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How the flexibility of human histone deacetylases influences ligand binding: an overview.
Drug Discovery Today
Over the past decade, human histone deacetylases (HDACs) have become interesting as therapeutic targets because of the benefits that their modulation might provide in aging-related disorders. Recently, studies using crystallography and computational chemistry have provided information on the structure and conformational changes related to HDAC-mediated recognition events. Through the description of the key mass and one-off movements observed in metal-dependent HDACs, here we highlight the impact of flexibility on drug-binding affinity and specificity. The collected information will be useful for not only a better understanding of the biological functions of HDACs, but also the conception of new selective binders.
Animals, Binding Sites, Catalytic Domain, Drug Design, Histone Deacetylase Inhibitors/chemistry, Histone Deacetylase Inhibitors/metabolism, Histone Deacetylases/chemistry, Histone Deacetylases/metabolism, Humans, Isoenzymes, Ligands, Models, Molecular, Protein Binding, Protein Conformation, Structure-Activity Relationship, Substrate Specificity
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