Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment

被引:53
|
作者
Wu, Xianbo [1 ]
Xu, Yihua [2 ]
Liang, Qi [3 ]
Yang, Xinwei [1 ]
Huang, Jianli [4 ]
Wang, Jie [4 ]
Zhang, Hong [5 ]
Shi, Jianyou [6 ]
机构
[1] Chengdu Sport Univ, Sch Sports Med & Hlth, Chengdu, Peoples R China
[2] Chengdu Univ Tradit Chinese Med, Sch Basic Med Sci, Chengdu, Peoples R China
[3] Southwest Jiaotong Univ, Coll Med, Chengdu, Peoples R China
[4] Guizhou Univ Tradit Chinese Med, Clin Coll Med 1, Guiyang, Peoples R China
[5] Hosp Chengdu Univ Tradit Chinese Med, Chengdu, Peoples R China
[6] Univ Elect Sci & Technol China, Sichuan Acad Med Sci & Sichuan Prov Peoples Hosp, Sch Med, Personalized Drug Therapy Key Lab Sichuan Prov, Chengdu, Peoples R China
基金
中国国家自然科学基金;
关键词
PI3K; mTOR; dual inhibitor; tumour; PI3K-Akt-mTOR pathway; cancer treament; SAR; PHOSPHATIDYLINOSITOL 3-KINASE/MAMMALIAN TARGET; ISOFORM-SPECIFIC INHIBITION; I PI3 KINASE; MAMMALIAN TARGET; HIGHLY POTENT; BIOLOGICAL EVALUATION; ANTITUMOR EFFICACY; XL765; SAR245409; MTOR INHIBITION; BRAIN-PENETRANT;
D O I
10.3389/fphar.2022.875372
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The PI3K-Akt-mTOR pathway is a viable target for cancer treatment and can be used to treat various malignant tumours, including follicular lymphoma and breast cancer. Both enzymes, PI3K and mTOR, are critical in this pathway. Hence, in recent years, an array of inhibitors targeting these two targets have been studied, showing dual PI3K/mTOR inhibition compared with single targeting small molecule inhibitors. Inhibitors not only inhibit cell proliferation but also promote cell apoptosis. These inhibitors show high potency and little drug resistance even at low doses, suggesting that PI3K/mTOR inhibitors are promising cancer drugs. Herein, we summarised the recent research of PI3K/mTOR dual inhibitors-for example, structure-activity relationship, pharmacokinetics, and clinical practice, and briefly commented on them.
引用
收藏
页数:17
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