Stabilization of the c-myc gene promoter quadruplex by specific ligands' inhibitors of telomerase

Biochemical and Biophysical Research Communications
Thibault LemarteleurJean-François Riou

Abstract

A parallel G-quadruplex structure was recently identified in the NHE III(1) element of the c-myc gene promoter that functioned as a transcriptional repressor. Different series of telomeric G-quadruplex interacting ligands reported to block telomerase activity were evaluated in a new PCR stop assay on the c-myc quadruplex (Pu22myc). Results indicated that the cationic porphyrin TMPyP4 previously described to stabilize c-myc quadruplex and to cause transcription inhibition efficiently inhibited the assay but with a narrow selectivity when parallel experiments were performed with an oligonucleotide (Pu22mu) containing mutations in the guanine repeat which is unable to form a quadruplex. Other ligands presented potent inhibitory properties with IC(50) in the submicromolar range. 307A, a new 2,6-pyridin-dicarboxamide derivative was found to present the highest selectivity as compared to Pu22mu oligonucleotide (>90-fold). Comparison with telomeric G-quadruplex using TRAP-G4 and PCR stop assays also indicated that ligands 307A, telomestatin, and TMPyP4 are equipotent against both c-myc and telomeric sequences while other ligands displayed some partial selectivity (2- to 6-fold) towards one of these sequences. This work provides eviden...Continue Reading

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