title: Small-molecular modulators of cancer-associated epigenetic mechanisms.
abstract: DNA methylation and posttranslational histone modifications regulate expression of various genes independently of changes in the DNA sequence. Such epigenetic mechanisms play important roles in controlling cellular functions, including the cell cycle, immunoresponses and signal transduction. On the other hand, epigenetic aberrations are associated with oncogenesis and proliferation of cancer cells, and epigenetic alterations have been identified in many human cancer cells. Furthermore, chemical-biological approaches have uncovered relationships between epigenetic dysregulation and cancer, and several small molecules that modulate epigenetic mechanisms have already been approved for cancer therapy. In this review, we deal with chemical epigenetics relevant to cancer therapy, focusing especially on small molecules that regulate epigenetic mechanisms related to DNA methylation and histone modification.
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Taishogun, Kyoto 603-8334, Japan.
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Naoki
authors.initials: N
authors.lastname: Miyata
mesh_terms: D000107:Acetylation / Q000187:drug effects; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D019175:DNA Methylation / Q000187:drug effects; D044127:Epigenesis, Genetic / Q000187:drug effects*; D006657:Histones / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism; D011499:Protein Processing, Post-Translational / Q000187:drug effects; D054852:Small Molecule Libraries
chemical_list: D000970:Antineoplastic Agents; D006657:Histones; D054852:Small Molecule Libraries