-
1
-
-
0034951751
-
Alzheimer's disease: Insights from epidemiology
-
McDowell I: Alzheimer's disease: Insights from epidemiology. Aging (2001) 13:143-162.
-
(2001)
Aging
, vol.13
, pp. 143-162
-
-
McDowell, I.1
-
2
-
-
0035075379
-
Experimental approaches and drugs in development for the treatment of dementia
-
Emre M, Qizilbash N: Experimental approaches and drugs in development for the treatment of dementia. Expert Opin Investig Drugs (2001) 10:607-617. This review summarizes the therapeutic approaches currently under investigation for the treatment of AD.
-
(2001)
Expert Opin Investig Drugs
, vol.10
, pp. 607-617
-
-
Emre, M.1
Qizilbash, N.2
-
3
-
-
0035303563
-
Muscarinic agonists and antagonists in the treatment of Alzheimer's disease
-
Greenlee W, Clader J, Asberom T, McCombie S, Ford J, Guzik H, Kozlowski J, Li S, Liu C, Lowe D, Vice S, Zhao H, Zhou G, Billard W, Binch H, Crosby R, Duffy R, Lachowicz J, Coffin V, Watkins R, Ruperto V, Strader C, Taylor L, Cox K: Muscarinic agonists and antagonists in the treatment of Alzheimer's disease. Farmaco (2001) 56:247-250.
-
(2001)
Farmaco
, vol.56
, pp. 247-250
-
-
Greenlee, W.1
Clader, J.2
Asberom, T.3
McCombie, S.4
Ford, J.5
Guzik, H.6
Kozlowski, J.7
Li, S.8
Liu, C.9
Lowe, D.10
Vice, S.11
Zhao, H.12
Zhou, G.13
Billard, W.14
Binch, H.15
Crosby, R.16
Duffy, R.17
Lachowicz, J.18
Coffin, V.19
Watkins, R.20
Ruperto, V.21
Strader, C.22
Taylor, L.23
Cox, K.24
more..
-
4
-
-
0035424943
-
Therapeutic opportunities from muscarinic receptor research
-
Eglen RM, Choppin A, Watson N: Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci (2001) 22:409-414.
-
(2001)
Trends Pharmacol Sci
, vol.22
, pp. 409-414
-
-
Eglen, R.M.1
Choppin, A.2
Watson, N.3
-
5
-
-
0032815284
-
Recent advances in cholinergic drugs for Alzheimer's disease
-
Clader JW: Recent advances in cholinergic drugs for Alzheimer's disease. Curr Opin Drug Discovery Dev (1999) 2:311-320.
-
(1999)
Curr Opin Drug Discovery Dev
, vol.2
, pp. 311-320
-
-
Clader, J.W.1
-
6
-
-
0034701238
-
The origins of Alzheimer disease: A is for amyloid
-
Selkoe DJ: The origins of Alzheimer disease: A is for amyloid. J Am Med Assoc (2000) 283:1615-1617. This article summarizes the evidence in support of the amyloid hypothesis.
-
(2000)
J Am Med Assoc
, vol.283
, pp. 1615-1617
-
-
Selkoe, D.J.1
-
7
-
-
0038117796
-
Correlation between elevated levels of amyloid β-peptide in the brain and cognitive decline
-
Naslund J, Haroutunian V, Mohs R, Davis KL, Davies P, Greengard P, Buxbaum JD: Correlation between elevated levels of amyloid β-peptide in the brain and cognitive decline. J Am Med Assoc (2000) 283:1571-1577. One of the most emphatic studies to date to suggest that high levels of Aβ contribute to AD onset.
-
(2000)
J Am Med Assoc
, vol.283
, pp. 1571-1577
-
-
Naslund, J.1
Haroutunian, V.2
Mohs, R.3
Davis, K.L.4
Davies, P.5
Greengard, P.6
Buxbaum, J.D.7
-
8
-
-
0035866060
-
β-amyloid stimulation of microglia and monocytes results in TNFα-dependent expression of inducible nitric oxide synthase and neuronal apoptosis
-
Combs CK, Karlo JC, Kao S-C, Landreth GE: β-Amyloid stimulation of microglia and monocytes results in TNFα-dependent expression of inducible nitric oxide synthase and neuronal apoptosis. J Neurosci (2001) 21:1179-1188.
-
(2001)
J Neurosci
, vol.21
, pp. 1179-1188
-
-
Combs, C.K.1
Karlo, J.C.2
Kao, S.-C.3
Landreth, G.E.4
-
9
-
-
0035072746
-
β-amyloid therapies in Alzheimer's disease
-
Jhee S, Shiovitz T, Crawford AW, Cutler NR: β-Amyloid therapies in Alzheimer's disease. Expert Opin Investig Drugs (2001) 10:593-605. This review summarizes the current approaches aimed at reducing Aβ secretion, and covers other strategies such as immunization therapy.
-
(2001)
Expert Opin Investig Drugs
, vol.10
, pp. 593-605
-
-
Jhee, S.1
Shiovitz, T.2
Crawford, A.W.3
Cutler, N.R.4
-
10
-
-
0032930444
-
Inhibition of β-amyloid formation as a therapeutic strategy
-
Moore CD, Wolfe MS: Inhibition of β-amyloid formation as a therapeutic strategy. Exp Opin Ther Pat (1999) 9:135-146.
-
(1999)
Exp Opin Ther Pat
, vol.9
, pp. 135-146
-
-
Moore, C.D.1
Wolfe, M.S.2
-
11
-
-
0033536163
-
Immunization with amyloid-β attenuates Alzheimer-disease-like pathology in the PDAPP mouse
-
Schenk D, Barbour R, Dunn W, Gordon G, Grajeda H, Guido T, Hu K, Huang J, Johnson-Wood K, Khan K, Kholodenko D, Lee M, Liao Z, Lieberburg I, Motter R, Mutter L, Soriano F, Shopp G, Vasquez N, Vandevert C, Walker S, Wogulis M, Yednock T, Games D, Seubert P: Immunization with amyloid-β attenuates Alzheimer-disease-like pathology in the PDAPP mouse. Nature (1999) 400:173-177. First report on the efficacy of immunization therapy in preventing plaque formation and reducing AD behavioral impairments in PDAPP transgenic mice.
