Farnesoid X receptor modulators 2014-present: a patent review

Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH

(2017) Hualing Xiao et al.   ACS Medicinal Chemistry Letters

BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis

(2017) Adriana Carino et al.   Scientific Reports

An Intestinal Microbiota–Farnesoid X Receptor Axis Modulates Metabolic Disease

(2016) Frank J. Gonzalez et al.   GASTROENTEROLOGY

Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases

(2016) Yanping Xu   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders

(2016) Roberto Pellicciari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists

(2016) Valentina Sepe et al.   Scientific Reports

Navigation in bile acid chemical space: discovery of novel FXR and GPBAR1 ligands

(2016) Claudia Finamore et al.   Scientific Reports

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

(2015) Valentina Sepe et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

(2015) Sungsoon Fang et al.   NATURE MEDICINE

Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling

(2015) Sabrina Cipriani et al.   PLoS One

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

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

Bile Acid-Activated Receptors, Intestinal Microbiota, and the Treatment of Metabolic Disorders

(2015) Stefano Fiorucci et al.   TRENDS IN MOLECULAR 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

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

Dual Activation of the Bile Acid Nuclear Receptor FXR and G-Protein-Coupled Receptor TGR5 Protects Mice against Atherosclerosis

(2014) Shinobu Miyazaki-Anzai et al.   PLoS One

Bile Acid Receptor Activation Modulates Hepatic Monocyte Activity and Improves Nonalcoholic Fatty Liver Disease

(2013) Rachel H. McMahan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The TGR5 receptor mediates bile acid–induced itch and analgesia

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

The global NAFLD epidemic

(2013) Rohit Loomba et al.   Nature Reviews Gastroenterology & Hepatology

Natural Ligands for Nuclear Receptors: Biology and Potential Therapeutic Applications

(2012) Maria Valeria D'Auria et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Development of FXR, PXR and CAR Agonists and Antagonists for Treatment of Liver Disorders

(2012) Stefano Fiorucci et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Discovery That Theonellasterol a Marine Sponge Sterol Is a Highly Selective FXR Antagonist That Protects against Liver Injury in Cholestasis

(2012) Barbara Renga et al.   PLoS One

Marine sponge steroids as nuclear receptor ligands

(2012) Stefano Fiorucci et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Farnesoid X receptor suppresses constitutive androstane receptor activity at the multidrug resistance protein-4 promoter

(2011) Barbara Renga et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion

(2011) HE Parker et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Targeting Farnesoid-X-Receptor: From Medicinal Chemistry to Disease Treatment

(2009) S. Fiorucci et al.   CURRENT MEDICINAL CHEMISTRY

Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis

(2009) Songwen Zhang et al.   JOURNAL OF HEPATOLOGY

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 acids: regulation of synthesis

(2009) John Y. L. Chiang   JOURNAL OF LIPID RESEARCH

Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR)

(2009) Brenton Flatt et al.   JOURNAL OF MEDICINAL CHEMISTRY

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