Multidisciplinary approaches for targeting the secretase protein family as a therapeutic route for Alzheimer's disease

Dual BACE-1/GSK-3β Inhibitors to Combat Alzheimer's Disease: A Focused Review

(2018) Angela Rampa et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead

(2018) Devendra Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain

(2018) Lei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of the α-Secretase Processing of AβPP as a Therapeutic Approach in Alzheimer's Disease

(2018) Bruno Vincent et al.   JOURNAL OF ALZHEIMERS DISEASE

The Many Substrates of Presenilin/γ-Secretase

(2018) Annakaisa Haapasalo et al.   JOURNAL OF ALZHEIMERS DISEASE

BACE inhibitors in clinical development for the treatment of Alzheimer’s disease

(2018) Francesco Panza et al.   Expert Review of Neurotherapeutics

Design, synthesis, in-silico and biological evaluation of novel donepezil derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease

(2017) Chandra Bhushan Mishra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease

(2017) Hamadeh Tarazi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Intramembrane proteases as drug targets

(2017) Steven H. L. Verhelst   FEBS Journal

Multi-modal MRI investigation of volumetric and microstructural changes in the hippocampus and its subfields in mild cognitive impairment, Alzheimer's disease, and dementia with Lewy bodies

(2017) Elijah Mak et al.   INTERNATIONAL PSYCHOGERIATRICS

Acylguanidine Beta Secretase 1 Inhibitors: A Combined Experimental and Free Energy Perturbation Study

(2017) Henrik Keränen et al.   Journal of Chemical Theory and Computation

A capillary electrophoresis-mass spectrometry based method for the screening of β-secretase inhibitors as potential Alzheimer's disease therapeutics

(2017) Jan Schejbal et al.   JOURNAL OF CHROMATOGRAPHY A

Polymethoxyflavones: Novel β-Secretase (BACE1) Inhibitors from Citrus Peels

(2017) Kumju Youn et al.   Nutrients

Language background in early life may be related to neuropsychiatry symptoms in patients with Alzheimer disease

(2017) Yi-Chien Liu et al.   BMC Geriatrics

Statins and the Squalene Synthase Inhibitor Zaragozic Acid Stimulate the Non-Amyloidogenic Pathway of Amyloid-β Protein Precursor Processing by Suppression of Cholesterol Synthesis

(2017) Elzbieta Kojro et al.   JOURNAL OF ALZHEIMERS DISEASE

Multistep Modeling Strategy To Improve the Binding Affinity Prediction of PET Tracers to Aβ42: Case Study with Styrylbenzoxazole Derivatives

(2016) Kanagasabai Balamurugan et al.   ACS Chemical Neuroscience

Dual Signal Amplification Electrochemical Biosensor for Monitoring the Activity and Inhibition of the Alzheimer’s Related Protease β-Secretase

(2016) Fengli Qu et al.   ANALYTICAL CHEMISTRY

Specific combinations of presenilins and Aph1s affect the substrate specificity and activity of γ-secretase

(2016) Yoji Yonemura et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Design and optimization of tricyclic gamma-secretase modulators

(2016) Jianliang Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Physiological and pathological roles of the γ-secretase complex

(2016) Courtney M. Carroll et al.   BRAIN RESEARCH BULLETIN

Regulation of the α-secretase ADAM10 at transcriptional, translational and post-translational levels

(2016) Bruno Vincent   BRAIN RESEARCH BULLETIN

Discovery of new selective cytotoxic agents against Bcl-2 expressing cancer cells using ligand-based modeling

(2016) Nour H. Aboalhaija et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Multiple Targets for the Management of Alzheimer’s Disease

(2016) Syed Ahmad et al.   CNS & Neurological Disorders-Drug Targets

Extending accessible chemical space for the identification of novel leads

(2016) Jürgen Bajorath   Expert Opinion on Drug Discovery

From Common to Rare Variants: The Genetic Component of Alzheimer Disease

(2016) Gaël Nicolas et al.   HUMAN HEREDITY

Application of Free Energy Perturbation for the Design of BACE1 Inhibitors

(2016) Myriam Ciordia et al.   Journal of Chemical Information and Modeling

Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3β Inhibitors

(2016) Rita Maria Concetta Di Martino et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer’s Disease Agents

(2016) Serena Montanari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Gamma Secretase Modulators: New Alzheimer’s Drugs on the Horizon?

