Table 2.
PROTAC or hydrophobic-tagged PARP inhibitors.
| PROTAC | ||||
|---|---|---|---|---|
| PARP Binder | E3 Ligase Binder | Tested Cell | Note | Ref. |
| Olaparib | CRBN ligand | MDA-MB-436 (BRCA1 mutated breast cancer cells), Capan-1 (BRCA2 mutated pancreatic cancer cells), SW620 (colon cancer cell) | Inhibition of tumor growth, Xenograft assay | [77] |
| Rucaparib | CRBN ligand | Primary rat neonatal cardiomyocytes, C2C12 (myoblast) | PARP1 non-trapping, No genotoxic induced cell death | [81] |
| Olaparib | CRBN ligand | SW620 | Increased apoptosis | [78] |
| Niraparib | MDM2 ligand | MDA-MB-231 (TNBC) | Induction of PARP1 cleavage, increased apoptosis | [79] |
| Hydrophobic Tagging | ||||
| PARP Binder | Hydrophobic Moiety | Tested Cell | Note | Ref. |
| Olaparib | Fluorene | MDA-MB-231, MDA-MB-468 (TNBC), HCC1937 (BRCA1 mutated breast cancer cells) |
Increased apoptosis and ER stress | [82] |