Publication Date
11-14-2022
Journal
Chemical Society Reviews
DOI
10.1039/d2cs00362g
PMID
36285735
PMCID
PMC9669245
PubMedCentral® Posted Date
11-14-2023
PubMedCentral® Full Text Version
Author MSS
Published Open-Access
yes
Keywords
Proteolysis, Ubiquitin-Protein Ligases, Drug Discovery
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.
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