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0033518251
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Purification and cloning of amyloid precursor protein fi-secretase from human brain
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Sinha, S.; Anderson, J. P.; Barbour, R.; Basi, G. S.; Caccavello, R.; Davis, D.; Doan, M.; Dovey, H. F.; Frigon, N.; Hong, J.; Croak, K.; Jewett, N.; Keim, P.; Knops, J.; Lieberburg, I.; Power, M.; Tan, H.; Tatsuno, G.; Tung, J.; Schenk, D.; Seubert, P.; Suomensaari, S. M.; Wang, S.; Walker, D.; Zhao, J.; McConologue, L.; John, V. Purification and cloning of amyloid precursor protein fi-secretase from human brain. Nature 1999, 402, 537-540.
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0033518264
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Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity
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Yan, R.; Bienkowski, M. J.; Shuck, M. E.; Miao, H.; Tory, M. C.; Pauley, A. M.; Brashier, J. R.; Stratman, N. C.; Mathews, R. W.; Buhl, A. E.; Carter, D. B.; Tomasselli, A. G.; Parodi, L. A.; Heinrickson, R. L.; Gurney, M. Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity. Nature 1999, 402, 533-536.
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β-secretase cleavage of Alzhemeier's amyloid precursor protein by the transmembrane aspartic protease BACE
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Vassar, R.; Bennett, B. D.; Babu-Khan, S.; Mendiaz, E. A.; Denis, P.; Teplow, D. B.; Ross, S.; Amarante, P.; Loeloff, R.; Luo, Y.; Fisher, S.; Fuller, J.; Edenson, S.; Lile, J.; Jarosinski, M. A.; Biere, A. L.; Curran, E.; Burgess, T.; Louis, J. C.; Collins, F.; Treanor, J.; Rogers, G.; Citron, M. β-Secretase cleavage of Alzhemeier's amyloid precursor protein by the transmembrane aspartic protease BACE. Science 1999, 286, 735-741.
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BACE knockout mice are healthy despite lacking the primary β-secretase activity in brain: Implications for Alzheimer's disease therapeutics
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(a) Roberds, S. L.; Anderson, J.; Basi, G.; Bienkowski, M. J.; Branstetter, D. G.; Chen, K. S.; Freedman, S. B.; Frigon, N. L.; Games, D.; Hu, K.; Johnson-Wood, K.; Kappenman, K. E.; Kawabe, T. T.; Kola, I.; Kuehn, R.; Lee, M.; Liu, W.; Motter, R.; Nichols, N. F.; Power, M.; Robertson, D. W.; Schenk, D.; Schoor, M.; Shopp, G. M.; Shuck, M. E.; Sinha, S.; Svensson, K. A.; Tatsuno, G.; Tintrup, H.; Wijsman, J.; Wright, S.; McConlogue, L. BACE knockout mice are healthy despite lacking the primary β-secretase activity in brain: implications for Alzheimer's disease therapeutics. Hum. Mol. Genet. 2001, 10, 1317-1324.
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Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation
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(b) Luo, Y.; Bolon, B.; Kahn, S.; Bennett, B. D.; Babu-Khan, S.; Denis, P.; Fan, W.; Kha, H.; Zhang, J.; Gong, Y.; Martin, L.; Louis, J.-C.; Yan, Q.; Richards, W. G.; Citron, M.; Vassar, R. Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation. Nat. Neurosci. 2001, 4, 231-232.
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9
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0035112647
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(c) Cai, H.; Wang, Y.; McCarthy, D.; Wen, H.; Borchelt, D. R.; Price, D. L.; Wong, P. C. BACE1 is the major β-secretase for generation of Aβ peptides by neurons. Nat. Neurosci. 2001, 4, 233-234.
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10
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Design of substrate-based inhibitors of human β-secretase
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Tung, J. S.; Davis, D. L.; Anderson, J. P.; Walker, D. E.; Mamo, S.; Jewett, N.; Hom, R. K.; Sinha, S.; Thorsett, E. D.; John, V. Design of substrate-based inhibitors of human β-secretase. J. Med. Chem. 2002, 45, 259-262.
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11
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84986472268
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Synthesis of α-hydroxycarboxylic acids by aeration of lithiated carboxylic acids in tetrahydrofuran solution
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Moersch, G. W.; Zwiesler, M. L. Synthesis of α-hydroxycarboxylic acids by aeration of lithiated carboxylic acids in tetrahydrofuran solution. Synthesis 1971, 12, 647-648.
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Moersch, G.W.1
Zwiesler, M.L.2
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12
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0038523209
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note
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+ (CI) 216.1.
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13
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0024834418
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Synthesis of N-Boc statine and epi-statine
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(a) The 3,5-difluorophenylstatine portion of inhibitor 38 was synthesized from commercial 3,5-difluorophenylalanine (Synthetech) through the procedure outlined in the following. Wuts, P. G. M.; Putt, S. R. Synthesis of N-Boc statine and epi-statine. Synthesis 1989, 951-953. (b) It could be surmised that the active isomer is the R form. However, X-ray crystallography of the isomer for definitive proof of this was not performed.
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(1989)
Synthesis
, pp. 951-953
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Wuts, P.G.M.1
Putt, S.R.2
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14
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0024834418
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note
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(a) The 3,5-difluorophenylstatine portion of inhibitor 38 was synthesized from commercial 3,5-difluorophenylalanine (Synthetech) through the procedure outlined in the following. Wuts, P. G. M.; Putt, S. R. Synthesis of N-Boc statine and epi-statine. Synthesis 1989, 951-953. (b) It could be surmised that the active isomer is the R form. However, X-ray crystallography of the isomer for definitive proof of this was not performed.
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15
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0038184591
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note
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The method for determination of in vitro Aβ reduction in human embryonic kidney cells and the immunoprecipitation protocol using these cells have been previously described in ref 3.
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16
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0027258149
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Cells with a familial Alzheimer's disease mutation produce authentic beta-peptide
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Dovey, H. R.; Suomensaari-Chrysler, S.; Lieberburg, L.; Sinha, S.; Keim, P. S. Cells with a familial Alzheimer's disease mutation produce authentic beta-peptide. NeuroReport 1993, 4, 1039-1042.
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Dovey, H.R.1
Suomensaari-Chrysler, S.2
Lieberburg, L.3
Sinha, S.4
Keim, P.S.5
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