Discovery of farnesoid X receptor and its role in bile acid metabolism

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

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

TGR5 Regulates Macrophage Inflammation in Nonalcoholic Steatohepatitis by Modulating NLRP3 Inflammasome Activation

(2021) Yong Shi et al.   Frontiers in Immunology

Hypothalamic bile acid-TGR5 signaling protects from obesity

(2021) Ashley Castellanos-Jankiewicz et al.   Cell Metabolism

Downregulation of TGR5 (GPBAR1) in biliary epithelial cells contributes to the pathogenesis of sclerosing cholangitis

(2021) Maria Reich et al.   JOURNAL OF HEPATOLOGY

Atorvastatin protects against liver and vascular damage in a model of diet induced steatohepatitis by resetting FXR and GPBAR1 signaling

(2021) Silvia Marchianò et al.   FASEB JOURNAL

Intestine-liver crosstalk in Type 2 Diabetes and non-alcoholic fatty liver disease

(2021) Margaux Nawrot et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Bile acid receptors FXR and TGR5 signaling in fatty liver diseases and therapy

(2020) John Y. L. Chiang et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

FXR Agonists as Therapy for Liver Disease

(2020) Jay H. Hoofnagle   HEPATOLOGY

Gut microbiota and human NAFLD: disentangling microbial signatures from metabolic disorders

(2020) Judith Aron-Wisnewsky et al.   Nature Reviews Gastroenterology & Hepatology

Obeticholic acid improves hepatic bile acid excretion in patients with primary biliary cholangitis

(2020) Kristoffer Kjærgaard et al.   JOURNAL OF HEPATOLOGY

Bariatric surgery reveals a gut-restricted TGR5 agonist with anti-diabetic effects

(2020) Snehal N. Chaudhari et al.   Nature Chemical Biology

Hepatic autophagy deficiency remodels gut microbiota for an adaptive protection via FGF15-FGFR4 signaling

(2020) Shengmin Yan et al.   Cellular and Molecular Gastroenterology and Hepatology

Transcriptomic profiling across the nonalcoholic fatty liver disease spectrum reveals gene signatures for steatohepatitis and fibrosis

(2020) Olivier Govaere et al.   Science Translational Medicine

Combination Therapies Including Cilofexor and Firsocostat for Bridging Fibrosis and Cirrhosis Attributable to NASH

(2020) Rohit Loomba et al.   HEPATOLOGY

Hepatokines and adipokines in NASH-related hepatocellular carcinoma

(2020) Ozlem Kucukoglu et al.   JOURNAL OF HEPATOLOGY

Intestinal TGR5 agonism improves hepatic steatosis and insulin sensitivity in Western diet-fed mice

(2019) Patricia D. Finn et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

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

(2019) Michael Trauner et al.   HEPATOLOGY

Deficiency of both farnesoid X receptor and Takeda G protein-coupled receptor 5 exacerbated liver fibrosis in mice

(2019) Jessica M. Ferrell et al.   HEPATOLOGY

Gut microbial metabolites in obesity, NAFLD and T2DM

(2019) Emanuel E. Canfora et al.   Nature Reviews Endocrinology

Bile salt hydrolases: Gatekeepers of bile acid metabolism and host-microbiome crosstalk in the gastrointestinal tract

(2019) Matthew H. Foley et al.   PLoS Pathogens

NGM 282 Improves Liver Fibrosis and Histology in 12 Weeks in Patients with Nonalcoholic Steatohepatitis

(2019) Stephen A. Harrison et al.   HEPATOLOGY

Bile Acids as Metabolic Regulators and Nutrient Sensors

(2019) John Y. L. Chiang et al.   Annual Review of Nutrition

Mitochondrial oxysterol biosynthetic pathway gives evidence for CYP7B1 as controller of regulatory oxysterols

(2019) Genta Kakiyama et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

From NASH to HCC: current concepts and future challenges

(2019) Quentin M. Anstee et al.   Nature Reviews Gastroenterology & Hepatology

Hepatocellular Carcinoma

(2019) Augusto Villanueva   NEW ENGLAND JOURNAL OF MEDICINE

Ursodeoxycholic acid is a GPBAR1 agonist and resets liver/intestinal FXR signaling in a model of diet-induced dysbiosis and NASH