-
(1999)
Nature
, vol.400
, pp. 173-177
-
-
Schenk, D.1
Barbour, R.2
Dunn, W.3
Gordon, G.4
Grajeda, H.5
Guido, T.6
Hu, K.7
Huang, J.8
Johnson-Wood, K.9
Khan, K.10
Kholodenko, D.11
Lee, M.12
Liao, Z.13
Lieberburg, I.14
Motter, R.15
Mutter, L.16
Soriano, F.17
Shopp, G.18
Vasquez, N.19
Vandevert, C.20
Walker, S.21
Wogulis, M.22
Yednock, T.23
Games, D.24
Seubert, P.25
more..
-
12
-
-
0000676441
-
Companies halt first Alzheimer vaccine trial
-
Steinberg D: Companies halt first Alzheimer vaccine trial. The Scientist (2002) 16:22-23.
-
(2002)
The Scientist
, vol.16
, pp. 22-23
-
-
Steinberg, D.1
-
13
-
-
0035411641
-
β-amyloid aggregation inhibitors for the treatment of Alzheimer's disease: Dream or reality?
-
Talaga P: β-Amyloid aggregation inhibitors for the treatment of Alzheimer's disease: Dream or reality? Mini Rev Med Chem (2001) 1:175-186.
-
(2001)
Mini Rev Med Chem
, vol.1
, pp. 175-186
-
-
Talaga, P.1
-
14
-
-
0035968743
-
Aspirin and nonsteroidal anti-inflammatory drugs inhibit amyloid-β aggregation
-
Thomas T, Nadackal TG, Thomas K: Aspirin and nonsteroidal anti-inflammatory drugs inhibit amyloid-β aggregation. Neuroreport (2001) 12:3263-3267.
-
(2001)
Neuroreport
, vol.12
, pp. 3263-3267
-
-
Thomas, T.1
Nadackal, T.G.2
Thomas, K.3
-
15
-
-
0035927426
-
Secretase targets for Alzheimer's disease: Identification and therapeutic potential
-
Wolfe MS: Secretase targets for Alzheimer's disease: Identification and therapeutic potential. J Med Chem (2001) 44:2039-2060. A comprehensive review on AD and APP secretases that details the pharmacological characterization of each β- and γ-secretase and the elements supporting the hypothesis that presenilin is γ-secretase (an aspartyl protease), as well as proposing a model for the γ-secretase active site. This review also covers some of the current inhibitors under investigation.
-
(2001)
J Med Chem
, vol.44
, pp. 2039-2060
-
-
Wolfe, M.S.1
-
16
-
-
0034915965
-
Progress towards testing the amyloid hypothesis: Inhibitors of APP processing
-
Olson RE, Copeland RA, Seiffert D: Progress towards testing the amyloid hypothesis: Inhibitors of APP processing. Curr Opin Drug Discovery Dev (2001) 4:390-401. Recent review on APP secretases and β- and γ-secretase inhibitors.
-
(2001)
Curr Opin Drug Discovery Dev
, vol.4
, pp. 390-401
-
-
Olson, R.E.1
Copeland, R.A.2
Seiffert, D.3
-
17
-
-
0035424693
-
Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme
-
Slack BE, Ma LK, Seah CC: Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme. Biochem J (2001) 357:787-794.
-
(2001)
Biochem J
, vol.357
, pp. 787-794
-
-
Slack, B.E.1
Ma, L.K.2
Seah, C.C.3
-
18
-
-
14444272986
-
Evidence that tumor necrosis factor-α converting enzyme is involved in regulated α-secretase cleavage of the Alzheimer amyloid protein precursor
-
Buxbaum JD, Liu K-N, Luo Y, Slack JL, Stocking KL, Peschon JJ, Johnson RS, Castner BJ, Cerretti DP, Black RA: Evidence that tumor necrosis factor-α converting enzyme is involved in regulated α-secretase cleavage of the Alzheimer amyloid protein precursor. J Biol Chem (1998) 273:27765-27767.
-
(1998)
J Biol Chem
, vol.273
, pp. 27765-27767
-
-
Buxbaum, J.D.1
Liu, K.-N.2
Luo, Y.3
Slack, J.L.4
Stocking, K.L.5
Peschon, J.J.6
Johnson, R.S.7
Castner, B.J.8
Cerretti, D.P.9
Black, R.A.10
-
19
-
-
0035089318
-
Constitutive α-secretase cleavage of the β-amyloid precursor protein in the furin-deficient LoVo cell line: Involvement of the pro-hormone convertase 7 and the disintegrin metalloprotease ADAM10
-
Lopez-Perez E, Zhang Y, Frank SJ, Creemers J, Seidah N, Checler F: Constitutive α-secretase cleavage of the β-amyloid precursor protein in the furin-deficient LoVo cell line: Involvement of the pro-hormone convertase 7 and the disintegrin metalloprotease ADAM10. J Neurochem (2001) 76:1532-1539.
-
(2001)
J Neurochem
, vol.76
, pp. 1532-1539
-
-
Lopez-Perez, E.1
Zhang, Y.2
Frank, S.J.3
Creemers, J.4
Seidah, N.5
Checler, F.6
-
20
-
-
0035826909
-
Low cholesterol stimulates the nonamyloidogenic pathway by its effect on the α-secretase ADAM 10
-
Kojro E, Gimpl G, Lammich S, Marz W, Fahrenholz F: Low cholesterol stimulates the nonamyloidogenic pathway by its effect on the α-secretase ADAM 10. Proc Natl Acad Sci USA (2001) 98:5815-5820.
