A Close Look at BACE1 Inhibitors for Alzheimer’s Disease Treatment

Physiological Aβ Concentrations Produce a More Biomimetic Representation of the Alzheimer’s Disease Phenotype in iPSC Derived Human Neurons

(2018) Bonnie J. Berry et al.   ACS Chemical Neuroscience

Synaptic vesicle cycle and amyloid β: Biting the hand that feeds

(2018) Saak V. Ovsepian et al.   Alzheimers & Dementia

Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function

(2018) Kaichuan Zhu et al.   BIOLOGICAL PSYCHIATRY

Microglia-Mediated Neuroprotection, TREM2 , and Alzheimer’s Disease: Evidence From Optical Imaging

(2018) Carlo Condello et al.   BIOLOGICAL PSYCHIATRY

Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibition Impairs Synaptic Plasticity via Seizure Protein 6

(2018) Kaichuan Zhu et al.   BIOLOGICAL PSYCHIATRY

Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead

(2018) Devendra Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

BACE1 deletion in the adult mouse reverses preformed amyloid deposition and improves cognitive functions

(2018) Xiangyou Hu et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Click chemistry-mediated biotinylation reveals a function for the protease BACE1 in modulating the neuronal surface glycoproteome

(2018) Julia Herber et al.   MOLECULAR & CELLULAR PROTEOMICS

BACE1 elevation engendered by GGA3 deletion increases β-amyloid pathology in association with APP elevation and decreased CHL1 processing in 5XFAD mice

(2018) WonHee Kim et al.   Molecular Neurodegeneration

Reactive astrocytes in Alzheimer’s disease: A double-edged sword

(2018) Heejung Chun et al.   NEUROSCIENCE RESEARCH

Randomized Trial of Verubecestat for Mild-to-Moderate Alzheimer’s Disease

(2018) Michael F. Egan et al.   NEW ENGLAND JOURNAL OF MEDICINE

BACE1-cleavage of Sez6 and Sez6L is elevated in Niemann-Pick type C disease mouse brains

(2018) Mirsada Causevic et al.   PLoS One

Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment

(2018) Judite R. M. Coimbra et al.   Frontiers in Chemistry

The BACE‐1 inhibitor CNP520 for prevention trials in Alzheimer's disease

(2018) Ulf Neumann et al.   EMBO Molecular Medicine

Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer’s disease: randomized, double-blind, placebo-controlled study

(2018) Maarten Timmers et al.   Alzheimers Research & Therapy

A promising, novel, and unique BACE1 inhibitor emerges in the quest to prevent Alzheimer's disease

(2018) Justyna A Dobrowolska Zakaria et al.   EMBO Molecular Medicine

Amyloid-Beta and Phosphorylated Tau Accumulations Cause Abnormalities at Synapses of Alzheimer’s disease Neurons

(2017) Ravi Rajmohan et al.   JOURNAL OF ALZHEIMERS DISEASE

BACE1 Inhibitor Lanabecestat (AZD3293) in a Phase 1 Study of Healthy Japanese Subjects: Pharmacokinetics and Effects on Plasma and Cerebrospinal Fluid Aβ Peptides

(2017) Kei Sakamoto et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Apolipoprotein E and Alzheimer’s disease: the influence of apolipoprotein E on amyloid-β and other amyloidogenic proteins

(2017) Tien-Phat V. Huynh et al.   JOURNAL OF LIPID RESEARCH

BACE1 Cleavage Site Selection Critical for Amyloidogenesis and Alzheimer's Pathogenesis

(2017) Shuting Zhang et al.   JOURNAL OF NEUROSCIENCE

Gene-environment interaction between lead and Apolipoprotein E4 causes cognitive behavior deficits in mice

(2017) Anna K. Engstrom et al.   Molecular Neurodegeneration

The release and trans-synaptic transmission of Tau via exosomes

(2017) Yipeng Wang et al.   Molecular Neurodegeneration

Late onset Alzheimer’s disease genetics implicates microglial pathways in disease risk

(2017) Anastasia G. Efthymiou et al.   Molecular Neurodegeneration

Aβ accumulation causes MVB enlargement and is modelled by dominant negative VPS4A

(2017) Katarina Willén et al.   Molecular Neurodegeneration

Soluble oligomeric amyloid-β induces calcium dyshomeostasis that precedes synapse loss in the living mouse brain

(2017) Michal Arbel-Ornath et al.   Molecular Neurodegeneration

BACE1 Function and Inhibition: Implications of Intervention in the Amyloid Pathway of Alzheimer’s Disease Pathology

(2017) Gerald Koelsch   MOLECULES

Alzheimer's Disease–Related Dementias Summit 2016: National research priorities

(2017) Roderick A. Corriveau et al.   NEUROLOGY

Diagnostic impact of [18F]flutemetamol PET in early-onset dementia

(2017) Marissa D. Zwan et al.   Alzheimers Research & Therapy

The role of astrocytes in amyloid production and Alzheimer's disease

(2017) Georgia R. Frost et al.   Open Biology

Role of BACE1 in Alzheimer’s synaptic function

(2017) Brati Das et al.   Translational Neurodegeneration

Amyloid-β as a Modulator of Synaptic Plasticity

(2017) Mordhwaj S. Parihar et al.   JOURNAL OF ALZHEIMERS DISEASE

Preclinical Alzheimer's disease: Definition, natural history, and diagnostic criteria

(2016) Bruno Dubois et al.   Alzheimers & Dementia

RESULTS FROM A FIRST-IN-HUMAN STUDY WITH THE BACE INHIBITOR CNP520

(2016) Mike Ufer et al.   Alzheimers & Dementia

TDP-43 stage, mixed pathologies, and clinical Alzheimer’s-type dementia

(2016) Bryan D. James et al.   BRAIN

Physiological and pathological roles of the γ-secretase complex

(2016) Courtney M. Carroll et al.   BRAIN RESEARCH BULLETIN

Ion channel regulation by β-secretase BACE1 – enzymatic and non-enzymatic effects beyond Alzheimer's disease

(2016) Sandra Lehnert et al.   Channels

Alzheimer's disease: A review from the pathophysiology to diagnosis, new perspectives for pharmacological treatment

(2016) Leide dos Santos Picanç et al.   CURRENT MEDICINAL CHEMISTRY

The amyloid hypothesis of Alzheimer's disease at 25 years

(2016) Dennis J Selkoe et al.   EMBO Molecular Medicine

AZD3293: Pharmacokinetic and Pharmacodynamic Effects in Healthy Subjects and Patients with Alzheimer’s Disease

(2016) Gvido Cebers et al.   JOURNAL OF ALZHEIMERS DISEASE

AZD3293: A Novel, Orally Active BACE1 Inhibitor with High Potency and Permeability and Markedly Slow Off-Rate Kinetics

(2016) Susanna Eketjäll et al.   JOURNAL OF ALZHEIMERS DISEASE

Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

(2016) Jack D. Scott et al.   JOURNAL OF MEDICINAL CHEMISTRY

Functions of the Alzheimer’s Disease Protease BACE1 at the Synapse in the Central Nervous System

(2016) Kathryn M. Munro et al.   JOURNAL OF MOLECULAR NEUROSCIENCE

Acetylated tau destabilizes the cytoskeleton in the axon initial segment and is mislocalized to the somatodendritic compartment

(2016) Peter Dongmin Sohn et al.   Molecular Neurodegeneration

Alzheimer’s disease-like APP processing in wild-type mice identifies synaptic defects as initial steps of disease progression

(2016) Mickael Audrain et al.   Molecular Neurodegeneration

Inhibiting BACE1 to reverse synaptic dysfunctions in Alzheimer’s disease

(2016) Riqiang Yan et al.   NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS  -amyloid in animal models and in Alzheimers disease patients

(2016) M. E. Kennedy et al.   Science Translational Medicine

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

(2016) Andrea M. Zuhl et al.   Nature Communications

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

(2016) Derya R. Shimshek et al.   Scientific Reports

Specific Inhibition of β-Secretase Processing of the Alzheimer Disease Amyloid Precursor Protein

(2016) Saoussen Ben Halima et al.   Cell Reports

Stepping closer to treating Alzheimer’s disease patients with BACE1 inhibitor drugs

(2016) Riqiang Yan   Translational Neurodegeneration

Pharmacological Inhibition of BACE1 Impairs Synaptic Plasticity and Cognitive Functions

(2015) Severin Filser et al.   BIOLOGICAL PSYCHIATRY

Neurological dysfunctions associated with altered BACE1-dependent Neuregulin-1 signaling

(2015) Xiangyou Hu et al.   JOURNAL OF NEUROCHEMISTRY

Genetic Disorders with Tau Pathology: A Review of the Literature and Report of Two Patients with Tauopathy and Positive Family Histories

(2015) Pawel Tacik et al.   Neurodegenerative Diseases

Swedish mutant APP-based BACE1 binding site peptide reduces APP β-cleavage and cerebral Aβ levels in Alzheimer’s mice

(2015) Song Li et al.   Scientific Reports

Long-term treatment with active Aβ immunotherapy with CAD106 in mild Alzheimer’s disease

(2015) Martin R Farlow et al.   Alzheimers Research & Therapy

TDP-43 is a key player in the clinical features associated with Alzheimer’s disease

