Article
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
Journal of medicinal chemistry - 7 Sept 2006
Kinzel Olaf, Fattori Daniela, Muraglia Ester, Gallinari Paola, Nardi Maria Chiara, Paolini Chantal, Roscilli Giuseppe, Toniatti Carlo, Gonzalez Paz Odalys, Laufer Ralph, Lahm Armin, Tramontano Anna, Cortese Riccardo, De Francesco Raffaele, Ciliberto Gennaro, Koch Uwe
Abstract excerpt
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....
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