메뉴 건너뛰기




Volumn 10, Issue 1, 2015, Pages

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice

Author keywords

Alzheimer's disease; Amyloid ; BACE 1; Inhibitor; Neuroinflammation

Indexed keywords

AMYLOID BETA PROTEIN; BETA SECRETASE INHIBITOR; NB 360; TRITON X 100; UNCLASSIFIED DRUG; AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA-PROTEIN (1-42); ASPARTIC PROTEINASE; BACE1 PROTEIN, MOUSE; HYBRID PROTEIN; NB-360; NERVE PROTEIN; NEUROPROTECTIVE AGENT; PEPTIDE FRAGMENT; PICOLINIC ACID DERIVATIVE; SECRETASE; THIAZINE DERIVATIVE;

EID: 84941317195     PISSN: None     EISSN: 17501326     Source Type: Journal    
DOI: 10.1186/s13024-015-0033-8     Document Type: Article
Times cited : (90)

References (31)
  • 1
    • 84879829589 scopus 로고    scopus 로고
    • Biochemistry of amyloid β-protein and amyloid deposits in Alzheimer disease
    • 3367542 22675658
    • Masters CL, Selkoe DJ. Biochemistry of amyloid β-protein and amyloid deposits in Alzheimer disease. Cold Spring Harb Perspect Med. 2012;2:a006262.
    • (2012) Cold Spring Harb Perspect Med , vol.2 , pp. a006262
    • Masters, C.L.1    Selkoe, D.J.2
  • 2
    • 84892695519 scopus 로고    scopus 로고
    • Two phase 3 trials of bapineuzumab in mild-to-moderate Alzheimer's disease
    • 4159618 1:CAS:528:DC%2BC2cXhs1Ggt7o%3D 24450891
    • Salloway S, Sperling R, Fox NC, Blennow K, Klunk W, Raskind M, et al. Two phase 3 trials of bapineuzumab in mild-to-moderate Alzheimer's disease. N Engl J Med. 2014;370:322-33.
    • (2014) N Engl J Med , vol.370 , pp. 322-333
    • Salloway, S.1    Sperling, R.2    Fox, N.C.3    Blennow, K.4    Klunk, W.5    Raskind, M.6
  • 3
    • 84892748542 scopus 로고    scopus 로고
    • Alzheimer's disease cooperative study steering committee; Solanezumab study group phase 3 trials of solanezumab for mild-to-moderate Alzheimer's disease
    • 1:CAS:528:DC%2BC2cXhs1Ggt70%3D 24450890
    • Doody RS, Thomas RG, Farlow M, Iwatsubo T, Vellas B, Joffe S, et al. Alzheimer's disease cooperative study steering committee; Solanezumab study group phase 3 trials of solanezumab for mild-to-moderate Alzheimer's disease. N Engl J Med. 2014;370:311-21.
    • (2014) N Engl J Med , vol.370 , pp. 311-321
    • Doody, R.S.1    Thomas, R.G.2    Farlow, M.3    Iwatsubo, T.4    Vellas, B.5    Joffe, S.6
  • 4
    • 84921531052 scopus 로고    scopus 로고
    • Anti-inflammatory drugs and risk of Alzheimer's disease: An updated systematic review and meta-analysis
    • Wang J, Tan L, Wang HF, Tan CC, Meng XF, Wang C, et al. Anti-inflammatory drugs and risk of Alzheimer's disease: an updated systematic review and meta-analysis. J Alz Dis. 2015;44:385-96.
    • (2015) J Alz Dis , vol.44 , pp. 385-396
    • Wang, J.1    Tan, L.2    Wang, H.F.3    Tan, C.C.4    Meng, X.F.5    Wang, C.6
  • 5
    • 84875250937 scopus 로고    scopus 로고
    • Amyloid β deposition, neurodegeneration, and cognitive decline in sporadic Alzheimer's disease: A prospective cohort study
    • 1:CAS:528:DC%2BC3sXksFejsrw%3D 23477989
    • Villemagne VL, Burnham S, Bourgeat P, Brown B, Ellis KA, Salvado O, et al. Amyloid β deposition, neurodegeneration, and cognitive decline in sporadic Alzheimer's disease: a prospective cohort study. Lancet Neurol. 2013;12:357-67.
