School of Bioengineering and Biosciences, Lovely Professional University, Jalandhar (144411), Punjab, India.
Department of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, NC 27599, USA.
Mini Rev Med Chem. 2024;24(16):1496-1520. doi: 10.2174/0113895575270904231129062137.
Sarcoma is a heterogeneous group of malignancies often resistant to conventional chemotherapy and radiation therapy. The phosphatidylinositol-3-kinase/ protein kinase B /mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway has emerged as a critical cancer target due to its central role in regulating key cellular processes such as cell growth, proliferation, survival, and metabolism. Dysregulation of this pathway has been implicated in the development and progression of bone sarcomas (BS) and soft tissue sarcomas (STS). PI3K/Akt/mTOR inhibitors have shown promising preclinical and clinical activity in various cancers. These agents can inhibit the activation of PI3K, Akt, and mTOR, thereby reducing the downstream signaling events that promote tumor growth and survival. In addition, PI3K/Akt/mTOR inhibitors have been shown to enhance the efficacy of other anticancer therapies, such as chemotherapy and radiation therapy. The different types of PI3K/Akt/mTOR inhibitors vary in their specificity, potency, and side effect profiles and may be effective depending on the specific sarcoma type and stage. The molecular targeting of PI3K/Akt/mToR pathway using drugs, phytochemicals, nanomaterials (NMs), and microbe-derived molecules as Pan-PI3K inhibitors, selective PI3K inhibitors, and dual PI3K/mTOR inhibitors have been delineated. While there are still challenges to be addressed, the preclinical and clinical evidence suggests that these inhibitors may significantly improve patient outcomes. Further research is needed to understand the potential of these inhibitors as sarcoma therapeutics and to continue developing more selective and effective agents to meet the clinical needs of sarcoma patients.
肉瘤是一组异质性恶性肿瘤,通常对常规化疗和放疗具有耐药性。磷脂酰肌醇-3-激酶/蛋白激酶 B/哺乳动物雷帕霉素靶蛋白(PI3K/Akt/mTOR)信号通路已成为一个关键的癌症靶点,因为它在调节细胞生长、增殖、存活和代谢等关键细胞过程中起着核心作用。该通路的失调与骨肉瘤(BS)和软组织肉瘤(STS)的发生和发展有关。PI3K/Akt/mTOR 抑制剂在各种癌症的临床前和临床研究中显示出了良好的疗效。这些药物可以抑制 PI3K、Akt 和 mTOR 的激活,从而减少促进肿瘤生长和存活的下游信号事件。此外,PI3K/Akt/mTOR 抑制剂已被证明可以增强其他抗癌疗法的疗效,如化疗和放疗。不同类型的 PI3K/Akt/mTOR 抑制剂在特异性、效力和副作用谱方面存在差异,并且可能根据特定的肉瘤类型和分期有效。已经确定了使用药物、植物化学物质、纳米材料(NMs)和微生物衍生分子作为 Pan-PI3K 抑制剂、选择性 PI3K 抑制剂和双重 PI3K/mTOR 抑制剂对 PI3K/Akt/mToR 通路进行分子靶向。尽管仍然存在需要解决的挑战,但临床前和临床证据表明,这些抑制剂可能显著改善患者的预后。需要进一步研究以了解这些抑制剂作为肉瘤治疗药物的潜力,并继续开发更具选择性和有效的药物来满足肉瘤患者的临床需求。