Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.
Journal Article (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
Digital Object Identifier (DOI)
- 10.1016/s0014-5793(02)02858-2
Language
- eng
Conference Location
- England