    • (2013) Lancet Neurol , vol.12 , pp. 357-367
    • Villemagne, V.L.1    Burnham, S.2    Bourgeat, P.3    Brown, B.4    Ellis, K.A.5    Salvado, O.6
  • 6
    • 84903190262 scopus 로고    scopus 로고
    • Function, therapeutic potential and cell biology of BACE proteases: Current status and future prospects
    • 4086641 1:CAS:528:DC%2BC2cXhtVSqtL7M 24646365
    • Vassar R, Kuhn PH, Haass C, Kennedy ME, Rajendran L, Wong PC, et al. Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects. J Neurochem. 2014;130:4-28.
    • (2014) J Neurochem , vol.130 , pp. 4-28
    • Vassar, R.1    Kuhn, P.H.2    Haass, C.3    Kennedy, M.E.4    Rajendran, L.5    Wong, P.C.6
  • 7
    • 84894090892 scopus 로고    scopus 로고
    • Targeting the β secretase BACE1 for Alzheimer's disease therapy
    • 4086426 1:CAS:528:DC%2BC2cXis1Cntbo%3D 24556009
    • Yan R, Vassar R. Targeting the β secretase BACE1 for Alzheimer's disease therapy. Lancet Neurol. 2014;13:319-29.
    • (2014) Lancet Neurol , vol.13 , pp. 319-329
    • Yan, R.1    Vassar, R.2
  • 8
    • 84899097978 scopus 로고    scopus 로고
    • The evolution of amidine-based brain penetrant BACE1 inhibitors
    • 1:CAS:528:DC%2BC2cXlvVSqsrY%3D 24704031
    • Oehlrich D, Prokopcova H, Gijsen HJM. The evolution of amidine-based brain penetrant BACE1 inhibitors. Bioorg Med Chem Lett. 2014;24:2033-45.
    • (2014) Bioorg Med Chem Lett , vol.24 , pp. 2033-2045
    • Oehlrich, D.1    Prokopcova, H.2    Gijsen, H.J.M.3
  • 9
    • 84868562686 scopus 로고    scopus 로고
    • Design and Synthesis of β-Site Amyloid predursor Protein Cleaving enzyme (BACE1) inhibitors with in vivo Brain reduction of β-Amyloid Peptides
    • 1:CAS:528:DC%2BC38Xht1OmtL%2FM 22924815
    • Swahn B-M, Kolmodin K, Karlström S, von Berg S, Söderman P, Holenz J, et al. Design and Synthesis of β-Site Amyloid predursor Protein Cleaving enzyme (BACE1) inhibitors with in vivo Brain reduction of β-Amyloid Peptides. J Med Chem. 2012;55:9346-61.
    • (2012) J Med Chem , vol.55 , pp. 9346-9361
    • Swahn, B.-M.1    Kolmodin, K.2    Karlström, S.3    Von Berg, S.4    Söderman, P.5    Holenz, J.6
  • 10
    • 84921521397 scopus 로고    scopus 로고
    • The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans
    • 25609634
    • May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, et al. The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. J Neurosci. 2015;35:1199-210.
    • (2015) J Neurosci , vol.35 , pp. 1199-1210
    • May, P.C.1    Willis, B.A.2    Lowe, S.L.3    Dean, R.A.4    Monk, S.A.5    Cocke, P.J.6
  • 11
    • 81255143061 scopus 로고    scopus 로고
    • Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
    • 1:CAS:528:DC%2BC3MXhsFaksL7F 22090477
    • May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. J Neurosci. 2011;31:16507-16.
