Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DE4ZHS1)

DME Name Glutathione S-transferase alpha-1 (GSTA1)
Synonyms
Glutathione S-transferase A1; Androst-5-ene-3,17-dione isomerase; 13-hydroperoxyoctadecadienoate peroxidase; GST HA subunit 1; GST class-alpha member 1; GST-epsilon; N-terminally processed glutathione S-transferase A1; GSTA1; GSTA1-1; GTH1
Gene Name GSTA1
UniProt ID
GSTA1_HUMAN
INTEDE ID
DME0011
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
2938
EC Number EC: 2.5.1.18
Transferase
Alkyl/aryl transferase
Alkyl/aryl transferase
EC: 2.5.1.18
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MAEKPKLHYFNARGRMESTRWLLAAAGVEFEEKFIKSAEDLDKLRNDGYLMFQQVPMVEI
DGMKLVQTRAILNYIASKYNLYGKDIKERALIDMYIEGIADLGEMILLLPVCPPEEKDAK
LALIKEKIKNRYFPAFEKVLKSHGQDYLVGNKLSRADIHLVELLYYVEELDSSLISSFPL
LKALKTRISNLPTVKKFLQPGSPRKPPMDEKSLEEARKIFRF
Function
This enzyme catalyzes the isomerization of D5-androstene-3,17-dione (AD) into D4-androstene- 3,17-dione. Through its glutathione-dependent peroxidase activity toward the fatty acid hydroperoxide (13S)- hydroperoxy-(9Z,11E)-octadecadienoate/13-HPODE, it is also involved in the metabolism of oxidized linoleic acid.
KEGG Pathway
Chemical carcinogenesis (hsa05204 )
Drug metabolism - cytochrome P450 (hsa00982 )
Drug metabolism - other enzymes (hsa00983 )
Fluid shear stress and atherosclerosis (hsa05418 )
Glutathione metabolism (hsa00480 )
Hepatocellular carcinoma (hsa05225 )
Metabolic pathways (hsa01100 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Pathways in cancer (hsa05200 )
Platinum drug resistance (hsa01524 )
Reactome Pathway
Glutathione conjugation (R-HSA-156590 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
16 Approved Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [1]
Amyl nitrite DMJKO05 Angina pectoris BA40 Approved [2]
Artemisinin DMOY7W3 Malaria 1F40-1F45 Approved [3]
Busulfan DMXYJ9C Chronic myelogenous leukaemia 2A20.0 Approved [4]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [5]
Clofibrate DMPC1J7 Dysbetalipoproteinemia 5C80.2 Approved [6]
DTI-015 DMXZRW0 Brain cancer 2A00 Approved [7]
Ethacrynic acid DM60QMR Edema MG29 Approved [8]
Fosfomycin DMVGPMX Bacterial infection 1A00-1C4Z Approved [9]
Isosorbide Dinitrate DMBI4JG Anal fissure DB50.0 Approved [10]
Melphalan DMOLNHF Hematologic disease 3C0Z Approved [11]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [12]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [13]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [14]
Thiotepa DMIZKOP Breast cancer 2C60-2C65 Approved [15]
Trabectedin DMG3Y89 Leiomyosarcoma 2B58 Approved [16]
⏷ Show the Full List of 16 Approved Drug(s)
2 Clinical Trial Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
Selinexor DMBD4K3 Multiple myeloma 2A83 Phase 3 [17]
PEITC DMOMN31 Prostate cancer 2C82.0 Phase 2 [18]

Molecular Expression Atlas (MEA) of This DME

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DME
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 7.81E-01 -5.69E-02 -1.99E-01
Alopecia ED70 Skin from scalp 1.49E-04 1.64E-01 6.42E-01
Alzheimer's disease 8A20 Entorhinal cortex 3.34E-01 -6.03E-03 -3.30E-02
Ankylosing spondylitis FA92.0 Pheripheral blood 8.64E-01 1.55E-01 1.03E+00
Aortic stenosis BB70 Calcified aortic valve 9.32E-01 -9.55E-02 -2.31E-01
Apnea 7A40 Hyperplastic tonsil 9.97E-01 -5.87E-02 -1.79E-01
Arthropathy FA00-FA5Z Peripheral blood 1.93E-01 -2.20E-01 -7.61E-01
Asthma CA23 Nasal and bronchial airway 1.01E-05 2.37E-01 4.59E-01
Atopic dermatitis EA80 Skin 3.88E-02 -7.96E-03 -3.97E-02
