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Review
. 2021 Oct;26(10):2377-2383.
doi: 10.1016/j.drudis.2021.04.010. Epub 2021 Apr 17.

Frontiers in PROTACs

Gregory R Hughes  1 , Ashley P Dudey  2 , Andrew M Hemmings  3 , Andrew Chantry  4
Affiliations
Review

Frontiers in PROTACs

Gregory R Hughes et al. Drug Discov Today. 2021 Oct.

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.

Keywords: Drug discovery; PROTACs; Ubiquitin ligases.

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Conflict of interest statement

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.

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