蛋白激酶B/Akt抑制剂 |
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引用本文: | 郝茜,钟嫄,王朋,赵桂森. 蛋白激酶B/Akt抑制剂[J]. 生命的化学, 2011, 0(4) |
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作者姓名: | 郝茜 钟嫄 王朋 赵桂森 |
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作者单位: | 山东大学药学院药物化学研究所; |
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基金项目: | 国家自然科学基金项目(21072115)资助 |
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摘 要: | 磷脂酰肌醇-3-激酶(phosphatidylinositol 3-kinase,PI3K)/蛋白激酶B(protein kinase B,PKB/Akt)信号通路在细胞生长与存活中起着关键作用,PI3K/Akt通路的过度激活在多种肿瘤中常见。Akt激酶本身以及Akt激酶上游调节分子,例如PTEN和PI3K,在超过50%的人类肿瘤中均有异常变化。因此Akt成为肿瘤预防和肿瘤靶向治疗的热点之一。许多小分子化合物通过不同机制抑制Akt活性,根据小分子抑制剂与激酶的结合部位和化学结构不同,主要分为ATP竞争性抑制剂、Akt变构抑制剂和磷脂酰肌醇类似物抑制剂。本文综述了PI3K/Akt通路与肿瘤的关系和Akt抑制剂的研究现状,为新型抗癌药物的设计研究提供参考。
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关 键 词: | 抗肿瘤 PI3K/Akt信号通路 Akt抑制剂 |
Research progress of protein kinase B/Akt inhibitors |
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Abstract: | PI3K(phosphatidylinositol 3-kinase)/Akt(protein kinase B,PKB) signaling pathway plays a key role in cell growth and survival.Excessive activation of PI3K/Akt pathway has been found in many tumors.In more than 50% of human tumors,Akt or/and its upstream regulatory molecules(such as PTEN and PI3K) changes abnormally.So Akt has become a hot target for cancer prevention and therapy.Recently,many effective small-molecule Akt inhibitors with different mechanisms have been found.According to the binding site and/o... |
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Keywords: | anti-tumor agent PI3K/Akt signaling pathway Akt inhibitor |
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