Cited by 89Estrogen and related hormone effectsReceptor Mechanisms and SignalingNeuroscience and Neuropharmacology Research

G‐Protein Oestrogen Receptor 1: Trials and Tribulations of a Membrane Oestrogen Receptor

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Srivastava, D. P., Evans, P. D.·2013·Journal of Neuroendocrinology

Abstract

Oestrogens are now recognised to be able to initiate rapid, fast responses, in addition to their classical, longer‐term actions. There is a growing appreciation of the potential implications of this mode of action for oestrogenic signalling in both neuronal and non‐neuronal systems. As such, much effort has been made to determine the mechanisms that are critical for transducing these rapid effects into cellular responses. Recently, an orphan G‐protein‐coupled receptor (GPCR), termed GPR 30, was identified as an oestrogen‐sensitive receptor in cancer cells. This receptor, now term G‐protein oestrogen receptor 1 (GPER 1) has been the subject of many investigations, and a role for this receptor in the nervous system is now emerging. In this review, we highlight some of the more recent advances in our understanding of the distribution and subcellular localisation of this receptor in the brain, as well as some of the evidence for the potential role that this receptor may play in the brain. We then discuss some of the controversies surrounding the pharmacology of this receptor, and attempt to reconcile these by suggesting that the ‘agonist‐specific coupling’ model of GPCR function may provide a potential explanation for some of the divergent reports of GPER 1 pharmacology.

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Crossref · 10.1111/jne.12071

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Authors
Srivastava, D. P., & Evans, P. D.
Affiliations
  • King's College London (GB)
  • Babraham Institute (GB)
Corresponding author
  • Srivastava, D. P.
  • Evans, P. D.
Venue
Journal of Neuroendocrinology
Publisher
Wiley
Published
2013-10-28
Volume
25
Issue
11
Pages
1219-1230
ISSN
  • 0953-8194 (ISSN-L)
  • 1365-2826
OpenAlex
W2029530971
Cited by
89
References
97
Citations by year
2025: 2 · 2024: 2 · 2023: 2 · 2021: 3 · 2020: 12 · 2019: 6 · 2018: 9 · 2017: 9 · 2016: 12 · 2015: 19 · 2014: 10 · 2013: 3
FWCI
1.80
Type
journal article
Language
en
Open access
Locations
  • Journal of Neuroendocrinology (publishedVersion)
  • PubMed (publishedVersion)
  • Research Portal (King's College London) (publishedVersion, other-oa)
Funders
  • Royal Society UK
  • National Alliance for Research on Schizophrenia and Depression
  • The Psychiatry Research Trust
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Keywords
GPR30, estrogen signaling, GPCR pharmacology, subcellular localization, brain distribution
MeSH terms
Animals, Brain, Humans, Receptors, Estrogen, Signal Transduction, Receptors, G-Protein-Coupled

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