HTS003M - ChemiSCREEN™ CXCR3 Chemokine Receptor Membrane Preparation

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    CXCR3 is a 7-TM GPCR that is selective for the CXC chemokines IP10, ITAC 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). ChemiScreenTM CXCR3 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression. Thus, they are ideal HTS tools for screening of agonists of CXCR3 receptor interactions. The membrane preparations exhibit a Kd of 2.6 nM for [125I]-IP-10. With 5 mg/well of CXCR3 Membrane Prep and 0.1 nM [125I]-IP-10, a greater than 10-fold signal-to-background ratio was obtained.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles.
    Applications: Radioligand Binding Assay
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous CXCR3 receptor expression
    Reference 1: 1. Balashov KE, et al. (1999) CCR5(+) and CXCR3(+) T cells are increased in multiple sclerosis and their ligands MIP-1 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. Sep 1- 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.