Targeting G protein–coupled receptor kinases to G protein–coupled receptors

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

Activation of a G proteincoupled receptor by its endogenous ligand triggers the innate immune response of Caenorhabditis elegans

The innate defenses of the nematode Caenorhabditis elegans have diverged considerably from those of other animals. Perhaps most strikingly, C. elegans has lost the transcription factor NF-κB, key for defense in most animal species, and lacks functional orthologs of many known innate defense receptors1. On the other hand, core signaling pathways involved in innate immunity across a broad range o...

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...

Toxicology G Protein - Coupled Receptor Kinases

The importance of G protein-coupled receptor (GPCR) kinases (GRKs) as regulators of GPCR signaling has been widely recognized. In humans, GRKs constitute a family of seven protein kinases involved in the phosphorylation and desensitization of agonist-activated GPCRs in many physiological processes. The GPCR desensitization process is initiated by GRKs, but involves several subsequent steps incl...

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...