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2v5w

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[[Image:2v5w.gif|left|200px]]
[[Image:2v5w.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2v5w |SIZE=350|CAPTION= <scene name='initialview01'>2v5w</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2v5w", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Mcm+Binding+Site+For+Chain+L'>AC1</scene>
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|LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=ALY:N(6)-ACETYLLYSINE'>ALY</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=MCM:7-AMINO-4-METHYL-CHROMEN-2-ONE'>MCM</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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|DOMAIN=
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{{STRUCTURE_2v5w| PDB=2v5w | SCENE= }}
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|RELATEDENTRY=[[1t64|1T64]], [[1t67|1T67]], [[1t69|1T69]], [[1vkg|1VKG]], [[1w22|1W22]], [[2v5x|2V5X]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2v5w FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2v5w OCA], [http://www.ebi.ac.uk/pdbsum/2v5w PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2v5w RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HDAC8-SUBSTRATE COMPLEX'''
'''CRYSTAL STRUCTURE OF HDAC8-SUBSTRATE COMPLEX'''
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[[Category: Vannini, A.]]
[[Category: Vannini, A.]]
[[Category: Volpari, C.]]
[[Category: Volpari, C.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: chromatin]]
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[[Category: Chromatin]]
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[[Category: chromatin regulator]]
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[[Category: Chromatin regulator]]
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[[Category: deacetylation]]
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[[Category: Deacetylation]]
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[[Category: hdac]]
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[[Category: Hdac]]
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[[Category: hdac8]]
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[[Category: Hdac8]]
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[[Category: histone deacetylase]]
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[[Category: Histone deacetylase]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: nuclear protein]]
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[[Category: Nuclear protein]]
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[[Category: nucleus]]
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[[Category: Nucleus]]
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[[Category: p53]]
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[[Category: P53]]
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[[Category: peptidic substrate]]
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[[Category: Peptidic substrate]]
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[[Category: repressor]]
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[[Category: Repressor]]
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[[Category: transcription]]
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[[Category: Transcription]]
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[[Category: transcription regulation]]
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[[Category: Transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:13:59 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:08:34 2008''
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Revision as of 15:14, 4 May 2008

Image:2v5w.gif

Template:STRUCTURE 2v5w

CRYSTAL STRUCTURE OF HDAC8-SUBSTRATE COMPLEX


Overview

Histone deacetylases (HDACs)-an enzyme family that deacetylates histones and non-histone proteins-are implicated in human diseases such as cancer, and the first-generation of HDAC inhibitors are now in clinical trials. Here, we report the 2.0 A resolution crystal structure of a catalytically inactive HDAC8 active-site mutant, Tyr306Phe, bound to an acetylated peptidic substrate. The structure clarifies the role of active-site residues in the deacetylation reaction and substrate recognition. Notably, the structure shows the unexpected role of a conserved residue at the active-site rim, Asp 101, in positioning the substrate by directly interacting with the peptidic backbone and imposing a constrained cis-conformation. A similar interaction is observed in a new hydroxamate inhibitor-HDAC8 structure that we also solved. The crucial role of Asp 101 in substrate and inhibitor recognition was confirmed by activity and binding assays of wild-type HDAC8 and Asp101Ala, Tyr306Phe and Asp101Ala/Tyr306Phe mutants.

About this Structure

2V5W is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Substrate binding to histone deacetylases as shown by the crystal structure of the HDAC8-substrate complex., Vannini A, Volpari C, Gallinari P, Jones P, Mattu M, Carfi A, De Francesco R, Steinkuhler C, Di Marco S, EMBO Rep. 2007 Sep;8(9):879-84. Epub 2007 Aug 10. PMID:17721440 Page seeded by OCA on Sun May 4 18:13:59 2008

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