Pharmacological characterization of the chemokine receptor, CCR5

Mueller, A., Mahmoud, N. G., Goedecke, M. C., McKeating, J. A. and Strange, P. G. (2002) Pharmacological characterization of the chemokine receptor, CCR5. British Journal of Pharmacology, 135 (4). pp. 1033-1043. ISSN 0007-1188

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Abstract

1 We investigated the effects of a number of naturally occurring chemokines (MIP-1alpha:, MIP-1beta, RANTES, MCP-2, MCP-3, MCP-4) on different processes linked to the chemokine receptor CCR5 in recombinant CHO cells expressing the receptor at different levels. 2 Internalization of CCR5 following chemokine treatment was studied and MIP-1alpha, MIP-1beta and RANTES (50 nM) were able to induce internalization (similar to50%) of the receptor. Internalization due to MCP-2, MCP-3 and MCP-4 was less (similar to20%). 3 Phosphorylation of CCR5 following chemokine treatment was studied and MIP-1alpha, MIP-1beta and RANTES (50 nM) were able to induce phosphorylation of CCR5 whereas the other chemokines did not induce CCR5 phosphorylation. 4 MIP-1alpha, MIP-1beta, RANTES and MCP-2 were able to stimulate [S-35]-GTPgammaS binding, an index of receptor/G protein activation, whereas MCP-3 and MCP-4 had no effect in this assay. MCP-2 was a partial agonist (similar to80%) compared to MIP-1alpha,, MIP-1beta and RANTES, which gave similar maximal stimulations in this assay. 5 MIP-1alpha, MIP-Ifl, RANTES, MCP-2 and MCP-4 were able to stimulate increases in intracellular calcium ions via activation of CCR5 whereas MCP-3 was without effect. 6 It is concluded that different chemokines interacting with CCR5 mediate different patterns of cellular responses.

Item Type: Article
Uncontrolled Keywords: desensitization,functional expression,[s-35]-gtp gamma s binding,internalization,gamma-s binding,rantes,cells,protein-coupled receptors,chemokine receptor ccr5,hiv-1,internalization,cxcr4,chemokines,phosphorylation,inhibition
Faculty \ School: Faculty of Science > School of Pharmacy
University of East Anglia > Faculty of Science > Research Groups > Pharmaceutical Cell Biology
Depositing User: Rachel Smith
Date Deposited: 31 May 2011 15:58
Last Modified: 25 Jul 2018 07:29
URI: https://ueaeprints.uea.ac.uk/id/eprint/31560
DOI:

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