Triple helix-specific ligands.
A triple helix is formed upon binding of an oligodeoxynucleotide to the major groove of duplex DNA. A benzo[e]pyridoindole derivative (BePI) strongly stabilized this structure and showed preferential binding to a triplex rather than to a duplex. Energy transfer experiments suggest that BePI intercalates within the triple helix. Sequence-specific inhibition of transcription initiation of a specific gene by Escherichia coli RNA polymerase by a triplex-forming oligodeoxynucleotide is strongly enhanced when the triplex is stabilized by BePI. Upon irradiation with ultraviolet light, BePI induces covalent modifications of the target within the triple helix structure.
Mergny
J L
JL
Laboratoire de Biophysique, Institut National de la Santé et de la Recherche Médicale, Paris, France.
Duval-Valentin
G
G
Nguyen
C H
CH
Perrouault
L
L
Faucon
B
B
Rougée
M
M
Montenay-Garestier
T
T
Bisagni
E
E
Hélène
C
C
D001483:Base Sequence; D002243:Carbolines / Q000378:metabolism; D004247:DNA / Q000235:genetics / Q000378:metabolism*; D012321:DNA-Directed RNA Polymerases / Q000235:genetics / Q000378:metabolism; D004926:Escherichia coli / Q000235:genetics*; D006358:Hot Temperature; D066298:In Vitro Techniques; D008024:Ligands; D008969:Molecular Sequence Data; D009693:Nucleic Acid Hybridization; D014158:Transcription, Genetic
D002243:Carbolines; D008024:Ligands; C051802:triplex DNA; D004247:DNA; D012321:DNA-Directed RNA Polymerases