Epigenetic disruption of the RARγ complex impairs its function to bookmark AR enhancer interactions required for

Sajad A Wani1, Shahid Hussain2,3, Jaimie S Gray1

  • 1Division of Pharmaceutics and Pharmacology, The Ohio State University, Columbus, OH 43210.

Insights

This study reveals how retinoic acid receptor gamma (RARγ), modulated by miR-96, bookmarks enhancers in prostate cancer (PCa) cells. This mechanism influences Androgen Receptor (AR) activity and promotes differentiation, impacting aggressive PCa phenotypes.

Area of Science:

  • Genomics
  • Molecular Biology
  • Cancer Research

Background:

  • Prostate cancer (PCa) progression involves complex genomic mechanisms and lineage plasticity.
  • The role of retinoic acid receptor gamma (RARγ) in governing Androgen Receptor (AR) cistrome-transcriptome relationships remains understudied.
  • Understanding these mechanisms is crucial for identifying therapeutic targets in aggressive PCa.

Approach:

  • Investigated RARγ's cistromic function in PCa cell models.
  • Analyzed RARγ complex composition, including cofactors and RNA processing proteins.
  • Identified miR-96 bound and regulated gene targets, including m6A-marked elements.
  • Examined RARγ's impact on AR cistrome, chromatin accessibility (H3K27ac), and cell cycle (G2/M).
  • Assessed the antagonism between RARγ and the lineage regulator ONECUT2.

Key Points:

  • RARγ complex is enriched with RNA processing and bookmarking factors.
  • RARγ enhances the AR cistrome at active enhancers and super-enhancers, overlapping with bookmarking factors.
  • RARγ promotes nucleosome-free chromatin and enhances the AR cistrome in G2/M cells.
  • RARγ antagonizes the transcriptional activity of ONECUT2.
  • Gene programs regulated by miR-96 or antagonized by RARγ are linked to alternative lineages and aggressive PCa.

Conclusions:

  • RARγ, modulated by miR-96, bookmarks enhancer sites during mitosis.
  • These RARγ-bookmarked sites are essential for AR-mediated transcriptional competence and luminal differentiation.
  • RARγ's function antagonizes ONECUT2, influencing lineage plasticity and aggressive PCa phenotypes.
  • This study uncovers a novel role for RARγ in regulating prostate cancer cell fate and progression.