], "span2": [43, 53]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"998": {"label": 8, "data": {"text": "Fumarate reductase (FRD) is the key enzyme in fumarate respiration induced by anaerobic growth of bacteria.", "entity1": "Fumarate reductase", "entity2": "fumarate", "span1": [0, 18], "span2": [46, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14804": {"label": 3, "data": {"text": "Furthermore, TSA also decreased cellular ROS and H(2)O(2) accumulation induced by TGF-\u03b2, whereas it elevated intracellular GSH level and cellular total antioxidant capacity.", "entity1": "TGF-\u03b2", "entity2": "TSA", "span1": [82, 87], "span2": [13, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3753": {"label": 3, "data": {"text": "The pretreatment with 20\u00a0mg\u2009L(-1) La(III) could alleviate the effects of UV-B radiation on the activities of nitrate reductase, glutamine synthetase, glutamate synthase, and glutamate dehydrogenase, promoting amino acid conversion and protein synthesis in soybean seedlings.", "entity1": "glutamate synthase", "entity2": "La(III)", "span1": [150, 168], "span2": [34, 41]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"6810": {"label": 2, "data": {"text": "Based on HMG-CoA reductase inhibition, pitavastatin-induced apoA-I more efficiently than simvastatin and atorvastatin.", "entity1": "apoA-I", "entity2": "simvastatin", "span1": [60, 66], "span2": [89, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10227": {"label": 3, "data": {"text": "Thalidomide prevents alcoholic liver injury in rats through suppression of Kupffer cell sensitization and TNF-alpha production.", "entity1": "TNF-alpha", "entity2": "Thalidomide", "span1": [106, 115], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7649": {"label": 5, "data": {"text": "When Panx1 was coexpressed with purinergic P2X(7) receptor (P2X(7)R), DIDS was found to act as a P2X(7)R antagonist to inhibit ATP-evoked currents, but none of the other compounds inhibited P2X(7)R currents.", "entity1": "P2X(7)R", "entity2": "DIDS", "span1": [97, 104], "span2": [70, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5571": {"label": 8, "data": {"text": "Dimethylarginine dimethylaminohydrolase 1 (DDAH1) is an enzyme that metabolizes methylated arginine to citrulline and methylamine, thus working to produce nitric oxide (NO).", "entity1": "DDAH1", "entity2": "methylamine", "span1": [43, 48], "span2": [118, 129]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3017": {"label": 1, "data": {"text": "Computational modeling showed the direct interaction of the carboxylic acid moiety of statins with the catalytic site of HDAC2.", "entity1": "HDAC2", "entity2": "carboxylic acid", "span1": [121, 126], "span2": [60, 75]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14839": {"label": 1, "data": {"text": "Fluorescence lifetime analysis and effect of magnesium ions on binding of NADH to human aldehyde dehydrogenase 1.", "entity1": "human aldehyde dehydrogenase 1", "entity2": "NADH", "span1": [82, 112], "span2": [74, 78]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7575": {"label": 4, "data": {"text": "Administration of cevimeline hydrochloride, an M3 muscarinic receptor agonist (10 mg/kg for 7 days po), but not pilocarpine (0.3 mg/kg for 7 days po), recovered the AQP5 protein level reduced by CTD and increased the AQP1 protein level above the control one.", "entity1": "M3 muscarinic receptor", "entity2": "cevimeline hydrochloride", "span1": [47, 69], "span2": [18, 42]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"11748": {"label": 0, "data": {"text": "We therefore propose that this proline residue might be involved in the stability and activity of Ves a 1s.", "entity1": "Ves a 1s", "entity2": "proline", "span1": [98, 106], "span2": [31, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2706": {"label": 3, "data": {"text": "Sitagliptin, an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, improves glycaemic control by inhibiting DPP-4 inactivation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide.", "entity1": "DPP-4", "entity2": "Sitagliptin", "span1": [45, 50], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2740": {"label": 3, "data": {"text": "Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL.", "entity1": "SRC", "entity2": "dasatinib", "span1": [134, 137], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6392": {"label": 4, "data": {"text": "In alpha(2A)-adrenoceptor transfected cells the rank order of agonist potency was A-54741 (mean pEC(50)=8.96)>dexmedetomidine (8.88)>UK-14304 (8.42)>B-HT 920 (7.05)>noradrenaline (6.92).", "entity1": "alpha(2A)-adrenoceptor", "entity2": "UK-14304", "span1": [3, 25], "span2": [133, 141]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 4, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1477": {"label": 3, "data": {"text": "However, AII receptor blockers differ from ACE inhibitors with respect to side effects, and induce