-
(2001)
Proc Natl Acad Sci USA
, vol.98
, pp. 5815-5820
-
-
Kojro, E.1
Gimpl, G.2
Lammich, S.3
Marz, W.4
Fahrenholz, F.5
-
21
-
-
0033772113
-
Decreased prevalence of Alzheimer's disease associated with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors
-
Wolozin B, Kellman W, Ruosseau P, Celesia GC, Siegel G: Decreased prevalence of Alzheimer's disease associated with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Arch Neurol (2000) 57:1439-1443.
-
(2000)
Arch Neurol
, vol.57
, pp. 1439-1443
-
-
Wolozin, B.1
Kellman, W.2
Ruosseau, P.3
Celesia, G.C.4
Siegel, G.5
-
22
-
-
0035159756
-
The β-secretase, BACE: A prime drug target for Alzheimer's disease
-
Vassar R: The β-secretase, BACE: A prime drug target for Alzheimer's disease. J Mol Neurosci (2001) 17:157-170. A comprehensive review on the characterization of BACE1 and BACE2 secretases, including a summary of knockout studies that suggest a therapeutic potential for BACE1 inhibitors.
-
(2001)
J Mol Neurosci
, vol.17
, pp. 157-170
-
-
Vassar, R.1
-
23
-
-
0034613320
-
Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor
-
Hong L, Koelsch G, Lin X, Wu S, Terzyan S, Ghosh AK, Zhang XC, Tang J: Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor. Science (2000) 290:150-153. Reports the high-resolution structure of the protease domain of BACE complexed with a nanomolar potency inhibitor.
-
(2000)
Science
, vol.290
, pp. 150-153
-
-
Hong, L.1
Koelsch, G.2
Lin, X.3
Wu, S.4
Terzyan, S.5
Ghosh, A.K.6
Zhang, X.C.7
Tang, J.8
-
24
-
-
0035116273
-
Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation
-
Luo Y, Bolon B, Kahn S, Bennett BD, Babu-Khan S, Denis P, Fan W, Kha H, Zhang J, Gong Y, Martin L, Louis J-C, Yan Q, Richards WG, 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.
-
(2001)
Nat Neurosci
, vol.4
, pp. 231-232
-
-
Luo, Y.1
Bolon, B.2
Kahn, S.3
Bennett, B.D.4
Babu-Khan, S.5
Denis, P.6
Fan, W.7
Kha, H.8
Zhang, J.9
Gong, Y.10
Martin, L.11
Louis, J.-C.12
Yan, Q.13
Richards, W.G.14
Citron, M.15
Vassar, R.16
-
25
-
-
0037122704
-
Design of substrate-based inhibitors of human β-secretase
-
Tung JS, Davis DL, Anderson JP, Walker DE, Mamo S, Jewett N, Hom RK, Sinha S, Thorsett ED, John, V: Design of substrate-based inhibitors of human β-secretase. J Med Chem (2002) 45:259-262.
-
(2002)
J Med Chem
, vol.45
, pp. 259-262
-
-
Tung, J.S.1
Davis, D.L.2
Anderson, J.P.3
Walker, D.E.4
Mamo, S.5
Jewett, N.6
Hom, R.K.7
Sinha, S.8
Thorsett, E.D.9
John, V.10
-
26
-
-
0034718209
-
Presenilin structure, function and role in Alzheimer disease
-
Fraser PE, Yang D-S, Yu G, Levesque L, Nishimura M, Arawaka S, Serpell LC, Rogaeva E, St George-Hyslop P: Presenilin structure, function and role in Alzheimer disease. Biochim Biophys Acta (2000) 1502:1-15. Includes a comprehensive list of presenilin mutations associated with FAD early onset.
-
(2000)
Biochim Biophys Acta
, vol.1502
, pp. 1-15
-
-
Fraser, P.E.1
Yang, D.-S.2
Yu, G.3
Levesque, L.4
Nishimura, M.5
Arawaka, S.6
Serpell, L.C.7
Rogaeva, E.8
St. George-Hyslop, P.9
-
27
-
-
0037022644
-
Activity-dependent isolation of the presenilin-γ-secretase complex reveals nicastrin and a γ substrate
-
Esler WP, Kimberly WT, Ostaszewski BL, Ye W, Diehl TS, Selkoe DJ, Wolfe MS: Activity-dependent isolation of the presenilin-γ-secretase complex reveals nicastrin and a γ substrate. Proc Natl Acad Sci USA (2002) 99:2720-2725.
-
(2002)
Proc Natl Acad Sci USA
, vol.99
, pp. 2720-2725
-
-
Esler, W.P.1
Kimberly, W.T.2
Ostaszewski, B.L.3
Ye, W.4
Diehl, T.S.5
Selkoe, D.J.6
Wolfe, M.S.7
-
28
-
-
0035923750
-
Interaction with telencephalin and the amyloid precursor protein predicts a ring structure for presenilins
-
Annaert WG, Esselens C, Baert V, Boeve C, Snellings G, Cupers P, Craessaerts K, De Strooper B: Interaction with telencephalin and the amyloid precursor protein predicts a ring structure for presenilins. Neuron (2001) 32:579-589. Propose a ring-like structure for the PS1 binding pocket in which binding and cleavage of C99 constitute two separate events.
-
(2001)
Neuron
, vol.32
, pp. 579-589
-
-
Annaert, W.G.1
Esselens, C.2
Baert, V.3
Boeve, C.4
Snellings, G.5
Cupers, P.6
Craessaerts, K.7
De Strooper, B.8
-
29
-
-
0034705204
-
In search of γ-secretase: Presenilin at the cutting edge
-
Selkoe DJ, Wolfe MS: In search of γ-secretase: Presenilin at the cutting edge. Proc Natl Acad Sci USA (2000) 97:5690-5692. This review summarizes the evidence connecting presenilin to γ-secretase activity.
-
(2000)
Proc Natl Acad Sci USA
, vol.97
, pp. 5690-5692
-
-
Selkoe, D.J.1
Wolfe, M.S.2
-
30
-
-
0033775709
-
Total inactivation of γ-secretase activity in presenilin-deficient embryonic stem cells
-
Herreman A, Semeels L, Annaert W, Collen D, Schoonjans L, De Strooper B: Total inactivation of γ-secretase activity in presenilin-deficient embryonic stem cells. Nat Cell Biol (2000) 2:461-462.
