Characterization of the minor groove environment in a drug-DNA complex: Bisbenzimide bound to the poly[d(AT)·poly[d(AT)]duplex

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Abstract

We compare the fluorescence properties of bisbenzimide (also known as Hoechst 33258) bound to the minor groove of the poly[d(AT)·poly[d(AT)]duplex with the corresponding fluorescence properties of bisbenzimide dissolved in neat organic solvents and mixed organic/aqueous solvents. Based on these comparisons, we conclude that the minor groove of the bisbenzimide-poly[d(AT)·poly[d(AT)]complex is quite nonpolar and exhibits a local dielectric constant of ≃ 20 D. We discuss how this insight influences our understanding of the molecular forces that dictate and control the binding affinities and specificities of minor groove-directed DNA binding ligands.

Original languageEnglish (US)
Pages (from-to)8939-8942
Number of pages4
JournalProceedings of the National Academy of Sciences of the United States of America
Volume85
Issue number23
DOIs
StatePublished - 1988

All Science Journal Classification (ASJC) codes

  • General

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