Mechanistic Impact of Different Ligand Scaffolds on FXR Modulation Suggests Avenues to Selective Modulators

Efficacy and safety of drugs for nonalcoholic steatohepatitis

(2021) Bo Shen et al.   Journal of Digestive Diseases

The role of farnesoid X receptor in metabolic diseases, and gastrointestinal and liver cancer

(2021) Lulu Sun et al.   Nature Reviews Gastroenterology & Hepatology

The identification of farnesoid X receptor modulators as treatment options for nonalcoholic fatty liver disease

(2021) Stefano Fiorucci et al.   Expert Opinion on Drug Discovery

Bile acids and their receptors in metabolic disorders

(2021) Stefano Fiorucci et al.   PROGRESS IN LIPID RESEARCH

Heterodimer formation with retinoic acid receptor RXRα modulates coactivator recruitment by peroxisome proliferator-activated receptor PPARγ

(2021) Whitney Kilu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Recent Advances in the Medicinal Chemistry of Farnesoid X Receptor

(2021) Yuanying Fang et al.   JOURNAL OF MEDICINAL CHEMISTRY

L-thyroxin and the non-classical thyroid hormone TETRAC are potent activators of PPARγ

(2020) Leonie Gellrich et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nuclear receptor crosstalk — defining the mechanisms for therapeutic innovation

(2020) Karolien De Bosscher et al.   Nature Reviews Endocrinology

Obeticholic acid for the treatment of nonalcoholic steatohepatitis

(2020) Raj A. Shah et al.   Expert Review of Gastroenterology & Hepatology

Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD

(2020) Yanlin Zhu et al.   Frontiers in Pharmacology

Bile acid modulators for the treatment of nonalcoholic steatohepatitis (NASH)

(2020) Stefano Fiorucci et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Design and Structural Optimization of Dual FXR/PPARδ Activators

(2020) Simone Schierle et al.   JOURNAL OF MEDICINAL CHEMISTRY

FDA rejects NASH drug

(2020) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

The orphan nuclear receptor Nurr1 is responsive to non-steroidal anti-inflammatory drugs

(2020) Sabine Willems et al.   Communications Chemistry

Therapeutic modulation of retinoid X receptors – SAR and therapeutic potential of RXR ligands and recent patents

(2019) Simone Schierle et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Molecular tuning of farnesoid X receptor partial agonism

(2019) Daniel Merk et al.   Nature Communications

The gut-liver axis in liver disease: pathophysiological basis for therapy

(2019) Agustín Albillos et al.   JOURNAL OF HEPATOLOGY

A randomized trial of obeticholic acid monotherapy in patients with primary biliary cholangitis

(2018) Kris V. Kowdley et al.   HEPATOLOGY

Progress and challenges of selective Farnesoid X Receptor modulation

(2018) Vittoria Massafra et al.   PHARMACOLOGY & THERAPEUTICS

The nuclear receptor superfamily: A structural perspective

(2018) Emily R. Weikum et al.   PROTEIN SCIENCE

A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis

(2017) Jurema Schmidt et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

NSAIDs Ibuprofen, Indometacin and Diclofenac do not interact with Farnesoid X Receptor

(2015) Jurema Schmidt et al.   Scientific Reports

Nuclear Receptors, RXR, and the Big Bang

(2014) Ronald M. Evans et al.   CELL

Medicinal Chemistry and Pharmacological Effects of Farnesoid X Receptor (FXR) Antagonists

(2014) Christina Lamers et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Extending the Structure–Activity Relationship of Anthranilic Acid Derivatives As Farnesoid X Receptor Modulators: Development of a Highly Potent Partial Farnesoid X Receptor Agonist

(2014) Daniel Merk 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

An evolving understanding of nuclear receptor coregulator proteins

(2013) Christopher J Millard et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Nuclear receptor coregulators: modulators of pathology and therapeutic targets

(2012) David M. Lonard et al.   Nature Reviews Endocrinology

Farnesoid X receptor activation inhibits inflammation and preserves the intestinal barrier in inflammatory bowel disease

(2011) R. M. Gadaleta et al.   GUT

Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist

(2009) Song Feng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

FXR: a metabolic regulator and cell protector

(2008) Yan-Dong Wang et al.   CELL RESEARCH

Analyzing real-time PCR data by the comparative CT method

(2008) Thomas D Schmittgen et al.   Nature Protocols