The G protein-coupled oestrogen receptor GPER in health and disease: an update

Sex differences in immune responses

Klein, S. L., & Flanagan, K. L. (2016) · Nature Reviews Immunology · doi:10.1038/nri.2016.90 · Cited by 6,370

Cloning of a novel receptor expressed in rat prostate and ovary.

Kuiper, G. G. J. M., Enmark, E., Pelto‐Huikko, M., Nilsson, S., & Gustafsson, J.-Α. (1996) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.93.12.5925 · Cited by 4,802

Endocrine-Disrupting Chemicals: An Endocrine Society Scientific Statement

Diamanti-Kandarakis, E., Bourguignon, J.-P., Giudice, L. C., Hauser, R., Prins, G. S., Soto, A. M., Zoeller, R. T., & Gore, A. C. (2009) · Endocrine Reviews · doi:10.1210/er.2009-0002 · Cited by 4,585

A transmembrane intracellular estrogen receptor mediates rapid cell signaling

Revankar, C. M., Cimino, D. F., Sklar, L. A., Arterburn, J. B., & Prossnitz, E. R. (2005) · Science · doi:10.1126/science.1106943 · Cited by 2,302

ERβ: Identification and characterization of a novel human estrogen receptor

Mosselman, S., Polman, J., & Dijkema, R. (1996) · FEBS Letters · doi:10.1016/0014-5793(96)00782-x · Cited by 2,269

Sex and gender: modifiers of health, disease, and medicine

Mauvais-Jarvis, F., Bairey Merz, N., Barnes, P. J., Brinton, R. D., Carrero, J.-J., DeMeo, D. L., De Vries, G. J., Epperson, C. N., Govindan, R., Klein, S. L., et al. (2020) · The Lancet · doi:10.1016/s0140-6736(20)31561-0 · Cited by 2,001

Rate of Pregnancy-Related Relapse in Multiple Sclerosis

Confavreux, C., Hutchinson, M., Hours, M. M., Cortinovis-Tourniaire, P., & Moreau, T. (1998) · New England Journal of Medicine · doi:10.1056/nejm199807303390501 · Cited by 1,559

Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors

Daub, H., Weiß, F. U., Wallasch, C., & Ullrich, A. (1996) · Nature · doi:10.1038/379557a0 · Cited by 1,476

Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells

Thomas, P., Pang, Y., Filardo, E. J., & Dong, J. (2004) · Endocrinology · doi:10.1210/en.2004-1064 · Cited by 1,410

Estrogen-Induced Activation of Erk-1 and Erk-2 Requires the G Protein-Coupled Receptor Homolog, GPR30, and Occurs via Trans-Activation of the Epidermal Growth Factor Receptor through Release of HB-EGF

Filardo, E. J., Quinn, J. A., Bland, K. I., & Frackelton, A. R. (2000) · Molecular Endocrinology · doi:10.1210/mend.14.10.0532 · Cited by 1,387

The role of estrogens in control of energy balance and glucose homeostasis

Mauvais-Jarvis, F., Clegg, D. J., & Hevener, A. L. (2013) · Endocrine Reviews · doi:10.1210/er.2012-1055 · Cited by 1,329

A two-step mechanism for the interaction of estradiol with rat uterus.

Jensen, E. V., Suzuki, T., Kawashima, T., Stumpf, W. E., Jungblut, P. W., & DeSombre, E. R. (1968) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.59.2.632 · Cited by 1,015

The G-protein-coupled estrogen receptor GPER in health and disease

Prossnitz, E. R., & Barton, M. (2011) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2011.122 · Cited by 925 · cited 1×

Estrogen Action Via the G Protein-Coupled Receptor, GPR30: Stimulation of Adenylyl Cyclase and cAMP-Mediated Attenuation of the Epidermal Growth Factor Receptor-to-MAPK Signaling Axis

Filardo, E. J., Quinn, J. A., Frackelton, A. R., & Bland, K. I. (2002) · Molecular Endocrinology · doi:10.1210/mend.16.1.0758 · Cited by 907

Tamoxifen: a most unlikely pioneering medicine

Jordan, V. C. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1031 · Cited by 832

Virtual and biomolecular screening converge on a selective agonist for GPR30

Bologa, C., Revankar, C. M., Young, S. M., Edwards, B. S., Arterburn, J. B., Kiselyov, A. S., Parker, M. A., Tkachenko, S. E., Savchuk, N., Sklar, L. A., et al. (2006) · Nature Chemical Biology · doi:10.1038/nchembio775 · Cited by 819

Pyrazole Ligands: Structure−Affinity/Activity Relationships and Estrogen Receptor-α-Selective Agonists

Stauffer, S. R., Coletta, C. J., Tedesco, R., Nishiguchi, G., Carlson, K. E., Sun, J., Katzenellenbogen, B. S., & Katzenellenbogen, J. A. (2000) · Journal of Medicinal Chemistry · doi:10.1021/jm000170m · Cited by 760

Estrogen receptors alpha (ERα) and beta (ERβ): Subtype-selective ligands and clinical potential

Paterni, I., Granchi, C., Katzenellenbogen, J. A., & Minutolo, F. (2014) · Steroids · doi:10.1016/j.steroids.2014.06.012 · Cited by 736

Cloning of the human estrogen receptor cDNA.

Walter, P., Green, S., Greene, G. L., Krust, A., Bornert, J., Jeltsch, J., Staub, A., Jensen, E. Ø., Scrace, G., & Waterfield, M. D. (1985) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.82.23.7889 · Cited by 731

A receptor molecule for estrogens: isolation from the rat uterus and preliminary characterization.

Toft, D. O., & Górski, J. (1966) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.55.6.1574 · Cited by 682

Estrogen Receptor-β Potency-Selective Ligands: Structure−Activity Relationship Studies of Diarylpropionitriles and Their Acetylene and Polar Analogues

Meyers, M. J., Sun, J., Carlson, K. E., Marriner, G. A., Katzenellenbogen, B. S., & Katzenellenbogen, J. A. (2001) · Journal of Medicinal Chemistry · doi:10.1021/jm010254a · Cited by 678

Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: A potential novel mechanism of endocrine disruption

Thomas, P., & Dong, J. (2006) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2006.09.017 · Cited by 604

Identification of a Gene (GPR30) with Homology to the G-Protein-Coupled Receptor Superfamily Associated with Estrogen Receptor Expression in Breast Cancer

Carmeci, C., Thompson, D. A., Ring, H. Z., Francke, U., & Weigel, R. J. (1997) · Genomics · doi:10.1006/geno.1997.4972 · Cited by 590

In vivo effects of a GPR30 antagonist

Dennis, M. K., Burai, R., Ramesh, C., Petrie, W. K., Alcon, S. N., Nayak, T. K., Bologa, C., Leitão, A., Brailoiu, E., Deliu, E., et al. (2009) · Nature Chemical Biology · doi:10.1038/nchembio.168 · Cited by 533

Guide to Receptors and Channels (GRAC), 3rd edition

Alexander, S. P. H., Mathie, A. A., & Peters, J. A. (2008) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707746 · Cited by 510

Estrogens protect pancreatic β-cells from apoptosis and prevent insulin-deficient diabetes mellitus in mice

May, C. L., Chu, K., Hu, M., Ortega, C. S., Simpson, E. R., Korach, K. S., Tsai, M., & Mauvais‐Jarvis, F. (2006) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0602956103 · Cited by 508

AN OVARIAN HORMONE

Allen, E., & Doisy, E. A. (1923) · JAMA · doi:10.1001/jama.1923.02650100027012 · Cited by 479

The estrogen receptor: a model for molecular medicine.

Jensen, E. V., & Jordan, V. C. (2003) · PubMed · Cited by 470

The G Protein-coupled Receptor GPR30 Mediates c-fos Up-regulation by 17β-Estradiol and Phytoestrogens in Breast Cancer Cells

Maggiolini, M., Vivacqua, A., Fasanella, G., Recchia, A. G., Sisci, D., Pezzi, V., Montanaro, D., Musti, A. M., Picard, D., & Andò, S. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m403588200 · Cited by 448

Deletion of the G Protein-Coupled Receptor 30 Impairs Glucose Tolerance, Reduces Bone Growth, Increases Blood Pressure, and Eliminates Estradiol-Stimulated Insulin Release in Female Mice

Mårtensson, U. E. A., Salehi, A. A., Windahl, S. H., Gomez, M. F., Swärd, K., Daszkiewicz-Nilsson, J., Wendt, A., Andersson, N., Hellstrand, P., Grände, P., et al. (2008) · Endocrinology · doi:10.1210/en.2008-0623 · Cited by 419

Adenosine 3',5'-monophosphate in rat uterus: acute elevation by estrogen.

