Macrocyclic Hexaoxazoles as Sequence- and Mode-Selective G-Quadruplex Binders

Authors

  • Masayuki Tera,

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei Tokyo 184–8588 (Japan), Fax: (+81) 42-388-7295
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  • Hiromichi Ishizuka,

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei Tokyo 184–8588 (Japan), Fax: (+81) 42-388-7295
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  • Motoki Takagi Dr.,

    1. Biological Information Research Center, National Institute of Advanced Industrial Science and Technology, Koto-ku, Tokyo 135-0064 (Japan)
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  • Masami Suganuma Dr.,

    1. Research Institute for Clinical Oncology, Saitama Cancer Center, Ina, Kitaadachi-gun, Saitama 362–0806 (Japan)
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  • Kazuo Shin-ya Dr.,

    1. Biological Information Research Center, National Institute of Advanced Industrial Science and Technology, Koto-ku, Tokyo 135-0064 (Japan)
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  • Kazuo Nagasawa Prof. Dr.

    1. Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, 2-24-16 Nakamachi, Koganei Tokyo 184–8588 (Japan), Fax: (+81) 42-388-7295
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  • We thank Prof. Ikebukuro (TUAT) for helpful discussions. This work was supported by a Grant-in-Aid for Scientific Research on Priority Areas (17035025) from The Ministry of Education, Culture, Sports, Science, and Technology (MEXT).

Abstract

original image

Gut gebunden: Die Synthese makrocyclischer Hexaoxazole mit kationischen Seitenketten, die G-Quadruplexe binden, wird beschrieben. Sie sind selektiv für die telo24-DNA-Sequenz und stabilisieren telo24 in der antiparallelen Form stark (siehe Bild). Außerdem wurde eine gute Telomerase-Inhibierung durch diese Verbindungen sowohl in zellfreien als auch in zellbasierten Assays nachgewiesen.

Ancillary