Future Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors.

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Future Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors. is …
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P356DOI10.1007/S40259-016-0168-3
P698PubMed publication ID27023706

P50authorGenevieve EvinQ89079991
P2093author name stringGenevieve Evin
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A transcriptionally [correction of transcriptively] active complex of APP with Fe65 and histone acetyltransferase Tip60Q28205099
Alzheimer's disease-do tauists and baptists finally shake hands?Q28215968
Control of peripheral nerve myelination by the beta-secretase BACE1Q28264800
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Alzheimer's disease: the amyloid cascade hypothesisQ29547160
Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and gamma-secretase activityQ29616491
The precursor of Alzheimer's disease amyloid A4 protein resembles a cell-surface receptorQ29618322
Immunization with amyloid-beta attenuates Alzheimer-disease-like pathology in the PDAPP mouseQ29619237
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ASP1 (BACE2) cleaves the amyloid precursor protein at the beta-secretase siteQ33925646
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Clinical effects of Abeta immunization (AN1792) in patients with AD in an interrupted trial.Q34417339
The Alzheimer's β-secretase BACE1 localizes to normal presynaptic terminals and to dystrophic presynaptic terminals surrounding amyloid plaques.Q39755143
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Normal cellular processing of the beta-amyloid precursor protein results in the secretion of the amyloid beta peptide and related moleculesQ41526761
Peripherally administered antibodies against amyloid beta-peptide enter the central nervous system and reduce pathology in a mouse model of Alzheimer diseaseQ41753192
Tau deletion impairs intracellular β-amyloid-42 clearance and leads to more extracellular plaque deposition in gene transfer modelsQ42231018
Bace2 is a β cell-enriched protease that regulates pancreatic β cell function and massQ42726932
Bace1 and Neuregulin-1 cooperate to control formation and maintenance of muscle spindlesQ42768388
Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brainQ43516537
Aspartyl protease inhibitor pepstatin binds to the presenilins of Alzheimer's disease.Q43667985
A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activityQ43793656
Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepinesQ44033487
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Beta-secretase protein and activity are increased in the neocortex in Alzheimer diseaseQ44132132
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Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.Q45908140
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An effector-reduced anti-β-amyloid (Aβ) antibody with unique aβ binding properties promotes neuroprotection and glial engulfment of Aβ.Q47393680
Structure-guided design of β-secretase (BACE-1) inhibitorsQ48091068
Beta-site amyloid precursor protein cleaving enzyme 1 levels become elevated in neurons around amyloid plaques: implications for Alzheimer's disease pathogenesisQ48217048
Mechanism of amyloid removal in patients with Alzheimer disease treated with gantenerumabQ48852013
3,4-Dihydro-1,3,5-triazin-2(1H)-ones as the First Dual BACE-1/GSK-3β Fragment Hits against Alzheimer's DiseaseQ50440639
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Vaccine development for Alzheimer's disease: a shot of good news.Q52019724
Safety and biomarker effects of solanezumab in patients with Alzheimer's disease.Q53158136
Candidate .gamma.-Secretases in the Generation of the Carboxyl Terminus of the Alzheimer's Disease .beta.A4 Amyloid: Possible Involvement of Cathepsin DQ53200409
A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity.Q53220934
Alzheimer disease: Solanezumab-prospects for meaningful interventions in AD?Q53369812
Bace1 modulates myelination in the central and peripheral nervous system.Q53588736
The novel BACE inhibitor MK-8931 dramatically lowers CSF beta-amyloid in patients with mild-to-moderate Alzheimer's diseaseQ56566644
Alzheimer's disease risk genes and mechanisms of disease pathogenesisQ34425904
Evidence that tumor necrosis factor alpha converting enzyme is involved in regulated alpha-secretase cleavage of the Alzheimer amyloid protein precursorQ34475374
The β-secretase-derived C-terminal fragment of βAPP, C99, but not Aβ, is a key contributor to early intraneuronal lesions in triple-transgenic mouse hippocampusQ34477111
Reduced sodium channel Na(v)1.1 levels in BACE1-null miceQ34624269
BACE inhibitors as potential therapeutics for Alzheimer's diseaseQ34655697
Mild oxidative stress induces redistribution of BACE1 in non-apoptotic conditions and promotes the amyloidogenic processing of Alzheimer's disease amyloid precursor proteinQ34684198
Immunological approaches as therapy for Alzheimer's diseaseQ35040852
Axonal and Schwann cell BACE1 is equally required for remyelination of peripheral nervesQ35142894
Long-term treatment with active Aβ immunotherapy with CAD106 in mild Alzheimer's diseaseQ35540628
Developing β-secretase inhibitors for treatment of Alzheimer's diseaseQ35746998
η-Secretase processing of APP inhibits neuronal activity in the hippocampusQ35760228
The gamma-secretase complex: machinery for intramembrane proteolysisQ35803148
Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3β InhibitorsQ35876179
The mechanism of γ-Secretase dysfunction in familial Alzheimer diseaseQ36000134
Amyloid-β 11C-PiB-PET imaging results from 2 randomized bapineuzumab phase 3 AD trialsQ36005648
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic miceQ36027275
Secretome protein enrichment identifies physiological BACE1 protease substrates in neuronsQ36103683
The neural cell adhesion molecules L1 and CHL1 are cleaved by BACE1 protease in vivoQ36122127
Qualitative changes in human γ-secretase underlie familial Alzheimer's diseaseQ36286058
β-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigmentQ36379519
TRPC6 specifically interacts with APP to inhibit its cleavage by γ-secretase and reduce Aβ production.Q36417516
BACE1 is at the crossroad of a toxic vicious cycle involving cellular stress and β-amyloid production in Alzheimer's diseaseQ36427048
Unusual phenotypic alteration of beta amyloid precursor protein (betaAPP) maturation by a new Val-715 --> Met betaAPP-770 mutation responsible for probable early-onset Alzheimer's diseaseQ36459592
The role of γ-secretase activating protein (GSAP) and imatinib in the regulation of γ-secretase activity and amyloid-β generationQ36562023
A contrast in safety, pharmacokinetics and pharmacodynamics across age groups after a single 50 mg oral dose of the γ-secretase inhibitor avagacestatQ36562466
Systematic proteomic analysis identifies β-site amyloid precursor protein cleaving enzyme 2 and 1 (BACE2 and BACE1) substrates in pancreatic β-cellsQ36760343
Amyloid-beta protein clearance and degradation (ABCD) pathways and their role in Alzheimer's diseaseQ36764094
BACE2 processes PMEL to form the melanosome amyloid matrix in pigment cellsQ36967843
AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate KineticsQ37053876
Peripheral anti-A beta antibody alters CNS and plasma A beta clearance and decreases brain A beta burden in a mouse model of Alzheimer's diseaseQ37118356
Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer diseaseQ37192883
A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous systemQ37316153
Mutations in amyloid precursor protein affect its interactions with presenilin/gamma-secretaseQ37319340
BACE1 regulates voltage-gated sodium channels and neuronal activityQ37355641
P433issue3
P921main subjectAlzheimer's diseaseQ11081
P304page(s)173-194
P577publication date2016-06-01
P1433published inBioDrugsQ4914612
P1476titleFuture Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors
P478volume30

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