Plasminogen activator inhibitor

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{{STRUCTURE_1c5g| PDB=1c5g | SIZE=400| SCENE= |right|CAPTION=Human plasminogen activator inhibitor 1, [[1c5g]] }}
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<StructureSection load='' size='450' side='right' caption='Human plasminogen activator inhibitor 1 complex with inhibitor (PDB entry [[4aqh]])' scene='47/476005/Cv/1'>
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== Function ==
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'''Plasminogen activator inhibitor''' (PAI) is a serine protease inhibitor.<br />
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* '''PAI-1''' inhibits tissue plasminogen activator and urokinase<ref>PMID:15634264</ref>.<br />
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* '''PAI-2''' is secreted by the placenta and is present during pregnancy<ref>PMID:18690354</ref>.<br />
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* '''PAI-3''' or '''protein C inhibitor''' inhibits enzymes in blood coagulation<ref>PMID:12139754</ref>.
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'''Plasminogen activator inhibitor''' (PAI) is a serine protease inhibitor. PAI-1 inhibits tissue plasminogen activator and urokinase. PAI-2 is secreted by the placenta and is present during pregnancy. PAI-3 inhibits enzymes in blood coagulation.
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== Relevance ==
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Inhibitors of PAI-1 are tested as therapeutical strategy against renal and cardiovascular diseases<ref>PMID:19322185</ref>.
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{{TOC limit|limit=2}}
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== Structural highlights ==
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A <scene name='47/476005/Cv/4'>PAI-1 inhibitor tested for its therapeutic value is bound in the active site</scene><ref>PMID:23155046</ref>. Water molecules are shown as red spheres.
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</StructureSection>
== 3D Structures of plasminogen activator inhibitor ==
== 3D Structures of plasminogen activator inhibitor ==
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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{{#tree:id=OrganizedByTopic|openlevels=0|
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===PAI-1===
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*Plasminogen activator inhibitor-1
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[[1c5g]], [[1lj5]] - hPAI-1 – human<br />
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[[1b3k]], [[1db2]], [[1dvm]], [[1dvn]], [[3cvm]], [[3eox]], [[3q02]], [[3q03]], [[3r4l]] - hPAI-1 (mutant)<br />
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[[1a7c]], [[9pai]] – hPAI-1 (mutant) + polypeptide <br />
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[[4g8r]], [[4g8o]] – hPAI-1 + inactivator<br />
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[[4ic0]] - hPAI-1 (mutant) + gallate<br />
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[[3ut3]] - hPAI-1 (mutant) + inhibitor<br />
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[[3aqh]] - hPAI-1 + inhibitor<br />
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[[1oc0]] - hPAI-1 (mutant) + vitronectin<br />
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[[3pb1]] - hPAI-1 (mutant) + urokinase (mutant)<br />
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[[3lw2]] – PAI-1 - mouse<br />
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[[4kds]] – PAI-1 – trout<br />
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[[4dte]] – PAI-1 – zebra fish<br />
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===PAI-2===
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**[[1c5g]], [[1lj5]] - hPAI-1 – human<br />
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**[[1b3k]], [[1db2]], [[1dvm]], [[1dvn]], [[3cvm]], [[3eox]], [[3q02]], [[3q03]], [[3r4l]] - hPAI-1 (mutant)<br />
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**[[1a7c]], [[9pai]] – hPAI-1 (mutant) + polypeptide <br />
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**[[4g8r]], [[4g8o]] – hPAI-1 + inactivator<br />
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**[[4ic0]] - hPAI-1 (mutant) + gallate<br />
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**[[3ut3]] - hPAI-1 (mutant) + inhibitor<br />
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**[[4aqh]], [[7aqf]], [[7aqg]] - hPAI-1 + inhibitor<br />
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**[[1oc0]] - hPAI-1 (mutant) + vitronectin<br />
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**[[3pb1]] - hPAI-1 (mutant) + urokinase (mutant)<br />
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**[[6i8s]] - hPAI-1 (mutant) + antibody<br />
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**[[6gwn]], [[6gwp]], [[6gwq]], [[6zrv]] - hPAI-1 (mutant) + nanobody<br />
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**[[5zlz]] - hPAI-1 (mutant) + tissue-type PA<br />
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**[[5brr]] - hPAI-1 (mutant) + plasminogen activator catalytic domain (mutant) <br />
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**[[3lw2]] – PAI-1 - mouse<br />
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**[[4kds]] – PAI-1 – trout<br />
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**[[4dte]] – PAI-1 – zebra fish<br />
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[[1by7]] - hPAI-2 (mutant)<br />
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*Plasminogen activator inhibitor-2
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[[1jrr]], [[2arq]], [[2arr]] - hPAI-2 (mutant) + polypeptide
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===PAI-3===
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**[[1by7]] - hPAI-2 (mutant)<br />
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**[[1jrr]], [[2arq]], [[2arr]] - hPAI-2 (mutant) + polypeptide
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[[2ol2]] – hPAI-3<br />
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*Plasminogen activator inhibitor-3
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[[2hi9]] - hPAI-3 residues 25-387<br />
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[[1lq8]], [[3dy0]] – hPAI-3 cleaved
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**[[2ol2]] – hPAI-3<br />
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**[[2hi9]] - hPAI-3 residues 25-387<br />
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**[[1lq8]], [[3dy0]] – hPAI-3 cleaved
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}}
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== References ==
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<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]

Current revision

Human plasminogen activator inhibitor 1 complex with inhibitor (PDB entry 4aqh)

Drag the structure with the mouse to rotate

3D Structures of plasminogen activator inhibitor

Updated on 12-January-2022

References

  1. Lijnen HR. Pleiotropic functions of plasminogen activator inhibitor-1. J Thromb Haemost. 2005 Jan;3(1):35-45. PMID:15634264 doi:http://dx.doi.org/10.1111/j.1538-7836.2004.00827.x
  2. Lobov S, Croucher DR, Saunders DN, Ranson M. Plasminogen activator inhibitor type 2 inhibits cell surface associated tissue plasminogen activator in vitro: potential receptor interactions. Thromb Haemost. 2008 Aug;100(2):319-29. PMID:18690354
  3. Meijers JC, Marquart JA, Bertina RM, Bouma BN, Rosendaal FR. Protein C inhibitor (plasminogen activator inhibitor-3) and the risk of venous thrombosis. Br J Haematol. 2002 Aug;118(2):604-9. PMID:12139754
  4. Ha H, Oh EY, Lee HB. The role of plasminogen activator inhibitor 1 in renal and cardiovascular diseases. Nat Rev Nephrol. 2009 Apr;5(4):203-11. doi: 10.1038/nrneph.2009.15. PMID:19322185 doi:http://dx.doi.org/10.1038/nrneph.2009.15
  5. Fjellstrom O, Deinum J, Sjogren T, Johansson C, Geschwindner S, Nerme V, Legnehed A, McPheat J, Olsson K, Bodin C, Paunovic A, Gustafsson D. Characterization of a small molecule inhibitor of plasminogen activator inhibitor type 1 that accelerates the transition into the latent conformation. J Biol Chem. 2013 Jan 11;288(2):873-85. doi: 10.1074/jbc.M112.371732. Epub 2012, Nov 15. PMID:23155046 doi:http://dx.doi.org/10.1074/jbc.M112.371732

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