Rapid routes of synthesis of oligonucleotide conjugates from non-protectedoligonucleotides and ligands possessing different nucleophilic or electrophilic functional groups
Gn. Grimm et al., Rapid routes of synthesis of oligonucleotide conjugates from non-protectedoligonucleotides and ligands possessing different nucleophilic or electrophilic functional groups, NUCLEOS NUC, 19(10-12), 2000, pp. 1943-1965
Optimized methods are described for post-synthetic conjugation of non-prote
cted oligodeoxyribonucleotides tol different ligands. Methods for the termi
nal functionalization of oligonucleotides by amino, sulfhydryl, thiophospha
te or carboxyl groups using different chemical reactions and linkers in bot
h organic and aqueous media are described and compared. Experimental condit
ions for subsequent coupling of ligands containing aliphatic and aromatic a
mines, aromatic alcohols, carboxylic, sulfhydryl, alkylating, aldehydic and
other reactive nucleophilic and electrophilic groups to oligonucleotides w
ere established, including covalent linkage to other oligonucleotides.