Dual epigenetic modifiers for cancer therapy

Abstract

Epigenetic drug discovery is an emerging strategy for the treatment of cancer and other pathologies. Here, we discuss our recent discovery of first-in-class dual reversible inhibitors of the histone methyltransferase activity of G9a/EHMT2 and DNA methyltransferases showing in vivo efficacy in human tumors. Current and future investigation lines are presented.

Keywords

• cancer
• dnmt
• drug discovery
• epigenetic
• g9a