Role of EZH2 in cancer stem cells: from biological insight to a therapeutic target

Oncotarget. 2017 Jun 6;8(23):37974-37990. doi: 10.18632/oncotarget.16467.


Epigenetic modifications in cancer stem cells largely result in phenotypic and functional heterogeneity in many solid tumors. Increasing evidence indicates that enhancer of zeste homolog 2 (EZH2), the catalytic subunit of Polycomb repressor complex 2, is highly expressed in cancer stem cells of numerous malignant tumors and has a critical function in cancer stem cell expansion and maintenance. Here, we review up-to-date information regarding EZH2 expression patterns, functions, and molecular mechanisms in cancer stem cells in various malignant tumors and discuss the therapeutic potential of targeting EZH2 in tumors.

Keywords: EZH2; cancer stem cells; histone lysine methylation; polycomb repressive complex; sphere.

Publication types

  • Review

MeSH terms

  • Enhancer of Zeste Homolog 2 Protein / genetics*
  • Enhancer of Zeste Homolog 2 Protein / metabolism
  • Epigenesis, Genetic / genetics*
  • Humans
  • Neoplastic Stem Cells / metabolism*
  • Neoplastic Stem Cells / pathology
  • Polycomb Repressive Complex 2 / genetics*


  • EZH2 protein, human
  • Enhancer of Zeste Homolog 2 Protein
  • Polycomb Repressive Complex 2