Function
Plasminogen activator inhibitor (PAI) is a serine protease inhibitor.
- PAI-1 inhibits tissue plasminogen activator and urokinase[1].
- PAI-2 is secreted by the placenta and is present during pregnancy[2].
- PAI-3 or protein C inhibitor inhibits enzymes in blood coagulation[3].
Relevance
Inhibitors of PAI-1 are tested as therapeutical strategy against renal and cardiovascular diseases[4].
Structural highlights
A PAI-1 inhibitor tested for its therapeutic value is bound in the active site[5]. Water molecules are shown as red spheres.
- ↑ Lijnen HR. Pleiotropic functions of plasminogen activator inhibitor-1. J Thromb Haemost. 2005 Jan;3(1):35-45. PMID:15634264 doi:https://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:https://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:https://dx.doi.org/10.1074/jbc.M112.371732
