GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release

Trends Endocrinol Metab. 2005 Oct;16(8):362-7. doi: 10.1016/j.tem.2005.08.005.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Epidermal Growth Factor / metabolism*
  • Estrogens / metabolism
  • Humans
  • Models, Biological
  • Receptors, Estrogen / physiology*
  • Receptors, G-Protein-Coupled / physiology*
  • Second Messenger Systems / physiology

Substances

  • Estrogens
  • GPER1 protein, human
  • Receptors, Estrogen
  • Receptors, G-Protein-Coupled
  • Epidermal Growth Factor
  • Adenylyl Cyclases