Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Identifieur interne : 002F01 ( Main/Exploration ); précédent : 002F00; suivant : 002F02Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells.
Auteurs : P. Thomas [États-Unis] ; Y. Pang ; E J Filardo ; J. DongSource :
- Endocrinology [ 0013-7227 ] ; 2005.
Descripteurs français
- KwdFr :
- Adenylate Cyclase (métabolisme), Humains, Lignée cellulaire tumorale, Membrane cellulaire (métabolisme), Oestrogènes (métabolisme), Oestrogènes (pharmacologie), Protéines membranaires (métabolisme), Radio-isotopes du soufre, Rein (cytologie), Récepteurs couplés aux protéines G (génétique), Récepteurs couplés aux protéines G (métabolisme), Récepteurs des oestrogènes (métabolisme), Sous-unités alpha Gs des protéines G (métabolisme), Transduction du signal (physiologie), Transfection, Tumeurs du sein.
- MESH :
- cytologie : Rein.
- génétique : Récepteurs couplés aux protéines G.
- métabolisme : Adenylate Cyclase, Membrane cellulaire, Oestrogènes, Protéines membranaires, Récepteurs couplés aux protéines G, Récepteurs des oestrogènes, Sous-unités alpha Gs des protéines G.
- pharmacologie : Oestrogènes.
- physiologie : Transduction du signal.
- Humains, Lignée cellulaire tumorale, Radio-isotopes du soufre, Transfection, Tumeurs du sein.
English descriptors
- KwdEn :
- Adenylyl Cyclases (metabolism), Breast Neoplasms, Cell Line, Tumor, Cell Membrane (metabolism), Estrogens (metabolism), Estrogens (pharmacology), GTP-Binding Protein alpha Subunits, Gs (metabolism), Humans, Kidney (cytology), Membrane Proteins (metabolism), Receptors, Estrogen (metabolism), Receptors, G-Protein-Coupled (genetics), Receptors, G-Protein-Coupled (metabolism), Signal Transduction (physiology), Sulfur Radioisotopes, Transfection.
- MESH :
- chemical , genetics : Receptors, G-Protein-Coupled.
- chemical , metabolism : Adenylyl Cyclases, Estrogens, GTP-Binding Protein alpha Subunits, Gs, Membrane Proteins, Receptors, Estrogen, Receptors, G-Protein-Coupled.
- cytology : Kidney.
- metabolism : Cell Membrane.
- chemical , pharmacology : Estrogens.
- physiology : Signal Transduction.
- Breast Neoplasms, Cell Line, Tumor, Humans, Sulfur Radioisotopes, Transfection.
Abstract
Although nonclassical estrogen actions initiated at the cell surface have been described in many tissues, the identities of the membrane estrogen receptors (mERs) mediating these actions remain unclear. Here we show that GPR30, an orphan receptor unrelated to nuclear estrogen receptors, has all the binding and signaling characteristics of a mER. A high-affinity (dissociation constant 2.7 nm), limited capacity, displaceable, single binding site specific for estrogens was detected in plasma membranes of SKBR3 breast cancer cells that express GPR30 but lack nuclear estrogen receptors. Progesterone-induced increases and small interfering RNA-induced decreases in GPR30 expression in SKBR3 cells were accompanied by parallel changes in specific estradiol-17beta (E2) binding. Plasma membranes of human embryonic kidney 293 cells transfected with GPR30, but not those of untransfected cells, and human placental tissues that express GPR30 also displayed high-affinity, specific estrogen binding typical of mERs. E2 treatment of transfected cell membranes caused activation of a stimulatory G protein that is directly coupled to the receptor, indicating GPR30 is a G protein-coupled receptor (GPCR), and also increased adenylyl cyclase activity. The finding that the antiestrogens tamoxifen and ICI 182,780, and an environmental estrogen, ortho,para-dichlorodiphenyldichloroethylene (o,p'-DDE), have high binding affinities to the receptor and mimic the actions of E2 has important implications for both the development and treatment of estrogen-dependent breast cancer. GPR30 is structurally unrelated to the recently discovered family of GPCR-like membrane progestin receptors. The identification of a second distinct class of GPCR-like steroid membrane receptors suggests a widespread role for GPCRs in nonclassical steroid hormone actions.
