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CYP2 family C
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).
Enzymes
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CYP2A6
C
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CYP2A7 C Show summary »« Hide summary
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CYP2A13 C Show summary »« Hide summary
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CYP2B6
C
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CYP2C8
C
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CYP2C9
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CYP2C18 Show summary »« Hide summary
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CYP2C19 C Show summary »« Hide summary
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CYP2D6
C
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CYP2E1
C
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CYP2F1 C Show summary »« Hide summary
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CYP2J2 C Show summary »« Hide summary
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CYP2R1 C Show summary »« Hide summary
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CYP2S1 Show summary »« Hide summary
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CYP2U1 Show summary »« Hide summary
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CYP2W1 Show summary »« Hide summary
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References
1. Backman JT, Filppula AM, Niemi M, Neuvonen PJ. (2016) Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol. Rev., 68 (1): 168-241. [PMID:26721703]
2. Bae SH, Kwon MJ, Choi EJ, Zheng YF, Yoon KD, Liu KH, Bae SK. (2013) Potent inhibition of cytochrome P450 2B6 by sibutramine in human liver microsomes. Chem. Biol. Interact., 205 (1): 11-9. [PMID:23777987]
3. Bertilsson L, Henthorn TK, Sanz E, Tybring G, Säwe J, Villén T. (1989) Importance of genetic factors in the regulation of diazepam metabolism: relationship to S-mephenytoin, but not debrisoquin, hydroxylation phenotype. Clin. Pharmacol. Ther., 45 (4): 348-55. [PMID:2495208]
4. Cheng JB, Motola DL, Mangelsdorf DJ, Russell DW. (2003) De-orphanization of cytochrome P450 2R1: a microsomal vitamin D 25-hydroxilase. J. Biol. Chem., 278 (39): 38084-93. [PMID:12867411]
5. Crosignani S, Jorand-Lebrun C, Campbell G, Pretre A, Grippi-Vallotton, T, Quattropani, A, Bouscary-Desforges G, Bombrun A, Missotten, M, Humbert Y et al.. (2011) Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids. ACS Med Chem Lett, 2: 938-942.
6. Daly AK, Rettie AE, Fowler DM, Miners JO. (2017) Pharmacogenomics of CYP2C9: Functional and Clinical Considerations. J Pers Med, 8 (1). [PMID:29283396]
7. Desta Z, Zhao X, Shin JG, Flockhart DA. (2002) Clinical significance of the cytochrome P450 2C19 genetic polymorphism. Clin Pharmacokinet, 41 (12): 913-58. [PMID:12222994]
8. Fontana E, Dansette PM, Poli SM. (2005) Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr. Drug Metab., 6 (5): 413-54. [PMID:16248836]
9. Foti RS, Rock DA, Han X, Flowers RA, Wienkers LC, Wahlstrom JL. (2012) Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19. J. Med. Chem., 55 (3): 1205-14. [PMID:22239545]
10. Fukami T, Nakajima M, Sakai H, McLeod HL, Yokoi T. (2006) CYP2A7 polymorphic alleles confound the genotyping of CYP2A6*4A allele. Pharmacogenomics J., 6 (6): 401-12. [PMID:16636685]
11. Ha-Duong NT, Dijols S, Marques-Soares C, Minoletti C, Dansette PM, Mansuy D. (2001) Synthesis of sulfaphenazole derivatives and their use as inhibitors and tools for comparing the active sites of human liver cytochromes P450 of the 2C subfamily. J. Med. Chem., 44 (22): 3622-31. [PMID:11606127]
12. Helsby NA, Ward SA, Edwards G, Howells RE, Breckenridge AM. (1990) The pharmacokinetics and activation of proguanil in man: consequences of variability in drug metabolism. Br J Clin Pharmacol, 30 (4): 593-8. [PMID:2291871]
13. Lafite P, Dijols S, Buisson D, Macherey AC, Zeldin DC, Dansette PM, Mansuy D. (2006) Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2. Bioorg. Med. Chem. Lett., 16 (10): 2777-80. [PMID:16495056]
14. Lewis DF, Ito Y, Lake BG. (2009) Molecular modelling of CYP2F substrates: comparison of naphthalene metabolism by human, rat and mouse CYP2F subfamily enzymes. Drug Metabol Drug Interact, 24 (2-4): 229-57. [PMID:20408502]
15. Llerena A, Dorado P, Peñas-Lledó EM. (2009) Pharmacogenetics of debrisoquine and its use as a marker for CYP2D6 hydroxylation capacity. Pharmacogenomics, 10 (1): 17-28. [PMID:19102711]
16. 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]
17. 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]
18. 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]
19. 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]
20. Sykes MJ, McKinnon RA, Miners JO. (2008) Prediction of metabolism by cytochrome P450 2C9: alignment and docking studies of a validated database of substrates. J. Med. Chem., 51 (4): 780-91. [PMID:18237107]
21. Turpeinen M, Zanger UM. (2012) Cytochrome P450 2B6: function, genetics, and clinical relevance. Drug Metabol Drug Interact, 27 (4): 185-97. [PMID:23152403]
22. 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]
23. 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]
24. 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]
25. Yamano S, Tatsuno J, Gonzalez FJ. (1990) The CYP2A3 gene product catalyzes coumarin 7-hydroxylation in human liver microsomes. Biochemistry, 29 (5): 1322-9. [PMID:2322567]
26. 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]
27. 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]
How to cite this family page
Database page citation:
CYP2 family. Accessed on 19/05/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=262.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: Enzymes. Br J Pharmacol. 174 Suppl 1: S272-S359.
