title: FXR agonists as therapeutic agents for non-alcoholic fatty liver disease.
abstract: Non-alcoholic fatty liver disease (NAFLD) is the hepatic manifestation of the metabolic syndrome and a risk factor for both cardiovascular and hepatic related morbidity and mortality. The increasing prevalence of this disease requires novel therapeutic approaches to prevent disease progression. Farnesoid X receptors are bile acid receptors with roles in lipid, glucose, and energy homeostasis. Synthetic farnesoid X receptor (FXR) agonists have been developed to specifically target these receptors for therapeutic use in NAFLD patients. Here, we present a review of bile acid physiology and how agonism of FXR receptors has been examined in pre-clinical and clinical NAFLD. Early evidence suggests a potential role for synthetic FXR agonists in the management of NAFLD; however, additional studies are needed to clarify their effects on lipid and glucose parameters in humans.
authors.affiliation: Division of Gastroenterology, University of Pennsylvania, 421 Curie Boulevard, 907 Biomedical Research Building, Philadelphia, PA, 19104, USA, Rotonya.Carr@uphs.upenn.edu.
authors.forename: Rotonya M
authors.initials: RM
authors.lastname: Carr
authors.forename: Andrea E
authors.initials: AE
authors.lastname: Reid
mesh_terms: D001647:Bile Acids and Salts / Q000378:metabolism; D002635:Chenodeoxycholic Acid / Q000031:analogs & derivatives* / Q000627:therapeutic use; D002756:Cholagogues and Choleretics / Q000627:therapeutic use*; D005235:Fatty Liver, Alcoholic / Q000188:drug therapy; D006801:Humans; D016328:NF-kappa B / Q000378:metabolism; D065626:Non-alcoholic Fatty Liver Disease / Q000188:drug therapy* / Q000378:metabolism; D047493:PPAR alpha / Q000378:metabolism; D019764:Phosphoenolpyruvate Carboxykinase (ATP) / Q000378:metabolism; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000378:metabolism; D051780:Sterol Regulatory Element Binding Protein 1 / Q000378:metabolism; D014580:Ursodeoxycholic Acid / Q000627:therapeutic use*; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D001647:Bile Acids and Salts; D002635:Chenodeoxycholic Acid; D002756:Cholagogues and Choleretics; D016328:NF-kappa B; D047493:PPAR alpha; D019764:Phosphoenolpyruvate Carboxykinase (ATP); D018160:Receptors, Cytoplasmic and Nuclear; D051780:Sterol Regulatory Element Binding Protein 1; D014580:Ursodeoxycholic Acid; D000099150:Receptor, Farnesoid X-Activated; C497387:SREBF1 protein, human; C464660:obeticholic acid; C000597251:PCK2 protein, human