Proteasome inhibitors recent progress and future directions

Marie Wehenkel, Yik Khuan Ho, Kyung Bo Kim

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

3 Scopus citations

Abstract

The proteasome continues to be an attractive target for cancer drug discovery and was validated as such by the successful development of bortezomib. Despite its remarkable efficacy, concerns regarding side effects and drug resistance limit the widespread application of bortezomib. Thus, there has been a heightened interest in the development of a new class of proteasome inhibitors. In this chapter, we discuss recent efforts towards the development of proteasome inhibitors. In addition, we discuss a novel class of compounds targeting an alternative proteasome, the immunoproteasome.

Original languageEnglish
Title of host publicationModulation of Protein Stability in Cancer Therapy
Pages99-119
Number of pages21
DOIs
StatePublished - 2009

Keywords

  • Catalytic β-subunits
  • Immunoproteasome-specific inhibitors, Activity-based probes
  • N-terminal nucleophile protease
  • Pharmacophores
  • Proteasome inhibitors
  • Subunit-specific inhibitors
  • Ubiquitin-proteasome system

ASJC Scopus subject areas

  • General Biochemistry, Genetics and Molecular Biology

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