Issue 22, 2022

Applications of covalent chemistry in targeted protein degradation

Abstract

Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are currently two exciting strategies in the fields of chemical biology and drug discovery. Extensive research in these two fields has been conducted, and significant progress in these fields has resulted in many clinical candidates, some of which have been approved by FDA. Recently, a novel concept termed covalent PROTACs that combine these two strategies has emerged and gained an increasing interest in the past several years. Herein, we briefly review and highlight the mechanism and advantages of TCIs and PROTACs, respectively, and the recent development of covalent PROTACs using irreversible and reversible covalent chemistry.

Graphical abstract: Applications of covalent chemistry in targeted protein degradation

Article information

Article type
Review Article
Submitted
09 may. 2022
First published
26 oct. 2022

Chem. Soc. Rev., 2022,51, 9243-9261

Applications of covalent chemistry in targeted protein degradation

D. Lu, X. Yu, H. Lin, R. Cheng, E. Y. Monroy, X. Qi, M. C. Wang and J. Wang, Chem. Soc. Rev., 2022, 51, 9243 DOI: 10.1039/D2CS00362G

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