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Anthraquinones Inhibit Tau Aggregation and Dissolve Alzheimer’s Paired Helical Filaments in Vitro and in Cells* (EMODIN)
http://www.mpasmb-hamburg.mpg.de/mand-pdf/Pickhardt_et_al_(2005)_JBC.pdf
1. The abnormal aggregation of tau protein into paired helical filaments (PHFs) is one of the hallmarks of Alzheimer’s disease.
2. Compounds sharing a core structure of Hydroxyanthraquinone inhibit PHF assembly.
3. PHFs can be dissolved by Inhibitor Compounds: Inhibiting the aggregation is one important aspect of a potential therapeutic compound, but even more important may be the ability to dissolve preformed filaments.
We tested 200,000 compounds in a high throughput screen for their capability of interfering with the aggregation of tau protein. Several members of the class of hydroxyanthraquinone and related structures were found. They all share a tricyclic aromatic ring system with some modifications. Emodin and compound PHF016 belong to the class of hydroxyanthraquinones, whereas compound PHF005 represents a benzophenone derivative. Daunorubicin and adriamycin are enlarged with a further ring system to the naphthacendione structure and a sugar moiety.
http://www.mpasmb-hamburg.mpg.de/mand-pdf/Pickhardt_et_al_(2005)_JBC.pdf
1. The abnormal aggregation of tau protein into paired helical filaments (PHFs) is one of the hallmarks of Alzheimer’s disease.
2. Compounds sharing a core structure of Hydroxyanthraquinone inhibit PHF assembly.
3. PHFs can be dissolved by Inhibitor Compounds: Inhibiting the aggregation is one important aspect of a potential therapeutic compound, but even more important may be the ability to dissolve preformed filaments.
We tested 200,000 compounds in a high throughput screen for their capability of interfering with the aggregation of tau protein. Several members of the class of hydroxyanthraquinone and related structures were found. They all share a tricyclic aromatic ring system with some modifications. Emodin and compound PHF016 belong to the class of hydroxyanthraquinones, whereas compound PHF005 represents a benzophenone derivative. Daunorubicin and adriamycin are enlarged with a further ring system to the naphthacendione structure and a sugar moiety.
