publication . Article . 2003

Potent inhibition of HhaI DNA methylase by the aglycon of 2-(1H)-pyrimidinone riboside (zebularine) at the GCGC recognition domain.

Judith K. Christman; James A. Kelley; Dana Vanbemmel; Ramon Eritja; Victor E. Marquez;
Open Access English
  • Published: 01 Jan 2003
  • Publisher: Wiley-Blackwell
  • Country: Spain
A short oligodeoxynucleotide (ODN) with 2-(1H)-pyrimidinone at the HhaI DNA methyltransferase target site (GCGC) is shown to induce a level of inhibition of methyl transfer and thermal stability of the complex with the enzyme identical to that achieved with a similar ODN substituted with 5-azacytosine. The drugs responsible for these effects - zebularine and 5-azacytidine/2′-deoxy-5-azacytidine - are contrasted in terms of chemical stability and possible metabolic activation by a brief structure-activity analysis.
free text keywords: 2′-deoxy-5- azacytidine, 2-(1H)-pyrimidinone, 5-azacytidine, 5-azacytosine, Cytidine deaminase inhibitor, DNA methyltransferase, Gene reactivation, Methylation inhibitor, Zebularine, Chemistry, Cytidine, chemistry.chemical_compound, Enzyme, chemistry.chemical_classification, DNA, Biochemistry, Structure–activity relationship, Riboside
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