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Journal of Biomolecular Screening
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*Compound via MeSH
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*3-METHYLCHOLANTHRENE
*THEOPHYLLINE
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A Fluorescent Cell-Based Assay for Cytochrome P-450 Isozyme 1A2 Induction and Inhibition

James H. Kelly

Amphioxus Cell Technologies, Inc., Houston, TX

Norman L. Sussman

Amphioxus Cell Technologies, Inc., Houston, TX

High throughput lead optimization requires simple, homogeneous cell-based assays capable of defining the drug-like properties of first-round screening hits. Induction and inhibition of the Phase I drug-metabolizing enzymes are central to this process. We report here an assay for induction and inhibition of cytochrome P-450 (CYP) isozyme 1A2 that meets these requirements. It utilizes HepG2/C3A, a human liver cell line, and ethoxyresorufiln. Using methylcholanthrene, CYP1A2 can be induced dramatically, and it is inhibited by furafylline, a mechanism-based inhibitor of this enzyme.

Journal of Biomolecular Screening, Vol. 5, No. 4, 249-253 (2000)
DOI: 10.1177/108705710000500407
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