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Role of farnesoid X receptor in cholestasis
Journal of Digestive Diseases, 2016The nuclear receptor farnesoid X receptor (FXR) plays an important role in physiological bile acid synthesis, secretion and transport. Defects of FXR regulation in these processes can cause cholestasis and subsequent pathological changes. FXR regulates the synthesis and uptake of bile acid via enzymes.
Zhi Qing, Yuan, Ke Wei, Li
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Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis
Drug Discovery Today, 2012Nonalcoholic fatty liver disease (NAFLD) is a highly prevalent chronic liver condition evolving in a proportion of patients into nonalcoholic steatohepatitis (NASH), an aggressive form of NAFLD associated with increased cardiovascular mortality and significant risk of progressive liver disease, including fibrosis, cirrhosis and hepatocellular carcinoma.
Luciano, Adorini +2 more
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Liver X Receptor and Farnesoid X Receptor as Therapeutic Targets
The American Journal of Cardiology, 2007Despite the success of existing therapies, new therapies targeted toward dyslipidemia are still needed. Liver X receptor (LXR) and farnesoid X receptor (FXR) represent 2 very different attractive targets for new therapeutic development. LXR is a nuclear receptor that primarily acts to rid cells and the body of excess cholesterol. LXR agonists have been
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Farnesoid X receptor antagonist exacerbates dyslipidemia in mice
Pharmacological Reports, 2018The effects of farnesoid X receptor (FXR) antagonists on plasma lipid profile in mice have not been investigated thus far. The aim of this study was to investigate the antidyslipidemic effects of an FXR antagonist in dyslipidemic mice, and to clarify the mechanisms underlying the lipid modulatory effect.Compound-T0 (1-100 mg/kg) was orally administered
Yuichiro, Amano +4 more
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Expert opinion on investigational drugs, 2004
Bile acids are end products of cholesterol metabolism. They are exclusively synthesised by the liver and subsequently secreted via the bile duct into the intestine to facilitate the absorption of dietary fat and fat-soluble vitamins. Nuclear receptors are ligand-activated transcription factors.
Claudel, T +3 more
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Bile acids are end products of cholesterol metabolism. They are exclusively synthesised by the liver and subsequently secreted via the bile duct into the intestine to facilitate the absorption of dietary fat and fat-soluble vitamins. Nuclear receptors are ligand-activated transcription factors.
Claudel, T +3 more
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Expert Opinion on Drug Discovery, 2013
Farnesoid X receptor (FXR) is an ascending target for metabolic and inflammatory diseases. As a nuclear receptor, FXR exhibits many physiological effects in transcription control of several genes. Therefore, the development of synthetic FXR ligands requires elaborate in vitro test systems to characterize novel ligands and to estimate their in vivo ...
Daniel, Merk +2 more
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Farnesoid X receptor (FXR) is an ascending target for metabolic and inflammatory diseases. As a nuclear receptor, FXR exhibits many physiological effects in transcription control of several genes. Therefore, the development of synthetic FXR ligands requires elaborate in vitro test systems to characterize novel ligands and to estimate their in vivo ...
Daniel, Merk +2 more
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Farnesoid X receptor agonists in biliary tract disease
Current Opinion in Gastroenterology, 2009The farnesoid X receptor (FXR) is a member of ligand-activated nuclear receptor superfamily. FXR is a bile sensor and is part of a complex network of nuclear receptors that includes also the constitutive androstane receptor and the pregnane X receptor.
FIORUCCI, Stefano, BALDELLI, Franco
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Molecular Nutrition & Food Research, 2019
SCOPE Trimethylamine N-oxide (TMAO), the metabolite of choline generated by gut microbiota, is associated with nonalcoholic fatty liver disease (NAFLD) and could influence bile acid (BA) metabolism.
Xu-ying Tan +9 more
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SCOPE Trimethylamine N-oxide (TMAO), the metabolite of choline generated by gut microbiota, is associated with nonalcoholic fatty liver disease (NAFLD) and could influence bile acid (BA) metabolism.
Xu-ying Tan +9 more
semanticscholar +1 more source
Farnesoid X receptor modulators: a patent review
Expert Opinion on Therapeutic Patents, 2010The farnesoid X receptor (FXR) is a key regulator of cholesterol homeostasis, triglyceride synthesis and lipogenesis. Given some patients' inability to tolerate existing medications, such as the statins, for cholesterol reduction, there is a pressing need for additional medicines to treat dyslipidemia.
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