2024-03-29T11:42:12Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1248062020-05-28T13:37:30Zcom_10261_5063com_10261_5col_10261_5066
Potent Inhibition of HhaI DNA Methylase by the Aglycon of 2-(1H)-Pyrimidinone Riboside (Zebularine) at the GCGC Recognition Domain
Márquez, Víctor E.
Kelley, James A.
Eritja Casadellà, Ramón
Vanbemmel, Dana
Christman, Judith K.
2′-deoxy-5- azacytidine
2-(1H)-pyrimidinone
5-azacytidine
5-azacytosine
Cytidine deaminase inhibitor
DNA methyltransferase
Gene reactivation
Methylation inhibitor
Zebularine
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.
Peer reviewed
2015-11-11T07:36:43Z
2015-11-11T07:36:43Z
2003
artículo
http://purl.org/coar/resource_type/c_6501
Annals of the New York Academy of Sciences
http://hdl.handle.net/10261/124806
10.1196/annals.1281.014
en
Postprint
DOI: 10.1196/annals.1281.014
Sí
open
Wiley-Blackwell