-
(2000)
Nat Cell Biol
, vol.2
, pp. 461-462
-
-
Herreman, A.1
Semeels, L.2
Annaert, W.3
Collen, D.4
Schoonjans, L.5
De Strooper, B.6
-
31
-
-
0033779635
-
Presenilins are required for γ-secretase cleavage of β-APP and transmembrane cleavage of Notch1
-
Zhang Z, Nadeau P, Song W, Donoviel D, Yuan M, Bernstein A, Yankner BA: Presenilins are required for γ-secretase cleavage of β-APP and transmembrane cleavage of Notch1. Nat Cell Biol (2000) 2:463-465.
-
(2000)
Nat Cell Biol
, vol.2
, pp. 463-465
-
-
Zhang, Z.1
Nadeau, P.2
Song, W.3
Donoviel, D.4
Yuan, M.5
Bernstein, A.6
Yankner, B.A.7
-
32
-
-
0035942322
-
Biochemical characterization of the γ-secretase activity that produces β-amyloid peptides
-
Zhang L, Song L, Terracina G, Liu Y, Pramanik B, Parker E: Biochemical characterization of the γ-secretase activity that produces β-amyloid peptides. Biochemistry (2001) 40:5049-5055. Description of a cell-free γ-secretase assay.
-
(2001)
Biochemistry
, vol.40
, pp. 5049-5055
-
-
Zhang, L.1
Song, L.2
Terracina, G.3
Liu, Y.4
Pramanik, B.5
Parker, E.6
-
33
-
-
0034621824
-
Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1
-
Li Y-M, Xu M, Lai M-T, Huang Q, Castro JL, DiMuzio-Mower J, Harrison T, Lellis C, Nadin A, Neduvelil JG, Register RB, Sardana MK, Shearman MS, Smith AL, Shi X-P, Yin K-C, Shafer JA, Gardell SJ: Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1. Nature (2000) 405:689-694. Provides evidence that an ethylenehydroxy γ-secretase inhibitor binds directly to PS1.
-
(2000)
Nature
, vol.405
, pp. 689-694
-
-
Li, Y.-M.1
Xu, M.2
Lai, M.-T.3
Huang, Q.4
Castro, J.L.5
DiMuzio-Mower, J.6
Harrison, T.7
Lellis, C.8
Nadin, A.9
Neduvelil, J.G.10
Register, R.B.11
Sardana, M.K.12
Shearman, M.S.13
Smith, A.L.14
Shi, X.-P.15
Yin, K.-C.16
Shafer, J.A.17
Gardell, S.J.18
-
34
-
-
0033780472
-
Transition-state analogue inhibitors of γ-secretase bind directly to presenilin-1
-
Esler WP, Kimberly WT, Ostaszewski BL, Diehl TS, Moore CL, Tsai J-Y, Rahmati T, Xia W, Selkoe DJ, Wolfe MS: Transition-state analogue inhibitors of γ-secretase bind directly to presenilin-1. Nat Cell Biol (2000) 2:428-434. Provides evidence that a difluoroethylenealcohol γ-secretase inhibitor binds directly to PS1.
-
(2000)
Nat Cell Biol
, vol.2
, pp. 428-434
-
-
Esler, W.P.1
Kimberly, W.T.2
Ostaszewski, B.L.3
Diehl, T.S.4
Moore, C.L.5
Tsai, J.-Y.6
Rahmati, T.7
Xia, W.8
Selkoe, D.J.9
Wolfe, M.S.10
-
35
-
-
0034602419
-
Presenilin-1 and -2 are molecular targets for γ-secretase inhibitors
-
Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R: Presenilin-1 and -2 are molecular targets for γ-secretase inhibitors. J Biol Chem (2000) 275:34086-34091. Provides evidence that a small molecule γ-secretase inhibitor binds directly to PS1 and PS2. Describes the γ-secretase inhibitory potency of proprietary compounds from Elan and DuPont as measured in a cell-free assay.
-
(2000)
J Biol Chem
, vol.275
, pp. 34086-34091
-
-
Seiffert, D.1
Bradley, J.D.2
Rominger, C.M.3
Rominger, D.H.4
Yang, F.5
Meredith J.E., Jr.6
Wang, Q.7
Roach, A.H.8
Thompson, L.A.9
Spitz, S.M.10
Higaki, J.N.11
Prakash, S.R.12
Combs, A.P.13
Copeland, R.A.14
Arneric, S.P.15
Hartig, P.R.16
Robertson, D.W.17
Cordell, B.18
Stern, A.M.19
Olson, R.E.20
Zaczek, R.21
more..
-
36
-
-
0034618705
-
Difluoro ketone peptidomimeties suggest a large S1 pocket for Alzheimer's γ-secretase: Implication for inhibitor design
-
Moore CL, Leatherwood DD, Diehl TS, Selkoe DJ, Woffe MS: Difluoro ketone peptidomimeties suggest a large S1 pocket for Alzheimer's γ-secretase: Implication for inhibitor design. J Med Chem (2000) 43:3434-3442.
-
(2000)
J Med Chem
, vol.43
, pp. 3434-3442
-
-
Moore, C.L.1
Leatherwood, D.D.2
Diehl, T.S.3
Selkoe, D.J.4
Woffe, M.S.5
-
37
-
-
0034254585
-
L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid β-protein precursor γ-secretase activity
-
Shearman MS, Beher D, Clarke EE, Lewis HD, Harrison T, Hunt P, Nadin A, Smith AL, Stevenson G, Castro JL: L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid β-protein precursor γ-secretase activity. Biochemistry (2000) 39:8698-8704.
