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

Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • Warabi, K; Richardson, MD; Barry, WT; Yamaguchi, K; Roush, ED; Nishimura, K; Kwatra, MM

Published Date

  • June 19, 2002

Published In

Volume / Issue

  • 521 / 1-3

Start / End Page

  • 140 - 144

PubMed ID

  • 12067742

International Standard Serial Number (ISSN)

  • 0014-5793

Language

  • eng

Conference Location

  • England