DOI: 10.1210/en.2004-1064
PubMed: 15539556
Affiliations:
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Le document en format XML
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<term>Cell Line, Tumor</term>
<term>Cell Membrane (metabolism)</term>
<term>Estrogens (metabolism)</term>
<term>Estrogens (pharmacology)</term>
<term>GTP-Binding Protein alpha Subunits, Gs (metabolism)</term>
<term>Humans</term>
<term>Kidney (cytology)</term>
<term>Membrane Proteins (metabolism)</term>
<term>Receptors, Estrogen (metabolism)</term>
<term>Receptors, G-Protein-Coupled (genetics)</term>
<term>Receptors, G-Protein-Coupled (metabolism)</term>
<term>Signal Transduction (physiology)</term>
<term>Sulfur Radioisotopes</term>
<term>Transfection</term>
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<keywords scheme="KwdFr" xml:lang="fr"><term>Adenylate Cyclase (métabolisme)</term>
<term>Humains</term>
<term>Lignée cellulaire tumorale</term>
<term>Membrane cellulaire (métabolisme)</term>
<term>Oestrogènes (métabolisme)</term>
<term>Oestrogènes (pharmacologie)</term>
<term>Protéines membranaires (métabolisme)</term>
<term>Radio-isotopes du soufre</term>
<term>Rein (cytologie)</term>
<term>Récepteurs couplés aux protéines G (génétique)</term>
<term>Récepteurs couplés aux protéines G (métabolisme)</term>
<term>Récepteurs des oestrogènes (métabolisme)</term>
<term>Sous-unités alpha Gs des protéines G (métabolisme)</term>
<term>Transduction du signal (physiologie)</term>
<term>Transfection</term>
<term>Tumeurs du sein</term>
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<term>GTP-Binding Protein alpha Subunits, Gs</term>
<term>Membrane Proteins</term>
<term>Receptors, Estrogen</term>
<term>Receptors, G-Protein-Coupled</term>
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<term>Oestrogènes</term>
<term>Protéines membranaires</term>
<term>Récepteurs couplés aux protéines G</term>
<term>Récepteurs des oestrogènes</term>
<term>Sous-unités alpha Gs des protéines G</term>
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<term>Sulfur Radioisotopes</term>
<term>Transfection</term>
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<term>Lignée cellulaire tumorale</term>
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<front><div type="abstract" xml:lang="en">Although nonclassical estrogen actions initiated at the cell surface have been described in many tissues, the identities of the membrane estrogen receptors (mERs) mediating these actions remain unclear. Here we show that GPR30, an orphan receptor unrelated to nuclear estrogen receptors, has all the binding and signaling characteristics of a mER. A high-affinity (dissociation constant 2.7 nm), limited capacity, displaceable, single binding site specific for estrogens was detected in plasma membranes of SKBR3 breast cancer cells that express GPR30 but lack nuclear estrogen receptors. Progesterone-induced increases and small interfering RNA-induced decreases in GPR30 expression in SKBR3 cells were accompanied by parallel changes in specific estradiol-17beta (E2) binding. Plasma membranes of human embryonic kidney 293 cells transfected with GPR30, but not those of untransfected cells, and human placental tissues that express GPR30 also displayed high-affinity, specific estrogen binding typical of mERs. E2 treatment of transfected cell membranes caused activation of a stimulatory G protein that is directly coupled to the receptor, indicating GPR30 is a G protein-coupled receptor (GPCR), and also increased adenylyl cyclase activity. The finding that the antiestrogens tamoxifen and ICI 182,780, and an environmental estrogen, ortho,para-dichlorodiphenyldichloroethylene (o,p'-DDE), have high binding affinities to the receptor and mimic the actions of E2 has important implications for both the development and treatment of estrogen-dependent breast cancer. GPR30 is structurally unrelated to the recently discovered family of GPCR-like membrane progestin receptors. The identification of a second distinct class of GPCR-like steroid membrane receptors suggests a widespread role for GPCRs in nonclassical steroid hormone actions.</div>
</front>
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