HTS032C - ChemiSCREEN™ Human GPR54 KiSS1 Receptor Calcium-Optimized Stable Cell Line

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HTS032C
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  • Product Description

    GPR54 (also known as AXOR12) is a Gq-coupled GPCR that binds to a series of peptides, termed kisspeptins or metastin, derived from the KiSS-1 gene (Kotani et al., 2001;  Muir et al., 2001).  The KiSS-1 gene inhibits metastatic activity of melanoma and other tumor cell lines, and clinical evidence supports a role for KiSS-1 and GPR54 in inhibition of metastasis in human cancer (Harms et al., 2003).  Kisspeptins and GPR54 also play a central role in hypothalamic regulation of puberty, by directly governing the release of gonadotropin-releasing hormone from the hypothalamus (Messager et al., 2005;  Shahab et al., 2005).  In addition, mutations in GPR54 in mice and humans result in hypogonadotropic hypogonadism (Colledge, 2004;  Seminara et al., 2004).  The cloned human GPR54-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant GPR54 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 agonists and antagonists of GPR54.

    Additional Resource :  HTS032C051115 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 GPR54 cDNA (Accession Number: NM_032551) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Colledge WH (2004) GPR54 and puberty. Trends Endocrinol. Metab. 15: 448-53.
    Reference 2: 2. Harms JF et al. (2003) KISS1 metastasis suppression and emergent pathways. Clin. Exp. Metastasis 20: 11-8.
    Reference 3: 3. Kotani M et al. (2001) The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276: 34631-6.
    Reference 4: 4. Kotani M et al. (2001) The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276: 34631-6.
    Reference 5: 5. Muir AI et al. (2001) AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1. J. Biol. Chem. 276: 28969-75.
    Reference 6: 6. Shahab M et al. (2005) Increased hypothalamic GPR54 signaling: a potential mechanism for initiation of puberty in primates. Proc. Natl. Acad. Sci. USA 102: 2129-34.
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