Abstract
Histone H3.3 was identified as an arsenic-binding protein of S-dimethylarsino-glutathione (ZIO-101, darinaparsin®) in leukemia cells by GE-ICP-MS. Such a binding results in TRAIL-induced apoptosis. We further validate histone H3.3 as a vital target for ZIO-101, offering new information on the mode of action of arsenic-based anticancer agents.
MeSH terms
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects*
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Arsenicals / chemistry
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Arsenicals / pharmacology*
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Glutathione / analogs & derivatives*
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Glutathione / chemistry
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Glutathione / pharmacology
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Histones / antagonists & inhibitors*
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Histones / metabolism
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Humans
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Leukemia, Promyelocytic, Acute / drug therapy*
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Leukemia, Promyelocytic, Acute / pathology
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Molecular Structure
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TNF-Related Apoptosis-Inducing Ligand / antagonists & inhibitors*
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TNF-Related Apoptosis-Inducing Ligand / metabolism
Substances
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Antineoplastic Agents
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Arsenicals
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Histones
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TNF-Related Apoptosis-Inducing Ligand
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TNFSF10 protein, human
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darinaparsin
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Glutathione