-
(2000)
Biochemistry
, vol.39
, pp. 8698-8704
-
-
Shearman, M.S.1
Beher, D.2
Clarke, E.E.3
Lewis, H.D.4
Harrison, T.5
Hunt, P.6
Nadin, A.7
Smith, A.L.8
Stevenson, G.9
Castro, J.L.10
-
38
-
-
0033535553
-
Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and γ-secretase activity
-
Wolfe MS, Xia W, Ostaszewski BL, Diehl TS, Kimberly WT, Selkoe DJ: Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and γ-secretase activity. Nature (1999) 398:513-517. One of the first reports to suggest that presenilin-1 is an essential cofactor for γ-secretase activity or is itself γ-secretase, a transmembrane aspartyl protease.
-
(1999)
Nature
, vol.398
, pp. 513-517
-
-
Wolfe, M.S.1
Xia, W.2
Ostaszewski, B.L.3
Diehl, T.S.4
Kimberly, W.T.5
Selkoe, D.J.6
-
39
-
-
0000792598
-
The transmembrane aspartates in presenilin 1 and 2 are obligatory for γ-secretase activity and amyloid β-protein generation
-
Kimberly WT, Xia W, Rahmati T, Wolfe MS, Selkoe DJ: The transmembrane aspartates in presenilin 1 and 2 are obligatory for γ-secretase activity and amyloid β-protein generation. J Biol Chem (2000) 275:3173-3178.
-
(2000)
J Biol Chem
, vol.275
, pp. 3173-3178
-
-
Kimberly, W.T.1
Xia, W.2
Rahmati, T.3
Wolfe, M.S.4
Selkoe, D.J.5
-
40
-
-
0035834145
-
PS1 N- and C-terminal fragments form a complex that functions in APP processing and Notch signaling
-
Levitan D, Lee J, Song L, Manning R, Wong G, Parker E, Zhang L: PS1 N- and C-terminal fragments form a complex that functions in APP processing and Notch signaling. Proc Natl Acad Sci USA (2001) 98:12186-12190.
-
(2001)
Proc Natl Acad Sci USA
, vol.98
, pp. 12186-12190
-
-
Levitan, D.1
Lee, J.2
Song, L.3
Manning, R.4
Wong, G.5
Parker, E.6
Zhang, L.7
-
41
-
-
0033783140
-
Presenilin-1 differentially facilitates endoproteolysis of the β-amyloid precursor protein and Notch
-
Capell A, Steiner H, Romig H, Keck S, Baader M, Grim MG, Baumeister R, Haass C: Presenilin-1 differentially facilitates endoproteolysis of the β-amyloid precursor protein and Notch. Nat Cell Biol (2000) 2:205-211.
-
(2000)
Nat Cell Biol
, vol.2
, pp. 205-211
-
-
Capell, A.1
Steiner, H.2
Romig, H.3
Keck, S.4
Baader, M.5
Grim, M.G.6
Baumeister, R.7
Haass, C.8
-
42
-
-
0033575224
-
Rank-order of potencies for inhibition of the secretion of Aβ40 and Aβ42 suggests that both are generated by a single γ-secretase
-
Durkins JT, Murphy S, Husten EJ, Trusko SP, Savage MJ, Rotella DP, Greeberg BD, Siman R: Rank-order of potencies for inhibition of the secretion of Aβ40 and Aβ42 suggests that both are generated by a single γ-secretase. J Biol Chem (1999) 274:20499-20504.
-
(1999)
J Biol Chem
, vol.274
, pp. 20499-20504
-
-
Durkins, J.T.1
Murphy, S.2
Husten, E.J.3
Trusko, S.P.4
Savage, M.J.5
Rotella, D.P.6
Greeberg, B.D.7
Siman, R.8
-
43
-
-
0033598365
-
A combinatorial approach to the identification of dipeptide aldehyde inhibitors of β-amyloid production
-
Higaki JN, Chakravarty S, Bryant CM, Cowart LR, Harden P, Scardina JM, Mavunkel B, Luedtke GR, Cordell B: A combinatorial approach to the identification of dipeptide aldehyde inhibitors of β-amyloid production. J Med Chem (1999) 42:3889-3898.
-
(1999)
J Med Chem
, vol.42
, pp. 3889-3898
-
-
Higaki, J.N.1
Chakravarty, S.2
Bryant, C.M.3
Cowart, L.R.4
Harden, P.5
Scardina, J.M.6
Mavunkel, B.7
Luedtke, G.R.8
Cordell, B.9
-
44
-
-
0037066084
-
Endoproteolysis of presenilin in vitro: Inhibition by γ-secretase inhibitors
-
Campbell WA, Iskandar M-K, Reed MLO, Xia W: Endoproteolysis of presenilin in vitro: Inhibition by γ-secretase inhibitors. Biochemistry (2002) 41:3372-3379. This report leads to the suggestion that presenilinase activity could be regulated separately from γ-secretase activity.
-
(2002)
Biochemistry
, vol.41
, pp. 3372-3379
-
-
Campbell, W.A.1
Iskandar, M.-K.2
Reed, M.L.O.3
Xia, W.4
-
45
-
-
0035977071
-
Pharmacological knock-down of the presenilin 1 heterodimer by a novel γ-secretase inhibitor: Implications for presenilin biology
-
Beher D, Wrigley JDJ, Nadin A, Evin G, Masters CL, Harrison T, Castro JL, Shearman MS: Pharmacological knock-down of the presenilin 1 heterodimer by a novel γ-secretase inhibitor: Implications for presenilin biology. J Biol Chem (2001) 276:45394-45402. This report leads to the suggestion that presenilinase activity could be regulated separately from γ-secretase activity.
-
(2001)
J Biol Chem
, vol.276
, pp. 45394-45402
-
-
Beher, D.1
Wrigley, J.D.J.2
Nadin, A.3
Evin, G.4
Masters, C.L.5
Harrison, T.6
Castro, J.L.7
Shearman, M.S.8
-
46
-
-
0037916392
-
γ-secretase tolerates both D and L amino acids in (hydroxyethyl)urea peptidomimetics
-
Orlando, FL, USA:MEDI-038
-
Bakshi P, Diehl TS, Wolfe MS: γ-Secretase tolerates both D and L amino acids in (hydroxyethyl)urea peptidomimetics. 223rd ACS Meeting, Orlando, FL, USA (2002):MEDI-038.
