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Page 1
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. Burton CR, et al. Among authors: polson c. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase.
Prasad CV, Vig S, Smith DW, Gao Q, Polson CT, Corsa JA, Guss VL, Loo A, Barten DM, Zheng M, Felsenstein KM, Roberts SB. Prasad CV, et al. Among authors: polson ct. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3535-8. doi: 10.1016/j.bmcl.2004.04.056. Bioorg Med Chem Lett. 2004. PMID: 15177468
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Prasad CV, Zheng M, Vig S, Bergstrom C, Smith DW, Gao Q, Yeola S, Polson CT, Corsa JA, Guss VL, Loo A, Wang J, Sleczka BG, Dangler C, Robertson BJ, Hendrick JP, Roberts SB, Barten DM. Prasad CV, et al. Among authors: polson ct. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4006-11. doi: 10.1016/j.bmcl.2007.04.082. Epub 2007 Apr 30. Bioorg Med Chem Lett. 2007. PMID: 17502137
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Deshpande MS, Felsenstein KM, Guss VL, Hansel SB, Johnson G, Keavy DJ, Lau WY, Mock J, Prasad CV, Polson CT, Sloan CP, Smith DW, Wallace OB, Wang HH, Williams A, Zheng M. Parker MF, et al. Among authors: polson ct. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606371
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. Parker MF, et al. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. doi: 10.1016/j.bmcl.2007.08.047. Epub 2007 Aug 26. Bioorg Med Chem Lett. 2007. PMID: 17869509
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bergstrom CP, Sloan CP, Wang HH, Parker MF, Smith DW, Zheng M, Hansel SB, Polson CT, Barber LE, Bursuker I, Guss VL, Corsa JA, Barten DM, Felsenstein KM, Roberts SB. Bergstrom CP, et al. Bioorg Med Chem Lett. 2008 Jan 1;18(1):175-8. doi: 10.1016/j.bmcl.2007.10.105. Epub 2007 Nov 1. Bioorg Med Chem Lett. 2008. PMID: 18023581
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Bergstrom CP, Sloan CP, Lau WY, Smith DW, Zheng M, Hansel SB, Polson CT, Corsa JA, Barten DM, Felsenstein KM, Roberts SB. Bergstrom CP, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):464-8. doi: 10.1016/j.bmcl.2007.11.102. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18178084
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. Albright CF, et al. Among authors: polson c. J Pharmacol Exp Ther. 2013 Mar;344(3):686-95. doi: 10.1124/jpet.112.199356. Epub 2012 Dec 28. J Pharmacol Exp Ther. 2013. PMID: 23275065
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. Meredith JE Jr, et al. Among authors: polson c. J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499745
52 results