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

Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application

(2015) Valentina Sepe et al.   Future Medicinal Chemistry

Efficacy of Obeticholic Acid in Patients With Primary Biliary Cirrhosis and Inadequate Response to Ursodeoxycholic Acid

(2015) Gideon M. Hirschfield et al.   GASTROENTEROLOGY

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

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

Dissociation of Intestinal and Hepatic Activities of FXR and LXR  Supports Metabolic Effects of Terminal Ileum Interposition in Rodents

(2013) A. Mencarelli et al.   DIABETES

The TGR5 receptor mediates bile acid–induced itch and analgesia

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

Farnesoid X receptor: from medicinal chemistry to clinical applications

(2012) Stefano Fiorucci et al.   Future Medicinal Chemistry

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

Functional Characterization of the Semisynthetic Bile Acid Derivative INT-767, a Dual Farnesoid X Receptor and TGR5 Agonist

(2010) G. Rizzo et al.   MOLECULAR PHARMACOLOGY

Farnesoid X receptor agonists in biliary tract disease

(2009) Stefano Fiorucci et al.   CURRENT OPINION IN GASTROENTEROLOGY

TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders

(2009) Atul Tiwari et al.   DRUG DISCOVERY TODAY

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

Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure−Activity Relationships, and Molecular Modeling Studies

(2008) Hiroyuki Sato et al.   JOURNAL OF MEDICINAL CHEMISTRY