机构：[1]State Key Laboratory of Biotherapy/Collaborative Innovation Center forBiotherapy, West China Hospital, West China Medical School,Sichuan University, Chengdu, Sichuan 610041, P. R. China.四川大学华西医院[2]Institute of Clinical Trials, West China Hospital, Sichuan University,Chengdu, Sichuan, 610041, P. R. China四川大学华西医院[3]College of Chemistry and Life Science, Chengdu Normal University,Chengdu 611130, P. R. China[4]Department of Clinical Pharmacy, Sichuan Cancer Hospital & Institute,Sichuan Cancer Center, School of Medicine, University of Electronic Science andTechnology of China, Chengdu, 610041, P. R. China临床药学部临床药学部四川省肿瘤医院[5]School of Life Science and Engineering, Southwest JiaoTong University,Chengdu, Sichuan, 611756, P. R. China.
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.
基金：
the National Natural Science
Foundation of China (81702946, 82073687) and the National
S&T Major Special Project on Major New Drug Innovations of
China (2018ZX09201018).
第一作者机构：[1]State Key Laboratory of Biotherapy/Collaborative Innovation Center forBiotherapy, West China Hospital, West China Medical School,Sichuan University, Chengdu, Sichuan 610041, P. R. China.
共同第一作者：
通讯作者：
推荐引用方式(GB/T 7714)：
Zhang Qiangsheng,Hu Xi,Li Lu,et al.The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor.[J].CHEMICAL COMMUNICATIONS.2021,57(24):3006-3009.doi:10.1039/d0cc04670a.
APA：
Zhang Qiangsheng,Hu Xi,Li Lu,Zhang Lidan,Wan Guoquan...&Yu Luoting.(2021).The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor..CHEMICAL COMMUNICATIONS,57,(24)
MLA：
Zhang Qiangsheng,et al."The discovery of SKLB-0335 as a paralog-selective EZH2 covalent inhibitor.".CHEMICAL COMMUNICATIONS 57..24(2021):3006-3009
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