G Protein-coupled receptor kinase 2 (GRK2): A novel modulator of insulin resistance

Arch Physiol Biochem. 2011 Jul;117(3):125-30. doi: 10.3109/13813455.2011.584693. Epub 2011 May 26.


G protein-coupled receptor kinase 2 (GRK2) is emerging as a key, integrative node in many signalling pathways. Besides its canonical role in the modulation of the signalling mediated by many G protein-coupled receptors (GPCR), this protein can display a very complex network of functional interactions with a variety of signal transduction partners, in a stimulus, cell type, or context-specific way. We review herein recent data showing that GRK2 can regulate insulin-triggered transduction cascades at different levels and that this protein plays a relevant role in insulin resistance and obesity in vivo, what uncovers GRK2 as a potential therapeutic target in the treatment of these disorders.

Publication types

  • Review

MeSH terms

  • Adipocytes / cytology
  • Adipocytes / metabolism
  • Adiposity / physiology
  • Animals
  • G-Protein-Coupled Receptor Kinase 2 / metabolism*
  • Humans
  • Insulin / metabolism
  • Insulin Resistance / physiology*
  • Obesity / physiopathology
  • Obesity / therapy
  • Receptor, Insulin / metabolism
  • Receptors, G-Protein-Coupled / metabolism
  • Signal Transduction / physiology


  • Insulin
  • Receptors, G-Protein-Coupled
  • Receptor, Insulin
  • G-Protein-Coupled Receptor Kinase 2