In vivo synthetic chemistry of proteolysis targeting chimeras (PROTACs)

Research output: Contribution to journalReview articlepeer-review

Abstract

Chemical knockdown of therapeutic targets using proteolysis targeting chimeras (PROTACs) is a rapidly developing field in drug discovery, but PROTACs are bifunctional molecules that generally show poor bioavailability due to their relatively high molecular weight. Recent developments aimed at the development of next-generation PROTACs include the in vivo synthesis of PROTAC molecules, and the exploitation of PROTACs as chemical tools for in vivo synthesis of ubiquitinated proteins. This short review covers recent advances in these areas and discusses the prospects for in vivo synthetic PROTAC technology.

Original languageEnglish
Article number116221
JournalBioorganic and Medicinal Chemistry
Volume41
DOIs
Publication statusPublished - 2021 Jul 1

Keywords

  • CLIPTACs
  • Chemical protein knockdown
  • In vivo synthetic chemistry
  • PROTACs
  • Ubiquitination

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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