基于PI3K/Akt/mTOR信号通路的自噬调节剂研究进展  

Research progress of autophagy modulators targeting PI3K/Akt/mTOR signaling pathway

作　　者：邹春阳 陈晨 王凤秋 阮馨慧[1,2] 吕洁 ZOU Chun-yang;CHEN Chen;WANG Feng-qiu;RUAN Xin-hui;LÜJie(Department of Pharmacy,Liaoning Vocational College of Medicine,Shenyang 110101,China;Liaoning Institute of Basic Medicine,Shenyang 110101,China)

机构地区：[1]辽宁医药职业学院药学系,辽宁沈阳110101 [2]辽宁省基础医学研究所,辽宁沈阳110101

出　　处：《中国药物化学杂志》2021年第10期825-833,共9页Chinese Journal of Medicinal Chemistry

摘　　要：细胞自噬与多种疾病的发生密切相关。在神经退行性疾病、代谢性疾病、遗传性肝脏疾病、心脏疾病及肿瘤等疾病中均出现异常自噬。通过小分子药物调节相关疾病中的自噬功能,有可能成为疾病治疗的新策略。目前研究阐明,PI3K/Akt/mTOR信号通路与自噬的发生关系密切,小分子药物通过干扰该通路中相关激酶来调控细胞自噬。本文针对PI3K/Akt/mTOR信号通路中可以调控自噬发生的泛PI3K抑制剂、PI3K/mTOR双重抑制剂、泛mTOR抑制剂、mTOR1抑制剂及Akt抑制剂进行了全面综述,以期为自噬调控剂的开发提供一定的借鉴。Autophagy is closely related to a great deal of diseases.Abnormal autophagy commonly occurred in various diseases,such as neurodegenerative disease,metabolic disease,genetic liver disease,cardiac disease and cancer.It may become new treatment strategy for above-mentioned diseases that small molecules adjust the function of autophagy to normal level.At present,the relationship between the autophagy and PI3 K/Akt/mTOR signaling pathway has been elucidated.The related kinase inhibitors against this pathway really displayed the regulation ability on autophagy.This paper comprehensively reviewed the recent research on autophagy modulators,including pan-PI3 K inhibitors,dual PI3 K/mTOR inhibitors,pan-mTOR inhibitors,mTOR1 inhibitors and AKT inhibitors and so on.■.

关 键 词：自噬 PI3K/Akt/mTOR信号通路 泛PI3K抑制剂 PI3K/mTOR双重抑制剂 mTOR1抑制剂 

分 类 号：R914[医药卫生—药物化学]