Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects

Axonal BACE1 dynamics and targeting in hippocampal neurons: a role for Rab11 GTPase

(2014) Virginie Buggia-Prévot et al.   Molecular Neurodegeneration

A Paired RNAi and RabGAP Overexpression Screen Identifies Rab11 as a Regulator of β-Amyloid Production

(2014) Vinod Udayar et al.   Cell Reports

A Function for EHD Family Proteins in Unidirectional Retrograde Dendritic Transport of BACE1 and Alzheimer’s Disease Aβ Production

(2014) Virginie Buggia-Prévot et al.   Cell Reports

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

Bace1 and Neuregulin-1 cooperate to control formation and maintenance of muscle spindles

(2013) Cyril Cheret et al.   EMBO JOURNAL

Increased Expression of Reticulon 3 in Neurons Leads to Reduced Axonal Transport of β Site Amyloid Precursor Protein-cleaving Enzyme 1

(2013) Minzi Deng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Systematic Proteomic Analysis Identifies β-Site Amyloid Precursor Protein Cleaving Enzyme 2 and 1 (BACE2 and BACE1) Substrates in Pancreatic β-Cells

(2013) Ina Stützer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Loss of Bace2 in zebrafish affects melanocyte migration and is distinct from Bace1 knock out phenotypes

(2013) Frauke van Bebber et al.   JOURNAL OF NEUROCHEMISTRY

Intramembranous Valine Linked to Schizophrenia Is Required for Neuregulin 1 Regulation of the Morphological Development of Cortical Neurons

(2013) Y. Chen et al.   JOURNAL OF NEUROSCIENCE

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

Genetics of dementia

(2013) Clement T Loy et al.   LANCET

Validating therapeutic targets through human genetics

(2013) Robert M. Plenge et al.   NATURE REVIEWS DRUG DISCOVERY

A Matter of Balance: Role of Neurexin and Neuroligin at the Synapse

(2013) Marie Louise Bang et al.   NEUROCHEMICAL RESEARCH

ADAM10 Missense Mutations Potentiate β-Amyloid Accumulation by Impairing Prodomain Chaperone Function

(2013) Jaehong Suh et al.   NEURON

A Phase 3 Trial of Semagacestat for Treatment of Alzheimer's Disease

(2013) Rachelle S. Doody et al.   NEW ENGLAND JOURNAL OF MEDICINE

Altered Social Behaviours in Neurexin 1α Knockout Mice Resemble Core Symptoms in Neurodevelopmental Disorders

(2013) Hannah Mary Grayton et al.   PLoS One

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

(2013) L. Rochin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Addressing Safety Liabilities of TfR Bispecific Antibodies That Cross the Blood-Brain Barrier

(2013) J. A. Couch et al.   Science Translational Medicine

BACE1 Regulates Hippocampal Astrogenesis via the Jagged1-Notch Pathway

(2013) Xiangyou Hu et al.   Cell Reports

The Genetics of Alzheimer Disease

(2013) R. E. Tanzi   Cold Spring Harbor Perspectives in Medicine

Molecular mechanisms of cognitive dysfunction following traumatic brain injury

(2013) Kendall R. Walker et al.   Frontiers in Aging Neuroscience

Safety and Tolerability of the γ-Secretase Inhibitor Avagacestat in a Phase 2 Study of Mild to Moderate Alzheimer Disease

(2012) Vladimir Coric et al.   ARCHIVES OF NEUROLOGY

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

(2012) Jared N. Cumming et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Multicenter, Randomized, Double-Blind, Placebo-Controlled, Single-Ascending Dose Study of the Oral γ-Secretase Inhibitor BMS-708163 (Avagacestat): Tolerability Profile, Pharmacokinetic Parameters, and Pharmacodynamic Markers

(2012) Gary Tong et al.   CLINICAL THERAPEUTICS

BACE1 Dependent Neuregulin Processing: Review

(2012) Daniel Fleck et al.   Current Alzheimer Research

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

High Affinity Neurexin Binding to Cell Adhesion G-protein-coupled Receptor CIRL1/Latrophilin-1 Produces an Intercellular Adhesion Complex

(2012) Antony A. Boucard 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

BACE1 Protein Endocytosis and Trafficking Are Differentially Regulated by Ubiquitination at Lysine 501 and the Di-leucine Motif in the Carboxyl Terminus

(2012) Eugene L. Kang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Adaptor protein 2–mediated endocytosis of the β-secretase BACE1 is dispensable for amyloid precursor protein processing

