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Proteinase‐activated receptor expression and function in the brain
Author(s) -
Noorbakhsh Farshid,
Power Christopher
Publication year - 2003
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.10320
Subject(s) - biology , receptor , central nervous system , signal transduction , neuroscience , protease activated receptor , g protein coupled receptor , nervous system , neuroprotection , pathogenesis , microbiology and biotechnology , thrombin , immunology , genetics , platelet
Proteinase‐activated receptors (PARs) represent a novel family of G‐protein coupled receptors that mediate the diverse biologic effects of proteinases on target cells. Four different members of the PAR family have been identified so far: PAR 1 , PAR 3 , and PAR 4 act as receptors for thrombin, and PAR 2 is activated by trypsin/tryptase. It is now known that all four subtypes of PARs are widely expressed in the central nervous system, and there is increasing evidence to suggest roles for proteinases and PARs in development and pathogenesis in the nervous system. Harnessing different G proteins and a variety of signal transduction cascades, PARs can affect neural cell proliferation, morphology, and electrical activities. PARs have also been considered as major players in neuroinflammatory/degenerative processes in which they play both neuroprotective and neuropathogenic roles. The advent of PARs agonistic and antagonistic peptides, which selectively activate their cognate receptor and mediate a broad spectrum of PAR‐executed effects in the nervous system, makes these peptides attractive therapeutic possibilities. Herein we review different aspects of PARs activities in the normal development and function of the brain and address some evidence related to PARs roles in nervous system pathogenesis with a focus on neuroinflammatory/degenerative disorders. Drug Dev. Res. 60:51–57, 2003. © 2003 Wiley‐Liss, Inc.