(2016) Matthew G. Bursavich et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Culprit Is in the Cave: The Core Sites Explain the Binding Profiles of Amyloid-Specific Tracers

(2016) N. Arul Murugan et al.   Journal of Physical Chemistry Letters

Age, APOE and sex: Triad of risk of Alzheimer’s disease

(2016) Brandalyn C. Riedel et al.   JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY

In Silico Mining for Antimalarial Structure-Activity Knowledge and Discovery of Novel Antimalarial Curcuminoids

(2016) Birgit Viira et al.   MOLECULES

Current pharmacotherapy and putative disease-modifying therapy for Alzheimer’s disease

(2016) Akanksha Kulshreshtha et al.   NEUROLOGICAL SCIENCES

Oxidative stress: A major pathogenesis and potential therapeutic target of antioxidative agents in Parkinson’s disease and Alzheimer’s disease

(2016) Tianfang Jiang et al.   PROGRESS IN NEUROBIOLOGY

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

(2016) Soraia Barão et al.   TRENDS IN NEUROSCIENCES

Looking for inhibitors of the dengue virus NS5 RNA-dependent RNA-polymerase using a molecular docking approach

(2016) Vicente Galiano et al.   Drug Design Development and Therapy

Specific Inhibition of β-Secretase Processing of the Alzheimer Disease Amyloid Precursor Protein

(2016) Saoussen Ben Halima et al.   Cell Reports

Systematic substrate identification indicates a central role for the metalloprotease ADAM10 in axon targeting and synapse function

(2016) Peer-Hendrik Kuhn et al.   eLife

Probing the origins of human acetylcholinesterase inhibition via QSAR modeling and molecular docking

(2016) Saw Simeon et al.   PeerJ

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

(2016) Riqiang Yan   Translational Neurodegeneration

Computational approaches in target identification and drug discovery

(2016) Theodora Katsila et al.   Computational and Structural Biotechnology Journal

2015 Alzheimer's disease facts and figures

(2015)   Alzheimers & Dementia

Learning by Failing: Ideas and Concepts to Tackle γ-Secretases in Alzheimer's Disease and Beyond

(2015) Bart De Strooper et al.   Annual Review of Pharmacology and Toxicology

Potent benzoazepinone γ-secretase modulators with improved bioavailability

(2015) Joey L. Methot et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

On the Origins of Hepatitis C Virus NS5B Polymerase Inhibitory Activity Using Machine Learning Approaches

(2015) Apilak Worachartcheewan et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Computer-Aided Drug Design of Bioactive Natural Products

(2015) Veda Prachayasittikul et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Maximizing computational tools for successful drug discovery

(2015) Chanin Nantasenamat et al.   Expert Opinion on Drug Discovery

Prevalence of dementia in East Asia: a synthetic review of time trends

(2015) Yu-Tzu Wu et al.   INTERNATIONAL JOURNAL OF GERIATRIC PSYCHIATRY

Investigation of flap flexibility of β-secretase using molecular dynamic simulations

(2015) Hezekiel M. Kumalo et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

Investigation of the Binding Profiles of AZD2184 and Thioflavin T with Amyloid-β(1–42) Fibril by Molecular Docking and Molecular Dynamics Methods

(2015) Guanglin Kuang et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Molecular dynamics simulation study reveals potential substrate entry path into γ-secretase/presenilin-1

(2015) Ren Kong et al.   JOURNAL OF STRUCTURAL BIOLOGY

Fluorescent turn-on determination of the activity of peptidases using peptide templated gold nanoclusters

(2015) Junjun Luo et al.   MICROCHIMICA ACTA

Current and future implications of basic and translational research on amyloid-β peptide production and removal pathways

