Identification of a new G-quadruplex motif in the KRAS promoter and design of pyrene-modified G4-decoys with antiproliferative activity in pancreatic cancer cells.

@article{Cogoi2009IdentificationOA,
  title={Identification of a new G-quadruplex motif in the KRAS promoter and design of pyrene-modified G4-decoys with antiproliferative activity in pancreatic cancer cells.},
  author={Susanna Cogoi and Manikandan Paramasivam and Vyacheslav V Filichev and Imrich G{\'e}ci and Erik Bo Pedersen and Luigi E Xodo},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 2},
  pages={564-8}
}
A new quadruplex motif located in the promoter of the human KRAS gene, within a nuclease hypersensitive element (NHE), has been characterized. Oligonucleotides mimicking this quadruplex are found to compete with a DNA-protein complex between NHE and a nuclear extract from pancreatic cancer cells. When modified with (R)-1-O-[4-1-(1-pyrenylethynyl) phenylmethyl]glycerol insertions (TINA), the quadruplex oligonucleotides showed a dramatic increase of the T(m) (deltaT(m) from 22 to 32 degrees C… CONTINUE READING