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| Verfasst von: | Liang, Ting [VerfasserIn]  |
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| | Liu, Shiru [VerfasserIn] |
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| | Dang, Baiyun [VerfasserIn] |
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| | Luan, Xiaofa [VerfasserIn] |
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| | Guo, Yifan [VerfasserIn] |
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| | Steimbach, Raphael R. [VerfasserIn] |
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| | Hu, Jiadong [VerfasserIn] |
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| | Lu, Long [VerfasserIn] |
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| | Yue, Peiyu [VerfasserIn] |
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| | Wang, Ruotian [VerfasserIn] |
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| | Zheng, Meng [VerfasserIn] |
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| | Gao, Jinming [VerfasserIn] |
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| | Yin, Xia [VerfasserIn] |
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| | Chen, Xin [VerfasserIn] |
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| Titel: | Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease |
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| Verf.angabe: | Ting Liang, Shiru Liu, Baiyun Dang, Xiaofa Luan, Yifan Guo, Raphael R. Steimbach, Jiadong Hu, Long Lu, Peiyu Yue, Ruotian Wang, Meng Zheng, Jinming Gao, Xia Yin, Xin Chen |
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| E-Jahr: | 2024 |
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| Jahr: | 5 September 2024 |
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| Umfang: | 18 S. |
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| Illustrationen: | Illustrationen |
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| Fussnoten: | Online verfügbar 24 June 2024, Version des Artikel 25 June 2024 ; Gesehen am 08.01.2025 |
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| Titel Quelle: | Enthalten in: European journal of medicinal chemistry |
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| Ort Quelle: | Amsterdam [u.a.] : Elsevier Science, 1987 |
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| Jahr Quelle: | 2024 |
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| Band/Heft Quelle: | 275(2024) vom: Sept., Artikel-ID 116624, Seite 1-18 |
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| ISSN Quelle: | 1768-3254 |
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| Abstract: | With the intensive research on the pathogenesis of Alzheimer's disease (AD), inhibition of HDAC6 appears to be a potential therapeutic approach for AD. In this paper, a series of tetrahydro-β-carboline derivatives with hydroxamic acid group were fast synthesized. Among all, the most potent 15 selectively inhibited HDAC6 with IC50 of 15.2 nM and markedly increased acetylated alpha-tubulin levels. In cellular assay, 15 showed excellent neurotrophic effect by increasing the expression of GAP43 and Beta-3 tubulin markers. Besides, 15 showed neuroprotective effects in PC12 or SH-SY5Y cells against H2O2 and 6-OHDA injury through activation of Nrf2, catalase and Prx II, and significantly reduced H2O2-induced reactive oxygen species (ROS) production. In vivo, 15 significantly attenuated zebrafish anxiety-like behaviour and memory deficits in a SCOP-induced zebrafish model of AD. To sum up, multifunctional 15 might be a good lead to develop novel tetrahydrocarboline-based agents for the treatment of AD. |
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| DOI: | doi:10.1016/j.ejmech.2024.116624 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1016/j.ejmech.2024.116624 |
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| | Volltext: https://www.sciencedirect.com/science/article/pii/S022352342400504X |
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| | DOI: https://doi.org/10.1016/j.ejmech.2024.116624 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | Alzheimer's disease |
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| | HDAC6 inhibitor |
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| | Multimechanism |
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| | Selectivity |
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| | Tetrahydrocarboline |
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| K10plus-PPN: | 1913786013 |
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| Verknüpfungen: | → Zeitschrift |
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Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease / Liang, Ting [VerfasserIn]; 5 September 2024 (Online-Ressource)
