A Structure-Guided Approach to an Orthogonal Estrogen-Receptor-Based Gene Switch Activated by Ligands Suitable for in Vivo Studies
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- 作者：Olaf Kinzel ; Daniela Fattori ; Ester Muraglia ; Paola Gallinari ; Maria Chiara Nardi ; Chantal Paolini ; Giuseppe Roscilli ; Carlo Toniatti ; Odalys Gonzalez Paz ; Ralph Laufer ; Armin Lahm ; Anna Tramontano ; R
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：September 7, 2006
- 年：2006
- 卷：49
- 期：18
- 页码：5404 - 5407
- 全文大小：152K
- 年卷期：v.49,no.18(September 7, 2006)
- ISSN：1520-4804
文摘
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 tetrahydrofluorenonesactive on the wild-type estrogen receptor (ER) an inactive analogue ischosen as a new lead compound. Coevolution of receptor mutants andligands leads to an ER-based gene switch suitable for studies in animalmodels.