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Nat Rev Drug Discov. 2012 Jan 3;11(1):69-86. doi: 10.1038/nrd3615.

Targeting proteinase-activated receptors: therapeutic potential and challenges.

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Department of Physiology and Pharmacology, Faculty of Medicine, University of Calgary, Alberta T2N 4N1, Canada.


Proteinase-activated receptors (PARs), a family of four seven-transmembrane G protein-coupled receptors, act as targets for signalling by various proteolytic enzymes. PARs are characterized by a unique activation mechanism involving the proteolytic unmasking of a tethered ligand that stimulates the receptor. Given the emerging roles of these receptors in cancer as well as in disorders of the cardiovascular, musculoskeletal, gastrointestinal, respiratory and central nervous system, PARs have become attractive targets for the development of novel therapeutics. In this Review we summarize the mechanisms by which PARs modulate cell function and the roles they can have in physiology and diseases. Furthermore, we provide an overview of possible strategies for developing PAR antagonists.

[Indexed for MEDLINE]

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