Extended target sequence specificity of PNA-minor-groove binder conjugates

Conjugal bliss. We show that a peptide nucleic acid–Hoechst conjugate (see scheme) kinetically and sequence preferentially guides the PNA moiety to target a binding site proximal to an A–T region that has an affinity for the minor‐groove binder. These results demonstrate a new strategy for constructing DNA recognition ligands composed of a sequence‐guiding domain that increases the target specificity and a DNA‐modification domain that determines the biological activity of the conjugate.