A novel chemoradiation targeting stem and nonstem pancreatic cancer cells by repurposing disulfiram

Cancer Lett. 2017 Nov 28:409:9-19. doi: 10.1016/j.canlet.2017.08.028. Epub 2017 Aug 30.

Abstract

Pancreatic ductal adenocarcinoma (PDAC) has a 5-year relative survival rate of 8% and is projected to be the second leading cause of cancer death by 2030, underscoring the urgency to develop new strategies to improve current therapeutic modalities for PDAC. Targeting pancreatic cancer stem cells (PCSCs), which are resistant to radiation and chemotherapy, is a promising strategy. A novel approach which can be readily clinically translated is to repurpose disulfiram (DSF), a drug for treating alcoholism, to target PCSCs. Chemoradiation or the combination of chemotherapy agents FOLFIRINOX, currently standard care for PDAC, can increase stemness in some established or primary PDAC cell lines. However, DSF in the presence of exogenously or endogenously supplied copper (Cu), when combined with chemotherapy or chemoradiation, targets both PCSCs and nonstem PDAC cells. Previously, we demonstrated that DSF/Cu effectively targets breast cancer stem cells in the context of fractionated radiation (FIR) by inhibiting the NF-κB-stemness gene pathway. Therefore, the hypothesis that PCSCs can be effectively targeted by incorporating DSF/Cu into the standard chemoradiation regimen consisting of 5-FU and FIR was investigated and found to be effective in vitro in targeting PCSCs, identified as either ALDHbright or CD24+/CD44+/ESA+ or sphere-forming cells, as well as nonstem PDAC cells. In vivo, the combination of IR+5-FU+DSF/Cu was more effective (72.46%) than either IR+5-FU (30.32%) or IR+FOLFIRINOX therapy (43.04%) in inhibiting growth of the mouse Panc02 tumor. These encouraging results provide a solid foundation for clinical trials to improve the outcomes of the current standard chemoradiation therapy regimen for PDAC.

Keywords: Chemoradiation; Chemoradiotherapy-resistance; Disulfiram; PDAC; Stem cells.

Publication types

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

MeSH terms

  • Acetaldehyde Dehydrogenase Inhibitors / pharmacology
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Carcinoma, Pancreatic Ductal / drug therapy*
  • Carcinoma, Pancreatic Ductal / genetics
  • Carcinoma, Pancreatic Ductal / pathology
  • Carcinoma, Pancreatic Ductal / radiotherapy*
  • Cell Line, Tumor
  • Chemoradiotherapy
  • Copper / pharmacology
  • Disulfiram / pharmacology*
  • Drug Repositioning
  • Female
  • Fluorouracil / pharmacology
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / pathology
  • Neoplastic Stem Cells / radiation effects*
  • Pancreatic Neoplasms / drug therapy*
  • Pancreatic Neoplasms / genetics
  • Pancreatic Neoplasms / pathology
  • Pancreatic Neoplasms / radiotherapy*
  • Radiation-Sensitizing Agents / pharmacology
  • Random Allocation

Substances

  • Acetaldehyde Dehydrogenase Inhibitors
  • Radiation-Sensitizing Agents
  • Copper
  • cuprous chloride
  • Disulfiram
  • Fluorouracil