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 / Olaf, Kinzel; Daniela, Fattori; Ester, Muraglia; Paola, Gallinari; Maria Chiara, Nardi; Chantal, Paolini; Giuseppe, Roscilli; Carlo, Toniatti; O., Gonzales Paz; Ralph, Laufer; Armin, Lahm; Tramontano, Anna; Riccardo, Cortese; Raffaele De, Francesco. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 49:18(2006), pp. 5404-5407. [10.1021/jm060516e]

A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies

TRAMONTANO, ANNA;
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.
2006
01 Pubblicazione su rivista::01a Articolo in rivista
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies / Olaf, Kinzel; Daniela, Fattori; Ester, Muraglia; Paola, Gallinari; Maria Chiara, Nardi; Chantal, Paolini; Giuseppe, Roscilli; Carlo, Toniatti; O., Gonzales Paz; Ralph, Laufer; Armin, Lahm; Tramontano, Anna; Riccardo, Cortese; Raffaele De, Francesco. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 49:18(2006), pp. 5404-5407. [10.1021/jm060516e]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/126973
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