The kinetics of G-protein-coupled receptor activation and deactivation has, so far, been measured only indirectly, most frequently by assessing the production of various second messengers. We have developed methods based on fluorescence resonance energy transfer to quantify the kinetics of receptor activation by agonist (measured as conformational change in the receptor), the kinetics of G-protein activation (measured as G-protein subunit rearrangement) and the kinetics of receptor inactivation by arrestins (measured as receptor–arrestin interaction). Using these methods, we show that receptor activation by agonists and signalling to G-proteins occur on the subsecond time scale, whereas receptor desensitization is limited by receptor phosphorylation and proceeds more slowly.
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November 2004
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Conference Article|
October 26 2004
Kinetics of G-protein-coupled receptor signalling and desensitization
C. Krasel;
C. Krasel
1Institute for Pharmacology and Toxicology, Versbacher Str. 9, D-97078 Würzburg, Germany
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J.-P. Vilardaga;
J.-P. Vilardaga
1Institute for Pharmacology and Toxicology, Versbacher Str. 9, D-97078 Würzburg, Germany
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M. Bünemann;
M. Bünemann
1Institute for Pharmacology and Toxicology, Versbacher Str. 9, D-97078 Würzburg, Germany
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M.J. Lohse
M.J. Lohse
1
1Institute for Pharmacology and Toxicology, Versbacher Str. 9, D-97078 Würzburg, Germany
1To whom correspondence should be addressed (email lohse@toxi.uni-wuerzburg.de).
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Biochem Soc Trans (2004) 32 (6): 1029–1031.
Article history
Received:
June 18 2004
Citation
C. Krasel, J.-P. Vilardaga, M. Bünemann, M.J. Lohse; Kinetics of G-protein-coupled receptor signalling and desensitization. Biochem Soc Trans 1 November 2004; 32 (6): 1029–1031. doi: https://doi.org/10.1042/BST0321029
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