Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 18, Pages 5404-5407Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060516e
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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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