    • (2011) J Neurosci , vol.31 , pp. 16507-16516
    • May, P.C.1    Dean, R.A.2    Lowe, S.L.3    Martenyi, F.4    Sheehan, S.M.5    Boggs, L.N.6
  • 12
    • 84930339289 scopus 로고    scopus 로고
    • Retinal toxicity induced by a novel β-secretase inhibitor in the sprague-dawley rat
    • Fielden MR, Werner J, Jamison JA, Coppi A, Hickman D, Dunn RT, et al. Retinal toxicity induced by a novel β-secretase inhibitor in the sprague-dawley rat. Toxicol Pathol. 2015;43:581-92.
    • (2015) Toxicol Pathol , vol.43 , pp. 581-592
    • Fielden, M.R.1    Werner, J.2    Jamison, J.A.3    Coppi, A.4    Hickman, D.5    Dunn, R.T.6
  • 13
    • 0032568397 scopus 로고    scopus 로고
    • Physicochemical high throughput screening: Parallel artificial membrane permeability assay in the description of passive absorption processes
    • 1:CAS:528:DyaK1cXhs12kt70%3D 9544199
    • Kansy M, Senner F, Gubernator K. Physicochemical high throughput screening: parallel artificial membrane permeability assay in the description of passive absorption processes. J Med Chem. 1998;41:1007-10.
    • (1998) J Med Chem , vol.41 , pp. 1007-1010
    • Kansy, M.1    Senner, F.2    Gubernator, K.3
  • 14
    • 38749087222 scopus 로고    scopus 로고
    • In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system
    • 1:CAS:528:DC%2BD1cXht1yktbc%3D 17962372
    • Feng B, Mills JB, Davidson RE, Mireles RJ, Janiszewski JS, Troutman MD, et al. In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos. 2008;36:268-75.
    • (2008) Drug Metab Dispos , vol.36 , pp. 268-275
    • Feng, B.1    Mills, J.B.2    Davidson, R.E.3    Mireles, R.J.4    Janiszewski, J.S.5    Troutman, M.D.6
  • 15
    • 84881245274 scopus 로고    scopus 로고
    • A canine model of human aging and Alzheimer's disease
    • 3937962 1:CAS:528:DC%2BC3sXmtV2rsrs%3D 23528711
    • Head E. A canine model of human aging and Alzheimer's disease. Biochim Biophys Acta. 2013;1832:1384-9.
    • (2013) Biochim Biophys Acta , vol.1832 , pp. 1384-1389
    • Head, E.1
  • 16
    • 84879411945 scopus 로고    scopus 로고
    • Cerebrospinal fluid β-Amyloid turnover in the mouse, dog, monkey and human evaluated by systematic quantitative analyses
    • 1:CAS:528:DC%2BC3sXhtVCgsr3E
    • Lu Y, Barton HA, Leung L, Zhang L, Hajos-Korcsok E, Nolan CE, et al. Cerebrospinal fluid β-Amyloid turnover in the mouse, dog, monkey and human evaluated by systematic quantitative analyses. Neurodeg Dis. 2013;12:36-50.
    • (2013) Neurodeg Dis , vol.12 , pp. 36-50
    • Lu, Y.1    Barton, H.A.2    Leung, L.3    Zhang, L.4    Hajos-Korcsok, E.5    Nolan, C.E.6
  • 17
    • 80052656815 scopus 로고    scopus 로고
    • The Swedish APP mutation alters the effect of genetically reduced BACE1 expression on the APP processing
    • 1:CAS:528:DC%2BC3MXhtlyiurvL 21812781
    • Rabe S, Reichwald J, Ammaturo D, de Strooper B, Saftig P, Neumann U, et al. The Swedish APP mutation alters the effect of genetically reduced BACE1 expression on the APP processing. J Neurochem. 2011;119:231-9.
