Bile acids and their receptors

Molecular Aspects of Medicine

Volumn 56, Issue , 2017, Pages 2-9

  Martinot, Emmanuelle ^a,b,c,d   Sèdes, Lauriane ^a,b,c,d   Baptissart, Marine ^a,b,c,d   Lobaccaro, Jean Marc ^a,b,c,d   Caira, Françoise ^a,b,c,d   Beaudoin, Claude ^a,b,c,d   Volle, David H ^a,b,c,d  

^a Faculté de Médecine   (France)

^b Lab des Adaptations Metaboliques a l'Exercice en Conditions Physiologiques et Pathologiques   (France)

^c CNRS   (France)

^d CRNH AUVERGNE   (France)

Author keywords

Bile acid; Homeostasis; Intestine; Liver; Receptors

Indexed keywords

BILE ACID; FARNESOID X RECEPTOR; G PROTEIN COUPLED RECEPTOR; GLUCOSE; RECEPTOR; STEROID; TRIACYLGLYCEROL; CELL RECEPTOR; CHOLESTEROL; FARNESOID X-ACTIVATED RECEPTOR; GPBAR1 PROTEIN, HUMAN;

BILE ACID METABOLISM; BILE ACID SYNTHESIS; BIOTRANSFORMATION; ENERGY METABOLISM; ENTEROHEPATIC CIRCULATION; ENZYME POLYMORPHISM; GLUCOSE METABOLISM; HUMAN; INFLAMMATION; INTESTINE; LIVER; MALIGNANT NEOPLASM; NONHUMAN; PATHOPHYSIOLOGY; REVIEW; TGR5 GENE; ANIMAL; CYTOLOGY; GENE EXPRESSION REGULATION; GENETIC POLYMORPHISM; GENETICS; HOMEOSTASIS; INTESTINE FLORA; LIVER TUMOR; METABOLISM; MICROBIOLOGY; PATHOLOGY; PHYSIOLOGY; SIGNAL TRANSDUCTION;

ANIMALS; BILE ACIDS AND SALTS; BIOTRANSFORMATION; CHOLESTEROL; GASTROINTESTINAL MICROBIOME; GENE EXPRESSION REGULATION, NEOPLASTIC; HOMEOSTASIS; HUMANS; INTESTINES; LIVER; LIVER NEOPLASMS; POLYMORPHISM, GENETIC; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION;

EID: 85011307870     PISSN: 00982997     EISSN: 18729452     Source Type: Journal    
DOI: 10.1016/j.mam.2017.01.006     Document Type: Review

References (109)

