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Discovery of novel biaryl urea derivatives against IL-1/3 release with low toxicity based on NEK7 inhibitor

文献类型：期刊论文

作者Wang, Leibo2; Zhu, Kehan1,3; Tian, Ziyang2,6; Wang, Haoyu1,3; Jia, Yulei2,6; Feng, Chunlan1; Qi, Luyao1,3; Tang, Wei1,3,6; Hu, Youhong2,4,5,6
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2025-02-05
卷号283页码:12
关键词NLRP3 inflammasome NEK7 NLRP3-NEK7 Inhibitors
ISSN号0223-5234
DOI10.1016/j.ejmech.2024.117125
英文摘要Aberrant activation of NLRP3 inflammasome is involved in various inflammatory diseases, making it a promising target for therapeutic intervention. NEK7, a member of the NIMA-related kinase (NEK) family, functions as a key NLRP3-binding protein and plays a crucial role in the regulation of NLRP3 inflammasome assembly and activation. Thus, disrupting NLRP3-NEK7 interactions by targeting NEK7 could be a promising strategy to inhibit the activation of NLRP3 inflammasome. In this work, a series of novel urea derivatives were designed and synthesized based on the reported NEK7 inhibitors. Among these, compound 23 exhibited potent activity against IL-1/3 release with low cytotoxicity. Moreover, compound 23 enhanced the thermal stability of NEK7 and disrupted the NLRP3-NEK7 interaction, thereby regulating NLRP3 inflammasome assembly.
WOS关键词NLRP3 INFLAMMASOME ; ACTIVATION ; PROTEIN ; KINASE
WOS研究方向Pharmacology & Pharmacy
WOS记录号WOS:001377930400001
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/315055]  
专题新药研究国家重点实验室
通讯作者Tang, Wei; Hu, Youhong
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Lab Antiinflammat & Immunopharmacol, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
2.UCAS, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, 1 Xiangshanzhi Rd, Hangzhou 310024, Peoples R China
3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 ZuChongZhi Rd, Shanghai 201203, Peoples R China
5.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, 198 East Binhai Rd, Yantai 264117, Shandong, Peoples R China
6.Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 110039, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Leibo,Zhu, Kehan,Tian, Ziyang,et al. Discovery of novel biaryl urea derivatives against IL-1/3 release with low toxicity based on NEK7 inhibitor[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2025,283:12.
APA Wang, Leibo.,Zhu, Kehan.,Tian, Ziyang.,Wang, Haoyu.,Jia, Yulei.,...&Hu, Youhong.(2025).Discovery of novel biaryl urea derivatives against IL-1/3 release with low toxicity based on NEK7 inhibitor.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,283,12.
MLA Wang, Leibo,et al."Discovery of novel biaryl urea derivatives against IL-1/3 release with low toxicity based on NEK7 inhibitor".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 283(2025):12.

入库方式： OAI收割

来源：上海药物研究所

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