A Review of Research on mTOR Inhibitors

作者：Tang Yan^*; Gong Yuesong; Xu Yungen; You Qidong

来源：Chinese Journal of Organic Chemistry, 2011, 31(7): 1144-1154.

• mTOR inhibitor
• rapamycin
• anti-tumor
• immunosuppression

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.

• 出版日期2011-7
• 单位中国药科大学