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GPER1 / GPR30

G protein-coupled estrogen receptor 1

G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP production, calcium mobilization and tyrosine kinase Src inducing the release of heparin-bound epidermal growth factor (HB-EGF) and subsequent transactivation of the epidermal growth factor receptor (EGFR), activating downstream signaling pathways such as PI3K/Akt and ERK/MAPK. Mediates pleiotropic functions among others in the cardiovascular, endocrine, reproductive, immune and central nervous systems. Has a role in cardioprotection by reducing cardiac hypertrophy and perivascular fibrosis in a RAMP3-dependent manner. Regulates arterial blood pressure by stimulating vasodilation and reducing vascular smooth muscle and microvascular endothelial cell proliferation. Plays a role in blood glucose homeostasis contributing to the insulin secretion response by pancreatic beta cells. Triggers mitochondrial apoptosis during pachytene spermatocyte differentiation. Stimulates uterine epithelial cell proliferation. Enhances uterine contractility in response to oxytocin. Contributes to thymic atrophy by inducing apoptosis. Attenuates TNF-mediated endothelial expression of leukocyte adhesion molecules. Promotes neuritogenesis in developing hippocampal neurons. Plays a role in acute neuroprotection against NMDA-induced excitotoxic neuronal death. Increases firing activity and intracellular calcium oscillations in luteinizing hormone-releasing hormone (LHRH) neurons. Inhibits early osteoblast proliferation at growth plate during skeletal development. Inhibits mature adipocyte differentiation and lipid accumulation. Involved in the recruitment of beta-arrestin 2 ARRB2 at the plasma membrane in epithelial cells. Functions also as a receptor for aldosterone mediating rapid regulation of vascular contractibility through the PI3K/ERK signaling pathway. Involved in cancer progression regulation. Stimulates cancer-associated fibroblast (CAF) proliferation by a rapid genomic response through the EGFR/ERK transduction pathway. Associated with EGFR, may act as a transcription factor activating growth regulatory genes (c-fos, cyclin D1). Promotes integrin alpha-5/beta-1 and fibronectin (FN) matrix assembly in breast cancer cells.

Gene Name: G protein-coupled estrogen receptor 1
Family/Subfamily: GPCR , Transmembrane Estrogen Receptor
Synonyms: GPER1, CMKRL2, CEPR, FEG-1, G-protein coupled receptor 30, G protein-coupled receptor 30, GPCR-Br, GPER, Heptahelix receptor, LERGU, LyGPR, MER, GPR30, IL8-related receptor DRY12, LERGU2, Chemokine receptor-like 2, DRY12, Membrane estrogen receptor
Target Sequences: NM_001505 NP_001496.1 Q99527

Publications (23)

1
Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Thomas P, Pang Y, Filardo EJ and Dong J. Endocrinology. 2005 146:624-32. (ICC; Human) [PubMed:15539556] Related Antibodies: LS-A1183.
2
Impaired leukocyte influx in cervix of postterm women not responding to prostaglandin priming. Sahlin L, Stjernholm-Vladic Y, Roos N, Masironi B, Ekman-Ordeberg G. Reproductive biology and endocrinology : RB&E. 2008 6:36. (IHC-P; Human) [Full Text Article] [PubMed:18764934] [PMC:PMC2551600] Related Antibodies: LS-A4272.
3
Estrogenic GPR30 signalling induces proliferation and migration of breast cancer cells through CTGF. Pandey DP, Lappano R, Albanito L, Madeo A, Maggiolini M, Picard D. The EMBO journal. 2009 28:523-32. (WB; Human) [Full Text Article] [PubMed:19153601] [PMC:PMC2657575] Related Antibodies: LS-A1183.
4
Identification of the estrogen receptor GPER in neoplastic and non-neoplastic human testes. Rago V, Romeo F, Giordano F, Maggiolini M, Carpino A. Reproductive biology and endocrinology : RB&E. 2011 9:135. (WB, IHC-P; Human) [Full Text Article] [PubMed:21974818] [PMC:PMC3200171] Related Antibodies: LS-A4271.
5
GPR30 regulates the EGFR-Akt cascade and predicts lower survival in patients with ovarian cancer. Fujiwara S, Terai Y, Kawaguchi H, Takai M, Yoo S, Tanaka Y, Tanaka T, Tsunetoh S, Sasaki H, Kanemura M, Tanabe A, Yamashita Y, Ohmichi M. Journal of ovarian research. 2012 5:35. (WB; Human) [Full Text Article] [PubMed:23163984] Related Antibodies: LS-A4272.
