Potential therapeutic applications of farnesoid X receptor (FXR) modulators

Bibliography

• KLIEWER SA, LEHMANN JM, WILLSON TM: Orphan nuclear receptors: shifting endocrinology into reverse. Science (1999) 284:757-760.
   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) 3:543-553.
   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) 284:1365-1368.
   PubMed Web of Science ®Google Scholar
• MAKISHIMA M, OKAMOTO AY, REPA JJ et al.: Identification of a nuclear receptor for bile acids. Science (1999) 284:1362-1365.
   PubMed Web of Science ®Google Scholar
• CHEN W, OWSLEY E, YANG Y et al.: Nuclear receptor-mediated repression of human cholesterol 7α-hydroxylase gene transcription by bile acids J. Lipid Res. (2001) 42:402-412.
   Google Scholar
• GOODWIN B, JONES SA, PRICE RR et al.: A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol. Cell (2000) 6:517-526.
   PubMed Web of Science ®Google Scholar
• LU TT, MAKISHIMA M, REPA JJ et al.: Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol. Cell (2000) 6:507-515.
   PubMed Web of Science ®Google Scholar
• ANANTHANARAYANAN M, BALASUBRAMANIAN N, MAKISHIMA M et al.: Human bile salt export pump promoter is activated by the farnesoid X receptor/bile acid receptor. J. Biol. Chem. (2001) 276:28857-28865.
   PubMed Web of Science ®Google Scholar
• YU J, LO JL, HUANG L et al.: Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity. J. Biol. Chem (2002) 277:31441-31447.
   PubMed Web of Science ®Google Scholar
• DENSON LA, STURM E, ECHAVERRIA W et al.: The orphan nuclear receptor SHP mediates bile acid-induced inhibition of the rat bile acid transporter ntcp. Gastroenterology (2001) 121:140-147.
   PubMed Web of Science ®Google Scholar
• SINAL CJ, TOHKIN M, MIYATA M et al.: Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell (2000) 102:731-744.
   PubMed Web of Science ®Google Scholar
• KOK T, HULZEBOS CV, WOLTERS H et al.: Enterohepatic circulation of bile salts in farnesoid X receptor-deficient mice: efficient intestinal bile salt absorption in the absence of ileal bile acid-binding protein. J. Biol. Chem. (2003) 278:41930-41937.
   PubMed Web of Science ®Google Scholar
• DURAN-SANDOVAL D, MAUTINO G, MARTIN G et al.: Glucose regulates the expression of the farnesoid X receptor in liver. Diabetes (2004) 53:890-898.
   PubMed Web of Science ®Google Scholar
• STAYROOK KR, BRAMLETT KS, SAVKUR RS et al.: Regulation of carbohydrate metabolism by the farnesoid X receptor. Endocrinology (2005) 146:984-991.
   PubMed Web of Science ®Google Scholar
• DURAN-SANDOVAL D, CARIOU B, FRUCHART JC et al.: Potential regulatory role of the farnesoid X receptor in the metabolic syndrome. Biochimie (2005) 87:93-98.
   PubMedGoogle Scholar
• PELLICCIARI R, COSTANTINO G, FIORUCCI S: Farnesoid X receptor: from structure to potential clinical applications. J. Med. Chem. (2005) 48:5383-5403.
   PubMed Web of Science ®Google Scholar
• MALONEY PR, PARKS DJ, HAFFNER CD et al.: Identification of a chemical tool for the orphan nuclear receptor FXR. J. Med. Chem. (2000) 43:2971-2974.
   PubMed Web of Science ®Google Scholar
• NICOLAOU KC, EVANS RM, ROECKER AJ et al.: Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries. Org. Biomol. Chem. (2003) 1:908-920.
   PubMed Web of Science ®Google Scholar
• DOWNERS M, VERDECIA MA, ROECKER AJ et al.: A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol. Cell. (2003) 11:1079-92.
   PubMedGoogle Scholar
• DUSSAULT I, BEARD R, LIN M et al.: Identification of gene-selective modulators of the bile acid receptor FXR. J. Biol. Chem. (2003) 278:7027-7033.
   PubMed Web of Science ®Google Scholar
• PELLICCIARI R, FIORUCCI S, CAMAIONI E et al.: 6α-Ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J. Med. Chem. (2002) 45:3569-3972.
   PubMed Web of Science ®Google Scholar
• MI LZ, DEVARAKONDA S, HARP JM et al.: Structural basis for bile acid binding and activation of the nuclear receptor FXR. Mol. Cell (2003) 11:1093-1100.