1. Ananthanarayanan, M., Balasubramanian, N., Makishima, M., Mangelsdorf, D.J., Suchy, F.J., Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor. J. Biol. Chem. 276 (2001), 28857–28865, 10.1074/jbc.M011610200.
2. Andersén, E., Hellström, P., Hellström, K., Cholesterol biosynthesis in nonketotic diabetics before and during insulin therapy. Diabetes Res. Clin. Pract. 3 (1987), 207–214.
3. Andersén, E., Karlaganis, G., Sjövall, J., Altered bile acid profiles in duodenal bile and urine in diabetic subjects. Eur. J. Clin. Invest. 18 (1988), 166–172.
4. Angelin, B., Einarsson, K., Hellström, K., Leijd, B., Effects of cholestyramine and chenodeoxycholic acid on the metabolism of endogenous triglyceride in hyperlipoproteinemia. J. Lipid Res. 19 (1978), 1017–1024.
5. Armstrong, C.P., Dixon, J.M., Taylor, T.V., Davies, G.C., Surgical experience of deeply jaundiced patients with bile duct obstruction. Br. J. Surg. 71 (1984), 234–238.
6. Baptissart, M., Martinot, E., Vega, A., Sédes, L., Rouaisnel, B., de Haze, A., Baron, S., Schoonjans, K., Caira, F., Volle, D.H., Bile acid-FXRα pathways regulate male sexual maturation in mice. Oncotarget 7 (2016), 19468–19482, 10.18632/oncotarget.7153.
7. Barbier, O., Torra, I.P., Sirvent, A., Claudel, T., Blanquart, C., Duran-Sandoval, D., Kuipers, F., Kosykh, V., Fruchart, J.-C., Staels, B., FXR induces the UGT2B4 enzyme in hepatocytes: a potential mechanism of negative feedback control of FXR activity. Gastroenterology 124 (2003), 1926–1940.
8. Bateson, M.C., Maclean, D., Evans, J.R., Bouchier, I.A., Chenodeoxycholic acid therapy for hypertriglyceridaemia in men. Br. J. Clin. Pharmacol. 5 (1978), 249–254.
9. Beil, U., Crouse, J.R., Einarsson, K., Grundy, S.M., Effects of interruption of the enterohepatic circulation of bile acids on the transport of very low density-lipoprotein triglycerides. Metabolism 31 (1982), 438–444.
10. Betteridge, D.J., Bhatnager, D., Bing, R.F., Durrington, P.N., Evans, G.R., Flax, H., Jay, R.H., Lewis-Barned, N., Mann, J., Matthews, D.R., Treatment of familial hypercholesterolaemia. United Kingdom lipid clinics study of pravastatin and cholestyramine. Br. Med. J. 304 (1992), 1335–1338.
11. Bianco, A.C., Salvatore, D., Gereben, B., Berry, M.J., Larsen, P.R., Biochemistry, cellular and molecular biology, and physiological roles of the iodothyronine selenodeiodinases. Endocr. Rev. 23 (2002), 38–89, 10.1210/edrv.23.1.0455.
12. Boland, L.L., Folsom, A.R., Rosamond, W.D., Atherosclerosis risk in communities (ARIC) study investigators. Hyperinsulinemia, dyslipidemia, and obesity as risk factors for hospitalized gallbladder disease. A prospective study. Ann. Epidemiol. 12 (2002), 131–140.
13. Buchwald, H., Varco, R.L., Matts, J.P., Long, J.M., Fitch, L.L., Campbell, G.S., Pearce, M.B., Yellin, A.E., Edmiston, W.A., Smink, R.D., Effect of partial ileal bypass surgery on mortality and morbidity from coronary heart disease in patients with hypercholesterolemia. Report of the Program on the Surgical Control of the Hyperlipidemias (POSCH). N. Engl. J. Med. 323 (1990), 946–955, 10.1056/NEJM199010043231404.
14. Cainzos, M., Potel, J., Puente, J.L., Anergy in jaundiced patients. Br. J. Surg. 75 (1988), 147–149.
15. Calmus, Y., Guechot, J., Podevin, P., Bonnefis, M.T., Giboudeau, J., Poupon, R., Differential effects of chenodeoxycholic and ursodeoxycholic acids on interleukin 1, interleukin 6 and tumor necrosis factor-alpha production by monocytes. Hepatol. Balt. Md 16 (1992), 719–723.
16. Cameron, R.G., Imaida, K., Tsuda, H., Ito, N., Promotive effects of steroids and bile acids on hepatocarcinogenesis initiated by diethylnitrosamine. Cancer Res. 42 (1982), 2426–2428.
17. Carter, B.A., Taylor, O.A., Prendergast, D.R., Zimmerman, T.L., Von Furstenberg, R., Moore, D.D., Karpen, S.J., Stigmasterol, a soy lipid-derived phytosterol, is an antagonist of the bile acid nuclear receptor FXR. Pediatr. Res. 62 (2007), 301–306, 10.1203/PDR.0b013e3181256492.
