DNA methylation as a target for drug design

Christina M. Bender, Jean Marc Zingg, Peter A. Jones

Research output: Contribution to journalReview articlepeer-review

73 Scopus citations


DNA methylation is essential for normal embryonic development. Distinctive genomic methylation patterns must be formed and maintained with high fidelity to ensure the inactivities of specific promoters during development. The mutagenic and epigenetic aspects of DNA methylation are especially interesting because they may lead to the inactivation of genes which are involved in human carcinogenesis. The mutagenicity of 5- Methylcytosine (5mC) and the role of promoter hypermethylation in gene silencing, particularly in cancer, suggest a clinical significance for the design of novel DNA methylation inhibitors which may be utilized to reverse the effects of DNA methylation.

Original languageEnglish (US)
Pages (from-to)175-187
Number of pages13
JournalPharmaceutical Research
Issue number2
StatePublished - 1998
Externally publishedYes


  • 5-Aza-2'-deoxycytidine
  • 5-Methylcytosine
  • Cancer
  • DNA methylation

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)


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