less cough, a side effect which may be related to bradykinin or other mediators such as substance P. Within the class of AII blockers, eprosartan differs from other currently available agents in terms of chemical structure, as it is a non-biphenyl, non-tetrazole, non-peptide antagonist with a dual pharmacological mode of action.", "entity1": "AII", "entity2": "eprosartan", "span1": [220, 223], "span2": [234, 244]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3357": {"label": 1, "data": {"text": "The structural and functional data reveal that the levosimendan class of Ca(2+)-sensitizers work by binding to the regulatory domain of cTnC and stabilizing the pivotal cTnC-cTnI regulatory unit via a network of hydrophobic and electrostatic interactions, in contrast to the destabilizing effects of antagonists such as W7 at the same interface.", "entity1": "cTnI", "entity2": "levosimendan", "span1": [174, 178], "span2": [51, 63]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12545": {"label": 1, "data": {"text": "The compound is more beta-lactamase stable than ampicillin and has no major delay in entry into the periplasmic space as do some penicillins.", "entity1": "beta-lactamase", "entity2": "ampicillin", "span1": [21, 35], "span2": [48, 58]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7174": {"label": 8, "data": {"text": "Upon differentiation, osteoclasts express vesicular glutamate transporter 1 (VGLUT1), which is essential for vesicular storage and subsequent exocytosis of glutamate in neurons.", "entity1": "vesicular glutamate transporter 1", "entity2": "glutamate", "span1": [42, 75], "span2": [156, 165]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"7407": {"label": 8, "data": {"text": "Bile acid coenzyme A:amino acid N-acyltransferase (BAT) is responsible for the amidation of bile acids with the amino acids glycine and taurine.", "entity1": "BAT", "entity2": "bile acids", "span1": [51, 54], "span2": [92, 102]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12824": {"label": 8, "data": {"text": "In the present study, age-related changes of pyridoxal 5'-phosphate (PLP) synthesizing enzymes, pyridoxal kinase (PLK) and pyridoxine 5'-phosphate oxidase (PNPO), their protein contents and activities were examined in the gerbil hippocampus proper.", "entity1": "pyridoxine 5'-phosphate oxidase", "entity2": "pyridoxal 5'-phosphate", "span1": [123, 154], "span2": [45, 67]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4852": {"label": 3, "data": {"text": "Here we found that the anticancer agent cucurbitacin I, a Jak2 inhibitor, reduced the activation of Rac1 and motility in response to the ErbB3 ligand heregulin in breast cancer cells.", "entity1": "Jak2", "entity2": "cucurbitacin I", "span1": [58, 62], "span2": [40, 54]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9624": {"label": 1, "data": {"text": "Here, we report that MgATP and MgADP, but not the Mg salt of gamma-thio-ATP, stabilize the binding of prebound 8-azido-[alpha-32P]ATP to SUR1.", "entity1": "SUR1", "entity2": "MgATP", "span1": [137, 141], "span2": [21, 26]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"4899": {"label": 3, "data": {"text": "4-{[(4-Cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenyl sulfamate and its ortho-halogenated (F, Cl, Br) derivatives are first-generation dual aromatase and sulfatase inhibitors (DASIs).", "entity1": "aromatase", "entity2": "Br", "span1": [148, 157], "span2": [106, 108]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7544": {"label": 3, "data": {"text": "Phenelzine causes an increase in brain ornithine that is prevented by prior monoamine oxidase inhibition.", "entity1": "monoamine oxidase", "entity2": "Phenelzine", "span1": [76, 93], "span2": [0, 10]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14301": {"label": 0, "data": {"text": "Amino acid residues at the N- and C-termini are essential for the folding of active human butyrylcholinesterase polypeptide.", "entity1": "human butyrylcholinesterase", "entity2": "Amino acid", "span1": [84, 111], "span2": [0, 10]}, "weak_labels": [0, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5777": {"label": 9, "data": {"text": "This binding was not significantly inhibited by the lysine analogue epsilon-amino caproic acid (EACA), indicating that plasminogen binding was not just through lysine binding sites as suggested for other plasminogen binding sites.", "entity1": "plasminogen", "entity2": "lysine", "span1": [119, 130], "span2": [160, 166]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"7038": {"label": 8, "data": {"text": "The tissue RA level is maintained through a cascade of metabolic reactions where retinal dehydrogenases (RALDHs) catalyze the terminal reaction of RA biosynthesis from retinal, a rate-limiting step.", "entity1": "retinal dehydrogenases", "entity2": "retinal", "span1": [81, 103], "span2": [168, 175]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"14384": {"label": 