Individualized strategies to target specific mechanisms of disease in malignant melanoma patients displaying unique mutational signatures

Oncotarget. 2015 Sep 22;6(28):25452-65. doi: 10.18632/oncotarget.4545.

Abstract

Targeted treatment of advanced melanoma could benefit from the precise molecular characterization of melanoma samples. Using a melanoma-specific selection of 217 genes, we performed targeted deep sequencing of a series of biopsies, from advanced melanoma cases, with a Breslow index of ≥ 4 mm, and/or with a loco-regional infiltration in lymph nodes or presenting distant metastasis, as well of a collection of human cell lines. This approach detected 3-4 mutations per case, constituting unique mutational signatures associated with specific inhibitor sensitivity. Functionally, case-specific combinations of inhibitors that simultaneously targeted MAPK-dependent and MAPK-independent mechanisms were most effective at inhibiting melanoma growth, against each specific mutational background. These observations were challenged by characterizing a freshly resected biopsy from a metastatic lesion located in the skin and soft tissue and by testing its associated therapy ex vivo and in vivo using melanocytes and patient-derived xenografted mice, respectively. The results show that upon mutational characterization of advanced melanoma patients, specific mutational profiles can be used for selecting drugs that simultaneously target several deregulated genes/pathways involved in tumor generation or progression.

Keywords: BRAF; MAPK; melanoma; somatic mutations; targeted therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Biomarkers, Tumor / genetics*
  • Biopsy
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • DNA Mutational Analysis / methods*
  • Gene Expression Profiling / methods*
  • Genetic Predisposition to Disease
  • Humans
  • Lymphatic Metastasis
  • Melanocytes / drug effects
  • Melanocytes / metabolism
  • Melanocytes / pathology
  • Melanoma / drug therapy*
  • Melanoma / genetics*
  • Melanoma / secondary
  • Mice, Inbred BALB C
  • Mice, Inbred NOD
  • Mice, Nude
  • Molecular Targeted Therapy
  • Mutation*
  • Patient Selection
  • Phenotype
  • Precision Medicine*
  • Predictive Value of Tests
  • Protein Kinase Inhibitors / therapeutic use
  • Signal Transduction / drug effects
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / genetics*
  • Skin Neoplasms / pathology
  • Time Factors
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Protein Kinase Inhibitors