Total stepwise solid-phase synthesis of oligonucleotide-(3'-->N)-peptide conjugates.
[structure: see text] An efficient total stepwise solid-phase synthesis of oligonucleotide-(3'-->N)-peptide conjugates is described that makes use of either a controlled pore glass support or macroporous polystyrene beads. Extending our previous homoserine linker approach, we prepared a range of conjugates containing one of four different cell or nuclear penetration peptides together with oligonucleotides containing 2'-deoxynucleoside or 2'-O-methylribonucleoside phosphodiesters, or gapmers containing 2'-deoxyphosphorothioates. The route also allows incorporation of a fluorescent label within the conjugate for cell uptake studies.
Stetsenko
Dmitry A
DA
Medical Research Council, Laboratory of Molecular Biology, Cambridge CB2 2QH, UK.
Malakhov
Andrey D
AD
Gait
Michael J
MJ
D000595:Amino Acid Sequence; D002851:Chromatography, High Pressure Liquid; D005456:Fluorescent Dyes; D008969:Molecular Sequence Data; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry*; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry*; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013194:Staining and Labeling
D005456:Fluorescent Dyes; D009841:Oligonucleotides; D010455:Peptides