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Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening

Author:
GuoCuiping Guo and Yu Chang contributed equally to this work., Cuiping, Chang, Yu, Wang, Xin, Zhang, Chengqian, Hao, Piliang, Ding, Ke, Li, Zhengqiu
Source:
Chemical communications 2019 v.55 no.6 pp. 834-837
ISSN:
1364-548X
Subject:
chemical compounds, chemical reactions, drugs, image analysis, moieties, protein composition, proteome, screening
Abstract:
Activity-based protein profiling (ABPP) and bioimaging have been powerful approaches for in situ drug screening and target identification. However, these approaches are still hindered by the preparation of high-quality probes. To address this challenge, we developed a series of novel minimalist linkers for irreversible inhibitors by incorporation of various bioorthogonal handles into an α,β-unsaturated amide, a common moiety of many irreversible inhibitors. The linker-containing probes have been demonstrated to be suitable for simultaneous protein labelling, live cell imaging and drug screening.
Agid:
6269197