DNA triple helix stabilisation by a naphthylquinoline dimer.
We have used DNase I footprinting to examine the effect of a novel naphthylquinoline dimer, designed as a triplex-specific bis-intercalator, on the stability of intermolecular DNA triplexes. We find that this compound efficiently promotes triplex formation between the 9-mer oligonucleotide 5'-TTTTTTCTT and its oligopurine duplex target at concentrations as low as 0.1 microM, enhancing the triplex stability by at least 1000-fold. This compound, which is the first reported example of a triplex bis-intercalator, is about 30 times more potent than the simple monofunctional ligand.
Keppler
M
M
Division of Biochemistry and Molecular Biology, School of Biological Sciences, University of Southampton, UK.
Zegrocka
O
O
Strekowski
L
L
Fox
K R
KR
D001483:Base Sequence; D004247:DNA / Q000737:chemistry* / Q000187:drug effects*; D018983:DNA Footprinting; D003850:Deoxyribonuclease I; D019281:Dimerization; D004355:Drug Stability; D066298:In Vitro Techniques; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D009690:Nucleic Acid Conformation / Q000187:drug effects*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*
D007364:Intercalating Agents; D008024:Ligands; D011804:Quinolines; C102232:naphthylquinoline triple-helix-binding ligand; D004247:DNA; D003850:Deoxyribonuclease I