Autism 6A02 Whole blood 3.66E-01 1.84E-01 4.98E-01
Autoimmune uveitis 9A96 Peripheral monocyte 1.90E-01 2.89E-01 1.82E+00
Autosomal dominant monocytopenia 4B04 Whole blood 4.04E-02 2.11E-01 2.03E+00
Bacterial infection of gingival 1C1H Gingival tissue 4.94E-02 -1.14E-01 -3.54E-01
Batten disease 5C56.1 Whole blood 5.64E-01 -3.64E-02 -2.49E-01
Behcet's disease 4A62 Peripheral blood 8.39E-01 3.29E-04 1.97E-03
Bipolar disorder 6A60-6A6Z Prefrontal cortex 6.99E-01 -2.21E-02 -1.01E-01
Bladder cancer 2C94 Bladder tissue 4.10E-01 6.86E-02 1.32E-01
Breast cancer 2C60-2C6Z Breast tissue 6.32E-16 -2.72E-01 -5.86E-01
Cardioembolic stroke 8B11.20 Whole blood 4.49E-01 -2.59E-02 -7.59E-02
Cervical cancer 2C77 Cervical tissue 1.22E-05 -3.14E-01 -1.80E+00
Childhood onset rheumatic disease FA20.Z Peripheral blood 9.92E-01 -1.76E-01 -2.90E-01
Chronic hepatitis C 1E51.1 Whole blood 2.15E-01 -4.67E-02 -3.41E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 4.30E-03 2.36E-01 8.19E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 3.99E-02 -2.06E-01 -6.25E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 9.03E-01 -2.45E-02 -1.10E-01
Colon cancer 2B90 Colon tissue 1.89E-01 2.86E-02 9.46E-02
Coronary artery disease BA80-BA8Z Peripheral blood 7.07E-01 -3.34E-01 -5.47E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 5.13E-02 -2.00E-01 -7.37E-01
Endometriosis GA10 Endometrium tissue 8.37E-01 1.52E-02 5.74E-02
Familial hypercholesterolemia 5C80.00 Peripheral blood 2.71E-01 -1.10E-01 -4.63E-01
Familial hypercholesterolemia 5C80.00 Whole blood 9.60E-03 -1.31E-01 -5.02E-01
Gastric cancer 2B72 Gastric tissue 5.48E-01 8.83E-02 3.40E-01
Glioblastopma 2A00.00 Nervous tissue 9.34E-77 4.82E-01 1.43E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 3.30E-01 4.03E-01 1.15E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 6.84E-01 1.31E-01 1.90E-01
Head and neck cancer 2D42 Head and neck tissue 1.19E-18 -4.14E-01 -1.19E+00
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 3.78E-01 -1.02E-01 -4.79E-01
Huntington's disease 8A01.10 Whole blood 5.96E-01 1.08E-02 3.53E-02
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 8.04E-02 1.03E-01 5.71E-01
Immunodeficiency 4A00-4A20 Peripheral blood 7.27E-06 -4.57E-01 -4.65E+00
Influenza 1E30 Whole blood 2.71E-01 2.18E-02 1.46E-01
Interstitial cystitis GC00.3 Bladder tissue 8.17E-02 -4.36E-03 -2.39E-02
Intracranial aneurysm 8B01.0 Intracranial artery 1.93E-01 -7.30E-02 -2.63E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 4.13E-01 5.35E-03 1.81E-02
Ischemic stroke 8B11 Peripheral blood 3.07E-02 -1.67E-01 -8.04E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 2.87E-01 -4.38E-02 -7.36E-02
Lateral sclerosis 8B60.4 Skin 2.83E-01 -1.52E-01 -7.40E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 4.27E-01 1.12E-01 3.15E-01
Liver cancer 2C12.0 Liver tissue 7.89E-01 -8.55E-03 -2.56E-02
Liver failure DB99.7-DB99.8 Liver tissue 7.08E-03 4.12E-01 1.58E+00
Lung cancer 2C25 Lung tissue 2.53E-09 9.65E-02 3.65E-01
Lupus erythematosus 4A40 Whole blood 1.33E-03 -1.75E-01 -3.27E-01
Major depressive disorder 6A70-6A7Z Hippocampus 7.60E-01 -1.03E-02 -4.60E-02
Major depressive disorder 6A70-6A7Z Whole blood 5.43E-02 -1.04E-01 -2.90E-01
Melanoma 2C30 Skin 5.09E-01 -1.42E-01 -2.28E-01
Multiple myeloma 2A83.1 Peripheral blood 5.13E-01 1.94E-01 4.12E-01
Multiple myeloma 2A83.1 Bone marrow 1.08E-02 -3.40E-01 -1.29E+00
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 2.06E-02 -5.41E-01 -9.66E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 1.34E-02 7.48E-02 3.66E-01
Myelofibrosis 2A20.2 Whole blood 1.45E-01 -1.13E-01 -9.73E-01
