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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MDPI AG
2017-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/22/12/2058 |
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| author | Jun Zhang Lin-Lin Meng Jing-Jing Wei Peng Fan Sha-Sha Liu Wei-Yu Yuan You-Xing Zhao Du-Qiang Luo |
| author_facet | Jun Zhang Lin-Lin Meng Jing-Jing Wei Peng Fan Sha-Sha Liu Wei-Yu Yuan You-Xing Zhao Du-Qiang Luo |
| author_sort | Jun Zhang |
| collection | DOAJ |
| 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 IC50 value of 3.24 μM and 0.59 μM. |
| first_indexed | 2024-12-13T07:43:13Z |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T07:43:13Z |
| publishDate | 2017-11-01 |
| publisher | MDPI AG |
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| series | Molecules |
| spelling | doaj.art-85ffaa343efc4e40ae661c8b3371daf52022-12-21T23:54:54ZengMDPI AGMolecules1420-30492017-11-012212205810.3390/molecules22122058molecules22122058PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosoroseaJun Zhang0Lin-Lin Meng1Jing-Jing Wei2Peng Fan3Sha-Sha Liu4Wei-Yu Yuan5You-Xing Zhao6Du-Qiang Luo7College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaCollege of Pharmaceutical Science, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaInstitute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaProtein 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 μM and 0.59 μM.https://www.mdpi.com/1420-3049/22/12/2058Isaria fumosoroseaPTP1Bpyrrolidinedione |
| spellingShingle | Jun Zhang Lin-Lin Meng Jing-Jing Wei Peng Fan Sha-Sha Liu Wei-Yu Yuan You-Xing Zhao Du-Qiang Luo PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea Molecules Isaria fumosorosea PTP1B pyrrolidinedione |
| 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 | Isaria fumosorosea PTP1B pyrrolidinedione |
| url | https://www.mdpi.com/1420-3049/22/12/2058 |
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