Tau protein aggregation: Key features to improve drug discovery screening

Structure-based classification of tauopathies

(2021) Yang Shi et al.   NATURE

Modulation of tau protein aggregation using ‘Trojan’ sequences

(2020) Gaurav Pandey et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Mechanisms of Anticholinesterase Interference with Tau Aggregation Inhibitor Activity in a Tau-Transgenic Mouse Model

(2020) Gernot Riedel et al.   Current Alzheimer Research

Understanding the disrupting mechanism of the Tau aggregation motif “306 VQIVYK311 ” by phenylthiazolyl-hydrazides inhibitors

(2020) Elena Moreno-Castillo et al.   JOURNAL OF MOLECULAR RECOGNITION

Tau immunotherapies: Lessons learned, current status and future considerations

(2020) L.A. Sandusky-Beltran et al.   NEUROPHARMACOLOGY

The C291R Tau Variant Forms Different Types of Protofibrils

(2020) Thomas K. Karikari et al.   Frontiers in Molecular Neuroscience

Screening of tau protein kinase inhibitors in a tauopathy-relevant cell-based model of tau hyperphosphorylation and oligomerization

(2020) Hamad Yadikar et al.   PLoS One

PHF-Core Tau as the Potential Initiating Event for Tau Pathology in Alzheimer’s Disease

(2020) Nabil Itzi Luna-Viramontes et al.   Frontiers in Cellular Neuroscience

Selection of a d-Enantiomeric Peptide Specifically Binding to PHF6 for Inhibiting Tau Aggregation in Transgenic Mice

(2020) Xiancheng Zhang et al.   ACS Chemical Neuroscience

α-Linolenic acid inhibits Tau aggregation and modulates Tau conformation

(2020) Smita Eknath Desale et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

The two Cysteines of Tau protein are functionally distinct and contribute differentially to its pathogenicity in vivo

(2020) Engie Prifti et al.   JOURNAL OF NEUROSCIENCE

Characterization of tau binding by gosuranemab

(2020) Richelle Sopko et al.   NEUROBIOLOGY OF DISEASE

Solid-state NMR investigation of the involvement of the P2 region in tau amyloid fibrils

(2020) Adriana Savastano et al.   Scientific Reports

New Insights Into Drug Discovery Targeting Tau Protein

(2020) Yoshiyuki Soeda et al.   Frontiers in Molecular Neuroscience

It’s all about tau

(2019) Cheril Tapia-Rojas et al.   PROGRESS IN NEUROBIOLOGY

A walk through tau therapeutic strategies

(2019) Santosh Jadhav et al.   Acta Neuropathologica Communications

Editorial: Multi-Target-Directed Ligands (MTDL) as Challenging Research Tools in Drug Discovery: From Design to Pharmacological Evaluation

(2019) Stefano Alcaro et al.   Frontiers in Chemistry

The Amazon rain forest plant Uncaria tomentosa (cat’s claw) and its specific proanthocyanidin constituents are potent inhibitors and reducers of both brain plaques and tangles

(2019) Alan D. Snow et al.   Scientific Reports

Recent therapeutic strategies targeting beta amyloid and tauopathies in Alzheimer's disease

(2019) Yamini Madav et al.   BRAIN RESEARCH BULLETIN

Simulation Studies of Amyloidogenic Polypeptides and Their Aggregates

(2019) Ioana M. Ilie et al.   CHEMICAL REVIEWS

Considerations for the Use of Polyphenols as Therapies in Neurodegenerative Diseases

(2019) Justine Renaud et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Elucidating Tau function and dysfunction in the era of cryo-EM

(2019) Guy Lippens et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antagonistic Activity of Naphthoquinone-Based Hybrids toward Amyloids Associated with Alzheimer’s Disease and Type-2 Diabetes

(2019) Ashim Paul et al.   ACS Chemical Neuroscience

How worthwhile is methylene blue as a treatment of malaria?

