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4g8r

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{{STRUCTURE_4g8r| PDB=4g8r | SCENE= }}
 
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===Crystal Structure of a novel small molecule inactivator bound to plasminogen activator inhibitor-1===
 
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{{ABSTRACT_PUBMED_24297881}}
 
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==Disease==
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==Crystal Structure of a novel small molecule inactivator bound to plasminogen activator inhibitor-1==
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[[http://www.uniprot.org/uniprot/PAI1_HUMAN PAI1_HUMAN]] Defects in SERPINE1 are the cause of plasminogen activator inhibitor-1 deficiency (PAI-1D) [MIM:[http://omim.org/entry/613329 613329]]. It is a hematologic disorder characterized by increased bleeding after trauma, injury, or surgery. Affected females have menorrhagia. The bleeding defect is due to increased fibrinolysis of fibrin blood clots due to deficiency of plasminogen activator inhibitor-1, which inhibits tissue and urinary activators of plasminogen.<ref>PMID:9207454</ref> Note=High concentrations of SERPINE1 seem to contribute to the development of venous but not arterial occlusions.
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<StructureSection load='4g8r' size='340' side='right'caption='[[4g8r]], [[Resolution|resolution]] 2.19&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4g8r]] 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=4G8R OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G8R 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]] 2.19&#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=96P:(2S)-3-({[3-(TRIFLUOROMETHYL)PHENOXY]CARBONYL}AMINO)PROPANE-1,2-DIYL+BIS(3,4,5-TRIHYDROXYBENZOATE)'>96P</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=4g8r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g8r OCA], [https://pdbe.org/4g8r PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g8r RCSB], [https://www.ebi.ac.uk/pdbsum/4g8r PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g8r ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/PAI1_HUMAN PAI1_HUMAN] Defects in SERPINE1 are the cause of plasminogen activator inhibitor-1 deficiency (PAI-1D) [MIM:[https://omim.org/entry/613329 613329]. It is a hematologic disorder characterized by increased bleeding after trauma, injury, or surgery. Affected females have menorrhagia. The bleeding defect is due to increased fibrinolysis of fibrin blood clots due to deficiency of plasminogen activator inhibitor-1, which inhibits tissue and urinary activators of plasminogen.<ref>PMID:9207454</ref> Note=High concentrations of SERPINE1 seem to contribute to the development of venous but not arterial occlusions.
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== Function ==
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[https://www.uniprot.org/uniprot/PAI1_HUMAN PAI1_HUMAN] Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis.<ref>PMID:15853774</ref>
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==Function==
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==See Also==
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[[http://www.uniprot.org/uniprot/PAI1_HUMAN PAI1_HUMAN]] Serine protease inhibitor. This inhibitor acts as 'bait' for tissue plasminogen activator, urokinase, protein C and matriptase-3/TMPRSS7. Its rapid interaction with PLAT may function as a major control point in the regulation of fibrinolysis.<ref>PMID:15853774</ref>
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*[[Plasminogen activator inhibitor|Plasminogen activator inhibitor]]
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== References ==
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==About this Structure==
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<references/>
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[[4g8r]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4G8R OCA].
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__TOC__
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</StructureSection>
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==Reference==
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[[Category: Homo sapiens]]
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<ref group="xtra">PMID:024297881</ref><references group="xtra"/><references/>
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[[Category: Large Structures]]
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[[Category: Lawrence, D A.]]
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[[Category: Lawrence DA]]
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[[Category: Li, S H.]]
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[[Category: Li S-H]]
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[[Category: Stuckey, J A.]]
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[[Category: Stuckey JA]]
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[[Category: Blood clotting]]
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[[Category: Blood clotting-inhibitor complex]]
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[[Category: Inhibitor]]
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[[Category: Pai-1]]
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[[Category: Serpin]]
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Current revision

Crystal Structure of a novel small molecule inactivator bound to plasminogen activator inhibitor-1

PDB ID 4g8r

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