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3-(3-Phenoxybenzyl)amino-β-carboline: A novel antitumor drug targeting α-tubulin
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2011-06-22 , DOI: 10.1016/j.bmcl.2011.06.061
Reiko Ikeda , Masaki Kurosawa , Takazumi Okabayashi , Ayako Takei , Masamichi Yoshiwara , Tadashi Kumakura , Norio Sakai , Osamu Funatsu , Akinori Morita , Masahiko Ikekita , Yumi Nakaike , Takeo Konakahara

3-(3-Phenoxybenzyl)amino-β-carboline showed extremely-high activity; the IC value was 0.074μM. To verify -induced cell death types, we observed the chromatin condensation, the DNA fragmentation and activated caspase-3 using Hoechst 33342, agarose electrophoresis and western blot, and suggesting -induced cell death type was apoptosis. Flow cytometry showed that -treated cell was induced SubG1 cell population after G2/M cell cycle arrest. In addition, using affinity chromatography and peptide mass fingerprinting, we found that interacting protein with this compound was α-tubulin protein.

中文翻译:

3-(3-苯氧基苄基)氨基-β-咔啉:一种靶向α-微管蛋白的新型抗肿瘤药物

3-(3-苯氧基苄基)氨基-β-咔啉表现出极高的活性;IC值为0.074μM。为了验证诱导的细胞死亡类型,我们使用Hoechst 33342、琼脂糖电泳和蛋白质印迹观察了染色质浓缩、DNA断裂和激活的caspase-3,并提示诱导的细胞死亡类型为凋亡。流式细胞术显示经处理的细胞在G2/M细胞周期停滞后被诱导为SubG1细胞群。此外,利用亲和色谱和肽质量指纹图谱分析,我们发现与该化合物相互作用的蛋白是α-微管蛋白。
更新日期:2011-06-22
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