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Discovery of ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureidyl derivatives as selective non-steroidal agonists of the G-protein coupled bile acid receptor-1.

Di Leva FS, Festa C, Carino A, De Marino S, Marchianò S, Di Marino D, Finamore C, Monti MC, Zampella A, Fiorucci S, Limongelli V.

Sci Rep. 2019 Feb 21;9(1):2504. doi: 10.1038/s41598-019-38840-z.


Chemistry and Pharmacology of GPBAR1 and FXR Selective Agonists, Dual Agonists, and Antagonists.

De Marino S, Festa C, Sepe V, Zampella A.

Handb Exp Pharmacol. 2019 Jun 15. doi: 10.1007/164_2019_237. [Epub ahead of print]


Investigation on bile acid receptor regulators. Discovery of cholanoic acid derivatives with dual G-protein coupled bile acid receptor 1 (GPBAR1) antagonistic and farnesoid X receptor (FXR) modulatory activity.

Sepe V, Renga B, Festa C, Finamore C, Masullo D, Carino A, Cipriani S, Distrutti E, Fiorucci S, Zampella A.

Steroids. 2016 Jan;105:59-67. doi: 10.1016/j.steroids.2015.11.003. Epub 2015 Dec 1.


Structure-based drug design targeting the cell membrane receptor GPBAR1: exploiting the bile acid scaffold towards selective agonism.

Di Leva FS, Festa C, Renga B, Sepe V, Novellino E, Fiorucci S, Zampella A, Limongelli V.

Sci Rep. 2015 Nov 16;5:16605. doi: 10.1038/srep16605.


Navigation in bile acid chemical space: discovery of novel FXR and GPBAR1 ligands.

Finamore C, Festa C, Renga B, Sepe V, Carino A, Masullo D, Biagioli M, Marchianò S, Capolupo A, Monti MC, Fiorucci S, Zampella A.

Sci Rep. 2016 Jul 6;6:29320. doi: 10.1038/srep29320.


Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties.

Finamore C, Baronissi G, Marchianò S, Di Leva FS, Carino A, Monti MC, Limongelli V, Zampella A, Fiorucci S, Sepe V.

Molecules. 2019 Mar 16;24(6). pii: E1043. doi: 10.3390/molecules24061043.


Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling.

Cipriani S, Renga B, D'Amore C, Simonetti M, De Tursi AA, Carino A, Monti MC, Sepe V, Zampella A, Fiorucci S.

PLoS One. 2015 Jul 15;10(7):e0129866. doi: 10.1371/journal.pone.0129866. eCollection 2015.


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.


Insights on FXR selective modulation. Speculation on bile acid chemical space in the discovery of potent and selective agonists.

Sepe V, Festa C, Renga B, Carino A, Cipriani S, Finamore C, Masullo D, Del Gaudio F, Monti MC, Fiorucci S, Zampella A.

Sci Rep. 2016 Jan 7;6:19008. doi: 10.1038/srep19008.


Steroidal scaffolds as FXR and GPBAR1 ligands: from chemistry to therapeutical application.

Sepe V, Distrutti E, Limongelli V, Fiorucci S, Zampella A.

Future Med Chem. 2015;7(9):1109-35. doi: 10.4155/fmc.15.54. Review.


The Pharmacology of Bile Acids and Their Receptors.

Fiorucci S, Distrutti E.

Handb Exp Pharmacol. 2019 Jun 15. doi: 10.1007/164_2019_238. [Epub ahead of print]


Modification on ursodeoxycholic acid (UDCA) scaffold. discovery of bile acid derivatives as selective agonists of cell-surface G-protein coupled bile acid receptor 1 (GP-BAR1).

Sepe V, Renga B, Festa C, D'Amore C, Masullo D, Cipriani S, Di Leva FS, Monti MC, Novellino E, Limongelli V, Zampella A, Fiorucci S.

J Med Chem. 2014 Sep 25;57(18):7687-701. doi: 10.1021/jm500889f. Epub 2014 Sep 7.


Decoding the vasoregulatory activities of bile acid-activated receptors in systemic and portal circulation: role of gaseous mediators.

Fiorucci S, Zampella A, Cirino G, Bucci M, Distrutti E.

Am J Physiol Heart Circ Physiol. 2017 Jan 1;312(1):H21-H32. doi: 10.1152/ajpheart.00577.2016. Epub 2016 Oct 7. Review.


Targeting the transsulfuration-H2S pathway by FXR and GPBAR1 ligands in the treatment of portal hypertension.

Fiorucci S, Distrutti E.

Pharmacol Res. 2016 Sep;111:749-756. doi: 10.1016/j.phrs.2016.07.040. Epub 2016 Jul 27. Review.


Activation of the bile acid receptor GPBAR1 protects against gastrointestinal injury caused by non-steroidal anti-inflammatory drugs and aspirin in mice.

Cipriani S, Mencarelli A, Bruno A, Renga B, Distrutti E, Santucci L, Baldelli F, Fiorucci S.

Br J Pharmacol. 2013 Jan;168(1):225-37. doi: 10.1111/j.1476-5381.2012.02128.x.


Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.

Xiao H, Li P, Li X, He H, Wang J, Guo F, Zhang J, Wei L, Zhang H, Shi Y, Hou L, Shen L, Chen Z, Du C, Fu S, Zhang P, Hao F, Wang P, Xu D, Liang W, Tian X, Zhang A, Cheng X, Yang L, Wang X, Zhang X, Li J, Chen S.

ACS Med Chem Lett. 2017 Oct 31;8(12):1246-1251. doi: 10.1021/acsmedchemlett.7b00318. eCollection 2017 Dec 14.


Structural Insight into the Binding Mode of FXR and GPBAR1 Modulators.

Di Leva FS, Di Marino D, Limongelli V.

Handb Exp Pharmacol. 2019 Jun 4. doi: 10.1007/164_2019_234. [Epub ahead of print]


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.


Systemic bile acid sensing by G protein-coupled bile acid receptor 1 (GPBAR1) promotes PYY and GLP-1 release.

Ullmer C, Alvarez Sanchez R, Sprecher U, Raab S, Mattei P, Dehmlow H, Sewing S, Iglesias A, Beauchamp J, Conde-Knape K.

Br J Pharmacol. 2013 Jun;169(3):671-84. doi: 10.1111/bph.12158.


Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice.

Maruyama T, Tanaka K, Suzuki J, Miyoshi H, Harada N, Nakamura T, Miyamoto Y, Kanatani A, Tamai Y.

J Endocrinol. 2006 Oct;191(1):197-205.


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