Ascididemin and meridine stabilise G-quadruplexes and inhibit telomerase in vitro
Guittat, L.; De Cian, A.; Rosu, F.; Gabelica, V.; De Pauw, E.; Delfourne, E.; Mergny, J.-L. (2005). Ascididemin and meridine stabilise G-quadruplexes and inhibit telomerase in vitro. Biochim. Biophys. Acta, Gen. subj. 1724(3): 375-384. https://hdl.handle.net/10.1016/j.bbagen.2005.04.023
In: Biochimica et Biophysica Acta. G, General subjects. Elsevier: Amsterdam. ISSN 0304-4165; e-ISSN 1872-8006, meer
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| Trefwoord |
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| Author keywords |
telomeres; telomerase inhibitor; G-quadruplex; G-quartet; DNA ligand |
| Auteurs | | Top |
- Guittat, L.
- De Cian, A.
- Rosu, F.
- Gabelica, V.
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- De Pauw, E., meer
- Delfourne, E.
- Mergny, J.-L.
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| Abstract |
Ascididemin and Meridine are two marine compounds with pyridoacridine skeletons known to exhibit interesting antitumour activities. These molecules have been reported to behave like DNA intercalators. In this study, dialysis competition assay and mass spectrometry experiments were used to determine the affinity of ascididemin and meridine for DNA structures among duplexes, triplexes, quadruplexes and single-strands. Our data confirm that ascididemin and meridine interact with DNA but also recognize triplex and quadruplex structures. These molecules exhibit a significant preference for quadruplexes over duplexes or single-strands. Meridine is a stronger quadruplex ligand and therefore a stronger telomerase inhibitor than ascididemin (IC50= 11 and > 80 µM, respectively in a standard TRAP assay). |
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