Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).
We synthesized biarylalanine-containing hydroxamic acids and tested them on immunoprecipitated HDAC1 and HDAC6 and show a subtype selectivity for HDAC6 that was confirmed in cells by Western blot (tubulin vs histones). We obtained an X-ray structure with a HDAC6-selective inhibitor with the bacterial deacetylase HDAH. Docking studies were carried out ... using HDAC1 and HDAC6 protein models. Antiproliferative activity was shown on cancer cells for selected compounds.
Mesh Terms:
Blotting, Western, Cell Line, Tumor, Cell Proliferation, Computer Simulation, Crystallography, X-Ray, Enzyme Inhibitors, Histone Deacetylase 1, Histone Deacetylase Inhibitors, Histone Deacetylases, Histones, Humans, Hydroxamic Acids, Phenylalanine, Protein Binding, Tubulin
Blotting, Western, Cell Line, Tumor, Cell Proliferation, Computer Simulation, Crystallography, X-Ray, Enzyme Inhibitors, Histone Deacetylase 1, Histone Deacetylase Inhibitors, Histone Deacetylases, Histones, Humans, Hydroxamic Acids, Phenylalanine, Protein Binding, Tubulin
Bioorg. Med. Chem.
Date: Feb. 15, 2008
PubMed ID: 18054239
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