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Stapled Peptide Inhibitors of Autophagy Adapter LC3B.
ChemBioChem ( IF 2.6 ) Pub Date : 2020-05-14 , DOI: 10.1002/cbic.202000212
Robert A Cerulli 1 , Livia Shehaj 2 , Hawley Brown 2 , Jennifer Pace 2 , Yang Mei 2 , Joshua A Kritzer 2
Affiliation  

Combined with chemotherapy: Autophagy inhibitors have shown anti‐proliferative activity when co‐administered with standard chemotherapies. Peptides derived from the FYCO1 LC3‐interacting region (LIR) motif were prepared for structure‐activity characterization with the autophagy adapter protein, LC3B. Additionally, artificial amino acids and diversity‐oriented peptide stapling were used to generate LC3B‐selective peptide inhibitors with improved affinity and stability.
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中文翻译:


自噬接头 LC3B 的钉合肽抑制剂。



与化疗联合使用:自噬抑制剂与标准化疗联合使用时显示出抗增殖活性。制备源自 FYCO1 LC3 相互作用区 (LIR) 基序的肽,用于使用自噬衔接蛋白 LC3B 进行结构活性表征。此外,还使用人工氨基酸和面向多样性的肽装订来生成具有改善的亲和力和稳定性的 LC3B 选择性肽抑制剂。
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更新日期:2020-05-14
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