Bile acid receptors as targets for drug development

Bile salt biotransformations by human intestinal bacteria

Ridlon, J. M., Kang, D.-J., & Hylemon, P. B. (2006) · Journal of Lipid Research · doi:10.1194/jlr.r500013-jlr200 · Cited by 2,829

Identification of a nuclear receptor for bile acids

Makishima, M., Okamoto, A. Y., Repa, J. J., Tu, H., Learned, R. M., Luk, A., Hull, M. V., Lustig, K. D., Mangelsdorf, D. J., & Shan, B. (1999) · Science · doi:10.1126/science.284.5418.1362 · Cited by 2,714

Gut microbiota regulates bile acid metabolism by reducing the levels of tauro-beta-muricholic acid, a naturally occurring FXR antagonist

Sayin, S. I., Wahlström, A., Felin, J., Jäntti, S., Marschall, H.-U., Bamberg, K., Angelin, B., Hyötyläinen, T., Orešič, M., & Bäckhed, F. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.01.003 · Cited by 2,331

Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation

Watanabe, M., Houten, S. M., Mataki, C., Christoffolete, M. A., Kim, B. W., Sato, H., Messaddeq, N., Harney, J. W., Ezaki, O., Kodama, T., et al. (2006) · Nature · doi:10.1038/nature04330 · Cited by 2,220

The Enzymes, Regulation, and Genetics of Bile Acid Synthesis

Russell, D. W. (2003) · Annual Review of Biochemistry · doi:10.1146/annurev.biochem.72.121801.161712 · Cited by 2,069

A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis

Goodwin, B., Jones, S. A., Price, R. R., Watson, M. A., McKee, D. D., Moore, L. B., Galardi, C., Wilson, J. G., Lewis, M. C., Roth, M. E., et al. (2000) · Molecular Cell · doi:10.1016/s1097-2765(00)00051-4 · Cited by 1,940

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

Thomas, C., Gioiello, A., Noriega, L., Strehle, A., Oury, J., Rizzo, G., Macchiarulo, A., Yamamoto, H., Mataki, C., Pruzanski, M., et al. (2009) · Cell Metabolism · doi:10.1016/j.cmet.2009.08.001 · Cited by 1,885

Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis

Inagaki, T., Choi, M., Moschetta, A., Peng, L., Cummins, C. L., McDonald, J. G., Luo, G., Jones, S. A., Goodwin, B., Richardson, J. A., et al. (2005) · Cell Metabolism · doi:10.1016/j.cmet.2005.09.001 · Cited by 1,865

EASL Clinical Practice Guidelines: management of cholestatic liver diseases

European Association for the Study of the Liver (2009) · Journal of Hepatology · doi:10.1016/j.jhep.2009.04.009 · Cited by 1,729

A G Protein-coupled Receptor Responsive to Bile Acids

Kawamata, Y., Fujii, R., Hosoya, M., Harada, M., Yoshida, H., Miwa, M., Fukusumi, S., Habata, Y., Itoh, T., Shintani, Y., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m209706200 · Cited by 1,628

The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

Lehmann, J., McKee, D. D., Watson, M. A., Willson, T. M., Moore, J. T., & Kliewer, S. A. (1998) · Journal of Clinical Investigation · doi:10.1172/jci3703 · Cited by 1,577

An Orphan Nuclear Receptor Activated by Pregnanes Defines a Novel Steroid Signaling Pathway

Kliewer, S. A., Moore, J. T., Wade, L., Staudinger, J. L., Watson, M. A., Jones, S. A., McKee, D. D., Oliver, B. B., Willson, T. M., Zetterström, R. H., et al. (1998) · Cell · doi:10.1016/s0092-8674(00)80900-9 · Cited by 1,534

The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity

Staudinger, J. L., Goodwin, B. J., Jones, S. A., Hawkins‐Brown, D., MacKenzie, K. I., Latour, A. M., Liu, Y., Klaassen, C. D., Brown, K. K., Reinhard, J. F., et al. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.051551698 · Cited by 1,378

Identification of a nuclear receptor that is activated by farnesol metabolites

Forman, B. M., Goode, E., Chen, J., Oro, A. E., Bradley, D. J., Perlmann, T., Noonan, D. J., Burka, L. T., McMorris, T., Lamph, W. W., et al. (1995) · Cell · doi:10.1016/0092-8674(95)90530-8 · Cited by 1,210

Vitamin D Receptor As an Intestinal Bile Acid Sensor

Makishima, M., Lu, T. T., Xie, W., Whitfield, G. K., Domoto, H., Evans, R. M., Haussler, M. R., & Mangelsdorf, D. J. (2002) · Science · doi:10.1126/science.1070477 · Cited by 1,176

Regulation of antibacterial defense in the small intestine by the nuclear bile acid receptor

Inagaki, T., Moschetta, A., Lee, Y.-K., Peng, L., Zhao, G., Downes, M., Yu, R. T., Shelton, J. M., Richardson, J. A., Repa, J. J., et al. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0509592103 · Cited by 1,164

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

Bennett, B. J., Vallim, T. Q. D. A., Wang, Z., Shih, D. M., Meng, Y., Gregory, J., Allayee, H., Lee, R., Graham, M., Crooke, R., et al. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2012.12.011 · Cited by 1,070

Studies of Intestinal Digestion and Absorption in the Human1

Borgström, B., Dahlqvist, A., Lundh, G., & Sjövall, J. (1957) · Journal of Clinical Investigation · doi:10.1172/jci103549 · Cited by 1,048

Anatomical profiling of nuclear receptor expression reveals a hierarchical transcriptional network

Bookout, A. L., Jeong, Y., Downes, M., Yu, R. T., Evans, R. M., & Mangelsdorf, D. J. (2006) · Cell · doi:10.1016/j.cell.2006.06.049 · Cited by 1,015

Identification of membrane-type receptor for bile acids (M-BAR)

Maruyama, T., Miyamoto, Y., Nakamura, T., Tamai, Y., Okada, H., Sugiyama, E., Nakamura, T., Itadani, H., & Tanaka, K. (2002) · Biochemical and Biophysical Research Communications · doi:10.1016/s0006-291x(02)02550-0 · Cited by 993

St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor

Moore, L. B., Goodwin, B. J., Jones, S. A., Wisely, G. B., Serabjit‐Singh, C. J., Willson, T. M., Collins, J. L., & Kliewer, S. A. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.130155097 · Cited by 946

Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease

Mudaliar, S., Henry, R. R., Sanyal, A. J., Morrow, L., Marschall, H., Kipnes, M., Adorini, L., Sciacca, C. I., Clopton, P., Castelloe, E., et al. (2013) · Gastroenterology · doi:10.1053/j.gastro.2013.05.042 · Cited by 931

Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor

Kast, H. R., Goodwin, B., Tarr, P. T., Jones, S. A., Anisfeld, A. M., Stoltz, C. M., Tontonoz, P., Kliewer, S., Willson, T. M., & Edwards, P. A. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m109326200 · Cited by 916

Identification of a human nuclear receptor defines a new signaling pathway for CYP 3 A induction

Bertilsson, G., Heidrich, J., Svensson, K., Åsman, M., Jendeberg, L., Sydow‐Báckman, M., OHLSSON, R. I., Postlind, H., Blomquist, P., & Berkenstam, A. L. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.21.12208 · Cited by 876

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

Gadaleta, R. M., van Erpecum, K. J., Oldenburg, B., Willemsen, E. C. L., Renooij, W., Murzilli, S., Klomp, L. W. J., Siersema, P. D., Schipper, M. E. I., Danese, S., et al. (2011) · Gut · doi:10.1136/gut.2010.212159 · Cited by 870

Human Bile Salt Export Pump Promoter Is Transactivated by the Farnesoid X Receptor/Bile Acid Receptor

Ananthanarayanan, M., Balasubramanian, N., Makishima, M., Mangelsdorf, D. J., & Suchy, F. J. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m011610200 · Cited by 804

Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1

Katsuma, S., Hirasawa, A., & Tsujimoto, G. (2005) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2005.01.139 · Cited by 789

6α-Ethyl-Chenodeoxycholic Acid (6-ECDCA), a Potent and Selective FXR Agonist Endowed with Anticholestatic Activity

Pellicciari, R., Fiorucci, S., Camaioni, E., Clerici, C., Costantino, G., Maloney, P. R., Morelli, A., Parks, D. J., & Willson, T. M. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm025529g · Cited by 743

Bile acid transporters

Dawson, P. A., Lan, T., & Rao, A. (2009) · Journal of Lipid Research · doi:10.1194/jlr.r900012-jlr200 · Cited by 683

The Pregnane X Receptor: A Promiscuous Xenobiotic Receptor That Has Diverged during Evolution

Jones, S. A., Moore, L. B., Shenk, J. L., Wisely, G. B., Hamilton, G. A., McKee, D. D., Tomkinson, N. C. O., LeCluyse, E. L., Lambert, M. H., Willson, T. M., et al. (2000) · Molecular Endocrinology · doi:10.1210/mend.14.1.0409 · Cited by 672

Nuclear Pregnane X Receptor and Constitutive Androstane Receptor Regulate Overlapping but Distinct Sets of Genes Involved in Xenobiotic Detoxification

Maglich, J. M., Stoltz, C. M., Goodwin, B. J., Hawkins‐Brown, D., Moore, J. T., & Kliewer, S. A. (2002) · Molecular Pharmacology · doi:10.1124/mol.62.3.638 · Cited by 662

Nuclear Receptor-Dependent Bile Acid Signaling Is Required for Normal Liver Regeneration

Huang, W., Ma, K., Zhang, J., Qatanani, M., Cuvillier, J., Liu, J., Dong, B., Huang, X., & Moore, D. D. (2006) · Science · doi:10.1126/science.1121435 · Cited by 645

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

Pols, T. W. H., Nomura, M., Harach, T., Sasso, G. L., Oosterveer, M. H., Thomas, C., Rizzo, G., Gioiello, A., Adorini, L., Pellicciari, R., et al. (2011) · Cell Metabolism · doi:10.1016/j.cmet.2011.11.006 · Cited by 643

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

Kir, S., Beddow, S. A., Samuel, V. T., Miller, P., Previs, S. F., Suino-Powell, K., Xu, H. E., Shulman, G. I., Kliewer, S. A., & Mangelsdorf, D. J. (2011) · Science · doi:10.1126/science.1198363 · Cited by 637

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

Zhou, J., Febbraio, M., Wada, T., Zhai, Y., Kuruba, R., He, J., Lee, J. H., Khadem, S., Ren, S., Li, S., et al. (2007) · Gastroenterology · doi:10.1053/j.gastro.2007.11.037 · Cited by 620

Endocrine functions of bile acids

Houten, S. M., 渡辺, 光., & Auwerx, J. H. (2006) · The EMBO Journal · doi:10.1038/sj.emboj.7601049 · Cited by 595

Differential regulation of bile acid homeostasis by the farnesoid X receptor in liver and intestine

Kim, I., Ahn, S.-H., Inagaki, T., Choi, M., Ito, S., Guo, G. L., Kliewer, S. A., & Gonzalez, F. J. (2007) · Journal of Lipid Research · doi:10.1194/jlr.m700330-jlr200 · Cited by 589

Colonic Secretion of Water and Electrolytes Induced by Bile Acids: Perfusion Studies in Man

Mekhjian, H. S., Phillips, S. F., & Hofmann, A. F. (1971) · Journal of Clinical Investigation · doi:10.1172/jci106644 · Cited by 584

Vitamin D Receptor: New Assignments for an Already Busy Receptor

Norman, A. W. (2006) · Endocrinology · doi:10.1210/en.2006-0946 · Cited by 583

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

Peterli, R., Wölnerhanssen, B. K., Peters, T. T. A., Devaux, N., Kern, B. E., Christoffel-Courtin, C., Drewe, J., von Flüe, M., & Beglinger, C. (2009) · Annals of Surgery · doi:10.1097/sla.0b013e3181ae32e3 · Cited by 567

A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR

Urizar, N. L., Liverman, A. D. B., Dodds, D. T., Silva, F. V., Ordentlich, P., Yan, Y. G., Gonzalez, F. J., Heyman, R. A., Mangelsdorf, D. J., & Moore, D. D. (2002) · Science · doi:10.1126/science.1072891 · Cited by 553

The Farnesoid X Receptor Modulates Adiposity and Peripheral Insulin Sensitivity in Mice

Cariou, B., van Harmelen, K., Durán-Sandoval, D., van Dijk, T. H., Grefhorst, A., Abdelkarim, M., Caron, S., Torpier, G., Fruchart, J., Gonzalez, F. J., et al. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m510258200 · Cited by 546

IS URSODEOXYCHOLIC ACID AN EFFECTIVE TREATMENT FOR PRIMARY BILIARY CIRRHOSIS?

