Next Article in Journal
Chemistry and Bioactivity of Briaranes from the South China Sea Gorgonian Dichotella gemmacea
Next Article in Special Issue
Phomopsichin A–D; Four New Chromone Derivatives from Mangrove Endophytic Fungus Phomopsis sp. 33#
Previous Article in Journal
Novel Conopeptides of Largely Unexplored Indo Pacific Conus sp.
Previous Article in Special Issue
Dihydroisocoumarins from the Mangrove-Derived Fungus Penicillium citrinum
Article Menu

Export Article

Open AccessArticle
Mar. Drugs 2016, 14(11), 200; doi:10.3390/md14110200

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
*
Author to whom correspondence should be addressed.
Academic Editor: Russell Kerr
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)
View Full-Text   |   Download PDF [959 KB, uploaded 28 October 2016]   |  

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 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
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top