FXR, a target for different diseases

Histology and Histopathology

Volumn 23, Issue 5, 2008, Pages 621-627

  Huang, Wendong ^a   Wang, Yan Dong ^a   Chen, Wei Dong ^a  

^a CITY OF HOPE NATIONAL MEDICAL CENTER   (United States)

Author keywords

Bile acid; FXR; Metabolism; Nuclear receptor

Indexed keywords

ANTIMETABOLITE; BILE ACID; CELL RECEPTOR; DNA BINDING PROTEIN; FARNESOID X RECEPTOR; FARNESOID X-ACTIVATED RECEPTOR; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG;

ANIMAL; GENE EXPRESSION REGULATION; GENETICS; HOMEOSTASIS; HUMAN; LIVER REGENERATION; LIVER TUMOR; METABOLIC DISORDER; METABOLISM; PHYSIOLOGY; RAT; REVIEW;

ANIMALS; ANTIMETABOLITES; BILE ACIDS AND SALTS; DNA-BINDING PROTEINS; GENE EXPRESSION REGULATION; HOMEOSTASIS; HUMANS; LIVER NEOPLASMS; LIVER REGENERATION; METABOLIC DISEASES; RATS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; TRANSCRIPTION FACTORS;

EID: 40349098552     PISSN: 02133911     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (50)

