Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

William Farnaby (Lead / Corresponding author), Manfred Koegl (Lead / Corresponding author), Darryl B. McConnell, Alessio Ciulli

Research output: Contribution to journalReview articlepeer-review

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.

Original languageEnglish
Pages (from-to)175-183
Number of pages9
JournalCurrent Opinion in Pharmacology
Volume57
Early online date30 Mar 2021
DOIs
Publication statusPublished - Apr 2021

Keywords

  • Targeted protein degradation
  • PROTACs
  • Cancer
  • Bifunctional molecules
  • Drug discovery
  • Target selectivity
  • Drug resistance

Fingerprint Dive into the research topics of 'Transforming targeted cancer therapy with PROTACs: A forward-looking perspective'. Together they form a unique fingerprint.

Cite this