Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00306
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| PDC Name |
Peptide-drug conjugate 10
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Neuroblastoma
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| Structure |
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| Peptide Name |
oxmCPP
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Peptide Info | ||||
| Drug Name |
Doxorubicin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
Disulfide bond
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Linker Info | ||||
| Formula |
C119H183N41O35S2
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 2812.159 | ||||
| Lipid-water partition coefficient (xlogp) | -12.8107 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 41 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 49 | |||||
| Rotatable Bond Count (rotbonds) | 79 | |||||
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 | Neuroblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.47 ± 0.91 µM
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| Administration Time | 72 h | ||||
| Evaluation Method | CellTiter-Glo luminescent cell viability assay | ||||
| Description |
The cytotoxic effect of the peptide-drug conjugate on Kelly-WT cells was comparable to that of 9, but not as strong as the one of the native drug. Contrary to the other utilized substances, the antiproliferative action of the bioconjugate in wild-type and drug-resistant cells was nearly the same. In comparison with doxorubicin the cytotoxicity of 10 against Kelly-ADR cells was increased by a factor of 3 according to the obtained IC50 values. Even the unmodified dimer had roughly the same cytotoxic effect on Kelly-ADR cells as doxorubicin.
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| In Vitro Model | Neuroblastoma | Kelly-WT cell | CVCL_2092 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.76 ± 0.33 µM
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| Administration Time | 72 h | ||||
| Evaluation Method | CellTiter-Glo luminescent cell viability assay | ||||
| Description |
The cytotoxic effect of the peptide-drug conjugate on Kelly-WT cells was comparable to that of 9, but not as strong as the one of the native drug. Contrary to the other utilized substances, the antiproliferative action of the bioconjugate in wild-type and drug-resistant cells was nearly the same. In comparison with doxorubicin the cytotoxicity of 10 against Kelly-ADR cells was increased by a factor of 3 according to the obtained IC50 values. Even the unmodified dimer had roughly the same cytotoxic effect on Kelly-ADR cells as doxorubicin.
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| In Vitro Model | Neuroblastoma | Kelly-ADR cell | CVCL_2092 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Neuroblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
3.66 ± 0.77 µM
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| Administration Time | 72 h | ||||
| Evaluation Method | CellTiter-Glo luminescent cell viability assay | ||||
| Description |
The obtained IC50 values for 9 (6.73 ± 2.44 uM) and 10 (3.66 ± 0.77 uM) were higher than for doxorubicin (0.90 ± 0.12 uM).
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
References