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Page 1
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: zaczek r. 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
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: zaczek r. 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.
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Thompson LA, Liauw AY, Ramanjulu MM, Kasireddy-Polam P, Mercer SE, Maduskuie TP, Glicksman M, Roach AH, Meredith JE, Liu RQ, Combs AP, Higaki JN, Cordell B, Seiffert D, Zaczek RC, Robertson DW, Olson RE. Thompson LA, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. doi: 10.1016/j.bmcl.2006.01.055. Epub 2006 Feb 10. Bioorg Med Chem Lett. 2006. PMID: 16473009
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. Gillman KW, et al. Among authors: zaczek r. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900185 Free PMC article.
Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF. Kostich W, et al. Among authors: zaczek r. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13. J Pharmacol Exp Ther. 2016. PMID: 27411717 Free PMC article.
112 results