2v5x

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{{STRUCTURE_2v5x| PDB=2v5x | SCENE= }}
{{STRUCTURE_2v5x| PDB=2v5x | SCENE= }}
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'''CRYSTAL STRUCTURE OF HDAC8-INHIBITOR COMPLEX'''
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===CRYSTAL STRUCTURE OF HDAC8-INHIBITOR COMPLEX===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 17721440 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17721440}}
==About this Structure==
==About this Structure==
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[[Category: Transcription]]
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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 18:14:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:33:27 2008''

Revision as of 14:33, 27 July 2008

Image:2v5x.png

Template:STRUCTURE 2v5x

CRYSTAL STRUCTURE OF HDAC8-INHIBITOR COMPLEX

Template:ABSTRACT PUBMED 17721440

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 Sun Jul 27 17:33:27 2008

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