Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.
G protein-coupled receptor kinases (GRKs) phosphorylate agonist-occupied G protein-coupled receptors, leading to receptor desensitization. Seven GRKs, designated GRK1 through 7, have been characterized. GRK5 is negatively regulated by protein kinase C. We investigated whether human substance P receptor (hSPR) is a substrate of GRK5. We report that membrane-bound hSPR is ... phosphorylated by purified GRK5, and that both the rate and extent of phosphorylation increase dramatically in the presence of substance P. The phosphorylation has a high stoichiometry (20+/-4 mol phosphate/mol hSPR) and a low K(m) (1.7+/-0.1 nM). These data provide the first evidence that hSPR is a substrate of GRK5.
Mesh Terms:
Amino Acid Sequence, Animals, Catalysis, Cell Line, Cell Membrane, G-Protein-Coupled Receptor Kinase 5, GTP-Binding Proteins, Humans, Kinetics, Molecular Sequence Data, Phosphorylation, Protein-Serine-Threonine Kinases, Receptors, Neurokinin-1, Spodoptera, Substance P, Substrate Specificity
Amino Acid Sequence, Animals, Catalysis, Cell Line, Cell Membrane, G-Protein-Coupled Receptor Kinase 5, GTP-Binding Proteins, Humans, Kinetics, Molecular Sequence Data, Phosphorylation, Protein-Serine-Threonine Kinases, Receptors, Neurokinin-1, Spodoptera, Substance P, Substrate Specificity
FEBS Lett.
Date: Jun. 19, 2002
PubMed ID: 12067742
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