Bile acid receptors as targets for drug development

[1]  S. Mudaliar,et al.  Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease. , 2013, Gastroenterology.

[2]  C. Sadowsky,et al.  A 24‐Week, Randomized, Controlled Trial of Rivastigmine Patch 13.3 mg/24 h Versus 4.6 mg/24 h in Severe Alzheimer's Dementia , 2013, CNS Neuroscience & Therapeutics.

[3]  T. V. van Berkel,et al.  Nuclear receptor atlas of female mouse liver parenchymal, endothelial, and Kupffer cells. , 2013, Physiological genomics.

[4]  F. Cattaruzza,et al.  The TGR5 receptor mediates bile acid-induced itch and analgesia. , 2013, The Journal of clinical investigation.

[5]  H. Gohlke,et al.  α5β1‐integrins are sensors for tauroursodeoxycholic acid in hepatocytes , 2013, Hepatology.

[6]  D. Moore,et al.  Farnesoid X receptor inhibits gankyrin in mouse livers and prevents development of liver cancer , 2013, Hepatology.

[7]  Brian J. Bennett,et al.  Trimethylamine-N-oxide, a metabolite associated with atherosclerosis, exhibits complex genetic and dietary regulation. , 2013, Cell metabolism.

[8]  S. Morini,et al.  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, Gut.

[9]  F. Bäckhed,et al.  Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist. , 2013, Cell metabolism.

[10]  F. Cattaruzza,et al.  The receptor TGR5 mediates the prokinetic actions of intestinal bile acids and is required for normal defecation in mice. , 2013, Gastroenterology.

[11]  M. Miyazaki,et al.  Synthetic Farnesoid X Receptor Agonists Induce High-Density Lipoprotein-Mediated Transhepatic Cholesterol Efflux in Mice and Monkeys and Prevent Atherosclerosis in Cholesteryl Ester Transfer Protein Transgenic Low-Density Lipoprotein Receptor (−/−) Mice , 2012, Journal of Pharmacology and Experimental Therapeutics.

[12]  T. Vilsbøll,et al.  Effect of bile acid sequestrants on glycaemic control: protocol for a systematic review with meta-analysis of randomised controlled trials , 2012, BMJ Open.

[13]  K. V. van Erpecum,et al.  Anti-inflammatory and metabolic actions of FXR: insights into molecular mechanisms. , 2012, Biochimica et biophysica acta.

[14]  U. Deuschle,et al.  FXR Controls the Tumor Suppressor NDRG2 and FXR Agonists Reduce Liver Tumor Growth and Metastasis in an Orthotopic Mouse Xenograft Model , 2012, PloS one.

[15]  S. Kliewer,et al.  Nuclear Receptors HNF4α and LRH-1 Cooperate in Regulating Cyp7a1 in Vivo* , 2012, The Journal of Biological Chemistry.

[16]  Rainer Wilcken,et al.  Lithocholic acid is an endogenous inhibitor of MDM4 and MDM2 , 2012, Proceedings of the National Academy of Sciences.

[17]  W. Xie,et al.  Targeting xenobiotic receptors PXR and CAR for metabolic diseases. , 2012, Trends in pharmacological sciences.

[18]  R. Jalan,et al.  Serum autotaxin is increased in pruritus of cholestasis, but not of other origin and responds to therapeutic interventions , 2015 .

[19]  A. Zinsmeister,et al.  Increased bile acid biosynthesis is associated with irritable bowel syndrome with diarrhea. , 2012, Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association.

[20]  L. Adorini,et al.  Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis. , 2012, Drug discovery today.

[21]  M. Downes,et al.  FXR and PXR: Potential therapeutic targets in cholestasis , 2012, The Journal of Steroid Biochemistry and Molecular Biology.

[22]  S. Ong,et al.  Role of CAR and PXR in xenobiotic sensing and metabolism , 2012, Expert opinion on drug metabolism & toxicology.

[23]  L. Adorini,et al.  Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists. , 2012, Bioorganic & medicinal chemistry.

[24]  F. Gonzalez,et al.  Pregnane X receptor as a target for treatment of inflammatory bowel disorders. , 2012, Trends in pharmacological sciences.

