PI3K and mTOR inhibitors - a new generation of targeted anticancer agents
PI3K and mTOR inhibitors - a new generation of targeted anticancer agents
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DOI：
10.1016/j.ceb.2008.12.011
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发表时间：
2009-04-01
影响因子：
7.5
通讯作者：
Garcia-Echeverria, Carlos
中科院分区：
文献类型：
--
作者：
Brachmann, Saskia;Fritsch, Christine;Garcia-Echeverria, Carlos
流行病学和实验研究支持磷酸肌醇3-激酶（PI 3 K）/哺乳动物雷帕霉素靶蛋白（mTOR）通路在人类癌症生物学中的重要作用。在过去的几年中，这种信号级联的许多组分一直是激烈的药物发现活动的主题。本文综述了PI 3 K和mTOR激酶抑制剂的研究进展，重点介绍了目前正在进行临床试验的药物。潜在的组合策略，安全性问题，这新一代的抗癌药物的耐药机制进行了讨论。
Epidemiological and experimental studies support an important role of the phosphoinosite 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) pathway in the biology of human cancers. Over the past few years a number of components of this signaling cascade have been the subject of intense drug discovery activities. This article summarizes progress made in the identification of kinase inhibitors of PI3K and mTOR, with an emphasis placed on drugs currently undergoing clinical trials. Potential combination strategies, safety concerns, and resistance mechanisms for this new generation of anticancer agents are also discussed.