Frontiers in PROTACs

Hughes, Gregory R., Dudey, Ashley P., Hemmings, Andrew M. ORCID: and Chantry, Andrew (2021) Frontiers in PROTACs. Drug Discovery Today, 26 (10). pp. 2377-2383. ISSN 1359-6446

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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.

Item Type: Article
Uncontrolled Keywords: drug discovery,protacs,ubiquitin ligases,pharmacology,drug discovery ,/dk/atira/pure/subjectarea/asjc/3000/3004
Faculty \ School: Faculty of Science
Faculty of Science > School of Biological Sciences
Faculty of Science > School of Chemistry
UEA Research Groups: Faculty of Science > Research Groups > Chemistry of Life Processes
Faculty of Science > Research Centres > Centre for Molecular and Structural Biochemistry
Faculty of Science > Research Groups > Molecular Microbiology
Faculty of Science > Research Groups > Plant Sciences
Faculty of Science > Research Groups > Cells and Tissues
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Depositing User: LivePure Connector
Date Deposited: 20 Apr 2021 23:49
Last Modified: 21 Apr 2023 01:00
DOI: 10.1016/j.drudis.2021.04.010


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