EZH2 oncogenic activity in castration-resistant prostate cancer cells is Polycomb-independent

Science. 2012 Dec 14;338(6113):1465-9. doi: 10.1126/science.1227604.

Abstract

Epigenetic regulators represent a promising new class of therapeutic targets for cancer. Enhancer of zeste homolog 2 (EZH2), a subunit of Polycomb repressive complex 2 (PRC2), silences gene expression via its histone methyltransferase activity. We found that the oncogenic function of EZH2 in cells of castration-resistant prostate cancer is independent of its role as a transcriptional repressor. Instead, it involves the ability of EZH2 to act as a coactivator for critical transcription factors including the androgen receptor. This functional switch is dependent on phosphorylation of EZH2 and requires an intact methyltransferase domain. Hence, targeting the non-PRC2 function of EZH2 may have therapeutic efficacy for treating metastatic, hormone-refractory prostate cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Castration
  • Cell Line, Tumor
  • Cohort Studies
  • Enhancer of Zeste Homolog 2 Protein
  • Gene Expression Regulation, Neoplastic
  • Gene Silencing
  • Humans
  • Jumonji Domain-Containing Histone Demethylases / metabolism
  • Male
  • Methyltransferases / chemistry
  • Methyltransferases / genetics
  • Methyltransferases / metabolism
  • Mice
  • Mice, Inbred ICR
  • Mice, SCID
  • Oncogene Proteins / genetics
  • Oncogene Proteins / metabolism*
  • Polycomb Repressive Complex 2 / genetics
  • Polycomb Repressive Complex 2 / metabolism*
  • Prostatic Neoplasms / genetics
  • Prostatic Neoplasms / metabolism*
  • Prostatic Neoplasms / mortality
  • Protein Structure, Tertiary
  • Receptors, Androgen / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Oncogene Proteins
  • Receptors, Androgen
  • Jumonji Domain-Containing Histone Demethylases
  • KDM6B protein, human
  • Methyltransferases
  • EZH2 protein, human
  • Enhancer of Zeste Homolog 2 Protein
  • Polycomb Repressive Complex 2

Associated data

  • GEO/GSE39461