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

Sharma G, Hu C, Staquicini DI, Brigman JL, Liu M, Mauvais-Jarvis F, Pasqualini R, Arap W, Arterburn JB, Hathaway HJ, Prossnitz ER.

Sci Transl Med. 2020 Jan 29;12(528). pii: eaau5956. doi: 10.1126/scitranslmed.aau5956.


A Selective Ligand for Estrogen Receptor Proteins Discriminates Rapid and Genomic Signaling.

Revankar CM, Bologa CG, Pepermans RA, Sharma G, Petrie WK, Alcon SN, Field AS, Ramesh C, Parker MA, Savchuk NP, Sklar LA, Hathaway HJ, Arterburn JB, Oprea TI, Prossnitz ER.

Cell Chem Biol. 2019 Dec 19;26(12):1692-1702.e5. doi: 10.1016/j.chembiol.2019.10.009. Epub 2019 Nov 6.


FTY720-Mitoxy reduces toxicity associated with MSA-like α-synuclein and oxidative stress by increasing trophic factor expression and myelin protein in OLN-93 oligodendroglia cell cultures.

Vargas-Medrano J, Segura-Ulate I, Yang B, Chinnasamy R, Arterburn JB, Perez RG.

Neuropharmacology. 2019 Nov 1;158:107701. doi: 10.1016/j.neuropharm.2019.107701. Epub 2019 Jul 7.


Bimolecular Cross-Metathesis of a Tetrasubstituted Alkene with Allylic Sulfones.

Sapkota RR, Jarvis JM, Schaub TM, Talipov MR, Arterburn JB.

ChemistryOpen. 2019 Feb 14;8(2):201-205. doi: 10.1002/open.201800296. eCollection 2019 Feb.


Obligatory role for GPER in cardiovascular aging and disease.

Meyer MR, Fredette NC, Daniel C, Sharma G, Amann K, Arterburn JB, Barton M, Prossnitz ER.

Sci Signal. 2016 Nov 1;9(452):ra105. doi: 10.1126/scisignal.aag0240.


Preclinical Metabolism, Pharmacokinetics and In Vivo Analysis of New Blood-Brain-Barrier Penetrant Fingolimod Analogues: FTY720-C2 and FTY720-Mitoxy.

Enoru JO, Yang B, Krishnamachari S, Villanueva E, DeMaio W, Watanyar A, Chinnasamy R, Arterburn JB, Perez RG.

PLoS One. 2016 Sep 9;11(9):e0162162. doi: 10.1371/journal.pone.0162162. eCollection 2016.


Erratum: G Protein-coupled Estrogen Receptor Protects from Atherosclerosis.

Meyer MR, Fredette NC, Howard TA, Hu C, Ramesh C, Daniel C, Amann K, Arterburn JB, Barton M, Prossnitz ER.

Sci Rep. 2015 Sep 16;5:13510. doi: 10.1038/srep13510. No abstract available.


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

Prossnitz ER, Arterburn JB.

Pharmacol Rev. 2015 Jul;67(3):505-40. doi: 10.1124/pr.114.009712. Review.


G protein-coupled estrogen receptor protects from atherosclerosis.

Meyer MR, Fredette NC, Howard TA, Hu C, Ramesh C, Daniel C, Amann K, Arterburn JB, Barton M, Prossnitz ER.

Sci Rep. 2014 Dec 23;4:7564. doi: 10.1038/srep07564. Erratum in: Sci Rep. 2015;5:13510.


Novel FTY720-Based Compounds Stimulate Neurotrophin Expression and Phosphatase Activity in Dopaminergic Cells.

Vargas-Medrano J, Krishnamachari S, Villanueva E, Godfrey WH, Lou H, Chinnasamy R, Arterburn JB, Perez RG.

ACS Med Chem Lett. 2014 May 27;5(7):782-6. doi: 10.1021/ml500128g. eCollection 2014 Jul 10.


GPER-targeted, 99mTc-labeled, nonsteroidal ligands demonstrate selective tumor imaging and in vivo estrogen binding.

Nayak TK, Ramesh C, Hathaway HJ, Norenberg JP, Arterburn JB, Prossnitz ER.

Mol Cancer Res. 2014 Nov;12(11):1635-43. doi: 10.1158/1541-7786.MCR-14-0289. Epub 2014 Jul 16.


G protein-coupled estrogen receptor-selective ligands modulate endometrial tumor growth.

