BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling

Sci Signal. 2014 Mar 25;7(318):ra30. doi: 10.1126/scisignal.2004815.

Abstract

Melanoma is a highly metastatic and lethal form of skin cancer. The protein kinase BRAF is mutated in about 40% of melanomas, and BRAF inhibitors improve progression-free and overall survival in these patients. However, after a relatively short period of disease control, most patients develop resistance because of reactivation of the RAF-ERK (extracellular signal-regulated kinase) pathway, mediated in many cases by mutations in RAS. We found that BRAF inhibition induces invasion and metastasis in RAS mutant melanoma cells through a mechanism mediated by the reactivation of the MEK (mitogen-activated protein kinase kinase)-ERK pathway, increased expression and secretion of interleukin 8, and induction of protease-dependent invasion. These events were accompanied by a cell morphology switch from predominantly rounded to predominantly elongated cells. We also observed similar responses in BRAF inhibitor-resistant melanoma cells. These data show that BRAF inhibitors can induce melanoma cell invasion and metastasis in tumors that develop resistance to these drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Cell Shape / physiology
  • Dimethyl Sulfoxide
  • Drug Resistance, Neoplasm
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Indoles / pharmacology
  • Interleukin-8 / metabolism
  • MAP Kinase Signaling System / physiology*
  • Melanoma / physiopathology*
  • Mice
  • Mice, Nude
  • Neoplasm Invasiveness / genetics
  • Neoplasm Invasiveness / physiopathology*
  • Neoplasm Metastasis / physiopathology*
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins B-raf / genetics
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Skin Neoplasms / physiopathology*
  • Statistics, Nonparametric
  • Sulfonamides / pharmacology

Substances

  • Indoles
  • Interleukin-8
  • PLX 4720
  • Sulfonamides
  • Proto-Oncogene Proteins B-raf
  • Hras protein, mouse
  • Proto-Oncogene Proteins p21(ras)
  • Dimethyl Sulfoxide