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Discovery of isoindoline-2(1H)-carboxamide STING inhibitors as anti-inflammatory agents

文献类型：期刊论文

作者Zhou, Xiaoqian2,3,4; Zang, Shumin1,5; Yao, Shanyan2; Zhou, Hongfei2,5; Wang, Xiyuan1; Geng, Meiyu1,5,6; Zhan, Zhengsheng2,5; Xie, Zuoquan1,5; Duan, Wenhu2,5
刊名MOLECULAR DIVERSITY
出版日期2025-12-11
页码13
关键词Isoindoline-2(1H)-carboxamide Stimulator of interferon genes SAR Inhibitors
ISSN号1381-1991
DOI10.1007/s11030-025-11424-y
英文摘要STING (stimulator of interferon genes) is an endoplasmic reticulum-resident membrane-spanning protein that is widely expressed in mammalian cells and functions as a central regulator for the innate immunity. Aberrant activation of the STING axis due to loss-of-function or gain-of-function mutation leads to various autoimmune and autoinflammatory disorders such as Aicardi-Gouti & egrave;res syndrome, systemic lupus erythematosus, and STING-associated vasculopathy with onset in infancy. Here we report the design, synthesis, and structure-activity relationship (SAR) of the isoindoline-2(1H)-carboxamide STING inhibitors. SAR study allowed us to identify compound 3b as a potent STING inhibitor with human- and mouse-STING inhibitory IC50 values of 6.2 and 12.5 nM, respectively. It also markedly suppressed the activation of the STING pathway in both human and murine cells. Furthermore, compound 3b exhibited preferable in vivo protective efficacy against cisplatin-induced acute kidney injury.
WOS关键词LIGAND
资助项目Shanghai Institute of Materia Medica, Chinese Academy of Sciences[SIMM0320231002] ; Shandong Laboratory Program[SYS202205]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001635929000001
出版者SPRINGER
源URL[http://119.78.100.183/handle/2S10ELR8/322336]  
专题国家级研究中心_原创新药研究全国重点实验室
通讯作者Zhan, Zhengsheng; Xie, Zuoquan; Duan, Wenhu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Small Mol Drug Res Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
3.Lingang Lab, Shanghai 200031, Peoples R China
4.ShanghaiTech Univ, Sch Phys Sci & Technol, Shanghai 201210, Peoples R China
5.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
6.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
推荐引用方式
GB/T 7714		 Zhou, Xiaoqian,Zang, Shumin,Yao, Shanyan,et al. Discovery of isoindoline-2(1H)-carboxamide STING inhibitors as anti-inflammatory agents[J]. MOLECULAR DIVERSITY,2025:13.
APA Zhou, Xiaoqian.,Zang, Shumin.,Yao, Shanyan.,Zhou, Hongfei.,Wang, Xiyuan.,...&Duan, Wenhu.(2025).Discovery of isoindoline-2(1H)-carboxamide STING inhibitors as anti-inflammatory agents.MOLECULAR DIVERSITY,13.
MLA Zhou, Xiaoqian,et al."Discovery of isoindoline-2(1H)-carboxamide STING inhibitors as anti-inflammatory agents".MOLECULAR DIVERSITY (2025):13.

入库方式： OAI收割

来源：上海药物研究所

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