Targeting epigenetic regulations in cancer

Bo Ning, Wenyuan Li, Wei Zhao, Rongfu Wang

Research output: Contribution to journalReview articlepeer-review

58 Scopus citations


Epigenetic regulation of gene expression is a dynamic and reversible process with DNA methylation, histone modifications, and chromatin remodeling. Recently, groundbreaking studies have demonstrated the importance of DNA and chromatin regulatory proteins from different aspects, including stem cell, development, and tumor genesis. Abnormal epigenetic regulation is frequently associated with diseases and drugs targeting DNA methylation and histone acetylation have been approved for cancer therapy. Although the network of epigenetic regulation is more complex than people expect, new potential druggable chromatin-associated proteins are being discovered and tested for clinical application. Here we review the key proteins that mediate epigenetic regulations through DNA methylation, the acetylation and methylation of histones, and the reader proteins that bind to modified histones. We also discuss cancer associations and recent progress of pharmacological development of these proteins.

Original languageEnglish (US)
Pages (from-to)97-109
Number of pages13
JournalActa Biochimica et Biophysica Sinica
Issue number1
StatePublished - May 27 2015
Externally publishedYes


  • DNA methylation
  • anti-cancer drugs
  • epigenetic regulation
  • histone modification
  • inhibitors

ASJC Scopus subject areas

  • General Medicine


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