Drug discovery considerations in the development of covalent inhibitors
Drug discovery considerations in the development of covalent inhibitors
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DOI：
10.1016/j.bmcl.2013.10.003
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发表时间：
2014-01-01
影响因子：
2.7
通讯作者：
Shafer, Cynthia M.
中科院分区：
文献类型：
--
作者：
Mah, Robert;Thomas, Jason R.;Shafer, Cynthia M.
近年来，通过临床试验或被FDA批准的具有共价作用机制的候选药物的数量显著增加。随着对共价抑制剂的兴趣增加，表征和优化这些抑制剂的技术挑战变得显而易见。已经开发了一些新的工具来帮助这一过程，但这些工具尚未得到广泛使用。这篇评论将突出一些方法和工具，用于起诉共价抑制剂药物发现计划。(C)2013作者由爱思唯尔有限公司出版。保留所有权利。
In recent years, the number of drug candidates with a covalent mechanism of action progressing through clinical trials or being approved by the FDA has increased significantly. And as interest in covalent inhibitors has increased, the technical challenges for characterizing and optimizing these inhibitors have become evident. A number of new tools have been developed to aid this process, but these have not gained wide-spread use. This review will highlight a number of methods and tools useful for prosecuting covalent inhibitor drug discovery programs. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.