6
Severe pulmonary hypertension in aging female apolipoprotein E-deficient mice is rescued by estrogen replacement therapy. Umar S, Partow-Navid R, Ruffenach G, Iorga A, Moazeni S, Eghbali M. Biology of sex differences. 2017 March;8:9. (Human) [Full Text Article] [PubMed:28344760] [PMC:PMC5360087] Related Antibodies: LS-A4272.
7
A genetic polymorphism repurposes the G-protein coupled and membrane-associated estrogen receptor GPER to a transcription factor-like molecule promoting paracrine signaling between stroma and breast carcinoma cells. Pupo M, Bodmer A, Berto M, Maggiolini M, Dietrich PY, Picard D. Oncotarget. 2017 July;8:46728-46744. (Human) [Full Text Article] [PubMed:28596490] [PMC:PMC5564519] Related Antibodies: LS-A4272.
8
Nuclear G protein-coupled oestrogen receptor (GPR30) predicts poor survival in patients with ovarian cancer. Zhu CX, Xiong W, Wang ML, Yang J, Shi HJ, Chen HQ, Niu G. The Journal of international medical research. 2018 February;46:723-731. [Full Text Article] [PubMed:29239277] [PMC:PMC5971494] Related Antibodies: LS-A4290.
9
Estrogen receptors are found in glia and at extranuclear neuronal sites in the dorsal striatum of female rats: evidence for cholinergic but not dopaminergic colocalization. Anne Almey, Edward J Filardo, Teresa A Milner, Wayne G Brake. Endocrinology. 2012 November;153:5373-83. [Full Text Article] [PubMed:22919059] [PMC:PMC3473205] Related Antibodies: LS-A4290.
10
The G-Protein-Coupled Estrogen Receptor (GPER) Regulates Trimethylation of Histone H3 at Lysine 4 and Represses Migration and Proliferation of Ovarian Cancer Cells In Vitro. Nan Han, Sabine Heublein , Udo Jeschke , Christina Kuhn , Anna Hester, Bastian Czogalla, Sven Mahner, Miriam Rottmann, Doris Mayr, Elisa Schmoeckel, Fabian Trillsch. Cells. 2021 Mar;10:619. [Full Text Article] [PubMed:33799631] [PMC:PMC8001910]
11
Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal - and -opioid receptor heterodimerization and female-specific spinal morphine antinociception. Liu NJ, Chakrabarti S, Schnell S, Wessendorf M, Gintzler AR. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2011 31:11836-45. (IHC-Fr; Rat) [Full Text Article] [PubMed:21849544] [PMC:PMC3321927] Related Antibodies: LS-A4272.
12
Regulation of ERRalpha gene expression by estrogen receptor agonists and antagonists in SKBR3 breast cancer cells: differential molecular mechanisms mediated by g protein-coupled receptor GPR30/GPER-1. Li Y, Birnbaumer L, Teng CT. Molecular endocrinology (Baltimore, Md.). 2010 May;24:969-80. [Full Text Article] [PubMed:20211987] [PMC:PMC2870941] Related Antibodies: LS-A4272.
13
Stallion spermatozoa: putative target of estrogens; presence of the estrogen receptors ESR1, ESR2 and identification of the estrogen-membrane receptor GPER. Arkoun B, Gautier C, Delalande C, Barrier-Battut I, Gu[Character e9]non I, Goux D, Boura[Character ef]ma-Lelong H. General and comparative endocrinology. 2014 May;200:35-43. [Full Text Article] [PubMed:24607572] Related Antibodies: LS-A4272, LS-A1184, LS-A4271.
14
Estradiol and GPER Activation Differentially Affect Cell Proliferation but Not GPER Expression in the Hippocampus of Adult Female Rats. Duarte-Guterman P, Lieblich SE, Chow C, Galea LA. PloS one. 2015 10:e0129880. (IF; Rat) [Full Text Article] [PubMed:26075609] [PMC:PMC4468121] Related Antibodies: LS-A4272.
15
G protein-coupled receptor 30 localizes to the endoplasmic reticulum and is not activated by estradiol. Otto C, Rohde-Schulz B, Schwarz G, Fuchs I, Klewer M, Brittain D, Langer G, Bader B, Prelle K, Nubbemeyer R, Fritzemeier KH. Endocrinology. 2008 149:4846-56. (IF; Human, Monkey, Hamster) [Full Text Article] [PubMed:18566127] Related Antibodies: LS-A4272.
16
The G protein-coupled receptor GPR30 mediates the proliferative effects induced by 17beta-estradiol and hydroxytamoxifen in endometrial cancer cells. Vivacqua A, Bonofiglio D, Recchia AG, Musti AM, Picard D, Andò S and Maggiolini M. Molecular endocrinology (Baltimore, Md.). 2006 20:631-46. (WB; Human) [PubMed:16239258] [PMC:PMC3060528] Related Antibodies: LS-A1183.
