Protein-Protein Interaction Modulators for Epigenetic Therapies

Adv Protein Chem Struct Biol. 2018;110:65-84. doi: 10.1016/bs.apcsb.2017.06.002. Epub 2017 Jul 25.


Targeting protein-protein interactions (PPIs) is becoming an attractive approach for drug discovery. This is particularly true for difficult or emerging targets, such as epitargets that may be elusive to drugs that fall into the traditional chemical space. The chemical nature of the PPIs makes attractive the use of peptides or peptidomimetics to selectively modulate such interactions. Despite the fact peptide-based drug discovery has been challenging, the use of peptides as leads compounds for drug discovery is still a valid strategy. This chapter discusses the current status of PPIs in epigenetic drug discovery. A special emphasis is made on peptides and peptide-like compounds as potential drug candidates.

Keywords: Chemical space; DNA methyltransferases; Drug discovery; Peptides.

Publication types

  • Review

MeSH terms

  • Drug Discovery
  • Epigenesis, Genetic / drug effects*
  • Epigenesis, Genetic / genetics
  • Humans
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Protein Binding / drug effects
  • Proteins / antagonists & inhibitors*
  • Proteins / chemistry
  • Proteins / genetics


  • Peptides
  • Proteins