A strategy to obtain a fully orthogonal estrogen-receptor-based gene switch responsive to molecules with acceptable pharmacological properties is presented. From a series of tetrahydrofluorenones active on the wild-type estrogen receptor (ER) an inactive analogue is chosen as a new lead compound. Coevolution of receptor mutants and ligands leads to an ER-based gene switch suitable for studies in animal models.
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies / O. Kinzel, D. Fattori, E. Muraglia, P. Gallinari, M.C. Nardi, C. Paolini, G. Roscilli, C. Toniatti, O. Gonzalez Paz, R. Laufer, A. Lahm, A. Tramontano, R. Cortese, R. De Francesco, G. Ciliberto, U. Koch. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 49:18(2006), pp. 5404-5407.
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies
R. De Francesco;
2006
Abstract
A strategy to obtain a fully orthogonal estrogen-receptor-based gene switch responsive to molecules with acceptable pharmacological properties is presented. From a series of tetrahydrofluorenones active on the wild-type estrogen receptor (ER) an inactive analogue is chosen as a new lead compound. Coevolution of receptor mutants and ligands leads to an ER-based gene switch suitable for studies in animal models.
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