(Q39087660)

English

Population PKPD modeling of BACE1 inhibitor-induced reduction in Aβ levels in vivo and correlation to in vitro potency in primary cortical neurons from mouse and guinea pig.

scientific article published on 3 October 2013

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scholarly article

1 reference

Europe PubMed Central

9 September 2017

Population PKPD modeling of BACE1 inhibitor-induced reduction in Aβ levels in vivo and correlation to in vitro potency in primary cortical neurons from mouse and guinea pig. (English)

1 reference

Europe PubMed Central

9 September 2017

author name string

Juliette Janson

1

1 reference

Europe PubMed Central

9 September 2017

Susanna Eketjäll

2

1 reference

Europe PubMed Central

9 September 2017

Karin Tunblad

3

1 reference

Europe PubMed Central

9 September 2017

Fredrik Jeppsson

4

1 reference

Europe PubMed Central

9 September 2017

Stefan Von Berg

5

1 reference

Europe PubMed Central

9 September 2017

Camilla Niva

6

1 reference

Europe PubMed Central

9 September 2017

Ann-Cathrin Radesäter

7

1 reference

Europe PubMed Central

9 September 2017

Johanna Fälting

8

1 reference

Europe PubMed Central

9 September 2017

Sandra A G Visser

9

1 reference

Europe PubMed Central

9 September 2017

publication date

3 October 2013

1 reference

Europe PubMed Central

9 September 2017

Pharmaceutical Research

1 reference

Europe PubMed Central

9 September 2017

31

1 reference

Europe PubMed Central

9 September 2017

3

1 reference

Europe PubMed Central

9 September 2017

670-683

1 reference

Europe PubMed Central

9 September 2017

Clinical diagnosis of Alzheimer's disease: report of the NINCDS-ADRDA Work Group under the auspices of Department of Health and Human Services Task Force on Alzheimer's Disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Alzheimer's Disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

2012 Alzheimer's disease facts and figures

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

The amyloid hypothesis for Alzheimer's disease: a critical reappraisal

1 reference

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21 January 2018

The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

1 reference

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21 January 2018

γ-Secretase inhibitors and modulators for Alzheimer's disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Alzheimer's disease and the amyloid β-protein

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Regulated intramembrane proteolysis--lessons from amyloid precursor protein processing

1 reference

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21 January 2018

The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics

1 reference

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21 January 2018

Visualization of A beta 42(43) and A beta 40 in senile plaques with end-specific A beta monoclonals: evidence that an initially deposited species is A beta 42(43).

1 reference

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21 January 2018

Evidence that A beta 42 is the real culprit in Alzheimer's disease.

1 reference

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21 January 2018

Genes and mechanisms involved in beta-amyloid generation and Alzheimer's disease

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21 January 2018

Alzheimer's disease: strategies for disease modification

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21 January 2018

REVIEW: γ-Secretase inhibitors for the treatment of Alzheimer's disease: The current state.

1 reference

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21 January 2018

Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Purification and cloning of amyloid precursor protein beta-secretase from human brain

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Membrane-anchored aspartyl protease with Alzheimer's disease beta-secretase activity

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

BACE1 structure and function in health and Alzheimer's disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

The proteins BACE1 and BACE2 and beta-secretase activity in normal and Alzheimer's disease brain.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

A locus for familial early-onset Alzheimer's disease on the long arm of chromosome 14, proximal to the alpha 1-antichymotrypsin gene.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

A mutation in APP protects against Alzheimer’s disease and age-related cognitive decline

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Design and synthesis of β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of β-amyloid peptides

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Discovery of AZD3839, a Potent and Selective BACE1 Inhibitor Clinical Candidate for the Treatment of Alzheimer Disease

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

A noncompetitive BACE1 inhibitor TAK-070 ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease.

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Beta-secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

New aminoimidazoles as β-secretase (BACE-1) inhibitors showing amyloid-β (Aβ) lowering in brain

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy

1 reference

https://api.crossref.org/works/10.1007%2FS11095-013-1189-Y

21 January 2018

Brain and choroid plexus blood volumes in vertebrates

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21 January 2018

P-glycoprotein and mutlidrug resistance-associated proteins limit the brain uptake of saquinavir in mice

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21 January 2018

Development of a high-throughput brain slice method for studying drug distribution in the central nervous system

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21 January 2018

Comparison of four basic models of indirect pharmacodynamic responses

1 reference

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21 January 2018

The novel beta-secretase inhibitor KMI-429 reduces amyloid beta peptide production in amyloid precursor protein transgenic and wild-type mice

1 reference

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21 January 2018

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

1 reference

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21 January 2018

Flavonols and flavones as BACE-1 inhibitors: structure-activity relationship in cell-free, cell-based and in silico studies reveal novel pharmacophore features

1 reference

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21 January 2018

Guinea-pig primary cell cultures provide a model to study expression and amyloidogenic processing of endogenous amyloid precursor protein

1 reference

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21 January 2018

Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for beta- and beta'-cleavage sites by human and murine BACE1.

1 reference

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21 January 2018

The functional gamma-secretase inhibitor prevents production of amyloid beta 1-34 in human and murine cell lines

1 reference

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21 January 2018

Pharmacodynamic-pharmacokinetic integration as a guide to medicinal chemistry

1 reference

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21 January 2018

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

1 reference

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https://pubmed.ncbi.nlm.nih.gov/24092053

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The virtue of translational PKPD modeling in drug discovery: selecting the right clinical candidate while sparing animal lives

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https://pubmed.ncbi.nlm.nih.gov/24092053

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Integrating experimentation and quantitative modeling to enhance discovery of Beta amyloid lowering therapeutics for Alzheimer's disease

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A technique for serial collection of cerebrospinal fluid from the cisterna magna in mouse

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Identifiers

10.1007/S11095-013-1189-Y

1 reference

Europe PubMed Central

9 September 2017

1 reference

Europe PubMed Central

9 September 2017

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