Desensitization of G protein-coupled receptors and neuronal functions.

  title={Desensitization of G protein-coupled receptors and neuronal functions.},
  author={Raul R. Gainetdinov and Richard T. Premont and Laura M. Bohn and Robert J. Lefkowitz and Marc G. Caron},
  journal={Annual review of neuroscience},
G protein-coupled receptors (GPCRs) have proven to be the most highly favorable class of drug targets in modern pharmacology. Over 90% of nonsensory GPCRs are expressed in the brain, where they play important roles in numerous neuronal functions. GPCRs can be desensitized following activation by agonists by becoming phosphorylated by members of the family of G protein-coupled receptor kinases (GRKs). Phosphorylated receptors are then bound by arrestins, which prevent further stimulation of G… 

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