A G Protein–Coupled Receptor For Estrogen: The End Of The Search?

Table 1.

Putative Membrane Estrogen Receptors (mER), Their Distribution, and Their Defining Characteristics

Name Distribution (Tissues/Cell Lines) Characteristics References
*GABA, γ-amino butyric acid; POMC, proopiomelanocortin; MAPK, mitogen-activated protein kinase; ERK, extracellular-regulated kinase; PKA, protein kinase A; PKC, protein kinase C; E2, estradiol.
pER Mouse liver, skeleton, neurons, vasculature, retina, Carcinoma of breast, endometrium, prostate Serine phosphatase activity Located on cell surface and/or nuclear membrane (20)
ER-X Mouse brain neocortex, uterus Developmentally-regulated MAPK/ERK activation [(3) review], (19)
GPR30 Heart, breast, lung, CNS, vascular endothelium, leukocytes, Tumor cell lines: MCF-7 and SKBR3 MAPK/ERK activation
 Adenylyl cyclase activation
 PKA activation
 PKC activation
 Activation of Src’s tyrosine kinase
 Intracellular Ca2+ mobilization
 c-fos activation EGF receptor transactivation [(2, 3) reviews], (7, 13, 14, 2426)
Unidentified CHO-K1, COS7 cells Rat2-fibroblasts MAPK activation (12)
Unidentified Isolated endometrial cells Binds E2 (12)
Unidentified Mouse cerebral cortical explants MAPK/ERK and B-Raf activation (8)
Unidentified Guinea pig hypothalamic GABA*, POMC, and dopamine neurons Modulation of μ-opioid and GABAB neurotransmission
 PKC activation
 Located on cell surface
 Gq activation Located on cell surface (15), [(17) review]
Unidentified Guinea pig hypothalamic (β-endorphin) neurons Attenuation of μ-opioid agonist activation of inwardly rectifying K+ conductance
 Involvement of PKA (16)
Unidentified GT1-7 neuronal cell line Modulation of acetylcholine-induced calcium mobilization (18)

This Article

  1. MI June 2005 vol. 5 no. 3 158-161