Discrimination of amino acids mediating Ras binding from noninteracting residues affecting raf activation by double mutant analysis

J Biol Chem. 1997 Nov 21;272(47):29927-33. doi: 10.1074/jbc.272.47.29927.

Abstract

The contribution of residues outside the Ras binding domain of Raf (RafRBD) to Ras-Raf interaction and Ras-dependent Raf activation has remained unresolved. Here, we utilize a double mutant approach to identify complementary interacting amino acids that are involved in Ras-Raf interaction and activation. Biochemical analysis demonstrates that Raf-Arg59 and Raf-Arg67 from RafRBD are interacting residues complementary to Ras-Glu37 located in the Ras effector region. Raf-Arg59 and Raf-Arg67 also mediate interaction with Ras-Glu37 in Ras-dependent Raf activation. The characteristics observed here can be used as criteria for a role of residues from other regions of Raf in Ras-Raf interaction and activation. We developed a quantitative two-hybrid system as a tool to investigate the effect of point mutations on protein-protein interactions that elude biochemical analysis of bacterially expressed proteins. This assay shows that Raf-Ser257 in the RafCR2 domain does not contribute to Ras-Raf interaction and that the Raf-S257L mutation does not restore Raf binding to Ras-E37G. Yet, Raf-S257L displays high constitutive kinase activity and further activation by Ras-G12V/E37G is still impaired as compared with activation by Ras-G12V. This strongly suggests that the RafCR2 domain is an independent domain involved in the control of Raf activity and a common mechanism for constitutively activating mutants may be the interference with the inactive ground state of the kinase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Substitution
  • Animals
  • Binding Sites
  • Cell Line
  • DNA Mutational Analysis / methods*
  • Glutamic Acid / metabolism
  • Mutagenesis, Site-Directed
  • Protein Binding
  • Proto-Oncogene Proteins c-raf / genetics
  • Proto-Oncogene Proteins c-raf / metabolism*
  • Rabbits
  • Saccharomyces cerevisiae
  • Serine / metabolism
  • Transcriptional Activation
  • ras Proteins / genetics
  • ras Proteins / metabolism*

Substances

  • Glutamic Acid
  • Serine
  • Proto-Oncogene Proteins c-raf
  • ras Proteins