H3K9 methyltransferases and demethylases control lung tumor-propagating cells and lung cancer progression

Nat Commun. 2018 Nov 19;9(1):4559. doi: 10.1038/s41467-018-07077-1.

Abstract

Epigenetic regulators are attractive anticancer targets, but the promise of therapeutic strategies inhibiting some of these factors has not been proven in vivo or taken into account tumor cell heterogeneity. Here we show that the histone methyltransferase G9a, reported to be a therapeutic target in many cancers, is a suppressor of aggressive lung tumor-propagating cells (TPCs). Inhibition of G9a drives lung adenocarcinoma cells towards the TPC phenotype by de-repressing genes which regulate the extracellular matrix. Depletion of G9a during tumorigenesis enriches tumors in TPCs and accelerates disease progression metastasis. Depleting histone demethylases represses G9a-regulated genes and TPC phenotypes. Demethylase inhibition impairs lung adenocarcinoma progression in vivo. Therefore, inhibition of G9a is dangerous in certain cancer contexts, and targeting the histone demethylases is a more suitable approach for lung cancer treatment. Understanding cellular context and specific tumor populations is critical when targeting epigenetic regulators in cancer for future therapeutic development.

Publication types

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

MeSH terms

  • Adenocarcinoma of Lung / metabolism
  • Animals
  • Carcinogenesis
  • Cell Line, Tumor / drug effects
  • Cell Survival
  • Disease Models, Animal
  • Disease Progression*
  • Extracellular Matrix / genetics
  • Histone Demethylases / drug effects
  • Histone Demethylases / metabolism*
  • Histone Methyltransferases / metabolism*
  • Histone-Lysine N-Methyltransferase / drug effects
  • Histone-Lysine N-Methyltransferase / metabolism
  • Lung Neoplasms / genetics
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / pathology
  • Organoids / anatomy & histology
  • Phenotype
  • Proto-Oncogene Proteins p21(ras) / genetics

Substances

  • Histone Demethylases
  • Histone Methyltransferases
  • G9a protein, mouse
  • GLP protein, mouse
  • Histone-Lysine N-Methyltransferase
  • Hras protein, mouse
  • Proto-Oncogene Proteins p21(ras)