-
1
-
-
79960040736
-
Progress in the development of beta-secretase inhibitors for Alzheimer's disease
-
Albert JS (2009) Progress in the development of beta-secretase inhibitors for Alzheimer's disease. Prog Med Chem 48:133-161.
-
(2009)
Prog Med Chem
, vol.48
, pp. 133-161
-
-
Albert, J.S.1
-
2
-
-
79957452852
-
A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo
-
Atwal JK, Chen Y, Chiu C, Mortensen DL, Meilandt WJ, Liu Y, Heise CE, Hoyte K, Luk W, Lu Y, et al. (2011) A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo. Sci Transl Med 3:84ra43.
-
(2011)
Sci Transl Med
, vol.3
-
-
Atwal, J.K.1
Chen, Y.2
Chiu, C.3
Mortensen, D.L.4
Meilandt, W.J.5
Liu, Y.6
Heise, C.E.7
Hoyte, K.8
Luk, W.9
Lu, Y.10
-
3
-
-
79959342377
-
Aminodihydrothiazine derivatives as BACE inhibitors for the treatment of Alzheimer's disease
-
inventors. Eli Lilly and Company, Audia JE, Mergott DJ, Sheehan SM, and Watson BM, assignees World patent WO2009/134617 A1. 2009 November 5
-
Audia JE, Mergott DJ, Sheehan SM and Watson BM (2009), inventors. Eli Lilly and Company, Audia JE, Mergott DJ, Sheehan SM, and Watson BM, assignees. Aminodihydrothiazine derivatives as BACE inhibitors for the treatment of Alzheimer's disease. World patent WO2009/134617 A1. 2009 November 5.
-
(2009)
-
-
Audia, J.E.1
Mergott, D.J.2
Sheehan, S.M.3
Watson, B.M.4
-
4
-
-
84864143044
-
BACE inhibitors
-
inventors. Eli Lilly and Company, Audia JE, Mergott DJ, Shi C, Vaught GM, Watson BM, and Winneroski LL Jr, assignees. World patent WO2011/005738 A1. 2011 January 13
-
Audia JE, Mergott DJ, Shi C, Vaught GM, Watson BM, and Winneroski LL Jr (2011), inventors. Eli Lilly and Company, Audia JE, Mergott DJ, Shi C, Vaught GM, Watson BM, and Winneroski LL Jr, assignees. BACE inhibitors. World patent WO2011/005738 A1. 2011 January 13.
-
(2011)
-
-
Audia, J.E.1
Mergott, D.J.2
Shi, C.3
Vaught, G.M.4
Watson, B.M.5
Winneroski Jr., L.L.6
-
5
-
-
19944430290
-
Dynamics of β-amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor
-
DOI 10.1124/jpet.104.075408
-
Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, Robertson BJ, et al. (2005) Dynamics of β-amyloid reductions in brain, cerebrospinal fluid, and plasma of β-amyloid precursor protein transgenic mice treated with a γ-secretase inhibitor. J Pharmacol Exp Ther 312:635-643. (Pubitemid 40189561)
-
(2005)
Journal of Pharmacology and Experimental Therapeutics
, vol.312
, Issue.2
, pp. 635-643
-
-
Barten, D.M.1
Guss, V.L.2
Corsa, J.A.3
Loo, A.4
Hansel, S.B.5
Zheng, M.6
Munoz, B.7
Srinivasan, K.8
Wang, B.9
Robertson, B.J.10
Polson, C.T.11
Wang, J.12
Roberts, S.B.13
Hendrick, J.P.14
Anderson, J.J.15
Loy, J.K.16
Denton, R.17
Verdoorn, T.A.18
Smith, D.W.19
Felsenstein, K.M.20
more..
-
6
-
-
33745920161
-
Human amyloid-β synthesis and clearance rates as measured in cerebrospinal fluid in vivo
-
DOI 10.1038/nm1438, PII NM1438
-
Bateman RJ, Munsell LY, Morris JC, Swarm R, Yarasheski KE, and Holtzman DM (2006) Human amyloid-β synthesis and clearance rates as measured in cerebrospinal fluid in vivo. Nat Med 12:856-861. (Pubitemid 44050079)
-
(2006)
Nature Medicine
, vol.12
, Issue.7
, pp. 856-861
-
-
Bateman, R.J.1
Munsell, L.Y.2
Morris, J.C.3
Swarm, R.4
Yarasheski, K.E.5
Holtzman, D.M.6
-
7
-
-
66749084437
-
A γ-secretase inhibitor decreases amyloid-β production in the central nervous system
-
Bateman RJ, Siemers ER, Mawuenyega KG, Wen G, Browning KR, Sigurdson WC, Yarasheski KE, Friedrich SW, Demattos RB, May PC, et al. (2009) A γ-secretase inhibitor decreases amyloid-β production in the central nervous system. Ann Neurol 66:48-54.
