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PI3K and mTOR inhibitors: a new generation of targeted anticancer agents

机译:PI3K和mTOR抑制剂:新一代靶向抗癌药

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摘要

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.
机译:流行病学和实验研究支持磷酸肌醇3-激酶(PI3K)/雷帕霉素(mTOR)途径的哺乳动物靶标在人类癌症生物学中的重要作用。在过去的几年中,这种信号级联反应的许多组成部分一直是激烈的药物发现活动的主题。本文总结了PI3K和mTOR激酶抑制剂的鉴定进展,重点介绍了目前正在进行临床试验的药物。还讨论了新一代抗癌药的潜在组合策略,安全性问题和耐药机制。

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