Inside HDACs with more selective HDAC inhibitors.
Inhibitors of histone deacetylases (HDACs) are nowadays part of the therapeutic arsenal mainly against cancers, with four compounds approved by the Food and Drug Administration. During the last five years, several groups have made continuous efforts to improve this class of compounds, designing more selective compounds or compounds with multiple capacities. After a survey of the HDAC biology and structures, this review summarizes the results of the chemists working in this field, and highlights when possible the behavior of the molecules inside their targets.
Laboratoire Ecologie et Biologie des Interactions, Equipe « SEVE Sucres & Echanges Végétaux-Environnement », Université de Poitiers, UMR CNRS 7267, F-86073 Poitiers Cedex 09, France; Réseau Epigénétique du Cancéropôle Grand Ouest, France.
Joëlle
J
Roche
Institut de Chimie des Milieux et Matériaux de Poitiers, UMR CNRS 7285, 4 rue Michel Brunet, TSA 51106, B28, F-86073 Poitiers Cedex 09, France; Réseau Epigénétique du Cancéropôle Grand Ouest, France. Electronic address: philippe.bertrand@univ-poitiers.fr.
Philippe
P
Bertrand
D000818:Animals; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism*; D006801:Humans; D009930:Organic Chemicals / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D013379:Substrate Specificity
D056572:Histone Deacetylase Inhibitors; D009930:Organic Chemicals; D006655:Histone Deacetylases
Epigenetics; HDAC inhibitors; Histone acetylation; Molecular modelling; Synthesis