G Protein–Coupled Receptor Kinase 4

Novel features of G protein-coupled receptor kinase 4.

The defining characteristic of G protein-coupled receptor homologous desensitization is that the receptor must be occupied by an agonist or in an activated conformation that mimics an agonist-induced state. In most instances, the mechanistic basis for this characteristic is the high selectivity of G protein-coupled receptor kinases for the activated receptor. In this issue, Rankin et al. (p. 75...

G protein-coupled receptor kinase 4: role in hypertension.

T he kidney plays an important role in the long-term control of blood pressure and is the major organ involved in the regulation of sodium homeostasis. 1 The inappropriate sodium retention in hypertension results from enhanced renal sodium transport per se or a failure to respond appropriately to signals that decrease renal sodium transport in the face of increased sodium intake. Humans with po...

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

The D1 dopamine receptor is constitutively phosphorylated by G protein-coupled receptor kinase 4.

G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate agonist-activated GPCRs, initiating their homologous desensitization. In this article, we present data showing that GRK4 constitutively phosphorylates the D1 receptor in the absence of agonist activation. This constitutive phosphorylation is mediated exclusively by the alpha isoform of GRK4; the beta, gamma, and delta isoforms are i...

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...