Targeting Epigenetic Regulators for Endometrial Cancer Therapy: Its Molecular Biology and Potential Clinical Applications

Int J Mol Sci. 2021 Feb 25;22(5):2305. doi: 10.3390/ijms22052305.

Abstract

Endometrial cancer is one of the most frequently diagnosed gynecological malignancies worldwide. However, its prognosis in advanced stages is poor, and there are only few available treatment options when it recurs. Epigenetic changes in gene function, such as DNA methylation, histone modification, and non-coding RNA, have been studied for the last two decades. Epigenetic dysregulation is often reported in the development and progression of various cancers. Recently, epigenetic changes in endometrial cancer have also been discussed. In this review, we give the main points of the role of DNA methylation and histone modification in endometrial cancer, the diagnostic tools to determine these modifications, and inhibitors targeting epigenetic regulators that are currently in preclinical studies and clinical trials.

Keywords: DNA methylation; endometrial cancer; epigenetics; histone acetylation; histone methylation; histone modification.

Publication types

  • Review

MeSH terms

  • Acetylation
  • Chromatin Immunoprecipitation Sequencing
  • DNA Methylation / drug effects
  • Disease Progression
  • Endometrial Neoplasms / drug therapy
  • Endometrial Neoplasms / genetics
  • Endometrial Neoplasms / metabolism*
  • Epigenesis, Genetic / drug effects
  • Female
  • Gene Expression Regulation / drug effects
  • Gene Expression Regulation / genetics
  • Histones / metabolism*
  • Humans
  • Methylation / drug effects*
  • Neoplasm Recurrence, Local / drug therapy
  • Neoplasm Recurrence, Local / metabolism*
  • RNA, Untranslated / genetics
  • RNA, Untranslated / metabolism*

Substances

  • Histones
  • RNA, Untranslated