Discovery of a Potent Deubiquitinase (DUB) Small-Molecule Activity-Based Probe Enables Broad Spectrum DUB Activity Profiling in Living Cells**,Angewandte Chemie International Edition

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Discovery of a Potent Deubiquitinase (DUB) Small-Molecule Activity-Based Probe Enables Broad Spectrum DUB Activity Profiling in Living Cells**
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2023-10-01 , DOI: 10.1002/anie.202311190
Daniel Conole _{1,

2} , Fangyuan Cao ₁ , Christopher W Am Ende ₃ , Liang Xue ₄ , Sheila Kantesaria ₃ , Dahye Kang ₄ , Jun Jin ₅ , Dafydd Owen ₄ , Linda Lohr ₃ , Monica Schenone ₄ , Jaimeen D Majmudar ₄ , Edward W Tate ₁

Affiliation

IMP-2373 is the first activity-based probe (ABP) that captures the activity of a large portion of the “DUBome” across multiple deubiquitinase (DUB) sub-classes with limited off-target effects in living cells, providing a complementary tool to ubiquitin ABPs, which function only in lysates. IMP-2373 enables researchers to profile DUB inhibitors target engagement and selectivity in cells, and to understand DUB activity in disease-relevant systems.

中文翻译：

发现一种有效的去泛素酶 (DUB) 小分子活性探针，可实现活细胞中广谱 DUB 活性分析**

IMP-2373 是第一个基于活性的探针 (ABP)，可捕获多个去泛素酶 (DUB) 子类中大部分“DUBome”的活性，在活细胞中脱靶效应有限，为泛素 ABP，仅在裂解物中发挥作用。IMP-2373 使研究人员能够分析 DUB 抑制剂在细胞中的靶点参与和选择性，并了解疾病相关系统中的 DUB 活性。

更新日期：2023-10-01

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