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G protein-coupled oestrogen receptor 1 (GPER1)/GPR30: a new player in cardiovascular and metabolic oestrogenic signalling

Nilsson, Bengt-Olof LU ; Olde, Björn LU and Leeb-Lundberg, Fredrik LU (2011) In British Journal of Pharmacology 163(6). p.1131-1139
Abstract
Oestrogens are important sex hormones central to health and disease in both genders that have protective effects on the cardiovascular and metabolic systems. These hormones act in complex ways via both genomic and non-genomic mechanisms. The genomic mechanisms are relatively well characterized, whereas the non-genomic ones are only beginning to be explored. Two oestrogen receptors (ER), ER alpha and ER beta, have been described that act as nuclear transcription factors but can also associate with the plasma membrane and influence cytosolic signalling. ERa has been shown to mediate both anti-atherogenic effects and pro-survival effects in pancreatic beta-cells. In recent years, a third membrane-bound ER has emerged, G protein-coupled... (More)
Oestrogens are important sex hormones central to health and disease in both genders that have protective effects on the cardiovascular and metabolic systems. These hormones act in complex ways via both genomic and non-genomic mechanisms. The genomic mechanisms are relatively well characterized, whereas the non-genomic ones are only beginning to be explored. Two oestrogen receptors (ER), ER alpha and ER beta, have been described that act as nuclear transcription factors but can also associate with the plasma membrane and influence cytosolic signalling. ERa has been shown to mediate both anti-atherogenic effects and pro-survival effects in pancreatic beta-cells. In recent years, a third membrane-bound ER has emerged, G protein-coupled receptor 30 or G protein-coupled oestrogen receptor 1 (GPER1), which mediates oestrogenic responses in cardiovascular and metabolic regulation. Both GPER1 knock-out models and pharmacological agents are now available to study GPER1 function. These tools have revealed that GPER1 activation may have several beneficial effects in the cardiovascular system including vasorelaxation, inhibition of smooth muscle cell proliferation, and protection of the myocardium against ischaemia/reperfusion injury, and in the metabolic system including stimulation of insulin release and protection against pancreatic beta-cell apoptosis. Thus, GPER1 is emerging as a candidate therapeutic target in both cardiovascular and metabolic disease. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
G protein-coupled receptor, oestrogen, cardiovascular regulation, metabolic regulation, cellular signalling, non-genomic mechanisms
in
British Journal of Pharmacology
volume
163
issue
6
pages
1131 - 1139
publisher
The British Pharmacological Society
external identifiers
  • wos:000292098700007
  • scopus:79959768665
  • pmid:21250980
ISSN
1476-5381
DOI
10.1111/j.1476-5381.2011.01235.x
language
English
LU publication?
yes
id
45edea0d-7eb5-45e5-8c42-85b7bd9bee3d (old id 2049193)
date added to LUP
2011-08-02 08:59:34
date last changed
2017-09-10 03:53:20
@article{45edea0d-7eb5-45e5-8c42-85b7bd9bee3d,
  abstract     = {Oestrogens are important sex hormones central to health and disease in both genders that have protective effects on the cardiovascular and metabolic systems. These hormones act in complex ways via both genomic and non-genomic mechanisms. The genomic mechanisms are relatively well characterized, whereas the non-genomic ones are only beginning to be explored. Two oestrogen receptors (ER), ER alpha and ER beta, have been described that act as nuclear transcription factors but can also associate with the plasma membrane and influence cytosolic signalling. ERa has been shown to mediate both anti-atherogenic effects and pro-survival effects in pancreatic beta-cells. In recent years, a third membrane-bound ER has emerged, G protein-coupled receptor 30 or G protein-coupled oestrogen receptor 1 (GPER1), which mediates oestrogenic responses in cardiovascular and metabolic regulation. Both GPER1 knock-out models and pharmacological agents are now available to study GPER1 function. These tools have revealed that GPER1 activation may have several beneficial effects in the cardiovascular system including vasorelaxation, inhibition of smooth muscle cell proliferation, and protection of the myocardium against ischaemia/reperfusion injury, and in the metabolic system including stimulation of insulin release and protection against pancreatic beta-cell apoptosis. Thus, GPER1 is emerging as a candidate therapeutic target in both cardiovascular and metabolic disease.},
  author       = {Nilsson, Bengt-Olof and Olde, Björn and Leeb-Lundberg, Fredrik},
  issn         = {1476-5381},
  keyword      = {G protein-coupled receptor,oestrogen,cardiovascular regulation,metabolic regulation,cellular signalling,non-genomic mechanisms},
  language     = {eng},
  number       = {6},
  pages        = {1131--1139},
  publisher    = {The British Pharmacological Society},
  series       = {British Journal of Pharmacology},
  title        = {G protein-coupled oestrogen receptor 1 (GPER1)/GPR30: a new player in cardiovascular and metabolic oestrogenic signalling},
  url          = {http://dx.doi.org/10.1111/j.1476-5381.2011.01235.x},
  volume       = {163},
  year         = {2011},
}