Tau-Centric Targets and Drugs in Clinical Development for the Treatment of Alzheimer’s Disease

Treatment of Alzheimer's Disease with the GSK-3 Inhibitor Tideglusib: A Pilot Study

(2018) Teodoro del Ser et al.   JOURNAL OF ALZHEIMERS DISEASE

2015 Alzheimer's disease facts and figures

(2015)   Alzheimers & Dementia

Effects of oxidized and reduced forms of methylthioninium in two transgenic mouse tauopathy models

(2015) Valeria Melis et al.   BEHAVIOURAL PHARMACOLOGY

Pathological Interface Between Oligomeric Alpha-Synuclein and Tau in Synucleinopathies

(2015) Urmi Sengupta et al.   BIOLOGICAL PSYCHIATRY

Early investigational drugs targeting tau protein for the treatment of Alzheimer’s disease

(2015) Keshav Anand et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Further understanding of tau phosphorylation: implications for therapy

(2015) Miguel Medina et al.   Expert Review of Neurotherapeutics

Protein Folding and Mechanisms of Proteostasis

(2015) José Díaz-Villanueva et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cellular Models of Aggregation-dependent Template-directed Proteolysis to Characterize Tau Aggregation Inhibitors for Treatment of Alzheimer Disease

(2015) Charles R. Harrington et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Methylene Blue Improves Brain Mitochondrial ABAD Functions and Decreases Aβ in a Neuroinflammatory Alzheimer’s Disease Mouse Model

(2015) Aya Zakaria et al.   MOLECULAR NEUROBIOLOGY

Critical role of acetylation in tau-mediated neurodegeneration and cognitive deficits

(2015) Sang-Won Min et al.   NATURE MEDICINE

Human secreted tau increases amyloid-beta production

(2015) Jessica Bright et al.   NEUROBIOLOGY OF AGING

Tau immunotherapy for Alzheimer's disease

(2015) Jan Torleif Pedersen et al.   TRENDS IN MOLECULAR MEDICINE

Nontoxic singlet oxygen generator as a therapeutic candidate for treating tauopathies

(2015) Sahabudeen Sheik Mohideen et al.   Scientific Reports

Further understanding of tau phosphorylation: implications for therapy

(2015) Miguel Medina et al.   Expert Review of Neurotherapeutics

The relationship between truncation and phosphorylation at the C-terminus of tau protein in the paired helical filaments of Alzheimer's disease

(2015) Paola Flores-Rodríguez et al.   Frontiers in Neuroscience

Preventive methylene blue treatment preserves cognition in mice expressing full-length pro-aggregant human Tau

(2015) Katja Hochgräfe et al.   Acta Neuropathologica Communications

Methylene Blue Protects Astrocytes against Glucose Oxygen Deprivation by Improving Cellular Respiration

(2015) Gourav Roy Choudhury et al.   PLoS One

Alzheimer disease therapeutics: Focus on the disease and not just plaques and tangles

(2014) Khalid Iqbal et al.   BIOCHEMICAL PHARMACOLOGY

Neuronal uptake of tau/pS422 antibody and reduced progression of tau pathology in a mouse model of Alzheimer‘s disease

(2014) Ludovic Collin et al.   BRAIN

Different pathways of molecular pathophysiology underlie cognitive and motor tauopathy phenotypes in transgenic models for Alzheimer’s disease and frontotemporal lobar degeneration

(2014) V. Melis et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Structure and Mechanism of Action of Tau Aggregation Inhibitors

(2014) Katryna Cisek et al.   Current Alzheimer Research

Amyloid-directed monoclonal antibodies for the treatment of Alzheimer’s disease: the point of no return?

