Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy

[Display omitted] •A series of EGFR-PROTACs were designed, synthesized, and evaluated for their biological activities.•13 exhibited excellent anti-proliferative activities against HCC-827 cells.•13 can efficiently induce EGFR protein degradation and inhibit phosphorylation of downstream pathways in...

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Veröffentlicht in:	Bioorganic chemistry 2022-03, Vol.120, p.105605-105605, Article 105605
Hauptverfasser:	Shi, Shi, Du, Yu, Huang, Lei, Cui, Jiaqi, Niu, Jing, Xu, Yungen, Zhu, Qihua
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis Degrader EGFR In vivo efficiency PROTAC
Online-Zugang:	Volltext
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