Poupon, R. Y., Poupon, R., Calmus, Y., Chrétien, Y., Ballet, F., & Darnis, F. (1987) · The Lancet · doi:10.1016/s0140-6736(87)91610-2 · Cited by 534

An Orphan Nuclear Hormone Receptor That Lacks a DNA Binding Domain and Heterodimerizes with Other Receptors

Seol, W., Choi, H.-S., & Moore, D. D. (1996) · Science · doi:10.1126/science.272.5266.1336 · Cited by 528

The Farnesoid X Receptor

Claudel, T., Staels, B., & Kuipers, F. (2005) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/01.atv.0000178994.21828.a7 · Cited by 506

Bile Acids Induce Inflammatory Genes in Hepatocytes

Allen, K., Jaeschke, H., & Copple, B. L. (2011) · The American Journal of Pathology · doi:10.1016/j.ajpath.2010.11.026 · Cited by 501

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

Wang, Y., Chen, W., Yu, D. D., FORMAN, B. M., & Huang, W. (2011) · Hepatology · doi:10.1002/hep.24525 · Cited by 496

A New Orphan Member of the Nuclear Hormone Receptor Superfamily That Interacts with a Subset of Retinoic Acid Response Elements

Baes, M. I., Gulick, T., Choi, H.-S., Martinoli, M., Simha, D., & Moore, D. D. (1994) · Molecular and Cellular Biology · doi:10.1128/mcb.14.3.1544 · Cited by 496

The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis

Fiorucci, S., Antonelli, E., Rizzo, G., Renga, B., Mencarelli, A., Riccardi, L., Orlandi, S., Pellicciari, R., & Morelli, A. (2004) · Gastroenterology · doi:10.1053/j.gastro.2004.08.001 · Cited by 472

Regurgitation of bile acids from leaky bile ducts causes sclerosing cholangitis in Mdr2 (Abcb4) knockout mice

Fickert, P., Fuchsbichler, A., Wagner, M., Zollner, G., Kaser, A., Tilg, H., Krause, R. G. E., Lammert, F., Langner, C., Zatloukal, K., et al. (2004) · Gastroenterology · doi:10.1053/j.gastro.2004.04.009 · Cited by 468

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

Pols, T. W. H., Noriega, L. G., Nomura, M., Auwerx, J., & Schoonjans, K. (2011) · Journal of Hepatology · doi:10.1016/j.jhep.2010.12.004 · Cited by 454

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

Potthoff, M. J., Boney-Montoya, J., Choi, M., He, T., Sunny, N. E., Satapati, S., Suino-Powell, K., Xu, H. E., Gerard, R. D., Finck, B. N., et al. (2011) · Cell Metabolism · doi:10.1016/j.cmet.2011.03.019 · Cited by 431

Lysophosphatidic Acid Is a Potential Mediator of Cholestatic Pruritus

Kremer, A. E., Martens, J. J. W. W., Kulik, W., Ruëff, F., Kuiper, E. M. M., van Buuren, H. R., van Erpecum, K. J., Kondrackiene, J., Prieto, J., Rust, C., et al. (2010) · Gastroenterology · doi:10.1053/j.gastro.2010.05.009 · Cited by 410

A Chemical, Genetic, and Structural Analysis of the Nuclear Bile Acid Receptor FXR

Downes, M., Verdecia, M. A., Roecker, A. J., Hughes, R. O., Hogenesch, J. B., Kast-Woelbern, H. R., Bowman, M. E., Ferrer, J.-L., Anisfeld, A. M., Edwards, P. A., et al. (2003) · Molecular Cell · doi:10.1016/s1097-2765(03)00104-7 · Cited by 396

Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors

Seol, W., Choi, H.-S., & Moore, D. D. (1995) · Molecular Endocrinology · doi:10.1210/mend.9.1.7760852 · Cited by 389

FXR: a metabolic regulator and cell protector

Wang, Y.-D., Chen, W.-D., Moore, D. D., & Huang, W. (2008) · Cell Research · doi:10.1038/cr.2008.289 · Cited by 389

The TGR5 receptor mediates bile acid–induced itch and analgesia

Alemi, F., Kwon, E., Poole, D. P., Lieu, T., Lyo, V., Cattaruzza, F., Cevikbas, F., Steinhoff, M. S., Nassini, R., Materazzi, S., et al. (2013) · Journal of Clinical Investigation · doi:10.1172/jci64551 · Cited by 387

The receptor TGR5 mediates the prokinetic actions of intestinal bile acids and is required for normal defecation in mice

Alemi, F., Poole, D. P., Chiu, J., Schoonjans, K., Cattaruzza, F., Grider, J. R., Bunnett, N. W., & Corvera, C. U. (2013) · Gastroenterology · doi:10.1053/j.gastro.2012.09.055 · Cited by 362

A Mouse Model of Hepatocellular Carcinoma

Nicholes, K., Guillet, S., Tomlinson, E., Hillan, K., Wright, B., Frantz, G. D., Pham, T. A., Dillard-Telm, L., Tsai, S. P., Stephan, J.-P., et al. (2002) · The American Journal of Pathology · doi:10.1016/s0002-9440(10)61177-7 · Cited by 359

Spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice

Kim, I., Morimura, K., Shah, Y., Yang, Q., Ward, J. M., & Gonzalez, F. J. (2007) · Carcinogenesis · doi:10.1093/carcin/bgl249 · Cited by 357

Pregnane X Receptor (PXR), Constitutive Androstane Receptor (CAR), and Benzoate X Receptor (BXR) Define Three Pharmacologically Distinct Classes of Nuclear Receptors

Moore, L. B., Maglich, J. M., McKee, D. D., Wisely, B., Willson, T. M., Kliewer, S. A., Lambert, M. H., & Moore, J. T. (2002) · Molecular Endocrinology · doi:10.1210/mend.16.5.0828 · Cited by 356

Expression cloning and characterization of the hamster ileal sodium-dependent bile acid transporter.