(2014) Francesco Panza et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Microtubule-associated protein tau as a therapeutic target in Alzheimer's disease

(2014) Khalid Iqbal et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Amyloid-based immunotherapy for Alzheimer's disease in the time of prevention trials: the way forward

(2014) Francesco Panza et al.   Expert Review of Clinical Immunology

Advances in the therapy of Alzheimer’s disease: targeting amyloid beta and tau and perspectives for the future

(2014) Harald Hampel et al.   Expert Review of Neurotherapeutics

The green tea polyphenol (−)-epigallocatechin gallate prevents the aggregation of tau protein into toxic oligomers at substoichiometric ratios

(2014) Heike J. Wobst et al.   FEBS LETTERS

Tau-Based Therapeutic Approaches for Alzheimer's Disease - A Mini-Review

(2014) Allal Boutajangout et al.   GERONTOLOGY

Methylene blue upregulates Nrf2/ARE genes and prevents tau-related neurotoxicity

(2014) Cliona Stack et al.   HUMAN MOLECULAR GENETICS

Methylene Blue Modulates β-Secretase, Reverses Cerebral Amyloidosis, and Improves Cognition in Transgenic Mice

(2014) Takashi Mori et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Clinical trials and late-stage drug development for Alzheimer's disease: an appraisal from 1984 to 2014

(2014) L. S. Schneider et al.   JOURNAL OF INTERNAL MEDICINE

Davunetide in patients with progressive supranuclear palsy: a randomised, double-blind, placebo-controlled phase 2/3 trial

(2014) Adam L Boxer et al.   LANCET NEUROLOGY

The Glutathione System: A New Drug Target in Neuroimmune Disorders

(2014) Gerwyn Morris et al.   MOLECULAR NEUROBIOLOGY

A phase 2 trial of the GSK-3 inhibitor tideglusib in progressive supranuclear palsy

(2014) Eduardo Tolosa et al.   MOVEMENT DISORDERS

Methylene blue does not reverse existing neurofibrillary tangle pathology in the rTg4510 mouse model of tauopathy

(2014) Tara L. Spires-Jones et al.   NEUROSCIENCE LETTERS

First-in-man tau vaccine targeting structural determinants essential for pathological tau–tau interaction reduces tau oligomerisation and neurofibrillary degeneration in an Alzheimer’s disease model

(2014) Eva Kontsekova et al.   Alzheimers Research & Therapy

Mechanistic Basis of Phenothiazine-Driven Inhibition of Tau Aggregation

(2013) Elias Akoury et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Tau-aggregation inhibitor therapy for Alzheimer's disease

(2013) Claude M. Wischik et al.   BIOCHEMICAL PHARMACOLOGY

“Prion-Like” Templated Misfolding in Tauopathies

(2013) Florence Clavaguera et al.   BRAIN PATHOLOGY

Dimethyl fumarate: a Janus-faced substance?

(2013) Frieder Kees   EXPERT OPINION ON PHARMACOTHERAPY

Structural Determinants of Tau Aggregation Inhibitor Potency

(2013) Kelsey N. Schafer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Aminothienopyridazines and Methylene Blue Affect Tau Fibrillization via Cysteine Oxidation

(2013) Alex Crowe et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antibody Uptake into Neurons Occurs Primarily via Clathrin-dependent Fcγ Receptor Endocytosis and Is a Prerequisite for Acute Tau Protein Clearance

(2013) Erin E. Congdon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Two Novel Tau Antibodies Targeting the 396/404 Region Are Primarily Taken Up by Neurons and Reduce Tau Protein Pathology

(2013) Jiaping Gu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Progress and Developments in Tau Aggregation Inhibitors for Alzheimer Disease

(2013) Bruno Bulic et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of Tau Filament Formation by Conformational Modulation

(2013) Elias Akoury et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

NAP (davunetide) modifies disease progression in a mouse model of severe neurodegeneration: Protection against impairments in axonal transport

(2013) Yan Jouroukhin et al.   NEUROBIOLOGY OF DISEASE

Therapeutic and preventive effects of methylene blue on Alzheimer's disease pathology in a transgenic mouse model

(2013) V. Paban et al.   NEUROPHARMACOLOGY

Efficacy and Safety of A Liposome-Based Vaccine against Protein Tau, Assessed in Tau.P301L Mice That Model Tauopathy

(2013) Clara Theunis et al.   PLoS One

Methylene blue induces macroautophagy through 5′ adenosine monophosphate-activated protein kinase pathway to protect neurons from serum deprivation

(2013) Luokun Xie et al.   Frontiers in Cellular Neuroscience

Tau protein kinases: Involvement in Alzheimer's disease

(2012) Ludovic Martin et al.   AGEING RESEARCH REVIEWS

Methylthioninium chloride (methylene blue) induces autophagy and attenuates tauopathy in vitro and in vivo

