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Items: 1 to 50 of 96

1.

Ursodeoxycholic acid is a GPBAR1 agonist and resets liver/intestinal FXR signaling in a model of diet-induced dysbiosis and NASH.

Carino A, Biagioli M, Marchianò S, Fiorucci C, Zampella A, Monti MC, Scarpelli P, Ricci P, Distrutti E, Fiorucci S.

Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Oct;1864(10):1422-1437. doi: 10.1016/j.bbalip.2019.07.006. Epub 2019 Jul 17.

PMID:
31325638
2.

GPBAR1 Functions as Gatekeeper for Liver NKT Cells and provides Counterregulatory Signals in Mouse Models of Immune-Mediated Hepatitis.

Biagioli M, Carino A, Fiorucci C, Marchianò S, Di Giorgio C, Roselli R, Magro M, Distrutti E, Bereshchenko O, Scarpelli P, Zampella A, Fiorucci S.

Cell Mol Gastroenterol Hepatol. 2019;8(3):447-473. doi: 10.1016/j.jcmgh.2019.06.003. Epub 2019 Jun 18.

3.

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;256:137-165. doi: 10.1007/164_2019_237. Review.

PMID:
31201554
4.

Transcriptome Analysis of Dual FXR and GPBAR1 Agonism in Rodent Model of NASH Reveals Modulation of Lipid Droplets Formation.

Carino A, Marchianò S, Biagioli M, Fiorucci C, Zampella A, Monti MC, Morretta E, Bordoni M, Di Giorgio C, Roselli R, Ricci P, Distrutti E, Fiorucci S.

Nutrients. 2019 May 21;11(5). pii: E1132. doi: 10.3390/nu11051132.

5.

Characterisation of the Dynamic Interactions between Complex N-Glycans and Human CD22.

Di Carluccio C, Crisman E, Manabe Y, Forgione RE, Lacetera A, Amato J, Pagano B, Randazzo A, Zampella A, Lanzetta R, Fukase K, Molinaro A, Crocker PR, Martín-Santamaría S, Marchetti R, Silipo A.

Chembiochem. 2019 May 16. doi: 10.1002/cbic.201900295. [Epub ahead of print]

PMID:
31095840
6.

Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists.

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

ACS Med Chem Lett. 2019 Jan 10;10(4):504-510. doi: 10.1021/acsmedchemlett.8b00534. eCollection 2019 Apr 11.

PMID:
30996787
7.

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
8.

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.

9.

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.

10.

Agonism for the bile acid receptor GPBAR1 reverses liver and vascular damage in a mouse model of steatohepatitis.

Carino A, Marchianò S, Biagioli M, Bucci M, Vellecco V, Brancaleone V, Fiorucci C, Zampella A, Monti MC, Distrutti E, Fiorucci S.

FASEB J. 2019 Feb;33(2):2809-2822. doi: 10.1096/fj.201801373RR. Epub 2018 Oct 10.

PMID:
30303744
11.

Bile Acids Activated Receptors Regulate Innate Immunity.

Fiorucci S, Biagioli M, Zampella A, Distrutti E.

Front Immunol. 2018 Aug 13;9:1853. doi: 10.3389/fimmu.2018.01853. eCollection 2018. Review.

12.

Farnesoid X receptor modulators 2014-present: a patent review.

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

Expert Opin Ther Pat. 2018 May;28(5):351-364. doi: 10.1080/13543776.2018.1459569. Epub 2018 Apr 13. Review.

PMID:
29649907
13.

Disruption of TFGβ-SMAD3 pathway by the nuclear receptor SHP mediates the antifibrotic activities of BAR704, a novel highly selective FXR ligand.

Carino A, Biagioli M, Marchianò S, Scarpelli P, Zampella A, Limongelli V, Fiorucci S.

Pharmacol Res. 2018 May;131:17-31. doi: 10.1016/j.phrs.2018.02.033. Epub 2018 Mar 9.

PMID:
29530598
14.

Gpbar1 agonism promotes a Pgc-1α-dependent browning of white adipose tissue and energy expenditure and reverses diet-induced steatohepatitis in mice.

Carino A, Cipriani S, Marchianò S, Biagioli M, Scarpelli P, Zampella A, Monti MC, Fiorucci S.

Sci Rep. 2017 Oct 20;7(1):13689. doi: 10.1038/s41598-017-13102-y.

15.

The Bile Acid Receptor GPBAR1 Regulates the M1/M2 Phenotype of Intestinal Macrophages and Activation of GPBAR1 Rescues Mice from Murine Colitis.

Biagioli M, Carino A, Cipriani S, Francisci D, Marchianò S, Scarpelli P, Sorcini D, Zampella A, Fiorucci S.

J Immunol. 2017 Jul 15;199(2):718-733. doi: 10.4049/jimmunol.1700183. Epub 2017 Jun 12.

16.

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.

17.

Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics.

Capolupo A, Esposito R, Zampella A, Festa C, Riccio R, Casapullo A, Tosco A, Monti MC.

