Combination with γ-secretase inhibitor prolongs treatment efficacy of BRAF inhibitor in BRAF-mutated melanoma cells

Cancer Lett. 2016 Jun 28;376(1):43-52. doi: 10.1016/j.canlet.2016.03.028. Epub 2016 Mar 18.

Abstract

Oncogenic triggering of the MAPK pathway in melanocytes results in senescence, and senescence escape is considered as one critical step for melanocytic transformation. In melanoma, induction of a senescent-like state by BRAF-inhibitors (BRAFi) in a fraction of treated cells - instead of killing - contributes to the repression of tumor growth, but may also provide a source for relapse. Here, we demonstrate that NOTCH activation in melanocytes is not only growth-promoting but it also protects these cells against oncogene-induced senescence. In turn, treatment of melanoma cells with an inhibitor of the NOTCH-activating enzyme γ-secretase led to induction of a senescent-like status in a fraction of the cells but overall achieved only a moderate inhibition of melanoma cell growth. However, combination of γ-secretase inhibitor (GSI) with BRAFi markedly increased the treatment efficacy particularly in long-term culture. Moreover, even melanoma cells starting to regrow after continuous BRAFi treatment - the major problem of BRAFi therapy in patients - can still be affected by the combination treatment. Thus, combining GSI with BRAFi increases the therapeutic efficacy by, at least partially, prolonging the senescent-like state of treated cells.

Keywords: BRAF inhibition; Melanoma; Notch; Senescence.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Amyloid Precursor Protein Secretases / metabolism
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Cell Cycle Checkpoints
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cellular Senescence / drug effects*
  • Cyclin-Dependent Kinase 6 / metabolism
  • Drug Resistance, Neoplasm
  • Humans
  • Melanocytes / drug effects*
  • Melanocytes / enzymology
  • Melanocytes / pathology
  • Melanoma / drug therapy*
  • Melanoma / enzymology
  • Melanoma / genetics
  • Melanoma / pathology
  • Mutation*
  • Phosphorylation
  • Protease Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
  • Proto-Oncogene Proteins B-raf / genetics
  • Proto-Oncogene Proteins B-raf / metabolism
  • Receptor, Notch1 / genetics
  • Receptor, Notch1 / metabolism
  • Retinoblastoma Protein / metabolism
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / enzymology
  • Skin Neoplasms / genetics
  • Skin Neoplasms / pathology
  • Time Factors
  • Transfection

Substances

  • NOTCH1 protein, human
  • Notch1 protein, mouse
  • Protease Inhibitors
  • Protein Kinase Inhibitors
  • Receptor, Notch1
  • Retinoblastoma Protein
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf
  • CDK6 protein, human
  • Cyclin-Dependent Kinase 6
  • Amyloid Precursor Protein Secretases