4h42

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{{STRUCTURE_4h42| PDB=4h42 | SCENE= }}
 
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===Synthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA===
 
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==Disease==
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==Synthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA==
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[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[http://omim.org/entry/601709 601709]]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
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<StructureSection load='4h42' size='340' side='right'caption='[[4h42]], [[Resolution|resolution]] 2.01&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4h42]] is a 1 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=4H42 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4H42 FirstGlance]. <br>
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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]] 2.01&#8491;</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=11E:N-[(2-AMINO-1,3-BENZOTHIAZOL-6-YL)CARBONYL]GLYCINE'>11E</scene>, <scene name='pdbligand=PG6:1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE'>PG6</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4h42 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4h42 OCA], [https://pdbe.org/4h42 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4h42 RCSB], [https://www.ebi.ac.uk/pdbsum/4h42 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4h42 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Defects in PLAU are the cause of Quebec platelet disorder (QPD) [MIM:[https://omim.org/entry/601709 601709]. QPD is an autosomal dominant bleeding disorder due to a gain-of-function defect in fibrinolysis. Although affected individuals do not exhibit systemic fibrinolysis, they show delayed onset bleeding after challenge, such as surgery. The hallmark of the disorder is markedly increased PLAU levels within platelets, which causes intraplatelet plasmin generation and secondary degradation of alpha-granule proteins.<ref>PMID:20007542</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
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==Function==
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==See Also==
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[[http://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
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== References ==
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==About this Structure==
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<references/>
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[[4h42]] is a 1 chain structure with 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=4H42 OCA].
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__TOC__
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</StructureSection>
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==Reference==
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<references group="xtra"/><references/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: U-plasminogen activator]]
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[[Category: Large Structures]]
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[[Category: Fang, X.]]
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[[Category: Fang X]]
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[[Category: Gao, D.]]
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[[Category: Gao D]]
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[[Category: Hong, Z B.]]
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[[Category: Hong Z-B]]
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[[Category: Huang, M D.]]
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[[Category: Huang M-D]]
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[[Category: Jiang, L G.]]
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[[Category: Jiang L-G]]
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[[Category: Wang, J D.]]
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[[Category: Wang J-D]]
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[[Category: Yu, H Y.]]
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[[Category: Yu H-Y]]
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[[Category: Yuan, C.]]
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[[Category: Yuan C]]
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[[Category: Zhang, X.]]
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[[Category: Zhang X]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-inhibitor complex]]
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[[Category: Plasminogen activation]]
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[[Category: Protease]]
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[[Category: Serine protease]]
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Current revision

Synthesis of a Weak Basic uPA Inhibitor and Crystal Structure of Complex with uPA

PDB ID 4h42

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