Rheb inhibits C-raf activity and B-raf/C-raf heterodimerization

J Biol Chem. 2006 Sep 1;281(35):25447-56. doi: 10.1074/jbc.M605273200. Epub 2006 Jun 27.

Abstract

The Ras-Raf-MEK signaling cascade is critical for normal development and is activated in many forms of cancer. We have recently shown that B-Raf kinase interacts with and is inhibited by Rheb, the target of the GTPase-activating domain of the tuberous sclerosis complex 2 gene product tuberin. Here, we demonstrate for the first time that activation of Rheb is associated with decreased B-Raf and C-Raf phosphorylation at residues Ser-446 and Ser-338, respectively, concomitant with a decrease in the activities of both kinases and decreased heterodimerization of B-Raf and C-Raf. Importantly, the impact of Rheb on B-Raf/C-Raf heterodimerization and kinase activity are rapamycin-insensitive, indicating that they are independent of Rheb activation of the mammalian target of rapamycin-Raptor complex. In addition, we found that Rheb inhibits the association of B-Raf with H-Ras. Taken together, these results support a central role of Rheb in the regulation of the Ras/B-Raf/C-Raf/MEK signaling network.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Dimerization
  • Gene Expression Regulation
  • Humans
  • Monomeric GTP-Binding Proteins / physiology*
  • Neuropeptides / physiology*
  • Phosphorylation
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins B-raf / chemistry
  • Proto-Oncogene Proteins B-raf / metabolism*
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-raf / chemistry
  • Proto-Oncogene Proteins c-raf / metabolism
  • Ras Homolog Enriched in Brain Protein
  • Serine / chemistry
  • Signal Transduction
  • Sirolimus / pharmacology

Substances

  • Neuropeptides
  • RHEB protein, human
  • Ras Homolog Enriched in Brain Protein
  • Serine
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf
  • Proto-Oncogene Proteins c-raf
  • Monomeric GTP-Binding Proteins
  • Sirolimus