The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients (Q39222469)

10 September 2017

title

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients (English)

1 reference

10 September 2017

0 references

10

Lynn A Hyde

1 reference

10 September 2017

Matthew E Kennedy

1

1 reference

10 September 2017

Andrew W Stamford

2

1 reference

10 September 2017

Xia Chen

3

1 reference

10 September 2017

Kathleen Cox

4

1 reference

10 September 2017

Jared N Cumming

5

1 reference

10 September 2017

Marissa F Dockendorf

6

1 reference

10 September 2017

Michael Egan

7

1 reference

10 September 2017

Larry Ereshefsky

8

1 reference

10 September 2017

Robert A Hodgson

9

1 reference

10 September 2017

Stanford Jhee

11

1 reference

10 September 2017

Huub J Kleijn

12

1 reference

10 September 2017

Reshma Kuvelkar

13

1 reference

10 September 2017

Wei Li

14

1 reference

10 September 2017

Britta A Mattson

15

1 reference

10 September 2017

Hong Mei

16

1 reference

10 September 2017

John Palcza

17

1 reference

10 September 2017

Jack D Scott

18

1 reference

10 September 2017

Michael Tanen

19

1 reference

10 September 2017

Matthew D Troyer

20

1 reference

10 September 2017

Jack L Tseng

21

1 reference

10 September 2017

Julie A Stone

22

1 reference

10 September 2017

Eric M Parker

23

1 reference

10 September 2017

Mark S Forman

24

1 reference

10 September 2017

language of work or name

English

0 references

publication date

1 November 2016

1 reference

Science Translational Medicine

10 September 2017

published in

1 reference

10 September 2017

volume

8

1 reference

10 September 2017

issue

363

1 reference

10 September 2017

page(s)

363ra150

1 reference

Stages of the pathologic process in Alzheimer disease: age categories from 1 to 100 years

10 September 2017

cites work

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

The amyloid hypothesis of Alzheimer's disease at 25 years

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Targeting the β secretase BACE1 for Alzheimer's disease therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Soluble oligomers of the amyloid beta-protein impair synaptic plasticity and behavior

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Three dimensions of the amyloid hypothesis: time, space and 'wingmen'

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Phenotypic and biochemical analyses of BACE1- and BACE2-deficient mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

BACE1 gene deletion prevents neuron loss and memory deficits in 5XFAD APP/PS1 transgenic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

The Alzheimer disease protective mutation A2T modulates kinetic and thermodynamic properties of amyloid-β (Aβ) aggregation

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Molecular mechanisms of Alzheimer disease protection by the A673T allele of amyloid precursor protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

BACE1 Physiological Functions May Limit Its Use as Therapeutic Target for Alzheimer's Disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Utility of unbound plasma drug levels and P-glycoprotein transport data in prediction of central nervous system exposure

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Control of peripheral nerve myelination by the beta-secretase BACE1

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Bace1 modulates myelination in the central and peripheral nervous system.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Bace2 is a β cell-enriched protease that regulates pancreatic β cell function and mass

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

BACE2 processes PMEL to form the melanosome amyloid matrix in pigment cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Fluctuations of CSF amyloid-beta levels: implications for a diagnostic and therapeutic biomarker.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

A critique of the drug discovery and phase 3 clinical programs targeting the amyloid hypothesis for Alzheimer disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Systems Pharmacology Analysis of the Amyloid Cascade after β-Secretase Inhibition Enables the Identification of an Aβ42 Oligomer Pool

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Beta-site amyloid precursor protein cleaving enzyme 1 levels become elevated in neurons around amyloid plaques: implications for Alzheimer's disease pathogenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Antagonistic Effects of BACE1 and APH1B-γ-Secretase Control Axonal Guidance by Regulating Growth Cone Collapse

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

BACE1 inhibition induces a specific cerebrospinal fluid β-amyloid pattern that identifies drug effects in the central nervous system

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

β-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigment

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

BACE1 deficiency causes altered neuronal activity and neurodegeneration

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Retinal Toxicity Induced by a Novel β-secretase Inhibitor in the Sprague-Dawley Rat.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Cathepsin D deficiency induces persistent neurodegeneration in the absence of Bax-dependent apoptosis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Roles of Meltrin beta /ADAM19 in the processing of neuregulin

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Learning by failing: ideas and concepts to tackle γ-secretases in Alzheimer's disease and beyond

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

21 January 2018

1 reference

https://api.crossref.org/works/10.1126%2FSCITRANSLMED.AAD9704

10.1126/SCITRANSLMED.AAD9704

21 January 2018

Identifiers

DOI

1 reference

10 September 2017

1 reference