Farnesoid X receptor (FXR) agonists induce hepatocellular apoptosis and impair hepatic functions via FXR/SHP pathway

A structurally optimized FXR agonist, MET409, reduced liver fat content over 12 weeks in patients with non-alcoholic steatohepatitis

(2021) Stephen A. Harrison et al.   JOURNAL OF HEPATOLOGY

FXR agonists for NASH: How are they different and what difference do they make?

(2021) Claus Kremoser   JOURNAL OF HEPATOLOGY

Bile acids and their receptors in metabolic disorders

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

FXR in liver physiology: Multiple faces to regulate liver metabolism

(2021) Katrin Panzitt et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Yangonin modulates lipid homeostasis, ameliorates cholestasis and cellular senescence in alcoholic liver disease via activating nuclear receptor FXR

(2021) Lina Kong et al.   PHYTOMEDICINE

Attacking the PI3K/Akt/mTOR signaling pathway for targeted therapeutic treatment in human cancer

(2021) Le Yu et al.   SEMINARS IN CANCER BIOLOGY

Methyl eugenol attenuates liver ischemia reperfusion injury via activating PI3K/Akt signaling

(2021) Mengqin Wang et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Obeticholic acid for the treatment of nonalcoholic steatohepatitis: Expectations and concerns

(2020) Stergios A. Polyzos et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Cell Plasticity in Liver Regeneration

(2020) Weiping Li et al.   TRENDS IN CELL BIOLOGY

A randomized, placebo-controlled, phase II study of obeticholic acid for primary sclerosing cholangitis

(2020) Kris V. Kowdley et al.   JOURNAL OF HEPATOLOGY

Bile acids aggravate nonalcoholic steatohepatitis and cardiovascular disease in SHRSP5/Dmcr rat model

(2020) Shusei Yamamoto et al.   EXPERIMENTAL AND MOLECULAR PATHOLOGY

FXR Isoforms Control Different Metabolic Functions in Liver Cells via Binding to Specific DNA Motifs

(2020) Jose Miguel Ramos Pittol et al.   GASTROENTEROLOGY

Opposite effects of the FXR agonist obeticholic acid on Mafg and Nrf2 mediate the development of acute liver injury in rodent models of cholestasis

(2020) Adriana Carino et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Pyridoxal isonicotinoyl hydrazone inhibition of FXR is involved in the pathogenesis of isoniazid-induced liver injury

(2020) Guoqiang Zhang et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Systematic review and meta-analysis of randomized controlled trials on the effects of obeticholic acid on the blood lipid profile: Insights into liver disorders and liver cancer

(2020) Lin Guan et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Farnesoid X receptor activation impairs liver progenitor cell‐mediated liver regeneration via the PTEN‐PI3K‐AKT‐mTOR axis in zebrafish

(2020) Kyounghwa Jung et al.   HEPATOLOGY

The potential diagnostic and therapeutic applications of exosomes in drug-induced liver injury

(2020) Lanlan Zhao et al.   TOXICOLOGY LETTERS

The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC

(2019) Michael Trauner et al.   HEPATOLOGY

FRI-303-How to develop a differentiated FXR agonist: GS-9674 shows a reduced side effect profile in mice, monkeys amd human phase 1 studies compared to its predecessor Px-102

(2019) Eva Hambruch et al.   JOURNAL OF HEPATOLOGY

Drug-induced liver injury severity and toxicity (DILIst): binary classification of 1279 drugs by human hepatotoxicity

(2019) Shraddha Thakkar et al.   DRUG DISCOVERY TODAY

Farnesoid X nuclear receptor agonists for the treatment of nonalcoholic steatohepatitis

(2019) Vasiliki Venetsanaki et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

FXR activation alleviates tacrolimus-induced post-transplant diabetes mellitus by regulating renal gluconeogenesis and glucose uptake

(2019) Ling Li et al.   Journal of Translational Medicine

Obeticholic acid for the treatment of non-alcoholic steatohepatitis: interim analysis from a multicentre, randomised, placebo-controlled phase 3 trial

(2019) Zobair M Younossi et al.   LANCET

Down-regulation of SOX17, GATA4 and FoxA2 promotes differentiation potential of hepatocytes from human hematopoietic stem cells

(2019) Pasupuleti Santhosh Kumar et al.   TISSUE & CELL

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non–Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers

(2019) Michael K. Badman et al.   Clinical Pharmacology in Drug Development

Improving prognosis in primary biliary cholangitis – Therapeutic options and strategy

