Sequence-selective intercalation of antitumour bis-naphthalimides into DNA. Evidence for an approach via the major groove.

@article{Bailly1996SequenceselectiveIO,
  title={Sequence-selective intercalation of antitumour bis-naphthalimides into DNA. Evidence for an approach via the major groove.},
  author={C. Bailly and M. Bra{\~n}a and M. Waring},
  journal={European journal of biochemistry},
  year={1996},
  volume={240 1},
  pages={
          195-208
        }
}
LU 79553, a bis-naphthalimide drug highly active against human solid tumour xenografts, has been shown to bis-intercalate into DNA with a helix-unwinding angle of 37 degrees. Footprinting experiments with DNase I reveal that the drug is selective for mixed nucleotide sequences characterised by an alternating purine-pyrimidine motif, particularly those containing GpT (ApC) and TpG (CpA) steps. Derivatives bearing nitro or amino substituents on the naphthalimide chromophores bind at essentially… Expand
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