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Issue 95, 2017
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Quantitative chemoproteomic profiling reveals multiple target interactions of spongiolactone derivatives in leukemia cells

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Abstract

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.

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

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Supplementary files

Article information


Submitted
28 Jun 2017
Accepted
07 Nov 2017
First published
08 Nov 2017

Chem. Commun., 2017,53, 12818-12821
Article type
Communication

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

M. H. Wright, Y. Tao, J. Drechsel, J. Krysiak, S. Chamni, A. Weigert-Munoz, N. L. Harvey, D. Romo and S. A. Sieber, Chem. Commun., 2017, 53, 12818
DOI: 10.1039/C7CC04990K

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