J Nat Prod. 2017 Apr 28;80(4):909-915. doi: 10.1021/acs.jnatprod.6b00793. Epub 2017 Mar 3.

PMID:
28256837
18.

Hyodeoxycholic acid derivatives as liver X receptor α and G-protein-coupled bile acid receptor agonists.

De Marino S, Carino A, Masullo D, Finamore C, Marchianò S, Cipriani S, Di Leva FS, Catalanotti B, Novellino E, Limongelli V, Fiorucci S, Zampella A.

Sci Rep. 2017 Feb 24;7:43290. doi: 10.1038/srep43290.

19.

BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis.

Carino A, Cipriani S, Marchianò S, Biagioli M, Santorelli C, Donini A, Zampella A, Monti MC, Fiorucci S.

Sci Rep. 2017 Feb 16;7:42801. doi: 10.1038/srep42801.

20.

Decoding the role of the nuclear receptor SHP in regulating hepatic stellate cells and liver fibrogenesis.

Cipriani S, Carino A, Masullo D, Zampella A, Distrutti E, Fiorucci S.

Sci Rep. 2017 Jan 24;7:41055. doi: 10.1038/srep41055.

21.

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.

22.

The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines.

Carino A, Graziosi L, D'Amore C, Cipriani S, Marchianò S, Marino E, Zampella A, Rende M, Mosci P, Distrutti E, Donini A, Fiorucci S.

Oncotarget. 2016 Sep 20;7(38):61021-61035. doi: 10.18632/oncotarget.10477.

23.

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.

24.

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.

25.

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.

PMID:
26607331
26.

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.

27.

Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1.

Renga B, Cipriani S, Carino A, Simonetti M, Zampella A, Fiorucci S.

PLoS One. 2015 Nov 5;10(11):e0141082. doi: 10.1371/journal.pone.0141082. eCollection 2015.

28.

Farnesoid X receptor modulators (2011 - 2014): a patent review.

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

Expert Opin Ther Pat. 2015;25(8):885-96. doi: 10.1517/13543776.2015.1045413. Review.

PMID:
26183029
29.

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.

30.

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.

PMID:
26132522
31.

Cystathionine γ-lyase, a H2S-generating enzyme, is a GPBAR1-regulated gene and contributes to vasodilation caused by secondary bile acids.

Renga B, Bucci M, Cipriani S, Carino A, Monti MC, Zampella A, Gargiulo A, d'Emmanuele di Villa Bianca R, Distrutti E, Fiorucci S.

Am J Physiol Heart Circ Physiol. 2015 Jul 1;309(1):H114-26. doi: 10.1152/ajpheart.00087.2015. Epub 2015 May 1.

32.

Molecular decodification of gymnemic acids from Gymnema sylvestre. Discovery of a new class of liver X receptor antagonists.

Renga B, Festa C, De Marino S, Di Micco S, D'Auria MV, Bifulco G, Fiorucci S, Zampella A.

Steroids. 2015 Apr;96:121-31. doi: 10.1016/j.steroids.2015.01.024. Epub 2015 Feb 7.

PMID:
25668616
33.

Theonellasterone, a steroidal metabolite isolated from a Theonella sponge, protects peroxiredoxin-1 from oxidative stress reactions.

Margarucci L, Monti MC, Tosco A, Esposito R, Zampella A, Sepe V, Mozzicafreddo M, Riccio R, Casapullo A.

Chem Commun (Camb). 2015 Jan 31;51(9):1591-3. doi: 10.1039/c4cc09205h.

PMID:
25503482
34.

Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands.

Festa C, Renga B, D'Amore C, Sepe V, Finamore C, De Marino S, Carino A, Cipriani S, Monti MC, Zampella A, Fiorucci S.

J Med Chem. 2014 Oct 23;57(20):8477-95. doi: 10.1021/jm501273r. Epub 2014 Oct 9.

PMID:
25247751
35.

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.

PMID:
25162837
36.

Bioactive cembrane derivatives from the Indian Ocean soft coral, Sinularia kavarattiensis.

Lillsunde KE, Festa C, Adel H, De Marino S, Lombardi V, Tilvi S, Nawrot DA, Zampella A, D'Souza L, D'Auria MV, Tammela P.

Mar Drugs. 2014 Jul 3;12(7):4045-68. doi: 10.3390/md12074045.

37.

Marine and semi-synthetic hydroxysteroids as new scaffolds for pregnane X receptor modulation.

Sepe V, Di Leva FS, D'Amore C, Festa C, De Marino S, Renga B, D'Auria MV, Novellino E, Limongelli V, D'Souza L, Majik M, Zampella A, Fiorucci S.

Mar Drugs. 2014 May 27;12(6):3091-115. doi: 10.3390/md12063091.

38.

Incisterols, highly degraded marine sterols, are a new chemotype of PXR agonists.

Chianese G, Sepe V, Limongelli V, Renga B, D'Amore C, Zampella A, Taglialatela-Scafati O, Fiorucci S.

Steroids. 2014 May;83:80-5. doi: 10.1016/j.steroids.2014.02.003. Epub 2014 Feb 28.

