Targeting FXR in cholestasis: hype or hope

Bibliography

• Chiang JY. Regulation of bile acid synthesis: pathways, nuclear receptors, and mechanisms. J Hepatol 2004;40(3):539-51
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Rizzo G, Donini A, et al. Targeting farnesoid X receptor for liver and metabolic disorders. Trends Mol Med 2007;13(7):298-309
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Mencarelli A, Palladino G, Cipriani S. Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders. Trends Pharmacol Sci 2009;30(11):570-80
   PubMed Web of Science ®Google Scholar
• Makishima M, Okamoto AY, Repa JJ, et al. Identification of a nuclear receptor for bile acids. Science 1999;284(5418):1362-5
   PubMed Web of Science ®Google Scholar
• Parks DJ, Blanchard SG, Bledsoe RK, et al. Bile acids: natural ligands for an orphan nuclear receptor. Science 1999;284(5418):1365-8
   PubMed Web of Science ®Google Scholar
• Wang H, Chen J, Hollister K, et al. Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol Cell 1999;3(5):543-53
   PubMed Web of Science ®Google Scholar
• Xie W, Radominska-Pandya A, Shi Y, et al. An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids. Proc Natl Acad Sci USA 2001;98(6):3375-80
   PubMed Web of Science ®Google Scholar
• Makishima M, Lu TT, Xie W, et al. Vitamin D receptor as an intestinal bile acid sensor. Science 2002;296(5571):1313-16
   PubMed Web of Science ®Google Scholar
• Maruyama T, Miyamoto Y, Nakamura T, et al. Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun 2002;298(5):714-19
   PubMed Web of Science ®Google Scholar
• Sheikh Abdul Kadir SH, Miragoli M, Abu-Hayyeh S, et al. Bile acid-induced arrhythmia is mediated by muscarinic M2 receptors in neonatal rat cardiomyocytes. PLoS One 2010;5(3):e9689
   PubMed Web of Science ®Google Scholar
• Bukiya AN, Singh AK, Parrill AL, Dopico AM. The steroid interaction site in transmembrane domain 2 of the large conductance, voltage- and calcium-gated potassium (BK) channel accessory beta1 subunit. Proc Natl Acad Sci USA 2011;108(50):20207-12
   PubMed Web of Science ®Google Scholar
• Sommerfeld A, Reinehr R, Häussinger D. Bile acid-induced epidermal growth factor receptor activation in quiescent rat hepatic stellate cells can trigger both proliferation and apoptosis. J Biol Chem 2009;284(33):22173-83
   Google Scholar
• Rizzo G, Renga B, Antonelli E, et al. The methyl transferase PRMT1 functions as co-activator of farnesoid X receptor (FXR)/9-cis retinoid X receptor and regulates transcription of FXR responsive genes. Mol Pharmacol 2005;68(2):551-8
   PubMedGoogle Scholar
• Kerr TA, Saeki S, Schneider M, et al. Loss of nuclear receptor SHP impairs but does not eliminate negative feedback regulation of bile acid synthesis. Dev Cell 2002;2(6):713-20
   PubMed Web of Science ®Google Scholar
• Wang L, Lee YK, Bundman D, et al. Redundant pathways for negative feedback regulation of bile acid production. Dev Cell 2002;2(6):721-31
   PubMed Web of Science ®Google Scholar
• Holt JA, Luo G, Billin AN, et al. Definition of a novel growth factor-dependent signal cascade for the suppression of bile acid biosynthesis. Genes Dev 2003;17(13):1581-91
   PubMed Web of Science ®Google Scholar
• Inagaki T, Choi M, Moschetta A, et al. Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis. Cell Metab 2005;2(4):217-25
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Baldelli F. Farnesoid receptor agonists in biliary tract disease. Curr Opin Gastroenterol 2009;25(3):252-9
   Google Scholar
• Renga B, Mencarelli A, D’Amore C, et al. Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis. PLoS One 2012;7(1):e30443
   PubMedGoogle Scholar
• Renga B, Migliorati M, Mencarelli A, et al. Farnesoid X receptor suppresses constitutive androstane receptor activity at the multidrug resistance protein-4 promoter. Biochim Biophys Acta 2011;1809(3):157-65
   PubMed Web of Science ®Google Scholar
• Alemi F, Kwon E, Poole DP, et al. The TGR5 receptor mediates bile acid-induced itch and analgesia. J Clin Invest 2013;123:1513-30
   PubMed Web of Science ®Google Scholar
• Magyar I, Loi HG, Feher T. Plasma bile acid levels and liver disease. Acta Med Acad Sci Hung 1981;38(2):109-15
   Google Scholar
• Schoenfield LJ, Sjorvall J, Perman E. Bile acids on the skin of patients with pruritic hepatobiliary disease. Nature 1967;213:93-4
   Web of Science ®Google Scholar
• Kirby J, Heaton KW, Burton JL. Pruritic effect of bile salts. Br Med J 1974;4(5946):693-5
   PubMed Web of Science ®Google Scholar
• Varadi DP. Pruritus induced by crude bile and purified bile acids. Experimental production of pruritus in human skin. Arch Dermatol 1974;109(5):678-81
   Google Scholar
• Mela M, Mancuso A, Burroughs AK. Review article: pruritus in cholestatic and other liver diseases. Aliment Pharmacol Ther 2003;17(7):857-70
   PubMed Web of Science ®Google Scholar
• Hashimoto T, Ohata H, Momose K. Itch-scratch responses induced by lysophosphatidic acid in mice. Pharmacol 2004;72(1):51-6
   Google Scholar
• Kremer AE, Martens JJ, Kulik W, et al. Lysophosphatidic acid is a potential mediator of cholestatic pruritus. Gastroenterology 2010;139(3):1008-18