3, "data": {"text": "Furthermore, the EGFR inhibitor AG1478 inhibited EGF-induced MMP-9 expression, cell migration and invasion, as well as the activation of PI3K/Akt, suggesting that PI3K/Akt activation occur downstream of EGFR activation.", "entity1": "EGF", "entity2": "AG1478", "span1": [49, 52], "span2": [32, 38]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3233": {"label": 3, "data": {"text": "A series of phenolic acids and phenol natural products, such as p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, ferulic acid, gallic acid, syringic acid, quercetin, and ellagic acid, were investigated for their inhibitory effects against the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1).", "entity1": "EC 4.2.1.1", "entity2": "phenol", "span1": [286, 296], "span2": [31, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3875": {"label": 2, "data": {"text": "Transduction with constitutively active forms of GSK-3\u03b2 could protect against the downregulation of p65 and upregulation of cleaved-PARP that are induced by cinobufagin treatment.", "entity1": "PARP", "entity2": "cinobufagin", "span1": [132, 136], "span2": [157, 168]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, 2, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7580": {"label": 3, "data": {"text": "threo-methylphenidate inhibits the dopamine transporter and the norepinephrine transporter, resulting in elevations of these monoamines after impulse release.", "entity1": "dopamine transporter", "entity2": "threo-methylphenidate", "span1": [35, 55], "span2": [0, 21]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"6347": {"label": 5, "data": {"text": "Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280.", "entity1": "AT1", "entity2": "tasosartan", "span1": [18, 21], "span2": [198, 208]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9559": {"label": 2, "data": {"text": "The observed inhibition on IFN-gamma, GM-CSF, and IL-3 mRNA was blocked by the selective beta2AR antagonist ICI 118,551 (10(-6) M) and by timolol (10(-6) M), a nonselective antagonist.", "entity1": "IFN-gamma", "entity2": "ICI 118,551", "span1": [27, 36], "span2": [108, 119]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"714": {"label": 3, "data": {"text": "The stimulatory effect of [Ca(2+)](i) induced by a submaximal concentration of Ang II (10(-7) mol/L) was blocked by torasemide (IC(50)=0.5+/-0.3 nmol/L).", "entity1": "Ang II", "entity2": "torasemide", "span1": [79, 85], "span2": [116, 126]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1257": {"label": 3, "data": {"text": "The selective PDE 4 inhibitors, and to a certain extent the PDE3 inhibitors amrinone and milrinone, reduced the GM-CSF release in a concentration dependent manner.", "entity1": "PDE 4", "entity2": "amrinone", "span1": [14, 19], "span2": [76, 84]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8854": {"label": 2, "data": {"text": "Activation of STAT3, which is phosphorylated by the IL-6 signaling pathways and thus is necessary for Th17 differentiation, was strongly stimulated by I3S and TCDD.", "entity1": "STAT3", "entity2": "TCDD", "span1": [14, 19], "span2": [159, 163]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5222": {"label": 2, "data": {"text": "Also, vinblastine enhances the phosphorylation of Ras homologous protein A, the accumulation of reactive oxygen species, the release of intracellular Ca(2+), as well as the activation of apoptosis signal-regulating kinase 1, c-jun-N-terminal kinase, p38, inhibitor of kappaB\u03b1 (I\u03baB\u03b1) kinase, and inositol requiring enzyme 1\u03b1.", "entity1": "p38", "entity2": "vinblastine", "span1": [250, 253], "span2": [6, 17]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2173": {"label": 1, "data": {"text": "Drug binding interactions in the inner cavity of HERG channels: molecular insights from structure-activity relationships of clofilium and ibutilide analogs.", "entity1": "HERG", "entity2": "ibutilide", "span1": [49, 53], "span2": [138, 147]}, "weak_labels": [-1, -1, -1, 1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13866": {"label": 3, "data": {"text": "Mitiglinide reduced fasting plasma glucose and GA levels after 4 weeks and Hb(A1c) levels after 8 weeks.", "entity1": "Hb(A1c)", "entity2": "Mitiglinide", "span1": [75, 82], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11919": {"label": 1, "data": {"text": "We studied accumulation of lipid metabolites [triglycerides (TAGs), diglycerides (DAGs)] and ceramides in relation to insulin signaling and expression and phosphorylation of PTP1B by preincubating rat skeletal muscle cells (L6 myotubes) with three saturated and three unsaturated free fatty acids (FFAs) (200 \u03bcM).", "entity1": "insulin", "entity2": "ceramides", "span1": [118, 125], "span2": [93, 102]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13578": {"label": 1, "data": {"text": "Exposure of Jurkat cells to either (5S,10R)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,b]cyclohepten-5,10-imine [(+)-MK 801] or D-(-)-2-amino-5-phosphonopentanoic acid (D-AP5), two selective NMDA receptor antagonists, limited cell growth by inhibiting cell cycle progression and inducing apoptosis, whereas l-glutamate (1 microM) and NMDA (10 microM) significantly increased (137.2+/-22.0%; P<0.01) Jurkat T cell adhesion to fibronectin.", "entity1": "fibronectin", "entity2": "NMDA", "span1": [422, 433], "span2": [331, 335]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, 3, -1, -1, 5, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"6764": {"label": 2, "data": {"text": "Novel mechanism of action for hydralazine: induction of hypoxia-inducible factor-1alpha, vascular endothelial growth factor, and angiogenesis by inhibition of prolyl hydroxylases.", "entity1": "vascular endothelial growth factor", "entity2": "hydralazine", "span1": [89, 123], "span2": [30, 41]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5782": {"label": 3, "data": {"text": "Inhibition of binding of both plasminogen and plasmin to gp330 by benzamidine was similar, although EACA inhibited the binding of plasmin to gp330 slightly more than the binding of plasminogen to gp330.", "entity1": "plasmin", "entity2": "benzamidine", "span1": [46, 53], "span2": [66, 77]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"654": {"label": 3, "data": {"text": "We have examined the effects of the synthetic matrix metalloproteinase inhibitor, batimastat (BB-94) and the angiotensin-converting enzyme inhibitor, captopril, on metalloproteinase activity of murine Lewis-lung-carcinoma cells (3LL) in vitro, and on local growth and lung metastasis of the same tumor implanted intramuscularly in syngeneic C57BL/6 mice.", "entity1": "matrix metalloproteinase", "entity2": "BB-94", "span1": [46, 70], "span2": [94, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1]},
	"14440": {"label": 2, "data": {"text": "Fungicide prochloraz and environmental pollutant dioxin induce the ABCG2 transporter in bovine mammary epithelial cells by the arylhydrocarbon receptor signaling pathway.", "entity1": "ABCG2", "entity2": "prochloraz", "span1": [67, 72], "span2": [10, 20]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"5448": {"label": 3, "data": {"text": "Moreover, we found that juglone significantly inhibited the expression levels of androgen receptor (AR) and prostate-specific antigen (PSA) in a dose-dependent manner, as well as abrogated up-regulation of AR and PSA genes with and/or without dihydrotestosterone (DHT).", "entity1": "prostate-specific antigen", "entity2": "juglone", "span1": [108, 133], "span2": [24, 31]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2228": {"label": 1, "data": {"text": "Computer modeling suggests that the KITD816V mutation destabilizes the inactive conformation of the KIT activation loop to which imatinib binds, but it is not predicted to impair binding of KIT by dasatinib.", "entity1": "KIT activation loop", "entity2": "imatinib", "span1": [100, 119], "span2": [129, 137]}, "weak_labels": [-1, -1, 0, 1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"3121": {"label": 8, "data": {"text": "alpha-Tocopherol transfer protein (alpha-TTP), the product of the gene responsible for familial isolated vitamin E deficiency, plays an important role in maintaining the plasma alpha-tocopherol level by mediating the secretion of alpha-tocopherol by the liver.", "entity1": "alpha-TTP", "entity2": "alpha-tocopherol", "span1": [35, 44], "span2": [177, 193]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"11024": {"label": 3, "data": {"text": "Comparison of captopril and enalapril to study the role of the sulfhydryl-group in improvement of endothelial dysfunction with ACE inhibitors in high dieted methionine mice.", "entity1": "ACE", "entity2": "sulfhydryl", "span1": [127, 130], "span2": [63, 73]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"903": {"label": 7, "data": {"text": "They are compatible with a novel, non-classical, redox-active contribution of H(4)biopterin to the catalysis of the nitric oxide synthase reaction.", "entity1": "nitric oxide synthase", "entity2": "H(4)biopterin", "span1": [116, 137], "span2": [78, 91]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"8222": {"label": 1, "data": {"text": "With the exception of three residues, the specific amino acids that form the putative binding pocket for ICA in ERG are conserved in EAG.", "entity1": "EAG", "entity2": "ICA", "span1": [133, 136], "span2": [105, 108]}, "weak_labels": [0, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3678": {"label": 3, "data": {"text": "Artemisinic acid inhibits melanogenesis through downregulation of C/EBP \u03b1-dependent expression of HMG-CoA reductase gene.", "entity1": "C/EBP \u03b1", "entity2": "Artemisinic acid", "span1": [66, 73], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"14362": {"label": 3, "data": {"text": "The quinolizidine alkaloids (natural products) such as oxymatrine, sophoridine, sophocarpine and matrine carry the common molecular structure of O=C=N-C-C-C-N that possessed positive ionotropic effect and hERG blocking activity.", "entity1": "hERG", "entity2": "O=C=N-C-C-C-N", "span1": [205, 209], "span2": [145, 158]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, 9]},
