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. Author manuscript; available in PMC: 2020 Aug 24.
Published in final edited form as: Methods Mol Biol. 2020;2078:83–97. doi: 10.1007/978-1-4939-9929-3_6

Table 3.

Methods for site-specific incorporation of an azide handle onto an antibody.

Approach Scheme a Click Chemistry Drug-Linker b Reported DAR (Expected DAR) Ref.
Glycan Remodeling graphic file with name nihms-1601833-t0009.jpg SPAAC DIBO-Dox 4.5 (4) [31]
Glycan Remodeling graphic file with name nihms-1601833-t0010.jpg SPAAC BCN-Dox BCN-MMAE BCN-MMAF BCN-maytansine BCN DUMSA >1.9 (2) [34]
CuAAC Alkyne-PBD >1.9 (2) 3.8 (4) [37]
Unnatural amino acid (UAA) mutagenesis graphic file with name nihms-1601833-t0011.jpg SPAAC DBCO-MMAF 1.2–1.9 (2) [32]
UAA mutagenesis graphic file with name nihms-1601833-t0012.jpg CuAAC SPAAC Alkyne-PBD Alkyne-AF BCN-AF 1.8 ->1.9 (2) [35]
Enzymatic modification of peptide tag graphic file with name nihms-1601833-t0013.jpg SPAAC DBCO-MMAE >1.9 (2) [33]
Enzymatic modification of peptide tag graphic file with name nihms-1601833-t0014.jpg SPAAC DBCO-MMAE 3.3 (4) [48]
a

GalNAz: azido-modified N-acetyl-D-galactosamine; PNGase F: N-glycosidase F.

b

DIBO: dibenzocyclooctyne; BCN: bicyclo[6.1.0]nonyne; DUMSA: duocarmycin SA; PBD: pyrrolobenzodiazepine dimer; DBCO: dibenzoazacyclooctyne. Regarding the drug-linkers listed, only the functional group and the drug are specified. The linker connecting these two moieties may vary.