Petrie WK, Dennis MK, Hu C, Dai D, Arterburn JB, Smith HO, Hathaway HJ, Prossnitz ER.

Obstet Gynecol Int. 2013;2013:472720. doi: 10.1155/2013/472720. Epub 2013 Nov 27.


GPER-1 agonist G1 induces vasorelaxation through activation of epidermal growth factor receptor-dependent signalling pathway.

Jang EJ, Seok YM, Arterburn JB, Olatunji LA, Kim IK.

J Pharm Pharmacol. 2013 Oct;65(10):1488-99. doi: 10.1111/jphp.12113. Epub 2013 Aug 6.


Aldosterone increases cardiac vagal tone via G protein-coupled oestrogen receptor activation.

Brailoiu GC, Benamar K, Arterburn JB, Gao E, Rabinowitz JE, Koch WJ, Brailoiu E.

J Physiol. 2013 Sep 1;591(17):4223-35. doi: 10.1113/jphysiol.2013.257204. Epub 2013 Jul 22.


Bradycardic effects mediated by activation of G protein-coupled estrogen receptor in rat nucleus ambiguus.

Brailoiu GC, Arterburn JB, Oprea TI, Chitravanshi VC, Brailoiu E.

Exp Physiol. 2013 Mar;98(3):679-91. doi: 10.1113/expphysiol.2012.069377. Epub 2012 Oct 26.


Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30.

Burai R, Ramesh C, Nayak TK, Dennis MK, Bryant BK, Prossnitz ER, Arterburn JB.

PLoS One. 2012;7(10):e46861. doi: 10.1371/journal.pone.0046861. Epub 2012 Oct 15.


Mechanisms of G protein-coupled estrogen receptor-mediated spinal nociception.

Deliu E, Brailoiu GC, Arterburn JB, Oprea TI, Benamar K, Dun NJ, Brailoiu E.

J Pain. 2012 Aug;13(8):742-54. doi: 10.1016/j.jpain.2012.05.011.


G protein-coupled estrogen receptor 1-mediated effects in the rat myometrium.

Tica AA, Dun EC, Tica OS, Gao X, Arterburn JB, Brailoiu GC, Oprea TI, Brailoiu E.

Am J Physiol Cell Physiol. 2011 Nov;301(5):C1262-9. doi: 10.1152/ajpcell.00501.2010. Epub 2011 Aug 24.


Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.

Rodriguez D, Ramesh C, Henson LH, Wilmeth L, Bryant BK, Kadavakollu S, Hirsch R, Montoya J, Howell PR, George JM, Alexander D, Johnson DL, Arterburn JB, Shuster CB.

Bioorg Med Chem. 2011 Sep 15;19(18):5446-53. doi: 10.1016/j.bmc.2011.07.054. Epub 2011 Jul 30.


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

Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, Bologa CG, Oprea TI, Yamaguchi Y, Hayashi S, Sklar LA, Hathaway HJ, Arterburn JB, Prossnitz ER.

J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66. doi: 10.1016/j.jsbmb.2011.07.002. Epub 2011 Jul 14.


Design and synthesis of a new class of membrane-permeable triazaborolopyridinium fluorescent probes.

Hapuarachchige S, Montaño G, Ramesh C, Rodriguez D, Henson LH, Williams CC, Kadavakkollu S, Johnson DL, Shuster CB, Arterburn JB.

J Am Chem Soc. 2011 May 4;133(17):6780-90. doi: 10.1021/ja2005175. Epub 2011 Apr 7.


GPR30 expression is required for the mineralocorticoid receptor-independent rapid vascular effects of aldosterone.

Gros R, Ding Q, Sklar LA, Prossnitz EE, Arterburn JB, Chorazyczewski J, Feldman RD.

Hypertension. 2011 Mar;57(3):442-51. doi: 10.1161/HYPERTENSIONAHA.110.161653. Epub 2011 Jan 17.


Influence of charge on cell permeability and tumor imaging of GPR30-targeted 111in-labeled nonsteroidal imaging agents.

Nayak TK, Dennis MK, Ramesh C, Burai R, Atcher RW, Sklar LA, Norenberg JP, Hathaway HJ, Arterburn JB, Prossnitz ER.

ACS Chem Biol. 2010 Jul 16;5(7):681-90. doi: 10.1021/cb1000636.


A novel nucleoside analog, 1-beta-d-ribofuranosyl-3-ethynyl-[1,2,4]triazole (ETAR), exhibits efficacy against a broad range of flaviviruses in vitro.

