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

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.

SUBMITTER: Balasubramanian S

PROVIDER: S-EPMC3119469 | biostudies-literature | 2011 Apr

REPOSITORIES: biostudies-literature

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

Balasubramanian Shankar S Hurley Laurence H LH Neidle Stephen S

Nature reviews. Drug discovery 20110401 4

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 possib ...[more]

PMID: 21455236

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