Protease-activated Receptor 2 Opportunities for Anti-inflammatory Drug Discovery

摘要

Protease-activated receptors (PARs) are unusual members of the GPCR family because they are activated by cleavage of their N-terminal region by an extracellular protease. PARs 1,3 and 4 are receptors for thrombin. PAR-2 is activated by trypsin and/or tryptase. PAR-2 may be involved in inflammation and fibrosis and may be a potential therapeutic target. Various drug discovery strategies are being used to find both agonists and antagonists selective for PAR-2.