Target discovery of ebselen with a biotinylated probe

Zhenzhen Chen; Zhongyao Jiang; Nan Chen; Qian Shi; Lili Tong; Fanpeng Kong; Xiufen Cheng; Hao Chen; Chu Wang; Bo Tang

doi:10.1039/C8CC04258F

Target discovery of ebselen with a biotinylated probe†

Zhenzhen Chen,‡^a Zhongyao Jiang,‡^a Nan Chen,‡^b Qian Shi,^a Lili Tong,^a Fanpeng Kong,^a Xiufen Cheng,^a Hao Chen,

^c Chu Wang

*^b and Bo Tang

*^a

Author affiliations

* Corresponding authors

^a College of Chemistry, Chemical Engineering and Materials Science, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Institute of Molecular and Nano Science, Shandong Normal University, Jinan 250014, P. R. China
E-mail: tangb@sdnu.edu.cn

^b Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing, China
E-mail: chuwang@pku.edu.cn

^c Department of Chemistry and Biochemistry, Ohio University, Athens, Ohio 45701, USA

Abstract

Despite numerous studies on ebselen over the past decade, its cellular targets remain obscure. Here we synthesized a biotinylated ebselen probe (biotin-ebselen) and characterized ebselen-binding proteins via an efficient activity-based protein profiling (ABPP) method, which allowed for the robust identification of 462 targeted proteins in HeLa cells. This first work of global target profiling of ebselen will be helpful to re-design ebselen-based therapy appropriately in clinical trials.

Chemical Communications

Target discovery of ebselen with a biotinylated probe†

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