Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B.
Wiese, Jutta , Aldemir, Hülya, Schmaljohann, Rolf, Gulder, Tobias and Imhoff, Johannes F.
(2017)
Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B.
Marine Drugs, 15
(6).
p. 191.
DOI 10.3390/md15060191.
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Abstract
In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of the human protein tyrosine phosphatase 1B (PTP1B), a target in the signaling pathway of insulin. A new asperentin analog is produced by an Aspergillus sydowii strain isolated from the sediment of the deep Mediterranean Sea. Asperentin B (1) contains an additional phenolic hydroxy function at C-6 and exhibits an IC50 value against PTP1B of 2 μM in vitro, which is six times stronger than the positive control, suramin. Interestingly, asperentin (2) did not show any inhibition of this enzymatic activity. Asperentin B (1) is discussed as possible therapeutic agents for type 2 diabetes and sleeping sickness.
Document Type: | Article |
---|---|
Keywords: | PTP1B; cladosporin; asperentin; Aspergillus; deep-sea |
Research affiliation: | OceanRep > The Future Ocean - Cluster of Excellence OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MI Marine Microbiology |
Refereed: | Yes |
Open Access Journal?: | Yes |
DOI etc.: | 10.3390/md15060191 |
ISSN: | 1660-3397 |
Related URLs: | |
Projects: | Future Ocean |
Expeditions/Models/Experiments: | |
Date Deposited: | 07 Jul 2017 12:28 |
Last Modified: | 23 Sep 2019 19:02 |
URI: | http://oceanrep.geomar.de/id/eprint/38765 |
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