(2015) C. Bohm et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

η-Secretase processing of APP inhibits neuronal activity in the hippocampus

(2015) Michael Willem et al.   NATURE

An atomic structure of human γ-secretase

(2015) Xiao-chen Bai et al.   NATURE

Targeting protein aggregation for the treatment of degenerative diseases

(2015) Yvonne S. Eisele et al.   NATURE REVIEWS DRUG DISCOVERY

Structural basis of human γ-secretase assembly

(2015) Linfeng Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synthesis, molecular docking and biological evaluation of new thiazolopyrimidine carboxylates as potential antidiabetic and antibacterial agents

(2015) Iram Batool et al.   RESEARCH ON CHEMICAL INTERMEDIATES

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability

(2015) Martin Pettersson et al.   ACS Medicinal Chemistry Letters

Delta-secretase cleaves amyloid precursor protein and regulates the pathogenesis in Alzheimer’s disease

(2015) Zhentao Zhang et al.   Nature Communications

Discovery of novel 1,2,3-triazole derivatives as anticancer agents using QSAR and in silico structural modification

(2015) Veda Prachayasittikul et al.   SpringerPlus

Multitarget Drug Discovery for Alzheimer's Disease: Triazinones as BACE-1 and GSK-3β Inhibitors

(2014) Federica Prati et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Soluble γ-Secretase Modulators Selectively Inhibit the Production of the 42-Amino Acid Amyloid β Peptide Variant and Augment the Production of Multiple Carboxy-Truncated Amyloid β Species

(2014) Steven L. Wagner et al.   BIOCHEMISTRY

Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: Synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis

(2014) Imtiaz Khan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

Synthesis, anticancer activity and QSAR study of 1,4-naphthoquinone derivatives

(2014) Veda Prachayasittikul et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Potency Prediction of β-Secretase (BACE-1) Inhibitors Using Density Functional Methods

(2014) Katarina Roos et al.   Journal of Chemical Information and Modeling

Screening of β-secretase and acetylcholinesterase inhibitors from plant resources

(2014) Kazuya Murata et al.   Journal of Natural Medicines

Metallothioneins and Synthetic Metal Chelators as Potential Therapeutic Agents for Removal of Aberrant Metal Ions from Metal-Aβ Species

(2014) Ning Xia et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Three-dimensional structure of human γ-secretase

(2014) Peilong Lu et al.   NATURE

Molecular Investigations of Protriptyline as a Multi-Target Directed Ligand in Alzheimer's Disease

(2014) Sneha B. Bansode et al.   PLoS One

Collaborative Mining and Interpretation of Large-Scale Data for Biomedical Research Insights

(2014) Georgia Tsiliki et al.   PLoS One

β-secretase inhibitor; a promising novel therapeutic drug in Alzheimer’s disease

(2014) Kelly Willemijn Menting et al.   Frontiers in Aging Neuroscience

Development of Dual Inhibitors against Alzheimer’s Disease Using Fragment-Based QSAR and Molecular Docking

(2014) Manisha Goyal et al.   Biomed Research International

Sensitive and Continuous Screening of Inhibitors of β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) at Single SPR Chips

(2013) Xinyao Yi et al.   ANALYTICAL CHEMISTRY

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: Structure based design and in vivo reduction of amyloid β-peptides

(2013) Heinrich Rueeger et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Brain amyloid-β oligomers in ageing and Alzheimer’s disease

(2013) Sylvain E. Lesné et al.   BRAIN

Acetylcholinesterase inhibitors as Alzheimer therapy: From nerve toxins to neuroprotection

(2013) Manjinder Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Steroids as γ-secretase modulators

(2013) Joo In Jung et al.   FASEB 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

Structure-based design and analysis of MAO-B inhibitors for Parkinson’s disease: using in silico approaches

(2013) Pavan Kare et al.   MOLECULAR DIVERSITY

Virtual Screening and Structure-Based Discovery of Indole Acylguanidines as Potent β-secretase (BACE1) Inhibitors

