Journal Article FZJ-2017-03092

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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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2015
Soc. Cambridge

Chemical communications 51(76), 14310 - 14313 () [10.1039/C5CC05065K]

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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.

Classification:

Contributing Institute(s):
  1. Computational Biomedicine (IAS-5)
  2. Computational Biomedicine (INM-9)
Research Program(s):
  1. 899 - ohne Topic (POF3-899) (POF3-899)

Database coverage:
Medline ; Creative Commons Attribution-NonCommercial CC BY-NC 3.0 ; OpenAccess ; Allianz-Lizenz / DFG ; Current Contents - Physical, Chemical and Earth Sciences ; Ebsco Academic Search ; IF >= 5 ; JCR ; NCBI Molecular Biology Database ; NationallizenzNationallizenz ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection
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Institute Collections > INM > INM-9
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 Record created 2017-04-17, last modified 2024-06-25