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

Bioorg Chem. 2021 May:110:104804. doi: 10.1016/j.bioorg.2021.104804. Epub 2021 Mar 6.

Abstract

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.

Keywords: Biological activities; RNA G-quadruplexes; Small molecules; Structural features.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Dose-Response Relationship, Drug
  • Drug Development*
  • G-Quadruplexes / drug effects
  • Molecular Structure
  • RNA / drug effects*
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship

Substances

  • Small Molecule Libraries
  • RNA