18. Carulli, N., Ponz de Leon, M., Podda, M., Zuin, M., Strata, A., Frigerio, G., Digrisolo, A., Chenodeoxycholic acid and ursodeoxycholic acid effects in endogenous hypertriglyceridemias. A controlled double-blind trial. J. Clin. Pharmacol. 21 (1981), 436–442.
19. Catalano, S., Malivindi, R., Giordano, C., Gu, G., Panza, S., Bonofiglio, D., Lanzino, M., Sisci, D., Panno, M.L., Andò, S., Farnesoid X receptor, through the binding with steroidogenic factor 1-responsive element, inhibits aromatase expression in tumor Leydig cells. J. Biol. Chem. 285 (2010), 5581–5593, 10.1074/jbc.M109.052670.
20. Cipriani, S., Mencarelli, A., Chini, M.G., Distrutti, E., Renga, B., Bifulco, G., Baldelli, F., Donini, A., Fiorucci, S., The bile acid receptor GPBAR-1 (TGR5) modulates integrity of intestinal barrier and immune response to experimental colitis. PloS One, 6, 2011, e25637, 10.1371/journal.pone.0025637.
21. Claudel, T., Inoue, Y., Barbier, O., Duran-Sandoval, D., Kosykh, V., Fruchart, J., Fruchart, J.-C., Gonzalez, F.J., Staels, B., Farnesoid X receptor agonists suppress hepatic apolipoprotein CIII expression. Gastroenterology 125 (2003), 544–555.
22. Claudel, T., Sturm, E., Duez, H., Torra, I.P., Sirvent, A., Kosykh, V., Fruchart, J.-C., Dallongeville, J., Hum, D.W., Kuipers, F., Staels, B., Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element. J. Clin. Invest. 109 (2002), 961–971, 10.1172/JCI14505.
23. de Aguiar Vallim, T.Q., Tarling, E.J., Ahn, H., Hagey, L.R., Romanoski, C.E., Lee, R.G., Graham, M.J., Motohashi, H., Yamamoto, M., Edwards, P.A., MAFG is a transcriptional repressor of bile acid synthesis and metabolism. Cell Metab. 21 (2015), 298–310, 10.1016/j.cmet.2015.01.007.
24. De Fabiani, E., Mitro, N., Gilardi, F., Caruso, D., Galli, G., Crestani, M., Coordinated control of cholesterol catabolism to bile acids and of gluconeogenesis via a novel mechanism of transcription regulation linked to the fasted-to-fed cycle. J. Biol. Chem. 278 (2003), 39124–39132, 10.1074/jbc.M305079200.
25. De Santis, A., Attili, A.F., Ginanni Corradini, S., Scafato, E., Cantagalli, A., De Luca, C., Pinto, G., Lisi, D., Capocaccia, L., Gallstones and diabetes: a case-control study in a free-living population sample. Hepatol. Balt. Md 25 (1997), 787–790, 10.1002/hep.510250401.
26. Degirolamo, C., Modica, S., Vacca, M., Di Tullio, G., Morgano, A., D'Orazio, A., Kannisto, K., Parini, P., Moschetta, A., Prevention of spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice by intestinal-specific farnesoid X receptor reactivation. Hepatol. Balt. Md 61 (2015), 161–170, 10.1002/hep.27274.
27. Denson, L.A., Sturm, E., Echevarria, W., Zimmerman, T.L., Makishima, M., Mangelsdorf, D.J., Karpen, S.J., The orphan nuclear receptor, shp, mediates bile acid-induced inhibition of the rat bile acid transporter, ntcp. Gastroenterology 121 (2001), 140–147.
28. Drivas, G., James, O., Wardle, N., Study of reticuloendothelial phagocytic capacity in patients with cholestasis. Br. Med. J. 1 (1976), 1568–1569.
29. Duran-Sandoval, D., Mautino, G., Martin, G., Percevault, F., Barbier, O., Fruchart, J.-C., Kuipers, F., Staels, B., Glucose regulates the expression of the farnesoid X receptor in liver. Diabetes 53 (2004), 890–898.
30. 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., Weinberger, C., Identification of a nuclear receptor that is activated by farnesol metabolites. Cell 81 (1995), 687–693.
31. Funaoka, M., Komatsu, M., Toyoshima, I., Mikami, K., Ono, T., Hoshino, T., Kato, J., Kuramitsu, T., Ishii, T., Masamune, O., Tauroursodeoxycholic acid enhances phagocytosis of the cultured rat Kupffer cell. J. Gastroenterol. Hepatol. 14 (1999), 652–658.
32. 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., Penna, G., Laverny, G., Adorini, L., Moschetta, A., van Mil, S.W.C., Farnesoid X receptor activation inhibits inflammation and preserves the intestinal barrier in inflammatory bowel disease. Gut 60 (2011), 463–472, 10.1136/gut.2010.212159.
