Issue 7, 2021

Recent advances in the development of covalent inhibitors

Abstract

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.

Graphical abstract: Recent advances in the development of covalent inhibitors

Article information

Article type
Review Article
Submitted
03 mar 2021
Accepted
23 apr 2021
First published
04 maj 2021

RSC Med. Chem., 2021,12, 1037-1045

Recent advances in the development of covalent inhibitors

H. Kim, Y. S. Hwang, M. Kim and S. B. Park, RSC Med. Chem., 2021, 12, 1037 DOI: 10.1039/D1MD00068C

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