Recent progress in the discovery of epigenetic inhibitors for the treatment of cancer

Sharad K. Verma

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


Epigenetics investigates heritable changes in gene transcription that do not involve a change in DNA sequence, and an increased understanding in the role of epigenetic misregulation as a key contributor to cancer has triggered the development of epigenetic targeted cancer therapies. Among these include efforts around a class of enzymes known as histone methyltransferases (HMTs). The level of interest in the development of HMT inhibitors as a class of anticancer agents has signifi cantly grown beyond academic settings, and in the last 5 years whole research groups from biotech and big pharma have been dedicated to this area. There are now multiple reports describing small-molecule HMT inhibitors, including chemical probes and drug candidates entering the clinic as fi rst-in-class agents. Recent progress in this emerging area is the topic of this chapter.

Original languageEnglish (US)
Pages (from-to)677-688
Number of pages12
JournalMethods in Molecular Biology
StatePublished - 2015


  • Chromatin
  • Epigenetics
  • Histone methyltransferases
  • Nucleosome
  • Posttranslational modifi cation
  • S-Adenosylmethionine (SAM)

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics


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