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A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
Sblano S, Cerchia C, Laghezza A, Piemontese L, Brunetti L, Leuci R, Gilardi F, Thomas A, Genovese M, Santi A, Tortorella P, Paoli P, Lavecchia A, Loiodice F. Sblano S, et al. Among authors: gilardi f. Eur J Med Chem. 2022 May 5;235:114240. doi: 10.1016/j.ejmech.2022.114240. Epub 2022 Mar 16. Eur J Med Chem. 2022. PMID: 35325635
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.
Montanari R, Saccoccia F, Scotti E, Crestani M, Godio C, Gilardi F, Loiodice F, Fracchiolla G, Laghezza A, Tortorella P, Lavecchia A, Novellino E, Mazza F, Aschi M, Pochetti G. Montanari R, et al. Among authors: gilardi f. J Med Chem. 2008 Dec 25;51(24):7768-76. doi: 10.1021/jm800733h. J Med Chem. 2008. PMID: 19053776
Structural insight into peroxisome proliferator-activated receptor gamma binding of two ureidofibrate-like enantiomers by molecular dynamics, cofactor interaction analysis, and site-directed mutagenesis.
Pochetti G, Mitro N, Lavecchia A, Gilardi F, Besker N, Scotti E, Aschi M, Re N, Fracchiolla G, Laghezza A, Tortorella P, Montanari R, Novellino E, Mazza F, Crestani M, Loiodice F. Pochetti G, et al. Among authors: gilardi f. J Med Chem. 2010 Jun 10;53(11):4354-66. doi: 10.1021/jm9013899. J Med Chem. 2010. PMID: 20462215
Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
Porcelli L, Gilardi F, Laghezza A, Piemontese L, Mitro N, Azzariti A, Altieri F, Cervoni L, Fracchiolla G, Giudici M, Guerrini U, Lavecchia A, Montanari R, Di Giovanni C, Paradiso A, Pochetti G, Simone GM, Tortorella P, Crestani M, Loiodice F. Porcelli L, et al. Among authors: gilardi f. J Med Chem. 2012 Jan 12;55(1):37-54. doi: 10.1021/jm201306q. Epub 2011 Dec 2. J Med Chem. 2012. PMID: 22081932
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
Carrieri A, Giudici M, Parente M, De Rosas M, Piemontese L, Fracchiolla G, Laghezza A, Tortorella P, Carbonara G, Lavecchia A, Gilardi F, Crestani M, Loiodice F. Carrieri A, et al. Among authors: gilardi f. Eur J Med Chem. 2013 May;63:321-32. doi: 10.1016/j.ejmech.2013.02.015. Epub 2013 Feb 24. Eur J Med Chem. 2013. PMID: 23502212
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
Piemontese L, Fracchiolla G, Carrieri A, Parente M, Laghezza A, Carbonara G, Sblano S, Tauro M, Gilardi F, Tortorella P, Lavecchia A, Crestani M, Desvergne B, Loiodice F. Piemontese L, et al. Among authors: gilardi f. Eur J Med Chem. 2015 Jan 27;90:583-94. doi: 10.1016/j.ejmech.2014.11.044. Epub 2014 Nov 24. Eur J Med Chem. 2015. PMID: 25497132
110 results