1vkg

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[[Image:1vkg.jpg|left|200px]]
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{{STRUCTURE_1vkg| PDB=1vkg | SCENE= }}
{{STRUCTURE_1vkg| PDB=1vkg | SCENE= }}
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'''Crystal Structure of Human HDAC8 complexed with CRA-19156'''
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===Crystal Structure of Human HDAC8 complexed with CRA-19156===
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==Overview==
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Modulation of the acetylation state of histones plays a pivotal role in the regulation of gene expression. Histone deacetylases (HDACs) catalyze the removal of acetyl groups from lysines near the N termini of histones. This reaction promotes the condensation of chromatin, leading to repression of transcription. HDAC deregulation has been linked to several types of cancer, suggesting a potential use for HDAC inhibitors in oncology. Here we describe the first crystal structures of a human HDAC: the structures of human HDAC8 complexed with four structurally diverse hydroxamate inhibitors. This work sheds light on the catalytic mechanism of the HDACs, and on differences in substrate specificity across the HDAC family. The structure also suggests how phosphorylation of Ser39 affects HDAC8 activity.
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(as it appears on PubMed at http://www.pubmed.gov), where 15242608 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15242608}}
==About this Structure==
==About this Structure==
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[[Category: Histone deacetylase]]
[[Category: Histone deacetylase]]
[[Category: Zinc hydrolase]]
[[Category: Zinc hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:38:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:24:47 2008''

Revision as of 16:24, 28 July 2008

Image:1vkg.png

Template:STRUCTURE 1vkg

Crystal Structure of Human HDAC8 complexed with CRA-19156

Template:ABSTRACT PUBMED 15242608

About this Structure

1VKG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases., Somoza JR, Skene RJ, Katz BA, Mol C, Ho JD, Jennings AJ, Luong C, Arvai A, Buggy JJ, Chi E, Tang J, Sang BC, Verner E, Wynands R, Leahy EM, Dougan DR, Snell G, Navre M, Knuth MW, Swanson RV, McRee DE, Tari LW, Structure. 2004 Jul;12(7):1325-34. PMID:15242608

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