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

共 85 条

[1]

Adams Deanna G, 2008, Curr Chem Genomics, V1, P54, DOI 10.2174/1875397300801010054

[2] Enzyme-linked immunosorbent assay for trkA tyrosine kinase activity [J].

Angeles, TS ;

Steffler, C ;

Bartlett, BA ;

Hudkins, RL ;

Stephens, RM ;

Kaplan, DR ;

Dionne, CA .

ANALYTICAL BIOCHEMISTRY, 1996, 236 (01) :49-55

[3] Miniaturized, ultra-high throughput screening of tyrosine kinases using homogeneous, competitive fluorescence immunoassays [J].

Beasley, JR ;

McCoy, PM ;

Walker, TL ;

Dunn, DA .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2004, 2 (02) :141-151

[4] Oncogenic kinase signalling [J].

Blume-Jensen, P ;

Hunter, T .

NATURE, 2001, 411 (6835) :355-365

[5] Tyrosine protein kinase assays [J].

Boutin, JA .

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES, 1996, 684 (1-2) :179-199

[6] Development and application of fluorescence polarization assays in drug discovery [J].

Burke, TJ ;

Loniello, KR ;

Beebe, JA ;

Ervin, KM .

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, 2003, 6 (03) :183-194

[7] Identification of small-molecule inhibitors of protein kinase B (PKB/AKT) in an AlphaScreen™ high-throughput screen [J].

Burns, Samantha ;

Travers, Jonathan ;

Collins, Ian ;

Rowlands, Martin G. ;

Newbatt, Yvette ;

Thompson, Neil ;

Garrett, Michelle D. ;

Workman, Paul ;

Aherne, Wynne .

JOURNAL OF BIOMOLECULAR SCREENING, 2006, 11 (07) :822-827

[8] Tyrosine kinase inhibitors: Rationale, mechanisms of action, and implications for drug resistance [J].

Busse, D ;

Yakes, FM ;

Lenferink, AEG ;

Arteaga, CL .

SEMINARS IN ONCOLOGY, 2001, 28 (05) :47-55

[9] Image-based chemical screening [J].

Carpenter, Anne E. .

NATURE CHEMICAL BIOLOGY, 2007, 3 (08) :461-465

[10] A generic, homogenous method for measuring kinase and inhibitor activity via adenosine 5′-diphosphate accumulation [J].

Charter, Neil W. ;

Kauffman, Lindy ;

Singh, Raj ;

Eglen, Richard M. .

JOURNAL OF BIOMOLECULAR SCREENING, 2006, 11 (04) :390-399

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