Molecular Physiology of Bile Acid Signaling in Health, Disease and Aging

Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis

(2020) Donatella Chianelli et al.   JOURNAL OF MEDICINAL CHEMISTRY

The nuclear receptor FXR inhibits Glucagon-Like Peptide-1 secretion in response to microbiota-derived Short-Chain Fatty Acids

(2020) Sarah Ducastel et al.   Scientific Reports

Ursodeoxycholic acid enriches intestinal bile salt hydrolase-expressing Bacteroidetes in cholestatic pregnancy

(2020) Caroline Ovadia et al.   Scientific Reports

Bacterial metabolism of bile acids promotes generation of peripheral regulatory T cells

(2020) Clarissa Campbell et al.   NATURE

Ileo-colonic delivery of conjugated bile acids improves glucose homeostasis via colonic GLP-1-producing enteroendocrine cells in human obesity and diabetes

(2020) Gerardo Calderon et al.   EBioMedicine

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

TGR5 Protects Against Colitis in Mice, but Vertical Sleeve Gastrectomy Increases Colitis Severity

(2019) Darline Garibay et al.   OBESITY SURGERY

Bile acid supplementation decreases body mass gain in C57BL/6J but not 129S6/SvEvTac mice without increasing energy expenditure

(2019) Tobias Fromme et al.   Scientific Reports

FXR Regulates Intestinal Cancer Stem Cell Proliferation

(2019) Ting Fu et al.   CELL

Donor metabolic characteristics drive effects of faecal microbiota transplantation on recipient insulin sensitivity, energy expenditure and intestinal transit time

(2019) Pieter de Groot et al.   GUT

Farnesoid X Receptor alters adipose tissue architecture in mice and limits storage capacity leading to metabolic derangements

(2019) Tim van Zutphen et al.   JOURNAL OF LIPID RESEARCH

Diet-induced remission in chronic enteropathy is associated with altered microbial community structure and synthesis of secondary bile acids

(2019) Shuai Wang et al.   Microbiome

Glucagon-like peptide 1 (GLP-1)

(2019) T.D. Müller et al.   Molecular Metabolism

Liver Injury in Patients with Cholestatic Liver Disease Treated with Obeticholic Acid

(2019) John E Eaton et al.   HEPATOLOGY

Impact of obeticholic acid on the lipoprotein profile in patients with non-alcoholic steatohepatitis

(2019) Mohammad Shadab Siddiqui et al.   JOURNAL OF HEPATOLOGY

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

β-Catenin regulation of farnesoid X receptor signaling and bile acid metabolism during murine cholestasis

(2018) Michael D. Thompson 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

The exercise-inducible bile acid receptor Tgr5 improves skeletal muscle function in mice

(2018) Takashi Sasaki et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

INT-767 prevents NASH and promotes visceral fat brown adipogenesis and mitochondrial function

(2018) Paolo Comeglio et al.   JOURNAL OF ENDOCRINOLOGY

Simultaneous inhibition of FXR and TGR5 exacerbates atherosclerotic formation

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

INT-767 improves histopathological features in a diet-induced ob/ob mouse model of biopsy-confirmed non-alcoholic steatohepatitis

(2018) Jonathan D Roth et al.   WORLD JOURNAL OF GASTROENTEROLOGY

GLP-2 receptor signaling controls circulating bile acid levels but not glucose homeostasis in Gcgr −/− mice and is dispensable for the metabolic benefits ensuing after vertical sleeve gastrectomy

(2018) Anita Patel et al.   Molecular Metabolism

Takeda G Protein-Coupled Receptor 5-Mechanistic Target of Rapamycin Complex 1 Signaling Contributes to the Increment of Glucagon-Like Peptide-1 Production after Roux-en-Y Gastric Bypass

(2018) Hening Zhai et al.   EBioMedicine

Fibroblast Growth Factor 15/19 – From Basic Functions to Therapeutic Perspectives

(2018) Emmanuel Somm et al.   ENDOCRINE REVIEWS

Relationship Between Three Commonly Used Non-invasive Fibrosis Biomarkers and Improvement in Fibrosis Stage in Patients With NASH

(2018) Naga Chalasani et al.   LIVER INTERNATIONAL

Dietary soybean protein ameliorates high-fat diet-induced obesity by modifying the gut microbiota-dependent biotransformation of bile acids

(2018) Keita Watanabe et al.   PLoS One

Methionine Restriction Extends Lifespan in Progeroid Mice and Alters Lipid and Bile Acid Metabolism

