期刊
FEBS JOURNAL
卷 277, 期 5, 页码 1118-1125出版社
WILEY-BLACKWELL PUBLISHING, INC
DOI: 10.1111/j.1742-4658.2009.07463.x
关键词
acridine; anticancer; drug; drug-like; in vivo; medicinal chemistry; pharmacology; quadruplex; telomerase; telomere
资金
- Cancer Research UK
The 3'-ends of human chromosomal DNA terminate in short single-stranded guanine-rich tandem-repeat sequences. In cancer cells, these are associated with the telomere-maintenance enzyme telomerase together with the end-binding protein hPOT1. Small molecules that can compete with these proteins and induce the single-stranded DNA to form quadruplex-ligand complexes are, in effect, able to expose these 3'-ends, which results in the activation of a DNA damage response and selective inhibition of cell growth. Several of these G-quadruplex binding molecules have shown promising anticancer activity in tumour xenograft models, which indicate that the approach may be applicable to the treatment of a wide range of human cancers. This minireview summarizes the available data on these compounds and the challenges posed for drug discovery.
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