[25]  J. Auwerx,et al.  TGR5 potentiates GLP-1 secretion in response to anionic exchange resins , 2012, Scientific Reports.

[26]  D. Gouma,et al.  The human gallbladder secretes fibroblast growth factor 19 into bile: Towards defining the role of fibroblast growth factor 19 in the enterobiliary tract , 2012, Hepatology.

[27]  L. Desnoyers,et al.  FGF19 and cancer. , 2012, Advances in experimental medicine and biology.

[28]  D. Rajpal,et al.  Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes. , 2012, American journal of physiology. Endocrinology and metabolism.

[29]  J. Auwerx,et al.  TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. , 2011, Cell metabolism.

[30]  K. Yoshinari,et al.  Fibroblast growth factor 19 treatment ameliorates disruption of hepatic lipid metabolism in farnesoid X receptor (Fxr)-null mice. , 2011, Biological & pharmaceutical bulletin.

[31]  A. Hofmann.  Faculty Opinions recommendation of The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor κ light-chain enhancer of activated B cells (NF-κB) in mice. , 2011 .

[32]  B. M. Forman,et al.  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, Hepatology.

[33]  A. Baghdasaryan,et al.  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, Hepatology.

[34]  A. Moschetta,et al.  Proteomics for the discovery of nuclear bile acid receptor FXR targets☆ , 2011, Biochimica et biophysica acta.

[35]  Wen Xie,et al.  Nuclear receptor PXR, transcriptional circuits and metabolic relevance. , 2011, Biochimica et biophysica acta.

[36]  F. Baldelli,et al.  Farnesoid X receptor agonist for the treatment of liver and metabolic disorders: focus on 6-ethyl-CDCA. , 2011, Mini reviews in medicinal chemistry.

[37]  S. Kliewer,et al.  FGF15/19 regulates hepatic glucose metabolism by inhibiting the CREB-PGC-1α pathway. , 2011, Cell metabolism.

[38]  J. Auwerx,et al.  The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation. , 2011, Journal of hepatology.

[39]  J. Stoker,et al.  Alterations of Hormonally Active Fibroblast Growth Factors after Roux-en-Y Gastric Bypass Surgery , 2011, Digestive Diseases.

[40]  S. Kliewer,et al.  The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling. , 2011, Molecular endocrinology.

[41]  S. Kliewer,et al.  FGF19 as a Postprandial, Insulin-Independent Activator of Hepatic Protein and Glycogen Synthesis , 2011, Science.

[42]  Marco Migliorati,et al.  Farnesoid X receptor suppresses constitutive androstane receptor activity at the multidrug resistance protein-4 promoter. , 2011, Biochimica et biophysica acta.

[43]  Shawn P Williams,et al.  Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene. , 2011, Bioorganic & medicinal chemistry letters.

[44]  P. Siersema,et al.  Farnesoid X receptor activation inhibits inflammation and preserves the intestinal barrier in inflammatory bowel disease , 2011, Gut.

[45]  H. Jaeschke,et al.  Bile acids induce inflammatory genes in hepatocytes: a novel mechanism of inflammation during obstructive cholestasis. , 2011, The American journal of pathology.

[46]  A. N. Meyer,et al.  The Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling , 2010, PloS one.

[47]  C. Trautwein,et al.  Nor-ursodeoxycholic acid reverses hepatocyte-specific nemo-dependent steatohepatitis , 2010, Gut.

[48]  K. Zilles,et al.  The bile acid receptor TGR5 (Gpbar‐1) acts as a neurosteroid receptor in brain , 2010, Glia.

[49]  T. Rao,et al.  Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5. , 2010, Bioorganic & medicinal chemistry letters.

[50]  U. Beuers,et al.  The biliary HCO3− umbrella: A unifying hypothesis on pathogenetic and therapeutic aspects of fibrosing cholangiopathies , 2010, Hepatology.

[51]  L. Adorini,et al.  Functional Characterization of the Semisynthetic Bile Acid Derivative INT-767, a Dual Farnesoid X Receptor and TGR5 Agonist , 2010, Molecular Pharmacology.

[52]  J. Prieto,et al.  Lysophosphatidic acid is a potential mediator of cholestatic pruritus. , 2010, Gastroenterology.

[53]  U. Deuschle,et al.  Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. , 2010, Bioorganic & medicinal chemistry letters.

[54]  L. Adorini,et al.  Diabetic Nephropathy Is Accelerated by Farnesoid X Receptor Deficiency and Inhibited by Farnesoid X Receptor Activation in a Type 1 Diabetes Model , 2010, Diabetes.

[55]  P. Jansen,et al.  Glycosylation of fibroblast growth factor receptor 4 is a key regulator of fibroblast growth factor 19–mediated down‐regulation of cytochrome P450 7A1 , 2010, Hepatology.

[56]  B. Lemon,et al.  Separating mitogenic and metabolic activities of fibroblast growth factor 19 (FGF19) , 2010, Proceedings of the National Academy of Sciences.

[57]  S. Hill,et al.  Journal of Steroid Biochemistry and Molecular Biology the Pxr Is a Drug Target for Chronic Inflammatory Liver Disease , 2022 .

[58]  S. Strom,et al.  A novel bile acid-activated vitamin D receptor signaling in human hepatocytes. , 2010, Molecular endocrinology.

[59]  S. Kliewer,et al.  Regulation of Bile Acid Synthesis by Fat-soluble Vitamins A and D* , 2010, The Journal of Biological Chemistry.

[60]  A. Nederveen,et al.  The hepatic response to FGF19 is impaired in patients with nonalcoholic fatty liver disease and insulin resistance. , 2010, American journal of physiology. Gastrointestinal and liver physiology.

[61]  B. M. Forman,et al.  Farnesoid X receptor alleviates age‐related proliferation defects in regenerating mouse livers by activating forkhead box m1b transcription , 2009, Hepatology.

[62]  K. Behrns.  Improvement in Glucose Metabolism After Bariatric Surgery: Comparison of Laparoscopic Roux-en-Y Gastric Bypass and Laparoscopic Sleeve Gastrectomy: A Prospective Randomized Trial , 2010 .

[63]  K. Zatloukal,et al.  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, The American journal of pathology.

[64]  T. Sauerbruch,et al.  p-ANCAs in autoimmune liver disorders recognise human β-tubulin isotype 5 and cross-react with microbial protein FtsZ , 2009, Gut.

[65]  J. Auwerx,et al.  Discovery of 6alpha-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, Journal of medicinal chemistry.

[66]  J. Auwerx,et al.  TGR5-mediated bile acid sensing controls glucose homeostasis. , 2009, Cell metabolism.

[67]  D. Häussinger,et al.  The membrane‐bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders , 2009, Hepatology.

[68]  Thomas K. H. Chang.  Activation of Pregnane X Receptor (PXR) and Constitutive Androstane Receptor (CAR) by Herbal Medicines , 2009, The AAPS Journal.

[69]  C. Beglinger,et al.  Improvement in Glucose Metabolism After Bariatric Surgery: Comparison of Laparoscopic Roux-en-Y Gastric Bypass and Laparoscopic Sleeve Gastrectomy: A Prospective Randomized Trial , 2009, Annals of surgery.

[70]  M. Evans,et al.  Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/− and apoE−/− mice Published, JLR Papers in Press, January 27, 2009. , 2009, Journal of Lipid Research.

[71]  D. Besselsen,et al.  Constitutive Androstane Receptor-Mediated Changes in Bile Acid Composition Contributes to Hepatoprotection from Lithocholic Acid-Induced Liver Injury in Mice , 2009, Drug Metabolism and Disposition.

[72]  D. Gouma,et al.  High expression of the bile salt‐homeostatic hormone fibroblast growth factor 19 in the liver of patients with extrahepatic cholestasis , 2009, Hepatology.

[73]  D. Wendum,et al.  Bile salts control the antimicrobial peptide cathelicidin through nuclear receptors in the human biliary epithelium. , 2009, Gastroenterology.

[74]  J. Chiang,et al.  Mechanism of Vitamin D Receptor Inhibition of Cholesterol 7α-Hydroxylase Gene Transcription in Human Hepatocytes , 2009, Drug Metabolism and Disposition.

