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

被引：102

作者：

Lappano, Rosamaria ^{[1
]}

Rosano, Camillo ^{[2
]}

De Marco, Paola ^{[1
]}

De Francesco, Ernestina Marianna ^{[1
]}

Pezzi, Vincenzo ^{[1
]}

Maggiolini, Marcello ^{[1
]}

机构：

[1] Univ Calabria, Dipartimento Farmacobiol, I-87036 Arcavacata Di Rende, CS, Italy

[2] Ist Nazl Ric Cancro IST, Dipartimento Bioinformat & Prote Strutturale, Genoa, Italy

来源：

MOLECULAR AND CELLULAR ENDOCRINOLOGY | 2010年 / 320卷 / 1-2期

关键词：

Estriol; Estrogen receptor; GPR30; Estrogen signaling; Breast cancer cells; PROTEIN-COUPLED RECEPTOR; TISSUE-GROWTH-FACTOR; SEX-STEROID HORMONES; GENE-EXPRESSION; G-PROTEIN-COUPLED-RECEPTOR-30; GPR30; ESTRADIOL; 17-BETA-ESTRADIOL; WOMEN; MCF-7; ACTIVATION;

D O I：

10.1016/j.mce.2010.02.006

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

Estrogens are structurally related steroids that regulate important physiological processes. 17 beta-estradiol (E2) is reversibly oxidized to estrone (E1) and both E2 and E1 can be irreversibly converted to estriol (E3), which also originates directly from androstenedione. The action of E2 has been traditionally explained by the binding to the estrogen receptor (ER) alpha and ER beta, however the G protein-coupled receptor (GPR) 30 has been recently involved in the rapid signaling triggered by estrogens. Although the role of E2 in the development of breast cancer has been largely documented, the contribution of E3 still remains to be completely evaluated. Here, we demonstrate for the first time that E3 acts as a GPR30 antagonist since it was able to inhibit the GPR30-mediated responses such as the rapid ERK activation, the up-regulation of target genes like c-fos and connective tissue growth factor, the proliferative effects observed in ER-negative SkBr3 cells. (C) 2010 Elsevier Ireland Ltd. All rights reserved.

引用

页码：162 / 170

页数：9

共 71 条

[1] RETRACTED: G-Protein-Coupled Receptor 30 and Estrogen Receptor-α Are Involved in the Proliferative Effects Induced by Atrazine in Ovarian Cancer Cells (Retracted article. See vol. 122, pg. A42, 2014) [J].