1u6q

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[[Image:1u6q.png|left|200px]]
 
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{{STRUCTURE_1u6q| PDB=1u6q | SCENE= }}
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==Substituted 2-Naphthamadine inhibitors of Urokinase==
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<StructureSection load='1u6q' size='340' side='right'caption='[[1u6q]], [[Resolution|resolution]] 2.02&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1u6q]] 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=1U6Q OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1U6Q 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]] 2.02&#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=745:TRANS-6-(2-PHENYLCYCLOPROPYL)-NAPHTHALENE-2-CARBOXAMIDINE'>745</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=1u6q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1u6q OCA], [https://pdbe.org/1u6q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1u6q RCSB], [https://www.ebi.ac.uk/pdbsum/1u6q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1u6q 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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/u6/1u6q_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1u6q ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.
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===Substituted 2-Naphthamadine inhibitors of Urokinase===
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Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.,Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. PMID:15582418<ref>PMID:15582418</ref>
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{{ABSTRACT_PUBMED_15582418}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 1u6q" style="background-color:#fffaf0;"></div>
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[[1u6q]] 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=1U6Q OCA].
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==See Also==
==See Also==
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*[[Urokinase|Urokinase]]
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:015582418</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[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: Bruncko, M.]]
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[[Category: Bruncko M]]
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[[Category: Dalton, C R.]]
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[[Category: Dalton CR]]
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[[Category: Geyer, A.]]
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[[Category: Geyer A]]
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[[Category: Giranda, V L.]]
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[[Category: Giranda VL]]
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[[Category: Kaminski, M K.]]
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[[Category: Kaminski MK]]
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[[Category: McClellan, W.]]
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[[Category: McClellan W]]
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[[Category: Nienaber, V L.]]
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[[Category: Nienaber VL]]
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[[Category: Rockway, T R.]]
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[[Category: Rockway TR]]
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[[Category: Sauer, D R.]]
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[[Category: Sauer DR]]
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[[Category: Wendt, M D.]]
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[[Category: Wendt MD]]
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[[Category: Hydrolase]]
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Current revision

Substituted 2-Naphthamadine inhibitors of Urokinase

PDB ID 1u6q

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