Polyimidazole conjugated oligonucleotides reach the nucleus of HeLa cells.
Oligonucleotide models bearing 6, 12 or 18 histamine residues were synthesized on solid support and labeled with fluorescein. Only the oligo with 6 histamine residues showed a high uptake in HeLa cells with a nuclear localization. Experiment a 4 degrees C or with bafilomicyn A1 suggest that uptake proceeded by an endocytosis mechanism followed by a destabilization of the membrane. Once in the cytoplasm the oligo reached rapidly the nucleus.
Morvan
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F
Laboratoire de Chimie Organique Biomoléculaire de Synthèse, UMR 5625 CNRS-UM II, Université Montpellier II, Place E. Bataillon, 34095 Montpellier, France.
Castex
C
C
Vivès
E
E
Imbach
J L
JL
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002467:Cell Nucleus / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology; D019793:Fluorescein / Q000737:chemistry; D006367:HeLa Cells; D006632:Histamine / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000493:pharmacokinetics*; D018942:Macrolides; D008856:Microscopy, Fluorescence; D009841:Oligonucleotides / Q000737:chemistry / Q000493:pharmacokinetics*; D063065:Organophosphonates / Q000737:chemistry; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013936:Thymidine / Q000031:analogs & derivatives / Q000493:pharmacokinetics
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007093:Imidazoles; D018942:Macrolides; D009841:Oligonucleotides; D063065:Organophosphonates; C057620:bafilomycin A; D006632:Histamine; D019793:Fluorescein; D013936:Thymidine