S-Dimethylarsino-glutathione (darinaparsin®) targets histone H3.3, leading to TRAIL-induced apoptosis in leukemia cells.

Authors :: Xu X
Wang H
Li H
Hu X
Zhang Y
Guan X
Toy PH
Sun H
Source :: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2019 Oct 29; Vol. 55 (87), pp. 13120-13123.
Publication Year :: 2019
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.

Subjects :: Antineoplastic Agents chemistry
Arsenicals chemistry
Cell Line, Tumor
Drug Screening Assays, Antitumor
Glutathione chemistry
Glutathione pharmacology
Histones metabolism
Humans
Leukemia, Promyelocytic, Acute pathology
Molecular Structure
TNF-Related Apoptosis-Inducing Ligand metabolism
Antineoplastic Agents pharmacology
Apoptosis drug effects
Arsenicals pharmacology
Glutathione analogs & derivatives
Histones antagonists & inhibitors
Leukemia, Promyelocytic, Acute drug therapy
TNF-Related Apoptosis-Inducing Ligand antagonists & inhibitors

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