Benzoindoloquinolines interact with DNA tetraplexes and inhibit telomerase.
Telomeric G-rich single-stranded DNA can adopt a G-tetraplex structure which has been shown to inhibit telomerase activity. We have examined benzoindoloquinolines derivatives for their ability to stabilize an intramolecular G-quadruplex. The increase in T(m) value of the G-quadruplex was associated with telomerase inhibition in vitro.
Alberti
Patrizia
P
Laboratoire de Biophysique, Muséum National d'Histoire Naturelle, INSERM U 201, CNRS UMR 8646, 43 rue Cuvier, 75231 Paris cedex 05, France.
Schmitt
Philippe
P
Nguyen
Chi-Hung
CH
Rivalle
Christian
C
Hoarau
Magali
M
Grierson
David S
DS
Mergny
Jean-Louis
JL
D004247:DNA / Q000737:chemistry*; D004277:DNA, Single-Stranded / Q000737:chemistry*; D054856:G-Quadruplexes; D006147:Guanine / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D009690:Nucleic Acid Conformation; D011804:Quinolines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D019914:Taq Polymerase / Q000037:antagonists & inhibitors / Q000737:chemistry; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D016615:Telomere / Q000201:enzymology
D004277:DNA, Single-Stranded; D008024:Ligands; D011804:Quinolines; D006147:Guanine; D004247:DNA; D019914:Taq Polymerase; D019098:Telomerase