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Effect of estrogens and antiestrogens (AEs) on estrogen receptor (ER) half-life was analyzed in MCF-7 cells by assessing its progressive disappearance after covalent labeling in situ with [ 3 H]tamoxifen aziridine ([ 3 H]TAZ). Cells were incubated for 1 h with 20 nM [ 3 H]TAZ either in the absence or presence of a 500-fold excess of unlabeled estradiol (E 2 ) (non-specific...
Two 11β-derivatives of estradiol (E 2 ) were tested for their potential antiestrogenic activity in the MCF-7 breast cancer model: one contained a phenoxydimethylaminoethyl side-chain (RU 39 411), the other a pentafluoropentylsulfinyl side-chain (RU 58 668). The former compound displayed mixed estrogenic/antiestrogenic properties, while the latter indicated only an antiestrogenic activity...
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