ArticleJournal of medicinal chemistry2009
Structure-activity relationship of cyanine tau aggregation inhibitors.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
25 citing papers in PubMed.
- Molecular Deformation Is a Key Factor in Screening Aggregation Inhibitor for Intrinsically Disordered Protein Tau.ACS central science · 2024Article
- Sedimentation and Laser Light Scattering Methods for Quantifying Synthetic Tau Aggregation Propensity.Methods in molecular biology (Clifton, N.J.) · 2024Article
- Structure, physicochemical properties, and adsorption performance of the ethyl cellulose/bentonite composite films.Cellulose (London, England) · 2022Article
- Sulfur-containing therapeutics in the treatment of Alzheimer's disease.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021Article
- Therapeutic Strategies to Reduce the Toxicity of Misfolded Protein Oligomers.International journal of molecular sciences · 2020Review
- Pharmacological Modulators of Tau Aggregation and Spreading.Brain sciences · 2020Review
- Review
- Targeting Amyloid Aggregation: An Overview of Strategies and Mechanisms.International journal of molecular sciences · 2018Review
- Interactions between Microtubule-Associated Protein Tau (MAPT) and Small Molecules.Cold Spring Harbor perspectives in medicine · 2017Review
- Detection and Quantification Methods for Fibrillar Products of In Vitro Tau Aggregation Assays.Methods in molecular biology (Clifton, N.J.) · 2017Article
- Analyzing Tau Aggregation with Electron Microscopy.Methods in molecular biology (Clifton, N.J.) · 2016Article
- Tau-Centric Targets and Drugs in Clinical Development for the Treatment of Alzheimer's Disease.BioMed research international · 2016Review
- Azaphilones inhibit tau aggregation and dissolve tau aggregates in vitro.ACS chemical neuroscience · 2015Article
- Structure and mechanism of action of tau aggregation inhibitors.Current Alzheimer research · 2014Review
- Structural determinants of Tau aggregation inhibitor potency.The Journal of biological chemistry · 2013Article
- Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation.The Journal of biological chemistry · 2013Article
- Cornel Iridoid Glycoside Attenuates Tau Hyperphosphorylation by Inhibition of PP2A Demethylation.Evidence-based complementary and alternative medicine : eCAM · 2013Article
- Potential synergy between tau aggregation inhibitors and tau chaperone modulators.Alzheimer's research & therapy · 2013Review
- Tau as a therapeutic target in neurodegenerative disease.Pharmacology & therapeutics · 2012Review
- Advances in tau-based drug discovery.Expert opinion on drug discovery · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors.
Funding
Abstract
A structure-activity relationship for symmetrical cyanine inhibitors of human tau aggregation was elaborated using a filter trap assay. Antagonist activity depended on cyanine heterocycle, polymethine bridge length, and the nature of meso- and N-substituents. One potent member of the series, 3,3'-diethyl-9-methylthiacarbocyanine iodide (compound 11), retained submicromolar potency and had calculated physical properties consistent with blood-brain barrier and cell membrane penetration. Exposure of organotypic slices prepared from JNPL3 transgenic mice (which express human tau harboring the aggregation prone P301L tauopathy mutation) to compound 11 for one week revealed a biphasic dose response relationship. Low nanomolar concentrations decreased insoluble tau aggregates to half those observed in slices treated with vehicle alone. In contrast, high concentrations (> or =300 nM) augmented tau aggregation and produced abnormalities in tissue tubulin levels. These data suggest that certain symmetrical carbocyanine dyes can modulate tau aggregation in the slice biological model at concentrations well below those associated with toxicity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.