Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B
AbstractIn 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
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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.
Wiese J, Aldemir H, Schmaljohann R, Gulder TAM, Imhoff JF. Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B. Marine Drugs. 2017; 15(6):191.Chicago/Turabian Style
Wiese, Jutta; Aldemir, Hülya; Schmaljohann, Rolf; Gulder, Tobias A.M.; Imhoff, Johannes F. 2017. "Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B." Mar. Drugs 15, no. 6: 191.
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