Pellicciari R - Search Results

1

Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists.

Marinozzi M, Carotti A, Sansone E, Macchiarulo A, Rosatelli E, Sardella R, Natalini B, Rizzo G, Adorini L, Passeri D, De Franco F, Pruzanski M, Pellicciari R. Marinozzi M, et al. Among authors: pellicciari r. Bioorg Med Chem. 2012 Jun 1;20(11):3429-45. doi: 10.1016/j.bmc.2012.04.021. Epub 2012 Apr 20. Bioorg Med Chem. 2012. PMID: 22564381

2

Molecular dynamics simulation of the ligand binding domain of farnesoid X receptor. Insights into helix-12 stability and coactivator peptide stabilization in response to agonist binding.

Costantino G, Entrena-Guadix A, Macchiarulo A, Gioiello A, Pellicciari R. Costantino G, et al. Among authors: pellicciari r. J Med Chem. 2005 May 5;48(9):3251-9. doi: 10.1021/jm049182o. J Med Chem. 2005. PMID: 15857131

3

Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.

Meyer U, Costantino G, Macchiarulo A, Pellicciari R. Meyer U, et al. Among authors: pellicciari r. J Med Chem. 2005 Nov 3;48(22):6948-55. doi: 10.1021/jm0505056. J Med Chem. 2005. PMID: 16250653

4

Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.

Pellicciari R, Gioiello A, Costantino G, Sadeghpour BM, Rizzo G, Meyer U, Parks DJ, Entrena-Guadix A, Fiorucci S. Pellicciari R, et al. J Med Chem. 2006 Jul 13;49(14):4208-15. doi: 10.1021/jm060294k. J Med Chem. 2006. PMID: 16821780

5

Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.

Pellicciari R, Sato H, Gioiello A, Costantino G, Macchiarulo A, Sadeghpour BM, Giorgi G, Schoonjans K, Auwerx J. Pellicciari R, et al. J Med Chem. 2007 Sep 6;50(18):4265-8. doi: 10.1021/jm070633p. Epub 2007 Aug 9. J Med Chem. 2007. PMID: 17685603

6

Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.

Pellicciari R, Gioiello A, Macchiarulo A, Thomas C, Rosatelli E, Natalini B, Sardella R, Pruzanski M, Roda A, Pastorini E, Schoonjans K, Auwerx J. Pellicciari R, et al. J Med Chem. 2009 Dec 24;52(24):7958-61. doi: 10.1021/jm901390p. J Med Chem. 2009. PMID: 20014870

7

Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.

Gioiello A, Macchiarulo A, Carotti A, Filipponi P, Costantino G, Rizzo G, Adorini L, Pellicciari R. Gioiello A, et al. Among authors: pellicciari r. Bioorg Med Chem. 2011 Apr 15;19(8):2650-8. doi: 10.1016/j.bmc.2011.03.004. Epub 2011 Mar 10. Bioorg Med Chem. 2011. PMID: 21459580

8

Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: role of the chirality on the biological activity.

Marinozzi M, Carotti A, Sardella R, Buonerba F, Ianni F, Natalini B, Passeri D, Rizzo G, Pellicciari R. Marinozzi M, et al. Among authors: pellicciari r. Bioorg Med Chem. 2013 Jul 1;21(13):3780-9. doi: 10.1016/j.bmc.2013.04.038. Epub 2013 Apr 23. Bioorg Med Chem. 2013. PMID: 23684233

9

Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.

Liscio P, Carotti A, Asciutti S, Karlberg T, Bellocchi D, Llacuna L, Macchiarulo A, Aaronson SA, Schüler H, Pellicciari R, Camaioni E. Liscio P, et al. Among authors: pellicciari r. J Med Chem. 2014 Mar 27;57(6):2807-12. doi: 10.1021/jm401356t. Epub 2014 Feb 24. J Med Chem. 2014. PMID: 24527792 Free PMC article.

10

Bile acid derivatives as ligands of the farnesoid x receptor: molecular determinants for bile acid binding and receptor modulation.

Gioiello A, Cerra B, Mostarda S, Guercini C, Pellicciari R, Macchiarulo A. Gioiello A, et al. Among authors: pellicciari r. Curr Top Med Chem. 2014;14(19):2159-74. doi: 10.2174/1568026614666141112100208. Curr Top Med Chem. 2014. PMID: 25388535 Review.

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