DNA binding by analogues of the bifunctional intercalator TANDEM

Andrew J. Hampshire, David A. Rusling, Stephanie Bryan, David Paumier, Simon J. Dawson, John P. Malkinson, Mark Searcey, Keith R. Fox

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


We have used DNase I footprinting to study the binding strength and DNA sequence selectivity of novel derivatives of the quinoxaline bis-intercalator TANDEM. Replacing the valine residues in the cyclic octadepsipeptide with lysines does not affect the selectivity for TpA but leads to a 50-fold increase in affinity. In contrast, replacing both of the quinoxaline chromophores with naphthalene rings abolishes binding, while changing a single ring decreases the affinity, and footprints are observed at only the best binding sites (especially TATATA). By using fragments with different lengths of [(AT)n], we demonstrate that these ligands bind best to the center of the longer (AT)n tracts.
Original languageEnglish
Pages (from-to)7900-7906
Number of pages7
Issue number30
Publication statusPublished - 3 Jul 2008

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