33. Gnerre, C., Blättler, S., Kaufmann, M.R., Looser, R., Meyer, U.A., Regulation of CYP3A4 by the bile acid receptor FXR: evidence for functional binding sites in the CYP3A4 gene. Pharmacogenetics 14 (2004), 635–645.
34. Gomez-Ospina, N., Potter, C.J., Xiao, R., Manickam, K., Kim, M.-S., Kim, K.H., Shneider, B.L., Picarsic, J.L., Jacobson, T.A., Zhang, J., He, W., Liu, P., Knisely, A.S., Finegold, M.J., Muzny, D.M., Boerwinkle, E., Lupski, J.R., Plon, S.E., Gibbs, R.A., Eng, C.M., Yang, Y., Washington, G.C., Porteus, M.H., Berquist, W.E., Kambham, N., Singh, R.J., Xia, F., Enns, G.M., Moore, D.D., Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis. Nat. Commun., 7, 2016, 10713, 10.1038/ncomms10713.
35. 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., Kliewer, S.A., A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol. Cell 6 (2000), 517–526.
36. Grober, J., Zaghini, I., Fujii, H., Jones, S.A., Kliewer, S.A., Willson, T.M., Ono, T., Besnard, P., 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 (1999), 29749–29754.
37. Guo, C., Qi, H., Yu, Y., Zhang, Q., Su, J., Yu, D., Huang, W., Chen, W.-D., Wang, Y.-D., The G-protein-coupled bile acid receptor Gpbar1 (TGR5) inhibits gastric inflammation through antagonizing NF-κB signaling pathway. Front. Pharmacol., 6, 2015, 287, 10.3389/fphar.2015.00287.
38. Halpern, B.N., Biozzi, G., Nicol, T., Bilbey, D.L., Effect of experimental biliary obstruction on the phagocytic activity of the reticulo-endothelial system. Nature 180 (1957), 503–504.
39. Higashiyama, H., Kinoshita, M., Asano, S., Immunolocalization of farnesoid X receptor (FXR) in mouse tissues using tissue microarray. Acta histochem. 110 (2008), 86–93, 10.1016/j.acthis.2007.08.001.
40. Hill, M.J., Bile flow and colon cancer. Mutat. Res. 238 (1990), 313–320.
41. Hoekstra, M., van der Sluis, R.J., Li, Z., Oosterveer, M.H., Groen, A.K., Van Berkel, T.J.C., FXR agonist GW4064 increases plasma glucocorticoid levels in C57BL/6 mice. Mol. Cell. Endocrinol. 362 (2012), 69–75, 10.1016/j.mce.2012.05.010.
42. Holt, J.A., Luo, G., Billin, A.N., Bisi, J., McNeill, Y.Y., Kozarsky, K.F., Donahee, M., Wang, D.Y., Mansfield, T.A., Kliewer, S.A., Goodwin, B., Jones, S.A., Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesis. Genes Dev. 17 (2003), 1581–1591, 10.1101/gad.1083503.
43. Hov, J.R., Keitel, V., Laerdahl, J.K., Spomer, L., Ellinghaus, E., ElSharawy, A., Melum, E., Boberg, K.M., Manke, T., Balschun, T., Schramm, C., Bergquist, A., Weismüller, T., Gotthardt, D., Rust, C., Henckaerts, L., Onnie, C.M., Weersma, R.K., Sterneck, M., Teufel, A., Runz, H., Stiehl, A., Ponsioen, C.Y., Wijmenga, C., Vatn, M.H. IBSEN Study Group, Stokkers, P.C.F., Vermeire, S., Mathew, C.G., Lie, B.A., Beuers, U., Manns, M.P., Schreiber, S., Schrumpf, E., Häussinger, D., Franke, A., Karlsen, T.H., Mutational characterization of the bile acid receptor TGR5 in primary sclerosing cholangitis. PloS One, 5, 2010, e12403, 10.1371/journal.pone.0012403.
44. Inagaki, T., Choi, M., Moschetta, A., Peng, L., Cummins, C.L., McDonald, J.G., Luo, G., Jones, S.A., Goodwin, B., Richardson, J.A., Gerard, R.D., Repa, J.J., Mangelsdorf, D.J., Kliewer, S.A., Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis. Cell Metab. 2 (2005), 217–225, 10.1016/j.cmet.2005.09.001.
45. Ishibashi, S., Schwarz, M., Frykman, P.K., Herz, J., Russell, D.W., Disruption of cholesterol 7alpha-hydroxylase gene in mice. I. Postnatal lethality reversed by bile acid and vitamin supplementation. J. Biol. Chem. 271 (1996), 18017–18023.
46. Ito, S., Fujimori, T., Furuya, A., Satoh, J., Nabeshima, Y., Nabeshima, Y.-I., Impaired negative feedback suppression of bile acid synthesis in mice lacking betaKlotho. J. Clin. Invest. 115 (2005), 2202–2208, 10.1172/JCI23076.
47. Kardassis, D., Roussou, A., Papakosta, P., Boulias, K., Talianidis, I., Zannis, V.I., Synergism between nuclear receptors bound to specific hormone response elements of the hepatic control region-1 and the proximal apolipoprotein C-II promoter mediate apolipoprotein C-II gene regulation by bile acids and retinoids. Biochem. J. 372 (2003), 291–304, 10.1042/BJ20021532.
48. Kast, H.R., Nguyen, C.M., Sinal, C.J., Jones, S.A., Laffitte, B.A., Reue, K., Gonzalez, F.J., Willson, T.M., Edwards, P.A., Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids. Mol. Endocrinol. Balt. Md 15 (2001), 1720–1728, 10.1210/mend.15.10.0712.
49. Kawamata, Y., Fujii, R., Hosoya, M., Harada, M., Yoshida, H., Miwa, M., Fukusumi, S., Habata, Y., Itoh, T., Shintani, Y., Hinuma, S., Fujisawa, Y., Fujino, M., A G protein-coupled receptor responsive to bile acids. J. Biol. Chem. 278 (2003), 9435–9440, 10.1074/jbc.M209706200.
50. Keitel, V., Donner, M., Winandy, S., Kubitz, R., Häussinger, D., Expression and function of the bile acid receptor TGR5 in Kupffer cells. Biochem. Biophys. Res. Commun. 372 (2008), 78–84, 10.1016/j.bbrc.2008.04.171.
51. Kim, I., Morimura, K., Shah, Y., Yang, Q., Ward, J.M., Gonzalez, F.J., Spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice. Carcinogenesis 28 (2007), 940–946, 10.1093/carcin/bgl249.
52. Kitazawa, S., Studies on initiating activity of secondary bile acids for rat hepatocarcinogenesis. Hokkaido Igaku Zasshi 68 (1993), 110–120.
53. Knisely, A.S., Strautnieks, S.S., Meier, Y., Stieger, B., Byrne, J.A., Portmann, B.C., Bull, L.N., Pawlikowska, L., Bilezikçi, B., Ozçay, F., László, A., Tiszlavicz, L., Moore, L., Raftos, J., Arnell, H., Fischler, B., Németh, A., Papadogiannakis, N., Cielecka-Kuszyk, J., Jankowska, I., Pawłowska, J., Melín-Aldana, H., Emerick, K.M., Whitington, P.F., Mieli-Vergani, G., Thompson, R.J., Hepatocellular carcinoma in ten children under five years of age with bile salt export pump deficiency. Hepatol. Balt. Md 44 (2006), 478–486, 10.1002/hep.21287.
54. Kong, B., Wang, L., Chiang, J.Y.L., Zhang, Y., Klaassen, C.D., Guo, G.L., Mechanism of tissue-specific farnesoid X receptor in suppressing the expression of genes in bile-acid synthesis in mice. Hepatol. Balt. Md 56 (2012), 1034–1043, 10.1002/hep.25740.
55. Laffitte, B.A., Kast, H.R., Nguyen, C.M., Zavacki, A.M., Moore, D.D., Edwards, P.A., Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor. J. Biol. Chem. 275 (2000), 10638–10647.
56. Leiss, O., von Bergmann, K., Different effects of chenodeoxycholic acid and ursodeoxycholic acid on serum lipoprotein concentrations in patients with radiolucent gallstones. Scand. J. Gastroenterol. 17 (1982), 587–592, 10.3109/00365528209181063.
57. Lu, T.T., Makishima, M., Repa, J.J., Schoonjans, K., Kerr, T.A., Auwerx, J., Mangelsdorf, D.J., Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol. Cell 6 (2000), 507–515.
58. Lu, Y., Heydel, J.-M., Li, X., Bratton, S., Lindblom, T., Radominska-Pandya, A., Lithocholic acid decreases expression of UGT2B7 in Caco-2 cells: a potential role for a negative farnesoid X receptor response element. Drug Metab. Dispos. Biol. Fate Chem. 33 (2005), 937–946, 10.1124/dmd.104.003061.
59. Ma, K., Saha, P.K., Chan, L., Moore, D.D., Farnesoid X receptor is essential for normal glucose homeostasis. J. Clin. Invest. 116 (2006), 1102–1109, 10.1172/JCI25604.
60. 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., Identification of a nuclear receptor for bile acids. Science 284 (1999), 1362–1365.
61. Maloney, P.R., Parks, D.J., Haffner, C.D., Fivush, A.M., Chandra, G., Plunket, K.D., Creech, K.L., Moore, L.B., Wilson, J.G., Lewis, M.C., Jones, S.A., Willson, T.M., Identification of a chemical tool for the orphan nuclear receptor FXR. J. Med. Chem. 43 (2000), 2971–2974.
