Bile Acids: Natural Ligands for an Orphan Nuclear Receptor
Abstract
Bile acids regulate the transcription of genes that control cholesterol homeostasis through molecular mechanisms that are poorly understood. Physiological concentrations of free and conjugated chenodeoxycholic acid, lithocholic acid, and deoxycholic acid activated the farnesoid X receptor (FXR; NR1H4), an orphan nuclear receptor. As ligands, these bile acids and their conjugates modulated interaction of FXR with a peptide derived from steroid receptor coactivator 1. These results provide evidence for a nuclear bile acid signaling pathway that may regulate cholesterol homeostasis.
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In the presence of CDCA, which is present under physiological conditions, DCA and LCA appear to be antagonists of the FXR receptor.
“However, in the presence of CDCA, which is present under physiological conditions, DCA and LCA appear to be antagonists of the FXR receptor (Parks et al., 1999; Yu et al., 2002).”
From <i>Akkermansia muciniphila</i> alleviates <scp>high‐fat‐diet</scp> ‐related metabolic‐associated fatty liver disease by modulating gut microbiota and bile acids (2023) · cites this paper as Parks et al., 1999
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The nuclear receptor superfamily: the second decade
Mangelsdorf, D. J., Thummel, C., Beato, M., Herrlich, P., Schütz, G., Umesono, K., Blumberg, B., Kastner, P., Mark, M., Chambon, P., et al. (1995) · Cell · doi:10.1016/0092-8674(95)90199-x · Cited by 6,964 · see citing works
A signature motif in transcriptional co-activators mediates binding to nuclear receptors
Heery, D. M., Kalkhoven, E., Hoare, S., & Parker, M. G. (1997) · Nature · doi:10.1038/42750 · Cited by 2,134 · see citing works
Russell, D. W., & Setchell, K. D. R. (1992) · Biochemistry · doi:10.1021/bi00135a001 · Cited by 819 · see citing works
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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 · see citing works
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 · see citing works
Bile acid-microbiota crosstalk in gastrointestinal inflammation and carcinogenesis
Jia, W., Xie, G., & Jia, W. (2018) · Nature Reviews Gastroenterology & Hepatology · doi:10.1038/nrgastro.2017.119 · Cited by 1,924 · see citing works
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 · see citing works
Self-citationTargeted Disruption of the Nuclear Receptor FXR/BAR Impairs Bile Acid and Lipid Homeostasis
Sinal, C. J., Tohkin, M., Miyata, M., Ward, J. M., Lambert, G., & Gonzalez, F. J. (2000) · Cell · doi:10.1016/s0092-8674(00)00062-3 · Cited by 1,819 · see citing works
Role of Bile Acids and Bile Acid Receptors in Metabolic Regulation
Lefebvre, P., Cariou, B., Lien, F., Kuipers, F., & Staels, B. (2009) · Physiological Reviews · doi:10.1152/physrev.00010.2008 · Cited by 1,678 · see citing works
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 · see citing works
Molecular Basis for Feedback Regulation of Bile Acid Synthesis by Nuclear Receptors
Lu, T. T., Makishima, M., Repa, J. J., Schoonjans, K., Kerr, T. A., Auwerx, J., & Mangelsdorf, D. J. (2000) · Molecular Cell · doi:10.1016/s1097-2765(00)00050-2 · Cited by 1,487 · see citing works
Targeting bile‐acid signalling for metabolic diseases
