Luminogenic cytochrome P450 assays.

Abstract:

:Luminogenic cytochrome P450 (CYP) assays couple CYP enzyme activity to firefly luciferase luminescence in a technology called P450-Glo(TM) (Promega). Luminogenic substrates are used in assays of human CYP1A1, -1A2, -1B1, -2C8, -2C9, -2C19, -2D6, -2J2, -3A4, -3A7, -4A11, -4F3B, -4F12 and -19. The assays detect dose-dependent CYP inhibition by test compounds against recombinant CYP enzymes or liver microsomes. Induction or inhibition of CYP activities in cultured hepatocytes is measured in a nonlytic approach that leaves cells intact for additional analysis. Luminogenic CYP assays offer advantages of speed and safety over HPLC and radiochemical-based methods. Compared with fluorogenic methods the approach offers advantages of improved sensitivity and decreased interference between optical properties of test compound and CYP substrate. These homogenous assays are sensitive and robust tools for high-throughput CYP screening in early drug discovery.

authors

Cali JJ,Ma D,Sobol M,Simpson DJ,Frackman S,Good TD,Daily WJ,Liu D

doi

10.1517/17425255.2.4.629

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

629-45

issue

4

eissn

1742-5255

issn

1744-7607

journal_volume

2

pub_type

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