国际肿瘤学杂志

国际肿瘤学杂志 ›› 2014, Vol. 41 ›› Issue (10): 740-743.doi: １０．３７６０／ｃｍａ．ｊ．ｉｓｓｎ．１６７３４２２Ｘ．２０１４．１０．００７

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雷帕霉素耐药机制及其逆转途径

 陈柯君, 吕书晴   

  1. ２００４３３上海，第二军医大学附属长海医院血液科
  • 出版日期:2014-10-29 发布日期:2014-10-11
  • 通讯作者: 吕书晴，Ｅｍａｉｌ：ｌｓｑ７２１９＠ｓｏｈｕ．ｃｏｍ E-mail:ｌｓｑ７２１９＠ｓｏｈｕ．ｃｏｍ
  • 基金资助:

    国家自然科学基金（３０８７３０４２、８１１００３６１）

Resistant mechanism about rapamycin and solution

 CHEN  Ke-Jun, LYU Shu-Qing   

  1. Department of Hematology, Changhai Hospital, Second Military Medical University, Shanghai 200433, China
  • Online:2014-10-29 Published:2014-10-11
  • Contact: Lyu Shuqing E-mail:ｌｓｑ７２１９＠ｓｏｈｕ．ｃｏｍ

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摘要： 雷帕霉素靶蛋白（ｍＴＯＲ）信号通路与肿瘤细胞的增殖、周期调控等多种病理过程密切相 关。雷帕霉素通过抑制 ｍＴＯＲ起到抗肿瘤作用，但其容易产生耐药等缺点导致临床应用受限，耐药机制 主要与 ｍＴＯＲ受抑后负反馈激活磷脂酰肌醇３激酶蛋白激酶 Ｂ（ＰＩ３ＫＡｋｔ）有关。ｍＴＯＲ通路相关蛋白 的双重抑制剂等药物有望逆转其耐药。

关键词: 西罗莫司, 抗药性, 雷帕霉素靶蛋白

Abstract: mTOR signaling pathway is closely related to cell proliferation, cell cycle and other pathological processes about tumor. Rapamycin plays an antitumor     effect through inhibiting mTOR, but it prone to drug resistance, which leads to limited clinical application. Its resistant mechanism is related with the activation of PI3KAkt, which is regulated with negative feedback. Dual inhibitors of related proteins of mTOR pathway  are expected to reverse the drug resistance.

Key words:

margin-bottom: 0pt, text-indent: 23.52pt, text-align: justify">font-family: '宋体', mso-spacerun: 'yes'">Sirolimus, Drug resistance, mammalian target of rapamycin