Unraveling the complexities of the Raf/MAP kinase pathway for pharmacological intervention

Trends Mol Med. 2002;8(4 Suppl):S27-31. doi: 10.1016/s1471-4914(02)02307-9.


The Ras-MAP kinase pathway has attracted much attention from academic and pharmaceutical laboratories because of its central role in regulating tumor cell growth and survival, differentiation and angiogenesis. Although the central players in this pathway -Ras, Raf, and MEK - have been well studied, how best to exploit them for therapeutic gain has eluded oncology researchers in the past. Several small-molecule inhibitors that target specific steps of the MAP kinase cascade have recently entered the clinical arena. While we await answers on their ultimate therapeutic use, the availability of translational assays for monitoring target suppression will no doubt play a significant role in optimizing our chances of success.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • MAP Kinase Kinase Kinase 1*
  • MAP Kinase Signaling System / drug effects*
  • Neoplasms / enzymology*
  • Protein-Serine-Threonine Kinases / antagonists & inhibitors
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-raf / metabolism
  • Signal Transduction / physiology


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Protein-Serine-Threonine Kinases
  • Proto-Oncogene Proteins c-raf
  • MAP Kinase Kinase Kinase 1
  • MAP3K1 protein, human