Triple helix-specific ligands

  • J. L. Mergny
  • , G. Duval-Valentin
  • , C. H. Nguyen
  • , L. Perrouault
  • , B. Faucon
  • , M. Rougée
  • , T. Montenay-Garestier
  • , E. Bisagni
  • , C. Hélène

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)1681-1684
Number of pages4
JournalScience
Volume256
Issue number5064
DOIs
Publication statusPublished - 1 Jan 1992

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