Role of endocytosis in signalling and regulation of G-protein-coupled receptors

Biochem Soc Trans. 2001 Aug;29(Pt 4):500-4. doi: 10.1042/bst0290500.


Many G-protein-coupled receptors (GPCRs) undergo agonist-induced endocytosis. Endocytosis contributes to distinct processes that regulate the number and functional activity of receptors present in the plasma membrane, contributing to the well described processes of receptor sequestration and down-regulation. Emerging evidence suggests additional functions of endocytosis in mediating GPCR signalling via certain effector pathways, such as mitogen-activated protein kinase modules. The diverse functions of endocytosis raise fundamental questions about the nature of the vesicular carriers and membrane pathways that mediate the endocytic trafficking of specific GPCRs. Insights into the biochemical and functional properties of endocytic vesicles containing internalized opioid and adrenergic receptors will be discussed. Progress towards understanding the mechanisms that control the specificity with which distinct GPCRs are sorted to specialized subpopulations of endocytic vesicles will be highlighted.

Publication types

  • Review

MeSH terms

  • Animals
  • Down-Regulation
  • Endocytosis / physiology*
  • GTP-Binding Proteins / physiology*
  • Homeostasis
  • Lysosomes / physiology
  • Receptors, Cell Surface / agonists
  • Receptors, Cell Surface / physiology*
  • Signal Transduction / physiology*


  • Receptors, Cell Surface
  • GTP-Binding Proteins