2vcg

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[[Image:2vcg.jpg|left|200px]]
[[Image:2vcg.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2vcg |SIZE=350|CAPTION= <scene name='initialview01'>2vcg</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_2vcg", creates the "Structure Box" on the page.
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|SITE= <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>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=S17:METHYL+4-BROMO-N-[8-(HYDROXYAMINO)-8-OXOOCTANOYL]-L-PHENYLALANINATE'>S17</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2vcg| PDB=2vcg | SCENE= }}
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|RELATEDENTRY=[[1zz1|1ZZ1]], [[1zz0|1ZZ0]], [[1zz3|1ZZ3]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2vcg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vcg OCA], [http://www.ebi.ac.uk/pdbsum/2vcg PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2vcg RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF A HDAC-LIKE PROTEIN HDAH FROM BORDETELLA SP. WITH THE BOUND INHIBITOR ST-17'''
'''CRYSTAL STRUCTURE OF A HDAC-LIKE PROTEIN HDAH FROM BORDETELLA SP. WITH THE BOUND INHIBITOR ST-17'''
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[[Category: Ficner, R.]]
[[Category: Ficner, R.]]
[[Category: Strasser, A.]]
[[Category: Strasser, A.]]
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[[Category: hdac-like amidohydrolase]]
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[[Category: Hdac-like amidohydrolase]]
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[[Category: hdah]]
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[[Category: Hdah]]
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[[Category: histone deacetylase-like amidohydrolase]]
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[[Category: Histone deacetylase-like amidohydrolase]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:35:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:10:56 2008''
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Revision as of 15:35, 4 May 2008

Image:2vcg.jpg

Template:STRUCTURE 2vcg

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.. 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. 2008 Feb 15;16(4):2011-33. Epub 2007 Nov 4. PMID:18054239 Page seeded by OCA on Sun May 4 18:35:34 2008

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