The G Protein-Coupled Estrogen Receptor (GPER-1): A Novel Regulator in the Kidney

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Authors

  • Zijun Liu Department of General Surgery, Nanjing First Hospital, Nanjing Medical University, Nanjing, China
  • Na Liu Department of Nephrology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, China
  • Shibin Cheng Department of Pediatrics, Women & Infants Hospital, Warren Alpert Medical School of Brown University, Providence, RI, USA Gender has a crucial influence on incidence and prognosis of chronic and acute kid - ney diseases since women generally have a lower morbidity and mortality compared to men.

DOI:

https://doi.org/10.17140/NPOJ-1-e002

Keywords:

antiestrogens, estrogens, Genestein

Abstract

Gender has a crucial influence on incidence and prognosis of chronic and acute kidney diseases since women generally have a lower morbidity and mortality compared to men.1,2
Several studies have reported the capability of estrogen to promote homeostatic and protective
effects in the kidney via a pregenomic mechanism that is mediated by G protein-coupled receptor 30 (GPR30), but not by classic Estrogen Receptors (ER), ERα or ERβ.2 GPR30 was first
cloned as an orphan receptor from a Burkitt’s lymphoma cell line3 and then confirmed in other
cell lines.4 Prior studies have demonstrated that GPR30 is a specific, high affinity, Gs
-coupled
estrogen membrane receptor activated by naturally occurring and synthetic estrogens and antiestrogens including estradiol-17β, G1, tamoxifen, ICI182,780, Genestein and Bisphenol A,
but not by cortisol, progesterone or testosterone in both mammals and fish.5-15 Thus, GPR30
was designated G protein-coupled estrogen receptor-1 (GPER-1) by the International Union of
Pharmacology in 2007

References

Hutchens MP, Fujiyoshi T, Komers R, Herson PS, Anderson S. Estrogen protects renal endothelial barrier function from isch-emia-reperfusion in vitro and in vivo. Am. J. Physiol. Renal. Phys-iol. 2012; 303: F377-F385. doi: 10.1152/ajprenal.00354.2011

Li YC, Ding XS, Li HM, Zhang Y, Bao J. Role of G protein-coupled estrogen receptor 1 in modulating transforming growth factor-β stimulated mesangial cell extracellular matrix synthesis and migration. Mol Cell Endocrinol. 2014; 391(1-2): 50-59. doi: 10.1016/j.mce.2014.04.014

Owman C, Blay P, Nilsson C, Lolait SJ. Cloning of hu-man cDNA encoding a novel heptahelix receptor expressed in Burkitt’s lymphoma and widely distributed in brain and periph-eral tissues. Biochem Biophys Res Commun. 1996; 228(2): 285- 292. doi: 10.1006/bbrc.1996.1654

Han G, Li F, Yu X, White RE. GPER: a novel target for non-genomic estrogenaction in the cardiovascular system. Pharma-col Res. 2013; 71: 53-60. doi: 10.1016/j.phrs.2013.02.008

Filardo EJ, Thomas P. GPR30: a seven-transmembrane-spanning estrogenreceptor that triggers EGF release. Trends Endocrinol. Metab. 2005; 16: 362-367. doi: 10.1016/j. tem.2005.08.005

Filardo EJ, Thomas P. Mini review: G protein-coupled estro-gen receptor-1, GPER-1: its mechanism of action and role in female reproductive cancer, renal and vascular physiology. En-docrinology. 2012; 153: 2953-2962. doi: 10.1210/en.2012-1061

Filardo EJ, Quinn JA, Bland KI, Frackelton Jr, AR. Estrogen-induced activation of Erk-1 and Erk-2 requires the G protein-coupled receptor homolog, GPR30, and occurs via trans-activa-tion of the epidermal growth factor receptor through release of HB-EGF. Mol. Endocrinol. 2000; 14: 1649-1660.

Filardo EJ, Quinn JA, Frackelton Jr AR, Bland KI. Estrogen action via the G protein-coupled receptor, GPR30: stimulation of adenylyl cyclase and cAMP mediated attenuation of the epi-dermal growth factor receptor-to-MAPK signaling axis. Mol. Endocrinol. 2002; 16: 70-84.

