HTS037C - ChemiSCREEN™ Human PAR-2 Receptor Calcium-Optimized Stable Cell Line

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    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).  The cloned human PAR2-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant PAR2 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway.  Thus, the cell line is an ideal tool for screening for antagonists of interactions between PAR2 and its ligands.

    Additional Resource :  HTS037C060315 Datasheet

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    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human PAR2 cDNA (Accession Number: AY336105) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Cocks TM et al. (1999) A protective role for protease-activated receptors in the airways. Nature 398: 156-60.
    Reference 2: 2. Coelho AM et al. (2003) Proteinase-activated receptor-2: physiological and pathophysiological roles. Curr. Med. Chem. Cardiovasc. Hematol. Agents. 1: 61-72.
    Reference 3: 3. Hansen KK et al. (2005) A major role for proteolytic activity and proteinase-activated receptor-2 in the pathogenesis of infectious colitis. Proc. Natl. Acad. Sci. USA. 102: 8363-8.
    Reference 4: 4. Kawabata et al. (2004) Potent and metabolically stable agonists for protease-activated receptor-2: evaluation of activity in multiple assay systems in vitro and in vivo. J. Pharmacol. Exp. Ther. 309: 1098-1107.
    Reference 5: 5. Lindner JR et al. (2000) Delayed onset of inflammation in protease-activated receptor-2-deficient mice. J. Immunol. 165: 6504-10.
    Reference 6: 6. Macfarlane SR et al. (2001) Proteinase-activated receptors. Pharmacol Rev. 53: 245-82.