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Expert Opinion on Therapeutic Targets Volume 12, 2008 - Issue 8
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Review

DNA methylation: A promising target for the twenty-first century

Paula A Abreu Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil +55 21 26292294; +55 21 26292284; [email protected]; Federal Fluminense University, Biology Institute, Neuroimmunology Postgraduate course, CEP 24020-150 Niterói, Rio de Janeiro, Brazil
,
Gisela Dellamora-Ortiz Federal University of Rio de Janeiro, Faculty of Pharmacy, CEP 21941-590, Rio de Janeiro, RJ, Brazil
,
Luiz R Leão-Ferreira Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil +55 21 26292294; +55 21 26292284; [email protected]
,
Maria Gouveia Federal Fluminense University, Biology Institute, Neuroimmunology Postgraduate course, CEP 24020-150 Niterói, Rio de Janeiro, Brazil
,
Esteban Braggio National Institute of Cancer, Marrow Bone Transplant Center, CEP 21941-590, Rio de Janeiro, RJ, Brazil
,
Ilana Zalcberg National Institute of Cancer, Marrow Bone Transplant Center, CEP 21941-590, Rio de Janeiro, RJ, Brazil
,
Dilvani O Santos Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil +55 21 26292294; +55 21 26292284; [email protected]
,
Saulo Bourguinhon Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil +55 21 26292294; +55 21 26292284; [email protected]
,
Lucio M Cabral Federal University of Rio de Janeiro, Faculty of Pharmacy, CEP 21941-590, Rio de Janeiro, RJ, Brazil
,
Carlos R Rodrigues Federal University of Rio de Janeiro, Faculty of Pharmacy, CEP 21941-590, Rio de Janeiro, RJ, Brazil
&
Helena C Castro Federal Fluminense University, Biology Institute, Department of Celular and Molecular Biology, CEP 24020-150 Niterói, Rio de Janeiro, Brazil +55 21 26292294; +55 21 26292284; [email protected]; Federal Fluminense University, Biology Institute, Neuroimmunology Postgraduate course, CEP 24020-150 Niterói, Rio de Janeiro, Brazil
 show all
Pages 1035-1047 | Published online: 12 Jul 2008
 
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Abstract

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/methods: 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. Results/conclusion: 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.

Acknowledgements

Fellowships granted to Helena C Castro by FAPERJ are gratefully acknowledged. This work was partially supported by CNPq, FAPERJ, and UFF.

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