HTS001M - ChemiSCREEN™ CXCR1 Chemokine Receptor Membrane Preparation

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    CXCR1 (also known as IL-8RA) is a Gi/o-coupled GPCR expressed on neutrophils, CD8(+) T cells, and intestinal epithelial cells (Murphy, 1997; Sturm et al., 2005; Takata et al., 2004). CXCR1 binds specifically to the chemokine interleukin-8 (IL-8), whereas a related receptor, CXCR2, binds promiscuously to IL-8 and several other chemokines. CXCR1 has been proposed to be the primary regulator of neutrophil response to IL-8 in sepsis (Cummings et al., 1999). Antagonists of CXCR1 and CXCR2 have been developed and display efficacy in animal models of reperfusion injury (Bertini, et al., 2004; Kaneider et al., 2005). CXCR1 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 CXCR1 interaction with IL-8. The membrane preparations exhibit a Kd of 0.2 nM for [125I]-IL-8. With 5 mg/well of CXCR1 Membrane Prep and 0.1 nM [125I]-IL-8, a greater than 5-fold signal-to-background ratio is obtained.

    Additional Resource: HTS001M161014_Datasheet

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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
    Species: Human CXCR1 Receptor (Accession number M68932)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous CXCR1 expression.
    Reference 1: 1. Bertini R et al. (2004) Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc. Natl. Acad. Sci. USA 101(32):11791-6.
    Reference 2: 2. Cummings CJ et al. (1999) Expression and function of the chemokine receptors CXCR1 and CXCR2 in sepsis. J. Immunol. 162(4):2341-6.
    Reference 3: 3. Kaneider NC et al. (2005) Reversing systemic inflammatory response syndrome with chemokine receptor pepducins. Nat Med. 11(6):661-5.
    Reference 4: 4. Murphy PM (1997) Neutrophil receptors for interleukin-8 and related CXC chemokines. Semin. Hematol. 34:311-8.
    Reference 5: 5. Sturm A et al. (2005) CXCL8 modulates human intestinal epithelial cells through a CXCR1 dependent pathway. Cytokine 29(1):42-8.
    Reference 6: 6. Takata H et al. (2004) Cutting edge: expression of chemokine receptor CXCR1 on human effector CD8+ T cells. J. Immunol. 173(4):2231-5.