Measuring the tyrosine kinase activity: a review of biochemical and cellular assay technologies

被引：16

作者：

Jia, Yong ^{[1
]}

Gu, Xiang-Ju ^{[2
]}

Brinker, Achim ^{[2
]}

Warmuth, Markus ^{[1
]}

机构：

[1] Genom Inst Novartis Res Fdn, Dept Kinase Biol, San Diego, CA 92121 USA

[2] Genom Inst Novartis Res Fdn, Dept Lead Discovery, San Diego, CA 92121 USA

来源：

EXPERT OPINION ON DRUG DISCOVERY | 2008年 / 3卷 / 08期

关键词：

assay; biochemical; cellular; phospho-specific antibodies; radiometric; tyrosine kinase;

D O I：

10.1517/17460441.3.8.959

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Background: The increasing number of kinases as potential drug targets, in combination with the need to screen large compound collections, demands the kinase assays to be homogeneous, non-radioactive, robust, sensitive, easy to miniaturize, and high-throughput. Objective: This review will focus on some of the chief biochemical and cellular kinase assay technologies and their applications in tyrosine kinase drug discovery. Methods: Recent literatures on these tyrosine kinase assay technologies are reviewed, each assay principle, advantages and drawbacks, as well as their potential utilities in tyrosine kinase drug discovery are discussed. Results/conclusion: There is no perfect assay yet; the choice of assay technology relies on the consideration of many factors including the intrinsic properties of the assay, intended application, cost, timeline, synergy with other in-house assay technologies and the expertise, familiarity and comfort level with certain technologies.

引用

页码：959 / 978

页数：20

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