Dual-target EZH2 inhibitor: latest advances in medicinal chemistry

被引：3
作者：
Wei, Lai [1 ,2 ,3 ]
Mei, Dan [1 ,2 ,3 ]
Hu, Sijia [1 ,2 ,3 ]
Du, Shufang [1 ,2 ,3 ]
机构：
[1] Sichuan Univ, West China Hosp, State Key Lab Oral Dis, Stomatol Dept Orthodont, Chengdu 610041, Sichuan, Peoples R China
[2] Sichuan Univ, Natl Ctr Stomatol, Chengdu 610041, Sichuan, Peoples R China
[3] Sichuan Univ, Natl Clin Res Ctr Oral Dis, Chengdu 610041, Sichuan, Peoples R China
来源：
FUTURE MEDICINAL CHEMISTRY | 2024年 / 16卷 / 15期
关键词：
AR; BMI1; DNMTs; drug design; EHMT2 (G9a); EZH2; inhibitors; structure-activity relationship; SMALL-MOLECULE INHIBITOR; GROUP PROTEIN EZH2; HOMOLOG; EZH2; ANDROGEN RECEPTOR; STEM-CELLS; SELECTIVE-INHIBITION; CANCER-CELLS; POLYCOMB; METHYLATION; COMPLEX;
D O I：
10.1080/17568919.2024.2380243
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, plays a crucial role in tumor progression by regulating gene expression. EZH2 inhibitors have emerged as promising anti-tumor agents due to their potential in cancer treatment strategies. However, single-target inhibitors often face limitations such as drug resistance and side effects. Dual-target inhibitors, exemplified by EZH1/2 inhibitor HH-2853(28), offer enhanced efficacy and reduced adverse effects. This review highlights recent advancements in dual inhibitors targeting EZH2 and other proteins like BRD4, PARP1, and EHMT2, emphasizing rational design, structure-activity relationships, and safety profiles, suggesting their potential in clinical applications.
引用
收藏
页码：1561 / 1582
页数：22
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