-
(2009)
Ann Neurol
, vol.66
, pp. 48-54
-
-
Bateman, R.J.1
Siemers, E.R.2
Mawuenyega, K.G.3
Wen, G.4
Browning, K.R.5
Sigurdson, W.C.6
Yarasheski, K.E.7
Friedrich, S.W.8
Demattos, R.B.9
May, P.C.10
-
8
-
-
77952400306
-
Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β rebound
-
Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, et al. (2010) Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β rebound. J Neurosci 30:6743-6750.
-
(2010)
J Neurosci
, vol.30
, pp. 6743-6750
-
-
Cook, J.J.1
Wildsmith, K.R.2
Gilberto, D.B.3
Holahan, M.A.4
Kinney, G.G.5
Mathers, P.D.6
Michener, M.S.7
Price, E.A.8
Shearman, M.S.9
Simon, A.J.10
-
9
-
-
33847165406
-
Macromolecules involved in production and metabolism of beta-amyl oid at the brain barriers
-
DOI 10.1016/j.brainres.2006.12.022, PII S0006899306035542
-
Crossgrove JS, Smith EL, and Zheng W (2007) Macromolecules involved in production and metabolism of β-amyloid at the brain barriers. Brain Res 1138:187-195. (Pubitemid 46281881)
-
(2007)
Brain Research
, vol.1138
, Issue.1
, pp. 187-195
-
-
Crossgrove, J.S.1
Smith, E.L.2
Zheng, W.3
-
10
-
-
84864143043
-
Demonstrating proof of principle in Alzheimer's disease (AD): The role of CSF 'dynabridging' studies
-
International Society for CNS Clinical Trials and Methodology, Nashville, TN
-
Ereshefsky L, Jhee S, Yen M and Moran S (2008) Demonstrating proof of principle in Alzheimer's disease (AD): the role of CSF 'dynabridging' studies, in Proceedings of the ISCTM 2008 Autumn Conference; 2008 Oct 6-7; Toronto, ON, Canada. International Society for CNS Clinical Trials and Methodology, Nashville, TN.
-
(2008)
Proceedings of the ISCTM 2008 Autumn Conference; 2008 Oct 6-7; Toronto, ON, Canada
-
-
Ereshefsky, L.1
Jhee, S.2
Yen, M.3
Moran, S.4
-
11
-
-
0026597063
-
Alzheimer's disease: The amyloid cascade hypothesis
-
Hardy JA and Higgins GA (1992) Alzheimer's disease: the amyloid cascade hypothesis. Science 256:184-185.
-
(1992)
Science
, vol.256
, pp. 184-185
-
-
Hardy, J.A.1
Higgins, G.A.2
-
12
-
-
79960566232
-
Dynamics of Aβ42 reduction in plasma, CSF and brain of rats treated with the γ-secretase modulator, GSM-10h
-
Hawkins J, Harrison DC, Ahmed S, Davis RP, Chapman T, Marshall I, Smith B, Mead TL, Medhurst A, Giblin GM, et al. (2011) Dynamics of Aβ42 reduction in plasma, CSF and brain of rats treated with the γ-secretase modulator, GSM-10h. Neurodegener Dis 8:455-464.
-
(2011)
Neurodegener Dis
, vol.8
, pp. 455-464
-
-
Hawkins, J.1
Harrison, D.C.2
Ahmed, S.3
Davis, R.P.4
Chapman, T.5
Marshall, I.6
Smith, B.7
Mead, T.L.8
Medhurst, A.9
Giblin, G.M.10
-
13
-
-
50849088334
-
Alternative pathways for production of β-amyloid peptides of Alzheimer's disease
-
Hook V, Schechter I, Demuth HU, and Hook G (2008) Alternative pathways for production of β-amyloid peptides of Alzheimer's disease. Biol Chem 389:993-1006.
