Results 81 to 90 of about 2,458 (158)

Targeting the transsulfuration-H2S pathway by FXR and GPBAR1 ligands in the treatment of portal hypertension

, 2016
Cirrhosis is a end-stage disease of the liver in which fibrogenesis, angiogenesis and distortion of intrahepatic microcirculation lead to increased intrahepatic resistance to portal blood flow, a condition known as portal hypertension.
FIORUCCI, Stefano
core   +1 more source

The G-protein-coupled bile acid receptor Gpbar1 (TGR5) inhibits gastric inflammation through antagonizing NF-kB signaling pathway

Frontiers in Pharmacology, 2015
Gpbar1 (TGR5), a membrane-bound bile acid receptor, is well known for its roles in regulation of energy homeostasis and glucose metabolism. Here we show that mice lacking TGR5 were much more susceptible to lipopolysaccharide (LPS)-induced acute gastric ...
Cong eGuo, Hui eQi, Yingjie eYu, Qiqi eZhang, Jia eSu, Donna eYu, Wendong eHuang, Wei-Dong eChen, YAN-DONG eWANG   +8 more
doaj   +1 more source

Hydrophobic bile salts inhibit gallbladder smooth muscle function via stimulation of GPBAR1 receptors and activation of KATP channels

, 2010
Hydrophobic bile salts are thought to contribute to the disruption of gallbladder smooth muscle (GBSM) function that occurs in gallstone disease, but their mechanism of action is unknown. The current study was undertaken to determine how hydrophobic bile
Godfrey, Cody, Mawe, Gary M., Watson, Conall A., Onesmo B. Balemba, Conall A. Watson, Gary M. Mawe, Balemba, Onesmo B., Nelson, Mark T.; id_orcid, Carlos U. Corvera, Corvera, Carlos U., Lavoie, Brigitte, Cody Godfrey, Vassileva, Galya, Galya Vassileva, Mark T. Nelson, Brigitte Lavoie   +15 more
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Discovery of potent dual GPBAR1/CysLT1R modulator for the treatment of metabolic fatty liver disease

, 2021
Nonalcoholic steatohepatitis (NASH) is a highly prevalent human disorder for which no approved treatment is currently available. Several mediators are involved in the development of liver inflammation and fibrosis in NAFLD/NASH patients.
marchianò, S (via Mendeley Data)
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Crosstalk between FXR and TGR5 controls glucagon-like peptide 1 secretion to maintain glycemic homeostasis

Laboratory Animal Research, 2018
Though bile acids have been well known as digestive juice, recent studies have demonstrated that bile acids bind to their endogenous receptors, including Farnesoid X receptor (FXR) and G protein-coupled bile acid receptor 1 (GPBAR1; TGR5) and serve as ...
Hyeonhui Kim, Sungsoon Fang
doaj   +1 more source

Exploring inflammatory bowel disease therapy targets through druggability genes: a Mendelian randomization study

Frontiers in Immunology
BackgroundInflammatory bowel disease is an incurable group of recurrent inflammatory diseases of the intestine. Mendelian randomization has been utilized in the development of drugs for disease treatment, including the therapeutic targets for IBD that ...
Shuangjing Zhu, Yunzhi Lin, Zhen Ding
doaj   +1 more source

The G Protein-Coupled Bile Acid Receptor TGR5 (Gpbar1) Modulates Endothelin-1 Signaling in Liver

Cells, 2019
TGR5 (Gpbar1) is a G protein-coupled receptor responsive to bile acids (BAs), which is expressed in different non-parenchymal cells of the liver, including biliary epithelial cells, liver-resident macrophages, sinusoidal endothelial cells (LSECs), and ...
Caroline Klindt, Maria Reich, Birte Hellwig, Jan Stindt, Jörg Rahnenführer, Jan G. Hengstler, Karl Köhrer, Kristina Schoonjans, Dieter Häussinger, Verena Keitel   +9 more
doaj   +1 more source

Structure-based drug design targeting the cell membrane receptor GPBAR1: exploiting the bile acid scaffold towards selective agonism

, 2015
Bile acids can regulate nutrient metabolism through the activation of the cell membrane receptor GPBAR1 and the nuclear receptor FXR. Developing an exogenous control over these receptors represents an attractive strategy for the treatment of ...
NOVELLINO, ETTORE, Fiorucci, Stefano, ZAMPELLA, ANGELA, SEPE, VALENTINA, FESTA, CARMEN, Di Leva, Francesco Saverio, LIMONGELLI, VITTORIO, Renga, Barbara   +7 more
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Effect of betulinic acid on ANIT induced cholestasis in GPBAR1^+/+ and-^/- mice.

, 2015
GPBAR1+/+ and GPBAR1-/- mice were administered with ANIT or with the combination of ANIT plus betulinic acid for 5 days. (A) Body weight; (B) Scratching test was performed at day 5.
Barbara Renga (134135), Claudio D’Amore (770255), Angela Zampella (186821), Valentina Sepe (186788), Stefano Fiorucci (134151), Sabrina Cipriani (134132), Antonio Angelo De Tursi (770257), Maria Chiara Monti (186804), Michele Simonetti (770256), Adriana Carino (277117)   +9 more
core   +1 more source

A gut–brain axis regulating glucose metabolism mediated by bile acids and competitive fibroblast growth factor actions at the hypothalamus

Molecular Metabolism, 2018
Objective: Bile acids have been implicated as important regulators of glucose metabolism via activation of FXR and GPBAR1. We have previously shown that FGF19 can modulate glucose handling by suppressing the activity of hypothalamic AGRP/NPY neurons.
Shunmei Liu, Genevieve Marcelin, Clemence Blouet, Jae Hoon Jeong, Young-Hwan Jo, Gary J. Schwartz, Streamson Chua, Jr.   +6 more
doaj   +1 more source