Abstract
This article was republished on December 3rd, 2013 because of incorrect figure order. Please download this article again to view the figures.
Highlights
In the last years, tricyclic acridine-containing compounds have been investigated as small molecule chemotherapeutic anticancer agents [1,2]
In summary we have used fluorescence titration assays, competitive dialysis, NMR studies and molecular dynamics simulations in order to determine the binding properties of preclinical 9-amino acridines to DNA
Detailed structural studies by NMR and molecular dynamic simulation on G-quadruplex telomeric complex showed the core of both 9-amino acridines intercalates directly between the virtual planes made by the four A and G
Summary
Tricyclic acridine-containing compounds have been investigated as small molecule chemotherapeutic anticancer agents [1,2]. Studies on the mechanism of action of acridine drugs have shown these compounds are potent inhibitors of topoisomerase and telomerase function in replicating cells [3], which leads to apoptosis and cell death. DNA topoisomerases exist in various eukaryotic and prokaryotic forms [5] and are classified in two large groups, namely type I and type II. Anti-cancer drugs targeting topoisomerase can be classified as either catalytic inhibitors or ‘‘topoisomerase poisons’’ depending on their mechanism of action [6]. The latter can be further sub-classified into two groups: non-intercalating compounds such as etoposide, and intercalators such amsacrine and doxorubicin [7]
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