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Updated: Jun 20, 2026

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy
Published on: April 9, 2017
GPR30/GPER1: searching for a role in estrogen physiology
Björn Olde1, L M Fredrik Leeb-Lundberg
1Unit of Drug Target Discovery, Department of Experimental Medical Science, Lund University, SE-22184 Lund, Sweden.
Abstract:
Estrogens are sex hormones that are central to health and disease in both genders. These hormones have long been recognized to act in complex ways, both through relatively slow genomic mechanisms and via fast non-genomic mechanisms. Several recent in vitro studies suggest that GPR30, or G protein-coupled estrogen receptor 1 (GPER1), is a functional membrane estrogen receptor involved in non-genomic estrogen signaling. However, this function is not universally accepted. Studies concerning the role of GPER1 in vivo are now beginning to appear but with divergent results. In this review we discuss current knowledge on the physiological role of GPER1 in the nervous system as well as in reproduction, metabolism, bone, and in the cardiovascular and immune systems.
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