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Vascular PAR-1: Activity and Antagonism

Authors :
Ninian N. Lang
Ingibjörg J. Guðmundsdóttir
David E. Newby
Source :
Cardiovascular Therapeutics. 29:349-361
Publication Year :
2010
Publisher :
Wiley, 2010.

Abstract

Despite major advances in antiplatelet therapies, recurrent cardiovascular events remain high after acute coronary syndrome. Furthermore, incremental benefits achieved in the reduction of atherothrombotic events have almost always been at the expense of hemorrhagic side effects. Thrombin is the most potent platelet activating factor known and it makes important interactions with the endothelium and vascular smooth muscle with proinflammatory, proatherogenic effects. Distinct from its activity within the coagulation cascade, thrombin mediates these effects via protease-activated receptor type 1 (PAR-1) in man. This review discusses the role of PAR-1 in the vasculature and the development of novel PAR-1 antagonists. These drugs may provide important antiatherothrombotic effects without attendant bleeding complications and could represent a major breakthrough for the treatment of cardiovascular diseases.

Details

ISSN :
17555914
Volume :
29
Database :
OpenAIRE
Journal :
Cardiovascular Therapeutics
Accession number :
edsair.doi...........feda4ce008a877c34e45dbd8cbecf272
Full Text :
https://doi.org/10.1111/j.1755-5922.2010.00140.x