Inhibitors of DNA Methylation, Histone Deacetylation, and Histone Demethylation. A Perfect Combination for Cancer Therapy.

Research output: Chapter in Book/Report/Conference proceedingConference contribution

Abstract

Epigenetic silencing and inappropriate activation of gene expression are frequent events during the initiation and progression of cancer. These events involve a complex interplay between the hypermethylation of CpG dinucleotides within gene promoter and enhancer regions, the recruitment of transcriptional corepressors and the deacetylation and/or methylation of histone tails. These epigenetic regulators act in concert to block transcription or interfere with the maintenance of chromatin boundary regions. However, DNA/histone methylation and histone acetylation states are reversible, enzyme-mediated processes and as such, have emerged as promising targets for cancer therapy. This review will focus on the potential benefits and synergistic/additive effects of combining DNA-demethylating agents and histone deacetylase inhibitors or lysine-specific demethylase inhibitors together in epigenetic therapy for solid tumors and will highlight what is known regarding the mechanisms of action that contribute to the antitumor response.

Original languageEnglish (US)
Title of host publicationAdvances in Cancer Research, 2016
EditorsPaul B. Fisher, Kenneth D. Tew
PublisherAcademic Press Inc.
Pages55-111
Number of pages57
ISBN (Print)9780128047897
DOIs
StatePublished - Jan 1 2016

Publication series

NameAdvances in Cancer Research
Volume130
ISSN (Print)0065-230X
ISSN (Electronic)2162-5557

Keywords

  • DNA methyltransferase inhibitors
  • Drug synergy
  • Epigenetic therapy
  • Histone deacetylation and methylation inhibitors
  • Solid tumors

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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