Thomas, C., Pellicciari, R., Pruzanski, M., Auwerx, J., & Schoonjans, K. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2619 · Cited by 1,422 · see citing works
Godoy, P., Hewitt, N. J., Albrecht, U., Andersen, M. E., Ansari, N., Bhattacharya, S., Bode, J. G., Bolleyn, J., Borner, C., Böttger, J., et al. (2013) · Archives of Toxicology · doi:10.1007/s00204-013-1078-5 · Cited by 1,280 · see citing works
Pleiotropic Roles of Bile Acids in Metabolism
de Aguiar Vallim, T. Q., Tarling, E. J., & Edwards, P. A. (2013) · Cell Metabolism · doi:10.1016/j.cmet.2013.03.013 · Cited by 1,209 · see citing works
Bile acids and the gut microbiota: metabolic interactions and impacts on disease
Collins, S. L., Stine, J. G., Bisanz, J. E., Okafor, C. D., & Patterson, A. D. (2023) · Nature Reviews Microbiology · doi:10.1038/s41579-022-00805-x · Cited by 1,214 · see citing works
Dietary lipids, gut microbiota and lipid metabolism
Schoeler, M., & Caesar, R. (2019) · Reviews in Endocrine and Metabolic Disorders · doi:10.1007/s11154-019-09512-0 · Cited by 1,163 · see citing works
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 · see citing works
Bile salt transporters: molecular characterization, function, and regulation
Trauner, M., & Boyer, J. L. (2003) · Physiological Reviews · doi:10.1152/physrev.00027.2002 · Cited by 999 · see citing works
Bile acid signaling in metabolic disease and drug therapy
Li, T., & Chiang, J. Y. L. (2014) · Pharmacological Reviews · doi:10.1124/pr.113.008201 · Cited by 935 · see citing works
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 · see citing works
Self-citationBacterial metabolism of bile acids promotes generation of peripheral regulatory T cells
Campbell, C., McKenney, P. T., Konstantinovsky, D., Isaeva, O. I., Schizas, M., Verter, J., Mai, C., Jin, W.-B., Guo, C.-J., Violante, S., et al. (2020) · Nature · doi:10.1038/s41586-020-2193-0 · Cited by 901 · see citing works
Postler, T. S., & Ghosh, S. (2017) · Cell Metabolism · doi:10.1016/j.cmet.2017.05.008 · Cited by 876 · see citing works
Transcriptional integration of metabolism by the nuclear sterol-activated receptors LXR and FXR
Calkin, A. C., & Tontonoz, P. (2012) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm3312 · Cited by 779 · see citing works
Jiao, N., Baker, S. S., Chapa-Rodriguez, A., Liu, W., Nugent, C. A., Tsompana, M., Mastrandrea, L., Buck, M. J., Baker, R. D., Genco, R. J., et al. (2018) · Gut · doi:10.1136/gutjnl-2017-314307 · Cited by 737 · see citing works
Systemic gut microbial modulation of bile acid metabolism in host tissue compartments
Swann, J. R., Want, E. J., Geier, F. M., Spagou, K., Wilson, I. D., Sidaway, J. E., Nicholson, J. K., & Holmes, E. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1006734107 · Cited by 726 · see citing works
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 · see citing works
Self-citationBile acids as regulatory molecules
Hylemon, P. B., Zhou, H., Pandak, W. M., Ren, S., Gil, G., & Dent, P. (2009) · Journal of Lipid Research · doi:10.1194/jlr.r900007-jlr200 · Cited by 694 · see citing works
The bile acid receptor FXR is a modulator of intestinal innate immunity
Vavassori, P., Mencarelli, A., Renga, B., Distrutti, E., & Fiorucci, S. (2009) · The Journal of Immunology · doi:10.4049/jimmunol.0803978 · Cited by 655 · see citing works
Bile acids and nonalcoholic fatty liver disease: Molecular insights and therapeutic perspectives