[75]  E. Distrutti,et al.  Antiatherosclerotic effect of farnesoid X receptor. , 2009, American journal of physiology. Heart and circulatory physiology.

[76]  M. Makishima,et al.  Vitamin D3 Modulates the Expression of Bile Acid Regulatory Genes and Represses Inflammation in Bile Duct-Ligated Mice , 2009, Journal of Pharmacology and Experimental Therapeutics.

[77]  Stefan Westin,et al.  Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR). , 2009, Journal of medicinal chemistry.

[78]  F. Lammert,et al.  EASL Clinical Practice Guidelines: management of cholestatic liver diseases. , 2009, Journal of hepatology.

[79]  D. Moore,et al.  FXR: a metabolic regulator and cell protector , 2008, Cell Research.

[80]  J. Inoue,et al.  PPARalpha gene expression is up-regulated by LXR and PXR activators in the small intestine. , 2008, Biochemical and biophysical research communications.

[81]  J. W. Becker,et al.  Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation , 2008, Proceedings of the National Academy of Sciences.

[82]  J. Auwerx,et al.  Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. , 2008, Journal of medicinal chemistry.

[83]  Jie Zhou,et al.  Hepatic fatty acid transporter Cd36 is a common target of LXR, PXR, and PPARgamma in promoting steatosis. , 2008, Gastroenterology.

[84]  S. Kliewer,et al.  Differential regulation of bile acid homeostasis by the farnesoid X receptor in liver and intestine Published, JLR Papers in Press, August 24, 2007. , 2007, Journal of Lipid Research.

[85]  J. Auwerx,et al.  Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea. , 2007, Biochemical and biophysical research communications.

[86]  B. Lemon,et al.  Co-receptor Requirements for Fibroblast Growth Factor-19 Signaling* , 2007, Journal of Biological Chemistry.

[87]  T. Jiang,et al.  Farnesoid X Receptor Modulates Renal Lipid Metabolism, Fibrosis, and Diabetic Nephropathy , 2007, Diabetes.

[88]  T. Langmann,et al.  Lithocholic acid induction of the FGF19 promoter in intestinal cells is mediated by PXR. , 2007, World journal of gastroenterology.

[89]  H. Kusuhara,et al.  Glucuronidation Converting Methyl 1-(3,4-Dimethoxyphenyl)-3-(3-ethylvaleryl)-4-hydroxy-6,7,8-trimethoxy-2-naphthoate (S-8921) to a Potent Apical Sodium-Dependent Bile Acid Transporter Inhibitor, Resulting in a Hypocholesterolemic Action , 2007, Journal of Pharmacology and Experimental Therapeutics.

[90]  J. Ward,et al.  Spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice. , 2007, Carcinogenesis.

[91]  D. Häussinger,et al.  The G‐protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells , 2007, Hepatology.

[92]  T. Ogihara,et al.  Prevention and Treatment of Obesity, Insulin Resistance, and Diabetes by Bile Acid–Binding Resin , 2007, Diabetes.

[93]  A. Hofmann.  Biliary secretion and excretion in health and disease: current concepts. , 2007, Annals of hepatology.

[94]  B. Brewer,et al.  Effects of FXR in foam-cell formation and atherosclerosis development. , 2006, Biochimica et biophysica acta.

[95]  A. Norman,et al.  Minireview: vitamin D receptor: new assignments for an already busy receptor. , 2006, Endocrinology.

[96]  S. Kliewer,et al.  Identification of a hormonal basis for gallbladder filling , 2006, Nature Medicine.

[97]  P. Edwards,et al.  FXR Deficiency Causes Reduced Atherosclerosis in Ldlr−/− Mice , 2006, Arteriosclerosis, thrombosis, and vascular biology.

[98]  R. Evans,et al.  Anatomical Profiling of Nuclear Receptor Expression Reveals a Hierarchical Transcriptional Network , 2006, Cell.

[99]  D. Mangelsdorf,et al.  Pregnane X Receptor Is a Target of Farnesoid X Receptor* , 2006, Journal of Biological Chemistry.

[100]  J. Boyer,et al.  Upregulation of a basolateral FXR-dependent bile acid efflux transporter OSTα-OSTβ in cholestasis in humans and rodents , 2006 .