Wong, M. H., Oelkers, P. M., Craddock, A. L., & Dawson, P. A. (1994) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)42263-0 · Cited by 353

The Biliary HCO3 − Umbrella: A Unifying Hypothesis on Pathogenetic and Therapeutic Aspects of Fibrosing Cholangiopathies

Beuers, U., Hohenester, S., de Buy Wenniger, L. J. M., Kremer, A. E., Jansen, P. L. M., & Elferink, R. P. J. O. (2010) · Hepatology · doi:10.1002/hep.23810 · Cited by 351

Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea

Sato, H., Genet, C., Strehle, A., Thomas, C., Lobstein, A., Wagner, A., Mioskowski, C., Auwerx, J. H., & Saladin, R. (2007) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2007.06.130 · Cited by 349

Chronic nonhemolytic unconjugated hyperbilirubinemia with glucuronyl transferase deficiency

Arias, I. M., Gartner, L. M., Cohen, M., Ben-Ezzer, J., & Levi, A. J. (1969) · The American Journal of Medicine · doi:10.1016/0002-9343(69)90224-1 · Cited by 338

The Vitamin D Receptor Is Present in Caveolae-Enriched Plasma Membranes and Binds 1α,25(OH)2-Vitamin D3in Vivo and in Vitro

Huhtakangas, J. A., Olivera, C. J., Bishop, J. E., Zanello, L. P., & Norman, A. W. (2004) · Molecular Endocrinology · doi:10.1210/me.2004-0116 · Cited by 337

The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells

Keitel, V., Reinehr, R., Gatsios, P., Rupprecht, C., Görg, B., Selbach, O., Häussinger, D., & Kubitz, R. (2007) · Hepatology · doi:10.1002/hep.21458 · Cited by 316

Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure−Activity Relationships, and Molecular Modeling Studies

Sato, H., Macchiarulo, A., Thomas, C., Gioiello, A., Une, M., Hofmann, A. F., Saladin, R., Schoonjans, K., Pellicciari, R., & Auwerx, J. H. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm7015864 · Cited by 311

Upregulation of a basolateral FXR-dependent bile acid efflux transporter OSTα-OSTβ in cholestasis in humans and rodents

Boyer, J. L., Trauner, M. A., Mennone, A., Soroka, C. J., Cai, S., Moustafa, T., Zollner, G., Lee, J., & Ballatori, N. (2006) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.00539.2005 · Cited by 305

Natural Structural Variants of the Nuclear Receptor Farnesoid X Receptor Affect Transcriptional Activation

Zhang, Y., Kast-Woelbern, H. R., & Edwards, P. A. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m209505200 · Cited by 295

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

Kremer, A. E., van Dijk, R., Leckie, P., Schaap, F. G., Kuiper, E. M. M., Mettang, T., Reiners, K. S., Raap, U., van Buuren, H. R., van Erpecum, K. J., et al. (2012) · Hepatology · doi:10.1002/hep.25748 · Cited by 291

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

Keitel, V., Cupisti, K., Ullmer, C., Knoefel, W. T., Kubitz, R., & Häussinger, D. (2009) · Hepatology · doi:10.1002/hep.23032 · Cited by 290

Identification of a hormonal basis for gallbladder filling

Choi, M., Moschetta, A., Bookout, A. L., Peng, L., Umetani, M., Holmstrom, S. R., Suino-Powell, K. M., Xu, H. E., Richardson, J. A., Gerard, R. D., et al. (2006) · Nature Medicine · doi:10.1038/nm1501 · Cited by 290

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

Schaap, F. G., Gaag, N. A. V. D., Gouma, D. J., & Jansen, P. L. M. (2008) · Hepatology · doi:10.1002/hep.22771 · Cited by 281

Differential Transactivation by Two Isoforms of the Orphan Nuclear Hormone Receptor CAR

Choi, H., Chung, M., Tzameli, I., Simha, D., Lee, Y., Seol, W., & Moore, D. D. (1997) · Journal of Biological Chemistry · doi:10.1074/jbc.272.38.23565 · Cited by 279

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

Keitel, V., Görg, B., Bidmon, H. J., Zemtsova, I., Spomer, L., Zilles, K., & Häussinger, D. (2010) · Glia · doi:10.1002/glia.21049 · Cited by 274

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

Li, T., Holmstrom, S. R., Kır, S., Umetani, M., Schmidt, D. R., Kliewer, S. A., & Mangelsdorf, D. J. (2011) · Molecular Endocrinology · doi:10.1210/me.2010-0460 · Cited by 271

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

Pellicciari, R., Gioiello, A., Macchiarulo, A., Thomas, C., Rosatelli, E., Natalini, B., Sardella, R., Pruzanski, M., Roda, A., Pastorini, E., et al. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm901390p · Cited by 269

Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis

Adorini, L., Pruzanski, M., & Shapiro, D. (2012) · Drug Discovery Today · doi:10.1016/j.drudis.2012.05.012 · Cited by 259

Role of CAR and PXR in xenobiotic sensing and metabolism

Wang, Y., Ong, S. S., Chai, S. C., & Chen, T. (2012) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1517/17425255.2012.685237 · Cited by 258

A Novel Constitutive Androstane Receptor-Mediated and CYP3A-Independent Pathway of Bile Acid Detoxification

Saini, S. P. S., Sonoda, J., Xu, L., Toma, D., Uppal, H., Mu, Y., Ren, S., Moore, D. D., Evans, R. M., & Xie, W. (2004) · Molecular Pharmacology · doi:10.1124/mol.65.2.292 · Cited by 256

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

Beuers, U. H., Bilzer, M., CHITTATTU, A., Kullak-Ublick, G. A., KEPPLER, D. O. R., Paumgartner, G., & Dombrowski, F. (2001) · Hepatology · doi:10.1053/jhep.2001.24034 · Cited by 251

Expression and activation of the farnesoid X receptor in the vasculature

Bishop‐Bailey, D., Walsh, D. T., & Warner, T. D. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0400046101 · Cited by 242

Farnesoid X Receptor Modulates Renal Lipid Metabolism, Fibrosis, and Diabetic Nephropathy

Jiang, T., Wang, X. X., Scherzer, P., Wilson, P. V., Tallman, J., Takahashi, H., Li, J., Iwahashi, M., Sutherland, E. M., Arend, L. J., et al. (2007) · Diabetes · doi:10.2337/db06-1642 · Cited by 232

