Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (07): 1144-1154. Previous Articles     Next Articles

Reports

mTOR抑制剂的研究概况

唐琰1,贡岳松2,徐云根*,1,尤启冬1   

  1. (1中国药科大学药物化学教研室 南京 21009)
    (2 Department of Neurology, Drexel University College of Medicine, Philadelphia, PA 19102, USA)
  • 收稿日期:2010-08-16 修回日期:2011-01-19 出版日期:2011-07-25 发布日期:2011-03-01
  • 通讯作者: 徐云根 E-mail:xyg64@126.com

A Review of Research on mTOR Inhibitors

Tang Yan1 Gong Yuesong2 Xu Yun-gen*,1 You Qidong1   

  1. (1 Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 21009)
    (2 Department of Neurology, Drexel University College of Medicine, Philadelphia, PA 19102, USA)
  • Received:2010-08-16 Revised:2011-01-19 Online:2011-07-25 Published:2011-03-01
  • Contact: Yun-Gen XU E-mail:xyg64@126.com

mTOR, a serine/threonine kinase, is a target molecule of rapamycin. In cells, mTOR acts as the catalytic subunit of two functionally distinct complexes, called mTORC1 and mTORC2. These complexes coordinate a variety of processes that include gene transcription, protein translation initiation, ribosome biosynthesis, apoptosis and many other biological processes. Dysregulation of mTOR signal pathway is closely related with tumorigenesis. Inhibition of mTOR pathway leads to an effective block of abnormal signal transduction and blocks the development of cancer. Traditional mTOR inhibitors are rapamycin and its derivatives, among which everolimus and temsirolimus have already been approved for the treatment of renal-cell carcinoma. In addition, a number of small molecule inhibitors of mTOR, including several PI3K/mTOR dual inhibitors, have been developed. NVP-BEZ235, PKI587, PKI179, GSK2126458, AZD8055 and WYE-354 have entered the clinical stage.

Key words: mTOR inhibitor, rapamycin, anti-tumor, immunosuppression