The present disclosure relates to a novel enzymatic approach according to the invention using an unprecedented sortase-catalyzed transpeptidation reaction between a substrate comprising LPXTG (SEQ ID NO: 11) peptide motif and biomolecules such as aminosugars, hydroxyamino acids, hydroxyamino acid esters, aminolipids, polyamines nucleic acids or derivatives thereof or any molecule having such moieties or any compound having such moieties to obtain a bioconjugates useful for target delivery of a compound. The present disclosure provides bioconjugates obtained by the novel sortase catalysed transpeptidedation reaction.