title: Regulation of K(ATP) channel by 17β-estradiol in pancreatic β-cells.
abstract: ATP-sensitive potassium channels (K(ATP)) regulate electrical activity and insulin secretion in pancreatic β-cells. When glucose concentration increases, the [ATP]/[ADP] ratio rises closing K(ATP) channels, and the membrane potential depolarizes, triggering insulin secretion. This pivotal role of K(ATP) channels is used not only by glucose but also by neurotransmitters, hormones and other physiological agents to modulate electrical and secretory β-cell response. In recent years, it has been demonstrated that estrogens and estrogen receptors are involved in glucose homeostasis, and that they can modulate the electrical activity and insulin secretion of pancreatic β-cells. The hormone 17β-estradiol (E2), at physiological levels, is implicated in maintaining normal insulin sensitivity for β-cell function. Long term exposure to E2 increases insulin content, insulin gene expression and insulin release via the estrogen receptor α (ERα), while rapid responses to E2 can regulate K(ATP) channels increasing cGMP levels through the estrogen receptor β (ERβ) and type A guanylate cyclase receptor (GC-A). This review summarizes the main actions of 17β-estradiol on K(ATP) channels and the subsequent insulin release in pancreatic β-cells.
authors.affiliation: Instituto de Bioingeniería and CIBER de Diabetes y Enfermedades Metabólicas Asociadas (CIBERDEM), Universidad Miguel Hernández de Elche, 03202 Elche, Alicante, Spain. sergi.soriano@umh.es
authors.forename: Sergi
authors.initials: S
authors.lastname: Soriano
authors.forename: Cristina
authors.initials: C
authors.lastname: Ripoll
authors.forename: Esther
authors.initials: E
authors.lastname: Fuentes
authors.forename: Alejandro
authors.initials: A
authors.lastname: Gonzalez
authors.forename: Paloma
authors.initials: P
authors.lastname: Alonso-Magdalena
authors.forename: Ana B
authors.initials: AB
authors.lastname: Ropero
authors.forename: Ivan
authors.initials: I
authors.lastname: Quesada
authors.forename: Angel
authors.initials: A
authors.lastname: Nadal
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism; D000818:Animals; D004958:Estradiol / Q000378:metabolism*; D004967:Estrogens / Q000378:metabolism*; D006801:Humans; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000378:metabolism*; D054086:KATP Channels / Q000378:metabolism*; D024661:Potassium Channels, Inwardly Rectifying / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism; D050705:Receptors, Guanylate Cyclase-Coupled / Q000378:metabolism; D064233:Sulfonylurea Receptors
chemical_list: D018528:ATP-Binding Cassette Transporters; D004967:Estrogens; D007328:Insulin; D054086:KATP Channels; D024661:Potassium Channels, Inwardly Rectifying; D011955:Receptors, Drug; D011960:Receptors, Estrogen; D064233:Sulfonylurea Receptors; D004958:Estradiol; D050705:Receptors, Guanylate Cyclase-Coupled