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

Wiese, Jutta, Imhoff, Johannes F., Gulder, Tobias, Labes, Antje and Schmaljohann, Rolf (2016) Marine Fungi as Producers of Benzocoumarins, a New Class of Inhibitors of Glycogen-Synthase-Kinase 3β Marine Drugs, 14 (12). p. 200. DOI 10.3390/md14110200.

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Abstract

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

Document Type: Article
Keywords: GSK-3β; pannorin; alternariol; alternariol-9-methyl ether; Aspergillus; Botrytinia; deep-sea
Research affiliation: OceanRep > The Future Ocean - Cluster of Excellence
OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MN Marine natural products chemistry
OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MI Marine Microbiology
Kiel University
Refereed: Yes
DOI etc.: 10.3390/md14110200
ISSN: 1660-3397
Related URLs:
Projects: Future Ocean
Date Deposited: 02 Nov 2016 10:16
Last Modified: 19 Dec 2017 12:42
URI: http://eprints.uni-kiel.de/id/eprint/34530

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