A novel intestinal-restricted FXR agonist

Hong Wang; Zhou Zhao; Jiyu Zhou; Yitong Guo; Guangji Wang; Haiping Hao; Xiaowei Xu

doi:10.1016/j.bmcl.2017.06.003

A novel intestinal-restricted FXR agonist

Hong Wang
, Zhou Zhao
, Jiyu Zhou
, Yitong Guo
, Guangji Wang
, Haiping Hao
, Xiaowei Xu

China Pharmaceutical University

Research output: Contribution to journal › Article › peer-review

31 Scopus citations

Abstract

In this study, a new intestinal-restricted FXR agonist named fexaramine-3 (Fex-3) was developed and investigated both in vitro and in vivo. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1 which is involved in bile acids syntheses better than the reported intestinal-restricted FXR agonist fexaramine (Fex). We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. And the study of utilizing Fex-3 to reduce obesity was undergoing.

Original language	English
Pages (from-to)	3386-3390
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2017.06.003
State	Published - 2017
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Agonist
Farnesoid X receptor
Fexaramine
Intestinal-restricted

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10.1016/j.bmcl.2017.06.003

Cite this

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title = "A novel intestinal-restricted FXR agonist",

abstract = "In this study, a new intestinal-restricted FXR agonist named fexaramine-3 (Fex-3) was developed and investigated both in vitro and in vivo. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1 which is involved in bile acids syntheses better than the reported intestinal-restricted FXR agonist fexaramine (Fex). We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. And the study of utilizing Fex-3 to reduce obesity was undergoing.",

keywords = "Agonist, Farnesoid X receptor, Fexaramine, Intestinal-restricted",

author = "Hong Wang and Zhou Zhao and Jiyu Zhou and Yitong Guo and Guangji Wang and Haiping Hao and Xiaowei Xu",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Ltd",

year = "2017",

doi = "10.1016/j.bmcl.2017.06.003",

language = "英语",

volume = "27",

pages = "3386--3390",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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}

TY - JOUR

T1 - A novel intestinal-restricted FXR agonist

AU - Wang, Hong

AU - Zhao, Zhou

AU - Zhou, Jiyu

AU - Guo, Yitong

AU - Wang, Guangji

AU - Hao, Haiping

AU - Xu, Xiaowei

PY - 2017

Y1 - 2017

N2 - In this study, a new intestinal-restricted FXR agonist named fexaramine-3 (Fex-3) was developed and investigated both in vitro and in vivo. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1 which is involved in bile acids syntheses better than the reported intestinal-restricted FXR agonist fexaramine (Fex). We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. And the study of utilizing Fex-3 to reduce obesity was undergoing.

AB - In this study, a new intestinal-restricted FXR agonist named fexaramine-3 (Fex-3) was developed and investigated both in vitro and in vivo. Fex-3 could selectively activate intestinal FXR and promote the expression of BSEP and SHP while suppressing CYP7A1 which is involved in bile acids syntheses better than the reported intestinal-restricted FXR agonist fexaramine (Fex). We demonstrated that Fex-3 targeted on FXR in ileum and has better selectivity than Fex. And the study of utilizing Fex-3 to reduce obesity was undergoing.

KW - Agonist

KW - Farnesoid X receptor

KW - Fexaramine

KW - Intestinal-restricted

UR - https://www.scopus.com/pages/publications/85020835910

U2 - 10.1016/j.bmcl.2017.06.003

DO - 10.1016/j.bmcl.2017.06.003

M3 - 文章

C2 - 28629595

AN - SCOPUS:85020835910

SN - 0960-894X

VL - 27

SP - 3386

EP - 3390

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

A novel intestinal-restricted FXR agonist

Abstract

UN SDGs

Keywords

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