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Updated: Aug 19, 2025

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Published on: July 25, 2020
Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents
Maria Antonietta Occhiuzzi1, Gernando Lico1, Giuseppina Ioele1
1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy.
Abstract:
The biochemical role of the PI3K/PKB/mTOR signalling pathway in cell-cycle regulation is now well known. During the onset and development of different forms of cancer it becomes overactive reducing apoptosis and allowing cell proliferation. Therefore, this pathway has become an important target for the treatment of various forms of malignant tumors, including breast cancer and follicular lymphoma. Recently, several more or less selective inhibitors targeting these proteins have been identified. In general, drugs that act on multiple targets within the entire pathway are more efficient than single targeting inhibitors. Multiple inhibitors exhibit high potency and limited drug resistance, resulting in promising anticancer agents. In this context, the present survey focuses on small molecule drugs capable of modulating the PI3K/PKB/mTOR signalling pathway, thus representing drugs or drug candidates to be used in the pharmacological treatment of different forms of cancer.
Insights
The PI3K/PKB/mTOR pathway drives cancer by promoting cell proliferation. Inhibitors targeting this pathway, especially multi-target drugs, show promise for effective cancer treatment with limited resistance.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- The PI3K/PKB/mTOR signaling pathway is crucial for cell-cycle regulation.
- Overactivation of this pathway contributes to cancer development by inhibiting apoptosis and promoting cell proliferation.
- This pathway is a key therapeutic target for various cancers, including breast cancer and follicular lymphoma.
Purpose of the Study:
- To review small molecule drugs targeting the PI3K/PKB/mTOR signaling pathway.
- To highlight the potential of these drugs as anticancer agents.
Main Methods:
- Literature review of small molecule inhibitors targeting the PI3K/PKB/mTOR pathway.
- Analysis of drug efficacy and resistance profiles.
Main Results:
- Several selective and non-selective inhibitors targeting the PI3K/PKB/mTOR pathway have been identified.
- Multi-target inhibitors demonstrate greater efficiency, potency, and reduced drug resistance compared to single-target inhibitors.
- These inhibitors represent promising drug candidates for cancer treatment.
Conclusions:
- Small molecule drugs modulating the PI3K/PKB/mTOR pathway are valuable in cancer therapy.
- Targeting this pathway offers a promising strategy for developing novel anticancer agents.
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