A novel small-molecule antagonizes PRMT5-mediated KLF4 methylation for targeted therapy

一种新型小分子拮抗 PRMT5 介导的 KLF4 甲基化用于靶向治疗

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作者:Zhuan Zhou, Zhiwei Feng, Dong Hu, Peng Yang, Mert Gur, Ivet Bahar, Massimo Cristofanilli, William J Gradishar, Xiang-Qun Xie, Yong Wan

Background

Triple negative breast cancers (TNBCs) have a poor prognosis and are not amenable to endocrine- or HER2-targeted therapies. The malignant and invasive feature of TNBCs is correlated with its high cancer stem cell population. Recent

Methods

We have developed a small molecule inhibitor, WX2-43, that specifically intercepts the interaction between PRMT5 and KLF4, thereby enhancing KLF4 degradation. Findings:

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