Rationale for RAS mutation-tailored therapies

Future Oncol. 2017 Feb;13(3):263-271. doi: 10.2217/fon-2016-0363. Epub 2016 Oct 12.


RAS mutations are among the most common genetic alterations found in cancerous tumors but rational criteria or strategies for targeting RAS-dependent tumors are only recently emerging. Clinical and laboratory data suggest that patient selection based on specific RAS mutations will be an essential component of these strategies. A thorough understanding of the biochemical and structural properties of mutant RAS proteins form the theoretical basis for these approaches. Direct inhibition of KRAS G12C by covalent inhibitors is a notable recent example of the RAS mutation-tailored approach that establishes a paradigm for other RAS mutation-centered strategies.

Keywords: GTPase; RAS; cancer; isoforms.

Publication types

  • Review

MeSH terms

  • Alleles
  • Cell Transformation, Neoplastic / genetics
  • Cell Transformation, Neoplastic / metabolism
  • Gene Expression Regulation, Neoplastic
  • Genotype
  • Humans
  • Molecular Targeted Therapy*
  • Mutation*
  • Neoplasms / diagnosis
  • Neoplasms / genetics*
  • Neoplasms / mortality
  • Neoplasms / therapy*
  • Patient Outcome Assessment
  • Prognosis
  • Protein Isoforms
  • ras Proteins / genetics*
  • ras Proteins / metabolism


  • Protein Isoforms
  • ras Proteins