Recent progress in targeting the Raf/MEK/ERK pathway with inhibitors in cancer drug discovery

Curr Opin Pharmacol. 2005 Aug;5(4):350-6. doi: 10.1016/j.coph.2005.04.007.

Abstract

Since the discovery that activating mutations of the Ras GTPase were associated with 30% or more of human cancers, the RAF/MEK/ERK pathway has been the focus of intense drug discovery effort. Within the new class of molecularly targeted anti-cancer agents progressing through the late stages of clinical development, BAY 43-9006 and PD0325901 have shown considerable promise.

Publication types

  • Review

MeSH terms

  • Animals
  • Benzamides / chemistry
  • Benzamides / therapeutic use
  • Benzenesulfonates / chemistry
  • Benzenesulfonates / therapeutic use
  • Clinical Trials as Topic
  • Diphenylamine / analogs & derivatives
  • Diphenylamine / chemistry
  • Diphenylamine / therapeutic use
  • Extracellular Signal-Regulated MAP Kinases / antagonists & inhibitors*
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / physiopathology
  • Niacinamide / analogs & derivatives
  • Phenylurea Compounds
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / therapeutic use
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-raf / metabolism
  • Pyridines / chemistry
  • Pyridines / therapeutic use
  • Signal Transduction / drug effects*
  • Signal Transduction / physiology
  • Sorafenib

Substances

  • Benzamides
  • Benzenesulfonates
  • PD 0325901
  • Phenylurea Compounds
  • Protein Kinase Inhibitors
  • Pyridines
  • Niacinamide
  • Diphenylamine
  • Sorafenib
  • Proto-Oncogene Proteins c-raf
  • Extracellular Signal-Regulated MAP Kinases