A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
Article Details
- CitationCopy 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
Drug Target Property Measurement pH Temperature (°C) Estradiol Estrogen receptor alpha IC 50 (nM) 46 N/A N/A Details Estradiol Estrogen receptor alpha IC 50 (nM) 1.6 N/A N/A Details Estradiol Estrogen receptor beta IC 50 (nM) 1.4 N/A N/A Details