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2viv

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==FRAGMENT-BASED DISCOVERY OF MEXILETINE DERIVATIVES AS ORALLY BIOAVAILABLE INHIBITORS OF UROKINASE-TYPE PLASMINOGEN ACTIVATOR==
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<StructureSection load='2viv' size='340' side='right' caption='[[2viv]], [[Resolution|resolution]] 1.72&Aring;' scene=''>
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==Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator==
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<StructureSection load='2viv' size='340' side='right'caption='[[2viv]], [[Resolution|resolution]] 1.72&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[2viv]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VIV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2VIV FirstGlance]. <br>
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<table><tr><td colspan='2'>[[2viv]] is a 1 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=2VIV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VIV FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=VG2:4-(2-AMINOETHOXY)-N-(3-CHLORO-5-PIPERIDIN-1-YLPHENYL)-3,5-DIMETHYLBENZAMIDE'>VG2</scene></td></tr>
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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=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=VG2:4-(2-AMINOETHOXY)-N-(3-CHLORO-5-PIPERIDIN-1-YLPHENYL)-3,5-DIMETHYLBENZAMIDE'>VG2</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1c5x|1c5x]], [[1gj9|1gj9]], [[1w0z|1w0z]], [[1fv9|1fv9]], [[1vja|1vja]], [[1gj8|1gj8]], [[1w11|1w11]], [[1sqo|1sqo]], [[1gjd|1gjd]], [[1w10|1w10]], [[1owk|1owk]], [[1w12|1w12]], [[1gi9|1gi9]], [[1o5a|1o5a]], [[1c5z|1c5z]], [[1owj|1owj]], [[1gi7|1gi7]], [[1o5b|1o5b]], [[1gjc|1gjc]], [[1sc8|1sc8]], [[1gja|1gja]], [[1o3p|1o3p]], [[1owe|1owe]], [[1sqa|1sqa]], [[1gjb|1gjb]], [[1f92|1f92]], [[1owi|1owi]], [[1kdu|1kdu]], [[1sqt|1sqt]], [[1f5l|1f5l]], [[1owd|1owd]], [[1ejn|1ejn]], [[1lmw|1lmw]], [[1u6q|1u6q]], [[1gi8|1gi8]], [[2jde|2jde]], [[1c5y|1c5y]], [[1w14|1w14]], [[1vj9|1vj9]], [[1w13|1w13]], [[1gj7|1gj7]], [[1c5w|1c5w]], [[1owh|1owh]], [[1o5c|1o5c]], [[2viw|2viw]], [[2viq|2viq]], [[2vin|2vin]], [[2vio|2vio]], [[2vip|2vip]]</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1c5x|1c5x]], [[1gj9|1gj9]], [[1w0z|1w0z]], [[1fv9|1fv9]], [[1vja|1vja]], [[1gj8|1gj8]], [[1w11|1w11]], [[1sqo|1sqo]], [[1gjd|1gjd]], [[1w10|1w10]], [[1owk|1owk]], [[1w12|1w12]], [[1gi9|1gi9]], [[1o5a|1o5a]], [[1c5z|1c5z]], [[1owj|1owj]], [[1gi7|1gi7]], [[1o5b|1o5b]], [[1gjc|1gjc]], [[1sc8|1sc8]], [[1gja|1gja]], [[1o3p|1o3p]], [[1owe|1owe]], [[1sqa|1sqa]], [[1gjb|1gjb]], [[1f92|1f92]], [[1owi|1owi]], [[1kdu|1kdu]], [[1sqt|1sqt]], [[1f5l|1f5l]], [[1owd|1owd]], [[1ejn|1ejn]], [[1lmw|1lmw]], [[1u6q|1u6q]], [[1gi8|1gi8]], [[2jde|2jde]], [[1c5y|1c5y]], [[1w14|1w14]], [[1vj9|1vj9]], [[1w13|1w13]], [[1gj7|1gj7]], [[1c5w|1c5w]], [[1owh|1owh]], [[1o5c|1o5c]], [[2viw|2viw]], [[2viq|2viq]], [[2vin|2vin]], [[2vio|2vio]], [[2vip|2vip]]</div></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/U-plasminogen_activator U-plasminogen activator], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></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/U-plasminogen_activator U-plasminogen activator], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.73 3.4.21.73] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2viv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2viv OCA], [http://pdbe.org/2viv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2viv RCSB], [http://www.ebi.ac.uk/pdbsum/2viv PDBsum]</span></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=2viv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2viv OCA], [https://pdbe.org/2viv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2viv RCSB], [https://www.ebi.ac.uk/pdbsum/2viv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2viv ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
== Disease ==
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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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[[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>
== Function ==
== Function ==
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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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[[https://www.uniprot.org/uniprot/UROK_HUMAN UROK_HUMAN]] Specifically cleaves the zymogen plasminogen to form the active enzyme plasmin.
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
Check<jmol>
<jmolCheckbox>
<jmolCheckbox>
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<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/vi/2viv_consurf.spt"</scriptWhenChecked>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/vi/2viv_consurf.spt"</scriptWhenChecked>
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
<text>to colour the structure by Evolutionary Conservation</text>
<text>to colour the structure by Evolutionary Conservation</text>
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==See Also==
==See Also==
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*[[Urokinase|Urokinase]]
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*[[Urokinase 3D Structures|Urokinase 3D Structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Human]]
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[[Category: Large Structures]]
[[Category: U-plasminogen activator]]
[[Category: U-plasminogen activator]]
[[Category: Callaghan, O]]
[[Category: Callaghan, O]]
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[[Category: Frederickson, M]]
[[Category: Frederickson, M]]
[[Category: Matthews, J E]]
[[Category: Matthews, J E]]
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[[Category: Mcmenamin, R]]
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[[Category: McMenamin, R]]
[[Category: Smith, D]]
[[Category: Smith, D]]
[[Category: Vinkovic, M]]
[[Category: Vinkovic, M]]
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[[Category: Inhibitor]]
[[Category: Inhibitor]]
[[Category: Kringle]]
[[Category: Kringle]]
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[[Category: Pharmaceutical]]
[[Category: Phosphorylation]]
[[Category: Phosphorylation]]
[[Category: Plasminogen activation]]
[[Category: Plasminogen activation]]
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[[Category: Polymorphism]]
[[Category: Protease]]
[[Category: Protease]]
[[Category: Secreted]]
[[Category: Secreted]]

Current revision

Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator

PDB ID 2viv

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