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Characterization of a small-molecule inhibitor targeting NEMO/IKK beta to suppress colorectal cancer growth

文献类型：期刊论文

作者Yu, Zhenlong2,3; Gao, Jian4; Zhang, Xiaolei5; Peng, Yulin2,3; Wei, Wenlong6; Xu, Jianrong1; Li, Zhenwei6; Wang, Chao3; Zhou, Meirong3; Tian, Xiangge2
刊名SIGNAL TRANSDUCTION AND TARGETED THERAPY
出版日期2022-03-09
卷号7期号:1页码:13
ISSN号2095-9907
DOI10.1038/s41392-022-00888-1
通讯作者Ye, Mingliang(mingliang@dicp.ac.cn) ; Guo, De-an(daguo@simm.ac.cn) ; Ma, Xiaochi(maxc1978@163.com)
英文摘要NEMO/IKK beta complex is a central regulator of NF-kappa B signaling pathway, its dissociation has been considered to be an attractive therapeutic target. Herein, using a combined strategy of molecular pharmacological phenotyping, proteomics and bioinformatics analysis, Shikonin (SHK) is identified as a potential inhibitor of the IKK beta/NEMO complex. It destabilizes IKK beta/NEMO complex with IC50 of 174 nM, thereby significantly impairing the proliferation of colorectal cancer cells by suppressing the NF-kappa B pathway in vitro and in vivo. In addition, we also elucidated the potential target sites of SHK in the NEMO/IKK beta complex. Our study provides some new insights for the development of potent small-molecule PPI inhibitors.
WOS关键词NF-KAPPA-B ; IKK-BETA ; SELECTIVE-INHIBITION ; INFLAMMATION ; SHIKONIN ; ACTIVATION ; APOPTOSIS ; IMMUNITY ; PEPTIDE ; PATHWAY
资助项目National Natural Science Foundation of China[81930112] ; National Natural Science Foundation of China[82004089] ; National Key Research and Development Program of China[2018YFC1705900] ; National Key Research and Development Program of China[2020YFE0202200] ; Distinguished professor of Liaoning Province[XLYC2002008] ; Dalian Science and Technology Leading Talents Project[2019RD15]
WOS研究方向Biochemistry & Molecular Biology ; Cell Biology
语种英语
出版者SPRINGERNATURE
WOS记录号WOS:000766191100001
源URL[http://119.78.100.183/handle/2S10ELR8/300197]  
专题中国科学院上海药物研究所
通讯作者Ye, Mingliang; Guo, De-an; Ma, Xiaochi
作者单位1.Shanghai Univ Tradit Chinese Med, Acad Integrat Med, 1200 Cailun Rd, Shanghai 201203, Peoples R China
2.Dalian Med Univ, Affiliated Hosp 2, Pharmaceut Res Ctr, Dalian 116000, Peoples R China
3.Dalian Med Univ, Coll Pharm, Coll Inst Integrat Med, Dalian 116044, Peoples R China
4.Xuzhou Med Univ, Jiangsu Key Lab New Drug Res & Clin Pharm, Xuzhou 221004, Jiangsu, Peoples R China
5.Chinese Acad Sci, Dalian Inst Chem Phys, Natl Chromatog R&A Ctr, CAS Key Lab Separat Sci Analyt Chem, Dalian 116023, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Natl Engn Res Ctr TCM Standardizat Technol, Shanghai 201203, Peoples R China
7.Dalian Univ, Dept Neurol, Xinhua Hosp 1, Dalian 116021, Peoples R China
推荐引用方式
GB/T 7714		 Yu, Zhenlong,Gao, Jian,Zhang, Xiaolei,et al. Characterization of a small-molecule inhibitor targeting NEMO/IKK beta to suppress colorectal cancer growth[J]. SIGNAL TRANSDUCTION AND TARGETED THERAPY,2022,7(1):13.
APA Yu, Zhenlong.,Gao, Jian.,Zhang, Xiaolei.,Peng, Yulin.,Wei, Wenlong.,...&Ma, Xiaochi.(2022).Characterization of a small-molecule inhibitor targeting NEMO/IKK beta to suppress colorectal cancer growth.SIGNAL TRANSDUCTION AND TARGETED THERAPY,7(1),13.
MLA Yu, Zhenlong,et al."Characterization of a small-molecule inhibitor targeting NEMO/IKK beta to suppress colorectal cancer growth".SIGNAL TRANSDUCTION AND TARGETED THERAPY 7.1(2022):13.

入库方式： OAI收割

来源：上海药物研究所

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