Development of a general methodology for labelling peptide–morpholino oligonucleotide conjugates using alkyne–azide click chemistry

Abstract

We describe a general methodology for fluorescent labelling of peptide conjugates of phosphorodiamidate morpholino oligonucleotides (PMOs) by alkyne functionalization of peptides, subsequent conjugation to PMOs and labelling with a fluorescent compound (Cy5-azide). Two peptide–PMO (PPMO) examples are shown. No detrimental effect of such labelled PMOs was seen in a biological assay.