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Related Experiment Videos

WD40 repeat domain proteins: a novel target class?

Matthieu Schapira1,2, Mike Tyers3,4, Maricel Torrent5

  • 1Structural Genomics Consortium, University of Toronto, Toronto, 101 College St, MaRS South Tower, Suite 700, Ontario M5G 1L7, Canada.

Nature Reviews. Drug Discovery
|October 14, 2017
PubMed
Summary

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This summary is machine-generated.

Targeting WD40 repeat domains with small molecules shows promise for drug discovery. These abundant protein domains, involved in disease pathways, offer new therapeutic opportunities despite early-stage research.

Area of Science:

  • Biochemistry
  • Drug Discovery
  • Structural Biology

Background:

  • Protein-protein interactions (PPIs) are crucial in biological processes.
  • Targeting PPIs with small molecules is a growing therapeutic strategy.
  • Successful inhibitors often target deep binding pockets, not flat surfaces.

Purpose of the Study:

  • To review the potential of WD40 repeat (WDR) domains as a novel drug target class.
  • To explore the druggability of WDR domains based on their structural features.
  • To assess the implications of targeting WDR domains for disease biology.

Main Methods:

  • Literature review of WDR domain structure and function.
  • Analysis of recent successful chemical probe development against WDR domains.

Related Experiment Videos

  • Evaluation of WDR domain-containing proteins in disease-associated pathways.

    • Main Results:

    • WDR domains possess a central peptide-binding pocket, suitable for small molecule inhibition.
    • Specific WDR domains (WDR5, EED) and other beta-propeller domains have been successfully targeted.
    • These domains are implicated in multiple disease-relevant pathways.

    Conclusions:

    • WDR domains represent a promising, albeit early-stage, target class for drug discovery.
    • The structural diversity and druggability of WDR pockets offer new avenues for therapeutic intervention.
    • Targeting WDR domains could unlock treatment strategies for diseases currently resistant to drug discovery.