Szego, C. M., & Davis, J. S. (1967) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.58.4.1711 · Cited by 406

G Protein–Coupled Receptor 30 (GPR30) Mediates Gene Expression Changes and Growth Response to 17β-Estradiol and Selective GPR30 Ligand G-1 in Ovarian Cancer Cells

Albanito, L., Madeo, A., Lappano, R., Vivacqua, A., Rago, V., Carpino, A., Oprea, T. I., Prossnitz, E. R., Musti, A. M., Andò, S., et al. (2007) · Cancer Research · doi:10.1158/0008-5472.can-06-2909 · Cited by 399

Regulatory role of G protein-coupled estrogen receptor for vascular function and obesity

Haas, E., Bhattacharya, I., Brailoiu, E., Damjanović, M., Brailoiu, G. C., Gao, X., Mueller-Guerre, L., Marjon, N. A., Gut, A., Minotti, R., et al. (2009) · Circulation Research · doi:10.1161/circresaha.108.190892 · Cited by 373

Distribution of GPR30, a Seven Membrane–Spanning Estrogen Receptor, in Primary Breast Cancer and its Association with Clinicopathologic Determinants of Tumor Progression

Filardo, E. J., Graeber, C. T., Quinn, J. A., Resnick, M. B., Giri, D. D., DeLellis, R. A., Steinhoff, M. M., & Sabo, E. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-0860 · Cited by 361

Estrogen modulates abdominal adiposity and protects female mice from obesity and impaired glucose tolerance

Stubbins, R., Holcomb, V. B., Hong, J., & Núñez, N. P. (2011) · European Journal of Nutrition · doi:10.1007/s00394-011-0266-4 · Cited by 356

Obesity and cancer: the role of adipose tissue and adipo-cytokines-induced chronic inflammation

Divella, R., Luca, R. D., Abbate, I., Naglieri, E., & Daniele, A. (2016) · Journal of Cancer · doi:10.7150/jca.16884 · Cited by 355

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, A., Musti, A., Picard, D., Andò, S., & Maggiolini, M. (2006) · Molecular Endocrinology · doi:10.1210/me.2005-0280 · Cited by 345

Obesity, insulin resistance and diabetes: sex differences and role of oestrogen receptors

Meyer, M. R., Clegg, D. J., Prossnitz, E. R., & Barton, M. (2011) · Acta Physiologica · doi:10.1111/j.1748-1716.2010.02237.x · Cited by 338

Discovery of Three Novel G-Protein-Coupled Receptor Genes

O’Dowd, B. F., Nguyen, T., Marchese, A., Cheng, R., Lynch, K. R., Heng, H. H., Kolakowski, L. F., & George, S. R. (1998) · Genomics · doi:10.1006/geno.1998.5095 · Cited by 335

Estrogenic GPR30 signalling induces proliferation and migration of breast cancer cells through CTGF

Pandey, D. P., Lappano, R., Albanito, L., Madeo, A., Maggiolini, M., & Picard, D. (2009) · The EMBO Journal · doi:10.1038/emboj.2008.304 · Cited by 327

Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity

Dennis, M. K., Field, A. S., Burai, R., Ramesh, C., Petrie, W. K., Bologa, C., Oprea, T. I., Yamaguchi, Y., Hayashi, S., Sklar, L. A., et al. (2011) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2011.07.002 · Cited by 312

Estrogen Receptor Signaling in the Immune System

Chakraborty, B., Byemerwa, J. K., Krebs, T., Lim, F., Chang, C., & McDonnell, D. P. (2022) · Endocrine Reviews · doi:10.1210/endrev/bnac017 · Cited by 283

International Union of Basic and Clinical Pharmacology. XCVII. G Protein–Coupled Estrogen Receptor and Its Pharmacologic Modulators

Prossnitz, E. R., & Arterburn, J. B. (2015) · Pharmacological Reviews · doi:10.1124/pr.114.009712 · Cited by 269

Endometrial cell calcium and oestrogen action

Pietras, R. J., & Szego, C. M. (1975) · Nature · doi:10.1038/253357a0 · Cited by 266

Twenty years of the G protein-coupled estrogen receptor GPER: Historical and personal perspectives

Barton, M., Filardo, E. J., Lolait, S. J., Thomas, P., Maggiolini, M., & Prossnitz, E. R. (2017) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2017.03.021 · Cited by 262

The G Protein–Coupled Receptor GPR30 Inhibits Proliferation of Estrogen Receptor–Positive Breast Cancer Cells

Ariazi, E. A., Brailoiu, E., Yerrum, S., Shupp, H. A., Slifker, M. J., Cunliffe, H. E., Black, M. A., Donato, A. L., Arterburn, J. B., Oprea, T. I., et al. (2010) · Cancer Research · doi:10.1158/0008-5472.can-09-3068 · Cited by 236

A NON-STEROIDAL ESTROGEN ANTAGONIST l-(p-2-DIETHYLAMINOETHOXYPHENYLH-PHENYL-2-p-METHOXYPHENYL ETHANOL

Lerner, L. J., HOLTHAUS, F. J., & THOMPSON, C. R. (1958) · Endocrinology · doi:10.1210/endo-63-3-295 · Cited by 233

Estrogen regulates Hippo signaling via GPER in breast cancer

Zhou, X., Wang, S., Wang, Z., Feng, X., Liu, P., Lv, X.-B., Li, F., Yu, F.-X., Sun, Y., Yuan, H., et al. (2015) · Journal of Clinical Investigation · doi:10.1172/jci79573 · Cited by 232

Cloning of Human cDNA Encoding a Novel Heptahelix Receptor Expressed in Burkitt's Lymphoma and Widely Distributed in Brain and Peripheral Tissues

Owman, C., Blay, P., Nilsson, C., & Lolait, S. J. (1996) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1996.1654 · Cited by 224

The effect of conjugated equine oestrogen on diabetes incidence: the Women’s Health Initiative randomised trial

Bonds, D. E., Lasser, N. L., Qi, L., Brzyski, R. G., Caan, B. J., HEISS, G. M., Limacher, M. C., LIU, J. H., Mason, E. D., Oberman, A., et al. (2006) · Diabetologia · doi:10.1007/s00125-005-0096-0 · Cited by 216

Activation of GPR30 inhibits the growth of prostate cancer cells through sustained activation of Erk1/2, c-jun/c-fos-dependent upregulation of p21, and induction of G2 cell-cycle arrest

Chan, Q. K. Y., Lam, H. C. M., Ng, C., Lee, A., Chan, E. S. Y., Ng, H., Ho, S., & Lau, K.-M. (2010) · Cell Death and Differentiation · doi:10.1038/cdd.2010.20 · Cited by 211

A novel genetic locus for low renin hypertension: familial hyperaldosteronism type II maps to chromosome 7 (7p22)

Lafferty, A. R. A., Torpy, D. J., Stowasser, M., Taymans, S. E., Lin, J. P., Huggard, P., Gordon, R. D., & Stratakis, C. A. (2000) · Journal of Medical Genetics · doi:10.1136/jmg.37.11.831 · Cited by 211

Cloning of cDNAs Encoding G Protein-Coupled Receptor Expressed in Human Endothelial Cells Exposed to Fluid Shear Stress

Takada, Y., Kato, C., Kondo, S., Korenaga, R., & Ando, J. (1997) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1997.7734 · Cited by 210

GPER deficiency in male mice results in insulin resistance, dyslipidemia, and a proinflammatory state

Sharma, G., Hu, C., Brigman, J. L., Zhu, G., Hathaway, H. J., & Prossnitz, E. R. (2013) · Endocrinology · doi:10.1210/en.2013-1357 · Cited by 210

GPR30 predicts poor survival for ovarian cancer

Smith, H. O., Arias‐Pulido, H., Kuo, D. Y., Howard, T. A., Qualls, C., Lee, S. J., Verschraegen, C. F., Hathaway, H. J., Joste, N. E., & Prossnitz, E. R. (2009) · Gynecologic Oncology · doi:10.1016/j.ygyno.2009.05.015 · Cited by 206

The novel estrogenic receptor GPR30 alleviates ischemic injury by inhibiting TLR4-mediated microglial inflammation

