Bile acid receptors as targets for drug development

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

Trimethylamine-N-Oxide, a Metabolite Associated with Atherosclerosis, Exhibits Complex Genetic and Dietary Regulation

(2013) Brian J. Bennett et al.   Cell Metabolism

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

The TGR5 receptor mediates bile acid–induced itch and analgesia

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

Nuclear receptor atlas of female mouse liver parenchymal, endothelial, and Kupffer cells

(2013) Zhaosha Li et al.   PHYSIOLOGICAL GENOMICS

Anti-inflammatory and metabolic actions of FXR: Insights into molecular mechanisms

(2012) Danielle A.A. Hollman et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists

(2012) Maura Marinozzi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Increased Bile Acid Biosynthesis Is Associated With Irritable Bowel Syndrome With Diarrhea

(2012) Banny S. Wong et al.   Clinical Gastroenterology and Hepatology

Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis

(2012) Luciano Adorini et al.   DRUG DISCOVERY TODAY

Role of CAR and PXR in xenobiotic sensing and metabolism

(2012) Yue-Ming Wang et al.   Expert Opinion on Drug Metabolism & Toxicology

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

α5β1-integrins are sensors for tauroursodeoxycholic acid in hepatocytes

(2012) Holger Gohlke et al.   HEPATOLOGY

Serum autotaxin is increased in pruritus of cholestasis, but not of other origin, and responds to therapeutic interventions

(2012) Andreas E. Kremer et al.   HEPATOLOGY

Farnesoid X receptor inhibits gankyrin in mouse livers and prevents development of liver cancer

(2012) Yanjun Jiang et al.   HEPATOLOGY

Nuclear Receptors HNF4α and LRH-1 Cooperate in RegulatingCyp7a1 in Vivo

(2012) Serkan Kir et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

FXR Controls the Tumor Suppressor NDRG2 and FXR Agonists Reduce Liver Tumor Growth and Metastasis in an Orthotopic Mouse Xenograft Model

(2012) Ulrich Deuschle et al.   PLoS One

Lithocholic acid is an endogenous inhibitor of MDM4 and MDM2

(2012) S. M. Vogel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting xenobiotic receptors PXR and CAR for metabolic diseases

(2012) Jie Gao et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Pregnane X receptor as a target for treatment of inflammatory bowel disorders

(2012) Jie Cheng et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

TGR5 potentiates GLP-1 secretion in response to anionic exchange resins

(2012) Taoufiq Harach et al.   Scientific Reports

Effect of bile acid sequestrants on glycaemic control: protocol for a systematic review with meta-analysis of randomised controlled trials

(2012) Morten Hansen et al.   BMJ Open

Bile Acids Induce Inflammatory Genes in Hepatocytes

(2011) Katryn Allen et al.   AMERICAN JOURNAL OF PATHOLOGY

Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes

(2011) Lihong Chen et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Farnesoid X receptor suppresses constitutive androstane receptor activity at the multidrug resistance protein-4 promoter

(2011) Barbara Renga et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Proteomics for the discovery of nuclear bile acid receptor FXR targets

(2011) Cissi Gardmo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Nuclear receptor PXR, transcriptional circuits and metabolic relevance

(2011) Chibueze A. Ihunnah et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

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

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

Alterations of Hormonally Active Fibroblast Growth Factors after Roux-en-Y Gastric Bypass Surgery

(2011) Peter L.M. Jansen et al.   DIGESTIVE DISEASES

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

(2011) R. M. Gadaleta et al.   GUT

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

Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2 −/− (Abcb4 −/− ) mouse cholangiopathy model by promoting biliary HCO 3− output

(2011) Anna Baghdasaryan 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

FXR and PXR: Potential therapeutic targets in cholestasis

(2011) Johan W. Jonker et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

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

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

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

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

Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists

(2010) Ulrich Abel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5

(2010) Mark R. Herbert et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Conformationally constrained farnesoid X receptor (FXR) agonists: Heteroaryl replacements of the naphthalene

(2010) Jonathan Y. Bass et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Diabetic Nephropathy Is Accelerated by Farnesoid X Receptor Deficiency and Inhibited by Farnesoid X Receptor Activation in a Type 1 Diabetes Model

