My Bibliography

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Pallai PV, Richman S, Struthers RS, Goodman M. Approaches to the synthesis of retro-inverso peptides. Int J Pept Protein Res. 1983 Jan;21(1):84-92. doi: 10.1111/j.1399-3011.1983.tb03081.x. PubMed PMID: 6826285.

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Pallai P, Struthers S, Goodman M, Rivier J, Vale W. Extended retro-inverso analogs of somatostatin. Biopolymers. 1983 Dec;22(12):2523-38. doi: 10.1002/bip.360221207. PubMed PMID: 6141815.

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Struthers RS, Rivier J, Hagler AT. Molecular dynamics and minimum energy conformations of GnRH and analogs. A methodology for computer-aided drug design. Ann N Y Acad Sci. 1985;439:81-96. doi: 10.1111/j.1749-6632.1985.tb25790.x. PubMed PMID: 3890664.

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Pallai PV, Struthers RS, Goodman M, Moroder L, Wunsch E, Vale W. Partial retro-inverso analogues of somatostatin: pairwise modifications at residues 7 and 8 and at residues 8 and 9. Biochemistry. 1985 Apr 9;24(8):1933-41. doi: 10.1021/bi00329a020. PubMed PMID: 2861848.

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Baniak EL 2nd, Rivier JE, Struthers RS, Hagler AT, Gierasch LM. Nuclear magnetic resonance analysis and conformational characterization of a cyclic decapeptide antagonist of gonadotropin-releasing hormone. Biochemistry. 1987 May 5;26(9):2642-56. doi: 10.1021/bi00383a036. PubMed PMID: 3300777.

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Hughes RJ, Struthers RS, Fong AM, Insel PA. Regulation of the atrial natriuretic peptide receptor on a smooth muscle cell. Am J Physiol. 1987 Dec;253(6 Pt 1):C809-16. doi: 10.1152/ajpcell.1987.253.6.C809. PubMed PMID: 2827497.

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Hughes RJ, Struthers RS, Fong AM, Insel PA. Receptor-induced degradation of atrial natriuretic peptide by a rabbit carotid artery smooth muscle cell. Mol Endocrinol. 1988 Feb;2(2):117-24. doi: 10.1210/mend-2-2-117. PubMed PMID: 2840569.

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Rivier J, Kupryszewski G, Varga J, Porter J, Rivier C, Perrin M, Hagler A, Struthers S, Corrigan A, Vale W. Design of potent cyclic gonadotropin releasing hormone antagonists. J Med Chem. 1988 Mar;31(3):677-82. doi: 10.1021/jm00398a030. PubMed PMID: 3279211.

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Struthers RS, Perrin MH, Vale W. Nucleotide regulation of growth hormone-releasing factor binding to rat pituitary receptors. Endocrinology. 1989 Jan;124(1):24-9. doi: 10.1210/endo-124-1-24. PubMed PMID: 2535806.

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Struthers RS, Tanaka G, Koerber SC, Solmajer T, Baniak EL, Gierasch LM, Vale W, Rivier J, Hagler AT. Design of biologically active, conformationally constrained GnRH antagonists. Proteins. 1990;8(4):295-304. doi: 10.1002/prot.340080403. PubMed PMID: 2091022.

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Struthers RS, Kitson DH, Hagler AT. Predicted three-dimensional structure of the protease inhibitor domain of the Alzheimer's disease beta-amyloid precursor. Proteins. 1991;9(1):1-11. doi: 10.1002/prot.340090102. PubMed PMID: 2017431.

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Struthers RS, Vale WW, Arias C, Sawchenko PE, Montminy MR. Somatotroph hypoplasia and dwarfism in transgenic mice expressing a non-phosphorylatable CREB mutant. Nature. 1991 Apr 18;350(6319):622-4. doi: 10.1038/350622a0. PubMed PMID: 1826763.

