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Small molecule WDR5 inhibitors down-regulate lncRNA expression.

Jen-Yao Chang1, Cora Neugebauer1, Anne Mues Genannt Koers1

  • 1Chemical Genomics Centre of the Max Planck Society, Max Planck Institute of Molecular Physiology Otto-Hahn-Strasse 11 44227 Dortmund Germany peter.t-hart@mpi-dortmund.mpg.de.

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WD repeat domain 5 (WDR5) is crucial for epigenetic gene regulation. Targeting WDR5’s WBM site with inhibitors can downregulate oncogenic lncRNAs, offering a new therapeutic strategy.

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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Biochemistry

Background:

  • WD repeat domain 5 (WDR5) functions as a scaffold protein in epigenetic gene regulation.
  • WDR5 interacts with both proteins and long non-coding RNAs (lncRNAs).
  • Specific binding sites on WDR5, including WBM and WIN, mediate distinct interactions.

Purpose of the Study:

  • To investigate the roles of WDR5's WBM and WIN binding sites in lncRNA binding and gene expression.
  • To develop and validate selective small molecule inhibitors for these WDR5 binding sites.
  • To assess the potential of targeting lncRNA-WDR5 interactions for therapeutic intervention.

Main Methods:

  • Characterization of WDR5 binding sites using selective peptide ligands and fluorescence polarization.
  • Development of small molecule inhibitors targeting WBM and WIN sites.
  • RNA immunoprecipitation assays to confirm inhibitor efficacy in disrupting lncRNA-WDR5 complexes.

Main Results:

  • Selective peptide ligands and small molecule inhibitors were developed for WDR5 binding sites.
  • A WBM site inhibitor effectively disrupted lncRNA-WDR5 complex formation.
  • Inhibitors showed differential sensitivity in downregulating WDR5-regulated lncRNAs, indicating targeted therapeutic potential.

Conclusions:

  • WDR5's WBM site is critical for lncRNA-protein interactions involved in epigenetic regulation.
  • Targeting lncRNA-WDR5 interactions with specific inhibitors offers a promising strategy to reduce oncogenic lncRNA expression.
  • This approach holds potential for developing novel cancer therapies.