title: Bioluminescent assays for cytochrome P450 enzymes.
abstract: The cytochrome P450 (CYP) family contains 57 enzymes in humans. The activity of CYPs against xenobiotics is a primary consideration in drug optimization efforts. Here we describe a series of bioluminescent assays that enable the rapid profiling of CYP activity against compound collections. The assays employ a coupled-enzyme format where firefly luciferase is used to measure CYP enzyme activity through metabolism of pro-luciferase substrates.
authors.affiliation: Novartis Institutes for Biomedical Research, Cambridge, MA, USA.
authors.forename: Douglas S
authors.initials: DS
authors.lastname: Auld
authors.forename: Henrike
authors.initials: H
authors.lastname: Veith
authors.forename: James J
authors.initials: JJ
authors.lastname: Cali
mesh_terms: D000818:Animals; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D057075:Enzyme Assays / Q000379:methods*; D006801:Humans; D008163:Luminescent Measurements / Q000379:methods*; D011485:Protein Binding
chemical_list: D003577:Cytochrome P-450 Enzyme System