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Modulation of G Protein-Coupled Receptors by an Estrogen Receptor that Activates Protein Kinase A
Molecular Pharmacology, 199717beta-Estradiol (E2) rapidly (
A H, Lagrange +2 more
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2016
The role of 2-methoxyestradiol is becoming a major area of investigation because of its therapeutic utility, though its mechanism is not fully explored. Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. However, studies aimed at establishing the binding affinities
Thomas, Thekkumkara +2 more
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The role of 2-methoxyestradiol is becoming a major area of investigation because of its therapeutic utility, though its mechanism is not fully explored. Recent studies have identified the G-protein-coupled receptor 30 (GPR30, GPER) as a high-affinity membrane receptor for 2-methoxyestradiol. However, studies aimed at establishing the binding affinities
Thomas, Thekkumkara +2 more
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Estrogen Signaling through the Transmembrane G Protein–Coupled Receptor GPR30
Annual Review of Physiology, 2008Steroids play an important role in the regulation of normal physiology and the treatment of disease. Steroid receptors have classically been described as ligand-activated transcription factors mediating long-term genomic effects in hormonally regulated tissues.
Eric R, Prossnitz +5 more
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The role of G protein-coupled estrogen receptor 1 on neurological disorders
Frontiers in Neuroendocrinology, 2019G protein-coupled estrogen receptor 1 (GPER) is a membrane-associated estrogen receptor (ER) associated with rapid estrogen-mediated effects. Over recent years GPER emerged has a potential therapeutic target to induce neuroprotection, avoiding the side effects elicited by the activation of classical ERs.
C, Roque +3 more
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Endocrinology
Abstract LH/choriogonadotropin (hCG) receptor (LHCGR) and the G protein-coupled estrogen receptor (GPER) are coexpressed in the ovary and support reproduction. The latter is involved in pathophysiological conditions and has been suggested as a potential therapeutic target.
Lazzaretti, Clara +16 more
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Abstract LH/choriogonadotropin (hCG) receptor (LHCGR) and the G protein-coupled estrogen receptor (GPER) are coexpressed in the ovary and support reproduction. The latter is involved in pathophysiological conditions and has been suggested as a potential therapeutic target.
Lazzaretti, Clara +16 more
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G protein-coupled estrogen receptor biased signaling in health and disease
Pharmacology & TherapeuticsG protein-coupled estrogen receptor (GPER) is now recognized for its pivotal role in cellular signaling, influencing diverse physiological processes and disease states. Unlike classical estrogen receptors, GPER exhibits biased signaling, wherein ligand binding triggers selective pathways over others, significantly impacting cellular responses.
Aisha, Bushi +8 more
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Cardioprotective role of G-Protein Coupled Estrogen Receptor 1 (GPER1)
Molecular Membrane Biology, 2015G-Protein Coupled Estrogen Receptor 1 (GPER1), also known as G-Protein Coupled Receptor 30 (GPR30) and initially considered an orphan receptor, has become one of the most important pharmacological targets in cardiovascular research. Since the gene encoding this putative receptor was cloned nearly 20 years ago, researchers have addressed its role in ...
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