HIGHLIGHTS
SUMMARY
As the cleavage step is much slower than the re-ligation step is, the concentration of the nicked DNA is low, but this "on-off" timing is crucial for the inhibition of the Topo I activity. Although several classes of aromatic molecules can intercalate into the nick, thereby forming ternary complex inhibitor/DNA/Topo I, the camptothecin derivatives require special synthetic efforts to be made. The true inhibitors bind Topo I in a nick, as it has found in a crystal_structure of a ternary complex of nicked DNA/Topo I and topotecan (TPT) between . . .
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