Neidle, S. (2010) Human telomeric G-quadruplex: the current status of telomeric G-quadruplexes as therapeutic targets in human cancer. FEBS Journal, 277 (5). pp. 1118-1125. 10.1111/j.1742-4658.2009.07463.x.
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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.
|Uncontrolled Keywords:||acridine;anticancer;drug;drug-like;in vivo;medicinal chemistry;pharmacology;quadruplex;telomerase;telomere|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Cancer Research UK Biomolecular Structure Group|
|Journal or Publication Title:||FEBS Journal|
|Deposited By:||Library Staff|
|Deposited On:||04 Feb 2011 09:48|
|Last Modified:||04 Feb 2011 09:48|
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