Abstract
| Original language | English |
|---|---|
| Pages (from-to) | 803-807 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 10 |
| DOIs | |
| Publication status | Published - 2002 |
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Keywords
- cytotoxicity
- molecular modelling
- human telomerase
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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 journal › Article
TY - JOUR
T1 - Molecular modelling and cytotoxicity of substituted anthraquinonesas inhibitors of human telomerase
AU - Cairns, D.
AU - Michalitsi, E.
AU - Jenkins, T.C.
AU - Mackay, S.P.
PY - 2002
Y1 - 2002
N2 - 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.
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.
KW - cytotoxicity
KW - molecular modelling
KW - human telomerase
U2 - 10.1016/S0968-0896(01)00337-6
DO - 10.1016/S0968-0896(01)00337-6
M3 - Article
VL - 10
SP - 803
EP - 807
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
ER -