Farnesoid X receptor modulators (2011 – 2014): a patent review

Inhibition of farnesoid X receptor signaling shows beneficial effects in human obesity

(2015) Frank J. Gonzalez et al.   JOURNAL OF HEPATOLOGY

Farnesoid X nuclear receptor ligand obeticholic acid for non-cirrhotic, non-alcoholic steatohepatitis (FLINT): a multicentre, randomised, placebo-controlled trial

(2015) Brent A Neuschwander-Tetri et al.   LANCET

Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance

(2015) Sungsoon Fang et al.   NATURE MEDICINE

Tissue-specific actions of the metabolic hormones FGF15/19 and FGF21

(2015) Bryn M. Owen et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Beyond Bile Acids: Targeting Farnesoid X Receptor (FXR) with Natural and Synthetic Ligands

(2014) Andrea Carotti et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Knocking on FXR's Door:The "Hammerhead"-Structure Series of FXRs Agonists - Amphiphilic Isoxazoles with Potent In Vitro and In Vivo Activities

(2014) Christian Gege et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Bile acid dysregulation, gut dysbiosis, and gastrointestinal cancer

(2014) Jessica Tsuei et al.   EXPERIMENTAL BIOLOGY AND MEDICINE

Design, Synthesis, and Biological Evaluation of Potent Dual Agonists of Nuclear and Membrane Bile Acid Receptors

(2014) Claudio D’Amore et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploitation of Cholane Scaffold for the Discovery of Potent and Selective Farnesoid X Receptor (FXR) and G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1) Ligands

(2014) Carmen Festa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Modification on Ursodeoxycholic Acid (UDCA) Scaffold. Discovery of Bile Acid Derivatives As Selective Agonists of Cell-Surface G-Protein Coupled Bile Acid Receptor 1 (GP-BAR1)

(2014) Valentina Sepe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy and Safety of the Farnesoid X Receptor Agonist Obeticholic Acid in Patients With Type 2 Diabetes and Nonalcoholic Fatty Liver Disease

(2013) Sunder Mudaliar et al.   GASTROENTEROLOGY

Obeticholic acid, a farnesoid X receptor agonist, improves portal hypertension by two distinct pathways in cirrhotic rats

(2013) Len Verbeke et al.   HEPATOLOGY

Pruritus in cholestasis: Facts and fiction

(2013) Ulrich Beuers et al.   HEPATOLOGY

The TGR5 receptor mediates bile acid–induced itch and analgesia

(2013) Farzad Alemi et al.   JOURNAL OF CLINICAL INVESTIGATION

Binding Mechanism of the Farnesoid X Receptor Marine Antagonist Suvanine Reveals a Strategy To Forestall Drug Modulation on Nuclear Receptors. Design, Synthesis, and Biological Evaluation of Novel Ligands

(2013) Francesco Saverio Di Leva et al.   JOURNAL OF MEDICINAL CHEMISTRY

FXR Controls the Tumor Suppressor NDRG2 and FXR Agonists Reduce Liver Tumor Growth and Metastasis in an Orthotopic Mouse Xenograft Model

(2012) Ulrich Deuschle et al.   PLoS One

Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties

(2011) Hans G.F. Richter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Farnesoid X Receptor Agonist for the Treatment of Liver and Metabolic Disorders: Focus on 6-ethyl-CDCA

(2011) S. Fiorucci et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes

(2010) Hans G.F. Richter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Farnesoid X receptor modulators: a patent review

(2010) Matthew Lantz Crawley   EXPERT OPINION ON THERAPEUTIC PATENTS

2 FARNESOID-X RECEPTOR AGONISTS: A NEW CLASS OF DRUGS FOR THE TREATMENT OF PBC? AN INTERNATIONAL STUDY EVALUATING THE ADDITION OF INT-747 TO URSODEOXYCHOLIC ACID

(2010) A. Mason et al.   JOURNAL OF HEPATOLOGY

Farnesoid X Receptor Critically Determines the Fibrotic Response in Mice but Is Expressed to a Low Extent in Human Hepatic Stellate Cells and Periductal Myofibroblasts

(2009) Peter Fickert et al.   AMERICAN JOURNAL OF PATHOLOGY

FXR activation reverses insulin resistance and lipid abnormalities and protects against liver steatosis in Zucker (fa/fa) obese rats

(2009) Sabrina Cipriani et al.   JOURNAL OF LIPID RESEARCH

Bile acid-activated receptors in the treatment of dyslipidemia and related disorders

(2009) Stefano Fiorucci et al.   PROGRESS IN LIPID RESEARCH

Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders

(2009) Stefano Fiorucci et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Evolution of the bile salt nuclear receptor FXR in vertebrates

(2008) Erica J. Reschly et al.   JOURNAL OF LIPID RESEARCH