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Items: 48

1.

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.

Boy KM, Guernon JM, Zuev DS, Xu L, Zhang Y, Shi J, Marcin LR, Higgins MA, Wu YJ, Krishnananthan S, Li J, Trehan A, Smith D, Toyn JH, Meredith JE, Burton CR, Kimura SR, Zvyaga T, Zhuo X, Lentz KA, Grace JE, Denton R, Morrison JS, Mathur A, Albright CF, Ahlijanian MK, Olson RE, Thompson LA, Macor JE.

ACS Med Chem Lett. 2019 Feb 17;10(3):312-317. doi: 10.1021/acsmedchemlett.8b00541. eCollection 2019 Mar 14.

2.

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
3.

Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.

Wu YJ, Guernon J, Rajamani R, Toyn JH, Ahlijanian MK, Albright CF, Muckelbauer J, Chang C, Camac D, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5729-5731. doi: 10.1016/j.bmcl.2016.10.055. Epub 2016 Oct 20.

PMID:
27816517
4.

Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine β-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.

Wu YJ, Guernon J, Shi J, Marcin L, Higgins M, Rajamani R, Muckelbauer J, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA.

J Med Chem. 2016 Sep 22;59(18):8593-600. doi: 10.1021/acs.jmedchem.6b01012. Epub 2016 Sep 7.

PMID:
27559936
5.

Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.

Toyn JH, Boy KM, Raybon J, Meredith JE Jr, Robertson AS, Guss V, Hoque N, Sweeney F, Zhuo X, Clarke W, Snow K, Denton RR, Zuev D, Thompson LA, Morrison J, Grace J, Berisha F, Furlong M, Wang JS, Lentz KA, Padmanabha R, Cook L, Wei C, Drexler DM, Macor JE, Albright CF, Gasior M, Olson RE, Hong Q, Soares HD, AbuTarif M, Ahlijanian MK.

J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. doi: 10.1124/jpet.116.232249. Epub 2016 Apr 20.

6.

The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers.

Soares HD, Gasior M, Toyn JH, Wang JS, Hong Q, Berisha F, Furlong MT, Raybon J, Lentz KA, Sweeney F, Zheng N, Akinsanya B, Berman RM, Thompson LA, Olson RE, Morrison J, Drexler DM, Macor JE, Albright CF, Ahlijanian MK, AbuTarif M.

J Pharmacol Exp Ther. 2016 Jul;358(1):138-50. doi: 10.1124/jpet.116.232256. Epub 2016 Apr 20.

7.

Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents.

Wu YJ, Guernon J, Yang F, Snyder L, Shi J, Mcclure A, Rajamani R, Park H, Ng A, Lewis H, Chang C, Camac D, Toyn JH, Ahlijanian MK, Albright CF, Macor JE, Thompson LA.

ACS Med Chem Lett. 2016 Jan 11;7(3):271-6. doi: 10.1021/acsmedchemlett.5b00432. eCollection 2016 Mar 10.

8.

Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators.

Wu YJ, Zhang Y, Toyn JH, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1554-1557. doi: 10.1016/j.bmcl.2016.02.016. Epub 2016 Feb 8.

PMID:
26898338
9.

Design and optimization of tricyclic gamma-secretase modulators.

Shi J, Zuev D, Xu L, Lentz KA, Grace JE, Toyn JH, Olson RE, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1498-502. doi: 10.1016/j.bmcl.2015.06.020. Epub 2015 Jun 12.

PMID:
26848108
10.

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).

Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20.

PMID:
26497283
11.

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.

12.

Interpreting Alzheimer's disease clinical trials in light of the effects on amyloid-β.

Toyn JH, Ahlijanian MK.

Alzheimers Res Ther. 2014 Mar 12;6(2):14. doi: 10.1186/alzrt244. eCollection 2014. Review.

13.

γ -Secretase Pharmacology: What Pharmacology Will Work for Alzheimer's Disease?

Toyn JH, Rowley A, Matsuoka Y, Tomita T, Imbimbo BP.

Int J Alzheimers Dis. 2013;2013:849128. doi: 10.1155/2013/849128. Epub 2013 Apr 18. No abstract available.

14.

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.

Albright CF, Dockens RC, Meredith JE Jr, Olson RE, Slemmon R, Lentz KA, Wang JS, Denton RR, Pilcher G, Rhyne PW, Raybon JJ, Barten DM, Burton C, Toyn JH, Sankaranarayanan S, Polson C, Guss V, White R, Simutis F, Sanderson T, Gillman KW, Starrett JE Jr, Bronson J, Sverdlov O, Huang SP, Castaneda L, Feldman H, Coric V, Zaczek R, Macor JE, Houston J, Berman RM, Tong G.

J Pharmacol Exp Ther. 2013 Mar;344(3):686-95. doi: 10.1124/jpet.112.199356. Epub 2012 Dec 28.

PMID:
23275065
15.

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
16.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.

PMID:
21974952
17.

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE).

Boy KM, Guernon JM, Shi J, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Marcinkeviciene J, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Lentz KA, Bronson JJ, Olson RE, Macor JE, Thompson LA 3rd.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6916-24. doi: 10.1016/j.bmcl.2011.06.109. Epub 2011 Jun 30.

PMID:
21782431
18.

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.

Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079.

