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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4983731 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.6b00208 | DOI Listing |
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