Molina Luis, Figueroa Carlos D, Bhoola Kanti D, Ehrenfeld Pamela
a Laboratory of Cellular Pathology, Institute of Anatomy, Histology & Pathology , Universidad Austral de Chile , Valdivia , Chile.
Expert Opin Ther Targets. 2017 Aug;21(8):755-766. doi: 10.1080/14728222.2017.1350264. Epub 2017 Jul 12.
Breast cancer is clinically classified as 'estrogen-positive' when at least 1% of cancer cells stain for the estrogen receptor alpha (ERα). However, recent research on both basic and clinical aspects of breast cancer suggests that GPER-1 (G protein-coupled estrogen receptor-1) may have an important role in breast cancer. Areas covered: This review provides a comprehensive and systematic literature search on GPER-1. We have focused on the role of GPER-1 in breast cancer and on resistance to endocrine therapy, an unsolved clinical issue still under discussion. Expert opinion: The discovery of GPER-1 as a novel estrogen receptor is unique and the signaling pathways activated by its stimulation, when compared to the classical nuclear ERα, indicate a potential role of GPER-1 in the genesis and mechanisms of drug resistance in breast cancer. Tumors expressing ERα represent the largest group of breast cancer patients indicating that more women eventually die from ERα-positive breast tumors than from other more malignant breast cancer subtypes such as HER2-positive and the triple negative groups. It is important to develop new strategies on endocrine therapy with regard to ERα and GPER-1 receptors to achieve innovative successful therapeutic tools.
当至少1%的癌细胞雌激素受体α（ERα）染色呈阳性时，乳腺癌在临床上被分类为“雌激素阳性”。然而，最近关于乳腺癌基础和临床方面的研究表明，G蛋白偶联雌激素受体-1（GPER-1）可能在乳腺癌中发挥重要作用。涵盖领域：本综述对GPER-1进行了全面系统的文献检索。我们重点关注了GPER-1在乳腺癌中的作用以及对内分泌治疗的耐药性，这是一个仍在讨论中的未解决临床问题。专家观点：GPER-1作为一种新型雌激素受体的发现独具特色，与经典的核ERα相比，其刺激激活的信号通路表明GPER-1在乳腺癌的发生和耐药机制中具有潜在作用。表达ERα的肿瘤代表了最大的乳腺癌患者群体，这表明最终死于ERα阳性乳腺肿瘤的女性比死于其他恶性程度更高的乳腺癌亚型（如HER2阳性和三阴性组）的女性更多。针对ERα和GPER-1受体制定新的内分泌治疗策略以实现创新的成功治疗工具很重要。
