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Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes

Protein tyrosine phosphatase 1B (PTP1B) is implicated as a negative regulator of insulin receptor (IR) signaling and a potential drug target for the treatment of type II diabetes and other associated metabolic syndromes. Therefore, small molecular inhibitors of PTP1B can be considered as an attracti...

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Autores principales: Chen, Yu-Peng, Yang, Chun-Gui, Wei, Pei-Yao, Li, Lin, Luo, Du-Qiang, Zheng, Zhi-Hui, Lu, Xin-Hua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270892/
https://www.ncbi.nlm.nih.gov/pubmed/24481115
http://dx.doi.org/10.3390/molecules19021663
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author Chen, Yu-Peng
Yang, Chun-Gui
Wei, Pei-Yao
Li, Lin
Luo, Du-Qiang
Zheng, Zhi-Hui
Lu, Xin-Hua
author_facet Chen, Yu-Peng
Yang, Chun-Gui
Wei, Pei-Yao
Li, Lin
Luo, Du-Qiang
Zheng, Zhi-Hui
Lu, Xin-Hua
author_sort Chen, Yu-Peng
collection PubMed
description Protein tyrosine phosphatase 1B (PTP1B) is implicated as a negative regulator of insulin receptor (IR) signaling and a potential drug target for the treatment of type II diabetes and other associated metabolic syndromes. Therefore, small molecular inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes diseases. In a continuing search for new protein phosphatase inhibitors from fungi, we have isolated a new compound, named penostatin J (1), together with three known ones, penostatin C (2), penostatin A (3), and penostatin B (4), from cultures of the entomogenous fungus Isaria tenuipes. The structure of penostatin J (1) was elucidated by extensive spectroscopic analysis. We also demonstrate for the first time that penostatin derivatives exhibit the best PTP1B inhibitory action. These findings suggest that penostatin derivatives are a potential novel kind of PTP1B inhibitors.
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spelling pubmed-62708922018-12-20 Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes Chen, Yu-Peng Yang, Chun-Gui Wei, Pei-Yao Li, Lin Luo, Du-Qiang Zheng, Zhi-Hui Lu, Xin-Hua Molecules Article Protein tyrosine phosphatase 1B (PTP1B) is implicated as a negative regulator of insulin receptor (IR) signaling and a potential drug target for the treatment of type II diabetes and other associated metabolic syndromes. Therefore, small molecular inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes diseases. In a continuing search for new protein phosphatase inhibitors from fungi, we have isolated a new compound, named penostatin J (1), together with three known ones, penostatin C (2), penostatin A (3), and penostatin B (4), from cultures of the entomogenous fungus Isaria tenuipes. The structure of penostatin J (1) was elucidated by extensive spectroscopic analysis. We also demonstrate for the first time that penostatin derivatives exhibit the best PTP1B inhibitory action. These findings suggest that penostatin derivatives are a potential novel kind of PTP1B inhibitors. MDPI 2014-01-29 /pmc/articles/PMC6270892/ /pubmed/24481115 http://dx.doi.org/10.3390/molecules19021663 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Chen, Yu-Peng
Yang, Chun-Gui
Wei, Pei-Yao
Li, Lin
Luo, Du-Qiang
Zheng, Zhi-Hui
Lu, Xin-Hua
Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title_full Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title_fullStr Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title_full_unstemmed Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title_short Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes
title_sort penostatin derivatives, a novel kind of protein phosphatase 1b inhibitors isolated from solid cultures of the entomogenous fungus isaria tenuipes
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270892/
https://www.ncbi.nlm.nih.gov/pubmed/24481115
http://dx.doi.org/10.3390/molecules19021663
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