细胞色素P450酶的生物发光测定法。

Bioluminescent assays for cytochrome P450 enzymes.

作者信息

Auld Douglas S, Veith Henrike, Cali James J

机构信息

Novartis Institutes for Biomedical Research, Cambridge, MA, USA.

出版信息

Methods Mol Biol. 2013;987:1-9. doi: 10.1007/978-1-62703-321-3_1.

DOI:10.1007/978-1-62703-321-3_1

PMID:23475663

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.

摘要

细胞色素P450（CYP）家族在人类中包含57种酶。CYP对异生素的活性是药物优化工作中的一个主要考虑因素。在此，我们描述了一系列生物发光测定法，这些方法能够快速分析CYP针对化合物库的活性。这些测定法采用偶联酶形式，其中萤火虫荧光素酶用于通过前体荧光素酶底物的代谢来测量CYP酶活性。