Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00088
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| PDC Name |
Cq-C4-PasTAT
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Malaria
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| Structure |
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| Peptide Name |
PasTAT
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Peptide Info | ||||
| Drug Name |
N1-(7-chloroquinolin-4-yl)butane-1,4-diamine
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Drug Info | ||||
| Linker Name |
Succinic Acid
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Linker Info | ||||
| Formula |
C130H212ClN47O24
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 2852.884 | ||||
| Lipid-water partition coefficient (xlogp) | -9.2434 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 37 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 35 | |||||
| Rotatable Bond Count (rotbonds) | 99 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Obtained from the Model Organism Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Malaria | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
8.5 µM
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| MOA of PDC |
The significant increase in the hemolytic activity of TP10 upon conjugation to the 4-aminoquinoline suggests that drug cargo prevents an otherwise active CPP carrier from exerting the desired cell penetrating/antiplasmodial action safely, as it produces conjugates that exert membranolytic activity.
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| Description |
Only three of the Cq-C4-CPP conjugates, namely, 5a, 5b, and 5g, displayed IC50 values below 10 μM, with TP10- and Transportan-derived conjugates 5a (IC50 = 1.52 μM) and 5b (IC50 = 5.20 μM) being the most active.
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| In Vivo Model | Plasmodium falciparum W2. | ||||
References