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...

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Autores principales: Zhang, Jun, Meng, Lin-Lin, Wei, Jing-Jing, Fan, Peng, Liu, Sha-Sha, Yuan, Wei-Yu, Zhao, You-Xing, Luo, Du-Qiang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
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.
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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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