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The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

Authors :
Kristin M. Riching
Elizabeth A. Caine
Marjeta Urh
Danette L. Daniels
Source :
Chemical Society Reviews. 51:6210-6221
Publication Year :
2022
Publisher :
Royal Society of Chemistry (RSC), 2022.

Abstract

Targeted protein degradation has exploded over the past several years due to preclinical and early clinical therapeutic success of numerous compounds, and the emergence of new degradation modalities, which has broadened the definition of what a degrader is. The most characterized and well-studied small molecule degraders are molecular glues and proteolysis targeting chimeras (PROTACs). These degraders induce a ternary complex between a target protein, degrader, and E3 ligase component, resulting in ubiquitination and subsequent degradation of the target protein

Details

ISSN :
14604744 and 03060012
Volume :
51
Database :
OpenAIRE
Journal :
Chemical Society Reviews
Accession number :
edsair.doi.dedup.....b10ef2acdb517d73a1cf6815ee34b30b
Full Text :
https://doi.org/10.1039/d2cs00339b