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Kinetics of G-protein-coupled receptor signallingand desensitization
Kinetics of G-protein-coupled receptor signallingand desensitization
A review (pdf file) by C. Krasel, J.-P. Vilardaga, M. Bunemann and M.J. Lohse. Institute for Pharmacology and Toxicology, Germany.
Abstract:
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.
Last update 21-Jan-2005, Rating of 0 votes.
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