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Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist?
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| Zeitschriftentitel: | British Journal of Pharmacology |
|---|---|
| Personen und Körperschaften: | |
| In: | British Journal of Pharmacology, 152, 2007, 8, S. 1145-1146 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Wiley
|
| Schlagwörter: |
| author_facet |
Mueller, A Mueller, A |
|---|---|
| author |
Mueller, A |
| spellingShingle |
Mueller, A British Journal of Pharmacology Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? Pharmacology |
| author_sort |
mueller, a |
| spelling |
Mueller, A 0007-1188 1476-5381 Wiley Pharmacology http://dx.doi.org/10.1038/sj.bjp.0707521 <jats:p>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 <jats:italic>in vivo</jats:italic> 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.</jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (2007) <jats:bold>152</jats:bold>, 1145–1146; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0707521">10.1038/sj.bjp.0707521</jats:ext-link>; published online 5 November 2007</jats:p> Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? British Journal of Pharmacology |
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| title |
Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
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Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_full |
Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
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Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
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Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
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Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_sort |
internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
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Pharmacology |
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http://dx.doi.org/10.1038/sj.bjp.0707521 |
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2007 |
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<jats:p>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 <jats:italic>in vivo</jats:italic> 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.</jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (2007) <jats:bold>152</jats:bold>, 1145–1146; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0707521">10.1038/sj.bjp.0707521</jats:ext-link>; published online 5 November 2007</jats:p> |
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| description | <jats:p>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 <jats:italic>in vivo</jats:italic> 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.</jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (2007) <jats:bold>152</jats:bold>, 1145–1146; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0707521">10.1038/sj.bjp.0707521</jats:ext-link>; published online 5 November 2007</jats:p> |
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| spelling | Mueller, A 0007-1188 1476-5381 Wiley Pharmacology http://dx.doi.org/10.1038/sj.bjp.0707521 <jats:p>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 <jats:italic>in vivo</jats:italic> 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.</jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (2007) <jats:bold>152</jats:bold>, 1145–1146; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0707521">10.1038/sj.bjp.0707521</jats:ext-link>; published online 5 November 2007</jats:p> Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? British Journal of Pharmacology |
| spellingShingle | Mueller, A, British Journal of Pharmacology, Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist?, Pharmacology |
| title | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_full | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_fullStr | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_full_unstemmed | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_short | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_sort | internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| title_unstemmed | Internalization: what does it tell us about pharmacokinetic and pharmacodynamic properties of an antagonist? |
| topic | Pharmacology |
| url | http://dx.doi.org/10.1038/sj.bjp.0707521 |