Lighting up the linear ubiquitin code: a bioluminescent sensor for M1-specific deubiquitinase activity and drug
Yuxin Zheng1, Manman Zhang1, Wutao Xie1
1Laboratory of Structural Biology and Drug Discovery, Laboratory of Ubiquitination and Targeted Therapy, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, Guangdong, 518055, China. huang.hao@pku.edu.cn.
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A luciferase-based reporter, N-Rluc-Ub-Ub-C-Rluc, was developed to selectively monitor M1-deubiquitinase activity via catalytic signal amplification. This high-throughput assay identified baicalein and lumacaftor as novel OTULIN inhibitors from an FDA-approved compound library, validated by STD-NMR and cellular assays. The reporter enables drug discovery targeting linear ubiquitin signaling without specialized synthesis.
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