Targeting mTOR: prospects for mTOR complex 2 inhibitors in cancer therapy

Oncogene. 2010 Jul 1;29(26):3733-44. doi: 10.1038/onc.2010.139. Epub 2010 Apr 26.


Small molecule inhibitors that selectively target cancer cells and not normal cells would be valuable anti-cancer therapeutics. The mammalian target of rapamycin complex 2 (mTORC2) is emerging as a promising candidate target for such an inhibitor. Recent studies in cancer biology indicate that mTORC2 activity is essential for the transformation and vitality of a number of cancer cell types, but in many normal cells, mTORC2 activity is less essential. These studies are intensifying interest in developing inhibitors that specifically target mTORC2. However, there are many open questions regarding the function and regulation of mTORC2 and its function in both normal and cancer cells. Here, we summarize exciting new research into the biology of mTORC2 signaling and highlight the current state and future prospects for mTOR-targeted therapy.

Publication types

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

MeSH terms

  • Animals
  • Humans
  • Intracellular Signaling Peptides and Proteins / drug effects*
  • Mechanistic Target of Rapamycin Complex 1
  • Multiprotein Complexes
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Protein Serine-Threonine Kinases / drug effects*
  • Proteins
  • TOR Serine-Threonine Kinases
  • Transcription Factors / metabolism*


  • CRTC2 protein, human
  • Intracellular Signaling Peptides and Proteins
  • Multiprotein Complexes
  • Proteins
  • Transcription Factors
  • MTOR protein, human
  • Mechanistic Target of Rapamycin Complex 1
  • Protein Serine-Threonine Kinases
  • TOR Serine-Threonine Kinases