Zhang, Z., Qin, P., Deng, Y., Ma, Z., Guo, H., Guo, H., Hou, Y., Wang, S., Zou, W., Sun, Y., et al. (2018) · Journal of Neuroinflammation · doi:10.1186/s12974-018-1246-x · Cited by 199

Importance of Extranuclear Estrogen Receptor-α and Membrane G Protein–Coupled Estrogen Receptor in Pancreatic Islet Survival

Liu, S., May, C. L., Wong, W. P. S., Ward, R. D., Clegg, D. J., Marcelli, M., Korach, K. S., & Mauvais‐Jarvis, F. (2009) · Diabetes · doi:10.2337/db09-0257 · Cited by 198

A novel estrogen receptor gper inhibits mitochondria permeability transition pore opening and protects the heart against ischemia-reperfusion injury

Bopassa, J. C., Eghbali, M., Toro, L., & Stefani, E. (2010) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.00588.2009 · Cited by 197

Estrogen anti-inflammatory activity on human monocytes is mediated through cross-talk between estrogen receptor ERα36 and GPR30/GPER1

Pelekanou, V., Kampa, M., Kiagiadaki, F., Deli, A., Theodoropoulos, P., Agrogiannis, G., Patsouris, E., Tsapis, A., Castanas, E., & Notas, G. (2016) · Journal of Leukocyte Biology · doi:10.1189/jlb.3a0914-430rr · Cited by 184

Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis

Blasko, E., Haskell, C. A., Leung, S., Gualtieri, G., Halks‐Miller, M., Mahmoudi, M., Dennis, M. K., Prossnitz, E. R., Karpus, W. J., & Horuk, R. (2009) · Journal of Neuroimmunology · doi:10.1016/j.jneuroim.2009.06.023 · Cited by 183

Nuclear Alternate Estrogen Receptor GPR30 Mediates 17β-Estradiol–Induced Gene Expression and Migration in Breast Cancer–Associated Fibroblasts

Madeo, A., & Maggiolini, M. (2010) · Cancer Research · doi:10.1158/0008-5472.can-10-0408 · Cited by 183

Estrogen receptors in uterine plasma membrane

Pietras, R. J., & Szego, C. M. (1979) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(79)90124-9 · Cited by 177

G-protein-coupled estrogen receptor GPR30 and tamoxifen resistance in breast cancer

Ignatov, A., Ignatov, T., Weißenborn, C., Eggemann, H., Bischoff, J., Semczuk, A., Roessner, A., Costa, S. D., & Kalinski, T. (2011) · Breast Cancer Research and Treatment · doi:10.1007/s10549-011-1584-1 · Cited by 172

Role of GPR30 in the mechanisms of tamoxifen resistance in breast cancer MCF-7 cells

Ignatov, A., Ignatov, T., Roessner, A., Costa, S. D., & Kalinski, T. (2009) · Breast Cancer Research and Treatment · doi:10.1007/s10549-009-0624-6 · Cited by 168

G Protein-Coupled Estrogen Receptor-Selective Ligands Modulate Endometrial Tumor Growth

Petrie, W. K., Dennis, M. K., Hu, C., Dai, D. D., Arterburn, J. B., Smith, H. O., Hathaway, H. J., & Prossnitz, E. R. (2013) · Obstetrics and Gynecology International · doi:10.1155/2013/472720 · Cited by 166

Differential Effects of 17β-Estradiol on Function and Expression of Estrogen Receptor α, Estrogen Receptor β, and GPR30 in Arteries and Veins of Patients With Atherosclerosis

Haas, E., Meyer, M. R., Schurr, U. P., Bhattacharya, I., Minotti, R., Nguyen, H. H., Heigl, A., Lachat, M. L., Genoni, M., & Barton, M. (2007) · Hypertension · doi:10.1161/hypertensionaha.107.089995 · Cited by 165

New insights into the molecular mechanisms underlying effects of estrogen on cholesterol gallstone formation

Wang, H. H., Liu, M., Clegg, D. J., Portincasa, P., & Wang, D. Q. ‐. (2009) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2009.06.006 · Cited by 160

Estrogen Rescues Preexisting Severe Pulmonary Hypertension in Rats

Umar, S., Iorga, A., Matori, H., Nadadur, R. D., Li, J., Maltese, F., van der Laarse, A., & Eghbali, M. (2011) · American Journal of Respiratory and Critical Care Medicine · doi:10.1164/rccm.201101-0078oc · Cited by 159

What have we learned about GPER function in physiology and disease from knockout mice

Prossnitz, E. R., & Hathaway, H. J. (2015) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2015.06.014 · Cited by 157

G Protein-coupled Estrogen Receptor Protects from Atherosclerosis

Meyer, M. R., Fredette, N. C., Howard, T. A., Hu, C., Ramesh, C., Daniel, C., Amann, K., Arterburn, J. B., Barton, M., & Prossnitz, E. R. (2014) · Scientific Reports · doi:10.1038/srep07564 · Cited by 156

Activation of G protein-coupled estrogen receptor signaling inhibits melanoma and improves response to immune checkpoint blockade

Natale, C. A., Li, J., Zhang, J., Dahal, A., Dentchev, T., Stanger, B. Z., & Ridky, T. W. (2018) · eLife · doi:10.7554/elife.31770 · Cited by 155

�ber ?Progynon? ein krystallisiertes weibliches Sexualhormon

Butenandt, A. (1929) · Die Naturwissenschaften · doi:10.1007/bf01506919 · Cited by 149

Membrane Estrogen Receptor Regulates Experimental Autoimmune Encephalomyelitis through Up-regulation of Programmed Death 1

Wang, C., Dehghani, B., Li, Y., Kaler, L. J., Proctor, T., Vandenbark, A. A., & Offner, H. (2009) · The Journal of Immunology · doi:10.4049/jimmunol.0803205 · Cited by 148

Crosstalk between Notch, HIF-1α and GPER in Breast Cancer EMT

Francesco, E. M. D., Maggiolini, M., & Musti, A. M. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19072011 · Cited by 148

Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo

Hutchens, M. P., Fujiyoshi, T., Komers, R., Herson, P. S., & Anderson, S. (2012) · American Journal of Physiology-Renal Physiology · doi:10.1152/ajprenal.00354.2011 · Cited by 148

Mechanisms of Estradiol-Induced Insulin Secretion by the G Protein-Coupled Estrogen Receptor GPR30/GPER in Pancreatic β-Cells

Sharma, G., & Prossnitz, E. R. (2011) · Endocrinology · doi:10.1210/en.2011-0091 · Cited by 143

Sex steroids regulate skin pigmentation through nonclassical membrane-bound receptors

Natale, C. A., Duperret, E. K., Zhang, J., Sadeghi, R. S., Dahal, A., O'Brien, K. T., Cookson, R., Winkler, J. D., & Ridky, T. W. (2016) · eLife · doi:10.7554/elife.15104 · Cited by 138

GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer

Mo, Z., Liu, M., Yang, F., Luo, H., Li, Z., Tu, G., & Yang, G. (2013) · Breast Cancer Research · doi:10.1186/bcr3581 · Cited by 134

GPER Mediates Activation of HIF1α/VEGF Signaling by Estrogens

Francesco, E. M. D., PELLEGRINO, M. A., Santolla, M. F., Lappano, R., Ricchio, E., Abonante, S., & Maggiolini, M. (2014) · Cancer Research · doi:10.1158/0008-5472.can-13-3590 · Cited by 133

TAMOXIFEN AS AN ANTI-TUMOUR AGENT: EFFECT ON OESTROGEN BINDING

Jordan, V. C., & DOWSE, L. J. (1976) · Journal of Endocrinology · doi:10.1677/joe.0.0680297 · Cited by 133

Activation of G protein‐coupled oestrogen receptor 1 at the onset of reperfusion protects the myocardium against ischemia/reperfusion injury by reducing mitochondrial dysfunction and mitophagy

Feng, Y., Madungwe, N. B., Junho, C. V. C., & Bopassa, J. C. (2017) · British Journal of Pharmacology · doi:10.1111/bph.14033 · Cited by 131

Inhibition of estrogen signaling in myeloid cells increases tumor immunity in melanoma

Chakraborty, B., Byemerwa, J. K., Shepherd, J., Haines, C., Baldi, R., Gong, W., Liu, W., Mukherjee, D., Artham, S., Lim, F., et al. (2021) · Journal of Clinical Investigation · doi:10.1172/jci151347 · Cited by 131

Contributions of sex to cerebrovascular function and pathology

Robison, L. S., Gannon, O. J., Salinero, A. E., & Zuloaga, K. L. (2018) · Brain Research · doi:10.1016/j.brainres.2018.12.030 · Cited by 129

