Combined inhibition of MEK and nuclear ERK translocation has synergistic antitumor activity in melanoma cells

Sci Rep. 2017 Nov 27;7(1):16345. doi: 10.1038/s41598-017-16558-0.

Abstract

Genetic alterations in BRAF, NRAS and NF1 that activate the ERK cascade, account for over 80% of metastatic melanomas. However, ERK cascade inhibitors have been proven beneficial almost exclusively for BRAF mutant melanomas. One of the hallmarks of the ERK cascade is the nuclear translocation of ERK1/2, which is important mainly for the induction of proliferation. This translocation can be inhibited by the NTS-derived peptide (EPE) that blocks the ERK1/2-importin7 interaction, inhibits the nuclear translocation of ERK1/2, and arrests active ERK1/2 in the cytoplasm. In this study, we found that the EPE peptide significantly reduced the viability of not only BRAF, but also several NRAS and NF1 mutant melanomas. Importantly, combination of the EPE peptide and trametinib showed synergy in reducing the viability of some NRAS mutant melanomas, an effect driven by the partial preservation of negative feedback loops. The same combination significantly reduced the viability of other melanoma cells, including those resistant to mono-treatment with EPE peptide and ERK cascade inhibitors. Our study indicates that targeting the nuclear translocation of ERK1/2, in combination with MEK inhibitors can be used for the treatment of different mutant melanomas.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Biomarkers, Tumor
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Survival
  • Drug Synergism
  • Extracellular Signal-Regulated MAP Kinases / metabolism*
  • Humans
  • MAP Kinase Signaling System / drug effects
  • Melanoma / genetics
  • Melanoma / metabolism*
  • Melanoma / pathology
  • Mitogen-Activated Protein Kinases / metabolism*
  • Nuclear Localization Signals / chemistry
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Protein Transport / drug effects
  • Proto-Oncogene Proteins B-raf / genetics
  • Proto-Oncogene Proteins B-raf / metabolism

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Nuclear Localization Signals
  • Peptides
  • Proto-Oncogene Proteins B-raf
  • Extracellular Signal-Regulated MAP Kinases
  • Mitogen-Activated Protein Kinases