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

Balasubramanian, S., Hurley, L.H. and Neidle, S. (2011) Targeting G-quadruplexes in gene promoters: a novel anticancer strategy? Nature Reviews. Drug discovery, 10 (4). pp. 261-275. 10.1038/nrd3428.

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DOI: 10.1038/nrd3428

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.

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Cancer Research UK Biomolecular Structure Group
ID Code:2290
Journal or Publication Title:Nature Reviews. Drug discovery
Deposited By:Library Staff
Deposited On:23 Jun 2011 16:41
Last Modified:23 Jun 2011 16:41

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