Recent advances in the development of covalent inhibitors,RSC Medicinal Chemistry

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Recent advances in the development of covalent inhibitors
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-5-4 , DOI: 10.1039/d1md00068c
Hyunsoo Kim ₁ , Yoon Soo Hwang ₁ , Mingi Kim ₁ , Seung Bum Park _{1,

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Affiliation

The use of covalent inhibitors in the field of drug discovery has attracted considerable attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market, and numerous covalent drug candidates are now under development. Therefore, interest in covalent drugs is expected to continue in the future. The purpose of this focused review is to provide an understanding of the development of covalent inhibitors by describing their inherent characteristics, possibilities, and limitations based on their mechanistic differences from noncovalent inhibitors. We also introduce the latest covalent warheads that can be applied to the development of potential covalent inhibitors.

中文翻译：

共价抑制剂开发的最新进展

共价抑制剂在药物发现领域的使用在 2000 年代引起了相当大的关注。因此，目前市场上有 50 多种共价药物，许多共价药物候选药物正在开发中。因此，预计未来对共价药物的兴趣将继续存在。这篇重点综述的目的是通过描述共价抑制剂的固有特征、可能性和限制，基于它们与非共价抑制剂的机制差异，提供对共价抑制剂发展的理解。我们还介绍了可用于开发潜在共价抑制剂的最新共价弹头。

更新日期：2021-05-04

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