G-protein-coupled receptor heteromer dynamics.
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.
Laboratory for GPCR Biology, Department of Pharmacology and Chemical Biology, University of Pittsburgh, School of Medicine, Pittsburgh, PA 15261, USA. jpv@pitt.edu
Jean-Pierre
JP
Vilardaga
Luigi F
LF
Agnati
Kjell
K
Fuxe
Francisco
F
Ciruela
D000818:Animals; D020962:Heterotrimeric GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D011485:Protein Binding; D055503:Protein Multimerization; D020836:Protein Structure, Quaternary; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000378:metabolism*; D015398:Signal Transduction
D043562:Receptors, G-Protein-Coupled; D020962:Heterotrimeric GTP-Binding Proteins