Interaction of an acridine dimer with DNA quadruplex structures. Alberti, P, Ren, J, Teulade-Fichou, M P, Guittat, L, Riou, J F, Chaires, J, Hélène, C, Vigneron, J P, Lehn, J M, & Mergny, J L Journal of biomolecular structure & dynamics, 19(3):505–13, December, 2001.
Paper abstract bibtex 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.
@article{Alberti2001,
title = {Interaction of an acridine dimer with {DNA} quadruplex structures.},
volume = {19},
issn = {0739-1102},
url = {http://www.ncbi.nlm.nih.gov/pubmed/11790148},
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.},
number = {3},
journal = {Journal of biomolecular structure \& dynamics},
author = {Alberti, P and Ren, J and Teulade-Fichou, M P and Guittat, L and Riou, J F and Chaires, J and Hélène, C and Vigneron, J P and Lehn, J M and Mergny, J L},
month = dec,
year = {2001},
pmid = {11790148},
keywords = {\#nosource, Acridines, Acridines: chemistry, Acridines: metabolism, Binding Sites, Bridged Compounds, Bridged Compounds: chemistry, Bridged Compounds: metabolism, Cytosine, Cytosine: chemistry, DNA, DNA: chemistry, DNA: metabolism, Dimerization, Enzyme Inhibitors, Enzyme Inhibitors: chemistry, Enzyme Inhibitors: metabolism, Fluorescence, Fluorescence: methods, Fluorescent Dyes, Fluorescent Dyes: metabolism, G-Quadruplexes, Guanine, Guanine: chemistry, Humans, Kinetics, Ligands, Nucleic Acid Conformation, Oligonucleotides, Oligonucleotides: chemistry, Rhodamines, Rhodamines: metabolism, Single-Stranded, Single-Stranded: chemistry, Spectrometry, Telomerase, Telomerase: metabolism, Telomere, Telomere: chemistry, Temperature},
pages = {505--13},
}
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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. 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