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Quantitative chemoproteomic profiling reveals multiple target interactions of spongiolactone derivatives in leukemia cells

https://doi.org/10.1039/C7CC04990K

Wright, M. H. ; Tao, Y. ; Drechsel, J. ; Krysiak, J. ; Chamni, S. ; Weigert-Munoz, A. ; Harvey, N. L. ; Romo, D. ; Sieber, S. A. ( January 2017 , Chemical Communications)

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.
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