The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
In vivo effects of a GPR30 antagonist
Open accessAbstract
Estrogen is central to many physiological processes throughout the human body. We have previously shown that the G protein-coupled receptor GPR30/GPER, in addition to classical nuclear estrogen receptors (ERα/β), activates cellular signaling pathways in response to estrogen. In order to distinguish between the actions of classical estrogen receptors and GPR30, we have previously characterized a selective agonist of GPR30, G-1 (1). To complement the pharmacological properties of G-1, we sought to identify an antagonist of GPR30 that displays similar selectivity against the classical estrogen receptors. Here we describe the identification and characterization of a G-1 analog, G15 (2) that binds to GPR30 with high affinity and acts as an antagonist of estrogen signaling through GPR30. In vivo administration of G15 reveals that GPR30 contributes to both uterine and neurological responses initiated by estrogen. The identification of this antagonist will accelerate the evaluation of the roles of GPR30 in human physiology.
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Cites
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A transmembrane intracellular estrogen receptor mediates rapid cell signaling
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Self-citationCryan, J. F., Mombereau, C., & Vassout, A. (2005) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2005.03.009 · Cited by 1,674
Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells
Thomas, P., Pang, Y., Filardo, E. J., & Dong, J. (2005) · Endocrinology · doi:10.1210/en.2004-1064 · Cited by 1,407
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Virtual and biomolecular screening converge on a selective agonist for GPR30
Bologa, C. G., Revankar, C. M., Young, S. M., Edwards, B. S., Arterburn, J. B., Kiselyov, A. S., Parker, M. A., Tkachenko, S. E., Savchuck, N. P., Sklar, L. A., et al. (2006) · Nature Chemical Biology · doi:10.1038/nchembio775 · Cited by 818
Self-citationCrystallographic comparison of the estrogen and progesterone receptor’s ligand binding domains
Tanenbaum, D. M., Wang, Y., Williams, S. P., & Sigler, P. B. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.11.5998 · Cited by 738
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Estrogen Signaling through the Transmembrane G Protein–Coupled Receptor GPR30
Prossnitz, E. R., Arterburn, J. B., Smith, H. O., Oprea, T. I., Sklar, L. A., & Hathaway, H. J. (2008) · Annual Review of Physiology · doi:10.1146/annurev.physiol.70.113006.100518 · Cited by 590
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Cited by
The G-protein-coupled estrogen receptor GPER in health and disease
Prossnitz, E. R., & Barton, M. (2011) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2011.122 · Cited by 925
“In 2009, the GPER-selective antagonist G15 ( Figure 1 ) was identified”
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Estrogens, Neuroinflammation, and Neurodegeneration
Villa, A., Vegeto, E., Poletti, A., & Maggi, A. (2016) · Endocrine Reviews · doi:10.1210/er.2016-1007 · Cited by 423
Estrogen biology: New insights into GPER function and clinical opportunities
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Self-citationThe unfolding stories of GPR30, a new membrane-bound estrogen receptor
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Metadata
- Authors
- Dennis, M. K., Burai, R., Ramesh, C., Petrie, W. K., Alcon, S. N., Nayak, T. K., Bologa, C. G., Leitao, A., Brailoiu, E., Deliu, E., Dun, N. J., Sklar, L. A., Hathaway, H. J., Arterburn, J. B., Oprea, T. I., & Prossnitz, E. R.
- Venue
- Nature Chemical Biology
- Published
- 2009-05-03
- Volume
- 5
- Issue
- 6
- Pages
- 421-427
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- OpenAlex
- W2076908209
- Cited by
- 532
- References
- 42
- FWCI
- 17.64
- Type
- journal article
- Language
- en
- Open access
- green
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- Dennis, M. K., Burai, R., Ramesh, C., Petrie, W. K., Alcon, S. N., Nayak, T. K., Bologa, C. G., Leitao, A., Brailoiu, E., Deliu, E., Dun, N. J., Sklar, L. A., Hathaway, H. J., Arterburn, J. B., Oprea, T. I., & Prossnitz, E. R. (2009). In vivo effects of a GPR30 antagonist. Nature Chemical Biology. https://doi.org/10.1038/nchembio.168
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