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Medientyp:
E-Artikel
Titel:
Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β
Beteiligte:
Wiese, Jutta
[Verfasser:in];
Imhoff, Johannes F.
[Verfasser:in];
Gulder, Tobias
[Verfasser:in];
Labes, Antje
[Verfasser:in];
Schmaljohann, Rolf
[Verfasser:in]
Erschienen:
MDPI, 2016
Sprache:
Englisch
DOI:
https://doi.org/10.3390/md14110200
Entstehung:
Anmerkungen:
Diese Datenquelle enthält auch Bestandsnachweise, die nicht zu einem Volltext führen.
Beschreibung:
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