Kinetics of G-protein-coupled receptor signals in intact cells

Br J Pharmacol. 2008 Mar;153 Suppl 1(Suppl 1):S125-32. doi: 10.1038/sj.bjp.0707656. Epub 2008 Jan 14.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Arrestins / metabolism
  • G-Protein-Coupled Receptor Kinases / metabolism
  • GTP-Binding Proteins / metabolism
  • GTP-Binding Proteins / physiology
  • Humans
  • Kinetics
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / drug effects
  • Receptors, G-Protein-Coupled / physiology*
  • Second Messenger Systems / drug effects
  • Second Messenger Systems / physiology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*

Substances

  • Arrestins
  • Receptors, G-Protein-Coupled
  • G-Protein-Coupled Receptor Kinases
  • GTP-Binding Proteins