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Evidence that EZH2 Deregulation is an Actionable Therapeutic Target for Prevention of Prostate Cancer

Deborah L Burkhart1, Katherine L Morel1, Kristine M Wadosky2

  • 1Department of Oncologic Pathology, Dana-Farber Cancer Institute, Boston, Massachusetts.

Cancer Prevention Research (Philadelphia, Pa.)
|September 12, 2020
PubMed

Insights

Targeting EZH2, a key protein in prostate cancer, reversed high-grade prostatic intraepithelial neoplasia (HG-PIN) in preclinical models. This suggests EZH2 inhibition is a promising strategy for prostate cancer prevention.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Research

Background:

  • Androgen-targeted therapies have shown limited success in prostate cancer chemoprevention.
  • Deregulation of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, is observed in high-grade prostatic intraepithelial neoplasia (HG-PIN).

Purpose of the Study:

  • To investigate the therapeutic potential of targeting EZH2 in prostate cancer.
  • To determine if disrupting EZH2 can reverse the HG-PIN phenotype and impact cancer progression.

Main Methods:

  • Utilized preclinical mouse and human models of prostate cancer.
  • Employed genetic and chemical methods to inhibit EZH2 expression and catalytic activity.
  • Assessed cellular proliferation and Tp53-dependent senescence following EZH2 inhibition.

Main Results:

  • Genetic and chemical disruption of EZH2 effectively reversed the HG-PIN phenotype in preclinical models.
  • Inhibition of EZH2 led to a significant reduction in cellular proliferation.
  • EZH2 inhibition induced Tp53-dependent senescence in prostate cancer cells.

Conclusions:

  • EZH2 is a critical factor in the development of HG-PIN and prostate cancer.
  • Targeting EZH2 represents a viable and actionable therapeutic strategy for prostate cancer prevention.
  • Further research into EZH2 inhibitors is warranted for clinical development.

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