%0 Journal Article
%A Palermo, Giulia
%A Minniti, Elirosa
%A Greco, Maria Laura
%A Riccardi, Laura
%A Simoni, Elena
%A Convertino, Marino
%A Marchetti, Chiara
%A Rosini, Michela
%A Sissi, Claudia
%A Minarini, Anna
%A De Vivo, Marco
%T An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512
%J Chemical communications
%V 51
%N 76
%@ 1364-548X
%C Cambridge
%I Soc.
%M FZJ-2017-03092
%P 14310 - 14313
%D 2015
%X 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.
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000361073400005
%$ pmid:26234198
%R 10.1039/C5CC05065K
%U https://juser.fz-juelich.de/record/829379