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Items: 42

1.

Selective estrogen receptor-beta (SERM-beta) compounds modulate raphe nuclei tryptophan hydroxylase-1 (TPH-1) mRNA expression and cause antidepressant-like effects in the forced swim test.

Clark JA, Alves S, Gundlah C, Rocha B, Birzin ET, Cai SJ, Flick R, Hayes E, Ho K, Warrier S, Pai L, Yudkovitz J, Fleischer R, Colwell L, Li S, Wilkinson H, Schaeffer J, Wilkening R, Mattingly E, Hammond M, Rohrer SP.

Neuropharmacology. 2012 Nov;63(6):1051-63. doi: 10.1016/j.neuropharm.2012.07.004. Epub 2012 Jul 13.

PMID:
22796107
2.

Control of rat tail skin temperature regulation by estrogen receptor-beta selective ligand.

Opas EE, Scafonas A, Nantermet PV, Wilkening RR, Birzin ET, Wilkinson H, Colwell LF, Schaeffer JM, Towler DA, Rodan GA, Schmidt A.

Maturitas. 2009 Sep 20;64(1):46-51. doi: 10.1016/j.maturitas.2009.07.007. Epub 2009 Aug 12.

PMID:
19679413
3.

Agonist-like SERM effects on ERalpha-mediated repression of MMP1 promoter activity predict in vivo effects on bone and uterus.

Scafonas A, Reszka AA, Kimmel DB, Hou XS, Su Q, Birzin ET, Kim S, Chen HY, Tan Q, Roher SP, Dininno F, Hammond ML, Rodan GA, Towler DA, Schmidt A.

J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):197-206. doi: 10.1016/j.jsbmb.2007.10.013. Epub 2008 Apr 20.

PMID:
18508261
4.

Androstene-3,5-dienes as ER-beta selective SERMs.

Blizzard TA, Gude C, Morgan JD 2nd, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Rohrer SP, Hammond ML.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.

PMID:
17890084
5.

Bridged androstenediol analogs as ER-beta selective SERMs.

Blizzard TA, Gude C, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Holmes MA, Rohrer SP, Hammond ML.

Bioorg Med Chem Lett. 2007 May 15;17(10):2944-8. Epub 2006 Dec 21.

PMID:
17448656
6.

Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.

Dykstra KD, Guo L, Birzin ET, Chan W, Yang YT, Hayes EC, DaSilva CA, Pai LY, Mosley RT, Kraker B, Fitzgerald PM, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2322-8. Epub 2007 Jan 25.

PMID:
17289385
7.

Antidiabetic activity of a highly potent and selective nonpeptide somatostatin receptor subtype-2 agonist.

Strowski MZ, Cashen DE, Birzin ET, Yang L, Singh V, Jacks TM, Nowak KW, Rohrer SP, Patchett AA, Smith RG, Schaeffer JM.

Endocrinology. 2006 Oct;147(10):4664-73. Epub 2006 Jul 20.

PMID:
16857751
8.

Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands.

Wildonger KJ, Ratcliffe RW, Mosley RT, Hammond ML, Birzin ET, Rohrer SP.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4462-6. Epub 2006 Jul 11.

PMID:
16815012
9.

Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.

Parker DL Jr, Meng D, Ratcliffe RW, Wilkening RR, Sperbeck DM, Greenlee ML, Colwell LF, Lambert S, Birzin ET, Frisch K, Rohrer SP, Nilsson S, Thorsell AG, Hammond ML.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4652-6. Epub 2006 Jun 13. Erratum in: Bioorg Med Chem Lett. 2006 Oct 15;16(20):5472.

PMID:
16777408
10.

Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.

Wilkening RR, Ratcliffe RW, Fried AK, Meng D, Sun W, Colwell L, Lambert S, Greenlee M, Nilsson S, Thorsell A, Mojena M, Tudela C, Frisch K, Chan W, Birzin ET, Rohrer SP, Hammond ML.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3896-901. Epub 2006 May 30.

PMID:
16730987
11.

The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.

Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2.

PMID:
16632357
12.

6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.

