Table 1 The summary and comparison of PROTACs targeting AR
From: PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
No. | PROTAC | Warhead | E3 ligase |
|---|---|---|---|
1 | ARD-69(1) | Pfizer’s AR antagonist derivative | VHL |
2 | ARD-61(2) | Pfizer’s AR antagonist derivative | VHL |
3 | ARD-266(3) | Pfizer’s AR antagonist derivative | VHL |
4 | ARD-2128(4) | Pfizer’s AR antagonist derivative | CRBN |
5 | ARD-2585(5) | Pfizer’s AR antagonist derivative | CRBN |
6 | 21-ARL(6) | Pfizer’s AR antagonist derivative | DCAF11 |
7 | TD-802(7) | Pfizer’s AR antagonist derivative | CRBN |
8 | A031(8) | Pfizer’s AR antagonist derivative | VHL |
9 | 9 | Pfizer’s AR antagonist derivative | CRBN |
10 | 10 | Enzalutamide derivatives | CRBN |
11 | PAP508(11) | Enzalutamide derivatives | CRBN |
12 | MTX-23(12) | AR-DBD binder | VHL |
13 | A16(13) | Enzalutamide derivatives | CRBN |
14 | 14 | AR-DBD binder | VHL |