1. Ananthanarayanan M., Balasubramanian N., Makishima M., Mangelsdorf D.J. and Suchy F.J. (2001). Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor. J. Biol. Chem. 276, 28857-28865.
2. Anisfeld A.M., Kast-Woelbern H.R., Lee H., Zhang Y., Lee F.Y. and Edwards P.A. (2005). Activation of the nuclear receptor FXR induces fibrinogen expression: a new role for bile acid signaling. J. Lipid Res. 46, 458-468.
3. Anisfeld A.M., Kast-Woelbern H.R., Meyer M.E., Jones S.A., Zhang Y., Williams K.J., Willson T. and Edwards P.A. (2003). Syndecan-1 Expression Is Regulated in an Isoform-specific Manner by the Farnesoid-X Receptor. J. Biol. Chem. 278, 20420-20428.
4. Barbier O., Torra I.P., Sirvent A., Claudel T., Blanquart C., Duran-Sandoval D., Kuipers F., Kosykh V., Fruchart J.C. and Staels B. (2003). FXR induces the UGT2B4 enzyme in hepatocytes: a potential mechanism of negative feedback control of FXR activity. Gastroenterology 124, 1926-1940.
5. Boland L.L., Folsom A.R. and Rosamond W.D. (2002). Hyperinsulinemia, dyslipidemia, and obesity as risk factors for hospitalized gallbladder disease. A prospective study. Ann. Epidemiol. 12, 131-140.
6. Cariou B., van Harmelen K., Duran-Sandoval D., van Dijk T., Grefhorst A., Bouchaert E., Fruchart J.C., Gonzalez F.J., Kuipers F. and Staels B. (2005). Transient impairment of the adaptive response to fasting in FXR-deficient mice. FEBS Lett. 579, 4076-4080.
7. Cariou B., van Harmelen K., Duran-Sandoval D., van Dijk T.H., Grefhorst A., Abdelkarim M., Caron S., Torpier G., Fruchart J.C., Gonzalez F.J., Kuipers F. and Staels B. (2006). The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice. J. Biol. Chem. 281, 11039-11049.
8. Chawla A., Repa J.J., Evans R.M. and Mangelsdorf D.J. (2001). Nuclear receptors and lipid physiology: opening the X-files. Science 294, 1866-1870.
9. Claudel T., Sturm E., Duez H., Pineda Torra I., Sirvent A., Kosykh V., Fruchart J.C., Dallongeville J., Hum D.W., Kuipers F., Staels B. (2002). Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element. J. Clin. Invest. 109, 961-971.
10. De Fabiani E., Mitro N., Gilardi F., Caruso D., Galli G. and Crestani M. (2003). Coordinated control of cholesterol catabolism to bile acids and of gluconeogenesis via a novel mechanism of transcription regulation linked to the fastedto- fed cycle. J. Biol. Chem. 278, 39124-39132.
11. Duran-Sandoval D., Mautino G., Martin G., Percevault F., Barbier O., Fruchart J.C., Kuipers F. and Staels B. (2004). Glucose regulates the expression of the farnesoid X receptor in liver. Diabetes 53, 890-898.
12. Edwards P.A., Kast H.R. and Anisfeld A.M. (2002). BAREing it all: the adoption of LXR and FXR and their roles in lipid homeostasis. J. Lipid Res. 43, 2-12.
13. Fiorucci S., Clerici C., Antonelli E., Orlandi S., Goodwin B., Sadeghpour B.M., Sabatino G., Russo G., Castellani D., Willson T.M., Pruzanski M., Pellicciari R. and Morelli A. (2005). Protective Effects of 6-Ethyl Chenodeoxycholic Acid, a Farnesoid X Receptor Ligand, in Estrogen-Induced Cholestasis. J. Pharmacol. Exp. Ther. 313, 604-612.
14. 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., Evans R.M. and Weinberger C. (1995). Identification of a nuclear receptor that is activated by farnesol metabolites. Cell 81, 687-693.
15. Glass C.K. (1994). Differential recognition of target genes by nuclear receptor monomers, dimers, and heterodimers. Endocr. Rev. 15, 391-407.
16. 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, Maloney P.R., Willson T.M. and Kliewer S.A. (2000). A Regulatory Cascade of the Nuclear Receptors FXR, SHP-1, and LRH-1 Represses Bile Acid Biosynthesis. Mol. Cell 6, 517-526.
17. Grober J., Zaghini I., Fujii H., Jones S.A., Kliewer S.A., Willson T.M., Ono T. and Besnard P. (1999). Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene. Involvement of the farnesoid X receptor/9-cis-retinoic acid receptor heterodimer. J. Biol. Chem. 274, 29749-29754.
18. Huang L., Zhao A., Lew J.-L., Zhang T., Hrywna Y., Thompson J.R., de Pedro N., Royo I., Blevins R.A., Peláez F., Wright S.D. and Cui J. (2003). Farnesoid X Receptor Activates Transcription of the Phospholipid Pump MDR3. J. Biol. Chem. 278, 51085-51090.
19. Huang W., Ma K., Zhang J., Qatanani M., Cuvillier J., Liu J., Dong B., Huang X. and Moore D.D. (2006). Nuclear receptor-dependent bile acid signaling is required for normal liver regeneration. Science 312, 233-236.
20. Hubbert M.L., Zhang Y., Lee F.Y. and Edwards P.A. (2007). Regulation of hepatic insig-2 by the farnesoid X-receptor. Mol. Endocrinol. 21, 1359-1369.
21. Huber R.M., Murphy K., Miao B., Link J.R., Cunningham M.R., Rupar M.J., Gunyuzlu P.L., Haws T. F., Kassam A., Powell F., Hollis G.F., Young P.R., Mukherjee R. and Burn T.C. (2002). Generation of multiple farnesoid-X-receptor isoforms through the use of alternative promoters. Gene 290, 35-43.
22. Jung D., Mangelsdorf D.J. and Meyer U.A. (2006). PXR is a target of FXR. J. Biol. Chem. 281, 19081-19091.
23. Jung D., Podvinec M., Meyer U.A., Mangelsdorf D.J., Fried M., Meier P.J. and Kullak-Ublick G.A. (2002). Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor. Gastroenterology 122, 1954-1966.
24. Kast H.R., Goodwin B., Tarr P.T., Jones S.A., Anisfeld A.M., Stoltz C.M., Tontonoz P., Kliewer S., Willson T.M. and Edwards P.A. (2002). Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor. J. Biol. Chem. 277, 2908-2915.
