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FEBS J. 2010 Mar;277(5):1118-25. doi: 10.1111/j.1742-4658.2009.07463.x. Epub 2009 Nov 27.

Human telomeric G-quadruplex: the current status of telomeric G-quadruplexes as therapeutic targets in human cancer.

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Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, London, 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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