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First published on September 15, 2004; DOI: 10.1124/mol.104.003103


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Received for publication May 25, 2004.
Revised August 10, 2004.
Accepted for publication September 7, 2004.

THE CARDIOVASCULAR ACTIONS OF PROTEASE-ACTIVATED RECEPTORS

Susan F. Steinberg 1*

1 Columbia University

* Address correspondence to: E-mail: sfs1{at}columbia.edu

Abstract

Protease-activated receptors (PARs) comprise a family of G protein coupled receptors with a unique proteolytic activation mechanism. PARs are activated by thrombin or other coagulation or inflammatory proteases formed at sites of tissue injury. PARs play a particularly important role in pathogenesis of clinical disorders characterized by chronic inflammation or smoldering activation of the coagulation cascade. Individual PARs have been linked to the regulation of a broad range of cellular functions. Recent studies identify PAR family members in the vasculature (including within atherosclerotic lesions) and in the heart. Here, PAR- triggered responses contribute to vasoregulation and influence cardiac electrical and mechanical activity. PAR activation also is linked to structural remodeling of the vasculature and the myocardium. This review focuses on the cardiovascular actions of PARs that play a role in normal cardiovascular physiology and are likely to contribute to cardiovascular diseases.


Key words: Thrombin/PAR, Ischemia/Reperfusion


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