Obligatory role for GPER in cardiovascular aging and disease.

ABSTRACT: Pharmacological activation of the heptahelical G protein-coupled estrogen receptor (GPER) by selective ligands counteracts multiple aspects of cardiovascular disease. We thus expected that genetic deletion or pharmacological inhibition of GPER would further aggravate such disease states, particularly with age. To the contrary, we found that genetic ablation of Gper in mice prevented cardiovascular pathologies associated with aging by reducing superoxide (⋅O₂^-) formation by NADPH oxidase (Nox) specifically through reducing the expression of the Nox isoform Nox1 Blocking GPER activity pharmacologically with G36, a synthetic, small-molecule, GPER-selective blocker (GRB), decreased Nox1 abundance and ⋅O₂^- production to basal amounts in cells exposed

SUBMITTER: Meyer MR 

PROVIDER: S-EPMC5124501 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature