Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00099
|
|||||
|---|---|---|---|---|---|---|
| Peptide Name |
p6
|
|||||
| Structure |
|
|||||
| Sequence |
NDLMNRA
|
|||||
| Peptide Type |
Linear
|
|||||
| PDC Transmembrane Types | Cell targeting peptides (CTPs) | |||||
| Formula |
C32H56N12O12S
|
|||||
| Isosmiles |
[H]NC(=O)C[C@H](N[H])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](C)C(=O)O
|
|||||
| InChI |
InChI=1S/C32H56N12O12S/c1-14(2)10-19(43-30(54)21(13-24(47)48)42-25(49)16(33)11-22(34)45)28(52)41-18(7-9-57-4)27(51)44-20(12-23(35)46)29(53)40-17(6-5-8-38-32(36)37)26(50)39-15(3)31(55)56/h14-21H,5-13,33H2,1-4H3,(H2,34,45)(H2,35,46)(H,39,50)(H,40,53)(H,41,52)(H,42,49)(H,43,54)(H,44,51)(H,47,48)(H,55,56)(H4,36,37,38)/t15-,16-,17-,18-,19-,20-,21-/m0/s1
|
|||||
| InChIKey |
LTQKWXOKPROJTI-BPSSIEEOSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
832.939
|
Polar area
|
425.8
|
||
|
Complexity
|
832.3861362
|
xlogp Value
|
-5.5947
|
|||
|
Heavy Count
|
57
|
Rot Bonds
|
29
|
|||
|
Hbond acc
|
13
|
Hbond Donor
|
13
|
|||
The Activity Data of This Peptide
| Peptide Activity Information 1 | [1] | |||||
| Binding rate | 2.17% | |||||
|---|---|---|---|---|---|---|
| Binding Affinity Assay |
To assess the binding capacity of the candidate peptides, peptide-FITC conjugates were incubated at 0, 4 or 8 ?M with 106 PBMC cells at 37 C for 30 min.
|
|||||
| Experimental Condition | Mouse peripheral mononuclear cell PBMC | |||||
| Peptide Activity Information 2 | [1] | |||||
| Binding rate | 6.90% | |||||
| Binding Affinity Assay |
To assess the binding capacity of the candidate peptides, peptide-FITC conjugates were incubated at 0, 4 or 8 ?M with 106 HL-60 cells at 37 C for 30 min.
|
|||||
| Experimental Condition | Human leukemic cell HL-60 | |||||
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
P6-chlorambucil [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | A20 growth inhibition |
22.00%
|
|||
| Administration Time | 72 h | ||||
| Administration Dosage | 50 µM | ||||
| Evaluation Method | XTT assay | ||||
| Description |
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.
Click to Show/Hide
|
||||
| In Vitro Model | Mouse reticulum cell sarcoma | A20 cell | CVCL_1940 | ||
P6-melphalan [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | A20 growth inhibition |
25.00%
|
|||
| Administration Time | 72 h | ||||
| Administration Dosage | 50 µM | ||||
| Evaluation Method | XTT assay | ||||
| Description |
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.
Click to Show/Hide
|
||||
| In Vitro Model | Mouse reticulum cell sarcoma | A20 cell | CVCL_1940 | ||
P6-bendamustine [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | A20 growth inhibition |
28.00%
|
|||
| Administration Time | 72 h | ||||
| Administration Dosage | 50 µM | ||||
| Evaluation Method | XTT assay | ||||
| Description |
Conjugation of the drugs to P4 affected their efficacy toward A20 cells. For chlorambucil and melphalan, conjugation reduced the cytotoxic effect and this was significant for chlorambucil at 25 μM (p = 0.0013). On the other hand, conjugation significantly improved the cytotoxic effect of bendamustine at 25 (p = 0.043) and 50 μM (p = 0.048). The efficacies of all P6-conjugates were significantly lower than those of P4-conjugates at concentrations above 10 μM.
Click to Show/Hide
|
||||
| In Vitro Model | Mouse reticulum cell sarcoma | A20 cell | CVCL_1940 | ||
References
