scholarly journals Dual Targeting of Bile Acid Receptor‐1 (TGR5) and Farnesoid X Receptor (FXR) Prevents Estrogen‐Dependent Bone Loss in Mice

2018 ◽  
Author(s):  
Zhenxi Li ◽  
Jinping Huang ◽  
Fanhua Wang ◽  
Wenjun Li ◽  
Xian Wu ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bone Loss ◽  
Farnesoid X Receptor ◽  
Acid Receptor ◽  
Dual Targeting ◽  
Bile Acid Receptor

Glucose sensing O-GlcNAcylation pathway regulates the nuclear bile acid receptor farnesoid X receptor (FXR)

Hepatology ◽  
2014 ◽  
Vol 59 (5) ◽  
pp. 2022-2033 ◽  
Author(s):  
Wahiba Berrabah ◽  
Pierrette Aumercier ◽  
Céline Gheeraert ◽  
Hélène Dehondt ◽  
Emmanuel Bouchaert ◽  
...  
Keyword(s):  
Bile Acid ◽  
Glucose Sensing ◽  
Farnesoid X Receptor ◽  
Acid Receptor ◽  
Bile Acid Receptor

scholarly journals Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1043 ◽  
Author(s):  
Claudia Finamore ◽  
Giuliana Baronissi ◽  
Silvia Marchianò ◽  
Francesco Di Leva ◽  
Adriana Carino ◽  
...  
Keyword(s):  
Bile Acid ◽  
Metabolic Disorders ◽  
Farnesoid X Receptor ◽  
Pharmacological Characterization ◽  
Acid Receptor ◽  
Pharmacokinetic Properties ◽  
Docking Calculations ◽  
Bile Acid Receptor ◽  
Receptor Modulators

As a cellular bile acid sensor, farnesoid X receptor (FXR) and the membrane G-coupled receptor (GPBAR1) participate in maintaining bile acid, lipid, and glucose homeostasis. To date, several selective and dual agonists have been developed as promising pharmacological approach to metabolic disorders, with most of them possessing an acidic conjugable function that might compromise their pharmacokinetic distribution. Here, guided by docking calculations, nonacidic 6-ethyl cholane derivatives have been prepared. In vitro pharmacological characterization resulted in the identification of bile acid receptor modulators with improved pharmacokinetic properties.

Neutraceutical Targeting of the Bile Acid Receptor, Farnesoid X Receptor, for Intestinal Disease

2020 ◽  
Vol 34 (S1) ◽  
pp. 1-1
Author(s):  
Ciara M. Fallon ◽  
Omprakash Edupuganti ◽  
Natalia K. Lajczak-McGinley ◽  
Helen Sheridan ◽  
Stephen J. Keely
Keyword(s):  
Bile Acid ◽  
Farnesoid X Receptor ◽  
Intestinal Disease ◽  
Acid Receptor ◽  
Bile Acid Receptor

scholarly journals The nuclear bile acid receptor FXR is activated by PGC-1α in a ligand-dependent manner

2004 ◽  
Vol 382 (3) ◽  
pp. 913-921 ◽  
Author(s):  
Eiko KANAYA ◽  
Takuma SHIRAKI ◽  
Hisato JINGAMI
Keyword(s):  
Bile Acid ◽  
Ligand Binding ◽  
Transcriptional Activation ◽  
Expression System ◽  
Binding Domain ◽  
Ligand Binding Domain ◽  
Farnesoid X Receptor ◽  
Dependent Manner ◽  
Acid Receptor ◽  
Bile Acid Receptor

The nuclear bile acid receptor FXR (farnesoid X receptor) is one of the key factors that suppress bile acid biosynthesis in the liver. PGC-1α [PPARγ (peroxisome-proliferator-activated receptor γ) co-activator-1α] is known to control energy homoeostasis in adipose tissue, skeletal muscle and liver. We performed cell-based reporter assays using the expression system of a GAL4–FXR chimaera, the ligand-binding domain of FXR fused to the DNA-binding domain of yeast GAL4, to find the co-activators for FXR. We found that the transcriptional activation of a reporter plasmid by a GAL4–FXR chimaera was strongly enhanced by PGC-1α, in a ligand-dependent manner. Transcriptional activation of the SHP (small heterodimer partner) gene by the FXR–RXRα (retinoid X receptor α) heterodimer was also enhanced by PGC-1α in the presence of CDCA (chenodeoxycholic acid). Co-immunoprecipitation and pull-down studies using glutathione S-transferase–PGC-1α fusion proteins revealed that the ligand-binding domain of FXR binds PGC-1α in a ligand-influenced manner both in vivo and in vitro. Furthermore, our studies revealed that SHP represses its own transcription, and the addition of excess amounts of PGC-1α can overcome the inhibitory effect of SHP. These observations indicate that PGC-1α mediates the ligand-dependent activation of FXR and transcription of SHP gene.

scholarly journals Intestine farnesoid X receptor agonist and the gut microbiota activate G‐protein bile acid receptor‐1 signaling to improve metabolism

Hepatology ◽  
2018 ◽  
Vol 68 (4) ◽  
pp. 1574-1588 ◽  
Author(s):  
Preeti Pathak ◽  
Cen Xie ◽  
Robert G. Nichols ◽  
Jessica M. Ferrell ◽  
Shannon Boehme ◽  
...  
Keyword(s):  
Bile Acid ◽  
Gut Microbiota ◽  
G Protein ◽  
Receptor Agonist ◽  
Farnesoid X Receptor ◽  
Acid Receptor ◽  
Bile Acid Receptor

Regulation of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by the Nuclear Bile Acid Receptor, Farnesoid X Receptor

2020 ◽  
Vol 34 (S1) ◽  
pp. 1-1
Author(s):  
Jessica S. Smyth ◽  
Anchalin Bussayajirapong ◽  
Natalia K. Lajczak-McGinley ◽  
Jennifer Foulke-Abel ◽  
Mark Donowitz ◽  
...  
Keyword(s):  
Cystic Fibrosis ◽  
Bile Acid ◽  
Farnesoid X Receptor ◽  
Transmembrane Conductance Regulator ◽  
Transmembrane Conductance ◽  
Acid Receptor ◽  
Bile Acid Receptor ◽  
Cystic Fibrosis Transmembrane
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