Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity.
We found that the selective stimulation of the intracellular, transmembrane G protein-coupled estrogen receptor (GPER), also known as GPR30, acutely lowers blood pressure after infusion in normotensive rats and dilates both rodent and human arterial blood vessels. Stimulation of GPER blocks vasoconstrictor-induced changes in intracellular calcium concentrations and vascular tone, as well as serum-stimulated cell proliferation of human vascular smooth muscle cells. Deletion of the GPER gene in mice abrogates vascular effects of GPER activation and is associated with visceral obesity. These findings suggest novel roles for GPER in protecting from cardiovascular disease and obesity.
Haas
Elvira
E
Departement für Innere Medizin, Klinik und Poliklinik für Innere Medizin, Universitätsspital Zürich, Rämistrasse 100, CH-8091 Zürich, Switzerland.
Bhattacharya
Indranil
I
Brailoiu
Eugen
E
Damjanović
Marlen
M
Brailoiu
G Cristina
GC
Gao
Xin
X
Mueller-Guerre
Laurence
L
Marjon
Nicole A
NA
Gut
André
A
Minotti
Roberta
R
Meyer
Matthias R
MR
Amann
Kerstin
K
Ammann
Emerita
E
Perez-Dominguez
Ana
A
Genoni
Michele
M
Clegg
Deborah J
DJ
Dun
Nae J
NJ
Resta
Thomas C
TC
Prossnitz
Eric R
ER
Barton
Matthias
M
D000818:Animals; D050197:Atherosclerosis / Q000378:metabolism*; D001794:Blood Pressure / Q000187:drug effects*; D004958:Estradiol / Q000494:pharmacology; D005260:Female; D006801:Humans; D008297:Male; D008323:Mammary Arteries / Q000187:drug effects; D051379:Mice; D008817:Mice, Mutant Strains; D009765:Obesity / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D014664:Vasodilation / Q000187:drug effects
C109584:GPER1 protein, human; C532507:GPER1 protein, mouse; C520305:Gper1 protein, rat; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled; D004958:Estradiol