在共价抑制剂的开发中药物发现的考虑因素。
Drug discovery considerations in the development of covalent inhibitors.
机构信息
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, Klybeckstrasse 141, CH-4057 Basel, Switzerland.
Developmental and Molecular Pathways, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA.
出版信息
Bioorg Med Chem Lett. 2014 Jan 1;24(1):33-9. doi: 10.1016/j.bmcl.2013.10.003. Epub 2013 Oct 10.
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.
近年来，具有共价作用机制的候选药物数量在临床试验中取得进展或被 FDA 批准的数量显著增加。随着对共价抑制剂的兴趣增加，用于表征和优化这些抑制剂的技术挑战变得明显。已经开发了许多新工具来辅助这个过程，但这些工具并没有得到广泛应用。这篇综述将重点介绍一些在进行共价抑制剂药物发现项目时有用的方法和工具。
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