General Information of This Peptide
Peptide ID
PEP00064
Peptide Name
KGFRWR
Structure
Sequence
KGFRWR
Peptide Type
Linear
PDC Transmembrane Types Cell-penetrating peptides (CPPs)
Formula
C40H60N14O7
Isosmiles
[H]NCCCC[C@H](N[H])C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](Cc1cn([H])c2ccccc12)C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)O
InChI
InChI=1S/C40H60N14O7/c41-17-7-6-13-27(42)34(56)50-23-33(55)51-31(20-24-10-2-1-3-11-24)36(58)52-29(15-8-18-47-39(43)44)35(57)54-32(21-25-22-49-28-14-5-4-12-26(25)28)37(59)53-30(38(60)61)16-9-19-48-40(45)46/h1-5,10-12,14,22,27,29-32,49H,6-9,13,15-21,23,41-42H2,(H,50,56)(H,51,55)(H,52,58)(H,53,59)(H,54,57)(H,60,61)(H4,43,44,47)(H4,45,46,48)/t27-,29-,30-,31-,32-/m0/s1
InChIKey
XJDKSQWPJKYMHZ-QDNWXXHKSA-N
Pharmaceutical Properties
Molecule Weight
849.011
Polar area
379.43
Complexity
848.4769403
xlogp Value
-2.3434
Heavy Count
61
Rot Bonds
29
Hbond acc
10
Hbond Donor
13
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
DOXKGFRWR [Investigative]
Obtained from the Model Organism Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Tumor volume
376 mm3
Description
The antitumor efficacy of the DOX-KGFRWR nanofiber was superior to all other treatments, with a final tumor volume of 376 mm3.
In Vivo Model SMMC7721 tumorbearing mice.
Half life period 24.52±13.17 h
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Percent survival
50%
Administration Time 40 days
Description
DOX-KGFRWR has significantly prolonged survival rates.
In Vivo Model SMMC7721 tumorbearing mice.
Half life period 24.52±13.17 h
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Percent survival > 40 days
Administration Time 30 days
Description
DOX-KGFRWR has significantly prolonged survival rates.
In Vivo Model SMMC7721 tumorbearing mice.
Half life period 24.52±13.17 h
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.27 µM
Description
The IC50 values for KGFRWR, DOX, and DOX-KGFRWR against the MMP2 enzyme were 14.19, 8.68, and 5.27 10-6 m, respectively.
In Vivo Model SMMC7721 pulmonary metastatic mouse model.
Half life period 24.52±13.17 h
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Migration rates
19.90%
Description
Cells treated with DOX and DOX-KGFRWR exhibited markedly decreased migration, with migration rates of 39.4% and 19.9%, respectively, compared with those in the control, indicating that DOX-KGWRFR exerted a stronger inhibiting effect on migration than DOX.
In Vitro Model Hepatocellular carcinoma SMMC-7721 cell CVCL_0534
Half life period 24.52±13.17 h
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Hepatocellular carcinoma
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
34.55 µg mL-1
Evaluation Method MTT assay
Description
The IC50 values for DOX-KGFRWR is 34.55 μg mL-1.
In Vitro Model Hepatocellular carcinoma SMMC-7721 cell CVCL_0534
Half life period 24.52±13.17 h
References
Ref 1 Drug-Bearing Supramolecular MMP Inhibitor Nanofibers for Inhibition of Metastasis and Growth of Liver Cancer. Adv Sci (Weinh). 2018 Jun 10;5(8):1700867. doi: 10.1002/advs.201700867. eCollection 2018 Aug.