Targeting the Unfolded Protein Response as a Potential Therapeutic Strategy in Renal Carcinoma Cells Exposed to Cyclosporine A

Anticancer Res. 2017 Mar;37(3):1049-1057. doi: 10.21873/anticanres.11416.

Abstract

Background/aim: Organ transplant patients treated with the immunosuppressive drug cyclosporine A often present malignant kidney tumors. Cyclosporine A can promote oncogenesis in a cell-intrinsic manner by increasing the production of vascular endothelial growth factor (VEGF).

Materials and methods: We explored the impact of cyclosporine A and the role of the unfolded protein response (UPR) on three human renal cell carcinoma (RCC) cell lines under normoxic and hypoxic (1% O2) conditions.

Results: Cyclosporine A regulated the expression of VEGF at the post-transcriptional level. Cyclosporine A induced the inositol requiring enzyme-1α (IRE1α) arm of the UPR and stabilized neosynthesized proteins in RCC cells. Toyocamycin, an inhibitor of IRE1α, abolished the clonogenic growth of RCC cells and reduced induction of VEGF by cyclosporine A under hypoxia.

Conclusion: Our findings highlight the impact of cyclosporine A on the proteostasis of RCC cells, and suggest the potential therapeutic interest of targeting the UPR against tumors arising in the context of organ transplantation.

Keywords: Cyclosporine A; renal cell carcinoma; toyocamycin; unfolded protein response; vascular endothelial growth factor.

MeSH terms

  • Carcinoma, Renal Cell / metabolism*
  • Cell Line, Tumor / drug effects
  • Cyclosporine / chemistry*
  • Endoribonucleases / metabolism
  • Gene Expression Regulation
  • Gene Expression Regulation, Neoplastic*
  • Humans
  • Hypoxia
  • Immunosuppressive Agents / chemistry*
  • Kidney Neoplasms / metabolism*
  • Oxygen / metabolism
  • Polymerase Chain Reaction
  • Protein Serine-Threonine Kinases / metabolism
  • Puromycin / chemistry
  • RNA Interference
  • RNA, Small Interfering / metabolism
  • Toyocamycin / chemistry
  • Unfolded Protein Response*
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Immunosuppressive Agents
  • RNA, Small Interfering
  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A
  • Puromycin
  • Cyclosporine
  • ERN1 protein, human
  • Protein Serine-Threonine Kinases
  • Endoribonucleases
  • Toyocamycin
  • Oxygen