Does GPER Really Function as a G Protein-Coupled Estrogen Receptor in vivo?

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dc.contributor.authorLuo, Jingen
dc.contributor.authorLiu, Dongminen
dc.contributor.departmentHuman Nutrition, Foods, and Exerciseen
dc.date.accessioned2020-05-06T12:35:00Zen
dc.date.available2020-05-06T12:35:00Zen
dc.date.issued2020-03-31en
dc.description.abstractEstrogen can elicit pleiotropic cellular responses via a diversity of estrogen receptors (ERs)-mediated genomic and rapid non-genomic mechanisms. Unlike the genomic responses, where the classical nuclear ER alpha and ER beta act as transcriptional factors following estrogen binding to regulate gene transcription in estrogen target tissues, the non-genomic cellular responses to estrogen are believed to start at the plasma membrane, leading to rapid activation of second messengers-triggered cytoplasmic signal transduction cascades. The recently acknowledged ER, GPR30 or GPER, was discovered in human breast cancer cells two decades ago and subsequently in many other cells. Since its discovery, it has been claimed that estrogen, ER antagonist fulvestrant, as well as some estrogenic compounds can directly bind to GPER, and therefore initiate the non-genomic cellular responses. Various recently developed genetic tools as well as chemical ligands greatly facilitated research aimed at determining the physiological roles of GPER in different tissues. However, there is still lack of evidence that GPER plays a significant role in mediating endogenous estrogen action in vivo. This review summarizes current knowledge about GPER, including its tissue expression and cellular localization, with emphasis on the research findings elucidating its role in health and disease. Understanding the role of GPER in estrogen signaling will provide opportunities for the development of new therapeutic strategies to strengthen the benefits of estrogen while limiting the potential side effects.en
dc.format.mimetypeapplication/pdfen
dc.identifier.doihttps://doi.org/10.3389/fendo.2020.00148en
dc.identifier.issn1664-2392en
dc.identifier.other148en
dc.identifier.pmid32296387en
dc.identifier.urihttp://hdl.handle.net/10919/97982en
dc.identifier.volume11en
dc.language.isoenen
dc.rightsCreative Commons Attribution 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en
dc.subjectGPR30en
dc.subjectGPERen
dc.subjectestrogen receptoren
dc.subjectestrogenen
dc.subjectphysiological roleen
dc.titleDoes GPER Really Function as a G Protein-Coupled Estrogen Receptor in vivo?en
dc.title.serialFrontiers in Endocrinologyen
dc.typeArticle - Refereeden
dc.type.dcmitypeTexten
dc.type.dcmitypeStillImageen

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