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Page 1
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. Among authors: zaczek rc. 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
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Dzierba CD, Sielecki TM, Arvanitis AG, Galka A, Johnson TL, Takvorian AG, Rafalski M, Kasireddy-Polam P, Vig S, Dasgupta B, Zhang G, Molski TF, Wong H, Zaczek RC, Lodge NJ, Combs AP, Gilligan PJ, Trainor GL, Bronson JJ, Macor JE. Dzierba CD, et al. Among authors: zaczek rc. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22749422
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Arvanitis AG, Rescinito JT, Arnold CR, Wilde RG, Cain GA, Sun JH, Yan JS, Teleha CA, Fitzgerald LW, McElroy J, Zaczek R, Hartig PR, Grossman S, Arneric SP, Gilligan PJ, Olson RE, Robertson DW. Arvanitis AG, et al. Bioorg Med Chem Lett. 2003 Jan 6;13(1):125-8. doi: 10.1016/s0960-894x(02)00833-8. Bioorg Med Chem Lett. 2003. PMID: 12467631
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. 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.
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R. Seiffert D, et al. J Biol Chem. 2000 Nov 3;275(44):34086-91. doi: 10.1074/jbc.M005430200. J Biol Chem. 2000. PMID: 10915801 Free article.
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE. Hartz RA, et al. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Dzierba CD, Takvorian AG, Rafalski M, Kasireddy-Polam P, Wong H, Molski TF, Zhang G, Li YW, Lelas S, Peng Y, McElroy JF, Zaczek RC, Taub RA, Combs AP, Gilligan PJ, Trainor GL. Dzierba CD, et al. Among authors: zaczek rc. J Med Chem. 2004 Nov 4;47(23):5783-90. doi: 10.1021/jm049737f. J Med Chem. 2004. PMID: 15509177
98 results