Estradiol and G1 Reduce Infarct Size and Improve Immunosuppression after Experimental Stroke

Zhang, B., Subramanian, S., Dziennis, S., Jia, J., Uchida, M., Akiyoshi, K., Migliati, E., Lewis, A. D., Vandenbark, A. A., Offner, H., et al. (2010) · The Journal of Immunology · doi:10.4049/jimmunol.0902339 · Cited by 127

Role of GPER in estrogen-dependent nitric oxide formation and vasodilation

Fredette, N. C., Meyer, M. R., & Prossnitz, E. R. (2017) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2017.05.006 · Cited by 126

The Women's Health Initiative trial and related studies: 10 years later: A clinician's view

Gurney, E. P., Nachtigall, M. J., Nachtigall, L. E., & Naftolin, F. N. (2013) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2013.10.009 · Cited by 125

Activation of GPR30 attenuates diastolic dysfunction and left ventricle remodelling in oophorectomized mRen2.Lewis rats

Wang, H., Jessup, J. A., Lin, M. S., Chagas, C., Lindsey, S. H., & Groban, L. (2012) · Cardiovascular Research · doi:10.1093/cvr/cvs090 · Cited by 121

The History of DES, Lessons to be Learned

Veurink, M., Koster, M. E., & den Berg, L. T. W. D. J. (2005) · Pharmacy World & Science · doi:10.1007/s11096-005-3663-z · Cited by 121

Sex and the kidneys: current understanding and research opportunities

Merz, C. N. B., Dember, L. M., Ingelfinger, J. R., Vinson, A. J., Neugarten, J., Sandberg, K. L., Sullivan, J. C., Maric‐Bilkan, C., Rankin, T. L., Kimmel, P. L., et al. (2019) · Nature Reviews Nephrology · doi:10.1038/s41581-019-0208-6 · Cited by 119

Expression and Signaling of G Protein-Coupled Estrogen Receptor 1 (GPER) in Rat Sertoli Cells1

Lucas, T. F. G., Royer, C., Siu, E. R., Lazari, M. F. M., & Porto, C. S. (2010) · Biology of Reproduction · doi:10.1095/biolreprod.110.084160 · Cited by 119

The G Protein-coupled Receptor 30 Is Up-regulated by Hypoxia-inducible Factor-1α (HIF-1α) in Breast Cancer Cells and Cardiomyocytes

Recchia, A. G., Francesco, E. M. D., Vivacqua, A., Sisci, D., Panno, M. L., Andò, S., & Maggiolini, M. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.172247 · Cited by 117

The G-protein coupled estrogen receptor, GPER: The inside and inside-out story

Gaudet, H. M., Cheng, S., Christensen, E. M., & Filardo, E. J. (2015) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2015.07.016 · Cited by 117

Dilation of Epicardial Coronary Arteries by the G Protein-Coupled Estrogen Receptor Agonists G-1 and ICI 182,780

Meyer, M. R., Baretella, O., Prossnitz, E. R., & Barton, M. (2010) · Pharmacology · doi:10.1159/000315497 · Cited by 116

Estrogen Receptor GPR30 Reduces Oxidative Stress and Proteinuria in the Salt-Sensitive Female mRen2.Lewis Rat

Lindsey, S. H., Yamaleyeva, L. M., Brosnihan, K. B., Gallagher, P. E., & Chappell, M. C. (2011) · Hypertension · doi:10.1161/hypertensionaha.111.175174 · Cited by 112

GPER Mediates Estrogen-Induced Signaling and Proliferation in Human Breast Epithelial Cells and Normal and Malignant Breast

Scaling, A. L., Prossnitz, E. R., & Hathaway, H. J. (2014) · Hormones and Cancer · doi:10.1007/s12672-014-0174-1 · Cited by 111

GPR30 mediates estrogen rapid signaling and neuroprotection

Tang, H., Zhang, Q., Yang, L., Dong, Y., Khan, M. B., Yang, F., Brann, D. W., & Wang, R. (2014) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2014.01.024 · Cited by 110

RHYTHMIC VASCULAR UTERINE CHANGES

Markee, J. E. (1932) · American Journal of Physiology-Legacy Content · doi:10.1152/ajplegacy.1932.100.1.32 · Cited by 110

Estrogen Activation of G-Protein–Coupled Estrogen Receptor 1 Regulates Phosphoinositide 3-Kinase and mTOR Signaling to Promote Liver Growth in Zebrafish and Proliferation of Human Hepatocytes

Chaturantabut, S., Shwartz, A., Evason, K. J., Cox, A. G., LaBella, K. A., Schepers, A. G., Yang, S. P., Acuña, M., Houvras, Y. J., Mâncio-Silva, L., et al. (2019) · Gastroenterology · doi:10.1053/j.gastro.2019.01.010 · Cited by 108

Preclinical efficacy of the GPER-selective agonist G-1 in mouse models of obesity and diabetes

Sharma, G., Hu, C., Staquicini, D. I., Brigman, J. L., Liu, M., Mauvais‐Jarvis, F., Pasqualini, R., Arap, W., Arterburn, J. B., Hathaway, H. J., et al. (2020) · Science Translational Medicine · doi:10.1126/scitranslmed.aau5956 · Cited by 108

Sexually dimorphic role of G protein-coupled estrogen receptor (GPER) in modulating energy homeostasis

Davis, K. E., Carstens, E. J., Irani, B. G., Gent, L. M., Hahner, L., & Clegg, D. J. (2014) · Hormones and Behavior · doi:10.1016/j.yhbeh.2014.02.004 · Cited by 107

Vasodilation by GPER in mesenteric arteries involves both endothelial nitric oxide and smooth muscle cAMP signaling

Lindsey, S. H., Liu, L., & Chappell, M. C. (2013) · Steroids · doi:10.1016/j.steroids.2013.10.017 · Cited by 107

A novel putative G‐protein‐coupled receptor expressed in lung, heart and lymphoid tissue

Kvingedal, A. M., & Smeland, E. B. (1997) · FEBS Letters · doi:10.1016/s0014-5793(97)00278-0 · Cited by 106

Hormonal Action of Plant Derived and Anthropogenic Non-Steroidal Estrogenic Compounds: Phytoestrogens and Xenoestrogens

Lóránd, T., Vigh, É., & Garai, J. (2010) · Current Medicinal Chemistry · doi:10.2174/092986710792927813 · Cited by 105

Induction of interleukin-10 in the T helper type 17 effector population by the G protein coupled estrogen receptor (GPER) agonist G-1

Brunsing, R. L., & Prossnitz, E. R. (2011) · Immunology · doi:10.1111/j.1365-2567.2011.03471.x · Cited by 104

Attenuation of Salt-Induced Cardiac Remodeling and Diastolic Dysfunction by the GPER Agonist G-1 in Female mRen2.Lewis Rats

Jessup, J. A., Lindsey, S. H., Wang, H., Chappell, M. C., & Groban, L. (2010) · PLoS ONE · doi:10.1371/journal.pone.0015433 · Cited by 104

Activation of G protein-coupled estrogen receptor induces endothelium-independent relaxation of coronary artery smooth muscle

Yu, X., Ma, H., Barman, S. A., Liu, A. T., Sellers, M., Stallone, J. N., Prossnitz, E. R., White, R. E., & Han, G. (2011) · American Journal of Physiology-Endocrinology and Metabolism · doi:10.1152/ajpendo.00037.2011 · Cited by 102

Cloning of a Novel Member of the G Protein-Coupled Receptor Family Related to Peptide Receptors

Feng, Y., & Gregor, P. (1997) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1997.6161 · Cited by 102

Anatomical location and redistribution of G protein-coupled estrogen receptor-1 during the estrus cycle in mouse kidney and specific binding to estrogens but not aldosterone

Cheng, S., Dong, J., Pang, Y., LaRocca, J. L., Hixon, M. L., Thomas, P., & Filardo, E. J. (2013) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2013.11.005 · Cited by 102

GPR30/GPER-1 mediates rapid decreases in TLR4 expression on murine macrophages

Rettew, J. A., McCall, S. H., & Marriott, I. (2010) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2010.07.017 · Cited by 99

Tamoxifen through GPER upregulates aromatase expression: a novel mechanism sustaining tamoxifen-resistant breast cancer cell growth

