Preparation of carbohydrate–oligonucleotide conjugates using the squarate spacer

Attachment of carbohydrates to oligonucleotides has proven to induce receptor-mediated endocytosis. A facile method for the formation of covalent linkages between glycans and oligonucleotides is herein described. Thus, use of 3,4-diethoxy-3-cyclobutene-1,2-dione as a linking reagent provides easy conjugation between carbohydrates bearing an amino group at the reducing end and oligonucleotides bearing an aminoalkyl modification.

Graphical abstractThe use of squarate as spacer in the preparation of carbohydrate–oligonucleotide conjugates is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide