Interplay between α-, β-, and γ-secretases determines biphasic amyloid-β protein level in the presence of a γ-secretase inhibitor. (Q39244758)

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17 February 2020

title

Interplay between α-, β-, and γ-secretases determines biphasic amyloid-β protein level in the presence of a γ-secretase inhibitor (English)

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17 February 2020

1

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17 February 2020

Claus Bendtsen

series ordinal

4

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17 February 2020

author name string

Jonathan Stott

series ordinal

2

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17 February 2020

Sandra A G Visser

series ordinal

3

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17 February 2020

language of work or name

English

0 references

publication date

14 November 2012

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Journal of Biological Chemistry

17 February 2020

published in

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17 February 2020

volume

288

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17 February 2020

issue

2

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17 February 2020

page(s)

785-792

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Has inhibition of Aβ production adequately been tested as therapeutic approach in mild AD? A model-based meta-analysis of γ-secretase inhibitor data

17 February 2020

cites work

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10 September 2017

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BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells

10 September 2017

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Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors

10 September 2017

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Inhibitors of γ-secretase stabilize the complex and differentially affect processing of amyloid precursor protein and other substrates

10 September 2017

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Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound

10 September 2017

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Allosteric modulation of PS1/gamma-secretase conformation correlates with amyloid beta(42/40) ratio

10 September 2017

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Alternative pathways for production of beta-amyloid peptides of Alzheimer's disease

10 September 2017

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Inhibitors of cathepsin B improve memory and reduce beta-amyloid in transgenic Alzheimer disease mice expressing the wild-type, but not the Swedish mutant, beta-secretase site of the amyloid precursor protein

10 September 2017

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Bistability from double phosphorylation in signal transduction. Kinetic and structural requirements

10 September 2017

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Human amyloid-beta synthesis and clearance rates as measured in cerebrospinal fluid in vivo

10 September 2017

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gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site

10 September 2017

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Putative function of ADAM9, ADAM10, and ADAM17 as APP alpha-secretase

10 September 2017

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Alzheimer's disease: molecular understanding predicts amyloid-based therapeutics

10 September 2017

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Product dependence and bifunctionality compromise the ultrasensitivity of signal transduction cascades

10 September 2017

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Biochemical characterization of the gamma-secretase activity that produces beta-amyloid peptides

10 September 2017

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Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1

10 September 2017

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Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE

10 September 2017

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Mutation of the beta-amyloid precursor protein in familial Alzheimer's disease increases beta-protein production

10 September 2017

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ADAM10 is the physiologically relevant, constitutive alpha-secretase of the amyloid precursor protein in primary neurons

10 September 2017

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Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease

14 September 2017

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The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression

14 September 2017

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Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.

14 September 2017

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Rank-order of potencies for inhibition of the secretion of abeta40 and abeta42 suggests that both are generated by a single gamma-secretase

14 September 2017

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Direct and potent regulation of gamma-secretase by its lipid microenvironment

25 September 2017

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A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity.

17 June 2018

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Modeling effect of a γ-secretase inhibitor on amyloid-β dynamics reveals significant role of an amyloid clearance mechanism

17 June 2018

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alpha-secretase mediated conversion of the amyloid precursor protein derived membrane stub C99 to C83 limits Abeta generation.

21 August 2018

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21 August 2018

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21 August 2018

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Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Al

21 August 2018

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DAPT-induced intracellular accumulations of longer amyloid beta-proteins: further implications for the mechanism of intramembrane cleavage by gamma-secretase.

21 August 2018

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Studies of Abeta pharmacodynamics in the brain, cerebrospinal fluid, and plasma in young (plaque-free) Tg2576 mice using the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[

21 August 2018

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In VivoAssessment of Brain Interstitial Fluid with Microdialysis Reveals Plaque-Associated Changes in Amyloid-β Metabolism and Half-Life

21 August 2018

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Employing a superior BACE1 cleavage sequence to probe cellular APP processing

21 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3543028

Apolipoprotein E influences amyloid-beta clearance from the murine periphery.

21 August 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3543028

Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines

21 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3543028

A placebo-controlled, multiple ascending dose study to evaluate the safety, pharmacokinetics and pharmacodynamics of avagacestat (BMS-708163) in healthy young and elderly subjects

21 August 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23152503

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Cell-free assays for gamma-secretase activity

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23152503

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1074/JBC.M112.419135

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23152503%20AND%20SRC:MED&resulttype=core&format=json

17 February 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23152503%20AND%20SRC:MED&resulttype=core&format=json

17 February 2020

PubMed publication ID

23152503

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23152503%20AND%20SRC:MED&resulttype=core&format=json