Recent advances in the development of small molecules targeting RNA G-quadruplexes for drug discovery

Extensive evidence indicates that RNA G-quadruplexes have associated with some important cellular events. Investigation of RNA G-quadruplexes is thus vital to revealing their biofunctions. Several small molecules have been developed to target RNA G-quadruplexes to date. Some of the small molecules showed significantly light-up fluorescence signals upon binding to RNA G-quadruplexes, while some of them regulated the biofunctions of RNA G-quadruplexes. In this mini-review, the small molecules divided into four kinds are expounded which focused mainly on their structural features and biological activities. Moreover, we raised the current challenges and promising prospects. This mini-review might contribute to exploiting more sophisticated small molecules targeting RNA G-quadruplexes with high specificity based on the reported chemical structural features.

Automated summary

Extensive evidence suggests the association of RNA G-quadruplexes with important cellular events, making investigation into them vital. Small molecules have been developed to target RNA G-quadruplexes, some of which exhibit light-up fluorescence signals upon binding, while others regulate their biofunctions. This mini-review classifies small molecules into four types based on their structural features and biological activities, and raises current challenges and promising prospects in the field.