Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations

[Display omitted] As one of the most promising anticancer target in protein arginine methyltransferase (PRMT) family, PRMT5 has been drawing more and more attentions, and many efforts have been devoted to develop its inhibitors. In this study, three PRMT5 inhibitors (9, 16, and 23) with novel scaffo...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-05, Vol.28 (9), p.1476-1483
Hauptverfasser:	Zhu, Kongkai, Jiang, Chengshi, Tao, Hongrui, Liu, Jingqiu, Zhang, Hua, Luo, Cheng
Format:	Artikel
Sprache:	eng
Schlagworte:	Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Models, Molecular Molecular docking Molecular dynamics simulation Molecular Structure PRMT5 inhibitor Protein-Arginine N-Methyltransferases - antagonists & inhibitors Protein-Arginine N-Methyltransferases - metabolism Resynthesis Small Molecule Libraries - chemical synthesis Small Molecule Libraries - chemistry Small Molecule Libraries - pharmacology Structure-Activity Relationship Virtual screening
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