中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists

文献类型:期刊论文

作者Zhou, Jia-Xu1,2; Li, Cui-Na2; Liu, Ya-Meng2; Lin, Su-Qin3; Wang, Ying2; Xie, Cen2; Nan, Fa-Jun1,2,4
刊名ACS OMEGA
出版日期2022-05-24
卷号7期号:20页码:17401-17405
ISSN号2470-1343
DOI10.1021/acsomega.2c01567
文献子类Article
英文摘要The farnesoid X receptor (FXR) plays an important role in the regulation of bile acid, lipid, and glucose homeostasis. Recent findings have shown that the inhibition of FXR is beneficial to improvement of related metabolic diseases and cholestasis. In the present work, 9,11-seco-cholesterol derivatives were designed and synthesized by cleaving the C ring of cholesterol and were identified as novel structures of FXR antagonists. Compound 9a displayed the best FXR antagonistic activity at the cellular level (IC50 = 4.6 mu M) and decreased the expression of the target genes of FXR in vivo.
WOS关键词FARNESOID-X-RECEPTOR ; NUCLEAR RECEPTOR ; BILE-ACIDS ; POTENT
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000834201100048
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/309344]  
专题新药研究国家重点实验室
通讯作者Xie, Cen; Nan, Fa-Jun
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210046, Peoples R China;
4.Bohai Rim Adv Res Inst Drug Discovery, Drug Discovery Shandong Lab, Yantai 264117, Shandong, Peoples R China
推荐引用方式
GB/T 7714
Zhou, Jia-Xu,Li, Cui-Na,Liu, Ya-Meng,et al. Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists[J]. ACS OMEGA,2022,7(20):17401-17405.
APA Zhou, Jia-Xu.,Li, Cui-Na.,Liu, Ya-Meng.,Lin, Su-Qin.,Wang, Ying.,...&Nan, Fa-Jun.(2022).Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists.ACS OMEGA,7(20),17401-17405.
MLA Zhou, Jia-Xu,et al."Discovery of 9,11-Seco-Cholesterol Derivatives as Novel FXR Antagonists".ACS OMEGA 7.20(2022):17401-17405.

入库方式: OAI收割

来源:上海药物研究所

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