Nuclear receptor PXR, transcriptional circuits and metabolic relevance

Ihunnah, C. A., Jiang, M., & Xie, W. (2011) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2011.01.014 · Cited by 230

Feedback regulation of bile acid biosynthesis in the rat

Shefer, S., Hauser, S., Bekersky, I., & Mosbach, E. H. (1969) · Journal of Lipid Research · doi:10.1016/s0022-2275(20)43025-1 · Cited by 228

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

d'Aldebert, E., Mve, M.-J. B. B., Mergey, M., Wendum, D., Firrincieli, D., Coilly, A., Fouassier, L., Corpechot, C., Poupon, R. Y., Housset, C., et al. (2008) · Gastroenterology · doi:10.1053/j.gastro.2008.12.040 · Cited by 225

SERUM-SICKNESS-LIKE SYNDROME WITH MEMBRANOUS GLOMERULOPATHY IN PATIENT ON CAPTOPRIL

Hoorntje, S., Weening, J. J., Kallenberg, C. M., Prins, E. L., & Donker, A. M. (1979) · The Lancet · doi:10.1016/s0140-6736(79)92303-1 · Cited by 225

PXR (NR1I2): splice variants in human tissues, including brain, and identification of neurosteroids and nicotine as PXR activators

Lamba, V. (2004) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2003.12.027 · Cited by 221

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

Baghdasaryan, A., Claudel, T., Gumhold, J., Silbert, D., Adorini, L., Roda, A., Vecchiotti, S., Gonzalez, F. J., Schoonjans, K., Strazzabosco, M., et al. (2011) · Hepatology · doi:10.1002/hep.24537 · Cited by 220

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

Wong, B. S., Camilleri, M., Carlson, P., McKinzie, S., Busciglio, I. A., Bondar, O. P., Dyer, R. B., Lamsam, J. L., & Zinsmeister, A. R. (2012) · Clinical Gastroenterology and Hepatology · doi:10.1016/j.cgh.2012.05.006 · Cited by 217

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

Schmidt, D. R., Holmstrom, S. R., Tacer, K. F., Bookout, A. L., Kliewer, S. A., & Mangelsdorf, D. J. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.116004 · Cited by 215

Mechanism of rifampicin and pregnane X receptor inhibition of human cholesterol 7α-hydroxylase gene transcription

Li, T., & Chiang, J. Y. L. (2004) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.00258.2004 · Cited by 212

URSODEOXYCHOLIC ACID TREATMENT OF GALLSTONES

Maton, P. N., Murphy, G. M., & Dowling, R. H. (1977) · The Lancet · doi:10.1016/s0140-6736(77)90358-0 · Cited by 210

Rat Pregnane X Receptor: Molecular Cloning, Tissue Distribution, and Xenobiotic Regulation

Zhang, H., LeCulyse, E., Liu, L., Hu, M., Matoney, L., Zhu, W., & Yan, B. (1999) · Archives of Biochemistry and Biophysics · doi:10.1006/abbi.1999.1307 · Cited by 205

Functional Characterization of the Semisynthetic Bile Acid Derivative INT-767, a Dual Farnesoid X Receptor and TGR5 Agonist

Rizzo, G., Passeri, D., Franco, F., Ciaccioli, G., Donadio, L., Rizzo, G., Orlandi, S., Sadeghpour, B. M., Wang, X. X., Jiang, T., et al. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.064501 · Cited by 203

Antiatherosclerotic effect of farnesoid X receptor

Mencarelli, A., Renga, B., Distrutti, E., & Fiorucci, S. (2008) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.01075.2008 · Cited by 199

Farnesoid X Receptor Regulates Bile Acid-Amino Acid Conjugation

Pircher, P. C., Kitto, J. L., Petrowski, M. L., Tangirala, R. K., Bischoff, E. D., Schulman, I. G., & Westin, S. K. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m302128200 · Cited by 197

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

Miao, J., Fang, S., Bae, Y., & Kemper, J. K. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m510713200 · Cited by 197

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

Uriarte, I., Fernandez-Barrena, M. G., Monte, M., Latasa, M., Chang, H. C. Y., Carotti, S., Vespasiani-Gentilucci, U., Morini, S., Vicente, E., Concepcion, A., et al. (2013) · Gut · doi:10.1136/gutjnl-2012-302945 · Cited by 196

Hepatocyte Nuclear Factor 1α: A Key Mediator of the Effect of Bile Acids on Gene Expression

Jung, D., & Kullak-Ublick, G. A. (2003) · Hepatology · doi:10.1053/jhep.2003.50100 · Cited by 192

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

Wang, X. X., Jiang, T., Shen, Y., Caldas, Y. A., Miyazaki‐Anzai, S., Santamaria, H., Urbanek, C., Solis, N., Scherzer, P., Lewis, L., et al. (2010) · Diabetes · doi:10.2337/db10-0019 · Cited by 191

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

Harach, T., Pols, T. W. H., Nomura, M., Maida, A., 渡辺, 光., Auwerx, J. H., & Schoonjans, K. (2012) · Scientific Reports · doi:10.1038/srep00430 · Cited by 183

FXR regulates organic solute transporters α and β in the adrenal gland, kidney, and intestine

Lee, H. C., Zhang, Y., Lee, F. Y., Nelson, S. F., Gonzalez, F. J., & Edwards, P. A. (2005) · Journal of Lipid Research · doi:10.1194/jlr.m500417-jlr200 · Cited by 180

Identification of Farnesoid X Receptor β as a Novel Mammalian Nuclear Receptor Sensing Lanosterol

Otte, K., Kranz, H., Kober, I., Thompson, P., Hoefer, M., Haubold, B., Remmel, B., Voss, H., Kaiser, C., Albers, M., et al. (2003) · Molecular and Cellular Biology · doi:10.1128/mcb.23.3.864-872.2003 · Cited by 176

Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR)

Flatt, B., Martin, R., Wang, T., Mahaney, P. E., Murphy, B., Gu, X., Foster, P., Li, J., Pircher, P. C., Petrowski, M. L., et al. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm8014124 · Cited by 171

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

Fickert, P., Fuchsbichler, A., Moustafa, T., Wagner, M., Zollner, G., Halilbasic, E., Stöger, U., Arrese, M., Pizarro, M., Solís, N., et al. (2009) · The American Journal of Pathology · doi:10.2353/ajpath.2009.090114 · Cited by 169

