Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00284
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| PDC Name |
PDC-PTX1
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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 |
Cyclic peptide [W(WR)4K(βAla)]
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Peptide Info | ||||
| Drug Name |
Paclitaxel
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Drug Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Glutaric acid
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Linker Info | ||||
| Peptide Modified Type |
Amino acid modifications; Cyclization modification
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| Modified Segment |
One arginine was replaced with one lysine
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| Formula |
C140H170N30O27
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 2705.083 | ||||
| Lipid-water partition coefficient (xlogp) | 4.78438 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 32 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 31 | |||||
| Rotatable Bond Count (rotbonds) | 49 | |||||
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 |
60%
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| Administration Time | 72 h | ||||
| Administration Dosage | 5 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
Antiproliferative results showed that PTX1 inhibited cell proliferation by 18.7%. The anti-proliferative activity of CPT1 was diminished by 1.9-fold as compared to CPT whereas the activity of CPT2 was comparable to CPT, since CPT2 reduced the cell viability to 61%.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Cell viability |
80%
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| Administration Time | 72 h | ||||
| Administration Dosage | 5 µM | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The cytotoxicity of PTX and PTX1 was further evaluated in the normal human embryonic kidney cells (HEK-293) at 5 uM which showed reduced cell proliferation by ~34% and 18%, respectively, after 72 h using MTT assay, as shown in Figure 2.
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| In Vitro Model | Normal | HEK-298 cell | Homo sapiens | ||
References