Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist?

Mueller, A. (2007) Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? British Journal of Pharmacology, 152 (8). pp. 1145-1146. ISSN 0007-1188

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Abstract

Chemokine receptors play an important role in trafficking leukocytes within the body, a process that depends on expression of the receptors on the cell surface. Expression levels are regulated by the rate of internalizing receptor compared to the rate of recycling/recovering receptor. Internalization is commonly induced by binding of agonists to their receptors that in turn use clathrin-coated pits or caveolae to internalize. Joplin and colleagues describe a novel usage of internalization assays to determine pharmacokinetic/pharmacodynamic relationships of an antagonist on CXCR3 in a murine system. Intriguingly their results show that internalization assays give robust data about the pharmacokinetics/pharmacodynamics of different agonists and antagonists in an in vivo model. This kind of assay will allow investigations of the pharmacological properties of agonists and antagonists in a completely different setting and also give new insight into the regulation of cell surface expression of chemokine receptors and other G protein-coupled receptors, which can lead to potential novel therapeutic targets.

Item Type: Article
Uncontrolled Keywords: chemokine receptor,chemokine,antagonist,internalization
Faculty \ School: Faculty of Science > School of Pharmacy
Depositing User: Rachel Smith
Date Deposited: 31 May 2011 11:53
Last Modified: 31 Oct 2019 13:50
URI: https://ueaeprints.uea.ac.uk/id/eprint/31568
DOI: 10.1038/sj.bjp.0707521

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