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.[1]References
- GPR30: a seven-transmembrane-spanning estrogen receptor that triggers EGF release. Filardo, E.J., Thomas, P. Trends Endocrinol. Metab. (2005) [Pubmed]
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