1g4k

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[[Image:1g4k.gif|left|200px]]
[[Image:1g4k.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1g4k |SIZE=350|CAPTION= <scene name='initialview01'>1g4k</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1g4k", 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=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=HQQ:5-METHYL-5-(4-PHENOXY-PHENYL)-PYRIMIDINE-2,4,6-TRIONE'>HQQ</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= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1g4k| PDB=1g4k | 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=1g4k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1g4k OCA], [http://www.ebi.ac.uk/pdbsum/1g4k PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1g4k RCSB]</span>
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}}
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'''X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin'''
'''X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin'''
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[[Category: Palermo, R.]]
[[Category: Palermo, R.]]
[[Category: Wang, P.]]
[[Category: Wang, P.]]
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[[Category: mmp]]
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[[Category: Mmp]]
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[[Category: stomelysin]]
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[[Category: Stomelysin]]
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[[Category: zinc ligand]]
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[[Category: Zinc ligand]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 17:07:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:36:31 2008''
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Revision as of 14:07, 2 May 2008

Image:1g4k.gif

Template:STRUCTURE 1g4k

X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin


Overview

A new class of matrix metalloproteinase (MMP) inhibitors has been identified by screening a collection of compounds against stromelysin. The inhibitors, 2,4,6-pyrimidine triones, have proven to be potent inhibitors of gelatinases A and B. An X-ray crystal structure of one representative compound bound to the catalytic domain of stromelysin shows that the compounds bind at the active site and ligand the active-site zinc. The pyrimidine triones mimic substrates in forming hydrogen bonds to key residues in the active site, and provide opportunities for placing appropriately chosen groups into the S1' specificity pocket of MMPS: A number of compounds have been synthesized and assayed against stromelysin, and the variations in potency are explained in terms of the binding mode revealed in the X-ray crystal structure.

About this Structure

1G4K is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

X-ray structure of a novel matrix metalloproteinase inhibitor complexed to stromelysin., Dunten P, Kammlott U, Crowther R, Levin W, Foley LH, Wang P, Palermo R, Protein Sci. 2001 May;10(5):923-6. PMID:11316871 Page seeded by OCA on Fri May 2 17:07:56 2008

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