-
(2002)
223rd ACS Meeting
-
-
Bakshi, P.1
Diehl, T.S.2
Wolfe, M.S.3
-
47
-
-
0038253948
-
Aβ modulation: The beginning of the end or the end of the beginning
-
Atlanta, GA, USA
-
Felsenstein KM: Aβ modulation: The beginning of the end or the end of the beginning. IBC Ninth Annual Alzheimer's Meeting, Atlanta, GA, USA (2001). Presentation of a potent and orally bioavailable inhibitor.
-
(2001)
IBC Ninth Annual Alzheimer's Meeting
-
-
Felsenstein, K.M.1
-
48
-
-
0033946796
-
Fenchylamine sulfonamide inhibitors of amyloid β peptide production by the γ-secretase proteolytic pathway: Potential small-molecule therapeutic agents for the treatment of Alzheimer's disease
-
Rishton GM, Retz DM, Tempest PA, Novotny J, Kahn S, Treanor JJS, Lile JD, Citron M: Fenchylamine sulfonamide inhibitors of amyloid β peptide production by the γ-secretase proteolytic pathway: Potential small-molecule therapeutic agents for the treatment of Alzheimer's disease. J Med Chem (2000) 43:2297-2299.
-
(2000)
J Med Chem
, vol.43
, pp. 2297-2299
-
-
Rishton, G.M.1
Retz, D.M.2
Tempest, P.A.3
Novotny, J.4
Kahn, S.5
Treanor, J.J.S.6
Lile, J.D.7
Citron, M.8
-
49
-
-
0037916393
-
Marked reduction of Aβ accumulation and β-amyloid plaque pathology in mice upon chronic treatment with a functional γ-secretase inhibitor
-
San Diego, CA, USA
-
May PC: Marked reduction of Aβ accumulation and β-amyloid plaque pathology in mice upon chronic treatment with a functional γ-secretase inhibitor. 31st Annual Society of Neuroscience Meeting, San Diego, CA, USA (2001). Presentation of a highly potent and orally bioavailable inhibitor that is effective at reducing plasma and cortical Aβ in transgenic pre-plaque mice with no apparent side effects with up to 90 days dosing.
-
(2001)
31st Annual Society of Neuroscience Meeting
-
-
May, P.C.1
-
50
-
-
0035163347
-
Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brain
-
Dovey HF, John V, Anderson JP, Chen LZ, de Saint Andrieu P, Fang LY, Freedman SB, Folmer B, Goldbach E, Holsztynska EJ, Hu KL et al: Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brain. J Neurochem (2001) 76:173-181. First demonstrated efficacy of a γ-secretase inhibitor in reducing Aβ brain levels in mice.
-
(2001)
J Neurochem
, vol.76
, pp. 173-181
-
-
Dovey, H.F.1
John, V.2
Anderson, J.P.3
Chen, L.Z.4
De Saint Andrieu, P.5
Fang, L.Y.6
Freedman, S.B.7
Folmer, B.8
Goldbach, E.9
Holsztynska, E.J.10
Hu, K.L.11
-
51
-
-
4944235526
-
γ-secretase/presenilin inhibitor causes Notch-deficient phenotype in Drosophila
-
San Diego, CA, USA
-
Wolfe MS: γ-Secretase/presenilin inhibitor causes Notch-deficient phenotype in Drosophila. 31st Annual Society of Neuroscience, San Diego, CA, USA (2001).
-
(2001)
31st Annual Society of Neuroscience
-
-
Wolfe, M.S.1
-
52
-
-
0035168194
-
Implication of APP secretases in Notch signaling
-
Hartmann D, Toumoy J, Saftig P, Annaert W, De Strooper B: Implication of APP secretases in Notch signaling. J Mol Neurosci (2001) 17:171-181. A comprehensive review of the Notch signaling system that covers the role and importance of presenilins in Notch1 cleavage and describes the pathological consequences of Notch signaling malfunction.
-
(2001)
J Mol Neurosci
, vol.17
, pp. 171-181
-
-
Hartmann, D.1
Toumoy, J.2
Saftig, P.3
Annaert, W.4
De Strooper, B.5
-
53
-
-
0035839591
-
Notch1 and amyloid precursor protein are competitive substrates for presenilin1-dependent γ-secretase cleavage
-
Berezovska O, Jack C, Deng A, Gastineau N, Rebeck GW, Hyman BT: Notch1 and amyloid precursor protein are competitive substrates for presenilin1-dependent γ-secretase cleavage. J Biol Chem (2001) 276:30018-30023.
-
(2001)
J Biol Chem
, vol.276
, pp. 30018-30023
-
-
Berezovska, O.1
Jack, C.2
Deng, A.3
Gastineau, N.4
Rebeck, G.W.5
Hyman, B.T.6
-
54
-
-
0036290522
-
γ-secretase-like cleavages of Notch and βAPP are mutually exclusive in human cells
-
Petit A, St George-Hyslop P, Fraser P, Checler F: γ-Secretase-like cleavages of Notch and βAPP are mutually exclusive in human cells. Biochem Biophys Res Commun (2002) 290:1408-1410. Description of a Notch processing cell-based assay.
-
(2002)
Biochem Biophys Res Commun
, vol.290
, pp. 1408-1410
-
-
Petit, A.1
St. George-Hyslop, P.2
Fraser, P.3
Checler, F.4
-
55
-
-
0035824391
-
γ-secretase cleavage and nuclear localization of ErbB-4 receptor tyrosine kinase
-
Ni C-Y, Murphy MP, Golde TE, Carpenter G: γ-Secretase cleavage and nuclear localization of ErbB-4 receptor tyrosine kinase. Science (2001) 294:2179-2181.
-
(2001)
Science
, vol.294
, pp. 2179-2181
-
-
Ni, C.-Y.1
Murphy, M.P.2
Golde, T.E.3
Carpenter, G.4
-
56
-
-
0037155219
-
Presenilin-dependent γ-secretase-like intramembrane cleavage of ErbB4
-
Lee H-J, Jung K-M, Huang YZ, Bennett LB, Lee JS, Mei L, Kim T-W: Presenilin-dependent γ-secretase-like intramembrane cleavage of ErbB4. J Biol Chem (2002) 277:6318-6323.
