Human substance P receptor undergoes agonist‐dependent phosphorylation by G protein‐coupled receptor kinase 5 in vitro

  title={Human substance P receptor undergoes agonist‐dependent phosphorylation by G protein‐coupled receptor kinase 5 in vitro},
  author={Kengo Warabi and Mark D. Richardson and William T. Barry and Keisuke Yamaguchi and Eric David Roush and Kinya Nishimura and Madan M. Kwatra},
  journal={FEBS Letters},

NK1 (substance P) receptor

NK1R plays a key role in many physiological and pathophysiological processes, including pain, inflammation, cancer, brain edema, traumatic brain injury, nausea and vomiting, affective disorders, and obesity.

Accelerating Alzheimer's pathogenesis by GRK5 deficiency via cholinergic dysfunction

The GRK5 deficiency appears to bring the two major hypotheses in Alzheimer’s disease together, whereas the GRK4 deficiency is the pivotal link, and any strategies that can break this cycle would be therapeutically beneficial for Alzheimer's patients.

The Mechanism and Function of Agonist-Induced Trafficking of Tachykinin Receptors

Biological responses to agonists of G-protein coupled receptors are regulated by control of the interactions of receptors with signaling proteins and through control of the levels of receptors that

Recycling and Resensitization of the Neurokinin 1 Receptor

A new function of Rab5a is identified as a control protein for directing concentration-dependent trafficking of the NK1R into different intracellular compartments and evidence that Rab4a and Rab11a contribute to G-protein-coupled receptor recycling from early endosomes is obtained.


  • Biology
  • 2017
(54) GENEMAP OF THE HUMANGENES (86). PCT No.: PCT/US2O06/033148 ASSOCATED WITH CROHNS DISEASE S371 (c)(1), (76) Inventors: Abdelmajid Belouchi, Ville (2), (4) Date: Oct. 1, 2008 St-Laurent (CA); John

UCSD MOLECULE PAGES NK 1 ( substance P ) receptor



G protein-coupled receptor kinases.

This review focuses on the regulation of GRK activity by a variety of allosteric and other factors: agonist-stimulated GPCRs, beta gamma subunits of heterotrimeric GTP- binding proteins, phospholipid cofactors, the calcium-binding proteins calmodulin and recoverin, posttranslational isoprenylation and palmitoylation, autophosphorylation, and protein kinase C-mediated GRK phosphorylation.

Regulation of the G Protein-coupled Receptor Kinase GRK5 by Protein Kinase C*

The results suggest that PKC might play an important role in modulating the ability of GRK5 to regulate receptor signaling and that GRK phosphorylation by PKC may serve as a disparate mechanism for regulating GRK activity.

Regulation of G protein-coupled receptor kinases.

Phosphorylation of the Type 1A Angiotensin II Receptor by G Protein-coupled Receptor Kinases and Protein Kinase C*

A role for receptor phosphorylation by one or several GRKs in the rapid agonist-induced desensitization of the type 1A angiotensin II receptor is suggested.

Protein kinases that phosphorylate activated G protein‐coupled receptors

All GRKs appear to play the same general cellular role of desensitizing activated G protein‐coupled receptors, but utilize distinctly individual means to the same end, which are just beginning to be defined.

Characterization of GRK2-catalyzed phosphorylation of the human substance P receptor in Sf9 membranes.

G protein-coupled receptor kinases (GRKs) phosphorylate agonist-occupied G protein-coupled receptors (GPCRs), resulting in GPCR desensitization. GRK2 is one of the better studied of the six known

Identification of the G Protein-coupled Receptor Kinase Phosphorylation Sites in the Human β2-Adrenergic Receptor*

The location of multiple GRK2 and GRK5 phosphoacceptor sites at the extreme carboxyl terminus of the β2AR is highly reminiscent of GRK1-mediated phosphorylation of rhodopsin.

Agonist-dependent phosphorylation of human muscarinic receptors in Spodoptera frugiperda insect cell membranes by G protein-coupled receptor kinases.

The approach of studying GRK-mediated phosphorylation of GPRs in their membrane-bound state identified the hm3 mAChRs as new substrates for GRKs and should aid in studies that elucidate GRK/GPR pairing.

Regulation of G Protein-coupled Receptor Kinases by Calmodulin and Localization of the Calmodulin Binding Domain*

It is demonstrated that calmodulin, another mediator of calcium signaling, is a potent inhibitor of GRK activity with a selectivity for GRK5 (IC50 ∼50 nm) > GRK6 ≫ GRK2 ( IC50 ∼2 μm) ≬ GRK1.