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Items: 1 to 20 of 96

1.

Novel Isoxazole Derivatives with Potent FXR Agonistic Activity Prevent Acetaminophen-Induced Liver Injury.

Sepe V, Marchianò S, Finamore C, Baronissi G, Di Leva FS, Carino A, Biagioli M, Fiorucci C, Cassiano C, Monti MC, Del Gaudio F, Novellino E, Limongelli V, Fiorucci S, Zampella A.

ACS Med Chem Lett. 2018 Dec 6;10(4):407-412. doi: 10.1021/acsmedchemlett.8b00423. eCollection 2019 Apr 11.

PMID:
30996771
2.

Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties.

Flesch D, Gabler M, Lill A, Gomez RC, Steri R, Schneider G, Stark H, Schubert-Zsilavecz M, Merk D.

Bioorg Med Chem. 2015 Jul 1;23(13):3490-8. doi: 10.1016/j.bmc.2015.04.035. Epub 2015 Apr 18.

PMID:
25934227
3.

Targeting Bile Acid Receptors: Discovery of a Potent and Selective Farnesoid X Receptor Agonist as a New Lead in the Pharmacological Approach to Liver Diseases.

Festa C, De Marino S, Carino A, Sepe V, Marchianò S, Cipriani S, Di Leva FS, Limongelli V, Monti MC, Capolupo A, Distrutti E, Fiorucci S, Zampella A.

Front Pharmacol. 2017 Mar 30;8:162. doi: 10.3389/fphar.2017.00162. eCollection 2017.

4.

Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.

Kinzel O, Steeneck C, Schlüter T, Schulz A, Gege C, Hahn U, Hambruch E, Hornberger M, Spalwisz A, Frick K, Perović-Ottstadt S, Deuschle U, Burnet M, Kremoser C.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3746-53. doi: 10.1016/j.bmcl.2016.05.070. Epub 2016 May 24.

PMID:
27268696
5.

Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.

Gege C, Kinzel O, Steeneck C, Schulz A, Kremoser C.

Curr Top Med Chem. 2014;14(19):2143-58. Review.

PMID:
25388536
6.

Relevance of FXR-p62/SQSTM1 pathway for survival and protection of mouse hepatocytes and liver, especially with steatosis.

Haga S, Yimin, Ozaki M.

BMC Gastroenterol. 2017 Jan 13;17(1):9. doi: 10.1186/s12876-016-0568-3.

7.

Design, Synthesis, and Biological Evaluation of Novel Nonsteroidal Farnesoid X Receptor (FXR) Antagonists: Molecular Basis of FXR Antagonism.

Huang H, Si P, Wang L, Xu Y, Xu X, Zhu J, Jiang H, Li W, Chen L, Li J.

ChemMedChem. 2015 Jul;10(7):1184-99. doi: 10.1002/cmdc.201500136. Epub 2015 May 15.

PMID:
25982493
8.

Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.

Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Parks DJ, Todd D, Williams SP, Wisely GB.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2969-73. doi: 10.1016/j.bmcl.2009.04.047. Epub 2009 Apr 18.

PMID:
19410460
9.

Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist.

Feng S, Yang M, Zhang Z, Wang Z, Hong D, Richter H, Benson GM, Bleicher K, Grether U, Martin RE, Plancher JM, Kuhn B, Rudolph MG, Chen L.

Bioorg Med Chem Lett. 2009 May 1;19(9):2595-8. doi: 10.1016/j.bmcl.2009.03.008. Epub 2009 Mar 9.

PMID:
19328688
10.

Restoration of enterohepatic bile acid pathways in pregnant mice following short term activation of Fxr by GW4064.

Moscovitz JE, Kong B, Buckley K, Buckley B, Guo GL, Aleksunes LM.

Toxicol Appl Pharmacol. 2016 Nov 1;310:60-67. doi: 10.1016/j.taap.2016.08.021. Epub 2016 Sep 5.

11.

Activation of the farnesoid X receptor attenuates triptolide-induced liver toxicity.

Jin J, Sun X, Zhao Z, Wang W, Qiu Y, Fu X, Huang M, Huang Z.

