The ins and outs of selective kinase inhibitor development
The ins and outs of selective kinase inhibitor development
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DOI：
10.1038/nchembio.1938
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发表时间：
2015-11-01
影响因子：
14.8
通讯作者：
Knapp, Stefan
中科院分区：
文献类型：
--
作者：
Mueller, Susanne;Chaikuad, Apirat;Knapp, Stefan
蛋白激酶已成为最成功的药物靶标家族之一。迄今为止，大多数选择性激酶抑制剂都是通过广泛的选择性筛选或通过发现独特的结合模式偶然发现的。在这里，我们讨论的设计策略可能会导致选择性抑制剂更广泛地覆盖激酶组，并形成更合理的开发方法。
Protein kinases have emerged as one of the most successful families of drug targets. To date, most selective kinase inhibitors have been discovered serendipitously either through broad selectivity screening or through the discovery of unique binding modes. Here we discuss design strategies that could lead to a broader coverage of the kinome with selective inhibitors and to a more rational approach for developing them.