Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00346
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| PDC Name |
T7-SN-38
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Glioblastoma
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| Structure |
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| Peptide Name |
DT7
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Peptide Info | ||||
| Receptor Name |
Transferrin receptor protein 1 (TFRC)
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Receptor Info | ||||
| Drug Name |
7-Ethyl-10-hydroxycamptothecin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Ahx-Val
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Linker Info | ||||
| Formula |
C124H163N25O28
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 2451.815 | ||||
| Lipid-water partition coefficient (xlogp) | 6.014 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 16 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 37 | |||||
| Rotatable Bond Count (rotbonds) | 73 | |||||
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 | Glioblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
70.07nM
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| Administration Time | 72 h | ||||
| Evaluation Method | XTT assay | ||||
| MOA of PDC |
In the present work, the cytotoxic drug SN-38 is coupled to the tumor-targeting T7 peptide via a cathepsin B cleavable VA peptide linker. This ensures that the drug remains covalently bound until it reaches the intended site of action, where Cat B is overexpressed to release the drug. Within this framework, our research pursuits entail the synthesis and characterization of a T7-SN-38-targeted drug conjugate using strain-promoted azide-alkyne cycloaddition (SPAAC). Our investigation extended to evaluating the cellular uptake and assessing the cytotoxicity of the drug conjugate in U87MG glioblastoma cells.
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| Description |
Further, IC50values of SN-38 and T7-SN-38 on U87MG cells at 72 h were determined. An estimated IC50value of 26.41nM was obtained for SN-38, which was considerably lower than an IC50value of 70.07nM obtained for the T7-SN-38 conjugate. These IC50data confirm the greater cytotoxicity of the pure drug compared to the conjugate at 72 h (p< 0.05).
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| In Vitro Model | Glioblastoma | U-87MG cell | CVCL_0022 | ||
References