Arab, J. P., Karpen, S. J., Dawson, P. A., Arrese, M., & Trauner, M. (2017) · Hepatology · doi:10.1002/hep.28709 · Cited by 634 · see citing works
Leesnitzer, L. M., Parks, D. J., Bledsoe, R. K., Cobb, J. E., Collins, J. L., Consler, T. G., Davis, R. G., Hull-Ryde, E. A., Lenhard, J. M., Patel, L., et al. (2002) · Biochemistry · doi:10.1021/bi0159581 · Cited by 566 · see citing works
Self-citationBile Acid-Activated Receptors, Intestinal Microbiota, and the Treatment of Metabolic Disorders
Fiorucci, S., & Distrutti, E. (2015) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2015.09.001 · Cited by 539 · see citing works
Yang, F., Huang, X., Yi, T., Yen, Y., Moore, D. D., & Huang, W. (2007) · Cancer Research · doi:10.1158/0008-5472.can-06-1078 · Cited by 488 · see citing works
Self-citationInteractions between gut bacteria and bile in health and disease
Long, S. L., Gahan, C. G. M., & Joyce, S. A. (2017) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2017.06.002 · Cited by 495 · see citing works
Bile acid nuclear receptor FXR and digestive system diseases
Ding, L., Yang, L., Wang, Z., & Huang, W. (2015) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2015.01.004 · Cited by 477 · see citing works
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 · see citing works
Molecular physiology of bile acid signaling in health, disease, and aging
Perino, A., Demagny, H., Velazquez-Villegas, L., & Schoonjans, K. (2021) · Physiological Reviews · doi:10.1152/physrev.00049.2019 · Cited by 481 · see citing works
Kong, B., Wang, L., Chiang, J. Y. L., Zhang, Y., Klaassen, C. D., & Guo, G. L. (2012) · Hepatology · doi:10.1002/hep.25740 · Cited by 456 · see citing works
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 · see citing works
Human Insulin Resistance Is Associated With Increased Plasma Levels of 12α-Hydroxylated Bile Acids
Haeusler, R. A., Astiarraga, B., Camastra, S., Accili, D., & Ferrannini, E. (2013) · Diabetes · doi:10.2337/db13-0639 · Cited by 444 · see citing works
Expression and function of the bile acid receptor TGR5 in Kupffer cells
Keitel, V., Donner, M., Winandy, S., Kubitz, R., & Häussinger, D. (2008) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2008.04.171 · Cited by 418 · see citing works
Bile Acids as Hormones: The FXR-FGF15/19 Pathway
Kliewer, S. A., & Mangelsdorf, D. J. (2015) · Digestive Diseases · doi:10.1159/000371670 · Cited by 424 · see citing works
Self-citationFXR: 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 · see citing works
Self-citationChu, H., Duan, Y., Yang, L., & Schnabl, B. (2019) · Gut · doi:10.1136/gutjnl-2018-316307 · Cited by 354 · see citing works
Degirolamo, C., Rainaldi, S., Bovenga, F., Murzilli, S., & Moschetta, A. (2014) · Cell Reports · doi:10.1016/j.celrep.2014.02.032 · Cited by 356 · see citing works
FXR, a multipurpose nuclear receptor
Lee, F. Y., Lee, H., Hubbert, M. L., Edwards, P. A., & Zhang, Y. (2006) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2006.08.002 · Cited by 344 · see citing works
A randomized controlled trial of high-dose ursodesoxycholic acid for nonalcoholic steatohepatitis
Ratziu, V., de Ledinghen, V., Oberti, F., Mathurin, P., Wartelle-Bladou, C., Renou, C., Sogni, P., Maynard, M., Larrey, D., Serfaty, L., et al. (2011) · Journal of Hepatology · doi:10.1016/j.jhep.2010.08.030 · Cited by 338 · see citing works
