Details of Drug-Metabolizing Enzyme (DME)
General Information of Drug-Metabolizing Enzyme (DME) (ID: DEJVYAZ)
DME Name | Cytochrome P450 2A6 (CYP2A6) | ||||
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Synonyms | Cytochrome P450 family 2 subfamily A member 6; Coumarin 7-hydroxylase; Cytochrome P450 IIA3; Cytochrome P450(I); CYP2A3; CYP2A6; CYPIIA6 | ||||
Gene Name | CYP2A6 | ||||
UniProt ID | |||||
INTEDE ID | |||||
3D Structure | |||||
Gene ID | |||||
EC Number | EC: 1.14.14.1 | ||||
Lineage | Species: Homo sapiens | ||||
Sequence |
MLASGMLLVALLVCLTVMVLMSVWQQRKSKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMK
ISERYGPVFTIHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSN GERAKQLRRFSIATLRDFGVGKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSN VISSIVFGDRFDYKDKEFLSLLRMMLGIFQFTSTSTGQLYEMFSSVMKHLPGPQQQAFQL LQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEKNPNTEFYLKNLVMTTLNLFI GGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMPYMEAVIHEIQ RFGDVIPMSLARRVKKDTKFRDFFLPKGTEVYPMLGSVLRDPSFFSNPQDFNPQHFLNEK GQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGF ATIPRNYTMSFLPR |
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Function |
This enzyme exhibits a high coumarin 7-hydroxylase activity. It can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. It is also competent in the metabolic activation of aflatoxin B1.
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KEGG Pathway | |||||
Reactome Pathway | |||||
Molecular Interaction Atlas (MIA) of This DME
Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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48 Approved Drug(s) Metabolized by This DME
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5 Clinical Trial Drug(s) Metabolized by This DME
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1 Discontinued Drug(s) Metabolized by This DME
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7 Investigative Drug(s) Metabolized by This DME
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Molecular Expression Atlas (MEA) of This DME
The Drug Therapeutic Target (DTT) Role of This DME
DME DTT Name | Cytochrome P450 2A6 (CYP2A6) | |||||||||||||||||||||||||||
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DME DTT Type | Successful | |||||||||||||||||||||||||||
1 Approved Drug(s) Targeting This DTT
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References
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14 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. Drug Metab Dispos. 2013 Mar;41(3):651-8. | ||||
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21 | Halothane-dependent lipid peroxidation in human liver microsomes is catalyzed by cytochrome P4502A6 (CYP2A6). Anesthesiology. 2001 Aug;95(2):509-14. | ||||
22 | Measurement of 4-hydroxylation of ifosfamide in human liver microsomes using the estimation of free and protein-bound acrolein and codetermination of keto- and carboxyifosfamide. J Cancer Res Clin Oncol. 2002 Jul;128(7):385-92. | ||||
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26 | Health control over the feeding of troops on the Western and 3d Belorussian Fronts during the Great Patriotic War years. Voen Med Zh. 1975 Jun;(6):86-8. | ||||
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28 | The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94. | ||||
29 | CYP2A6- and CYP2A13-catalyzed metabolism of the nicotine delta-5'(1')iminium ion. J Pharmacol Exp Ther. 2012 Nov;343(2):307-15. | ||||
30 | Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone. J Steroid Biochem Mol Biol. 2008 May;110(1-2):56-66. | ||||
31 | The metabolism of the piperazine-type phenothiazine neuroleptic perazine by the human cytochrome P-450 isoenzymes. Eur Neuropsychopharmacol. 2004 May;14(3):199-208. | ||||
32 | Structural comparison of cytochromes P450 2A6, 2A13, and 2E1 with pilocarpine. FEBS J. 2012 May;279(9):1621-31. | ||||
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36 | Rapid development of S-1 in the west for therapy of advanced gastric carcinoma. Gan To Kagaku Ryoho. 2006 Jun;33 Suppl 1:117-20. | ||||
37 | Metabolism of thalidomide in human microsomes, cloned human cytochrome P-450 isozymes, and Hansen's disease patients. J Biochem Mol Toxicol. 2000;14(3):140-7. | ||||
38 | UFT Capsules (uracil-tegafur). | ||||
39 | Psychotropic drug interactions with valproate. Clin Neuropharmacol. 2005 Mar-Apr;28(2):96-101. | ||||
40 | Identification of the cytochrome P450 and other enzymes involved in the in vitro oxidative metabolism of a novel antidepressant, Lu AA21004. Drug Metab Dispos. 2012 Jul;40(7):1357-65. | ||||
41 | Cytochrome P450 CYP1B1 interacts with 8-methoxypsoralen (8-MOP) and influences psoralen-ultraviolet A (PUVA) sensitivity. PLoS One. 2013 Sep 23;8(9):e75494. | ||||
42 | In vitro characterization of the human biotransformation pathways of aplidine, a novel marine anti-cancer drug. Invest New Drugs. 2007 Feb;25(1):9-19. | ||||
43 | Australian Public Assessment Report for asunaprevir. | ||||
44 | Cytochrome P450 enzymes involved in the metabolic pathway of the histamine 2 (H2)-receptor antagonist roxatidine acetate by human liver microsomes. Arzneimittelforschung. 2001;51(8):651-8. | ||||
45 | Activation of phenacetin O-deethylase activity by alpha-naphthoflavone in human liver microsomes. Xenobiotica. 1999 Sep;29(9):885-98. | ||||
46 | The participation of human hepatic P450 isoforms, flavin-containing monooxygenases and aldehyde oxidase in the biotransformation of the insecticide fenthion. Toxicol Appl Pharmacol. 2008 Dec 1;233(2):343-52. | ||||
47 | Site-specific oxidation of flavanone and flavone by cytochrome P450 2A6 in human liver microsomes. Xenobiotica. 2019 Jul;49(7):791-802. | ||||
48 | Roles of human CYP2A6 and 2B6 and rat CYP2C11 and 2B1 in the 10-hydroxylation of (-)-verbenone by liver microsomes. Drug Metab Dispos. 2003 Aug;31(8):1049-53. | ||||
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