Bile acids and their receptors in metabolic disorders

Circadian rhythms and bile acid homeostasis: a comprehensive review

(2020) Zaoqin Yu et al.   CHRONOBIOLOGY INTERNATIONAL

Cilofexor, a Nonsteroidal FXR Agonist, in Non‐Cirrhotic Patients with Nonalcoholic Steatohepatitis: A Phase 2 Randomized Controlled Trial

(2020) Keyur Patel et al.   HEPATOLOGY

FXR-dependent Rubicon induction impairs autophagy in models of human cholestasis

(2020) Katrin Panzitt et al.   JOURNAL OF HEPATOLOGY

Of mice and men: Murine bile acids explain species differences in the regulation of bile acid and cholesterol metabolism

(2020) Sara Straniero et al.   JOURNAL OF LIPID RESEARCH

Is CYP2C70 the key to new mouse models to understand bile acids in humans?

(2020) Grace L. Guo et al.   JOURNAL OF LIPID RESEARCH

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

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

Global chemical effects of the microbiome include new bile-acid conjugations

(2020) Robert A. Quinn et al.   NATURE

mTOR at the nexus of nutrition, growth, ageing and disease

(2020) Grace Y. Liu et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Structural basis of p62/SQSTM1 helical filaments and their role in cellular cargo uptake

(2020) Arjen J. Jakobi et al.   Nature Communications

FXR-mediated inhibition of autophagy contributes to FA-induced TG accumulation and accordingly reduces FA-induced lipotoxicity

(2020) Kun Wu et al.   Cell Communication and Signaling

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

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

Bile acid-activated receptors and the regulation of macrophages function in metabolic disorders

(2020) Stefano Fiorucci et al.   CURRENT OPINION IN PHARMACOLOGY

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

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

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

(2020) Jose Miguel Ramos Pittol et al.   GASTROENTEROLOGY

The therapeutic potential of FGF21 in metabolic diseases: from bench to clinic

(2020) Leiluo Geng et al.   Nature Reviews Endocrinology

Compound 18 Improves Glucose Tolerance in a Hepatocyte TGR5-dependent Manner in Mice

(2020) Marlena M. Holter et al.   Nutrients

Macrophage Sphingosine 1-Phosphate Receptor 2 Blockade Attenuates Liver Inflammation and Fibrogenesis Triggered by NLRP3 Inflammasome

(2020) Lei Hou et al.   Frontiers in Immunology

Metabolic consequences of ileal interruption of the enterohepatic circulation of bile acids

(2020) Ivo P. van de Peppel et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

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

The bile acid activated receptors GPBAR1 and FXR exert antagonistic effects on autophagy

(2020) Adriana Carino et al.   FASEB JOURNAL

Biological Functions of Autophagy Genes: A Disease Perspective

(2019) Beth Levine et al.   CELL

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

(2019) Michael Trauner et al.   HEPATOLOGY

Identification of a bilirubin receptor that may mediate a component of cholestatic itch

(2019) James Meixiong et al.   eLife

A review of analytical platforms for accurate bile acid measurement

(2019) Mainak Dutta et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

Ursodeoxycholic Acid Accelerates Bile Acid Enterohepatic Circulation

(2019) Yunjing Zhang et al.   BRITISH JOURNAL OF PHARMACOLOGY

Current Practice in the Diagnosis of Bile Acid Diarrhea

(2019) Priya Vijayvargiya et al.   GASTROENTEROLOGY

Activation of Mast-Cell-Expressed Mas-Related G-Protein-Coupled Receptors Drives Non-histaminergic Itch

(2019) James Meixiong et al.   IMMUNITY

Drugs and hepatic transporters: A review

(2019) Alexander Jetter et al.   PHARMACOLOGICAL RESEARCH

MRGPRX4 is a G protein-coupled receptor activated by bile acids that may contribute to cholestatic pruritus

(2019) James Meixiong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Transcriptome Analysis of Dual FXR and GPBAR1 Agonism in Rodent Model of NASH Reveals Modulation of Lipid Droplets Formation

(2019) Adriana Carino et al.   Nutrients

Obeticholic acid may increase the risk of gallstone formation in susceptible patients

(2019) Samer Al-Dury et al.   JOURNAL OF HEPATOLOGY

Autophagy markers LC3 and p62 accumulate in immune‐mediated necrotizing myopathy

(2019) Girolamo Francesco et al.   MUSCLE & NERVE

Long-term efficacy and safety of obeticholic acid for patients with primary biliary cholangitis: 3-year results of an international open-label extension study

