雷帕霉素耐药机制及其逆转途径

Resistant mechanism about rapamycin and solution

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.

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, hut it prone todrug 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.