Catalano, S., Giordano, C., Panza, S., Chemi, F., Bonofiglio, D., Lanzino, M., Rizza, P., Romeo, F., Fuqua, S. A. W., Maggiolini, M., et al. (2014) · Breast Cancer Research and Treatment · doi:10.1007/s10549-014-3017-4 · Cited by 97

Estrogen Inhibits LDL (Low-Density Lipoprotein) Transcytosis by Human Coronary Artery Endothelial Cells via GPER (G-Protein–Coupled Estrogen Receptor) and SR-BI (Scavenger Receptor Class B Type 1)

Ghaffari, S., Nabi, F. N., Sugiyama, M. G., & Lee, W. L. (2018) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.118.310792 · Cited by 97

Design of pathway preferential estrogens that provide beneficial metabolic and vascular effects without stimulating reproductive tissues

Madak‐Erdogan, Z., Kim, S. H., Gong, P., Zhao, Y. C., Zhang, H., Chambliss, K. L., Carlson, K. E., Mayne, C. G., Shaul, P. W., Korach, K. S., et al. (2016) · Science Signaling · doi:10.1126/scisignal.aad8170 · Cited by 95

Oleuropein and hydroxytyrosol activate GPER / GPR 30‐dependent pathways leading to apoptosis of ER ‐negative SKBR 3 breast cancer cells

Chimento, A., Casaburi, I., Rosano, C., Avena, P., Luca, A. D., Campana, C., Martire, E., Santolla, M. F., Maggiolini, M., Pezzi, V., et al. (2013) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.201300323 · Cited by 94

MIBE acts as antagonist ligand of both estrogen receptor α and GPER in breast cancer cells

Lappano, R., Santolla, M. F., Pupo, M., Sinicropi, M. S., Caruso, A., Rosano, C., & Maggiolini, M. (2012) · Breast Cancer Research · doi:10.1186/bcr3096 · Cited by 94

G Protein–Coupled Estrogen Receptor Regulates Mammary Tumorigenesis and Metastasis

Marjon, N. A., Hu, C., Hathaway, H. J., & Prossnitz, E. R. (2014) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-14-0128-t · Cited by 92

GPER-mediated proliferation and estradiol production in breast cancer-associated fibroblasts

Luo, H., Yang, G., Yu, T., Luo, S., Wu, C., Sun, Y., Liu, M., & Tu, G. (2014) · Endocrine Related Cancer · doi:10.1530/erc-13-0237 · Cited by 89

Activation of G protein-coupled receptor 30 modulates hormone secretion and counteracts cytokine-induced apoptosis in pancreatic islets of female mice

Balhuizen, A., Kumar, R., Amisten, S., Lundquist, I., & Salehi, A. A. (2010) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2010.01.030 · Cited by 85

GPER signalling in both cancer-associated fibroblasts and breast cancer cells mediates a feedforward IL1β/IL1R1 response

Marco, P. D., Lappano, R., Francesco, E. M. D., Cirillo, F., Pupo, M., Avino, S., Vivacqua, A., Abonante, S., Picard, D., & Maggiolini, M. (2016) · Scientific Reports · doi:10.1038/srep24354 · Cited by 83

Rescue of Pressure Overload‐Induced Heart Failure by Estrogen Therapy

Iorga, A., Li, J., Sharma, S., Umar, S., Bopassa, J. C., Nadadur, R. D., Centala, A., Ren, S. V., Saito, T., Toro, L., et al. (2016) · Journal of the American Heart Association · doi:10.1161/jaha.115.002482 · Cited by 82

Obligatory role for GPER in cardiovascular aging and disease

Meyer, M. R., Fredette, N. C., Daniel, C., Sharma, G., Amann, K., Arterburn, J. B., Barton, M., & Prossnitz, E. R. (2016) · Science Signaling · doi:10.1126/scisignal.aag0240 · Cited by 81

GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment

Cortés, E., Sarper, M., Robinson, B. K., Lachowski, D., Chronopoulos, A., Thorpe, S. D., Lee, D. A., & Hernández, A. E. D. R. (2018) · EMBO Reports · doi:10.15252/embr.201846556 · Cited by 81

Insulinotropic and Antidiabetic Effects of 17β-Estradiol and the GPR30 Agonist G-1 on Human Pancreatic Islets

Kumar, R., Balhuizen, A., Amisten, S., Lundquist, I., & Salehi, A. A. (2011) · Endocrinology · doi:10.1210/en.2010-1361 · Cited by 80

Two Novel GPER Agonists Induce Gene Expression Changes and Growth Effects in Cancer Cells

Lappano, R., Rosano, C., Santolla, M. F., Pupo, M., Francesco, E. M. D., Marco, P. D., Ponassi, M., Spallarossa, A., Ranise, A., & Maggiolini, M. (2012) · Current Cancer Drug Targets · doi:10.2174/156800912800673284 · Cited by 80

Regulation of Vascular Smooth Muscle Tone by Adipose-Derived Contracting Factor

Meyer, M. R., Fredette, N. C., Barton, M., & Prossnitz, E. R. (2013) · PLoS ONE · doi:10.1371/journal.pone.0079245 · Cited by 79

Estrogens and Coronary Artery Disease

Meyer, M. R., & Barton, M. (2016) · Advances in pharmacology · doi:10.1016/bs.apha.2016.05.003 · Cited by 79

GPER/Hippo-YAP signal is involved in Bisphenol S induced migration of triple negative breast cancer (TNBC) cells

Deng, Q., Jiang, G., Wu, Y., Li, J., Liang, W., Chen, L., Su, Q., Li, W., Du, J., Wong, C. K. C., et al. (2018) · Journal of Hazardous Materials · doi:10.1016/j.jhazmat.2018.05.013 · Cited by 77

G protein‐coupled oestrogen receptor promotes cell growth of non‐small cell lung cancer cells via YAP1/QKI/circNOTCH1/m6A methylated NOTCH1 signalling

Shen, Y., Li, C., Zhou, L. M., & Huang, J. (2020) · Journal of Cellular and Molecular Medicine · doi:10.1111/jcmm.15997 · Cited by 77

G protein‐coupled estrogen receptor and estrogen receptor ligands regulate colonic motility and visceral pain

Zielińska, M., Fichna, J., Bashashati, M., Habibi, S., Sibaev, A., Timmermans, J., & Storr, M. (2017) · Neurogastroenterology & Motility · doi:10.1111/nmo.13025 · Cited by 76

G protein-coupled estrogen receptor in colon function, immune regulation and carcinogenesis

Jacenik, D., Beswick, E. J., Krajewska, W. M., & Prossnitz, E. R. (2019) · World Journal of Gastroenterology · doi:10.3748/wjg.v25.i30.4092 · Cited by 76

G Protein-Coupled Estrogen Receptor 1 Mediates Acute Estrogen-Induced Cardioprotection via MEK/ERK/GSK-3β Pathway after Ischemia/Reperfusion

Kabir, M. E., Singh, H., Lü, R., Olde, B., Leeb-Lundberg, L. M. F., & Bopassa, J. C. (2015) · PLoS ONE · doi:10.1371/journal.pone.0135988 · Cited by 75

Activation of GPER suppresses epithelial mesenchymal transition of triple negative breast cancer cells via NF‐κB signals

Chen, Z.-J., Wei, W., Jiang, G.-M., Liu, H., Wei, W.-D., Yang, X., Wu, Y.-M., Liu, H., Wong, C. K. C., Du, J., et al. (2016) · Molecular Oncology · doi:10.1016/j.molonc.2016.01.002 · Cited by 75

Molecular cloning and tissue expression of a novel orphan G protein-coupled receptor from rat lung

Bonini, J. A., Anderson, S. M., & Steiner, D. F. (1997) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1997.6591 · Cited by 74

Pharmacologic Activation of the G Protein–Coupled Estrogen Receptor Inhibits Pancreatic Ductal Adenocarcinoma

Natale, C. A., Li, J., Pitarresi, J. R., Norgard, R. J., Dentchev, T., Capell, B. C., Seykora, J. T., Stanger, B. Z., & Ridky, T. W. (2020) · Cellular and Molecular Gastroenterology and Hepatology · doi:10.1016/j.jcmgh.2020.04.016 · Cited by 74

2-methoxyestradiol attenuates bleomycin-induced pulmonary hypertension and fibrosis in estrogen-deficient rats

Tofovic, S. P., Zhang, X., Jackson, E. K., Zhu, H., & Petruševska, G. (2009) · Vascular Pharmacology · doi:10.1016/j.vph.2009.06.002 · Cited by 73

