Protease-Activated Receptor Antagonists

Protease-activated receptors (PARs, also known as thrombin receptors) are G-protein-coupled receptors, activated by cleavage of their N-terminal domains by serine proteases. Hydrolysis reveals a tethered peptide ligand, which interacts with the receptor within extracellular loop-2 to affect transmembrane signaling. Four subtypes of receptors have so far been cloned (PAR_1-4).

PAR₁ is the most well characterized member of this receptor family and is activated by the endogenous serine protease ...