Lappano Rosamaria, Pisano Assunta, Maggiolini Marcello
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria , Rende , Italy.
Front Endocrinol (Lausanne). 2014 May 6;5:66. doi: 10.3389/fendo.2014.00066. eCollection 2014.
The G-protein-coupled estrogen receptor-1 (GPER, formerly known as GPR30) has attracted increasing interest, considering its ability to mediate estrogenic signaling in different cell types, including the hormone-sensitive tumors like breast cancer. As observed for other GPCR-mediated responses, the activation of the epidermal growth factor receptor is a fundamental integration point in the biological action triggered by GPER. A wide number of natural and synthetic compounds, including estrogens and anti-estrogens, elicit stimulatory effects in breast cancer through GPER up-regulation and activation, suggesting that GPER function is associated with breast tumor progression and tamoxifen resistance. GPER has also been proposed as a candidate biomarker in triple-negative breast cancer, opening a novel scenario for a more comprehensive assessment of breast tumor patients.
G蛋白偶联雌激素受体1（GPER，以前称为GPR30）因其能够在包括乳腺癌等激素敏感性肿瘤在内的不同细胞类型中介导雌激素信号传导而越来越受到关注。正如其他GPCR介导的反应一样，表皮生长因子受体的激活是GPER触发的生物学作用中的一个基本整合点。大量天然和合成化合物，包括雌激素和抗雌激素，通过GPER上调和激活在乳腺癌中产生刺激作用，这表明GPER功能与乳腺肿瘤进展和他莫昔芬耐药性有关。GPER也被提议作为三阴性乳腺癌的候选生物标志物，为更全面评估乳腺肿瘤患者开辟了一个新的局面。
