Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents

被引:50
作者
Occhiuzzi, Maria Antonietta [1 ]
Lico, Gernando [1 ]
Ioele, Giuseppina [1 ]
De Luca, Michele [1 ]
Garofalo, Antonio [1 ]
Grande, Fedora [1 ]
机构
[1] Univ Calabria, Dept Pharm Hlth & Nutr Sci, Arcavacata Di Rende, Italy
关键词
Protein kinases; Rapamycin; Dual inhibitors; Cancer therapy; DUAL PI3K/MTOR INHIBITOR; PHOSPHATIDYLINOSITOL 3-KINASE/MAMMALIAN TARGET; P70; S6; KINASE; PHOSPHOINOSITIDE; 3-KINASE; AKT INHIBITOR; IN-VITRO; SELECTIVE INHIBITOR; HIGHLY POTENT; PRECLINICAL EVALUATION; ANTITUMOR-ACTIVITY;
D O I
10.1016/j.ejmech.2022.114971
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 repre-senting drugs or drug candidates to be used in the pharmacological treatment of different forms of cancer.
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页数:28
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