The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor

被引：14

作者：

Zhang, Qiangsheng ^{[1
]}

Hu, Xi ^{[1
]}

Li, Lu ^{[2
]}

Zhang, Lidan ^{[1
]}

Wan, Guoquan ^{[1
]}

Feng, Qiang ^{[3
]}

Zhu, Yongxia ^{[4
]}

Wang, Ningyu ^{[5
]}

Liu, Zhihao ^{[1
]}

Yu, Luoting ^{[1
]}

机构：

[1] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, West China Med Sch,Collaborat Innovat Ctr Biother, Chengdu 610041, Sichuan, Peoples R China

[2] Sichuan Univ, West China Hosp, Inst Clin Trials, Chengdu 610041, Sichuan, Peoples R China

[3] Chengdu Normal Univ, Coll Chem & Life Sci, Chengdu 611130, Peoples R China

[4] Univ Elect Sci & Technol China, Sichuan Canc Hosp & Inst, Sichuan Canc Ctr, Sch Med,Dept Clin Pharm, Chengdu 610041, Peoples R China

[5] Southwest JiaoTong Univ, Sch Life Sci & Engn, Chengdu 611756, Sichuan, Peoples R China

来源：

CHEMICAL COMMUNICATIONS | 2021年 / 57卷 / 24期

基金：

中国国家自然科学基金;

关键词：

D O I：

10.1039/d0cc04670a

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

By targeting the unique Cys663 of EZH2, SKLB-0335 displays high paralog-selectivity on EZH2. Biochemical studies show that SKLB-0335 can covalently bind to EZH2 at its S-adenosylmethionine (SAM) pocket and inhibit H3K27Me3. SKLB-0335 could be an effective chemical probe with which to further investigate the specific biological functions of EZH2.

引用

页码：3006 / 3009

页数：4

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