Filardo EJ, GraeberCT, Quinn JA, et al. Distribution of GPR30, a seven membrane-spanning estrogen receptor, in primary breast cancer and its association with clinicopathologic determinants of tumor progression. Clin. Cancer Res. 2006; 12: 6359-6366. doi:

1158/1078-0432.CCR-06-0860 10. Filardo E, Quinn J, Pang Y, et al. Activation of the novel estrogen receptor G protein-coupled receptor 30 GPR30.at the plasma membrane. Endocrinology. 2007; 148: 3236-3245. doi: 10.1210/en.2006-1605

Thomas P, Dong J. Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental es-trogens: a potential novel mechanism of endocrine disruption. J. Steroid Biochem. Mol. Biol. 2006; 102: 175-179. doi: 10.1016/j. jsbmb.2006.09.017

Thomas P, Pang Y, Filardo EJ, Dong J. Identity of an estro-gen membranereceptor coupled to a G protein in human breast cancer cells. Endocrinology. 2005; 146: 624-632.

Thomas P,Alyea R, Pang Y, Peyton C, Dong J, BergAH. Con-servedestrogen binding and signaling functions of the G protein-coupled estrogen receptor 1 GPER1 in mammals and fish. Ste-roids. 2010; 75: 595-602. doi: 10.1016/j.steroids.2009.11.005

Pang Y, Thomas P. Progesterone signals through membrane progesterone receptors mPRs in MDA-MB-468 and mPR-transfected MDA-MB-231 breast cancer cells which lack full-length and N-terminally truncated isoforms of the nuclear pro-gesterone receptor. Steroids. 2011; 76: 921-928. doi: 10.1016/j. steroids.2011.01.008

Bologa CG, Revankar CM, Young SM, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat. Chem. Biol. 2006; 2: 207-212. doi: 10.1038/ nchembio775

Alexander SP, Mathie A, Peters JA. Guide to receptors and channels (GRAC). 5th edition. Br J Pharmacol. 2011; 154(Suppl 1): S1-S324. doi: 10.1111/j.1476-5381.2011.01649_1.x

Grimont A, Bloch-Faure M, El Abida B, Crambert G. Map-ping of sex hormone receptors and their modulators along the nephron of male and female mice. FEBS Lett. 2009; 583: 1644- 1648. doi: 10.1016/j.febslet.2009.04.032

Hazell GG, Yao ST, Roper JA, Prossnitz ER, O’Carroll AM, Lolait SJ. Localisation of GPR30, a novel G protein-coupled oestrogen receptor, suggests multiple functions in rodent brain and peripheral tissues. J. Endocrinol. 2009; 202: 223-236. doi: 10.1677/JOE-09-0066

Cheng SB, Graeber CT, Quinn JA, Filardo EJ. Retrograde transport of the transmembrane estrogen receptor, G-protein-coupled-receptor-30 GPR30/GPER from the plasma membrane towards the nucleus. Steroids. 2011; 76: 892-896. doi: 10.1016/j. steroids.2011.02.018

Lindsey SH, Yamaleyeva LM, Brosnihan KB, Gallagher PE, Chappell MC. Estrogen receptor GPR30 reduces oxidative stress and proteinuria in the salts ensitive female mRen2. Lewis rat. Hypertension. 2011; 58: 665-671. doi: 10.1161/HYPER-TENSIONAHA

Hofmeister MV, Damkier HH, Christensen BM, et al. 17beta-Estradiol inducesnongenomic effects in renal interca-lated cells through G protein-coupled estrogen receptor 1. Am J Physiol Renal Physiol. 2012; 302: F358-F368. doi: 10.1152/ ajprenal.00343.2011

Cheng SB, Dong J, Pang Y, et al. Anatomicallocation and redistribution of G protein-coupled estrogen receptor-1 during theestrus cycle in mouse kidney and specific binding to estro-gens but notaldosterone. Mol Cell Endocrinol. 2014; 382(2): 950-959. doi: 10.1016/j.mce.2013.11.005

Kurt AH, Buyukafsar K. Vasoconstriction induced by G1, a G-protein-coupledoestrogen receptor1 (GPER-1) agonist, in the isolated perfused rat kidney. Eur J Pharmacol. 2013; 702(1-3): 71-78. doi: 10.1016/j.ejphar.2013.01.020

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Published

2015-04-17

How to Cite

Zijun Liu, Na Liu, & Shibin Cheng. (2015). The G Protein-Coupled Estrogen Receptor (GPER-1): A Novel Regulator in the Kidney. Nephrology, 1(1), 24–26. https://doi.org/10.17140/NPOJ-1-e002

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Volume 1 Issue 1 2015

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