Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase

D. Cairns; E. Michalitsi; T.C. Jenkins; S.P. Mackay

doi:10.1016/S0968-0896(01)00337-6

Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase

D. Cairns, E. Michalitsi, T.C. Jenkins, S.P. Mackay

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article

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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.

Original language	English
Pages (from-to)	803-807
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
DOIs	https://doi.org/10.1016/S0968-0896(01)00337-6
Publication status	Published - 2002

Keywords

cytotoxicity
molecular modelling
human telomerase

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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.",

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AB - 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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KW - molecular modelling

KW - human telomerase

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DO - 10.1016/S0968-0896(01)00337-6

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