Estrogen biology: new insights into GPER function and clinical opportunities.
Estrogen biology: new insights into GPER function and clinical opportunities.
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DOI：
10.1016/j.mce.2014.02.002
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发表时间：
2014-05-25
影响因子：
4.1
通讯作者：
Barton M
中科院分区：
文献类型：
--
作者：
Prossnitz ER;Barton M
Estrogens play an important role in the regulation of normal physiology, aging and many disease states. Although the nuclear estrogen receptors have classically been described to function as ligand-activated transcription factors mediating genomic effects in hormonally regulated tissues, more recent studies reveal that estrogens also mediate rapid signaling events traditionally associated with G protein-coupled receptors. The G protein-coupled estrogen receptor GPER (formerly GPR30) has now become recognized as a major mediator of estrogen’s rapid cellular effects throughout the body. With the discovery of selective synthetic ligands for GPER, both agonists and antagonists, as well as the use of GPER knockout mice, significant advances have been made in our understanding of GPER function at the cellular, tissue and organismal levels. In many instances, the protective/beneficial effects of estrogen are mimicked by selective GPER agonism and are absent or reduced in GPER knockout mice, suggesting an essential or at least parallel role for GPER in the actions of estrogen. In this review, we will discuss recent advances and our current understanding of the role of GPER and certain drugs such as SERMs and SERDs in physiology and disease. We will also highlight novel opportunities for clinical development towards GPER-targeted therapeutics, for molecular imaging, as well as for theranostic approaches and personalized medicine.
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影响因子：
5
作者：
Abdelhamid, Ramy;Luo, Jia;VandeVrede, Lawren;Kundu, Indraneel;Michalsen, Bradley;Litosh, Vladislav A.;Schiefer, Isaac T.;Gherezghiher, Teshome;Yao, Ping;Qin, Zhihui;Thatcher, Gregory R. J.
通讯作者：
Thatcher, Gregory R. J.
DOI：
10.1007/978-1-4614-2364-5_4
发表时间：
2012-01-01
期刊：
RAMPS
影响因子：
--
作者：
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通讯作者：
Henley, Jeremy M.
影响因子：
3.7
作者：
Burai, Ritwik;Ramesh, Chinnasamy;Arterburn, Jeffrey B.
通讯作者：
Arterburn, Jeffrey B.
影响因子：
7.3
作者：
Alexander, Stephen P. H.;Mathie, Alistair;Peters, John A.
通讯作者：
Peters, John A.
影响因子：
3
作者：
Barton, Matthias;Meyer, Matthias R.;Prossnitz, Eric R.
通讯作者：
Prossnitz, Eric R.