DNA methylation: a promising target for the twenty-first century.
BACKGROUND
Over the last few years DNA methylation and its involvement in diseases such as cancer has become of great interest for applied research. Since reversal of aberrant DNA methylation may influence the behavior of tumors, the methylation of DNA CpG sites is a potential target for the development of inhibitors for use in cancer treatment.


OBJECTIVE
We briefly review the structural and mechanistic features of DNA methylation, including a structural analysis of the three main human DNA methyltransferases and some (pre)clinical results.


CONCLUSIONS
Despite side effects, data obtained to date still support the vision that DNA-methylation, possibly associated with the use of histone deacetylases (HDACs) and/or artificial transcription factors (ATFs), is a promising target for improving anticancer therapy in the 21st century.
Abreu
Paula A
PA
Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil.
Dellamora-Ortiz
Gisela
G
Leão-Ferreira
Luiz R
LR
Gouveia
Maria
M
Braggio
Esteban
E
Zalcberg
Ilana
I
Santos
Dilvani O
DO
Bourguinhon
Saulo
S
Cabral
Lucio M
LM
Rodrigues
Carlos R
CR
Castro
Helena C
HC
D000970:Antineoplastic Agents / Q000494:pharmacology*; D004247:DNA / Q000235:genetics / Q000378:metabolism*; D019175:DNA Methylation / Q000187:drug effects*; D015254:DNA Modification Methylases / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*
D000970:Antineoplastic Agents; D004247:DNA; D015254:DNA Modification Methylases