publication . Article . Other literature type . 2009

DNA (Cytosine-C5) Methyltransferase Inhibition by Oligodeoxyribonucleotides Containing 2-(1H)-Pyrimidinone (Zebularine Aglycon) at the Enzymatic Target Site

Van Bemmel, Dana M.; Brank, Adam S.; Eritja Casadellà, Ramón; Márquez, Víctor E.; Christman, Judith K.;
Open Access English
  • Published: 23 May 2009
  • Publisher: Elsevier
Abstract
Aberrant cytosine methylation in promoter regions leads to gene silencing associated with cancer progression. A number of DNA methyltransferase inhibitors are known to reactivate silenced genes; including 5-azacytidine and 2-(1H)-pyrimidinone riboside (zebularine). Zebularine is a more stable, less cytotoxic inhibitor compared to 5-azacytidine. To determine the mechanistic basis for this difference, we carried out a detailed comparisons of the interaction between purified DNA methyltransferases and oligodeoxyribonucleotides (ODNs) containing either 5-azacytosine or 2-(1H)-pyrimidinone in place of the cytosine targeted for methylation. When incorporated into smal...
Subjects
free text keywords: DNA methylation, Zebularine, 2(1H)-Pyrimidinone riboside, Article, DNA methyltransferase, 5-aza-2'-deoxycytidine
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publication . Article . Other literature type . 2009

DNA (Cytosine-C5) Methyltransferase Inhibition by Oligodeoxyribonucleotides Containing 2-(1H)-Pyrimidinone (Zebularine Aglycon) at the Enzymatic Target Site

Van Bemmel, Dana M.; Brank, Adam S.; Eritja Casadellà, Ramón; Márquez, Víctor E.; Christman, Judith K.;