2vcg

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Image:2vcg.jpg

2vcg, resolution 1.90Å

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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 , , , and as ligands. Known structural/functional Sites: , , , , , , , , , , , , , , , , , , and . 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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