Discovery of a first-in-class PROTAC degrader of histone lysine demethylase KDM4.

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Tác giả: Zhiwen Chen, Yuanhui Lai, Lijie Peng, Danni Rao, Ran Ren, Yaoliang Sun, Yiting Wang, Feifei Wu, Shilin Xu, Xiaolong Yang, Lei Yu, Zhang Zhang

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: France : European journal of medicinal chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 738494

Targeting histone lysine demethylase 4 (KDM4) has emerged as a promising approach for cancer therapy. Despite significant progress in developing KDM4 inhibitors, many of these compounds demonstrate poor selectivity or limited cellular efficacy, and none have received approval for marketing. In this study, we designed and synthesized a series of novel KDM4-targeted proteolysis targeting chimeras (PROTAC) degraders, as exemplified by compound 11 (RDN8011). RDN8011 effectively degrades KDM4A-C while sparing KDM4D, and displays potent antiproliferative activity in esophageal cancer cells. Furthermore, this compound inhibits histone H3 lysine demethylation and induces cell cycle arrest and apoptosis. Collectively, this study provides a valuable chemical tool for exploring the functions of KDM4, and presents a novel effective strategy for targeting KDM4 in cancer treatment.
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