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

Paula A. Abreu; Gisela Dellamora-Ortiz; Luiz R. Leão-Ferreira; Maria Gouveia; Esteban Braggio; Ilana Zalcberg; Dilvani O. Santos; Saulo Bourguinhon; Lucio M. Cabral; Carlos R. Rodrigues; Helena C. Castro

doi:10.1517/14728222.12.8.1035

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

Paula A. Abreu, Gisela Dellamora-Ortiz, Luiz R. Leão-Ferreira, Maria Gouveia, Esteban Braggio, Ilana Zalcberg, Dilvani O. Santos, Saulo Bourguinhon, Lucio M. Cabral, Carlos R. Rodrigues, Helena C. Castro

Cancer Biology

Research output: Contribution to journal › Review article › peer-review

14 Scopus citations

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.

Original language	English (US)
Pages (from-to)	1035-1047
Number of pages	13
Journal	Expert opinion on therapeutic targets
Volume	12
Issue number	8
DOIs	https://doi.org/10.1517/14728222.12.8.1035
State	Published - Aug 2008

Keywords

Cancer
CpG sites
DNA methylation
Methyltransferases

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Drug Discovery
Clinical Biochemistry

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10.1517/14728222.12.8.1035

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title = "DNA methylation: A promising target for the twenty-first century",

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.",

keywords = "Cancer, CpG sites, DNA methylation, Methyltransferases",

author = "Abreu, {Paula A.} and Gisela Dellamora-Ortiz and Le{\~a}o-Ferreira, {Luiz R.} and Maria Gouveia and Esteban Braggio and Ilana Zalcberg and Santos, {Dilvani O.} and Saulo Bourguinhon and Cabral, {Lucio M.} and Rodrigues, {Carlos R.} and Castro, {Helena C.}",

note = "Funding Information: Fellowships granted to Helena C Castro by FAPERJ are gratefully acknowledged. This work was partially supported by CNPq, FAPERJ, and UFF.",

year = "2008",

month = aug,

doi = "10.1517/14728222.12.8.1035",

language = "English (US)",

volume = "12",

pages = "1035--1047",

journal = "Expert opinion on therapeutic targets",

issn = "1472-8222",

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TY - JOUR

T1 - DNA methylation

T2 - A promising target for the twenty-first century

AU - Abreu, Paula A.

AU - Dellamora-Ortiz, Gisela

AU - Leão-Ferreira, Luiz R.

AU - Gouveia, Maria

AU - Braggio, Esteban

AU - Zalcberg, Ilana

AU - Santos, Dilvani O.

AU - Bourguinhon, Saulo

AU - Cabral, Lucio M.

AU - Rodrigues, Carlos R.

AU - Castro, Helena C.

N1 - Funding Information: Fellowships granted to Helena C Castro by FAPERJ are gratefully acknowledged. This work was partially supported by CNPq, FAPERJ, and UFF.

PY - 2008/8

Y1 - 2008/8

N2 - 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.

AB - 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.

KW - Cancer

KW - CpG sites

KW - DNA methylation

KW - Methyltransferases

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

Abstract

Keywords

ASJC Scopus subject areas

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