首页|LSD1、HDAC及其双靶点抑制剂在抗肿瘤应用中的研究进展

LSD1、HDAC及其双靶点抑制剂在抗肿瘤应用中的研究进展

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

lysine-specific demethylase 1(LSD1)histone deacetylase(HDAC)dual-targetinhibitors

延秋铭、叶理、陈念、查晓明

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中国药科大学工学院,江苏南京 211198

LSD1 HDAC 双靶点 抑制剂

2024

山东化工
山东省化工研究院 山东省化工信息中心

山东化工

影响因子:0.249
ISSN:1008-021X
年,卷(期):2024.53(15)