Assessment of cell line competence for studies of pharmacological GPR30 modulation

References

• Filardo EJ, Quinn JA, Frackelton AR Jr, Bland KI. 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. Mol Endocrinol 2002;16:70–84.
   PubMed Web of Science ®Google Scholar
• Revankar CM, Cimino DF, Sklar LA, et al. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science 2005;307:1625–30.
   PubMed Web of Science ®Google Scholar
• Filardo EJ, Quinn JA, Bland KI, Frackelton AR Jr. 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. Mol Endocrinol 2000;14:1649–60.
   PubMed Web of Science ®Google Scholar
• Maggiolini M, Vivacqua A, Fasanella G, et al. The G protein-coupled receptor GPR30 mediates c-fos up-regulation by 17beta-estradiol and phytoestrogens in breast cancer cells. J Biol Chem 2004;279:27008–16.
   PubMed Web of Science ®Google Scholar
• Gaudet HM, Cheng SB, Christensen EM, Filardo EJ. The G-protein coupled estrogen receptor, GPER: the inside and inside-out story. Mol Cell Endocrinol 2015;418:207–219.
   PubMed Web of Science ®Google Scholar
• Bologa CG, Revankar CM, Young SM, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol 2006;2:207–12.
   PubMed Web of Science ®Google Scholar
• Dennis MK, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist. Nat Chem Biol 2009;5:421–7.
   PubMed Web of Science ®Google Scholar
• Dennis MK, Field AS, Burai R, et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol 2011;127:358–66.
   PubMed Web of Science ®Google Scholar
• Sanden C, Broselid S, Cornmark L, et al. G protein-coupled estrogen receptor 1/G protein-coupled receptor 30 localizes in the plasma membrane and traffics intracellularly on cytokeratin intermediate filaments. Mol Pharmacol 2011;79:400–10.
   PubMed Web of Science ®Google Scholar
• Han G, White RE. G-protein-coupled estrogen receptor as a new therapeutic target for treating coronary artery disease. W J Cardiol 2014;6:367–75.
   PubMedGoogle Scholar
• Arefin S, Simoncini T, Wieland R, et al. Vasodilatory effects of the selective GPER agonist G-1 is maximal in arteries of postmenopausal women. Maturitas 2014;78:123–30.
   PubMed Web of Science ®Google Scholar
• Lindsey SH, Liu L, Chappell MC. Vasodilation by GPER in mesenteric arteries involves both endothelial nitric oxide and smooth muscle cAMP signaling. Steroids 2014;81:99–102.
   PubMed Web of Science ®Google Scholar
• Madak-Erdogan Z, Kieser KJ, Kim SH, et al. Nuclear and extranuclear pathway inputs in the regulation of global gene expression by estrogen receptors. Mol Endocrinol 2008;22:2116–27.
   PubMed Web of Science ®Google Scholar
• Otto C, Rohde-Schulz B, Schwarz G, et al. G protein-coupled receptor 30 localizes to the endoplasmic reticulum and is not activated by estradiol. Endocrinology 2008;149:4846–56.
   PubMed Web of Science ®Google Scholar
• Pedram A, Razandi M, Levin ER. Nature of functional estrogen receptors at the plasma membrane. Mol Endocrinol 2006;20: 1996–2009.
   PubMed Web of Science ®Google Scholar
• Levin ER. G protein-coupled receptor 30: estrogen receptor or collaborator? Endocrinology 2009;150:1563–5.
   PubMed Web of Science ®Google Scholar
• Langer G, Bader B, Meoli L, et al. A critical review of fundamental controversies in the field of GPR30 research. Steroids 2010; 75:603–10.
   PubMed Web of Science ®Google Scholar
• 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;148:3236–45.
   PubMed Web of Science ®Google Scholar
• Cheng SB, Quinn JA, Graeber CT, Filardo EJ. Down-modulation of the G-protein-coupled estrogen receptor, GPER, from the cell surface occurs via a trans-Golgi-proteasome pathway. J Biol Chem 2011;286:22441–55.
   PubMed Web of Science ®Google Scholar
• Kleuser B, Malek D, Gust R, et al. 17-Beta-estradiol inhibits transforming growth factor-beta signaling and function in breast cancer cells via activation of extracellular signal-regulated kinase through the G protein-coupled receptor 30. Mol Pharmacol 2008;74:1533–43.
