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BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Clarke B, et al. Among authors: riddell d. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1017-21. doi: 10.1016/j.bmcl.2007.12.019. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18166458
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Clarke B, et al. Among authors: riddell d. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1011-6. doi: 10.1016/j.bmcl.2007.12.017. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18171614
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Beswick P, Charrier N, Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Gleave R, Hawkins J, Hussain I, Johnson CN, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Skidmore J, Soleil V, Smith KJ, Stanway S, Stemp G, Stuart A, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Beswick P, et al. Among authors: riddell d. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1022-6. doi: 10.1016/j.bmcl.2007.12.020. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18171615
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J. Kreft A, et al. Among authors: riddell dr. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18556202
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: riddell dr. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
171 results