Investigational BACE inhibitors for the treatment of Alzheimer’s disease

Treatment Combinations for Alzheimer’s Disease: Current And Future Pharmacotherapy Options

(2019) Jeffrey L. Cummings et al.   JOURNAL OF ALZHEIMERS DISEASE

Genome-wide meta-analysis identifies new loci and functional pathways influencing Alzheimer’s disease risk

(2019) Iris E. Jansen et al.   NATURE GENETICS

A critical appraisal of amyloid-β-targeting therapies for Alzheimer disease

(2019) Francesco Panza et al.   Nature Reviews Neurology

Cover Feature: Highly Selective and Potent Human β-Secretase 2 (BACE2) Inhibitors against Type 2 Diabetes: Design, Synthesis, X-ray Structure and Structure-Activity Relationship Studies (ChemMedChem 5/2019)

(2019) Arun K. Ghosh et al.   ChemMedChem

Preliminary Results of a Trial of Atabecestat in Preclinical Alzheimer’s Disease

(2019) David Henley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Randomized Trial of Verubecestat for Prodromal Alzheimer’s Disease

(2019) Michael F. Egan et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Large Panel of Isogenic APP and PSEN1 Mutant Human iPSC Neurons Reveals Shared Endosomal Abnormalities Mediated by APP β-CTFs, Not Aβ

(2019) Dylan Kwart et al.   NEURON

Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function

(2018) Kaichuan Zhu 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

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

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

Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment

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

Lifestyle interventions to prevent cognitive impairment, dementia and Alzheimer disease

(2018) Miia Kivipelto et al.   Nature Reviews Neurology

Amyloid-β Peptide Is Needed for cGMP-Induced Long-Term Potentiation and Memory

(2017) Agostino Palmeri et al.   JOURNAL OF NEUROSCIENCE

Stop Alzheimer’s before it starts

(2017) Eric McDade et al.   NATURE

BACE inhibition-dependent repair of Alzheimer’s pathophysiology

(2017) Aylin D. Keskin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Physiological Functions of the β-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2

(2017) Riqiang Yan   Frontiers in Molecular Neuroscience

Amyloid-β as a Modulator of Synaptic Plasticity

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

A Physiological Role for Amyloid-β Protein: Enhancement of Learning and Memory

(2017) John E. Morley et al.   JOURNAL OF ALZHEIMERS DISEASE

Neuronal human BACE1 knockin induces systemic diabetes in mice

(2016) Kaja Plucińska et al.   DIABETOLOGIA

Analysis of 138 pathogenic mutations in presenilin-1 on the in vitro production of Aβ42 and Aβ40 peptides by γ-secretase

(2016) Linfeng Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Alzheimer’s disease due to loss of function: A new synthesis of the available data

(2016) Kasper P. Kepp   PROGRESS IN NEUROBIOLOGY

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

Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice

(2015) D. R. Thakker et al.   JOURNAL OF NEUROSCIENCE

The keystone of Alzheimer pathogenesis might be sought in Aβ physiology

(2015) D. Puzzo et al.   NEUROSCIENCE

Targeting Prodromal Alzheimer Disease With Avagacestat

(2015) Vladimir Coric et al.   JAMA Neurology

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

(2014) Robert Vassar et al.   JOURNAL OF NEUROCHEMISTRY

Regulation of Presynaptic Ca2+, Synaptic Plasticity and Contextual Fear Conditioning by a N-terminal  -Amyloid Fragment

(2014) J. L. M. Lawrence et al.   JOURNAL OF NEUROSCIENCE

Knock-In of Human BACE1 Cleaves Murine APP and Reiterates Alzheimer-like Phenotypes

(2014) K. Pluci ska et al.   JOURNAL OF NEUROSCIENCE

Targeting the β secretase BACE1 for Alzheimer's disease therapy

(2014) Riqiang Yan et al.   LANCET NEUROLOGY

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

Apolipoprotein E and Alzheimer disease: risk, mechanisms and therapy

(2013) Chia-Chen Liu et al.   Nature Reviews Neurology

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

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

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

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

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

A phase 2 randomized trial of ELND005, scyllo-inositol, in mild to moderate Alzheimer disease

(2011) S. Salloway et al.   NEUROLOGY

Endogenous amyloid-β is necessary for hippocampal synaptic plasticity and memory

(2010) Daniela Puzzo et al.   ANNALS OF NEUROLOGY

A Noncompetitive BACE1 Inhibitor TAK-070 Ameliorates A  Pathology and Behavioral Deficits in a Mouse Model of Alzheimer's Disease

(2010) H. Fukumoto et al.   JOURNAL OF NEUROSCIENCE

Decreased Clearance of CNS  -Amyloid in Alzheimer's Disease

(2010) K. G. Mawuenyega et al.   SCIENCE

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

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

Effect of Tarenflurbil on Cognitive Decline and Activities of Daily Living in Patients With Mild Alzheimer DiseaseA Randomized Controlled Trial

(2009) Robert C. Green   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Amyloid-β as a positive endogenous regulator of release probability at hippocampal synapses

(2009) Efrat Abramov et al.   NATURE NEUROSCIENCE