(2018) Maren H. Harms et al.   BEST PRACTICE & RESEARCH IN CLINICAL GASTROENTEROLOGY

Protective effect of dioscin against thioacetamide-induced acute liver injury via FXR/AMPK signaling pathway in vivo

(2018) Lingli Zheng et al.   BIOMEDICINE & PHARMACOTHERAPY

Obeticholic acid raises LDL-cholesterol and reduces HDL-cholesterol in the Diet-Induced NASH (DIN) hamster model

(2018) François Briand et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

An FXR Agonist Reduces Bile Acid Synthesis Independently of Increases in FGF19 in Healthy Volunteers

(2018) Amani Al-Khaifi et al.   GASTROENTEROLOGY

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

(2018) Kris V. Kowdley et al.   HEPATOLOGY

FXR activation by obeticholic acid or nonsteroidal agonists induces a human-like lipoprotein cholesterol change in mice with humanized chimeric liver

(2018) Romeo Papazyan et al.   JOURNAL OF LIPID RESEARCH

Progress and challenges of selective Farnesoid X Receptor modulation

(2018) Vittoria Massafra et al.   PHARMACOLOGY & THERAPEUTICS

Bile acids down-regulate the expression of Augmenter of Liver Regeneration (ALR) via SHP/HNF4α1 and independent of Egr-1

(2018) Sara Ibrahim et al.   EXPERIMENTAL AND MOLECULAR PATHOLOGY

Hepatocyte Nuclear Factor 4 alpha (HNF4α) Activation is Essential for Termination of Liver Regeneration

(2018) Ian Huck et al.   HEPATOLOGY

FXR agonist obeticholic acid induces liver growth but exacerbates biliary injury in rats with obstructive cholestasis

(2018) Rowan F. van Golen et al.   Scientific Reports

Combined obeticholic acid and apoptosis inhibitor treatment alleviates liver fibrosis

(2018) Jiyu Zhou et al.   Acta Pharmaceutica Sinica B

Hepatocyte nuclear factor 4A improves hepatic differentiation of immortalized adult human hepatocytes and improves liver function and survival

(2017) Hua-Lian Hang et al.   EXPERIMENTAL CELL RESEARCH

Vanadium pentoxide increased PTEN and decreased SHP1 expression in NK-92MI cells, affecting PI3K-AKT-mTOR and Ras-MAPK pathways

(2017) Francisco Gallardo-Vera et al.   Journal of Immunotoxicology

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)

(2017) David C. Tully et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanisms of bile acid mediated inflammation in the liver

(2017) Man Li et al.   MOLECULAR ASPECTS OF MEDICINE

Chrysin exerts neuroprotective effects against 3-Nitropropionic acid induced behavioral despair—Mitochondrial dysfunction and striatal apoptosis via upregulating Bcl-2 gene and downregulating Bax—Bad genes in male wistar rats

(2016) Sumathi Thangarajan et al.   BIOMEDICINE & PHARMACOTHERAPY

Modeling and Experimental Studies of Obeticholic Acid Exposure and the Impact of Cirrhosis Stage

(2016) JE Edwards et al.   CTS-Clinical and Translational Science

Role of farnesoid X receptor in cholestasis

(2016) Zhi Qing Yuan et al.   Journal of Digestive Diseases

Protective effects of SRT1720 via the HNF1α/FXR signalling pathway and anti-inflammatory mechanisms in mice with estrogen-induced cholestatic liver injury

(2016) Linxi Yu et al.   TOXICOLOGY LETTERS

Functional human induced hepatocytes (hiHeps) with bile acid synthesis and transport capacities: A novel in vitro cholestatic model

(2016) Xuan Ni et al.   Scientific Reports

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

(2015) Gideon M. Hirschfield et al.   GASTROENTEROLOGY

The Novel Organic Arsenical Darinaparsin Induces MAPK-Mediated and SHP1-Dependent Cell Death in T-cell Lymphoma and Hodgkin Lymphoma Cells and Human Xenograft Models

(2014) D. Ravi et al.   CLINICAL CANCER RESEARCH

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

Protective effects of farnesoid X receptor (FXR) on hepatic lipid accumulation are mediated by hepatic FXR and independent of intestinal FGF15 signal

(2014) Johannes Schmitt et al.   LIVER INTERNATIONAL

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

(2011) J. Prawitt et al.   DIABETES

Hepatic FXR: key regulator of whole-body energy metabolism

(2011) João Soeiro Teodoro et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM