Calcium Flux Assay

HTS033C - ChemiSCREEN™ Human GPR14 Urotensin II Receptor Calcium-Optimized Stable Cell Line

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    Urotensin II, a cyclic 11-13 residue peptide expressed in motoneurons of the spinal cord, acts as a potent vasoconstrictor (Coulouarn et al., 1998;  Ames et al., 1999).  The effects of urotensin II are mediated by binding to a GPCR, GPR14, which is expressed in endothelium, smooth muscle, heart and pancreas (Ames et al., 1999).  Genetic deletion of GPR14 in mice renders aortae refractile to the contractile activity of urotensin II without changing baseline hemodynamics (Behm et al., 2003).  Pharmacological inhibition of urotensin II/GPR14 interactions prevents renal insufficiency following renal artery ligation (Clozel et al., 2004).  Thus, GPR14 is an attractive target for a number of cardiovascular diseases.  The cloned human GPR14-expressing cell line is made in the Chem-2 host, which supports high levels of recombinant GPR14 expression on the cell surface and contains high levels of the promiscuous G protein Gα16 to couple the receptor to the calcium signaling pathway.  Thus, the cell line is an ideal tool for screening for antagonists of interactions between GPR14 and its ligands.  

    Additional Resource :  HTS033C051115 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-2, a suspension cell line endogenously expressing the promiscuous G protein, Gα15, and lacking endogenous expression of A3.
    Exongenous Gene Expression: GPR14 cDNA (Accession Number: AF_140631) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Ames R.S. et al. (1999). Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature 401:282-286.
    Reference 2: 2. Behm D.J. et al. (2003). Deletion of the UT receptor gene results in the selective loss of urotensin-II contractile activity in aortae isolated from UT receptor knockout mice. Br. J. Pharmacol. 139:464-472.
    Reference 3: 3. Clozel M. et al. (2004). Pharmacology of the Urotensin-II Receptor Antagonist ACT- 058362: First Demonstration of a Pathophysiological Role of the Urotensin System. J. Pharmacol. Exp. Ther., 2004 May 14, epub ahead of print.
    Reference 4: 4. Coulouarn Y. et al. (1998). Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord. Proc. Natl. Acad. Sci. USA 95:15803-15808.