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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.

SUBMITTER: Kim H

PROVIDER: S-EPMC8292994 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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Recent advances in the development of covalent inhibitors.

Kim Hyunsoo H Hwang Yoon Soo YS Kim Mingi M Park Seung Bum SB

RSC medicinal chemistry 20210504 7

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 li ...[more]

PMID: 34355176

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