G蛋白偶联的雌激素受体在体内的表达与功能

In vivo expression and function of G protein-coupled estrogen receptor 1/G protein-coupled receptor 30

G蛋白偶联的雌激素受体(Gprotein-coupled estrogen receptor1,GPER)曾被命名为G蛋白偶联受体30(Gprotein-coupled receptor30,GPR30),是近年发现的一种有别于雌激素经典核受体的功能性膜性受体,该受体广泛表达于海马、下丘脑、子宫、卵巢、乳腺、骨和心血管等全身多个系统、器官和组织,在细胞内主要定位于细胞膜、内质网、线粒体和高尔基体。GPER与雌激素结合,通过激活胞外信号调节激酶(extracellular signal regulated kinase,ERK)、磷脂酰肌醇3-激酶/蛋白激酶B(phosphatidyl inositol 3 kinases/phosphorylated proteinkinaseB,PI3K/AKT)、Ca2+和环磷酸腺苷(3'-5'-cyclic adenosine monophosphate,cAMP)等第二信使途径发挥快速非基因效应,在神经系统、生殖系统、运动系统和心血管系统中发挥重要的生理作用。

GPER（G protein-coupled estrogen receptor 1）, once named GPR30 （G protein-coupled receptor 30）, is a novel functional membranous estrogen receptor identified recently. This receptor is structurally different from the classic nuclear estrogen receptors but it has been also found to be expressed extensively in a wide range of systems and organs including brain, reproductive organs, bone and cardiovascular systems, etc. Subcellularly, it is localized in endoplasmic reticulum, mitochondrion and Golgi apparatus. After binding to estrogen, GPER exerts its physiological function in the nervous, reproductive, locomotor and cardiovascular systems via the non-genomic pathway by activating the secondary messenger systems such as extracellular signal regulated kinase （ERK）, phosphatidylinositol 3 kinases/phosphorylated protein kinase B （PI3K/AKT）, Ca^2＋ and/or cyclic adenosine monophosphate （cAMP）.