-
(2008)
Biol Chem
, vol.389
, pp. 993-1006
-
-
Hook, V.1
Schechter, I.2
Demuth, H.U.3
Hook, G.4
-
14
-
-
79951617234
-
Therapeutic intervention for Alzheimer's disease with γ-secretase inhibitors: Still a viable option?
-
Imbimbo BP, Panza F, Frisardi V, Solfrizzi V, D'Onofrio G, Logroscino G, Seripa D, and Pilotto A (2011) Therapeutic intervention for Alzheimer's disease with γ-secretase inhibitors: still a viable option? Expert Opin Investig Drugs 20:325-341.
-
(2011)
Expert Opin Investig Drugs
, vol.20
, pp. 325-341
-
-
Imbimbo, B.P.1
Panza, F.2
Frisardi, V.3
Solfrizzi, V.4
D'Onofrio, G.5
Logroscino, G.6
Seripa, D.7
Pilotto, A.8
-
15
-
-
0003633755
-
-
Institute of Laboratory Animal Resources 7th ed, Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington, DC
-
Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed, Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington, DC.
-
(1996)
Guide for the Care and Use of Laboratory Animals
-
-
-
16
-
-
80052266213
-
The amyloid cascade hypothesis for Alzheimer's disease: An appraisal for the development of therapeutics
-
Karran E, Mercken M, and De Strooper B (2011) The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics. Nat Rev Drug Discov 10:698-712.
-
(2011)
Nat Rev Drug Discov
, vol.10
, pp. 698-712
-
-
Karran, E.1
Mercken, M.2
De Strooper, B.3
-
17
-
-
70350059834
-
Recent advances in the identification of γ-secretase inhibitors to clinically test the Aβ oligomer hypothesis of Alzheimer's disease
-
Kreft AF, Martone R, and Porte A (2009) Recent advances in the identification of γ-secretase inhibitors to clinically test the Aβ oligomer hypothesis of Alzheimer's disease. J Med Chem 52:6169-6188.
-
(2009)
J Med Chem
, vol.52
, pp. 6169-6188
-
-
Kreft, A.F.1
Martone, R.2
Porte, A.3
-
18
-
-
35148844224
-
Moderate reduction of γ-secretase attenuates amyloid burden and limits mechanism-based liabilities
-
DOI 10.1523/JNEUROSCI.2152-07.2007
-
Li T, Wen H, Brayton C, Laird FM, Ma G, Peng S, Placanica L, Wu TC, Crain BJ, Price DL, et al. (2007) Moderate reduction of γ-secretase attenuates amyloid burden and limits mechanism-based liabilities. J Neurosci 27:10849-10859. (Pubitemid 47535873)
-
(2007)
Journal of Neuroscience
, vol.27
, Issue.40
, pp. 10849-10859
-
-
Li, T.1
Wen, H.2
Brayton, C.3
Laird, F.M.4
Ma, G.5
Peng, S.6
Placanica, L.7
Wu, T.C.8
Crain, B.J.9
Price, D.L.10
Eberhart, C.G.11
Wong, P.C.12
-
19
-
-
81555204259
-
Quantitative pharmacokinetic/ pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors
-
Lu Y, Zhang L, Nolan CE, Becker SL, Atchison K, Robshaw AE, Pustilnik LR, Osgood SM, Miller EH, Stepan AF, et al. (2011) Quantitative pharmacokinetic/ pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors. J Pharmacol Exp Ther 339:922-934.
-
(2011)
J Pharmacol Exp Ther
, vol.339
, pp. 922-934
-
-
Lu, Y.1
Zhang, L.2
Nolan, C.E.3
Becker, S.L.4
Atchison, K.5
Robshaw, A.E.6
Pustilnik, L.R.7
Osgood, S.M.8
Miller, E.H.9
Stepan, A.F.10
-
20
-
-
84879411429
-
Cerebrospinal fluid Aβ turnover in the mouse, dog, monkey, and human evaluated by systematic quantitative analyses
-
in press
-
Lu Y, Barton HA, Leung L, Zhang L, Hajos-Korcsok E, Nolan CE, Liu J, Becker SL, Wood KM, Robshaw AE, et al. (2012) Cerebrospinal fluid Aβ turnover in the mouse, dog, monkey, and human evaluated by systematic quantitative analyses. Neurodegenerative Dis, in press.
