Table IV.
Site-Specific Conjugation Technologies
| Description | Methodology | DAR | Conjugation chemistry | Companies | Ref |
|---|---|---|---|---|---|
| Engineered Cysteine Residues | Cysteine substitution | 2 or 4 | Maleimide, Bromoacetamide | Genentech, MedImmune, Seattle Genetics | (32) |
| Non-natural Amino Acids/Glycans | Seleno cysteine | 2 | Maleimide | NCI | (33) |
| p-AcPhe | 2 or 4 | Oxime | Allozyne, Ambrx | (34) | |
| FGE (formylglycine generating enzyme) | 2 or 4 | Oxime, Pictet-Spengler | Catalent Pharma Solutions | (35, 36) | |
| Azide or alkynyl nnAA or glycan | 1 to 2 | Click chemistry | Sutro, Allozyne, Synaffix | (37) | |
| Enzymatic | Glycotransferase | 2 | 2-keto-Gal | NCI | (38) |
| BTG (bacterial transglutaminase) | 2 or 4 | Gln with Lys | Innate Pharma Pfizer |
http://innate-pharma.com/sites/default/files/iph_poster_world_adc_frankfurt_2014.pdf |
|
| Sortase A | 2 or 4 | Hydrolysis of Thr-Gly in LPxTG motif | NBE Therapeutics | http://www.nbe-therapeutics.com |