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GPER Mediates Non-Genomic Effects of Estrogen

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Estrogen Receptors

Part of the book series: Methods in Molecular Biology ((MIMB,volume 1366))

Abstract

Estrogens are important modulators of a broad spectrum of physiological functions in humans. However, despite their beneficial actions, a number of lines of evidence correlate the sustained exposure to exogenous estrogen with increased risk of the onset of various cancers. Mainly these steroid hormones induce their effects by binding and activating estrogen receptors (ERα and ERβ). These receptors belong to the family of ligand-regulated transcription factors, and upon activation they regulate the expression of different target genes by binding directly to specific DNA sequences. On the other hand, in recent years it has become clear that the G protein-coupled estrogen receptor 30 (GPR30/GPER) is able to mediate non-genomic action of estrogens in different cell contexts. In particular, GPER has been shown to specifically bind estrogens, and in turn to functionally cross-react with diverse cell signaling systems such as the epidermal growth factor receptor (EGFR) pathway, the Notch signaling pathway and the mitogen-activated protein kinases (MAPK) pathway. In this chapter we will present some of the different experimental techniques currently used to demonstrate the functional role of GPER in mediating non-genomic actions of estrogens, such as the dual luciferase assay, assessment of the involvement of GPER in the stimulation of cell migration in breast cancer cell lines and in cancer-associated fibroblasts, and chromatin immunoprecipitation assay. Overall, the experimental procedures described herein represent key instruments for assessing the biological role of GPER in mediating non-genomic signals of estrogen.

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Authors and Affiliations

  1. Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy

    Marco Pupo, Marcello Maggiolini & Anna Maria Musti

  2. Institute for Clinical Neurobiology, University of Würzburg, Würzburg, Germany

    Anna Maria Musti

Authors
  1. Marco Pupo
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  2. Marcello Maggiolini
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  3. Anna Maria Musti
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Corresponding author

Correspondence to Anna Maria Musti .

Editor information

Editors and Affiliations

  1. University of South Dakota Sanford School of Medicine, Vermillion, South Dakota, USA

    Kathleen M. Eyster

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Pupo, M., Maggiolini, M., Musti, A.M. (2016). GPER Mediates Non-Genomic Effects of Estrogen. In: Eyster, K.M. (eds) Estrogen Receptors. Methods in Molecular Biology, vol 1366. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-3127-9_37

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  • DOI: https://doi.org/10.1007/978-1-4939-3127-9_37

  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-3126-2

  • Online ISBN: 978-1-4939-3127-9

  • eBook Packages: Springer Protocols

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