CYP3A
Cytochrome P450, family 3, subfamily A, also known as CYP3A, is a human gene.[1]
The CYP3A locus includes all the known members of the 3A subfamily of the cytochrome P450 superfamily of genes. These genes encode monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. The CYP3A cluster consists of four genes:
The region also contains two pseudogenes:
as well as several extra exons which may or may not be included in transcripts produced from this region. Previously another CYP3A member, CYP3A3, was thought to exist; however, it is now thought that this sequence represents a transcript variant of CYP3A4.[1]
References
Further reading
- Smith G, Stubbins MJ, Harries LW, Wolf CR (1999). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily". Xenobiotica. 28 (12): 1129–65. doi:10.1080/004982598238868. PMID 9890157.
- Lamba JK, Lin YS, Schuetz EG, Thummel KE (2003). "Genetic contribution to variable human CYP3A-mediated metabolism". Adv. Drug Deliv. Rev. 54 (10): 1271–94. doi:10.1016/S0169-409X(02)00066-2. PMID 12406645.
- Finta C, Zaphiropoulos PG (2001). "The human cytochrome P450 3A locus. Gene evolution by capture of downstream exons". Gene. 260 (1–2): 13–23. doi:10.1016/S0378-1119(00)00470-4. PMID 11137287.
- Gellner K, Eiselt R, Hustert E, et al. (2001). "Genomic organization of the human CYP3A locus: identification of a new, inducible CYP3A gene". Pharmacogenetics. 11 (2): 111–21. doi:10.1097/00008571-200103000-00002. PMID 11266076.
- Miyazawa M, Shindo M, Shimada T (2002). "Roles of cytochrome P450 3A enzymes in the 2-hydroxylation of 1,4-cineole, a monoterpene cyclic ether, by rat and human liver microsomes". Xenobiotica. 31 (10): 713–23. doi:10.1080/00498250110065595. PMID 11695850.
- Reid JM, Kuffel MJ, Ruben SL, et al. (2002). "Rat and human liver cytochrome P-450 isoform metabolism of ecteinascidin 743 does not predict gender-dependent toxicity in humans". Clin. Cancer Res. 8 (9): 2952–62. PMID 12231541.
- Martínez C, García-Martín E, Pizarro RM, et al. (2002). "Expression of paclitaxel-inactivating CYP3A activity in human colorectal cancer: implications for drug therapy". Br. J. Cancer. 87 (6): 681–6. doi:10.1038/sj.bjc.6600494. PMC 2364247. PMID 12237780.
- Dowling TC, Briglia AE, Fink JC, et al. (2003). "Characterization of hepatic cytochrome p4503A activity in patients with end-stage renal disease". Clin. Pharmacol. Ther. 73 (5): 427–34. doi:10.1016/S0009-9236(03)00056-0. PMID 12732843.
- Sunman JA, Hawke RL, LeCluyse EL, Kashuba AD (2004). "Kupffer cell-mediated IL-2 suppression of CYP3A activity in human hepatocytes". Drug Metab. Dispos. 32 (3): 359–63. doi:10.1124/dmd.32.3.359. PMID 14977871.
- Somogyi AA, Menelaou A, Fullston SV (2005). "CYP3A4 mediates dextropropoxyphene N-demethylation to nordextropropoxyphene: human in vitro and in vivo studies and lack of CYP2D6 involvement". Xenobiotica. 34 (10): 875–87. doi:10.1080/00498250400008371. PMID 15764408.
- Thompson EE, Kuttab-Boulos H, Yang L, et al. (2006). "Sequence diversity and haplotype structure at the human CYP3A cluster". Pharmacogenomics J. 6 (2): 105–14. doi:10.1038/sj.tpj.6500347. PMID 16314882.
- Bochud M, Eap CB, Elston RC, et al. (2006). "Association of CYP3A5 genotypes with blood pressure and renal function in African families". J. Hypertens. 24 (5): 923–9. doi:10.1097/01.hjh.0000222763.84605.4a. PMID 16612255.
- Cheung CY, Op den Buijsch RA, Wong KM, et al. (2006). "Influence of different allelic variants of the CYP3A and ABCB1 genes on the tacrolimus pharmacokinetic profile of Chinese renal transplant recipients". Pharmacogenomics. 7 (4): 563–74. doi:10.2217/14622416.7.4.563. PMID 16753004.
- Rais N, Chawla YK, Kohli KK (2007). "CYP3A phenotypes and genotypes in North Indians". Eur. J. Clin. Pharmacol. 62 (6): 417–22. doi:10.1007/s00228-006-0105-3. PMID 16758258.
- Kirby B, Kharasch ED, Thummel KT, et al. (2007). "Simultaneous measurement of in vivo P-glycoprotein and cytochrome P450 3A activities". Journal of clinical pharmacology. 46 (11): 1313–9. doi:10.1177/0091270006292625. PMID 17050796.
- He P, Court MH, Greenblatt DJ, von Moltke LL (2007). "Human pregnane X receptor: genetic polymorphisms, alternative mRNA splice variants, and cytochrome P450 3A metabolic activity". Journal of clinical pharmacology. 46 (11): 1356–69. doi:10.1177/0091270006292125. PMID 17050801.
- Watanabe A, Nakamura K, Okudaira N, et al. (2007). "Risk assessment for drug-drug interaction caused by metabolism-based inhibition of CYP3A using automated in vitro assay systems and its application in the early drug discovery process". Drug Metab. Dispos. 35 (7): 1232–8. doi:10.1124/dmd.107.015016. PMID 17392390.
- Kharasch ED, Walker A, Isoherranen N, et al. (2007). "Influence of CYP3A5 genotype on the pharmacokinetics and pharmacodynamics of the cytochrome P4503A probes alfentanil and midazolam". Clin. Pharmacol. Ther. 82 (4): 410–26. doi:10.1038/sj.clpt.6100237. PMID 17554244.
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CYP1 | |
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CYP2 | |
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CYP3 (CYP3A) | |
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CYP4 | |
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CYP5-20 | |
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CYP21-51 | |
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Activity | |
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Regulation | |
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Classification | |
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Types | |
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