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

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

Author information

1
Department of Chemistry, University of Cambridge, Cambridge CB21EW, UK. sb10031@cam.ac.uk

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.

PMID:
21455236
PMCID:
PMC3119469
DOI:
10.1038/nrd3428
[Indexed for MEDLINE]
Free PMC Article

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