Selective recognition and stabilization of new ligands targeting the potassium form of the human telomeric G-quadruplex DNA

Yi Hwa Lin, Show Mei Chuang, Pei Ching Wu, Chun Liang Chen, Sivakamavalli Jeyachandran, Shou Chen Lo, Hsu Shan Huang, Ming Hon Hou

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Abstract

The development of a ligand that is capable of distinguishing among the wide variety of G-quadruplex structures and targeting telomeres to treat cancer is particularly challenging. In this study, the ability of two anthraquinone telomerase inhibitors (NSC749235 and NSC764638) to target telomeric G-quadruplex DNA was probed. We found that these ligands specifically target the potassium form of telomeric G-quadruplex DNA over the DNA counterpart. The characteristic interaction with the telomeric G-quadruplex DNA and the anticancer activities of these ligands were also explored. The results of this present work emphasize our understanding of the binding selectivity of anthraquinone derivatives to G-quadruplex DNA and assists in future drug development for G-quadruplex-specific ligands.

Original languageEnglish
Article number31019
JournalScientific Reports
Volume6
DOIs
Publication statusPublished - Aug 11 2016

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