PMID:
21078556
19.

Viable mouse gene ablations that robustly alter brain Aβ levels are rare.

Toyn JH, Lin XA, Thompson MW, Guss V, Meredith JE Jr, Sankaranarayanan S, Barrezueta N, Corradi J, Majumdar A, Small DL, Hansard M, Lanthorn T, Westphal RS, Albright CF.

BMC Neurosci. 2010 Nov 5;11:143. doi: 10.1186/1471-2202-11-143.

20.

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE.

ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10.

21.

Application of quantitative LC-MS surrogate peptide methodology in the analysis of the amyloid beta peptide (Abeta) biosynthetic intermediate protein APP-betaCTF.

Cantone JL, Xu-Lin A, Toyn JH, Drexler DM.

J Neurosci Methods. 2009 Jun 15;180(2):255-60. doi: 10.1016/j.jneumeth.2009.03.018. Epub 2009 Mar 31.

PMID:
19464516
22.

Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.

Wu YJ, Zhang Y, Good AC, Burton CR, Toyn JH, Albright CF, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2009 May 15;19(10):2654-60. doi: 10.1016/j.bmcl.2009.03.144. Epub 2009 Apr 5.

PMID:
19375914
23.

[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
24.

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.

25.

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
26.

Qualitative and quantitative characterization of the amyloid beta peptide (Abeta) population in biological matrices using an immunoprecipitation-LC/MS assay.

Ford MJ, Cantone JL, Polson C, Toyn JH, Meredith JE, Drexler DM.

J Neurosci Methods. 2008 Mar 15;168(2):465-74. doi: 10.1016/j.jneumeth.2007.11.019. Epub 2007 Nov 29.

PMID:
18187205
27.

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.

28.

Amino-caprolactam derivatives as gamma-secretase inhibitors.

Parker MF, Bronson JJ, Barten DM, Corsa JA, Du W, Felsenstein KM, Guss VL, Izzarelli D, Loo A, McElhone KE, Marcin LR, Padmanabha R, Pak R, Polson CT, Toyn JH, Varma S, Wang J, Wong V, Zheng M, Roberts SB.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. Epub 2007 Aug 26.

PMID:
17869509
29.

Soluble Abeta and cognitive function in aged F-344 rats and Tg2576 mice.

Lindner MD, Hogan JB, Krause RG, Machet F, Bourin C, Hodges DB Jr, Corsa JA, Barten DM, Toyn JH, Stock DA, Rose GM, Gribkoff VK.

Behav Brain Res. 2006 Oct 2;173(1):62-75. Epub 2006 Jul 7.

PMID:
16828889
31.

Plasmid construction by linker-assisted homologous recombination in yeast.

Gunyuzlu PL, Hollis GF, Toyn JH.

Biotechniques. 2001 Dec;31(6):1246, 1248, 1250. No abstract available.

32.
33.

A yeast genetic assay for caspase cleavage of the amyloid-beta precursor protein.

Gunyuzlu PL, White WH, Davis GL, Hollis GF, Toyn JH.

Mol Biotechnol. 2000 May;15(1):29-37.

PMID:
10911620
34.

A counterselection for the tryptophan pathway in yeast: 5-fluoroanthranilic acid resistance.

Toyn JH, Gunyuzlu PL, White WH, Thompson LA, Hollis GF.

Yeast. 2000 Apr;16(6):553-60.

35.

A Bub2p-dependent spindle checkpoint pathway regulates the Dbf2p kinase in budding yeast.

Fesquet D, Fitzpatrick PJ, Johnson AL, Kramer KM, Toyn JH, Johnston LH.

EMBO J. 1999 May 4;18(9):2424-34.

36.

DNA replication is completed in Saccharomyces cerevisiae cells that lack functional Cdc14, a dual-specificity protein phosphatase.

Fitzpatrick PJ, Toyn JH, Millar JB, Johnston LH.

Mol Gen Genet. 1998 May;258(4):437-41.

PMID:
9648751
37.

Swi5 controls a novel wave of cyclin synthesis in late mitosis.

Aerne BL, Johnson AL, Toyn JH, Johnston LH.

Mol Biol Cell. 1998 Apr;9(4):945-56.

38.

DBF2 protein kinase binds to and acts through the cell cycle-regulated MOB1 protein.

Komarnitsky SI, Chiang YC, Luca FC, Chen J, Toyn JH, Winey M, Johnston LH, Denis CL.

Mol Cell Biol. 1998 Apr;18(4):2100-7.

39.
40.
41.

Rme1, a negative regulator of meiosis, is also a positive activator of G1 cyclin gene expression.

Toone WM, Johnson AL, Banks GR, Toyn JH, Stuart D, Wittenberg C, Johnston LH.

EMBO J. 1995 Dec 1;14(23):5824-32.

42.
43.

The activation of DNA replication in yeast.

Toyn JH, Toone WM, Morgan BA, Johnston LH.

Trends Biochem Sci. 1995 Feb;20(2):70-3. Review.

PMID:
7701565
44.
45.

P40SDB25, a putative CDK inhibitor, has a role in the M/G1 transition in Saccharomyces cerevisiae.

Donovan JD, Toyn JH, Johnson AL, Johnston LH.

Genes Dev. 1994 Jul 15;8(14):1640-53.

48.

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