GPER/GPR30 and Regulation of Vascular Tone and Blood Pressure.
GPER/GPR30 and Regulation of Vascular Tone and Blood Pressure.
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DOI：
10.2174/1871522211108040255
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发表时间：
2011
期刊：
影响因子：
--
通讯作者：
Barton M
中科院分区：
文献类型：
--
作者：
Meyer MR;Prossnitz ER;Barton M
17β-雌二醇等天然雌激素是内源性血管扩张剂，与高血压的性别差异有关。这些激素激活雌激素受体 ERα 和 ERβ，介导部分雌激素依赖性血管舒张。此外，还发现了一种新的 G 蛋白偶联雌激素结合受体，称为 GPER/GPR30，它在心血管系统中表达。使用选择性靶向 GPER/GPR30 的基因敲除动物或药物，已证明该受体作为涉及一氧化氮 (NO) 和降血压活性的急性雌激素依赖性血管舒张介质的重要作用。越来越多的证据表明，GPER/GPR30 负责控制血管张力，表明该受体可能代表绝经后女性（也可能是男性）高血压药物治疗的新药物靶点。
Natural estrogens such as 17β-estradiol are endogenous vasodilators and have been implicated in the gender differences of hypertension. These hormones activate estrogen receptors ERα and ERβ, which mediate part of estrogen-dependent vasodilation. In addition, a novel G protein-coupled estrogen-binding receptor termed GPER/GPR30 has been identified that is expressed in the cardiovascular system. Using knock-out animals or drugs selectively targeting GPER/GPR30, a significant role for this receptor as a mediator of acute estrogen-dependent vasodilation involving nitric oxide (NO) and blood pressure-lowering activity has been demonstrated. The accumulating evidence that GPER/GPR30 is responsible for control of vascular tone indicates that this receptor may represent a novel drug target for pharmacologic treatment of hypertension in postmenopausal women and possibly also men.