DNA demethylating agents and histone deacetylase inhibitors in hematologic malignancies

Cancer J. Jan-Feb 2007;13(1):40-8. doi: 10.1097/PPO.0b013e31803c7359.


The pivotal role of aberrant promoter methylation in gene silencing and cancer development has fueled the interest in DNA methyltransferase inhibitors as novel anticancer drugs. Modulation of gene expression through targeting of epigenetic marks is one of the emerging and promising strategies that has demonstrated successful clinical outcome in hematologic malignancies. Epigenetic modifiers, including DNA methyltransferase inhibitors and histone deacetylase inhibitors, have demonstrated significant clinical activity; several are or are likely to soon be approved by the U.S. Food and Drug Administration. However, the exact mechanism of the clinical response achieved is not fully understood. This review focuses on the pharmacology of the known DNA methyltransferase and histone deacetylase inhibitors and their potential as promising anticancer drugs.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials as Topic
  • DNA Modification Methylases / antagonists & inhibitors*
  • DNA Modification Methylases / chemistry
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / therapeutic use*
  • Hematologic Neoplasms / drug therapy*
  • Hematologic Neoplasms / metabolism
  • Histone Deacetylase Inhibitors*
  • Humans


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • DNA Modification Methylases