Myocardial infarction BA41-BA50 Peripheral blood 2.43E-02 -5.81E-01 -5.08E-01
Myopathy 8C70.6 Muscle tissue 3.92E-02 -1.12E-01 -9.67E-01
Neonatal sepsis KA60 Whole blood 8.41E-19 -4.50E-01 -1.37E+00
Neuroectodermal tumour 2A00.11 Brain stem tissue 5.59E-01 1.34E-02 4.29E-02
Non-alcoholic fatty liver disease DB92 Liver tissue 1.16E-01 -1.38E-01 -1.09E+00
Obesity related type 2 diabetes 5A11 Omental adipose tissue 8.26E-01 -6.97E-02 -4.09E-01
Olive pollen allergy CA08.00 Peripheral blood 5.52E-01 -4.10E-01 -5.81E-01
Oral cancer 2B6E Oral tissue 5.97E-01 2.72E-02 6.34E-02
Osteoarthritis FA00-FA0Z Synovial tissue 9.02E-02 1.09E-01 3.63E-01
Osteoporosis FB83.1 Bone marrow 4.64E-01 5.37E-02 3.64E-01
Ovarian cancer 2C73 Ovarian tissue 5.69E-01 6.53E-02 1.11E-01
Pancreatic cancer 2C10 Pancreas 2.88E-01 -1.17E-01 -3.32E-01
Parkinson's disease 8A00.0 Substantia nigra tissue 5.78E-01 3.39E-02 1.54E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 2.36E-02 -2.56E-01 -9.34E-01
Pituitary cancer 2D12 Pituitary tissue 2.87E-02 4.55E-01 1.34E+00
Pituitary gonadotrope tumour 2D12 Pituitary tissue 7.62E-03 3.60E-01 1.19E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 6.41E-01 -1.48E-02 -8.17E-02
Polycythemia vera 2A20.4 Whole blood 6.13E-01 -4.84E-02 -3.91E-01
Pompe disease 5C51.3 Biceps muscle 1.43E-02 -5.34E-01 -1.35E+00
Preterm birth KA21.4Z Myometrium 6.54E-01 2.10E-02 6.44E-02
Prostate cancer 2C82 Prostate 2.01E-04 9.51E-01 1.46E+00
Psoriasis EA90 Skin 1.22E-03 -1.91E-01 -4.49E-01
Rectal cancer 2B92 Rectal colon tissue 9.24E-01 -2.85E-01 -4.78E-01
Renal cancer 2C90-2C91 Kidney 4.44E-01 3.21E-02 1.06E-01
Retinoblastoma 2D02.2 Uvea 2.02E-02 2.60E-01 1.48E+00
Rheumatoid arthritis FA20 Synovial tissue 7.05E-04 -3.17E-01 -1.86E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 3.29E-01 6.28E-02 3.09E-01
Schizophrenia 6A20 Prefrontal cortex 9.35E-01 -4.12E-03 -1.61E-02
Schizophrenia 6A20 Superior temporal cortex 7.10E-01 -3.54E-02 -3.59E-01
Scleroderma 4A42.Z Whole blood 4.26E-01 -1.02E-01 -4.36E-01
Seizure 8A60-8A6Z Whole blood 9.61E-01 4.59E-02 1.31E-01
Sensitive skin EK0Z Skin 2.89E-01 -2.08E-01 -1.18E+00
Sepsis with septic shock 1G41 Whole blood 1.26E-24 -2.77E-01 -8.84E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.55E-01 1.31E-01 5.73E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 7.48E-02 -2.08E-01 -6.96E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 8.31E-01 -2.54E-02 -3.08E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 7.06E-02 8.98E-02 1.17E+00
Skin cancer 2C30-2C3Z Skin 2.11E-02 7.54E-02 1.47E-01
Thrombocythemia 3B63 Whole blood 6.46E-01 -1.31E-02 -1.16E-01
Thrombocytopenia 3B64 Whole blood 6.55E-01 -7.75E-01 -4.45E-01
Thyroid cancer 2D10 Thyroid 2.60E-31 -4.63E-01 -1.72E+00
Tibial muscular dystrophy 8C75 Muscle tissue 3.52E-02 -2.32E-01 -1.06E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 3.12E-01 2.23E-01 9.80E-01
Type 2 diabetes 5A11 Liver tissue 6.81E-01 8.35E-02 4.77E-01
Ureter cancer 2C92 Urothelium 4.60E-01 -1.27E-02 -3.76E-02
Uterine cancer 2C78 Endometrium tissue 4.62E-01 -5.05E-02 -1.52E-01
Vitiligo ED63.0 Skin 9.62E-01 7.13E-04 5.91E-03
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⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Glutathione S-transferase A1 (GSTA1) DTT Info
DME DTT Type Literature-reported

References

1 Retinoid X receptor alpha regulates the expression of glutathione s-transferase genes and modulates acetaminophen-glutathione conjugation in mouse liver. Mol Pharmacol. 2005 Dec;68(6):1590-6.
