Cover Picture: A DNA Methyltransferase Modulator Inspired by Peyssonenyne Natural Product Structures (ChemMedChem 12/2012)

Authors

  • Dr. Patricia García-Domínguez,

    1. Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo (Spain)
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  • Mélanie Weiss,

    1. Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC)/CNRS/INSERM/ULP, BP 163, 67404 Illkirch Cedex, C.U. de Strasbourg (France)
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  • Ilaria Lepore,

    1. Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. de Crecchio 7, 80138 Napoli (Italy)
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  • Prof. Dr. Rosana Álvarez,

    1. Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo (Spain)
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  • Prof. Dr. Lucia Altucci,

    Corresponding author
    1. Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. de Crecchio 7, 80138 Napoli (Italy)
    2. CNR-IGB, via P. Castellino, 80100 Napoli (Italy)
    • Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. de Crecchio 7, 80138 Napoli (Italy)
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  • Prof. Dr. Hinrich Gronemeyer,

    Corresponding author
    1. Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC)/CNRS/INSERM/ULP, BP 163, 67404 Illkirch Cedex, C.U. de Strasbourg (France)
    • Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC)/CNRS/INSERM/ULP, BP 163, 67404 Illkirch Cedex, C.U. de Strasbourg (France)
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  • Prof. Dr. Ángel R. de Lera

    Corresponding author
    1. Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo (Spain)
    • Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo (Spain)
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Abstract

original image

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.

Cartoon 1.

Ancillary