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Issue 6, 2008
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Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

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Abstract

Maintenance of telomeres—specialized complexes that protect the ends of chromosomes, is undertaken by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but is absent in most normal cells. Targeting telomere maintenance mechanisms could potentially halt tumour growth across a broad spectrum of cancer types, with little cytotoxic effect outside cancer cells. Here, we describe in detail a new class of G-quadruplex binding ligands synthesized using a click chemistry approach. These ligands comprise a 1,3-di(1,2,3-triazol-4-yl)benzene pharmacophore, and display high levels of selectivity for interaction with G-quadruplex DNA vs. duplex DNA. The ability of these ligands to inhibit the enzymatic activity of telomerase correlates with their ability to stabilize quadruplex DNA, and with estimates of affinity calculated by molecular modeling.

Graphical abstract: Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

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Publication details

The article was received on 01 Feb 2008, accepted on 03 Mar 2008 and first published on 08 Apr 2008


Article type: Paper
DOI: 10.1039/B801822G
Citation: Mol. BioSyst., 2008,4, 629-642
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    Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

    A. D. Moorhouse, S. Haider, M. Gunaratnam, D. Munnur, S. Neidle and J. E. Moses, Mol. BioSyst., 2008, 4, 629
    DOI: 10.1039/B801822G

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