The DOI matches its Crossref record; 56 of the 56 references it cites were found in a registry or an index.
Activation of the Novel Estrogen Receptor G Protein-Coupled Receptor 30 (GPR30) at the Plasma Membrane
Open accessAbstract
G protein-coupled receptor 30 (GPR30), a seven-transmembrane receptor (7TMR), is associated with rapid estrogen-dependent, G protein signaling and specific estrogen binding. At present, the subcellular site of GPR30 action is unclear. Previous studies using antibodies and fluorochrome-labeled estradiol (E2) have failed to detect GPR30 on the cell surface, suggesting that GPR30 may function uniquely among 7TMRs as an intracellular receptor. Here, we show that detectable expression of GPR30 on the surface of transfected HEK-293 cells can be selected by fluorescence-activated cell sorting. Expression of GPR30 on the cell surface was confirmed by confocal microscopy using the lectin concanavalin A as a plasma membrane marker. Stimulation of GPR30-expressing HEK-293 cells with 17β-E2 caused sequestration of GPR30 from the cell surface and resulted in its codistribution with clathrin and mobilization of intracellular calcium stores. Evidence that GPR30 signals from the cell surface was obtained from experiments demonstrating that the cell-impermeable E2-protein conjugates E2-BSA and E2-horseradish peroxidase promote GPR30-dependent elevation of intracellular cAMP concentrations. Subcellular fractionation studies further support the plasma membrane as a site of GPR30 action with specific [3H]17β-E2 binding and G protein activation associated with plasma membrane but not microsomal, or other fractions, prepared from HEK-293 or SKBR3 breast cancer cells. These results suggest that GPR30, like other 7TMRs, functions as a plasma membrane receptor.
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A transmembrane intracellular estrogen receptor mediates rapid cell signaling
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Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells
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Self-citationTyrosine kinase/p21ras/MAP-kinase pathway activation by estradiol-receptor complex in MCF-7 cells.
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Cited by
Estrogen receptor signaling mechanisms
(2019) · Advances in Protein Chemistry and Structural Biology · doi:10.1016/bs.apcsb.2019.01.001 · Cited by 988
Estrogen Effects on Cognitive and Synaptic Health Over the Lifecourse
Hara, Y., Waters, E. M., McEwen, B. S., & Morrison, J. H. (2015) · Physiological Reviews · doi:10.1152/physrev.00036.2014 · Cited by 470
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Self-citationThe unfolding stories of GPR30, a new membrane-bound estrogen receptor
Maggiolini, M., & Picard, D. (2010) · Journal of Endocrinology · doi:10.1677/joe-09-0242 · Cited by 360
Bisphenol-A acts as a potent estrogen via non-classical estrogen triggered pathways
Alonso-Magdalena, P., Ropero, A. B., Soriano, S., García-Arévalo, M., Ripoll, C., Fuentes, E., Quesada, I., & Nadal, Á. (2012) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2011.12.012 · Cited by 358
Metadata
- Authors
- Filardo, E., Quinn, J., Pang, Y., Graeber, C., Shaw, S., Dong, J., & Thomas, P.
- Venue
- Endocrinology
- Publisher
- The Endocrine Society
- Published
- 2007-07-01
- Volume
- 148
- Issue
- 7
- Pages
- 3236-3245
- ISSN
- 0013-7227 (ISSN-L)
- 1945-7170
- OpenAlex
- W1967479320
- Cited by
- 450
- References
- 56
- FWCI
- 18.76
- Type
- journal article
- Language
- en
- Open access
- bronze
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