Zhang Liqiu, Zhao Hengyu, Cui Zhongqi, Lv Yueshan, Zhang Wenjia, Ma Xiaoyu, Zhang Jianan, Sun Banghao, Zhou Danyang, Yuan Lijie
Teaching Experiment Center of Biotechnology, Harbin Medical University, Harbin, P.R. China.
Daqing Oilfield General Hospital, Daqing, P.R. China.
Oncotarget. 2017 May 9;8(19):31119-31132. doi: 10.18632/oncotarget.16094.
Glioblastoma (GBM) is associated with poor prognosis due to its resistance to surgery, irradiation, and conventional chemotherapy. Thus, efficient therapeutic approaches for the treatment of GBM are urgently needed. HSP70 is an antiapoptotic protein that participates in the inhibition of both mitochondrial and membrane receptor apoptosis pathways and is highly expressed in glioma tissues. Here, we investigated a derivative of apoptin; specifically, a chicken anemia viral protein with selective toxicity toward cancer cells that can inhibit hyperactive molecules, including HSP70. Our earlier studies demonstrated that apoptin directly binds to the promoter of HSP70 and inhibits HSP70 transcription, which contributes to HSP70 downregulation. This study provides the first demonstration of the therapeutic potential of an apoptin-derived peptide for the treatment of GBM by identifying the minimal region of the apoptin domain required for interaction with the heat-shock element (HSE). This apoptin-derived peptide (ADP) inhibits glioma cell proliferation and tumor growth as well as exhibits an increased ability to promote apoptosis in GBM cells compared with rapamycin and temozolomide. ADP treatment inhibited xenograft tumor growth and increased the overall health and survival of nude mice implanted with GBM cells. These effects were measured in tumors obtained from cell lines and were observed in both intracranial and subcutaneous xenografts. In conclusion, we provide the first demonstration that ADP has therapeutic potential for the treatment of human GBM. Specifically, this study suggests that ADP is a potent candidate for drug development based on its favorable toxicity and pharmacokinetic profiles as well as its time- and cost-saving benefits.
胶质母细胞瘤(GBM)因其对手术、放疗和传统化疗具有抗性,故而预后较差。因此,迫切需要有效的治疗方法来治疗GBM。热休克蛋白70(HSP70)是一种抗凋亡蛋白,参与抑制线粒体和膜受体凋亡途径,且在胶质瘤组织中高表达。在此,我们研究了凋亡素的一种衍生物;具体而言,是一种对癌细胞具有选择性毒性的鸡贫血病毒蛋白,它能够抑制包括HSP70在内的过度活跃分子。我们早期的研究表明,凋亡素直接与HSP70的启动子结合并抑制HSP70转录,这有助于HSP70的下调。本研究通过确定凋亡素结构域与热休克元件(HSE)相互作用所需的最小区域,首次证明了一种凋亡素衍生肽治疗GBM的潜在治疗价值。与雷帕霉素和替莫唑胺相比,这种凋亡素衍生肽(ADP)可抑制胶质瘤细胞增殖和肿瘤生长,并且在GBM细胞中表现出更强的促进凋亡的能力。ADP治疗可抑制异种移植瘤生长,并提高接种GBM细胞的裸鼠的整体健康状况和存活率。这些效应在从细胞系获得的肿瘤中得到测量,并且在颅内和皮下异种移植瘤中均观察到。总之,我们首次证明ADP对治疗人类GBM具有潜在治疗价值。具体而言,本研究表明,基于其良好的毒性和药代动力学特征以及节省时间和成本的优势,ADP是药物开发的有力候选者。