GPER regulates endothelin-dependent vascular tone and intracellular calcium

Meyer, M. R., Field, A. S., Kanagy, N. L., Barton, M., & Prossnitz, E. R. (2012) · Life Sciences · doi:10.1016/j.lfs.2012.01.007 · Cited by 72

Activation of G protein‐coupled receptor 30 protects neurons by regulating autophagy in astrocytes

Wang, X., Yue, J., Hu, L., Tian, Z., Zhang, K., Yang, L., Zhang, H., Guo, Y., Feng, B., Liu, H., et al. (2019) · Glia · doi:10.1002/glia.23697 · Cited by 71

Use of PROTACS as molecular probes of angiogenesis

Bargagna‐Mohan, P., Baek, S., Lee, H., Kim, K., & Mohan, R. (2005) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2005.04.008 · Cited by 70

GPER is involved in the stimulatory effects of aldosterone in breast cancer cells and breast tumor-derived endothelial cells

Rigiracciolo, D. C., Scarpelli, A., Lappano, R., Pisano, A., Santolla, M. F., Avino, S., Marco, P. D., Bussolati, B., Maggiolini, M., & Francesco, E. M. D. (2015) · Oncotarget · doi:10.18632/oncotarget.6475 · Cited by 70

G protein-coupled estrogen receptor deficiency accelerates liver tumorigenesis by enhancing inflammation and fibrosis

Wei, T., Chen, W., Wen, L., Zhang, J., Zhang, Q., Yang, J., Liu, H., Chen, B. W., Zhou, Y., Feng, X., et al. (2016) · Cancer Letters · doi:10.1016/j.canlet.2016.08.012 · Cited by 70

The G Protein-coupled Estrogen Receptor (GPER) Agonist G-1 Expands the Regulatory T-cell Population Under TH17-polarizing Conditions

Brunsing, R. L., Owens, K., & Prossnitz, E. R. (2013) · Journal of Immunotherapy · doi:10.1097/cji.0b013e31828d8e3b · Cited by 69

G protein-coupled estrogen receptor is involved in the anti-inflammatory effects of genistein in microglia

Du, Z., Feng, X., Li, N., Qu, J., Feng, L., Chen, L., & Chen, W. (2018) · Phytomedicine · doi:10.1016/j.phymed.2018.03.039 · Cited by 69

The effects of (−)-epicatechin on endothelial cells involve the G protein-coupled estrogen receptor (GPER)

Moreno‐Ulloa, A., Méndez-Luna, D., Beltrán‐Partida, E., Castillo, C., Guevara, G., Ramírez‐Sánchez, I., Correa‐Basurto, J., Ceballos, G. M., & Villarreal, F. J. (2015) · Pharmacological Research · doi:10.1016/j.phrs.2015.08.014 · Cited by 67

G Protein–Coupled Estrogen Receptor Agonist Improves Cerebral Microvascular Function After Hypoxia/Reoxygenation Injury in Male and Female Rats

Murata, T., Dietrich, H. H., Xiang, C., & Dacey, R. G. (2013) · Stroke · doi:10.1161/strokeaha.112.678177 · Cited by 67

GPR30-Expressing Gastric Chief Cells Do Not Dedifferentiate But Are Eliminated via PDK-Dependent Cell Competition During Development of Metaplasia

Hata, M., Kinoshita, H., Hayakawa, Y., Konishi, M., Tsuboi, M., Oya, Y., Kurokawa, K., Hayata, Y., Nakagawa, H., Tateishi, K., et al. (2020) · Gastroenterology · doi:10.1053/j.gastro.2020.01.046 · Cited by 67

G-protein-coupled estrogen receptor activation upregulates interleukin-1 receptor antagonist in the hippocampus after global cerebral ischemia: implications for neuronal self-defense

Bai, N., Zhang, Q., Zhang, W., Liu, B., Yang, F., Brann, D. W., & Wang, R. (2020) · Journal of Neuroinflammation · doi:10.1186/s12974-020-1715-x · Cited by 65

GPER/ERK&AKT/NF-κB pathway is involved in cadmium-induced proliferation, invasion and migration of GPER-positive thyroid cancer cells

Zhu, P., Liao, L.-Y., Zhao, T., Mo, X.-M., Chen, G. Y., & Liu, Z. (2016) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2016.12.007 · Cited by 64

(-)-Epicatechin stimulates mitochondrial biogenesis and cell growth in C2C12 myotubes via the G-protein coupled estrogen receptor

Moreno‐Ulloa, A., Miranda‐Cervantes, A., Licea-Navarro, A. F., Mansour, C. M., Beltrán‐Partida, E., Donis‐Maturano, L., la Herrán, H. C. D.-D., Villarreal, F. J., & Álvarez‐Delgado, C. (2018) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2018.01.014 · Cited by 63

Pregnancy Augments G Protein Estrogen Receptor (GPER) Induced Vasodilation in Rat Uterine Arteries via the Nitric Oxide - cGMP Signaling Pathway

Tropea, T., Francesco, E. M. D., Rigiracciolo, D. C., Maggiolini, M., Wareing, M., Osol, G., & Mandalà, M. (2015) · PLoS ONE · doi:10.1371/journal.pone.0141997 · Cited by 62

GPER1 is required to protect fetal health from maternal inflammation

Harding, A. T., Goff, M., Froggatt, H. M., Lim, J. K., & Heaton, N. S. (2021) · Science · doi:10.1126/science.aba9001 · Cited by 62

GPER Mediates a Feedforward FGF2/FGFR1 Paracrine Activation Coupling CAFs to Cancer Cells toward Breast Tumor Progression

Santolla, M. F., Vivacqua, A., Lappano, R., Rigiracciolo, D. C., Cirillo, F., Galli, G. R., Talia, M., Brunetti, G., Miglietta, A., Belfiore, A., et al. (2019) · Cells · doi:10.3390/cells8030223 · Cited by 61

Dehydroepiandrosterone Activation of G-protein-coupled Estrogen Receptor Rapidly Stimulates MicroRNA-21 Transcription in Human Hepatocellular Carcinoma Cells

Teng, Y., Radde, B. N., Litchfield, L. M., Ivanova, M. M., Prough, R. A., Clark, B. J., Doll, M. A., Hein, D. W., & Klinge, C. M. (2015) · Journal of Biological Chemistry · doi:10.1074/jbc.m115.641167 · Cited by 60

G-Protein-Coupled Estrogen Receptor Antagonist G15 Decreases Estrogen-Induced Development of Non-Small Cell Lung Cancer

Liu, C., Liao, Y., Fan, S., Fu, X., Xiong, J., Zhou, S., Zou, M., & Wang, J. (2017) · Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics · doi:10.3727/096504017x15035795904677 · Cited by 60

Estrogen induces two distinct cholesterol crystallization pathways by activating ERα and GPR30 in female mice

de Bari, O., Wang, T. Y., Liu, M., Portincasa, P., & Wang, D. Q. ‐. (2015) · Journal of Lipid Research · doi:10.1194/jlr.m059121 · Cited by 60

Rapid Aldosterone-Mediated Signaling in the DCT Increases Activity of the Thiazide-Sensitive NaCl Cotransporter

Cheng, L., Poulsen, S. B., Wu, Q., Esteva‐Font, C., Olesen, E. T. B., Peng, L., Olde, B., Leeb-Lundberg, L. M. F., Pisitkun, T., Rieg, T., et al. (2019) · Journal of the American Society of Nephrology · doi:10.1681/asn.2018101025 · Cited by 59

Activation of G protein-coupled estrogen receptor 1 (GPER-1) ameliorates blood-brain barrier permeability after global cerebral ischemia in ovariectomized rats

Lu, D., Qu, Y., Shi, F., Feng, D., Tao, K. X., Gao, G., He, S., & Zhao, T. (2016) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2016.06.044 · Cited by 58

Innate Sex Bias of Staphylococcus aureus Skin Infection Is Driven by α-Hemolysin

Castleman, M. J., Pokhrel, S., Triplett, K. D., Kusewitt, D. F., Elmore, B. O., Joyner, J. A., Femling, J., Sharma, G., Hathaway, H. J., Prossnitz, E. R., et al. (2017) · The Journal of Immunology · doi:10.4049/jimmunol.1700810 · Cited by 58

Attenuation of Microbiotal Dysbiosis and Hypertension in a CRISPR/Cas9 Gene Ablation Rat Model of GPER1

Waghulde, H., Cheng, X., Galla, S., Mell, B., Cai, J., Pruett‐Miller, S. M., Vázquez, G., Patterson, A. D., Kumar, M. V., & Joe, B. (2018) · Hypertension · doi:10.1161/hypertensionaha.118.11175 · Cited by 58

Issue Information

(2020) · The FASEB Journal · doi:10.1096/fsb2.21134 · Cited by 57

G-protein-coupled receptor 30/adenylyl cyclase/protein kinase A pathway is involved in estradiol 17ß-D-glucuronide-induced cholestasis

Zucchetti, A. E., Barosso, I. R., Boaglio, A. C., Basiglio, C. L., Miszczuk, G. S., Larocca, M. C., Ruiz, L. M., Davio, C. A., Roma, M. G., Crocenzi, F. A., et al. (2013) · Hepatology · doi:10.1002/hep.26752 · Cited by 56

Neuroprotection in Parkinsonian-treated mice via estrogen receptor α activation requires G protein-coupled estrogen receptor 1

Bourque, M., Morissette, M., & Paolo, T. D. (2015) · Neuropharmacology · doi:10.1016/j.neuropharm.2015.04.006 · Cited by 56

Activation of G-protein coupled estrogen receptor 1 improves early-onset cognitive impairment via PI3K/Akt pathway in rats with traumatic brain injury.

