Abstract
Proteinase-activated receptors are a family of seven-transmembrane G-protein-coupled receptors. Activation of PARs is initiated through cleavage of the N-terminus, unmasking a tethered ligand that can then interact with the receptor and lead to its activation. PARs exhibit both anti- and pro-inflammatory properties, although recent evidence has pointed towards a detrimental role for PARs, particularly PAR-2, in arthritis. Initial research using PAR-2 knockout mice identified PAR-2 as a key mediator of chronic joint inflammation. Further research examined the role of PAR-2 in human articular cell types, demonstrating upregulation of PAR-2 in cells from an inflammatory background compared with non-inflammatory cells, with PAR-2 levels being further upregulated by pro-inflammatory cytokines and growth factors. To date, there is no clinical evidence of a role for PAR-2 in vivo in humans, although recent studies utilizing human joint tissue and articular cells are emerging.
Original language | English |
---|---|
Pages (from-to) | 334-338 |
Number of pages | 5 |
Journal | Current Opinion in Pharmacology |
Volume | 56 |
Issue number | 3 |
Early online date | 21 Mar 2007 |
DOIs | |
Publication status | Published - 30 Jun 2007 |
Keywords
- PAR2
- Arthritis
- Proteinase-activated receptor