Alexandru Oana, Horescu Cristina, Sevastre Ani-Simona, Cioc Catalina Elena, Baloi Carina, Oprita Alexandru, Dricu Anica
Department of Neurology, University of Medicine and Pharmacy of Craiova and Clinical Hospital of Neuropsychiatry Craiova, Craiova, Romania.
Unit of Biochemistry, University of Medicine and Pharmacy of Craiova, Craiova, Romania.
Contemp Oncol (Pozn). 2020;24(1):55-66. doi: 10.5114/wo.2020.94726. Epub 2020 Mar 30.
From all central nervous system tumors, gliomas are the most common. Nowadays, researchers are looking for more efficient treatments for these tumors, as well as ways for early diagnosis. Receptor tyrosine kinases (RTKs) are major targets for oncology and the development of small-molecule RTK inhibitors has been proven successful in cancer treatment. Mutations or aberrant activation of the RTKs and their intracellular signaling pathways are linked to several malignant diseases, including glioblastoma. The progress in the understanding of malignant glioma evolution has led to RTK targeted therapies with high capacity to improve the therapeutic response while reducing toxicity. In this review, we present the most important RTKs (i.e. EGFR, IGFR, PDGFR and VEGFR) currently used for developing cancer therapeutics together with the potential of RTK-related drugs in glioblastoma treatment. Also, we focus on some therapeutic agents that are currently at different stages of research or even in clinical phases and proved to be suitable as re-purposing candidates for glioblastoma treatment.
在所有中枢神经系统肿瘤中，胶质瘤最为常见。如今，研究人员正在寻找针对这些肿瘤更有效的治疗方法以及早期诊断方法。受体酪氨酸激酶（RTK）是肿瘤学的主要靶点，小分子RTK抑制剂的研发已在癌症治疗中被证明是成功的。RTK及其细胞内信号通路的突变或异常激活与包括胶质母细胞瘤在内的多种恶性疾病有关。对恶性胶质瘤演变的认识进展已带来了RTK靶向治疗，其具有在降低毒性的同时提高治疗反应的高能力。在本综述中，我们介绍了目前用于开发癌症治疗药物的最重要的RTK（即表皮生长因子受体、胰岛素样生长因子受体、血小板衍生生长因子受体和血管内皮生长因子受体）以及RTK相关药物在胶质母细胞瘤治疗中的潜力。此外，我们关注一些目前处于不同研究阶段甚至临床阶段且被证明适合作为胶质母细胞瘤治疗重新利用候选药物的治疗剂。
