Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β
AbstractThe 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. View Full-Text
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Wiese, J.; Imhoff, J.F.; Gulder, T.A.M.; Labes, A.; Schmaljohann, R. Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β. Mar. Drugs 2016, 14, 200.
Wiese J, Imhoff JF, Gulder TAM, Labes A, Schmaljohann R. Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β. Marine Drugs. 2016; 14(11):200.Chicago/Turabian Style
Wiese, Jutta; Imhoff, Johannes F.; Gulder, Tobias A.M.; Labes, Antje; Schmaljohann, Rolf. 2016. "Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β." Mar. Drugs 14, no. 11: 200.
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