Blog
About

13
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

      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.

      Journal of Medicinal Chemistry

      pharmacology, Base Sequence, chemistry, Pyrenes, Promoter Regions, Genetic, pathology, Pancreatic Neoplasms, Humans, analogs & derivatives, Glycerol, Genes, ras, G-Quadruplexes, Electrophoretic Mobility Shift Assay, drug effects, Cell Proliferation, Cell Line, Tumor

      Read this article at

      ScienceOpenPublisherPubMed
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          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.

          Related collections

          Author and article information

          Journal
          19099510
          10.1021/jm800874t

          Comments

          Comment on this article