(2019) Michael Trauner et al.   Lancet Gastroenterology & Hepatology

FGF19‐mediated upregulation of SOX18 promotes hepatocellular carcinoma metastasis by transactivating FGFR4 and FLT4

(2019) Jie Chen et al.   HEPATOLOGY

A Human-like Bile Acid Pool Induced by Deletion of Cyp2c70 Modulates Effects of Farnesoid X Receptor Activation in Mice

(2019) Jan Freark de Boer et al.   JOURNAL OF LIPID RESEARCH

MRGPRX4 is a bile acid receptor for human cholestatic itch

(2019) Huasheng Yu et al.   eLife

Bile acid metabolites control TH17 and Treg cell differentiation

(2019) Saiyu Hang et al.   NATURE

A randomized, double-blind, multicenter, phase 2b study to evaluate the safety and efficacy of a combination of tropifexor and cenicriviroc in patients with nonalcoholic steatohepatitis and liver fibrosis: Study design of the TANDEM trial

(2019) Marcos Pedrosa et al.   Contemporary Clinical Trials

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

Microbial bile acid metabolites modulate gut RORγ+ regulatory T cell homeostasis

(2019) Xinyang Song et al.   NATURE

Clinical and metabolic effects associated with weight changes and obeticholic acid in non-alcoholic steatohepatitis

(2018) B. Hameed et al.   ALIMENTARY PHARMACOLOGY & THERAPEUTICS

Effects of NGM282, an FGF19 variant, on colonic transit and bowel function in functional constipation: a randomized phase 2 trial

(2018) Ibironke Oduyebo et al.   AMERICAN JOURNAL OF GASTROENTEROLOGY

Farnesoid X receptor modulators 2014-present: a patent review

(2018) Valentina Sepe et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Mechanisms of MAFG Dysregulation in Cholestatic Liver Injury and Development of Liver Cancer

(2018) Ting Liu et al.   GASTROENTEROLOGY

Bile acids in glucose metabolism in health and disease

(2018) Hagit Shapiro et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Diet1, bile acid diarrhea, and FGF15/19: mouse model and human genetic variants

(2018) Jessica M. Lee et al.   JOURNAL OF LIPID RESEARCH

Future trends in the treatment of non-alcoholic steatohepatitis

(2018) Stefano Fiorucci et al.   PHARMACOLOGICAL RESEARCH

Inborn Errors of Bile Acid Metabolism

(2018) James E. Heubi et al.   Clinics in Liver Disease

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

Small Heterodimer Partner and Fibroblast Growth Factor 19 Inhibit Expression of NPC1L1 in Mouse Intestine and Cholesterol Absorption

(2018) Young-Chae Kim et al.   GASTROENTEROLOGY

FGF19 amplification reveals an oncogenic dependency upon autocrine FGF19/FGFR4 signaling in head and neck squamous cell carcinoma

(2018) Lixia Gao et al.   ONCOGENE

Role of TGR5 (GPBAR1) in Liver Disease

(2018) Dieter Häussinger et al.   SEMINARS IN LIVER DISEASE

Bile Acids and Their Derivatives as Potential Modifiers of Drug Release and Pharmacokinetic Profiles

(2018) Nebojša Pavlović et al.   Frontiers in Pharmacology

An RORγt Oral Inhibitor Modulates IL-17 Responses in Peripheral Blood and Intestinal Mucosa of Crohn's Disease Patients

(2018) Helena Bassolas-Molina et al.   Frontiers in Immunology

Developments in bile salt based therapies: A critical overview

(2018) Joanne M. Donkers et al.   BIOCHEMICAL PHARMACOLOGY

Fibroblast Growth Factor 21—Metabolic Role in Mice and Men

(2017) Harald Staiger et al.   ENDOCRINE REVIEWS

Regulation of selective autophagy: the p62/SQSTM1 paradigm

(2017) Trond Lamark et al.   Essays in Biochemistry

Intestinal Farnesoid X Receptor Controls Transintestinal Cholesterol Excretion in Mice

(2017) Jan Freark de Boer et al.   GASTROENTEROLOGY

Interactions between bile salts, gut microbiota, and hepatic innate immunity

(2017) Kristin Schubert et al.   IMMUNOLOGICAL REVIEWS

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

RNA-binding protein ZFP36L1 maintains posttranscriptional regulation of bile acid metabolism

