Peptide-drug Conjugate Information

General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00095
PDC Name
Cq-TR-TP10
PDC Status
Investigative
Indication
In total 1 Indication(s)
Malaria
Structure
Peptide Name
TP10
  Peptide Info 
Drug Name
N1-(7-chloroquinolin-4-yl)butane-1,4-diamine
  Drug Info 
Linker Name
6-(4-(amino(carboxy)methyl)-1H-1,2,3-triazol-1-yl)hexanoic acid
  Linker Info 
Formula
C127H213ClN34O25
#Ro5 Violations (Lipinski): 4 Molecular Weight 2651.767
Lipid-water partition coefficient (xlogp) -0.2147
Hydrogen Bond Donor Count (hbonddonor) 31
Hydrogen Bond Acceptor Count (hbondacc) 35
Rotatable Bond Count (rotbonds) 97
Full List of Activity Data of This Peptide-drug Conjugate
Obtained from the Model Organism Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Malaria
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.2 ± 0.2 µM
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.
In Vivo Model Plasmodium falciparum 3D7.
References
Ref 1 Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates. Molecules. 2019 Dec 12;24(24):4559. doi: 10.3390/molecules24244559.