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Page 1
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 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 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
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Pu J, Kreft AF, Aschmies SH, Atchison KP, Berkowitz J, Caggiano TJ, Chlenov M, Diamantidis G, Harrison BL, Hu Y, Huryn D, Steven Jacobsen J, Jin M, Lipinski K, Lu P, Martone RL, Morris K, Sonnenberg-Reines J, Riddell DR, Sabalski J, Sun SC, Wagner E, Wang Y, Xu Z, Zhou H, Resnick L. Pu J, et al. Among authors: riddell dr. Bioorg Med Chem. 2009 Jul 1;17(13):4708-17. doi: 10.1016/j.bmc.2009.04.052. Epub 2009 May 3. Bioorg Med Chem. 2009. PMID: 19443228
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA. O'Neill BT, et al. Among authors: riddell d. J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29613789
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.
Brodney MA, Beck EM, Butler CR, Barreiro G, Johnson EF, Riddell D, Parris K, Nolan CE, Fan Y, Atchison K, Gonzales C, Robshaw AE, Doran SD, Bundesmann MW, Buzon L, Dutra J, Henegar K, LaChapelle E, Hou X, Rogers BN, Pandit J, Lira R, Martinez-Alsina L, Mikochik P, Murray JC, Ogilvie K, Price L, Sakya SM, Yu A, Zhang Y, O'Neill BT. Brodney MA, et al. Among authors: riddell d. J Med Chem. 2015 Apr 9;58(7):3223-52. doi: 10.1021/acs.jmedchem.5b00191. Epub 2015 Apr 1. J Med Chem. 2015. PMID: 25781223 Free PMC article.
171 results