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一种新的分子胶水途径:快速发现 NFKB1 降解剂。

A new avenue for molecular glues: Rapid discovery of a NFKB1 degrader.

机构信息

Department of Chemistry and Biochemistry, University of California San Diego, La Jolla, CA, USA.

Department of Chemistry and Biochemistry, University of California San Diego, La Jolla, CA, USA; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, CA, USA.

出版信息

Cell Chem Biol. 2023 Apr 20;30(4):340-342. doi: 10.1016/j.chembiol.2023.04.002.

Abstract

Targeted protein degradation using molecular glues is a powerful method for targeting traditionally undruggable proteins. One challenge in molecular glue discovery is the absence of rational discovery methods. Here, King et al. leverage covalent library screening with chemoproteomics platforms to rapidly discover a molecular glue targeting NFKB1 via UBE2D recruitment.

摘要

利用分子胶进行靶向蛋白降解是靶向传统上不可成药蛋白的一种强大方法。分子胶发现的一个挑战是缺乏合理的发现方法。在这里,King 等人利用共价文库筛选与化学生物学平台相结合,快速发现了一种通过 UBE2D 招募靶向 NFKB1 的分子胶。

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