2v5w: Difference between revisions

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[[Image:2v5w.gif|left|200px]]
[[Image:2v5w.gif|left|200px]]


{{Structure
<!--
|PDB= 2v5w |SIZE=350|CAPTION= <scene name='initialview01'>2v5w</scene>, resolution 2.00&Aring;
The line below this paragraph, containing "STRUCTURE_2v5w", creates the "Structure Box" on the page.
|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>
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
|ACTIVITY=  
or leave the SCENE parameter empty for the default display.
|GENE=  
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|DOMAIN=
{{STRUCTURE_2v5w| PDB=2v5w  | SCENE= }}  
|RELATEDENTRY=[[1t64|1T64]], [[1t67|1T67]], [[1t69|1T69]], [[1vkg|1VKG]], [[1w22|1W22]], [[2v5x|2V5X]]
|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>
}}


'''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.]]
[[Category: alternative splicing]]
[[Category: Alternative splicing]]
[[Category: chromatin]]
[[Category: Chromatin]]
[[Category: chromatin regulator]]
[[Category: Chromatin regulator]]
[[Category: deacetylation]]
[[Category: Deacetylation]]
[[Category: hdac]]
[[Category: Hdac]]
[[Category: hdac8]]
[[Category: Hdac8]]
[[Category: histone deacetylase]]
[[Category: Histone deacetylase]]
[[Category: hydrolase]]
[[Category: Hydrolase]]
[[Category: nuclear protein]]
[[Category: Nuclear protein]]
[[Category: nucleus]]
[[Category: Nucleus]]
[[Category: p53]]
[[Category: P53]]
[[Category: peptidic substrate]]
[[Category: Peptidic substrate]]
[[Category: repressor]]
[[Category: Repressor]]
[[Category: transcription]]
[[Category: Transcription]]
[[Category: transcription regulation]]
[[Category: Transcription regulation]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 18:13:59 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:08:34 2008''

Revision as of 15:14, 4 May 2008

File: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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