Physiology and Pharmacology Publications
Proteinase-Activated Receptors
Document Type
Article
Publication Date
2-15-2013
Journal
Encyclopedia of Biological Chemistry: Second Edition
First Page
601
Last Page
606
URL with Digital Object Identifier
10.1016/B978-0-12-378630-2.00398-4
Abstract
© 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.