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Struthers RS, Gaddy-Kurten D, Vale WW. Activin inhibits binding of transcription factor Pit-1 to the growth hormone promoter. Proc Natl Acad Sci U S A. 1992 Dec 1;89(23):11451-5. doi: 10.1073/pnas.89.23.11451. PubMed PMID: 1454833; PubMed Central PMCID: PMC50569.

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Millar RP, Zhu YF, Chen C, Struthers RS. Progress towards the development of non-peptide orally-active gonadotropin-releasing hormone (GnRH) antagonists: therapeutic implications. Br Med Bull. 2000;56(3):761-72. doi: 10.1258/0007142001903346. Review. PubMed PMID: 11255560.

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Rivier JE, Struthers RS, Porter J, Lahrichi SL, Jiang G, Cervini LA, Ibea M, Kirby DA, Koerber SC, Rivier CL. Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists. J Med Chem. 2000 Mar 9;43(5):784-96. doi: 10.1021/jm990115h. PubMed PMID: 10715147.

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Rivier JE, Porter J, Cervini LA, Lahrichi SL, Kirby DA, Struthers RS, Koerber SC, Rivier CL. Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists. J Med Chem. 2000 Mar 9;43(5):797-806. doi: 10.1021/jm9901172. PubMed PMID: 10715148.

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Koerber SC, Rizo J, Struthers RS, Rivier JE. Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling. J Med Chem. 2000 Mar 9;43(5):819-28. doi: 10.1021/jm990118u. PubMed PMID: 10715150.

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Rivier JE, Jiang G, Struthers RS, Koerber SC, Porter J, Cervini LA, Kirby DA, Craig AG, Rivier CL. Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists. J Med Chem. 2000 Mar 9;43(5):807-18. doi: 10.1021/jm990116+. PubMed PMID: 10715149.

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Zhu YF, Wilcoxen K, Saunders J, Guo Z, Gao Y, Connors PJ Jr, Gross TD, Tucci FC, Struthers RS, Reinhart GJ, Xie Q, Chen C. A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):403-6. doi: 10.1016/s0960-894x(01)00780-6. PubMed PMID: 11814807.

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Zhu YF, Struthers RS, Connors PJ Jr, Gao Y, Gross TD, Saunders J, Wilcoxen K, Reinhart GJ, Ling N, Chen C. Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):399-402. doi: 10.1016/s0960-894x(01)00779-x. PubMed PMID: 11814806.

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Wilcoxen KM, Zhu YF, Connors PJ, Saunders J, Gross TD, Gao Y, Reinhart GJ, Struthers RS, Chen C. Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2179-83. doi: 10.1016/s0960-894x(02)00370-0. PubMed PMID: 12127532.

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Gross TD, Zhu YF, Saunders J, Wilcoxen KM, Gao Y, Connors PJ Jr, Guo Z, Struthers RS, Reinhart GJ, Chen C. Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2185-7. doi: 10.1016/s0960-894x(02)00371-2. PubMed PMID: 12127533.

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Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, Struthers RS, Reinhart GJ, Wang X, Saunders J, Chen C. A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3491-5. doi: 10.1016/s0960-894x(02)00745-x. PubMed PMID: 12419391.

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Zhu YF, Guo Z, Gross TD, Gao Y, Connors PJ Jr, Struthers RS, Xie Q, Tucci FC, Reinhart GJ, Wu D, Saunders J, Chen C. Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists. J Med Chem. 2003 Apr 24;46(9):1769-72. doi: 10.1021/jm0205402. PubMed PMID: 12699396.

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Zhu YF, Gross TD, Guo Z, Connors PJ Jr, Gao Y, Tucci FC, Struthers RS, Reinhart GJ, Saunders J, Chen TK, Killam Bonneville AL, Chen C. Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists. J Med Chem. 2003 May 22;46(11):2023-6. doi: 10.1021/jm034041s. PubMed PMID: 12747774.

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Guo Z, Zhu YF, Tucci FC, Gao Y, Struthers RS, Saunders J, Gross TD, Xie Q, Reinhart GJ, Chen C. Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3311-5. doi: 10.1016/s0960-894x(03)00620-6. PubMed PMID: 12951116.

