Głuszyńska, A;
Juskowiak, B;
Kuta-Siejkowska, M;
Hoffmann, M;
Haider, S;
(2018)
Carbazole ligands as c-myc G-quadruplex binders.
International Journal of Biological Macromolecules
, 114
pp. 479-490.
10.1016/j.ijbiomac.2018.03.135.
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Accepted Manuscript Int. J Biol. Macromol. 2018.pdf - Accepted Version Download (1MB) | Preview |
Abstract
The interactions of c-myc G-quadruplex with three carbazole derivatives were investigated by UV-Vis spectrophotometry, fluorescence, CD spectroscopy, and molecular modeling. The results showed that a combination of carbazole scaffold functionalized with ethyl, triazole and imidazole groups resulted in stabilization of the intramolecular G-quadruplex formed by the DNA sequence derived from the NHE III1 region of c-myc oncogene (Pu22). Binding to the G-quadruplex Pu22 resulted in the significant increase in fluorescence intensity of complexed ligands 1-3. All ligands were capable of interacting with G4 DNA with binding stoichiometry indicating that two ligand molecules bind to G-quadruplex with comparable affinity, which agrees with binding model of end-stacking on terminal G-tetrads.
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