Conserved estrogen binding and signaling functions of the G protein-coupled estrogen receptor 1 (GPER) in mammals and fish.
Conserved estrogen binding and signaling functions of the G protein-coupled estrogen receptor 1 (GPER) in mammals and fish.
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DOI：
10.1016/j.steroids.2009.11.005
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发表时间：
2010-08
期刊：
影响因子：
2.7
通讯作者：
Berg, A. H.
中科院分区：
文献类型：
--
作者：
Thomas, P.;Alyea, R.;Pang, Y.;Peyton, C.;Dong, J.;Berg, A. H.
最近几个研究小组的研究表明，G蛋白雌激素受体-1，以前被称为GPR30，在多种人类癌细胞中介导17β-雌二醇(E_2)激活的信号转导通路，并表现出典型的膜雌激素受体的E_2结合。然而，GPER作为雌激素受体的重要性受到了奥托和他的同事的质疑。讨论了在研究重组类固醇膜受体功能方面的一些缺陷，这些缺陷可能解释了这些研究人员的否定结果。GPER的特性也已经在硬骨鱼大西洋鱼中进行了研究，在那里它被证明介导了E2对卵母细胞成熟的抑制。对新发现的远亲脊椎动物同源蛋白的研究对于确定其基本的、进化上保守的功能是有价值的。因此，对大黄鱼和人类GPERs的功能进行了比较。比较表明，大黄鱼和人GPER具有非常相似的雌激素结合特性，即典型的雌激素膜受体，并通过刺激性G蛋白(Gs)激活相同的雌激素信号通路，导致cAMP产生增加。这些结果表明，GPER的雌激素结合和雌激素信号传递功能在脊椎动物进化的早期就已经出现，早在硬骨鱼和四足动物分化之前，超过2亿年前。这一发现表明，在哺乳动物和鱼类这两个远亲脊椎动物中，通过GPER传递的雌激素膜信号在很长一段时间内都是保守的，这表明这是GPER在脊椎动物中的基本功能，并可能是其主要的生理作用。
Recent studies by several research groups have shown that G-protein estrogen receptor-1, GPER, formerly known as GPR30, mediates 17β-estradiol (E2) activation of signal transduction pathways in a variety of human cancer cells and displays E2 binding typical of a membrane estrogen receptor. However, the importance of GPER as an estrogen receptor has been questioned by Otto and coworkers. Some of the pitfalls in investigating the functions of recombinant steroid membrane receptors that may explain the negative results of these investigators are discussed. The characteristics of GPER have also been investigated in a teleost fish, Atlantic croaker, where it has been shown to mediate E2 inhibition of oocyte maturation. Investigations on newly discovered homologous proteins from distantly-related vertebrate groups are valuable for determining their fundamental, evolutionarily-conserved functions. Therefore, the functions of croaker and human GPERs were compared. The comparisons show that croaker and human GPER have very similar estrogen binding characteristics, typical of estrogen membrane receptors, and activate the same estrogen signaling pathways via stimulatory G proteins (Gs) resulting in increased cAMP production. These results suggest that the estrogen binding and estrogen signaling functions of GPER arose early in vertebrate evolution, prior to the divergence of the teleosts from the tetrapods, more than 200 million years ago. The finding that estrogen membrane signaling through GPER has been conserved for such a long period in two distantly-related vertebrate groups, mammals and fish, suggests that this is a fundamental function of GPER in vertebrates, and likely its major physiological role.
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影响因子：
3.6
作者：
Braun, AM;Thomas, P
通讯作者：
Thomas, P
影响因子：
15.9
作者：
Chen, Z;Yuhanna, IS;Shaul, PW
通讯作者：
Shaul, PW
影响因子：
2.7
作者：
Kim, Kyuny Hee;Moriarty, Katie;Bender, Jeffrey R.
通讯作者：
Bender, Jeffrey R.
DOI：
10.1016/s0960-0760(01)00190-x
发表时间：
2002-02-01
影响因子：
4.1
作者：
Filardo, EJ
通讯作者：
Filardo, EJ
影响因子：
--
作者：
Filardo, EJ;Quinn, JA;Bland, KI
通讯作者：
Bland, KI