title: Emerging roles of GPER in diabetes and atherosclerosis.
abstract: The G protein-coupled estrogen receptor (GPER) is a 7-transmembrane receptor implicated in rapid estrogen signaling. Originally cloned from vascular endothelial cells, GPER plays a central role in the regulation of vascular tone and cell growth as well as lipid and glucose homeostasis. This review highlights our knowledge of the physiological and pathophysiological functions of GPER in the pancreas, peripheral and immune tissues, and the arterial vasculature. Recent findings on its roles in obesity, diabetes, and atherosclerosis, including GPER-dependent regulation of lipid metabolism and inflammation, are presented. The therapeutic potential of targeting GPER-dependent pathways in chronic diseases such as coronary artery disease and diabetes and in the context of menopause is also discussed.
authors.affiliation: Molecular Internal Medicine, University of Zurich, Switzerland. Electronic address: barton@access.uzh.ch.
authors.forename: Matthias
authors.initials: M
authors.lastname: Barton
authors.affiliation: Department of Internal Medicine, University of New Mexico Health Sciences Center, Albuquerque, NM 87120, USA; UNM Cancer Center, University of New Mexico Health Sciences Center, Albuquerque, NM 87120, USA. Electronic address: eprossnitz@salud.unm.edu.
authors.forename: Eric R
authors.initials: ER
authors.lastname: Prossnitz
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000627:therapeutic use; D050197:Atherosclerosis / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism*; D002317:Cardiovascular Agents / Q000627:therapeutic use; D003920:Diabetes Mellitus / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism*; D006801:Humans; D007004:Hypoglycemic Agents / Q000627:therapeutic use; D008024:Ligands; D050356:Lipid Metabolism / Q000187:drug effects; D008954:Models, Biological; D058990:Molecular Targeted Therapy; D009765:Obesity / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism*; D009928:Organ Specificity; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D019440:Anti-Obesity Agents; D002317:Cardiovascular Agents; C109584:GPER1 protein, human; D007004:Hypoglycemic Agents; D008024:Ligands; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled
keywords: GPER; atherosclerosis; diabetes; estrogen receptor; rapid signaling