CYP3A

CYP3A
Identifiers
Aliases	CYP3A, cytochrome P450, family 3, subfamily A, CYP3
External IDs	GeneCards: CYP3A; OMA:CYP3A - orthologs
Orthologs Species Human Mouse Entrez 1574 n/a Ensembl n/a n/a UniProt n a n/a RefSeq (mRNA) NM_000775 n/a RefSeq (protein) n/a n/a Location (UCSC) n/a n/a PubMed search n/a
Wikidata
View/Edit Human

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

• Smith G, Stubbins MJ, Harries LW, Wolf CR (December 1998). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily". Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 28 (12): 1129–65. doi:10.1080/004982598238868. PMID 9890157.
• Lamba JK, Lin YS, Schuetz EG, Thummel KE (November 2002). "Genetic contribution to variable human CYP3A-mediated metabolism". Advanced Drug Delivery Reviews. 54 (10): 1271–94. doi:10.1016/S0169-409X(02)00066-2. PMID 12406645.
• Finta C, Zaphiropoulos PG (December 2000). "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.
• Miyazawa M, Shindo M, Shimada T (October 2001). "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. doi:10.1080/00498250110065595. PMID 11695850. S2CID 41495172.
• Reid JM, Kuffel MJ, Ruben SL, Morales JJ, Rinehart KL, Squillace DP, Ames MM (September 2002). "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. PMID 12231541.
• Martínez C, García-Martín E, Pizarro RM, García-Gamito FJ, Agúndez JA (September 2002). "Expression of paclitaxel-inactivating CYP3A activity in human colorectal cancer: implications for drug therapy". British Journal of Cancer. 87 (6): 681–6. doi:10.1038/sj.bjc.6600494. PMC 2364247. PMID 12237780.
• Dowling TC, Briglia AE, Fink JC, Hanes DS, Light PD, Stackiewicz L, Karyekar CS, Eddington ND, Weir MR, Henrich WL (May 2003). "Characterization of hepatic cytochrome p4503A activity in patients with end-stage renal disease". Clinical Pharmacology and Therapeutics. 73 (5): 427–34. doi:10.1016/S0009-9236(03)00056-0. PMID 12732843.
• Sunman JA, Hawke RL, LeCluyse EL, Kashuba AD (March 2004). "Kupffer cell-mediated IL-2 suppression of CYP3A activity in human hepatocytes". Drug Metabolism and Disposition. 32 (3): 359–63. doi:10.1124/dmd.32.3.359. PMID 14977871.
• Somogyi AA, Menelaou A, Fullston SV (October 2004). "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. doi:10.1080/00498250400008371. PMID 15764408. S2CID 7680532.
• Thompson EE, Kuttab-Boulos H, Yang L, Roe BA, Di Rienzo A (2006). "Sequence diversity and haplotype structure at the human CYP3A cluster". The Pharmacogenomics Journal. 6 (2): 105–14. doi:10.1038/sj.tpj.6500347. PMID 16314882.
• Bochud M, Eap CB, Elston RC, Bovet P, Maillard M, Schild L, Shamlaye C, Burnier M (May 2006). "Association of CYP3A5 genotypes with blood pressure and renal function in African families". Journal of Hypertension. 24 (5): 923–9. doi:10.1097/01.hjh.0000222763.84605.4a. PMID 16612255. S2CID 30703443.
• Cheung CY, Op den Buijsch RA, Wong KM, Chan HW, Chau KF, Li CS, Leung KT, Kwan TH, de Vrie JE, Wijnen PA, van Dieijen-Visser MP, Bekers O (June 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 (June 2006). "CYP3A phenotypes and genotypes in North Indians". European Journal of Clinical Pharmacology. 62 (6): 417–22. doi:10.1007/s00228-006-0105-3. PMID 16758258. S2CID 24149704.
• Kirby B, Kharasch ED, Thummel KT, Narang VS, Hoffer CJ, Unadkat JD (November 2006). "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 (November 2006). "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, Okazaki O, Sudo K (July 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 Metabolism and Disposition. 35 (7): 1232–8. doi:10.1124/dmd.107.015016. PMID 17392390. S2CID 11204475.
• Kharasch ED, Walker A, Isoherranen N, Hoffer C, Sheffels P, Thummel K, Whittington D, Ensign D (October 2007). "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. doi:10.1038/sj.clpt.6100237. PMID 17554244.