| Literature DB >> 33799000 |
William Farnaby1, Manfred Koegl2, Darryl B McConnell3, Alessio Ciulli4.
Abstract
Small-molecule targeted protein degraders have in recent years made a great impact on the strategies of many industry and academic cancer research endeavours. We seek here to provide a concise perspective on the opportunities and challenges that lie ahead for bifunctional degrader molecules, so-called 'Proteolysis Targeting Chimeras (PROTACs),' in the context of cancer therapy. We highlight high-profile studies that support the potential for PROTAC approaches to broaden drug target scope, address drug resistance, enhance target selectivity and provide tissue specificity, but also assess where the modality is yet to fully deliver in these contexts. Future opportunities presented by the unique bifunctional nature of these molecules are also discussed.Entities:
Keywords: Bifunctional molecules; Cancer; Drug discovery; Drug resistance; PROTACs; Target selectivity; Targeted protein degradation
Year: 2021 PMID: 33799000 DOI: 10.1016/j.coph.2021.02.009
Source DB: PubMed Journal: Curr Opin Pharmacol ISSN: 1471-4892 Impact factor: 5.547