Regulation of receptor trafficking by GRKs and arrestins

Annu Rev Physiol. 2007:69:451-82. doi: 10.1146/annurev.physiol.69.022405.154712.


To ensure that extracellular stimuli are translated into intracellular signals of appropriate magnitude and specificity, most signaling cascades are tightly regulated. One of the major mechanisms involved in the regulation of G protein-coupled receptors (GPCRs) involves their endocytic trafficking. GPCR endocytic trafficking entails the targeting of receptors to discrete endocytic sites at the plasma membrane, followed by receptor internalization and intracellular sorting. This regulates the level of cell surface receptors, the sorting of receptors to degradative or recycling pathways, and in some cases the specific signaling pathways. In this chapter we discuss the mechanisms that regulate receptor endocytic trafficking, emphasizing the role of GPCR kinases (GRKs) and arrestins in this process.

Publication types

  • Review

MeSH terms

  • Animals
  • Arrestins / genetics*
  • Arrestins / physiology*
  • Endocytosis / physiology
  • Humans
  • Models, Molecular
  • Protein Serine-Threonine Kinases / genetics*
  • Protein Serine-Threonine Kinases / physiology*
  • Protein Transport
  • Receptors, G-Protein-Coupled / genetics*
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction / genetics
  • Signal Transduction / physiology
  • Transport Vesicles / physiology


  • Arrestins
  • Receptors, G-Protein-Coupled
  • Protein Serine-Threonine Kinases