PMID:
24582706
39.

Plakilactones G and H from a marine sponge. Stereochemical determination of highly flexible systems by quantitative NMR-derived interproton distances combined with quantum mechanical calculations of (13)C chemical shifts.

Di Micco S, Zampella A, D'Auria MV, Festa C, De Marino S, Riccio R, Butts CP, Bifulco G.

Beilstein J Org Chem. 2013 Dec 30;9:2940-9. doi: 10.3762/bjoc.9.331. eCollection 2013 Dec 30.

40.

Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges.

Sepe V, D'Amore C, Ummarino R, Renga B, D'Auria MV, Novellino E, Sinisi A, Taglialatela-Scafati O, Nakao Y, Limongelli V, Zampella A, Fiorucci S.

Eur J Med Chem. 2014 Feb 12;73:126-34. doi: 10.1016/j.ejmech.2013.12.005. Epub 2013 Dec 15.

PMID:
24388834
41.

Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors.

D'Amore C, Di Leva FS, Sepe V, Renga B, Del Gaudio C, D'Auria MV, Zampella A, Fiorucci S, Limongelli V.

J Med Chem. 2014 Feb 13;57(3):937-54. doi: 10.1021/jm401873d. Epub 2014 Jan 17.

PMID:
24387325
42.

Solomonsterol A, a marine pregnane-X-receptor agonist, attenuates inflammation and immune dysfunction in a mouse model of arthritis.

Mencarelli A, D'Amore C, Renga B, Cipriani S, Carino A, Sepe V, Perissutti E, D'Auria MV, Zampella A, Distrutti E, Fiorucci S.

Mar Drugs. 2013 Dec 24;12(1):36-53. doi: 10.3390/md12010036.

43.

Structural insights into Estrogen Related Receptor-β modulation: 4-methylenesterols from Theonella swinhoei sponge as the first example of marine natural antagonists.

Di Micco S, Renga B, Carino A, D'Auria MV, Zampella A, Riccio R, Fiorucci S, Bifulco G.

Steroids. 2014 Feb;80:51-63. doi: 10.1016/j.steroids.2013.11.017. Epub 2013 Dec 4.

PMID:
24315836
44.

New tridecapeptides of the theonellapeptolide family from the Indonesian sponge Theonella swinhoei.

Sinisi A, Calcinai B, Cerrano C, Dien HA, Zampella A, D'Amore C, Renga B, Fiorucci S, Taglialatela-Scafati O.

Beilstein J Org Chem. 2013 Aug 13;9:1643-51. doi: 10.3762/bjoc.9.188. eCollection 2013.

45.

FXR mediates a chromatin looping in the GR promoter thus promoting the resolution of colitis in rodents.

Renga B, D'Amore C, Cipriani S, Mencarelli A, Carino A, Sepe V, Zampella A, Distrutti E, Fiorucci S.

Pharmacol Res. 2013 Nov;77:1-10. doi: 10.1016/j.phrs.2013.08.008. Epub 2013 Sep 1.

PMID:
24004655
46.

Heteronemin, a marine sponge terpenoid, targets TDP-43, a key factor in several neurodegenerative disorders.

Cassiano C, Esposito R, Tosco A, Zampella A, D'Auria MV, Riccio R, Casapullo A, Monti MC.

Chem Commun (Camb). 2014 Jan 14;50(4):406-8. doi: 10.1039/c3cc45454a.

PMID:
23963116
47.

Isoswinholide B and swinholide K, potently cytotoxic dimeric macrolides from Theonella swinhoei.

Sinisi A, Calcinai B, Cerrano C, Dien HA, Zampella A, D'Amore C, Renga B, Fiorucci S, Taglialatela-Scafati O.

Bioorg Med Chem. 2013 Sep 1;21(17):5332-8. doi: 10.1016/j.bmc.2013.06.015. Epub 2013 Jun 15.

PMID:
23830699
48.

Oxygenated polyketides from Plakinastrella mamillaris as a new chemotype of PXR agonists.

Festa C, D'Amore C, Renga B, Lauro G, De Marino S, D'Auria MV, Bifulco G, Zampella A, Fiorucci S.

Mar Drugs. 2013 Jul 2;11(7):2314-27. doi: 10.3390/md11072314.

49.

Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands.

Di Leva FS, Festa C, D'Amore C, De Marino S, Renga B, D'Auria MV, Novellino E, Limongelli V, Zampella A, Fiorucci S.

J Med Chem. 2013 Jun 13;56(11):4701-17. doi: 10.1021/jm400419e. Epub 2013 May 24.

PMID:
23656455
50.

Perthamide C inhibits eNOS and iNOS expression and has immunomodulating activity in vivo.

Bucci M, Cantalupo A, Vellecco V, Panza E, Monti MC, Zampella A, Ianaro A, Cirino G.

PLoS One. 2013;8(3):e57801. doi: 10.1371/journal.pone.0057801. Epub 2013 Mar 12. Retraction in: PLoS One. 2019 Aug 30;14(8):e0222175.

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