GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release.
Heterotrimeric G proteins and seven-transmembrane-spanning (7TM) receptors are implicated in rapid estrogen signaling. The orphan 7TM receptor GPR30 is linked to estrogen-mediated activation of adenylyl cyclase, release of epidermal growth factor (EGF)-related ligands, and specific estrogen binding. GPR30 acts independently of estrogen receptors, ERalpha and ERbeta, and probably functions as a heptahelical ER. 7TM receptors elicit signals that stimulate second messengers, and convey intracellular signals via EGF receptors. Identification of GPR30 as a Gs-coupled 7TM receptor that triggers release of heparin-binding EGF establishes its role in cell signaling cascades initiated by estrogens, and explains their capacity to activate second messengers and promote EGF-like effects. Thus, estrogen can signal by the same mechanism as various other hormones, through a specific 7TM receptor.
Filardo
Edward J
EJ
Department of Medicine, Rhode Island Hospital and Brown University School of Medicine, Providence, RI 02903, USA. edward_filardo@brown.edu
Thomas
Peter
P
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D004815:Epidermal Growth Factor / Q000378:metabolism*; D004967:Estrogens / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D011960:Receptors, Estrogen / Q000502:physiology*; D043562:Receptors, G-Protein-Coupled / Q000502:physiology*; D015290:Second Messenger Systems / Q000502:physiology
D004967:Estrogens; C109584:GPER1 protein, human; D011960:Receptors, Estrogen; D043562:Receptors, G-Protein-Coupled; D004815:Epidermal Growth Factor; D000262:Adenylyl Cyclases