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- W3136366119 abstract "• A new small-molecule ligand Cp-1 , a carbazole-quinolinum core bridged with a phenylboronic acid side chain was established. • Cp-1 specifically ‘‘light-up’’ in response to G-Quadruplex DNA through end-stacking binding mode. • The practical applications in living cells were achieved. Telomeric DNA acts as mitotic clock being gradually reduced at each cell division cycle, which will lead the cell to senescence and apoptosis. The G-rich sequences at telomeres can adopt G-quadruplex structures, which have been shown to directly inhibit the enzyme telomerase. The rational design of small-molecule ligands, with a particular focus on the structural features required for selectively binding to G-quadruplex structures, is significant and useful in biochemistry and clinical diagnosis. Here, a new small-molecule ligand Cp-1 , a carbazole-quinolinum core bridged with a phenylboronic acid side chain, has been synthesized and characterized by NMR spectroscopy and mass spectrometry. The binding affinity and selectivity towards telomeric G-quadruplex DNA have been determined by fluorescence spectroscopy, UV/Vis titrations, CD spectroscopy and molecular docking study. These studies have shown that the ligand Cp-1 has higher binding affinity and selectivity towards telomeric G-quadruplex over duplex DNA. Binding mode analysis indicated Cp-1 interacted with G-quadruplex DNA mainly through end-stacking mode. Further, the ligand could enter live cells and localize in the cytoplasm as shown by confocal fluorescence microscopy." @default.
- W3136366119 created "2021-03-29" @default.
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- W3136366119 date "2021-04-01" @default.
- W3136366119 modified "2023-09-25" @default.
- W3136366119 title "Carbazole derivative as an effective telomeric G-quadruplex DNA binder" @default.
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- W3136366119 doi "https://doi.org/10.1016/j.tetlet.2021.153004" @default.
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