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The synthesis of peptide-oligonucleotide conjugates by a fragment coupling approach

1998; Elsevier BV; Volume: 54; Issue: 41 Linguagem: Inglês

10.1016/s0040-4020(98)00731-5

1464-5416

Suzanne Peyrottes, Béatrice Mestre, Fabienne Burlina, Michael J. Gait,

DNA and Nucleic Acid Chemistry

Solid-phase synthesis of several peptide-oligonucleotide conjugates has been achieved using a peptide fragment coupling strategy on a controlled pore glass support. The conjugates contain either a hydrophobic tetrapeptide LGIG or an 8-residue basic peptide of the HIV-1 Tat protein coupled to one of two oligodeoxyribonucleotides, an oligoribonucleotide or a mixed ribo/2′-O-methyl oligonucleotide. Improved yields were obtained when internucleotide β-cyanoethyl groups were removed from the support-bound oligonucleotide prior to peptide fragment coupling, and by use of a long alkyl spacer in the linkage between peptide and oligonucleotide.