Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics

Do Hee Kim, Taebo Sim

Research output: Contribution to journalArticle

29 Citations (Scopus)


Aberrant activation of Raf signaling pathway is frequently found in various human tumors, it has been considered as distinct and promising molecular target for cancer therapeutics. B-Raf is most attractive drug target out of three Raf isoforms (A-Raf, B-Raf and C-Raf) because it exhibits high kinase activity due to frequent mutations in human tumors. However, most recently, it has been reported that Raf isoforms show the cross-activation in the presence of specific B-Raf inhibitors, which brings about the paradoxical p-ERK activation as well as tumor promoting effect. According to these findings, it remains controversy whether pan-Raf kinase inhibitor is more valuable and promising rather than specific B-Raf inhibitor under certain conditions in terms of cancer therapeutics. In this short review, novel Raf kinase inhibitors undergoing clinical investigation are introduced. Moreover, the paradoxical p-ERK activation is discussed with specific B-Raf inhibitors, PLX4032/4720 compounds.

Original languageEnglish
Pages (from-to)605-615
Number of pages11
JournalArchives of Pharmacal Research
Issue number4
Publication statusPublished - 2012 Apr 1


  • Cancer
  • Molecular-targeted inhibitor
  • PLX4720/4032
  • Raf kinase
  • Sorafenib

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Medicine
  • Organic Chemistry

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