Farnesoid X receptor: from medicinal chemistry to clinical applications

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

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

Farnesoid X Receptor Deficiency Improves Glucose Homeostasis in Mouse Models of Obesity

(2011) J. Prawitt et al.   DIABETES

Lowering Bile Acid Pool Size with a Synthetic Farnesoid X Receptor (FXR) Agonist Induces Obesity and Diabetes through Reduced Energy Expenditure

(2011) Mitsuhiro Watanabe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Theonellasterols and Conicasterols fromTheonella swinhoei. Novel Marine Natural Ligands for Human Nuclear Receptors

(2011) Simona De Marino et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Sulfated Sterols from Marine Invertebrates as a New Class of Marine Natural Antagonists of Farnesoid-X-Receptor

(2011) Valentina Sepe et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Bile Acid Receptor GPBAR-1 (TGR5) Modulates Integrity of Intestinal Barrier and Immune Response to Experimental Colitis

(2011) Sabrina Cipriani et al.   PLoS One

The bile acid sensor FXR regulates insulin transcription and secretion

(2010) Barbara Renga et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

The nuclear receptor FXR is expressed in pancreatic β-cells and protects human islets from lipotoxicity

(2010) Iuliana Ristea Popescu et al.   FEBS LETTERS

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

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

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

Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/−and apoE−/−mice

(2009) Helen B. Hartman et al.   JOURNAL OF LIPID RESEARCH

Bile acids: regulation of synthesis

(2009) John Y. L. Chiang   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

Antiatherosclerotic effect of farnesoid X receptor

(2008) Andrea Mencarelli et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064

(2008) Adwoa Akwabi-Ameyaw et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Novel Compounds That Activate Farnesoid X Receptor: the Diversity of Their Effects on Gene Expression

(2008) Takuo Suzuki et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation

(2008) S. M. Soisson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA