4. Minor Groove Binders as Therapeutic Agents

This article describes the current state-of-the-art in the development of small- and medium-sized molecules that interact with double-stranded DNA (dsDNA) by minor groove binding. The supramolecular structure of dsDNA is described and how this informs the development of minor groove binding agents. The structure and biological activity of biologically derived, bioinspired, and synthetic minor groove binders (MGBs) are then evaluated. The therapeutic applications of MGBs as antiinfectives and anticancer agents are presented.