17
Inhibition of the AKT/mTOR and erbB pathways by gefitinib, perifosine and analogs of gonadotropin-releasing hormoneI andII to overcome tamoxifen resistance in breast cancer cells. Block M, Gr[Character fc]ndker C, Fister S, Kubin J, Wilkens L, Mueller MD, Hemmerlein B, Emons G, G[Character fc]nthert AR. International journal of oncology. 2012 Nov;41:1845-54. [Full Text Article] [PubMed:22922893] Related Antibodies: LS-A1183.
18
Nuclear alternate estrogen receptor GPR30 mediates 17beta-estradiol-induced gene expression and migration in breast cancer-associated fibroblasts. Madeo A, Maggiolini M. Cancer research. 2010 Jul;70:6036-46. [Full Text Article] [PubMed:20551055] Related Antibodies: LS-A4271.
19
Identification of G protein-coupled estrogen receptor in human and pig spermatozoa. Rago V, Giordano F, Brunelli E, Zito D, Aquila S, Carpino A. Journal of anatomy. 2014 Jun;224:732-6. [Full Text Article] [PubMed:24697543] Related Antibodies: LS-A4271.
20
Expression pattern of G protein-coupled receptor 30 in LacZ reporter mice. Isensee J, Meoli L, Zazzu V, Nabzdyk C, Witt H, Soewarto D, Effertz K, Fuchs H, Gailus-Durner V, Busch D, Adler T, de Angelis MH, Irgang M, Otto C, Noppinger PR. Endocrinology. 2009 Apr;150:1722-30. [Full Text Article] [PubMed:19095739] Related Antibodies: LS-A4271.
21
G protein-coupled receptor 30 expression is up-regulated by EGF and TGF alpha in estrogen receptor alpha-positive cancer cells. Vivacqua A, Lappano R, De Marco P, Sisci D, Aquila S, De Amicis F, Fuqua SA, And[Character f2] S, Maggiolini M. Molecular endocrinology (Baltimore, Md.). 2009 Nov;23:1815-26. [Full Text Article] [PubMed:19749156] Related Antibodies: LS-A4271.
22
c-Jun activation is required for 4-hydroxytamoxifen-induced cell death in breast cancer cells. Madeo A, Vinciguerra M, Lappano R, Galgani M, Gasperi-Campani A, Maggiolini M, Musti AM. Oncogene. 2010 Feb;29:978-91. [Full Text Article] [PubMed:19935718] Related Antibodies: LS-A4271.
23
Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells. Lappano R, Rosano C, De Marco P, De Francesco EM, Pezzi V, Maggiolini M. Molecular and cellular endocrinology. 2010 May;320:162-70. [Full Text Article] [PubMed:20138962] Related Antibodies: LS-A4271.
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GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC of human breast carcinoma. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval.
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Neuroscience
GPER1 / GPR30 Rabbit anti-Human Polyclonal (N-Terminus) Antibody
Human
IF, IHC, IHC-P, WB
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC of human breast carcinoma. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval.
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Neuroscience
GPER1 / GPR30 Rabbit anti-Human Polyclonal (C-Terminus) Antibody
Dog, Rat, Human, Monkey
IF, IHC, IHC-Fr, IHC-P, WB
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC staining of human breast carcinoma. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval.
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Neuroscience
GPER1 / GPR30 Rabbit anti-Human Polyclonal (Cytoplasmic Domain) Antibody
Human
ICC, IHC, IHC-P, WB
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPER1 / GPR30 antibody IHC of human Colon, Carcinoma. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval.
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Neuroscience
GPER1 / GPR30 Rabbit anti-Human Polyclonal (Extracellular Domain) Antibody
Human
IF, IHC, IHC-P
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC of human brain, hippocampus. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval.
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Neuroscience
GPER1 / GPR30 Rabbit anti-Human Polyclonal (Extracellular Domain) Antibody
Human, Monkey
IF, IHC, IHC-P, WB
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC of human skeletal muscle. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval. Antibody dilution 5-7.5 ug/ml.
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Neuroscience
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (Extracellular Domain) Antibody
Human
ELISA, IHC, IHC-P
Unconjugated
50 µg/$440
GPER1 / GPR30 Antibody - Anti-GPR30 antibody IHC of human adrenal. Immunohistochemistry of formalin-fixed, paraffin-embedded tissue after heat-induced antigen retrieval. Antibody concentration 3.75 ug/ml.
