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

Publication ,  Journal Article
Warabi, K; Richardson, MD; Barry, WT; Yamaguchi, K; Roush, ED; Nishimura, K; Kwatra, MM
Published in: FEBS Lett
June 19, 2002

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.

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Published In

FEBS Lett

DOI

ISSN

0014-5793

Publication Date

June 19, 2002

Volume

521

Issue

1-3

Start / End Page

140 / 144

Location

England

Related Subject Headings

  • Substrate Specificity
  • Substance P
  • Spodoptera
  • Receptors, Neurokinin-1
  • Protein Serine-Threonine Kinases
  • Phosphorylation
  • Molecular Sequence Data
  • Kinetics
  • Humans
  • GTP-Binding Proteins
 

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Warabi, K., Richardson, M. D., Barry, W. T., Yamaguchi, K., Roush, E. D., Nishimura, K., & Kwatra, M. M. (2002). Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro. FEBS Lett, 521(1–3), 140–144. https://doi.org/10.1016/s0014-5793(02)02858-2
Warabi, Kengo, Mark D. Richardson, William T. Barry, Keisuke Yamaguchi, Eric D. Roush, Kinya Nishimura, and Madan M. Kwatra. “Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.FEBS Lett 521, no. 1–3 (June 19, 2002): 140–44. https://doi.org/10.1016/s0014-5793(02)02858-2.
Warabi K, Richardson MD, Barry WT, Yamaguchi K, Roush ED, Nishimura K, et al. Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro. FEBS Lett. 2002 Jun 19;521(1–3):140–4.
Warabi, Kengo, et al. “Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.FEBS Lett, vol. 521, no. 1–3, June 2002, pp. 140–44. Pubmed, doi:10.1016/s0014-5793(02)02858-2.
Warabi K, Richardson MD, Barry WT, Yamaguchi K, Roush ED, Nishimura K, Kwatra MM. Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro. FEBS Lett. 2002 Jun 19;521(1–3):140–144.
Journal cover image

Published In

FEBS Lett

DOI

ISSN

0014-5793

Publication Date

June 19, 2002

Volume

521

Issue

1-3

Start / End Page

140 / 144

Location

England

Related Subject Headings

  • Substrate Specificity
  • Substance P
  • Spodoptera
  • Receptors, Neurokinin-1
  • Protein Serine-Threonine Kinases
  • Phosphorylation
  • Molecular Sequence Data
  • Kinetics
  • Humans
  • GTP-Binding Proteins