FXR Deficiency Causes Reduced Atherosclerosis inLdlr−/−Mice

Zhang, Y., Wang, X., Vales, C., Lee, F. Y., Lee, H. C., Lusis, A. J., & Edwards, P. A. (2006) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/01.atv.0000235697.35431.05 · Cited by 168

Tauroursodesoxycholate-induced choleresis involves p38MAPK activation and translocation of the bile salt export pump in rats

Kurz, A. K., Graf, D., Schmitt, M., Dahl, S. V., & Häussinger, D. (2001) · Gastroenterology · doi:10.1053/gast.2001.26262 · Cited by 167

Prevention and Treatment of Obesity, Insulin Resistance, and Diabetes by Bile Acid–Binding Resin

Kobayashi, M., Ikegami, H., Fujisawa, T., Nojima, K., Kawabata, Y., Noso, S., Babaya, N., Itoi‐Babaya, M., Yamaji, K., Hiromine, Y., et al. (2006) · Diabetes · doi:10.2337/db06-0353 · Cited by 166

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

Cheng, J., Shah, Y. M., & Gonzalez, F. J. (2012) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2012.03.003 · Cited by 162

Targeting xenobiotic receptors PXR and CAR for metabolic diseases

Gao, J., & Xie, W. (2012) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2012.07.003 · Cited by 158

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

Schreuder, T. C. M. A., Marsman, H. A., Leníček, M., van Werven, J. R., Nederveen, A. J., Jansen, P. L. M., & Schaap, F. G. (2010) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.00322.2009 · Cited by 158

FXR and PXR: Potential therapeutic targets in cholestasis

Jonker, J. W., Liddle, C., & Downes, M. (2011) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2011.06.012 · Cited by 156

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

Hartman, H. B., Gardell, S. J., Petucci, C. J., Wang, S., Krueger, J. A., & Evans, M. J. (2009) · Journal of Lipid Research · doi:10.1194/jlr.m800619-jlr200 · Cited by 155

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

Terjung, B., Söhne, J., Lechtenberg, B., Gottwein, J. M., Muennich, M., Herzog, V., Mähler, M., Sauerbruch, T., & Spengler, U. (2009) · Gut · doi:10.1136/gut.2008.157818 · Cited by 153

Pregnane X Receptor Is a Target of Farnesoid X Receptor

Jung, D., Mangelsdorf, D. J., & Meyer, U. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m600116200 · Cited by 148

Ursodeoxycholic acid in the Ursidae: biliary bile acids of bears, pandas, and related carnivores.

Hagey, L. R., Crombie, D. L., Espinosa, E., Carey, M. C., Igimi, H., & Hofmann, A. (1993) · Journal of Lipid Research · doi:10.1016/s0022-2275(20)35109-9 · Cited by 147

Biliary secretion and excretion in health and disease: Current concepts

Hofmann, A. F. (2007) · Annals of Hepatology · doi:10.1016/s1665-2681(19)31949-0 · Cited by 145

Nuclear Receptors HNF4α and LRH-1 Cooperate in Regulating Cyp7a1 in Vivo

Kır, S., Zhang, Y., Gerard, R. D., Kliewer, S. A., & Mangelsdorf, D. J. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.421834 · Cited by 142

The Human Gallbladder Secretes Fibroblast Growth Factor 19 Into Bile: Towards Defining the Role of Fibroblast Growth Factor 19 in the Enterobiliary Tract

Zweers, S. J. L. B., Booij, K. A. C., Komuta, M., Roskams, T., Gouma, D. J., Jansen, P. L. M., & Schaap, F. G. (2011) · Hepatology · doi:10.1002/hep.24702 · Cited by 141

Co-receptor Requirements for Fibroblast Growth Factor-19 Signaling

Wu, X., Ge, H., Gupte, J., Weiszmann, J., Shimamoto, G., Stevens, J., Hawkins, N., Lemon, B., Shen, W., Xu, J., et al. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.c700130200 · Cited by 140

Bile Acids Up-regulate Death Receptor 5/TRAIL-receptor 2 Expression via a c-Jun N-terminal Kinase-dependent Pathway Involving Sp1

Higuchi, H., Grambihler, A., Canbay, A. E., Bronk, S. F., & Gores, G. J. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m309476200 · Cited by 140

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

Han, S., Li, T., Ellis, E. C. S., Strom, S. C., & Chiang, J. Y. L. (2010) · Molecular Endocrinology · doi:10.1210/me.2009-0482 · Cited by 138

Effectiveness of Colesevelam Hydrochloride in Decreasing LDL Cholesterol in Patients With Primary Hypercholesterolemia: A 24-Week Randomized Controlled Trial

Insull, W., Toth, P. D., Mullican, W. S., Hunninghake, D. B., Burke, S. K., Donovan, J. M., & Davidson, M. H. (2001) · Mayo Clinic Proceedings · doi:10.4065/76.10.971 · Cited by 138

Effects of FXR in foam-cell formation and atherosclerosis development

Guo, G. L., Santamarina-Fojo, S., Akiyama, T. E., Amar, M. J., Paigen, B. J., Brewer, B., & Gonzalez, F. J. (2006) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2006.09.018 · Cited by 133

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

Jansen, P. L. M., van Werven, J. R., Aarts, E. O., Berends, F. J., Janssen, I. M. C., Stoker, J., & Schaap, F. G. (2011) · Digestive Diseases · doi:10.1159/000324128 · Cited by 130

Identification and characterization of noncalcemic, tissue-selective, nonsecosteroidal vitamin D receptor modulators

Ma, Y. (2006) · Journal of Clinical Investigation · doi:10.1172/jci25901 · Cited by 118

Farnesoid X Receptor Alleviates Age-Related Proliferation Defects in Regenerating Mouse Livers by Activating Forkhead Box M1b Transcription

Chen, W.-D., Wang, Y.-D., Zhang, L., Shiah, S., Wang, M., Yang, F., Yu, D., Forman, B. M., & Huang, W. (2010) · Hepatology · doi:10.1002/hep.23390 · Cited by 115

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

Hollman, D. A. A., Milona, A., van Erpecum, K. J., & van Mil, S. W. C. (2012) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2012.07.004 · Cited by 112

Chenodeoxycholic acid inhibits increased cholesterol and cholestanol synthesis in patients with cerebrotendinous Xanthomatosis

