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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
CYP1, 2 and 3 family enzymes are involved in the biotransformation of xenobiotics, including clinically used drugs. Polymorphisms, particularly in the CYP2 family, impact upon an individual's response to drugs [31], including the risk of adverse drug reactions, drug efficacy and dose requirement.
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18. Mahli A, Erwin Thasler W, Hellerbrand C. (2019) Establishment of a p-nitrophenol oxidation-based assay for the analysis of CYP2E1 activity in intact hepatocytes in vitro. Toxicol Mech Methods, 29 (3): 219-223. [PMID:30380359]
19. Miners JO, Smith KJ, Robson RA, McManus ME, Veronese ME, Birkett DJ. (1988) Tolbutamide hydroxylation by human liver microsomes. Kinetic characterisation and relationship to other cytochrome P-450 dependent xenobiotic oxidations. Biochem Pharmacol, 37 (6): 1137-44. [PMID:3355588]
20. Pelkonen O, Rautio A, Raunio H, Pasanen M. (2000) CYP2A6: a human coumarin 7-hydroxylase. Toxicology, 144 (1-3): 139-47. [PMID:10781881]
21. Qi X, Dou T, Wang Z, Wu J, Yang L, Zeng S, Deng M, Lü M, Liang S. (2019) Inhibition of human cytochrome P450 2A6 by 7-hydroxycoumarin analogues: Analysis of the structure-activity relationship and isoform selectivity. Eur J Pharm Sci, 136: 104944. [PMID:31163215]
22. Solanki M, Pointon A, Jones B, Herbert K. (2018) Cytochrome P450 2J2: Potential Role in Drug Metabolism and Cardiotoxicity. Drug Metab Dispos, 46 (8): 1053-1065. [PMID:29695613]
23. Su T, Bao Z, Zhang QY, Smith TJ, Hong JY, Ding X. (2000) Human cytochrome P450 CYP2A13: predominant expression in the respiratory tract and its high efficiency metabolic activation of a tobacco-specific carcinogen, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone. Cancer Res, 60 (18): 5074-9. [PMID:11016631]
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26. Walsky RL, Obach RS. (2007) A comparison of 2-phenyl-2-(1-piperidinyl)propane (ppp), 1,1',1''-phosphinothioylidynetrisaziridine (thioTEPA), clopidogrel, and ticlopidine as selective inactivators of human cytochrome P450 2B6. Drug Metab Dispos, 35 (11): 2053-9. [PMID:17682072]
27. Webster SP, McBride A, Binnie M, Sooy K, Seckl JR, Andrew R, Pallin TD, Hunt HJ, Perrior TR, Ruffles VS et al.. (2017) Selection and early clinical evaluation of the brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor UE2343 (Xanamem™). Br J Pharmacol, 174 (5): 396-408. [PMID:28012176]
28. Wu S, Moomaw CR, Tomer KB, Falck JR, Zeldin DC. (1996) Molecular cloning and expression of CYP2J2, a human cytochrome P450 arachidonic acid epoxygenase highly expressed in heart. J Biol Chem, 271 (7): 3460-8. [PMID:8631948]
29. Wu Z, Lee D, Joo J, Shin JH, Kang W, Oh S, Lee DY, Lee SJ, Yea SS, Lee HS et al.. (2013) CYP2J2 and CYP2C19 are the major enzymes responsible for metabolism of albendazole and fenbendazole in human liver microsomes and recombinant P450 assay systems. Antimicrob Agents Chemother, 57 (11): 5448-56. [PMID:23959307]
30. Yano JK, Denton TT, Cerny MA, Zhang X, Johnson EF, Cashman JR. (2006) Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization. J Med Chem, 49 (24): 6987-7001. [PMID:17125252]
31. Zanger UM, Schwab M. (2013) Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation. Pharmacol Ther, 138 (1): 103-41. [PMID:23333322]
32. Zeldin DC, DuBois RN, Falck JR, Capdevila JH. (1995) Molecular cloning, expression and characterization of an endogenous human cytochrome P450 arachidonic acid epoxygenase isoform. Arch Biochem Biophys, 322 (1): 76-86. [PMID:7574697]
Kathryn Burns
Nuala Ann Helsby |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.
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