Biology:CYP3A

Short description: Human gene

Generic protein structure example

Cytochrome P450, family 3, subfamily A, also known as CYP3A, is a human gene locus. A homologous locus is found in mice.

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:

• CYP3A4,
• CYP3A5,
• CYP3A7, and
• CYP3A43.

The region also contains four pseudogenes:

• CYP3A51P,
• CYP3A52P,
• CYP3A54P, and
• CYP3A137P.

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.

Further reading

• "Molecular genetics of the human cytochrome P450 monooxygenase superfamily". Xenobiotica; the Fate of Foreign Compounds in Biological Systems 28 (12): 1129–65. December 1998. doi:10.1080/004982598238868. PMID 9890157. 
• "Genetic contribution to variable human CYP3A-mediated metabolism". Advanced Drug Delivery Reviews 54 (10): 1271–94. November 2002. doi:10.1016/S0169-409X(02)00066-2. PMID 12406645. 
• "The human cytochrome P450 3A locus. Gene evolution by capture of downstream exons". Gene 260 (1–2): 13–23. December 2000. doi:10.1016/S0378-1119(00)00470-4. PMID 11137287. 
• "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; the Fate of Foreign Compounds in Biological Systems 31 (10): 713–23. October 2001. doi:10.1080/00498250110065595. PMID 11695850. 
• "Rat and human liver cytochrome P-450 isoform metabolism of ecteinascidin 743 does not predict gender-dependent toxicity in humans". Clinical Cancer Research 8 (9): 2952–62. September 2002. PMID 12231541. 
• "Expression of paclitaxel-inactivating CYP3A activity in human colorectal cancer: implications for drug therapy". British Journal of Cancer 87 (6): 681–6. September 2002. doi:10.1038/sj.bjc.6600494. PMID 12237780. 
• "Characterization of hepatic cytochrome p4503A activity in patients with end-stage renal disease". Clinical Pharmacology and Therapeutics 73 (5): 427–34. May 2003. doi:10.1016/S0009-9236(03)00056-0. PMID 12732843. 
• "Kupffer cell-mediated IL-2 suppression of CYP3A activity in human hepatocytes". Drug Metabolism and Disposition 32 (3): 359–63. March 2004. doi:10.1124/dmd.32.3.359. PMID 14977871. 
• "CYP3A4 mediates dextropropoxyphene N-demethylation to nordextropropoxyphene: human in vitro and in vivo studies and lack of CYP2D6 involvement". Xenobiotica; the Fate of Foreign Compounds in Biological Systems 34 (10): 875–87. October 2004. doi:10.1080/00498250400008371. PMID 15764408. 
• "Sequence diversity and haplotype structure at the human CYP3A cluster". The Pharmacogenomics Journal 6 (2): 105–14. 2006. doi:10.1038/sj.tpj.6500347. PMID 16314882. 
• "Association of CYP3A5 genotypes with blood pressure and renal function in African families". Journal of Hypertension 24 (5): 923–9. May 2006. doi:10.1097/01.hjh.0000222763.84605.4a. PMID 16612255. 
• "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. June 2006. doi:10.2217/14622416.7.4.563. PMID 16753004. 
• "CYP3A phenotypes and genotypes in North Indians". European Journal of Clinical Pharmacology 62 (6): 417–22. June 2006. doi:10.1007/s00228-006-0105-3. PMID 16758258. 
• "Simultaneous measurement of in vivo P-glycoprotein and cytochrome P450 3A activities". Journal of Clinical Pharmacology 46 (11): 1313–9. November 2006. doi:10.1177/0091270006292625. PMID 17050796. 
• "Human pregnane X receptor: genetic polymorphisms, alternative mRNA splice variants, and cytochrome P450 3A metabolic activity". Journal of Clinical Pharmacology 46 (11): 1356–69. November 2006. doi:10.1177/0091270006292125. PMID 17050801. 
• "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 Metabolism and Disposition 35 (7): 1232–8. July 2007. doi:10.1124/dmd.107.015016. PMID 17392390. 
• "Influence of CYP3A5 genotype on the pharmacokinetics and pharmacodynamics of the cytochrome P4503A probes alfentanil and midazolam". Clinical Pharmacology and Therapeutics 82 (4): 410–26. October 2007. doi:10.1038/sj.clpt.6100237. PMID 17554244.