Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 10, Issue 4, Pages 261-275Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3428
Keywords
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Funding
- US National Institutes of Health [CA95060, GM085585, CA122952]
- National Foundation for Cancer Research [VONHOFF0601]
- Leukemia & Lymphoma Society [6225-08]
- Biotechnology and Biological Sciences Research Council of the UK
- Cancer Research UK
- European Union
- BBSRC [BB/E012752/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E012752/1] Funding Source: researchfish
- Cancer Research UK [11961] Funding Source: researchfish
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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.
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