B-Raf kinase inhibitors for cancer treatment

Curr Opin Investig Drugs. 2007 Jun;8(6):452-6.


The Raf-MEK-ERK signaling pathway is critical for cell survival, growth, proliferation and tumorigenesis. Among the three isoforms of Raf protein kinases, in vitro and in vivo studies have shown that B-Raf functions as the primary MEK activator. B-Raf is one of the most frequently mutated genes in human cancers with a high prevalence in melanoma, and many of the B-Raf mutations activate the kinase activity of B-Raf. B-Raf kinase represents an excellent target for anticancer therapy based on preclinical target validation, epidemiology and drugability. Several small-molecule inhibitors of B-Raf kinase are currently undergoing clinical evaluation, with others due to enter clinical development in the near future.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Benzenesulfonates / pharmacology
  • Benzenesulfonates / therapeutic use
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Humans
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology*
  • Niacinamide / analogs & derivatives
  • Phenylurea Compounds
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
  • Pyridines / pharmacology
  • Pyridines / therapeutic use
  • Sorafenib


  • Antineoplastic Agents
  • Benzenesulfonates
  • Enzyme Inhibitors
  • Imidazoles
  • Phenylurea Compounds
  • Pyridines
  • SB-590885
  • Niacinamide
  • Sorafenib
  • Proto-Oncogene Proteins B-raf