Furan based cyclic homo-oligopeptides bind G-quadruplex selectively and repress c-MYC transcription.
We demonstrate the synthesis and selective binding of two novel furan based tricyclic homo-oligopeptides to G-quadruplex and using Real Time PCR show its repressive effect on c-MYC transcription. CD spectroscopy and FRET melting studies show that these ligands can induce G-quadruplex structures in the G rich 22 mer c-MYC DNA sequence and further stabilize the structure. Using real time polymerase chain reaction we observed that up to 70% downregulation of c-MYC transcripts upon ligand treatment in HeLa cells.
Agarwal
Tani
T
Proteomics and Structural Biology Unit, Institute of Genomics and Integrative Biology, CSIR, New Delhi 110 007, India.
Roy
Saumya
S
Chakraborty
Tushar Kanti
TK
Maiti
Souvik
S
D002942:Circular Dichroism; D031541:Fluorescence Resonance Energy Transfer; D005663:Furans / Q000737:chemistry*; D054856:G-Quadruplexes; D006367:HeLa Cells; D006801:Humans; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology; D016271:Proto-Oncogene Proteins c-myc / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D014158:Transcription, Genetic
D005663:Furans; D010456:Peptides, Cyclic; D016271:Proto-Oncogene Proteins c-myc; C039281:furan