(2017) Elizabeth J. Tarling et al.   JOURNAL OF CLINICAL INVESTIGATION

Nutrient-sensing nuclear receptors PPARα and FXR control liver energy balance

(2017) Geoffrey A. Preidis et al.   JOURNAL OF CLINICAL INVESTIGATION

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

Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance

(2017) Manuel Lasalle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Treatment of primary biliary cholangitis ursodeoxycholic acid non-responders: A systematic review

(2017) Duminda Suraweera et al.   LIVER INTERNATIONAL

Interactions between gut bacteria and bile in health and disease

(2017) Sarah L. Long et al.   MOLECULAR ASPECTS OF MEDICINE

Non-cell-autonomous activation of IL-6/STAT3 signaling mediates FGF19-driven hepatocarcinogenesis

(2017) Mei Zhou et al.   Nature Communications

Hyodeoxycholic acid derivatives as liver X receptor α and G-protein-coupled bile acid receptor agonists

(2017) Simona De Marino et al.   Scientific Reports

BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis

(2017) Adriana Carino et al.   Scientific Reports

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

Characterizing Factors Associated With Differences in FGF19 Blood Levels and Synthesis in Patients With Primary Bile Acid Diarrhea

(2016) Ian M Johnston et al.   AMERICAN JOURNAL OF GASTROENTEROLOGY

Chenodeoxycholic acid requires activation of EGFR, EPAC, and Ca2+ to stimulate CFTR-dependent Cl− secretion in human colonic T84 cells

(2016) Jada C. Domingue et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties

(2016) Olaf Kinzel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects

(2016) Saswata Talukdar et al.   Cell Metabolism

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

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

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

(2016) Cen Xie et al.   DIABETES

Therapeutic potential of Takeda-G-protein-receptor-5 (TGR5) agonists. Hope or hype?

(2016) R. J. Hodge et al.   DIABETES OBESITY & METABOLISM

An Intestinal Microbiota–Farnesoid X Receptor Axis Modulates Metabolic Disease

(2016) Frank J. Gonzalez et al.   GASTROENTEROLOGY

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

(2016) Chuansheng Guo et al.   IMMUNITY

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

(2016) Chuansheng Guo et al.   IMMUNITY

Activation of Transmembrane Bile Acid Receptor TGR5 Modulates Pancreatic Islet α Cells to Promote Glucose Homeostasis

(2016) Divya P. Kumar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Regulation of fibroblast growth factor 15/19 and 21 on metabolism: in the fed or fasted state

(2016) Dandan Guan et al.   Journal of Translational Medicine

A Novel Small Molecule Activator of Nuclear Receptor SHP Inhibits HCC Cell Migration via Suppressing Ccl2

(2016) Z. Yang et al.   MOLECULAR CANCER THERAPEUTICS

RORγt, a multitask nuclear receptor at mucosal surfaces

(2016) G Eberl   Mucosal Immunology

Transient inhibition of ROR-γt therapeutically limits intestinal inflammation by reducing TH17 cells and preserving group 3 innate lymphoid cells

(2016) David R Withers et al.   NATURE MEDICINE

A new frontier in FGF21 biology

(2016) Matthew J. Potthoff   Nature Reviews Endocrinology

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

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

Sphingosine 1-phosphate and sphingosine kinases in health and disease: Recent advances

(2016) Susan Pyne et al.   PROGRESS IN LIPID RESEARCH

Metabolic fibroblast growth factors (FGFs): Mediators of energy homeostasis

(2016) Kathleen R. Markan et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines

(2016) Adriana Carino et al.   Oncotarget

Fibroblast growth factor receptor 4 (FGFR4) and fibroblast growth factor 19 (FGF19) autocrine enhance breast cancer cells survival

(2016) Kai Hung Tiong et al.   Oncotarget

Chenodeoxycholic acid activates NLRP3 inflammasome and contributes to cholestatic liver fibrosis

(2016) Zizhen Gong et al.   Oncotarget

Bacterial bile salt hydrolase: an intestinal microbiome target for enhanced animal health

(2016) Wenjing Geng et al.   ANIMAL HEALTH RESEARCH REVIEWS

Fibroblast activation protein (FAP) as a novel metabolic target

(2016) Miguel Angel Sánchez-Garrido et al.   Molecular Metabolism

Bcl2 is a critical regulator of bile acid homeostasis by dictating Shp and lncRNA H19 function