(2018) Clea Bárcena et al.   Cell Reports

Agonism for the bile acid receptor GPBAR1 reverses liver and vascular damage in a mouse model of steatohepatitis

(2018) Adriana Carino et al.   FASEB JOURNAL

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

(2018) Elliot S. Friedman et al.   GASTROENTEROLOGY

Gut microbiota and intestinal FXR mediate the clinical benefits of metformin

(2018) Lulu Sun et al.   NATURE MEDICINE

Metabolite-Sensing G Protein Coupled Receptor TGR5 Protects Host From Viral Infection Through Amplifying Type I Interferon Responses

(2018) Qingqing Xiong et al.   Frontiers in Immunology

Intestinal Farnesoid X Receptor Controls Transintestinal Cholesterol Excretion in Mice

(2017) Jan Freark de Boer et al.   GASTROENTEROLOGY

New therapeutic concepts in bile acid transport and signaling for management of cholestasis

(2017) Michael Trauner et al.   HEPATOLOGY

Small heterodimer partner deletion prevents hepatic steatosis and when combined with farnesoid X receptor loss protects against type 2 diabetes in mice

(2017) Oludemilade Akinrotimi et al.   HEPATOLOGY

A dual agonist of farnesoid X receptor (FXR) and the G protein–coupled receptor TGR5, INT-767, reverses age-related kidney disease in mice

(2017) Xiaoxin X. Wang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

nor Ursodeoxycholic acid improves cholestasis in primary sclerosing cholangitis

(2017) Peter Fickert et al.   JOURNAL OF HEPATOLOGY

The Bile Acid Receptor GPBAR1 Regulates the M1/M2 Phenotype of Intestinal Macrophages and Activation of GPBAR1 Rescues Mice from Murine Colitis

(2017) Michele Biagioli et al.   JOURNAL OF IMMUNOLOGY

Treatment with the natural FXR agonist chenodeoxycholic acid reduces clearance of plasma LDL whilst decreasing circulating PCSK9, lipoprotein(a) and apolipoprotein C-III

(2017) M. Ghosh Laskar et al.   JOURNAL OF INTERNAL MEDICINE

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

Farnesoid X Receptor Activation Attenuates Intestinal Ischemia Reperfusion Injury in Rats

(2017) Laurens J. Ceulemans et al.   PLoS One

Gpbar1 agonism promotes a Pgc-1α-dependent browning of white adipose tissue and energy expenditure and reverses diet-induced steatohepatitis in mice

(2017) Adriana Carino et al.   Scientific Reports

Bile acids destabilise HIF-1α and promote anti-tumour phenotypes in cancer cell models

(2016) J. P. Phelan et al.   BMC CANCER

Administration of tauroursodeoxycholic acid enhances osteogenic differentiation of bone marrow-derived mesenchymal stem cells and bone regeneration

(2016) Byung-Hyun Cha et al.   BONE

Intestinal Crosstalk between Bile Acids and Microbiota and Its Impact on Host Metabolism

(2016) Annika Wahlström et al.   Cell Metabolism

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

(2016) Cen Xie et al.   DIABETES

Effects of obeticholic acid on lipoprotein metabolism in healthy volunteers

(2016) R. Pencek et al.   DIABETES OBESITY & METABOLISM

An Intestinal Microbiota–Farnesoid X Receptor Axis Modulates Metabolic Disease

(2016) Frank J. Gonzalez et al.   GASTROENTEROLOGY

Microbiota-induced obesity requires farnesoid X receptor

(2016) Ava Parséus et al.   GUT

G-protein-coupled bile acid receptor plays a key role in bile acid metabolism and fasting-induced hepatic steatosis in mice

(2016) Ajay C. Donepudi et al.   HEPATOLOGY

Farnesoid X receptor activation increases reverse cholesterol transport by modulating bile acid composition and cholesterol absorption in mice

(2016) Yang Xu et al.   HEPATOLOGY

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

(2016) Juan P. Arab et al.   HEPATOLOGY

Antibiotic effects on gut microbiota and metabolism are host dependent

(2016) Shiho Fujisaka et al.   JOURNAL OF CLINICAL INVESTIGATION

Gut Microbiota Orchestrates Energy Homeostasis during Cold

(2015) Claire Chevalier et al.   CELL

Interactions between Diet, Bile Acid Metabolism, Gut Microbiota, and Inflammatory Bowel Diseases

(2015) Suzanne Devkota et al.   DIGESTIVE DISEASES

Bile Acids Trigger GLP-1 Release Predominantly by Accessing Basolaterally Located G Protein–Coupled Bile Acid Receptors

