General Information of Drug-Metabolizing Enzyme (DME ID: DME0011)
DME Name Glutathione S-transferase alpha-1 (GSTA1), Homo sapiens DME Info
UniProt ID
GSTA1_HUMAN
EC Number    EC: 2.5.1.18     (Click to Show/Hide the Complete EC Tree)
Transferase
Alkyl/aryl transferase
Alkyl/aryl transferase
EC: 2.5.1.18
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Interactome
Interactions between Xenobiotics and DME (XEOTIC)
      Fungicide(s), Herbicide(s) or Insecticide(s)
                  Pesticide/Insecticide Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Dicrotophos Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01050   XEOTIC Info Gene Form mRNA
                                 Classification Pesticide/Insecticide
                                 DME Modulation Dicrotophos inhibits the expression of DME GSTA1 [1]
      Health or Environmental Toxicant(s)
                  Acute Toxic Substance Click to Show/Hide the Full List of Xenobiotics:        6 Xenobiotics
                              2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01119   XEOTIC Info Gene Form mRNA
                                 Classification Acute Toxic Substance
                                 DME Modulation 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine inhibits the expression of DME GSTA1 [2]
                              3-methylpyridine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01140   XEOTIC Info Gene Form Protein
                                 Classification Acute Toxic Substance
                                 DME Modulation 3-methylpyridine inhibits the drug-metabolizing activity of DME GSTA1 [3]
                              Chlorpyrifos Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01248   XEOTIC Info Gene Form Protein
                                 Classification Acute Toxic Substance
                                 DME Modulation Chlorpyrifos induces the drug-metabolizing activity of DME GSTA1 [4]
                              Kaempferol Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01353   XEOTIC Info Gene Form mRNA
                                 Classification Acute Toxic Substance
                                 DME Modulation Kaempferol up-regulates the expression of DME GSTA1 [5]
                              Okadaic acid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01409   XEOTIC Info Gene Form mRNA
                                 Classification Acute Toxic Substance
                                 DME Modulation Okadaic acid inhibits the expression of DME GSTA1 [6]
                              Usnic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01497   XEOTIC Info Gene Form Protein
                                 Classification Acute Toxic Substance
                                 DME Modulation Usnic acid induces the drug-metabolizing activity of DME GSTA1 [7]
                  Biotoxin Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Dinophysistoxin 1 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00813   XEOTIC Info Gene Form mRNA
                                 Classification Biotoxin
                                 DME Modulation Dinophysistoxin 1 inhibits the expression of DME GSTA1 [8]
                              Azaspiracid Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01502   XEOTIC Info Gene Form mRNA
                                 Classification Marine Algal Toxin
                                 DME Modulation Azaspiracid inhibits the expression of DME GSTA1 [8]
                  Carcinogen Click to Show/Hide the Full List of Xenobiotics:        3 Xenobiotics
                              Benzo(a)pyrene Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00898   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen
                                 DME Modulation Benzo(a)pyrene inhibits the expression of DME GSTA1 [9], [10]
                              Ethyl methanesulfonate Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00772   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen
                                 DME Modulation Ethyl methanesulfonate up-regulates the expression of DME GSTA1 [11]
                              Aflatoxin B1 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00806   XEOTIC Info Gene Form mRNA
                                 Classification Carcinogen-mycotoxin
                                 DME Modulation Aflatoxin B1 inhibits the expression of DME GSTA1 [12], [13]
                  Environmental Pollutant Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Polychlorinated dibenzodioxin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00917   XEOTIC Info Gene Form mRNA
                                 Classification Environmental Pollutant
                                 DME Modulation Polychlorinated dibenzodioxin up-regulates the expression of DME GSTA1 [14]
                  Health Hazard/Toxicant Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Alpha-linolenic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00873   XEOTIC Info Gene Form mRNA
                                 Classification Health Hazard
                                 DME Modulation Alpha-linolenic acid up-regulates the expression of DME GSTA1 [15]
                              Diethylhexyl phthalate Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01004   XEOTIC Info Gene Form mRNA
                                 Classification Health Hazard
                                 DME Modulation Diethylhexyl phthalate up-regulates the expression of DME GSTA1 [16]
      Natural Product(s), Extract(s) or Medicine(s)
                  Natural Mixture Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Tobacco smoke pollution Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00821   XEOTIC Info Gene Form mRNA
                                 Classification Natural Mixture
                                 DME Modulation Tobacco smoke pollution inhibits the expression of DME GSTA1 [17]
                  Natural Product Click to Show/Hide the Full List of Xenobiotics:        4 Xenobiotics
                              Arachidoyl-coenzyme A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00901   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Arachidoyl-coenzyme A inhibits the drug-metabolizing activity of DME GSTA1 [18]
                              Bilirubin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00877   XEOTIC Info Gene Form mRNA
                                 Classification Natural Product
                                 DME Modulation Bilirubin up-regulates the expression of DME GSTA1 [19]
