Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin
Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin
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DOI：
10.1021/acs.jmedchem.8b01774
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发表时间：
2019-02-14
影响因子：
7.3
通讯作者：
Georg, Gunda I.
中科院分区：
文献类型：
--
作者：
Coulup, Sara K.;Huang, David S.;Georg, Gunda I.
Pironetin 是唯一经晶体学证实的靶向 a-微管蛋白的天然产物，对敏感和耐药的 A2780 卵巢癌细胞系表现出有效的细胞毒活性，但在体内的活性有限。我们现在报道 Pironetin 的半衰期很短（
Pironetin, the only crystallographically confirmed natural product to target a-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is only marginally active in vivo. We now report that pironetin has a short half-life (