DNA Hypomethylating Drugs in Cancer Therapy

  1. Patricia Kropf2
  1. 1Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140
  2. 2Fox Chase Cancer Center, Temple Health, Philadelphia, Pennsylvania 19111
  1. Correspondence: jpissa{at}temple.edu

Abstract

Aberrant DNA methylation is a critically important modification in cancer cells, which, through promoter and enhancer DNA methylation changes, use this mechanism to activate oncogenes and silence of tumor-suppressor genes. Targeting DNA methylation in cancer using DNA hypomethylating drugs reprograms tumor cells to a more normal-like state by affecting multiple pathways, and also sensitizes these cells to chemotherapy and immunotherapy. The first generation hypomethylating drugs azacitidine and decitabine are routinely used for the treatment of myeloid leukemias and a next-generation drug (guadecitabine) is currently in clinical trials. This review will summarize preclinical and clinical data on DNA hypomethylating drugs as a cancer therapy.

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    1. Published in Advance February 3, 2017, doi: 10.1101/cshperspect.a026948 Cold Spring Harb Perspect Med 7: Copyright © 2017 Cold Spring Harbor Laboratory Press; all rights reserved
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