Research article summary (published 20 Mar 2007):

Activation of the novel estrogen receptor G protein-coupled receptor 30 (GPR30) at the plasma membrane.

Full Abstract

G protein-coupled receptor 30 (GPR30), a seven-transmembrane receptor (7TMR), is associated with rapid estrogen-dependent, G protein signaling and specific estrogen binding. At present, the subcellular site of GPR30 action is unclear. Previous studies using antibodies and fluorochrome-labeled estradiol (E2) have failed to detect GPR30 on the cell surface, suggesting that GPR30 may function uniquely among 7TMRs as an intracellular receptor. Here, we show that detectable expression of GPR30 on the surface of transfected HEK-293 cells can be selected by fluorescence-activated cell sorting. Expression of GPR30 on the cell surface was confirmed by confocal microscopy using the lectin concanavalin A as a plasma membrane marker. Stimulation of GPR30-expressing HEK-293 cells with 17beta-E2 caused sequestration of GPR30 from the cell surface and resulted in its codistribution with clathrin and mobilization of intracellular calcium stores. Evidence that GPR30 signals from the cell surface was obtained from experiments demonstrating that the cell-impermeable E2-protein conjugates E2-BSA and E2-horseradish peroxidase promote GPR30-dependent elevation of intracellular cAMP concentrations. Subcellular fractionation studies further support the plasma membrane as a site of GPR30 action with specific [3H]17beta-E2 binding and G protein activation associated with plasma membrane but not microsomal, or other fractions, prepared from HEK-293 or SKBR3 breast cancer cells. These results suggest that GPR30, like other 7TMRs, functions as a plasma membrane receptor.

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Author information

Author/s: Filardo, E (E); Quinn, J (J); Pang, Y (Y); Graeber, C (C); Shaw, S (S); Dong, J (J); Thomas, P (P);

Affiliation: Department of Medicine, Brown University, and Rhode Island Hospital, 593 Eddy Street, Aldrich Building, Room 718, Providence, Rhode Island 02903, USA. edward_filardo(-atsign-)brown.edu

Grants: RR P20 RR017695 (Agency:NCRR NIH HHS)

Journal and publication information

Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.

Journal: Endocrinology (Endocrinology), published in United States. (Language: eng)

Reference: 2007-Jul; vol 148 (issue 7) : pp 3236-45

Dates: Created 2007/06/18; Completed 2007/10/02; Revised 2007/12/03;

PMID: 17379646, status: MEDLINE (last retrieval date: 12/26/2008)

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Animals Blotting, Western Calcium - metabolism Cell Line Cell Line, Tumor Cell Membrane - metabolism Clathrin - metabolism Concanavalin A - metabolism Estradiol - metabolism; pharmacology Estrogens - metabolism Female Flow Cytometry

Flow Cytometry Gene Expression - drug effects Humans Immunoprecipitation Mice Mice, Inbred BALB C Microscopy, Confocal Protein Binding Receptors, Estrogen - genetics; metabolism Receptors, G-Protein-Coupled - genetics; metabolism Recombinant Fusion Proteins - genetics; metabolism Signal Transduction - drug effects

Associated Chemicals: Clathrin (0) ; Estrogens (0) ; GPER protein, human (0) ; Receptors, Estrogen (0) ; Receptors, G-Protein-Coupled (0) ; Recombinant Fusion Proteins (0) ; Concanavalin A (11028-71-0) ; Estradiol (50-28-2) ; Calcium (7440-70-2)

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