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Mar. Drugs 2017, 15(6), 191; doi:10.3390/md15060191

Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B

1
GEOMAR Helmholtz Center for Ocean Research Kiel, RD3 Marine Microbiology, Düsternbrooker Weg 20, 24105 Kiel, Germany
2
Department of Chemistry and Center for Integrated Protein Science Munich (CIPSM), Biosystems Chemistry, Technical University of Munich, Lichtenbergstraße 4, 85747 Garching, Germany
*
Authors to whom correspondence should be addressed.
Academic Editor: Russell Kerr
Received: 31 January 2017 / Revised: 13 June 2017 / Accepted: 17 June 2017 / Published: 21 June 2017
(This article belongs to the Special Issue Marine Fungal Natural Products)
View Full-Text   |   Download PDF [594 KB, uploaded 21 June 2017]   |  

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. View Full-Text
Keywords: PTP1B; cladosporin; asperentin; Aspergillus; deep-sea PTP1B; cladosporin; asperentin; Aspergillus; deep-sea
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MDPI and ACS Style

Wiese, J.; Aldemir, H.; Schmaljohann, R.; Gulder, T.A.M.; Imhoff, J.F. Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B. Mar. Drugs 2017, 15, 191.

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