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Keywords:

  • DNA methyltransferase;
  • epigenetics;
  • natural products;
  • total synthesis
Thumbnail image of graphical abstract

The front cover picture shows a knight that represents a derivative of the natural product peyssonenyne, a novel DNA methyl transferase (DNMT) epigenetic modulator, armed with a reactive diynone weapon. This chemical warrior was found to be toxic to normal human fibroblasts (BJ, left maze) and mouse embryo fibroblasts (MEF), but not to immortalized human fibroblasts (BJEL, right maze), a unique effect not observed with the classical DNMT inhibitor azacytidine. Based on this toxicity for normal cells, short-term or local application of this epigenetic modulator holds potential for therapy of diseases based on hyperproliferation of fibroblasts or other (pathological) scarring diseases. For more details, see the Full Paper by Lucia Altucci, Hinrich Gronemeyer, Ángel R. de Lera et al. on p. 2101 ff.. Illustration created by Alex Pelayo.