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Items: 36

1.

Synergistic inhibition of Aβ production by combinations of γ-secretase modulators.

Robertson AS, Iben LG, Wei C, Meredith JE Jr, Drexler DM, Banks M, Vite GD, Olson RE, Thompson LA, Albright CF, Ahlijanian MK, Toyn JH.

Eur J Pharmacol. 2017 Oct 5;812:104-112. doi: 10.1016/j.ejphar.2017.07.019. Epub 2017 Jul 8.

PMID:
28690193
2.

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF.

Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8.

3.

Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist.

Luo G, Chen L, Hu S, Huang Y, Mattson G, Iben LG, Russell JW, Clarke WJ, Hogan JB, Antal-Zimanyi I, Poindexter GS.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3814-7. doi: 10.1016/j.bmcl.2013.04.095. Epub 2013 May 15.

PMID:
23726344
4.

Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.

Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd.

J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2.

PMID:
23030502
5.

Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.

Hu S, Huang Y, Deshpande M, Luo G, Bruce MA, Chen L, Mattson G, Iben LG, Zhang J, Russell JW, Clarke WJ, Hogan JB, Ortiz A, Flint O, Henwood A, Gao Q, Antal-Zimanyi I, Poindexter GS.

ACS Med Chem Lett. 2012 Jan 4;3(3):222-6. doi: 10.1021/ml200265m. eCollection 2012 Mar 8.

6.

[3H]BMS-599240--a novel tritiated ligand for the characterization of BACE1 inhibitors.

Iben LG, Kopcho L, Marcinkeviciene J, Zheng C, Thompson LA, Albright CF, Toyn JH.

Eur J Pharmacol. 2008 Sep 28;593(1-3):10-5. doi: 10.1016/j.ejphar.2008.06.112. Epub 2008 Jul 11.

PMID:
18655784
7.

The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.

Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH.

J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23.

8.

Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist.

Antal-Zimanyi I, Bruce MA, Leboulluec KL, Iben LG, Mattson GK, McGovern RT, Hogan JB, Leahy CL, Flowers SC, Stanley JA, Ortiz AA, Poindexter GS.

Eur J Pharmacol. 2008 Aug 20;590(1-3):224-32. doi: 10.1016/j.ejphar.2008.06.032. Epub 2008 Jun 12.

PMID:
18573246
9.

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.

Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF.

J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22.

PMID:
18499745
10.

Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.

Iben LG, Olson RE, Balanda LA, Jayachandra S, Robertson BJ, Hay V, Corradi J, Prasad CV, Zaczek R, Albright CF, Toyn JH.

J Biol Chem. 2007 Dec 21;282(51):36829-36. Epub 2007 Oct 11.

11.

Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice.

Goldstein ME, Cao Y, Fiedler T, Toyn J, Iben L, Barten DM, Pierdomenico M, Corsa J, Prasad CV, Olson RE, Li YW, Zaczek R, Albright CF.

J Pharmacol Exp Ther. 2007 Oct;323(1):102-8. Epub 2007 Jul 19.

PMID:
17640949
12.

Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.

Gillman KW, Higgins MA, Poindexter GS, Browning M, Clarke WJ, Flowers S, Grace JE Jr, Hogan JB, McGovern RT, Iben LG, Mattson GK, Ortiz A, Rassnick S, Russell JW, Antal-Zimanyi I.

Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. Epub 2006 May 11.

PMID:
16697206
13.

(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.

Sun LQ, Takaki K, Chen J, Bertenshaw S, Iben L, Mahle CD, Ryan E, Wu D, Gao Q, Xu C.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1345-9.

PMID:
15713384
14.

Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.

Karageorge GN, Bertenshaw S, Iben L, Xu C, Sarbin N, Gentile A, Dubowchik GM.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5881-4.

PMID:
15501061
15.

N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.

Sun LQ, Takaki K, Chen J, Iben L, Knipe JO, Pajor L, Mahle CD, Ryan E, Xu C.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5157-60.

PMID:
15380218
16.

Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.

Boy KM, Dee M, Yevich J, Torrente J, Gao Q, Iben L, Stark A, Mattson RJ.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4467-70.

PMID:
15357973
17.

Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.

Sun LQ, Chen J, Bruce M, Deskus JA, Epperson JR, Takaki K, Johnson G, Iben L, Mahle CD, Ryan E, Xu C.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3799-802.

PMID:
15203165
18.

4-Substituted anilides as selective melatonin MT2 receptor agonists.

Epperson JR, Deskus JA, Gentile AJ, Iben LG, Ryan E, Sarbin NS.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1023-6.

PMID:
15013015
19.

