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Updated: Jul 20, 2026

Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters
Published on: November 26, 2013
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in
Olaf Kinzel1, Daniela Fattori, Ester Muraglia
1IRBM (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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