Global ETD Search
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Showing 1 to 6 of 6 for “"HDAC8"”.
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Structural Studies of Two Related Metallohydrolases: Human Histone Deacetylase 8 and Malarial Arginase
… and other proteins in eukaryotic cells. Isozyme HDAC8 is perhaps the archetypical member of the class I HDAC family and serves as a paradigm for studying structure-function relationships. We report the structures of HDAC8 complexes in a new crystal form. Comparison of unliganded and liganded …
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Entwicklung eines HTS-geeigneten Enzymtests für Histondeacetylasen zur Entwicklung von HDAC-Inhibitoren
… des Assays mit HDAC aus Rattenleber bzw. humaner HDAC8 und Standardinhibitoren sowie die Auffindung von Hemmern in einer kleinen Substanzbibliothek belegte dessen Eignung für HTS-Anwendungen. Der HDAC-Assay konnte im folgenden, vor allem durch die Entwicklung des neuen fluorogenen Substrates …
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An evaluation of cancer biomarkers in normal ovarian epithelial cells and ovarian cancer cell lines
… genes: HDAC1, HDAC2, HDCA3, HDAC5, HDAC6, HDAC7, HDAC8, LPAR1, LPAR2, MUC16 and FOSL1, against normal housekeeping genes GAPDH and HPRT. In addition, immunocytochemistry was also used in the validation process of the aforementioned genes. Significance: ovarian cancer cells express gene signatures, …
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Classical And Ab Initio Qm/mm Simulations Of Bacterial Enzymes
… tested as potential radiotracers, onto HDAC4 and HDAC8 enzymes to calculate/compare their relative binding affinities. The trends in the increase in affinity, of the novel substrates for HDAC4 and HDAC8 active sites calculated by molecular docking, agreed with the experimentally shown trends.</p>
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Part 1 Synthesis of a potent histone deacetylase inhibitor; Part 2 Studies towards a stabilized helix-turn-helix peptide
… with an IC50 value of 46 ± 15 nM, and against HDAC8 with an IC50 value of 208 ± 20 nM. The potent HDAC inhibitory activity of the HDAC inhibitor demonstrates the importance of the rim recognition region in the design of HDIs. The hydrophobic cyclic turn mimic allows the formation of a tight …
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Targeting Histone Deacetylases (Hdac) For The Treatment of Soft Tissue Sarcoma
… which include HDAC1, 2, 3, and 8. Recently, HDAC8-specific inhibitors (HDAC8i) have been created and tested in various cancer cell lines. Lastly, the potential therapeutic efficacy of HDAC8i was investigated in human (NF1-associated and sporadic) and NF1-associated murine-derived MPNST. …