62. Maran, R.R.M., Thomas, A., Roth, M., Sheng, Z., Esterly, N., Pinson, D., Gao, X., Zhang, Y., Ganapathy, V., Gonzalez, F.J., Guo, G.L., Farnesoid X receptor deficiency in mice leads to increased intestinal epithelial cell proliferation and tumor development. J. Pharmacol. Exp. Ther. 328 (2009), 469–477, 10.1124/jpet.108.145409.
63. Maruyama, T., Miyamoto, Y., Nakamura, T., Tamai, Y., Okada, H., Sugiyama, E., Nakamura, T., Itadani, H., Tanaka, K., Identification of membrane-type receptor for bile acids (M-BAR). Biochem. Biophys. Res. Commun. 298 (2002), 714–719.
64. Maruyama, T., Tanaka, K., Suzuki, J., Miyoshi, H., Harada, N., Nakamura, T., Miyamoto, Y., Kanatani, A., Tamai, Y., Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice. J. Endocrinol. 191 (2006), 197–205, 10.1677/joe.1.06546.
65. Marzolini, C., Tirona, R.G., Gervasini, G., Poonkuzhali, B., Assem, M., Lee, W., Leake, B.F., Schuetz, J.D., Schuetz, E.G., Kim, R.B., A common polymorphism in the bile acid receptor farnesoid X receptor is associated with decreased hepatic target gene expression. Mol. Endocrinol. Balt. Md 21 (2007), 1769–1780, 10.1210/me.2007-0025.
66. Meyer-Gerspach, A.C., Steinert, R.E., Keller, S., Malarski, A., Schulte, F.H., Beglinger, C., Effects of chenodeoxycholic acid on the secretion of gut peptides and fibroblast growth factors in healthy humans. J. Clin. Endocrinol. Metab. 98 (2013), 3351–3358, 10.1210/jc.2012-4109.
67. Minter, R.M., Fan, M.-H., Sun, J., Niederbichler, A., Ipaktchi, K., Arbabi, S., Hemmila, M.R., Remick, D.G., Wang, S.C., Su, G.L., Altered Kupffer cell function in biliary obstruction. Surgery 138 (2005), 236–245, 10.1016/j.surg.2005.04.001.
68. Mölgaard, J., von Schenck, H., Olsson, A.G., Comparative effects of simvastatin and cholestyramine in treatment of patients with hypercholesterolaemia. Eur. J. Clin. Pharmacol. 36 (1989), 455–460.
69. Myant, N.B., Mitropoulos, K.A., Cholesterol 7 alpha-hydroxylase. J. Lipid Res. 18 (1977), 135–153.
70. Owsley, E., Chiang, J.Y.L., Guggulsterone antagonizes farnesoid X receptor induction of bile salt export pump but activates pregnane X receptor to inhibit cholesterol 7alpha-hydroxylase gene. Biochem. Biophys. Res. Commun. 304 (2003), 191–195.
71. 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., Bile acids: natural ligands for an orphan nuclear receptor. Science 284 (1999), 1365–1368.
72. Patti, M.-E., Houten, S.M., Bianco, A.C., Bernier, R., Larsen, P.R., Holst, J.J., Badman, M.K., Maratos-Flier, E., Mun, E.C., Pihlajamaki, J., Auwerx, J., Goldfine, A.B., Serum bile acids are higher in humans with prior gastric bypass: potential contribution to improved glucose and lipid metabolism. Obes. Silver Spring Md 17 (2009), 1671–1677, 10.1038/oby.2009.102.
73. Pellicciari, R., Gioiello, A., Macchiarulo, A., Thomas, C., Rosatelli, E., Natalini, B., Sardella, R., Pruzanski, M., Roda, A., Pastorini, E., Schoonjans, K., Auwerx, J., Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J. Med. Chem. 52 (2009), 7958–7961, 10.1021/jm901390p.
74. Pircher, P.C., Kitto, J.L., Petrowski, M.L., Tangirala, R.K., Bischoff, E.D., Schulman, I.G., Westin, S.K., Farnesoid X receptor regulates bile acid-amino acid conjugation. J. Biol. Chem. 278 (2003), 27703–27711, 10.1074/jbc.M302128200.
75. Potthoff, M.J., Potts, A., He, T., Duarte, J.A.G., Taussig, R., Mangelsdorf, D.J., Kliewer, S.A., Burgess, S.C., Colesevelam suppresses hepatic glycogenolysis by TGR5-mediated induction of GLP-1 action in DIO mice. Am. J. Physiol. Gastrointest. Liver Physiol. 304 (2013), G371–G380, 10.1152/ajpgi.00400.2012.
76. Prieur, X., Coste, H., Rodriguez, J.C., The human apolipoprotein AV gene is regulated by peroxisome proliferator-activated receptor-alpha and contains a novel farnesoid X-activated receptor response element. J. Biol. Chem. 278 (2003), 25468–25480, 10.1074/jbc.M301302200.
77. Pullinger, C.R., Eng, C., Salen, G., Shefer, S., Batta, A.K., Erickson, S.K., Verhagen, A., Rivera, C.R., Mulvihill, S.J., Malloy, M.J., Kane, J.P., Human cholesterol 7alpha-hydroxylase (CYP7A1) deficiency has a hypercholesterolemic phenotype. J. Clin. Invest. 110 (2002), 109–117, 10.1172/JCI15387.
