Two-hit wonders: The expanding universe of multitargeting epigenetic agents

Angel R. De Lera, A. Ganesan

Research output: Contribution to journalArticlepeer-review

31 Citations (Scopus)


Multitargeting involves the application of molecules that are deliberately intended to bind to two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and drug discovery, the rational design of multitargeting agents has evolved to a sophisticated level, and there are now five examples that have reached clinical trials. This review covers recent developments in the field and future prospects.
Original languageEnglish
Pages (from-to)135-154
Number of pages20
JournalCurrent Opinion in Chemical Biology
Early online date9 Aug 2020
Publication statusPublished - Aug 2020


  • Chemical probes
  • Drug discovery
  • Epigenetics
  • Multitargeting agents

Cite this