Pharmacodynamic responses to DNA methyltransferase inhibition

Elizabeth Griffiths, Richard L. Momparler, Adam R. Karpf

Research output: Chapter in Book/Report/Conference proceedingChapter

1 Scopus citations


The DNA methyltransferase inhibitors, 5-azacytidine and decitabine, were initially developed at high dose for clinical use as classical cytotoxic agents and only later reidentified as epigenetically active drugs capable of reexpressing genes silenced by DNA methylation. Their clinical activity in myeloid malignancy has resulted in rapid acceptance into clinical practice for the treatment of patients with MDS and AML, a group of patients for whom other treatment strategies have been largely ineffective. Despite widespread clinical use in these patients, the mechanisms responsible for their efficacy remain opaque, and controversy remains regarding the relative contributions of demethylation of silenced tumor suppressor genes with induction of apoptosis and differentiation, induction of CG antigens expression with resultant antitumor immunity, and DNA damage events.

Original languageEnglish (US)
Title of host publicationEpigenetic Therapy of Cancer
Subtitle of host publicationPreclinical Models and Treatment Approaches
PublisherSpringer-Verlag Berlin Heidelberg
Number of pages18
ISBN (Electronic)9783642384042
ISBN (Print)364238403X, 9783642384035
StatePublished - Apr 1 2014

ASJC Scopus subject areas

  • General Medicine


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