期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 1, 页码 33-39出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.10.003
关键词
Covalent inhibitor; Targeted covalent inhibitor (TCI); Mechanism-based inhibitor; k(inact)/K-i; Warhead reactivity; Activity-based protein profiling (ABPP); Click chemistry
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.
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