-
(2012)
Neurodegenerative Dis
-
-
Lu, Y.1
Barton, H.A.2
Leung, L.3
Zhang, L.4
Hajos-Korcsok, E.5
Nolan, C.E.6
Liu, J.7
Becker, S.L.8
Wood, K.M.9
Robshaw, A.E.10
-
21
-
-
84872602810
-
Central and peripheral pharmacokinetic and pharmacodynamic effects of the beta-site APP cleavage enzyme (BACE1) inhibitor LY2811376 in humans
-
Alzheimer's Association, Chicago, IL
-
Martenyi F, Lowe S, Dean RA, Monk SA, Gonzales C, Friedrich S, May PC, Audia JE, Citron M, LaBell ES, et al. (2010) Central and peripheral pharmacokinetic and pharmacodynamic effects of the beta-site APP cleavage enzyme (BACE1) inhibitor LY2811376 in humans, in Proceedings of the Alzheimer's Association International Conference; 2010 July 10-15; Honolulu, HI. Alzheimer's Association, Chicago, IL.
-
(2010)
Proceedings of the Alzheimer's Association International Conference; 2010 July 10-15; Honolulu, HI
-
-
Martenyi, F.1
Lowe, S.2
Dean, R.A.3
Monk, S.A.4
Gonzales, C.5
Friedrich, S.6
May, P.C.7
Audia, J.E.8
Citron, M.9
LaBell, E.S.10
-
22
-
-
78650678688
-
Decreased clearance of CNS β-amyloid in Alzheimer's disease
-
Mawuenyega KG, Sigurdson W, Ovod V, Munsell L, Kasten T, Morris JC, Yarasheski KE, and Bateman RJ (2010) Decreased clearance of CNS β-amyloid in Alzheimer's disease. Science 330:1774.
-
(2010)
Science
, vol.330
, pp. 1774
-
-
Mawuenyega, K.G.1
Sigurdson, W.2
Ovod, V.3
Munsell, L.4
Kasten, T.5
Morris, J.C.6
Yarasheski, K.E.7
Bateman, R.J.8
-
23
-
-
81255143061
-
Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
-
May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, et al. (2011) Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor J Neurosci 31:16507-16516.
-
(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
Monk, S.A.7
Mathes, B.M.8
Mergott, D.J.9
Watson, B.M.10
-
24
-
-
34548847452
-
Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP transgenic mice
-
DOI 10.1074/jbc.M611687200
-
McConlogue L, Buttini M, Anderson JP, Brigham EF, Chen KS, Freedman SB, Games D, Johnson-Wood K, Lee M, Zeller M, et al. (2007) Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP transgenic mice. J Biol Chem 282:26326-26334. (Pubitemid 47443774)
-
(2007)
Journal of Biological Chemistry
, vol.282
, Issue.36
, 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
Games, D.7
Johnson-Wood, K.8
Lee, M.9
Zeller, M.10
Liu, W.11
Motter, R.12
Sinha, S.13
-
25
-
-
84872596919
-
BMS-708163, a Notch-sparing GSI, decreases central Aβ in rats, dogs, and humans with a therapeutic margin relative to Notch toxicity
-
Kenes International, Geneva, Switzerland
-
Meredith J, Albright CF, Dockens RC, Olson RE, Lentz KA, Wang JS, Denton RR, Pilcher G, Zaczek R, Macor JE, et al. (2011) BMS-708163, a Notch-sparing GSI, decreases central Aβ in rats, dogs, and humans with a therapeutic margin relative to Notch toxicity, in Proceedings of the 10th International Conference on Alzheimer's & Parkinson's Diseases; 2011 Mar 9-13; Barcelona, Spain. Kenes International, Geneva, Switzerland.
-
(2011)
Proceedings of the 10th International Conference on Alzheimer's & Parkinson's Diseases; 2011 Mar 9-13; Barcelona, Spain
-
-
Meredith, J.1
Albright, C.F.2
Dockens, R.C.3
Olson, R.E.4
Lentz, K.A.5
Wang, J.S.6
Denton, R.R.7
Pilcher, G.8
Zaczek, R.9
Macor, J.E.10
-
26
-
-
79952904028
-
Novel γ-secretase modulators: A review of patents from 2008 to 2010
-
Pettersson M, Kauffman GW, am Ende CW, Patel NC, Stiff C, Tran TP, and Johnson DS (2011) Novel γ-secretase modulators: a review of patents from 2008 to 2010. Expert Opin Ther Pat 21:205-226.
