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G protein-coupled receptor kinases

J A Pitcher1, N J Freedman, R J Lefkowitz

  • 1Howard Hughes Medical Institute, Department of Medicine (Cardiology), Duke University Medical Center, Durham, North Carolina 27710, USA. pitch001@mc.duke.edu

Annual Review of Biochemistry
|October 6, 1998
PubMed
Summary

G protein-coupled receptor kinases (GRKs) regulate G protein-coupled receptors (GPCRs) by phosphorylation. This review details how various factors control GRK activity, impacting GPCR signaling and desensitization.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cell Signaling

Background:

  • G protein-coupled receptor kinases (GRKs) are serine/threonine protein kinases.
  • GRKs phosphorylate activated G protein-coupled receptors (GPCRs), leading to desensitization.
  • GPCRs are crucial for cellular signal transduction.

Purpose of the Study:

  • To review the diverse regulatory mechanisms controlling GRK activity.
  • To highlight the importance of GRKs in GPCR regulation in vitro and in vivo.

Main Methods:

  • Literature review of studies using recombinant proteins, cell culture, and transgenic models.
  • Analysis of allosteric and other factors influencing GRK activity.

Main Results:

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  • GRK activity is modulated by GPCRs, G protein beta gamma subunits, phospholipids, calcium-binding proteins (calmodulin, recoverin), and posttranslational modifications (isoprenylation, palmitoylation).
  • Autophosphorylation and protein kinase C-mediated phosphorylation also regulate GRK function.
  • These regulatory factors are critical for fine-tuning GPCR signaling pathways.

    • Conclusions:

    • GRKs play a vital role in the regulation of a wide range of GPCRs.
    • Understanding GRK regulation is essential for comprehending cellular responses to external stimuli.
    • The intricate regulatory network of GRKs impacts numerous physiological processes.