组蛋白伴侣FACT复合物抑制剂CBL0137-卵巢癌治疗新方向  

Histone chaperone FACT complex inhibitor CBL0137-A new direction for ovarian cancer treatment

作　　者：蒋郁竹 夏百荣[1] 娄阁[1] Jiang Yuzhu;Xia Bairong;Lou Ge(Harbin Medical University Cancer Hospital,Heilongjiang Harbin 150081,China)

机构地区：[1]哈尔滨医科大学附属肿瘤医院,黑龙江哈尔滨150081

出　　处：《现代肿瘤医学》2020年第13期2351-2354,共4页Journal of Modern Oncology

基　　金：国家自然科学基金项目(编号:81872507,81872430)。

摘　　要：卵巢癌作为三大妇科恶性肿瘤之一,即使研究了很多治疗方法,其生存率也并不理想。虽然大部分患者可以在标准治疗中得到缓解,但最终都会出现复发和耐药。对于复发性卵巢癌患者来说,关键目标在于寻找更加前沿的治疗策略,以提高治愈率。CBL0137作为组蛋白伴侣分子FACT复合物的小分子抑制剂,可以直接调控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,并且在胰腺癌、肾癌、小细胞肺癌和神经胶质细胞瘤中证实了其抗肿瘤作用。本篇综述,总结了目前卵巢癌药物治疗方法,阐述了CBL0137在多种癌症中表现出的抗肿瘤活性以及过程中涉及的多个靶点的抗肿瘤机制,总结了在卵巢癌中相应靶点的表达情况及最新研究进展。最后对CBL0137在卵巢癌治疗中的潜力进行了总结和展望。Ovarian cancer is one of the three major gynecological malignancies.Even if many treatments are studied,the survival rate is not ideal.Although most patients can be relieved in standard treatment,there will eventually be recurrence and resistance.For patients with recurrent ovarian cancer,the key goal is to find more advanced treatment strategies to improve the cure rate.As a small molecule inhibitor of the histone chaperone FACT complex,CBL0137 can directly regulate FACT-promoting transcriptional activity,down-regulate NF-κB,activate p53,thereby inhibiting tumor growth,and its anti-tumor effect has been confirmed in pancreatic cancer,renal cancer,and small cells lung cancer and glioma.This review summarizes current drug treatments for ovarian cancer,describes the anti-tumor activity exhibited by CBL0137 in various cancers,and the anti-tumor mechanisms of multiple targets involved in the process,summarizes the status of the presentation and the latest research progress of corresponding targets in ovarian cancer.Finally,the potential of CBL0137 in the treatment of ovarian cancer was summarized and prospected.

关 键 词：CBL0137 FACT P53 NOTCH HSF-1 卵巢癌 化疗药物 

分 类 号：R737.31[医药卫生—肿瘤]