title: The cancer epigenome: Concepts, challenges, and therapeutic opportunities.
abstract: Cancer biology is profoundly influenced by changes in the epigenome. Because the dynamic plasticity of the epigenome lends itself well to therapeutic manipulation, the past few years have witnessed an unprecedented investment in the development, characterization, and translation of targeted epigenetic therapies. In this review, I provide a broad context for recent developments that offer a greater understanding of how epigenetic regulators facilitate the initiation, maintenance, and evolution of cancer. I discuss newly developed epigenetic therapies and the cellular and molecular mechanisms that may govern sensitivity and resistance to these agents. I also review the rationale for future combination therapies involving existing and emerging epigenetic drugs.
authors.affiliation: Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, University of Melbourne, Melbourne, VIC, Australia; Centre for Cancer Research, University of Melbourne, Melbourne, VIC, Australia; and Department of Haematology, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia.
authors.forename: Mark A
authors.identifier: 0000-0002-5464-5029
authors.initials: MA
authors.lastname: Dawson
mesh_terms: D042002:Chromatin Assembly and Disassembly / Q000235:genetics; D019175:DNA Methylation / Q000187:drug effects; D015195:Drug Design; D044127:Epigenesis, Genetic / Q000187:drug effects*; D006801:Humans; D007521:Isocitrate Dehydrogenase / Q000037:antagonists & inhibitors; D058990:Molecular Targeted Therapy; D009154:Mutation; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics*; D000072417:Protein Domains; D054852:Small Molecule Libraries / Q000494:pharmacology / Q000627:therapeutic use; D014158:Transcription, Genetic / Q000187:drug effects
chemical_list: D054852:Small Molecule Libraries; C538784:IDH2 protein, human; D007521:Isocitrate Dehydrogenase; C543588:IDH1 protein, human