Bile acids as endogenous etiologic agents in gastrointestinal cancer
Bernstein, H., Bernstein, C., Payne, C. M., & Dvorak, K. (2009) · World Journal of Gastroenterology · doi:10.3748/wjg.15.3329 · Cited by 340 · see citing works
Sorg, J. A., & Sonenshein, A. L. (2010) · Journal of Bacteriology · doi:10.1128/jb.00610-10 · Cited by 332 · see citing works
Bile acid is a significant host factor shaping the gut microbiome of diet-induced obese mice
Zheng, X., Huang, F., Zhao, A., Lei, S., Zhang, Y., Xie, G., Chen, T., Qu, C., Rajani, C., Dong, B., et al. (2017) · BMC Biology · doi:10.1186/s12915-017-0462-7 · Cited by 323 · see citing works
Ridlon, J. M., Ikegawa, S., Alves, J. M. P., Zhou, B., Kobayashi, A., Iida, T., Mitamura, K., Tanabe, G., Serrano, M., De Guzman, A., et al. (2013) · Journal of Lipid Research · doi:10.1194/jlr.m038869 · Cited by 319 · see citing works
Guo, G. L., Lambert, G., Negishi, M., Ward, J. M., Brewer, H. B., Kliewer, S. A., Gonzalez, F. J., & Sinal, C. J. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m307145200 · Cited by 312 · see citing works
Self-citationZhang, S., Wang, J., Liu, Q., & Harnish, D. C. (2009) · Journal of Hepatology · doi:10.1016/j.jhep.2009.03.025 · Cited by 290 · see citing works
Bile acid signaling pathways from the enterohepatic circulation to the central nervous system
Mertens, K. L., Kalsbeek, A., Soeters, M. R., & Eggink, H. M. (2017) · Frontiers in Neuroscience · doi:10.3389/fnins.2017.00617 · Cited by 287 · see citing works
Bile acids are nutrient signaling hormones
Zhou, H., & Hylemon, P. B. (2014) · Steroids · doi:10.1016/j.steroids.2014.04.016 · Cited by 285 · see citing works
Modica, S., Petruzzelli, M., Bellafante, E., Murzilli, S., Salvatore, L., Celli, N., Di Tullio, G., Palasciano, G., Moustafa, T., Halilbasic, E., et al. (2012) · Gastroenterology · doi:10.1053/j.gastro.2011.10.028 · Cited by 275 · see citing works
Verbeke, L., Farre, R., Trebicka, J., Komuta, M., Roskams, T., Klein, S., Elst, I. V., Windmolders, P., Vanuytsel, T., Nevens, F., et al. (2014) · Hepatology · doi:10.1002/hep.26939 · Cited by 258 · see citing works
Coordinate transcriptional regulation of bile acid homeostasis and drug metabolism
Eloranta, J. J., & Kullak-Ublick, G. A. (2005) · Archives of Biochemistry and Biophysics · doi:10.1016/j.abb.2004.09.019 · Cited by 260 · see citing works
Trimethylamine-N-oxide (TMAO)-induced atherosclerosis is associated with bile acid metabolism
Ding, L., Chang, M., Guo, Y., Zhang, L., Xue, C., Yanagita, T., Zhang, T., & Wang, Y. (2018) · Lipids in Health and Disease · doi:10.1186/s12944-018-0939-6 · Cited by 250 · see citing works
Cholic acid mediates negative feedback regulation of bile acid synthesis in mice
Li-Hawkins, J., Gåfvels, M., Olin, M., Lund, E. G., Andersson, U., Schuster, G., Björkhem, I., Russell, D. W., & Eggertsen, G. (2002) · Journal of Clinical Investigation · doi:10.1172/jci0216309 · Cited by 227 · see citing works
New therapeutic concepts in bile acid transport and signaling for management of cholestasis
Trauner, M., Fuchs, C. D., Halilbasic, E., & Paumgartner, G. (2017) · Hepatology · doi:10.1002/hep.28991 · Cited by 227 · see citing works
Metabolic Messengers: bile acids
Perino, A., & Schoonjans, K. (2022) · Nature Metabolism · doi:10.1038/s42255-022-00559-z · Cited by 223 · see citing works
Intestinal absorption of bile acids in health and disease
