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Issue 6, 2019
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Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening

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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.

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

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Publication details

The article was received on 31 Oct 2018, accepted on 12 Dec 2018 and first published on 14 Dec 2018


Article type: Communication
DOI: 10.1039/C8CC08685K
Citation: Chem. Commun., 2019,55, 834-837
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    Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening

    C. Guo, Y. Chang, X. Wang, C. Zhang, P. Hao, K. Ding and Z. Li, Chem. Commun., 2019, 55, 834
    DOI: 10.1039/C8CC08685K

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