2v5x

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|PDB= 2v5x |SIZE=350|CAPTION= <scene name='initialview01'>2v5x</scene>, resolution 2.25&Aring;
|PDB= 2v5x |SIZE=350|CAPTION= <scene name='initialview01'>2v5x</scene>, resolution 2.25&Aring;
|SITE= <scene name='pdbsite=AC1:V5x+Binding+Site+For+Chain+B'>AC1</scene>
|SITE= <scene name='pdbsite=AC1:V5x+Binding+Site+For+Chain+B'>AC1</scene>
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene> and <scene name='pdbligand=V5X:(2R)-N~8~-HYDROXY-2-{[(5-METHOXY-2-METHYL-1H-INDOL-3-YL)ACETYL]AMINO}-N~1~-[2-(2-PHENYL-1H-INDOL-3-YL)ETHYL]OCTANEDIAMIDE'>V5X</scene>
+
|LIGAND= <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=V5X:(2R)-N~8~-HYDROXY-2-{[(5-METHOXY-2-METHYL-1H-INDOL-3-YL)ACETYL]AMINO}-N~1~-[2-(2-PHENYL-1H-INDOL-3-YL)ETHYL]OCTANEDIAMIDE'>V5X</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
|ACTIVITY=
|ACTIVITY=
|GENE=
|GENE=
 +
|DOMAIN=
 +
|RELATEDENTRY=[[1t64|1T64]], [[1t67|1T67]], [[1t69|1T69]], [[1vkg|1VKG]], [[1w22|1W22]], [[2v5w|2V5W]]
 +
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2v5x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2v5x OCA], [http://www.ebi.ac.uk/pdbsum/2v5x PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2v5x RCSB]</span>
}}
}}
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[[Category: Vannini, A.]]
[[Category: Vannini, A.]]
[[Category: Volpari, C.]]
[[Category: Volpari, C.]]
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[[Category: K]]
 
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[[Category: V5X]]
 
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[[Category: ZN]]
 
[[Category: alternative splicing]]
[[Category: alternative splicing]]
[[Category: chromatin]]
[[Category: chromatin]]
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[[Category: transcription regulation]]
[[Category: transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:43:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:08:38 2008''

Revision as of 02:08, 31 March 2008

Image:2v5x.jpg


PDB ID 2v5x

Drag the structure with the mouse to rotate
, resolution 2.25Å
Sites:
Ligands: , ,
Related: 1T64, 1T67, 1T69, 1VKG, 1W22, 2V5W


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



CRYSTAL STRUCTURE OF HDAC8-INHIBITOR 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

2V5X 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 Mon Mar 31 05:08:38 2008

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