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Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue 期刊论文

编号：

e1c30010-6fb2-4840-b240-7a38ed4ba9a6
作者：

Qiu, Yan#^[1]Sun, Yingmin#^[1]Xu, Danqing^[2];Yang, Yuanyuan^[1];Liu, Xiaojian^[1];Wei, Yuda^[1];Chen, Yanhao^[1];Feng, Zhuanghui^[1];Li, Shuang^[1];Reyadul Ferdous, Md^[1];Zhao, Yongxu^[1];Xu, Hongxi(徐宏喜)^[2,3]Lao, Yuanzhi(劳远至)*^[2,3]Ding, Qiurong*^[1,4]
语种：

英文
期刊：

EBIOMEDICINE ISSN：2352-3964 2018 年 37 卷 (344 - 355) ; NOV
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关键词：

Uncoupling protein 1 Brown adipose FDA-approved drug library Obesity Sutent
摘要：

Background: The pharmacological activation of thermogenesis in brown adipose tissue has long been considered promising strategies to treat obesity. However, identification of safe and effective agents remains a challenge. In this study, we addressed this challenge by developing a cellular system with a fluorescence readout, and applied in a high-throughput manner to screen for FDA-approved drugs that may activate endogenous UCP1 expression in adipocytes.
Methods: We have generated a Ucp1-2A-GFP reporter mouse, in which GFP intensity serves as a surrogate of the endogenous expression level of UCP1 protein; and immortalized brown adipocytes were derived from this mouse model and applied in drug screening. Candidate drugs were further tested in mouse models either fed with normal chow or high fat diet to induce obesity.
Findings: By using the cellular screening platform, we identified a group of FDA-approved drugs that can upregulate UCP1 expression in brown adipocyte, including previously known UCP1 activators and new candidate drugs. Further studies focusing on a previously unreported drug-sutent, revealed that sutent treatment could increase the energy expenditure and inhibit lipid synthesis in mouse adipose and liver tissues, resulting in improved metabolism and resistance to obesity.
Interpretation: This study offered an easy-to-use cellular screening system for UCP1 activators, and provided a candidate list of FDA-approved drugs that can potentially treat obesity. Further study of these candidates may shed new light on the drug discovery towards obesity. (C) 2018 The Authors. Published by Elsevier B.V.
推荐引用方式
GB/T 7714：

Qiu Yan,Sun Yingmin,Xu Danqing, et al. Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue [J].EBIOMEDICINE,2018,37:344-355.
APA：

Qiu Yan,Sun Yingmin,Xu Danqing,Yang Yuanyuan,&Ding Qiurong.(2018).Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue .EBIOMEDICINE,37:344-355.
MLA：

Qiu Yan, et al. "Screening of FDA-approved drugs identifies sutent as a modulator of UCP1 expression in brown adipose tissue" .EBIOMEDICINE 37(2018):344-355.
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