Lighting up the linear Ubiquitin Code: A Bioluminescent Sensor for M1-Specific Deubiquitinase Activity and Drug Discovery

Yuxin Zheng; Manman Zhang; Wutao Xie; Xiaogang Niu; Congjun Xu; HB Zhai; Hao Huang

doi:10.1039/d5cc07195j

January 1, 2026Chemical Communications

Lighting up the linear Ubiquitin Code: A Bioluminescent Sensor for M1-Specific Deubiquitinase Activity and Drug Discovery

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Key Points

The study aims to develop a bioluminescent sensor to monitor M1-deubiquitinase activity and identify potential inhibitors.
Developed a luciferase-based reporter (N-Rluc-Ub-Ub-C-Rluc) for monitoring activity.
Utilized catalytic signal amplification for enhanced detection.
Conducted high-throughput screening of FDA-approved compounds.
Identified Baicalein and Lumacaftor as novel OTULIN inhibitors.
Demonstrated selective monitoring of M1-deubiquitinase activity.

Implication

High-throughput assay identifies novel OTULIN inhibitors in drug discovery using a bioluminescent sensor.

Abstract

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...

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Cite This Study

Zheng et al. (2026) studied this question.

synapsesocial.com/papers/69d9e58f78050d08c1b75c85 https://doi.org/10.1039/d5cc07195j

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Lighting up the linear Ubiquitin Code: A Bioluminescent Sensor for M1-Specific Deubiquitinase Activity and Drug Discovery

Key Points

Implication

Abstract

Discussion

Cite This Study

Lighting up the linear Ubiquitin Code: A Bioluminescent Sensor for M1-Specific Deubiquitinase Activity and Drug Discovery

Key Points

Implication

Abstract

Discussion

Cite This Study

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