DNA Methylation

DNA methylation is a modification of cytosine nucleotides catalyzed by DNA methyltransferases.1 This process is important for genomic stability and epigenetic gene silencing in normal cells as well as cellular differentiation during development.2,3 Methylation occurs at CpG dinucleotides, which are often enriched at promoter regions of genes.2,4 In normal tissues, promoter regions are usually unmethylated. Aberrant DNA hypermethylation contributes to gene silencing, including that of tumor suppressor genes, which may promote development and progression of certain cancers.4-9 Aberrant DNA methylation has been observed in correlative studies in a number of malignancies, including myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), breast cancer, and lung cancer.6-11

As the roles of epigenetic modifications in various malignancies are dissected, epigenetic modifying therapies may increasingly play a role in the treatment of cancer.12

mRNA, messenger RNA.

The safety and efficacy of the agents and/or uses under investigation have not been established. There is no guarantee that the agents will receive health authority approval or become commercially available in any country for the uses being investigated


  1. Santini V. Expert Rev Hematol. 2009;2:121-127. PMID: 21083445
  2. Santini V, et al. Ann Intern Med. 2001;134:573-586. PMID: 11281740
  3. Karpf AR, Matsui S. Cancer Res. 2005;65:8635-8639. PMID: 16204030
  4. Esteller M. N Engl J Med. 2008;358:1148-1159. PMID: 18337604
  5. Gronbaek K, et al. APMIS. 2007;115:1039-1059. PMID: 18042143
  6. Figueroa ME, et al. Blood. 2009;114:3448-3458. PMID: 19652201
  7. Aggerholm A, et al. Eur J Haematol. 2006;76:23-32. PMID: 16343268
  8. Jiang Y, et al. Blood. 2009;113:1315-1325. PMID: 18832655
  9. Melki JR, et al. Cancer Res. 1999;59:3730-3740. PMID: 10446989
  10. Avraham A, et al. PLoS ONE. 2014;9:e91805. PMID: 24651077
  11. Shames DS, et al. PLoS Med. 2006;3:e486. PMID: 17194187
  12. Dawson MA, Kouzarides T. Cell. 2012;150:12-27. PMID: 22770212