Targeting the mTOR kinase domain: the second generation of mTOR inhibitors.

  title={Targeting the mTOR kinase domain: the second generation of mTOR inhibitors.},
  author={Yan-jie Zhang and Yanwen Duan and X. F. Steven Zheng},
  journal={Drug discovery today},
  volume={16 7-8},
The mTOR signaling pathway is dysregulated in ∼50% of all human malignancies and is a major cancer drug target. Although rapamycin analogs (rapalogs) have shown clinical efficacy in a subset of cancers, they do not fully exploit the antitumor potential of mTOR targeting. Because the mTOR kinase domain is important for rapamycin-sensitive and -insensitive functions, mTOR catalytic inhibitors have been developed recently as the second generation of anti-mTOR agents. Importantly, they have shown… CONTINUE READING

From This Paper

Figures, tables, and topics from this paper.


Publications citing this paper.
Showing 1-10 of 65 extracted citations


Publications referenced by this paper.
Showing 1-10 of 59 references

A first-in-human, Phase l study to evaluate the dual PI3K/ mTOR inhibitor GDC-0980 administered QD in patients with advanced solid tumors or non-Hodgkin’s lymphoma

  • S Dolly
  • J. Clin. Oncol
  • 2010

Activity of the novel dual phosphatidylinositol 3-kinase/ mammalian target of rapamycin inhibitor NVP-BEZ235 against T-cell acute lymphoblastic leukemia

  • F Chiarini
  • Cancer Res
  • 2010

Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR–ABL-expressing leukemic cells

  • N Carayol
  • Proc. Natl Acad. Sci. U. S. A
  • 2010

Similar Papers

Loading similar papers…