Page 37 - Read Online

receptor. Science 1999;284:1365-8. cell proliferation and tumor development. J Pharmacol Exp Ther
16. Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, 2009;328:469-77.
Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones 31. Smith DL, Keshavan P, Avissar U, Ahmed K, Zucker SD. Sodium
SA, Willson TM. Identification of a chemical tool for the orphan taurocholate inhibits intestinal adenoma formation in APCMin/+
nuclear receptor FXR. J Med Chem 2000;43:2971-4. mice, potentially through activation of the farnesoid X receptor.
17. Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Carcinogenesis 2010;31:1100-9.
Maloney PR, Morelli A, Parks DJ, Willson TM. 6alpha-ethyl- 32. De Gottardi A, Touri F, Maurer CA, Perez A, Maurhofer O, Ventre G,
chenodeoxycholic acid (6-ECDCA), a potent and selective FXR Bentzen CL, Niesor EJ, Dufour JF. The bile acid nuclear receptor FXR
agonist endowed with anticholestatic activity. J Med Chem and the bile acid binding protein IBABP are differently expressed in
2002;45:3569-72. colon cancer. Dig Dis Sci 2004;49:982-9.
18. Flatt B, Martin R, Wang TL, Mahaney P, Murphy B, Gu XH, Foster 33. Lax S, Schauer G, Prein K, Kapitan M, Silbert D, Berghold A, Berger
P, Li J, Pircher P, Petrowski M, Schulman I, Westin S, Wrobel J, A, Trauner M. Expression of the nuclear bile acid receptor/farnesoid
Yan G, Bischoff E, Daige C, Mohan R. Discovery of XL335 (WAY- X receptor is reduced in human colon carcinoma compared to
362450), a highly potent, selective, and orally active agonist of the nonneoplastic mucosa independent from site and may be associated
farnesoid X receptor (FXR). J Med Chem 2009;52:904-7. with adverse prognosis. Int J Cancer 2012;130:2232-9.
19. Fang S, Suh JM, Reilly SM, Yu E, Osborn O, Lackey D, Yoshihara 34. Ullman TA, Itzkowitz SH. Intestinal inflammation and cancer.
E, Perino A, Jacinto S, Lukasheva Y, Atkins AR, Khvat A, Schnabl Gastroenterology 2011;140:1807-16.
B, Yu RT, Brenner DA, Coulter S, Liddle C, Schoonjans K, Olefsky 35. Gadaleta RM, Cariello M, Sabba C, Moschetta A. Tissue-specific
JM, Saltiel AR, Downes M, Evans RM. Intestinal FXR agonism actions of FXR in metabolism and cancer. Biochim Biophys Acta
promotes adipose tissue browning and reduces obesity and insulin 2015;1851:30-9.
resistance. Nat Med 2015;21:159-65. 36. Stojancevic M, Stankov K, Mikov M. The impact of farnesoid X
20. Urizar NL, Liverman AB, Dodds DT, Silva FV, Ordentlich P, Yan Y, receptor activation on intestinal permeability in inflammatory bowel
Gonzalez FJ, Heyman RA, Mangelsdorf DJ, Moore DD. A natural disease. Can J Gastroenterol 2012;26:631-7.
product that lowers cholesterol as an antagonist ligand for FXR. 37. Torres J, Bao X, Iuga AC, Chen A, Harpaz N, Ullman T, Cohen BL,
Science 2002;296:1703-6. Pineton de Chambrun G, Asciutti S, Odin JA, Sachar DB, Gaskins
21. Dussault I, Beard R, Lin M, Hollister K, Chen J, Xiao JH, HR, Setchell K, Colombel JF, Itzkowitz SH. Farnesoid X receptor
Chandraratna R, Forman BM. Identification of gene-selective expression is decreased in colonic mucosa of patients with primary
modulators of the bile acid receptor FXR. J Biol Chem sclerosing cholangitis and colitis-associated neoplasia. Inflamm Bowel
2003;278:7027-33. Dis 2013;19:275-82.
22. Bookout AL, Jeong Y, Downes M, Yu RT, Evans RM, Mangelsdorf 38. Peng Z, Raufman JP, Xie G. Src-mediated cross-talk between
DJ. Anatomical profiling of nuclear receptor expression reveals a farnesoid X and epidermal growth factor receptors inhibits
hierarchical transcriptional network. Cell 2006;126:789-99. human intestinal cell proliferation and tumorigenesis. PLoS One
