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

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, Riccardo Cortese, Raffaele De Francesco, Gennaro Ciliberto, Uwe Koch

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)5404-5407
Number of pages4
JournalJournal of Medicinal Chemistry
Volume49
Issue number18
DOIs
Publication statusPublished - Sep 7 2006

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Switch Genes
Estrogen Receptors
Genes
Switches
Ligands
Lead compounds
Animals
Animal Models
Pharmacology
Molecules

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

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

In: Journal of Medicinal Chemistry, Vol. 49, No. 18, 07.09.2006, p. 5404-5407.

Research output: Contribution to journalArticle

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 2006, 'A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies', Journal of Medicinal Chemistry, vol. 49, no. 18, pp. 5404-5407. https://doi.org/10.1021/jm060516e
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. / A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies. In: Journal of Medicinal Chemistry. 2006 ; Vol. 49, No. 18. pp. 5404-5407.
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AU - Nardi, Maria Chiara

AU - Paolini, Chantal

AU - Roscilli, Giuseppe

AU - Toniatti, Carlo

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AU - Laufer, Ralph

AU - Lahm, Armin

AU - Tramontano, Anna

AU - Cortese, Riccardo

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