| PI3K/mTOR双重抑制剂的研究进展 |
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| 引用本文： | 宣 伟,邵 藤,李义平,张三奇. PI3K/mTOR双重抑制剂的研究进展[J]. 医学教育探索, 2012, 27(2): 133-137 |
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| 作者姓名： | 宣 伟 邵 藤 李义平 张三奇 |
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| 作者单位： | 西安交通大学 医学院 药学系，陕西 西安 710061 |
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| 摘 要： | 磷脂酰肌醇3-激酶/哺乳动物雷帕霉素靶蛋白（phosphoinosmde-3-kinase/the mammalian target of rapamycin，PI3K/mTOR）双重抑制剂已经成为抗肿瘤药物研发的热点之一。本文介绍芳基脲类和3-吡啶基杂环类等PI3K/mTOR双重抑制剂的化学结构，根据其结构特点及其与PI3Kγ共结晶模式，剖析了两类抑制剂药效团的基本结构。
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| 关 键 词： | PI3K/mTOR双重抑制剂；药效团；抗肿瘤药物 |
Research progress on PI3K/mTOR dual inhibitors |
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| XUAN Wei,SHAO Teng,LI Yi-ping and ZHANG San-qi. Research progress on PI3K/mTOR dual inhibitors[J]. Researches in Medical Education, 2012, 27(2): 133-137 |
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| Authors: | XUAN Wei SHAO Teng LI Yi-ping ZHANG San-qi |
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| Affiliation: | Department of Pharmacy, School of Medicine, Xi'an Jiaotong University, Xi'an 710061, China |
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| Abstract: | phosphoinosmde-3-kinase/the mammalian target of rapamycin (PI3K/mTOR) dual inhibitor is emerging as a hotspot in antitumor drugs research. This review introducesthe chemical structures of PI3K/mTOR dual inhibitors which can be sorted into arylureas and 3-pyridinyl heterocycles. The basic pharmacophore structures were suggested according to the structure characteristics of dual inhibitor and tits co-crystal structure with PI3K. |
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| Keywords: | phosphoinosmde-3-kinase/the mammalian target of rapamycin (PI3K/mTOR) dual inhibitor pharmacophore antitumor drugs |
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