1. Frontiers in PROTACs.
- Author
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Hughes GR, Dudey AP, Hemmings AM, and Chantry A
- Subjects
- Drug Discovery methods, Humans, Proteasome Endopeptidase Complex metabolism, Proteolysis, Drug Development methods, Molecular Targeted Therapy, Proteins metabolism
- Abstract
Targeting protein-protein interactions (PPI) is a key focus in the development of new and emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI targeting notoriously difficult. This leaves many therapeutically captivating targets 'undruggable'. Despite these challenges, there has been extraordinary progress circumventing this issue by hijacking the ubiquitin proteasome system (UPS) to target selected substrates for destruction using target-based degradation (TBD) strategies, including bifunctional molecules known as proteolysis-targeting chimeras (PROTACs). In this review, we discuss some of the most recent innovative concepts emerging from PROTAC research and related technologies., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2021 Elsevier Ltd. All rights reserved.)
- Published
- 2021
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