mTOR抑制剂抗动脉粥样硬化的研究进展

雷帕霉素靶蛋白(m TOR)是哺乳动物细胞中的Ser/Thr激酶,存在m TORC1和m TORC2两种复合体,调控细胞增殖、迁移及血管生成。大环内酯类免疫抑制剂雷帕霉素(RAPA)及其衍生物(rapalogs)可抑制m TORC1的功能,减缓动脉粥样硬化(AS)的发生发展。然而长期应用rapalogs会导致m TORC1抵抗及m TORC2抑制,产生血脂异常等。临床上采取联合用药、间歇性给药或低剂量给药等措施应对。

Research progress of mTOR inhibitors for anti-atherosclerosis

Mammalian target of rapamycin ( mTOR) is a kind of Ser/Thr kinase existing in mammalian cells can regulate cell proliferation, migration and angiogenesis.mTOR including two different complex forms as mTORC1 and mTORC2 .Rapamycin and rapalogs were soon found to have powerful immunosuppressant prop-erties and thus be valuable for preventing the progress of the artery atheromatous by inhibiting the function of mTORC1.But long-term rapalogs administration may increase the side actions such as mTORC1 resistance, mTORC2 inhibition, dyslipidemia.The clinical application of drug combination and dosage optimization may reduce adverse events.