Wang, Z.-F., Pan, Z.-Y., Xu, C.-S., & Li, Z.-Q. (2017) · Biochemical and Biophysical Research Communications - BBRC · doi:10.1016/j.bbrc.2016.11.138 · Cited by 56

GPER mediates differential effects of estrogen on colon cancer cell proliferation and migration under normoxic and hypoxic conditions

Bustos, V., Nolan, Á. M., Nijhuis, A. M., Harvey, H. M., Parker, A., Poulsom, R., McBryan, J., Thomas, W., Silver, A. R., & Harvey, B. J. (2017) · Oncotarget · doi:10.18632/oncotarget.20653 · Cited by 56

Expression and functional roles of G-protein-coupled estrogen receptor (GPER) in human eosinophils

Tamaki, M., Konno, Y., Kobayashi, Y., Takeda, M., Itoga, M., Moritoki, Y., Oyamada, H., Kayaba, H., Chihara, J., & Ueki, S. (2014) · Immunology Letters · doi:10.1016/j.imlet.2014.03.012 · Cited by 55

Protective Role of GPER Agonist G‐1 on Cardiotoxicity Induced by Doxorubicin

Francesco, E. M. D., Rocca, C., Scavello, F., Amelio, D., Pasqua, T., Rigiracciolo, D. C., Scarpelli, A., Avino, S., Cirillo, F., Amodio, N., et al. (2016) · Journal of Cellular Physiology · doi:10.1002/jcp.25585 · Cited by 55

G protein-coupled estrogen receptor enhances melanogenesis via cAMP-protein kinase (PKA) by upregulating microphthalmia-related transcription factor-tyrosinase in melanoma

Sun, M., Xie, H., Tang, Y., Lin, S., Li, J., Sun, S., Hu, X., Huang, Y., Shi, W., & Jian, D. (2016) · The Journal of Steroid Biochemistry and Molecular Biology · doi:10.1016/j.jsbmb.2016.06.012 · Cited by 54

G protein-coupled estrogen receptor mediates anti-inflammatory action in Crohn’s disease

Jacenik, D., Zielińska, M., Mokrowiecka, A., Michlewska, S., Malecka-Panas, E. I., Kordek, R., Fichna, J., & Krajewska, W. M. (2019) · Scientific Reports · doi:10.1038/s41598-019-43233-3 · Cited by 54

Effect of Age, Estrogen Status, and Late-Life GPER Activation on Cardiac Structure and Function in the Fischer344×Brown Norway Female Rat

Alencar, A. K. N., da Silva, J. S., Lin, M., Silva, A. M., Sun, X., Ferrario, C. M., Cheng, C., Sudo, R. T., Zapata‐Sudo, G., Wang, H., et al. (2016) · The Journals of Gerontology Series A · doi:10.1093/gerona/glw045 · Cited by 54

GPER Agonist G1 Attenuates Neuroinflammation and Dopaminergic Neurodegeneration in Parkinson Disease

Guan, J., Yang, B., Fan, Y., & Zhang, J. (2017) · Neuroimmunomodulation · doi:10.1159/000478908 · Cited by 53

G Protein-Coupled Estrogen Receptor in Cancer and Stromal Cells: Functions and Novel Therapeutic Perspectives

Pepermans, R. A., Sharma, G., & Prossnitz, E. R. (2021) · Cells · doi:10.3390/cells10030672 · Cited by 53

Ameliorative effect of membrane-associated estrogen receptor G protein coupled receptor 30 activation on object recognition memory in mouse models of Alzheimer's disease

Kubota, T., Matsumoto, H., & Kirino, Y. (2016) · Journal of Pharmacological Sciences · doi:10.1016/j.jphs.2016.06.005 · Cited by 52

G Protein-Coupled Estrogen Receptor 1 Regulates Human Neutrophil Functions

Rodenas, M. C., Tamassia, N., Cabas, I., Calzetti, F., Meseguer, J., Cassatella, M. A., Ayala, A. G., & Mulero, V. (2017) · Biomedicine Hub · doi:10.1159/000454981 · Cited by 52

Estradiol activates epithelial sodium channels in rat alveolar cells through the G protein-coupled estrogen receptor

Greenlee, M. M., Mitzelfelt, J. D., Yu, L., Yue, Q., Duke, B. J., Harrell, C. S., Neigh, G. N., & Eaton, D. C. (2013) · American Journal of Physiology-Lung Cellular and Molecular Physiology · doi:10.1152/ajplung.00008.2013 · Cited by 51

Dehydroepiandrosterone alleviates intestinal inflammatory damage via GPR30-mediated Nrf2 activation and NLRP3 inflammasome inhibition in colitis mice

Cao, J., Lu, M., Yan, W., Li, L., & Ma, H. (2021) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2021.06.025 · Cited by 51

Green tea polyphenols inhibit human vascular smooth muscle cell proliferation stimulated by native low-density lipoprotein

Locher, R., Emmanuele, L., Suter, P. M., Vetter, W., & Barton, M. (2002) · European Journal of Pharmacology · doi:10.1016/s0014-2999(01)01535-7 · Cited by 50

17β-Estradiol induces nongenomic effects in renal intercalated cells through G protein-coupled estrogen receptor 1

Hofmeister, M. V., Damkier, H. H., Christensen, B. M., Olde, B., Leeb-Lundberg, L. M. F., Fenton, R. A., Prætorius, H. A., & Prætorius, J. (2011) · American Journal of Physiology-Renal Physiology · doi:10.1152/ajprenal.00343.2011 · Cited by 50

Icariin modulates mitochondrial function and apoptosis in high glucose-induced glomerular podocytes through G protein-coupled estrogen receptors

Qiao, C., Ye, W., Li, S., Wang, H., & Ding, X. (2018) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2018.01.014 · Cited by 50

Alterations in the estrogen receptor profile of cardiovascular tissues during aging

Gurrala, R., Kilanowski‐Doroh, I., Hutson, D. D., Ogola, B. O., Zimmerman, M. A., Katakam, P. V. G., Satou, R., Mostany, R., & Lindsey, S. H. (2021) · GeroScience · doi:10.1007/s11357-021-00331-3 · Cited by 50

Activation of GPER Induces Differentiation and Inhibition of Coronary Artery Smooth Muscle Cell Proliferation

Li, F., Yu, X., Szynkarski, C. K., Meng, C., Zhou, B., Barhoumi, R., White, R. E., Heaps, C. L., Stallone, J. N., & Han, G. (2013) · PLoS ONE · doi:10.1371/journal.pone.0064771 · Cited by 49

Targeting GPR30 with G-1: a new therapeutic target for castration-resistant prostate cancer

Lam, H., Ouyang, B., Chen, J., Ying, J., Wang, J., Wu, C., Li, J., Medvedovic, M., Vessella, R. L., & Ho, S. (2014) · Endocrine Related Cancer · doi:10.1530/erc-14-0402 · Cited by 49

G-Protein Estrogen Receptor as a Regulator of Low-Density Lipoprotein Cholesterol Metabolism

Hussain, Y., Ding, Q., Connelly, P. W., Brunt, J., Ban, M. R., McIntyre, A. D., Huff, M. W., Gros, R., Hegele, R. A., & Feldman, R. D. (2014) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.114.304326 · Cited by 49

