G-protein-coupled receptor heteromer dynamics

J Cell Sci. 2010 Dec 15;123(Pt 24):4215-20. doi: 10.1242/jcs.063354.

Abstract

G-protein-coupled receptors (GPCRs) represent the largest family of cell surface receptors, and have evolved to detect and transmit a large palette of extracellular chemical and sensory signals into cells. Activated receptors catalyze the activation of heterotrimeric G proteins, which modulate the propagation of second messenger molecules and the activity of ion channels. Classically thought to signal as monomers, different GPCRs often pair up with each other as homo- and heterodimers, which have been shown to modulate signaling to G proteins. Here, we discuss recent advances in GPCR heteromer systems involving the kinetics of the early steps in GPCR signal transduction, the dynamic property of receptor-receptor interactions, and how the formation of receptor heteromers modulate the kinetics of G-protein signaling.

Publication types

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

MeSH terms

  • Animals
  • Heterotrimeric GTP-Binding Proteins / metabolism
  • Humans
  • Protein Binding
  • Protein Multimerization*
  • Protein Structure, Quaternary
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction*

Substances

  • Receptors, G-Protein-Coupled
  • Heterotrimeric GTP-Binding Proteins