Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders

The first examples of threonine tyrosine kinase (TTK) PROTACs were designed and synthesized. Two of the most potent molecules, 8e and 8j, demonstrated strong TTK degradation in COLO-205 human colorectal cancer cells with DC50 values of 1.7 and 3.1 nM, respectively. Proteasome-mediated degradation by...

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Veröffentlicht in:	Journal of medicinal chemistry 2022-02, Vol.65 (3), p.2313-2328
Hauptverfasser:	Lu, Jibu, Huang, Yongjun, Huang, Jing, He, Rui, Huang, Minhao, Lu, Xiaoyun, Xu, Yong, Zhou, Fengtao, Zhang, Zhang, Ding, Ke
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Cell Line, Tumor Cell Proliferation - drug effects Drug Design Humans Ligands Male Mice Mice, SCID Neoplasms - drug therapy Proteasome Endopeptidase Complex - metabolism Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Protein-Tyrosine Kinases - chemistry Protein-Tyrosine Kinases - metabolism Proteolysis - drug effects Structure-Activity Relationship Transplantation, Heterologous Von Hippel-Lindau Tumor Suppressor Protein - chemistry Von Hippel-Lindau Tumor Suppressor Protein - metabolism
Online-Zugang:	Volltext
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