	"2070": {"label": 3, "data": {"text": "Apolipoprotein E3 (apoE3) safeguards pig proximal tubular LLC-PK1 cells against reduction in SGLT1 activity induced by gentamicin C.", "entity1": "SGLT1", "entity2": "gentamicin C", "span1": [93, 98], "span2": [119, 131]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"878": {"label": 5, "data": {"text": "In addition, by comparing the combined administration of (+/-)pindolol with either WAY100635, GR127935 or isamoltane, we have determined that (+/-)pindolol produces much of its acute potentiation of fluoxetine-induced increases in extracellular 5-HT via its action at the 5-HT(1B/D) receptor in addition to any activity it has at the presynaptic 5-HT(1A) receptor.", "entity1": "5-HT(1A)", "entity2": "(+/-)pindolol", "span1": [346, 354], "span2": [142, 155]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"4374": {"label": 2, "data": {"text": "We investigated the effects of the dose of and the number of times an inducer was administered and the duration of induction of hepatic and intestinal cytochrome P450 3A (CYP3A) in rats using dexamethasone 21-phosphate (DEX-P) and midazolam (MDZ) as an inducer and a substrate to CYP3A, respectively.", "entity1": "CYP3A", "entity2": "MDZ", "span1": [280, 285], "span2": [242, 245]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"11323": {"label": 1, "data": {"text": "METHODS: Sedative and cardiovascular responses to etomidate and the alpha2-agonist, dexmedetomidine, were determined in mice deficient in alpha2-receptor subtypes.", "entity1": "alpha2-receptor", "entity2": "etomidate", "span1": [138, 153], "span2": [50, 59]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12419": {"label": 0, "data": {"text": "Moreover, limited cleavage of SNAP-25 was conferred onto the protease from BoNT/E when fused to the N-terminus of BoNT/A.", "entity1": "BoNT/A", "entity2": "N", "span1": [114, 120], "span2": [100, 101]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13840": {"label": 8, "data": {"text": "Mammalian glutamate dehydrogenase (GDH) is a homohexameric enzyme that catalyzes the reversible oxidative deamination of l-glutamate to 2-oxoglutarate using NAD(P)(+) as coenzyme.", "entity1": "GDH", "entity2": "l-glutamate", "span1": [35, 38], "span2": [121, 132]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1]},
	"145": {"label": 1, "data": {"text": "These data demonstrate that loperamide differently modifies the stimulatory action of LVP and CRH on ACTH secretion: namely, LVP and loperamide act in an additive manner, while CRH and loperamide interact in a non additive way.", "entity1": "LVP", "entity2": "loperamide", "span1": [86, 89], "span2": [28, 38]}, "weak_labels": [-1, -1, -1, -1, 1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3437": {"label": 2, "data": {"text": "Epi increased both WNT6/Wnt6 and Cav1 expression in human GC cells and within the tumor area of a murine model of GC (CEA424-SV40 TAg).", "entity1": "Cav1", "entity2": "Epi", "span1": [33, 37], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13528": {"label": 1, "data": {"text": "Moreover, the CDO active site is essentially unreactive toward NO in the absence of substrate, suggesting an obligate ordered binding of l-cysteine prior to NO.", "entity1": "CDO", "entity2": "l-cysteine", "span1": [14, 17], "span2": [137, 147]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"8112": {"label": 3, "data": {"text": "The mechanism revealed that wogonin inhibited H2O2-induced phosphorylation of caveolin-1 (cav-1) associating with the suppression of stabilization of VE-cadherin and \u03b2-catenin.", "entity1": "caveolin-1", "entity2": "wogonin", "span1": [78, 88], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11370": {"label": 1, "data": {"text": "PKC-delta in particular showed a different pattern of translocation in response to I3A and PMA.", "entity1": "PKC-delta", "entity2": "I3A", "span1": [0, 9], "span2": [83, 86]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1880": {"label": 1, "data": {"text": "Monodemethylated mifepristone bound to rabbit thymic GR with higher affinity than monodemethylated CDB-2914 or CDB-4124.", "entity1": "rabbit thymic GR", "entity2": "CDB-4124", "span1": [39, 55], "span2": [111, 119]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2135": {"label": 9, "data": {"text": "The effect of troglitazone on ENT1 was PPAR(gamma)-independent and kinetic studies revealed that troglitazone was a competitive inhibitor of ENT1.", "entity1": "PPAR(gamma)", "entity2": "troglitazone", "span1": [39, 50], "span2": [14, 