Division of Molecular Endocrinology, Department of Molecular Oncology, King Faisal Specialist Hospital and Research Centre, PO Box 3354, Research Center (MBC 03), Riyadh, 11211, Saudi Arabia.
Semin Cancer Biol. 2019 Dec;59:125-132. doi: 10.1016/j.semcancer.2019.07.009. Epub 2019 Jul 16.
Phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway is one of the major cellular signaling pathways that plays an important role in basic intracellular functions. The PI3K/Akt/mTOR pathway regulates cell proliferation, growth, cell size, metabolism, and motility. Component genes of this pathway have been extensively studied and found to be commonly activated in human cancer. Inhibition of this pathway has been shown to lead to regression of human tumors and has been studied in preclinical setup and evaluated in many clinical trials at various levels. Some inhibitors of this pathway are approved by the Food and Drug Administration after their potency and safety have been shown in clinical trials. This review discusses the recent trends in exploiting the PI3K/Akt/mTOR pathway towards the molecular targeted therapy using small molecule inhibitors in human cancer.
磷脂酰肌醇 3-激酶（PI3K）/Akt/哺乳动物雷帕霉素靶蛋白（mTOR）信号通路是主要的细胞信号通路之一，在基本的细胞内功能中发挥着重要作用。PI3K/Akt/mTOR 通路调节细胞增殖、生长、细胞大小、代谢和运动。该通路的组成基因已被广泛研究，并且在人类癌症中普遍被发现被激活。抑制该通路已被证明可导致人类肿瘤消退，并已在临床前研究中进行研究，并在多个层面的临床试验中进行了评估。一些该通路的抑制剂在临床试验中显示出其效力和安全性后已被美国食品和药物管理局批准。本综述讨论了利用小分子抑制剂在人类癌症中针对 PI3K/Akt/mTOR 通路进行分子靶向治疗的最新趋势。
