Goldstein David M, Gray Nathanael S, Zarrinkar Patrick P
Roche Palo Alto, 3431 Hillview Avenue, R6-201, Palo Alto, California 94304, USA.
Nat Rev Drug Discov. 2008 May;7(5):391-7. doi: 10.1038/nrd2541.
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.
为了充分发挥激酶作为药物靶点的潜力,需要有高效发现抑制剂的新策略。与传统的线性抑制剂发现过程不同,高通量激酶谱分析通过在一次筛选中针对数百个靶点检测化合物,实现了一种并行方法。同时确定化合物的效力和选择性,根据现有先导化合物的质量而非仅依据靶点生物学来选择要研究的靶点。