Ticho, A. L., Malhotra, P., Dudeja, P. K., Gill, R. K., & Alrefai, W. A. (2019) · Comprehensive physiology · doi:10.1002/cphy.c190007 · Cited by 215 · see citing works
Rao, A., Kosters, A., Mells, J. E., Zhang, W., Setchell, K. D. R., Amanso, A. M., Wynn, G. M., Xu, T., Keller, B. T., Yin, H., et al. (2016) · Science Translational Medicine · doi:10.1126/scitranslmed.aaf4823 · Cited by 211 · see citing works
Kumar, D. P., Rajagopal, S., Mahavadi, S., Mirshahi, F., Grider, J. R., Murthy, K. S., & Sanyal, A. J. (2012) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2012.09.104 · Cited by 206 · see citing works
The biosynthesis, signaling, and neurological functions of bile acids
Kiriyama, Y., & Nochi, H. (2019) · Biomolecules · doi:10.3390/biom9060232 · Cited by 204 · see citing works
Novel therapeutic targets for cholestatic and fatty liver disease
Trauner, M., & Fuchs, C. D. (2022) · Gut · doi:10.1136/gutjnl-2021-324305 · Cited by 204 · see citing works
Sun, R., Yang, N., Kong, B., Cao, B., Feng, D., Yu, X., Ge, C., Huang, J., Shen, J., Wang, P., et al. (2017) · Molecular Pharmacology · doi:10.1124/mol.116.106617 · Cited by 199 · see citing works
Gaieb, Z., Liu, S., Gathiaka, S., Chiu, M., Yang, H., Shao, C., Feher, V. A., Walters, W. P., Kuhn, B., Rudolph, M. G., et al. (2018) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-017-0088-4 · Cited by 193 · see citing works
Prieur, X., Coste, H., & Rodríguez, J. C. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m301302200 · Cited by 194 · see citing works
Host genotype and gut microbiome modulate insulin secretion and diet-induced metabolic phenotypes
Kreznar, J. H., Keller, M. P., Traeger, L. L., Rabaglia, M. E., Schueler, K. L., Stapleton, D. S., Zhao, W., Vivas, E. I., Yandell, B. S., Broman, A. T., et al. (2017) · Cell Reports · doi:10.1016/j.celrep.2017.01.062 · Cited by 177 · see citing works
The bile acid membrane receptor TGR5: a valuable metabolic target
Pols, T. W. H., Noriega, L. G., Nomura, M., Auwerx, J., & Schoonjans, K. (2011) · Digestive Diseases · doi:10.1159/000324126 · Cited by 185 · see citing works
Molecular basis of bile acid-FXR-FGF15/19 signaling axis
Katafuchi, T., & Makishima, M. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23116046 · Cited by 193 · see citing works
Baghdasaryan, A., Fuchs, C. D., Österreicher, C. H., Lemberger, U. J., Halilbasic, E., Påhlman, I., Graffner, H., Krones, E., Fickert, P., Wahlström, A., et al. (2016) · Journal of Hepatology · doi:10.1016/j.jhep.2015.10.024 · Cited by 187 · see citing works
Fiorucci, S., Rizzo, G., Antonelli, E., Renga, B., Mencarelli, A., Riccardi, L., Orlandi, S., Pruzanski, M., Morelli, A., & Pellicciari, R. (2005) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.084905 · Cited by 183 · see citing works
Role of gut microbiota in functional constipation
Zhang, S., Wang, R., Li, D., Zhao, L., & Zhu, L. (2021) · Gastroenterology Report · doi:10.1093/gastro/goab035 · Cited by 175 · see citing works
“CYP7A1 [49, 50], and consequently elevated de novo BA synthesis”
BackgroundBile acids and their receptors
Martinot, E., Sèdes, L., Baptissart, M., Lobaccaro, J.-M., Caira, F., Beaudoin, C., & Volle, D. H. (2017) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2017.01.006 · Cited by 162 · see citing works