(2019) Adriana Carino et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Regulations of bile acid metabolism in mouse models with hydrophobic bile acid composition

(2019) Akira Honda et al.   JOURNAL OF LIPID RESEARCH

Animal models to study bile acid metabolism

(2018) Jianing Li et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

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

(2018) Kris V. Kowdley et al.   HEPATOLOGY

Intestine farnesoid X receptor agonist and the gut microbiota activate G-protein bile acid receptor-1 signaling to improve metabolism

(2018) Preeti Pathak et al.   HEPATOLOGY

Reciprocal interactions between bile acids and gut microbiota in human liver diseases

(2018) Tadashi Ikegami et al.   HEPATOLOGY RESEARCH

Fructose and sugar: A major mediator of non-alcoholic fatty liver disease

(2018) Thomas Jensen et al.   JOURNAL OF HEPATOLOGY

Simultaneous inhibition of FXR and TGR5 exacerbates atherosclerotic formation

(2018) Shinobu Miyazaki-Anzai et al.   JOURNAL OF LIPID RESEARCH

Increased Bile Acids and FGF19 After Sleeve Gastrectomy and Roux-en-Y Gastric Bypass Correlate with Improvement in Type 2 Diabetes in a Randomized Trial

(2018) Reza Nemati et al.   OBESITY SURGERY

Postprandial FGF19-induced phosphorylation by Src is critical for FXR function in bile acid homeostasis

(2018) Sangwon Byun et al.   Nature Communications

Targeting FXR and FGF19 to Treat Metabolic Diseases—Lessons Learned From Bariatric Surgery

(2018) Nadejda Bozadjieva et al.   DIABETES

Conversion of chenodeoxycholic acid to cholic acid by human CYP8B1

(2018) Linbing Fan et al.   BIOLOGICAL CHEMISTRY

FXR-Dependent Modulation of the Human Small Intestinal Microbiome by the Bile Acid Derivative Obeticholic Acid

(2018) Elliot S. Friedman et al.   GASTROENTEROLOGY

Effect of NGM282, an FGF19 analogue, in primary sclerosing cholangitis: A multicenter, randomized, double-blind, placebo-controlled phase II trial

(2018) Gideon M. Hirschfield et al.   JOURNAL OF HEPATOLOGY

Gut microbiota and intestinal FXR mediate the clinical benefits of metformin

(2018) Lulu Sun et al.   NATURE MEDICINE

Bile Acid Control of Metabolism and Inflammation in Obesity, Type 2 Diabetes, Dyslipidemia, and Nonalcoholic Fatty Liver Disease

(2017) Oscar Chávez-Talavera et al.   GASTROENTEROLOGY

Hepatic bile acid uptake in humans and mice: Multiple pathways and expanding potential role for gut-liver signaling

(2017) Paul A. Dawson   HEPATOLOGY

The role of sphingosine 1-phosphate receptor 2 in bile-acid-induced cholangiocyte proliferation and cholestasis-induced liver injury in mice

(2017) Yongqing Wang et al.   HEPATOLOGY

The presence and severity of nonalcoholic steatohepatitis is associated with specific changes in circulating bile acids

(2017) Puneet Puri et al.   HEPATOLOGY

Farnesoid X receptor induces Takeda G-protein receptor 5 cross-talk to regulate bile acid synthesis and hepatic metabolism

(2017) Preeti Pathak et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

nor Ursodeoxycholic acid improves cholestasis in primary sclerosing cholangitis

(2017) Peter Fickert et al.   JOURNAL OF HEPATOLOGY

Global burden of NAFLD and NASH: trends, predictions, risk factors and prevention

(2017) Zobair Younossi et al.   Nature Reviews Gastroenterology & Hepatology

Bile acid profiles over 5 years after gastric bypass and duodenal switch: results from a randomized clinical trial

