2vcg | pdb_00002vcg
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CRYSTAL STRUCTURE OF A HDAC-LIKE PROTEIN HDAH FROM BORDETELLA SP. WITH THE BOUND INHIBITOR ST-17
Overview
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.
About this Structure
2VCG is a Single protein structure of sequence from Alcaligenes sp. with ZN, K, CL, S17 and GOL as ligands. Known structural/functional Sites: AC1, AC2, AC3, AC4, AC5, AC6, AC7, AC8, AC9, BC1, BC2, BC3, BC4, BC5, BC6, BC7, BC8, BC9, CC1 and CC2. Full crystallographic information is available from OCA.
Reference
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs)., Schafer S, Saunders L, Eliseeva E, Velena A, Jung M, Schwienhorst A, Strasser A, Dickmanns A, Ficner R, Schlimme S, Sippl W, Verdin E, Jung M, Bioorg Med Chem. 2007 Nov 4;. PMID:18054239
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