Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
about
Combotherapy and current concepts as well as future strategies for the treatment of Alzheimer's diseaseComputational Insights into Substrate and Site Specificities, Catalytic Mechanism, and Protonation States of the Catalytic Asp Dyad of β -SecretasePresumed LRP1-targeting transport peptide delivers β-secretase inhibitor to neurons in vitro with limited efficiencyDiscovery of AZD3839, a Potent and Selective BACE1 Inhibitor Clinical Candidate for the Treatment of Alzheimer DiseaseDiscovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ ReductionDiscovery, Design, and Optimization of Isoxazole Azepine BET InhibitorsInChI in the wild: an assessment of InChIKey searching in GoogleIdentification of an Atg8-Atg3 protein-protein interaction inhibitor from the medicines for Malaria Venture Malaria Box active in blood and liver stage Plasmodium falciparum parasitesBrain pyroglutamate amyloid-β is produced by cathepsin B and is reduced by the cysteine protease inhibitor E64d, representing a potential Alzheimer's disease therapeuticBACE1 inhibition induces a specific cerebrospinal fluid β-amyloid pattern that identifies drug effects in the central nervous systemTracking 20 years of compound-to-target output from literature and patentsAmyloid-precursor-protein-lowering small molecules for disease modifying therapy of Alzheimer's diseaseA tale of two drug targets: the evolutionary history of BACE1 and BACE2Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitorsBACE1 across species: a comparison of the in vivo consequences of BACE1 deletion in mice and ratsPreclinical trials in autosomal dominant AD: implementation of the DIAN-TU trial.Biomarkers in amyloid-β immunotherapy trials in Alzheimer's disease.Recent Progress in Alzheimer's Disease Research, Part 3: Diagnosis and Treatment.CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition.Building a pipeline to discover and validate novel therapeutic targets and lead compounds for Alzheimer's disease.Amyloid β production is regulated by β2-adrenergic signaling-mediated post-translational modifications of the ryanodine receptor.Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects.Therapeutic perspectives of drugs targeting Toll-like receptors based on immune physiopathology theory of Alzheimer's disease.Combined treatment with a BACE inhibitor and anti-Aβ antibody gantenerumab enhances amyloid reduction in APPLondon mice.BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's diseaseLessons from a BACE1 inhibitor trial: off-site but not off base.Targeting the β secretase BACE1 for Alzheimer's disease therapy.Modulation of amyloid precursor protein expression reduces β-amyloid deposition in a mouse model.Striking reduction of amyloid plaque burden in an Alzheimer's mouse model after chronic administration of carmustine.Development of a novel β-secretase binding assay using the AlphaScreen platform.Independent information from cerebrospinal fluid amyloid-β and florbetapir imaging in Alzheimer's diseaseDiurnal patterns of soluble amyloid precursor protein metabolites in the human central nervous system.Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.Alzheimer's Disease: Lessons Learned from Amyloidocentric Clinical Trials.Advances in recent patent and clinical trial drug development for Alzheimer's disease.Electroacupuncture Reduces Aβ Production and BACE1 Expression in SAMP8 Mice.An integrated multi-study analysis of intra-subject variability in cerebrospinal fluid amyloid-β concentrations collected by lumbar puncture and indwelling lumbar catheter.Near-infrared fluorescence molecular imaging of amyloid beta species and monitoring therapy in animal models of Alzheimer's disease.Future Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors.A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.
P2860
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P2860
Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
description
2011 nî lūn-bûn
@nan
2011 թուականի Նոյեմբերին հրատարակուած գիտական յօդուած
@hyw
2011 թվականի նոյեմբերին հրատարակված գիտական հոդված
@hy
2011年の論文
@ja
2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
name
Robust central reduction of am ...... peptidic β-secretase inhibitor
@ast
Robust central reduction of am ...... peptidic β-secretase inhibitor
@en
Robust central reduction of am ...... peptidic β-secretase inhibitor
@nl
type
label
Robust central reduction of am ...... peptidic β-secretase inhibitor
@ast
Robust central reduction of am ...... peptidic β-secretase inhibitor
@en
Robust central reduction of am ...... peptidic β-secretase inhibitor
@nl
prefLabel
Robust central reduction of am ...... peptidic β-secretase inhibitor
@ast
Robust central reduction of am ...... peptidic β-secretase inhibitor
@en
Robust central reduction of am ...... peptidic β-secretase inhibitor
@nl
P2093
P3181
P1476
Robust central reduction of am ...... peptidic β-secretase inhibitor
@en
P2093
Brian M Mathes
Brian M Watson
Celedon R Gonzales
D Greg Hall
David E Timm
David O Calligaro
Dustin J Mergott
Elizabeth Smith Labell
Ferenc Martenyi
James E Audia
P304
16507-16516
P3181
P356
10.1523/JNEUROSCI.3647-11.2011
P407
P577
2011-11-01T00:00:00Z