| 11814869 |
Cairns D, Michalitsi E, Jenkins TC, Mackay SP: Molecular modelling and cytotoxicity of substituted anthraquinones as inhibitors of human telomerase. Bioorg Med Chem. 2002 Mar;10(3):803-7.
Molecular modelling has been carried out for a number of amine-functionalised anthraquinone derivatives to determine their extent of binding to G-tetraplex DNA and their ability to inhibit the enzymes telomerase and Taq polymerase. The results are compared to data obtained from a modified TRAP assay and show good correlation between the two methods. The findings suggest that anthraquinone derivatives of this type inhibit telomerase by stabilisation of four-stranded tetraplex structures associated with guanine-rich telomeric DNA regions. |
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