A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
J Med Chem
; 49(18): 5404-7, 2006 Sep 07.
Article
em En
| MEDLINE
| ID: mdl-16942012
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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Base de dados:
MEDLINE
Assunto principal:
Receptores de Estrogênio
/
Fluorenos
Limite:
Humans
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article