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Protease-activated receptor-2 (PAR-2): a potential new target in arthritis

Ferrell, W.R. and Lockhart, J.C. and Plevin, R.J. (2008) Protease-activated receptor-2 (PAR-2): a potential new target in arthritis. Drugs of the Future, 33 (3). pp. 241-248. ISSN 0377-8282

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Abstract

Protease-activated receptors (PARs) are a novel family of seven-transmembrane G-protein-coupled receptors. The unique feature of this family is that activation is initiated by cleavage of the N-terminus by serine or other proteases, thereby unmasking a tethered ligand that then interacts with the receptor, leading to activation. PARs have been described in the context of inflammation, and recent evidence indicates a particular role for the second member of this family, PAR-2, in arthritis. Synovial expression of this receptor is greatly upregulated in murine models of arthritis, and both acute and chronic experimental monoarthritis are substantially attenuated in Par2 knockout mice, suggesting a key role for PAR-2 in inflammatory joint disease. These findings translate to inflammatory disease in humans, since PAR-2 expression is upregulated in synovial tissues from patients with rheumatoid arthritis (RA), and appears to be an upstream regulator of proinflammatory cytokine generation, including tumor necrosis factor alpha (TNF-alpha). These findings identify PAR-2 as a new therapeutic target in the management of RA, and the challenge is now to develop potent and selective agents to prevent activation of this receptor.

Item type: Article
ID code: 19730
Keywords: arthritis, inflammatory joint disease, protease-activated receptor-2, PAR-2, Pharmacy and materia medica, Therapeutics. Pharmacology
Subjects: Medicine > Pharmacy and materia medica
Medicine > Therapeutics. Pharmacology
Department: Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
Related URLs:
    Depositing user: Strathprints Administrator
    Date Deposited: 26 May 2010 18:32
    Last modified: 12 Mar 2012 11:13
    URI: http://strathprints.strath.ac.uk/id/eprint/19730

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