Plasminogen activator inhibitor-1.
Plasminogen activator inhibitor-1 (PAI-1) is an important component of the plasminogen/plasmin system as it is the main inhibitor of tissue-type and urokinase-type plasminogen activator. Consequently, PAI-1 plays an important role in cardiovascular diseases (mainly through inhibition of t-PA) and in cell migration and tumor development (mainly through inhibition of u-PA). As a member of the serpin superfamily, PAI-1 shares important structural properties with other serpins. However, PAI-1 also exhibits unique conformational and functional properties. The current paper provides an overview of the knowledge on PAI-1 gathered since its discovery two decades ago. We are discussing (a) its structural properties and their subsequent association with the functional properties, (b) its role in a wide variety of (patho)physiological processes and (c) a number of strategies to interfere with its functional properties eventually aiming at pharmacological modulation of this risk factor.
Gils
Ann
A
Laboratory for Pharmaceutical Biology and Phytopharmacology, Katholieke Universsiteit Leuven, Van Evenstraat 4, B-3000 Leuven, Belgium. ann.gils@pharm.kuleuven.ac.be
Declerck
Paul J
PJ
D002318:Cardiovascular Diseases / Q000378:metabolism*; D002465:Cell Movement; D005342:Fibrinolysis / Q000187:drug effects*; D006801:Humans; D017395:Plasminogen Activator Inhibitor 1 / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011485:Protein Binding; D012307:Risk Factors; D013379:Substrate Specificity; D013927:Thrombosis / Q000378:metabolism
D017395:Plasminogen Activator Inhibitor 1