(2016) Yuxia Zhang et al.   Scientific Reports

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

(2016) Valentina Sepe et al.   Scientific Reports

Upregulation of bile acid receptor TGR5 and nNOS in gastric myenteric plexus is responsible for delayed gastric emptying after chronic high-fat feeding in rats

(2015) Hui Zhou et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Cystathionine γ-lyase, a H2S-generating enzyme, is a GPBAR1-regulated gene and contributes to vasodilation caused by secondary bile acids

(2015) Barbara Renga et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

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

(2015) Björn Schittenhelm et al.   ENDOCRINOLOGY

Farnesoid X receptor modulators (2011 – 2014): a patent review

(2015) Valentina Sepe et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Interactions Between Nuclear Receptor SHP and FOXA1 Maintain Oscillatory Homocysteine Homeostasis in Mice

(2015) Hiroyuki Tsuchiya et al.   GASTROENTEROLOGY

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

Temporal changes in bile acid levels and 12α-hydroxylation after Roux-en-Y gastric bypass surgery in type 2 diabetes

(2015) R Dutia et al.   INTERNATIONAL JOURNAL OF OBESITY

Interplay between FGF21 and insulin action in the liver regulates metabolism

(2015) Brice Emanuelli et al.   JOURNAL OF CLINICAL INVESTIGATION

Progression from Nonalcoholic Fatty Liver to Nonalcoholic Steatohepatitis Is Marked by a Higher Frequency of Th17 Cells in the Liver and an Increased Th17/Resting Regulatory T Cell Ratio in Peripheral Blood and in the Liver

(2015) Monika Rau et al.   JOURNAL OF IMMUNOLOGY

Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes

(2015) Hongliang Duan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Farnesoid X receptor agonist CDCA reduces blood pressure and regulates vascular tone in spontaneously hypertensive rats

(2015) Chenyu Li et al.   Journal of the American Society of Hypertension

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

LC3- and p62-based biochemical methods for the analysis of autophagy progression in mammalian cells

(2015) Peidu Jiang et al.   METHODS

Retinoic acid receptors: From molecular mechanisms to cancer therapy

(2015) Alessandra di Masi et al.   MOLECULAR ASPECTS OF MEDICINE

Minireview: Roles of Fibroblast Growth Factors 19 and 21 in Metabolic Regulation and Chronic Diseases

(2015) Fangfang Zhang et al.   MOLECULAR ENDOCRINOLOGY

Innate lymphoid cells in the initiation, regulation and resolution of inflammation

(2015) Gregory F Sonnenberg et al.   NATURE MEDICINE

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

(2015) Sungsoon Fang et al.   NATURE MEDICINE

FGF 19 and Bile Acids Increase Following Roux-en-Y Gastric Bypass but Not After Medical Management in Patients with Type 2 Diabetes

(2015) Saachi Sachdev et al.   OBESITY SURGERY

Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling

(2015) Sabrina Cipriani et al.   PLoS One

Individual bile acids have differential effects on bile acid signaling in mice

(2015) Peizhen Song et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Bile Acid-Activated Receptors, Intestinal Microbiota, and the Treatment of Metabolic Disorders

(2015) Stefano Fiorucci et al.   TRENDS IN MOLECULAR MEDICINE

TGR5 and Immunometabolism: Insights from Physiology and Pharmacology

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

Small heterodimer partner interacts with NLRP3 and negatively regulates activation of the NLRP3 inflammasome

(2015) Chul-Su Yang et al.   Nature Communications

Farnesoid X receptor inhibits glucagon-like peptide-1 production by enteroendocrine L cells

(2015) Mohamed-Sami Trabelsi et al.   Nature Communications

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

(2015) Changtao Jiang et al.   Nature Communications

Bile acids induce hepatic differentiation of mesenchymal stem cells

(2015) Iris Sawitza et al.   Scientific Reports

Bioenergetic cues shift FXR splicing towards FXRα2 to modulate hepatic lipolysis and fatty acid metabolism

(2015) Jorge C. Correia et al.   Molecular Metabolism

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

Genetic variation in GPBAR1 predisposes to quantitative changes in colonic transit and bile acid excretion

(2014) Michael Camilleri et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Separating Tumorigenicity from Bile Acid Regulatory Activity for Endocrine Hormone FGF19

