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Role of farnesoid X receptor in inflammation and resolution
Inflammation Research, 2014The aim of this paper is to review the developments of farnesoid X receptor (FXR) biology, its ligands, and various functions, in particular we discuss the anti-inflammatory and anti-fibrotic role in chronic inflammatory diseases.FXR is a ligand-dependent transcription factor belonging to the nuclear hormone receptor superfamily.
Firdose Begum, Shaik +2 more
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Progesterone Metabolites as Farnesoid X Receptor Inhibitors
Digestive Diseases, 2015Sulfated progesterone metabolites rise 100-fold in the third trimester of human pregnancy and have been shown to be elevated further in the gestational disorder intrahepatic cholestasis of pregnancy (ICP). Typical concentrations of progesterone sulfates range from 1 to 10 µmol/L in an uncomplicated pregnancy and rise to approximately 40 µmol/L in ICP ...
Abu-Hayyeh, Shadi, Williamson, Catherine
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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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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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Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor
Journal of Medicinal Chemistry, 2021Farnesoid X receptor (FXR) is an important regulator of bile acid, lipid, amino acid, and glucose homeostasis, hepatic inflammation, regeneration, and fibrosis. FXR has been recognized as a promising drug target for various metabolic diseases such as lipid disorders, nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and ...
Yuanying Fang +3 more
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On the Evolution of Bile Salts and the Farnesoid X Receptor in Vertebrates
Physiological and Biochemical Zoology, 2018In recent decades, our knowledge of bile salts has undergone a vast development, and bile salts are now known not only for their detergent properties that aid in the absorption of dietary lipids but also for their interaction with specific nuclear and membrane receptors. In particular, it has been realized that the response of the farnesoid X receptor (
Frisch, Kim; id_orcid 0000-0001-9691-2853 +1 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 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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Oleanolic acid is a selective farnesoid X receptor modulator
Phytotherapy Research, 2009AbstractOleanolic acid (OA) is an ingredient found in some Traditional Chinese Medicine remedies for treating liver ailments. Bile acid biosynthesis and catabolism are in part controlled in the liver by transcription factor farnesoid X receptor (FXR). It was hypothesized that OA may act through FXR to mediate some of its beneficial health effects.
Wenming, Liu, Chiwai, Wong
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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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