PAR2: Small Molecules and Peptides

Protease-Activated Receptor 2 (PAR2) is a protease activated 7-transmembrane G-protein-coupled receptor. Human PAR2 contains a cleavage site for trypsin, mast cell tryptase or coagulation factor VIIa or Xa, 11 amino acids (aa) C-terminal to the signal sequence. Cleavage creates a tethered ligand that activates the 361 aa receptor. PAR2 is expressed in kidney, pancreas, stomach, intestine, airway, skin, bladder and brain; activation stimulates release of inflammatory and nociceptive mediators. PAR2 is downregulated by ubiquination, endocytosis and degradation. Mature human PAR2 shows 78% amino acid identity with mouse PAR2 over the extracellular portions.