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Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment

Xianbo Wu, Yihua Xu, Qi Liang, Xinwei Yang, Jianli Huang, Jie Wang, Hong Zhang, Jianyou Shi

2022Frontiers in Pharmacology127 citationsDOIOpen Access PDF

Abstract

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. Clinical Trial Registration: https://clinicaltrials.gov .

Topics & Concepts

PI3K/AKT/mTOR pathwayDiscovery and development of mTOR inhibitorsMedicineCancer researchPharmacologyCancerTemsirolimusEverolimusProtein kinase BApoptosisChemistryOncologyInternal medicineBiochemistryPI3K/AKT/mTOR signaling in cancerCancer Mechanisms and TherapyChronic Lymphocytic Leukemia Research