(2019) Olaf Müller et al.   Expert Review of Anti-Infective Therapy

The complexity of tau in Alzheimer’s disease

(2019) Nima N. Naseri et al.   NEUROSCIENCE LETTERS

Tau local structure shields an amyloid-forming motif and controls aggregation propensity

(2019) Dailu Chen et al.   Nature Communications

Purpurin modulates Tau-derived VQIVYK fibrillization and ameliorates Alzheimer’s disease-like symptoms in animal model

(2019) Guru Krishnakumar Viswanathan et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Disclosing the Mechanism of Spontaneous Aggregation and Template-Induced Misfolding of the Key Hexapeptide (PHF6) of Tau Protein Based on Molecular Dynamics Simulation

(2019) Hongli Liu et al.   ACS Chemical Neuroscience

Structure-based inhibitors halt prion-like seeding by Alzheimer's disease–and tauopathy–derived brain tissue samples

(2019) Paul Matthew Seidler et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Prospective Repurposing of Dantrolene as a Multitarget Agent for Alzheimer’s Disease

(2019) Bolognino et al.   MOLECULES

New Antiparasitic Bis‐Naphthoquinone Derivatives

(2019) Jana Jentzsch et al.   CHEMISTRY & BIODIVERSITY

Usnic acid derivatives as tau-aggregation and neuroinflammation inhibitors

(2019) Cun-Jian Shi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tau-Cofactor Complexes as Building Blocks of Tau Fibrils

(2019) Yann Fichou et al.   Frontiers in Neuroscience

Structural Basis of Small Molecule Targetability of Monomeric Tau Protein

(2018) Róbert Kiss et al.   ACS Chemical Neuroscience

Integrating in vitro and in silico approaches to evaluate the “dual functionality” of palmatine chloride in inhibiting and disassembling Tau-derived VQIVYK peptide fibrils

(2018) Esraa Haj et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Inhibition of tau-derived hexapeptide aggregation and toxicity by a self-assembled cyclic d,l-α-peptide conformational inhibitor

(2018) A. Belostozky et al.   CHEMICAL COMMUNICATIONS

Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

(2018) Mengchen Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Modeling Prion-Like Processing of Tau Protein in Alzheimer’s Disease for Pharmaceutical Development

(2018) Claude M. Wischik et al.   JOURNAL OF ALZHEIMERS DISEASE

Tau-targeting therapies for Alzheimer disease

(2018) Erin E. Congdon et al.   Nature Reviews Neurology

Enfermedad de Alzheimer de inicio precoz y de inicio tardío: ¿son la misma entidad?

(2018) P. Tellechea et al.   NEUROLOGIA

Clearance of Amyloid Beta and Tau in Alzheimer’s Disease: from Mechanisms to Therapy

(2018) Shu-Hui Xin et al.   NEUROTOXICITY RESEARCH

Tau and neuroinflammation: What impact for Alzheimer's Disease and Tauopathies?

(2018) Cyril Laurent et al.   Biomedical Journal

Synthesis and evaluation of 1,2,3,4-tetrahydro-1-acridone analogues as potential dual inhibitors for amyloid-beta and tau aggregation

(2018) Peng Lv et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Biomarkers for Alzheimer's disease: current status and prospects for the future

(2018) K. Blennow et al.   JOURNAL OF INTERNAL MEDICINE

A new era for understanding amyloid structures and disease

(2018) Matthew G. Iadanza et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Continental and Antarctic Lichens: isolation, identification and molecular modeling of the depside tenuiorin from the Antarctic lichen Umbilicaria antarctica as tau protein inhibitor

(2018) Francisco Salgado et al.   NATURAL PRODUCT RESEARCH

Alzheimer's disease: The right drug, the right time

(2018) Todd E. Golde et al.   SCIENCE

Tau protein aggregation in Alzheimer's disease: An attractive target for the development of novel therapeutic agents

(2017) Marie Jouanne et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Curcumin Inhibits Tau Aggregation and Disintegrates Preformed Tau Filaments in vitro

(2017) Jitendra Subhash Rane et al.   JOURNAL OF ALZHEIMERS DISEASE

Rosmarinic acid prevents fibrillization and diminishes vibrational modes associated to β sheet in tau protein linked to Alzheimer’s disease

(2017) Alberto Cornejo et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

The Essential Medicinal Chemistry of Curcumin

(2017) Kathryn M. Nelson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Vitamin K and osteoporosis: Myth or reality?

