Discovery of potent and selective HER2 PROTAC degrader based Tucatinib with improved efficacy against HER2 positive cancers

HER2 is a validated therapeutic target for HER2 positive breast cancer and gastric cancer. TKIs have significantly improved the prognosis of patients with HER2 positive cancer. However, the pan-HER TKIs always caused gastrointestinal and skin side effects, and acquired drug resistance inevitable com...

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Veröffentlicht in:	European journal of medicinal chemistry 2022-12, Vol.244, p.114775-114775, Article 114775
Hauptverfasser:	Hu, Mingxing, Li, Yujue, Li, Jiaxuan, Zhou, Haoxuan, Liu, Chengyali, liu, Zi, Gong, Youling, Ying, Binwu, Xie, Yongmei
Format:	Artikel
Sprache:	eng
Schlagworte:	anti-tumor CADD HER2 PROTAC Structural optimization
Online-Zugang:	Volltext
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