Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2010 Mar;1(3):197-209.
doi: 10.1177/1947601910365081.

DNA demethylating antineoplastic strategies: a comparative point of view

Stefano Amatori  1 , Irene Bagaloni, Benedetta Donati, Mirco Fanelli
Affiliations

DNA demethylating antineoplastic strategies: a comparative point of view

Stefano Amatori et al. Genes Cancer. 2010 Mar.

Abstract

Despite the involvement of genetic alterations in neoplastic cell transformation, it is increasingly evident that abnormal epigenetic patterns, such as those affecting DNA methylation and histone posttranslational modifications (PTMs), play an essential role in the early stages of tumor development. This finding, together with the evidence that epigenetic changes are reversible, enabled the development of new antineoplastic therapeutic approaches known as epigenetic therapies. Epigenetic modifications are involved in the control of gene expression, and their aberrant distribution is thought to participate in neoplastic transformation by causing the deregulation of crucial cellular pathways. Epigenetic drugs are able to revert the defective gene expression profile of cancer cells and, consequently, reestablish normal molecular pathways. Considering the emerging interest in epigenetic therapeutics, this review focuses on the approaches affecting DNA methylation, evaluates novel strategies and those already approved for clinical use, and compares their therapeutic potential.

Keywords: 5-aza-2′-deoxycytidine; 5-azacytidine; DNA demethylating drugs; DNMT inhibitors; epigenetic therapy.

PubMed Disclaimer

Conflict of interest statement

The authors declared no potential conflicts of interest with respect to the authorship and/or publication of this article.

Figures

Figure 1.
Figure 1.
Major effects and cellular responses mediated by azanucleosides.
See this image and copyright information in PMC

References

    1. Jones PA, Baylin SB. The epigenomics of cancer. Cell 2007;4:683-92 - PMC - PubMed
    1. Bestor TH. The DNA methyltransferases of mammals. Hum Mol Genet 2000;9:2395-402 - PubMed
    1. Okano M, Bell DW, Haber DA, Li E. DNA methyltransferases Dnmt3a and Dnmt3b are essential for de novo methylation and mammalian development. Cell 1999;99:247-57 - PubMed
    1. Antequera F. Structure, function and evolution of CpG island promoters. Cell Mol Life Sci 2003;60:1647-58 - PMC - PubMed
    1. Irizarry RA, Ladd-Acosta C, Wen B, Wu Z, Montano C, Onyango P, et al. Genome-wide methylation analysis of human colon cancer reveals similar hypo- and hypermethylation at conserved tissue-specific CpG island shores. Nat Genet 2009;41:178-86 - PMC - PubMed

LinkOut - more resources