2vcg

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.

2VCG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Alcaligenes_sp. Alcaligenes sp.] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=K:'>K</scene>, <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=S17:'>S17</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Known structural/functional Sites: <scene name='pdbsite=AC1:Gol Binding Site For Chain D'>AC1</scene>, <scene name='pdbsite=AC2:Gol Binding Site For Chain C'>AC2</scene>, <scene name='pdbsite=AC3:Zn Binding Site For Chain A'>AC3</scene>, <scene name='pdbsite=AC4:Zn Binding Site For Chain B'>AC4</scene>, <scene name='pdbsite=AC5:Zn Binding Site For Chain C'>AC5</scene>, <scene name='pdbsite=AC6:Zn Binding Site For Chain D'>AC6</scene>, <scene name='pdbsite=AC7:Zn Binding Site For Chain D'>AC7</scene>, <scene name='pdbsite=AC8:K Binding Site For Chain A'>AC8</scene>, <scene name='pdbsite=AC9:K Binding Site For Chain B'>AC9</scene>, <scene name='pdbsite=BC1:K Binding Site For Chain C'>BC1</scene>, <scene name='pdbsite=BC2:K Binding Site For Chain D'>BC2</scene>, <scene name='pdbsite=BC3:K Binding Site For Chain A'>BC3</scene>, <scene name='pdbsite=BC4:K Binding Site For Chain B'>BC4</scene>, <scene name='pdbsite=BC5:K Binding Site For Chain C'>BC5</scene>, <scene name='pdbsite=BC6:K Binding Site For Chain D'>BC6</scene>, <scene name='pdbsite=BC7:S17 Binding Site For Chain D'>BC7</scene>, <scene name='pdbsite=BC8:S17 Binding Site For Chain C'>BC8</scene>, <scene name='pdbsite=BC9:S17 Binding Site For Chain A'>BC9</scene>, <scene name='pdbsite=CC1:S17 Binding Site For Chain B'>CC1</scene> and <scene name='pdbsite=CC2:Cl Binding Site For Chain D'>CC2</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VCG OCA].

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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18054239 18054239]

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