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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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The phosphate-group of DNA as a potential target for RSU-1069, a nitroimidazole-aziridine radiosensitizer.

Strand breakage of plasmid DNA by parent and radiation-reduced RSU-1069 (2.0-8.0 mmol dm-3) has been measured in air over 4 hr at 310K. Reduced RSU-1069 was shown to be approximately 4 times as efficient as the parent compound at causing strand breakage. The aziridine moiety of both parent and reduced RSU-1069 is required for strand break production and, furthermore, is capable of alkylating inorganic phosphate (k = 1.0 X 10(-3) dm3 mol-1 s-1) and a series of nucleotides (k = 0.8 - 2.1 X 10(-3) dm3 mol-1 s-1) at pH 7. 0. From the determined rate constants and the nature of the adducts observed, it was shown that phosphate is a target on nucleotides, although additional sites probably exist particularly, on dGMP and dAMP. The mechanism of action of RSU-1069 is discussed in terms of its ability to act as a cytotoxic agent, radiosensitizer and bioreductive drug.[1]

References

  1. The phosphate-group of DNA as a potential target for RSU-1069, a nitroimidazole-aziridine radiosensitizer. Silver, A.R., O'Neill, P., Jenkins, T.C., McNeil, S.S. Int. J. Radiat. Oncol. Biol. Phys. (1986) [Pubmed]
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