A patent review of KDM4 histone demethylase inhibitors (2014-present)
文献类型：期刊论文
| 作者 | Yang, Xiaolong2,3; Han, Yuyan2,3; Yu, Lei1; Xu, Shilin2,3,4 |
| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
 |
| 出版日期 | 2026-01-16 |
| 页码 | 17 |
| 关键词 | KDM4 JMJD2 histone demethylase epigenetics inhibitor |
| ISSN号 | 1354-3776 |
| DOI | 10.1080/13543776.2026.2614491 |
| 通讯作者 | Xu, Shilin(slxu@simm.ac.cn) |
| 英文摘要 | IntroductionThe KDM4 family of histone demethylases, characterized by a conserved JmjC catalytic domain, comprises six subtypes: KDM4A - F. Aberrant expression of these enzymes has been associated with tumorigenesis across various malignancies, highlighting their potential as therapeutic targets in oncology. To date, a series of KDM4 inhibitors have been developed, among which TACH101 is undergoing clinical evaluation for cancer treatment.Areas coveredThis review provides a comprehensive overview of the patent literature on KDM4 inhibitors, derived from a systematic search utilizing the Cortellis Drug Discovery Intelligence database. A total of 17 patent applications, published within the period from June 2014 to May 2025, were identified and critically analyzed.Expert opinionSignificant progress has been achieved in the development of KDM4 inhibitors; however, most current compounds continue to face major challenges, including poor membrane permeability, limited cellular potency, and low isoform specificity. Strategies such as designing inhibitors with novel scaffolds, developing covalent inhibitors, advancing protein degraders, and targeting non-catalytic domains may provide viable solutions to these limitations. In addition, the physiological and pathological roles of KDM4 remain insufficiently characterized. Further in-depth investigations into the biological functions of KDM4 will be essential to guide the rational design and facilitate the clinical translation of KDM4-targeted therapeutics. |
| WOS关键词 | LYSINE DEMETHYLASE ; JMJD2 FAMILY ; METHYLATION ; CHROMATIN ; GASC1 ; TRIMETHYLATION ; IDENTIFICATION ; REVERSAL ; DOMAIN ; GENE |
| 资助项目 | Strategic Priority Research Program of the Chinese Academy of Sciences[XDB1260000] ; Shanghai Institute of Materia Medica of the Chinese Academy of Sciences[NOS. SIMM0220231001] ; National Key Research and Development Program of China[2023YFA1800804] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001662080400001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/322643]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xu, Shilin |
| 作者单位 | 1.Tongji Univ, Canc Ctr, Shanghai Peoples Hosp 10, Sch Med, Shanghai, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing, Peoples R China 4.Univ Chinese Acad Sci, Sch Pharmaceut Sci & Technol, Hangzhou Inst Adv Study, Hangzhou, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Xiaolong,Han, Yuyan,Yu, Lei,et al. A patent review of KDM4 histone demethylase inhibitors (2014-present)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2026:17. |
| APA | Yang, Xiaolong,Han, Yuyan,Yu, Lei,&Xu, Shilin.(2026).A patent review of KDM4 histone demethylase inhibitors (2014-present).EXPERT OPINION ON THERAPEUTIC PATENTS,17. |
| MLA | Yang, Xiaolong,et al."A patent review of KDM4 histone demethylase inhibitors (2014-present)".EXPERT OPINION ON THERAPEUTIC PATENTS (2026):17. |
入库方式： OAI收割
来源：上海药物研究所
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