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
Current Medicinal Chemistry
Title: Plasminogen Activator Inhibitor-1
Volume: 11 Issue: 17
Author(s): Ann Gils and Paul J. Declerck
Affiliation:
Keywords: pai-1, serpin, fibrinolysis, thrombosis
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.
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Cite this article as:
Gils Ann and Declerck J. Paul, Plasminogen Activator Inhibitor-1, Current Medicinal Chemistry 2004; 11 (17) . https://dx.doi.org/10.2174/0929867043364595
DOI https://dx.doi.org/10.2174/0929867043364595 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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