-
(2011)
Expert Opin Ther Pat
, vol.21
, pp. 205-226
-
-
Pettersson, M.1
Kauffman, G.W.2
Ende, C.W.3
Patel, N.C.4
Stiff, C.5
Tran, T.P.6
Johnson, D.S.7
-
27
-
-
59149083352
-
First demonstration of cerebrospinal fluid and plasma Aβ lowering with oral administration of a β-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates
-
Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, et al. (2009) First demonstration of cerebrospinal fluid and plasma Aβ lowering with oral administration of a β-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. J Pharmacol Exp Ther 328:131-140.
-
(2009)
J Pharmacol Exp Ther
, vol.328
, pp. 131-140
-
-
Sankaranarayanan, S.1
Holahan, M.A.2
Colussi, D.3
Crouthamel, M.C.4
Devanarayan, V.5
Ellis, J.6
Espeseth, A.7
Gates, A.T.8
Graham, S.L.9
Gregro, A.R.10
-
28
-
-
16044373524
-
Secreted amyloid β-protein similar to that in the senile plaques of Alzheimer's disease is increased in vivo by the presenilin 1 and 2 and APP mutations linked to familial Alzheimer's disease
-
DOI 10.1038/nm0896-864
-
Scheuner D, Eckman C, Jensen M, Song X, Citron M, Suzuki N, Bird TD, Hardy J, Hutton M, Kukull W, et al. (1996) Secreted amyloid β-protein similar to that in the senile plaques of Alzheimer's disease is increased in vivo by the presenilin 1 and 2 and APP mutations linked to familial Alzheimer's disease. Nat Med 2:864-870. (Pubitemid 26296755)
-
(1996)
Nature Medicine
, vol.2
, Issue.8
, pp. 864-870
-
-
Scheuner, D.1
Eckman, C.2
Jensen, M.3
Song, X.4
Citron, M.5
Suzuki, N.6
Bird, T.D.7
Hardy, J.8
Hutton, M.9
Kukull, W.10
Larson, E.11
Levy-Lahad, E.12
Viitanen, M.13
Peskind, E.14
Poorkaj, P.15
Schellenberg, G.16
Tanzi, R.17
Wasco, W.18
Lannfelt, L.19
Selkoe, D.20
Younkin, S.21
more..
-
29
-
-
37349072443
-
Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-β after inhibition of γ-secretase
-
DOI 10.1097/WNF.0b013e31805b7660, PII 0000282620071100000001
-
Siemers ER, Dean RA, Friedrich S, Ferguson-Sells L, Gonzales C, Farlow MR, and May PC (2007) Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase. Clin Neuropharmacol 30:317-325. (Pubitemid 350307310)
-
(2007)
Clinical Neuropharmacology
, vol.30
, Issue.6
, pp. 317-325
-
-
Siemers, E.R.1
Dean, R.A.2
Friedrich, S.3
Ferguson-Sells, L.4
Gonzales, C.5
Farlow, M.R.6
May, P.C.7
-
31
-
-
84872615423
-
Pharmacokinetic/pharmacodynamic analysis of beta-amyloid response following modulation of the gamma secretase enzyme
-
Alzheimer's Association, Chicago, IL
-
Wang EQ, Tseng E, Lu Y, Becker SL, Hudson E, Zhang L, Wood KM, Bales KR, Marconi M, et al. (2010) Pharmacokinetic/pharmacodynamic analysis of beta-amyloid response following modulation of the gamma secretase enzyme, in Proceedings of the Alzheimer's Association International Conference; 2010 July 10-15; Honolulu, HI. Alzheimer's Association, Chicago, IL.
-
(2010)
Proceedings of the Alzheimer's Association International Conference; 2010 July 10-15; Honolulu, HI
-
-
Wang, E.Q.1
Tseng, E.2
Lu, Y.3
Becker, S.L.4
Hudson, E.5
Zhang, L.6
Wood, K.M.7
Bales, K.R.8
Marconi, M.9
|