HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter

doi:10.1016/j.metabol.2018.03.016

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	HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter
	Xu, Xin 3,4; Shi, Xiaofan 3,4; Chen, Yidi 2; Zhou, Tingting 3,4; Wang, Jiaying 2; Xu, Xing 1; Chen, Lili3,4 ; Hu, Lihong 2,3,4; Shen, Xu2,3,4
刊名	Metabolism: clinical and experimental
	2018-08
卷号	85 页码:126-138
ISSN号	1532-8600
DOI	10.1016/j.metabol.2018.03.016
文献子类	Article
英文摘要	Farnesoid X receptor (FXR) as a member of nuclear receptor is tightly associated with glucose metabolism. Accumulated evidence has addressed the potential of FXR antagonist in the treatment of type 2 diabetes mellitus (T2DM), although the related mechanisms remain unclear. Here, we determined a specific FXR antagonist HS218 (N-benzyl-N-(3-(tert-butyl)-4-hydroxyphenyl)-2,4-dichlorobenzamide), which exhibited high activities in suppressing gluconeogenesis and ameliorating glucose homeostasis in db/db and HFD/STZ-induced T2DM mice. We would like to investigate the mechanisms underlying FXR antagonism in the regulation of gluconeogenesis by using HS218 as a probe.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266319]
专题	上海中药现代化研究中心药理学第三研究室
通讯作者	Hu, Lihong; Shen, Xu
作者单位	1.Shanghai Key Laboratory for Bone and Joint Diseases, Shanghai Institute of Traumatology and Orthopaedics, Shanghai Ruijin Hospital, Shanghai Jiaotong University School of Medicine, Shanghai 200025, China 2.State Key Laboratory Cultivation Base for TCM Quality and Efficacy, School of Medicine and Life Sciences, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China; 3.University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, China; 4.Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 555 Zuchongzhi Road, Shanghai 201203, China;
推荐引用方式 GB/T 7714	Xu, Xin,Shi, Xiaofan,Chen, Yidi,et al. HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter[J]. Metabolism: clinical and experimental,2018,85:126-138.
APA	Xu, Xin.,Shi, Xiaofan.,Chen, Yidi.,Zhou, Tingting.,Wang, Jiaying.,...&Shen, Xu.(2018).HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter.Metabolism: clinical and experimental,85,126-138.
MLA	Xu, Xin,et al."HS218 as an FXR antagonist suppresses gluconeogenesis by inhibiting FXR binding to PGC-1α promoter".Metabolism: clinical and experimental 85(2018):126-138.