Prevention of Akt phosphorylation is a key to targeting cancer stem-like cells by mTOR inhibition

Hum Cell. 2020 Oct;33(4):1197-1203. doi: 10.1007/s13577-020-00416-9. Epub 2020 Aug 26.

Abstract

CD133 expression in pancreatic cancer correlates with poor prognosis and increased metastasis. CD133+ pancreatic cancer cells exhibit cancer stem cell (CSC)-like properties. We established a CD133+ cell-rich subline from Capan-1 pancreatic cancer cells as a pancreatic CSC model and compared the effects of KU-0063794, a dual mTORC1/mTORC2 inhibitor, against those of mTORC1-specific rapamycin. We found that KU-0063794 prevents sphere formation, a self-renewal index, at high concentrations. Rapamycin inhibited sphere formation but to a lesser degree. In the present study, we aimed to determine the mechanistic roles of mTOR complex 2 (mTORC2) in maintaining CSC-like properties. By examining the PI3K/Akt/mTOR signaling pathway, we observed lower Akt phosphorylation in KU-0063794-treated cells. Phosphorylation of mTORC1 downstream effectors was inhibited by both inhibitors. Thus, mTORC2 activates Akt and modulate stem-like properties, whereas mTORC1 downstream signaling correlates directly with stem-like properties.

Keywords: CD133; Mechanistic/mammalian target of rapamycin (mTOR); Pancreatic cancer stem cells; mTOR complex 1 (mTORC1); mTOR complex 2 (mTORC2).

MeSH terms

  • AC133 Antigen / genetics
  • AC133 Antigen / metabolism
  • Gene Expression
  • Humans
  • Mechanistic Target of Rapamycin Complex 1 / genetics
  • Mechanistic Target of Rapamycin Complex 1 / metabolism
  • Mechanistic Target of Rapamycin Complex 2 / genetics
  • Mechanistic Target of Rapamycin Complex 2 / metabolism
  • Morpholines / pharmacology*
  • Neoplastic Stem Cells / pathology*
  • Pancreatic Neoplasms / genetics*
  • Pancreatic Neoplasms / pathology*
  • Phosphorylation / drug effects
  • Phosphorylation / genetics
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Pyrimidines / pharmacology*
  • Signal Transduction / drug effects
  • Signal Transduction / genetics
  • TOR Serine-Threonine Kinases / genetics*
  • TOR Serine-Threonine Kinases / metabolism*
  • TOR Serine-Threonine Kinases / physiology
  • Tumor Cells, Cultured

Substances

  • AC133 Antigen
  • Morpholines
  • PROM1 protein, human
  • Pyrimidines
  • Ku 0063794
  • MTOR protein, human
  • Mechanistic Target of Rapamycin Complex 1
  • Mechanistic Target of Rapamycin Complex 2
  • Proto-Oncogene Proteins c-akt
  • TOR Serine-Threonine Kinases