TY - JOUR
T1 - Interaction of an acridine dimer with dna quadruplex structures
AU - Alberti, Patrizia
AU - Ren, Jinsong
AU - Teulade-Fichou, Marie Paule
AU - Guittat, Lionel
AU - Riou, Jean François
AU - Chaires, Jonathan B.
AU - Hélène, Claude
AU - Vigneron, Jean Pierre
AU - Lehn, Jean Marie
AU - Mergny, Jean Louis
PY - 2001/1/1
Y1 - 2001/1/1
N2 - 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 μM 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 IC50 value of 0.75 μM in a standard TRAP assay.
AB - 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 μM 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 IC50 value of 0.75 μM in a standard TRAP assay.
U2 - 10.1080/07391102.2001.10506758
DO - 10.1080/07391102.2001.10506758
M3 - Article
C2 - 11790148
AN - SCOPUS:18244384536
SN - 0739-1102
VL - 19
SP - 505
EP - 513
JO - Journal of Biomolecular Structure and Dynamics
JF - Journal of Biomolecular Structure and Dynamics
IS - 3
ER -
