Population PKPD Modeling of BACE1 Inhibitor-Induced Reduction in Aβ Levels In Vivo and Correlation to In Vitro Potency in Primary Cortical Neurons from Mouse and Guinea Pig

2012 Alzheimer’s disease facts and figures

(2012)   Alzheimers & Dementia

Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy

(2012) Britt-Marie Swahn et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

New Aminoimidazoles as β-Secretase (BACE-1) Inhibitors Showing Amyloid-β (Aβ) Lowering in Brain

(2012) Ylva Gravenfors et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid

(2012) Matthew M. Weiss et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors

(2012) Thomas A. Dineen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Cyclic Sulfone Hydroxyethylamines as Potent and Selective β-Site APP-Cleaving Enzyme 1 (BACE1) Inhibitors: Structure-Based Design and in Vivo Reduction of Amyloid β-Peptides

(2012) Heinrich Rueeger 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

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

(2012) Thorlakur Jonsson et al.   NATURE

Pharmacodynamic-Pharmacokinetic Integration as a Guide to Medicinal Chemistry

(2011) Johan Gabrielsson et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

γ-Secretase inhibitors and modulators for Alzheimer’s disease

(2011) Michael S. Wolfe   JOURNAL OF NEUROCHEMISTRY

Regulated intramembrane proteolysis - lessons from amyloid precursor protein processing

(2011) Stefan F. Lichtenthaler et al.   JOURNAL OF NEUROCHEMISTRY

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

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

High-throughput analysis of standardized pharmacokinetic studies in the rat using sample pooling and UPLC–MS/MS

(2011) Tjerk Bueters et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Quantitative Pharmacokinetic/Pharmacodynamic Analyses Suggest That the 129/SVE Mouse Is a Suitable Preclinical Pharmacology Model for Identifying Small-Molecule  -Secretase Inhibitors

(2011) Y. Lu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics

(2011) Eric Karran et al.   NATURE REVIEWS DRUG DISCOVERY

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

(2010) Anh P. Truong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

REVIEW: γ-Secretase Inhibitors for the Treatment of Alzheimer's Disease: The Current State

(2010) Francesco Panza et al.   CNS Neuroscience & Therapeutics

β-Secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice

(2010) Wan-Pin Chang et al.   FASEB JOURNAL

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

Alzheimer's disease: strategies for disease modification

(2010) Martin Citron   NATURE REVIEWS DRUG DISCOVERY

Alzheimer's Disease

(2010) Henry W. Querfurth et al.   NEW ENGLAND JOURNAL OF MEDICINE

Development of a High-Throughput Brain Slice Method for Studying Drug Distribution in the Central Nervous System

(2009) M. Friden et al.   DRUG METABOLISM AND DISPOSITION

Recent Advances in the Identification of γ-Secretase Inhibitors To Clinically Test the Aβ Oligomer Hypothesis of Alzheimer’s Disease

(2009) Anthony F. Kreft et al.   JOURNAL OF MEDICINAL CHEMISTRY

The amyloid hypothesis for Alzheimer’s disease: a critical reappraisal

(2009) John Hardy   JOURNAL OF NEUROCHEMISTRY

Flavonols and flavones as BACE-1 inhibitors: Structure–activity relationship in cell-free, cell-based and in silico studies reveal novel pharmacophore features

(2008) Yoshiari Shimmyo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

BACE1 Structure and Function in Health and Alzheimers Disease

(2008) Sarah Cole et al.   Current Alzheimer Research

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