Issue 95, 2017

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

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

Supplementary files

Article information

Article type
Communication
Submitted
28 Jun 2017
Accepted
07 Nov 2017
First published
08 Nov 2017

Chem. Commun., 2017,53, 12818-12821

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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