Competing G protein‐coupled receptor kinases balance G protein and β‐arrestin signaling

Competing G protein-coupled receptor kinases balance G protein and β-arrestin signaling

Seven-transmembrane receptors (7TMRs) are involved in nearly all aspects of chemical communications and represent major drug targets. 7TMRs transmit their signals not only via heterotrimeric G proteins but also through β-arrestins, whose recruitment to the activated receptor is regulated by G protein-coupled receptor kinases (GRKs). In this paper, we combined experimental approaches with comput...

Competing G protein-coupled receptor kinases balance G protein and b-arrestin signaling

1 BIOS Group, INRA, UMR85, Unité Physiologie de la Reproduction et des Comportements, Nouzilly, France, 2 CNRS, UMR7247, Nouzilly, France, 3 Université François Rabelais, Tours, France, 4 IFCE, Nouzilly, France, 5 Contraintes Team, INRIA Paris-Rocquencourt, Le Chesnay, France, 6 Department of Medicine, Duke University Medical Center, Howard Hughes Medical Institute, Durham, NC, USA, 7 Sisyphe T...

G protein-coupled receptor kinases.

G protein-coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein-coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization. This review focuses on the regulation of GRK activity...

G-protein Coupled Receptor Dimerization

A growing body of evidence suggests that GPCRs exist and function as dimers or higher oligomers. The evidence for GPCR dimerization comes from biochemical, biophysical and functional studies. In addition, researchers have shown the occurrence of heterodimerization between different members of the GPCR family. Two receptors can interact with each other to make a dimer through their extracellular...

A direct and functional interaction between the trimeric G protein Go and Rab5 in G proteincoupled receptor signaling