26]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10753": {"label": 3, "data": {"text": "These findings suggest that the mechanism of antiproliferative toxicity of capecitabine is at least partly due to TS inhibitory activity of its active metabolite 5-fluoro-2'-deoxyuridine monophosphate (FdUMP).", "entity1": "TS", "entity2": "capecitabine", "span1": [114, 116], "span2": [75, 87]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"11455": {"label": 1, "data": {"text": "A previous crystal structure of a microcystin bound to the catalytic subunit of protein phosphatase-1 (PP-1c) showed distinct changes in the active site region when compared with protein phosphatase-1 structures bound to other toxins.", "entity1": "PP-1c", "entity2": "microcystin", "span1": [103, 108], "span2": [34, 45]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"13412": {"label": 9, "data": {"text": "The mRNA expression of PtdSer synthase 1 (PSS1) and PtdSer synthase 2 (PSS2) was not reduced by ethanol.", "entity1": "PtdSer synthase 1", "entity2": "ethanol", "span1": [23, 40], "span2": [96, 103]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"5735": {"label": 1, "data": {"text": "Taken together, our results suggested that Rg1 protected against A\u03b225-35-induced apoptosis at least in part by two complementary GR-dependent ERK phosphorylation pathways: (1) down-regulating HIF-1\u03b1 initiated protein nitrotyrosination, and (2) inhibiting mitochondrial apoptotic cascades.", "entity1": "GR", "entity2": "Rg1", "span1": [129, 131], "span2": [43, 46]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, 3, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"4281": {"label": 3, "data": {"text": "Interestingly, ursolic acid increased the phosphorylation of AMPK and coenzyme A carboxylase and also enhanced phosphorylation of GSK3\u03b2 at inactive form serine 9, whereas ursolic acid attenuated the phosphorylation of AKT and mTOR in HepG2 cells.", "entity1": "AKT", "entity2": "ursolic acid", "span1": [218, 221], "span2": [171, 183]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3676": {"label": 3, "data": {"text": "Furthermore, cAMP production and protein kinase A (PKA) activity were suppressed by artemisinic acid.", "entity1": "protein kinase A", "entity2": "artemisinic acid", "span1": [33, 49], "span2": [84, 100]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"2091": {"label": 3, "data": {"text": "The purpose of the present study was to test our hypothesis that amiloride, a specific u-PA inhibitor, effectively decreases u-PA activity in cornea as well as in tear fluid and favourably affects corneal healing.", "entity1": "u-PA", "entity2": "amiloride", "span1": [87, 91], "span2": [65, 74]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8716": {"label": 3, "data": {"text": "The mRNA levels of SOD1, CAT, GPx and Txnrd1 were increased significantly (P<0.05) in the combined Na2SeO3+NaAsO2 treatment group.", "entity1": "SOD1", "entity2": "NaAsO2", "span1": [19, 23], "span2": [107, 113]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"7711": {"label": 1, "data": {"text": "(18)F-AV-45 displayed excellent binding affinity to Abeta plaques in the AD brain by ex vivo autoradiography in transgenic AD model mice.", "entity1": "Abeta", "entity2": "(18)F-AV-45", "span1": [52, 57], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, 1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"2761": {"label": 3, "data": {"text": "Interestingly, a Val-349 to Ile mutant was inhibited with equal potency to human COX-2 with 2,6-dichloro-, 2,6-dimethyl-, or 2-chloro-6-methyl-substituted inhibitors and, in the case of lumiracoxib, actually showed an increase in potency.", "entity1": "Val-349 to Ile", "entity2": "lumiracoxib", "span1": [17, 31], "span2": [186, 197]}, "weak_labels": [-1, -1, 0, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12027": {"label": 1, "data": {"text": "Mechanism of iodide-dependent catalatic activity of thyroid peroxidase and lactoperoxidase.", "entity1": "thyroid peroxidase", "entity2": "iodide", "span1": [52, 70], "span2": [13, 19]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1586": {"label": 3, "data": {"text": "The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of a series of pyrano[2,3-b]quinolines (2, 3), [1,8]naphthyridines (5, 6), 4-amino-2,3-diaryl-5,6,7,8-tetrahydrofuro[2,3-b]quinolines (11-13)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine (14), 4-amino-5,6,7,8-tetrahydro-2,3-diphenylthieno[2,3-b]quinoline (15)/ 4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]thieno[2,3-b]pyridine (16) are described.", "entity1": "BuChE", "entity2": "4-amino-6,7,8,9-tetrahydro-2,3-diphenyl-5H-cyclohepta[e]furo[2,3-b]pyridine", "span1": [59, 64], "span2": [231, 306]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3694": {"label": 3, "data": {"text": "8-pCPT-2'-O-Me-cAMP-AM potentiation of insulin secretion stimulated by tolbutamide was markedly inhibited by 2-APB (25 \u03bcM) and