(2014) M. Zhou et al.   CANCER RESEARCH

Bile acids and the gut microbiome

(2014) Jason M. Ridlon et al.   CURRENT OPINION IN GASTROENTEROLOGY

FGF21 Maintains Glucose Homeostasis by Mediating the Cross Talk Between Liver and Brain During Prolonged Fasting

(2014) Q. Liang et al.   DIABETES

Circulating FGF21 Is Liver Derived and Enhances Glucose Uptake During Refeeding and Overfeeding

(2014) K. R. Markan et al.   DIABETES

4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists

(2014) Qingan Zou et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Fibroblast Growth Factor 21 Limits Lipotoxicity by Promoting Hepatic Fatty Acid Activation in Mice on Methionine and Choline-Deficient Diets

(2014) Ffolliott M. Fisher et al.   GASTROENTEROLOGY

The Bile Acid Receptor TGR5 Activates the TRPA1 Channel to Induce Itch in Mice

(2014) TinaMarie Lieu et al.   GASTROENTEROLOGY

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

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

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

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

First Results from the LUX Dark Matter Experiment at the Sanford Underground Research Facility

(2014) D. S. Akerib et al.   PHYSICAL REVIEW LETTERS

Dual Activation of the Bile Acid Nuclear Receptor FXR and G-Protein-Coupled Receptor TGR5 Protects Mice against Atherosclerosis

(2014) Shinobu Miyazaki-Anzai et al.   PLoS One

Microbiota-Dependent Crosstalk Between Macrophages and ILC3 Promotes Intestinal Homeostasis

(2014) A. Mortha et al.   SCIENCE

Ciliary subcellular localization of TGR5 determines the cholangiocyte functional response to bile acid signaling

(2013) Anatoliy I. Masyuk et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Fibroblast Growth Factor 23 and Klotho: Physiology and Pathophysiology of an Endocrine Network of Mineral Metabolism

(2013) Ming Chang Hu et al.   Annual Review of Physiology

Differential activation of the human farnesoid X receptor depends on the pattern of expressed isoforms and the bile acid pool composition

(2013) Javier Vaquero et al.   BIOCHEMICAL PHARMACOLOGY

Cloning and analysis of bile salt hydrolase genes from Lactobacillus plantarum CGMCC No. 8198

(2013) Xiang-Chao Gu et al.   BIOTECHNOLOGY LETTERS

Diet1 Functions in the FGF15/19 Enterohepatic Signaling Axis to Modulate Bile Acid and Lipid Levels

(2013) Laurent Vergnes et al.   Cell Metabolism

Adiponectin Mediates the Metabolic Effects of FGF21 on Glucose Homeostasis and Insulin Sensitivity in Mice

(2013) Zhuofeng Lin et al.   Cell Metabolism

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

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

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

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

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

Crosstalk between hydrogen sulfide and nitric oxide in endothelial cells

(2013) Zaid Altaany et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

The TGR5 receptor mediates bile acid–induced itch and analgesia

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

Bile acids PKA-dependently induce a switch of the IL-10/IL-12 ratio and reduce proinflammatory capability of human macrophages

(2013) Katrin Haselow et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Mechanistic insights into isoform-dependent and species-specific regulation of bile salt export pump by farnesoid X receptor

(2013) Xiulong Song et al.   JOURNAL OF LIPID RESEARCH

Understanding nuclear receptor form and function using structural biology

(2013) Fraydoon Rastinejad et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

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

Clinical application of transcriptional activators of bile salt transporters

(2013) Anna Baghdasaryan et al.   MOLECULAR ASPECTS OF MEDICINE

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

(2013) Fei Li et al.   Nature Communications

Activation of G protein-coupled bile acid receptor, TGR5, induces smooth muscle relaxation via both Epac- and PKA-mediated inhibition of RhoA/Rho kinase pathway

(2012) Senthilkumar Rajagopal et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic β cells

(2012) Divya P. Kumar et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

βKlotho Is Required for Fibroblast Growth Factor 21 Effects on Growth and Metabolism

(2012) Xunshan Ding et al.   Cell Metabolism

A Ceramide-Centric View of Insulin Resistance

(2012) Jose A. Chavez et al.   Cell Metabolism

2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)

(2012) Rainer E. Martin et al.   ChemMedChem

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 Receptor TGR5 Mediates the Prokinetic Actions of Intestinal Bile Acids and Is Required for Normal Defecation in Mice