Sun W, Cama LD, Birzin ET, Warrier S, Locco L, Mosley R, Hammond ML, Rohrer SP.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1468-72. Epub 2006 Jan 18.

PMID:
16412638
13.

Androstenediol analogs as ER-beta-selective SERMs.

Blizzard TA, Gude C, Morgan JD 2nd, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Sharma N, Fitzgerald PM, Rohrer SP, Hammond ML.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):834-8. Epub 2005 Nov 23.

PMID:
16309907
14.

Antagonist-induced, activation function-2-independent estrogen receptor alpha phosphorylation.

Lipfert L, Fisher JE, Wei N, Scafonas A, Su Q, Yudkovitz J, Chen F, Warrier S, Birzin ET, Kim S, Chen HY, Tan Q, Schmidt A, Dininno F, Rohrer SP, Hammond ML, Rodan GA, Freedman LP, Reszka AA.

Mol Endocrinol. 2006 Mar;20(3):516-33. Epub 2005 Oct 13.

PMID:
16223974
15.

Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.

Blizzard TA, Morgan JD 2nd, Chan W, Birzin ET, Pai LY, Hayes EC, DaSilva CA, Mosley RT, Yang YT, Rohrer SP, Dininno F, Hammond ML.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5124-8. Epub 2005 Oct 3.

PMID:
16203138
16.

Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.

Blizzard TA, DiNinno F, Chen HY, Kim S, Wu JY, Chan W, Birzin ET, Yang YT, Pai LY, Hayes EC, DaSilva CA, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3912-6.

PMID:
15993065
17.

Synthesis and binding affinities of novel SRIF-mimicking beta-D-glucosides satisfying the requirement for a pi-cloud at C1.

Angeles AR, Neagu I, Birzin ET, Thornton ER, Smith AB 3rd, Hirschmann R.

Org Lett. 2005 Mar 17;7(6):1121-4.

PMID:
15760154
18.

Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs.

Tan Q, Blizzard TA, Morgan JD 2nd, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, Warrier S, Yudkovitz J, Wilkinson HA, Sharma N, Fitzgerald PM, Li S, Colwell L, Fisher JE, Adamski S, Reszka AA, Kimmel D, DiNinno F, Rohrer SP, Freedman LP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1675-81.

PMID:
15745820
19.

Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.

Liu J, Birzin ET, Chan W, Yang YT, Pai LY, Dasilva C, Hayes EC, Mosley RT, Dininno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):715-8.

PMID:
15664843
20.

Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers.

Blizzard TA, Dininno F, Morgan JD 2nd, Chen HY, Wu JY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Fitzgerald PM, Sharma N, Li Y, Zhang Z, Hayes EC, Dasilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):107-13.

PMID:
15582421
21.

Estrogen receptor ligands. Part 8: Dihydrobenzoxathiin SERAMs with heteroatom-substituted side chains.

Blizzard TA, DiNinno F, Morgan JD 2nd, Wu JY, Chen HY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3865-8.

PMID:
15225686
22.

Estrogen receptor ligands. Part 7: Dihydrobenzoxathiin SERAMs with bicyclic amine side chains.

Blizzard TA, DiNinno F, Morgan JD 2nd, Chen HY, Wu JY, Gude C, Kim S, Chan W, Birzin ET, Tien Yang Y, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3861-4.

PMID:
15225685
23.

Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins.

Tan Q, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3753-5.

PMID:
15203156
24.

Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains.

Tan Q, Birzin ET, Chan W, Tien Yang Y, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3747-51.

PMID:
15203155
25.

Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.

Kim S, Wu J, Chen HY, Birzin ET, Chan W, Yang YT, Colwell L, Li S, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2741-5.

PMID:
15125925
26.

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

Chen HY, Kim S, Wu JY, Birzin ET, Chan W, Yang YT, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 May 17;14(10):2551-4.

PMID:
15109649
27.

A beta-lactamase-dependent Gal4-estrogen receptor beta transactivation assay for the ultra-high throughput screening of estrogen receptor beta agonists in a 3456-well format.

