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2j83

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[[Image:2j83.jpg|left|200px]]
[[Image:2j83.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2j83 |SIZE=350|CAPTION= <scene name='initialview01'>2j83</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2j83", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Gol+Binding+Site+For+Chain+B'>AC1</scene>
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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=CME:S,S-(2-HYDROXYETHYL)THIOCYSTEINE'>CME</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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|DOMAIN=
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{{STRUCTURE_2j83| PDB=2j83 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2j83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2j83 OCA], [http://www.ebi.ac.uk/pdbsum/2j83 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2j83 RCSB]</span>
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'''ULILYSIN METALLOPROTEASE IN COMPLEX WITH BATIMASTAT.'''
'''ULILYSIN METALLOPROTEASE IN COMPLEX WITH BATIMASTAT.'''
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[[Category: Sola, M.]]
[[Category: Sola, M.]]
[[Category: Tallant, C.]]
[[Category: Tallant, C.]]
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[[Category: batimastat]]
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[[Category: Batimastat]]
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[[Category: bb-94]]
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[[Category: Bb-94]]
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[[Category: cancer]]
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[[Category: Cancer]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: hydroxamate inhibitor]]
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[[Category: Hydroxamate inhibitor]]
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[[Category: hypothetical protein]]
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[[Category: Hypothetical protein]]
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[[Category: igf]]
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[[Category: Igf]]
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[[Category: igfbp protease]]
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[[Category: Igfbp protease]]
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[[Category: metalloprotease]]
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[[Category: Metalloprotease]]
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[[Category: metzincin]]
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[[Category: Metzincin]]
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[[Category: pappalysin]]
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[[Category: Pappalysin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:29:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:54:22 2008''
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Revision as of 05:29, 4 May 2008

Image:2j83.jpg

Template:STRUCTURE 2j83

ULILYSIN METALLOPROTEASE IN COMPLEX WITH BATIMASTAT.


Overview

Human pappalysin-1 is a multi-domain metalloprotease engaged in the homeostasis of insulin-like growth factors and the founding member of the pappalysin family within the metzincin clan of metalloproteases. We have recently identified an archaeal relative, ulilysin, encompassing only the protease domain. It is a 262-residue active protease with a novel 3D structure with two subdomains separated by an active-site cleft. Despite negligible overall sequence similarity, noticeable similarity is found with other metzincin prototypes, adamalysins/ADAMs and matrix metalloproteinases. Ulilysin has been crystallised in a product complex with an arginine-valine dipeptide occupying the active-site S(1') and S(2') positions and in a complex with the broad-spectrum hydroxamic acid-based metalloprotease inhibitor, batimastat. This molecule inhibits mature ulilysin with an IC(50) value of 61 microM under the conditions assayed. The binding of batimastat to ulilysin evokes binding to vertebrate matrix metalloproteases but is much weaker. These data give insight into substrate specificity and mechanism of action and inhibition of the novel pappalysin family.

About this Structure

2J83 is a Single protein structure of sequence from Methanosarcina acetivorans. Full crystallographic information is available from OCA.

Reference

Substrate specificity of a metalloprotease of the pappalysin family revealed by an inhibitor and a product complex., Garcia-Castellanos R, Tallant C, Marrero A, Sola M, Baumann U, Gomis-Ruth FX, Arch Biochem Biophys. 2007 Jan 1;457(1):57-72. Epub 2006 Oct 24. PMID:17097044 Page seeded by OCA on Sun May 4 08:29:12 2008

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