Biological Activity
PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1 It binds to NCTC 2544 cells expressing human PAR2 (Ki = 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50 = 0.075 μM).2 PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1 It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3 PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4
References
1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996)
2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005)
3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001)
4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)
