Abstract
G-protein-coupled receptors (GPCRs) are the largest group of cell
surface receptors. They are stimulated by a variety of stimuli and
signal to different classes of effectors, including several types
of ion channels and second messenger-generating enzymes. Recent technical
advances, most importantly in the optical recording with energy transfer
techniques--fluorescence and bioluminescence resonance energy transfer,
FRET and BRET--, have permitted a detailed kinetic analysis of the
individual steps of the signalling chain, ranging from ligand binding
to the production of second messengers in intact cells. The transfer
of information, which is initiated by ligand binding, triggers a
signalling cascade that displays various rate-controlling steps at
different levels. This review summarizes recent findings illustrating
the speed and the complexity of this signalling system.
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