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Page 1
Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.
Hussain I, Hawkins J, Harrison D, Hille C, Wayne G, Cutler L, Buck T, Walter D, Demont E, Howes C, Naylor A, Jeffrey P, Gonzalez MI, Dingwall C, Michel A, Redshaw S, Davis JB. Hussain I, et al. Among authors: hawkins j. J Neurochem. 2007 Feb;100(3):802-9. doi: 10.1111/j.1471-4159.2006.04260.x. J Neurochem. 2007. PMID: 17156133 Free article.
TASTPM mice expressing amyloid precursor protein and presenilin-1 mutant transgenes are sensitive to γ-secretase modulation and amyloid-β₄₂ lowering by GSM-10h.
Hussain I, Harrison DC, Hawkins J, Chapman T, Marshall I, Facci L, Ahmed S, Brackenborough K, Skaper SD, Mead TL, Smith BB, Giblin GM, Hall A, Gonzalez MI, Richardson JC. Hussain I, et al. Among authors: hawkins j. Neurodegener Dis. 2011;8(1-2):15-24. doi: 10.1159/000313903. Epub 2010 Aug 4. Neurodegener Dis. 2011. PMID: 20689247
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: hawkins j. 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: hawkins j. 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
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Charrier N, Clarke B, Demont E, Dingwall C, Dunsdon R, Hawkins J, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: hawkins j. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3669-73. doi: 10.1016/j.bmcl.2009.03.150. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19477642
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: hawkins j. 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
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: hawkins j. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3664-8. doi: 10.1016/j.bmcl.2009.03.165. Epub 2009 Apr 17. Bioorg Med Chem Lett. 2009. PMID: 19428244
1,736 results