Table 2 Thapsigargin derivative compounds
From: Targeting oncogenic Notch signaling with SERCA inhibitors
Structure | Compound | Binding site | IC50 (μM) | Cell line/in vivo | References | Clinical trials |
|---|---|---|---|---|---|---|
| Mipsagargin (G202) | M3, M4 (Gln250), M5, M7 A phospholipid head group from the ER membrane interacts with the free amino acid of 12ADTβAsp, near the binding pocket for CPA | 10.964 ± 0.4 | Bladder cancer (PSMA−) | [137] | NCT01056029 NCT02067156 NCT01777594 NCT02607553 |
0.191 ± 0.029 | Prostate cancer (PSMA+) | |||||
N/A | Prostate and breast cancer xenografted models | |||||
| JQ-FT | N/A | 1–10 | T-ALL | [145] | N/A |
N/A | T-ALL xenografted model |
