Issue 11, 2019

Expanding the “minimalist” small molecule tagging approach to different bioactive compounds

Abstract

“Minimalist” small molecule tagging (MSMT) is a promising approach that easily converts bioactive compounds into affinity-based probes (AfBPs) for proteomic studies. In this work, seven bioactive compounds targeting diversified protein classes were installed with “minimalist” linkers through common reactions to generate the corresponding AfBPs. These probes were evaluated for cell-based protein profiling and target validation. Among them, the entinostat-derived probe EN and the camptothecin-derived probe CA were further utilized in cellular imaging and SILAC-based large-scale target identification. Our extensive studies suggest that the “minimalist” small molecule tagging approach could be expanded to different classes of bioactive compounds for modification into AfBPs as a dual functional tool for both proteomics and cellular imaging.

Graphical abstract: Expanding the “minimalist” small molecule tagging approach to different bioactive compounds

Supplementary files

Article information

Article type
Paper
Submitted
21 Dec 2018
Accepted
11 Feb 2019
First published
21 Feb 2019

Org. Biomol. Chem., 2019,17, 3010-3017

Expanding the “minimalist” small molecule tagging approach to different bioactive compounds

W. Lang, C. Yuan, B. Zhu, S. Pan, J. Liu, J. Luo, S. Nie, Q. Zhu, J. Lee and J. Ge, Org. Biomol. Chem., 2019, 17, 3010 DOI: 10.1039/C8OB03175D

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