The DOI matches its Crossref record; 275 of the 278 references it cites were found in a registry or an index.
Small molecule therapeutics for tauopathy in Alzheimer’s disease: Walking on the path of most resistance
Open accessAbstract
Alzheimer's disease (AD) is the most common form of dementia characterized by presence of extracellular amyloid plaques and intracellular neurofibrillary tangles composed of tau protein. Currently there are close to 50 million people living with dementia and this figure is expected to increase to 75 million by 2030 putting a huge burden on the economy due to the health care cost. Considering the effects on quality of life of patients and the increasing burden on the economy, there is an enormous need of new disease modifying therapies to tackle this disease. The current therapies are dominated by only symptomatic treatments including cholinesterase inhibitors and N-methyl-D-aspartate receptor blockers but no disease modifying treatments exist so far. After several failed attempts to develop drugs against amyloidopathy, tau targeting approaches have been in the main focus of drug development against AD. After an overview of the tauopathy in AD, this review summarizes recent findings on the development of small molecules as therapeutics targeting tau modification, aggregation, and degradation, and tau-oriented multi-target directed ligands. Overall, this work aims to provide a comprehensive and critical overview of small molecules which are being explored as a lead candidate for discovering drugs against tauopathy in AD.
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“Methylene blue blocks the polymerisation of tau in vitro by trapping the tau monomers in an aggregation-incompetent conformation.”
From Role of Tau Protein in Neurodegenerative Diseases and Development of Its Targeted Drugs: A Literature Review (2024) · cites this paper as [190]
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Metadata
- Authors
- Wang, L., Bharti, Kumar, R., Pavlov, P. F., & Winblad, B.
- Affiliations
- Karolinska Institutet (SE)
- Karolinska University Hospital (SE)
- Corresponding author
- Winblad, Bengt
- Venue
- European Journal of Medicinal Chemistry
- Publisher
- Elsevier BV
- Published
- 2021-01
- Volume
- 209
- Pages
- 112915
- ISSN
- 0223-5234 (ISSN-L)
- OpenAlex
- W3092711150
- Cited by
- 92
- References
- 278
- Citations by year
- 2026: 5 · 2025: 21 · 2024: 15 · 2023: 22 · 2022: 21 · 2021: 7
- FWCI
- 1.63
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- European Journal of Medicinal Chemistry (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- Loo och Hans Ostermans Stiftelse för Medicinsk Forskning
- Gun och Bertil Stohnes Stiftelse
- Margareta af Ugglas Foundation
- Vetenskapsrådet (2015\u201302774, 2018\u201302843)
- Banaras Hindu University
- Karolinska Institutet
- Hjärnfonden
- Magnus Bergvalls Stiftelse
- Gunvor och Josef Anérs Siftelse
- Stiftelsen för Gamla Tjänarinnor
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Pharmacology (medical) › Cholinesterase and Neurodegenerative Diseases
- Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
- Keywords
- Alzheimer's disease, tauopathy, tau protein, small molecule drugs, tau aggregation, tau degradation, multi-target-directed ligands, disease-modifying therapy, drug development, neurofibrillary tangles
- MeSH terms
- Alzheimer Disease, Animals, Cholinesterase Inhibitors, Cholinesterases, Curcumin, Humans, Phosphorylation, Protein Processing, Post-Translational, Quinazolines, Thiadiazoles, Receptors, N-Methyl-D-Aspartate, Neurofibrillary Tangles, tau Proteins, Neuroprotective Agents, Benzodioxoles, Plaque, Amyloid, Molecular Targeted Therapy, Protein Aggregation, Pathological
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