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

Article Details

Citation
Copy to clipboard

Kinzel O, Fattori D, Muraglia E, Gallinari P, Nardi MC, Paolini C, Roscilli G, Toniatti C, Gonzalez Paz O, Laufer R, Lahm A, Tramontano A, Cortese R, De Francesco R, Ciliberto G, Koch U

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

J Med Chem. 2006 Sep 7;49(18):5404-7.

PubMed ID
16942012 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)46N/AN/ADetails
EstradiolEstrogen receptor alphaIC 50 (nM)1.6N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)1.4N/AN/ADetails