   PubMed Web of Science ®Google Scholar
• FUKUCHI J, SONG C, DAI Q et al.: 5β-Cholane activators of the farnesoid X receptor. J. Steroid Biochem. Mol. Biol. (2005) 94:311-318.
   PubMedGoogle Scholar
• FORMAN BM, UMESONO K, CHEN J et al.: Unique response pathways are established by allosteric interactions among nuclear hormone receptors. Cell (1995) 81:541-550.
   PubMed Web of Science ®Google Scholar
• CARSON-JURICA MA, SCHRADER WT, O’MALLEY BW: Steroid receptor family: structure and functions. Endocr. Rev. (1990) 11:201-222.
   PubMed Web of Science ®Google Scholar
• SEO YW, SANYAL S, KIM HJ et al.: FOR, a novel orphan nuclear receptor related to farnesoid X receptor. J. Biol. Chem. (2002) 277:17836-17844.
   PubMedGoogle Scholar
• BISHOP-BAILEY D, WALSH DT, WARNER TD: Expression and activation of the farnesoid X receptor in the vasculature. Proc. Natl. Acad. Sci. USA (2004) 101:3668-3673.
   PubMed Web of Science ®Google Scholar
• TRAUNER M, MEIER PJ, BOYER JL: Molecular pathogenesis of cholestasis. N. Engl. J. Med. (1998) 339:1217-1227.
   PubMed Web of Science ®Google Scholar
• PAUMGARTNER G, BEUERS U: Ursodeoxycholic acid in cholestatic liver disease: mechanisms of action and therapeutic use revisited. Hepatology (2002) 36:525-531.
   PubMed Web of Science ®Google Scholar
• CLAUDEL T, STURM E, KUIPERS F, STAELS B: The farnesoid X receptor: a novel drug target? Expert. Opin. Investig. Drugs (2004) 13:1135-1148.
   PubMed Web of Science ®Google Scholar
• FRIEDMAN SL: Liver fibrosis – from bench to bedside. J. Hepatol. (2003) 38:S38-S53.
   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) 127:1497-1512.
   PubMed Web of Science ®Google Scholar
• SINGH RB, NIAZ MA, CHOSH S: Hypolipidemic and antioxidant effects of Commiphora mukul as an adjunct to dietary therapy in patients with hypercholesterolemia. Cardiovasc. Drugs Ther. (1994) 4:659-664.
   Google Scholar
• SINAL CJ, GONZALEZ FJ: Guggulsterone: an old approach to a new problem. Trends Endocrinol. Metab. (2002) 132:275-276.
   Google Scholar
• BROBST DE, DING X, CREECH KL et al.: Guggulsterone activates multiple nuclear receptors and induces cyp3a gene expression through pregnane X receptor. J. Pharm. Exp. Ther. (2004) 310:528-535.
   PubMed Web of Science ®Google Scholar
• BURRIS TP, MONTROSE C, HOUCK KA et al.: The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol. Pharmacol. (2005) 67:948-954.
   PubMed Web of Science ®Google Scholar
• UNIZAR NL, LIVERMAN AB, DODDS DT et al.: A natural product that lowers cholesterol as an antagonist ligand for FXR. Science (2002) 296:1703-1706.
   PubMedGoogle Scholar
• WU J, XIA C, MEIER J et al.: The hypolipidemic natural product guggulsterone act as an antagonist of the bile acid receptor. Mol. Endocrinol. (2002) 16:1590-1597.
   PubMed Web of Science ®Google Scholar
• CUI J, HUANG L, ZHAO A et al.: Guggulsterone is a farnesoid X receptor antagonist in a coactivator association assays but acts to enhance transcription of bile salt export pump. J. Biol. Chem. (2003) 278:10214-10220.
   PubMed Web of Science ®Google Scholar
• SZAPARY PO, WOLFE ML, BOLEDON LT et al.: Guggulipid for the treatment of hypercholesterolemia. A randomized controlled trial. JAMA (2003) 290:765-772.
   PubMed Web of Science ®Google Scholar
• BOLAND LL, FOLSOM AR, ROSAMOND WD: Hyperinsulinemia, dyslipidemia, and obesity as risk factors for hospitalized gallbladder disease: a prospective study. Ann. Epidemiol. (2002) 12:131-140.
   PubMed Web of Science ®Google Scholar