| Autor: |
Housaindokht, Mohammad Reza, Verdian ‐ Doghaei, Asma |
| Zdroj: |
Luminescence: Journal of Biological & Chemical Luminescence; Feb2016, Vol. 31 Issue 1, p22-29, 8p |
| Abstrakt: |
Telomerase inhibition through G-quadruplex stabilization by small molecules is of great interest as a novel anticancer therapeutic strategy. Here, we show that newly synthesized Cu-complex binds to G-quadruplex DNA and induces changes in its stability. This biophysical interaction was investigated in vitro using spectroscopic, voltammetric and computational techniques. The binding constant for this complex to G-quadruplex using spectroscopic and electrochemical methods is in the order of 105. The binding stoichiometry was investigated using spectroscopic techniques and corresponded to a ratio of 1:1. Fluorescence ti-tration results reveal that Cu-complex is quenched in the presence of G-quadruplex DNA. Analysis of the fluorescence emission at different temperatures shows that ΔH° > 0, ΔS° > 0 and AC < 0, and indicates that hydrophobic interactions played a major role in the binding processes. MD simulation results suggested that this ligand could stabilize the G-quadruplex structure. An optimized docked model of the G-quadruplex-ligand mixture confirmed the experimental results. Based on the results, we conclude that Cu-complex as an anticancer candidate can bind and stabilize the G-quadruplex DNA structure. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
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