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
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| 刊名 | ACS OMEGA
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| 出版日期 | 2022-05-24 |
| 卷号 | 7期号:20页码:17401-17405 |
| ISSN号 | 2470-1343 |
| DOI | 10.1021/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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