Table 3.
PROTAC and SNIPER used for Antibody Drug Conjugates. Reproduced with permission from Dragovich et al. [143] Copyright 2020 Elsevier.
| MCF7-Neo/HER2 (ER-α) | MCF7 Parental (ER-α) | ||||
|---|---|---|---|---|---|
| Chemotypes | Ligase | DC50 (nM) | Dmax | DC50 (nM) | Dmax |
| fulvestrant | - | 0.38 ± 0.07 | 84% | 0.45 ± 0.01 | 87% |
| SNIPER-5 | XIAP | 1.6 ± 0.12 | 85% | 0.68 ± 0.13 | 87% |
| VHL-PROTAC-6 | VHL | 4.9 ± 0.57 | 92% | 2.7 ± 0.71 | 92% |
| VHL-PROTAC-7 | VHL | 7.9 ± 0.71 | 57% | 5.2 ± 0.01 | 54% |
| SNIPER-8 | XIAP | 305 ± 103 | 76% | 131 ± 2.1 | 75% |
| endoxifen | - | 1.1 ± 0.37 | 48% | 1.6 ± 0.01 | 49% |