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A label-free method for identifying electroactive G-quadruplex-binding ligand
Authors:Yan Jin  Yunxia Qiao
Institution:Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education, Key Laboratory of Analytical Chemistry for Life Science of Shaanxi Province, School of Chemistry and Materials Science, Shaanxi Normal University, Xi''an 710062, PR China;China State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha 410082, PR China
Abstract:Ligands of G-quadruplex have received great attention because of their potential anticancer activity. Here, we designed a label-free electrochemical method to identify electrochemically active molecules that stabilize G-quadruplexes in homogeneous medium. Daunorubicin (DNR) was used as model drug. In the presence of GDNA, the voltammetry of DNR changed. The binding constant (β) and binding-site number (m) of GDNA  mDNR are simultaneously obtained from dependence of the current on the amount of added GDNA in voltammetry, concluding that β = (2.37 ± 2.25) × 107 M? 1and m was near 1, respectively. Control experiment was performed, indicating that this method can specific identify G-quadruplex-binding ligand. The interaction mechanism of DNR with GDNA was also investigated by circular dichroism (CD). The result demonstrated that it is a simple and selective method for identification electroactive ligand with potential anticancer activity.
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