Hauptseite > Publikationsdatenbank > An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512 |
Journal Article | FZJ-2017-03092 |
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2015
Soc.
Cambridge
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Please use a persistent id in citations: http://hdl.handle.net/2128/14219 doi:10.1039/C5CC05065K
Abstract: Combined computational–experimental analyses explain and quantify the spermine-vectorized F14512's boosted potency as a topoII poison. We found that an optimized polyamine moiety boosts drug binding to the topoII/DNA cleavage complex, rather than to the DNA alone. These results provide new structural bases and key reference data for designing new human topoII poisons.
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