Enhancement of the Antileukemic Action of the Inhibitors of DNA and Histone Methylation: 5-Aza-2'-Deoxycytidine and 3-Deazaneplanocin-A by Vitamin C.

ABSTRACT: Epigenetic gene silencing by DNA methylation and histone methylation by EZH2 play an important role in the development of acute myeloid leukemia (AML). EZH2 catalyzes the trimethylation of histone H3-lysine 27-trimethylated (H3K27me3). These epigenetic alterations silence the expression of the genes that suppress leukemogenesis. Reversal of this gene silencing by 5-aza-2'-deoxycytidine (5-Aza-CdR), an inhibitor of DNA methylation, and by 3-deazaneplanocin-A (DZNep), an inhibitor of EZH2, results in synergistic gene reactivation and antileukemic interaction. The objective of this study is to determine if the addition of another epigenetic agent could further enhance the antileukemic action of these inhibitors of DNA and histone methylation. Vitamin C (Vit C) is reported to enhance the antin

SUBMITTER: Momparler RL 

PROVIDER: S-EPMC8594729 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature