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

Balasubramanian, S; Hurley, LH; Neidle, S; (2011) Targeting G-quadruplexes in gene promoters: a novel anticancer strategy? Nat Rev Drug Discov , 10 (4) pp. 261-275. 10.1038/nrd3428.

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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.

Type: Article
Title: Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
Location: England
DOI: 10.1038/nrd3428
Keywords: Animals, Antineoplastic Agents, Drug Delivery Systems, Drug Design, G-Quadruplexes, Humans, Neoplasms, Promoter Regions, Genetic
UCL classification: UCL > School of Life and Medical Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
URI: http://discovery.ucl.ac.uk/id/eprint/1351755
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