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

GuoCuiping Guo and Yu Chang contributed equally to this work., Cuiping, Chang, Yu, Wang, Xin, Zhang, Chengqian, Hao, Piliang, Ding, Ke, Li, Zhengqiu
Chemical communications 2019 v.55 no.6 pp. 834-837
chemical compounds, chemical reactions, drugs, image analysis, moieties, protein composition, proteome, screening
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.