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

Chem Commun (Camb). 2021 Feb 24. doi: 10.1039/d0cc04670a. Online ahead of print.ABSTRACTBy 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.PMID:33623946 | DOI:10.1039/d0cc04670a

Source: Chemical Communications - February 24, 2021 Category: Chemistry Authors: Qiangsheng Zhang Xi Hu Lu Li Lidan Zhang Guoquan Wan Qiang Feng Yongxia Zhu Ningyu Wang Zhihao Liu Luoting Yu Source Type: research