Antiestrogens: Studies using an in vitro estrogen-responsive uterine system

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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 languageEnglish (US)
Pages (from-to)1152-1159
Number of pages8
JournalBiochemical and Biophysical Research Communications
Issue number4
StatePublished - Feb 20 1973

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology


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