Abstract:
: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) and a strong antiproliferative effects in Panc-1 cells.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Cogoi S,Paramasivam M,Filichev V,Géci I,Pedersen EB,Xodo LEdoi
10.1021/jm800874tsubject
Has Abstractpub_date
2009-01-22 00:00:00pages
564-8issue
2eissn
0022-2623issn
1520-4804pii
10.1021/jm800874tjournal_volume
52pub_type
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