McDowell M, Gonzales SR, Kumarapperuma SC, Jeselnik M, Arterburn JB, Hanley KA.

Antiviral Res. 2010 Jul;87(1):78-80. doi: 10.1016/j.antiviral.2010.04.007. Epub 2010 Apr 21.


Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs.

Burai R, Ramesh C, Shorty M, Curpan R, Bologa C, Sklar LA, Oprea T, Prossnitz ER, Arterburn JB.

Org Biomol Chem. 2010 May 7;8(9):2252-9. doi: 10.1039/c001307b. Epub 2010 Mar 16.


The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.

Ariazi EA, Brailoiu E, Yerrum S, Shupp HA, Slifker MJ, Cunliffe HE, Black MA, Donato AL, Arterburn JB, Oprea TI, Prossnitz ER, Dun NJ, Jordan VC.

Cancer Res. 2010 Feb 1;70(3):1184-94. doi: 10.1158/0008-5472.CAN-09-3068. Epub 2010 Jan 19.


Synthesis and characterization of iodinated tetrahydroquinolines targeting the G protein-coupled estrogen receptor GPR30.

Ramesh C, Nayak TK, Burai R, Dennis MK, Hathaway HJ, Sklar LA, Prossnitz ER, Arterburn JB.

J Med Chem. 2010 Feb 11;53(3):1004-14. doi: 10.1021/jm9011802.


Discovery of selective probes and antagonists for G-protein-coupled receptors FPR/FPRL1 and GPR30.

Arterburn JB, Oprea TI, Prossnitz ER, Edwards BS, Sklar LA.

Curr Top Med Chem. 2009;9(13):1227-36. Review.


Synthesis and anti-Hantaan virus activity of N(1)-3-fluorophenyl-inosine.

Chung DH, Strouse JJ, Sun Y, Arterburn JB, Parker WB, Jonsson CB.

Antiviral Res. 2009 Jul;83(1):80-5. doi: 10.1016/j.antiviral.2009.03.007. Epub 2009 Apr 2.


In vivo effects of a GPR30 antagonist.

Dennis MK, Burai R, Ramesh C, Petrie WK, Alcon SN, Nayak TK, Bologa CG, Leitao A, Brailoiu E, Deliu E, Dun NJ, Sklar LA, Hathaway HJ, Arterburn JB, Oprea TI, Prossnitz ER.

Nat Chem Biol. 2009 Jun;5(6):421-7. doi: 10.1038/nchembio.168.


Expression of estrogen receptor GPR30 in the rat spinal cord and in autonomic and sensory ganglia.

Dun SL, Brailoiu GC, Gao X, Brailoiu E, Arterburn JB, Prossnitz ER, Oprea TI, Dun NJ.

J Neurosci Res. 2009 May 15;87(7):1610-9. doi: 10.1002/jnr.21980.


Duplex high-throughput flow cytometry screen identifies two novel formylpeptide receptor family probes.

Young SM, Bologa CM, Fara D, Bryant BK, Strouse JJ, Arterburn JB, Ye RD, Oprea TI, Prossnitz ER, Sklar LA, Edwards BS.

Cytometry A. 2009 Mar;75(3):253-63. doi: 10.1002/cyto.a.20645.


Preclinical development of a neutral, estrogen receptor-targeted, tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative for imaging of breast and endometrial cancers.

Nayak TK, Hathaway HJ, Ramesh C, Arterburn JB, Dai D, Sklar LA, Norenberg JP, Prossnitz ER.

J Nucl Med. 2008 Jun;49(6):978-86. doi: 10.2967/jnumed.107.048546. Epub 2008 May 15.


The ins and outs of GPR30: a transmembrane estrogen receptor.

Prossnitz ER, Oprea TI, Sklar LA, Arterburn JB.

J Steroid Biochem Mol Biol. 2008 Apr;109(3-5):350-3. doi: 10.1016/j.jsbmb.2008.03.006. Epub 2008 Mar 6. Review.


Synthesis of 1-beta-D-ribofuranosyl-3-ethynyl-[1,2,4]triazole and its in vitro and in vivo efficacy against Hantavirus.

Chung DH, Kumarapperuma SC, Sun Y, Li Q, Chu YK, Arterburn JB, Parker WB, Smith J, Spik K, Ramanathan HN, Schmaljohn CS, Jonsson CB.