2 Subunit specificity and organ distribution of glutathione transferase-catalysed S-nitrosoglutathione formation from alkyl nitrites in the rat. Biochem Pharmacol. 1997 Jan 10;53(1):117-20.
3 Inhibition of glutathione S-transferases by antimalarial drugs possible implications for circumventing anticancer drug resistance. Int J Cancer. 2002 Feb 10;97(5):700-5.
4 Glutathione S-transferase M1 polymorphism: a risk factor for hepatic venoocclusive disease in bone marrow transplantation. Blood. 2004 Sep 1;104(5):1574-7.
5 Role of glutathione S-transferase P1-1 in the cellular detoxification of cisplatin. Mol Cancer Ther. 2008 Oct;7(10):3247-55.
6 Characterization and formation of the glutathione conjugate of clofibric acid. Drug Metab Dispos. 1995 Jan;23(1):119-23.
7 Expression of glutathione S-transferase T1 (GSTT1) in human brain tumours. Histol Histopathol. 2006 Nov;21(11):1199-207.
8 Purification and biochemical properties of glutathione S-transferase from Lactuca sativa. J Biochem Mol Biol. 2005 Mar 31;38(2):232-7.
9 Formation of an adduct between fosfomycin and glutathione: a new mechanism of antibiotic resistance in bacteria. Antimicrob Agents Chemother. 1988 Oct;32(10):1552-6.
10 Nitroglycerin and isosorbide dinitrate stimulation of glutathione disulfide efflux from perfused rat liver. Biochem Pharmacol. 1989 Nov 1;38(21):3807-10.
11 Metabolism of melphalan by rat liver microsomal glutathione S-transferase. Chem Biol Interact. 2005 Apr 15;152(2-3):101-6.
12 Comparison of basal glutathione S-transferase activities and of the influence of phenobarbital, butylated hydroxy-anisole or 5,5'-diphenylhydantoin on enzyme activity in male rodents. Comp Biochem Physiol C. 1987;88(1):91-3.
13 Human glutathione transferase A3-3, a highly efficient catalyst of double-bond isomerization in the biosynthetic pathway of steroid hormones. J Biol Chem. 2001 Aug 31;276(35):33061-5.
14 Combined glutathione-S-transferase M1 and T1 genetic polymorphism and tacrine hepatotoxicity. Clin Pharmacol Ther. 2000 Apr;67(4):432-7.
15 Differential catalytic efficiency of allelic variants of human glutathione S-transferase Pi in catalyzing the glutathione conjugation of thiotepa. Arch Biochem Biophys. 1999 Jun 1;366(1):89-94.
16 In vitro characterization of the human biotransformation and CYP reaction phenotype of ET-743 (Yondelis, Trabectidin), a novel marine anti-cancer drug. Invest New Drugs. 2006 Jan;24(1):3-14.
17 FDA label of Selinexor. The 2020 official website of the U.S. Food and Drug Administration.
18 Pharmacokinetics and pharmacodynamics of phenethyl isothiocyanate: implications in breast cancer prevention. AAPS J. 2014 Jul;16(4):705-13.