Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase
Cairns, D. and Michalitsi, E. and Jenkins, T.C. and Mackay, S.P. (2002) Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase. Bioorganic and Medicinal Chemistry Letters, 10. pp. 803-807. ISSN 0960-894X
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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.
| Author(s): | Cairns, D., Michalitsi, E., Jenkins, T.C. and Mackay, S.P. | Item type: | Article |
|---|---|
| ID code: | 37878 |
| Keywords: | cytotoxicity , molecular modelling, human telomerase, Pharmacy and materia medica, Biochemistry, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Molecular Biology, Clinical Biochemistry |
| Subjects: | Medicine > Pharmacy and materia medica |
| Department: | Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences |
| Depositing user: | Pure Administrator |
| Date deposited: | 24 Feb 2012 15:16 |
| Last modified: | 17 May 2019 02:08 |
| URI: | https://strathprints.strath.ac.uk/id/eprint/37878 |
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