Salen, G., Meriwether, T. W., & Nicolau, G. (1975) · Biochemical Medicine · doi:10.1016/0006-2944(75)90020-4 · Cited by 110

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

Chang, T. K. H. (2009) · The AAPS Journal · doi:10.1208/s12248-009-9135-y · Cited by 108

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

Han, S., & Chiang, J. Y. L. (2008) · Drug Metabolism and Disposition · doi:10.1124/dmd.108.025155 · Cited by 108

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

Wu, X., Ge, H., Lemon, B. D., Vonderfecht, S. L., Baribault, H., Weiszmann, J., Gupte, J., Gardner, J., Lindberg, R. A., Wang, Z., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1009427107 · Cited by 104

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

Chen, L., Yao, X., Young, A., McNulty, J. A., Anderson, D., Liu, Y., Nystrom, C., Croom, D. K., Ross, S. A., Collins, J. L., et al. (2011) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00323.2011 · Cited by 103

Combined loss of orphan receptors PXR and CAR heightens sensitivity to toxic bile acids in mice

Uppal, H., Toma, D., Saini, S. P. S., Ren, S., Jones, T. J., & Xie, W. (2005) · Hepatology · doi:10.1002/hep.20512 · Cited by 102

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

Hambruch, E., Miyazaki‐Anzai, S., Hahn, U. K., Matysik, S., Boettcher, A., Perović‐Ottstadt, S., Schlüter, T., Kinzel, O. D., Krol, H. D., Deuschle, U., et al. (2012) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.112.196519 · Cited by 100

Inhibition of ileal bile acid transport and reduced atherosclerosis in apoE−/− mice by SC-435

Bhat, B. G., Rapp, S. R., Beaudry, J. A., Napawan, N., Butteiger, D. N., Hall, K. A., Null, C. L., Luo, Y., & Keller, B. T. (2003) · Journal of Lipid Research · doi:10.1194/jlr.m200469-jlr200 · Cited by 99

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

Soisson, S. M., Parthasarathy, G., Adams, A. D., Sahoo, S. P., Sitlani, A., Sparrow, C. P., Cui, J., & Becker, J. W. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0710981105 · Cited by 92

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

Deuschle, U., Schüler, J. B., Schulz, A., Schlüter, T., Kinzel, O. D., Abel, U. R., & Kremoser, C. (2012) · PLoS ONE · doi:10.1371/journal.pone.0043044 · Cited by 81

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

Ogura, M., Nishida, S., Ishizawa, M., Sakurai, K., Shimizu, M., Matsuo, S., Amano, S., Uno, S., & Makishima, M. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.145987 · Cited by 81

FGF19 and Cancer

Lin, B. C., & Desnoyers, L. (2012) · Advances in experimental medicine and biology · doi:10.1007/978-1-4614-0887-1_12 · Cited by 78

The PXR is a drug target for chronic inflammatory liver disease

Wallace, K., Cowie, D. E., Konstantinou, D. K., Hill, S. J., Tjelle, T. E., Axon, A., Koruth, M., White, S. A., Carlsen, H., Mann, D. A., et al. (2010) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2010.04.012 · Cited by 78

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

Miyata, M., Sakaida, Y., Matsuzawa, H., Yoshinari, K., & Yamazoe, Y. (2011) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.34.1885 · Cited by 77

α5β1-integrins are sensors for tauroursodeoxycholic acid in hepatocytes

Gohlke, H., Schmitz, B., Sommerfeld, A., Reinehr, R., & Häussinger, D. (2013) · Hepatology · doi:10.1002/hep.25992 · Cited by 77

Farnesoid X Receptor Agonist for the Treatment of Liver and Metabolic Disorders: Focus on 6-ethyl-CDCA

Fiorucci, S., Cipriani, S., Mencarelli, A., Baldelli, F., Bifulco, G., & Zampella, A. (2011) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/138955711796355258 · Cited by 76

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

Renga, B., Migliorati, M., Mencarelli, A., Cipriani, S., D’Amore, C., Distrutti, E., & Fiorucci, S. (2011) · Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms · doi:10.1016/j.bbagrm.2011.01.008 · Cited by 75

Lithocholic acid is an endogenous inhibitor of MDM4 and MDM2

Vogel, S., Bauer, M. R., Joerger, A. C., Wilcken, R., Brandt, T., Veprintsev, D. B., Rutherford, T. J., Fersht, A. R., & Boeckler, F. M. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1215060109 · Cited by 74

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

Beilke, L. D., Aleksunes, L. M., Holland, R. D., Besselsen, D. G., Beger, R. D., Klaassen, C. D., & Cherrington, N. J. (2009) · Drug Metabolism and Disposition · doi:10.1124/dmd.108.023317 · Cited by 73

Structural Determinants for Vitamin D Receptor Response to Endocrine and Xenobiotic Signals

Adachi, R., Shulman, A. I., Yamamoto, K., Shimomura, I., Yamada, S., Mangelsdorf, D. J., & Makishima, M. (2003) · Molecular Endocrinology · doi:10.1210/me.2003-0244 · Cited by 71

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

Jiang, Y., Iakova, P. A., Jin, J., Sullivan, E. M., Sharin, V. G., Hong, I., Anakk, S., Mayor, A., Darlington, G., Finegold, M. J., et al. (2012) · Hepatology · doi:10.1002/hep.26146 · Cited by 66

Effect of Jaundice on Rheumatoid Arthritis

Hench, P. S. (1938) · BMJ · doi:10.1136/bmj.2.4050.394 · Cited by 61

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

Abel, U. R., Schlüter, T., Schulz, A., Hambruch, E., Steeneck, C., Hornberger, M., Hoffmann, T. K., Perović‐Ottstadt, S., Kinzel, O. D., Burnet, M. W. M., et al. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.06.084 · Cited by 61

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

Bass, J. Y., Caravella, J. A., Chen, L., Creech, K. L., Deaton, D. N., Madauss, K. P., Marr, H. B., McFadyen, R. B., Miller, A. B., Mills, W. Y., et al. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.12.089 · Cited by 60

The Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling

Drafahl, K. A., McAndrew, C. W., Meyer, A. N., Haas, M., & Donoghue, D. J. (2010) · PLoS ONE · doi:10.1371/journal.pone.0014412 · Cited by 60

Inhibition of ileal bile acid transport lowers plasma cholesterol levels by inactivating hepatic farnesoid X receptor and stimulating cholesterol 7α-hydroxylase

