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Science 21 May 1999:
Vol. 284. no. 5418, pp. 1362 - 1365
DOI: 10.1126/science.284.5418.1362
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Reports

Identification of a Nuclear Receptor for Bile Acids

Makoto Makishima, 1* Arthur Y. Okamoto, 2* Joyce J. Repa, 1* Hua Tu, 2 R. Marc Learned, 2 Alvin Luk, 2 Mitchell V. Hull, 2 Kevin D. Lustig, 2 David J. Mangelsdorf, 1dagger Bei Shan 2

Bile acids are essential for the solubilization and transport of dietary lipids and are the major products of cholesterol catabolism. Results presented here show that bile acids are physiological ligands for the farnesoid X receptor (FXR), an orphan nuclear receptor. When bound to bile acids, FXR repressed transcription of the gene encoding cholesterol 7alpha -hydroxylase, which is the rate-limiting enzyme in bile acid synthesis, and activated the gene encoding intestinal bile acid-binding protein, which is a candidate bile acid transporter. These results demonstrate a mechanism by which bile acids transcriptionally regulate their biosynthesis and enterohepatic transport.

1 Howard Hughes Medical Institute and Department of Pharmacology, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75235-9050, USA.
2 Tularik Incorporated, Two Corporate Drive, South San Francisco, CA 94080, USA.
*   These authors contributed equally to this work.

dagger    To whom correspondence should be addressed. E-mail: davo.mango{at}email.swmed.edu

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Am J Physiol Gastrointest Liver Physiol 290, G550-G556
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The nuclear receptor for bile acids, FXR, transactivates human organic solute transporter-{alpha} and -beta genes.
J.-F. Landrier, J. J. Eloranta, S. R. Vavricka, and G. A. Kullak-Ublick (2006)
Am J Physiol Gastrointest Liver Physiol 290, G476-G485
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Downregulation of Endothelin-1 by Farnesoid X Receptor in Vascular Endothelial Cells.
F. He, J. Li, Y. Mu, R. Kuruba, Z. Ma, A. Wilson, S. Alber, Y. Jiang, T. Stevens, S. Watkins, et al. (2006)
Circ. Res. 98, 192-199
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A role for FXR and human FGF-19 in the repression of paraoxonase-1 gene expression by bile acids.
D. M. Shih, H. R. Kast-Woelbern, J. Wong, Y.-R. Xia, P. A. Edwards, and A. J. Lusis (2006)
J. Lipid Res. 47, 384-392
   Abstract »    Full Text »    PDF »
Bile Acids Decrease Hepatic Paraoxonase 1 Expression and Plasma High-Density Lipoprotein Levels Via FXR-Mediated Signaling of FGFR4.
A. Gutierrez, E. P. Ratliff, A. M. Andres, X. Huang, W. L. McKeehan, and R. A. Davis (2006)
Arterioscler Thromb Vasc Biol 26, 301-306
   Abstract »    Full Text »    PDF »
Gallbladder histopathology during murine gallstone formation: relation to motility and concentrating function.
K. J. van Erpecum, D. Q-H. Wang, A. Moschetta, D. Ferri, M. Svelto, P. Portincasa, J.-J. Hendrickx, M. Schipper, and G. Calamita (2006)
J. Lipid Res. 47, 32-41
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The Human Na+-Taurocholate Cotransporting Polypeptide Gene Is Activated by Glucocorticoid Receptor and Peroxisome Proliferator-Activated Receptor-{gamma} Coactivator-1{alpha}, and Suppressed by Bile Acids via a Small Heterodimer Partner-Dependent Mechanism.
J. J. Eloranta, D. Jung, and G. A. Kullak-Ublick (2006)
Mol. Endocrinol. 20, 65-79
   Abstract »    Full Text »    PDF »
FXR regulates organic solute transporters {alpha} and {alpha} in the adrenal gland, kidney, and intestine.
H. Lee, Y. Zhang, F. Y. Lee, S. F. Nelson, F. J. Gonzalez, and P. A. Edwards (2006)
J. Lipid Res. 47, 201-214
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Ileal Bile Acid-binding Protein, Functionally Associated with the Farnesoid X Receptor or the Ileal Bile Acid Transporter, Regulates Bile Acid Activity in the Small Intestine.
M. Nakahara, N. Furuya, K. Takagaki, T. Sugaya, K. Hirota, A. Fukamizu, T. Kanda, H. Fujii, and R. Sato (2005)
J. Biol. Chem. 280, 42283-42289
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Cross-Talk between Farnesoid-X-Receptor (FXR) and Peroxisome Proliferator-Activated Receptor {gamma} Contributes to the Antifibrotic Activity of FXR Ligands in Rodent Models of Liver Cirrhosis.
S. Fiorucci, G. Rizzo, E. Antonelli, B. Renga, A. Mencarelli, L. Riccardi, A. Morelli, M. Pruzanski, and R. Pellicciari (2005)
J. Pharmacol. Exp. Ther. 315, 58-68
   Abstract »    Full Text »    PDF »
The Farnesoid X Receptor: A Molecular Link Between Bile Acid and Lipid and Glucose Metabolism.
T. Claudel, B. Staels, and F. Kuipers (2005)
Arterioscler Thromb Vasc Biol 25, 2020-2030
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Expression of the Pregnane X Receptor in Mice Antagonizes the Cholic Acid-Mediated Changes in Plasma Lipoprotein Profile.
D. Masson, L. Lagrost, A. Athias, P. Gambert, C. Brimer-Cline, L. Lan, J. D. Schuetz, E. G. Schuetz, and M. Assem (2005)
Arterioscler Thromb Vasc Biol 25, 2164-2169
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{alpha}-Crystallin Is a Target Gene of the Farnesoid X-activated Receptor in Human Livers.
F. Y. Lee, H. R. Kast-Woelbern, J. Chang, G. Luo, S. A. Jones, M. C. Fishbein, and P. A. Edwards (2005)
J. Biol. Chem. 280, 31792-31800
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The Farnesoid X Receptor Modulates Hepatic Carbohydrate Metabolism during the Fasting-Refeeding Transition.
D. Duran-Sandoval, B. Cariou, F. Percevault, N. Hennuyer, A. Grefhorst, T. H. van Dijk, F. J. Gonzalez, J.-C. Fruchart, F. Kuipers, and B. Staels (2005)
J. Biol. Chem. 280, 29971-29979
   Abstract »    Full Text »    PDF »
Retinoid X Receptor Heterodimers in the Metabolic Syndrome.
A. I. Shulman and D. J. Mangelsdorf (2005)
N. Engl. J. Med. 353, 604-615
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