Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00143
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| Peptide Name |
E1-7
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| Structure |
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| Sequence |
VGGLSHR
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| Peptide Type |
Linear
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| PDC Transmembrane Types | Cell-penetrating peptides (CPPs) | |||||
| Formula |
C30H52N12O9
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| Isosmiles |
[H]N/C(N)=N/CCC[C@H](NC(=O)[C@H](Cc1cn([H])cn1)NC(=O)[C@H](CO[H])NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)CNC(=O)[C@@H](N[H])C(C)C)C(=O)O
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| InChI |
InChI=1S/C30H52N12O9/c1-15(2)8-19(39-23(45)12-36-22(44)11-37-28(49)24(31)16(3)4)25(46)42-21(13-43)27(48)41-20(9-17-10-34-14-38-17)26(47)40-18(29(50)51)6-5-7-35-30(32)33/h10,14-16,18-21,24,43H,5-9,11-13,31H2,1-4H3,(H,34,38)(H,36,44)(H,37,49)(H,39,45)(H,40,47)(H,41,48)(H,42,46)(H,50,51)(H4,32,33,35)/t18-,19-,20-,21-,24-/m0/s1
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| InChIKey |
JJXROHNCXAXNBC-TVJXPIDLSA-N
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| Pharmaceutical Properties |
Molecule Weight
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724.821
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Polar area
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351.23
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Complexity
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724.3980212
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xlogp Value
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-4.7163
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Heavy Count
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51
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Rot Bonds
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25
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Hbond acc
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11
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Hbond Donor
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12
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The Activity Data of This Peptide
| Peptide Activity Information 1 | [1] | |||||
| Abs 410nm | 0.05 | |||||
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| Binding Affinity Assay |
Medulloblastoma cells (DAOY) were plated into 96-multiwell ELISA plates (1 103 cells/well) the day prior to the assay. Cells were incubated in fresh culture medium without serum for 1 h at 37 °C and then fixed with freshly prepared 4% paraformaldehyde for 20 min at room temperature. Cells were washed three times in PBS and blocked for 1 h at room temperature in PBS containing 2% nonfat skim milk powder. The selected phage clones and a negative control M13KE phage were added (5 1010 pfu/well) individually to the cells and incubated for 90 min at room temperature. The phages were removed and cells washed in PBS containing 0.05% Tween. Anti-M13 antibody conjugated to horseradish peroxidase (HRP) was added to each well and incubated at room temperature for 1 h. Cells were washed with PBS containing 0.05% Tween and incubated with 2,2-azino-bis (3-ethylbenzothiazoline-6 sulfonic acid, ABTS) for 30 min at room temperature. The color reaction was stopped using HCl and the optimal density (OD) for each sample was measured at 410 nm using a microplate reader (PerkinElmer Victor3 plate reader).
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| Experimental Condition | Medulloblastoma cells | |||||
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
E1-7 doxorubicin [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Medulloblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
130 ± 1.27 nM
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| Administration Time | 72 h | ||||
| Description |
This was confirmed with E1-7 doxorubicin conjugate (4) displaying a 5-fold reduction in cytotoxicity compared to E1-3 doxorubicin conjugate (3) (IC50 values of 130 ± 1.27 nM and 25 ± 1.22 nM, respectively) and 14-fold reduction in cytotoxicity compared to free doxorubicin (5) (IC50 values of 130 ± 1.27 nM and 8.8 ± 1.31 nM, respectively) (Figure 7).
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| In Vitro Model | Medulloblastoma | Medulloblastoma cell | Homo sapiens | ||
References