Antiviral Res. 2008 Jul;79(1):19-27. doi: 10.1016/j.antiviral.2008.02.003. Epub 2008 Mar 17.


Estrogen signaling through the transmembrane G protein-coupled receptor GPR30.

Prossnitz ER, Arterburn JB, Smith HO, Oprea TI, Sklar LA, Hathaway HJ.

Annu Rev Physiol. 2008;70:165-90. doi: 10.1146/annurev.physiol.70.113006.100518. Review.


GPR30: a novel therapeutic target in estrogen-related disease.

Prossnitz ER, Sklar LA, Oprea TI, Arterburn JB.

Trends Pharmacol Sci. 2008 Mar;29(3):116-23. doi: 10.1016/ Epub 2008 Feb 11.


Bisphenol A directly targets tubulin to disrupt spindle organization in embryonic and somatic cells.

George O, Bryant BK, Chinnasamy R, Corona C, Arterburn JB, Shuster CB.

ACS Chem Biol. 2008 Mar 20;3(3):167-79. doi: 10.1021/cb700210u. Epub 2008 Jan 29.


Ribavirin reveals a lethal threshold of allowable mutation frequency for Hantaan virus.

Chung DH, Sun Y, Parker WB, Arterburn JB, Bartolucci A, Jonsson CB.

J Virol. 2007 Nov;81(21):11722-9. Epub 2007 Aug 15.


Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30.

Revankar CM, Mitchell HD, Field AS, Burai R, Corona C, Ramesh C, Sklar LA, Arterburn JB, Prossnitz ER.

ACS Chem Biol. 2007 Aug 17;2(8):536-44. Epub 2007 Jul 27.


Structural effects on the phosphorylation of 3-substituted 1-beta-D-ribofuranosyl-1,2,4-triazoles by human adenosine kinase.

Kumarapperuma SC, Sun Y, Jeselnik M, Chung K, Parker WB, Jonsson CB, Arterburn JB.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3203-7. Epub 2007 Mar 12.


GPR30: A G protein-coupled receptor for estrogen.

Prossnitz ER, Arterburn JB, Sklar LA.

Mol Cell Endocrinol. 2007 Feb;265-266:138-42. Epub 2007 Jan 11. Review.


Characterization of a radiolabeled small molecule targeting leukocyte function-associated antigen-1 expression in lymphoma and leukemia.

Poria RB, Norenberg JP, Anderson TL, Erion J, Wagner CR, Arterburn JB, Larson RS.

Cancer Biother Radiopharm. 2006 Oct;21(5):418-26.


Linkage effects on binding affinity and activation of GPR30 and estrogen receptors ERalpha/beta with tridentate pyridin-2-yl hydrazine tricarbonyl-Re/(99m)Tc(I) chelates.

Ramesh C, Bryant B, Nayak T, Revankar CM, Anderson T, Carlson KE, Katzenellenbogen JA, Sklar LA, Norenberg JP, Prossnitz ER, Arterburn JB.

J Am Chem Soc. 2006 Nov 15;128(45):14476-7.


Steroid-binding G-protein-coupled receptors: new drug discovery targets for old ligands.

Prossnitz ER, Arterburn JB, Edwards BS, Sklar LA, Oprea TI.

Expert Opin Drug Discov. 2006 Jul;1(2):137-50. doi: 10.1517/17460441.1.2.137.


Synthesis of a biotin-derived alkyne for pd-catalyzed coupling reactions.

Corona C, Bryant BK, Arterburn JB.

Org Lett. 2006 Apr 27;8(9):1883-6.


Virtual and biomolecular screening converge on a selective agonist for GPR30.

Bologa CG, Revankar CM, Young SM, Edwards BS, Arterburn JB, Kiselyov AS, Parker MA, Tkachenko SE, Savchuck NP, Sklar LA, Oprea TI, Prossnitz ER.

Nat Chem Biol. 2006 Apr;2(4):207-12. Epub 2006 Mar 5.


A transmembrane intracellular estrogen receptor mediates rapid cell signaling.

Revankar CM, Cimino DF, Sklar LA, Arterburn JB, Prossnitz ER.

Science. 2005 Mar 11;307(5715):1625-30. Epub 2005 Feb 10.


Potential importance of error catastrophe to the development of antiviral strategies for hantaviruses.

Jonsson CB, Milligan BG, Arterburn JB.

Virus Res. 2005 Feb;107(2):195-205. Review.


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