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Estrogen receptors alpha (ERalpha) and beta (ERbeta) have distinct functions and differential expression in certain tissues. These differences have stimulated the search for subtype-selective ligands. Therapeutically, such ligands offer the potential to target specific tissues or pathways regulated by one receptor subtype without affecting the other. As(More)
Radiolabeled estrogens 17 beta-[3H]estradiol and diethylstilbestrol ( [3H]DES) and the antiestrogen [3H]monohydroxytamoxifen ( [3H]MHT) all bind with high affinity to the extranuclear estrogen receptor (ER) from the MCF-7 human breast tumor cell line (Kd = 3 X 10(-10), 2 X 10(-10), and 0.63 X 10(-10) M, respectively). A polyclonal antibody raised in a goat(More)
This study compares the specific uptake and retention of the Z and E isomers of 17 alpha-iodovinyl-11 beta-methoxyestradiol (IVME2) in estrogen target tissues in immature female rats following intraperitoneal injection. Estrogen receptor binding studies in vitro showed that the Z-IVME2 had greater affinity than the E-IVME2, but our initial in vivo data,(More)
In order to assess prostatic tissue as a target for receptor-mediated estrogen action, we have examined the regulation of estrogen (ER) and progestin receptors (PgR) by estrogen, antiestrogen, and progesterone in cytosolic and nuclear fractions of the R3327H (Dunning) prostatic adenocarcinoma of the rat. Twenty micrograms diethylstilbestrol (DES) with or(More)
SUMMARY The potent antiestrogen, Parke-Davis CI628, was evalu ated for its ability to effect regression of 7,12-dimethyl benz(a)anthracene-induced mammary tumors in the Sprague-Dawley rat. Chronic administration of this anties trogen resulted in regression of the majority of the tumors; about one-fourth of the tumors disappeared. The desired inhibition of(More)
A series of three 1,1-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)-ethylene derivatives was prepared and evaluated as potential estrogen receptor imaging agents. The compounds display high binding affinity compared to estradiol, with the 2-iodo and 2-bromo-derivatives expressing higher affinity than the parent 2-nonhalogenated derivative. Evaluation in immature(More)
As part of our program to develop novel ligands for the estrogen receptor, we synthesized the series of isomeric 17alpha-(trifluoromethyl)phenylvinyl estradiols using our solid-phase organic synthesis methodology. The compounds were evaluated for their relative binding affinity (RBA) using the ERalpha-LBD and in vivo potency using the immature rat(More)
While theoretically feasible, estrogen receptor (ER)-directed radiotherapy of hormone-dependent cancers has not been realized because no ER-seeking ligand with an appropriate radiotoxic potential has been identified. Since an appropriate nuclide is a key component we studied the 4.4-h half-life, Auger electron-emitting nuclide bromine-80m. When incorporated(More)