23. Yang X, Downes M, Yu RT, Bookout AL, He W, Straume M, 2012;7:e48461.
Mangelsdorf DJ, Evans RM. Nuclear receptor expression links the 39. Yang F, Hu Y, Liu HX, Wan YJ. miR-22-silenced cyclin A
circadian clock to metabolism. Cell 2006;126:801-10. expression in colon and liver cancer cells is regulated by bile acid
24. Modica S, Gofflot F, Murzilli S, D’Orazio A, Salvatore L, Pellegrini receptor. J Biol Chem 2015;290:6507-15.
F, Nicolucci A, Tognoni G, Copetti M, Valanzano R, Veschi S, 40. Gadaleta RM, Oldenburg B, Willemsen EC, Spit M, Murzilli S,
Mariani-Costantini R, Palasciano G, Schoonjans K, Auwerx J, Salvatore L, Klomp LW, Siersema PD, van Erpecum KJ, van Mil
Moschetta A. The intestinal nuclear receptor signature with SW. Activation of bile salt nuclear receptor FXR is repressed by
epithelial localization patterns and expression modulation in pro-inflammatory cytokines activating NF-kappaB signaling in the
tumors. Gastroenterology 2010;138:636-48, 48e1-12. intestine. Biochim Biophys Acta 2011;1812:851-8.
25. Modica S, Cariello M, Morgano A, Gross I, Vegliante MC, Murzilli 41. Zhou X, Cao L, Jiang C, Xie Y, Cheng X, Krausz KW, Qi Y, Sun
S, Salvatore L, Freund JN, Sabba C, Moschetta A. Transcriptional L, Shah YM, Gonzalez FJ, Wang G, Hao H. PPARalpha-UGT axis
regulation of the intestinal nuclear bile acid farnesoid X receptor activation represses intestinal FXR-FGF15 feedback signalling and
(FXR) by the caudal-related homeobox 2 (CDX2). J Biol Chem exacerbates experimental colitis. Nat Commun 2014;5:4573.
2014;289:28421-32. 42. Berg A. Nutrition, development, and population growth. Popul
26. Bailey AM, Zhan L, Maru D, Shureiqi I, Pickering CR, Kiriakova Bull 1973;29:3-37.
G, Izzo J, He N, Wei C, Baladandayuthapani V, Liang H, Kopetz S, 43. Chao A, Thun MJ, Connell CJ, McCullough ML, Jacobs EJ, Flanders
Powis G, Guo GL. FXR silencing in human colon cancer by DNA WD, Rodriguez C, Sinha R, Calle EE. Meat consumption and
methylation and KRAS signaling. Am J Physiol Gastrointest Liver risk of colorectal cancer. JAMA 2005;293:172-82.
Physiol 2014;306:G48-58. 44. Kirkegaard H, Johnsen NF, Christensen J, Frederiksen K,
27. Cabrerizo R, Castano GO, Burgueno AL, Fernandez Gianotti Overvad K, Tjonneland A. Association of adherence to lifestyle
T, Gonzalez Lopez Ledesma MM, Flichman D, Pirola CJ, recommendations and risk of colorectal cancer: a prospective
Sookoian S. Promoter DNA methylation of farnesoid X receptor Danish cohort study. BMJ 2010;341:c5504.
and pregnane X receptor modulates the intrahepatic cholestasis of 45. Bajor A, Gillberg PG, Abrahamsson H. Bile acids: short and long term
pregnancy phenotype. PLoS One 2014;9:e87697. effects in the intestine. Scand J Gastroenterol 2010;45:645-64.
28. Lou G, Li Y, Chen B, Chen M, Chen J, Liao R, Zhang Y, Wang 46. McGarr SE, Ridlon JM, Hylemon PB. Diet, anaerobic bacterial
Y, Zhou D. Functional analysis on the 5’-flanking region of human metabolism, and colon cancer: a review of the literature. J Clin
FXR gene in HepG2 cells. Gene 2007;396:358-68. Gastroenterol 2005;39:98-109.
29. Modica S, Murzilli S, Salvatore L, Schmidt DR, Moschetta 47. Bianchini F, Caderni G, Dolara P, Fantetti L, Kriebel D. Effect of
A. Nuclear bile acid receptor FXR protects against intestinal dietary fat, starch and cellulose on fecal bile acids in mice. J Nutr
tumorigenesis. Cancer Res 2008;68:9589-94. 1989;119:1617-24.
30. Maran RR, Thomas A, Roth M, Sheng Z, Esterly N, Pinson D, Gao 48. Reddy BS, Hedges AR, Laakso K, Wynder EL. Metabolic
X, Zhang Y, Ganapathy V, Gonzalez FJ, Guo GL. Farnesoid X epidemiology of large bowel cancer: fecal bulk and constituents of
receptor deficiency in mice leads to increased intestinal epithelial high-risk North American and low-risk Finnish population. Cancer

Journal of Cancer Metastasis and Treatment ¦ Volume 2 ¦ Issue 1 ¦ January 15, 2016 ¦ 27