Calcium Flux Assay

HTS125C - ChemiScreen™ Human Recombinant SST4 Somatostatin Receptor Calcium-Optimized Stable Cell Line

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    Somatostatin is a 14 or 28 amino acid regulatory peptide that inhibits hormone secretion from the pituitary, pancreas, and other endocrine sites. A family of 6 GPCRs, sst1, sst2A, sst2B, sst3, sst4 and sst5, mediate the biological activity of somatostatins. The somatostatin receptors couple to Gi to inhibit cAMP production, and also increase MAP kinase signalling. Several tumors have been shown to overexpress somatostatin receptors, and binding of somatostatin to these tumor cells stimulates or inhibits proliferation, depending on the receptor subtypes expressed (Olias et al., 2004). Somatostatin has been implicated in seizure susceptibility in animal models, and activation of sst4 with selective agonists increases seizure activity (Moneta et al., 2002). The cloned human SST4-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant SST4 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 the SST4 and its ligands.

    Additional Resource :  HTS125C060515 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 SST4 cDNA (Accession Number: NM_001052) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Moneta D et al. (2002) Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur. J. Neurosci. 16: 843-9.
    Reference 2: 2. Olias G et al. (2004) Regulation and function of somatostatin receptors. J. Neurochem. 89: 1057-1091.