title: Modulation of epigenetic targets for anticancer therapy: clinicopathological relevance, structural data and drug discovery perspectives.
abstract: Research on cancer epigenetics has flourished in the last decade. Nevertheless growing evidence point on the importance to understand the mechanisms by which epigenetic changes regulate the genesis and progression of cancer growth. Several epigenetic targets have been discovered and are currently under validation for new anticancer therapies. Drug discovery approaches aiming to target these epigenetic enzymes with small-molecules inhibitors have produced the first pre-clinical and clinical outcomes and many other compounds are now entering the pipeline as new candidate epidrugs. The most studied targets can be ascribed to histone deacetylases and DNA methyltransferases, although several other classes of enzymes are able to operate post-translational modifications to histone tails are also likely to represent new frontiers for therapeutic interventions. By acknowledging that the field of cancer epigenetics is evolving with an impressive rate of new findings, with this review we aim to provide a current overview of pre-clinical applications of smallmolecules for cancer pathologies, combining them with the current knowledge of epigenetic targets in terms of available structural data and drug design perspectives.
authors.affiliation: Department of Experimental Pathology, Alma Mater Studiorum - University of Bologna, Via S.Giacomo 14, 40126 Bologna, Italy.
authors.forename: Federico
authors.initials: F
authors.lastname: Andreoli
authors.forename: Arménio Jorge Moura
authors.initials: AJ
authors.lastname: Barbosa
authors.forename: Marco Daniele
authors.initials: MD
authors.lastname: Parenti
authors.forename: Alberto
authors.initials: A
authors.lastname: Del Rio
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D018450:Disease Progression; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods; D044127:Epigenesis, Genetic; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents