title: Cytochrome p450 assays.
abstract: Cytochrome P450s (CYPs) play a major role in drug detoxification, and inhibition of CYP-mediated metabolism may lead to accumulation of toxic drug levels in the plasma. To prevent adverse drug-drug interactions, new drug candidates are routinely tested for their ability to inhibit these enzymes. This unit describes a variety of protocols for evaluating new chemical entities as inhibitors of CYP activity. An example protocol illustrates a high-throughput screening format using a fluorogenic probe, and a method for evaluating a test compound as a time-dependent inhibitor of CYP is also described.
authors.affiliation: Merck Research Labs, West Point, Pennsylvania, USA.
authors.forename: Enock
authors.initials: E
authors.lastname: Delaporte
authors.forename: A David
authors.initials: AD
authors.lastname: Rodrigues
mesh_terms: D000818:Animals; D003374:Coumarins / Q000494:pharmacology; D065607:Cytochrome P-450 Enzyme Inhibitors; D003915:Dextromethorphan / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D008617:Mephenytoin / Q000494:pharmacology; D017239:Paclitaxel / Q000494:pharmacology; D010615:Phenacetin / Q000494:pharmacology; D013739:Testosterone / Q000494:pharmacology
chemical_list: D003374:Coumarins; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D013739:Testosterone; D003915:Dextromethorphan; C030123:coumarin; D010615:Phenacetin; D017239:Paclitaxel; D008617:Mephenytoin