Design and synthesis of benzoxazole derivatives as novel melatoninergic ligands.

Sun LQ, Chen J, Takaki K, Johnson G, Iben L, Mahle CD, Ryan E, Xu C.

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1197-200.

PMID:
14980664
20.

Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.

Sun LQ, Chen J, Mattson RJ, Epperson JR, Deskus JA, Li WS, Takaki K, Hodges DB, Iben L, Mahle CD, Ortiz A, Molstad D, Ryan E, Yeleswaram K, Xu C, Luo G.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4381-4.

PMID:
14643330
21.

beta-alanine dipeptides as MC4R agonists.

Ruel R, Herpin TF, Iben L, Luo G, Martel A, Mason H, Mattson G, Poirier B, Ruediger EH, Shi D, Thibault C, Yu G, Antal Zimanyi I, Poindexter GS, Macor JE.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4341-4.

PMID:
14643322
22.

Differentially functionalized diamines as novel ligands for the NPY2 receptor.

Andres CJ, Antal Zimanyi I, Deshpande MS, Iben LG, Grant-Young K, Mattson GK, Zhai W.

Bioorg Med Chem Lett. 2003 Sep 1;13(17):2883-5.

PMID:
14611849
23.

Indanyl piperazines as melatonergic MT2 selective agents.

Mattson RJ, Catt JD, Keavy D, Sloan CP, Epperson J, Gao Q, Hodges DB, Iben L, Mahle CD, Ryan E, Yocca FD.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1199-202.

PMID:
12643943
24.

Dihydropyridine neuropeptide Y Y(1) receptor antagonists.

Poindexter GS, Bruce MA, LeBoulluec KL, Monkovic I, Martin SW, Parker EM, Iben LG, McGovern RT, Ortiz AA, Stanley JA, Mattson GK, Kozlowski M, Arcuri M, Antal-Zimanyi I.

Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82.

PMID:
11814801
25.

Structural organization and chromosomal localization of three human galanin receptor genes.

Iismaa TP, Fathi Z, Hort YJ, Iben LG, Dutton JL, Baker E, Sutherland GR, Shine J.

Ann N Y Acad Sci. 1998 Dec 21;863:56-63.

PMID:
9928159
26.

Molecular characterization, pharmacological properties and chromosomal localization of the human GALR2 galanin receptor.

Fathi Z, Battaglino PM, Iben LG, Li H, Baker E, Zhang D, McGovern R, Mahle CD, Sutherland GR, Iismaa TP, Dickinson KE, Zimanyi IA.

Brain Res Mol Brain Res. 1998 Jul 15;58(1-2):156-69.

PMID:
9685625
27.

Cloning, pharmacological characterization and distribution of a novel galanin receptor .

Fathi Z, Cunningham AM, Iben LG, Battaglino PB, Ward SA, Nichol KA, Pine KA, Wang J, Goldstein ME, Iismaa TP, Zimanyi IA.

Brain Res Mol Brain Res. 1998 Jan;53(1-2):348. No abstract available.

PMID:
9473722
28.

Cloning, pharmacological characterization and distribution of a novel galanin receptor.

Fathi Z, Cunningham AM, Iben LG, Battaglino PB, Ward SA, Nichol KA, Pine KA, Wang J, Goldstein ME, Iismaa TP, Zimanyi IA.

Brain Res Mol Brain Res. 1997 Nov;51(1-2):49-59. Erratum in: Brain Res Mol Brain Res 1998 Jan;53(1-2):348.

PMID:
9427506
29.

Cloning and characterization of the rat GALR1 galanin receptor from Rin14B insulinoma cells.

Parker EM, Izzarelli DG, Nowak HP, Mahle CD, Iben LG, Wang J, Goldstein ME.

Brain Res Mol Brain Res. 1995 Dec 28;34(2):179-89.

PMID:
8750821
30.

Cloning, expression, and tissue distribution of a fifth melanocortin receptor subtype.

Fathi Z, Iben LG, Parker EM.

Neurochem Res. 1995 Jan;20(1):107-13.

PMID:
7739752
31.
32.

Characterization of human 5-HT1 receptors expressed in Sf9 insect cells.

Parker EM, Grisel DA, Iben LG, Nowak HP, Mahle CD, Yocca FD, Gaughan GT.

Eur J Pharmacol. 1994 Jun 15;268(1):43-53.

PMID:
7925611
33.
35.
36.

Hepatic uptake of propranolol.

Anderson JH, Anderson RC, Iben LS.

J Pharmacol Exp Ther. 1978 Jul;206(1):172-80.

PMID:
660547

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