Plasminogen activator inhibitor
From Proteopedia
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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'> | |
| - | + | == Function == | |
'''Plasminogen activator inhibitor''' (PAI) is a serine protease inhibitor.<br /> | '''Plasminogen activator inhibitor''' (PAI) is a serine protease inhibitor.<br /> | ||
| - | * '''PAI-1''' inhibits tissue plasminogen activator and urokinase.<br /> | + | * '''PAI-1''' inhibits tissue plasminogen activator and urokinase<ref>PMID:15634264</ref>.<br /> |
| - | * '''PAI-2''' is secreted by the placenta and is present during pregnancy.<br /> | + | * '''PAI-2''' is secreted by the placenta and is present during pregnancy<ref>PMID:18690354</ref>.<br /> |
| - | * '''PAI-3''' inhibits enzymes in blood coagulation. | + | * '''PAI-3''' or '''protein C inhibitor''' inhibits enzymes in blood coagulation<ref>PMID:12139754</ref>. |
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| + | == Relevance == | ||
| + | Inhibitors of PAI-1 are tested as therapeutical strategy against renal and cardiovascular diseases<ref>PMID:19322185</ref>. | ||
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| + | == Structural highlights == | ||
| + | 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 == | ||
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**[[4ic0]] - hPAI-1 (mutant) + gallate<br /> | **[[4ic0]] - hPAI-1 (mutant) + gallate<br /> | ||
**[[3ut3]] - hPAI-1 (mutant) + inhibitor<br /> | **[[3ut3]] - hPAI-1 (mutant) + inhibitor<br /> | ||
| - | **[[4aqh]] - hPAI-1 + inhibitor<br /> | + | **[[4aqh]], [[7aqf]], [[7aqg]] - hPAI-1 + inhibitor<br /> |
**[[1oc0]] - hPAI-1 (mutant) + vitronectin<br /> | **[[1oc0]] - hPAI-1 (mutant) + vitronectin<br /> | ||
**[[3pb1]] - hPAI-1 (mutant) + urokinase (mutant)<br /> | **[[3pb1]] - hPAI-1 (mutant) + urokinase (mutant)<br /> | ||
| + | **[[6i8s]] - hPAI-1 (mutant) + antibody<br /> | ||
| + | **[[6gwn]], [[6gwp]], [[6gwq]], [[6zrv]] - hPAI-1 (mutant) + nanobody<br /> | ||
| + | **[[5zlz]] - hPAI-1 (mutant) + tissue-type PA<br /> | ||
| + | **[[5brr]] - hPAI-1 (mutant) + plasminogen activator catalytic domain (mutant) <br /> | ||
**[[3lw2]] – PAI-1 - mouse<br /> | **[[3lw2]] – PAI-1 - mouse<br /> | ||
**[[4kds]] – PAI-1 – trout<br /> | **[[4kds]] – PAI-1 – trout<br /> | ||
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**[[1lq8]], [[3dy0]] – hPAI-3 cleaved | **[[1lq8]], [[3dy0]] – hPAI-3 cleaved | ||
}} | }} | ||
| + | == References == | ||
| + | <references/> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
Current revision
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3D Structures of plasminogen activator inhibitor
Updated on 12-January-2022
References
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
