Chemical Inhibition of Human Thymidylate Kinase and Structural Insights into the Phosphate Binding Loop and Ligand-Induced Degradation

Targeting thymidylate kinase (TMPK) that catalyzes the phosphotransfer reaction for formation of dTDP from dTMP is a new strategy for anticancer treatment. This study is to understand the inhibitory mechanism of a previously identified human TMPK (hTMPK) inhibitor YMU1 (1a) by molecular docking, iso...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-11, Vol.59 (21), p.9906-9918
Hauptverfasser:	Chen, Yi-Hsuan, Hsu, Hua-Yi, Yeh, Ming-Tyng, Chen, Chen-Cheng, Huang, Chang-Yu, Chung, Ying-Hsuan, Chang, Zee-Fen, Kuo, Wei-Chen, Chan, Nei-Li, Weng, Jui-Hsia, Chung, Bon-chu, Chen, Yu-Ju, Jian, Cheng-Bang, Shen, Ching-Chieh, Tai, Hwan-Ching, Sheu, Sheh-Yi, Fang, Jim-Min
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites - drug effects Calorimetry Cell Line Cell Survival - drug effects Crystallography, X-Ray Dose-Response Relationship, Drug Humans Mice Models, Molecular Molecular Structure Nucleoside-Phosphate Kinase - antagonists & inhibitors Nucleoside-Phosphate Kinase - metabolism Phosphates - metabolism Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Proteolysis - drug effects Structure-Activity Relationship
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