(2017) Hilde Risstad et al.   Surgery for Obesity and Related Diseases

Bile Acid-Mediated Sphingosine-1-Phosphate Receptor 2 Signaling Promotes Neuroinflammation during Hepatic Encephalopathy in Mice

(2017) Matthew McMillin et al.   Frontiers in Cellular Neuroscience

Nonalcoholic Fatty Liver Disease: Pathogenesis and Disease Spectrum

(2016) Timothy Hardy et al.   Annual Review of Pathology-Mechanisms of Disease

An Intestinal Farnesoid X Receptor–Ceramide Signaling Axis Modulates Hepatic Gluconeogenesis in Mice

(2016) Cen Xie et al.   DIABETES

An Intestinal Microbiota–Farnesoid X Receptor Axis Modulates Metabolic Disease

(2016) Frank J. Gonzalez et al.   GASTROENTEROLOGY

Vertical sleeve gastrectomy activates GPBAR-1/TGR5 to sustain weight loss, improve fatty liver, and remit insulin resistance in mice

(2016) Lili Ding et al.   HEPATOLOGY

Bile acids and nonalcoholic fatty liver disease: Molecular insights and therapeutic perspectives

(2016) Juan P. Arab et al.   HEPATOLOGY

Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome

(2016) Chuansheng Guo et al.   IMMUNITY

Cholesterol 7α-hydroxylase-deficient mice are protected from high-fat/high-cholesterol diet-induced metabolic disorders

(2016) Jessica M. Ferrell et al.   JOURNAL OF LIPID RESEARCH

Cyp2c70 is responsible for the species difference in bile acid metabolism between mice and humans

(2016) Shogo Takahashi et al.   JOURNAL OF LIPID RESEARCH

Gut commensal Bacteroides acidifaciens prevents obesity and improves insulin sensitivity in mice

(2016) J-Y Yang et al.   Mucosal Immunology

A Placebo-Controlled Trial of Obeticholic Acid in Primary Biliary Cholangitis

(2016) Frederik Nevens et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis

(2016) Natalia Gomez-Ospina et al.   Nature Communications

Farnesoid X Receptor Signaling Shapes the Gut Microbiota and Controls Hepatic Lipid Metabolism

(2016) Limin Zhang et al.   mSystems

Bile Acids and Dysbiosis in Non-Alcoholic Fatty Liver Disease

(2016) Marialena Mouzaki et al.   PLoS One

Detection of FGF15 in Plasma by Stable Isotope Standards and Capture by Anti-peptide Antibodies and Targeted Mass Spectrometry

(2015) Takeshi Katafuchi et al.   Cell Metabolism

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

(2015) Gideon M. Hirschfield et al.   GASTROENTEROLOGY

TGR5 is essential for bile acid-dependent cholangiocyte proliferation in vivo and in vitro

(2015) Maria Reich et al.   GUT

TGR5 contributes to glucoregulatory improvements after vertical sleeve gastrectomy in mice

(2015) Anne K McGavigan et al.   GUT

Activation of sphingosine kinase 2 by endoplasmic reticulum stress ameliorates hepatic steatosis and insulin resistance in mice

(2015) Su-Yeon Lee et al.   HEPATOLOGY

Conjugated bile acid-activated S1P receptor 2 is a key regulator of sphingosine kinase 2 and hepatic gene expression

(2015) Masayuki Nagahashi et al.   HEPATOLOGY

Ursodeoxycholic acid exerts farnesoid X receptor-antagonistic effects on bile acid and lipid metabolism in morbid obesity

(2015) Michaela Mueller et al.   JOURNAL OF HEPATOLOGY

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

Novel therapeutic targets in primary biliary cirrhosis

(2015) Jessica K. Dyson et al.   Nature Reviews Gastroenterology & Hepatology

Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction

(2015) Changtao Jiang et al.   Nature Communications

Cytoplasmic Tyrosine Phosphatase Shp2 Coordinates Hepatic Regulation of Bile Acid and FGF15/19 Signaling to Repress Bile Acid Synthesis

