Dynamics of β-Amyloid Reductions in Brain, Cerebrospinal Fluid, and Plasma of β-Amyloid Precursor Protein Transgenic Mice Treated with a γ-Secretase Inhibitor

Barten, D.M.; Guss, V.L.; Corsa, J.A.; Loo, A.; Hansel, S.B.; Zheng, M.; Munoz, B.; Srinivasan, K.; Wang, B.; Robertson, B.J.; Polson, C.T.; Wang, J.; Roberts, S.B.; Hendrick, J.P.; Anderson, J.J.; Loy, J.K.; Denton, R.; Verdoorn, T.A.; Smith, D.W.; Felsenstein, K.M.

doi:10.1124/jpet.104.075408

Cited by 176Alzheimer's disease research and treatmentsDementia and Cognitive Impairment ResearchCholinesterase and Neurodegenerative Diseases

Dynamics of β-Amyloid Reductions in Brain, Cerebrospinal Fluid, and Plasma of β-Amyloid Precursor Protein Transgenic Mice Treated with a γ-Secretase Inhibitor

Barten, D.M., Guss, V.L., Corsa, J.A., Loo, A., Hansel, S.B., Zheng, M., Munoz, B., Srinivasan, K. +12 more·2005·The Journal of Pharmacology and Experimental Therapeutics

DOI 10.1124/jpet.104.075408

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Abstract

gamma-Secretase inhibitors are one promising approach to the development of a therapeutic for Alzheimer's disease (AD). gamma-Secretase inhibitors reduce brain beta-amyloid peptide (Abeta), which is believed to be a major contributor in the etiology of AD. Transgenic mice overexpressing the human beta-amyloid precursor protein (APP) are valuable models to examine the dynamics of Abeta changes with gamma-secretase inhibitors in plaque-free and plaque-bearing animals. BMS-299897 2-[(1R)-1-[[(4-chlorophenyl)sulfony](2,5-difluorophenyl)amino]ethyl]-5-fluorobenzenepropanoic acid, a gamma-secretase inhibitor, showed dose- and time dependent reductions of Abeta in brain, cerebrospinal fluid (CSF), and plasma in young transgenic mice, with a significant correlation between brain and CSF Abeta levels. Because CSF and brain interstitial fluid are distinct compartments in composition and location, this correlation could not be assumed. In contrast, aged transgenic mice with large accumulations of Abeta in plaques showed reductions in CSF Abeta in the absence of measurable changes in plaque Abeta in the brain after up to 2 weeks of treatment. Hence, CSF Abeta levels were a valuable measure of gamma-secretase activity in the central nervous system in either the presence or absence of plaques. Transgenic mice were also used to examine potential side effects due to Notch inhibition. BMS-299897 was 15-fold more effective at preventing the cleavage of APP than of Notch in vitro. No changes in…

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The half-life of Aβ clearance in previous studies ranged from 30 min to 2 h.
“The half-life of Aβ clearance in these studies ranged from 30 min to 2 h.”
From Measurement of apolipoprotein E and amyloid β clearance rates in the mouse brain using bolus stable isotope labeling (2012) · cites this paper as [50]
Previous studies have measured Aβ clearance from the brain either using 35S]methionine labeling or by measuring the disappearance of Aβ following the pharmacological inhibition of Aβ production.
“Previous studies have measured Aβ clearance from the brain either using 35 S]methionine labeling [48], or by measuring the disappearance of Aβ following the pharmacological inhibition of Aβ production [49-51].”
From Measurement of apolipoprotein E and amyloid β clearance rates in the mouse brain using bolus stable isotope labeling (2012) · cites this paper as [50]

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Dynamics of Aβ Turnover and Deposition in Different β-Amyloid Precursor Protein Transgenic Mouse Models Following γ-Secretase Inhibition
Abramowski, D., Wiederhold, K.-H., Furrer, U., Jaton, A.-L., Neuenschwander, A., Runser, M.-J., Danner, S., Reichwald, J., Ammaturo, D., Staab, D., et al. (2008) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.140327 · Cited by 89 · see citing works
??-Secretase Inhibitors for Alzheimer??s Disease
Barten, D. M., Meredith, J. E., Zaczek, R. C., Houston, J. G., & Albright, C. F. (2006) · Drugs in R&D · doi:10.2165/00126839-200607020-00003 · Cited by 127 · see citing works
Self-citation
Modulation of γ-Secretase Reduces β-Amyloid Deposition in a Transgenic Mouse Model of Alzheimer's Disease
Kounnas, M. Z., Danks, A. M., Cheng, S., Tyree, C. M., Ackerman, E. S., Zhang, X., Ahn, K., Nguyen, P. A. H., Comer, D., Mao, L., et al. (2010) · Neuron · doi:10.1016/j.neuron.2010.08.018 · Cited by 253 · see citing works
Acute Retention of Urine
Badenoch, A. W. (1955) · BMJ · doi:10.1136/bmj.2.4930.36 · Cited by 3 · see citing works

Authors: Barten, D. M., Guss, V. L., Corsa, J. A., Loo, A., Hansel, S. B., Zheng, M., Munoz, B., Srinivasan, K., Wang, B., Robertson, B. J., Polson, C. T., Wang, J., Roberts, S. B., Hendrick, J. P., Anderson, J. J., Loy, J. K., Denton, R., Verdoorn, T. A., Smith, D. W., & Felsenstein, K. M.
Affiliations: Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
ORCID: Robertson, B.J.
Wang, J.
Verdoorn, T.A.
Venue: The Journal of Pharmacology and Experimental Therapeutics
Publisher: Elsevier BV
Published: 2005-02
Volume: 312
Issue: 2
Pages: 635-643
ISSN: 0022-3565 (ISSN-L)
DOI: 10.1124/jpet.104.075408
OpenAlex: W2167864502
Cited by: 159
References: 44
Citations by year: 2025: 1 · 2024: 1 · 2023: 1 · 2022: 1 · 2021: 2 · 2020: 1 · 2018: 1 · 2017: 6 · 2016: 3 · 2015: 3 · 2014: 8 · 2013: 5 · 2012: 13
FWCI: 12.50
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
Keywords: amyloid-beta, gamma-secretase inhibitors, Alzheimer's disease, APP transgenic mice, cerebrospinal fluid, amyloid plaques, Notch signaling, CD8+ thymocytes, intestinal goblet cells, amyloid precursor protein
MeSH terms: Aging, Animals, Brain Chemistry, Cell Separation, Dose-Response Relationship, Drug, Enzyme-Linked Immunosorbent Assay, Flow Cytometry, Humans, Membrane Proteins, Mice, Inbred C57BL, Mice, Transgenic, Endopeptidases, Protease Inhibitors, T-Lymphocytes, Blotting, Western, Amyloid beta-Peptides, Aspartic Acid Endopeptidases, Amyloid beta-Protein Precursor, Immunoprecipitation, Mice, Receptors, Notch, Amyloid Precursor Protein Secretases, Plaque, Amyloid

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Dynamics of β-Amyloid Reductions in Brain, Cerebrospinal Fluid, and Plasma of β-Amyloid Precursor Protein Transgenic Mice Treated with a γ-Secretase Inhibitor

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