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A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies |
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| Authors: | 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 |
| Affiliation: | IRBM (Merck Research Laboratories Rome), Via Pontina km 30,600, 00040 Pomezia, Rome, Italy. olaf_kinzel@merck.com |
| 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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