78. Ramadori, G., Armbrust, T., Cytokines in the liver. Eur. J. Gastroenterol. Hepatol. 13 (2001), 777–784.
79. Ricketts, M.-L., Boekschoten, M.V., Kreeft, A.J., Hooiveld, G.J.E.J., Moen, C.J.A., Müller, M., Frants, R.R., Kasanmoentalib, S., Post, S.M., Princen, H.M.G., Porter, J.G., Katan, M.B., Hofker, M.H., Moore, D.D., The cholesterol-raising factor from coffee beans, cafestol, as an agonist ligand for the farnesoid and pregnane X receptors. Mol. Endocrinol. Balt. Md 21 (2007), 1603–1616, 10.1210/me.2007-0133.
80. Rogler, G., Brand, K., Vogl, D., Page, S., Hofmeister, R., Andus, T., Knuechel, R., Baeuerle, P.A., Schölmerich, J., Gross, V., Nuclear factor kappaB is activated in macrophages and epithelial cells of inflamed intestinal mucosa. Gastroenterology 115 (1998), 357–369.
81. Roughneen, P.T., Drath, D.B., Kulkarni, A.D., Rowlands, B.J., Impaired nonspecific cellular immunity in experimental cholestasis. Ann. Surg. 206 (1987), 578–582.
82. Ruhl, C.E., Everhart, J.E., Association of diabetes, serum insulin, and C-peptide with gallbladder disease. Hepatol. Balt. Md 31 (2000), 299–303, 10.1002/hep.510310206.
83. Sanz, E., Evanoff, R., Quintana, A., Evans, E., Miller, J.A., Ko, C., Amieux, P.S., Griswold, M.D., McKnight, G.S., RiboTag analysis of actively translated mRNAs in Sertoli and Leydig cells in vivo. PloS One, 8, 2013, e66179, 10.1371/journal.pone.0066179.
84. Sato, H., Genet, C., Strehle, A., Thomas, C., Lobstein, A., Wagner, A., Mioskowski, C., Auwerx, J., Saladin, R., Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea. Biochem. Biophys. Res. Commun. 362 (2007), 793–798, 10.1016/j.bbrc.2007.06.130.
85. Schwarz, M., Lund, E.G., Setchell, K.D., Kayden, H.J., Zerwekh, J.E., Björkhem, I., Herz, J., Russell, D.W., Disruption of cholesterol 7alpha-hydroxylase gene in mice. II. Bile acid deficiency is overcome by induction of oxysterol 7alpha-hydroxylase. J. Biol. Chem. 271 (1996), 18024–18031.
86. Scott-Conner, C.E., Grogan, J.B., The pathophysiology of biliary obstruction and its effect on phagocytic and immune function. J. Surg. Res. 57 (1994), 316–336, 10.1006/jsre.1994.1151.
87. Seol, W., Choi, H.S., Moore, D.D., An orphan nuclear hormone receptor that lacks a DNA binding domain and heterodimerizes with other receptors. Science 272 (1996), 1336–1339.
88. Seol, W., Choi, H.S., Moore, D.D., Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors. Mol. Endocrinol. Balt. Md 9 (1995), 72–85, 10.1210/mend.9.1.7760852.
89. Song, C.S., Echchgadda, I., Baek, B.S., Ahn, S.C., Oh, T., Roy, A.K., Chatterjee, B., Dehydroepiandrosterone sulfotransferase gene induction by bile acid activated farnesoid X receptor. J. Biol. Chem. 276 (2001), 42549–42556, 10.1074/jbc.M107557200.
90. Stayrook, K.R., Bramlett, K.S., Savkur, R.S., Ficorilli, J., Cook, T., Christe, M.E., Michael, L.F., Burris, T.P., Regulation of carbohydrate metabolism by the farnesoid X receptor. Endocrinology 146 (2005), 984–991, 10.1210/en.2004-0965.
91. Sung, J.J., Go, M.Y., Reversible Kupffer cell suppression in biliary obstruction is caused by hydrophobic bile acids. J. Hepatol. 30 (1999), 413–418.
92. Thomas, C., Auwerx, J., Schoonjans, K., Bile acids and the membrane bile acid receptor TGR5–connecting nutrition and metabolism. Thyroid. Off. J. Am. Thyroid. Assoc. 18 (2008), 167–174, 10.1089/thy.2007.0255.
93. Thomas, C., Gioiello, A., Noriega, L., Strehle, A., Oury, J., Rizzo, G., Macchiarulo, A., Yamamoto, H., Mataki, C., Pruzanski, M., Pellicciari, R., Auwerx, J., Schoonjans, K., TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 10 (2009), 167–177, 10.1016/j.cmet.2009.08.001.
94. Urizar, N.L., Liverman, A.B., Dodds, D.T., Silva, F.V., Ordentlich, P., Yan, Y., Gonzalez, F.J., Heyman, R.A., Mangelsdorf, D.J., Moore, D.D., A natural product that lowers cholesterol as an antagonist ligand for FXR. Science 296 (2002), 1703–1706, 10.1126/science.1072891.