(2012) Yogikala Prabhu et al.   MOLECULAR BIOLOGY OF THE CELL

BACE1 is at the crossroad of a toxic vicious cycle involving cellular stress and β-amyloid production in Alzheimer’s disease

(2012) Linda Chami et al.   Molecular Neurodegeneration

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

(2012) Thorlakur Jonsson et al.   NATURE

Retromers in Alzheimer’s Disease

(2012) Barbara M. Siegenthaler et al.   Neurodegenerative Diseases

Activity-Dependent Proteolytic Cleavage of Neuroligin-1

(2012) Kunimichi Suzuki et al.   NEURON

Clinical and Biomarker Changes in Dominantly Inherited Alzheimer's Disease

(2012) Randall J. Bateman et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2012) Andrew W. Stamford et al.   ACS Medicinal Chemistry Letters

The precision of axon targeting of mouse olfactory sensory neurons requires the BACE1 protease

(2012) Luxiang Cao et al.   Scientific Reports

The Membrane-Bound Aspartyl Protease BACE1: Molecular and Functional Properties in Alzheimer’s Disease and Beyond

(2012) Bastian Dislich et al.   Frontiers in Physiology

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

Bace2 Is a β Cell-Enriched Protease that Regulates Pancreatic β Cell Function and Mass

(2011) Daria Esterházy et al.   Cell Metabolism

APP and APLP2 are essential at PNS and CNS synapses for transmission, spatial learning and LTP

(2011) Sascha W Weyer et al.   EMBO JOURNAL

Cleavage of Neuregulin-1 by BACE1 or ADAM10 Protein Produces Differential Effects on Myelination

(2011) Xiaoyang Luo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

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

Identification of BACE1 cleavage sites in human voltage-gated sodium channel beta 2 subunit

(2011) Manuel T Gersbacher et al.   Molecular Neurodegeneration

The Alzheimer's β-secretase enzyme BACE1 is required for accurate axon guidance of olfactory sensory neurons and normal glomerulus formation in the olfactory bulb

(2011) Tharinda W Rajapaksha et al.   Molecular Neurodegeneration

TACE (ADAM17) inhibits Schwann cell myelination

(2011) Rosa La Marca et al.   NATURE NEUROSCIENCE

ADP ribosylation factor 6 (ARF6) controls amyloid precursor protein (APP) processing by mediating the endosomal sorting of BACE1

(2011) R. Sannerud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Therapeutic Antibody Targeting BACE1 Inhibits Amyloid-  Production in Vivo

(2011) J. K. Atwal et al.   Science Translational Medicine

Boosting Brain Uptake of a Therapeutic Antibody by Reducing Its Affinity for a Transcytosis Target

(2011) Y. J. Yu et al.   Science Translational Medicine

ADAM10 is the physiologically relevant, constitutive α-secretase of the amyloid precursor protein in primary neurons

(2010) Peer-Hendrik Kuhn et al.   EMBO JOURNAL

Ubiquitin Regulates GGA3-mediated Degradation of BACE1

(2010) Eugene L. Kang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Secretion Stimulates Intramembrane Proteolysis of a Secretory Granule Membrane Enzyme

(2010) Chitra Rajagopal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Reduced Sodium Channel Nav1.1 Levels in BACE1-null Mice

(2010) Doo Yeon Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Cyclic Acylguanidines as Highly Potent and Selective β-Site Amyloid Cleaving Enzyme (BACE) Inhibitors: Part I—Inhibitor Design and Validation∥(1)

(2010) Zhaoning Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

(2010) Yu-Sen Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bepridil and Amiodarone Simultaneously Target the Alzheimer's Disease  - and  -Secretase via Distinct Mechanisms

(2010) S. Mitterreiter et al.   JOURNAL OF NEUROSCIENCE

The Disintegrin/Metalloproteinase ADAM10 Is Essential for the Establishment of the Brain Cortex

(2010) E. Jorissen et al.   JOURNAL OF NEUROSCIENCE

BACE1 Deficiency Causes Altered Neuronal Activity and Neurodegeneration

(2010) X. Hu et al.   JOURNAL OF NEUROSCIENCE

Peptidylgycine α-amidating monooxygenase and copper: A gene-nutrient interaction critical to nervous system function

(2010) Danielle Bousquet-Moore et al.   JOURNAL OF NEUROSCIENCE RESEARCH

Drugs for AIDS

(2010) S. Ray et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

BACE1-/- mice exhibit seizure activity that does not correlate with sodium channel level or axonal localization

