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Mueller, A. 
ORCID: https://orcid.org/0000-0003-0774-0434
(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
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 |
| UEA Research Groups: | Faculty of Science > Research Groups > Pharmaceutical Cell Biology (former - to 2017) Faculty of Science > Research Groups > Molecular and Tissue Pharmacology |
| Depositing User: | Rachel Smith |
| Date Deposited: | 31 May 2011 11:53 |
| Last Modified: | 24 Oct 2022 01:27 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/31568 |
| DOI: | 10.1038/sj.bjp.0707521 |
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