[101]  Ji Miao,et al.  Functional Inhibitory Cross-talk between Constitutive Androstane Receptor and Hepatic Nuclear Factor-4 in Hepatic Lipid/Glucose Metabolism Is Mediated by Competition for Binding to the DR1 Motif and to the Common Coactivators, GRIP-1 and PGC-1α* , 2006, Journal of Biological Chemistry.

[102]  Folkert Kuipers,et al.  The Farnesoid X Receptor Modulates Adiposity and Peripheral Insulin Sensitivity in Mice* , 2006, Journal of Biological Chemistry.

[103]  D. Moore,et al.  Nuclear Receptor-Dependent Bile Acid Signaling Is Required for Normal Liver Regeneration , 2006, Science.

[104]  J. Auwerx,et al.  Endocrine functions of bile acids , 2006, The EMBO journal.

[105]  S. Iturria,et al.  Identification and characterization of noncalcemic, tissue-selective, nonsecosteroidal vitamin D receptor modulators. , 2006, The Journal of clinical investigation.

[106]  S. Kliewer,et al.  Regulation of antibacterial defense in the small intestine by the nuclear bile acid receptor. , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[107]  Dae-Joong Kang,et al.  Bile salt biotransformations by human intestinal bacteria Published, JLR Papers in Press, November 18, 2005. , 2006, Journal of Lipid Research.

[108]  J. Auwerx,et al.  Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation , 2006, Nature.

[109]  S. Nelson,et al.  FXR regulates organic solute transporters α and β in the adrenal gland, kidney, and intestine Published, JLR Papers in Press, October 26, 2005. , 2006, Journal of Lipid Research.

[110]  C. Strassburg,et al.  Successful treatment of severe unconjugated hyperbilirubinemia via induction of UGT1A1 by rifampicin. , 2006, Journal of hepatology.

[111]  Roger Kurlan,et al.  Current Concepts , 2022 .

[112]  S. Kliewer,et al.  Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis. , 2005, Cell metabolism.

[113]  B. Staels,et al.  The Farnesoid X receptor: a molecular link between bile acid and lipid and glucose metabolism. , 2005, Arteriosclerosis, thrombosis, and vascular biology.

[114]  G. Tsujimoto,et al.  Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1. , 2005, Biochemical and biophysical research communications.

[115]  Thomas J. Jones,et al.  Combined loss of orphan receptors PXR and CAR heightens sensitivity to toxic bile acids in mice , 2005, Hepatology.

[116]  J. Chiang,et al.  Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7 alpha-hydroxylase gene transcription. , 2005, American journal of physiology. Gastrointestinal and liver physiology.

[117]  D. Rader,et al.  Molecular Link Between Bile Acid and Lipid and Glucose Metabolism , 2005 .

[118]  A. Norman,et al.  The Vitamin D Receptor Is Present in Caveolae-Enriched Plasma Membranes and Binds 1α,25(OH)2-Vitamin D3 in Vivo and in Vitro , 2004 .

[119]  A. Morelli,et al.  The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis. , 2004, Gastroenterology.

[120]  S. Strom,et al.  PXR (NR1I2): splice variants in human tissues, including brain, and identification of neurosteroids and nicotine as PXR activators. , 2004, Toxicology and applied pharmacology.

[121]  Guorong Xu,et al.  Inhibition of ileal bile acid transport lowers plasma cholesterol levels by inactivating hepatic farnesoid X receptor and stimulating cholesterol 7 alpha-hydroxylase. , 2004, Metabolism: clinical and experimental.

[122]  H. Tilg,et al.  Regurgitation of bile acids from leaky bile ducts causes sclerosing cholangitis in Mdr2 (Abcb4) knockout mice. , 2004, Gastroenterology.

[123]  T. Warner,et al.  Expression and activation of the farnesoid X receptor in the vasculature. , 2004, Proceedings of the National Academy of Sciences of the United States of America.

[124]  R. Evans,et al.  A novel constitutive androstane receptor-mediated and CYP3A-independent pathway of bile acid detoxification. , 2004, Molecular pharmacology.

