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  • Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO-K1 cells

    Author(s)
    Longden, James
    Cooke, E-L
    Hill, SJ
    Griffith University Author(s)
    Longden, James
    Year published
    2008
    Metadata
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    Abstract
    Background and purpose: The CCR5 chemokine receptor is a member of the G protein-coupled receptor (GPCR) family that is expressed by macrophages, memory T-lymphocytes and dendritic cells and is activated by chemotactic proteins (e.g. MIP-1a [CCL3], MIP-1ߠ[CCL4] and RANTES [CCL5]). CCR5 is also the principal co-receptor for macrophage-tropic strains of human immunodeficiency virus-1 (HIV-1) and some chemokines can inhibit HIV-1 infection by stimulating CCR5 receptor endocytosis. The aim of this study was to evaluate the effect of CCR5 antagonists on CCR5 endocytosis. Experimental approach: The effects of CCR5 agonists and ...
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    Background and purpose: The CCR5 chemokine receptor is a member of the G protein-coupled receptor (GPCR) family that is expressed by macrophages, memory T-lymphocytes and dendritic cells and is activated by chemotactic proteins (e.g. MIP-1a [CCL3], MIP-1ߠ[CCL4] and RANTES [CCL5]). CCR5 is also the principal co-receptor for macrophage-tropic strains of human immunodeficiency virus-1 (HIV-1) and some chemokines can inhibit HIV-1 infection by stimulating CCR5 receptor endocytosis. The aim of this study was to evaluate the effect of CCR5 antagonists on CCR5 endocytosis. Experimental approach: The effects of CCR5 agonists and antagonists on receptor internalization in CHO cells, expressing a C-terminal green fluorescent protein-tagged human CCR5 receptor (CCR5-GFP), were quantified using a confocal imaging plate reader. Key results: MIP-1a [CCL3], MIP-1ߠ[CCL4] and RANTES [CCL5] were all able to stimulate potently the internalization of CCR5-GFP. This effect was inhibited by the non-peptide antagonist TAK 779. The CCR5 peptide antagonist met-RANTES antagonized MIP-1a-mediated increases in intracellular free calcium but was also able to stimulate a substantial internalization of the human CCR5-GFP receptor. However, CHO cells exhibited an aminopeptidase activity that was able to metabolize sufficient met-RANTES into an agonist metabolite capable of stimulating calcium mobilization via CCR5 receptors in naﶥ cells. Conclusions and implications: These data suggest that there is an endogenous aminopeptidase activity on the surface of CHO cells, that produces a slow internalization of the receptor following a time-dependent conversion of receptor-bound met-RANTES from a CCR5 receptor antagonist into a CCR5 agonist molecule. 頲008 Nature Publishing Group All rights reserved.
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    Journal Title
    British Journal of Pharmacology
    Volume
    153
    Issue
    7
    DOI
    https://doi.org/10.1038/sj.bjp.0707691
    Subject
    Pharmacology and Pharmaceutical Sciences not elsewhere classified
    Pharmacology and Pharmaceutical Sciences
    Publication URI
    http://hdl.handle.net/10072/23247
    Collection
    • Journal articles

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