Figure 1.

General scheme for enzymatic remodeling of antibody glycan (a⟶b) followed by metal-free click chemistry conjugation of payload (b⟶c). The drug-to-antibody ratio (DAR) can be tailored (DAR2 or DAR4) by using a linear of branched BCN-linker-drug construct (y = 1 or 2).

GlycoConnect™ technology encompasses a two-step process to convert a monoclonal antibody into an antibody-drug conjugate, abbreviated as ADC. In the first step two enzymes work together to trim the antibody glycan down to the core GlcNAc, followed by attachment of a monosaccharide functionalized with an azido group. In the second step a cyclooctyne-linker-drug is attached by means of metal-free click chemistry of the cyclooctyne – in this case BCN – with the azide. The linker-drug also features a highly polar HydraSpace™ moiety for solubility.