(2012) Farzad Alemi et al.   GASTROENTEROLOGY

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

Bile acids induce monocyte differentiation toward interleukin-12 hypo-producing dendritic cells via a TGR5-dependent pathway

(2012) Riko Ichikawa et al.   IMMUNOLOGY

Molecular cloning, characterization and comparison of bile salt hydrolases fromLactobacillus johnsoniiPF01

(2012) J.P. Chae et al.   JOURNAL OF APPLIED MICROBIOLOGY

Orphan Nuclear Receptor Small Heterodimer Partner Negatively Regulates Growth Hormone-mediated Induction of Hepatic Gluconeogenesis through Inhibition of Signal Transducer and Activator of Transcription 5 (STAT5) Transactivation

(2012) Yong Deuk Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Activation of the Farnesoid X Receptor Induces Hepatic Expression and Secretion of Fibroblast Growth Factor 21

(2012) Holly A. Cyphert et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dual actions of fibroblast growth factor 19 on lipid metabolism

(2012) Xinle Wu et al.   JOURNAL OF LIPID RESEARCH

Design, Synthesis, and Antidiabetic Activity of 4-Phenoxynicotinamide and 4-Phenoxypyrimidine-5-carboxamide Derivatives as Potent and Orally Efficacious TGR5 Agonists

(2012) Hongliang Duan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Transcriptional integration of metabolism by the nuclear sterol-activated receptors LXR and FXR

(2012) Anna C. Calkin et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Discovery That Theonellasterol a Marine Sponge Sterol Is a Highly Selective FXR Antagonist That Protects against Liver Injury in Cholestasis

(2012) Barbara Renga et al.   PLoS One

Targeting FGFR4 Inhibits Hepatocellular Carcinoma in Preclinical Mouse Models

(2012) Dorothy M. French et al.   PLoS One

FGF21 Requires βklotho to Act In Vivo

(2012) Andrew C. Adams et al.   PLoS One

Regulation of Amphiregulin Gene Expression by β-Catenin Signaling in Human Hepatocellular Carcinoma Cells: A Novel Crosstalk between FGF19 and the EGFR System

(2012) Maria U. Latasa et al.   PLoS One

Effect of bypassing the proximal gut on gut hormones involved with glycemic control and weight loss

(2012) Dimitri J. Pournaras et al.   Surgery for Obesity and Related Diseases

Marine sponge steroids as nuclear receptor ligands

(2012) Stefano Fiorucci et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Fibroblast Growth Factor 19 Treatment Ameliorates Disruption of Hepatic Lipid Metabolism in Farnesoid X Receptor (Fxr)-Null Mice

(2011) Masaaki Miyata et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Identification of a Therapeutic Strategy Targeting Amplified FGF19 in Liver Cancer by Oncogenomic Screening

(2011) Eric T. Sawey et al.   CANCER CELL

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

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

(2011) J. Prawitt et al.   DIABETES

Adipogenesis and insulin sensitivity in obesity are regulated by retinoid-related orphan receptor gamma

(2011) Bettina Meissburger et al.   EMBO Molecular Medicine

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

(2011) Elaine Studer et al.   HEPATOLOGY

Urinary bile acid sulfate levels in patients with primary biliary cirrhosis

(2011) Ryo Miura et al.   HEPATOLOGY RESEARCH

Development and evolution of RORγt+ cells in a microbe’s world

(2011) Gérard Eberl   IMMUNOLOGICAL REVIEWS

Pronounced variation in bile acid synthesis in humans is related to gender, hypertriglyceridaemia and circulating levels of fibroblast growth factor 19

(2011) C. Gälman et al.   JOURNAL OF INTERNAL MEDICINE

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

RORγt+ innate lymphoid cells regulate intestinal homeostasis by integrating negative signals from the symbiotic microbiota

(2011) Shinichiro Sawa et al.   NATURE IMMUNOLOGY

The orphan nuclear receptor SHP acts as a negative regulator in inflammatory signaling triggered by Toll-like receptors

(2011) Jae-Min Yuk et al.   NATURE IMMUNOLOGY

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

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

(2011) S. Kir et al.   SCIENCE

The hepatic response to FGF19 is impaired in patients with nonalcoholic fatty liver disease and insulin resistance

(2010) Tim C. M. A. Schreuder et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

A Role of the Bile Salt Receptor FXR in Atherosclerosis

(2010) Jurre Hageman et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain

(2010) Verena Keitel et al.   GLIA

Gender-dependent effect of Gpbar1 genetic deletion on the metabolic profiles of diet-induced obese mice

