HTS015M - ChemiSCREEN™ CX3CR1 Chemokine Receptor Membrane Preparation

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    CX3CR1 is a GPCR expressed on natural killer cells, cytotoxic T lymphocytes, and macrophages. The sole ligand for CX3CR1, fractalkine, is an unusual chemokine that is expressed as a transmembrane molecule with a CX3C domain and a mucin domain (Imai et al., 1997). Fractalkine is highly expressed on endothelial cells activated by TNFa and other proinflammatory cytokines, and fractalkine/CX3CR1 interactions mediate recruitment of macrophages into the atherosclerotic plaque (Lesnick et al., 2003; McDermott et al., 2003). In addition, fractalkine and CX3CR1 have been implicated in the pathogenesis of glomerulonephritis, HIV infection and rheumatoid arthritis (Ito et al., 2002; Faure et al., 2003; Nanki et al., 2002). CX3CR1 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 antagonists of CX3CR1 interactions with fractalkine. The membrane preparations exhibit a Kd of 0.05-0.1 nM for [125I]-fractalkine. With 2.5 mg/well CX3CR1 Membrane Prep and 0.05 nM [125I]-fractalkine, a greater than 5-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. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Species: Human CX3CR1 (Accession number U28934)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous CX3CR1 expression.
    Reference 1: 1. Faure S et al. (2003) Deleterious genetic influence of CX3CR1 genotypes on HIV-1 disease progression. J Acquir. Immune Defic. Syndr. 32: 335-7.
    Reference 2: 2. Imai T et al. (1997) Identification and molecular characterization of fractalkine receptor CX3CR1, which mediates both leukocyte migration and adhesion. Cell 91: 521-30.
    Reference 3: 3. Ito Y et al. (2002) Fractalkine expression and the recruitment of CX3CR1+ cells in the prolonged mesangial proliferative glomerulonephritis. Kidney Int. 61: 2044-57.
    Reference 4: 4. Lesnick P et al. (2003) Decreased atherosclerosis in CX3CR1-/- mice reveals a role for fractalkine in atherogenesis. J. Clin. Invest. 111: 333-40.
    Reference 5: 5. McDermott DH et al. (2003) Chemokine receptor mutant CX3CR1-M280 has impaired adhesive function and correlates with protection from cardiovascular disease in humans. J. Clin. Invest. 111: 1241-50.
    Reference 6: 6. Nanki T et al. (2002) Migration of CX3CR1-positive T cells producing type 1 cytokines and cytotoxic molecules into the synovium of patients with rheumatoid arthritis. Arthritis Rheum. 46: 2878-83.