Submicromolar, Selective G-Quadruplex Ligands from One Pot: Thermodynamic and Structural Studies of Human Telomeric DNA Binding by Azacyanines

Authors

  • Özgül Persil Çetinkol,

    1. School of Chemistry and Biochemistry, Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, Georgia 30332-0400 (USA), Fax: (+1) 404-894-2295
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    • These authors contributed equally to this work.

  • Aaron E. Engelhart,

    1. School of Chemistry and Biochemistry, Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, Georgia 30332-0400 (USA), Fax: (+1) 404-894-2295
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    • These authors contributed equally to this work.

  • Rupesh K. Nanjunda,

    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, Atlanta, Georgia 30303-3083 (USA)
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  • W. David Wilson Prof.,

    1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, Atlanta, Georgia 30303-3083 (USA)
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  • Nicholas V. Hud Prof.

    1. School of Chemistry and Biochemistry, Parker H. Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, Georgia 30332-0400 (USA), Fax: (+1) 404-894-2295
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Abstract

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Bound to work: A molecular architecture with a shape that is slightly larger than a Watson–Crick base pair was investigated as a potential G-quadruplex ligand. Azacyanines, which possess this architecture, were found to bind on the end of the quadruplex stack (as shown in the figure) and to exhibit high selectivity over duplex binding. The chemical properties, ease of synthesis, and great potential for modification make the azacyanines and their analogues attractive for development as G-quadruplex ligands in drug development.

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