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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Plasminogen Activator Inhibitor-1

Author(s): Ann Gils and Paul J. Declerck

Volume 11, Issue 17, 2004

Page: [2323 - 2334] Pages: 12

DOI: 10.2174/0929867043364595

Price: $65

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: pai-1, serpin, fibrinolysis, thrombosis


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