title: Histone deacetylation in epigenetics: an attractive target for anticancer therapy.
abstract: The reversible histone acetylation and deacetylation are epigenetic phenomena that play critical roles in the modulation of chromatin topology and the regulation of gene expression. Aberrant transcription due to altered expression or mutation of genes that encode histone acetyltransferase (HAT) or histone deacetylase (HDAC) enzymes or their binding partners, has been clearly linked to carcinogenesis. The histone deacetylase inhibitors are a new promising class of anticancer agents (some of which in clinical trials), that inhibit the proliferation of tumor cells in culture and in vivo by inducing cell-cycle arrest, terminal differentiation, and/or apoptosis. This report reviews the chemistry and the biology of HDACs and HDAC inhibitors, laying particular emphasis on agents actually in clinical trials for cancer therapy and on new potential anticancer lead compounds more selective and less toxic.
authors.affiliation: Istituto Pasteur, Fondazione Cenci-Bolognetti, Dipartimento di Studi Farmaceutici, Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Roma, Italy. antonello.mai@uniroma1.it
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
authors.forename: Silvio
authors.initials: S
authors.lastname: Massa
authors.forename: Dante
authors.initials: D
authors.lastname: Rotili
authors.forename: Ilaria
authors.initials: I
authors.lastname: Cerbara
authors.forename: Sergio
authors.initials: S
authors.lastname: Valente
authors.forename: Riccardo
authors.initials: R
authors.lastname: Pezzi
authors.forename: Silvia
authors.initials: S
authors.lastname: Simeoni
authors.forename: Rino
authors.initials: R
authors.lastname: Ragno
mesh_terms: D000107:Acetylation; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D042002:Chromatin Assembly and Disassembly; D019175:DNA Methylation; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D044127:Epigenesis, Genetic; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy* / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases