Parallel DNA G-quadruplex induced and stabilized by curaxin CBL0137
| Autor: | Jing-Wei Kong, Shuo-Xing Dou, Wei Li, Hui Li, Peng-Ye Wang |
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| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Chinese Physics Letters. |
| ISSN: | 1741-3540 0256-307X |
| Popis: | G-quadruplex (G4) is one of the higher-order DNA structures in guanine-rich sequences which are widely distributed across the genome. Due to their presence in oncogenic promoters and telomeres, G4 DNA structures become the novel targets in anticancer drug designs. Curaxin CBL0137, as a important candidate anticancer drug, can effectively inhibit the growth of multiple cancers. Although there is evidence that anticancer activity of curaxin is associated with its ability to bind DNA and change the DNA topology, its therapeutic target and the underlying anti-cancer mechanism are still unclear. Here we show, for the first time, that curaxin CBL0137 induces G4 folding from anti-parallel to parallel structures, by single-molecule fluorescence resonance energy transfer (FRET) technique. More importantly, we have found that curaxin CBL0137 promotes G4 folding as well as stabilizes the folded G4 structures with long loops, giving a novel insight into effects of curaxin CBL0137 on DNA structures. Our work provides new ideas for the therapeutic mechanism of curaxin CBL0137 and for the design of new G4-targeting anticancer drugs. |
| Databáze: | OpenAIRE |
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