Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 21, Issue 21, Pages 7798-7807Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201500347
Keywords
G-quadruplexes; ligands; NMR spectroscopy; platinum; structures
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Funding
- Slovenian Research Agency (ARRS) [P1-0242, J1-6733]
- French Research Agency (ANR, G-Quad)
- COST action of STSM action [CM1105]
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This study provides insights into the interactions of Pt-ttpy, that is, a metallo-organic heterocycle-comprising platinum(II) complex of terpyridine, and G-quadruplexes adopted by G-rich DNA from the transcriptional regulatory element of the c-myc gene, a well-known attractive target for artificial modulation of oncogene expression. A previously noted drug-like potential of Pt-ttpy relies on its antiproliferative activity on cancer cells and its increased selectivity for G-quadruplex binding attributed to the combination of distinct interacting modes. The predominant interaction between the herein used models of a parallel G-quadruplex exhibiting short propeller-type loops and Pt-ttpy occurs through stacking to the outer G-quartets. The presence of adenine versus thymine residue at the 5'-end overhanging region allows the coordinative binding of Pt-ttpy to the G-quadruplex structure. Interestingly, Pt-ttpy triggers the formation of the G-quadruplex even in the absence of cations. Furthermore, NMR-based characterisation revealed common structural features of Pt-ttpy-G-quadruplex complexes in the presence and absence of cations, which indicate that cations may be expelled from the cores of the corresponding structures.
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