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Nucleic Acids Symposium Series 2006 50(1):183-184; doi:10.1093/nass/nrl091
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© 2006 Oxford University Press

The recognition of higher-order G–quadruplex by chiral cyclic-helicene molecules

Yan Xu1,2, Shinya Yamazaki3, Hideji Osuga3 and Hiroshi Sugiyama1

1 Department of Chemistry, Graduate School of Science, Kyoto University, Sakyo, Kyoto 606-8502, Japan, 2 SORST, Japan Science and Technology Agency, Faculty of Systems Engineering, Wakayama University, Sakaedani 930 Wakayama 640-8510, Japan, 3 Department of Materials Science and Chemistry, Faculty of Systems Engineering, Wakayama University, Sakaedani 930 Wakayama 640-8510, Japan

The G-quadruplex structures represent a new class of molecular targets for DNA-interactive compounds that might be useful for targeting telomeres. Here we describe a study on the structure-based design of cyclic helicenes displaying chiral and steric selection in binding to higher-order G-quadruplexes. We propose a new ligand-binding site for G-quadruplex-binding compounds. These results provide proof of concept for small molecule inhibitors of telomerase associated with higher-order G-quadruplex structures.


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