Plasminogen Activator Inhibitor-1

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Abstract:

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.

Keywords: fibrinolysis; pai-1; serpin; thrombosis

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867043364595

Affiliations: Laboratory for Pharmaceutical Biology and Phytopharmacology, Faculty of Pharmaceutical Sciences, Katholieke Universiteit Leuven, E. Van Evenstraat 4 B-3000 Leuven, Belgium.

Publication date: September 1, 2004

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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