雌激素受体GPER在乳腺癌中的研究现状

Research Status of Estrogen Receptor GPER in Breast Cancer

G蛋白偶联雌激素受体(G protein-coupled estrogen receptor,GPER,也称GPR30)在多种类型细胞中均可介导雌激素信号,其在乳腺癌、子宫内膜癌等激素敏感性肿瘤细胞中的作用尤为明显。雌激素及抗雌激素药物通过激活GPER促进下游信号通路的活化及靶基因的表达进而参与乳腺癌细胞的增殖、迁移、侵袭及他莫昔芬耐药等恶性生物学行为。目前发现表皮生长因子受体(epidermal growth factor receptor,EGFR)的转活是GPER引发下游生物学效应的关键靶点。此外,GPER还被认为是预测三阴乳腺癌患者预后的潜在生物学标志物之一,对GPER的深入研究可能为乳腺癌患者的综合性评估和临床治疗打开更广阔的前景。

The G protein-coupled estrogen receptor(GPER or GPR30) mediates estrogenic signal in different cell types, especially in the hormone-sensitive tumors including breast cancer and endometrial carcinoma. Estrogens and anti-estrogens promote the activation of the downstream signaling pathways and the expression of target genes through activating GPER, which involves in the malignant biological behaviors of breast cancer cells, such as cell proliferation, migration, invasion and tamoxifen resistance, etc. It has been reported that the key target for GPER signal to enhance the biological effects of its downstream is the transactivation of epidermal growth factor receptor(EGFR). Moreover, GPER has also been proposed as a candidate biomarker in the prognosis prediction of triple-negative breast cancer, opening broad prospects for a more comprehensive assessment and treatment of breast tumor patients.