(2013) Yiquan Zou et al.   MOLECULES

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

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

Pharmacological Characterization of Memoquin, a Multi-Target Compound for the Treatment of Alzheimer's Disease

(2013) Valeria Capurro et al.   PLoS One

Structural Interactions between Inhibitor and Substrate Docking Sites Give Insight into Mechanisms of Human PS1 Complexes

(2013) Yi Li et al.   STRUCTURE

The Faces of Personalized Medicine: A Framework for Understanding Its Meaning and Scope

(2013) W. Ken Redekop et al.   VALUE IN HEALTH

γ-Secretase Modulators and Presenilin 1 Mutants Act Differently on Presenilin/γ-Secretase Function to Cleave Aβ42 and Aβ43

(2013) Masayasu Okochi et al.   Cell Reports

Discovery of a Novel Pharmacological and Structural Class of Gamma Secretase Modulators Derived from the Extract of Actaea racemosa

(2012) Mark A. Findeis et al.   ACS Chemical Neuroscience

Fluorogenic Quantum Dot-Gold Nanoparticle Assembly for Beta Secretase Inhibitor Screening in Live Cell

(2012) Youngseon Choi et al.   ANALYTICAL CHEMISTRY

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

BMS-708,163 Targets Presenilin and Lacks Notch-Sparing Activity

(2012) Christina J. Crump et al.   BIOCHEMISTRY

Triazoloamides as potent γ-secretase modulators with reduced hERG liability

(2012) Christian Fischer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators

(2012) Martin Pettersson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer’s disease

(2012) Hongmei Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In silico search for an endogenous anti-Alzheimer’s molecule — Screening amino acid metabolic pathways

(2012) Autumn R. Meek et al.   CANADIAN JOURNAL OF CHEMISTRY

Structure-Based Design and Synthesis of Benzothiazole Phosphonate Analogues with Inhibitors of Human ABAD-Aβ for Treatment of Alzheimer’s Disease

(2012) Koteswara R. Valasani et al.   Chemical Biology & Drug Design

α-Secretase in Alzheimers Disease and Beyond: Mechanistic, Regulation and Function in the Shedding of Membrane Proteins

(2012) Bruno Vincent et al.   Current Alzheimer Research

Review of Bioinformatics and QSAR Studies of β-Secretase Inhibitors

(2012) Francisco Prado-Prado et al.   Current Bioinformatics

BACE inhibitory flavanones from Balanophora involucrata Hook. f.

(2012) Jiayi Tao et al.   FITOTERAPIA

Simple Structure-Based Approach for Predicting the Activity of Inhibitors of Beta-Secretase (BACE1) Associated with Alzheimer’s Disease

(2012) Anthony F. Nastase et al.   Journal of Chemical Information and Modeling

Design and Synthesis of a Novel Series of Bicyclic Heterocycles As Potent γ-Secretase Modulators

(2012) Francois Bischoff et al.   JOURNAL OF MEDICINAL 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

Structure-Based Design of Highly Selective β-Secretase Inhibitors: Synthesis, Biological Evaluation, and Protein–Ligand X-ray Crystal Structure

(2012) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Spirocyclic Sulfamides as β-Secretase 1 (BACE-1) Inhibitors for the Treatment of Alzheimer’s Disease: Utilization of Structure Based Drug Design, WaterMap, and CNS Penetration Studies To Identify Centrally Efficacious Inhibitors

(2012) Michael A. Brodney et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of a presenilin family intramembrane aspartate protease

(2012) Xiaochun Li et al.   NATURE

Etazolate, an α-secretase activator, reduces neuroinflammation and offers persistent neuroprotection following traumatic brain injury in mice

(2012) Eleni Siopi et al.   NEUROPHARMACOLOGY

Multi-Target Drugs: The Trend of Drug Research and Development

(2012) Jin-Jian Lu et al.   PLoS One

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

Exploring the binding of BACE-1 inhibitors using comparative binding energy analysis (COMBINE)

