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

页码：1561 / 1582

页数：22

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