1bqo

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Current revision (06:38, 7 February 2024) (edit) (undo)
 
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<StructureSection load='1bqo' size='340' side='right'caption='[[1bqo]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
<StructureSection load='1bqo' size='340' side='right'caption='[[1bqo]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[1bqo]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BQO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1BQO FirstGlance]. <br>
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<table><tr><td colspan='2'>[[1bqo]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BQO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1BQO FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=N25:1,3-BIS-(4-METHOXY-BENZENESULFONYL)-5,5-DIMETHYL-HEXAHYDRO-PYRIMIDINE-2-CARBOXYLIC+ACID+HYDROXYAMIDE'>N25</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] </span></td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=N25:1,3-BIS-(4-METHOXY-BENZENESULFONYL)-5,5-DIMETHYL-HEXAHYDRO-PYRIMIDINE-2-CARBOXYLIC+ACID+HYDROXYAMIDE'>N25</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1bqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1bqo OCA], [https://pdbe.org/1bqo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1bqo RCSB], [https://www.ebi.ac.uk/pdbsum/1bqo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1bqo ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1bqo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1bqo OCA], [https://pdbe.org/1bqo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1bqo RCSB], [https://www.ebi.ac.uk/pdbsum/1bqo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1bqo ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
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[[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN]] Defects in MMP3 are the cause of susceptibility to coronary heart disease type 6 (CHDS6) [MIM:[https://omim.org/entry/614466 614466]]. A multifactorial disease characterized by an imbalance between myocardial functional requirements and the capacity of the coronary vessels to supply sufficient blood flow. Decreased capacity of the coronary vessels is often associated with thickening and loss of elasticity of the coronary arteries. Note=A polymorphism in the MMP3 promoter region is associated with the risk of coronary heart disease and myocardial infarction, due to lower MMP3 proteolytic activity and higher extracellular matrix deposition in atherosclerotic lesions.<ref>PMID:8662692</ref> <ref>PMID:12477941</ref>
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[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN] Defects in MMP3 are the cause of susceptibility to coronary heart disease type 6 (CHDS6) [MIM:[https://omim.org/entry/614466 614466]. A multifactorial disease characterized by an imbalance between myocardial functional requirements and the capacity of the coronary vessels to supply sufficient blood flow. Decreased capacity of the coronary vessels is often associated with thickening and loss of elasticity of the coronary arteries. Note=A polymorphism in the MMP3 promoter region is associated with the risk of coronary heart disease and myocardial infarction, due to lower MMP3 proteolytic activity and higher extracellular matrix deposition in atherosclerotic lesions.<ref>PMID:8662692</ref> <ref>PMID:12477941</ref>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN]] Can degrade fibronectin, laminin, gelatins of type I, III, IV, and V; collagens III, IV, X, and IX, and cartilage proteoglycans. Activates procollagenase.
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[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN] Can degrade fibronectin, laminin, gelatins of type I, III, IV, and V; collagens III, IV, X, and IX, and cartilage proteoglycans. Activates procollagenase.
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Stromelysin 1]]
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[[Category: Almstead NG]]
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[[Category: Almstead, N G]]
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[[Category: Anastasio MV]]
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[[Category: Anastasio, M V]]
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[[Category: De B]]
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[[Category: De, B]]
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[[Category: Dunaway CM]]
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[[Category: Dunaway, C M]]
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[[Category: Dunham KLM]]
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[[Category: Dunham, K L.M]]
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[[Category: Gu F]]
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[[Category: Gu, F]]
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[[Category: Mcphail SJ]]
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[[Category: Mcphail, S J]]
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[[Category: Mieling GE]]
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[[Category: Mieling, G E]]
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[[Category: Natchus MG]]
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[[Category: Natchus, M G]]
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[[Category: Pikul S]]
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[[Category: Pikul, S]]
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[[Category: Rydel TJ]]
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[[Category: Rydel, T J]]
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[[Category: Snider CE]]
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[[Category: Snider, C E]]
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[[Category: Taiwo YO]]
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[[Category: Taiwo, Y O]]
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[[Category: Matrix metalloprotease]]
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[[Category: Metalloprotease]]
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[[Category: Osteoarthritis]]
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[[Category: Stromelysin]]
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[[Category: Structure-based drug design]]
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Current revision

DISCOVERY OF POTENT, ACHIRAL MATRIX METALLOPROTEINASE INHIBITORS

PDB ID 1bqo

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