                              Estradiol 3,17-disulfate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00912   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Estradiol 3,17-disulfate inhibits the drug-metabolizing activity of DME GSTA1 [20]
                              Lauroyl-coenzyme A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00902   XEOTIC Info Gene Form Protein
                                 Classification Natural Product
                                 DME Modulation Lauroyl-coenzyme A inhibits the drug-metabolizing activity of DME GSTA1 [18]
      Pharmaceutical Agent(s)
                  Approved/Marketed Drug Click to Show/Hide the Full List of Xenobiotics:      22 Xenobiotics
                              Acetaminophen Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00217   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Acetaminophen up-regulates the expression of DME GSTA1 [21]
                              Aemcolo Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00421   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Aemcolo up-regulates the expression of DME GSTA1 [22]
                              Arsenic trioxide Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00339   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Arsenic trioxide up-regulates the expression of DME GSTA1 [23], [24]
                              Carbamazepine Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00011   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Carbamazepine up-regulates the expression of DME GSTA1 [25]
                              Chlorambucil Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00014   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Chlorambucil inhibits the drug-metabolizing activity of DME GSTA1 [26]
                              Copper sulfate Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00117   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Copper sulfate inhibits the expression of DME GSTA1 [27]
                              Cyclosporine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00241   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Cyclosporine inhibits the expression of DME GSTA1 [28]
                              Dexamethasone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00088   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Dexamethasone induces the drug-metabolizing activity of DME GSTA1 [29]
                              Diclofenac Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00352   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Diclof DMEenac inhibits the drug-metabolizing activity of DME GSTA1 [30]
                              Dopamine hydrochloride Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00290   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Dopamine hydrochloride inhibits the drug-metabolizing activity of DME GSTA1 [31]
                              Estradiol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00090   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Estradiol inhibits the expression of DME GSTA1 [32]
                              Hydrocortisone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00264   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Hydrocortisone up-regulates the expression of DME GSTA1 and leads to increasing the drug-metabolizing activity of this enzyme [33]
                              Ketoconazole Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00251   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Ketoconazole inhibits the expression of DME GSTA1 [34]
                              Methotrexate Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00366   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Methotrexate up-regulates the expression of DME GSTA1 [35]
                              Mifepristone Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00127   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Mifepristone induces the drug-metabolizing activity of DME GSTA1 [36]
                              Phenobarbital Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00410   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Phenobarbital inhibits the drug-metabolizing activity of DME GSTA1 [37]
                              Phenytoin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00232   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Phenytoin up-regulates the expression of DME GSTA1 [19]
                              Rifampin Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00223   XEOTIC Info Gene Form Protein
                                 Classification Drug Approved by US FDA
                                 DME Modulation Rifampin induces the drug-metabolizing activity of DME GSTA1 [38]
                              Urethane Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00435   XEOTIC Info Gene Form mRNA
                                 Classification Drug Approved by US FDA
                                 DME Modulation Urethane inhibits the expression of DME GSTA1 [39]
                              Artemisinine Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00449   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Artemisinine inhibits the drug-metabolizing activity of DME GSTA1 [40]
                              Benzoic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00447   XEOTIC Info Gene Form Protein
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Benzoic acid induces the drug-metabolizing activity of DME GSTA1 [41]
                              Linoleic acid Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01367   XEOTIC Info Gene Form mRNA
                                 Classification Drug Marketed but not Approved by US FDA
                                 DME Modulation Linoleic acid up-regulates the expression of DME GSTA1 [15]
                  Drug in Phase 3 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              SGX301 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00579   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation SGX301 inhibits the drug-metabolizing activity of DME GSTA1 [42]
                              Sulforafan Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO01478   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 3
                                 DME Modulation Sulforafan induces the drug-metabolizing activity of DME GSTA1 [43]
                  Drug in Phase 2 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              MeIQx Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00609   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 2
                                 DME Modulation MeIQx inhibits the expression of DME GSTA1 [2], [44]
