Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
By Shankar Balasubramanian, L. Hurley, Stephen Neidle. Nature reviews. Drug discovery, 2011
1,529 citations recorded by the source corpus.
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.
Subfields: Molecular Biology
View Paper: https://www.semanticscholar.org/paper/9cf17b2465ee15e9f87dd6c06c749347893a2497
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In Molecular Biology
Citations in the corpus
- G-quadruplexes and their regulatory roles in biology (2015, background): “Knowledge of the precise 3D-structure (6) is important for the design of G-quadruplex stabilizing ligands used for probing the consequences of G-quadruplex stabilization on processes such as DNA replication and gene transcription, and as anticancer drugs to target Gquadruplexes in the promoters of o”
- 5′-UTR RNA G-quadruplexes: translation regulation and targeting (2012, background): “Data have continued to accumulate in the literature in support of transcription–associated roles for DNA PQSs, particularly for oncogenes, and the potential for such motifs to act as drug targets (29).”