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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?
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摘要 恶性胶质瘤(MG),尤其是多形性胶质母细胞瘤(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-κB,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。 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 recurrence 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.
作者 金明珠 徐煜 金卫林 JIN Ming-Zhu;XU Yu;JIN Wei-Lin(Shanghai Jiao Tong University School of Medicine,Shanghai 200025,China;Institute of Nano Biomedicine and Engineering,Shanghai Engineering Center for Intelligent Diagnosis and Treatment Instrument,School of Electronic Information and Electronic Engineering,Shanghai Jiao Tong University,Shanghai 200240,China)
出处 《转化医学电子杂志》 2018年第5期8-11,共4页 E-Journal of Translational Medicine
基金 上海交通大学医工交叉项目(YG2015MS20)
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 CBL0137 glioblastoma muhiforme chemotherapeutic agent facilitates chromatin transcription complex temozolomide
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