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Histone deacetylation in epigenetics: An attractive target for anticancer therapy
Author(s) -
Mai Antonello,
Massa Silvio,
Rotili Dante,
Cerbara Ilaria,
Valente Sergio,
Pezzi Riccardo,
Simeoni Silvia,
Ragno Rino
Publication year - 2005
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.20024
Subject(s) - acetylation , histone deacetylase , epigenetics , histone acetyltransferase , hdac11 , histone deacetylase 5 , histone , histone deacetylase 2 , biology , hdac4 , cancer epigenetics , chromatin , cancer research , epigenetic therapy , hdac10 , chromatin remodeling , histone methyltransferase , microbiology and biotechnology , genetics , gene expression , gene , dna methylation
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. © 2005 Wiley Periodicals, Inc.