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- W1969131445 abstract "The human mammary cancer cell line MCF-7 in culture was used to study the effect of tamoxifen and its derivatives: 4-hydroxytamoxifen (4-OH-Tam), N-desmethyltamoxifen (Dem-Tam) and cis-tamoxifen (cis-Tam) on the uptake and conversion of [3H]estrone sulfate (3H-E,S) to estradiol (E2). When [3H]-E1S (4 × 10−9 M) was incubated by itself (control) a great proportion of the radioactivity was found as [3H]E2, predominantly in the nuclear fraction. All of the antiestrogens (10−6 M–10−5 M) studied decreased the total uptake of radioactivity by the cells by 50–60% and the quantity of E2 formed. The calculated concentrations (in pg/mg DNA ± S.E.M.) of E2 (cytosol + 0.6 M KCl nuclear extract) with the anti-estrogens at 10−5 M were as follows: control 56 ± 3; Tam treated cells 4 ± 1; + 4-OH-Tam 2 ± 1; + Dem-Tam 5 ± 2; + cis-Tam 8 ± 4. A significant decrease in the concentrations of E2 was also observed in the mitochondria-microsomal fractions after the different treatments. It is suggested that the MCF-7 cells can use estrone-3-sulfate as a source of E2 and that the inhibitory effect of tamoxifen and its derivatives on the conversion of this sulfate to E2 could be involved in the anti-estrogenic process of these triphenylethylene derivatives." @default.
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- W1969131445 date "1988-06-01" @default.
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- W1969131445 title "Effect of tamoxifen and tamoxifen derivatives on the conversion of estrone sulfate to estradiol in the MCF-7 mammary cancer cell line" @default.
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- W1969131445 doi "https://doi.org/10.1016/0304-3835(88)90001-8" @default.
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