Peekhaus NT, Ferrer M, Chang T, Kornienko O, Schneeweis JE, Smith TS, Hoffman I, Mitnaul LJ, Chin J, Fischer PA, Blizzard TA, Birzin ET, Chan W, Inglese J, Strulovici B, Rohrer SP, Schaeffer JM.

Assay Drug Dev Technol. 2003 Dec;1(6):789-800.

PMID:
15090225
28.

Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.

Kim S, Wu JY, Birzin ET, Frisch K, Chan W, Pai LY, Yang YT, Mosley RT, Fitzgerald PM, Sharma N, Dahllund J, Thorsell AG, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

J Med Chem. 2004 Apr 22;47(9):2171-5.

PMID:
15084115
29.

Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.

Chen HY, Dykstra KD, Birzin ET, Frisch K, Chan W, Yang YT, Mosley RT, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1417-21.

PMID:
15006374
30.

Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!

Blizzard TA, Mosley RT, Birzin ET, Chan W, Hammond ML.

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1317-21.

PMID:
14980690
31.

Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.

Prasad V, Birzin ET, McVaugh CT, Van Rijn RD, Rohrer SP, Chicchi G, Underwood DJ, Thornton ER, Smith AB 3rd, Hirschmann R.

J Med Chem. 2003 May 8;46(10):1858-69.

PMID:
12723949
32.

2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).

Blizzard TA, Morgan JD 2nd, Mosley RT, Birzin ET, Frisch K, Rohrer SP, Hammond ML.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):479-83.

PMID:
12565955
33.

High-throughput receptor-binding methods for somatostatin receptor 2.

Birzin ET, Rohrer SP.

Anal Biochem. 2002 Aug 1;307(1):159-66.

PMID:
12137793
34.

Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.

Zhou C, Guo L, Morriello G, Pasternak A, Pan Y, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):415-7.

PMID:
11212124
35.

A combinatorial approach toward the discovery of non-peptide, subtype-selective somatostatin receptor ligands.

Berk SC, Rohrer SP, Degrado SJ, Birzin ET, Mosley RT, Hutchins SM, Pasternak A, Schaeffer JM, Underwood DJ, Chapman KT.

J Comb Chem. 1999 Sep-Oct;1(5):388-96.

PMID:
10748735
36.

Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.

Ye Z, Gao Y, Bakshi RK, Chen MH, Rohrer SP, Feighner SD, Pong SS, Howard AD, Blake A, Birzin ET, Locco L, Parmar RM, Chan WW, Schaeffer JM, Smith RG, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):5-8.

PMID:
10636230
37.

Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.

Pasternak A, Pan Y, Marino D, Sanderson PE, Mosley R, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):491-6.

PMID:
10091708
38.

Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.

Rohrer SP, Birzin ET, Mosley RT, Berk SC, Hutchins SM, Shen DM, Xiong Y, Hayes EC, Parmar RM, Foor F, Mitra SW, Degrado SJ, Shu M, Klopp JM, Cai SJ, Blake A, Chan WW, Pasternak A, Yang L, Patchett AA, Smith RG, Chapman KT, Schaeffer JM.

Science. 1998 Oct 23;282(5389):737-40. Erratum in: Science 1998 Nov 27;282(5394):1646.

39.

Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.

Yang L, Berk SC, Rohrer SP, Mosley RT, Guo L, Underwood DJ, Arison BH, Birzin ET, Hayes EC, Mitra SW, Parmar RM, Cheng K, Wu TJ, Butler BS, Foor F, Pasternak A, Pan Y, Silva M, Freidinger RM, Smith RG, Chapman K, Schaeffer JM, Patchett AA.

Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10836-41.

40.

Identification of neuron-specific ivermectin binding sites in Drosophila melanogaster and Schistocerca americana.

Rohrer SP, Birzin ET, Costa SD, Arena JP, Hayes EC, Schaeffer JM.

Insect Biochem Mol Biol. 1995 Jan;25(1):11-7.

PMID:
7711743
41.
42.

Ivermectin binding sites in sensitive and resistant Haemonchus contortus.

Rohrer SP, Birzin ET, Eary CH, Schaeffer JM, Shoop WL.

J Parasitol. 1994 Jun;80(3):493-7.

PMID:
8195956

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