Article
Investigation of the mechanisms underlying the differential effects of the K262R mutation of P450 2B6 on catalytic activity.
Molecular pharmacology - 1 Oct 2008
Bumpus Namandjé N, Hollenberg Paul F
Abstract excerpt
Human P450 2B6 is a polymorphic enzyme involved in the oxidative metabolism of a number of clinically relevant substrates. The lysine 262-to-arginine mutant of cytochrome P450 2B6 (P450 2B6.4) has been shown to have differential effects on P450 2B6 catalytic activity. We reported previously that the mutant enzyme was unable to metabolize 17-alpha-ethynylestradiol (17EE) or become inactivated by 17EE or efavirenz,...
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