    • (2011) J Neurochem , vol.119 , pp. 231-239
    • Rabe, S.1    Reichwald, J.2    Ammaturo, D.3    De Strooper, B.4    Saftig, P.5    Neumann, U.6
  • 18
    • 34548847452 scopus 로고    scopus 로고
    • Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice
    • 1:CAS:528:DC%2BD2sXpslGjt74%3D 17616527
    • McConlogue L, Buttini M, Anderson JP, Brigham EF, Chen KS, Freedman SB, et al. Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice. J Biol Chem. 2007;282:26326-34.
    • (2007) J Biol Chem , vol.282 , pp. 26326-26334
    • McConlogue, L.1    Buttini, M.2    Anderson, J.P.3    Brigham, E.F.4    Chen, K.S.5    Freedman, S.B.6
  • 19
    • 76249125728 scopus 로고    scopus 로고
    • β-Secretase inhibitor potency is decreased by aberrant β-cleavage location of the "swedish Mutant" amyloid precursor protein
    • 2804321 1:CAS:528:DC%2BC3cXjsVSntQ%3D%3D 19926793
    • Yamakawa H, Yagishita S, Futai E, Ishiura S. β-Secretase inhibitor potency is decreased by aberrant β-cleavage location of the "Swedish Mutant" amyloid precursor protein. J Biol Chem. 2010;285:1634-42.
    • (2010) J Biol Chem , vol.285 , pp. 1634-1642
    • Yamakawa, H.1    Yagishita, S.2    Futai, E.3    Ishiura, S.4
  • 20
    • 84929378421 scopus 로고    scopus 로고
    • Centrally delivered BACE1 inhibitor activates microglia, and reverses amyloid pathology and cognitive deficit in aged Tg2576 mice
    • 1:CAS:528:DC%2BC2MXosFWnt7g%3D
    • Thakker DR, Sankaranarayanan S, Weatherspoon MR, Harrison J, Pierdomenico M, Heisel JM, et al. Centrally delivered BACE1 inhibitor activates microglia, and reverses amyloid pathology and cognitive deficit in aged Tg2576 mice. J Neurosc. 2015;35:6931-6.
    • (2015) J Neurosc , vol.35 , pp. 6931-6936
    • Thakker, D.R.1    Sankaranarayanan, S.2    Weatherspoon, M.R.3    Harrison, J.4    Pierdomenico, M.5    Heisel, J.M.6
  • 21
    • 54349097757 scopus 로고    scopus 로고
    • Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition
    • 1:CAS:528:DC%2BD1cXhtlWns73E 18687920
    • Abramowski D, Wiederhold KH, Furrer U, Jaton AL, Neuenschwander A, Runser MJ, et al. Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition. J Pharmacol Exp Ther. 2008;327:411-24.
    • (2008) J Pharmacol Exp Ther , vol.327 , pp. 411-424
    • Abramowski, D.1    Wiederhold, K.H.2    Furrer, U.3    Jaton, A.L.4    Neuenschwander, A.5    Runser, M.J.6
  • 22
    • 84906536171 scopus 로고    scopus 로고
    • Combined treatment with a BACE inhibitor and anti-Aβ antibody gantenerumab enhances amyloid reduction in APPLondon mice
    • 4145168 1:CAS:528:DC%2BC2cXhsVynsrvI 25164658
    • Jacobsen H, Ozmen L, Caruso A, Narquizian R, Hilpert H, Jacobsen B, et al. Combined treatment with a BACE inhibitor and anti-Aβ antibody gantenerumab enhances amyloid reduction in APPLondon mice. J Neurosci. 2014;34:11621-30.
    • (2014) J Neurosci , vol.34 , pp. 11621-11630
    • Jacobsen, H.1    Ozmen, L.2    Caruso, A.3    Narquizian, R.4    Hilpert, H.5    Jacobsen, B.6
  • 23
    • 84895727288 scopus 로고    scopus 로고
    • Neuroinflammation in Alzheimer's disease: An understanding of physiology and pathology
    • 1:CAS:528:DC%2BC2cXktVSgtL4%3D 23919560
    • Obulesu M, Jhansilakshimi M. Neuroinflammation in Alzheimer's disease: an understanding of physiology and pathology. Int J Neurosci. 2014;124:227-35.
