Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells

R Lappano, C Rosano, P De Marco… - Molecular and cellular …, 2010 - Elsevier
… The action of E2 has been traditionally explained by the binding to the estrogen receptor (ER)
α and ERβ, however the G protein-coupled receptor (GPR) 30 has been recently involved …

Biology and receptor interactions of estriol and estriol derivatives in vitro and in vivo

BS Katzenellenbogen - Journal of Steroid Biochemistry, 1984 - Elsevier
… and effects of E, in vitro and in vivo. In these tissues and cells, E, has modest affinity for …
In human endometrium, we find that E, has an affinity for estrogen receptor 12% that of E, and …

Estriol and estradiol interactions with the estrogen receptor in vivo and in vitro

RE Müller, DM Beebe, E Bercel, AM Traish… - Journal of steroid …, 1984 - Elsevier
… In vim dissociation of these 2 estrogens from this nuclear bound receptor formed in viva …
5s estrogen receptor complexes causes rapid dissociation of E, or E,; this effect is dose-…

Estrogen receptor activation and the dissociation kinetics of estradiol, estriol, and estrone

BM WEICHMAN, AC NOTIDES - Endocrinology, 1980 - academic.oup.com
receptor produces the second, slower phase (9). In this report we analyze the binding kinetics
of estradiol, estriol, and estrone to the estrogen receptor … and effects on estrogen receptor

Estriol and estrone interaction with the estrogen receptor. II. Estriol and estrone-induced inhibition of the cooperative binding of [3H] estradiol to the estrogen receptor.

S Sasson, AC Notides - Journal of Biological Chemistry, 1983 - Elsevier
… to the estrogen receptor. We studied the effects of estriol and estrone on the positive
cooperativity of ['Hlestradiol binding to the partially purified, calf uterine estrogen receptor. The …

Effects of estriol on growth, gene expression and estrogen response element activation in human breast cancer cell lines

M Diller, S Schüler, S Buchholz, C Lattrich, O Treeck… - Maturitas, 2014 - Elsevier
… We used an established in vitro cell culture assay and compared the effect of E2 and E3
on growth of the estrogen receptor alpha-positive breast cancer cell lines MCF-7 and T-47D …

Contribution of estrogen receptors alpha and beta to the effects of estradiol in the brain

M Morissette, M Le Saux, M D'astous… - The Journal of steroid …, 2008 - Elsevier
… No or weak protective effects of estriol and estrone are observed for … estriol and estrone,
compared to 17β-E2, could explain the lack of weak neuroprotective activity of these estrogenic

Estrogen receptors and the estrone hypothesis in relation to endometrial and breast cancer

PK Siiteri, BE Schwarz, PC MacDonald - Gynecologic oncology, 1974 - Elsevier
… of the fact that estriol competes rather poorly with estradiol for receptor binding. However, …
above, it is of interest to examine the postulated protective effect of estriol more closely. As …

Estrogen receptor signaling mechanisms

N Fuentes, P Silveyra - Advances in protein chemistry and structural …, 2019 - Elsevier
… of estrogen receptor complexes to specific sequences in gene promoters (genomic effects),
or by … The hydroxylation of estradiol or 16α-hydroxyestrone forms estriol. In addition, catechol …

Effects of estrone, estradiol, and estriol on hormone-responsive human breast cancer in long-term tissue culture

M Lippman, ME Monaco, G Bolan - Cancer research, 1977 - AACR
… We conclude that estniol can bind to estrogen receptor and stimulate human breast
cancer in tissue culture. Our data do not support an antiestnogenic role for estniol in human …