Facultad de Medicina y Ciencia, Universidad San Sebastián, Lago Panguipulli 1390, 5501842, Puerto Montt, Chile.
Laboratory of Cellular Pathology, Institute of Anatomy, Histology and Pathology, Universidad Austral de Chile, Valdivia, Chile.
Clin Sci (Lond). 2018 Dec 13;132(24):2583-2598. doi: 10.1042/CS20180885. Print 2018 Dec 21.
Estrogens generated within endocrine organs and the reproductive system act as ligands for at least three types of estrogen receptors. Estrogen receptors α (ERα) and β (ERβ) belong to the so-called classical family of estrogen receptors, whereas the G protein-coupled receptor GPR30, also known as GPER-1, has been described as a novel estrogen receptor sited in the cell membrane of target cells. Furthermore, these receptors are under stimulation of a family of exogenous estrogens, known as phytoestrogens, which are a diverse group of non-steroidal plant compounds derived from plant food consumed by humans and animals. Because phytoestrogens are omnipresent in our daily diet, they are becoming increasingly important in both human health and disease. Recent evidence indicates that in addition to classical estrogen receptors, phytoestrogens also activate GPER-1 a relevant observation since GPER-1 is involved in several physiopathological disorders and especially in estrogen-dependent diseases such as breast cancer.The first estrogen receptors discovered were the classical ERα and ERβ, but from an evolutionary point of view G protein-coupled receptors trace their origins in history to over a billion years ago suggesting that estrogen receptors like GPER-1 may have been the targets of choice for ancient phytoestrogens and/or estrogens.This review provides a comprehensive and systematic literature search on phytoestrogens and its relationship with classical estrogen receptors and GPER-1 including its role in breast cancer, an issue still under discussion.
内分沁器官和生殖系统产生的雌激素作为至少三种类型的雌激素受体的配体。雌激素受体 α (ERα) 和 β (ERβ) 属于经典的雌激素受体家族，而 G 蛋白偶联受体 GPR30，也称为 GPER-1，被描述为一种位于靶细胞细胞膜上的新型雌激素受体。此外，这些受体受到外源性雌激素（称为植物雌激素）的刺激，植物雌激素是一类非甾体植物化合物，源自人类和动物食用的植物性食物。由于植物雌激素在我们的日常饮食中无处不在，它们在人类健康和疾病中变得越来越重要。最近的证据表明，除了经典的雌激素受体外，植物雌激素还能激活 GPER-1，这是一个相关的观察结果，因为 GPER-1 参与了几种生理病理紊乱，特别是在乳腺癌等雌激素依赖性疾病中。最早发现的雌激素受体是经典的 ERα 和 ERβ，但从进化的角度来看，G 蛋白偶联受体的起源可以追溯到十亿多年前，这表明像 GPER-1 这样的雌激素受体可能是古代植物雌激素和/或雌激素的首选靶标。这篇综述提供了一个全面和系统的文献搜索关于植物雌激素及其与经典雌激素受体和 GPER-1 的关系，包括其在乳腺癌中的作用，这是一个仍在讨论的问题。
