Metformin accelerates the growth of BRAF V600E-driven melanoma by upregulating VEGF-A

Cancer Discov. 2012 Apr;2(4):344-55. doi: 10.1158/2159-8290.CD-11-0280. Epub 2012 Mar 31.

Abstract

The antidiabetic drug metformin has antitumor activity in a variety of cancers because it blocks cell growth by inhibiting TORC1. Here, we show that melanoma cells that are driven by oncogenic BRAF are resistant to the growth-inhibitory effects of metformin because RSK sustains TORC1 activity even when AMP-activated protein kinase (AMPK) is activated. We further show that AMPK targets the dual-specificity protein phosphatase DUSP6 for degradation and this increases ERK activity, which then upregulates the VEGF-A protein. Critically, this drives angiogenesis and accelerates the growth of BRAF-driven tumors in mice. Unexpectedly, however, when VEGF signaling is inhibited, instead of accelerating tumor growth, metformin inhibits tumor growth. Thus, we show that BRAF-driven melanoma cells are resistant to the antigrowth effects of AMPK and that AMPK mediates cell-autonomous and cell-nonautonomous effects that accelerate the growth of these cells in vivo.

Significance: Metformin inhibits the growth of most tumor cells, but BRAF-mutant melanoma cells are resistant to metformin in vitro, and metformin accelerates their growth in vivo. Unexpectedly, VEGF inhibitors and metformin synergize to suppress the growth of BRAF-mutant tumors, revealing a combination of drugs that may be effective in these patients.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Animals
  • Axitinib
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Disease Models, Animal
  • Drug Synergism
  • Enzyme Activation
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Humans
  • Imidazoles / pharmacology
  • Indazoles / pharmacology
  • Melanoma / genetics*
  • Melanoma / metabolism
  • Melanoma / pathology*
  • Metformin / pharmacology*
  • Mice
  • Mutation*
  • Protein Kinase Inhibitors / pharmacology
  • Proto-Oncogene Proteins B-raf / genetics*
  • Proto-Oncogene Proteins B-raf / metabolism
  • Ribosomal Protein S6 Kinases / metabolism
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / genetics*
  • Vascular Endothelial Growth Factor A / metabolism
  • Xenograft Model Antitumor Assays

Substances

  • Imidazoles
  • Indazoles
  • Protein Kinase Inhibitors
  • Vascular Endothelial Growth Factor A
  • Metformin
  • Axitinib
  • Proto-Oncogene Proteins B-raf
  • Ribosomal Protein S6 Kinases
  • Extracellular Signal-Regulated MAP Kinases
  • AMP-Activated Protein Kinases