Sensitizing non-small cell lung cancer to BCL-xL-targeted apoptosis

Cell Death Dis. 2018 Sep 24;9(10):986. doi: 10.1038/s41419-018-1040-9.

Abstract

Lung cancer is the leading cause of death in the United States, with non-small cell lung cancers (NSCLC) accounting for 85% of all cases. By analyzing the expression profile of the pro-apoptotic and anti-apoptotic proteins, we have assigned NSCLCs into two distinct groups. While single agent treatment with the BCL-2/BCL-xL/BCL-w inhibitor ABT-263 (navitoclax) did not trigger apoptosis in either group, cells with a moderate to high level of MCL-1 expression were sensitive to ABT-263 treatment when MCL-1 expression was suppressed with a gene-specific siRNA. In contrast, those with a low MCL-1 expression did not undergo apoptosis upon combination treatment with ABT-263 and MCL-1 siRNA. Further studies revealed that cells with a low MCL-1 expression had low mitochondrial priming, and treatment with the chemotherapy drug docetaxel raised the mitochondrial priming level and consequently sensitized cells to ABT-263. These results establish a rationale for molecular profiling and a therapeutic strategy to treat NSCLC patients with pro-apoptotic anti-cancer drugs based on their MCL-1 expression level.

Publication types

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

MeSH terms

  • A549 Cells
  • Aniline Compounds / pharmacology*
  • Apoptosis / drug effects*
  • Apoptosis Regulatory Proteins / metabolism
  • Carcinoma, Non-Small-Cell Lung / metabolism*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Cell Polarity
  • Cell Survival / drug effects
  • Docetaxel / pharmacology*
  • Drug Resistance, Neoplasm / drug effects
  • Drug Synergism
  • Gene Knockout Techniques
  • Humans
  • Lung Neoplasms / metabolism*
  • Lung Neoplasms / pathology
  • Membrane Proteins / genetics
  • Membrane Proteins / metabolism*
  • Mitochondria / metabolism
  • Proto-Oncogene Proteins / metabolism
  • Sulfonamides / pharmacology*
  • Transfection
  • bcl-X Protein / metabolism*

Substances

  • Aniline Compounds
  • Apoptosis Regulatory Proteins
  • BBC3 protein, human
  • BCL2L1 protein, human
  • MLC1 protein, human
  • Membrane Proteins
  • Proto-Oncogene Proteins
  • Sulfonamides
  • bcl-X Protein
  • Docetaxel
  • navitoclax