G-1-Activated Membrane Estrogen Receptors Mediate Increased Contractility of the Human Myometrium
G-1-Activated Membrane Estrogen Receptors Mediate Increased Contractility of the Human Myometrium
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DOI：
10.1210/en.2010-0979
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发表时间：
2011-06-01
期刊：
影响因子：
4.8
通讯作者：
Smith, R.
中科院分区：
文献类型：
--
作者：
Maiti, K.;Paul, J. W.;Smith, R.
雌激素是分娩时子宫收缩力增强的关键介质。我们试图确定膜相关雌激素受体（例如最近描述的七次跨膜受体 G 蛋白偶联受体 30 (GPR30)）是否介导了部分这种效应。使用足月剖宫产术在临产前或临产后获得的人类子宫肌层，我们使用定量 RT-PCR 和蛋白质印迹法证明了 GPR30 mRNA 和蛋白质的存在。 GPR30 受体定位于细胞膜，通常与 calveolin-1 共定位。使用特定的雌激素膜受体激动剂 G-1 和子宫肌层外植体，我们发现膜受体激活导致 MAPK 和肌动蛋白修饰小热休克蛋白 27 磷酸化。使用与 G-1 或媒介物一起孵育的子宫肌条，我们证明雌激素膜受体激活增加了子宫肌层对催产素的收缩反应。这些数据表明，质膜雌激素受体 GPR30 的激活可能参与怀孕期间人类子宫肌层的生理学，并将其确定为改变子宫活动的潜在靶点。 （内分泌学152：2448-2455，2011）
Estrogens are key mediators of increased uterine contractility at labor. We sought to determine whether membrane-associated estrogen receptors, such as the recently described seven-transmembrane receptor G protein-coupled receptor 30 (GPR30), mediated some of this effect. Using human myometrium obtained at term cesarean section before or after the onset of labor, we demonstrated the presence of GPR30 mRNA and protein using quantitative RT-PCR and Western blotting. GPR30 receptor was localized to the cell membrane and often colocalized with calveolin-1. Using the specific estrogen membrane receptor agonist G-1 and myometrial explants, we showed that membrane receptor activation led to phosphorylation of MAPK and the actin-modifying small heat shock protein 27. Using myometrial strips incubated with G-1 or vehicle we demonstrated that estrogen membrane receptor activation increased the myometrial contractile response to oxytocin. These data suggest that activation of the plasma membrane estrogen receptor GPR30 likely participates in the physiology of the human myometrium during pregnancy and identifies it as a potential target to modify uterine activity. (Endocrinology 152: 2448-2455, 2011)