Protease-Activated Receptor-3 (1-6), PAR-3 (1-6), human
This is amino acids 1 to 6 fragment of the protease-activated receptor 3 (PAR-3). This synthetic peptide induces ERK activation in human carcinoma cells endogeneously expressing PAR1 and PAR3. This effect is completely abolished by single alanine substitution at positions 3, 4 and 6 in the peptide. PAR-3 allosterically regulates PAR1 signaling by receptor dimerization governing increased endothelial permeability. Targeting of PAR3 may mitigate the effects of PAR1 in activating endothelial responses such as vascular inflammation. However this peptide does not affect VEGF release or expression.
Kaufmann, R. et al. Regul. Pept. 125, 61( 2005), McLaughlin, J. et al. PNAS 104, 5662 (2007), Arisato, T. et al. Cell. Mol. Life Sci. 60, 1420 (2003).