(2014) Shuangwei Li et al.   Cell Metabolism

Conjugated bile acids promote cholangiocarcinoma cell invasive growth through activation of sphingosine 1-phosphate receptor 2

(2014) Runping Liu et al.   HEPATOLOGY

TGR5 reduces macrophage migration through mTOR-induced C/EBPβ differential translation

(2014) Alessia Perino et al.   JOURNAL OF CLINICAL INVESTIGATION

Intestinal farnesoid X receptor signaling promotes nonalcoholic fatty liver disease

(2014) Changtao Jiang et al.   JOURNAL OF CLINICAL INVESTIGATION

G-Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype

(2014) Klemens Högenauer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transcriptional regulation of autophagy by an FXR–CREB axis

(2014) Sunmi Seok et al.   NATURE

Nutrient-sensing nuclear receptors coordinate autophagy

(2014) Jae Man Lee et al.   NATURE

FXR is a molecular target for the effects of vertical sleeve gastrectomy

(2014) Karen K. Ryan et al.   NATURE

GPBAR1/TGR5 Mediates Bile Acid-Induced Cytokine Expression in Murine Kupffer Cells

(2014) Guiyu Lou et al.   PLoS One

Bile Acid Receptor TGR5 Agonism Induces NO Production and Reduces Monocyte Adhesion in Vascular Endothelial Cells

(2013) Taiki Kida et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Functions of autophagy in normal and diseased liver

(2013) Mark J. Czaja et al.   Autophagy

Gut Microbiota Regulates Bile Acid Metabolism by Reducing the Levels of Tauro-beta-muricholic Acid, a Naturally Occurring FXR Antagonist

(2013) Sama I. Sayin et al.   Cell Metabolism

Human Insulin Resistance Is Associated With Increased Plasma Levels of 12 -Hydroxylated Bile Acids

(2013) R. A. Haeusler et al.   DIABETES

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

The receptor TGR5 protects the liver from bile acid overload during liver regeneration in mice

(2013) Noémie Péan et al.   HEPATOLOGY

TGR5 signalling inhibits the production of pro-inflammatory cytokines byin vitrodifferentiated inflammatory and intestinal macrophages in Crohn's disease

(2013) Kazuaki Yoneno et al.   IMMUNOLOGY

Microbiome remodelling leads to inhibition of intestinal farnesoid X receptor signalling and decreased obesity

(2013) Fei Li et al.   Nature Communications

The Role of Bile After Roux-en-Y Gastric Bypass in Promoting Weight Loss and Improving Glycaemic Control

(2012) Dimitri J. Pournaras et al.   ENDOCRINOLOGY

Endocrine fibroblast growth factors 15/19 and 21: from feast to famine

(2012) M. J. Potthoff et al.   GENES & DEVELOPMENT

Mechanism of tissue-specific farnesoid X receptor in suppressing the expression of genes in bile-acid synthesis in mice

(2012) Bo Kong et al.   HEPATOLOGY

Dietary-fat-induced taurocholic acid promotes pathobiont expansion and colitis in Il10 −/− mice

(2012) Suzanne Devkota et al.   NATURE

Conjugated Bile Acids Associate with Altered Rates of Glucose and Lipid Oxidation after Roux-en-Y Gastric Bypass

(2012) M. Simonen et al.   OBESITY SURGERY

Ursodeoxycholic acid and bile-acid mimetics as therapeutic agents for cholestatic liver diseases: An overview of their mechanisms of action

(2012) Raoul Poupon   Clinics and Research in Hepatology and Gastroenterology

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

(2011) Thijs W.H. Pols et al.   Cell Metabolism

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

(2011) J. Prawitt et al.   DIABETES

Bile Acid Is a Host Factor That Regulates the Composition of the Cecal Microbiota in Rats

(2011) K.B.M. Saiful Islam et al.   GASTROENTEROLOGY

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

(2011) R. M. Gadaleta et al.   GUT

Conjugated bile acids activate the sphingosine-1-phosphate receptor 2 in primary rodent hepatocytes

