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• W2017001467 abstract "Estrogen receptors (ERs) regulate gene transcription through classic estrogen response elements (EREs) as well as AP-1 responsive genes. The common SERMs Raloxifene, Tamoxifen, and ICI164384 function as ER antagonists on EREs but as ERβ agonists/partial agonists on AP-1 responsive genes. While developing a mutant selective analog of Raloxifene, that is an antagonist of ERα(E353A), we discovered an antagonist of wild-type ERα and ERβ that is also an antagonist of ERβ/AP-1 response. The analog, DRL527, represses basal AP-1 gene expression and antagonizes Raloxifene stimulated AP-1 expression. Therefore DRL527 has a unique, previously unreported, ERE/AP-1 activity profile." @default.
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• W2017001467 date "2010-09-01" @default.
• W2017001467 modified "2023-09-27" @default.
• W2017001467 title "A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements" @default.
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• W2017001467 doi "https://doi.org/10.1016/j.bmcl.2010.06.151" @default.
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