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Literature DB >> 16706681

FXR: a target for cholestatic syndromes?

Abstract

The nuclear farnesoid X receptor (FXR) plays a pivotal role in maintaining bile acid homeostasis by regulating key genes involved in bile acid synthesis, metabolism and transport, including CYP7A1, UGT2B4, BSEP, MDR3, MRP2, ASBT, I-BABP, NTCP and OSTalpha-OSTbeta in humans. Altered expression or malfunction of these genes has been described in patients with cholestatic liver diseases. This review examines the rationale for the use of FXR ligand therapy in various cholestatic liver disorders and includes potential concerns.

Entities: Chemical Disease Gene Species

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Year: 2006 PMID： 16706681 DOI： 10.1517/14728222.10.3.409

Source DB: PubMed Journal: Expert Opin Ther Targets ISSN： 1472-8222 Impact factor: 6.902

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Cited

11 in total

1. Intestinal FXR-mediated FGF15 production contributes to diurnal control of hepatic bile acid synthesis in mice.

Authors: Johanna H M Stroeve; Gemma Brufau; Frans Stellaard; Frank J Gonzalez; Bart Staels; Folkert Kuipers
Journal: Lab Invest Date: 2010-06-07 Impact factor: 5.662

Review 2. New perspectives for the treatment of cholestasis: lessons from basic science applied clinically.

Authors: James L Boyer
Journal: J Hepatol Date: 2006-12-18 Impact factor: 25.083

3. The farnesoid X receptor regulates transcription of 3beta-hydroxysteroid dehydrogenase type 2 in human adrenal cells.

Authors: Yewei Xing; Karla Saner-Amigh; Yasuhiro Nakamura; Margaret M Hinshelwood; Bruce R Carr; J Ian Mason; William E Rainey
Journal: Mol Cell Endocrinol Date: 2008-11-18 Impact factor: 4.102

4. Targeting the Farnesoid X Receptor in Patients With Cholestatic Liver Disease.

Authors: Cynthia Levy
Journal: Gastroenterol Hepatol (N Y) Date: 2016-04

5. Blinded evaluation of farnesoid X receptor (FXR) ligands binding using molecular docking and free energy calculations.

Authors: Edithe Selwa; Eddy Elisée; Agustin Zavala; Bogdan I Iorga
Journal: J Comput Aided Mol Des Date: 2017-09-02 Impact factor: 3.686

10. Ethanolic extract of Commiphora mukul gum resin attenuates streptozotocin-induced alterations in carbohydrate and lipid metabolism in rats.

Authors: B Ramesh; R Karuna; S Sreenivasa Reddy; G Sudhakara; D Saralakumari
Journal: EXCLI J Date: 2013-06-19 Impact factor: 4.068

FXR: a target for cholestatic syndromes?

1. Intestinal FXR-mediated FGF15 production contributes to diurnal control of hepatic bile acid synthesis in mice.

Review 2. New perspectives for the treatment of cholestasis: lessons from basic science applied clinically.

3. The farnesoid X receptor regulates transcription of 3beta-hydroxysteroid dehydrogenase type 2 in human adrenal cells.

4. Targeting the Farnesoid X Receptor in Patients With Cholestatic Liver Disease.

5. Blinded evaluation of farnesoid X receptor (FXR) ligands binding using molecular docking and free energy calculations.

6. Baohuoside I inhibits FXR signaling pathway to interfere with bile acid homeostasis via targeting ER α degradation.

Review 7. Biosynthesis and trafficking of the bile salt export pump, BSEP: therapeutic implications of BSEP mutations.

Review 8. Epigenomic regulation of bile acid metabolism: emerging role of transcriptional cofactors.

9. BRD4 inhibition and FXR activation, individually beneficial in cholestasis, are antagonistic in combination.

10. Ethanolic extract of Commiphora mukul gum resin attenuates streptozotocin-induced alterations in carbohydrate and lipid metabolism in rats.