The G-protein-coupled estrogen receptor GPER in health and disease.
The G-protein-coupled estrogen receptor GPER in health and disease.
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G蛋白偶联的雌激素受体GPER在健康和疾病中。
DOI：
10.1038/nrendo.2011.122
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发表时间：
2011-08-16
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雌激素在整个身体中介导深远的影响，并调节女性和男性的生理和病理过程。绝经前妇女许多疾病发病率的降低归因于17β-雌二醇的存在，17 β-雌二醇是主要的和最有效的内源性雌激素。然而，除了内源性雌激素外，一些人造和植物衍生的分子也表现出雌激素活性。传统上，17β-雌二醇的作用归因于两种核雌激素受体（ER），ERα和ERβ，其作为配体激活的转录因子起作用。然而，17β-雌二醇也通过涉及跨膜ER的途径介导快速信号传导事件，如G蛋白偶联ER 1（GPER，以前称为GPR 30）。在过去的10年里，GPER被认为参与了快速信号传导和转录调控。随着在细胞实验和临床前研究中发现可以选择性调节GPER功能的GPER选择性配体，以及GPER敲除小鼠的使用，目前正在阐明GPER的更多潜在作用。本文综述了GPER在生殖、神经、内分泌、免疫和心血管系统中的生理作用，以及在包括癌症在内的多种疾病中的病理作用。GPER正在成为这些疾病的一个新的治疗靶点和预后指标。
Estrogens mediate profound effects throughout the body, and regulate physiological and pathological processes in both women and men. The decreased incidence of many diseases in premenopausal women is attributed to the presence of 17β-estradiol, the predominant and most potent endogenous estrogen. In addition to endogenous estrogens, however, several manmade and plant-derived molecules also exhibit estrogenic activity. Traditionally, the actions of 17β-estradiol are ascribed to two nuclear estrogen receptors (ERs), ERα and ERβ, which function as ligand-activated transcription factors. However, 17β-estradiol also mediates rapid signaling events via pathways that involve transmembrane ERs, such as G-protein-coupled ER 1, (GPER, formerly known as GPR30). In the past 10 years, GPER has been implicated in both rapid signaling and transcriptional regulation. With the discovery of GPER-selective ligands that can selectively modulate GPER function in cell experiments and preclinical studies, and the use of GPER-knockout mice, many more potential roles for GPER are currently being elucidated. This Review highlights the physiological roles of GPER in the reproductive, nervous, endocrine, immune and cardiovascular systems, as well as its pathological roles in a diverse array of disorders including cancer. GPER is emerging as a novel therapeutic target and prognostic indicator for these diseases.
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