Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00260
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| PDC Name |
P4-chlorambucil
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Tumor
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| Structure |
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| Peptide Name |
p4
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Peptide Info | ||||
| Drug Name |
Chlorambucil
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
Gamma-Aminobutyric Acid
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Linker Info | ||||
| Formula |
C47H69Cl2N11O14
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 1083.038 | ||||
| Lipid-water partition coefficient (xlogp) | -2.9962 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 12 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 15 | |||||
| Rotatable Bond Count (rotbonds) | 35 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | A20 growth inhibition |
70.00%
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| Administration Time | 72 h | ||||
| Administration Dosage | 50 µM | ||||
| Evaluation Method | XTT assay | ||||
| Description |
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.
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| In Vitro Model | Mouse reticulum cell sarcoma | A20 cell | CVCL_1940 | ||
References