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

scholarly journals Intestinal Farnesoid X Receptor and Takeda G Protein Couple Receptor 5 Signaling in Metabolic Regulation

2017 ◽  
Vol 35 (3) ◽  
pp. 241-245 ◽  
Author(s):  
John Y.L. Chiang ◽  
Preeti Pathak ◽  
Hailiang Liu ◽  
Ajay Donepudi ◽  
Jessica Ferrell ◽  
...  
Keyword(s):  
Bile Acid ◽  
G Protein ◽  
Metabolic Regulation ◽  
Therapeutic Potential ◽  
Critical Role ◽  
Hepatic Metabolism ◽  
Farnesoid X Receptor ◽  
Alcoholic Fatty Liver ◽  
Acid Receptor ◽  
Bile Acid Receptor

Bile acids play a critical role in the regulation of glucose, lipid and energy metabolisms by activating the nuclear bile acid receptor farnesoid X receptor (FXR) and membrane G protein-coupled bile acid receptor-1 (aka takeda G protein couple receptor 5, TGR5) signaling. Paradoxical roles of FXR in the regulation of glucose and lipid metabolism and metabolic disorder have been reported recently. The activation or inhibition of intestinal FXR signaling has been shown to improve insulin and glucose sensitivity and energy metabolism to prevent diabetes, obesity and non-alcoholic fatty liver disease (NAFLD). TGR5 has an anti-inflammatory function in the intestine and stimulates glucagon-like peptide-1 (GLP-1) secretion in the intestine to stimulate insulin secretion from the pancreas. The role of TGR5 in metabolism and metabolic regulation is not clear and warrants further study. FXR and TGR5 are co-expressed in the ileum and colon. These 2 bile acid-activated receptors may cooperate to stimulate GLP-1 secretion and improve hepatic metabolism. FXR and TGR5 dual agonists may have therapeutic potential for treating diabetes and NAFLD.

Exploitation of Cholane Scaffold for the Discovery of Potent and Selective Farnesoid X Receptor (FXR) and G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1) Ligands

2014 ◽  
Vol 57 (20) ◽  
pp. 8477-8495 ◽  
Author(s):  
Carmen Festa ◽  
Barbara Renga ◽  
Claudio D’Amore ◽  
Valentina Sepe ◽  
Claudia Finamore ◽  
...  
Keyword(s):  
Bile Acid ◽  
G Protein ◽  
Farnesoid X Receptor ◽  
Acid Receptor ◽  
Bile Acid Receptor ◽  
G Protein Coupled

scholarly journals The G protein coupled bile acid receptor TGR5 (Gpbar1) modulates endothelin-1 signaling in liver

2020 ◽  
Author(s):  
C Klindt ◽  
M Reich ◽  
B Hellweg ◽  
J Stindt ◽  
J Rahnenführer ◽  
...  
Keyword(s):  
Bile Acid ◽  
G Protein ◽  
Acid Receptor ◽  
Endothelin 1 ◽  
Bile Acid Receptor ◽  
G Protein Coupled

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
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