The Proteinase-Activated Receptors (PARs) are a diverse member of the G protein-coupled receptor (GPCR) family. They are activated primarily by proteases and are comprised of four types, with PAR1, PAR3, and PAR4 being activated by thrombin and PAR2 activated by trypsin. Upon protease cleavage, a tethered ligand is exposed at the N-terminus that is able activate intracellular signaling by binding to a conserved region in the second extracellular loop.1 PAR1 and PAR2 are expressed by a wide number of tumor cells including breast and colon cancers, suggesting a role in angiogenesis.2,3
PAR-activating peptides (PAR-APs) mimic the tethered ligand domains of the PARs and can activate by stimulating receptors in a protease-independent manner. Peptides International offers a variety of PAR-AP agonists and antagonists for your research needs.
1. M.D. Hollenberg and S.J. Compton, Pharm. Rev., 54, 203 (2002). (Review)
2. D. Darmoul, et al., Am. J. Patho., 162, 1503 (2003).
3. B. Even-Ram, et al., Nat. Med., 4, 909 (1998).
Don't miss out, this offer ends October 22 at 6:00 pm ET!
Please note: Limited time offer. Discounts cannot be applied to previous orders or combined with other discounts or offers. Discount will be taken at invoicing.