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Lead discovery and chemical biology approaches targeting the ubiquitin proteasome system.

Authors
  • Akinjiyan, Favour A1
  • Carbonneau, Seth1
  • Ross, Nathan T2
  • 1 Department of Chemical Biology and Therapeutics, Novartis Institute for Biomedical Research, 181 Massachusetts Avenue, Cambridge, MA 02139, USA.
  • 2 Department of Chemical Biology and Therapeutics, Novartis Institute for Biomedical Research, 181 Massachusetts Avenue, Cambridge, MA 02139, USA. Electronic address: [email protected]
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Oct 15, 2017
Volume
27
Issue
20
Pages
4589–4596
Identifiers
DOI: 10.1016/j.bmcl.2017.08.058
PMID: 28911816
Source
Medline
Keywords
License
Unknown

Abstract

Protein degradation is critical for proteostasis, and the addition of polyubiquitin chains to a substrate is necessary for its recognition by the 26S proteasome. Therapeutic intervention in the ubiquitin proteasome system has implications ranging from cancer to neurodegeneration. Novel screening methods and chemical biology tools for targeting E1-activating, E2-conjugating and deubiquitinating enzymes will be discussed in this review. Approaches for targeting E3 ligase-substrate interactions as well as the proteasome will also be covered, with a focus on recently described approaches.

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