title: 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.
authors: Institute of Genomics and Bioinformatics and Institute of Life Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Yi-Hwa
authors: YH
authors: Lin
authors: Institute of Biomedical Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Show-Mei
authors: SM
authors: Chuang
authors: Institute of Genomics and Bioinformatics and Institute of Life Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Pei-Ching
authors: PC
authors: Wu
authors: Graduate Institute of Life Sciences and School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan.
authors: Chun-Liang
authors: CL
authors: Chen
authors: Institute of Genomics and Bioinformatics and Institute of Life Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Sivakamavalli
authors: S
authors: Jeyachandran
authors: Institute of Genomics and Bioinformatics and Institute of Life Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Shou-Chen
authors: SC
authors: Lo
authors: Graduate Institute of Life Sciences and School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan.|Graduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei 110, Taiwan.
authors: Hsu-Shan
authors: HS
authors: Huang
authors: Institute of Genomics and Bioinformatics and Institute of Life Sciences, National Chung Hsing University, Taichung 402, Taiwan.
authors: Ming-Hon
authors: MH
authors: Hou
mesh_terms: D000880:Anthraquinones / Q000378:metabolism*; D000970:Antineoplastic Agents / Q000378:metabolism*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000378:metabolism*; D004847:Epithelial Cells / Q000187:drug effects / Q000502:physiology; D054856:G-Quadruplexes; D006801:Humans; D011188:Potassium / Q000378:metabolism*; D016615:Telomere / Q000378:metabolism*
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011188:Potassium