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Structure-Based Design of Stapled Peptides That Bind GABARAP and Inhibit Autophagy

2 Aug 2022

Abstract excerpt

The LC3/GABARAP family of proteins is involved in nearly every stage of autophagy. Inhibition of LC3/GABARAP proteins is a promising approach to blocking autophagy, which sensitizes advanced cancers to DNA-damaging chemotherapy. Here, we report the structure-based design of stapled peptides that inhibit GABARAP with nanomolar affinities. Small changes in staple structure produced stapled peptides with very...

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PMID: 35917476
DOI: 10.1021/jacs.2c04699

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