Phytomedicine. 2015 Sep 15;22(10):894-901. doi: 10.1016/j.phymed.2015.06.007. Epub 2015 Jul 3.

PMID:
26321738
12.

Identification of an Oleanane-Type Triterpene Hedragonic Acid as a Novel Farnesoid X Receptor Ligand with Liver Protective Effects and Anti-inflammatory Activity.

Lu Y, Zheng W, Lin S, Guo F, Zhu Y, Wei Y, Liu X, Jin S, Jin L, Li Y.

Mol Pharmacol. 2018 Feb;93(2):63-72. doi: 10.1124/mol.117.109900. Epub 2017 Nov 21.

PMID:
29162643
13.

Bile acid receptor agonist GW4064 regulates PPARγ coactivator-1α expression through estrogen receptor-related receptor α.

Dwivedi SK, Singh N, Kumari R, Mishra JS, Tripathi S, Banerjee P, Shah P, Kukshal V, Tyagi AM, Gaikwad AN, Chaturvedi RK, Mishra DP, Trivedi AK, Sanyal S, Chattopadhyay N, Ramachandran R, Siddiqi MI, Bandyopadhyay A, Arora A, Lundåsen T, Anakk SP, Moore DD, Sanyal S.

Mol Endocrinol. 2011 Jun;25(6):922-32. doi: 10.1210/me.2010-0512. Epub 2011 Apr 14.

14.

Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity.

Yu J, Lo JL, Huang L, Zhao A, Metzger E, Adams A, Meinke PT, Wright SD, Cui J.

J Biol Chem. 2002 Aug 30;277(35):31441-7. Epub 2002 Jun 6.

15.

Synthetic FXR agonist GW4064 is a modulator of multiple G protein-coupled receptors.

Singh N, Yadav M, Singh AK, Kumar H, Dwivedi SK, Mishra JS, Gurjar A, Manhas A, Chandra S, Yadav PN, Jagavelu K, Siddiqi MI, Trivedi AK, Chattopadhyay N, Sanyal S.

Mol Endocrinol. 2014 May;28(5):659-73. doi: 10.1210/me.2013-1353. Epub 2014 Mar 5.

16.

Activation of the nuclear receptor FXR enhances hepatocyte chemoprotection and liver tumor chemoresistance against genotoxic compounds.

Vaquero J, Briz O, Herraez E, Muntané J, Marin JJ.

Biochim Biophys Acta. 2013 Oct;1833(10):2212-9. doi: 10.1016/j.bbamcr.2013.05.006. Epub 2013 May 13.

17.

FXR agonist GW4064 alleviates endotoxin-induced hepatic inflammation by repressing macrophage activation.

Yao J, Zhou CS, Ma X, Fu BQ, Tao LS, Chen M, Xu YP.

World J Gastroenterol. 2014 Oct 21;20(39):14430-41. doi: 10.3748/wjg.v20.i39.14430.

18.

Farnesoid X receptor protects liver cells from apoptosis induced by serum deprivation in vitro and fasting in vivo.

Wang YD, Yang F, Chen WD, Huang X, Lai L, Forman BM, Huang W.

Mol Endocrinol. 2008 Jul;22(7):1622-32. doi: 10.1210/me.2007-0527. Epub 2008 Apr 24.

19.

Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and insulin resistance.

Ma Y, Huang Y, Yan L, Gao M, Liu D.

Pharm Res. 2013 May;30(5):1447-57. doi: 10.1007/s11095-013-0986-7. Epub 2013 Feb 1.

20.

Synthetic farnesoid X receptor agonists induce high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.

Hambruch E, Miyazaki-Anzai S, Hahn U, Matysik S, Boettcher A, Perović-Ottstadt S, Schlüter T, Kinzel O, Krol HD, Deuschle U, Burnet M, Levi M, Schmitz G, Miyazaki M, Kremoser C.

J Pharmacol Exp Ther. 2012 Dec;343(3):556-67. doi: 10.1124/jpet.112.196519. Epub 2012 Aug 23.

PMID:
22918042

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