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

Shankar Balasubramanian, Laurence H. Hurley, Stephen Neidle

Research output: Contribution to journalArticle

978 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)261-275
Number of pages15
JournalNature Reviews Drug Discovery
Volume10
Issue number4
DOIs
StatePublished - Apr 2011

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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