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000829379 1001_ $$0P:(DE-HGF)0$$aPalermo, Giulia$$b0
000829379 245__ $$aAn optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512
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000829379 520__ $$aCombined computational–experimental analyses explain and quantify the spermine-vectorized F14512's boosted potency as a topoII poison. We found that an optimized polyamine moiety boosts drug binding to the topoII/DNA cleavage complex, rather than to the DNA alone. These results provide new structural bases and key reference data for designing new human topoII poisons.
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000829379 7001_ $$0P:(DE-HGF)0$$aMinniti, Elirosa$$b1
000829379 7001_ $$0P:(DE-HGF)0$$aGreco, Maria Laura$$b2
000829379 7001_ $$0P:(DE-HGF)0$$aRiccardi, Laura$$b3
000829379 7001_ $$0P:(DE-HGF)0$$aSimoni, Elena$$b4
000829379 7001_ $$0P:(DE-HGF)0$$aConvertino, Marino$$b5
000829379 7001_ $$0P:(DE-HGF)0$$aMarchetti, Chiara$$b6
000829379 7001_ $$0P:(DE-HGF)0$$aRosini, Michela$$b7
000829379 7001_ $$0P:(DE-HGF)0$$aSissi, Claudia$$b8
000829379 7001_ $$0P:(DE-HGF)0$$aMinarini, Anna$$b9
000829379 7001_ $$0P:(DE-Juel1)167585$$aDe Vivo, Marco$$b10$$eCorresponding author
000829379 773__ $$0PERI:(DE-600)1472881-3$$a10.1039/C5CC05065K$$gVol. 51, no. 76, p. 14310 - 14313$$n76$$p14310 - 14313$$tChemical communications$$v51$$x1364-548X$$y2015
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