(2010) X. X. Wang et al.   DIABETES

Lysophosphatidic Acid Is a Potential Mediator of Cholestatic Pruritus

(2010) Andreas E. Kremer et al.   GASTROENTEROLOGY

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

(2010) Verena Keitel et al.   GLIA

Nor-ursodeoxycholic acid reverses hepatocyte-specific nemo-dependent steatohepatitis

(2010) N. Beraza et al.   GUT

Glycosylation of fibroblast growth factor receptor 4 is a key regulator of fibroblast growth factor 19-mediated down-regulation of cytochrome P450 7A1

(2010) Vassilis Triantis et al.   HEPATOLOGY

The biliary HCO3− umbrella: A unifying hypothesis on pathogenetic and therapeutic aspects of fibrosing cholangiopathies

(2010) Ulrich Beuers et al.   HEPATOLOGY

Regulation of Bile Acid Synthesis by Fat-soluble Vitamins A and D

(2010) Daniel R. Schmidt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

(2010) Thijs W.H. Pols et al.   JOURNAL OF HEPATOLOGY

The PXR is a drug target for chronic inflammatory liver disease

(2010) Karen Wallace et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

A Novel Bile Acid-Activated Vitamin D Receptor Signaling in Human Hepatocytes

(2010) Shuxin Han et al.   MOLECULAR ENDOCRINOLOGY

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 Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling

(2010) Kristine A. Drafahl et al.   PLoS One

Separating mitogenic and metabolic activities of fibroblast growth factor 19 (FGF19)

(2010) X. Wu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activation of Pregnane X Receptor (PXR) and Constitutive Androstane Receptor (CAR) by Herbal Medicines

(2009) Thomas K. H. Chang   AAPS Journal

Farnesoid X Receptor Critically Determines the Fibrotic Response in Mice but Is Expressed to a Low Extent in Human Hepatic Stellate Cells and Periductal Myofibroblasts

(2009) Peter Fickert et al.   AMERICAN JOURNAL OF PATHOLOGY

Improvement in Glucose Metabolism After Bariatric Surgery: Comparison of Laparoscopic Roux-en-Y Gastric Bypass and Laparoscopic Sleeve Gastrectomy

(2009) Ralph Peterli et al.   ANNALS OF SURGERY

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

Constitutive Androstane Receptor-Mediated Changes in Bile Acid Composition Contributes to Hepatoprotection from Lithocholic Acid-Induced Liver Injury in Mice

(2009) L. D. Beilke et al.   DRUG METABOLISM AND DISPOSITION

p-ANCAs in autoimmune liver disorders recognise human  -tubulin isotype 5 and cross-react with microbial protein FtsZ

(2009) B. Terjung et al.   GUT

Age-specific prognosis following spontaneous hepatitis B e antigen seroconversion in chronic hepatitis B

(2009) Yi-Cheng Chen et al.   HEPATOLOGY

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

(2009) Verena Keitel et al.   HEPATOLOGY

EASL Clinical Practice Guidelines: Management of cholestatic liver diseases

(2009)   JOURNAL OF HEPATOLOGY

Bile acid transporters

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

Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/−and apoE−/−mice

(2009) Helen B. Hartman et al.   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

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

Antiatherosclerotic effect of farnesoid X receptor

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

PPARα gene expression is up-regulated by LXR and PXR activators in the small intestine

(2008) Jun Inoue et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

FXR: a metabolic regulator and cell protector

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

Mechanism of Vitamin D Receptor Inhibition of Cholesterol 7 -Hydroxylase Gene Transcription in Human Hepatocytes

(2008) S. Han et al.   DRUG METABOLISM AND DISPOSITION

Bile Salts Control the Antimicrobial Peptide Cathelicidin Through Nuclear Receptors in the Human Biliary Epithelium

(2008) Emilie D'Aldebert et al.   GASTROENTEROLOGY

High expression of the bile salt-homeostatic hormone fibroblast growth factor 19 in the liver of patients with extrahepatic cholestasis

(2008) Frank G. Schaap 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

Vitamin D3 Modulates the Expression of Bile Acid Regulatory Genes and Represses Inflammation in Bile Duct-Ligated Mice

(2008) M. Ogura et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation

(2008) S. M. Soisson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hepatic Fatty Acid Transporter Cd36 Is a Common Target of LXR, PXR, and PPARγ in Promoting Steatosis

(2007) Jie Zhou et al.   GASTROENTEROLOGY