Ubiquitination of K-Ras enhances activation and facilitates binding to select downstream effectors

Sci Signal. 2011 Mar 8;4(163):ra13. doi: 10.1126/scisignal.2001518.

Abstract

The guanosine triphosphate (GTP)--loaded form of the guanosine triphosphatase (GTPase) Ras initiates multiple signaling pathways by binding to various effectors, such as the kinase Raf and phosphatidylinositol 3-kinase (PI3K). Ras activity is increased by guanine nucleotide exchange factors that stimulate guanosine diphosphate release and GTP loading and is inhibited by GTPase-activating proteins that stimulate GTP hydrolysis. KRAS is the most frequently mutated RAS gene in cancer. Here, we report that monoubiquitination of lysine-147 in the guanine nucleotide-binding motif of wild-type K-Ras could lead to enhanced GTP loading. Furthermore, ubiquitination increased the binding of the oncogenic Gly12Val mutant of K-Ras to the downstream effectors PI3K and Raf. Thus, monoubiquitination could enhance GTP loading on K-Ras and increase its affinity for specific downstream effectors, providing a previously unidentified mechanism for Ras activation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Sequence
  • Cell Line
  • Chromatography, Affinity
  • Guanosine Triphosphate / metabolism
  • Humans
  • Lysine / metabolism
  • Models, Molecular*
  • Molecular Sequence Data
  • Phosphatidylinositol 3-Kinases / metabolism
  • Protein Binding / physiology*
  • Proto-Oncogene Proteins / metabolism*
  • Proto-Oncogene Proteins p21(ras)
  • Tandem Mass Spectrometry
  • Ubiquitination / physiology*
  • raf Kinases / metabolism
  • ras Proteins / metabolism*

Substances

  • KRAS protein, human
  • Proto-Oncogene Proteins
  • Guanosine Triphosphate
  • Phosphatidylinositol 3-Kinases
  • raf Kinases
  • Proto-Oncogene Proteins p21(ras)
  • ras Proteins
  • Lysine