Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?

Nat Rev Drug Discov. 2011 Apr;10(4):261-75. doi: 10.1038/nrd3428.


G-quadruplexes are four-stranded DNA structures that are over-represented in gene promoter regions and are viewed as emerging therapeutic targets in oncology, as transcriptional repression of oncogenes through stabilization of these structures could be a novel anticancer strategy. Many gene promoter G-quadruplexes have physicochemical properties and structural characteristics that might make them druggable, and their structural diversity suggests that a high degree of selectivity might be possible. Here, we describe the evidence for G-quadruplexes in gene promoters and discuss their potential as therapeutic targets, as well as progress in the development of strategies to harness this potential through intervention with small-molecule ligands.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Drug Delivery Systems*
  • Drug Design
  • G-Quadruplexes* / drug effects
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Promoter Regions, Genetic


  • Antineoplastic Agents