(2010) Galya Vassileva et al.   JOURNAL OF ENDOCRINOLOGY

Microbiota-induced tertiary lymphoid tissues aggravate inflammatory disease in the absence of RORγt and LTi cells

(2010) Matthias Lochner et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Bile acids regulate hepatic gluconeogenic genes and farnesoid X receptor via Gαi-protein-coupled receptors and the AKT pathway

(2010) Risheng Cao et al.   JOURNAL OF LIPID RESEARCH

Structural Basis for Hydroxycholesterols as Natural Ligands of Orphan Nuclear Receptor RORγ

(2010) Lihua Jin et al.   MOLECULAR ENDOCRINOLOGY

Research Resource: Comprehensive Expression Atlas of the Fibroblast Growth Factor System in Adult Mouse

(2010) Klementina Fon Tacer et al.   MOLECULAR ENDOCRINOLOGY

A human gut microbial gene catalogue established by metagenomic sequencing

(2010) Junjie Qin et al.   NATURE

Expression and function of the bile acid receptor GpBAR1 (TGR5) in the murine enteric nervous system

(2010) D. P. Poole et al.   NEUROGASTROENTEROLOGY AND MOTILITY

The Bile Acid Sensor FXR Protects against Dyslipidemia and Aortic Plaques Development Induced by the HIV Protease Inhibitor Ritonavir in Mice

(2010) Andrea Mencarelli et al.   PLoS One

Involvement of the vitamin D receptor in energy metabolism: regulation of uncoupling proteins

(2009) Kari E. Wong et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia

(2009) Mark J. Evans et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

IL-17 and Th17 Cells

(2009) Thomas Korn et al.   Annual Review of Immunology

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Role of a novel bile acid receptor TGR5 in the development of oesophageal adenocarcinoma

(2009) J. Hong et al.   GUT

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

(2009) Verena Keitel et al.   HEPATOLOGY

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

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

The Bile Acid Sensor Farnesoid X Receptor Is a Modulator of Liver Immunity in a Rodent Model of Acute Hepatitis

(2009) A. Mencarelli et al.   JOURNAL OF IMMUNOLOGY

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

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

Glucose stimulates cholesterol 7α-hydroxylase gene transcription in human hepatocytes

(2009) Tiangang Li et al.   JOURNAL OF LIPID RESEARCH

Bile acids: analysis in biological fluids and tissues

(2009) William J. Griffiths et al.   JOURNAL OF LIPID RESEARCH

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

Bile acids: regulation of synthesis

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

Discovery of 6α-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity

(2009) Roberto Pellicciari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Serum Bile Acids Are Higher in Humans With Prior Gastric Bypass: Potential Contribution to Improved Glucose and Lipid Metabolism

(2009) Mary-Elizabeth Patti et al.   Obesity

Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation

(2009) Philippe Lefebvre et al.   PHYSIOLOGICAL REVIEWS

Selective activation of FGFR4 by an FGF19 variant does not improve glucose metabolism in ob/ob mice

(2009) X. Wu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

FGF21 induces PGC-1  and regulates carbohydrate and fatty acid metabolism during the adaptive starvation response

(2009) M. J. Potthoff et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Bile acid-activated receptors in the treatment of dyslipidemia and related disorders

(2009) Stefano Fiorucci et al.   PROGRESS IN LIPID RESEARCH

Antiatherosclerotic effect of farnesoid X receptor

(2008) Andrea Mencarelli et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

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

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

Inhibition of Growth Hormone Signaling by the Fasting-Induced Hormone FGF21

(2008) Takeshi Inagaki et al.   Cell Metabolism

Activation of the farnesoid X receptor represses PCSK9 expression in human hepatocytes

(2008) Cédric Langhi et al.   FEBS LETTERS

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

C-terminal Tail of FGF19 Determines Its Specificity toward Klotho Co-receptors

(2008) Xinle Wu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Adopting New Orphans into the Family of Metabolic Regulators

(2008) Sarah Hummasti et al.   MOLECULAR ENDOCRINOLOGY

Endocrine and paracrine role of bile acids

(2008) Verena Keitel et al.   WORLD JOURNAL OF GASTROENTEROLOGY

FGF-21/FGF-21 receptor interaction and activation is determined by βKlotho

(2007) Alexei Kharitonenkov et al.   JOURNAL OF CELLULAR PHYSIOLOGY