Cytochrome P450 2C8: substrates, inhibitors, pharmacogenetics, and clinical relevance.
Cytochrome P450 (CYP) 2C8 [corrected] has been a relatively neglected member of the human CYP2C family. Over the period from 2000 through 2003, PubMed searches with the key word CYP2C8 returned only 10% to 15% of the citations obtained for all of the CYP2C enzymes combined. However, in the past year a crystal structure for CYP2C8 has been described, new inhibitors and probe substrates for the enzyme have been in development, the first case study was published linking CYP2C8 genetic polymorphisms to a disease state, and there has been an increasing awareness of the role that CYP2C8 plays in the disposition of therapeutic agents, especially from the pharmacogenetic and drug-drug interaction perspectives. This report discusses baseline characteristics of the enzyme and summarizes recent developments in these areas and their clinical relevance.
Totah
Rheem A
RA
Department of Medicinal Chemistry, University of Washington, Seattle, WA 98195, USA.
Rettie
Allan E
AE
D001189:Aryl Hydrocarbon Hydroxylases / Q000037:antagonists & inhibitors* / Q000235:genetics* / Q000378:metabolism; D065727:Cytochrome P-450 CYP2C8; D006801:Humans; D010597:Pharmacogenetics; D011110:Polymorphism, Genetic / Q000187:drug effects / Q000235:genetics
D001189:Aryl Hydrocarbon Hydroxylases; C450259:CYP2C8 protein, human; D065727:Cytochrome P-450 CYP2C8