Calcium Flux Assay

HTS003C - ChemiSCREEN™ Human Recombinant CXCR3 Chemokine Receptor Calcium-Optimized Stable Cell Line

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    CXCR3 is a 7-TM GPCR that is selective for the CXC chemokines IP10, I-TAC and MIG (Loetscher et al., 1996). Binding of IP10 and MIG to CXCR3 induces Ca2+ mobilization, chemotaxis and inflammatory responses of T lymphocytes, and also act as potent inhibitors of angiogenesis. CXCR3 is highly expressed in IL-2-activated T lymphocytes in vitro (Loetscher et al., 1996), and in T lymphocytes present in inflamed tissues in rheumatoid arthritis and multiple sclerosis (Balashoy et al., 1999; Qin et al., 1998). In vivo, neutralization of CXCR3 inhibits experimentally induced type I diabetes (Frigerio et al., 2002), peritonitis (Xie et al., 2003), and post-lung transplantation bronchiolitis obliterans syndrome (Belperio et al., 2002). The cloned human CXCR3-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CXCR3 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 CXCR3 and its ligands

    Additional Resource :  HTS003C050615_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 CXCR3 cDNA (Accession Number: X95876) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Balashov, KE, et al. (1999) CCR5 (+) and CXCR3 (+) T cells are increased in multiple sclerosis and their ligands MIP-1alpha and IP-10 are expressed in demyelinating brain lesions.Proc. Natl. Acad. Sci. USA 96: 6873-8.
    Reference 2: 2. Belperio, JA, et al. (2002) Critical role for CXCR3 chemokine biology in the pathogenesis of bronchiolitis obliterans syndrome. J. Immunol. 169: 1037-1049.
    Reference 3: 3. Frigerio, S, et al. (2002) Beta cells are responsible for CXCR3-mediated T-cell infiltration in insulitis. Nat. Med. 8: 1414-20.
    Reference 4: 4. Loetscher M, et al. (1996) Chemokine receptor specific for IP10 and mig: structure, function, and expression in activated T-lymphocytes.J. Exp. Med. 184(3): 963-9.
    Reference 5: 5. Qin, S, et al. (1998) The chemokine receptors CXCR3 and CCR5 mark subsets of T cells associated with certain inflammatory reactions.J. Clin. Invest. 101: 746-54.
    Reference 6: 6. Xie, JH, et al. (2003) Antibody-mediated blockade of the CXCR3 chemokine receptor results in diminished recruitment of T helper 1 cells into sites of inflammation.J. Leukoc. Biol. 73: 771-7-80.