                  Drug in Phase 1 Clinical Trial Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Quercetin Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00538   XEOTIC Info Gene Form Protein
                                 Classification Highest Clinical Status: Phase 1
                                 DME Modulation Quercetin inhibits the drug-metabolizing activity of DME GSTA1 [45]
                              Xanthohumol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00636   XEOTIC Info Gene Form mRNA
                                 Classification Highest Clinical Status: Phase 1
                                 DME Modulation Xanthohumol inhibits the expression of DME GSTA1 [46]
                  Preclinical/Patented Drug Click to Show/Hide the Full List of Xenobiotics:        3 Xenobiotics
                              Oleoyl-coenzyme A Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01413   XEOTIC Info Gene Form mRNA
                                 Classification Drug in Preclinical Study
                                 DME Modulation Oleoyl-coenzyme A inhibits the expression of DME GSTA1 [6]
                              Eugenol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00885   XEOTIC Info Gene Form Protein
                                 Classification Patented Pharmaceutical Agent
                                 DME Modulation Eugenol inhibits the drug-metabolizing activity of DME GSTA1 [47]
                              K-7174 Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01348   XEOTIC Info Gene Form mRNA
                                 Classification Patented Pharmaceutical Agent
                                 DME Modulation K-7174 inhibits the expression of DME GSTA1 [48]
                  Investigative Agent Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              Beta-naphthoflavone Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01220   XEOTIC Info Gene Form mRNA
                                 Classification Investigative Agent
                                 DME Modulation Beta-naphthoflavone inhibits the expression of DME GSTA1 [49]
      Other Chemical Compound(s) or Element(s)
                  Food Additive Click to Show/Hide the Full List of Xenobiotics:        1 Xenobiotics
                              4-propylphenol Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO00929   XEOTIC Info Gene Form Protein
                                 Classification Food Additive
                                 DME Modulation 4-propylphenol inhibits the drug-metabolizing activity of DME GSTA1 [47]
                  Chemical Compound Click to Show/Hide the Full List of Xenobiotics:        2 Xenobiotics
                              Picolines Click to Show/Hide the Detail Inhibition
                                 XEOTIC ID XEO01020   XEOTIC Info Gene Form mRNA
                                 Classification Chemical Compound
                                 DME Modulation Picolines inhibits the expression of DME GSTA1 [50]
                              Tungsten Click to Show/Hide the Detail Induction
                                 XEOTIC ID XEO00793   XEOTIC Info Gene Form mRNA
                                 Classification Chemical Compound
                                 DME Modulation Tungsten up-regulates the expression of DME GSTA1 [51]
References
1 Molecular mechanisms of discrotophos-induced toxicity in HepG2 cells: The role of CSA in oxidative stress. Food Chem Toxicol. 2017 May;103:253-260.
2 Protective effects of xanthohumol against the genotoxicity of heterocyclic aromatic amines MeIQx and PhIP in bacteria and in human hepatoma (HepG2) cells. Food Chem Toxicol. 2012 Mar;50(3-4):949-55.
3 The influence of picolines on glutathione transferase activity and subunit composition in human liver derived Hep G2 cells. Biochem Pharmacol. 1994 Nov 16;48(10):1976-8.
4 Organophosphate pesticides increase the expression of alpha glutathione S-transferase in HepG2 cells. Toxicol In Vitro. 2011 Dec;25(8):2074-9.
5 Single and concerted effects of benzo[a]pyrene and flavonoids on the AhR and Nrf2-pathway in the human colon carcinoma cell line Caco-2. Toxicol In Vitro. 2011 Apr;25(3):671-83.
6 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
7 The thiazolidinedione drug troglitazone up-regulates nitric oxide synthase expression in vascular endothelial cells. J Diabetes Complications. 2006 Sep-Oct;20(5):336-42.
8 Whole genome mRNA transcriptomics analysis reveals different modes of action of the diarrheic shellfish poisons okadaic acid and dinophysis toxin-1 versus azaspiracid-1 in Caco-2 cells. Toxicol In Vitro. 2018 Feb;46:102-112.
9 Benzo[a]pyrene-induced changes in microRNA-mRNA networks. Chem Res Toxicol. 2012 Apr 16;25(4):838-49.
10 Adipose tissue stem cell-derived hepatic progenies as an in vitro model for genotoxicity testing. Arch Toxicol. 2018 May;92(5):1893-1903.
11 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
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13 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
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26 Role of multidrug resistance protein 1 (MRP1) and glutathione S-transferase A1-1 in alkylating agent resistanceKinetics of glutathione conjugate formation and efflux govern differential cellular sensitivity to chlorambucil versus melphalan toxicity. J Biol Chem. 2001 Mar 16;276(11):7952-6.
27 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
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29 Dexamethasone induces human glutathione S transferase alpha 1 (hGSTA1) expression through the activation of glucocorticoid receptor (hGR). Toxicology. 2017 Jun 15;385:59-66.
30 Simulation of interindividual differences in inactivation of reactive para-benzoquinone imine metabolites of diclofenac by glutathione S-transferases in human liver cytosol. Toxicol Lett. 2016 Jul 25;255:52-62.
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32 Genistein and bisphenol A exposure cause estrogen receptor 1 to bind thousands of sites in a cell type-specific manner. Genome Res. 2012 Nov;22(11):2153-62.
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47 Inhibition of rat, mouse, and human glutathione S-transferase by eugenol and its oxidation products. Chem Biol Interact. 1996 Jan 5;99(1-3):85-97.
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51 Metabolomics profiles delineate uridine deficiency contributes to mitochondria-mediated apoptosis induced by celastrol in human acute promyelocytic leukemia cells. Oncotarget. 2016 Jul 19;7(29):46557-46572.

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