3qn7

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[[Image:3qn7.jpg|left|200px]]
 
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==Potent and selective bicyclic peptide inhibitor (UK18) of human urokinase-type plasminogen activator(uPA)==
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The line below this paragraph, containing "STRUCTURE_3qn7", creates the "Structure Box" on the page.
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<StructureSection load='3qn7' size='340' side='right'caption='[[3qn7]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3qn7]] 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=3QN7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QN7 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]] 1.9&#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=ZBR:1,3,5-TRIS(BROMOMETHYL)BENZENE'>ZBR</scene></td></tr>
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{{STRUCTURE_3qn7| PDB=3qn7 | SCENE= }}
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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=3qn7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qn7 OCA], [https://pdbe.org/3qn7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qn7 RCSB], [https://www.ebi.ac.uk/pdbsum/3qn7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qn7 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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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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From a large combinatorial library of chemically constrained bicyclic peptides we isolated a selective and potent (K(i) = 53 nM) inhibitor of human urokinase-type plasminogen activator (uPA) and crystallized the complex. This revealed an extended structure of the peptide with both peptide loops engaging the target to form a large interaction surface of 701 A(2) with multiple hydrogen bonds and complementary charge interactions, explaining the high affinity and specificity of the inhibitor. The interface resembles that between two proteins and suggests that these constrained peptides have the potential to act as small protein mimics.
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===Potent and selective bicyclic peptide inhibitor (UK18) of human urokinase-type plasminogen activator(uPA)===
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Bicyclic peptide inhibitor reveals large contact interface with a protease target.,Angelini A, Cendron L, Chen S, Touati J, Winter G, Zanotti G, Heinis C ACS Chem Biol. 2012 May 18;7(5):817-21. doi: 10.1021/cb200478t. Epub 2012 Feb 15. PMID:22304751<ref>PMID:22304751</ref>
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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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<div class="pdbe-citations 3qn7" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_17692534}}, adds the Publication Abstract to the page
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 17692534 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_17692534}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[3qn7]] is a 2 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=3QN7 OCA].
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==Reference==
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<ref group="xtra">PMID:017692534</ref><ref group="xtra">PMID:008591045</ref><references group="xtra"/>
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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: Angelini, A.]]
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[[Category: Angelini A]]
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[[Category: Cendron, L.]]
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[[Category: Cendron L]]
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[[Category: Heinis, C.]]
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[[Category: Heinis C]]
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[[Category: Touati, J.]]
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[[Category: Touati J]]
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[[Category: Winter, G.]]
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[[Category: Winter G]]
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[[Category: Zanotti, G.]]
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[[Category: Zanotti G]]
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[[Category: Bicyclic peptide inhibitor]]
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[[Category: Chymotrypsin fold]]
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[[Category: Extracellular]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Serine protease]]
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Current revision

Potent and selective bicyclic peptide inhibitor (UK18) of human urokinase-type plasminogen activator(uPA)

PDB ID 3qn7

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