| Literature DB >> 11790148 |
P Alberti1, J Ren, M P Teulade-Fichou, L Guittat, J F Riou, J Chaires, C Hélène, J P Vigneron, J M Lehn, J L Mergny.
Abstract
The reactivation of telomerase activity in most cancer cells supports the concept that telomerase is a relevant target in oncology, and telomerase inhibitors have been proposed as new potential anticancer agents. The telomeric G-rich single-stranded DNA can adopt an intramolecular G-quadruplex structure in vitro, which has been shown to inhibit telomerase activity. The C-rich sequence can also adopt a quadruplex (intercalated) structure (i-DNA). Two acridine derivatives were shown to increase the melting temperature of the G- quadruplex and the C-quadruplex at 1 microM dye concentration. The increase in Tm value of the G-quadruplex was associated with telomerase inhibition in vitro. The most active compound, "BisA", showed an IC(50) value of 0.75 microM in a standard TRAP assay.Entities:
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Year: 2001 PMID： 11790148 DOI： 10.1080/07391102.2001.10506758
Source DB: PubMed Journal: J Biomol Struct Dyn ISSN： 0739-1102