   PubMed Web of Science ®Google Scholar
• Paixao J, Dinis TC, Almeida LM. Dietary anthocyanins protect endothelial cells against peroxynitrite-induced mitochondrial apoptosis pathway and Bax nuclear translocation: an in vitro approach. Apoptosis 2011;16:976–89.
   PubMed Web of Science ®Google Scholar
• Nolan T, Hands RE, Bustin SA. Quantification of mRNA using real-time RT-PCR. Nat Protoc 2006;1:1559–82.
   PubMed Web of Science ®Google Scholar
• Lapensee EW, Tuttle TR, Fox SR, Ben-Jonathan N. Bisphenol A at low nanomolar doses confers chemoresistance in estrogen receptor-alpha-positive and -negative breast cancer cells. Environ Health Perspect 2009;117:175–80.
   PubMed Web of Science ®Google Scholar
• Bindal RD, Katzenellenbogen JA. Bis(4-hydroxyphenyl)[2-(phenoxysulfonyl)phenyl]methane: isolation and structure elucidation of a novel estrogen from commercial preparations of phenol red (phenolsulfonphthalein). J Med Chem 1988;31:1978–83.
   PubMed Web of Science ®Google Scholar
• Prossnitz ER, Sklar LA, Oprea TI, Arterburn JB. GPR30: a novel therapeutic target in estrogen-related disease. Trends Pharmacol Sci 2008;29:116–23.
   PubMed Web of Science ®Google Scholar
• Kobilka BK. G protein coupled receptor structure and activation. Biochim Biophys Acta 2007;1768:794–807.
   PubMed Web of Science ®Google Scholar
• Palombella VJ, Rando OJ, Goldberg AL, Maniatis T. The ubiquitin-proteasome pathway is required for processing the NF-kappa B1 precursor protein and the activation of NF-kappa B. Cell 1994;78:773–85.
   PubMed Web of Science ®Google Scholar
• Wang CY, Mayo MW, Baldwin AS Jr. TNF- and cancer therapy-induced apoptosis: potentiation by inhibition of NF-kappaB. Science 1996;274:784–7.
   PubMed Web of Science ®Google Scholar
• Lobenhofer EK, Huper G, Iglehart JD, Marks JR. Inhibition of mitogen-activated protein kinase and phosphatidylinositol 3-kinase activity in MCF-7 cells prevents estrogen-induced mitogenesis. Cell Growth Differ 2000;11:99–110.
   PubMedGoogle Scholar
• Lobenhofer EK, Marks JR. Estrogen-induced mitogenesis of MCF-7 cells does not require the induction of mitogen-activated protein kinase activity. J Steroid Biochem Mol Biol 2000;75:11–20.
   PubMed Web of Science ®Google Scholar
• Caristi S, Galera JL, Matarese F, et al. Estrogens do not modify MAP kinase-dependent nuclear signaling during stimulation of early G(1) progression in human breast cancer cells. Cancer Res 2001;61:6360–6.
   PubMed Web of Science ®Google Scholar
• Gaben AM, Saucier C, Bedin M, et al. Mitogenic activity of estrogens in human breast cancer cells does not rely on direct induction of mitogen-activated protein kinase/extracellularly regulated kinase or phosphatidylinositol 3-kinase. Mol Endocrinol 2004;18:2700–13.
   PubMed Web of Science ®Google Scholar
• Brower SL, Roberts JR, Antonini JM, Miller MR. Difficulty demonstrating estradiol-mediated Erk1/2 phosphorylation in MCF-7 cells. J Steroid Biochem Mol Biol 2005;96:375–85.
   PubMed Web of Science ®Google Scholar
• Lannigan DA. Estrogen receptor phosphorylation. Steroids 2003;68:1–9.
   PubMed Web of Science ®Google Scholar
• Filardo EJ, Thomas P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 2012;153:2953–62.
   PubMed Web of Science ®Google Scholar
• Sousa C, Mendes A, Silva MM, et al. Synthetic strategies to afford estradiol derivatives with potential biological activity. 22nd International Symposium on Medicinal Chemistry, Berlin, Germany; September, 2012:219–220. Available from: http://www.wiley-vch.de/util/chem-epaper/ismc/ [last accessed 23 Mar 2016].
   Google Scholar