Hydrocarbon-stapled polypeptides for enhancement of endosome-lysosomal degradation

Yanxiang Zhao (Inventor), Shuai Wu (Inventor), Wenchao Yang (Inventor), Yunjiao He (Inventor), Xiaohua Li (Inventor), Xianxiu Qiu (Inventor)

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Abstract

The present invention relates to a Beclin 1-UVRAG complex structure which reveals a tightly packed coiled coil assembly with Beclin 1 and UVRAG residues complementing each other to form a stable dimeric complex. This potent physical interaction is critical for UVRAG-dependent EGFR degradation but less critical for autophagy. Targeting the Beclin 1 coiled coil domain with rationally designed stapled peptides leads to enhanced autophagy activity and EGFR degradation in non-small cell lung cancer (NSCLC) cell lines, suggesting translational value for these compounds.
Original languageEnglish
Patent numberUS10618939
IPC A61P35/00
Priority date29/06/16
Filing date14/03/18
Publication statusPublished - 14 Apr 2020

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