    • (2014) Int J Neurosci , vol.124 , pp. 227-235
    • Obulesu, M.1    Jhansilakshimi, M.2
  • 25
    • 84938284690 scopus 로고    scopus 로고
    • Neuroinflammation in Alzheimer's disease; A source of heterogeneity and target for personalized therapy
    • Latta CH, Brothers HM, Wilcock DM. Neuroinflammation in Alzheimer's disease; a source of heterogeneity and target for personalized therapy. Neuroscience, ahead of print. doi: 10.1016/j.neuroscience.2014.09.061.
    • Neuroscience, Ahead of Print
    • Latta, C.H.1    Brothers, H.M.2    Wilcock, D.M.3
  • 26
    • 84879544231 scopus 로고    scopus 로고
    • BACE2 processes PMEL to form the melanosome amyloid matrix in pigment cells
    • 3696817 1:CAS:528:DC%2BC3sXhtFejs7rK 23754390
    • Rochin L, Hurbain I, Serneels L, Fort C, Watt B, Leblanc P, et al. BACE2 processes PMEL to form the melanosome amyloid matrix in pigment cells. Proc Natl Acad Sci USA. 2013;110:10658-63.
    • (2013) Proc Natl Acad Sci USA , vol.110 , pp. 10658-10663
    • Rochin, L.1    Hurbain, I.2    Serneels, L.3    Fort, C.4    Watt, B.5    Leblanc, P.6
  • 27
    • 84875655895 scopus 로고    scopus 로고
    • Inflammation in Alzheimer disease -A brief review of the basic science and clinical literature
    • 3253025 22315714
    • Wyss-Coray T, Rogers J. Inflammation in Alzheimer disease-a brief review of the basic science and clinical literature. Cold Spring Harb Perspect Med. 2012;2:a006346.
    • (2012) Cold Spring Harb Perspect Med , vol.2 , pp. a006346
    • Wyss-Coray, T.1    Rogers, J.2
  • 28
    • 0037135111 scopus 로고    scopus 로고
    • The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics
    • Hardy J, Selkoe DJ. The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics. Science. 2002;297:253-6.
    • (2002) Science , vol.297 , pp. 253-256
    • Hardy, J.1    Selkoe, D.J.2
  • 29
    • 0035866672 scopus 로고    scopus 로고
    • High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes
    • 1:CAS:528:DC%2BD3MXosFSltA%3D%3D 11300874
    • Wohnsland F, Faller B. High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. J Med Chem. 2001;44:923-30.
    • (2001) J Med Chem , vol.44 , pp. 923-930
    • Wohnsland, F.1    Faller, B.2
  • 30
    • 34648813134 scopus 로고    scopus 로고
    • High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery
    • 1:CAS:528:DC%2BD2sXps1Kntb8%3D 17725338
    • Wan H, Rehngren M, Giordanetto F, Bergström F, Tunek A. High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. J Med Chem. 2007;50:4606-15.
    • (2007) J Med Chem , vol.50 , pp. 4606-4615
    • Wan, H.1    Rehngren, M.2    Giordanetto, F.3    Bergström, F.4    Tunek, A.5
  • 31
    • 4344648449 scopus 로고    scopus 로고
    • Abeta is targeted to the vasculature in a mouse model of hereditary cerebral hemorrhage with amyloidosis
    • 1:CAS:528:DC%2BD2cXmvFyqurs%3D 15311281
    • Herzig MC, Winkler DT, Burgermeister P, Pfeifer M, Kohler E, Schmidt SD, et al. Abeta is targeted to the vasculature in a mouse model of hereditary cerebral hemorrhage with amyloidosis. Nature Neurosci. 2004;7:954-60.
    • (2004) Nature Neurosci , vol.7 , pp. 954-960
    • Herzig, M.C.1    Winkler, D.T.2    Burgermeister, P.3    Pfeifer, M.4    Kohler, E.5    Schmidt, S.D.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.