-
(2002)
J Biol Chem
, vol.277
, pp. 6318-6323
-
-
Lee, H.-J.1
Jung, K.-M.2
Huang, Y.Z.3
Bennett, L.B.4
Lee, J.S.5
Mei, L.6
Kim, T.-W.7
-
57
-
-
0035912829
-
γ-secretase inhibitors repress thymocyte development
-
Hadland BK, Manley NR, Su D, Longmore GD, Moore CL, Wolfe MS, Schroeter EH, Kopan R: γ-Secretase inhibitors repress thymocyte development. Proc Natl Acad Sci USA (2001) 98:7487-7491.
-
(2001)
Proc Natl Acad Sci USA
, vol.98
, pp. 7487-7491
-
-
Hadland, B.K.1
Manley, N.R.2
Su, D.3
Longmore, G.D.4
Moore, C.L.5
Wolfe, M.S.6
Schroeter, E.H.7
Kopan, R.8
-
58
-
-
0035979234
-
Presenilin-dependent γ-secretase activity modulates thymocyte development
-
Doerfler P, Shearman MS, Perlmutter RM: Presenilin-dependent γ-secretase activity modulates thymocyte development. Proc Natl Acad Sci USA (2001) 98:9312-9317.
-
(2001)
Proc Natl Acad Sci USA
, vol.98
, pp. 9312-9317
-
-
Doerfler, P.1
Shearman, M.S.2
Perlmutter, R.M.3
-
59
-
-
0037040977
-
Identification and characterization of presenilinin-dependent Notch signaling
-
Berechid BE, Kitzmann M, Foltz DR, Roach AH, Seiffert D, Thompson LA, Olson RE, Bemstein A, Donoviel DB, Nye JS: Identification and characterization of presenilinin-dependent Notch signaling. J Biol Chem (2002) 277:8154-8165.
-
(2002)
J Biol Chem
, vol.277
, pp. 8154-8165
-
-
Berechid, B.E.1
Kitzmann, M.2
Foltz, D.R.3
Roach, A.H.4
Seiffert, D.5
Thompson, L.A.6
Olson, R.E.7
Bemstein, A.8
Donoviel, D.B.9
Nye, J.S.10
-
60
-
-
0035005101
-
New protease inhibitors prevent γ-secretase mediated production of Aβ40/42 without affecting Notch cleavage
-
Petit A, Bihel F, Alves da Costa C, Pourquie O, Checler F, Kraus J-L: New protease inhibitors prevent γ-secretase mediated production of Aβ40/42 without affecting Notch cleavage. Nat Cell Biol (2001) 3:507-511. Description of a Notch processing cell-based assay.
-
(2001)
Nat Cell Biol
, vol.3
, pp. 507-511
-
-
Petit, A.1
Bihel, F.2
Alves da Costa, C.3
Pourquie, O.4
Checler, F.5
Kraus, J.-L.6
-
61
-
-
0035902619
-
Peripheral anti-Aβ antibody alters CNS and plasma Aβ clearance and decreases brain Aβ burden in a mouse model of Alzheimer's disease
-
DeMattos RB, Bales KR, Cummins DJ, Dodart J-C, Paul SM, Holtzman DM: Peripheral anti-Aβ antibody alters CNS and plasma Aβ clearance and decreases brain Aβ burden in a mouse model of Alzheimer's disease. Proc Natl Acad Sci USA (2001) 98:8850-8855. One of the first reports to suggest that clearance of plasma Aβ could reduce brain Aβ burden by acting as a peripheral sink.
-
(2001)
Proc Natl Acad Sci USA
, vol.98
, pp. 8850-8855
-
-
DeMattos, R.B.1
Bales, K.R.2
Cummins, D.J.3
Dodart, J.-C.4
Paul, S.M.5
Holtzman, D.M.6
-
63
-
-
0038592546
-
-
(Hydroxyethyl)ureas as inhibitors of Alzheimer's β-amyloid production. WO-00214264 (2002)
-
BRIGHAM & WOMEN'S HOSPITAL INC (Wolfe MS, Selkoe DJ): (Hydroxyethyl)ureas as inhibitors of Alzheimer's β-amyloid production. WO-00214264 (2002).
-
-
-
Wolfe, M.S.1
Selkoe, D.J.2
-
64
-
-
0037578436
-
-
Novel sulfonamide compounds and their uses thereof. WO-00050391 (2000)
-
MERCK & CO/BRISTOL-MYERS SQUIBB CO (Smith DW, Munoz B, Srinivasan K, Bergstrom CP, Chaturvedula PV, Deshpande MS, Keavy DJ, Lau WY, Parker MF, Sloan CP, Wallace OB, Wang HH): Novel sulfonamide compounds and their uses thereof. WO-00050391 (2000). Patent covering a wide range of arylsulfonamides which may be related to a candidate from Bristol-Myers Squibb that was reported to have entered phase I clinical trials.
-
-
-
Smith, D.W.1
Munoz, B.2
Srinivasan, K.3
Bergstrom, C.P.4
Chaturvedula, P.V.5
Deshpande, M.S.6
Keavy, D.J.7
Lau, W.Y.8
Parker, M.F.9
Sloan, C.P.10
Wallace, O.B.11
Wang, H.H.12
-
65
-
-
0037578434
-
-
Sulphonamido-substituted bridged bicycloalkyl derivatives. WO-00170677 (2001)
-
MERCK SHARP & DOHME LTD (Belanger PC, Collins IJ, Hannam JC, Harrison T, Lewis SJ, Madin A, McIver EG, Nadin AJ, Neduvelil JG, Shearman MS, Smith AM, Sparey TJ, Stevenson GI, Teall MR): Sulphonamido-substituted bridged bicycloalkyl derivatives. WO-00170677 (2001).