(2017) Andrea Palermo et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Synaptic Dysfunction in Alzheimer’s Disease: Aβ, Tau, and Epigenetic Alterations

(2017) Ke Li et al.   MOLECULAR NEUROBIOLOGY

Practical considerations for choosing a mouse model of Alzheimer’s disease

(2017) Joanna L. Jankowsky et al.   Molecular Neurodegeneration

Cryo-EM structures of tau filaments from Alzheimer’s disease

(2017) Anthony W. P. Fitzpatrick et al.   NATURE

Structure-based inhibitors of tau aggregation

(2017) P. M. Seidler et al.   Nature Chemistry

Amyloidogenesis of Tau protein

(2017) Bartosz Nizynski et al.   PROTEIN SCIENCE

Propagation of Tau aggregates

(2017) Michel Goedert et al.   Molecular Brain

Apparent Behavioral Benefits of Tau Overexpression in P301L Tau Transgenic Mice

(2017) Dave Morgan et al.   JOURNAL OF ALZHEIMERS DISEASE

Selection and Characterization of Tau Binding ᴅ-Enantiomeric Peptides with Potential for Therapy of Alzheimer Disease

(2017) Christina Dammers et al.   PLoS One

Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors

(2016) Michiaki Okuda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tau and tauopathies

(2016) Thomas Arendt et al.   BRAIN RESEARCH BULLETIN

Selective Inhibition of Aggregation and Toxicity of a Tau-Derived Peptide using Its Glycosylated Analogues

(2016) Moran Frenkel-Pinter et al.   CHEMISTRY-A EUROPEAN JOURNAL

Inhibition of tau aggregation using a naturally-occurring cyclic peptide scaffold

(2016) Conan K. Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Feeling Nature’s PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS)

(2016) Jonathan B. Baell   JOURNAL OF NATURAL PRODUCTS

Beta-Amyloid and Tau-Protein: Structure, Interaction, and Prion-Like Properties

(2015) O. G. Tatarnikova et al.   BIOCHEMISTRY-MOSCOW

Interaction of Aβ1–42 Amyloids with Lipids Promotes “Off-Pathway” Oligomerization and Membrane Damage

(2015) Sarah Henry et al.   BIOMACROMOLECULES

NO-donor thiacarbocyanines as multifunctional agents for Alzheimer’s disease

(2015) Konstantin Chegaev et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Methylene Blue Attenuates Traumatic Brain Injury-Associated Neuroinflammation and Acute Depressive-Like Behavior in Mice

(2015) Ashley M. Fenn et al.   JOURNAL OF NEUROTRAUMA

Tau Assembly: The Dominant Role of PHF6 (VQIVYK) in Microtubule Binding Region Repeat R3

(2015) Pritam Ganguly et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Tau in physiology and pathology

(2015) Yipeng Wang et al.   NATURE REVIEWS NEUROSCIENCE

Toxic tau oligomer formation blocked by capping of cysteine residues with 1,2-dihydroxybenzene groups

(2015) Yoshiyuki Soeda et al.   Nature Communications

PE859, a Novel Tau Aggregation Inhibitor, Reduces Aggregated Tau and Prevents Onset and Progression of Neural Dysfunction In Vivo

(2015) Michiaki Okuda et al.   PLoS One

A novel in vivo model of tau propagation with rapid and progressive neurofibrillary tangle pathology: the pattern of spread is determined by connectivity, not proximity

