Mammalian target of rapamycin (mTOR) Inhibitors

Curr Oncol Rep. 2004 Mar;6(2):111-5. doi: 10.1007/s11912-004-0022-5.


Current efforts in anticancer drug development are targeting key factors in cell-cycle regulation. Mammalian target of rapamycin (mTOR) is one such protein kinase that facilitates cell growth by stimulating the cell to traverse the G1 to S phase of the cell cycle. Rapamycin is the first defined inhibitor of mTOR, and the demonstration of its antitumor activity has led to great interest in this pathway as an antitumor mechanism. Analogues with better pharmacologic properties have been developed and have entered clinical trials. Human cell lines of renal cell cancer, among several other tumors, are sensitive to growth inhibition via this pathway. Ongoing clinical trials are evaluating renal cell cancer and other malignancies using therapy with mTOR inhibitors. These agents are more likely to induce growth inhibition rather than tumor regression.

Publication types

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

MeSH terms

  • Antibiotics, Antineoplastic / pharmacology
  • Antibiotics, Antineoplastic / therapeutic use*
  • Cell Division / drug effects
  • Cell Line, Tumor
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Protein Kinase Inhibitors*
  • Protein Kinases*
  • Sirolimus / pharmacology
  • Sirolimus / therapeutic use*
  • TOR Serine-Threonine Kinases


  • Antibiotics, Antineoplastic
  • Protein Kinase Inhibitors
  • Protein Kinases
  • MTOR protein, human
  • TOR Serine-Threonine Kinases
  • Sirolimus