Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase

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

Research output: Contribution to journalArticle

48 Citations (Scopus)

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.
LanguageEnglish
Pages803-807
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume10
DOIs
Publication statusPublished - 2002

Fingerprint

Anthraquinones
Molecular modeling
Telomerase
Cytotoxicity
Taq Polymerase
G-Quadruplexes
DNA
Guanine
Amines
Assays
Stabilization
Enzymes

Keywords

  • cytotoxicity
  • molecular modelling
  • human telomerase

Cite this

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Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase. / Cairns, D.; Michalitsi, E.; Jenkins, T.C.; Mackay, S.P.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 10, 2002, p. 803-807.

Research output: Contribution to journalArticle

TY - JOUR

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AU - Michalitsi, E.

AU - Jenkins, T.C.

AU - Mackay, S.P.

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KW - molecular modelling

KW - human telomerase

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T2 - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

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