(2015) Cheryl A. Brighton et al.   ENDOCRINOLOGY

Role of FXR in β-Cells of Lean and Obese Mice

(2015) Björn Schittenhelm et al.   ENDOCRINOLOGY

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

(2015) Maria Reich et al.   GUT

Engineered fibroblast growth factor 19 reduces liver injury and resolves sclerosing cholangitis in Mdr2 -deficient mice

(2015) Mei Zhou 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

New paradigms in the treatment of hepatic cholestasis: From UDCA to FXR, PXR and beyond

(2015) Ulrich Beuers et al.   JOURNAL OF HEPATOLOGY

Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance

(2015) Sungsoon Fang et al.   NATURE MEDICINE

TGR5 and Immunometabolism: Insights from Physiology and Pharmacology

(2015) Alessia Perino et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice

(2015) Daniel A. Briere et al.   PLoS One

Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1

(2015) Barbara Renga et al.   PLoS One

Novel Mechanistic Insights into Ectodomain Shedding of EGFR Ligands Amphiregulin and TGF- : Impact on Gastrointestinal Cancers Driven by Secondary Bile Acids

(2014) N. S. Nagathihalli et al.   CANCER RESEARCH

Separating Tumorigenicity from Bile Acid Regulatory Activity for Endocrine Hormone FGF19

(2014) M. Zhou et al.   CANCER RESEARCH

Role of the Microbiota in Immunity and Inflammation

(2014) Yasmine Belkaid et al.   CELL

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

Comparative Metabolomics Reveals Endogenous Ligands of DAF-12, a Nuclear Hormone Receptor, Regulating C. elegans Development and Lifespan

(2014) Parag Mahanti et al.   Cell Metabolism

Control of hepatocyte proliferation and survival by Fgf receptors is essential for liver regeneration in mice

(2014) Susagna Padrissa-Altés et al.   GUT

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

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

Intestinal transport and metabolism of bile acids

(2014) Paul A. Dawson et al.   JOURNAL OF LIPID RESEARCH

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

Bile Acid Flux Is Necessary for Normal Liver Regeneration

(2014) Willscott E. Naugler   PLoS One

A GPBAR1 (TGR5) Small Molecule Agonist Shows Specific Inhibitory Effects on Myeloid Cell Activation In Vitro and Reduces Experimental Autoimmune Encephalitis (EAE) In Vivo

(2014) Nuruddeen D. Lewis et al.   PLoS One

FXR agonist GW4064 alleviates endotoxin-induced hepatic inflammation by repressing macrophage activation

(2014) Jun Yao   WORLD JOURNAL OF GASTROENTEROLOGY

Antibiotic-induced shifts in the mouse gut microbiome and metabolome increase susceptibility to Clostridium difficile infection

(2014) Casey M. Theriot et al.   Nature Communications

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

Comparative Effects of Prolonged and Intermittent Stimulation of the Glucagon-Like Peptide 1 Receptor on Gastric Emptying and Glycemia

(2013) M. M. Umapathysivam et al.   DIABETES

Farnesoid X receptor agonists attenuate colonic epithelial secretory function and prevent experimental diarrhoea in vivo

(2013) Magdalena S Mroz et al.   GUT

Identification of fibroblast growth factor 15 as a novel mediator of liver regeneration and its application in the prevention of post-resection liver failure in mice

(2013) Iker Uriarte et al.   GUT

Yin Yang 1 promotes hepatic steatosis through repression of farnesoid X receptor in obese mice

(2013) Yan Lu et al.   GUT

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

(2013) Noémie Péan et al.   HEPATOLOGY

SIRT1 controls liver regeneration by regulating bile acid metabolism through farnesoid X receptor and mammalian target of rapamycin signaling

(2013) Juan L. García-Rodríguez et al.   HEPATOLOGY

Glucose sensing O-GlcNAcylation pathway regulates the nuclear bile acid receptor farnesoid X receptor (FXR)

(2013) Wahiba Berrabah et al.   HEPATOLOGY

SUMOylation of the Farnesoid X Receptor (FXR) Regulates the Expression of FXR Target Genes

(2013) Natarajan Balasubramaniyan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Bile Acid Receptor Activation Modulates Hepatic Monocyte Activity and Improves Nonalcoholic Fatty Liver Disease

(2013) Rachel H. McMahan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hepatic glucose sensing is required to preserve β cell glucose competence

(2013) Pascal Seyer et al.   JOURNAL OF CLINICAL INVESTIGATION

Farnesoid X Receptor Inhibits the Transcriptional Activity of Carbohydrate Response Element Binding Protein in Human Hepatocytes

