雷帕霉素及其衍生物的抗肿瘤活性研究进展

哺乳动物雷帕霉素靶蛋白(the mammalian target of rapamycin,mTOR)在癌症代谢、生长、增殖、细胞周期等过程中起关键作用。由于mTOR信号通路在细胞周期进程中发挥了重要作用,而细胞周期进程调节异常与许多疾病尤其是癌症的发生、发展有关,因此mTOR信号通路的失调可引起多种癌症。mTOR的特异性抑制剂雷帕霉素及其衍生物能抑制mTOR的功能,使细胞阻滞在G1期,并引起凋亡。对雷帕霉素及其衍生物的抗肿瘤活性及所涉及的信号通路在抗肿瘤中的机制作一综述。

Progress of rapamycin and its derivatives in anti-tumor activity

The mammalian target of rapamycin(mTOR)plays a key role in cancer metabolism,growth,proliferation and cell cycle.Due to the important role of mTOR signaling pathway in cell cycle progression and cell cycle progression regulation abnormality associated with many diseases,especially the initial and development of cancer,hence,the disregulated mTOR signaling pathway can cause a variety of cancers.The function of mTOR can be inhibited by the mTOR specific inhibitor rapamycin and its derivatives,then the cells w...