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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: fiedler t. 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.
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: fiedler t. 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
Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF1R).
Vrudhula VM, Dasgupta B, Pin SS, Burris KD, Balanda LA, Fung LK, Fiedler T, Browman KE, Taber MT, Zhang J, Macor JE, Dubowchik GM. Vrudhula VM, et al. Among authors: fiedler t. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1905-9. doi: 10.1016/j.bmcl.2010.01.127. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20185312
2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy.
Dubowchik GM, Michne JA, Zuev D, Schwartz W, Scola PM, James CA, Ruediger EH, Pin SS, Burris KD, Balanda LA, Gao Q, Wu D, Fung L, Fiedler T, Browman KE, Taber MT, Zhang J. Dubowchik GM, et al. Among authors: fiedler t. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3997-4000. doi: 10.1016/j.bmcl.2003.08.055. Bioorg Med Chem Lett. 2003. PMID: 14592493
194 results