Merck Millipore PAR2 Membrane Preparation recombinant Human

The protease-activated receptor family of GPCRs has a unique mechanism of activation, in which protease cleaves a prodomain to reveal a peptide sequence that functions as a tethered ligand to activate the receptor (Macfarlane et al., 2001). PAR2 is specifically activated by trypsin and mast cell tryptase, and can also be activated by free peptide analogs of the tethered ligand, such as SLIGRL and furoyl-LIGRLO (Coelho et al., 2003; Kawabata et al., 2004). PAR2 is expressed in endothelium, gastrointestinal epithelium, macrophages, eosinophils and nociceptive afferent neurons. Activation of PAR2 in these cells and tissues promotes vasodilation, inflammation, allergy, hyperalgesia and intestinal permeability. Therefore, PAR2 is regarded as an attractive therapeutic target for colitis, asthma, myocardial ischemia/reperfusion injury, and pain (Cocks et al., 1999; Hansen et al., 2005; Lindner et al., 2000; McLean et al., 2002; Vergnolle et al., 2001). Chemicon's PAR2 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of antagonists of PAR2 interactions with its ligands. The membrane preparations exhibit an EC50 of 1.9 μM for furoyl-LIGRLO in a GTPγS binding assay.