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

Recent developments and applications of clickable photoprobes in medicinal chemistry and chemical biology

(2015) David J Lapinsky et al.   Future Medicinal Chemistry

Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design

(2015) Christopher R. Butler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Utilizing Structures of CYP2D6 and BACE1 Complexes To Reduce Risk of Drug–Drug Interactions with a Novel Series of Centrally Efficacious BACE1 Inhibitors

(2015) Michael A. Brodney et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central A  Pharmacodynamic Responses in Mice, Dogs, and Humans

(2015) P. C. May et al.   JOURNAL OF NEUROSCIENCE

Acetylation site specificities of lysine deacetylase inhibitors in human cells

(2015) Christian Schölz et al.   NATURE BIOTECHNOLOGY

Activity-Based Profiling of Proteases

(2014) Laura E. Sanman et al.   Annual Review of Biochemistry

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

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

Inhibitors of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1): Identification of (S)-7-(2-Fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′H-spiro[chromeno[2,3-b]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)

(2014) Thomas A. Dineen et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2014) Robert Vassar et al.   JOURNAL OF NEUROCHEMISTRY

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

(2014) Bryan R Lanning et al.   Nature Chemical Biology

Retinal Toxicity Induced by a Novel β-secretase Inhibitor in the Sprague-Dawley Rat

(2014) Mark R. Fielden et al.   TOXICOLOGIC PATHOLOGY

Cell Models to Study Regulation of Cell Transformation in Pathologies of Retinal Pigment Epithelium

(2014) Alla V. Kuznetsova et al.   Journal of Ophthalmology

Sequence context and crosslinking mechanism affect the efficiency of in vivo capture of a protein-protein interaction

(2013) Jody K. Lancia et al.   BIOPOLYMERS

γ-Secretase Modulator (GSM) Photoaffinity Probes Reveal Distinct Allosteric Binding Sites on Presenilin

(2013) Nikolay Pozdnyakov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

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

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

(2012) Jun Cai et al.   EMBO Molecular Medicine

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

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

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

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

Probing the Probes: Fitness Factors For Small Molecule Tools

(2010) Paul Workman et al.   CHEMISTRY & BIOLOGY

The Retinal Pigment Epithelium in Health and Disease

(2010) J. R. Sparrrow et al.   CURRENT MOLECULAR MEDICINE

The Role of Lysosomes in Limiting Drug Toxicity in Mice

(2010) R. A. Ndolo et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The secretases: enzymes with therapeutic potential in Alzheimer disease

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

Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds: strategic considerations

(2009) Johan Gabrielsson et al.   DRUG DISCOVERY TODAY

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

Cathepsin D—Many functions of one aspartic protease

(2008) Petr Benes et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY