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PI3K-Akt-mTOR信号通路抑制剂的耐药机制研究进展 被引量：3

Mechanisms of Resistance to PI3K-Akt-mTOR Signaling Pathway Inhibitors
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摘要 磷脂肌醇(PI3K)-蛋白激酶B(PKB,Akt)-雷帕霉素靶体蛋白(mTOR)通路抑制剂耐药现象的出现,与其上下游相关联的其他癌蛋白信号通路的反馈机制密切相关。目前已经报道的有关PI3K-Akt-mTOR通路抑制剂耐药机制,基本上可以分为与FOXO和激素受体相关,依赖于MYC,依赖于β-catenin,依赖于JAK/STAT通路,依赖于MAPK通路,及与AXL相关的耐药机制。PI3K-Akt-mTOR通路抑制剂的耐药,极大地影响了该类小分子靶向药物在临床上的使用,通过对其耐药性产生的机制进行探讨和总结,为临床上和其他药物联用克服该类靶向药物耐药提供策略。 The resistance to PI3K-Akt-mTOR pathway inhibitors has close relationship to the negative feedback of its context-dependent signal pathways. According to our current understanding, the resistant mechanisms could be divided into the following basic conditions： related to FOXO and hormone receptor, MYC-dependence, β-catenin-dependence, JAK/STAT pathway-dependence, MAPK pathway-dependence and related to AXL. The emergence of drug resistance to PI3K-Akt-mTOR pathway inhibitors has greatly limited their curative effect. The reported resistance mechanisms to PI3K-Akt-mTOR pathway inhibitors to search for potential strategies for overcoming resistance by drug combination were summarized.
作者 曹品容 孔应利 罗燕梅 黄维 许建华 叶敏
机构地区 福建医科大学药学院 福建省天然药物药理学重点实验室
出处 《中国药学杂志》 CAS CSCD 北大核心 2016年第4期253-258,共6页 Chinese Pharmaceutical Journal
基金 国家自然科学基金资助项目(81202561 81173096)
关键词 PI3K-Akt-mTOR信号通路 PI3K-Akt-mTOR信号通路抑制剂 耐药机制 PI3K-Akt-mTOR signaling pathway PI3K-Akt-mTOR signaling pathway inhibitor resistant mechanism
分类号 R965 [医药卫生—药理学]
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参考文献65

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二级参考文献99

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共引文献10

同被引文献26

引证文献3

二级引证文献28

中国药学杂志
2016年 第4期

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