(2012) Shu Liu et al.   BMC STRUCTURAL BIOLOGY

Polypharmacology: drug discovery for the future

(2012) A Srinivas Reddy et al.   Expert Review of Clinical Pharmacology

Structure–activity relationships for naturally occurring coumarins as β-secretase inhibitor

(2011) Shinsuke Marumoto et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Triazoles as γ-secretase modulators

(2011) Christian Fischer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on β-secretase (BACE-1)

(2011) Jung Keun Cho et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of pyrrolidine-based β-secretase inhibitors: Lead advancement through conformational design for maintenance of ligand binding efficiency

(2011) Shawn J. Stachel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Abnormal tau, mitochondrial dysfunction, impaired axonal transport of mitochondria, and synaptic deprivation in Alzheimer's disease

(2011) P. Hemachandra Reddy   BRAIN RESEARCH

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

(2011) Daria Esterházy et al.   Cell Metabolism

Current and Emerging Drug Treatment Options for Alzheimerʼs Disease

(2011) Nathan Herrmann et al.   DRUGS

Novel γ-secretase modulators: a review of patents from 2008 to 2010

(2011) Martin Pettersson et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Structure of γ-Secretase and Its Trimeric Pre-activation Intermediate by Single-particle Electron Microscopy

(2011) Fabiana Renzi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

First Principles-Based Calculations of Free Energy of Binding: Application to Ligand Binding in a Self-Assembling Superstructure

(2011) Stephen Fox et al.   Journal of Chemical Theory and Computation

Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious γ-Secretase Modulators in Vivo

(2011) Zhong-Yue Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)

(2011) Yuan Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of α-secretase cleavage

(2011) Rolf Postina   JOURNAL OF NEUROCHEMISTRY

Development of a specific ELISA to measure BACE1 levels in human tissues

(2011) Amanda Gonzales et al.   JOURNAL OF NEUROSCIENCE METHODS

Not(ch) just development: Notch signalling in the adult brain

(2011) Jessica L. Ables et al.   NATURE REVIEWS NEUROSCIENCE

Linking lipids to Alzheimer's disease: cholesterol and beyond

(2011) Gilbert Di Paolo et al.   NATURE REVIEWS NEUROSCIENCE

Docosahexaenoic Acid-Derived Neuroprotectin D1 Induces Neuronal Survival via Secretase- and PPARγ-Mediated Mechanisms in Alzheimer's Disease Models

(2011) Yuhai Zhao et al.   PLoS One

APP processing in Alzheimer's disease

(2011) Yun-wu Zhang et al.   Molecular Brain

E2012: A novel gamma-secretase modulator-pharmacology part

(2010) Toshihide Hashimoto et al.   Alzheimers & Dementia

Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent β-secretase inhibitory leads

(2010) Afaf Al-Nadaf et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Investigation of α-phenylnorstatine and α-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors

(2010) Fredrik Wångsell et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel pyrrolyl 2-aminopyridines as potent and selective human β-secretase (BACE1) inhibitors

(2010) Michael S. Malamas et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Purine derivatives as potent γ-secretase modulators

(2010) Alexey Rivkin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Cryptotanshinione upregulates α-secretase by activation PI3K pathway in cortical neurons

(2010) Zhengrong Mei et al.   BRAIN RESEARCH

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

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

Fragment-guided approach to incorporating structural information into a CoMFA study: BACE-1 as an example

(2010) Lívia Barros Salum et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

In vitro screening on β-amyloid peptide production of plants used in traditional medicine for cognitive disorders

(2010) Salim Hage et al.   JOURNAL OF ETHNOPHARMACOLOGY

Anti-amnesic activity of neferine with antioxidant and anti-inflammatory capacities, as well as inhibition of ChEs and BACE1

(2010) Hyun Ah Jung et al.   LIFE SCIENCES

Gamma-secretase activating protein is a therapeutic target for Alzheimer’s disease

