c-Src regulates Akt signaling in response to ghrelin via beta-arrestin signaling-independent and -dependent mechanisms

PLoS One. 2009;4(3):e4686. doi: 10.1371/journal.pone.0004686. Epub 2009 Mar 5.

Abstract

The aim of the present study was to identify the signaling mechanisms to ghrelin-stimulated activation of the serine/threonine kinase Akt. In human embryonic kidney 293 (HEK293) cells transfected with GHS-R1a, ghrelin leads to the activation of Akt through the interplay of distinct signaling mechanisms: an early G(i/o) protein-dependent pathway and a late pathway mediated by beta-arrestins. The starting point is the G(i/o)-protein dependent PI3K activation that leads to the membrane recruitment of Akt, which is phosphorylated at Y by c-Src with the subsequent phosphorylation at A-loop (T308) and HM (S473) by PDK1 and mTORC2, respectively. Once the receptor is activated, a second signaling pathway is mediated by beta-arrestins 1 and 2, involving the recruitment of at least beta-arrestins, c-Src and Akt. This beta-arrestin-scaffolded complex leads to full activation of Akt through PDK1 and mTORC2, which are not associated to the complex. In agreement with these results, assays performed in 3T3-L1 preadipocyte cells indicate that beta-arrestins and c-Src are implicated in the activation of Akt in response to ghrelin through the GHS-R1a. In summary this work reveals that c-Src is crucially involved in the ghrelin-mediated Akt activation. Furthermore, the results support the view that beta-arrestins act as both scaffolding proteins and signal transducers on Akt activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3-L1 Cells
  • Animals
  • Arrestins / metabolism*
  • CSK Tyrosine-Protein Kinase
  • Cell Line
  • Enzyme Activation
  • GTP-Binding Protein alpha Subunits, Gi-Go / metabolism
  • Ghrelin / metabolism*
  • Humans
  • Mice
  • Phosphorylation
  • Protein Transport
  • Protein-Tyrosine Kinases / physiology*
  • Proto-Oncogene Proteins / physiology*
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Receptors, Ghrelin / metabolism
  • Signal Transduction*
  • beta-Arrestins
  • src-Family Kinases

Substances

  • Arrestins
  • Ghrelin
  • Proto-Oncogene Proteins
  • Receptors, Ghrelin
  • beta-Arrestins
  • Protein-Tyrosine Kinases
  • CSK Tyrosine-Protein Kinase
  • src-Family Kinases
  • CSK protein, human
  • Proto-Oncogene Proteins c-akt
  • GTP-Binding Protein alpha Subunits, Gi-Go