Li, H., Xu, G., Shang, Q., Pan, L., Shefer, S., BATTA, A. K., Bollineni, J. S., Tint, G. S., Keller, B. T., & Salen, G. (2004) · Metabolism · doi:10.1016/j.metabol.2004.01.017 · Cited by 58

Lithocholic acid induction of the FGF19 promoter in intestinal cells is mediated by PXR

Wistuba, W. (2007) · World Journal of Gastroenterology · doi:10.3748/wjg.v13.i31.4230 · Cited by 57

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

Herbert, M. R., Siegel, D. L., Staszewski, L. M., Cayanan, C. S., Banerjee, U., Dhamija, S., Anderson, J., Fan, A., Wang, L., Rix, P. J., et al. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.08.014 · Cited by 57

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

Triantis, V., Saeland, E., Bijl, N., Elferink, R. P. J. O., & Jansen, P. L. M. (2010) · Hepatology · doi:10.1002/hep.23708 · Cited by 55

Ursodeoxycholate mobilizes intracellular Ca2+ and activates phosphorylase a in isolated hepatocytes

Bouscarel, B. E., Fromm, H., & Nussbaum, R. (1993) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1993.264.2.g243 · Cited by 52

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

Beraza, N., Ofner‐Ziegenfuß, L., Ehedego, H., Boekschoten, M. V., Bischoff, S. C., Müller, M. M., Trauner, M. A., & Trautwein, C. (2010) · Gut · doi:10.1136/gut.2010.223834 · Cited by 47

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

Marinozzi, M., Carotti, A., Sansone, E., Macchiarulo, A., Rosatelli, E., Sardella, R., Natalini, B., Rizzo, G., Adorini, L., Passeri, D., et al. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.04.021 · Cited by 46

Successful treatment of severe unconjugated hyperbilirubinemia via induction of UGT1A1 by rifampicin

Ellis, E. C. S., Wagner, M., Lammert, F., Németh, A., Gumhold, J., Strassburg, C. P., Kylander, C., Katsika, D., Trauner, M. A., Einarsson, C., et al. (2005) · Journal of Hepatology · doi:10.1016/j.jhep.2005.09.011 · Cited by 35

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

Li, Z., Kruijt, J. K., van der Sluis, R. J., van Berkel, T. J. C., & Hoekstra, M. (2013) · Physiological Genomics · doi:10.1152/physiolgenomics.00151.2012 · Cited by 31

Effect of acid-base balance and acetazolamide on ursodeoxycholate-induced biliary bicarbonate secretion

Marı́n, J. J. G., Dumont, M., Corbic, M., de Couet, G., & Erlinger, S. (1985) · American Journal of Physiology-Gastrointestinal and Liver Physiology · doi:10.1152/ajpgi.1985.248.1.g20 · Cited by 27

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

Inoue, J., SATOH, S.-I., Kita, M., Nakahara, M., Hachimura, S., Miyata, M., Nishimaki‐Mogami, T., & Sato, R. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.04.100 · Cited by 25

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

Sakamoto, S. X., Kusuhara, H., Miyata, K., Shimaoka, H., Kanazu, T., Matsuo, Y., Nomura, K., Okamura, N., Hara, S., Horie, K., et al. (2007) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.106.116426 · Cited by 24

Effects of corticosteroids on bilirubin metabolism in patients with Gilbert’s syndrome

Ohkubo, H., Okuda, K., & Iida, S. (1981) · Hepatology · doi:10.1002/hep.1840010213 · Cited by 19

Proteomics for the discovery of nuclear bile acid receptor FXR targets

Gardmo, C., Tamburro, A., Modica, S., & Moschetta, A. (2011) · Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease · doi:10.1016/j.bbadis.2011.03.009 · Cited by 17

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

Hansen, M., Sonne, D. P., Mikkelsen, S. U., Gluud, L. L., Vilsbøll, T., & Knop, F. K. (2012) · BMJ Open · doi:10.1136/bmjopen-2012-001803 · Cited by 7

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

Wahlstrom, A. M., Sayin, S. I., Marschall, H., & Bäckhed, F. (2016) · Cell Metabolism · doi:10.1016/j.cmet.2016.05.005 · Cited by 2,969

Gut microbiota-derived metabolites as key actors in inflammatory bowel disease

Lavelle, A., & Sokol, H. (2020) · Nature Reviews Gastroenterology & Hepatology · doi:10.1038/s41575-019-0258-z · Cited by 2,015

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Wu, H., Esteve, E., Tremaroli, V., Khan, M. T., Caesar, R., Mannerås-Holm, L., Ståhlman, M., Olsson, L. M., Serino, M., Planas-Fèlix, M., et al. (2017) · Nature Medicine · doi:10.1038/nm.4345 · Cited by 1,632

Adipose tissue distribution, inflammation and its metabolic consequences, including diabetes and cardiovascular disease

Chait, A., & den Hartigh, L. J. (2020) · Frontiers in Cardiovascular Medicine · doi:10.3389/fcvm.2020.00022 · Cited by 1,529

EASL Clinical Practice Guidelines: The diagnosis and management of patients with primary biliary cholangitis.

Hirschfield, G. M., Beuers, U., Corpechot, C., Invernizzi, P., Jones, D., Marzioni, M., & Schramm, C. (2017) · Journal of Hepatology · doi:10.1016/j.jhep.2017.03.022 · Cited by 1,480

Bile acid receptors as targets for drug

Schaap, G., Trauner, M. A., & Jansen, P. L. M. (2013)

Farnesoid X Receptor Agonists and Other Bile Acid Signaling Strategies for Treatment of Liver Disease

Halilbasic, E., Fuchs, C. D., Traussnigg, S., & Trauner, M. (2016) · Digestive Diseases · doi:10.1159/000445268 · Cited by 39

Bile Acid as Therapeutic Agents

Yamanashi, Y., Takada, T., & Suzuki, H. (2017) · Springer eBooks · doi:10.1007/978-4-431-56062-3_5 · Cited by 1

Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases

Xu, Y. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00342 · Cited by 75

Bile Acid Receptor Therapeutics Effects on Chronic Liver Diseases

Meadows, V., Kennedy, L. L., Kundu, D., Alpini, G. D., & Francis, H. (2020) · Frontiers in Medicine · doi:10.3389/fmed.2020.00015 · Cited by 31