PROTAC-induced proteolytic targeting

Kimberly Cornish Carmony, Kyung Bo Kim

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

29 Scopus citations

Abstract

Small-molecule modulators of protein activity are increasingly being utilized as tools to examine the functional roles of proteins. Operating at the post-translational level, these molecules provide enhanced temporal and spatial control and mitigate the potential for compensatory responses in comparison with classical genetic approaches. Proteolysis targeting chimeric molecules, or PROTACs, are small molecules that inhibit the function of their target proteins by targeting them for degradation by the ubiquitin proteasome system. This chapter summarizes strategies for PROTAC preparation and characterization.

Original languageEnglish
Title of host publicationUbiquitin Family Modifiers and the Proteasome
Subtitle of host publicationReviews and Protocols
EditorsJurgen Dohmen, Martin Scheffner
Pages627-638
Number of pages12
DOIs
StatePublished - 2012

Publication series

NameMethods in Molecular Biology
Volume832
ISSN (Print)1064-3745

Keywords

  • Chemical genetics
  • E3 ubiquitin ligase
  • PROTAC
  • Proteasome
  • Protein degradation
  • Small molecule
  • Ubiquitin

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics

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