(2014) Keith A. Josephs et al.   ACTA NEUROPATHOLOGICA

CSF amyloid lowering in human volunteers after 14 days’ oral administration of the novel BACE1 inhibitor E2609

(2014) Bruce Albala et al.   Alzheimers & Dementia

Lessons from a BACE1 inhibitor trial: Off-site but not off base

(2014) Debomoy K. Lahiri et al.   Alzheimers & Dementia

The evolution of amidine-based brain penetrant BACE1 inhibitors

(2014) Daniel Oehlrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Lessons from a Failed γ-Secretase Alzheimer Trial

(2014) Bart De Strooper   CELL

BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease

(2014) Arun K. Ghosh et al.   CHEMICAL SOCIETY REVIEWS

Tau Protein Modifications and Interactions: Their Role in Function and Dysfunction

(2014) Anna Mietelska-Porowska et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

β-Site Amyloid Precursor Protein Cleaving Enzyme 1(BACE1) Regulates Notch Signaling by Controlling the Cleavage of Jagged 1 (Jag1) and Jagged 2 (Jag2) Proteins

(2014) Wanxia He et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular Mechanisms of Alzheimer Disease Protection by the A673T Allele of Amyloid Precursor Protein

(2014) Janice A. Maloney et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting the β secretase BACE1 for Alzheimer's disease therapy

(2014) Riqiang Yan et al.   LANCET NEUROLOGY

BACE1 activity regulates cell surface contactin-2 levels

(2014) Vivek Gautam et al.   Molecular Neurodegeneration

Oligomeric Aβ-induced synaptic dysfunction in Alzheimer’s disease

(2014) Shichun Tu et al.   Molecular Neurodegeneration

Neuregulin-ERBB Signaling in the Nervous System and Neuropsychiatric Diseases

(2014) Lin Mei et al.   NEURON

Postsynaptic Target Specific Synaptic Dysfunctions in the CA3 Area of BACE1 Knockout Mice

(2014) Hui Wang et al.   PLoS One

BACE1 inhibitor drugs in clinical trials for Alzheimer’s disease

(2014) Robert Vassar   Alzheimers Research & Therapy

Comparative analysis of single and combined APP/APLP knockouts reveals reduced spine density in APP-KO mice that is prevented by APPsα expression

(2014) Sascha W Weyer et al.   Acta Neuropathologica Communications

The Alzheimer’s β-secretase BACE1 localizes to normal presynaptic terminals and to dystrophic presynaptic terminals surrounding amyloid plaques

(2013) Patty C. Kandalepas et al.   ACTA NEUROPATHOLOGICA

Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story

(2013) Andrew Stamford et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Allosteric inhibition of BACE1 by an exosite-binding antibody

(2013) Weiru Wang et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

BACE1 and presenilin/γ-secretase regulate proteolytic processing of KCNE1 and 2, auxiliary subunits of voltage-gated potassium channels

(2013) Carolyn C. Sachse et al.   FASEB JOURNAL

Structure-Based Design of β-Site APP Cleaving Enzyme 1 (BACE1) Inhibitors for the Treatment of Alzheimer’s Disease

(2013) Jing Yuan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dual Cleavage of Neuregulin 1 Type III by BACE1 and ADAM17 Liberates Its EGF-Like Domain and Allows Paracrine Signaling

(2013) D. Fleck et al.   JOURNAL OF NEUROSCIENCE

Amyloid-β and APP Deficiencies Cause Severe Cerebrovascular Defects: Important Work for an Old Villain

(2013) Salvadore Luna et al.   PLoS One

BACE1 Regulates Hippocampal Astrogenesis via the Jagged1-Notch Pathway

(2013) Xiangyou Hu et al.   Cell Reports

Proteolytic Degradation of Amyloid  -Protein

(2013) T. Saido et al.   Cold Spring Harbor Perspectives in Medicine

Cross-sectional and Longitudinal Analysis of the Relationship Between Aβ Deposition, Cortical Thickness, and Memory in Cognitively Unimpaired Individuals and in Alzheimer Disease

(2013) Vincent Doré et al.   JAMA Neurology

Novel peptidomimetics as BACE-1 inhibitors: Synthesis, molecular modeling, and biological studies

(2012) Stefania Butini et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Secretome protein enrichment identifies physiological BACE1 protease substrates in neurons

(2012) Peer-Hendrik Kuhn et al.   EMBO JOURNAL

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

(2012) Jun Cai et al.   EMBO Molecular Medicine

Familial Alzheimer Disease Presenilin-1 Mutations Alter the Active Site Conformation of γ-secretase

(2012) De-Ming Chau et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

β-Site Amyloid Precursor Protein (APP)-cleaving Enzyme 1 (BACE1)-deficient Mice Exhibit a Close Homolog of L1 (CHL1) Loss-of-function Phenotype Involving Axon Guidance Defects

