金明珠,徐煜,金卫林.组蛋白伴侣FACT复合物抑制剂CBL0137——恶性胶质瘤治疗新药物?[J].,2018,5(5):8-11.
组蛋白伴侣FACT复合物抑制剂CBL0137——恶性胶质瘤治疗新药物?
CBL0137 targeting histone chaperone FACT complex: a new chemotherapeutic agent for glioblastoma multiforme?
投稿时间:2018-04-22  最后修改时间:2018-04-26
DOI:10.12095/j.issn.2095-6894.2018.05.002
中文关键词:  CBL0137,恶性胶质瘤,化疗药物,FACT促染色质转录复合物,替莫唑胺
英文关键词:CBL0137; glioblastoma multiforme; chemotherapeutic agent; facilitates chromatin transcription complex; temozolomide
基金项目:上海交通大学医工交叉项目(YG2015MS20)
作者单位E-mail
金明珠 上海交通大学医学院 mingzhujin@sjtu.edu.cn 
徐煜 上海交通大学医学院  
金卫林 上海交通大学电子信息与电气工程学院 weilinjin@sjtu.edu.cn 
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中文摘要:
      【】恶性胶质瘤 (malignant gliomas, MG),尤其是多形性胶质母细胞瘤 (glioblastoma multiforme, GBM)是临床上最常见的致命中枢神经系统肿瘤,手术联合放化疗的综合治疗方案是其治疗的主要手段。然而,手术无法完全切除肿瘤病灶及一线化疗药物替莫唑胺耐药导致其治疗效果欠佳,且肿瘤极易复发。CBL0137作为组蛋白伴侣分子FACT复合物的小分子抑制剂,能透过血脑屏障,直接调控FACT促染色质转录活性,下调NF-?B,激活p53,从而抑制了肿瘤的生长。进一步临床试验的开展将推进CBL0137成为恶性胶质瘤治疗新药物。
英文摘要:
      【Abstract】Glioblastoma multiforme (GBM) is one of the most common primary central nervous system cancers. Surgery combined with   radiotherapy and chemotherapy is the main strategy for its treatment. However, the impossibility of complete removal of tumor lesions by   surgery and the drug resistance of the first?line chemotherapeutic agent temozolomide lead to the poor therapeutic effect, and tumor recur?   rence of GBM. CBL0137 can cross the blood?brain barrier, and inhibit the function of facilitates chromatin transcription (FACT) in   promoting the formation of chromatin transcription complexes, thus activate p53 and downregulate NF?κB in GBM. CBL0137 might bring   about a new opportunity for the treatment of GBM once tested by multiple clinical trials.
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