(2012) Erin E. Congdon et al.   Autophagy

Binding of methylene blue to a surface cleft inhibits the oligomerization and fibrillization of prion protein

(2012) Paola Cavaliere et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Methylene Blue Inhibits the Function of α7-Nicotinic Acetylcholine Receptors

(2012) Abdulla S. Al Mansouri et al.   CNS & Neurological Disorders-Drug Targets

Immunotherapy for Alzheimer’s disease: from anti-β-amyloid to tau-based immunization strategies

(2012) Francesco Panza et al.   Immunotherapy

Curcumin Prevents Aggregation in α-Synuclein by Increasing Reconfiguration Rate

(2012) Basir Ahmad et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Modulation of Tau Protein Fibrillization by Oleocanthal

(2012) Maria Chiara Monti et al.   JOURNAL OF NATURAL PRODUCTS

The Microtubule-Stabilizing Agent, Epothilone D, Reduces Axonal Dysfunction, Neurotoxicity, Cognitive Deficits, and Alzheimer-Like Pathology in an Interventional Study with Aged Tau Transgenic Mice

(2012) B. Zhang et al.   JOURNAL OF NEUROSCIENCE

The crystalline state of methylene blue: a zoo of hydrates

(2012) Timo Rager et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Neuroprotective Actions of Methylene Blue and Its Derivatives

(2012) Ethan Poteet et al.   PLoS One

Methylene Blue Reduced Abnormal Tau Accumulation in P301L Tau Transgenic Mice

(2012) Masato Hosokawa et al.   PLoS One

“Clicked” Sugar–Curcumin Conjugate: Modulator of Amyloid-β and Tau Peptide Aggregation at Ultralow Concentrations

(2011) Sukanta Dolai et al.   ACS Chemical Neuroscience

Phosphoprotein phosphatase 2A: a novel druggable target for Alzheimer’s disease

(2011) Michael Voronkov et al.   Future Medicinal Chemistry

Anti-tau oligomers passive vaccination for the treatment of Alzheimer disease

(2011) Rakez Kayed   Human vaccines & immunotherapeutics

Alternative Mitochondrial Electron Transfer as a Novel Strategy for Neuroprotection

(2011) Yi Wen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The toxicity of tau in Alzheimer disease: turnover, targets and potential therapeutics

(2011) Susanne M. Pritchard et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Novel Types of Frontotemporal Lobar Degeneration: Beyond Tau and TDP-43

(2011) Ian R. A. Mackenzie et al.   JOURNAL OF MOLECULAR NEUROSCIENCE

Passive immunization targeting pathological phospho-tau protein in a mouse model reduces functional decline and clears tau aggregates from the brain

(2011) Allal Boutajangout et al.   JOURNAL OF NEUROCHEMISTRY

Stages of the Pathologic Process in Alzheimer Disease: Age Categories From 1 to 100 Years

(2011) Heiko Braak et al.   JOURNAL OF NEUROPATHOLOGY AND EXPERIMENTAL NEUROLOGY

“Lest we forget you — methylene blue …”

(2011) R. Heiner Schirmer et al.   NEUROBIOLOGY OF AGING

The acetylation of tau inhibits its function and promotes pathological tau aggregation

(2011) Todd J. Cohen et al.   Nature Communications

Towards a Pharmacophore for Amyloid

(2011) Meytal Landau et al.   PLOS BIOLOGY

Role of monoamine oxidase, nitric oxide synthase and regional brain monoamines in the antidepressant-like effects of methylene blue and selected structural analogues

(2010) Brian H. Harvey et al.   BIOCHEMICAL PHARMACOLOGY

Methylene Blue Reduces Aβ Levels and Rescues Early Cognitive Deficit by Increasing Proteasome Activity

(2010) David X. Medina et al.   BRAIN PATHOLOGY

TAU Aggregation is a Therapeutic Target for Alzheimers Disease

(2010) A. Takashima   Current Alzheimer Research

Towards Disease-Modifying Treatment of Alzheimers Disease: Drugs Targeting β -Amyloid

(2010) V. Frisardi et al.   Current Alzheimer Research

Tau in Alzheimer Disease and Related Tauopathies

(2010) K. Iqbal et al.   Current Alzheimer Research

Aggregation of Detergent-insoluble Tau Is Involved in Neuronal Loss but Not in Synaptic Loss

