ERK pathway inhibitors: How low should we go? Academic Article uri icon

Overview

MeSH Major

  • Indazoles
  • MAP Kinase Signaling System
  • Neoplasms
  • Piperazines
  • Proto-Oncogene Proteins B-raf

abstract

  • Resistance to RAF inhibitors is generally accompanied by reactivation of extracellular signal-regulated kinase (ERK) signaling. SCH772984, a selective, ATP-competitive inhibitor of ERK1 and ERK2, is effective in BRAF-mutant models in which resistance is the result of ERK reactivation. SCH772984 may also have a role in the treatment of tumors in which ERK is dysregulated by mutant RAS, NF1, or activated receptor tyrosine kinases, settings in which current RAF inhibitors are ineffective.

publication date

  • July 2013

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1158/2159-8290.CD-13-0245

PubMed ID

  • 23847348

Additional Document Info

start page

  • 719

end page

  • 21

volume

  • 3

number

  • 7