Design, synthesis and evaluation of EZH2-based PROTACs targeting PRC2 complex in lymphoma

The novel EZH2 degrading agent E-3P-MDM2 induced robust cell viability inhibition in both HBL-1 (EZH2WT) and SU-DHL-6 (EZH2Y614N), which was much stronger than that of EPZ6438. E-3P-MDM2 can effectively degrade EZH2 of SU-DHL-6 cells in a concentration and dose-dependent manner, degrading EED and SU...

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Veröffentlicht in:	Bioorganic chemistry 2023-11, Vol.140, p.106762-106762, Article 106762
Hauptverfasser:	Xie, Huiru, Xu, Wei, Liang, Jing, Liu, Yang, Zhuo, Chenxi, Zou, Xiaoxue, Luo, Weihong, Xiao, Jianping, Lin, Yu, Chen, Lixia, Li, Hua
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-proliferative activity EPZ6438 EZH2 degradation PROTAC
Online-Zugang:	Volltext
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