Mencarelli, A., Renga, B., Migliorati, M., Cipriani, S., Distrutti, E., Santucci, L., & Fiorucci, S. (2009) · The Journal of Immunology · doi:10.4049/jimmunol.0901347 · Cited by 177 · see citing works
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 · see citing works
Fiorucci, S., Rizzo, G., Antonelli, E., Renga, B., Mencarelli, A., Riccardi, L., Morelli, A., Pruzanski, M., & Pellicciari, R. (2005) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.105.085597 · Cited by 177 · see citing works
Bahne, E., Sun, E. W. L., Young, R. L., Hansen, M., Sonne, D. P., Hansen, J. S., Rohde, U., Liou, A. P., Jackson, M. L., de Fontgalland, D., et al. (2018) · JCI Insight · doi:10.1172/jci.insight.93936 · Cited by 173 · see citing works
Farnesoid x receptor ligands inhibit vascular smooth muscle cell inflammation and migration
Li, Y. T. Y., Swales, K. E., Thomas, G. J., Warner, T. D., & Bishop-Bailey, D. (2007) · Arteriosclerosis, Thrombosis, and Vascular Biology · doi:10.1161/atvbaha.107.152694 · Cited by 171 · see citing works
Ahmad, N. N., Pfalzer, A., & Kaplan, L. M. (2013) · International Journal of Obesity · doi:10.1038/ijo.2013.38 · Cited by 163 · see citing works
SUMOylation inhibitors synergize with FXR agonists in combating liver fibrosis
Zhou, J., Cui, S., He, Q., Guo, Y., Pan, X., Zhang, P., Huang, N., Ge, C., Wang, G., Gonzalez, F. J., et al. (2020) · Nature Communications · doi:10.1038/s41467-019-14138-6 · Cited by 154 · see citing works
Nuclear receptors as therapeutic targets in cholestatic liver diseases
Zollner, G., & Trauner, M. (2009) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2008.00030.x · Cited by 146 · see citing works
Mechanisms of disease: inborn errors of bile acid synthesis
Sundaram, S. S., Bove, K. E., Lovell, M. A., & Sokol, R. J. (2008) · Nature Clinical Practice Gastroenterology & Hepatology · doi:10.1038/ncpgasthep1179 · Cited by 146 · see citing works
Simonen, M., Dali-Youcef, N., Kaminska, D., Venesmaa, S., Käkelä, P., Pääkkönen, M., Hallikainen, M., Kolehmainen, M., Uusitupa, M., Moilanen, L., et al. (2012) · Obesity Surgery · doi:10.1007/s11695-012-0673-5 · Cited by 145 · see citing works
How bile acids and the microbiota interact to shape host immunity
Lee, M. H., Nuccio, S.-P., Mohanty, I., Hagey, L. R., Dorrestein, P. C., Chu, H., & Raffatellu, M. (2024) · Nature Reviews Immunology · doi:10.1038/s41577-024-01057-x · Cited by 143 · see citing works
Wu, W., Kaicen, W., Bian, X., Yang, L., Ding, S., Li, Y., Li, S., Zhuge, A., & Li, L. (2023) · Microbial Biotechnology · doi:10.1111/1751-7915.14293 · Cited by 129 · see citing works
Degirolamo, C., Modica, S., Vacca, M., Di Tullio, G., Morgano, A., D'Orazio, A., Kannisto, K., Parini, P., & Moschetta, A. (2015) · Hepatology · doi:10.1002/hep.27274 · Cited by 121 · see citing works
Tiwari, A., & Maiti, P. (2009) · Drug Discovery Today · doi:10.1016/j.drudis.2009.02.005 · Cited by 122 · see citing works
Probiotics and the BSH-related cholesterol lowering mechanism: a Jekyll and Hyde scenario
Choi, S.-B., Lew, L.-C., Yeo, S.-K., Nair Parvathy, S., & Liong, M.-T. (2015) · Critical Reviews in Biotechnology · doi:10.3109/07388551.2014.889077 · Cited by 119 · see citing works
Masse, K. E., & Lu, V. B. (2023) · Frontiers in Endocrinology · doi:10.3389/fendo.2023.1169624 · Cited by 120 · see citing works
“FXR is a primary bile acid sensor, preferentially binding to CDCA in humans and CA to a weaker extent (119).”
