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Issue 76, 2015
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An 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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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.

Graphical abstract: An 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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Publication details

The article was received on 19 Jun 2015, accepted on 27 Jul 2015 and first published on 27 Jul 2015


Article type: Communication
DOI: 10.1039/C5CC05065K
Citation: Chem. Commun., 2015,51, 14310-14313
  • Open access: Creative Commons BY-NC license
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    An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512

    G. Palermo, E. Minniti, M. L. Greco, L. Riccardi, E. Simoni, M. Convertino, C. Marchetti, M. Rosini, C. Sissi, A. Minarini and M. De Vivo, Chem. Commun., 2015, 51, 14310
    DOI: 10.1039/C5CC05065K

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