Journal ArticleDOI
Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease.
Sunder Mudaliar,Robert R. Henry,Arun J. Sanyal,Linda Morrow,Hanns-Ulrich Marschall,Mark Kipnes,Luciano Adorini,Cathi Sciacca,Paul Clopton,E. Castelloe,Paul Dillon,Mark Pruzanski,David Shapiro +12 more
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TLDR
Administration of 25 or 50 mg OCA for 6 weeks was well tolerated, increased insulin sensitivity, and reduced markers of liver inflammation and fibrosis in patients with type 2 diabetes mellitus and nonalcoholic fatty liver disease.About:
This article is published in Gastroenterology.The article was published on 2013-09-01. It has received 794 citations till now. The article focuses on the topics: Insulin resistance & Nonalcoholic fatty liver disease.read more
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Journal ArticleDOI
Reciprocal regulation of farnesoid X receptor α activity and hepatitis B virus replication in differentiated HepaRG cells and primary human hepatocytes
Radreau Pauline,Marine Porcherot,Christophe Ramière,Karim Mouzannar,Vincent Lotteau,Patrice Andre +5 more
TL;DR: HBV replication and FXR regulation seem to be interdependent, and altered bile salt metabolism homeostasis might contribute to the persistence of HBV infection.
Journal ArticleDOI
Hepatic Farnesoid X-Receptor Isoforms α2 and α4 Differentially Modulate Bile Salt and Lipoprotein Metabolism in Mice
Marije Boesjes,Vincent W. Bloks,Jurre Hageman,Trijnie Bos,Theo H. van Dijk,Rick Havinga,Henk Wolters,Johan W. Jonker,Folkert Kuipers,Albert K. Groen +9 more
TL;DR: It is shown, for the first time, that hepatic FXRα2 andFXRα4 differentially modulate bile salt and lipoprotein metabolism in mice.
Journal ArticleDOI
FXR expression is associated with dysregulated glucose and lipid levels in the offspring kidney induced by maternal obesity
TL;DR: Glucose intolerance in the offspring of obese mothers was evident at weaning, with associated downregulation of renal FXR expression and upregulation of monocyte chemoattractant protein-1 (MCP-1) and transforming growth factor-β1 (TGF- β1) suggesting a potential protective role for FXR.
Journal ArticleDOI
Discovery of farnesoid X receptor and its role in bile acid metabolism
TL;DR: In this paper , a review of the discovery of FXR as a bile acid sensor in the regulation of Bile acid metabolism and as a metabolic regulator of lipid, glucose, and energy homeostasis is presented.
Journal ArticleDOI
Therapeutic Mechanisms of Bile Acids and Nor-Ursodeoxycholic Acid in Non-Alcoholic Fatty Liver Disease.
TL;DR: NorUDCA has unique biochemical and therapeutic properties, since it is relatively resistant to conjugation with glycine or taurine compared to UDCA, and it showed anti-fibrotic, anti-inflammatory, and anti-lipotoxic properties in several animal models.
References
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Diagnosis and Classification of Diabetes Mellitus
TL;DR: The chronic hyperglycemia of diabetes is associated with long-term damage, dys-function, and failure of differentorgans, especially the eyes, kidneys, nerves, heart, and blood vessels.
Journal ArticleDOI
Glucose clamp technique: a method for quantifying insulin secretion and resistance.
TL;DR: Methods for the quantification of beta-cell sensitivity to glucose (hyperglycemic clamp technique) and of tissue sensitivity to insulin (euglycemic insulin clamp technique] are described.
Journal ArticleDOI
Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis
Takeshi Inagaki,Mihwa Choi,Antonio Moschetta,Li Peng,Carolyn L. Cummins,Jeffrey G. McDonald,Guizhen Luo,Stacey A. Jones,Bryan Goodwin,James A. Richardson,Robert D. Gerard,Joyce J. Repa,David J. Mangelsdorf,Steven A. Kliewer +13 more
TL;DR: It is demonstrated that fibroblast growth factor 15 signals from intestine to liver to repress the gene encoding cholesterol 7alpha-hydroxylase (CYP7A1), which catalyzes the first and rate-limiting step in the classical bile acid synthetic pathway.
Journal ArticleDOI
Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist.
Sama I. Sayin,Annika Wahlström,Jenny Felin,Sirkku Jäntti,Hanns-Ulrich Marschall,Krister Bamberg,Bo Angelin,Tuulia Hyötyläinen,Matej Orešič,Fredrik Bäckhed,Fredrik Bäckhed +10 more
TL;DR: It is suggested that the gut microbiota not only regulates secondary bile acids metabolism but also inhibits bile acid synthesis in the liver by alleviating FXR inhibition in the ileum.
Journal ArticleDOI
Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation
TL;DR: Results suggest that modulation of FXR activity and BA metabolism may open new attractive pharmacological approaches for the treatment of the metabolic syndrome and type 2 diabetes.
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Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial
Brent A. Neuschwander-Tetri,Rohit Loomba,Arun J. Sanyal,Joel E. Lavine,Mark L. Van Natta,Manal F. Abdelmalek,Naga Chalasani,Srinivasan Dasarathy,Anna Mae Diehl,Bilal Hameed,Kris V. Kowdley,Arthur J. McCullough,Norah A. Terrault,Jeanne M. Clark,James Tonascia,Elizabeth M. Brunt,David E. Kleiner,Edward Doo +17 more