Table 1.
BCL6 targeted inhibitors.
| Type | Name | MW g/mol | Malignancy | IC50 | KD | In vivo model | In vivo dose | In vivo outcome | Challenges for translation | Reference |
|---|---|---|---|---|---|---|---|---|---|---|
| Peptide Inhibitors | BPI | 4,550.19 | DLBCL | 14.2 μmol/L | 20 μmol/L | NR | NR | NR | Easily degraded by proteases | (93) |
| F1324 | 1,765.04 | NR | 1 nmol/L | 0.57 nmol/L | NR | NR | NR | No inhibitory effects in vitro | (95) | |
| Apt48 | 1,536.74 | BL | NR | NR | NR | NR | NR | No cytotoxic effects, requires cytokines | (22) | |
| Reverse peptide inhibitors | RI-BPI | 4,510.12 | DLBCL | 16.5 μmol/L | 16 μmol/L | SU-DHL4 SU-DHL6 Toledo SCID mice | 150 & 500 μmol/L/day | ↓ TV ↑survival SU-DHL4/6 | Weak affinity + large MW | (94) |
| Glioma | 5–25 μmol/L | NR | JM94 | 50 mg/kg/day | ↓ TS ↑ response with EGFR I | (9) | ||||
| Small molecules | 79-6 | 457.28 | DLBCL | 24–93.6 μmol/L | 138 μmol/L | OCI-Ly7 SU-DHL6 Toledo SCID mice | 0.5–50 mg/kg/day | ↓TV OCI-Ly7 SU-DHL6 | Non apoptotic, BCL6 lymphoma specific | (95) |
| FX1 | 368.82 | NSCLC | 35 μmol/L | 4 μmol/L | OCI-Ly7 SU-DHL6 Toledo SCID mice | 25 & 50 mg/kg/day | ↓TV OCI-Ly7 SU-DHL6 | BCL6 lymphoma specific | (101) | |
| GSK137 | 374 | DLBCL | 10 nmol/L | 10 nmol/L | NR | NR | NR | Non cytotoxic | (101) | |
| BI-3802 | 485 | DLBCL | 20 nmol/L | <3 nmol/L | NR | NR | NR | Degrades BCL6 | (98,99) | |
| BI-3812 | 558 | DLBCL | 3 nmol/L | <3 nmol/L | NR | NR | NR | Bioavailability | (98,99) |
Abbreviations: IC50, inhibitory concentration 50%; KD, disassociation constant; NR, not reported in cancer models; TS, tumor size; TV, tumor volume.