Title: The Biochemistry, Physiology and Pathological roles of PAI-1 and the requirements for PAI-1 inhibition in vivo
Authors: Van De Craen, Britt
Declerck, Paul
Gils, Ann # ×
Issue Date: Oct-2012
Publisher: Pergamon Press
Series Title: Thrombosis Research vol:130 issue:4 pages:576-585
Abstract: Plasminogen activator inhibitor-1 (PAI-1) is the primary physiological inhibitor of both tissue-type plasminogen activator (t-PA) and urokinase-type plasminogen activator (u-PA) and is consequently one the most important inhibitors of the plasminogen/plasmin system. PAI-1 attenuates fibrinolysis and increased levels of active PAI-1 have been associated with an increased risk for cardiovascular diseases. PAI-1 knock-out mice as well as PAI-1 overexpressing mice have been generated and characterized to study the role of PAI-1 in vivo. A number of PAI-1 inhibitors have been generated to study the pharmacological effect of PAI-1 inhibition in vitro and in vivo. The current review provides an overview of 1) the biochemical features of PAI-1, 2) the role of PAI-1 in diverse pathologies, 3) the in vitro and in vivo data obtained with PAI-1 inhibitors and 4) the vitronectin, glycosylation and species dependency of PAI-1 inhibition.
ISSN: 0049-3848
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory for Pharmaceutical Biology (-)
× corresponding author
# (joint) last author

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