Hydrocarbon-stapled polypeptides for enhancement of endosome-lysosomal degradation

Yanxiang Zhao; Shuai Wu; Wenchao Yang; Yunjiao He; Xiaohua Li; Xianxiu Qiu

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)

Department of Applied Biology and Chemical Technology

Research output: Patents, agreements, assignments and companies › Patents granted

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 language	English
Patent number	US10618939
IPC	A61P35/00
Priority date	29/06/16
Filing date	14/03/18
Publication status	Published - 14 Apr 2020

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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.",

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AU - Wu, Shuai

AU - Yang, Wenchao

AU - He, Yunjiao

AU - Li, Xiaohua

AU - Qiu, Xianxiu

PY - 2020/4/14

Y1 - 2020/4/14

N2 - 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.

AB - 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.

M3 - Patents granted

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ER -

Hydrocarbon-stapled polypeptides for enhancement of endosome-lysosomal degradation

Abstract

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