Transformation-dependent silencing of tumor-selective apoptosis-inducing TRAIL by DNA hypermethylation is antagonized by decitabine

Mol Cancer Ther. 2011 Sep;10(9):1611-23. doi: 10.1158/1535-7163.MCT-11-0140. Epub 2011 Jun 22.

Abstract

TNF-related apoptosis-inducing ligand (TRAIL) kills tumor cells selectively. We asked how emerging tumor cells escape elimination by TRAIL and how tumor-specific killing by TRAIL could then be restored. We found that TRAIL expression is consistently downregulated in HRAS(G12V)-transformed cells in stepwise tumorigenesis models derived from four different tissues due to DNA hypermethylation of CpG clusters within the TRAIL promoter. Decitabine de-silenced TRAIL, which remained inducible by interferon, while induction of TRAIL by blocking the HRAS(G12V)-activated mitogen-activated protein kinase pathway was subordinated to epigenetic silencing. Decitabine induced apoptosis through upregulation of endogenous TRAIL in cooperation with favorable regulation of key players acting in TRAIL-mediated apoptosis. Apoptosis induction by exogenously added TRAIL was largely increased by decitabine. In vivo treatment of xenografted human HRAS(G12V)-transformed human epithelial kidney or syngenic mice tumors by decitabine blocked tumor growth induced TRAIL expression and apoptosis. Our results emphasize the potential of decitabine to enhance TRAIL-induced apoptosis in tumors and thus provide a rationale for combination therapies with decitabine to increase tumor-selective apoptosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / pharmacology*
  • Antimetabolites, Antineoplastic / therapeutic use
  • Apoptosis / drug effects
  • Apoptosis / genetics
  • Azacitidine / analogs & derivatives*
  • Azacitidine / pharmacology
  • Azacitidine / therapeutic use
  • Cell Line, Transformed
  • Cell Line, Tumor
  • Cell Transformation, Neoplastic / genetics*
  • DNA Methylation / drug effects*
  • Decitabine
  • Down-Regulation / genetics
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Epigenesis, Genetic
  • Gene Expression Regulation / drug effects
  • Gene Silencing*
  • HeLa Cells
  • Humans
  • Interferons / metabolism
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Proto-Oncogene Proteins p21(ras) / metabolism
  • Signal Transduction
  • TNF-Related Apoptosis-Inducing Ligand / genetics*
  • TNF-Related Apoptosis-Inducing Ligand / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Antimetabolites, Antineoplastic
  • Enzyme Inhibitors
  • TNF-Related Apoptosis-Inducing Ligand
  • Decitabine
  • Interferons
  • HRAS protein, human
  • Proto-Oncogene Proteins p21(ras)
  • Azacitidine