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Literature DB >> 27563406

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

Zongxing Qiu¹, Bernd Kuhn², Johannes Aebi², Xianfeng Lin¹, Haiyuan Ding¹, Zheng Zhou¹, Zhiheng Xu¹, Danqing Xu¹, Li Han¹, Cheng Liu¹, Hongxia Qiu¹, Yuxia Zhang¹, Wolfgang Haap², Claus Riemer², Martin Stahl², Ning Qin¹, Hong C Shen¹, Guozhi Tang¹.

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.

Entities: Chemical Gene

Keywords: ATG4B; autophagy; covalent inhibitor; fluoromethylketone; peptidomimetics

Year: 2016 PMID： 27563406 PMCID： PMC4983731 DOI： 10.1021/acsmedchemlett.6b00208

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

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