4.7 Review

Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment

Journal

FRONTIERS IN PHARMACOLOGY
Volume 13, Issue -, Pages -

Publisher

FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2022.875372

Keywords

PI3K; mTOR; dual inhibitor; tumour; PI3K-Akt-mTOR pathway; cancer treament; SAR

Funding

  1. National Natural Science Foundation of China [82073311]
  2. Key Research and Development Projects in Chengdu [2020-YF05-00058-SN]
  3. Key Research and Development Projects in Sichuan Province [2020YFS0399, 2019YFS0514]
  4. Clinical Research and Transformation Foundation of Sichuan Provincial People's Hospital [2021LZ03]
  5. Key Laboratory of Sports Medicine of Sichuan Province, Institute of Sports Medicine and Health, Chengdu Sport University [2022-A017]

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Studies have shown that PI3K/mTOR inhibitors are effective in cancer treatment, as they can inhibit cell proliferation and promote apoptosis. These inhibitors exhibit high potency and low drug resistance, indicating they have great potential as anticancer drugs.
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.

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