(2014) Zeshan Ahmed et al.   ACTA NEUROPATHOLOGICA

Tau aggregation and its interplay with amyloid-β

(2014) Rebecca M. Nisbet et al.   ACTA NEUROPATHOLOGICA

Shogaol–huprine hybrids: Dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties

(2014) F. Javier Pérez-Areales et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies

(2014) Ornella Di Pietro et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of dual targeting inhibitors against aggregations of amyloid-β and tau protein

(2014) Shinichiro Fuse et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Multitarget Biological Profiling of a Novel Family of Rhein Derivatives As Disease-Modifying Anti-Alzheimer Agents

(2014) Elisabet Viayna et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

Proteopathic tau seeding predicts tauopathy in vivo

(2014) B. B. Holmes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of several quinones on insulin aggregation

(2014) Hao Gong et al.   Scientific Reports

Amyloid-β and Tau

(2014) George S. Bloom   JAMA Neurology

Tau-Derived-Hexapeptide 306VQIVYK311 Aggregation Inhibitors: Nitrocatechol Moiety as A Pharmacophore In Drug Design

(2013) Tarek Mohamed et al.   ACS Chemical Neuroscience

Molecular mechanisms of neuropathological changes in Alzheimer’s disease: a review

(2013) Omar Šerý et al.   FOLIA NEUROPATHOLOGICA

Benefits of polyphenols on gut microbiota and implications in human health

(2013) Fernando Cardona et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Inhibition of Tau Filament Formation by Conformational Modulation

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

Tau pathology and neurodegeneration

(2013) Maria Grazia Spillantini et al.   LANCET NEUROLOGY

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

Developing Therapeutic Approaches to Tau, Selected Kinases, and Related Neuronal Protein Targets

(2013) V. M.-Y. Lee et al.   Cold Spring Harbor Perspectives in Medicine

Biochemistry and Cell Biology of Tau Protein in Neurofibrillary Degeneration

(2013) E.-M. Mandelkow et al.   Cold Spring Harbor Perspectives in Medicine

Tau Oligomers as Potential Targets for Immunotherapy for Alzheimers Disease and Tauopathies

(2011) C. A. Lasagna-Reeves et al.   Current Alzheimer Research

Tau as a Therapeutic Target for Alzheimers Disease

(2011) A. Boutajangout et al.   Current Alzheimer Research

In Vivo Microdialysis Reveals Age-Dependent Decrease of Brain Interstitial Fluid Tau Levels in P301S Human Tau Transgenic Mice

(2011) K. Yamada et al.   JOURNAL OF NEUROSCIENCE

Macrocyclic β-Sheet Peptides That Inhibit the Aggregation of a Tau-Protein-Derived Hexapeptide

(2011) Jing Zheng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structure-based design of non-natural amino-acid inhibitors of amyloid fibril formation

(2011) Stuart A. Sievers et al.   NATURE

New insights on the interaction mechanism between tau protein and oleocanthal, an extra-virgin olive-oil bioactive component

(2011) Maria Chiara Monti et al.   Food & Function

Tau protein and tau aggregation inhibitors

(2010) Bruno Bulic et al.   NEUROPHARMACOLOGY

Tau-directed drug discovery for Alzheimer's disease and related tauopathies: A focus on tau assembly inhibitors

(2009) Kurt R. Brunden et al.   EXPERIMENTAL NEUROLOGY

9,10-Anthraquinone hinders β-aggregation: How does a small molecule interfere with Aβ-peptide amyloid fibrillation?

(2009) Marino Convertino et al.   PROTEIN SCIENCE

Tau phosphorylation: the therapeutic challenge for neurodegenerative disease

(2009) Diane P. Hanger et al.   TRENDS IN MOLECULAR MEDICINE

Nucleation-dependent Tau Filament Formation

(2008) Erin E. Congdon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY