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Quantitative chemoproteomic profiling reveals multiple target interactions of spongiolactone derivatives in leukemia cells
Chemical Communications ( IF 4.9 ) Pub Date : 2017-11-08 00:00:00 , DOI: 10.1039/c7cc04990k
M. H. Wright 1, 2, 3, 4, 5 , Y. Tao 6, 7, 8, 9 , J. Drechsel 1, 2, 3, 4, 5 , J. Krysiak 1, 2, 3, 4, 5 , S. Chamni 2, 9, 10, 11 , A. Weigert-Munoz 1, 2, 3, 4, 5 , N. L. Harvey 2, 9, 10, 11 , D. Romo 6, 7, 8, 9 , S. A. Sieber 1, 2, 3, 4, 5
Affiliation  

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.

中文翻译:

定量化学计量学分析揭示了白血病细胞中海绵内酯衍生物的多个靶标相互作用

海绵内酯是海洋天然产物,具有不寻常的重排海绵骨架和稠合的β-内酯环。这些化合物具有潜在的抗癌特性,但其作用方式尚待探索。在这里,我们采用基于活性的蛋白质谱分析法来鉴定活癌细胞中更有效的海绵内酯衍生物的靶标,并将其与更简单的β-内酯的靶标进行比较。这些命中提供了对这种天然产品类别的共价作用机制的初步见解。
更新日期:2017-11-16
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