(2010) Tetsuya Kimura et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Epothilone D Improves Microtubule Density, Axonal Integrity, and Cognition in a Transgenic Mouse Model of Tauopathy

(2010) K. R. Brunden et al.   JOURNAL OF NEUROSCIENCE

Immunotherapy Targeting Pathological Tau Prevents Cognitive Decline in a New Tangle Mouse Model

(2010) A. Boutajangout et al.   JOURNAL OF NEUROSCIENCE

Phenothiazine-mediated rescue of cognition in tau transgenic mice requires neuroprotection and reduced soluble tau burden

(2010) John C O'Leary et al.   Molecular Neurodegeneration

Methylene blue fails to inhibit Tau and polyglutamine protein dependent toxicity in zebrafish

(2010) Frauke van Bebber et al.   NEUROBIOLOGY OF DISEASE

Tau Phosphorylation and Cleavage in Ethanol-Induced Neurodegeneration in the Developing Mouse Brain

(2010) Mariko Saito et al.   NEUROCHEMICAL RESEARCH

Beneficial network effects of methylene blue in an amnestic model

(2010) Penny D. Riha et al.   NEUROIMAGE

Acetylation of Tau Inhibits Its Degradation and Contributes to Tauopathy

(2010) Sang-Won Min et al.   NEURON

Phosphorylated and cleaved TDP-43 in ALS, FTLD and other neurodegenerative disorders and in cellular models of TDP-43 proteinopathy

(2010) Tetsuaki Arai et al.   NEUROPATHOLOGY

Tau protein and tau aggregation inhibitors

(2010) Bruno Bulic et al.   NEUROPHARMACOLOGY

Truncated tau at D421 is associated with neurodegeneration and tangle formation in the brain of Alzheimer transgenic models

(2009) Qipeng Zhang et al.   ACTA NEUROPATHOLOGICA

Adverse Effects of Methylene Blue on the Central Nervous System

(2009) Laszlo Vutskits et al.   ANESTHESIOLOGY

Identification of Aminothienopyridazine Inhibitors of Tau Assembly by Quantitative High-Throughput Screening

(2009) Alex Crowe et al.   BIOCHEMISTRY

Methylene blue and dimebon inhibit aggregation of TDP-43 in cellular models

(2009) Makiko Yamashita et al.   FEBS LETTERS

Propagation of Tau Misfolding from the Outside to the Inside of a Cell

(2009) Bess Frost et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure−Activity Relationship of Cyanine Tau Aggregation Inhibitors

(2009) Edward Chang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of tau fibrillization by oleocanthal via reaction with the amino groups of tau

(2009) Wenkai Li et al.   JOURNAL OF NEUROCHEMISTRY

Chemical Manipulation of Hsp70 ATPase Activity Regulates Tau Stability

(2009) U. K. Jinwal et al.   JOURNAL OF NEUROSCIENCE

Transmission and spreading of tauopathy in transgenic mouse brain

(2009) Florence Clavaguera et al.   NATURE CELL BIOLOGY

Strong Gametocytocidal Effect of Methylene Blue-Based Combination Therapy against Falciparum Malaria: A Randomised Controlled Trial

(2009) Boubacar Coulibaly et al.   PLoS One

Hyperphosphorylation of Microtubule-Associated Protein Tau: A Promising Therapeutic Target for Alzheimer Disease

(2008) C.-X. Gong et al.   CURRENT MEDICINAL CHEMISTRY

Interplay between Cyclin-Dependent Kinase 5 and Glycogen Synthase Kinase 3  Mediated by Neuregulin Signaling Leads to Differential Effects on Tau Phosphorylation and Amyloid Precursor Protein Processing

(2008) Y. Wen et al.   JOURNAL OF NEUROSCIENCE

A Neuronal Microtubule-Interacting Agent, NAPVSIPQ, Reduces Tau Pathology and Enhances Cognitive Function in a Mouse Model of Alzheimer's Disease

(2008) Y. Matsuoka et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Methylthioninium chloride reverses cognitive deficits induced by scopolamine: comparison with rivastigmine

(2008) Serena Deiana et al.   PSYCHOPHARMACOLOGY