2rjp

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{{STRUCTURE_2rjp| PDB=2rjp | SCENE= }}
{{STRUCTURE_2rjp| PDB=2rjp | SCENE= }}
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'''Crystal structure of ADAMTS4 with inhibitor bound'''
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===Crystal structure of ADAMTS4 with inhibitor bound===
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==Overview==
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Aggrecanases are now believed to be the principal proteinases responsible for aggrecan degradation in osteoarthritis. Given their potential as a drug target, we solved crystal structures of the two most active human aggrecanase isoforms, ADAMTS4 and ADAMTS5, each in complex with bound inhibitor and one wherein the enzyme is in apo form. These structures show that the unliganded and inhibitor-bound enzymes exhibit two essentially different catalytic-site configurations: an autoinhibited, nonbinding, closed form and an open, binding form. On this basis, we propose that mature aggrecanases exist as an ensemble of at least two isomers, only one of which is proteolytically active.
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(as it appears on PubMed at http://www.pubmed.gov), where 18042673 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18042673}}
==About this Structure==
==About this Structure==
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[[Category: Zinc]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 17:02:37 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 16:14:21 2008''

Revision as of 13:14, 27 July 2008

Image:2rjp.png

Template:STRUCTURE 2rjp

Crystal structure of ADAMTS4 with inhibitor bound

Template:ABSTRACT PUBMED 18042673

About this Structure

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

Reference

Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5., Mosyak L, Georgiadis K, Shane T, Svenson K, Hebert T, McDonagh T, Mackie S, Olland S, Lin L, Zhong X, Kriz R, Reifenberg EL, Collins-Racie LA, Corcoran C, Freeman B, Zollner R, Marvell T, Vera M, Sum PE, Lavallie ER, Stahl M, Somers W, Protein Sci. 2008 Jan;17(1):16-21. Epub 2007 Nov 27. PMID:18042673

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