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Covalent PROTACs: the best of both worlds?

Neil P. Grimster

2021RSC Medicinal Chemistry48 citationsDOIOpen Access PDF

Abstract

Covalent PROTACs combine the cutting edge research areas of targeted covalent inhibitors (TCIs) and proteolysis targeting chimeras (PROTACs). This nascent field of research has already demonstrated several interesting findings, and holds an immense amount of potential to expand the druggable proteome. In this opinion, we present some of these intriguing early findings and discuss the potential advantages and disadvantages of this approach.

Topics & Concepts

Covalent bondProteolysisChemistryBiochemistryOrganic chemistryEnzymeProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysCAR-T cell therapy research
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