PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea
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. Thus, small molecule inhibitors of PTP1B can be considered as an attractive app...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6149825/ https://www.ncbi.nlm.nih.gov/pubmed/29186763 http://dx.doi.org/10.3390/molecules22122058 |
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author | Zhang, Jun Meng, Lin-Lin Wei, Jing-Jing Fan, Peng Liu, Sha-Sha Yuan, Wei-Yu Zhao, You-Xing Luo, Du-Qiang |
author_facet | Zhang, Jun Meng, Lin-Lin Wei, Jing-Jing Fan, Peng Liu, Sha-Sha Yuan, Wei-Yu Zhao, You-Xing Luo, Du-Qiang |
author_sort | Zhang, Jun |
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. Thus, small molecule inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes and cancer diseases. In a continuing search for new PTP1B inhibitors, a new tetramic acid possessing a rare pyrrolidinedione skeleton named fumosorinone A (1), together with five known ones 2–6 were isolated from the entomogenous fungus Isaria fumosorosea. The structures of 2–6 were elucidated by extensive spectroscopic analysis. Fumosorinone A (1) and beauvericin (6) showed significant PTP1B inhibitory activity with IC(50) value of 3.24 μM and 0.59 μM. |
format | Online Article Text |
id | pubmed-6149825 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61498252018-11-13 PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea Zhang, Jun Meng, Lin-Lin Wei, Jing-Jing Fan, Peng Liu, Sha-Sha Yuan, Wei-Yu Zhao, You-Xing Luo, Du-Qiang 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. Thus, small molecule inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes and cancer diseases. In a continuing search for new PTP1B inhibitors, a new tetramic acid possessing a rare pyrrolidinedione skeleton named fumosorinone A (1), together with five known ones 2–6 were isolated from the entomogenous fungus Isaria fumosorosea. The structures of 2–6 were elucidated by extensive spectroscopic analysis. Fumosorinone A (1) and beauvericin (6) showed significant PTP1B inhibitory activity with IC(50) value of 3.24 μM and 0.59 μM. MDPI 2017-11-24 /pmc/articles/PMC6149825/ /pubmed/29186763 http://dx.doi.org/10.3390/molecules22122058 Text en © 2017 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 (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Zhang, Jun Meng, Lin-Lin Wei, Jing-Jing Fan, Peng Liu, Sha-Sha Yuan, Wei-Yu Zhao, You-Xing Luo, Du-Qiang PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title | PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title_full | PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title_fullStr | PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title_full_unstemmed | PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title_short | PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea |
title_sort | ptp1b inhibitors from the entomogenous fungi isaria fumosorosea |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6149825/ https://www.ncbi.nlm.nih.gov/pubmed/29186763 http://dx.doi.org/10.3390/molecules22122058 |
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