A unifying mechanism for cancer cell death through ion channel activation by HAMLET

PLoS One. 2013;8(3):e58578. doi: 10.1371/journal.pone.0058578. Epub 2013 Mar 7.

Abstract

Ion channels and ion fluxes control many aspects of tissue homeostasis. During oncogenic transformation, critical ion channel functions may be perturbed but conserved tumor specific ion fluxes remain to be defined. Here we used the tumoricidal protein-lipid complex HAMLET as a probe to identify ion fluxes involved in tumor cell death. We show that HAMLET activates a non-selective cation current, which reached a magnitude of 2.74±0.88 nA within 1.43±0.13 min from HAMLET application. Rapid ion fluxes were essential for HAMLET-induced carcinoma cell death as inhibitors (amiloride, BaCl2), preventing the changes in free cellular Na(+) and K(+) concentrations also prevented essential steps accompanying carcinoma cell death, including changes in morphology, uptake, global transcription, and MAP kinase activation. Through global transcriptional analysis and phosphorylation arrays, a strong ion flux dependent p38 MAPK response was detected and inhibition of p38 signaling delayed HAMLET-induced death. Healthy, differentiated cells were resistant to HAMLET challenge, which was accompanied by innate immunity rather than p38-activation. The results suggest, for the first time, a unifying mechanism for the initiation of HAMLET's broad and rapid lethal effect on tumor cells. These findings are particularly significant in view of HAMLET's documented therapeutic efficacy in human studies and animal models. The results also suggest that HAMLET offers a two-tiered therapeutic approach, killing cancer cells while stimulating an innate immune response in surrounding healthy tissues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Transport
  • Calcium / metabolism
  • Cell Death / drug effects
  • Cell Death / physiology*
  • Cell Line, Tumor
  • Cluster Analysis
  • Gene Expression Profiling
  • Humans
  • Immunity, Innate
  • Intracellular Space / metabolism
  • Ion Channels / antagonists & inhibitors
  • Ion Channels / metabolism*
  • Lactalbumin / immunology
  • Lactalbumin / metabolism*
  • Oleic Acids / immunology
  • Oleic Acids / metabolism*
  • Phosphorylation
  • Potassium / metabolism
  • Signal Transduction
  • Sodium / metabolism
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • HAMLET complex, human
  • Ion Channels
  • Oleic Acids
  • Lactalbumin
  • Sodium
  • p38 Mitogen-Activated Protein Kinases
  • Potassium
  • Calcium

Grants and funding

This study was supported by the Sharon D. Lund foundation grant and the American Cancer Society, the Swedish Cancer Society, the Medical Faculty (Lund University), the Söderberg Foundation, the Segerfalk Foundation, the Anna-Lisa and Sven-Erik Lundgren Foundation for Medical Research, the Knut and Alice Wallenberg Foundation, the Lund City Jubileumsfond, the John and Augusta Persson Foundation for Medical Research, the Maggie Stephens Foundation, the Gunnar Nilsson Cancer Foundation, the Inga-Britt and Arne Lundberg Foundation, the H. J. Forssman Foundation for Medical Research and the Royal Physiographic Society. Support was also obtained from the Danish Council for Independent Research (Medical sciences). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.