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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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.
| Creators(s): |
Ferrell, W.R., Lockhart, J.C. and Plevin, R.J.  ORCID: https://orcid.org/0000-0002-7849-1220;
| Item type: | Article |
|---|---|
| ID code: | 19730 |
| Keywords: | arthritis, inflammatory joint disease, protease-activated receptor-2, PAR-2, Pharmacy and materia medica, Therapeutics. Pharmacology, Pharmacology, Pharmacology (medical) |
| Subjects: | Medicine > Pharmacy and materia medica Medicine > Therapeutics. Pharmacology |
| Department: | Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences |
| Depositing user: | Strathprints Administrator |
| Date deposited: | 26 May 2010 17:32 |
| Last modified: | 20 Jan 2021 18:33 |
| URI: | https://strathprints.strath.ac.uk/id/eprint/19730 |
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