-
-
-
Belanger, P.C.1
Collins, I.J.2
Hannam, J.C.3
Harrison, T.4
Lewis, S.J.5
Madin, A.6
McIver, E.G.7
Nadin, A.J.8
Neduvelil, J.G.9
Shearman, M.S.10
Smith, A.M.11
Sparey, T.J.12
Stevenson, G.I.13
Teall, M.R.14
-
66
-
-
0037916394
-
-
Cycloalkyl, lactam, lactone and related compounds pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds. WO-09828268 (1998)
-
ELI LILLY & CO/ATHENA NEUROSCIENCE INC (Wu J, Tung JS, Thorsett ED, Pleiss MA, Nissen JS, Neitz J, Latimer LH, John V, Freedman S, Britton TC, Audia JE et al): Cycloalkyl, lactam, lactone and related compounds pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds. WO-09828268 (1998). Patent covering a series of caprolactams, including LY-411575.
-
-
-
Wu, J.1
Tung, J.S.2
Thorsett, E.D.3
Pleiss, M.A.4
Nissen, J.S.5
Neitz, J.6
Latimer, L.H.7
John, V.8
Freedman, S.9
Britton, T.C.10
Audia, J.E.11
-
67
-
-
0038253952
-
-
Succinoylamino carbocycles and heterocycles as inhibitors of Aβ protein production useful for treating Alzheimer's disease. WO-00160826 (2001)
-
DUPONT PHARMACEUTICALS CO (Olson RE, Maduskuie TP, Thompson LA, Tebben AJ, Wang N, Deng W, Liu H): Succinoylamino carbocycles and heterocycles as inhibitors of Aβ protein production useful for treating Alzheimer's disease. WO-00160826 (2001).
-
-
-
Olson, R.E.1
Maduskuie, T.P.2
Thompson, L.A.3
Tebben, A.J.4
Wang, N.5
Deng, W.6
Liu, H.7
-
68
-
-
0038253954
-
-
Lactams substituted by cyclic succinates as inhibitors of Aβ protein production. WO-00192235 (2001)
-
DUPONT PHARMACEUTICALS CO (Olson RE): Lactams substituted by cyclic succinates as inhibitors of Aβ protein production. WO-00192235 (2001).
-
-
-
Olson, R.E.1
-
69
-
-
0038253953
-
-
Cyclic lactams as inhibitors of Aβ protein production. WO-00174783 (2001)
-
DUPONT PHARMACEUTICALS CO (Olson RE, Yang MG): Cyclic lactams as inhibitors of Aβ protein production. WO-00174783 (2001).
-
-
-
Olson, R.E.1
Yang, M.G.2
-
70
-
-
0038592545
-
-
Cyclic lactams as inhibitors of Aβ protein production. WO-00174784 (2001)
-
DUPONT PHARMACEUTICALS CO (Yang MG, Liu H): Cyclic lactams as inhibitors of Aβ protein production. WO-00174784 (2001).
-
-
-
Yang, M.G.1
Liu, H.2
-
71
-
-
0038253955
-
-
Hydroxyalkanoyl aminolactams and related structures as inhibitors of Aβ protein production. WO-00119797 (2001)
-
DUPONT PHARMACEUTICALS CO (Olson RE, Liu H, Thompson LA): Hydroxyalkanoyl aminolactams and related structures as inhibitors of Aβ protein production. WO-00119797 (2001).
-
-
-
Olson, R.E.1
Liu, H.2
Thompson, L.A.3
-
72
-
-
0037578437
-
-
Substituted lactams as inhibitors of Aβ protein production. WO-00177086 (2001)
-
DUPONT PHARMACEUTICALS CO (Han W, Liu H, Olson RE, Yang MG): Substituted lactams as inhibitors of Aβ protein production. WO-00177086 (2001).
-
-
-
Han, W.1
Liu, H.2
Olson, R.E.3
Yang, M.G.4
-
73
-
-
0037578439
-
-
Amino lactam sulfonamides as inhibitors of Aβ protein production. WO-00127108 (2001)
-
DUPONT PHARMACEUTICALS CO (Thompson LA, Han AQ): Amino lactam sulfonamides as inhibitors of Aβ protein production. WO-00127108 (2001).
-
-
-
Thompson, L.A.1
Han, A.Q.2
-
74
-
-
0037578438
-
-
Benzodiazepine derivatives as APP modulators. WO-00190084 (2001)
-
MERCK SHARP & DOHME LTD (Castro Pineiro JL, Churcher I, Guiblin AR, Harfison T, Kerrad S, Madin A, Nadin AJ, Owens AP, Sparey TJ, Teall MR, Williams S): Benzodiazepine derivatives as APP modulators. WO-00190084 (2001).
-
-
-
Castro Pineiro, J.L.1
Churcher, I.2
Guiblin, A.R.3
Harfison, T.4
Kerrad, S.5
Madin, A.6
Nadin, A.J.7
Owens, A.P.8
Sparey, T.J.9
Teall, M.R.10
Williams, S.11
-
75
-
-
0038592549
-
-
Benzodiazepinone β-amyloid inhibitors: Arylacetamidoalanyl derivatives. US-2002002621 (2002)
-
BRISTOL-MYERS SQUIBB CO (Chaturvedula PV, Yeola S, Vig S): Benzodiazepinone β-amyloid inhibitors: Arylacetamidoalanyl derivatives. US-2002002621 (2002).
-
-
-
Chaturvedula, P.V.1
Yeola, S.2
Vig, S.3
-
76
-
-
0038253949
-
-
Lactams as inhibitors of A-β protein production. WO-00172324 (2001)
-
DUPONT PHARMACEUTICALS CO (Thompson LA): Lactams as inhibitors of A-β protein production. WO-00172324 (2001).
-
-
-
Thompson, L.A.1
-
77
-
-
0038592548
-
-
γ-Secretase inhibitors. US-20020013315 (2002)
-
MERCK & CO (Teall MR): γ-Secretase inhibitors. US-20020013315 (2002).
-
-
-
Teall, M.R.1
|