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GPER1 / GPR30 Goat anti-Human Polyclonal (aa357-370) Antibody
Dog, Human, Monkey
IHC, IHC-P
Unconjugated
50 µg/$460
GPER1 / GPR30 Antibody - GPER / GPR30 antibody Western blot of Fetal Kidney lysate. Antibody concentration 1 ug/ml.  This image was taken for the unconjugated form of this product. Other forms have not been tested.
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa276-325) Antibody
Human
WB
Unconjugated
100 µl/$424
GPER1 / GPR30 Antibody - Immunohistochemistry of paraffin-embedded human placenta tissue at dilution of 1:100
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa1-62) Antibody
Human
ELISA, IF, IHC, IHC-P, WB
Unconjugated
50 µg/$294; 100 µg/$360
GPER1 / GPR30 Antibody - WB of GPER1 / GPR30 antibody. Lane 1: COLO320 Cell Lysate. Lane 2: MCF-7 Cell Lysate. Lane 3: COS7 Cell Lysate.
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa275-288) Antibody
Human
WB
Unconjugated
10 µg/$318; 100 µg/$470
GPER1 / GPR30 Antibody - Western blot analysis of extracts of various cell lines, using GPER1 antibody at 1:1000 dilution. The secondary antibody used was an HRP Goat Anti-Rabbit IgG (H+L) at 1:10000 dilution. Lysates were loaded 25ug per lane and 3% nonfat dry milk in TBST was used for blocking. An ECL Kit was used for detection and the exposure time was 90s.
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GPER1 / GPR30 Rabbit anti-Human Polyclonal Antibody
Mouse, Rat, Human
WB
Unconjugated
20 µl/$275; 100 µl/$389
GPER1 / GPR30 Antibody - GPER Antibody western blot of mouse liver tissue lysates (35 ug/lane). The GPER antibody detected the GPER protein (arrow).
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) Antibody
Mouse, Human
WB
Unconjugated
400 µl/$393
GPER1 / GPR30 ELISA Kit
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Sandwich
96-Well Microplate
Human
0.313 - 20 ng/ml
Colorimetric - 450nm (TMB)
Plasma, Serum
1 Plate/$586
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa1-23) Antibody
Mouse, Rat, Human
IHC, IHC-P
Unconjugated
100 µl/$1,027
GPER1 / GPR30 Protein - 12.5% SDS-PAGE of human GPR30 stained with Coomassie Blue
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Wheat Germ Extract
GST
68.6 kDa
2 µg/$439
GPER1 / GPR30 ELISA Kit
Select
Sandwich
96-Well Strip Plate
Human
0.312 - 20 ng/ml
Colorimetric - 450nm (TMB)
Plasma, Serum
1 Plate/$669
GPER1 / GPR30 ELISA Kit
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Sandwich
96-Well Strip Plate
Rat
78 - 5000 pg/ml
Colorimetric - 450nm (TMB)
Plasma, Serum
1 Plate/$669
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) Antibody
Mouse, Human
ELISA, WB
Unconjugated
200 µl/$734
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) (Biotin) Antibody
Mouse, Human
ELISA, WB
Biotin Conjugated
200 µl/$952
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) (FITC) Antibody
Mouse, Human
ELISA, WB
FITC Conjugated
200 µl/$952
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) (APC) Antibody
Mouse, Human
ELISA, WB
APC Conjugated
200 µl/$952
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GPER1 / GPR30 Rabbit anti-Human Polyclonal (aa346-375) (Azide-free) (HRP) Antibody
Mouse, Human
ELISA, WB
HRP Conjugated, Azide-free
200 µl/$952
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GPER1 / GPR30 Rabbit anti-Human Polyclonal Antibody
Mouse, Rat, Human
ELISA, WB
Unconjugated
100 µg/$357
GPER1 / GPR30 Antibody - Immunofluorescence analysis of C6 cells using GPER1 Polyclonal Antibody at dilution of 1:100.Blue: DAPI for nuclear staining.
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GPER1 / GPR30 Rabbit anti-Human Polyclonal Antibody
Mouse, Rat, Human
IF
Unconjugated
60 µl/$331; 120 µl/$403; 200 µl/$529
GPER1 / GPR30 Antibody - Western blot analysis of GPR30 expression in HepG2 cells lysate. The lane on the left is treated with the antigen-specific peptide.
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GPER1 / GPR30 Rabbit anti-Human Polyclonal Antibody
Mouse, Rat, Human
Peptide-ELISA, WB
Unconjugated
100 µl/$379; 200 µl/$421
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For RESEARCH USE ONLY. Intended for use by laboratory professionals. Not intended for human diagnostic or therapeutic purposes.

The data on this page has been compiled from LifeSpan internal sources, the National Center for Biotechnology Information (NCBI), and The Universal Protein Resource (UniProt).