G-protein coupled estrogen receptor 1 expression in rat and human heart: Protective role during ischaemic stress.
G-protein coupled estrogen receptor 1, GPER, formerly known as GPR30, is a seven transmembrane domain receptor that mediates rapid estrogen responses in a wide variety of cell types. To date, little is known about the role of GPER during ischaemia/reperfusion injury. In this study, we report both mRNA and protein expression of GPER in the rat and human heart. The role of GPER in estrogen protection against ischaemic stress in the rat heart was also assessed using the isolated Langendorff system. Pre-treatment with 17beta-estradiol (E2) significantly decreased infarct size, (61.48+/-2.2% to 27.92+/-2.9% (P<0.001). Similarly, treatment with the GPER agonist G1 prior to 30-min global ischaemia followed by 120-min reperfusion significantly reduced infarct size from 61.48+/-2.2% to 23.85+/-3.2% (P<0.001), whilst addition of GPR30 antibody, abolished the protective effect of G1 (infarct size: 55.42+/-1.3%). The results suggest that GPER under cardiac stress exerts direct protection in the heart and may serve as a potential therapeutic target for cardiac drug therapy.
Patel
Vanlata H
VH
Endocrinology and Metabolism Group, Clinical Sciences Research Institute, Warwick Medical School, University of Warwick, Coventry CV4 7AL, UK.
Chen
Jing
J
Ramanjaneya
Manjunath
M
Karteris
Emmanouil
E
Zachariades
Elena
E
Thomas
Peter
P
Been
Martin
M
Randeva
Harpal S
HS
D000704:Analysis of Variance; D000818:Animals; D015153:Blotting, Western; D015870:Gene Expression; D006651:Histocytochemistry; D006801:Humans; D008297:Male; D017202:Myocardial Ischemia / Q000378:metabolism* / Q000473:pathology; D020011:Protective Agents / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled / Q000235:genetics / Q000378:metabolism*; D020133:Reverse Transcriptase Polymerase Chain Reaction; D017725:Ventricular Pressure
C109584:GPER1 protein, human; C520305:Gper1 protein, rat; D020011:Protective Agents; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled