[Stabilization of DNA triple helix using conjugates of oligonucleotides and synthetic ligands].
Possibility of stabilization of DNA triple helix is discussed using a covalent conjugation to the third strand (through its terminal phosphate) of ligands that have affinity to double and triple helices. Two types of stabilizers are considered: minor groove binders based on oligopyrroles and triplex-specific interacalators. As a target, a synthetic 29-mer duplex containing a natural polypurinic sequence of the human immunodeficiency provirus was employed. The stabilization with minor groove binders requires several conditions to be respected: a sufficiently long linker capable of reaching out the minor groove from the major one, a specific double-stranded structure of the oligopyrrole fragment and its in-phase fitness to the target sequence. The best stabilizers of a triplex turned out to be novel conjugates in which two parallel molecules containing six pyrrole units each are linked to the same 5'-phosphate of a 16-mer triplex-forming oligonucleotide. The stabilizing properties of these derivatives were comparable with those of benzoindoloquinoline (BIQ) intercalators attached to the terminal phosphate of triple-helix forming oligonucleotides.
Siniakov
A N
AN
Muséum National d'Histoire Naturelle, Laboratoire de Biophysique, INSERM U201-CNRS UMR 8646, 75231 Paris, France.
Riabinin
V A
VA
Grimm
G N
GN
Butorin
A S
AS
D004247:DNA / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D009690:Nucleic Acid Conformation; D009841:Oligonucleotides / Q000737:chemistry
D008024:Ligands; D009841:Oligonucleotides; D004247:DNA