Table 3.
Prodrugs with a peptide linker.
| Entry | Name | Target tissue | Protease trigger | Peptide linker sequence | Conjugate moiety | Payload drug | Ref |
|---|---|---|---|---|---|---|---|
| 1 | NTD | Cancer | Cathepsin B | GFLG | Tat cell penetration peptide | Doxorubicin (multiple) | 62 |
| 2 | PEG-vcTNF-α | Cancer | Cathepsin B | VCit | PEG | TNF-α | 63 |
| 3 | BMS936561 | Cancer | Cathepsin B | VCit | CD70 mAb | MED-A (duocarmycin derivative) | 64 |
| 4 | Dendrimer-GEM | Breast cancer | Cathepsin B | GFLG | PEG dendrimer | Gemcitabine | 65 |
| 5 | DEVD-Cysteamide-EMCS-doxorubicin | Cancer | Caspase-3 | RDEVD | none | Doxorubicin (modified) | 66 |
| 6 | uPA-cPPP | Cancer | Urokinase plasminogen activator (uPA) | GSGRSAG | Cyclopeptide template c-KAAPGAKAPG | Photosensitizer Pheophorbide A | 67 |
| 7 | GKAFRR-L12ADT | Prostate cancer | KLK2 | GKAFRR | none | Thapsigargin derivative L12ADT | 68 |
| 8 | Z-GP-EPI | Epithelia tumor | Fibroblast activation protein-α (FAPα) | Cbz-GP | none | Epirubicin | 69 |
| 9 | rTLM-PEG | Cancer | MMP-2 | PLGLAG | PEG | Cell-penetrating peptide-trichosanthin | 69 |
| 10 | BSD352 | Prostate cancer | KLK3 (PSA) | HSSKLQ | Tat cell penetration peptide | BH3 domain, anti-VEGF peptide (SP5.2), anti-bFGF peptide (DG2) | 70 |