Amuvatinib has cytotoxic effects against NRAS-mutant melanoma but not BRAF-mutant melanoma

Melanoma Res. 2014 Oct;24(5):448-53. doi: 10.1097/CMR.0000000000000103.

Abstract

Effective targeted therapy strategies are still lacking for the 15-20% of melanoma patients whose melanomas are driven by oncogenic NRAS. Here, we report on the NRAS-specific behavior of amuvatinib, a kinase inhibitor with activity against c-KIT, Axl, PDGFRα, and Rad51. An analysis of BRAF-mutant and NRAS-mutant melanoma cell lines showed the NRAS-mutant cohort to be enriched for targets of amuvatinib, including Axl, c-KIT, and the Axl ligand Gas6. Increasing concentrations of amuvatinib selectively inhibited the growth of NRAS-mutant, but not BRAF-mutant melanoma cell lines, an effect associated with induction of S-phase and G2/M-phase cell cycle arrest and induction of apoptosis. Mechanistically, amuvatinib was noted to either inhibit Axl, AKT, and MAPK signaling or Axl and AKT signaling and to induce a DNA damage response. In three-dimensional cell culture experiments, amuvatinib was cytotoxic against NRAS-mutant melanoma cell lines. Thus, we show for the first time that amuvatinib has proapoptotic activity against melanoma cell lines, with selectivity observed for those harboring oncogenic NRAS.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Apoptosis
  • Axl Receptor Tyrosine Kinase
  • Cell Culture Techniques
  • Cell Cycle
  • Cell Line, Tumor
  • Cohort Studies
  • DNA Damage
  • Genes, ras*
  • Humans
  • Inhibitory Concentration 50
  • Intercellular Signaling Peptides and Proteins / genetics
  • Ligands
  • Melanoma / drug therapy*
  • Melanoma / genetics
  • Mutation
  • Piperazines
  • Proteomics
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins B-raf / genetics*
  • Proto-Oncogene Proteins c-kit / metabolism
  • Pyrimidines / therapeutic use*
  • Receptor Protein-Tyrosine Kinases / metabolism
  • Signal Transduction
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / genetics
  • Thiourea

Substances

  • Intercellular Signaling Peptides and Proteins
  • Ligands
  • Piperazines
  • Proto-Oncogene Proteins
  • Pyrimidines
  • growth arrest-specific protein 6
  • Proto-Oncogene Proteins c-kit
  • Receptor Protein-Tyrosine Kinases
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf
  • Thiourea
  • amuvatinib
  • Axl Receptor Tyrosine Kinase
  • AXL protein, human