Disruption of the RAS-RAF1 Interaction: A New Synthetic Lethality Strategy for Selectively Blocking RAS-Driven Proliferation of Cancer Cells

Time: 5:00 pm
day: Day One Track G


  • Using our PPI-disruption identifying platform, ToRPPIDO, we have discovered several new compounds that allosterically disrupt the Ras-Raf1 protein-protein interaction by binding Raf1 in a new pocket distal to its Ras Binding Domain
  • STX200, a cell-permeable member of this set, exhibits a potent anti-proliferative activity against a variety of mutant RAS cancer lines
  • The anti-proliferative activity of STX200 is independent of the kinase activity of Raf1 in canonical MAPK signaling