Resveratrol inhibits Kv2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Dong, W., Chen, J.-C., He, Y., Xu, J., & Mei, Y. (2013) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00146.2013 · Cited by 49

2-Methoxyestradiol binding of GPR30 down-regulates angiotensin AT1 receptor

Koganti, S., Snyder, R. O., Gumaste, U., Karamyan, V. T., & Thekkumkara, T. (2013) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2013.10.064 · Cited by 48

Sex- and age-dependent effects of Gpr30 genetic deletion on the metabolic and cardiovascular profiles of diet-induced obese mice

Meoli, L., Isensee, J., Zazzu, V., Nabzdyk, C. S., Soewarto, D., Witt, H., Foryst‐Ludwig, A., Kintscher, U., & Ruíz, P. (2014) · Gene · doi:10.1016/j.gene.2014.02.036 · Cited by 47

G-protein-coupled estrogen receptor GPER-1 expression in hormone receptor-positive breast cancer is associated with poor benefit of tamoxifen

Ignatov, T., Claus, M., Naß, N., Haybaeck, J., Seifert, B., Kalinski, T., Ortmann, O., & Ignatov, A. (2018) · Breast Cancer Research and Treatment · doi:10.1007/s10549-018-5064-8 · Cited by 47

Estrogen Activation by Steroid Sulfatase Increases Colorectal Cancer Proliferation via GPER

Gilligan, L. C., Rahman, H. P., Hewitt, A.-M., Sitch, A. J., Gondal, A., Arvaniti, A., TAYLOR, A. E. R., Read, M. L., Morton, D. G., & Foster, P. (2017) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2016-3716 · Cited by 47

GPER in CAFs regulates hypoxia-driven breast cancer invasion in a CTGF-dependent manner

Ren, J., Guo, H., Wu, H., Tian, T., Dong, D., Zhang, Y., Sui, Y.-X., Zhang, Y., Zhao, D., Wang, S., et al. (2015) · Oncology Reports · doi:10.3892/or.2015.3779 · Cited by 46

Vasodilatory effects of the selective GPER agonist G-1 is maximal in arteries of postmenopausal women

Arefin, S., Simoncini, T., Wieland, R. S., Hammarqvist, F., Spina, S., Goglia, L., & Kublickiene, K. R. (2014) · Maturitas · doi:10.1016/j.maturitas.2014.04.002 · Cited by 46

A common hypofunctional genetic variant of GPER is associated with increased blood pressure in women

Feldman, R. D., Gros, R., Ding, Q., Hussain, Y., Ban, M. R., McIntyre, A. D., & Hegele, R. A. (2014) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.12471 · Cited by 46

17-β-estradiol enhances neutrophil extracellular trap formation by interaction with estrogen membrane receptor

Yasuda, H., Sonoda, A., Yamamoto, M., Kawashima, Y., Takishita, Y., Morita, A., Tsutsumi, T., Tsuchiya, M., & Sato, E. F. (2018) · Archives of Biochemistry and Biophysics · doi:10.1016/j.abb.2018.12.028 · Cited by 46

Evidence for G‐Protein–Coupled Estrogen Receptor as a Pronatriuretic Factor

Gohar, E. Y., Daugherty, E. M., Aceves, J. O., Sedaka, R., Obi, I. E., Allan, J. M., Soliman, R. H., Jin, C., Miguel, C. D., Lindsey, S. H., et al. (2020) · Journal of the American Heart Association · doi:10.1161/jaha.119.015110 · Cited by 46

Low dose of zearalenone elevated colon cancer cell growth through G protein-coupled estrogenic receptor

Lo, E. K. K., Lee, J. C., Turner, P. C., & El-Nezami, H. S. (2021) · Scientific Reports · doi:10.1038/s41598-021-86788-w · Cited by 46

G protein‐coupled estrogen receptor is involved in modulating colonic motor function via nitric oxide release in C57 BL /6 female mice

Li, Y., Xu, J., Jiang, F., Jiang, Z., Liu, C., Li, L., Luo, Y., Lu, R., Mu, Y., Liu, Y., et al. (2015) · Neurogastroenterology & Motility · doi:10.1111/nmo.12743 · Cited by 45

Estrogen signaling deregulation related with local immune response modulation in irritable bowel syndrome

Jacenik, D., Cygankiewicz, A. I., Fichna, J., Mokrowiecka, A., Malecka-Panas, E. I., & Krajewska, W. M. (2017) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2017.07.036 · Cited by 45

Activation of GPR30 with G1 attenuates neuronal apoptosis via src/EGFR/stat3 signaling pathway after subarachnoid hemorrhage in male rats

Peng, J., Zuo, Y., Huang, L., Okada, T., Liu, S., Zuo, G., Zhang, G., Tang, J., Xia, Y., & Zhang, J. H. (2019) · Experimental Neurology · doi:10.1016/j.expneurol.2019.113008 · Cited by 45

Estrogen-mediated inactivation of FOXO3a by the G protein-coupled estrogen receptor GPER

Zekas, E., & Prossnitz, E. R. (2015) · BMC Cancer · doi:10.1186/s12885-015-1699-6 · Cited by 44

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, P., & Picard, D. (2017) · Oncotarget · doi:10.18632/oncotarget.18156 · Cited by 44

Purification of estradiol receptor from rat uterus and blockade of its estrogen-binding function by specific antibody

Soloff, M. S., & Szego, C. M. (1969) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(69)90540-3 · Cited by 43

Activation of G protein-coupled estrogen receptor 1 induces coronary artery relaxation via Epac/Rap1-mediated inhibition of RhoA/Rho kinase pathway in parallel with PKA

Yu, X., Zhang, Q., Zhao, Y., Schwarz, B. J., Stallone, J. N., Heaps, C. L., & Han, G. (2017) · PLoS ONE · doi:10.1371/journal.pone.0173085 · Cited by 43

Cardioprotective and anti-inflammatory effects of G-protein coupled receptor 30 (GPR30) on postmenopausal type 2 diabetic rats

Azizian, H., Khaksari, M., Asadikaram, G., Esmailidehaj, M., & Farhadi, Z. (2018) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2018.09.028 · Cited by 43

Primary Osteoporosis Induced by Androgen and Estrogen Deficiency: The Molecular and Cellular Perspective on Pathophysiological Mechanisms and Treatments

Hsu, S.-H., Chen, L.-R., & Chen, K.-H. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms252212139 · Cited by 105

Identification, structure, and agonist design of an androgen membrane receptor

Yang, Z., Ping, Y.-Q., Wang, M., Zhang, C., Zhou, S., Xi, Y.-T., Zhu, K., Ding, W., Zhang, Q., Song, Z.-C., et al. (2025) · Cell · doi:10.1016/j.cell.2025.01.006 · Cited by 74

Treating ER-positive breast cancer: a review of the current FDA-approved SERMs and SERDs and their mechanisms of action

Kim, N., & Lukong, K. E. (2025) · Oncology Reviews · doi:10.3389/or.2025.1564642 · Cited by 73

Estrogen-immuno-neuromodulation disorders in menopausal depression

Zhang, Y., Tan, X., & Tang, C. (2024) · Journal of Neuroinflammation · doi:10.1186/s12974-024-03152-1 · Cited by 76

From physiology to pathology: Emerging roles of GPER in cardiovascular disease

Wang, Z., Liu, J., Chen, Y., Tang, Y., Chen, T., Zhou, C. S., Wang, S., Chang, R., Chen, Z., Yang, W., et al. (2025) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2025.108801 · Cited by 57

The G-protein-coupled estrogen receptor GPER in health and disease

Prossnitz, E. R., & Barton, M. (2011) · Nature Reviews Endocrinology · doi:10.1038/nrendo.2011.122 · Cited by 925

Estrogen biology: New insights into GPER function and clinical opportunities

Prossnitz, E. R., & Barton, M. (2014) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2014.02.002 · Cited by 404

G Protein–Coupled Estrogen Receptor GPER: Molecular Pharmacology and Therapeutic Applications

Arterburn, J. B., & Prossnitz, E. R. (2023) · The Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-031122-121944 · Cited by 114

Not lost in translation: Emerging clinical importance of the G protein-coupled estrogen receptor GPER

Barton, M. (2016) · Steroids · doi:10.1016/j.steroids.2016.02.016 · Cited by 57

GPER–novel membrane oestrogen receptor

Zimmerman, M. A., Budish, R. A., Kashyap, S. N., & Lindsey, S. H. (2016) · Clinical Science · doi:10.1042/cs20160114 · Cited by 114