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Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, Struthers RS, Reinhart GJ, Saunders J, Chen C. Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3317-22. doi: 10.1016/s0960-894x(03)00619-x. PubMed PMID: 12951117.

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Guo Z, Chen Y, Wu D, Zhu YF, Struthers RS, Saunders J, Xie Q, Chen C. Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3617-22. doi: 10.1016/s0960-894x(03)00746-7. PubMed PMID: 14505682.

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Guo Z, Zhu YF, Gross TD, Tucci FC, Gao Y, Moorjani M, Connors PJ Jr, Rowbottom MW, Chen Y, Struthers RS, Xie Q, Saunders J, Reinhart G, Chen TK, Bonneville AL, Chen C. Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists. J Med Chem. 2004 Feb 26;47(5):1259-71. doi: 10.1021/jm030472z. PubMed PMID: 14971906.

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Ott TR, Lio FM, Olshefski D, Liu XJ, Struthers RS, Ling N. Determinants of high-affinity binding and receptor activation in the N-terminus of CCL-19 (MIP-3 beta). Biochemistry. 2004 Mar 30;43(12):3670-8. doi: 10.1021/bi035895h. PubMed PMID: 15035637.

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Rowbottom MW, Tucci FC, Zhu YF, Guo Z, Gross TD, Reinhart GJ, Xie Q, Struthers RS, Saunders J, Chen C. Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2269-74. doi: 10.1016/j.bmcl.2004.02.004. PubMed PMID: 15081023.

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Kohout TA, Nicholas SL, Perry SJ, Reinhart G, Junger S, Struthers RS. Differential desensitization, receptor phosphorylation, beta-arrestin recruitment, and ERK1/2 activation by the two endogenous ligands for the CC chemokine receptor 7. J Biol Chem. 2004 May 28;279(22):23214-22. doi: 10.1074/jbc.M402125200. Epub 2004 Mar 30. PubMed PMID: 15054093.

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Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, Gao Y, Rowbottom MW, Struthers RS, Reinhart GJ, Xie Q, Chen TK, Bozigian H, Killam Bonneville AL, Fisher A, Jin L, Saunders J, Chen C. 3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor. J Med Chem. 2004 Jul 1;47(14):3483-6. doi: 10.1021/jm049791w. PubMed PMID: 15214774.

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Reinhart GJ, Xie Q, Liu XJ, Zhu YF, Fan J, Chen C, Struthers RS. Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus. J Biol Chem. 2004 Aug 13;279(33):34115-22. doi: 10.1074/jbc.M404474200. Epub 2004 May 21. PubMed PMID: 15155770.

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Rowbottom MW, Tucci FC, Connors PJ Jr, Gross TD, Zhu YF, Guo Z, Moorjani M, Acevedo O, Carter L, Sullivan SK, Xie Q, Fisher A, Struthers RS, Saunders J, Chen C. Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4967-73. doi: 10.1016/j.bmcl.2004.07.022. PubMed PMID: 15341961.

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Ott TR, Pahuja A, Nickolls SA, Alleva DG, Struthers RS. Identification of CC chemokine receptor 7 residues important for receptor activation. J Biol Chem. 2004 Oct 8;279(41):42383-92. doi: 10.1074/jbc.M401097200. Epub 2004 Jul 28. PubMed PMID: 15284247.

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Lavrador K, Murphy B, Saunders J, Struthers S, Wang X, Williams J. A screening library for peptide activated G-protein coupled receptors. 1. The test set. J Med Chem. 2004 Dec 30;47(27):6864-74. doi: 10.1021/jm040084c. PubMed PMID: 15615535.

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Guo Z, Wu D, Zhu YF, Tucci FC, Pontillo J, Saunders J, Xie Q, Struthers RS, Chen C. A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):693-8. doi: 10.1016/j.bmcl.2004.11.026. PubMed PMID: 15664839.

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Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C. 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization. J Med Chem. 2005 Feb 24;48(4):1169-78. doi: 10.1021/jm049218c. PubMed PMID: 15715483.

