Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors

Zongxing Qiu; Bernd Kuhn; Johannes D. Aebi; Xianfeng Lin; Haiyuan Ding; Zheng Zhou; Zhiheng Xu; Danqing Xu; Li Han; Cheng Liu; Hong-Xia Qiu; Yuxia Zhang; Wolfgang Haap; Claus Riemer; Martin Ståhl; Na Qin; Hong C. Shen; Guozhi Tang

doi:10.1021/acsmedchemlett.6b00208

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Abstract

ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B plays essential roles in the autophagosome formation and the autophagy pathway. Herein we disclose the design and structural modifications of a series of fluoromethylketone (FMK)-based peptidomimetics as highly potent ATG4B inhibitors. Their structure-activity relationship (SAR) and protease selectivity are also discussed.

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Qiu et al. (2016) studied this question.

synapsesocial.com/papers/6a75a45d42ce5c1965dd90a1 https://doi.org/10.1021/acsmedchemlett.6b00208

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Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors

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Abstract

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Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors

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