BackgroundChen, 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 · see citing works
Chen, W., Owsley, E., Yang, Y., Stroup, D., & Chiang, J. Y. L. (2001) · Journal of Lipid Research · doi:10.1016/s0022-2275(20)30272-8 · Cited by 112 · see citing works
Identification of Novel Pathways That Control Farnesoid X Receptor-mediated Hypocholesterolemia
Zhang, Y., Yin, L., Anderson, J., Ma, H., Gonzalez, F. J., Willson, T. M., & Edwards, P. A. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m109.083899 · Cited by 112 · see citing works
Self-citationRole of TGR5 (GPBAR1) in Liver Disease
Häussinger, D., & Keitel, V. (2018) · Seminars in Liver Disease · doi:10.1055/s-0038-1669940 · Cited by 106 · see citing works
Bile acids activated receptors in inflammatory bowel disease
Biagioli, M., Marchianò, S., Carino, A., Di Giorgio, C., Santucci, L., Distrutti, E., & Fiorucci, S. (2021) · Cells · doi:10.3390/cells10061281 · Cited by 103 · see citing works
Bile Acid-Activated Receptors: GPBAR1 (TGR5) and Other G Protein-Coupled Receptors
Keitel, V., Stindt, J., & Häussinger, D. (2019) · Handbook of Experimental Pharmacology · doi:10.1007/164_2019_230 · Cited by 98 · see citing works
Bile Acid Receptors and the Gut–Liver Axis in Nonalcoholic Fatty Liver Disease
Xue, R., Su, L., Lai, S., Wang, Y., Zhao, D., Fan, J., Chen, W., Hylemon, P. B., & Zhou, H. (2021) · Cells · doi:10.3390/cells10112806 · Cited by 95 · see citing works
The Commensal Microbe V eillonella as a Marker for Response to an FGF19 Analog in NASH
Loomba, R., Ling, L., Dinh, D. M., DePaoli, A. M., Lieu, H. D., Harrison, S. A., & Sanyal, A. J. (2021) · Hepatology · doi:10.1002/hep.31523 · Cited by 88 · see citing works
Nonsteroidal FXR Ligands: Current Status and Clinical Applications
Gege, C., Hambruch, E., Hambruch, N., Kinzel, O., & Kremoser, C. (2019) · Handbook of Experimental Pharmacology · doi:10.1007/164_2019_232 · Cited by 83 · see citing works
Role of bile acids in the regulation of the metabolic pathways
Taoka, H., Yokoyama, Y., Morimoto, K., Kitamura, N., Tanigaki, T., Takashina, Y., Tsubota, K., & Watanabe, M. (2016) · World Journal of Diabetes · doi:10.4239/wjd.v7.i13.260 · Cited by 80 · see citing works
Miyata, M., Takamatsu, Y., Kuribayashi, H., & Yamazoe, Y. (2009) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.109.160093 · Cited by 72 · see citing works
- Authors
- Parks, D. J., Blanchard, S. G., Bledsoe, R. K., Chandra, G., Consler, T. G., Kliewer, S. A., Stimmel, J. B., Willson, T. M., Zavacki, A. M., Moore, D. D., & Lehmann, J. M.
- Affiliations
- Molecular Biochemistry,
- Molecular Sciences,
- Molecular Endocrinology,
- Medicinal Chemistry, Glaxo Wellcome Research and Development, Research Triangle Park NC, 27709, USA.
- Baylor College of Medicine (US)
- Corresponding author
- Willson, Timothy M.
- Venue
- Science
- Published
- 1999-05-21
- Volume
- 284
- Issue
- 5418
- Pages
- 1365-1368
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2171398834
- Cited by
- 2,274
- References
- 3
- Citations by year
- 2026: 66 · 2025: 72 · 2024: 86 · 2023: 75 · 2022: 103 · 2021: 111 · 2020: 102 · 2019: 105 · 2018: 101 · 2017: 113 · 2016: 80 · 2015: 90 · 2014: 80 · 2013: 83 · 2012: 93
- FWCI
- 78.42
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (5f32dk009793-02)
- National Institute of Diabetes and Digestive and Kidney Diseases (R01DK053366, R01-DK53366, F32 DK09793)
- Topics
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Nuclear Receptors and Signaling
- Keywords
- bile acids, farnesoid X receptor, orphan nuclear receptor, cholesterol homeostasis, chenodeoxycholic acid, lithocholic acid, deoxycholic acid, bile acid conjugates, SRC-1, transcriptional regulation
- MeSH terms
- Receptor, Farnesoid X-Activated, Animals, Bile Acids and Salts, Carrier Proteins, Cell Line, Chenodeoxycholic Acid, Cholesterol, Deoxycholic Acid, DNA-Binding Proteins, Homeostasis, Humans, Ligands, Lithocholic Acid, Protein Conformation, Recombinant Fusion Proteins, Structure-Activity Relationship, Transcription Factors, Transfection, Signal Transduction, Receptors, Cytoplasmic and Nuclear, Symporters, Organic Anion Transporters, Sodium-Dependent, Mice, Histone Acetyltransferases, Nuclear Receptor Coactivator 1
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