Inhibition

HTS004C - ChemiSCREEN™ Human CXCR4 Receptor Calcium-Optimized Stable Cell Line

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HTS004C
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    The chemokine SDF-1α and its GPCR receptor CXCR4 have a one-to-one specificity that is unique among chemokines and their receptors. SDF-1α binds to CXCR4 expressed on hematopoietic and lymphopoietic cells, and directs their trafficking to and retention in hemato-and lymphatopoietic organs and sites of inflammation (Kucia et al., 2004). CXCR4 is expressed on several tumor cell lineages, and might be responsible for metastasis to sites of SDF-1α expression, such as bone and lymph nodes (Muller et al., 2001). In addition, CXCR4 is a coreceptor for the HIV envelope glycoprotein gp120 (Feng et al., 1996). Small molecule antagonists of CXCR4 have been developed and shown to inhibit infectivity of T-tropic HIV strains and to impair growth of brain tumors (Arakaki et al., 1999; Rubin et al., 2003). The cloned human recombinant CXCR4-expresssing cell lines is made in Chem-1 host, which support high levels of recombinant CXCR4 expression on the cell surface and contains high levels of the promiscuous G protein Ga15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between CXCR4 and its ligands

    Additional Resource :  HTS004C050715_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 CXCR4 cDNA (Accession Number: M99293) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Arakaki R et al. (1999) T134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure. J Virol. 73: 1719-23.
    Reference 2: 2. Feng Y et al. (1996) HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science 272: 872-7.
    Reference 3: 3. Kucia M et al. (2004) CXCR4-SDF-1 signaling, locomotion, chemotaxis and adhesion. J. Mol. Histol. 35: 233-45.
    Reference 4: 4. Muller A et al. (2001) Involvement of chemokine receptors in breast cancer metastasis. Nature 410: 50-6.
    Reference 5: 5. Rubin JB et al. (2003) A small-molecule antagonist of CXCR4 inhibits intracranial growth of primary brain tumors. Proc. Natl. Acad. Sci. USA. 100: 13513-8.
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