Calcium Flux Assay

HTS010RTA - Ready-to-Assay™ CCR5 Chemokine Receptor Frozen Cells

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    CCR5 is the receptor for CC chemokines MIP-1α, MIP-1β, and RANTES (Raport et al., 1996), and is preferentially expressed on Th1 lymphocytes (Loetscher et al., 1998). CCR5 is a coreceptor for macrophage-tropic HIV, and its ligands potently inhibit HIV replication in human leukocytes (Cocchi et al., 1995). In addition, HIV-infected patients with the nonfunctional CCR5Δ32 allele exhibit delayed onset of AIDS symptoms (Samson et al., 1996), and pharmacological antagonism of CCR5 inhibits HIV-1 infection (Strizki et al., 2001). Preclinical testing of small molecule antagonists of CCR5 has been hampered by low affinity of the compounds to rodent and dog CCR5, but two such compounds, maraviroc and AD101, have been shown to have potent antagonist activity at rhesus macaque CCR5, which differs from human CCR5 by 8 amino acids (Napier et al., 2005; Billick et al., 2004). One antagonist of human CCR5, SCH-C, does not block HIV entry through rhesus macaque CCR5, and one amino acid difference is responsible for the functional difference (Billick et al., 2004). The cloned rhesus macaque CCR5-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CCR5 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at CCR5.

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Entrez Gene Number: NM_001042773.2
    Protein Targets: CCR5
    Target Sub-family: Chemokine
    Species: Rhesus Macaque
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exogenous Gene Expression: rhesus macaque CCR5 cDNA (Accession Number: NM_001042773.2; see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Billick E et al. (2004) The differential sensitivity of human and rhesus macaque CCR5 to smallmolecule inhibitors of human immunodeficiency virus type 1 entry is explained by a single amino acid difference and suggests a mechanism of action for th
    Reference 2: 2. Cocchi F., et al. (1995) Identification of RANTES, MIP-1 alpha, and MIP-1 beta as the major HIVsuppressive factors produced by CD8+ T cells. Science 270: 1811-1815
    Reference 3: 3. Loetscher P, et al. (1998) CCR5 is characteristic of Th1 lymphocytes. Nature 391: 344-5.
    Reference 4: 4. Napier C et al. (2005) Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human. Biochem. Pharmacol. 71: 163-172.
    Reference 5: 5. Raport CJ et al. (1996) Molecular cloning and functional characterization of a novel human CC chemokine receptor (CCR5) for RANTES, MIP-1beta, and MIP-1alpha. J Biol Chem 271: 17161-6.
    Reference 6: 6. Samson M et al. (1996) Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene. Nature 382: 722-5.