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Science 19 June 1992:
Vol. 256. no. 5064, pp. 1681 - 1684
DOI: 10.1126/science.256.5064.1681
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Articles

Triple Helix-Specific Ligands

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

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 triplexforming 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.


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