1g4k

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[[Image:1g4k.gif|left|200px]]<br /><applet load="1g4k" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1g4k.gif|left|200px]]
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caption="1g4k, resolution 2.0&Aring;" />
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'''X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin'''<br />
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{{Structure
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|PDB= 1g4k |SIZE=350|CAPTION= <scene name='initialview01'>1g4k</scene>, resolution 2.0&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=HQQ:5-METHYL-5-(4-PHENOXY-PHENYL)-PYRIMIDINE-2,4,6-TRIONE'>HQQ</scene> and <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1G4K is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=CA:'>CA</scene>, <scene name='pdbligand=HQQ:'>HQQ</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1G4K OCA].
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1G4K is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1G4K OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11316871 11316871]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/11316871 11316871]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: zinc ligand]]
[[Category: zinc ligand]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:46:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 11:18:07 2008''

Revision as of 09:18, 20 March 2008

Image:1g4k.gif


PDB ID 1g4k

Drag the structure with the mouse to rotate
, resolution 2.0Å
Ligands: , , and
Activity: Stromelysin 1, with EC number 3.4.24.17
Coordinates: save as pdb, mmCIF, xml



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


Contents

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.

Disease

Known diseases associated with this structure: Coronary heart disease, susceptibility to OMIM:[185250]

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

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