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.
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)
出处
《山东化工》
CAS
2024年第15期146-149,152,共5页
Shandong Chemical Industry
关键词
LSD1
HDAC
双靶点
抑制剂
lysine-specific demethylase 1(LSD1)
histone deacetylase(HDAC)
dual-target
inhibitors