enhanced by the PKC inhibitor bisindolylmaleimide I (1 \u03bcM).", "entity1": "insulin", "entity2": "2-APB", "span1": [39, 46], "span2": [109, 114]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1971": {"label": 9, "data": {"text": "SNP inhibits the accumulation of HIF-1alpha, the regulatory subunit of HIF-1, and the transcriptional activation of HIF-1alpha via a mechanism that is not dependent on either NO or soluble guanylate cyclase.", "entity1": "soluble guanylate cyclase", "entity2": "SNP", "span1": [181, 206], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"12213": {"label": 1, "data": {"text": "This mechanism involves the calcium-dependent tyrosine kinase Pyk2, the non-receptor tyrosine kinase c-Src and the focal adhesion protein/steroid receptor co-factor, Hic-5.", "entity1": "Hic-5", "entity2": "calcium", "span1": [166, 171], "span2": [28, 35]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"9315": {"label": 3, "data": {"text": "The goal of the present study was to compare the effects of three potent reference renin inhibitors (remikiren, CGP 38560A, and enalkiren) in sodium-depleted normotensive squirrel monkeys.", "entity1": "renin", "entity2": "CGP 38560A", "span1": [83, 88], "span2": [112, 122]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3989": {"label": 3, "data": {"text": "Beta-glucogallin reduces the expression of lipopolysaccharide-induced inflammatory markers by inhibition of aldose reductase in murine macrophages and ocular tissues.", "entity1": "aldose reductase", "entity2": "Beta-glucogallin", "span1": [108, 124], "span2": [0, 16]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"1389": {"label": 3, "data": {"text": "Similar to gemfibrozil, clofibrate, another fibrate drug, also inhibited the expression of iNOS.", "entity1": "iNOS", "entity2": "gemfibrozil", "span1": [91, 95], "span2": [11, 22]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"2421": {"label": 8, "data": {"text": "Reduced synthesis of nitric oxide (NO) contributes to the endothelial dysfunction and may be related to limited availability of L-arginine, the common substrate of constitutive nitric-oxide synthase (NOS) and cytosolic arginase I and mitochondrial arginase II.", "entity1": "NOS", "entity2": "NO", "span1": [200, 203], "span2": [35, 37]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1, -1]},
	"6692": {"label": 2, "data": {"text": "TRPM8 (CMR1) is a Ca(2+)-permeable channel, which can be activated by low temperatures, menthol, eucalyptol and icilin.", "entity1": "CMR1", "entity2": "icilin", "span1": [7, 11], "span2": [112, 118]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8189": {"label": 3, "data": {"text": "In addition, we showed that c-Myc directly binds to and represses the promoter of miR-200 miRNAs, and its up-regulation in TAM-treated endometrial cancer cells leads to the down-regulation of miR-200 and eventually to EMT.", "entity1": "miR-200", "entity2": "TAM", "span1": [192, 199], "span2": [123, 126]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"8089": {"label": 2, "data": {"text": "E235 also activated DNA damage response signaling, resulting in increased levels of Ser15-phosphorylated p53, \u03b3-H2AX, and phosphorylated checkpoint kinase 2 (Chk2), although E235 does not appear to cause physical DNA damage.", "entity1": "phosphorylated checkpoint kinase 2", "entity2": "E235", "span1": [122, 156], "span2": [0, 4]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 9]},
	"14489": {"label": 8, "data": {"text": "The catalytic competence of cytochrome P450 in the synthesis of serotonin from 5-methoxytryptamine in the brain: an in vitro study.", "entity1": "cytochrome P450", "entity2": "5-methoxytryptamine", "span1": [28, 43], "span2": [79, 98]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10368": {"label": 3, "data": {"text": "GW660511X and omapatrilat reduced the production of BrBK1-5 and BrBK1-7 with more effect being observed with omapatrilat.", "entity1": "BrBK1-5", "entity2": "omapatrilat", "span1": [52, 59], "span2": [109, 120]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"14903": {"label": 8, "data": {"text": "We demonstrate that two flavin mono-oxygenase family members, FMO1 and FMO3, oxidize trimethylamine (TMA), derived from gut flora metabolism of choline, to TMAO.", "entity1": "FMO1", "entity2": "trimethylamine", "span1": [62, 66], "span2": [85, 99]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12268": {"label": 9, "data": {"text": "Likewise, no fatty acids bound to holo-alpha-lactalbumin, isolated using nondenaturing conditions, were detected by gas chromatography.", "entity1": "holo-alpha-lactalbumin", "entity2": "fatty acids", "span1": [34, 56], "span2": [13, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"15888": {"label": 8, "data": {"text": "Targeted disruption of the gene encoding the N-glycosyltransferase, prlH, abolished pyralomicin production, and recombinant expression of PrlA confirms the