RDN-8011(RDN-8011) - 药物靶点：KDM4_在研适应症：食管癌_专利_临床

概要

基本信息

药物类型

蛋白水解靶向嵌合体（PROTAC）

别名

靶点

KDM4

作用方式

抑制剂

作用机制

KDM4 抑制剂(lysine demethylase 4 inhibitors)

治疗领域

肿瘤消化系统疾病

在研适应症

食管癌

非在研适应症-

原研机构

在研机构

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

关联

100 项与 RDN-8011 相关的临床结果

登录后查看更多信息

100 项与 RDN-8011 相关的转化医学

登录后查看更多信息

100 项与 RDN-8011 相关的专利（医药）

登录后查看更多信息

1

项与 RDN-8011 相关的文献（医药）

2025-04-01·European Journal of Medicinal Chemistry

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

Article

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

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.

100 项与 RDN-8011 相关的药物交易

登录后查看更多信息