Recent progress on MAP kinase pathway inhibitors

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4047-56. doi: 10.1016/j.bmcl.2015.07.093. Epub 2015 Aug 1.


The RAS-RAF-MEK-ERK, or ERK signaling pathway propagates signals through an intracellular signal transduction cascade. Since approximately one third of human cancers are impacted by mutations in the ERK signaling pathway, intensive efforts to develop drugs targeting members of this cascade are ongoing. While efforts to develop drugs aimed at inhibiting RAS are still at an early stage, substantial progress in discovering clinical drugs targeting RAF, MEK, and ERK have been made. This review will highlight the recent progress in this area.

Keywords: B-RAF; ERK; Kinase; MAPK; MEK.

Publication types

  • Review

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Humans
  • MAP Kinase Signaling System / drug effects*
  • Molecular Structure
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Structure-Activity Relationship


  • Protein Kinase Inhibitors