Major Achievements in the Design of Quadruplex-Interactive Small Molecules

Organic small molecules that can recognize and bind to G-quadruplex and i-Motif nucleic acids have great potential as selective drugs or as tools in drug target discovery programs, or even in the development of nanodevices for medical diagnosis. Hundreds of quadruplex-interactive small molecules have been reported, and the challenges in their design vary with the intended application. Herein, we survey the major achievements on the therapeutic potential of such quadruplex ligands, their mode of binding, effects upon interaction with quadruplexes, and consider the opportunities and challenges for their exploitation in drug discovery.

Automated summary

Organic small molecules that can recognize and bind to G-quadruplex and i-Motif nucleic acids have great potential in selective drug development and medical diagnostic nanodevice applications. This article surveys the major achievements in the therapeutic potential of these quadruplex ligands, their binding modes, effects on quadruplex interactions, and explores the opportunities and challenges in drug discovery.