Targeting G-quadruplexes in gene promoters: a novel anticancer strategy?
摘要：
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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关键词：
Animals Humans Antineoplastic Agents Drug Delivery Systems Drug Design G-Quadruplexes Neoplasms Promoter Regions, Genetic
DOI：
10.1038/nrd3428
被引量：
年份：
2011
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