title: Measurement of in vitro cytochrome P450 2B6 activity.
abstract: Cytochrome P450 2B6 (CYP2B6) is responsible for the metabolism of a number of therapeutically relevant drugs and environmental chemicals. While not as frequently involved in xenobiotic metabolism as other more commonly studied P450 enzymes such as CYP3A, CYP2D6, or CYP2C9, its importance is becoming increasingly realized. Bupropion hydroxylase activity is an excellent indicator of in vitro CYP2B6 activity, and the metabolite formed is easily measured by HPLC/MS/MS. This assay allows the use of very low concentrations of human liver microsomes or recombinant enzyme, and it represents a selective, sensitive approach to assessing in vitro CYP2B6 activity, with minimal sample preparation.
authors.affiliation: Pfizer Global Research and Development, Groton, Connecticut, USA.
authors.forename: Robert L
authors.initials: RL
authors.lastname: Walsky
authors.forename: R Scott
authors.initials: RS
authors.lastname: Obach
mesh_terms: D001189:Aryl Hydrocarbon Hydroxylases / Q000032:analysis / Q000037:antagonists & inhibitors / Q000378:metabolism*; D001681:Biological Assay; D016642:Bupropion / Q000378:metabolism; D065702:Cytochrome P-450 CYP2B6; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D006900:Hydroxylation / Q000187:drug effects / Q000502:physiology; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*; D010084:Oxidation-Reduction; D010089:Oxidoreductases, N-Demethylating / Q000032:analysis / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D011994:Recombinant Proteins; D016642:Bupropion; D001189:Aryl Hydrocarbon Hydroxylases; C585599:CYP2B6 protein, human; D065702:Cytochrome P-450 CYP2B6; D010089:Oxidoreductases, N-Demethylating