FLUORESCENCE-BASED ASSAYS FOR SCREENING NINE CYTOCHROME P450 (P450) ACTIVITIES IN INTACT CELLS EXPRESSING INDIVIDUAL HUMAN P450 ENZYMES

• Published in: Drug metabolism and disposition Vol. 32; no. 7; pp. 699 - 706
• Main Authors: Donato, M Teresa, Jiménez, Nuria, Castell, José V, Gómez-Lechón, M José
• Format: Journal Article
• Language: English
• Published: Bethesda, MD American Society for Pharmacology and Experimental Therapeutics 01.07.2004
• Subjects: Analytical, structural and metabolic biochemistry; Biological and medical sciences; Cells, Cultured; Cytochrome P-450 Enzyme System - metabolism; Enzymes and enzyme inhibitors; Fluorescent Dyes; Fluorometry - methods; Fundamental and applied biological sciences. Psychology; Hepatocytes - enzymology; Humans; Microsomes, Liver - enzymology; Oxidoreductases; Time Factors; Screening; Enzymatic activity; Enzyme; Isozyme; Cytochrome P450; Fluorescence; Measurement method; In vitro

In this study we describe a battery of fluorescence assays for rapid measurement in intact cells of the activity of nine cytochromes P450 (P450s) involved in drug metabolism. The assays are based on the direct incubation of monolayers of cells expressing individual P450 enzymes with a fluorogenic su...