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- W1972410555 abstract "The DNA unwinding effects of some 9-aminoacridine derivatives were compared under reaction conditions that could be used to study drug-induced topoisomerase II inhibition. An assay was designed to determine drug-induced DNA unwinding by using L1210 topoisomerase I. 9-aminoacridines could be ranked by decreasing unwinding potency: compound C > 9-aminoacridine > o-AMSA > compound A > compound B > m-AMSA. Ethidium bromide was more potent than any of the 9-aminoacridines. This assay is a fast and simple method to compare DNA unwinding effects of intercalators. It led to the definition of a drug intrinsic unwinding constant (k). An additional finding was that all 9-aminoacridines and ethidium bromide inhibited L1210 topoisomerase I. Enzyme inhibiton was detectable at low enzyme concentrations (< 1 unit) and when the kinetics of topoisomerase I-mediated DNA relaxation was studied. Topoisomerase I inhibition was not associated with DNA swivelling or cleavage." @default.
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- W1972410555 date "1987-01-01" @default.
- W1972410555 modified "2023-10-17" @default.
- W1972410555 title "DNA unwinding and inhibition of mouse leukemia L1210 DNA topoisomerase I by intercalators" @default.
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- W1972410555 doi "https://doi.org/10.1093/nar/15.16.6713" @default.
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