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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.
Molecular determinants for the activating/blocking actions of the 2H-1,4-benzoxazine derivatives, a class of potassium channel modulators targeting the skeletal muscle KATP channels.
Tricarico D, Mele A, Camerino GM, Laghezza A, Carbonara G, Fracchiolla G, Tortorella P, Loiodice F, Camerino DC. Tricarico D, et al. Among authors: laghezza a. Mol Pharmacol. 2008 Jul;74(1):50-8. doi: 10.1124/mol.108.046615. Epub 2008 Apr 10. Mol Pharmacol. 2008. PMID: 18403717
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
73 results