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Open AccessArticle

Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β

1
GEOMAR Helmholtz Center for Ocean Research Kiel, Marine Microbiology, Düsternbrooker Weg 20, 24105 Kiel, Germany
2
Biosystems Chemistry, Department of Chemistry and Center for Integrated Protein Science Munich (CISPM), Technical University of Munich, Lichtenbergstraße 4, 85748 Garching, Germany
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Author to whom correspondence should be addressed.
Academic Editor: Russell Kerr
Mar. Drugs 2016, 14(11), 200; https://doi.org/10.3390/md14110200
Received: 12 August 2016 / Revised: 17 October 2016 / Accepted: 22 October 2016 / Published: 28 October 2016
(This article belongs to the Special Issue Marine Fungal Natural Products)
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 13 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
Keywords: GSK-3β; pannorin; alternariol; alternariol-9-methyl ether; Aspergillus; Botrytinia; deep-sea GSK-3β; pannorin; alternariol; alternariol-9-methyl ether; Aspergillus; Botrytinia; deep-sea
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MDPI and ACS Style

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.

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