Bisquinolinium compounds induce quadruplex-specific transcriptome changes in HeLa S3 cell lines

• Main Authors: Halder Rashi, Riou Jean-Francois, Teulade-Fichou Marie-Paule, Frickey Tancred, Hartig Jörg S
• Format: Article
• Language: English
• Published: BMC 2012-03-01
• Series: BMC Research Notes
• Online Access: http://www.biomedcentral.com/1756-0500/5/138

<p>Abstract</p> <p>Background</p> <p>Guanosine rich sequences capable of forming G-quadruplex (G4) motifs are enriched near the gene transcription start site (TSS) in the human genome. When probed at the single gene level, G-quadruplex motifs residing in promoter regions show substantial effects on gene transcription. Moreover, further changes in transcription levels are noticed when G4-motifs are targeted with G-quadruplex-specific small molecules.</p> <p>Results</p> <p>Global studies concerning general changes of the transcriptome via targeting promoter-based G-quadruplex motifs are very limited and have so far only been carried out with compounds displaying weak selectivity for quadruplex sequences. Here we utilize two G-quadruplex-specific bisquinolinium derivatives PhenDC3 and 360A and investigate their effects on the expression of the HeLa S3 transcriptome. Our results show wide-spread changes in the transcriptome with specificity for genes with G-quadruplex motifs near their transcription start sites (TSS). Using real-time PCR we further confirmed the specificity of PhenDC3 and 360A as potent molecules to target G-quadruplex-regulated genes.</p> <p>Conclusions</p> <p>Specific effects on quadruplex-containing genes have been observed utilizing whole-transcriptome analysis upon treatment of cultured cells with quadruplex-selective bisquinolinium compounds.</p>