(2010) Gen He et al.   NATURE

Network medicine: a network-based approach to human disease

(2010) Albert-László Barabási et al.   NATURE REVIEWS GENETICS

The secretases: enzymes with therapeutic potential in Alzheimer disease

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

Randomized controlled trial of atorvastatin in mild to moderate Alzheimer disease: LEADe

(2010) H. H. Feldman et al.   NEUROLOGY

Proteases and Proteolysis in Alzheimer Disease: A Multifactorial View on the Disease Process

(2010) Bart De Strooper   PHYSIOLOGICAL REVIEWS

Macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors with activity in vivo

(2009) Rainer Machauer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A conformational constraint improves a β-secretase inhibitor but for an unexpected reason

(2009) Ivory D. Hills et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and synthesis of cell potent BACE-1 inhibitors: Structure–activity relationship of P1′ substituents

(2009) Jennifer M. Sealy et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent

(2009) Nicolas Charrier et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application

(2009) Andreas Lerchner et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Piperidine-derived γ-secretase modulators

(2009) Adrian Hall et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Up-regulation of the α-secretase ADAM10 by retinoic acid receptors and acitretin

(2009) Frank Tippmann et al.   FASEB JOURNAL

Ginsenoside Rg1 inhibits β-secretase activityin vitroand protects against Aβ-induced cytotoxicity in PC12 cells

(2009) Yue-Hua Wang et al.   JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH

ADAM10, the Rate-limiting Protease of Regulated Intramembrane Proteolysis of Notch and Other Proteins, Is Processed by ADAMS-9, ADAMS-15, and the γ-Secretase

(2009) Thomas Tousseyn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Design and Synthesis of 5,5′-Disubstituted Aminohydantoins as Potent and Selective Human β-Secretase (BACE1) Inhibitors

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

A disintegrin and metalloproteinase (ADAM)-mediated ectodomain shedding of ADAM10

(2009) Edward Parkin et al.   JOURNAL OF NEUROCHEMISTRY

 -Secretase: Successive Tripeptide and Tetrapeptide Release from the Transmembrane Domain of  -Carboxyl Terminal Fragment

(2009) M. Takami et al.   JOURNAL OF NEUROSCIENCE

Development of a liquid chromatographic system with fluorescent detection for β-secretase immobilized enzyme reactor on-line enzymatic studies

(2009) Francesca Mancini et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

The rise of fragment-based drug discovery

(2009) Christopher W. Murray et al.   Nature Chemistry

Secreted amyloid precursor protein-α upregulates synaptic protein synthesis by a protein kinase G-dependent mechanism

(2009) Ana M. Claasen et al.   NEUROSCIENCE LETTERS

Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: Exploration of P1 phenoxy and benzyloxy residues

(2008) Marcus Bäck et al.   BIOORGANIC & MEDICINAL CHEMISTRY

BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells

(2008) Paul Beswick et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)

(2008) Brian Clarke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evolution of Tertiary Carbinamine BACE-1 Inhibitors: Aβ Reduction in Rhesus CSF upon Oral Dosing

(2008) Philippe G. Nantermet et al.   ChemMedChem

Cathepsin D—Many functions of one aspartic protease

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

Memapsin 2 (Beta-Secretase) Inhibitors: Drug Development

(2008) Arun Ghosh et al.   Current Alzheimer Research

Multi-target-Directed Ligands To Combat Neurodegenerative Diseases

(2008) Andrea Cavalli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cryoelectron Microscopy Structure of Purified γ-Secretase at 12 Å Resolution

(2008) Pamela Osenkowski et al.   JOURNAL OF MOLECULAR BIOLOGY

Effects of TNF -Converting Enzyme Inhibition on Amyloid   Production and APP Processing In Vitro and In Vivo

(2008) M. L. Kim et al.   JOURNAL OF NEUROSCIENCE

P-Glycoprotein Efflux and Other Factors Limit Brain Amyloid   Reduction by  -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitors in Mice

(2008) J. E. Meredith et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

Dietary supplementation with resveratrol reduces plaque pathology in a transgenic model of Alzheimer's disease

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