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

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.

SUBMITTER: Lin YH

PROVIDER: S-EPMC4980623 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature

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

Lin Yi-Hwa YH Chuang Show-Mei SM Wu Pei-Ching PC Chen Chun-Liang CL Jeyachandran Sivakamavalli S Lo Shou-Chen SC Huang Hsu-Shan HS Hou Ming-Hon MH

Scientific reports 20160811

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 ...[more]

PMID: 27511133

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