Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 8, Pages 802-806Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00208
Keywords
ATG4B; autophagy; covalent inhibitor; fluoromethylketone; peptidomimetics
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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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