Calcium Flux Assay

HTS001C - ChemiSCREEN™ Human Recombinant CXCR1 Chemokine Receptor Calcium-Optimized Stable Cell Line

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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 with high affinity to the chemokine interleukin-8 (IL-8) and much lower affinity to GRO?, whereas a related receptor, CXCR2, binds with equal affinity to IL-8 and GRO? (Hall et al., 1999). 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). Cloned human CXCR1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CXCR1 expression on the cell surface and contains high levels of the promiscuous G protein G?15 to couple the receptor to the calcium signaling pathway. These stability-tested cells are ready for fluorescence-based assays for agonists, antagonists and modulators at the CXCR1 receptor.

    Additional Resource: HTS001C030915_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 CXCR1 cDNA (Accession Number: M68932)
    GMO: This product contains genetically modified organisms.
    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. U S A. 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. Hall DA et al. (1999) Signalling by CXC-chemokine receptors 1 and 2 expressed in CHO cells: A comparison of calcium mobilization, inhibition of adenylyl cyclase and stimulation of GTPS binding induced by IL-8 and GROa. Br. J. Pharmacol. 126: 81
    Reference 4: 4. Kaneider NC et al. (2005) Reversing systemic inflammatory response syndrome with chemokine receptor pepducins. Nat. Med. 11(6):661-5.
    Reference 5: 5. Murphy PM (1997) Neutrophil receptors for interleukin-8 and related CXC chemokines. Semin. Hematol. 34: 311-8.
    Reference 6: 6. Sturm A et al. (2005) CXCL8 modulates human intestinal epithelial cells through a CXCR1 dependent pathway. Cytokine 29(1):42-8.