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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Abstract

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.

ORCID iDs

Cairns, D., Michalitsi, E., Jenkins, T.C. and Mackay, S.P. ORCID logoORCID: https://orcid.org/0000-0001-8000-6557;
  • Item type:Article
    ID code:37878
    Dates:
    Date
    Event
    2002
    Published
    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:20 Jan 2021 17:45
    URI:https://strathprints.strath.ac.uk/id/eprint/37878
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