Functional analysis of mutations within the kinase activation segment of B-Raf in human colorectal tumors

Cancer Res. 2003 Dec 1;63(23):8132-7.

Abstract

Mutations in the B-Raf gene have been reported in a number of human cancers, including colorectal carcinoma. More than 80% of the B-Raf mutations were V599E. Although other mutations have been reported, their functional consequences were unclear. Here, we examined the effect of colon tumor-associated B-Raf mutations within the kinase activation segment, including V599E, on extracellular signal-regulated kinase (Erk) and nuclear factor kappaB (NFkappaB) signaling, and on the transformation of NIH3T3 fibroblasts. Among the six mutations examined, only the B-Raf V599E and K600E mutations greatly increased Erk and NFkappaB signaling, and the transformation of NIH3T3 cells. The B-Raf F594L mutation moderately elevated Erk signaling and NIH3T3 transformation, but did not significantly increase NFkappaB signaling. Although the basal kinase activity of the B-Raf T598I mutant was comparable with that of wild-type, its oncogenic Ras-induced kinase activity was decreased to 60% of wild-type activity. The B-Raf D593V and G595R mutants showed severely reduced kinase activity and affected neither NFkappaB signaling nor NIH3T3 transforming activity. These results suggest that the B-Raf activation segment mutations other than V599E reported in colorectal tumors do not necessarily contribute to carcinogenesis by increasing kinase and transforming activities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 14-3-3 Proteins
  • Amino Acid Sequence
  • Animals
  • Cell Transformation, Neoplastic / genetics
  • Colorectal Neoplasms / enzymology*
  • Colorectal Neoplasms / genetics*
  • Enzyme Activation
  • HSP90 Heat-Shock Proteins / metabolism
  • Humans
  • MAP Kinase Kinase Kinase 1*
  • MAP Kinase Kinase Kinases / metabolism
  • Mice
  • Mitogen-Activated Protein Kinase Kinases / metabolism
  • Molecular Sequence Data
  • Mutation*
  • NF-kappa B / physiology
  • NIH 3T3 Cells
  • Proto-Oncogene Proteins B-raf
  • Proto-Oncogene Proteins c-raf / genetics*
  • Proto-Oncogene Proteins c-raf / metabolism
  • Signal Transduction / physiology
  • Transcription, Genetic
  • Tyrosine 3-Monooxygenase / metabolism

Substances

  • 14-3-3 Proteins
  • HSP90 Heat-Shock Proteins
  • NF-kappa B
  • Tyrosine 3-Monooxygenase
  • Braf protein, mouse
  • Proto-Oncogene Proteins B-raf
  • Proto-Oncogene Proteins c-raf
  • MAP Kinase Kinase Kinase 1
  • MAP Kinase Kinase Kinases
  • MAP3K1 protein, human
  • Map3k1 protein, mouse
  • Mitogen-Activated Protein Kinase Kinases