The ERAD inhibitor Eeyarestatin I is a bifunctional compound with a membrane-binding domain and a p97/VCP inhibitory group

ERAD 抑制剂 Eeyarestatin I 是一种双功能化合物,具有膜结合域和 p97/VCP 抑制基团

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作者:Qiuyan Wang, Bidhan A Shinkre, Jin-gu Lee, Marc A Weniger, Yanfen Liu, Weiping Chen, Adrian Wiestner, William C Trenkle, Yihong Ye

Background

Protein homeostasis in the endoplasmic reticulum (ER) has recently emerged as a therapeutic target for cancer treatment. Disruption of ER homeostasis

Significance

Our findings reveal a class of bifunctional chemical agents that can preferentially inhibit membrane-bound p97 to disrupt ER homeostasis and to induce tumor cell death. These results also suggest that the AAA ATPase p97 may be a potential drug target for cancer therapeutics.

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