Identification of potential dual agonists of FXR and TGR5 using e-pharmacophore based virtual screening

2015 ◽  
Vol 11 (5) ◽  
pp. 1305-1318 ◽  
Author(s):  
Thangaraj Sindhu ◽  
Pappu Srinivasan
Keyword(s):  
Bile Acid ◽  
Virtual Screening ◽  
Drug Development ◽  
G Protein ◽  
Farnesoid X Receptor ◽  
G Protein Coupled Receptor ◽  
Treatment Of Diabetes ◽  
Bile Acid Receptors ◽  
G Protein Coupled

Farnesoid X receptor and Takeda G-protein-coupled receptor-5 are well known bile acid receptors and act as promising targets for the drug development and treatment of diabetes.

scholarly journals Modulating G-Protein Coupled Receptor/G-Protein Signal Transduction by Small Molecules Suggested by Virtual Screening

2008 ◽  
Vol 51 (17) ◽  
pp. 5297-5303 ◽  
Author(s):  
Christina M. Taylor ◽  
Yaniv Barda ◽  
Oleg G. Kisselev ◽  
Garland R. Marshall
Keyword(s):  
Signal Transduction ◽  
Virtual Screening ◽  
Small Molecules ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Bile acid receptors FXR and TGR5 signaling in fatty liver diseases and therapy

2020 ◽  
Vol 318 (3) ◽  
pp. G554-G573 ◽  
Author(s):  
John Y. L. Chiang ◽  
Jessica M. Ferrell
Keyword(s):  
Bile Acid ◽  
Fatty Liver ◽  
Bile Acids ◽  
G Protein ◽  
Liver Diseases ◽  
Metabolic Diseases ◽  
Acid Synthesis ◽  
Bile Acid Synthesis ◽  
Bile Acid Receptors ◽  
G Protein Coupled

Bile acid synthesis is the most significant pathway for catabolism of cholesterol and for maintenance of whole body cholesterol homeostasis. Bile acids are physiological detergents that absorb, distribute, metabolize, and excrete nutrients, drugs, and xenobiotics. Bile acids also are signal molecules and metabolic integrators that activate nuclear farnesoid X receptor (FXR) and membrane Takeda G protein-coupled receptor 5 (TGR5; i.e., G protein-coupled bile acid receptor 1) to regulate glucose, lipid, and energy metabolism. The gut-to-liver axis plays a critical role in the transformation of primary bile acids to secondary bile acids, in the regulation of bile acid synthesis to maintain composition within the bile acid pool, and in the regulation of metabolic homeostasis to prevent hyperglycemia, dyslipidemia, obesity, and diabetes. High-fat and high-calorie diets, dysbiosis, alcohol, drugs, and disruption of sleep and circadian rhythms cause metabolic diseases, including alcoholic and nonalcoholic fatty liver diseases, obesity, diabetes, and cardiovascular disease. Bile acid-based drugs that target bile acid receptors are being developed for the treatment of metabolic diseases of the liver.

scholarly journals Deficiency of Both Farnesoid X Receptor and Takeda G Protein–Coupled Receptor 5 Exacerbated Liver Fibrosis in Mice

Hepatology ◽  
2019 ◽  
Vol 70 (3) ◽  
pp. 955-970 ◽  
Author(s):  
Jessica M. Ferrell ◽  
Preeti Pathak ◽  
Shannon Boehme ◽  
Tricia Gilliland ◽  
John Y. L. Chiang
Keyword(s):  
Liver Fibrosis ◽  
G Protein ◽  
Farnesoid X Receptor ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Dual Activation of the Bile Acid Nuclear Receptor FXR and G-Protein-Coupled Receptor TGR5 Protects Mice against Atherosclerosis

PLoS ONE ◽  
2014 ◽  
Vol 9 (9) ◽  
pp. e108270 ◽  
Author(s):  
Shinobu Miyazaki-Anzai ◽  
Masashi Masuda ◽  
Moshe Levi ◽  
Audrey L. Keenan ◽  
Makoto Miyazaki
Keyword(s):  
Bile Acid ◽  
G Protein ◽  
Nuclear Receptor ◽  
G Protein Coupled Receptor ◽  
Dual Activation ◽  
G Protein Coupled
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