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Ott TR, Pahuja A, Lio FM, Mistry MS, Gross M, Hudson SC, Wade WS, Simpson PB, Struthers RS, Alleva DG. A high-throughput chemotaxis assay for pharmacological characterization of chemokine receptors: Utilization of U937 monocytic cells. J Pharmacol Toxicol Methods. 2005 Mar-Apr;51(2):105-14. doi: 10.1016/j.vascn.2004.10.001. Epub 2004 Nov 5. PubMed PMID: 15767203.

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Perry SJ, Junger S, Kohout TA, Hoare SR, Struthers RS, Grigoriadis DE, Maki RA. Distinct conformations of the corticotropin releasing factor type 1 receptor adopted following agonist and antagonist binding are differentially regulated. J Biol Chem. 2005 Mar 25;280(12):11560-8. doi: 10.1074/jbc.M412914200. Epub 2005 Jan 14. PubMed PMID: 15653688.

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Guo Z, Chen Y, Huang CQ, Gross TD, Pontillo J, Rowbottom MW, Saunders J, Struthers S, Tucci FC, Xie Q, Wade W, Zhu YF, Wu D, Chen C. Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers. Bioorg Med Chem Lett. 2005 May 16;15(10):2519-22. doi: 10.1016/j.bmcl.2005.03.057. PubMed PMID: 15863308.

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Guo Z, Wu D, Zhu YF, Tucci FC, Regan CF, Rowbottom MW, Struthers RS, Xie Q, Reijmers S, Sullivan SK, Sai Y, Chen C. Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists. Bioorg Med Chem Lett. 2005 Aug 15;15(16):3685-90. doi: 10.1016/j.bmcl.2005.05.038. PubMed PMID: 15951171.

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Pontillo J, Guo Z, Wu D, Struthers RS, Chen C. Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4363-6. doi: 10.1016/j.bmcl.2005.06.057. PubMed PMID: 16046130.

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Tucci FC, Hu T, Mesleh MF, Bokser A, Allsopp E, Gross TD, Guo Z, Zhu YF, Struthers RS, Ling N, Chen C. Atropisomeric property of 1-(2,6-difluorobenzyl)-3-[(2R)-amino-2-phenethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyluracil. Chirality. 2005 Nov;17(9):559-64. doi: 10.1002/chir.20198. PubMed PMID: 16196024.

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Betz SF, Reinhart GJ, Lio FM, Chen C, Struthers RS. Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. J Med Chem. 2006 Jan 26;49(2):637-47. doi: 10.1021/jm0506928. PubMed PMID: 16420049.

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Sullivan SK, Hoare SR, Fleck BA, Zhu YF, Heise CE, Struthers RS, Crowe PD. Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism. Biochem Pharmacol. 2006 Sep 28;72(7):838-49. doi: 10.1016/j.bcp.2006.07.011. Epub 2006 Aug 22. PubMed PMID: 16930559.

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Ott TR, Lio FM, Olshefski D, Liu XJ, Ling N, Struthers RS. The N-terminal domain of CCL21 reconstitutes high affinity binding, G protein activation, and chemotactic activity, to the C-terminal domain of CCL19. Biochem Biophys Res Commun. 2006 Sep 29;348(3):1089-93. doi: 10.1016/j.bbrc.2006.07.165. Epub 2006 Aug 4. PubMed PMID: 16904643.

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Struthers RS, Chen T, Campbell B, Jimenez R, Pan H, Yen SS, Bozigian HP. Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902). J Clin Endocrinol Metab. 2006 Oct;91(10):3903-7. doi: 10.1210/jc.2006-1110. Epub 2006 Jul 18. PubMed PMID: 16849403.

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Betz SF, Lio FM, Gao Y, Reinhart GJ, Guo Z, Mesleh MF, Zhu YF, Struthers RS. Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling. J Med Chem. 2006 Oct 19;49(21):6170-6. doi: 10.1021/jm060580w. PubMed PMID: 17034124.