An inhibitor of mTOR reduces neoplasia and normalizes p70/S6 kinase activity in Pten+/- mice

Proc Natl Acad Sci U S A. 2001 Aug 28;98(18):10320-5. doi: 10.1073/pnas.171060098. Epub 2001 Aug 14.

Abstract

PTEN phosphatase acts as a tumor suppressor by negatively regulating the phosphoinositide 3-kinase (PI3K) signaling pathway. It is unclear which downstream components of this pathway are necessary for oncogenic transformation. In this report we show that transformed cells of PTEN(+/-) mice have elevated levels of phosphorylated Akt and activated p70/S6 kinase associated with an increase in proliferation. Pharmacological inactivation of mTOR/RAFT/FRAP reduced neoplastic proliferation, tumor size, and p70/S6 kinase activity, but did not affect the status of Akt. These data suggest that p70/S6K and possibly other targets of mTOR contribute significantly to tumor development and that inhibition of these proteins may be therapeutic for cancer patients with deranged PI3K signaling.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alleles
  • Animals
  • Base Sequence
  • Cell Transformation, Neoplastic / drug effects
  • DNA Primers / genetics
  • Female
  • Humans
  • Mice
  • Mice, Knockout
  • PTEN Phosphohydrolase
  • Phosphatidylinositol 3-Kinases / metabolism
  • Phosphoric Monoester Hydrolases / deficiency*
  • Phosphoric Monoester Hydrolases / genetics
  • Protein Kinase Inhibitors*
  • Protein Kinases*
  • Ribosomal Protein S6 Kinases / metabolism*
  • Signal Transduction
  • Sirolimus / analogs & derivatives
  • Sirolimus / pharmacology
  • TOR Serine-Threonine Kinases
  • Tumor Suppressor Proteins*
  • Uterine Neoplasms / drug therapy
  • Uterine Neoplasms / genetics
  • Uterine Neoplasms / metabolism
  • Uterine Neoplasms / pathology

Substances

  • DNA Primers
  • Protein Kinase Inhibitors
  • Tumor Suppressor Proteins
  • temsirolimus
  • Protein Kinases
  • MTOR protein, human
  • mTOR protein, mouse
  • Ribosomal Protein S6 Kinases
  • TOR Serine-Threonine Kinases
  • Phosphoric Monoester Hydrolases
  • PTEN Phosphohydrolase
  • PTEN protein, human
  • Sirolimus