95. Van Mil, S.W.C., Milona, A., Dixon, P.H., Mullenbach, R., Geenes, V.L., Chambers, J., Shevchuk, V., Moore, G.E., Lammert, F., Glantz, A.G., Mattsson, L.-A., Whittaker, J., Parker, M.G., White, R., Williamson, C., Functional variants of the central bile acid sensor FXR identified in intrahepatic cholestasis of pregnancy. Gastroenterology 133 (2007), 507–516, 10.1053/j.gastro.2007.05.015.
96. Vega, A., Martinot, E., Baptissart, M., De Haze, A., Vaz, F., Kulik, W., Damon-Soubeyrand, C., Baron, S., Caira, F., Volle, D.H., Bile acid alters male mouse fertility in metabolic syndrome context. PloS One, 10, 2015, e0139946, 10.1371/journal.pone.0139946.
97. Volle, D.H., Duggavathi, R., Magnier, B.C., Houten, S.M., Cummins, C.L., Lobaccaro, J.-M.A., Verhoeven, G., Schoonjans, K., Auwerx, J., The small heterodimer partner is a gonadal gatekeeper of sexual maturation in male mice. Genes Dev. 21 (2007), 303–315, 10.1101/gad.409307.
98. Wang, H., Chen, J., Hollister, K., Sowers, L.C., Forman, B.M., Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol. Cell 3 (1999), 543–553.
99. Wang, Y.-D., Chen, W.-D., Wang, M., Yu, D., Forman, B.M., Huang, W., Farnesoid X receptor antagonizes nuclear factor kappaB in hepatic inflammatory response. Hepatol. Balt. Md 48 (2008), 1632–1643, 10.1002/hep.22519.
100. Wang, Y.-D., Chen, W.-D., Yu, D., Forman, B.M., Huang, W., The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor κ light-chain enhancer of activated B cells (NF-κB) in mice. Hepatol. Balt. Md 54 (2011), 1421–1432, 10.1002/hep.24525.
101. Watanabe, M., Houten, S.M., Mataki, C., Christoffolete, M.A., Kim, B.W., Sato, H., Messaddeq, N., Harney, J.W., Ezaki, O., Kodama, T., Schoonjans, K., Bianco, A.C., Auwerx, J., Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 439 (2006), 484–489, 10.1038/nature04330.
102. Watanabe, M., Houten, S.M., Wang, L., Moschetta, A., Mangelsdorf, D.J., Heyman, R.A., Moore, D.D., Auwerx, J., Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. J. Clin. Invest. 113 (2004), 1408–1418, 10.1172/JCI21025.
103. Wu, J., Xia, C., Meier, J., Li, S., Hu, X., Lala, D.S., The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor. Mol. Endocrinol. Balt. Md 16 (2002), 1590–1597, 10.1210/mend.16.7.0894.
104. Wu, T., Bound, M.J., Standfield, S.D., Gedulin, B., Jones, K.L., Horowitz, M., Rayner, C.K., Effects of rectal administration of taurocholic acid on glucagon-like peptide-1 and peptide YY secretion in healthy humans. Diabetes Obes. Metab. 15 (2013), 474–477, 10.1111/dom.12043.
105. Xing, Y., Saner-Amigh, K., Nakamura, Y., Hinshelwood, M.M., Carr, B.R., Mason, J.I., Rainey, W.E., The farnesoid X receptor regulates transcription of 3beta-hydroxysteroid dehydrogenase type 2 in human adrenal cells. Mol. Cell. Endocrinol. 299 (2009), 153–162, 10.1016/j.mce.2008.11.006.
106. Yamagata, K., Daitoku, H., Shimamoto, Y., Matsuzaki, H., Hirota, K., Ishida, J., Fukamizu, A., Bile acids regulate gluconeogenic gene expression via small heterodimer partner-mediated repression of hepatocyte nuclear factor 4 and Foxo1. J. Biol. Chem. 279 (2004), 23158–23165, 10.1074/jbc.M314322200.
107. Yang, F., Huang, X., Yi, T., Yen, Y., Moore, D.D., Huang, W., Spontaneous development of liver tumors in the absence of the bile acid receptor farnesoid X receptor. Cancer Res. 67 (2007), 863–867, 10.1158/0008-5472.CAN-06-1078.
108. Zhang, M., Chiang, J.Y., Transcriptional regulation of the human sterol 12alpha-hydroxylase gene (CYP8B1): roles of heaptocyte nuclear factor 4alpha in mediating bile acid repression. J. Biol. Chem. 276 (2001), 41690–41699, 10.1074/jbc.M105117200.
109. Zhang, Y., Lee, F.Y., Barrera, G., Lee, H., Vales, C., Gonzalez, F.J., Willson, T.M., Edwards, P.A., Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc. Natl. Acad. Sci. U. S. A. 103 (2006), 1006–1011, 10.1073/pnas.0506982103.