TY - JOUR
T1 - Antiestrogens
T2 - Studies using an in vitro estrogen-responsive uterine system
AU - Katzenellebogen, Benita S.
AU - Katzenellenbogen, John A.
N1 - Funding Information:
* Supported by National Institutes
PY - 1973/2/20
Y1 - 1973/2/20
N2 - 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.
AB - 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.
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U2 - 10.1016/0006-291X(73)91526-X
DO - 10.1016/0006-291X(73)91526-X
M3 - Article
C2 - 4347895
AN - SCOPUS:0015930569
SN - 0006-291X
VL - 50
SP - 1152
EP - 1159
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 4
ER -