Quantitative chemoproteomic profiling reveals multiple target interactions of spongiolactone derivatives in leukemia cells
Quantitative chemoproteomic profiling reveals multiple target interactions of spongiolactone derivatives in leukemia cells
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定量化学蛋白质组学分析揭示了白血病细胞中海绵内酯衍生物的多个靶点相互作用
DOI：
10.1039/c7cc04990k
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发表时间：
2017
影响因子：
4.9
通讯作者：
Sieber, S. A.
中科院分区：
文献类型：
--
作者：
Wright, M. H.;Tao, Y.;Drechsel, J.;Krysiak, J.;Chamni, S.;Weigert-Munoz, A.;Harvey, N. L.;Romo, D.;Sieber, S. A.
海绵内酯是一种具有不寻常的重排海绵烷骨架和稠合β-内酯环的海洋天然产物。这些化合物具有潜在的抗癌特性，但其作用方式尚未探索。在这里，我们采用基于活性的蛋白质谱分析来鉴定活癌细胞中更有效的海绵内酯衍生物的靶点，并将其与更简单的β-内酯的靶点进行比较。这些命中提供了对这种天然产物类的共价作用机制的第一个见解。
The spongiolactones are marine natural products with an unusual rearranged spongiane skeleton and a fused β-lactone ring. These compounds have potential anticancer properties but their mode of action has yet to be explored. Here we employ activity-based protein profiling to identify the targets of a more potent spongiolactone derivative in live cancer cells, and compare these to the targets of a simpler β-lactone. These hits provide the first insights into the covalent mechanism of action of this natural product class.