Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 53, Issue 4, Pages 999-1002Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201308063
Keywords
bisquinolinium ligands; drug design; G-quadruplex DNA; NMR spectroscopy; interactions
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Funding
- Singapore Ministry of Education and Nanyang Technological University
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Phen-DC3 is a highly promising compound that specifically targets G-quadruplexes, with potent biological effects observed in vivo. We used NMR spectroscopy to solve the structure of the complex formed between Phen-DC3 and an intramolecular G-quadruplex derived from the c-myc promoter. Structural information revealed that Phen-DC3 interacts with the quadruplex through extensive -stacking with guanine bases of the top G-tetrad. On the basis of our structure, modifications are proposed for the development of this compound for selective targeting of a specific G-quadruplex conformation.
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