(2012) Brian Hitt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Neural Cell Adhesion Molecules L1 and CHL1 Are Cleaved by BACE1 Proteasein Vivo

(2012) Lujia Zhou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of plasma β-secretase (BACE1) activity and soluble amyloid precursor proteins as potential biomarkers for Alzheimer's disease

(2012) Guoxin Wu et al.   JOURNAL OF NEUROSCIENCE RESEARCH

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

(2012) Thorlakur Jonsson et al.   NATURE

Reduction in BACE1 decreases body weight, protects against diet-induced obesity and enhances insulin sensitivity in mice

(2011) Paul J. Meakin et al.   BIOCHEMICAL JOURNAL

Developing β-secretase inhibitors for treatment of Alzheimer’s disease

(2011) Arun K. Ghosh et al.   JOURNAL OF NEUROCHEMISTRY

Soluble Aβ oligomer production and toxicity

(2011) Megan E. Larson et al.   JOURNAL OF NEUROCHEMISTRY

Aβ-Degrading Enzymes: Potential for Treatment of Alzheimer Disease

(2011) James Scott Miners et al.   JOURNAL OF NEUROPATHOLOGY AND EXPERIMENTAL NEUROLOGY

Reduced BACE1 Activity Enhances Clearance of Myelin Debris and Regeneration of Axons in the Injured Peripheral Nervous System

(2011) M. H. Farah et al.   JOURNAL OF NEUROSCIENCE

Robust Central Reduction of Amyloid-  in Humans with an Orally Available, Non-Peptidic  -Secretase Inhibitor

(2011) P. C. May et al.   JOURNAL OF NEUROSCIENCE

An update on the toxicity of Aβ in Alzheimer’s disease

(2011) Jurgen Gotz   Neuropsychiatric Disease and Treatment

Tau in Alzheimer Disease and Related Tauopathies

(2010) K. Iqbal et al.   Current Alzheimer Research

Processing of the Synaptic Cell Adhesion Molecule Neurexin-3β by Alzheimer Disease α- and γ-Secretases

(2010) Nathalie Bot et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The secretases: enzymes with therapeutic potential in Alzheimer disease

(2010) Bart De Strooper et al.   Nature Reviews Neurology

Predicting memapsin 2 (β-secretase) hydrolytic activity

(2010) Xiaoman Li et al.   PROTEIN SCIENCE

Bridging Physiology and Pathology in AD

(2009) Dohoon Kim et al.   CELL

Targeting Aβ and tau in Alzheimer's disease, an early interim report

(2009) Todd E. Golde et al.   EXPERIMENTAL NEUROLOGY

The  -Secretase Enzyme BACE in Health and Alzheimer's Disease: Regulation, Cell Biology, Function, and Therapeutic Potential

(2009) R. Vassar et al.   JOURNAL OF NEUROSCIENCE

Alzheimer's disease: synaptic dysfunction and Aβ

(2009) Ganesh M Shankar et al.   Molecular Neurodegeneration

The Role of Apolipoprotein E in Alzheimer's Disease

(2009) Jungsu Kim et al.   NEURON

Synchronous Hyperactivity and Intercellular Calcium Waves in Astrocytes in Alzheimer Mice

(2009) K. V. Kuchibhotla et al.   SCIENCE

Function, regulation and therapeutic properties of β-secretase (BACE1)

(2009) Michael Willem et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Oxidative Stress Signaling in Alzheimers Disease

(2008) B. Su et al.   Current Alzheimer Research

BACE1 Knock-Outs Display Deficits in Activity-Dependent Potentiation of Synaptic Transmission at Mossy Fiber to CA3 Synapses in the Hippocampus

(2008) H. Wang et al.   JOURNAL OF NEUROSCIENCE

Rapid Microglial Response Around Amyloid Pathology after Systemic Anti-A  Antibody Administration in PDAPP Mice

(2008) J. Koenigsknecht-Talboo et al.   JOURNAL OF NEUROSCIENCE

Endocytosis Is Required for Synaptic Activity-Dependent Release of Amyloid-β In Vivo

(2008) John R. Cirrito et al.   NEURON

Linking Calcium to Aβ and Alzheimer's Disease

(2008) Kim N. Green et al.   NEURON

β-Secretase as a therapeutic target for Alzheimer’s disease

(2008) Arun K. Ghosh et al.   Neurotherapeutics

Stereologic estimates of total spinophilin-immunoreactive spine number in area 9 and the CA1 field: Relationship with the progression of Alzheimer's disease

(2007) Afia Akram et al.   NEUROBIOLOGY OF AGING