Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents

Eur J Med Chem. 2018 Oct 5:158:144-166. doi: 10.1016/j.ejmech.2018.09.005. Epub 2018 Sep 6.

Abstract

Frequent oncogenic mutations have been identified in MAPK (mitogen-activated protein kinase) signaling pathway components. As a result, MAPK pathway is associated with human cancer initiation, in particular RAF (rapidly accelerated fibrosarcoma) component. The mutation in RAF component leads to auto-activation of MAPK signaling pathway, stimulating the uncontrolled cell growth and proliferation. In last few years, diverse chemical scaffolds have been identified as RAF inhibitors. Most of these scaffolds show potent anti-cancer activity. The present review highlights the recent investigations of RAF inhibitors during the last five years.

Keywords: Anti-cancer agents; MAPK; RAF inhibitors.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Drug Discovery
  • Humans
  • MAP Kinase Signaling System / drug effects*
  • Models, Molecular
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • raf Kinases / antagonists & inhibitors*
  • raf Kinases / chemistry
  • raf Kinases / metabolism

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • raf Kinases