LSD1、HDAC及其双靶点抑制剂在抗肿瘤应用中的研究进展  

Research Progress of LSD1,HDAC and Their Dual-target Inhibitors in Anti-tumor Applications

作　　者：延秋铭 叶理 陈念 查晓明 Yan Qiuming;Ye Li;Chen Nian;Zha Xiaoming(School of Engineering,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学工学院,江苏南京211198

出　　处：《山东化工》2024年第15期146-149,152,共5页Shandong Chemical Industry

摘　　要：表观遗传学调控因其可逆性及在疾病进程中的关键作用,已成为肿瘤治疗的重要靶点。组蛋白赖氨酸特异性去甲基化酶(LSD1)与组蛋白去乙酰化酶(HDAC)是调控癌细胞基因表达的重要靶点,抑制这两种蛋白可以显示出显著的肿瘤治疗效果。本综述聚焦于LSD1和HDAC的单靶点及双靶点抑制剂的研究进展,探讨了这些抑制剂在抗肿瘤治疗中的应用。双靶点抑制剂通过同时抑制LSD1和HDAC活性,提供了超越单一抑制剂的抗癌效果,展示了改善治疗效果的潜力。文章细致回顾了这些抑制剂在临床前研究和临床试验中的表现,指出其优势与挑战,并对未来研究方向进行了展望。Epigenetic regulation has become a promising therapeutic target due to its reversibility and crucial role in disease progression.Particularly,lysine-specific demethylase 1(LSD1)and histone deacetylases(HDAC)play vital roles in the gene regulation of cancer cells.This review discusses the research progress on single-target inhibitors for LSD1 and HDAC,as well as their dual-target inhibitors.Dual-target inhibitors,by simultaneously inhibiting the activity of both LSD1 and HDAC,provide stronger antitumor effects than single-target inhibitors and hold potential to improve treatment outcomes for patients.This review explores in detail the application of these three types of inhibitors in preclinical and clinical trials.

关 键 词：LSD1 HDAC 双靶点 抑制剂 

分 类 号：TQ464.8[化学工程—制药化工] R914[医药卫生—药物化学]