Molecules | |
Selective G-Quadruplex DNA Recognition by a New Class of Designed Cyanines | |
Rupesh Nanjunda1  Eric A. Owens1  Leah Mickelson1  Tyler L. Dost1  Ekaterina M. Stroeva1  Hang T. Huynh1  Markus W. Germann1  Maged M. Henary1  | |
[1] Department of Chemistry, Georgia State University, 50 Decatur St., Atlanta, GA 30303, USA; E-Mails: | |
关键词:
G-quadruplex;
cyanines;
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DOI : 10.3390/molecules181113588 | |
来源: mdpi | |
【 摘 要 】
A variety of cyanines provide versatile and sensitive agents acting as DNA stains and sensors and have been structurally modified to bind in the DNA minor groove in a sequence dependent manner. Similarly, we are developing a new set of cyanines that have been designed to achieve highly selective binding to DNA G-quadruplexes with much weaker binding to DNA duplexes. A systematic set of structurally analogous trimethine cyanines has been synthesized and evaluated for quadruplex targeting. The results reveal that elevated quadruplex binding and specificity are highly sensitive to the polymethine chain length, heterocyclic structure and intrinsic charge of the compound. Biophysical experiments show that the compounds display significant selectivity for quadruplex binding with a higher preference for parallel stranded quadruplexes, such as cMYC. NMR studies revealed the primary binding through an end-stacking mode and SPR studies showed the strongest compounds have primary
【 授权许可】
CC BY
© 2013 by the authors; licensee MDPI, Basel, Switzerland.
【 预 览 】
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RO202003190032139ZK.pdf | 1736KB | download |