   PubMed Web of Science ®Google Scholar
• Dopico AM, Bukiya AN, Singh AK. Large conductance, calcium- and voltage-gated potassium (BK) channels: regulation by cholesterol. Pharmacol Ther 2012;135(2):133-50
   PubMed Web of Science ®Google Scholar
• Dopico AM, Bukiya AN, Singh AK. Large conductance, calcium- and voltage-gated potassium (BK) channels: regulation by cholesterol. Pharmacol Ther 2012;135(2):133-50
   PubMed Web of Science ®Google Scholar
• Pellicciari R, Fiorucci S, Camaioni E, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem 2002;45:17:3569-72
   PubMed Web of Science ®Google Scholar
• D’Amore C, Di Leva FS, Sepe V, et al. Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors. J Med Chem 2014;57(3):937-54
   Google Scholar
• Fiorucci S, Mencarelli A, Distrutti E, Zampella A. Farnesoid X receptor: from medicinal chemistry to clinical applications. Future Med Chem 2012;4(7):877-91
   PubMed Web of Science ®Google Scholar
• Poupon R. Ursodeoxycholic acid and bile-acid mimetics as therapeutic agents for cholestatic liver diseases: an overview of their mechanisms of action. Clin Res Hepatol Gastroenterol 2012;Sep;36(Suppl 1):S3-12
   PubMed Web of Science ®Google Scholar
• Eaton JE, Talwalkar JA, Lazaridis KN, et al. Pathogenesis of primary sclerosing cholangitis and advances in diagnosis and management. Gastroenterology 2013;145(3):521-36
   PubMed Web of Science ®Google Scholar
• Sinakos E, Samuel S, Enders F, et al. Inflammatory bowel disease in primary sclerosing cholangitis: a robust yet changing relationship. Inflamm Bowel Dis 2013;19(5):1004-9
   Google Scholar
• Hirschfield GM, Chapman RW, Karlsen TH, et al. The genetics of complex cholestatic disorders. Gastroenterology 2013;144(7):1357-74
   PubMed Web of Science ®Google Scholar
• Tabibian JH, Lindor KD. Primary sclerosing cholangitis: a review and update on therapeutic developments. Expert Rev Gastroenterol Hepatol 2013;7(2):103-14
   PubMed Web of Science ®Google Scholar
• Bacq Y, Sapey T, Brechot MC, et al. Intrahepatic cholestasis of pregnancy: a French prospective study. Hepatology 1997;26:358-64
   PubMed Web of Science ®Google Scholar
• Geenes V, Williamson C. Intrahepatic cholestasis of pregnancy. World J Gastroenterol 2009;15:2049-66
   PubMed Web of Science ®Google Scholar
• Jonker JW, Liddle C, Downes M. FXR and PXR: potential therapeutic targets in cholestasis. J Steroid Biochem Mol Biol 2012;130(3-5):147-58
   PubMed Web of Science ®Google Scholar
• Liu Y, Binz J, Numerick MJ, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest 2003;112:1678-87
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Clerici C, Antonelli E, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther 2005;313:604-12
   PubMed Web of Science ®Google Scholar
• Stedman C, Liddle C, Coulter S, et al. Benefit of farnesoid X receptor inhibition in obstructive cholestasis. Proc Natl Acad Sci USA 2006;103:11323-8
   PubMed Web of Science ®Google Scholar
• Marschall HU, Wagner M, Bodin K, et al. Fxr(-/-) mice adapt to biliary obstruction by enhanced phase I detoxification and renal elimination of bile acids. J Lipid Res 2006;47:582-92
   PubMed Web of Science ®Google Scholar
• Denk GU, Soroka CJ, Takeyama Y, et al. Multidrug resistance-associated protein 4 is up-regulated in liver but down-regulated in kidney in obstructive cholestasis in the rat. J Hepatol 2004;40:585-91
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Antonelli E, Rizzo G, et al. The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis. Gastroenterology 2004;127(5):1497-512
   PubMed Web of Science ®Google Scholar
• Fiorucci S, Zampella A, Distrutti E. Development of FXR, PXR and CAR agonists and antagonists for treatment of liver disorders. Curr Top Med Chem 2012;12(6):605-24
   Google Scholar
• Mason L, Luketic VA, Lindor KD, et al. Farnesoid - X receptor agonists: a new class of drugs for the treatment of PBC? An international study evaluating the addition of obeticholic acid (INT-747) to ursodeoxycholic acid [abstract]. Hepatology 2010;52(Suppl 1):357A
   Google Scholar
• Kowdley KV, Jones D, Luketic V, et al. An international study evaluating the farnesoid X receptor agonist obeticholic acid as monotherapy in PBC [abstract]. J Hepatol 2011;54(Suppl 1):S13
   Google Scholar
• Marschall HU, Luketic V, Lövgren-Sandblom A, et al. The farnesoid X receptor (FXR) agonist obeticholic acid (OCA) increases plasma FGF-19 concentrations and decreases bile acid synthesis in primary biliary cirrhosis (PBC) [abstract]. J Hepatol 2012;56(Suppl 2):S377
   Google Scholar
• Silveira MG, Lindor KD. Obeticholic acid and budesonide for the treatment of primary biliary cirrhosis. Expert Opin Pharmacother 2014;15(3):365-72
   PubMed Web of Science ®Google Scholar
• Yu DD, Lin W, Forman BM, Chen T. Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor. Bioorg Med Chem 2014;Jun;1;22(11):2919-38
   Google Scholar
• Lien F, Berthier A, Bouchaert E, et al. Metformin interferes with bile acid homeostasis through AMPK-FXR crosstalk. J Clin Invest 2014;124(3):1037-51
   Google Scholar