Three antiestrogens have been tested in vitro for their capacity to affect the cytosol binding and nuclear uptake of 17β-estradiol (E2) and induction of the synthesis of a specific uterine protein (IP). CI-628 competes with E2 for binding sites, inhibits IP induction, and is itself much less effective than E2 in promoting the IP response; U-11, 100A is a binding competitor and a weak inducer of IP synthesis, but does not antagonize the E2-induced IP response. Dimethylstilbestrol is an effective inhibitor of E2 binding, elicits a high IP response, but does not antagonize E2-induced IP synthesis. Higher concentrations of antiestrogens are required to inhibit nuclear binding of E2 than expected from their relative binding ability to cytosol.
|Original language||English (US)|
|Number of pages||8|
|Journal||Biochemical and Biophysical Research Communications|
|State||Published - Feb 20 1973|
ASJC Scopus subject areas
- Molecular Biology
- Cell Biology