25. Laffitte B.A., Kast H.R., Nguyen C.M., Zavacki A.M., Moore D.D. and Edwards P.A. (2000). Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor. J. Biol. Chem. 275, 10638-10647.
26. Lee H., Zhang Y., Lee F.Y., Nelson S.F., Gonzalez F.J. and Edwards P.A. (2006). FXR regulates organic solute transporters · and ' in the adrenal gland, kidney, and intestine. J. Lipid Res. 47, 201-214.
27. Li H., Chen F., Shang Q., Pan L., Shneider B.L., Chiang J.Y.L., Forman B.M., Ananthanarayanan M., Tint G.S., Salen G. and Xu G. (2005). FXR-activating ligands inhibit rabbit ASBT expression via FXR-SHP-FTF cascade. Am. J. Physiol. Gastrointest Liver Physiol. 288, G60-G66.
28. Li J., Pircher P.C., Schulman I.G. and Westin S.K. (2005). Regulation of Complement C3 Expression by the Bile Acid Receptor FXR. J. Biol. Chem. 280, 7427-7434.
29. Liu Y., Binz J., Numerick M.J., Dennis S., Luo G., Desai B., MacKenzie K.I., Mansfield T.A., Kliewer S.A., Goodwin B. and Jones S.A. (2003). Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 112:1678-87.
30. Ma K., Saha P.K., Chan L. and Moore D.D. (2006). Farnesoid X receptor is essential for normal glucose homeostasis. J. Clin. Invest. 116, 1102-1109.
31. Makishima M., Okamoto A.Y., Repa J.J., Tu H., Learned R.M., Luk A., Hull M.V., Lustig K.D., Mangelsdorf D.J. and Shan B. (1999). Identification of a Nuclear Receptor for Bile Acids. Science 284, 1362-1365.
32. Mangelsdorf D.J., Thummel C., Beato M., Herrlich P., Schutz G., Umesono K., Blumberg B., Kastner P., Mark M., Chambon P. and Evans R.M. (1995). The nuclear receptor superfamily: the second decade. Cell 83, 835-839.
33. Miyata M., Tozawa A., Otsuka H., Nakamura T., Nagata K., Gonzalez F.J. and Yamazoe Y. (2005). Role of Farnesoid X Receptor in the Enhancement of Canalicular Bile Acid Output and Excretion of Unconjugated Bile Acids: A Mechanism for Protection against Cholic Acid-Induced Liver Toxicity. J. Pharmacol. Exp. Ther. 312, 759-766.
34. Moschetta A., Bookout A.L. and Mangelsdorf D.J. (2004). Prevention of cholesterol gallstone disease by FXR agonists in a mouse model. Nat. Med. 10, 1352-1358.
35. 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. and Lehmann J.M. (1999). Bile acids: Natural ligands for an orphan nuclear receptor. Science 284, 1365-1368.
36. Pircher P.C., Kitto J.L., Petrowski M.L., Tangirala R.K., Bischoff E.D., Schulman I.G. and Westin S.K. (2003). Farnesoid X Receptor Regulates Bile Acid-Amino Acid Conjugation. J. Biol. Chem. 278, 27703-27711.
37. Russell D.W. (2003). The enzymes, regulation, and genetics of bile acid synthesis. Annu. Rev. Biochem. 72, 137-174.
38. Sinal C.J., Tohkin M., Miyata M., Ward J.M., Lambert G. and Gonzalez F.J. (2000). Links Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 102, 731-744.
39. Sirvent A., Claudel T., Martin G., Brozek J., Kosykh V., Darteil R., Hum D., Fruchart J. and Staels B. (2004a). The farnesoid X receptor induces very low density lipoprotein receptor gene expression. FEBS Lett. 566, 173-177.
40. Sirvent A., Verhoeven A.J.M., Jansen H., Kosykh V., Darteil R.J., Hum D.W., Fruchart J.-C. and Staels B. (2004b). Farnesoid X receptor represses hepatic lipase gene expression. J. Lipid Res. 45, 2110-2115.
41. Song C.S., Echchgadda I., Baek B.-S., Ahn S.C., Oh T., Roy A.K. and Chatterjee B. (2001). Dehydroepiandrosterone Sulfotransferase Gene Induction by Bile Acid Activated Farnesoid X Receptor. J. Biol.Chem. 276, 42549-42556.
42. Stayrook K.R., Bramlett K.S., Savkur R.S., Ficorilli J., Cook T., Christe M.E., Michael L.F. and Burris T.P. (2005). Regulation of Carbohydrate Metabolism by the Farnesoid X Receptor. Endocrinology 146, 984-991.
43. Trauner M., Meier P.J. and Boyer J.L. (1998). Molecular pathogenesis of cholestasis. N. Engl. J. Med. 339, 1217-1227.
44. Ueno Y., Moriyama M., Uchida T. and Arakawa Y. (2001) Irregular regeneration of hepatocytes is an important factor in the hepatocarcinogenesis of liver disease. Hepatology 33, 357-362.
45. Urizar N.L., Dowhan D.H. and Moore D.D. (2000). The farnesoid X-activated receptor mediates bile acid activation of phospholipid transfer protein gene expression. J. Biol. Chem. 275, 39313-39317.
46. Watanabe M., Houten S.M., Wang L., Moschetta A., Mangelsdorf D.J., Heyman R.A., Moore D.D. and Auwerx J. (2004). Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. J. Clin. Invest. 113, 1408-1418.
47. Yang F., Huang X., Yi T., Yen Y., Moore D.D., Huang W. (2007). Spontaneous development of liver tumors in the absence of the bile acid receptor farnesoid X receptor. Cancer Res. 67, 863-867.
48. Zhang Y., Castellani L.W., Sinal C.J., Gonzalez F.J. and Edwards P.A. (2004). Peroxisome proliferator-activated receptor-γ coactivator 1a (PGC-1a) regulates triglyceride metabolism by activation of the nuclear receptor FXR. Genes Dev. 18, 157-169.
49. Zhang Y., Kast-Woelbern H.R. and Edwards P.A. (2003). Natural structural variants of the nuclear receptor farnesoid X receptor affect transcriptional activation. J. Biol. Chem. 278, 104-110.
50. Zhang Y., Lee F.Y., Barrera G., Lee H., Vales C., Gonzalez F.J., Willson T.M. and Edwards P.A. (2006). Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc. Natl. Acad. Sci. USA 103, 1006-1011.