Title: Base specific interaction of reductively activated nitroimidazoles with DNA
Authors: Declerck, Paul ×
De Ranter, C J
Volckaert, Guido #
Issue Date: Nov-1983
Publisher: Elsevier on behalf of the Federation of European Biochemical Societies
Series Title: FEBS Letters vol:164 issue:1 pages:145-8
Abstract: To exert biological activity, nitroimidazole drugs require reductive activation in vivo. Nucleic acids are susceptible to the activated drug in vitro and are presumably the major target in vivo. We carried out electrolytical reduction of several 5-nitroimidazoles at a controlled potential either in the presence or prior to the addition of DNA. Using a nucleotide sequence specific test to analyse cleavage products, specific interaction of the reduced nitroimidazole intermediate(s) towards the guanine residues is prominent. Since the strand scission depends on subsequent piperidine treatment, it can be concluded that the primary interaction between the activated drug and guanine is a covalent modification weakening the glycosidic bond.
ISSN: 0014-5793
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Division of Gene Technology (-)
Laboratory for Pharmaceutical Biology (-)
× corresponding author
# (joint) last author

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