Toward drug repurposing in epigenetics: Olsalazine as a hypomethylating compound active in a cellular context

Oscar Méndez-Lucio, Jeremy Tran, José L. Medina-Franco, Nathalie Meurice, Mark Muller

Research output: Contribution to journalArticlepeer-review

57 Scopus citations


DNA hypomethylating drugs that act on DNA methyltransferase (DNMT) isoforms are promising anticancer agents. By using a well-characterized live-cell system to measure DNA methylation revisions (imprints), we characterize olsalazine, an approved anti-inflammatory drug, as a novel DNA hypomethylating agent. The cell-based screen used in this work is highly tractable, internally controlled, and well-suited for a drug repurposing strategy in epigenetics. Olsalazine very closely mimics the action of 5-aza-2'-deoxycytidine, a known hypomethylating drug, with minimal cytotoxicity at the concentrations tested. Olsalazine was identified by a rapid computer-guided similarity search of a database of approved drugs to a previously identified inhibitor of DNMTs. A bold new direction: Using a novel DNA methylation reprogramming system that operates in the context of living cells, we report the characterization of olsalazine, an anti-inflammatory drug, as a new DNA hypomethylating agent. The results come from cell-based assays that monitor the activity of DNA methyltransferase (DNMT) in living cells.

Original languageEnglish (US)
Pages (from-to)560-565
Number of pages6
Issue number3
StatePublished - Mar 2014


  • DNA methylation
  • cancer
  • drug discovery
  • drug repurposing
  • hypomethylating agents
  • similarity searching

ASJC Scopus subject areas

  • Drug Discovery
  • General Pharmacology, Toxicology and Pharmaceutics
  • Molecular Medicine
  • Biochemistry
  • Pharmacology
  • Organic Chemistry


Dive into the research topics of 'Toward drug repurposing in epigenetics: Olsalazine as a hypomethylating compound active in a cellular context'. Together they form a unique fingerprint.

Cite this