(2011) Elaine Studer et al.   HEPATOLOGY

The human gallbladder secretes fibroblast growth factor 19 into bile: Towards defining the role of fibroblast growth factor 19 in the enterobiliary tract

(2011) Serge J.L.B. Zweers et al.   HEPATOLOGY

Glucose and Insulin Induction of Bile Acid Synthesis

(2011) Tiangang Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ligand-Dependent Regulation of the Activity of the Orphan Nuclear Receptor, Small Heterodimer Partner (SHP), in the Repression of Bile Acid BiosyntheticCYP7A1andCYP8B1Genes

(2011) Ji Miao et al.   MOLECULAR ENDOCRINOLOGY

The G Protein-Coupled Bile Acid Receptor, TGR5, Stimulates Gallbladder Filling

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

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

Human Fatty Liver Disease: Old Questions and New Insights

(2011) J. C. Cohen et al.   SCIENCE

FGF19 as a Postprandial, Insulin-Independent Activator of Hepatic Protein and Glycogen Synthesis

(2011) S. Kir et al.   SCIENCE

The bile acid sensor FXR regulates insulin transcription and secretion

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

Defective Hepatic Autophagy in Obesity Promotes ER Stress and Causes Insulin Resistance

(2010) Ling Yang et al.   Cell Metabolism

Nuclear Receptor SHP, a Death Receptor That Targets Mitochondria, Induces Apoptosis and Inhibits Tumor Growth

(2010) Y. Zhang et al.   MOLECULAR AND CELLULAR BIOLOGY

Pathology of nonalcoholic fatty liver disease

(2010) Elizabeth M. Brunt   Nature Reviews Gastroenterology & Hepatology

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Genome-wide tissue-specific farnesoid X receptor binding in mouse liver and intestine

(2009) Ann M. Thomas et al.   HEPATOLOGY

Side chain structure determines unique physiologic and therapeutic properties of norursodeoxycholic acid in Mdr2−/− mice

(2009) Emina Halilbasic et al.   HEPATOLOGY

The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders

(2009) Verena Keitel et al.   HEPATOLOGY

Identification of Novel Pathways That Control Farnesoid X Receptor-mediated Hypocholesterolemia

(2009) Yanqiao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

New molecular insights into the mechanisms of cholestasis

(2009) Martin Wagner et al.   JOURNAL OF HEPATOLOGY

Bile acids: the role of peroxisomes

(2009) Sacha Ferdinandusse et al.   JOURNAL OF LIPID RESEARCH

Bile acids: regulation of synthesis

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

Autophagy regulates lipid metabolism

(2009) Rajat Singh et al.   NATURE

Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders

(2009) Stefano Fiorucci et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Expression and function of the bile acid receptor TGR5 in Kupffer cells

(2008) Verena Keitel et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Mechanisms of Cholestasis

(2008) Gernot Zollner et al.   Clinics in Liver Disease

Mechanisms of Hepatic Fibrogenesis

(2008) Scott L. Friedman   GASTROENTEROLOGY

Loss of orphan receptor small heterodimer partner sensitizes mice to liver injury from obstructive cholestasis

(2008) Young Joo Park et al.   HEPATOLOGY

Bile acids activate fibroblast growth factor 19 signaling in human hepatocytes to inhibit cholesterol 7α-hydroxylase gene expression

(2008) Kwang-Hoon Song et al.   HEPATOLOGY

Dietary cholesterol, rather than liver steatosis, leads to hepatic inflammation in hyperlipidemic mouse models of nonalcoholic steatohepatitis

(2008) Kristiaan Wouters et al.   HEPATOLOGY

Fructose consumption as a risk factor for non-alcoholic fatty liver disease

(2008) Xiaosen Ouyang et al.   JOURNAL OF HEPATOLOGY

Farnesoid X Receptor Protects Liver Cells from Apoptosis Induced by Serum Deprivationin Vitroand Fastingin Vivo

(2008) Yan-Dong Wang et al.   MOLECULAR ENDOCRINOLOGY

Targeting bile-acid signalling for metabolic diseases

(2008) Charles Thomas et al.   NATURE REVIEWS DRUG DISCOVERY