Abstract
Purpose: Serine proteinases such as thrombin and cathepsin-G are known to cleave and subsequently activate proteinase activated receptor-4 (PAR-4). In joints, selective peptide ligands that bind to PAR-4 cause sensitization of joint nociceptors and impart a marked pain response. Furthermore, blockade of PAR-4 with the antagonist pepducin p4Pal10 has been shown to reduce peripheral sensitization and joint pain, as well as ameliorating physiological signs of inflammation in an acute synovitis model.
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