Rapamycin passes the torch: a new generation of mTOR inhibitors

被引：813

作者：

Benjamin, Don ^{[1
]}

Colombi, Marco ^{[1
]}

Moroni, Christoph ^{[1
]}

Hall, Michael N. ^{[1
]}

机构：

[1] Univ Basel, Biozentrum, CH-4056 Basel, Switzerland

来源：

NATURE REVIEWS DRUG DISCOVERY | 2011年 / 10卷 / 11期

基金：

瑞士国家科学基金会;

关键词：

P70; S6; KINASE; SENSITIVE PHOSPHOPROTEOME REVEALS; TUBEROUS SCLEROSIS COMPLEX; REDUCES TUMOR-GROWTH; MAMMALIAN TARGET; CELL-GROWTH; LIFE-SPAN; ANTITUMOR-ACTIVITY; PALOMID; 529; 3-KINASE/MAMMALIAN TARGET;

D O I：

10.1038/nrd3531

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Mammalian target of rapamycin (mTOR) is an atypical protein kinase that controls growth and metabolism in response to nutrients, growth factors and cellular energy levels, and it is frequently dysregulated in cancer and metabolic disorders. Rapamycin is an allosteric inhibitor of mTOR, and was approved as an immunosuppressant in 1999. In recent years, interest has focused on its potential as an anticancer drug. However, the performance of rapamycin and its analogues (rapalogues) has been undistinguished despite isolated successes in subsets of cancer, suggesting that the full therapeutic potential of targeting mTOR has yet to be exploited. A new generation of ATP-competitive inhibitors that directly target the mTOR catalytic site display potent and comprehensive mTOR inhibition and are in early clinical trials.

引用

页码：868 / 880

页数：13

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