(2013) S. Caron et al.   MOLECULAR AND CELLULAR BIOLOGY

Obesity-induced gut microbial metabolite promotes liver cancer through senescence secretome

(2013) Shin Yoshimoto et al.   NATURE

The bile acid receptor, TGR5, regulates basal and cholinergic-induced secretory responses in rat colon

(2013) J. B. J. Ward et al.   NEUROGASTROENTEROLOGY AND MOTILITY

External biliary drainage and liver regeneration after major hepatectomy

(2012) R. Otao et al.   BRITISH JOURNAL OF SURGERY

Bile Acids Acutely Stimulate Insulin Secretion of Mouse  -Cells via Farnesoid X Receptor Activation and KATP Channel Inhibition

(2012) M. Dufer et al.   DIABETES

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

Crosstalk between the hepatologist and the cardiologist: A future place for the lithocholic acid as a coronary atheroma risk factor?

(2012) Henri Duboc et al.   HEPATOLOGY

α5β1-integrins are sensors for tauroursodeoxycholic acid in hepatocytes

(2012) Holger Gohlke et al.   HEPATOLOGY

Cirrhosis and other liver disease in cystic fibrosis

(2012) Thomas Flass et al.   Journal of Cystic Fibrosis

Farnesoid X Receptor Induces Murine Scavenger Receptor Class B Type I via Intron Binding

(2012) Guodong Li et al.   PLoS One

Bile Acid Binding Resin Improves Metabolic Control through the Induction of Energy Expenditure

(2012) Mitsuhiro Watanabe et al.   PLoS One

A Steroid Receptor-MicroRNA Switch Regulates Life Span in Response to Signals from the Gonad

(2012) Y. Shen et al.   SCIENCE

Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion

(2011) HE Parker et al.   BRITISH JOURNAL OF PHARMACOLOGY

FGF15/19 Regulates Hepatic Glucose Metabolism by Inhibiting the CREB-PGC-1α Pathway

(2011) Matthew J. Potthoff et al.   Cell Metabolism

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

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

Molecular Control of Systemic Bile Acid Homeostasis by the Liver Glucocorticoid Receptor

(2011) Adam J. Rose et al.   Cell Metabolism

Selective Activation of Nuclear Bile Acid Receptor FXR in the Intestine Protects Mice Against Cholestasis

(2011) Salvatore Modica et al.   GASTROENTEROLOGY

The G-Protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor kappa light-chain enhancer of activated B cells (NF-κB) in mice

(2011) Yan-Dong Wang et al.   HEPATOLOGY

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

(2011) Elaine Studer et al.   HEPATOLOGY

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

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

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

Farnesoid X Receptor (FXR) Activation and FXR Genetic Variation in Inflammatory Bowel Disease

(2011) Rian M. Nijmeijer et al.   PLoS One

Dose-Response of Five Bile Acids on Serum and Liver Bile Acid Concentrations and Hepatotoxicty in Mice

(2011) Peizhen Song et al.   TOXICOLOGICAL SCIENCES

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

(2010) Iuliana Ristea Popescu et al.   FEBS LETTERS

Effects of nuclear receptor FXR on the regulation of liver lipid metabolism in patients with non-alcoholic fatty liver disease

(2010) Zhao-Xia Yang et al.   Hepatology International

Constitutive androstane receptor activation stimulates faecal bile acid excretion and reverse cholesterol transport in mice

(2010) Anne Laure Sberna et al.   JOURNAL OF HEPATOLOGY

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

The normal mechanisms of pregnancy-induced liver growth are not maintained in mice lacking the bile acid sensor Fxr

(2009) Alexandra Milona et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Bile acid signaling pathways increase stability of Small Heterodimer Partner (SHP) by inhibiting ubiquitin-proteasomal degradation

(2009) J. Miao et al.   GENES & DEVELOPMENT

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

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

Fibroblast Growth Factor-19, a Novel Factor That Inhibits Hepatic Fatty Acid Synthesis

(2009) Sushant Bhatnagar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis

(2009) Songwen Zhang et al.   JOURNAL OF HEPATOLOGY

The Bile Acid Receptor FXR Is a Modulator of Intestinal Innate Immunity

(2009) P. Vavassori et al.   JOURNAL OF IMMUNOLOGY

Bile acid transporters

(2009) Paul A. Dawson et al.   JOURNAL OF LIPID RESEARCH

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

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

Farnesoid X receptor antagonizes nuclear factor κB in hepatic inflammatory response

(2008) Yan-Dong Wang et al.   HEPATOLOGY

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