Encyclopedia of Biological Chemistry: Second Edition
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© 2013 Elsevier Inc. All rights reserved. Serine proteinases signal to cells by cleaving and activating a four-member family of seven-transmembrane G-protein-coupled receptors (GPCRs) termed, proteinase-activated receptors (PARs). PARs are unique among GPCRs in having a mechanism of activation that involves the proteolytic cleavage and unmasking of a tethered ligand which activates the receptor. We provide here a brief overview of PAR expression in different tissues and the key roles for PARs in normal physiology and diseases. We also briefly describe the development of agonists and antagonists that can target this family of receptors.