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

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

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

(2016) Mihirbaran Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibiting BACE1 to reverse synaptic dysfunctions in Alzheimer’s disease

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

BACE1 Physiological Functions May Limit Its Use as Therapeutic Target for Alzheimer's Disease

(2016) Soraia Barão et al.   TRENDS IN NEUROSCIENCES

Inhibition of BACE2 counteracts hIAPP-induced insulin secretory defects in pancreatic β-cells

(2015) Gema Alcarraz-Vizán et al.   FASEB JOURNAL

A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice

(2015) Ulf Neumann et al.   Molecular Neurodegeneration

Three dimensions of the amyloid hypothesis: time, space and 'wingmen'

(2015) Erik S Musiek et al.   NATURE NEUROSCIENCE

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

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

Antagonistic Effects of BACE1 and APH1B-γ-Secretase Control Axonal Guidance by Regulating Growth Cone Collapse

(2015) Soraia Barão et al.   Cell Reports

Structural biology of presenilin 1 complexes

(2015) Yi Li et al.   Molecular Neurodegeneration

The evolution of amidine-based brain penetrant BACE1 inhibitors

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

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

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

The Normal and Pathologic Roles of the Alzheimer's β-secretase, BACE1

(2014) Patty Kandalepas et al.   Current Alzheimer Research

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

(2014) Robert Vassar et al.   JOURNAL OF NEUROCHEMISTRY

Targeting the β secretase BACE1 for Alzheimer's disease therapy

(2014) Riqiang Yan et al.   LANCET NEUROLOGY

Tau pathogenesis is promoted by Aβ1-42 but not Aβ1-40

(2014) Xiaoyan Hu et al.   Molecular Neurodegeneration

Oligomeric Aβ-induced synaptic dysfunction in Alzheimer’s disease

(2014) Shichun Tu et al.   Molecular Neurodegeneration

BACE1 inhibitor drugs in clinical trials for Alzheimer’s disease

(2014) Robert Vassar   Alzheimers Research & Therapy

The novel BACE inhibitor MK-8931 dramatically lowers CSF beta-amyloid in patients with mild-to-moderate Alzheimer's disease

(2013) Mark Forman et al.   Alzheimers & Dementia

Conformational restriction approach to β-secretase (BACE1) inhibitors III: Effective investigation of the binding mode by combinational use of X-ray analysis, isothermal titration calorimetry and theoretical calculations

(2013) Shuji Yonezawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Conformational restriction approach to BACE1 inhibitors II: SAR study of the isocytosine derivatives fixed with a cis-cyclopropane ring

(2013) Shuji Yonezawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

β-Secretase (BACE1) Inhibitors with High in Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer’s Disease

(2013) Hans Hilpert et al.   JOURNAL OF MEDICINAL 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

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

BACE1 Regulates Hippocampal Astrogenesis via the Jagged1-Notch Pathway

(2013) Xiangyou Hu et al.   Cell Reports

A tale of two drug targets: the evolutionary history of BACE1 and BACE2

(2013) Christopher Southan et al.   Frontiers in Genetics

Secretome protein enrichment identifies physiological BACE1 protease substrates in neurons

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

Discovery of AZD3839, a Potent and Selective BACE1 Inhibitor Clinical Candidate for the Treatment of Alzheimer Disease

(2012) Fredrik Jeppsson 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

Conformational Restriction Approach to β-Secretase (BACE1) Inhibitors: Effect of a Cyclopropane Ring To Induce an Alternative Binding Mode

(2012) Shuji Yonezawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β-Amyloid Peptides

(2012) Britt-Marie Swahn et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

(2011) Daria Esterházy et al.   Cell Metabolism

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

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

BACE2 plays a role in the insulin receptor trafficking in pancreatic β-cells

(2010) Silvia Casas et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

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

BACE1 Deficiency Causes Altered Neuronal Activity and Neurodegeneration

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

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

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

The secretases: enzymes with therapeutic potential in Alzheimer disease

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

Aminoimidazoles as Potent and Selective Human β-Secretase (BACE1) Inhibitors

(2009) Michael S. Malamas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves

(2008) Xiangyou Hu et al.   FASEB JOURNAL

Changes in γ-secretase activity and specificity caused by the introduction of consensus aspartyl protease active motif in Presenilin 1

(2008) Donald B Carter et al.   Molecular Neurodegeneration