activity of this enzyme as a sugar phosphate cyclase involved in the formation of the C7-cyclitol moiety.", "entity1": "prlH", "entity2": "pyralomicin", "span1": [68, 72], "span2": [84, 95]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"3893": {"label": 3, "data": {"text": "A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore.", "entity1": "Myc", "entity2": "10074-G5", "span1": [60, 63], "span2": [75, 83]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10797": {"label": 3, "data": {"text": "Simvastatin, an HMG-CoA reductase inhibitor with mild inhibition of LFA-1, induced the production of interleukin (IL)-18, tumor necrosis factor (TNF)-alpha and interferon (IFN)-gamma in human peripheral blood mononuclear cells (PBMC).", "entity1": "HMG-CoA reductase", "entity2": "Simvastatin", "span1": [16, 33], "span2": [0, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, 3, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1]},
	"7056": {"label": 9, "data": {"text": "Among them, tamibarotene (Am80) is an RARalpha- and RARbeta-specific (but RARgamma- and RXRs-nonbinding) synthetic retinoid that is effective in the treatment of psoriasis patients and relapsed APL.", "entity1": "RARgamma", "entity2": "Am80", "span1": [74, 82], "span2": [26, 30]}, "weak_labels": [-1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"3132": {"label": 1, "data": {"text": "The neuronal vesicular monoamine transporter (VMAT2) is the target molecule of action of some psychostimulants, such as methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA).", "entity1": "VMAT2", "entity2": "MDMA", "span1": [46, 51], "span2": [175, 179]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"8135": {"label": 3, "data": {"text": "Sal toxicity coincided with reduced pAkt level and its downstream effectors: pCREB, pGSK-3\u03b2, Bcl-2 and neurotrophins GDNF, BDNF suggesting repressed PI3K/Akt signaling.", "entity1": "Akt", "entity2": "Sal", "span1": [154, 157], "span2": [0, 3]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"5711": {"label": 3, "data": {"text": "Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17\u03b2-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.", "entity1": "prostaglandin F synthase", "entity2": "indomethacin", "span1": [129, 153], "span2": [36, 48]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"218": {"label": 2, "data": {"text": "In HEK-293 cells stably transfected with this receptor, serotonin elicits a potent stimulation of adenylyl cyclase activity, which is blocked by antipsychotic and antidepressant drugs.", "entity1": "adenylyl cyclase", "entity2": "serotonin", "span1": [98, 114], "span2": [56, 65]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"117": {"label": 1, "data": {"text": "Finally, the effects of felodipine and the three analogues on two processes which are dependent on myosin phosphorylation were examined, namely the actin-activated Mg2+-ATPase activity of myosin and the assembly of myosin filaments.", "entity1": "myosin", "entity2": "felodipine", "span1": [215, 221], "span2": [24, 34]}, "weak_labels": [-1, -1, -1, -1, -1, -1, 2, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12756": {"label": 2, "data": {"text": "The ratio of TGF-beta1 absorbed light value to GAPDH absorbed light value in the SHR group was 0.887+/-0.019, which was significantly higher than that in WKY group, imidapril group, and irbesartan group with the ratios of 0.780+/-0.018, 0.803+/-0.005, and 0.847+/-0.017, respectively (P<0.01).", "entity1": "GAPDH", "entity2": "imidapril", "span1": [47, 52], "span2": [165, 174]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"12069": {"label": 0, "data": {"text": "This lysine is contained in the sequence PFYAVKC, which is found in all known ODCs from eukaryotes.", "entity1": "ODCs", "entity2": "lysine", "span1": [78, 82], "span2": [5, 11]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]},
	"10999": {"label": 8, "data": {"text": "The functional characteristics of rabbit PAT1 in either mammalian cells or renal BBMV suggest that PAT1 is the low-affinity transporter of proline, glycine and hydroxyproline believed to be defective in patients with iminoglycinuria.", "entity1": "PAT1", "entity2": "hydroxyproline", "span1": [99, 103], "span2": [160, 174]}, "weak_labels": [-1, -1, -1, -1, -1, 1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 8, -1, -1, -1, -1]},
	"4351": {"label": 3, "data": {"text": "Subsequently, pinosylvin suppressed the nuclear translocation of \u03b2-catenin, one of downstream molecules of PI3K/Akt/GSK-3\u03b2 signaling, and these events led to the sequential downregulation of \u03b2-catenin-mediated transcription of target genes including BMP4, ID2, survivin, cyclin D1, MMP7, and c-Myc.", "entity1": "ID2", "entity2": "pinosylvin", "span1": [256, 259], "span2": [14, 24]}, "weak_labels": [-1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, 3, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1, -1]}
}