Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00312
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| PDC Name |
pHLIP-S-S-DOX
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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 |
pHLIP (GGEQ)
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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 | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
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| Modified Segment |
Dibenzocyclootyne-maleimide
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| Ternimal Modification |
C-terminal modification
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| Formula |
C224H321N47O69S2
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 4840.426 | ||||
| Lipid-water partition coefficient (xlogp) | -10.0784 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 60 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 67 | |||||
| Rotatable Bond Count (rotbonds) | 146 | |||||
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 | Cell viability |
18%
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| Administration Time | 72 h | ||||
| Administration Dosage | 10 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 16 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
20%
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| Administration Time | 72 h | ||||
| Administration Dosage | 1.3 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 13 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
22%
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| Administration Time | 72 h | ||||
| Administration Dosage | 2.5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 14 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
22%
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| Administration Time | 72 h | ||||
| Administration Dosage | 5.0 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 15 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
30%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.31 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 6 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
30%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.63 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).
Click to Show/Hide
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 7 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
30%
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| Administration Time | 72 h | ||||
| Administration Dosage | 1.3 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).
Click to Show/Hide
|
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 8 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
38%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.16 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
The cytotoxicity data for the pHLIP-PAMAM-DOX conjugate mirrored quite closely that of the pHLIP-S-S-DOX conjugate, particularly at the higher concentrations (>1.25 μM). However, at lower pHLIP concentrations (0.16 μM-0.63 μM), the PAMAM conjugate exhibited higher cytotoxicity than the single DOX conjugate (˜up to 17% higher toxicity).
Click to Show/Hide
|
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 9 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
42%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.63 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 12 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 10 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
45%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.31 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 11 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 11 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
50%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.16 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 10 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 12 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
90%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.63 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 19 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 13 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
95%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.16 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 17 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 14 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
98%
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| Administration Time | 72 h | ||||
| Administration Dosage | 0.31 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 18 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 15 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
99%
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| Administration Time | 72 h | ||||
| Administration Dosage | 10 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 23 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 16 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
100%
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| Administration Time | 72 h | ||||
| Administration Dosage | 1.3 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 20 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 17 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
100%
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| Administration Time | 72 h | ||||
| Administration Dosage | 2.5 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 21 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
| Experiment 18 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
100%
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| Administration Time | 72 h | ||||
| Administration Dosage | 5.0 µM | ||||
| Evaluation Method | MTS assay | ||||
| Description |
HeLa cells treated with pHLIP-S-S-DOX at low pH showed significant toxicity (˜50% viability at the lowest concentration tested (0.16 μM pHLIP)) which, in this construct, corresponds to the DOX concentration. Cellular viability tracked inversely with increasing pHLIP conjugate concentration, peaking at ˜18% viability at 22 μM.
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| In Vitro Model | Endocervical adenocarcinoma | HeLa cell | CVCL_0030 | ||
References