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LT175 is a novel PPARα/γ ligand with potent insulin-sensitizing effects and reduced adipogenic properties.
Gilardi F, Giudici M, Mitro N, Maschi O, Guerrini U, Rando G, Maggi A, Cermenati G, Laghezza A, Loiodice F, Pochetti G, Lavecchia A, Caruso D, De Fabiani E, Bamberg K, Crestani M. Gilardi F, et al. Among authors: laghezza a. J Biol Chem. 2014 Mar 7;289(10):6908-6920. doi: 10.1074/jbc.M113.506394. Epub 2014 Jan 22. J Biol Chem. 2014. PMID: 24451380 Free PMC article.
Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
Pochetti G, Godio C, Mitro N, Caruso D, Galmozzi A, Scurati S, Loiodice F, Fracchiolla G, Tortorella P, Laghezza A, Lavecchia A, Novellino E, Mazza F, Crestani M. Pochetti G, et al. Among authors: laghezza a. J Biol Chem. 2007 Jun 8;282(23):17314-24. doi: 10.1074/jbc.M702316200. Epub 2007 Apr 2. J Biol Chem. 2007. PMID: 17403688 Free article.
Molecular switch for CLC-K Cl- channel block/activation: optimal pharmacophoric requirements towards high-affinity ligands.
Liantonio A, Picollo A, Carbonara G, Fracchiolla G, Tortorella P, Loiodice F, Laghezza A, Babini E, Zifarelli G, Pusch M, Camerino DC. Liantonio A, et al. Among authors: laghezza a. Proc Natl Acad Sci U S A. 2008 Jan 29;105(4):1369-73. doi: 10.1073/pnas.0708977105. Epub 2008 Jan 23. Proc Natl Acad Sci U S A. 2008. PMID: 18216243 Free PMC article.
Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
Fracchiolla G, Lavecchia A, Laghezza A, Piemontese L, Trisolini R, Carbonara G, Tortorella P, Novellino E, Loiodice F. Fracchiolla G, et al. Among authors: laghezza a. Bioorg Med Chem. 2008 Nov 1;16(21):9498-510. doi: 10.1016/j.bmc.2008.09.045. Epub 2008 Sep 19. Bioorg Med Chem. 2008. PMID: 18835719
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: laghezza a. J Med Chem. 2008 Dec 25;51(24):7768-76. doi: 10.1021/jm800733h. J Med Chem. 2008. PMID: 19053776
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
Fracchiolla G, Laghezza A, Piemontese L, Tortorella P, Mazza F, Montanari R, Pochetti G, Lavecchia A, Novellino E, Pierno S, Conte Camerino D, Loiodice F. Fracchiolla G, et al. Among authors: laghezza a. J Med Chem. 2009 Oct 22;52(20):6382-93. doi: 10.1021/jm900941b. J Med Chem. 2009. PMID: 19775169
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