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Media type:
E-Article
Title:
Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β
Contributor:
Wiese, Jutta
[Author];
Imhoff, Johannes F.
[Author];
Gulder, Tobias
[Author];
Labes, Antje
[Author];
Schmaljohann, Rolf
[Author]
imprint:
MDPI, 2016
Language:
English
DOI:
https://doi.org/10.3390/md14110200
Origination:
Footnote:
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Description:
The glycogen-synthase-kinase 3 (GSK-3) is an important target in drug discovery. This enzyme is involved in the signaling pathways of type 2 diabetes, neurological disorders, cancer, and other diseases. Therefore, inhibitors of GSK-3 are promising drug candidates for the treatment of a broad range of diseases. Here we report pannorin (1), alternariol (2), and alternariol-9-methylether (3) to be promising inhibitors of the isoform GSK-3β showing sub-μM IC50 values. The in vitro inhibition is in the range of the known highly active GSK-3β inhibitor TDZD-8. Compounds 1–3 have a highly oxygenated benzocoumarin core structure in common, which suggests that this may be a new structural feature for efficient GSK-3β inhibition