Fine-tuning of GPCR activity by receptor-interacting proteins

Nat Rev Mol Cell Biol. 2009 Dec;10(12):819-30. doi: 10.1038/nrm2803.


G protein-coupled receptors (GPCRs) mediate physiological responses to various ligands, such as hormones, neurotransmitters and sensory stimuli. The signalling and trafficking properties of GPCRs are often highly malleable depending on the cellular context. Such fine-tuning of GPCR function can be attributed in many cases to receptor-interacting proteins that are differentially expressed in distinct cell types. In some cases these GPCR-interacting partners directly mediate receptor signalling, whereas in other cases they act mainly as scaffolds to modulate G protein-mediated signalling. Furthermore, GPCR-interacting proteins can have a big impact on the regulation of GPCR trafficking, localization and/or pharmacological properties.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Humans
  • Ligands
  • Protein Transport
  • Receptor-Interacting Protein Serine-Threonine Kinases / metabolism*
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction


  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptor-Interacting Protein Serine-Threonine Kinases