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PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea.


ABSTRACT: 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 IC50 value of 3.24 ?M and 0.59 ?M.

SUBMITTER: Zhang J 

PROVIDER: S-EPMC6149825 | biostudies-other | 2017 Nov

REPOSITORIES: biostudies-other

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PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea.

Zhang Jun J   Meng Lin-Lin LL   Wei Jing-Jing JJ   Fan Peng P   Liu Sha-Sha SS   Yuan Wei-Yu WY   Zhao You-Xing YX   Luo Du-Qiang DQ  

Molecules (Basel, Switzerland) 20171124 12


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  ...[more]

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