General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00263
PDC Name
P4-Melph-PEG-AuNP
PDC Status
Investigative
Indication
In total 1 Indication(s)
Tumor
Structure
Peptide Name
p4
 Peptide Info 
Drug Name
Melphalan
 Drug Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
 Target Info 
Linker Name
Amide bond
 Linker Info 
Peptide Modified Type
The modification of binding with chemical macromolecules
Modified Segment
PEG-AuNP
Formula
C42H61Cl2N11O13
#Ro5 Violations (Lipinski): 5 Molecular Weight 998.92
Lipid-water partition coefficient (xlogp) -4.3455
Hydrogen Bond Donor Count (hbonddonor) 12
Hydrogen Bond Acceptor Count (hbondacc) 15
Rotatable Bond Count (rotbonds) 30
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
45.00%
Administration Time 72 h
Administration Dosage 50 µM
Evaluation Method XTT assay
Description
All three P4-PDC-coated gold nanoparticles pre-incubated for 24 or 48 h induced statistically similar cytotoxicity in A20 to that induced by freshly prepared PDC4 and to coated particles without pre-incubation (the latter data not shown).
In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
78.00%
Administration Time 48 h
Administration Dosage 50 µM
Evaluation Method XTT assay
MOA of PDC
Vitamin C as a water-soluble vitamin is the reduced form of ascorbic acid. No significant adverse effect of taking high doses of vitamin C (over 2000 mg/day) has been reported due to the water-soluble feature of vitamin C. Vitamin C directly reacts with hydroxy, alkoxyl, and lipid peroxyl radicals and converts them to alcohol, water, and hydroperoxide lipid, respectively. It has been shown that taking vitamin C before radioiodine therapy can ameliorate the oxidative stress effect of radioiodine. The radioprotective effects of vitamin C are mainly due to its free radical scavenging activity.

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Description
All three P4-PDC-coated gold nanoparticles pre-incubated for 24 or 48 h induced statistically similar cytotoxicity in A20 to that induced by freshly prepared PDC4 and to coated particles without pre-incubation (the latter data not shown).
In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data A20 growth inhibition
80.00%
Administration Time 24 h
Administration Dosage 50 µM
Evaluation Method XTT assay
Description
All three P4-PDC-coated gold nanoparticles pre-incubated for 24 or 48 h induced statistically similar cytotoxicity in A20 to that induced by freshly prepared PDC4 and to coated particles without pre-incubation (the latter data not shown).
In Vitro Model Mouse reticulum cell sarcoma A20 cell CVCL_1940
References
Ref 1 Gold nanoparticles stabilize peptide-drug-conjugates for sustained targeted drug delivery to cancer cells. J Nanobiotechnology. 2018 Mar 30;16(1):34. doi: 10.1186/s12951-018-0362-1.