(2010) Brian D. Hitt et al.   Molecular Neurodegeneration

Biomarkers in Alzheimer's disease drug development

(2010) Kaj Blennow   NATURE MEDICINE

The secretases: enzymes with therapeutic potential in Alzheimer disease

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

Neural Map Formation in the Mouse Olfactory System

(2010) Hitoshi Sakano   NEURON

Soluble amyloid precursor protein (APP) regulates transthyretin and Klotho gene expression without rescuing the essential function of APP

(2010) H. Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A γ-secretase inhibitor decreases amyloid-β production in the central nervous system

(2009) Randall J. Bateman et al.   ANNALS OF NEUROLOGY

The LDL Receptor

(2009) Joseph L. Goldstein et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Fragment-Based Discovery of Nonpeptidic BACE-1 Inhibitors Using Tethering

(2009) Wenjin Yang et al.   BIOCHEMISTRY

Translational Medicine Lessons from Flurizan's Failure in Alzheimer's Disease (AD) Trial: Implication for Future Drug Discovery and Development for AD

(2009) Hong I. Wan et al.   CTS-Clinical and Translational Science

N-terminal Domains Elicit Formation of Functional Pmel17 Amyloid Fibrils

(2009) Brenda Watt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Amyloid Precursor Protein Regulates Cav1.2 L-type Calcium Channel Levels and Function to Influence GABAergic Short-Term Plasticity

(2009) L. Yang et al.   JOURNAL OF NEUROSCIENCE

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

Identification of β-Secretase (BACE1) Substrates Using Quantitative Proteomics

(2009) Matthew L. Hemming et al.   PLoS One

Mouse neurexin-1  deletion causes correlated electrophysiological and behavioral changes consistent with cognitive impairments

(2009) M. R. Etherton et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Recessive Mutation in the APP Gene with Dominant-Negative Effect on Amyloidogenesis

(2009) G. Di Fede et al.   SCIENCE

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

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

Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves

(2008) Xiangyou Hu et al.   FASEB JOURNAL

Increased anxiety-like behavior in mice lacking the inhibitory synapse cell adhesion molecule neuroligin 2

(2008) J. Blundell et al.   GENES BRAIN AND BEHAVIOR

Neuregulin-1, a key axonal signal that drives Schwann cell growth and differentiation

(2008) Carmen Birchmeier et al.   GLIA

Alzheimer Disease Aβ Production in the Absence ofS-Palmitoylation-dependent Targeting of BACE1 to Lipid Rafts

(2008) Kulandaivelu S. Vetrivel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Two Endoplasmic Reticulum (ER)/ER Golgi Intermediate Compartment-based Lysine Acetyltransferases Post-translationally Regulate BACE1 Levels

(2008) Mi Hee Ko et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Flotillin-Dependent Clustering of the Amyloid Precursor Protein Regulates Its Endocytosis and Amyloidogenic Processing in Neurons

(2008) A. Schneider et al.   JOURNAL OF NEUROSCIENCE

First Demonstration of Cerebrospinal Fluid and Plasma A  Lowering with Oral Administration of a  -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates

(2008) S. Sankaranarayanan et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Impairment of learning and memory in TAG-1 deficient mice associated with shorter CNS internodes and disrupted juxtaparanodes

(2008) Maria Savvaki et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

Aliskiren: the first renin inhibitor for clinical treatment

(2008) Chris Jensen et al.   NATURE REVIEWS DRUG DISCOVERY

Abnormal axonal guidance and brain anatomy in mouse mutants for the cell recognition molecules close homolog of L1 and NgCAM-related cell adhesion molecule

(2008) A. Heyden et al.   NEUROSCIENCE

Deficiency of Aph1B/C- -secretase disturbs Nrg1 cleavage and sensorimotor gating that can be reversed with antipsychotic treatment

(2008) T. Dejaegere et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Reduced social interaction and ultrasonic communication in a mouse model of monogenic heritable autism

(2008) S. Jamain et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Alteration of BACE1-dependent NRG1/ErbB4 signaling and schizophrenia-like phenotypes in BACE1-null mice

(2008) A. V. Savonenko et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Neuroligin-1 is required for normal expression of LTP and associative fear memory in the amygdala of adult animals

(2008) Juhyun Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Efficient Inhibition of the Alzheimer's Disease  -Secretase by Membrane Targeting

(2008) L. Rajendran et al.   SCIENCE

BACE1 gene deletion: Impact on behavioral function in a model of Alzheimer's disease

(2007) Dione Kobayashi et al.   NEUROBIOLOGY OF AGING