Stability, specific binding activity, and plasma concentration in mice of an oligodeoxynucleotide modified at 5'-terminal with poly(ethylene glycol).
Oligodeoxynucleotide (ODN) composed of 15 nucleotides was modified at 5'-terminal phosphate with hexylamine linker and chemically activated poly(ethylene glycol). This derivative showed improved characteristics in terms of enzymatic stability, binding activity, and in vivo retention in mouse. The data are discussed in comparison with those of corresponding unmodified and phosphorothioate ODNs.
Kawaguchi
T
T
Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
Asakawa
H
H
Tashiro
Y
Y
Juni
K
K
Sueishi
T
T
D000818:Animals; D001483:Base Sequence; D004355:Drug Stability; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008969:Molecular Sequence Data; D009841:Oligonucleotides / Q000097:blood* / Q000378:metabolism; D016376:Oligonucleotides, Antisense / Q000378:metabolism; D011092:Polyethylene Glycols / Q000494:pharmacology*; D012680:Sensitivity and Specificity; D015719:Single-Strand Specific DNA and RNA Endonucleases / Q000378:metabolism
D009841:Oligonucleotides; D016376:Oligonucleotides, Antisense; D011092:Polyethylene Glycols; D015719:Single-Strand Specific DNA and RNA Endonucleases