1kbc: Difference between revisions

Revision as of 22:32, 2 May 2008

PROCARBOXYPEPTIDASE TERNARY COMPLEX

OverviewOverview

Matrix metalloproteinases (MMP) are zinc endopeptidases involved in tissue remodelling. They have been implicated in a series of pathologies, including cancer, arthritis, joint destruction and Alzheimer's disease. Human neutrophil collagenase represents one of the three interstitial collagenases that cleave triple-helical collagen of type I, II and III. Its catalytic domain (residues Phe79-Gly242) has been heterologously expressed in Escherichia coli and crystallized as a non-covalent complex with the hydroxamate inhibitor BB-1909, which has distinct selectivity against different MMP, in a crystal form. The crystal structure, refined to 0.18-nm resolution, shows that BB-1909 is a right-hand-side inhibitor that binds to the S1'-S3' subsites and coordinates to the catalytic Zn2+ in a bidentate manner via the hydroxyl and carbonyl oxygen atoms of the hydroxamate group in a similar manner to batimastat. The collagenase/BB-1909 complex is described in detail and compared with the collagenase/batimastat complex. These studies provide information on MMP specificity and thus may assist the development of more-selective MMP inhibitors.

About this StructureAbout this Structure

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

ReferenceReference

1.8-A crystal structure of the catalytic domain of human neutrophil collagenase (matrix metalloproteinase-8) complexed with a peptidomimetic hydroxamate primed-side inhibitor with a distinct selectivity profile., Betz M, Huxley P, Davies SJ, Mushtaq Y, Pieper M, Tschesche H, Bode W, Gomis-Ruth FX, Eur J Biochem. 1997 Jul 1;247(1):356-63. PMID:9249047 Page seeded by OCA on Fri May 2 22:32:00 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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 [[Image:1kbc.jpg|left|200px]]
- {{Structure
+<!--
-|PDB= 1kbc |SIZE=350|CAPTION= <scene name='initialview01'>1kbc</scene>, resolution 1.8&Aring;
+The line below this paragraph, containing "STRUCTURE_1kbc", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=HLE:3-FORMYL-2-HYDROXY-5-METHYL-HEXANOIC+ACID+HYDROXYAMIDE'>HLE</scene>, <scene name='pdbligand=RIN:3-AMINO-AZACYCLOTRIDECAN-2-ONE'>RIN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Neutrophil_collagenase Neutrophil collagenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.34 3.4.24.34] </span>
+or leave the SCENE parameter empty for the default display.
-|GENE=
+-->
-|DOMAIN=
+{{STRUCTURE_1kbc|  PDB=1kbc  |  SCENE=  }}
-|RELATEDENTRY=
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1kbc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1kbc OCA], [http://www.ebi.ac.uk/pdbsum/1kbc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1kbc RCSB]</span>
-}}
 '''PROCARBOXYPEPTIDASE TERNARY COMPLEX'''
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 [[Category: Bode, W.]]
 [[Category: Gomis-Rueth, F X.]]
-[[Category: collagenase]]
+[[Category: Collagenase]]
-[[Category: hnc]]
+[[Category: Hnc]]
-[[Category: hydrolase]]
+[[Category: Hydrolase]]
-[[Category: hydrolytic enzyme]]
+[[Category: Hydrolytic enzyme]]
-[[Category: inhibitor]]
+[[Category: Inhibitor]]
-[[Category: matrixin]]
+[[Category: Matrixin]]
-[[Category: metalloproteinase]]
+[[Category: Metalloproteinase]]
-[[Category: mmp-8]]
+[[Category: Mmp-8]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 22:32:00 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:46:05 2008''