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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/2049193
- author
- Nilsson, Bengt-Olof
LU
; Olde, Björn
LU
and Leeb-Lundberg, Fredrik
LU
- organization
- publishing date
- 2011
- 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
- Wiley
- external identifiers
-
- wos:000292098700007
- scopus:79959768665
- pmid:21250980
- 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
- 2016-04-01 12:55:26
- date last changed
- 2022-04-21 18:38:48
@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}},
keywords = {{G protein-coupled receptor; oestrogen; cardiovascular regulation; metabolic regulation; cellular signalling; non-genomic mechanisms}},
language = {{eng}},
number = {{6}},
pages = {{1131--1139}},
publisher = {{Wiley}},
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}},
doi = {{10.1111/j.1476-5381.2011.01235.x}},
volume = {{163}},
year = {{2011}},
}