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

Zongxing Qiu,Bernd Kuhn,Johannes Aebi,Xianfeng Lin,Haiyuan Ding,Zheng Zhou,Zhiheng Xu,Danqing Xu,Li Han,Cheng Liu,Hongxia Qiu,Yuxia Zhang,Wolfgang Haap,Claus Riemer,Martin Stahl,Ning Qin,Hong C Shen,Guozhi Tang

ACS medicinal chemistry letters（2016）

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摘要

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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关键词

ATG4B,autophagy,covalent inhibitor,fluoromethylketone,peptidomimetics

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