A fluorescent cell-based assay for cytochrome P-450 isozyme 1A2 induction and inhibition

被引：28

作者：

Kelly, JH ^{[1
]}

Sussman, NL ^{[1
]}

机构：

[1] Amphioxus Cell Technol Inc, Houston, TX 77082 USA

来源：

JOURNAL OF BIOMOLECULAR SCREENING | 2000年 / 5卷 / 04期

关键词：

D O I：

10.1089/108705700416119

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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 ethoxyresorufin. Using methylcholanthrene, CYP1A2 can be induced dramatically, and it is inhibited by furafylline, a mechanism-based inhibitor of this enzyme.

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页码：249 / 253

页数：5

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