HTS032RTA - Ready-to-Assay™ KiSS1 KiSS1-Derived Peptide Receptor Frozen Cells

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    KiSS1 (also known as GPR54 and 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). Cloned human KiSS1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant KiSS1 expression on the cell surface for functional detection via the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists, and modulators at KiSS1.

    Additional Resource: HTS032RTA100914_Datasheet

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2. Media Component at 4ºC (-20ºC for prolonged storage).
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein
    Exongenous Gene Expression: Human KISSR1 cDNA (Accession Number: NM_032551- see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    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. Messager S et al. (2005) Kisspeptin directly stimulates gonadotropin-releasing hormone release via G protein-coupled receptor 54. Proc. Natl. Acad. Sci. USA 102: 1761-6.
    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.