title: Roles of G protein-coupled estrogen receptor GPER in metabolic regulation.
abstract: Metabolic homeostasis is differentially regulated in males and females. The lower incidence of obesity and associated diseases in pre-menopausal females points towards the beneficial role of the predominant estrogen, 17β-estradiol (E2). The actions of E2 are elicited by nuclear and extra-nuclear estrogen receptor (ER) α and ERβ, as well as the G protein-coupled estrogen receptor (GPER, previously termed GPR30). The roles of GPER in the regulation of metabolism are only beginning to emerge and much remains unclear. The present review highlights recent advances implicating the importance of GPER in metabolic regulation. Assessment of the specific metabolic roles of GPER employing GPER-deficient mice and highly selective GPER-targeted pharmacological agents, agonist G-1 and antagonists G-15 and G36, is also presented. Evidence from in vitro and in vivo studies involving either GPER deficiency or selective activation suggests that GPER is involved in body weight regulation, glucose and lipid homeostasis as well as inflammation. The therapeutic potential of activating GPER signaling through selective ligands for the treatment of obesity and diabetes is also discussed.
authors.affiliation: Division of Molecular Medicine, Department of Internal Medicine, University of New Mexico Health Sciences Center, Albuquerque, NM, 87131, United States.
authors.forename: Geetanjali
authors.initials: G
authors.lastname: Sharma
authors.affiliation: Diabetes Discovery and Gender Medicine Laboratory, Section of Endocrinology and Metabolism, Department of Medicine,Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, 70112, United States.
authors.forename: Franck
authors.initials: F
authors.lastname: Mauvais-Jarvis
authors.affiliation: Division of Molecular Medicine, Department of Internal Medicine, University of New Mexico Health Sciences Center, Albuquerque, NM, 87131, United States; University of New Mexico Comprehensive Cancer Center, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, United States. Electronic address: eprossnitz@salud.unm.edu.
authors.forename: Eric R
authors.initials: ER
authors.lastname: Prossnitz
mesh_terms: D000818:Animals; D004734:Energy Metabolism; D006801:Humans; D053858:Metabolic Networks and Pathways; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
chemical_list: D043562:Receptors, G-Protein-Coupled
keywords: Diabetes; Estrogen; GPER; Inflammation; Insulin resistance; Metabolism; Obesity