[125]  G. Gores,et al.  Bile Acids Up-regulate Death Receptor 5/TRAIL-receptor 2 Expression via a c-Jun N-terminal Kinase-dependent Pathway Involving Sp1* , 2004, Journal of Biological Chemistry.

[126]  M. Makishima,et al.  Structural determinants for vitamin D receptor response to endocrine and xenobiotic signals. , 2004, Molecular endocrinology.

[127]  D. Russell.  The enzymes, regulation, and genetics of bile acid synthesis. , 2003, Annual review of biochemistry.

[128]  S. Rapp,et al.  Inhibition of ileal bile acid transport and reduced atherosclerosis in apoE−/− mice by SC-435 Published, JLR Papers in Press, June 16, 2003. DOI 10.1194/jlr.M200469-JLR200 , 2003, Journal of Lipid Research.

[129]  R. Tangirala,et al.  Farnesoid X Receptor Regulates Bile Acid-Amino Acid Conjugation* , 2003, Journal of Biological Chemistry.

[130]  M. Bowman,et al.  A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. , 2003, Molecular cell.

[131]  Masataka Harada,et al.  A G Protein-coupled Receptor Responsive to Bile Acids* , 2003, The Journal of Biological Chemistry.

[132]  G. Kullak-Ublick,et al.  Hepatocyte nuclear factor 1α: A key mediator of the effect of bile acids on gene expression , 2003 .

[133]  G. Casari,et al.  Identification of Farnesoid X Receptor β as a Novel Mammalian Nuclear Receptor Sensing Lanosterol , 2003, Molecular and Cellular Biology.

[134]  Heidi R. Kast-Woelbern,et al.  Natural Structural Variants of the Nuclear Receptor Farnesoid X Receptor Affect Transcriptional Activation* , 2003, The Journal of Biological Chemistry.

[135]  G. Kullak-Ublick,et al.  Hepatocyte nuclear factor 1 alpha: a key mediator of the effect of bile acids on gene expression. , 2003, Hepatology.

[136]  Takao Nakamura,et al.  Identification of membrane-type receptor for bile acids (M-BAR). , 2002, Biochemical and biophysical research communications.

[137]  S. Kliewer,et al.  Nuclear pregnane x receptor and constitutive androstane receptor regulate overlapping but distinct sets of genes involved in xenobiotic detoxification. , 2002, Molecular pharmacology.

[138]  T. Willson,et al.  6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. , 2002, Journal of medicinal chemistry.

[139]  G. Frantz,et al.  A mouse model of hepatocellular carcinoma: ectopic expression of fibroblast growth factor 19 in skeletal muscle of transgenic mice. , 2002, The American journal of pathology.

[140]  M. Haussler,et al.  Vitamin D Receptor As an Intestinal Bile Acid Sensor , 2002, Science.

[141]  Timothy M Willson,et al.  Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors. , 2002, Molecular endocrinology.

[142]  D. Mangelsdorf,et al.  A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR , 2002, Science.

[143]  Paul T Tarr,et al.  Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor* , 2002, The Journal of Biological Chemistry.

[144]  D. Hunninghake,et al.  Effectiveness of colesevelam hydrochloride in decreasing LDL cholesterol in patients with primary hypercholesterolemia: a 24-week randomized controlled trial. , 2001, Mayo Clinic proceedings.

[145]  M. Makishima,et al.  Human Bile Salt Export Pump Promoter Is Transactivated by the Farnesoid X Receptor/Bile Acid Receptor* , 2001, The Journal of Biological Chemistry.

[146]  D. Häussinger,et al.  Tauroursodesoxycholate-induced choleresis involves p38(MAPK) activation and translocation of the bile salt export pump in rats. , 2001, Gastroenterology.

[147]  D. Keppler,et al.  Tauroursodeoxycholic acid inserts the apical conjugate export pump, Mrp2, into canalicular membranes and stimulates organic anion secretion by protein kinase C–dependent mechanisms in cholestatic rat liver , 2001, Hepatology.

[148]  T. Willson,et al.  The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[149]  L. Moore,et al.  A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. , 2000, Molecular cell.

[150]  L. Moore,et al.  St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[151]  L. Moore,et al.  The Pregnane X Receptor: A Promiscuous Xenobiotic Receptor That Has Diverged during Evolution , 2000 .

[152]  L. Moore,et al.  The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. , 2000, Molecular endocrinology.

[153]  H. Zhang,et al.  Rat pregnane X receptor: molecular cloning, tissue distribution, and xenobiotic regulation. , 1999, Archives of biochemistry and biophysics.

[154]  M. Makishima,et al.  Identification of a nuclear receptor for bile acids. , 1999, Science.

[155]  R Ohlsson,et al.  Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[156]  J. Lehmann,et al.  The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. , 1998, The Journal of clinical investigation.

[157]  J. Lehmann,et al.  An Orphan Nuclear Receptor Activated by Pregnanes Defines a Novel Steroid Signaling Pathway , 1998, Cell.

[158]  D. Moore,et al.  Differential Transactivation by Two Isoforms of the Orphan Nuclear Hormone Receptor CAR* , 1997, The Journal of Biological Chemistry.

[159]  D. Moore,et al.  An Orphan Nuclear Hormone Receptor That Lacks a DNA Binding Domain and Heterodimerizes with Other Receptors , 1996, Science.

[160]  Jasmine Chen,et al.  Identification of a nuclear receptor that is activated by farnesol metabolites , 1995, Cell.

[161]  Peter Oelkers,et al.  Bile acid transporters , 1995, Current opinion in lipidology.

[162]  D. Moore,et al.  Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors. , 1995, Molecular endocrinology.

[163]  D. Moore,et al.  A new orphan member of the nuclear hormone receptor superfamily that interacts with a subset of retinoic acid response elements , 1994, Molecular and cellular biology.

[164]  P. Dawson,et al.  Expression cloning and characterization of the hamster ileal sodium-dependent bile acid transporter. , 1994, The Journal of biological chemistry.

[165]  A. Hofmann,et al.  Ursodeoxycholic acid in the Ursidae: biliary bile acids of bears, pandas, and related carnivores. , 1993, Journal of lipid research.

[166]  B. Bouscarel,et al.  Ursodeoxycholate mobilizes intracellular Ca2+ and activates phosphorylase a in isolated hepatocytes. , 1993, The American journal of physiology.

[167]  Y. Chrétien,et al.  IS URSODEOXYCHOLIC ACID AN EFFECTIVE TREATMENT FOR PRIMARY BILIARY CIRRHOSIS? , 1987, The Lancet.

[168]  S. Erlinger,et al.  Effect of acid-base balance and acetazolamide on ursodeoxycholate-induced biliary bicarbonate secretion. , 1985, The American journal of physiology.

[169]  K. Okuda,et al.  Effects of corticosteroids on bilirubin metabolism in patients with Gilbert's syndrome , 1981, Hepatology.

[170]  R. Dowling,et al.  URSODEOXYCHOLIC ACID TREATMENT OF GALLSTONES Dose-response Study and Possible Mechanism of Action , 1977, The Lancet.

[171]  G. Edwards.  THE ALCOHOLIC DOCTOR A Case of Neglect , 1975, The Lancet.

[172]  G. Salen,et al.  Chenodeoxycholic acid inhibits increased cholesterol and cholestanol synthesis in patients with cerebrotendinous xanthomatosis. , 1975, Biochemical medicine.

[173]  M. Dumont,et al.  European Association for the Study of the Liver , 1971 .

[174]  H. Mekhjian,et al.  Colonic secretion of water and electrolytes induced by bile acids: perfusion studies in man. , 1971, The Journal of clinical investigation.

[175]  I. Bekersky,et al.  Feedback regulation of bile acid biosynthesis in the rat. , 1969, Journal of lipid research.

[176]  A. Levi,et al.  Chronic nonhemolytic unconjugated hyperbilirubinemia with glucuronyl transferase deficiency. Clinical, biochemical, pharmacologic and genetic evidence for heterogeneity. , 1969, The American journal of medicine.

[177]  B. Borgström,et al.  Studies of intestinal digestion and absorption in the human. , 1957, The Journal of clinical investigation.

[178]  P. Hench.  Effect of Jaundice on Rheumatoid Arthritis* , 1938, British medical journal.