High-throughput kinase profiling as a platform for drug discovery

被引:167
作者
Goldstein, David M. [2 ]
Gray, Nathanael S. [3 ]
Zarrinkar, Patrick P. [1 ]
机构
[1] Ambit Biosci, San Diego, CA 92121 USA
[2] Roche Palo Alto, Palo Alto, CA 94304 USA
[3] Harvard Univ, Sch Med, Dana Farber Canc Inst, Boston, MA 02115 USA
关键词
D O I
10.1038/nrd2541
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
To fully exploit the potential of kinases as drug targets, novel strategies for the efficient discovery of inhibitors are required. In contrast to the traditional, linear process of inhibitor discovery, high-throughput kinase profiling enables a parallel approach by interrogating compounds against hundreds of targets in a single screen. Compound potency and selectivity are determined simultaneously, providing a choice of targets to pursue that is guided by the quality of lead compounds available, rather than by target biology alone.
引用
收藏
页码:391 / 397
页数:7
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