2rjq

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[[Image:2rjq.jpg|left|200px]]
[[Image:2rjq.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2rjq |SIZE=350|CAPTION= <scene name='initialview01'>2rjq</scene>, resolution 2.600&Aring;
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The line below this paragraph, containing "STRUCTURE_2rjq", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BAT:4-(N-HYDROXYAMINO)-2R-ISOBUTYL-2S-(2-THIENYLTHIOMETHYL)SUCCINYL-L-PHENYLALANINE-N-METHYLAMIDE'>BAT</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= ADAMTS5, ADAMTS11, ADMP2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2rjq| PDB=2rjq | SCENE= }}
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|RELATEDENTRY=[[2rjp|2RJP]], [[3b2z|3B2Z]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2rjq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2rjq OCA], [http://www.ebi.ac.uk/pdbsum/2rjq PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2rjq RCSB]</span>
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}}
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'''Crystal structure of ADAMTS5 with inhibitor bound'''
'''Crystal structure of ADAMTS5 with inhibitor bound'''
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[[Category: Somers, W.]]
[[Category: Somers, W.]]
[[Category: Stahl, M.]]
[[Category: Stahl, M.]]
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[[Category: aggrecanase]]
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[[Category: Aggrecanase]]
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[[Category: cleavage on pair of basic residue]]
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[[Category: Cleavage on pair of basic residue]]
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[[Category: extracellular matrix]]
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[[Category: Extracellular matrix]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: metalloprotease domain]]
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[[Category: Metalloprotease domain]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: secreted]]
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[[Category: Secreted]]
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[[Category: zinc]]
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[[Category: Zinc]]
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[[Category: zymogen]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 17:02:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:01:14 2008''
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Revision as of 14:02, 4 May 2008

Image:2rjq.jpg

Template:STRUCTURE 2rjq

Crystal structure of ADAMTS5 with inhibitor bound


Overview

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.

About this Structure

2RJQ 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 Page seeded by OCA on Sun May 4 17:02:40 2008

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OCA

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