Multitarget Drugs: an Epigenetic Epiphany

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Abstract

Epigenetics refers to changes in a biological phenotype that are not due to an underlying change in genotype. In eukaryotes, epigenetics involves a set of chemical modifications of the DNA and the histone proteins in nucleosomes. These dynamic changes are carried out by enzymes and modulate protein–protein and protein–nucleic acid interactions to determine whether specific genes are expressed or silenced. Both the epigenetic enzymes and recognition domains are currently important drug discovery targets, particularly for the treatment of cancer. This review summarizes the progress of epigenetic targets that have reached a clinical stage: DNA methyltransferases, histone deacetylases, lysine methyltransferases, lysine demethylases, and bromodomains; this is followed by a comprehensive survey of multitarget drugs that have included an epigenetic target as one of their mechanisms of action.
Original languageEnglish
Pages (from-to)1227-1241
Number of pages15
JournalChemMedChem
Volume11
Issue number12
Early online date18 Feb 2016
DOIs
Publication statusPublished - 20 Jun 2016

Keywords

  • cancer
  • dual inhibitors
  • epigenetics
  • histone deacetylases
  • multitarget drugs

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