Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferase

Nicotinamide phosphoribosyltransferase (NAMPT) is a promising anticancer target. Using high throughput screening system targeting NAMPT, we obtained a potent NAMPT inhibitor MS0 (China Patent ZL201110447488.9) with excellent in vitro activity (IC50 = 9.87 ± 1.15nM) and anti-proliferative activity ag...

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Veröffentlicht in:	Scientific reports 2015-06, Vol.5 (1), p.10043, Article 10043
Hauptverfasser:	Xu, Tian-Ying, Zhang, Sai-Long, Dong, Guo-Qiang, Liu, Xin-Zhu, Wang, Xia, Lv, Xiao-Qun, Qian, Qi-Jun, Zhang, Ruo-Yu, Sheng, Chun-Quan, Miao, Chao-Yu
Format:	Artikel
Sprache:	eng
Schlagworte:	13/1 13/31 49/47 49/98 631/154/1435/2163 631/92/436/2388 631/92/556 631/92/609 82/29 82/80 82/81 82/83 Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor agents Berries Cancer Cell Line, Tumor Cell Proliferation - drug effects Drug Discovery Drug Evaluation, Preclinical Enzyme Activation - drug effects Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology High-throughput screening High-Throughput Screening Assays Humanities and Social Sciences Humans Inhibitors Inhibitory Concentration 50 Models, Molecular Molecular Conformation multidisciplinary Neoplastic Stem Cells - drug effects Neoplastic Stem Cells - metabolism Nicotinamide phosphoribosyltransferase Nicotinamide Phosphoribosyltransferase - antagonists & inhibitors Nicotinamide Phosphoribosyltransferase - chemistry Protein Binding Science Site-directed mutagenesis Small Molecule Libraries Structure-Activity Relationship Tumor cell lines
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